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Marine Bioactive
Compounds
D. PARGUNAN
Inspector of Fisheries
Marine bioactive compounds
*Marine flora and fauna are excellent sources of bioactive
compounds with therapeutic benefits.
*The biodiversity of the marine environment and its associated
chemical diversity contribute to an almost unlimited resource
of new bioactive compounds.
* Bioactive compounds can be isolated from various sources
including marine plants, animals, microorganisms and
sponges with unique set of molecules.
*Bioactive compounds extracted from these organisms are
effective against different infectious and non-infectious
diseases.
Marine bioactive compounds
*Investigations on marine natural products have focused on areas like
ā€¢ marine nutraceuticals,
ā€¢ biopolymers,
ā€¢ biofilms,
ā€¢ CNS-membrane active toxins and
ā€¢ ion channel effectors,
ā€¢ antifouling,
ā€¢ anti- cancer and antiviral agents,
ā€¢ tumor promoters,
ā€¢ anti-inflammatory agents,
*Encouraging a multidisciplinary approach between biologists, chemists, and
pharmacologists.
*It is also important to note that the number of com- pounds reported
annually is increasing steadily
*Marine organisms will continue to be sufficient sources of natural bioactive
substances.
Marine bioactive compounds
*Numerous marine bioactive compounds are utilized in different food
products at industrial scale.
*Marine products are rich in
ā€¢ proteins containing both essential and non-essential amino acids,
ā€¢ polysaccharides,
ā€¢ polyunsaturated fatty acids (PUFAs),
ā€¢ vitamins, minerals and many other nutrients
*These compounds can be isolated from
Fish and shellfish
molluscs (including mussel, oyster, scallop, abalone, snail and conch)
cephalopods (including squid, cuttlefish and octopus)
crustaceans (including crayfish, crab, shrimp and lobster),
echinoderms,
seaweeds and microalgae
Marine Biopolymers and Derivatives
*Fish processing generates solid wastes (skin, scales, and bones)
that can be as high as 80% of the original raw material and are
excellent sources of high value products.
*The utilization of fish wastes helps to eliminate harmful
environmental aspects of pollution and improve quality in fish
processing.
*An important waste reduction strategy for the industry is the
recovery of marketable by-products from fish wastes.
*The two most important marine biopolymers collagen as well as
the polysaccharide polymer, chitin, and their derivatives gelatin
and chitosan, respectively, are a promising entity in this regard.
Marine Biopolymers and Derivatives
Collagen
*Collagen in the form of elongated fibrils is mostly found in fibrous
tissues such as tendons, ligaments, and the skin.
*It is also abundant in corneas, bones, blood vessels, gut, vertebral
discs, dentine in teeth, and muscle tissue as a major component of the
endomysium.
*Collagen constitutes 1 to 2% of muscle tissue and accounts for 6% of
the weight of strong, tendinous muscles.
*The fibroblast is the most common cell that creates collagen.
*The name collagen comes from the Greek word ā€œkollaā€ denoting glue
and the suffix ā€œgenā€ meaning producing.
*Collagen finds wide application in food, pharmaceutical,
cosmetics,leather, and biomedical industries.
*One of the most useful biomaterials, mainly due to its biocompatibility,
biodegradability, low toxicity, and immunogenicity, compared to other
natural polymers
Collagen Application
ā€¢ Membranes for guided tissue
regeneration
ā€¢ Cartilage repair, arthritis treatment
ā€¢ Hemostats and tissue sealants
ā€¢ Corneal treatment
ā€¢ mAbs development for osteoarthritis
ā€¢ Attachment enhancer of cell culture
membrane(mouse neuroblastoma) and
diabetic
ā€¢ nephropathy indicator
ā€¢ Hemostat
ā€¢ Treatment of dystrophic epidermolysis
bullosa (DEB)
ā€¢ Regulator in early stages
fibrillogenesis
ā€¢ Antiangiogenic and antitumoral
properties
ā€¢ Contribute to matrix assembly of
vascular network during blood
vessel formation
ā€¢ Involved in inflammation and
vasculogenesis, regulate bone mass
ā€¢ Teeth formation
ā€¢ Drug target and biomarker
ā€¢ Retinal structure, closure of
ā€¢ neural tube
Bioactive Roles of Collagen
*Collagen becomes a very useful carrier for the delivery of various
kinds of drugs and agents like growth factors.
*Collagen is capable of being prepared into cross-linked
compacted solids or into latticelike gels.
*Resorbable forms of collagen have been used to dress oral
wounds, for closure of graft and extraction sites, and to promote
healing.
*Collagen-based membranes also have been used in periodontal
and implant therapy as barriers to prevent epithelial migration
and allow cells with regenerative capacity to repopulate the
defective area.
*Use of collagen scaffolds in bone sialoprotein-mediated bone
regeneration
Bioactive Roles of Collagen
*Medical collagen supplements, which are available as collagen
creams, collagen injections, and collagen capsules, replenish the
level of collagen in the body and reduce the signs of aging.
* The human skin has difficulty in absorbing animal collagen so
that collagen treatment had to be supplemented with a
hypodermic injection treatment, which typically is expensive and
carries the risk of infection.
*Animal (terrestrial vertebrates) collagen also has the potential to
spread bovine spongiform encephalopathy [BSE] better known as
mad cow disease and is another threat to humans.
*As a protein extracted from fish, it is mainly used as a surgical
suture, as biomimetic scaffold, and as a cosmetic aid to decrease
the appearance of wrinkles since collagen makes up to 70% of
protein in the skin and helps to keep it elastic.
Marine Biopolymers and Derivatives
Fish Gelatin
*Fish gelatin is a protein product produced by partial hydrolysis
of collagen-rich fish skin (or) scale material.
*The gelatin molecule is made up of amino acids joined together
by amide linkages in a long molecular chain.
*Gelatin is a versatile hydro- colloid and is widely applied in food,
pharmaceutical, cosmetic, medical, and photographic products.
*The most important properties of gelatin are thermoreversible gel
formation, texturing, thickening, high water-binding capacity,
emulsion formation and stabilization, foam formation, protective
colloidal function, and adhesion/ cohesion.
*Gelatin is widely used in the food industry such as an ingredient
to improve the elasticity, the consistency, and the stability of
foods
Uses of Gelatin
Applications in Food and Confectionery
*Gelatin desserts, all types of jellies, are examples of food products
that take advantage of the thermoreversible gel formation and the
ā€œmelt-in-the-mouthā€ texture of gelatin
*The addition of gelatin to dairy products improves the emulsifying
capacity as gelatin molecules associate to the surface of the fat
droplets and thereby reduce the surface tension towards the
aqueous phase.
*By adding gelatin to foamed milk-based desserts like yogurt,
curds, ice creams, and mousses, gelatin depresses the surface
tension of water, enabling formation of foam by mechanical
whipping or injection of gas.
*The meat processing industry also applies gelatin to their
products for several reasons, but the ability to bind water and
meat juices and to secure good texture and taste is very
important.
Uses of Gelatin
Applications in Food and Confectionery
*Gelatin is also widely used in low-fat (fat replacer), low-carb
(binding agent), and low-calorie (fat replacer and binding agent)
food products.
*The lower melting temperature in gel desserts made from fish
gelatins may acceler- ate flavor release
*The confectionery industry uses gelatin not only for its
thermoreversible gelling properties but also for foam formation
and stabilization, binding, emulsification, and controlling sugar
crystallization
Uses of Gelatin
Pharmaceutical Applications
*Gelatin is an important and versatile excipient for pharmaceutical
and medical applications.
*The widespread utilization of gelatin in pharmaceuticals and
medical devices is due to several excellent properties.
*It is established as a pharmaceutical excipient, tolerated in food
(nontoxic, non-allergenic), GRAS status, excellent
biocompatibility, high quality (purity), low immunological activity,
and controllable physical parameters.
*Gelatin is utilized in plasma substitutes used in emergency
medicine and surgery; in vitamin coatings, pastilles, and tablets;
in the production of globules, paste dressings, and sponges; and
in the formulation of new vaccines.
*About 90% of all gelatin of pharmaceutical grade is applied in
capsule production ā€“ soft and hard gelatin capsules.
Uses of Gelatin
Nutritional and Health Properties
*Gelatin is a high-quality source of protein and free of cholesterol
and sugar and contains practically no fat.
*Gelatin is easily digested and completely broken down by the
human organism.
*Gelatin is applied in food products to enrich the protein content
and to reduce the amount of carbohydrates, the salt
concentration, and the amount of fat in low-fat products and as a
carrier for vitamins.
*Some international studies suggest that gelatin may have a
preventive and regenerative effect on the skeleton and locomotor
system ā€“ especially bones, cartilage, tendons, and ligaments.
*It is also suggested that gelatin may help fortify hair if taken
regularly and strengthen the connective tissue, thus ensuring firm
skin, shiny hair, and strong fingernails.
Uses of Gelatin
Cosmetic Applications
*Collagen and gelatin (from bovine, porcine, and fish sources) play
important roles in skin and hair products as functional
ingredients.
* Gelatin hydrolysates are, for example, added to skin creams to
improve the water-binding capacity, to reduce transepidermal
water loss, and to improve skin feel.
*The classical food and cosmetic and pharmaceutical properties of
gelatin are based mainly on its gel-forming and viscoelastic
properties.
* Recently, and especially in the food industry, an increasing
number of new applications have been found for gelatin in
products such as emulsifiers, foaming agents, colloid stabilizers,
fining agents, biodegradable packaging materials, and
microencapsulating agents, in line with the growing trend to
replace synthetic agents with more natural ones.
Uses of Gelatin
Gelatin-Based Biomaterial Scaffolds
*Antimicrobial fish skin gelatin films are a promising entity in
retaining antibacterial activity and inhibiting bacterial
contaminants.
*Zinc oxide nanoparticles on the antimicrobial activity of films
based on tilapia skin and fish protein isolate provide safety and
extend the shelf life of packaged foods.
*Silver-copper nanoparticles had the same positive effect on the
antimicrobial properties of fish skin gelatin films and could
improve their mechanical and thermal properties.
*Chitosan is another agent that has been added to fish gelatin-
based films due to its antimicrobial action against a variety of
fungi and Gram-positive and Gram-negative bacteria.
*Chitosan-gelatin film could be used as active packaging to
preserve fish under refrigerated storage.
Chitin and Chitosan
* Chitin and chitosan are known natural polysaccharide-based biodegradable polymers,
which are extracted particularly from the exoskeletons of marine invertebrates. .
* Chitosans are deacetylated forms of chitin, and their polymers differ in their degree
of acetylation. Chitin, as well as chitosan, has high molecular weight, and both are
viscous and highly hydrophobic and are insoluble in water.
* Chitin and chitosan and their derivatives exhibit diverse bioactivities, including
ā€¢ antioxidant,
ā€¢ antihypertensive,
ā€¢ anti-inflammatory,
ā€¢ anticoagulant,
ā€¢ antitumor
ā€¢ anticancer,
ā€¢ antimicrobial,
ā€¢ hypocholesterolemic, and
ā€¢ antidiabetic effects
Chitin and Chitosan
* Chitin has excellent biocompatibility, nontoxicity, and wound healing properties
* Chitin has been widely applied in medical and healthcare fields for applications such
as release capsules for drugs, man-made kidney membranes,
* chitosan is used as a material for contact and intraocular lenses and found to
expedite blood clotting.
* chitin compounds are biodegradable makes them particularly appropriate for use in
drug delivery systems, as they can act as carriers that release drugs slowly ā€“ a
property extremely valuable in cancer chemotherapy.
* Chitin has been evidenced as a potent innate immune stimulator of macrophages and
other innate immune cells.
* Chitin is able to suppress allergen-induced type II allergic responses.
* A chitosan compound is also being investigated as an inhibitor of the AIDS virus
The bioactive and other roles of chitin and chitosan
Chitin/chitosan Applications
Beads Use in drug delivery systems
Microspheres Enzyme immobilization substrate
Nanoparticles As potent gene delivery vehicles
Encapsulation of sensitive drugs
Coatings Used in surface modification and as textile finishes
Fibers Used as medical textiles and surgical sutures
Nanofibers Useful for guided bone regeneration
Nonwoven bioactive
fibers
Acts as a scaffold for nerve tissue regeneration and
aid in the wound healing processes
Films Application in wound care formulations, as dialysis
membrane and antitumor agents and Used as a
semipermeable film for wound dressing
Powder Used as an adsorbent for pharmaceutical and
medical devices, surgical
glove powder, and enzyme immobilization
The bioactive and other roles of chitin and chitosan
Shaped objects Employability in orthopedics and manufacture of
contact lenses
Solutions Used in cosmetics, as bacteriostatic agent,
hemostatic agent, anticoagulants, antitumor agent,
gene delivery systems, and spermicidal
action
Gels Used as drug delivery vehicle, as implants, coating,
and in tissue
Engineering
Tablets Acts as a compressed diluent, disintegrating agent,
and excipient
Capsules Targeted drug delivery vehicle
Sponge Mucosal hemostatic dressing, wound dressing, drug
delivery, enzyme
entrapment, artificial skin
Proteoglycans and Glycosaminoglycans
Proteoglycans
*Proteoglycans (PGs) are a family of complex macromolecules
distinguished by the covalent attachment of one or more
glycosaminoglycan (GAG) chain(s) (N- and /or O-linked
oligosaccharides) with matrix proteins (core proteins).
*They are associated with each other and also with other major
structural components of the matrix, viz., collagen and elastin,
and play important roles in determining the structural
organization of the matrix and in fundamental biological
processes such as cell growth and development
Proteoglycans and Glycosaminoglycans
Proteoglycans
* Proteoglycans have a number of important biologic roles like
anticoagulant activity, anti-atherosclerotic, anti-inflammatory,
and also as fat- clearing agent.
*Proteoglycans act also as tissue organizers, influence cell growth
and the maturation of specialized tissues,
*Proteoglycans play a role as biological filters and modulate growth
factor activities, regulate collagen fibrillogenesis and skin tensile
strength, affect tumor cell growth and invasion, and influence
corneal transparency and neurite outgrowth.
Proteoglycans and Glycosaminoglycans
Glycosaminoglycans
*Structurally the simplest and best known of the heteropolysaccharides are
the glycosaminoglycans (GAGs).
*GAGs such as hyaluronic acid, heparin, and chondroitin sulfate have several
applications in the medical, veterinary, pharmaceutical, and cosmetic field.
*The use of powdered shark cartilage for wound healing and as
antiangiogenic, anti-arthritic, and antitumor agent from ancient times has
been attributed to the presence of glycosaminoglycans.
*Proteoglycans play a role as biological filters and modulate growth factor
activities, regulate collagen fibrillogenesis and skin tensile strength, affect
tumor cell growth and invasion, and influence corneal transparency and
neurite outgrowth.
Antioxidant Pigments and Polyphenols
Antioxidant Pigments
*Marine natural pigments have considerable medicinal potential and
promising applications in human health.
*The major categories of pigments by chemical structure occur either as
tetrapyrolles (chlorophyll and heme pigments), carotenoids, indole
derivatives (quinones and violacein), alkaloids (prodiginines and
tamb- jamines), polyenes, macrolides, peptides, or terpenoids.
*Many of these pigments have a variety of biological activities, including
antitumor, antibacterial, antioxidant, and anti-inflammatory activity
Antioxidant Pigments and Polyphenols
Carotenoids
*Carotenoids are widely present in marine environments and
responsible for the color of many important marine species of fish,
shellfish, and seaweeds.
*These yellow-to-orange-red pigments, called carotenoids, of
which there are over 700 different chemical formulations, are
typically divided into two subgroups,
*the carotenes (hydrocarbon carotenoids) and
*the xanthophylls (oxygenated carotenoids).
Antioxidant Pigments and Polyphenols
Carotenoids
*Commonly found carotenoids from aquatic animals are
astaxanthin, zeaxanthin, tunaxanthin, lutein, etc.
*Marine red and brown algae pro- duce Ī²-carotene, zeaxanthin,
fucoxanthin, and fucoxanthinol.
*Astaxanthin is the main carotenoid pigment found in aquatic
animals, while fucoxanthin is abundant in aquatic plants.
*These abundant representative marine carotenoids astaxanthin
and fucoxanthin have been reported to be effective antioxidants
and have higher biological activity than those of terrestrial origin
Pigment Bacterial source Bioactivity Color
Astaxanthin Agrobacterium aurantiacum Antioxidation Red
Cycloprodigiosin Pseudoalteromonas denitrificans Anticancer;
immunosuppressa
nt; antimalarial
Red
Heptyl prodigiosin Ī±-Proteobacteria Antiplasmodial Red
Indigoidine Streptomyces chromofuscus
ATCC 49982
Dye-industrial
applications
Blue
Melanins Vibrio cholerae, Shewanella colwelliana,
Cellulophaga tyrosinoxydans Protection from
UV irradiation
Black
Phenazine derivatives Bacillus sp. Cytotoxic Brownish
yellow
Pyocyanin and
pyorubrin (Phenazine
derivatives)
Pseudomonas aeruginosa Antibacterial Blue-
green
Scytonemin Cyanobacteria Protection from UV
irradiation
Yellow-
green
Anti-inflammatory,
antiproliferative
Tambjamines Pseudoalteromonas tunicata Antibiotic, anticancer Yellow
Tryptanthrin Cytophaga Antibiotic Deep
yellow
Violacein Pseudoalteromonas tunicate Antibiotic;
antiprotozoan;
anticancer
Violet
Natural pigments isolated from marine bacteria
Antioxidant Pigments and Polyphenols
Carotenoids - Astaxanthin
*Astaxanthin is the ā€œKing of Carotenoids.ā€ It is the red pigment that
gives salmon, shrimp, and flamingos their pink-red color.
*Astaxanthin is a red pigment from the xanthophyll oxygen-
carrying group of carotenoids.
*Many aquatic species including crustaceans utilize these algae
and plankton as food and store the pigment in their shell,
resulting in their pink-red exterior.
Antioxidant Pigments and Polyphenols
Carotenoids - Astaxanthin
*Astaxanthin functions as an intracellular oxygen reserve and
fishes and invertebrates fed on a diet containing optimal levels of
astaxanthin that show greater survivability rates when subjected
to poor oxygen environments as it is a potent antioxidant,
comparable to vitamin E.
*It may also offer protection against UV light.
*Antioxidant activity of astaxanthin has been reported to be several
times higher than that of other carotenoids and tocopherols
Antioxidant Pigments and Polyphenols
Carotenoids - Fucoxanthin
*Fucoxanthin is an important pigment found in aquatic plants.
*Fucoxanthins possess strong DPPH (2, 2-diphenyl-1-
picrylhydrazyl) radical scavenging activity.
*In addition to antioxidant activity, fucoxanthin from edible sea-
weeds exhibited anti-obesity effect and antidiabetic effect,
complemented by DHA synthesis in mouse liver.
Antioxidant Pigments and Polyphenols
Antioxidant Polyphenols
*A series of polyphenols including catechins (e.g., gallocatechins,
epicatechins, and catechin gallate), flavonols, and flavonoid
glycosides have also been identified in several red and brown
algae.
*Algal polyphenols exhibit their bioactive potential as potent free
radical scavengers and primary chain-breaking antioxidants.
*Phlorotannins are a group of polyphloroglucinol phenolics and are
mainly stored within cell organelles called physodes.
*Antidiabetic and antioxidant effects of methanol extract from the
brown algae, Ecklonia stolonifera, were reported
Seaweed Polysaccharides
*Abundant and renewable marine biomass, seaweeds are a part of the
human diet in many Asian countries and also traditionally been used as
medicines since ancient times.
* The earliest records of herbal medical seaweeds appeared in Chinese
literature about 2000 years ago.
*Several species of seaweed have the capacity to produce a diverse array
of secondary metabolites, which exhibit important and vital ecological
roles as defense.
*Seaweeds are also a rich source of bioactive polysaccharides. The
remarkable marine polysaccharides found in red and brown algae, viz.,
alginate, agar, and carrageenan,
*Provide numerous ingredients to the food, pharmaceutical, cosmetic,
textiles, paper, and
* Biotechnology industries as stabilizers, thickeners, emulsifier, and fillers
*Other seaweed hydrocolloids, besides those common seaweed
hydrocolloids (alginate, agar, and carrageenan), are fucoidan, laminarin,
mannitol, funoran, ulvan, etc
Seaweed Polysaccharides
*There are numerous commercial applications of marine polysaccharides
as food, beverages, and supplements.
* In addition, these molecules have many biological functions including
antimicrobial, anticoagulant, antiproliferative, antithrombotic, and anti-
inflammatory activity.
*These marine-derived secondary metabolites also have many human
health benefits which enable them to be applied as nutraceuticals.
*In the biomedical field, the polysaccharides from algae can be used in
controlled drug delivery, wound management, and regenerative medicine
*Seaweeds are classified into four principal group based on their
pigments, namely, red, brown, blue, and blue-green. Only the red
(Rhodophyceae) and brown (Phaeophyceae) seaweeds are important
sources of hydrocolloids
Seaweed Polysaccharides
Agar
*Agar - extracted from red seaweed (Rhodophyceae), specifically Gracilaria
sp., Gelidium sp., and Pterocladia/Gelidiella sp
*Agar consists of a mixture of two polysaccharides, namely, agarose and
agaropectin, with agarose making up about 70% of the mixture.
*Agarose is responsible for gelling, while agaropectin is responsible for
thickening properties.
*About 80% of agar produced globally is used for food applications, while
remaining 10ā€“20% is used in pharmaceutical and biotechnology
industries.
*Low-quality agar is used basically in food stuff (frozen foods, bakery
icings, meringues, dessert gels, candies, etc.), while some may extend to
industry applications for paper sizing, coating, adhesives, textile
printing/dyeing, casting, and impression.
Seaweed Polysaccharides
Agar
*Agar - extracted from red seaweed (Rhodophyceae), specifically Gracilaria
sp., Gelidium sp., and Pterocladia/Gelidiella sp
*Agar consists of a mixture of two polysaccharides, namely, agarose and
agaropectin, with agarose making up about 70% of the mixture.
*Agarose is responsible for gelling, while agaropectin is responsible for
thickening properties.
*About 80% of agar produced globally is used for food applications, while
remaining 10ā€“20% is used in pharmaceutical and biotechnology
industries.
*Low-quality agar is used basically in food stuff (frozen foods, bakery
icings, meringues, dessert gels, candies, etc.), while some may extend to
industry applications for paper sizing, coating, adhesives, textile
printing/dyeing, casting, and impression.
Seaweed Polysaccharides
Carrageenan
*Carrageenans are a class of sulfated galactans extracted from
different species of red seaweed (Rhodophyta). The main seaweed
species used in industrial scale for carrageenan production are
Kappaphycus alvarezii, Eucheuma denticulatum, Chondrus
crispus, and Gigartina sp.
*Carrageenans are hydrophilic linear hydrocolloids, consisting
mainly of potassium, sodium, magnesium, and calcium salts of
sulfated esters of D-galactose nd 3,6-anhydro-D-galactose
*Carrageenan has been widely used for drug delivery applications
in different isoforms including nanoparticles, micro stabilizers,
gelling agent, beads, micro- spheres, and microcapsules.
*Carrageenan-based hydrogels and carrageenan- graphene oxide
composites are widely employed for bone tissue engineering
Seaweed Polysaccharides
Alginate
*Alginate is distinguished from other hydrocolloids (agar and
carrageenan) because it is isolated from brown seaweed (Phaeophyceae)
specifically from outer layer of brown algae cell wall, as inner layer
makes up mostly of
*Alginate is widely used in industry because of its ability to retain water
and its gelling, viscosifying, and stabilizing properties.
*Alginate is an excellent stabilizing and thickening agent in food such as
jelly, ice cream, desserts, etc. due to its properties to chelate metal ions
to form highly
*Alginate oligosaccharides, low molecular polymer fragments obtained by
enzymatic depolymerization, and acid hydrolysis - unique
pharmaceutical properties - antioxidant, antifungal, anti-inflammatory,
and antibacterial activities viscous solutions cellulose.
Seaweed
Other Polysaccharide
Compound
Activity
U. pinnatifida, A.
platensis, Porphyridium
sp.
Fucoidans from
microalgae
Anticancer activity
Nanofiber production
BioGlue for soft tissue closure after
surgery, lubricants for
bone joints
A. nodosum, E. bicyclis,
Fucus sp., Laminaria
sp., U. pinnatifida, C.
vulgaris
Laminarin (Ī²-glucans)
Tissue regeneration
Burn wound dressings
Wound healing
Ulva rigida, Ulva spp. Ulvans
Nano fibers
Tissue engineering
Wound dressings
Bioactive Metabolites of Marine Algae,
Fungi and Bacteria
*Chemically the bioactive metabolites of marine flora include
ļ±brominated phenols,
ļ±oxygen heterocyclics,
ļ±nitrogen heterocyclics,
ļ±sulphur nitrogen heterocyclics, sterols,
ļ±terpenoids,
ļ± polysaccharides,
ļ±peptides and
ļ±proteins.
Bioactive Metabolites of Marine Algae,
metabolites Source use
Brominated Phenols The green, brown and red
algae
Symphyocladia gracilis,
Rhodomela larix and
Polysiphonia lanosa
Antibacterial and
antifungal activities
Brominated Oxygen
Heterocyclics
(laurencin and
laureatin)
The red algae Laurencia sp Larvicidal activities
Nitrogen Heterocyclics
(Domoic acid and the
kainic acid)
Marine algae
Chondria armata
Red alga Digenea simplex
Anthelmintic agent
Guanidine Derivatives
saxitoxin
Gonyaulax catenella - red tide Neurotropic effects
Phenazine Derivatives
caulerpicine, caulerpin
The marine alga
Caulerpa sp
Mild anesthetic
action when placed
in the mouth
Bioactive Metabolites of Marine Algae,
Metabolites Source use
Amino Acids and Amines
Laminine (L-lysine, L-arginine,
ethanolamine and choline)
Volatile amines, such as
methylamine, dimethylamine,
trimethylamine, ethylamine,
propylamine, isobutylamine,
isoamylamine, 2-
phenylethylamine and 2-
methylmercapto propylamine
Marine algae
Laminaria angustata
and Chondria amata
Red, green and brown
algae
Transitory
hypotensive effect
Sterols
Cholesterol, 22-
dehydrocholesterol and
demosterol
Red Algae
Rhodymenia palmata,
Porphyra purpurea, P.
umbilicalis and
Halosaccion
ramentaceum
Hypnea musciformis
Hypnea japonica
Reduce blood
cholesterol level
To reduce the
tendency to form
a fatty liver and
excessive fat
deposition in the
heart
Bioactive Metabolites of Marine Algae,
metabolites Source use
Sterols
Fucosterol
Brown Algae Reduce blood
cholesterol level
To reduce the tendency
to form a fatty liver and
excessive fat deposition
in the heart
chondrillasterol,
poriferasterol,
28-isofucosterol,
ergosterol and
cholesterol
Green algae
Sulfated
Polysaccharides
the rhodophyceae (red algae),
the phaeophyceae (brown algae),
the cyanophyceae (blue-green algae)
and the chlorophyceae (green algae)
Carrageenan Species of Chondrus, Eucheuma,
Gigartina and Iridea
Antiviral,
to stimulate the growth
of connective tissues,
anticoagulant and
antithrombic agent
Bioactive Metabolites of Marine Algae,
metabolites Source use
Alginic acid Brown algae
species of Fucus, Laminaria and
Macrocystis
sodium alginate from giant brown seaweed (Macrocystis pyrifera), horsetail kelp
(Laminaria digitata) and sugar kelp (Laminaria saccharina)
1. used mainly in the manufacture of ice cream where it serves as a stabilising
colloid. It is also used in cosmetics and pharmaceuticals.
2. useful adjuvent in immunisation against two strains of influenza virus.
3. Sodium alginate is also found effective in diminishing hyper calciuria in
urolithiasis, and found useful in the treatment of esophagitis
4. The most significant property of sodium alginate is the ability to remove
strontium 85 and strontium 87 from the body without seriously affecting the
availability of Ca, Na or K in the body.
5. This selective action of sodium alginate is of great potential to remove Sr-90
contamination due to fall out from atomic explosions.
Calcium alginate is reputed to be a hemostatic agent which stimulates the
clotting of blood in situ which is subsequently absorbed in the tissue
Bioactive Metabolites of Marine Algae,
metabolites Source use
Sulfated
Polysaccharides
Laminarin Laminaria cloustoni Anticoagulant
properties,
also reported to have
antilipidemic activity
like that of heparin
Agar and
Agarose
Red algae are the source of agar and
agarose
The genera Gelidium, Gracilaria,
Acanthopeltis and Pterocladia of the
Rhodophyceae are the main
producers
No direct medicinal
use, their use in
biomedical research
Bioactive Metabolites of Marine Bacteria
and Fungi,
*Bacteria and fungi are prime producers of the antagonistic
substances in terrestrial environment.
*Antibiotic, antiviral, antifungal, and antiyeast activities of these
organisms had been reported.
*Besides, a few growth stimulant properties which may be useful
in studies on wound healing, carcinogenic properties, and in the
study of cancers are reported
*many bacteria showing antimicrobial activity, a variant of the
ichthyotoxic Pseudomonas piscicida exhibited marked
antagonism to various micro-organisms
*A red coloured bacterium found to excrete vitamin B and
antibacterial substances into the sea water.
Bioactive Metabolites of Marine Bacteria
and Fungi,
*The bacteria and fungi from sea are also reported to produce
substances which affect
ā€¢ central nervous system (CNS),
ā€¢ respiratory system (RS),
ā€¢ neuromuscular system (NMS),
ā€¢ autonomic nervous system (ANS),
ā€¢ cardiovascular system (CVS) and
ā€¢ gastrointestinal system (GI).77
*Some of the substances are known to produce local effects such
as pain, necrosis, edema, parasthesias, pruritis etc
Bioactive Metabolites of Marine Bacteria
and Fungi,
metabolites Source use
Cephalosporins
Penicillinase
sensitive antibiotic
substance named
antibiotic N
Cephalosporium acremonium Active against Gram-
positive bacteria
Active against a
number of penicillin
resistant
Staphylococcus
Bromo pyrrole
antibiotic
Pseudomonas bromoutilis Activity against many
Gram-positive bacteria
Pyrrolnitrin , a
chloropyrrole
Pseudomonas pyrrocinia This compound was
marketed in Japan
under the name PYRO-
ACE - dermatophytic
fungal infections.
Red coloured
antibiotic named
prodigiosin
Serratia marcescens Antibiotic and
antifungal activities
use as a therapeutic
agent
Bioactive Metabolites of Marine Bacteria
and Fungi,
metabolites Source use
Aplysiatoxins
and oscillatoxins
isolated from
blue-green algae
Schizothrix calcicola and
Oscillatoria nigroviridis
Antileukaemic activity but their
high toxicity precludes their
medicinal use
Cytotoxic and fungicidal
nucleosides
Anatoxin-a Anabaena flosaquae Most potent nicotinic receptor
agonist.
Treating disorders associated with
defects in cholinergic regions of
the central nervous system
Ichthyotoxin Several species of green-
algae of the genus
Halimeda
Exhibits diverse biological
activities,
Inhibits the growth of marine
bacteria and fungi, cell division of
fertilized sea-urchin eggs and the
motility of sea-urchin sperms at 1
Āµg/mL
Bioactive Metabolites of Marine Bacteria
and Fungi,
Metabolites Source use
Avrainvilleol Green algae, Avrainvillea
longicaulis
Exhibits high order of antifeedant
activity in reef fish and also
inhibits the growth of
microorganisms.
Diterpenoids The genera Halimeda,
Penicillus and Udotea
Exhibit cytotoxic and
antimicrobial activities
Prenylated
aromatics,
unsaturated C11
hydrocarbons
Dictyopteris
plagiogramma and D.
australis
Sex attractants
Brominated
acetylenic
compounds
Laurentia nipponica Active against mosquito larvae
Trihydroxy
benzyl methyl
ethers
Grateloupia filicina Antibacterial activity against
Bacillus subtilis
Bioactive Metabolites of Micro Algae
*Micro algae represent a subset of single cell microorganisms.
*Generally grow autotropically using CO2 as the sole carbon source and
light as energy.
*These algae are ubiquitous in nature.
*Aquatic micro algae have been isolated in areas ranging from hot springs to
glacial ice flows.
*There are over 50,000 different species of micro algae of which only a few
have been characterised.
*Micro algae represent a major untapped resource of genetic potential for
valuable bioactive agents and biochemicals
*Proteinaceous.
*Rich in reserves of oils containing various amounts of eicosapentaenoic
acid (EPA) and docosahexaenoic acid (DHA). Considered to be responsible
to reduce incidence of coronary heart disease
*used for the production of labelled biochemicals.
*Phycobiliproteins can be commercially produced from Spirulina and the red
microalgae Porphyridium and Rhodella.
*Phycobiliproteins are widely used in clinical or research immunology
because they are very powerful and highly sensitive fluorescent properties
Bioactive Metabolites of Micro Algae
Metabolites Source use
Phycocyanin Cyanobateria
(Spirulina), Blue green
Algae
Potential effect to treat effectively
type-2 diabetes mellitus by
inhibiting Ī±-amylase and Ī±-
glucosidase.
Phycoerythrin Porphyridium cruentum
Red algae
Immunomodulating activity
Anticancer activity
Development of phycofluor probes
for immunodiagnostics.
ā€¢ Phycobiliproteins are used as colorants in food.
ā€¢ cosmetics such as lipstick and eyeliners in Japan, Thailand and China
ā€¢ Dainippon Ink and Chemicals produces a blue food colourant from Spirulina,
called Lina blue, that is used in chewing gum, ice slush, sweets, soft drinks,
dairy products and wasabi.
ā€¢ Heavy isotope labeled metabolites and Phycoerythrin (from Red algae and
cyanobacteria) used as fluorescent labels could have values far exceeding
$10,000 per kg.
ā€¢ Micro algae are also expected to furnish potent antiviral, antiAIDS, antibiotic
and other bioactive agents
Bioactive Metabolites of Marine
Invertebrates
Metabolites Source use
Avrainvilleol Green algae, Avrainvillea
longicaulis
Exhibits high order of antifeedant
activity in reef fish and also
inhibits the growth of
microorganisms.
Diterpenoids The genera Halimeda,
Penicillus and Udotea
Exhibit cytotoxic and
antimicrobial activities
Prenylated
aromatics,
unsaturated C11
hydrocarbons
Dictyopteris
plagiogramma and D.
australis
Sex attractants
Brominated
acetylenic
compounds
Laurentia nipponica Active against mosquito larvae
Trihydroxy
benzyl methyl
ethers
Grateloupia filicina Antibacterial activity against
Bacillus subtilis
ļƒ˜Hemolymph is the main source of AMPs in marine invertebrates,
even though other tissues may also contain these peptides.
AMPs Source Activity
Penaeidins Penaeus vannamei Microbicidal properties
Defensins, myticins, and
mytilins
Marine Mollusks
Mytilus galloprovincialis and
Mytilus edulis
Innate immune mechanisms
Scylla serrata
antimicrobial protein
S. serrata
Antimicrobial action against various
Gram-positive and Gram-negative
bacteria
Phoriospongin A and B
Australian marine sponges
(Phoriospongia sp. and
Callyspongia bilamellata)
Nematocide
Blood-depressing substance I
(BDS-I)
Sea anemone Antibacterial and neurotoxic (sodium
channel blocker)
Aurelin
Jelly fish (Aurelia aurita)
Antimicrobial
Centrocins, strongylocins
Green sea urchin
(Strongylocentrotus droebachiensis) Antimicrobial
*Marine peptides are important bioactive natural products that
are present in many marine species.
*These marine peptides have high potential nutraceutical and
medicinal values because of their broad spectra of bioactivities.
*The role of marine peptides as antimicrobial peptides (AMPs)
possessing antibacterial, antiviral, antifungal, and
antiprotozoal functions.
*Peptides containing histidine, tryptophan, and tyrosine
possessed antioxidative activity.
*The amino acids proline, alanine, and leucine contribute to
radical scavenging activity when located in the C-terminal in an
aminaocid sequence.
*Antioxidant peptide derived from different marine animals
exhibits varying potencies to free radical scavenging and
various antioxidant mechanisms.
*More than 100 species of marine fish are traditionally used in
medicines to treat tumors.
*The antitumor/cytotoxic marine peptides can be classified into four
types:
ā€¢ (i) linear depsipeptides (e.g., dolastatin 10);
ā€¢ (ii) cyclic depsipeptides (e.g., kaha- lalide F);
ā€¢ (iii) linear peptides (e.g., pardaxin); and
ā€¢ (iv) marine protein hydrolysates
*The digested hydrolysates of peptides from tuna dark mus- cle
exhibited antiproliferative activity on human breast cancer cell line
MCF-7.
*Peptide hydrolysates from oyster extract expressed in vivo antitumor
activity in BALB/c mice.
* Tunicate extract and squid gelatin hydrolysates also demonstrated
in vitro cytotoxic effect on several human cancer cell lines.
*Antihypertensive peptides or angiotensin-I converting enzyme
(ACE) inhibitory peptides have been isolated from fish protein
hydrolysates.
*Angiotensin-I converting enzyme (ACE) is a dipeptidyl
carboxypeptidase (EC. 3.4.15.1) important for the regulation of
blood pressure and normal heart function
*ACE-inhibiting peptides have been isolated from fish protein
hydroly- sate such as Alaska pollock skin hydrolysate,
Sardinella aurita, yellowfin sole, salmon muscle, sea bream
scales, and tuna frame proteins as well as squid and cuttlefish
hydrolysates.
*The cardiovascular protective peptides include bioactive
peptides which exhibit activities important to cardiovascular
health, including effects on blood pressure, oxidative stress
coagulation, atherosclerosis, and lipid metabolism.
*The anticoagulant peptide binds to coagulation factors in the
blood clotting intrinsic pathway and inhibits their molecular
interaction.
*The anti- atherosclerotic peptides showed their cardiovascular
protection effect by suppressing the inflammatory responses in
histamine-stimulated endothelial cells that may be related to
early atherosclerosis.
*Fish protein lowers serum cholesterol level by retarding
absorption and promoting excretion of cholesterol and bile acid
attributed to lowered micellar solubility of cholesterol and
enhanced bile acid-binding capacity
Neuropeptides
*Neuropeptides derived from marine species have potential as
natural and safe alternative to opioid drugs for anxiety and
stress management.
*Opioid- like peptides exhibit a positive effect on motivation,
emotion, behavior, stress, appetite, and pain management by
interacting with specific opioid receptors in the nervous,
endocrine, immune, and digestive systems.
*The gonadotropin-releasing hormone, which increases the
secretion of pituitary gonadotropin
*Neuroprotective Peptides Marine proteins and peptides
suppress the development of neurodegenerative diseases like
Parkinsonā€™s disease, Alzheimerā€™s disease, and multiple
sclerosis.
*Neuroprotective Peptides
*Neuroprotective Peptides Marine proteins and peptides
suppress the development of neurodegenerative diseases like
Parkinsonā€™s disease, Alzheimerā€™s disease, and multiple
sclerosis.
*Their neuroprotective action is brought about by the direct
inter- action of absorbed protein and peptide with a variety of
cellular and molecular tar- gets with enzyme/ion channels.
*The neuroprotective peptide (HTP-1) Gly-Thr-Glu-Asp-Glu-Leu-
Asp-Lys from the seahorse Hippocampus trimaculatus exerted a
protective action on PC12 cells and prevented them from the
deleterious action of Ī² amyloid plaques (amyloid Ī²42), which is
associated with the pathogenesis of Alzheimerā€™s disease.
*Analgesic Peptides Conopeptides from marine snail venoms have
attracted much interest in drug design for chronic neuropathic pain.
*Appetite-Suppressing Peptides Low-molecular-weight peptides from
fish and shrimp head protein hydrolysates have been found to be
effective for stimulating cholecystokinin release in STC-1 cells by
regulation of cholecystokinin release.
*Marine peptides may be employed as anorexigenic agents and may
interact with appetite-suppressing gut hormones including
cholecystokinin and glucagon-like peptide 1 to produce anti-obesity
effects.
*The neuroprotective peptide (HTP-1) Gly-Thr-Glu-Asp-Glu-Leu-Asp-
Lys from the seahorse Hippocampus trimaculatus exerted a protective
action on PC12 cells and prevented them from the deleterious action
of Ī² amyloid plaques (amyloid Ī²42), which is associated with the
pathogenesis of Alzheimerā€™s disease.
*Food Preservation According to Gomez-Guillen et al. (2011),
Antimicrobial peptides can also be used in natural
biopreservation to control spoilage and foodborne pathogens.
*The peptide CgPep33 from Pacific oysters is used to inhibit the
activity against gray mold disease in strawberries.
* CgPep33 can therefore be used as a substitute for fungicide to
control postharvest diseases and to extend the shelf life of
fruits and vegetables
*Protein hydrolysates also function as cryoprotectants, reduce
lipid oxidation, enhance water retention, and suppress
dehydration-induced denaturation of myofibrils in foods
* POTENTIAL USE OF MARINE DERIVED
COMPOUNDS IN COSMETICS
*Oceans are home to a wide range of microbial biodiversity, including
many organisms with high potential of producing bioactive compounds,
such as thraustochytrids
*Some compounds within marine organisms are already widely used
within the cosmetic industry, as
*they provide a renewable source for compounds used in bulk, such as
agar and carrageenan, used in cosmetics to increase the viscosity of
formulations. Smaller marine molecules are also used for:
ļƒ˜Promoting skin hydration
ļƒ˜Improving acne
ļƒ˜UV protection
ļƒ˜Reduce wrinkles
1. D. S. Bhakuni, D. S. Rawat (2005)- Bioactive Marine Natural
Products-Springer Netherlands.
2. Saleena Mathew, Maya Raman, Manjusha Kalarikkathara
Parameswaran, Dhanya Pulikkottil Rajan (2019), Fish and Fishery
Products Analysis_ A Theoretical and Practical Perspective-Springer
Singapore.
3. Blanca HernƔndez-Ledesma, Miguel Herrero (2013),Bioactive
Compounds from Marine Foods_ Plant and Animal Sources-Wiley-
Blackwell.
4. Centella, M.H., et al., Marine-derived bioactive compounds for
value-added applications in bio- and non-bio sectors, Journal of
Cleaner Production (2017).
5. http://dx.doi.org/10.1016/j.jclepro.2017.05.086
6. https://www.glycopedia.eu/e-chapters/from-chitin-to-
chitosan/article/extraction-of-chitin-preparation-of-chitosan
Marine Bioactive Compounds Sources Therapies

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Marine Bioactive Compounds Sources Therapies

  • 2. Marine bioactive compounds *Marine flora and fauna are excellent sources of bioactive compounds with therapeutic benefits. *The biodiversity of the marine environment and its associated chemical diversity contribute to an almost unlimited resource of new bioactive compounds. * Bioactive compounds can be isolated from various sources including marine plants, animals, microorganisms and sponges with unique set of molecules. *Bioactive compounds extracted from these organisms are effective against different infectious and non-infectious diseases.
  • 3. Marine bioactive compounds *Investigations on marine natural products have focused on areas like ā€¢ marine nutraceuticals, ā€¢ biopolymers, ā€¢ biofilms, ā€¢ CNS-membrane active toxins and ā€¢ ion channel effectors, ā€¢ antifouling, ā€¢ anti- cancer and antiviral agents, ā€¢ tumor promoters, ā€¢ anti-inflammatory agents, *Encouraging a multidisciplinary approach between biologists, chemists, and pharmacologists. *It is also important to note that the number of com- pounds reported annually is increasing steadily *Marine organisms will continue to be sufficient sources of natural bioactive substances.
  • 4.
  • 5. Marine bioactive compounds *Numerous marine bioactive compounds are utilized in different food products at industrial scale. *Marine products are rich in ā€¢ proteins containing both essential and non-essential amino acids, ā€¢ polysaccharides, ā€¢ polyunsaturated fatty acids (PUFAs), ā€¢ vitamins, minerals and many other nutrients *These compounds can be isolated from Fish and shellfish molluscs (including mussel, oyster, scallop, abalone, snail and conch) cephalopods (including squid, cuttlefish and octopus) crustaceans (including crayfish, crab, shrimp and lobster), echinoderms, seaweeds and microalgae
  • 6.
  • 7. Marine Biopolymers and Derivatives *Fish processing generates solid wastes (skin, scales, and bones) that can be as high as 80% of the original raw material and are excellent sources of high value products. *The utilization of fish wastes helps to eliminate harmful environmental aspects of pollution and improve quality in fish processing. *An important waste reduction strategy for the industry is the recovery of marketable by-products from fish wastes. *The two most important marine biopolymers collagen as well as the polysaccharide polymer, chitin, and their derivatives gelatin and chitosan, respectively, are a promising entity in this regard.
  • 8. Marine Biopolymers and Derivatives Collagen *Collagen in the form of elongated fibrils is mostly found in fibrous tissues such as tendons, ligaments, and the skin. *It is also abundant in corneas, bones, blood vessels, gut, vertebral discs, dentine in teeth, and muscle tissue as a major component of the endomysium. *Collagen constitutes 1 to 2% of muscle tissue and accounts for 6% of the weight of strong, tendinous muscles. *The fibroblast is the most common cell that creates collagen. *The name collagen comes from the Greek word ā€œkollaā€ denoting glue and the suffix ā€œgenā€ meaning producing. *Collagen finds wide application in food, pharmaceutical, cosmetics,leather, and biomedical industries. *One of the most useful biomaterials, mainly due to its biocompatibility, biodegradability, low toxicity, and immunogenicity, compared to other natural polymers
  • 9. Collagen Application ā€¢ Membranes for guided tissue regeneration ā€¢ Cartilage repair, arthritis treatment ā€¢ Hemostats and tissue sealants ā€¢ Corneal treatment ā€¢ mAbs development for osteoarthritis ā€¢ Attachment enhancer of cell culture membrane(mouse neuroblastoma) and diabetic ā€¢ nephropathy indicator ā€¢ Hemostat ā€¢ Treatment of dystrophic epidermolysis bullosa (DEB) ā€¢ Regulator in early stages fibrillogenesis ā€¢ Antiangiogenic and antitumoral properties ā€¢ Contribute to matrix assembly of vascular network during blood vessel formation ā€¢ Involved in inflammation and vasculogenesis, regulate bone mass ā€¢ Teeth formation ā€¢ Drug target and biomarker ā€¢ Retinal structure, closure of ā€¢ neural tube
  • 10. Bioactive Roles of Collagen *Collagen becomes a very useful carrier for the delivery of various kinds of drugs and agents like growth factors. *Collagen is capable of being prepared into cross-linked compacted solids or into latticelike gels. *Resorbable forms of collagen have been used to dress oral wounds, for closure of graft and extraction sites, and to promote healing. *Collagen-based membranes also have been used in periodontal and implant therapy as barriers to prevent epithelial migration and allow cells with regenerative capacity to repopulate the defective area. *Use of collagen scaffolds in bone sialoprotein-mediated bone regeneration
  • 11. Bioactive Roles of Collagen *Medical collagen supplements, which are available as collagen creams, collagen injections, and collagen capsules, replenish the level of collagen in the body and reduce the signs of aging. * The human skin has difficulty in absorbing animal collagen so that collagen treatment had to be supplemented with a hypodermic injection treatment, which typically is expensive and carries the risk of infection. *Animal (terrestrial vertebrates) collagen also has the potential to spread bovine spongiform encephalopathy [BSE] better known as mad cow disease and is another threat to humans. *As a protein extracted from fish, it is mainly used as a surgical suture, as biomimetic scaffold, and as a cosmetic aid to decrease the appearance of wrinkles since collagen makes up to 70% of protein in the skin and helps to keep it elastic.
  • 12.
  • 13.
  • 14. Marine Biopolymers and Derivatives Fish Gelatin *Fish gelatin is a protein product produced by partial hydrolysis of collagen-rich fish skin (or) scale material. *The gelatin molecule is made up of amino acids joined together by amide linkages in a long molecular chain. *Gelatin is a versatile hydro- colloid and is widely applied in food, pharmaceutical, cosmetic, medical, and photographic products. *The most important properties of gelatin are thermoreversible gel formation, texturing, thickening, high water-binding capacity, emulsion formation and stabilization, foam formation, protective colloidal function, and adhesion/ cohesion. *Gelatin is widely used in the food industry such as an ingredient to improve the elasticity, the consistency, and the stability of foods
  • 15. Uses of Gelatin Applications in Food and Confectionery *Gelatin desserts, all types of jellies, are examples of food products that take advantage of the thermoreversible gel formation and the ā€œmelt-in-the-mouthā€ texture of gelatin *The addition of gelatin to dairy products improves the emulsifying capacity as gelatin molecules associate to the surface of the fat droplets and thereby reduce the surface tension towards the aqueous phase. *By adding gelatin to foamed milk-based desserts like yogurt, curds, ice creams, and mousses, gelatin depresses the surface tension of water, enabling formation of foam by mechanical whipping or injection of gas. *The meat processing industry also applies gelatin to their products for several reasons, but the ability to bind water and meat juices and to secure good texture and taste is very important.
  • 16. Uses of Gelatin Applications in Food and Confectionery *Gelatin is also widely used in low-fat (fat replacer), low-carb (binding agent), and low-calorie (fat replacer and binding agent) food products. *The lower melting temperature in gel desserts made from fish gelatins may acceler- ate flavor release *The confectionery industry uses gelatin not only for its thermoreversible gelling properties but also for foam formation and stabilization, binding, emulsification, and controlling sugar crystallization
  • 17. Uses of Gelatin Pharmaceutical Applications *Gelatin is an important and versatile excipient for pharmaceutical and medical applications. *The widespread utilization of gelatin in pharmaceuticals and medical devices is due to several excellent properties. *It is established as a pharmaceutical excipient, tolerated in food (nontoxic, non-allergenic), GRAS status, excellent biocompatibility, high quality (purity), low immunological activity, and controllable physical parameters. *Gelatin is utilized in plasma substitutes used in emergency medicine and surgery; in vitamin coatings, pastilles, and tablets; in the production of globules, paste dressings, and sponges; and in the formulation of new vaccines. *About 90% of all gelatin of pharmaceutical grade is applied in capsule production ā€“ soft and hard gelatin capsules.
  • 18. Uses of Gelatin Nutritional and Health Properties *Gelatin is a high-quality source of protein and free of cholesterol and sugar and contains practically no fat. *Gelatin is easily digested and completely broken down by the human organism. *Gelatin is applied in food products to enrich the protein content and to reduce the amount of carbohydrates, the salt concentration, and the amount of fat in low-fat products and as a carrier for vitamins. *Some international studies suggest that gelatin may have a preventive and regenerative effect on the skeleton and locomotor system ā€“ especially bones, cartilage, tendons, and ligaments. *It is also suggested that gelatin may help fortify hair if taken regularly and strengthen the connective tissue, thus ensuring firm skin, shiny hair, and strong fingernails.
  • 19. Uses of Gelatin Cosmetic Applications *Collagen and gelatin (from bovine, porcine, and fish sources) play important roles in skin and hair products as functional ingredients. * Gelatin hydrolysates are, for example, added to skin creams to improve the water-binding capacity, to reduce transepidermal water loss, and to improve skin feel. *The classical food and cosmetic and pharmaceutical properties of gelatin are based mainly on its gel-forming and viscoelastic properties. * Recently, and especially in the food industry, an increasing number of new applications have been found for gelatin in products such as emulsifiers, foaming agents, colloid stabilizers, fining agents, biodegradable packaging materials, and microencapsulating agents, in line with the growing trend to replace synthetic agents with more natural ones.
  • 20. Uses of Gelatin Gelatin-Based Biomaterial Scaffolds *Antimicrobial fish skin gelatin films are a promising entity in retaining antibacterial activity and inhibiting bacterial contaminants. *Zinc oxide nanoparticles on the antimicrobial activity of films based on tilapia skin and fish protein isolate provide safety and extend the shelf life of packaged foods. *Silver-copper nanoparticles had the same positive effect on the antimicrobial properties of fish skin gelatin films and could improve their mechanical and thermal properties. *Chitosan is another agent that has been added to fish gelatin- based films due to its antimicrobial action against a variety of fungi and Gram-positive and Gram-negative bacteria. *Chitosan-gelatin film could be used as active packaging to preserve fish under refrigerated storage.
  • 21. Chitin and Chitosan * Chitin and chitosan are known natural polysaccharide-based biodegradable polymers, which are extracted particularly from the exoskeletons of marine invertebrates. . * Chitosans are deacetylated forms of chitin, and their polymers differ in their degree of acetylation. Chitin, as well as chitosan, has high molecular weight, and both are viscous and highly hydrophobic and are insoluble in water. * Chitin and chitosan and their derivatives exhibit diverse bioactivities, including ā€¢ antioxidant, ā€¢ antihypertensive, ā€¢ anti-inflammatory, ā€¢ anticoagulant, ā€¢ antitumor ā€¢ anticancer, ā€¢ antimicrobial, ā€¢ hypocholesterolemic, and ā€¢ antidiabetic effects
  • 22.
  • 23.
  • 24. Chitin and Chitosan * Chitin has excellent biocompatibility, nontoxicity, and wound healing properties * Chitin has been widely applied in medical and healthcare fields for applications such as release capsules for drugs, man-made kidney membranes, * chitosan is used as a material for contact and intraocular lenses and found to expedite blood clotting. * chitin compounds are biodegradable makes them particularly appropriate for use in drug delivery systems, as they can act as carriers that release drugs slowly ā€“ a property extremely valuable in cancer chemotherapy. * Chitin has been evidenced as a potent innate immune stimulator of macrophages and other innate immune cells. * Chitin is able to suppress allergen-induced type II allergic responses. * A chitosan compound is also being investigated as an inhibitor of the AIDS virus
  • 25. The bioactive and other roles of chitin and chitosan Chitin/chitosan Applications Beads Use in drug delivery systems Microspheres Enzyme immobilization substrate Nanoparticles As potent gene delivery vehicles Encapsulation of sensitive drugs Coatings Used in surface modification and as textile finishes Fibers Used as medical textiles and surgical sutures Nanofibers Useful for guided bone regeneration Nonwoven bioactive fibers Acts as a scaffold for nerve tissue regeneration and aid in the wound healing processes Films Application in wound care formulations, as dialysis membrane and antitumor agents and Used as a semipermeable film for wound dressing Powder Used as an adsorbent for pharmaceutical and medical devices, surgical glove powder, and enzyme immobilization
  • 26. The bioactive and other roles of chitin and chitosan Shaped objects Employability in orthopedics and manufacture of contact lenses Solutions Used in cosmetics, as bacteriostatic agent, hemostatic agent, anticoagulants, antitumor agent, gene delivery systems, and spermicidal action Gels Used as drug delivery vehicle, as implants, coating, and in tissue Engineering Tablets Acts as a compressed diluent, disintegrating agent, and excipient Capsules Targeted drug delivery vehicle Sponge Mucosal hemostatic dressing, wound dressing, drug delivery, enzyme entrapment, artificial skin
  • 27.
  • 28. Proteoglycans and Glycosaminoglycans Proteoglycans *Proteoglycans (PGs) are a family of complex macromolecules distinguished by the covalent attachment of one or more glycosaminoglycan (GAG) chain(s) (N- and /or O-linked oligosaccharides) with matrix proteins (core proteins). *They are associated with each other and also with other major structural components of the matrix, viz., collagen and elastin, and play important roles in determining the structural organization of the matrix and in fundamental biological processes such as cell growth and development
  • 29. Proteoglycans and Glycosaminoglycans Proteoglycans * Proteoglycans have a number of important biologic roles like anticoagulant activity, anti-atherosclerotic, anti-inflammatory, and also as fat- clearing agent. *Proteoglycans act also as tissue organizers, influence cell growth and the maturation of specialized tissues, *Proteoglycans play a role as biological filters and modulate growth factor activities, regulate collagen fibrillogenesis and skin tensile strength, affect tumor cell growth and invasion, and influence corneal transparency and neurite outgrowth.
  • 30. Proteoglycans and Glycosaminoglycans Glycosaminoglycans *Structurally the simplest and best known of the heteropolysaccharides are the glycosaminoglycans (GAGs). *GAGs such as hyaluronic acid, heparin, and chondroitin sulfate have several applications in the medical, veterinary, pharmaceutical, and cosmetic field. *The use of powdered shark cartilage for wound healing and as antiangiogenic, anti-arthritic, and antitumor agent from ancient times has been attributed to the presence of glycosaminoglycans. *Proteoglycans play a role as biological filters and modulate growth factor activities, regulate collagen fibrillogenesis and skin tensile strength, affect tumor cell growth and invasion, and influence corneal transparency and neurite outgrowth.
  • 31. Antioxidant Pigments and Polyphenols Antioxidant Pigments *Marine natural pigments have considerable medicinal potential and promising applications in human health. *The major categories of pigments by chemical structure occur either as tetrapyrolles (chlorophyll and heme pigments), carotenoids, indole derivatives (quinones and violacein), alkaloids (prodiginines and tamb- jamines), polyenes, macrolides, peptides, or terpenoids. *Many of these pigments have a variety of biological activities, including antitumor, antibacterial, antioxidant, and anti-inflammatory activity
  • 32. Antioxidant Pigments and Polyphenols Carotenoids *Carotenoids are widely present in marine environments and responsible for the color of many important marine species of fish, shellfish, and seaweeds. *These yellow-to-orange-red pigments, called carotenoids, of which there are over 700 different chemical formulations, are typically divided into two subgroups, *the carotenes (hydrocarbon carotenoids) and *the xanthophylls (oxygenated carotenoids).
  • 33. Antioxidant Pigments and Polyphenols Carotenoids *Commonly found carotenoids from aquatic animals are astaxanthin, zeaxanthin, tunaxanthin, lutein, etc. *Marine red and brown algae pro- duce Ī²-carotene, zeaxanthin, fucoxanthin, and fucoxanthinol. *Astaxanthin is the main carotenoid pigment found in aquatic animals, while fucoxanthin is abundant in aquatic plants. *These abundant representative marine carotenoids astaxanthin and fucoxanthin have been reported to be effective antioxidants and have higher biological activity than those of terrestrial origin
  • 34. Pigment Bacterial source Bioactivity Color Astaxanthin Agrobacterium aurantiacum Antioxidation Red Cycloprodigiosin Pseudoalteromonas denitrificans Anticancer; immunosuppressa nt; antimalarial Red Heptyl prodigiosin Ī±-Proteobacteria Antiplasmodial Red Indigoidine Streptomyces chromofuscus ATCC 49982 Dye-industrial applications Blue Melanins Vibrio cholerae, Shewanella colwelliana, Cellulophaga tyrosinoxydans Protection from UV irradiation Black Phenazine derivatives Bacillus sp. Cytotoxic Brownish yellow Pyocyanin and pyorubrin (Phenazine derivatives) Pseudomonas aeruginosa Antibacterial Blue- green Scytonemin Cyanobacteria Protection from UV irradiation Yellow- green Anti-inflammatory, antiproliferative Tambjamines Pseudoalteromonas tunicata Antibiotic, anticancer Yellow Tryptanthrin Cytophaga Antibiotic Deep yellow Violacein Pseudoalteromonas tunicate Antibiotic; antiprotozoan; anticancer Violet Natural pigments isolated from marine bacteria
  • 35. Antioxidant Pigments and Polyphenols Carotenoids - Astaxanthin *Astaxanthin is the ā€œKing of Carotenoids.ā€ It is the red pigment that gives salmon, shrimp, and flamingos their pink-red color. *Astaxanthin is a red pigment from the xanthophyll oxygen- carrying group of carotenoids. *Many aquatic species including crustaceans utilize these algae and plankton as food and store the pigment in their shell, resulting in their pink-red exterior.
  • 36. Antioxidant Pigments and Polyphenols Carotenoids - Astaxanthin *Astaxanthin functions as an intracellular oxygen reserve and fishes and invertebrates fed on a diet containing optimal levels of astaxanthin that show greater survivability rates when subjected to poor oxygen environments as it is a potent antioxidant, comparable to vitamin E. *It may also offer protection against UV light. *Antioxidant activity of astaxanthin has been reported to be several times higher than that of other carotenoids and tocopherols
  • 37. Antioxidant Pigments and Polyphenols Carotenoids - Fucoxanthin *Fucoxanthin is an important pigment found in aquatic plants. *Fucoxanthins possess strong DPPH (2, 2-diphenyl-1- picrylhydrazyl) radical scavenging activity. *In addition to antioxidant activity, fucoxanthin from edible sea- weeds exhibited anti-obesity effect and antidiabetic effect, complemented by DHA synthesis in mouse liver.
  • 38. Antioxidant Pigments and Polyphenols Antioxidant Polyphenols *A series of polyphenols including catechins (e.g., gallocatechins, epicatechins, and catechin gallate), flavonols, and flavonoid glycosides have also been identified in several red and brown algae. *Algal polyphenols exhibit their bioactive potential as potent free radical scavengers and primary chain-breaking antioxidants. *Phlorotannins are a group of polyphloroglucinol phenolics and are mainly stored within cell organelles called physodes. *Antidiabetic and antioxidant effects of methanol extract from the brown algae, Ecklonia stolonifera, were reported
  • 39. Seaweed Polysaccharides *Abundant and renewable marine biomass, seaweeds are a part of the human diet in many Asian countries and also traditionally been used as medicines since ancient times. * The earliest records of herbal medical seaweeds appeared in Chinese literature about 2000 years ago. *Several species of seaweed have the capacity to produce a diverse array of secondary metabolites, which exhibit important and vital ecological roles as defense. *Seaweeds are also a rich source of bioactive polysaccharides. The remarkable marine polysaccharides found in red and brown algae, viz., alginate, agar, and carrageenan, *Provide numerous ingredients to the food, pharmaceutical, cosmetic, textiles, paper, and * Biotechnology industries as stabilizers, thickeners, emulsifier, and fillers *Other seaweed hydrocolloids, besides those common seaweed hydrocolloids (alginate, agar, and carrageenan), are fucoidan, laminarin, mannitol, funoran, ulvan, etc
  • 40. Seaweed Polysaccharides *There are numerous commercial applications of marine polysaccharides as food, beverages, and supplements. * In addition, these molecules have many biological functions including antimicrobial, anticoagulant, antiproliferative, antithrombotic, and anti- inflammatory activity. *These marine-derived secondary metabolites also have many human health benefits which enable them to be applied as nutraceuticals. *In the biomedical field, the polysaccharides from algae can be used in controlled drug delivery, wound management, and regenerative medicine *Seaweeds are classified into four principal group based on their pigments, namely, red, brown, blue, and blue-green. Only the red (Rhodophyceae) and brown (Phaeophyceae) seaweeds are important sources of hydrocolloids
  • 41. Seaweed Polysaccharides Agar *Agar - extracted from red seaweed (Rhodophyceae), specifically Gracilaria sp., Gelidium sp., and Pterocladia/Gelidiella sp *Agar consists of a mixture of two polysaccharides, namely, agarose and agaropectin, with agarose making up about 70% of the mixture. *Agarose is responsible for gelling, while agaropectin is responsible for thickening properties. *About 80% of agar produced globally is used for food applications, while remaining 10ā€“20% is used in pharmaceutical and biotechnology industries. *Low-quality agar is used basically in food stuff (frozen foods, bakery icings, meringues, dessert gels, candies, etc.), while some may extend to industry applications for paper sizing, coating, adhesives, textile printing/dyeing, casting, and impression.
  • 42. Seaweed Polysaccharides Agar *Agar - extracted from red seaweed (Rhodophyceae), specifically Gracilaria sp., Gelidium sp., and Pterocladia/Gelidiella sp *Agar consists of a mixture of two polysaccharides, namely, agarose and agaropectin, with agarose making up about 70% of the mixture. *Agarose is responsible for gelling, while agaropectin is responsible for thickening properties. *About 80% of agar produced globally is used for food applications, while remaining 10ā€“20% is used in pharmaceutical and biotechnology industries. *Low-quality agar is used basically in food stuff (frozen foods, bakery icings, meringues, dessert gels, candies, etc.), while some may extend to industry applications for paper sizing, coating, adhesives, textile printing/dyeing, casting, and impression.
  • 43. Seaweed Polysaccharides Carrageenan *Carrageenans are a class of sulfated galactans extracted from different species of red seaweed (Rhodophyta). The main seaweed species used in industrial scale for carrageenan production are Kappaphycus alvarezii, Eucheuma denticulatum, Chondrus crispus, and Gigartina sp. *Carrageenans are hydrophilic linear hydrocolloids, consisting mainly of potassium, sodium, magnesium, and calcium salts of sulfated esters of D-galactose nd 3,6-anhydro-D-galactose *Carrageenan has been widely used for drug delivery applications in different isoforms including nanoparticles, micro stabilizers, gelling agent, beads, micro- spheres, and microcapsules. *Carrageenan-based hydrogels and carrageenan- graphene oxide composites are widely employed for bone tissue engineering
  • 44. Seaweed Polysaccharides Alginate *Alginate is distinguished from other hydrocolloids (agar and carrageenan) because it is isolated from brown seaweed (Phaeophyceae) specifically from outer layer of brown algae cell wall, as inner layer makes up mostly of *Alginate is widely used in industry because of its ability to retain water and its gelling, viscosifying, and stabilizing properties. *Alginate is an excellent stabilizing and thickening agent in food such as jelly, ice cream, desserts, etc. due to its properties to chelate metal ions to form highly *Alginate oligosaccharides, low molecular polymer fragments obtained by enzymatic depolymerization, and acid hydrolysis - unique pharmaceutical properties - antioxidant, antifungal, anti-inflammatory, and antibacterial activities viscous solutions cellulose.
  • 45. Seaweed Other Polysaccharide Compound Activity U. pinnatifida, A. platensis, Porphyridium sp. Fucoidans from microalgae Anticancer activity Nanofiber production BioGlue for soft tissue closure after surgery, lubricants for bone joints A. nodosum, E. bicyclis, Fucus sp., Laminaria sp., U. pinnatifida, C. vulgaris Laminarin (Ī²-glucans) Tissue regeneration Burn wound dressings Wound healing Ulva rigida, Ulva spp. Ulvans Nano fibers Tissue engineering Wound dressings
  • 46. Bioactive Metabolites of Marine Algae, Fungi and Bacteria *Chemically the bioactive metabolites of marine flora include ļ±brominated phenols, ļ±oxygen heterocyclics, ļ±nitrogen heterocyclics, ļ±sulphur nitrogen heterocyclics, sterols, ļ±terpenoids, ļ± polysaccharides, ļ±peptides and ļ±proteins.
  • 47. Bioactive Metabolites of Marine Algae, metabolites Source use Brominated Phenols The green, brown and red algae Symphyocladia gracilis, Rhodomela larix and Polysiphonia lanosa Antibacterial and antifungal activities Brominated Oxygen Heterocyclics (laurencin and laureatin) The red algae Laurencia sp Larvicidal activities Nitrogen Heterocyclics (Domoic acid and the kainic acid) Marine algae Chondria armata Red alga Digenea simplex Anthelmintic agent Guanidine Derivatives saxitoxin Gonyaulax catenella - red tide Neurotropic effects Phenazine Derivatives caulerpicine, caulerpin The marine alga Caulerpa sp Mild anesthetic action when placed in the mouth
  • 48. Bioactive Metabolites of Marine Algae, Metabolites Source use Amino Acids and Amines Laminine (L-lysine, L-arginine, ethanolamine and choline) Volatile amines, such as methylamine, dimethylamine, trimethylamine, ethylamine, propylamine, isobutylamine, isoamylamine, 2- phenylethylamine and 2- methylmercapto propylamine Marine algae Laminaria angustata and Chondria amata Red, green and brown algae Transitory hypotensive effect Sterols Cholesterol, 22- dehydrocholesterol and demosterol Red Algae Rhodymenia palmata, Porphyra purpurea, P. umbilicalis and Halosaccion ramentaceum Hypnea musciformis Hypnea japonica Reduce blood cholesterol level To reduce the tendency to form a fatty liver and excessive fat deposition in the heart
  • 49. Bioactive Metabolites of Marine Algae, metabolites Source use Sterols Fucosterol Brown Algae Reduce blood cholesterol level To reduce the tendency to form a fatty liver and excessive fat deposition in the heart chondrillasterol, poriferasterol, 28-isofucosterol, ergosterol and cholesterol Green algae Sulfated Polysaccharides the rhodophyceae (red algae), the phaeophyceae (brown algae), the cyanophyceae (blue-green algae) and the chlorophyceae (green algae) Carrageenan Species of Chondrus, Eucheuma, Gigartina and Iridea Antiviral, to stimulate the growth of connective tissues, anticoagulant and antithrombic agent
  • 50. Bioactive Metabolites of Marine Algae, metabolites Source use Alginic acid Brown algae species of Fucus, Laminaria and Macrocystis sodium alginate from giant brown seaweed (Macrocystis pyrifera), horsetail kelp (Laminaria digitata) and sugar kelp (Laminaria saccharina) 1. used mainly in the manufacture of ice cream where it serves as a stabilising colloid. It is also used in cosmetics and pharmaceuticals. 2. useful adjuvent in immunisation against two strains of influenza virus. 3. Sodium alginate is also found effective in diminishing hyper calciuria in urolithiasis, and found useful in the treatment of esophagitis 4. The most significant property of sodium alginate is the ability to remove strontium 85 and strontium 87 from the body without seriously affecting the availability of Ca, Na or K in the body. 5. This selective action of sodium alginate is of great potential to remove Sr-90 contamination due to fall out from atomic explosions. Calcium alginate is reputed to be a hemostatic agent which stimulates the clotting of blood in situ which is subsequently absorbed in the tissue
  • 51. Bioactive Metabolites of Marine Algae, metabolites Source use Sulfated Polysaccharides Laminarin Laminaria cloustoni Anticoagulant properties, also reported to have antilipidemic activity like that of heparin Agar and Agarose Red algae are the source of agar and agarose The genera Gelidium, Gracilaria, Acanthopeltis and Pterocladia of the Rhodophyceae are the main producers No direct medicinal use, their use in biomedical research
  • 52. Bioactive Metabolites of Marine Bacteria and Fungi, *Bacteria and fungi are prime producers of the antagonistic substances in terrestrial environment. *Antibiotic, antiviral, antifungal, and antiyeast activities of these organisms had been reported. *Besides, a few growth stimulant properties which may be useful in studies on wound healing, carcinogenic properties, and in the study of cancers are reported *many bacteria showing antimicrobial activity, a variant of the ichthyotoxic Pseudomonas piscicida exhibited marked antagonism to various micro-organisms *A red coloured bacterium found to excrete vitamin B and antibacterial substances into the sea water.
  • 53. Bioactive Metabolites of Marine Bacteria and Fungi, *The bacteria and fungi from sea are also reported to produce substances which affect ā€¢ central nervous system (CNS), ā€¢ respiratory system (RS), ā€¢ neuromuscular system (NMS), ā€¢ autonomic nervous system (ANS), ā€¢ cardiovascular system (CVS) and ā€¢ gastrointestinal system (GI).77 *Some of the substances are known to produce local effects such as pain, necrosis, edema, parasthesias, pruritis etc
  • 54. Bioactive Metabolites of Marine Bacteria and Fungi, metabolites Source use Cephalosporins Penicillinase sensitive antibiotic substance named antibiotic N Cephalosporium acremonium Active against Gram- positive bacteria Active against a number of penicillin resistant Staphylococcus Bromo pyrrole antibiotic Pseudomonas bromoutilis Activity against many Gram-positive bacteria Pyrrolnitrin , a chloropyrrole Pseudomonas pyrrocinia This compound was marketed in Japan under the name PYRO- ACE - dermatophytic fungal infections. Red coloured antibiotic named prodigiosin Serratia marcescens Antibiotic and antifungal activities use as a therapeutic agent
  • 55. Bioactive Metabolites of Marine Bacteria and Fungi, metabolites Source use Aplysiatoxins and oscillatoxins isolated from blue-green algae Schizothrix calcicola and Oscillatoria nigroviridis Antileukaemic activity but their high toxicity precludes their medicinal use Cytotoxic and fungicidal nucleosides Anatoxin-a Anabaena flosaquae Most potent nicotinic receptor agonist. Treating disorders associated with defects in cholinergic regions of the central nervous system Ichthyotoxin Several species of green- algae of the genus Halimeda Exhibits diverse biological activities, Inhibits the growth of marine bacteria and fungi, cell division of fertilized sea-urchin eggs and the motility of sea-urchin sperms at 1 Āµg/mL
  • 56. Bioactive Metabolites of Marine Bacteria and Fungi, Metabolites Source use Avrainvilleol Green algae, Avrainvillea longicaulis Exhibits high order of antifeedant activity in reef fish and also inhibits the growth of microorganisms. Diterpenoids The genera Halimeda, Penicillus and Udotea Exhibit cytotoxic and antimicrobial activities Prenylated aromatics, unsaturated C11 hydrocarbons Dictyopteris plagiogramma and D. australis Sex attractants Brominated acetylenic compounds Laurentia nipponica Active against mosquito larvae Trihydroxy benzyl methyl ethers Grateloupia filicina Antibacterial activity against Bacillus subtilis
  • 57. Bioactive Metabolites of Micro Algae *Micro algae represent a subset of single cell microorganisms. *Generally grow autotropically using CO2 as the sole carbon source and light as energy. *These algae are ubiquitous in nature. *Aquatic micro algae have been isolated in areas ranging from hot springs to glacial ice flows. *There are over 50,000 different species of micro algae of which only a few have been characterised. *Micro algae represent a major untapped resource of genetic potential for valuable bioactive agents and biochemicals *Proteinaceous. *Rich in reserves of oils containing various amounts of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). Considered to be responsible to reduce incidence of coronary heart disease *used for the production of labelled biochemicals. *Phycobiliproteins can be commercially produced from Spirulina and the red microalgae Porphyridium and Rhodella. *Phycobiliproteins are widely used in clinical or research immunology because they are very powerful and highly sensitive fluorescent properties
  • 58. Bioactive Metabolites of Micro Algae Metabolites Source use Phycocyanin Cyanobateria (Spirulina), Blue green Algae Potential effect to treat effectively type-2 diabetes mellitus by inhibiting Ī±-amylase and Ī±- glucosidase. Phycoerythrin Porphyridium cruentum Red algae Immunomodulating activity Anticancer activity Development of phycofluor probes for immunodiagnostics. ā€¢ Phycobiliproteins are used as colorants in food. ā€¢ cosmetics such as lipstick and eyeliners in Japan, Thailand and China ā€¢ Dainippon Ink and Chemicals produces a blue food colourant from Spirulina, called Lina blue, that is used in chewing gum, ice slush, sweets, soft drinks, dairy products and wasabi. ā€¢ Heavy isotope labeled metabolites and Phycoerythrin (from Red algae and cyanobacteria) used as fluorescent labels could have values far exceeding $10,000 per kg. ā€¢ Micro algae are also expected to furnish potent antiviral, antiAIDS, antibiotic and other bioactive agents
  • 59.
  • 60. Bioactive Metabolites of Marine Invertebrates Metabolites Source use Avrainvilleol Green algae, Avrainvillea longicaulis Exhibits high order of antifeedant activity in reef fish and also inhibits the growth of microorganisms. Diterpenoids The genera Halimeda, Penicillus and Udotea Exhibit cytotoxic and antimicrobial activities Prenylated aromatics, unsaturated C11 hydrocarbons Dictyopteris plagiogramma and D. australis Sex attractants Brominated acetylenic compounds Laurentia nipponica Active against mosquito larvae Trihydroxy benzyl methyl ethers Grateloupia filicina Antibacterial activity against Bacillus subtilis
  • 61. ļƒ˜Hemolymph is the main source of AMPs in marine invertebrates, even though other tissues may also contain these peptides. AMPs Source Activity Penaeidins Penaeus vannamei Microbicidal properties Defensins, myticins, and mytilins Marine Mollusks Mytilus galloprovincialis and Mytilus edulis Innate immune mechanisms Scylla serrata antimicrobial protein S. serrata Antimicrobial action against various Gram-positive and Gram-negative bacteria Phoriospongin A and B Australian marine sponges (Phoriospongia sp. and Callyspongia bilamellata) Nematocide Blood-depressing substance I (BDS-I) Sea anemone Antibacterial and neurotoxic (sodium channel blocker) Aurelin Jelly fish (Aurelia aurita) Antimicrobial Centrocins, strongylocins Green sea urchin (Strongylocentrotus droebachiensis) Antimicrobial
  • 62. *Marine peptides are important bioactive natural products that are present in many marine species. *These marine peptides have high potential nutraceutical and medicinal values because of their broad spectra of bioactivities. *The role of marine peptides as antimicrobial peptides (AMPs) possessing antibacterial, antiviral, antifungal, and antiprotozoal functions. *Peptides containing histidine, tryptophan, and tyrosine possessed antioxidative activity. *The amino acids proline, alanine, and leucine contribute to radical scavenging activity when located in the C-terminal in an aminaocid sequence. *Antioxidant peptide derived from different marine animals exhibits varying potencies to free radical scavenging and various antioxidant mechanisms.
  • 63. *More than 100 species of marine fish are traditionally used in medicines to treat tumors. *The antitumor/cytotoxic marine peptides can be classified into four types: ā€¢ (i) linear depsipeptides (e.g., dolastatin 10); ā€¢ (ii) cyclic depsipeptides (e.g., kaha- lalide F); ā€¢ (iii) linear peptides (e.g., pardaxin); and ā€¢ (iv) marine protein hydrolysates *The digested hydrolysates of peptides from tuna dark mus- cle exhibited antiproliferative activity on human breast cancer cell line MCF-7. *Peptide hydrolysates from oyster extract expressed in vivo antitumor activity in BALB/c mice. * Tunicate extract and squid gelatin hydrolysates also demonstrated in vitro cytotoxic effect on several human cancer cell lines.
  • 64. *Antihypertensive peptides or angiotensin-I converting enzyme (ACE) inhibitory peptides have been isolated from fish protein hydrolysates. *Angiotensin-I converting enzyme (ACE) is a dipeptidyl carboxypeptidase (EC. 3.4.15.1) important for the regulation of blood pressure and normal heart function *ACE-inhibiting peptides have been isolated from fish protein hydroly- sate such as Alaska pollock skin hydrolysate, Sardinella aurita, yellowfin sole, salmon muscle, sea bream scales, and tuna frame proteins as well as squid and cuttlefish hydrolysates.
  • 65. *The cardiovascular protective peptides include bioactive peptides which exhibit activities important to cardiovascular health, including effects on blood pressure, oxidative stress coagulation, atherosclerosis, and lipid metabolism. *The anticoagulant peptide binds to coagulation factors in the blood clotting intrinsic pathway and inhibits their molecular interaction. *The anti- atherosclerotic peptides showed their cardiovascular protection effect by suppressing the inflammatory responses in histamine-stimulated endothelial cells that may be related to early atherosclerosis. *Fish protein lowers serum cholesterol level by retarding absorption and promoting excretion of cholesterol and bile acid attributed to lowered micellar solubility of cholesterol and enhanced bile acid-binding capacity
  • 66. Neuropeptides *Neuropeptides derived from marine species have potential as natural and safe alternative to opioid drugs for anxiety and stress management. *Opioid- like peptides exhibit a positive effect on motivation, emotion, behavior, stress, appetite, and pain management by interacting with specific opioid receptors in the nervous, endocrine, immune, and digestive systems. *The gonadotropin-releasing hormone, which increases the secretion of pituitary gonadotropin *Neuroprotective Peptides Marine proteins and peptides suppress the development of neurodegenerative diseases like Parkinsonā€™s disease, Alzheimerā€™s disease, and multiple sclerosis.
  • 67. *Neuroprotective Peptides *Neuroprotective Peptides Marine proteins and peptides suppress the development of neurodegenerative diseases like Parkinsonā€™s disease, Alzheimerā€™s disease, and multiple sclerosis. *Their neuroprotective action is brought about by the direct inter- action of absorbed protein and peptide with a variety of cellular and molecular tar- gets with enzyme/ion channels. *The neuroprotective peptide (HTP-1) Gly-Thr-Glu-Asp-Glu-Leu- Asp-Lys from the seahorse Hippocampus trimaculatus exerted a protective action on PC12 cells and prevented them from the deleterious action of Ī² amyloid plaques (amyloid Ī²42), which is associated with the pathogenesis of Alzheimerā€™s disease.
  • 68. *Analgesic Peptides Conopeptides from marine snail venoms have attracted much interest in drug design for chronic neuropathic pain. *Appetite-Suppressing Peptides Low-molecular-weight peptides from fish and shrimp head protein hydrolysates have been found to be effective for stimulating cholecystokinin release in STC-1 cells by regulation of cholecystokinin release. *Marine peptides may be employed as anorexigenic agents and may interact with appetite-suppressing gut hormones including cholecystokinin and glucagon-like peptide 1 to produce anti-obesity effects. *The neuroprotective peptide (HTP-1) Gly-Thr-Glu-Asp-Glu-Leu-Asp- Lys from the seahorse Hippocampus trimaculatus exerted a protective action on PC12 cells and prevented them from the deleterious action of Ī² amyloid plaques (amyloid Ī²42), which is associated with the pathogenesis of Alzheimerā€™s disease.
  • 69. *Food Preservation According to Gomez-Guillen et al. (2011), Antimicrobial peptides can also be used in natural biopreservation to control spoilage and foodborne pathogens. *The peptide CgPep33 from Pacific oysters is used to inhibit the activity against gray mold disease in strawberries. * CgPep33 can therefore be used as a substitute for fungicide to control postharvest diseases and to extend the shelf life of fruits and vegetables *Protein hydrolysates also function as cryoprotectants, reduce lipid oxidation, enhance water retention, and suppress dehydration-induced denaturation of myofibrils in foods
  • 70. * POTENTIAL USE OF MARINE DERIVED COMPOUNDS IN COSMETICS *Oceans are home to a wide range of microbial biodiversity, including many organisms with high potential of producing bioactive compounds, such as thraustochytrids *Some compounds within marine organisms are already widely used within the cosmetic industry, as *they provide a renewable source for compounds used in bulk, such as agar and carrageenan, used in cosmetics to increase the viscosity of formulations. Smaller marine molecules are also used for: ļƒ˜Promoting skin hydration ļƒ˜Improving acne ļƒ˜UV protection ļƒ˜Reduce wrinkles
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