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Marine drugs

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The drugs which are obtained from marine organisms are know as marine drugs. these marine drugs are used since ancient times. chines and japanes are very famous to use these resources. And interstingly,innumarable products derived from the marine organisms in several 'crude forms' have been widely used across the globe by the traditional practitioners for thousands of years.

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Marine drugs

  1. 1. MARINE DRUGS K.Sudheer Kumar, Assistant professor. Dept.of pharmacognosy Chilkur Balaji college of Pharmacy Hyderabad. E-mail:sudheer.y2k8@gmail.com 1 K.Sudheer Kumar, Assistant professor. Dept.of pharmacognosy Chilkur Balaji college of Pharmacy Hyderabad. E-mail:sudheer.y2k8@gmail.com
  2. 2. INTRODUCTION The drugs which are obtained from marine organisms are know as marine drugs. these marine drugs are used since ancient times. chines and japanes are very famous to use these resources. And interstingly,innumarable products derived from the marine organisms in several 'crude forms' have been widely used across the globe by the traditional practitioners for thousands of years. Many of the species contain toxic compound the marine environment is a rich source of both biological and chemical diversity. This diversity has been the source of unique chemical compound the marine with the potential. Industrial development,has,pharmacetuicals,cosmetics,nutrtitional supplements molecular properties, fine chemical and chemicals. Marine toxins were reported to possess an extremely high potency with regard to their pharmacological actions, and, therefore, sometimes collectively referred to as' toxins‘ The drugs which are obtained from marine organisms are know as marine drugs. these marine drugs are used since ancient times. chines and japanes are very famous to use these resources. And interstingly,innumarable products derived from the marine organisms in several 'crude forms' have been widely used across the globe by the traditional practitioners for thousands of years. Many of the species contain toxic compound the marine environment is a rich source of both biological and chemical diversity. This diversity has been the source of unique chemical compound the marine with the potential. Industrial development,has,pharmacetuicals,cosmetics,nutrtitional supplements molecular properties, fine chemical and chemicals. Marine toxins were reported to possess an extremely high potency with regard to their pharmacological actions, and, therefore, sometimes collectively referred to as' toxins‘
  3. 3. MARINE NATURAL PRODUCTS • Many natural products from these organisms act as chemical weapons and are highly potent inhibitors of physiological processes. • Several show pharmacological activities and are effective against cancer, AIDS, arthritis • Variety of molecules show unique structural features and exhibit various types of biological activities • Marine drugs are highly potent bioactive molecules  In recent years a significant number of novel metabolites with potent pharmacological properties have been discovered from the marine organism although there are only a few marine drive from marine natural products are now in the clinical pipeline with more clinical development. MARINE NATURAL PRODUCTS • Many natural products from these organisms act as chemical weapons and are highly potent inhibitors of physiological processes. • Several show pharmacological activities and are effective against cancer, AIDS, arthritis • Variety of molecules show unique structural features and exhibit various types of biological activities • Marine drugs are highly potent bioactive molecules  In recent years a significant number of novel metabolites with potent pharmacological properties have been discovered from the marine organism although there are only a few marine drive from marine natural products are now in the clinical pipeline with more clinical development.
  4. 4. CLASSIFICATION OF DRUG MOLECULES OF MARINE ORGANISMS The enormous quantum of newer and potent drug molecule derived from the wide spectrum of marine organism across the world may be judiciously and logically classified based on their specific pharmacologic actions as stated below (A) Anti-neoplastic Agents (B) Cardiovascular active drugs (C) Marine toxins (D) Anti-biotic substances (E) Anti-inflammatory and antispasmodic agents (F) Miscellaneous pharmacologically active substance The enormous quantum of newer and potent drug molecule derived from the wide spectrum of marine organism across the world may be judiciously and logically classified based on their specific pharmacologic actions as stated below (A) Anti-neoplastic Agents (B) Cardiovascular active drugs (C) Marine toxins (D) Anti-biotic substances (E) Anti-inflammatory and antispasmodic agents (F) Miscellaneous pharmacologically active substance
  5. 5. (A) ANTI-NEOPLASTIC AGENTS The two prominent US-based research institute , namely :US NATIONAL CANCER INSTITUTE(NCI) and US NATIONAL SEA GRANT OFFICE (NSGO) have discovered thousands of pure and semi- pure compounds derived from the marine origin that distinctly exhibited anti-neoplastic activity in a good number of cell line ; beside, in vivo actions against both malignant tumors and leukemia's in various animal models. in the present context certain duly characterized drug molecules displaying know and potent activities. Crassin acetate: It is the member of cembronoids which are cyclic diterpenes. Biological source : It is obtained from the CARIBBEAN GORGONIAN pseudoplexaura porosa. (A) ANTI-NEOPLASTIC AGENTS The two prominent US-based research institute , namely :US NATIONAL CANCER INSTITUTE(NCI) and US NATIONAL SEA GRANT OFFICE (NSGO) have discovered thousands of pure and semi- pure compounds derived from the marine origin that distinctly exhibited anti-neoplastic activity in a good number of cell line ; beside, in vivo actions against both malignant tumors and leukemia's in various animal models. in the present context certain duly characterized drug molecules displaying know and potent activities. Crassin acetate: It is the member of cembronoids which are cyclic diterpenes. Biological source : It is obtained from the CARIBBEAN GORGONIAN pseudoplexaura porosa. USES : crassin acetate was observed to be comparatively inert to the mammalian system but on the contrary found to be extremely cytotoxic to human leukemic cells in vitro and also to the mouse fibroblasts. CHEMICAL STRUCTURE
  6. 6. SINULARIN Biological source: sinularin and its dihydro congener are obtained from sinularia flexibilis. Uses: It posses anticancer activities SINULARIN FLUDARABINE SYNONYM: 2-fluorovidarabine ,2F-AraA. CHARACTERISTIC FEATURES: 1. It is obtained as crystals from ethanol and water having mp 260 c 2. It shows specific optical rotation 3.It is sparingly soluble in water and organic solvents uses: it is used as a antineoplastic agent.
  7. 7. (B) CARDIOVASCULAR ACTIVE AGENTS During the past three decades a huge number of extracts, fraction and pure isolates from thousands of marine organism were subjected to thorough cardiovascular screening in various research laboratories around the world. Interestingly, most of these compounds did exhibit cardiovascular activities perhaps as frequently as observed antibiotic and antineoplastic activities. Unfortunately, as on date hardly any compound could surface out and obtain the FDA approval as a potential drugs. The cardiovascular active drugs may be broadly classified under the following two categories, namely: (a) cardiotonics (b) hypotensive compounds LAMININ :LAMININ : Biological source : Laminin is obtained from a marine algae laminaria angustata CHEMICAL STRUCTURE CHARACTERISTIC FEATURES : •It is the abundant structural component of the basal lamina •It is critical to the stability of the extracellular matrix and to the adhesion of cells to the basement membrane •It belongs to the family of HETEROTRIMERIC GLYCOPROTEINS composed of a heavy chain, which are linked by disulphide bonds to form an asymetrical cross- shaped structure. USES: •It shows hypotensive effect. •It also exhibits diverse biological activities.
  8. 8. ELDOISIN : It is a powerful hypotensive compound. it also shows strong vasodilator effects Biological source: Eldoisin is obtained from the posterior salivary glands of eledone spp.[small octopus ] eledone moschata chemical structure of eldoisinchemical structure of eldoisin CHARACTERISTIC FEATURES : •Eldoisin is obtained as a sesquihydrate powder that gets decomposed at 230 c •It has specific optical rotation •It is found to lose its activity gradually when incubated in blood. USES : 1. It is found to stimulate extra vascular smooth muscle. 2. Eldoisin acts as a potent vasodilator and hypotensive agent. 3. It also stimulate lacrimal secretion. 5. It causes salivation, and enhances capillary permeability in certain specific species.
  9. 9. SEPONGOSIN: It is chemically nucleoside (methoxy derivative of adenosine)derivative it reduces both the rate and the force of concentration of heart. Biological source: It is obtained from the caribbean sponge cryptotethia crypta and with a minor structural modification of the parent isolated nucleoside known as arabinosylnucleoside. USES: 1.It exhibited various coronary effects resembling to those of adenosine, for instance coronary vasodilation and negative inotropy. 2. It is found to exert more marked and pronounced long- acting effects. 3. It acts as a hypotensive at such as dose level at which adenosine is observed to be absolutely in active. 4. It reduces the rate as well as the force of concentration of heart.
  10. 10. C . MARINE TOXINS A host of marine toxins have been obtained from a wide variety of marine organisms in their crude, semi-pure and other forms between 1960-1970. However, during the eighties a good number of them possessing venomous and toxic properties and having most complex chemical structure have been isolated, characterized with the advent of rather exceedingly sophisticated analytical instruments and a concerted effort of dedicated marine chemists and pharmacologists across the globe. TETRODOTOXIN: It is frequently abbreviated as TTX, it is a potent neurotoxin Biological source: Tetrodotoxin is obtained from the ovaries and liver of a large number of tetraodontidae ; especially the spheroids rubripes (globe fish) it is also obtained from the puffer fish (tetradou species) which begin a top most delicacy in japanese cuisine. Biological source: Tetrodotoxin is obtained from the ovaries and liver of a large number of tetraodontidae ; especially the spheroids rubripes (globe fish) it is also obtained from the puffer fish (tetradou species) which begin a top most delicacy in japanese cuisine. SPHEROIDES RUBRIPES(GLOBE FISH) USES: Tetrodotoxin gets bound particularly to the Na+ channels on the outside of excitable membrane, thereby inducing Na+ influx in K+ influx within a few milliseconds of the accompanying membrane depolarization.
  11. 11. BREVETOXIN : Biological source : a plethora of polycyclic polyether metabolites have been obtained from the Dinoflagellate ptychodiscus brevis; and now the Brevetoxins are commonly known as from the generic nomenclature that is p.brevis toxins. chemical structure USES : •It exerts an excitatory effect on the isolated neuromuscular and other cells . •It cause both neurological and gastrointestinal disorder .
  12. 12. CIGUATERA TOXINS :The terminology “ciguatoxin” was first and fore most employed to enumerate a disease primarily caused due to the ingestion of marine snails . ciguatera poisoning was thought to be the ingestion of blue green algae. Biological source: Ciguatoxin (CTX) is found in Gymnothorax javanicus (Moray Eel) , besides in a variety of coral reef fish, for instances : Lutjanus bohar (Red snapper). USES: •It cause neurological problems •It cause cardiovascular and gastrointestinal problems. •CTX- is found to exert its actions at the ends specifically . •interestingly CTX acts as a cardiotonic at the nerve ends specifically. •where as at higher dose levels there is an apparent depression in both heart rate and in respiration. CHEMICAL STRUCTURE
  13. 13. ANTIMICROBIAL DRUGS Antimicrobial drugs substances have been isolated, characterized and studied extensively over the past three decades particularly from the vast domain of marine organism .A few examples are, brown and red algae. Antimicrobial drugs substances have been isolated, characterized and studied extensively over the past three decades particularly from the vast domain of marine organism .A few examples are, brown and red algae. ZONAROL Biological source : zonarol and iso- zonarol are both obtained from dictyopteris zonaroides (brown algae) . USES: Zonarol is used as anti inflammatory. CHEMICAL STRUCTURE
  14. 14. PREPACIFENOL Biological source: it is obtained from laurenica filformis, the two different species of algae. EUNICIN Biological source: Eunicin is obtained from Eunicia mammosa the Gorgonian corals. CHEMICAL STRUCTURE USES Anti microbial agent Biological source: Eunicin is obtained from Eunicia mammosa the Gorgonian corals. CHEMICAL STRUCTURE USES Anti microbial agent Anti biotic
  15. 15. D . ANTIBIOTICS Interestingly, between a span of almost twenty years (1969-1988) thousands of marine based extracts, fractions and pure isolates were evaluated for their antibiotic activity. However ,the success rate was not only miserable but absolutely no significant as on date not even a single marine derived antibiotic substance has able to either super ceded or gained enormous recognition with regard to their broad spectrum of activity and superb quality of the known and available antibiotics obtained from the innumerable terrestrial organisms, semi synthetic products, and purely synthetic ones . Nevertheless, the earnest efforts contributed by the marine- chemists across the globe have been able to evolve a few antibiotics from the various marine organisms, namely : okadaic acid , acanthifolicin and norhalichondrin A. these naturally occurring marine antibiotics shall now be disscused. Interestingly, between a span of almost twenty years (1969-1988) thousands of marine based extracts, fractions and pure isolates were evaluated for their antibiotic activity. However ,the success rate was not only miserable but absolutely no significant as on date not even a single marine derived antibiotic substance has able to either super ceded or gained enormous recognition with regard to their broad spectrum of activity and superb quality of the known and available antibiotics obtained from the innumerable terrestrial organisms, semi synthetic products, and purely synthetic ones . Nevertheless, the earnest efforts contributed by the marine- chemists across the globe have been able to evolve a few antibiotics from the various marine organisms, namely : okadaic acid , acanthifolicin and norhalichondrin A. these naturally occurring marine antibiotics shall now be disscused.
  16. 16. OKADAIC ACID Synonym : Halochondrine A (marine black sponge) Biological source: it is obtained from Halichondria (Okadai) CHEMICAL STRUCTURE CHARACTERISTIC FEATURES : 1. It is obtained from dichloromethane 2. It has specific optical rotation 3. It also reported as in crystal from USES : 1. It is important biochemical tool as tumour promoter and probe of cellular regulation 2.It is found to be far more cytotoxic to KB- cells 3. It is able to transport divalent cat ions eg: ca+ CHEMICAL STRUCTURE
  17. 17. ACANTHIFOLICIN Biological source : Acanthifolicin is obtained from pandaros acanthifolium (sponge) CHEMICAL STRUCTURE CHARACTERISTIC FEATURES : 1.It possesses an antibacterial activity 2. It also exerts cytotoxic actions 3. It is found to be lethal to mice at low dose level USES :1. It is probe of cellular regulation 2. It is more cytotoxic
  18. 18. NOR HALICHONDRIN-A Biological source : norhalichondrin A and several other halichondrin structural analogues have been obtained from halichondria okadai (sponge). CHARACTERISTIC FEATURES : •It is a polyether macrolide . •The structure activity correlation studies with regard to their derivative; and also their structural fragments are of significant biological interest USES: It is found to exert antitumor activity CHEMICAL STRUCTURE
  19. 19. E . ANTI-INFLAMMATORY and ANTI-SPASMODIC AGENT A plethora of chemical substance have been isolated from the broad spectrum of marine organisms which attribute either anti-inflammatory or antispasmodic activities . TETRADO TOXIN Biological source :Tetradotoxin is obtained from liver and ovaries of puffer fish USES: 1.It is used as anti- inflammatory 2. It has analgesic effect 3. it acts as muscle relaxant
  20. 20. F . MISCELLANEOUS PHARMACOLOGICALLY ACTIVE SUBSTANCE A good number of pharmacologically active substance have been isolated and characterized from marine organisms that invariably exhibit a variety of interesting actions . A few imported and typical example have been grouped together under this section latrunculins, kainic acid , domoic acid LATRUNCULINS Biological source: latruncullins are obtained from latrunculia magnifica keller (red sea sponge) they are also found in chromodoris elisabethina (pacific nudibraanch) and the spongia mycofijiensis (fijian) These are the first and foremost family of natural marine based products essentially having the 2- thiazolidinone moiety .it is classified into four toxics latrunculins A-D but c and d not well used Biological source: latruncullins are obtained from latrunculia magnifica keller (red sea sponge) they are also found in chromodoris elisabethina (pacific nudibraanch) and the spongia mycofijiensis (fijian) USES: 1. They are exclusively in establishing of molecular mechanism of motile processes 2. unlike cytochalasins the LAT-A and LAT- B do not afford any change in the polymerization rate of active filaments. CHEMICAL STRUCTURE
  21. 21. DOMOIC ACID Biological source: It is obtained from chondria armata okamura (rhodomelaceace)(red algae) also known as japanese as DOMOI and hence the name domoic acid. CHEMICAL STRUCTURECHEMICAL STRUCTURE Domoic acid is a neurotoxin that inhibits neurochemical processes, causing short-term memory loss, brain damage, and, in severe cases, death in humans. In marine mammals, domoic acid typically causes seizures and tremors.
  22. 22. CONCLUSION In short, the marine-world evidently & explicitly enjoys status of holding an enormous & tremendous potent towards epoch making discovery of a plethora of al to gather newer Lead Molecules in the development of medicinally potent therapeutic agents that are active against a variety of parasites & infectious ailments. With the advent of recent development & use of technologically advanced computer aided sophisticated analytical instruments have turned this novel dream like fiction into reality. CONCLUSION In short, the marine-world evidently & explicitly enjoys status of holding an enormous & tremendous potent towards epoch making discovery of a plethora of al to gather newer Lead Molecules in the development of medicinally potent therapeutic agents that are active against a variety of parasites & infectious ailments. With the advent of recent development & use of technologically advanced computer aided sophisticated analytical instruments have turned this novel dream like fiction into reality.
  23. 23. 23 Thank You!

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