This document summarizes research on the brown seaweed polysaccharide fucoidan. It discusses fucoidan's chemistry, sources, and various pharmacological applications. Specifically, it describes fucoidan's anti-angiogenic, anticoagulant, anticancer, anti-inflammatory, and potential use for treating diabetic retinopathy. The document also reviews fucoidan extraction methods and formulations for drug delivery applications.

1. Presented by
K.S. Raghavendra Prabu (II M.Tech)
Under the guidance of
Dr N. Subramanian
Associate Professor
Department of Pharmaceutical Technology
University College of Engineering
Anna University, BIT Campus
Tiruchirapalli-620024
Pharmacological Applications of
Brown seaweed: Fucoidan

2. Aim
To perform a literature survey about Fucoidan
to understand its chemistry, mechanism,
pharmacological activities and biological
applications for the further research work for
ocular treatment.

3. Objective
 To perform a complete literature review of
fucoidan from various published papers/online
sources/databases.
 To understand the various pharmaceutical
applications of fucoidan.

4. Fucoidan
 Fucoidan is a carbohydrate polysaccharide.
 Obtained from marine brown algae.
 Chemically, fucoidans cover major structural entities that denotes a family of fucose
containing sulfated polysaccharides, derived from different species.
 Fucoidan is a type of complex sulfated polysaccharide, mainly found in the cell wall
matrix of various brown seaweed species.
 White and hygroscopic
 Soluble in water, sparingly soluble in dimethyl sulfoxide and insoluble in ethanol.

5. Fucoidan
 Source : Fucus vesiculosus
 Composition: 44.1% fucose, 26.3% sulfate and 31.1% ash
 Main component unit of fucoidan was 1,2-α-fucose and most
of the sulfate groups were located at position C-4 of the
fucose units. (Conchie and Neill)
 IR spectrum confirmed that the sulfate group was substituted
at the axial C-4 position of the L-fucospynanose.
 GC/MS data of methylation, suggested that the core region of
fucoidan was primarily a polymer of α-(1→3) linked fucose
with sulfate groups filled at the C-4 position on fucose
residues.

6. Various Chemical composition of
Fucoidan from different sources
S. No Brown seaweed Chemical composition
1. Adenocytis utricularis fucose, galactose, mannose,
sulfate
2. Ascophyllum nodosum fucose(49%), xylose(10%),
GlcA(11%), sulfate
3. F. evanescens fucose/sulfate/acetate
(1/1.23/0.36)
4. F. distichus fucose/sulfate/acetate
(1/1.21/0.08)
5. F. vesiculosus fucose, sulfate
6. F. serratus L. fucose/sulfate/acetate
(1/1.23/0.36)
7. Macrocytis pyrifera fucose/galactose (18/1), sulfate

7. Distribution, Clearance, Half life of
Fucoidan
 Clearance - 0.88±0.46 mL/min
 Half life- 56.5±25.0 minutes
 Distribution volume 57.6±27.9 mL.
 Urinary excretion of LMW fucoidan was
33.2±2.1%.
 After intramuscular injection, plasma
concentration of LMW fucoidan were remained
in the 10 μg/mL range for 6 hours.

8. Pharmacological applications of Fucoidan
 Anti-angiogenetic activity
 Anticoagulant activity
 Anticancer activity
 Anti-proliferation activity
 Immunomodulation activity
 Anti-inflammation activity
 Antiviral, antibacterial, gastric mucosal protection and
neuroprotection activities.

9. Anti-angiogenetic activities
Administration of fucoidan causes
decreased vessels in the Matrigel plug and
CD31-stained capillaries in the tumor.
 Tumor size and weight were significantly
reduced in fucoidan treated mice
compared with that in control group.
(Fitton 2011).

10. Anticoagulant and antithrombotic
activities
 Fucose containing sulfated polysaccharide strongly
inhibits the activities of coagulation factors via
interaction with antithrombin III in both the extrinsic
and common coagulation pathways(Jung et al., 2007).
 It enhance AT III-mediated coagulation factor inhibition
in coagulation pathways.
 This contributes to its higher anticoagulant activity.

11. Immunomodulatory activities
 Many polysaccharides obtained from natural sources are considered as
biological response modifiers and have been shown to enhance various
immune responses (Li et al., 2008).
 Immunomodulatory effects of fucoidan purified from brown seaweed
Fucus vesiculosus on dendritic cells were reported. (Kim & Joo, 2008).
 Fucoidan post-translationally regulated MMP-9 secretion from U937
cells (Jintang et al., 2010).
 Fucoidan possesses immunomodulating activity to induce cytokines
and chemokines from macrophages and splenocytes (Yoo et al., 2007).

12. Anti-inflammatory activities
 Fucoidans inhibited leucocyte recruitment in an inflammation
model in rats, and neither the content of fucose and sulfate nor other
structural features of their polysaccharide backbones significantly
affected the efficacy of fucoidans in this model (Nifantiev et al.,
2007).
 In vitro evaluation of P-selectin-mediated neutrophil adhesion to
platelets under flow conditions revealed the polysacharide could
serve as P-selectin inhibitors.
 Therefore this forms a new development of potential drugs for
thrombosis, inflammation, and tumor progression.

13. Diabetic Retinopathy
 Diabetic Retinopathy (DR) is a
complication of diabetes associated with
irreversible loss of blindness.
 The first complication associated with
DR is vitreous hemorrhage in which the
new blood vessels bleed into a clear,
jelly-like substance that fills in the center
of the eyes.
 The second complication associated with
DR is referred to as retinal detachment
(Vislisel and Oetting 2010).
 In 2013, it was estimated that 20% (35.5
million) of world’s population with
undiagnosed diabetes live in India. (A. T.
Jotheeswaran,)

14. Fucoidan for Diabetic retinopathy
 Fucoidan defenses of the upregulated transcriptional factor HIF-1a
and VEGF.
 Fucoidan resembles calcium dobesilate and might serve as a
potential candidate drug for prevention and treatment of DR for
further development. (Dali Luo et al., 2013)

15. Formulations of fucoidan
 A number of marine-based polysaccharides,
such as agar, alginate, carrageenan, fucoidan,
chitosan and hyaluronan are utilized in
pharmaceutical dosage form as binders,
vehicles, disintegrating agents, gelling agents
and drug release sustaining agents.
Applications of marine polysaccharides, with
a special emphasis in multifunctional
excipients development for enhancing ,
1. Bioavailability
2. drug delivery applications.
As Binder
Due to the high concentration of hydroxyl
groups in the polysaccharide, generally have
a high water-binding capacity that makes wet
granulation easier

16. References
1. Ahmed Zayed, Kai Muffler, Thomas Hahn, Steffen Rupp, Doris Finkelmeier, Anke Burger-
Kentischer, Roland Ulber, (2016). Physicochemical and Biological Characterization of Fucoidan
from Fucus vesiculosus Purified by Dye Affinity Chromatography. Marine Drugs, Vol. 14, pp. 79-84;
doi:10.3390/md14040079
2. Bo Li, Fei Lu, Xinjun Wei, Ruixiang Zhao, (2008). Fucoidan: Structure and Bioactivity. Molecules,
Vol. 13, pp. 1671-1695. DOI: 10.3390/molecules13081671
3. Andriy Synytsy, Woo-Jung Kim, Sung-Min Kim, Radek Pohl, Alla Synytsya, František Kvasnicˇka,
Jana Cˇ opikova , Yong Il Park , (2010). Structure and antitumour activity of fucoidan isolated from
sporophyll of Korean brown seaweed Undaria pinnatifida. Carbohydrate polymers, Vol. 81, pp. 41-
48
4. Albana Cumashi, Natalia A. Ushakova, Marina E. Preobrazhenskaya, Armida D’Incecco, Antonio
Piccoli, et al., (2007). A comparative study of the anti-inflammatory, anticoagulant, antiangiogenic,
and antiadhesive activities of nine different fucoidans from brown seaweeds, Glycobiology, Vol. 17,
pp. 541-552
5. Farzaneh Atashrazm, Ray M. Lowenthal, Gregory M. Woods, Adele F. Holloway, Joanne L.
Dickinson, (2015). Fucoidan and Cancer: A Multifunctional Molecule with Anti-Tumor Potential.
Marine Drugs. Vol. 13, pp. 2327-2346, doi:10.3390/md13042327, Marine drugs
6. Hyuck-Jin Chung, Jungae Jeun, Soung-Jin Houng, Hee-Jin Jun, Dong-Keon Kweon, Sung-Joon Lee,
(2010). Toxicological Evaluation of Fucoidan from Undaria pinnatifi da In Vitro and In Vivo.
Phytotherapy Research Vol. 24, pp. 1078–1083. DOI: 10.1002/ptr.3138
7. Jean-François Deux, Anne Meddahi-Pellé,, Françoise Bree , Isabelle Bataille, Jean-Baptiste Michel
and Didier Letourneur (2008). Comparative Studies on the Mechanisms of Action of Four
Polysaccharides on Arterial Restenosis. Journal of Biomaterials Science, Vol 20, pp. 689-702

17. 8. Meng-Chuan Chen, Wen-Lin Hsu, Pai-An Hwang and Tz-Chong
Chou (2015). Low Molecular Weight Fucoidan Inhibits Tumor
Angiogenesis through Downregulation of HIF-1/VEGF Signaling
under Hypoxia. Marine drugs. Vol. 13, pp. 4436-4451
9. Stephen P Myers, Joan O’Connor , J Helen Fitton, Lyndon
Brooks, Margaret Rolfe, Paul Connellan, Hans Wohlmuth, Phil A
Cheras, Carol Morris, (2010). A combined phase I and II open
label study on the effects of a seaweed extract nutrient complex
on osteoarthritis. Biologics: Targets & Therapy, Vol. 4, pp. 33–44
10. Takeaki Nagamine, Kyoumi Nakazato, Satoru Tomioka,
Masahiko Iha, Katsuyuki Nakajima, (2014). Intestinal Absorption
of Fucoidan Extracted from the Brown Seaweed, Cladosiphon
okamuranus . RSC Advances, Vol, 3, pp. 48-64. DOI:
10.1039/c3ra23373a
11. Thomas Hahna, Siegmund Lang, Roland Ulbera, Kai Mufflera
(2012). Novel procedures for the extraction of fucoidan from
brown algae. Process Biochemistry, Vol. 47, pp. 1691-1698