Sumberdaya Farmasi

Perikanan-Kelautan
MARINE BIODIVERSITY AND THEIR
POTENTIAL FOR DEVELOPING
PHARMACEUTICAL AND COSMETICAL
INDUSTRY IN INDONESIA



 Marine Biodiversity Geotectonic Position

UNCLOS
Implementation

Dynamic Oceanography and International Sea Lines

Climate Variability
2
Sources • Coastal & marine organisms used
as traditional medicine
Banten, P. Seribu, Buton, Lombok,
Bali, Mentawai, Aceh, Kalimantan,
Bangka-Belitung, Maluku (Kayoa,
Jailolo)
• Marine algae, sponges, corals
 Banten, P. Seribu, Garut,
Sulawesi
• Symbiotic microorganisms of
coastal & marine organisms
• Thermophilic Microorganisms
from unique sources ( hot spring
bracksist +saline)
 Sample collection
Traditional knowledge Screening for bioative compound (non-target & target/m
Random Antiinfectives (antimicrobial)
Thermophilic microorganism Anticancer ( Cytotoxic, Topoisomerase inhibitor)
Antioxidant (anticholesterol & antiatherogenic, anticanc
Other traditional usage (UV-protector, androgenic, etc)
Novel enzime
Crude extracts

Identification Selected organisms Bioassay guided

Morphological fractionation
Biochemical
Molecular
Symbiont isolation Purification &
structure elucidation

Bioprocess Culture
Formulation
developme developme
Nutraceuticals, cosmetics Lead compound
nt nt
Feed, others
 Table . Some of samples and their biological activities
No Group Bioactivity Scientific name
1 Coastal plant Antioxidant, natural color, cytotoxic Pandanus sp
2 Coastal plant Antimicrobes, antioxidant, biodesinfectant Pemphis sp
3 Coastal plant Antimicrobe & Antioxidant, cytotoxic Ipomoea sp
4 Sea star Antioxidant Astropecten sp
5 Sea worm aprodisiax Eunice sp
6 Sea cucumber Antimicrobes, cytotoxic Sticopus sp
7 Sea slug Antioxidant, aprodisiax Discodoris sp
8 Mangrove Antimicrobe, sunscreen, cytotoxic Xylocarpus sp
9 Fish antifouling Carcharhinus sp
10 Algae Antimicrobe Entheromorpha sp
11 Coastal plant Antimicrobe Clerodendrum
12 Algae Antioxidant Gelidiella sp
13 Coastal plant Antimicrobe, antioxidant, cytotoxic Solanum sp
14 Sponge cytotoxic Stylotella sp
15 Sponge cytotoxic Stylissia sp
16 Sponge cytotoxic Axinella sp
17 Sponge Cytotoxic Acanthella sp
18 Algae Cytotoxic unidentified
 Source Substance Activity Price
sponge Manoalide Phospolipase A2 inhibitor $ 120 / mg
sponge Calyculin A Protein phopatase inhibitor $ 105 / 25 mg

sponge Luffariellolide Phospolipase A2 inhibitor $ 100 / mg

sponge 12-epi- Phospolipase A2 inhibitor $ 136 / mg
scalaridial
sponge Latrunculin B Actin polymerization $ 90 / mg
inhibitor
sponge Mycalolide B Actin polymerization $ 212 / 20 µg
inhibitor
sponge Swinholide A Actin microfilament $ 100 / 20 µg
disruptor
Dinoflagelata Okadaic acid Protein phospatase inhibitor $ 75 / 25 µg

Bryozoan Bryostatin 1 Protein kinase C activator $ 88 / 10 µg

BioMol [ www.biomol.com]
 RESULTS FROM THE ASSESSMENT OF BPPT
Secondary Metabolites from sponges
FromAxinella carteri
H2N
N

HN
O

HN
NH
O
3-Bromhymenialdisin Hymenialdisin
Debromhymenialdisin
•Insecticide
•Protein Phosphatase Inhibitor
•Insecticide
•Novel
•Insecticide
1

3
NH

4 O C H3
Aaptamin
•Antibacterial
9

5
8 •Cytotoxic
6 7 O C H3

FromAaptos Suberitoides
7
Click to Secondary
edit Master
Metabolitestitle style
from sponges
From Theonella swinhoei

Calyculin derivative
•Active against 51 cancer cell lines
•Insecticide
•Fungicide
•Protein phosphatase Inhibitor 2
•Novel
8
 Antimicrobes compound from marine algaeEucheuma serra ,Halimeda
opuntia danHydroclathrus clathratus (Warambadi, Sumba)

1. Fatty acids

8-Octadecenoic acid, methyl ester;

(E)-Methyl trans-8-octadecenoate

3-hydroxy-nonadeca-5,8,11,14-tetraenoic acid 3-hydroxy-20-methyl heneicosa-5,8,11-trienoic acid

1,2- Benzenedicarboxylic acid, dioctyl ester 1,2- Benzenedicarboxylic acid, diisooctyl ester

Methyl eicosa-5,8,11,14,17-pentaenoate Methyl arachidonate

1,2- Benzenedicarboxylic acid, dioctyl ester 1,2- Benzenedicarboxylic acid, diisooctyl ester

Methyl eicosa-5,8,11,14,17-pentaenoate Methyl arachidonate

2. Steroids

dihydrotestosteron acetic acid;

androstan-3-one,17-(acetyloxy)-,(5, 17)

Preg-15-en-20-one,17-methyl Cholest-5-en-3β-ol, 24-propylidene

1,2- Benzenedicarboxylic acid, dioctyl ester 1,2- Benzenedicarboxylic acid, diisooctyl ester

Methyl eicosa-5,8,11,14,17-pentaenoate
Methyl arachidonate
2. Steroids

androstan-11-one,3-(acetyloxy)-17-iodo-(17)
dihydrotestosteron acetic acid;
androstan-3-one,17-(acetyloxy)-,(5, 17)

Preg-15-en-20-one,17-methyl Cholest-5-en-3β-ol, 24-propylidene

3. Aldehydes

9-[3-(1-hydroxy-butyl)-oxiranyl]-nonanal

11-[3-(1-hydroxy-butyl)-oxiranyl]-undecanal

4. Ether

3,7,11-Trimethyl-1-(3-methyl-butoxy)-dodec-2-en
 SCREENING, ISOLATION AND IDENTIFICATION OF
TOPOISOMERASE INHIBITOR AS MOLECULAR TARGET
FOR ANTICANCER

• Cell based (cytotoxic)

• Target based (protein or
enzyme)
• Topoisomerases: essential
nuclear enzymes untuk DNA
replication.
– Topoisomerase I generates
single-stranded breaks,
– topoisomerase II introduces
double-stranded breaks.
• Topoisomerase inhibitors :
causing to cell death.
• All cell require topoisomerase,
however cancer cells need
more than normal cell
 Tabel 3. Topoisomerase Inhibitor Cancer Drugs

Target Indikasi Status Manufacturer

 Produk
Campto Topoisomerase I Colorectal cancer Market Aven tis an d
Merck
Hycamtin Topoisomerase I Small c ell lu n g Market GlaxoSmithKlin
cancer e
Lucanthone Topoisomerase II Brain tumor Phase II SuperGen
MLN576 To po iso m e rase I Various tumors Phase I Millennium
and II
Novantrone Topoisomerase II L e u ke mia an d Market OSI
n on -small cell
lung cancer
OSI211 Topoisomerase I Ovarian and mall Phase I OSI
cell lung cancers
Pegamoteca Topoisomerase I Gastroesopheagal Phase II Enzon
n cancer
Rubitecan Topoisomerase I Colorectal cancer Phase II SuperGen