Part C | 21.2
532 Part C Marine Genomics
of the ocean, which prevails over the diversity of land,
shows a huge promise as a source of potential natural
products in future. In a recent study, Leal et al. [21.1]
compiled yearly reviews from 1990 to 1999 and 2000 to
2009 on marine natural products, which were published
in the journal Natural Products Reports. The reviews
pointed out that there was a noticeable increase in the
discovery of new natural products from porifera in the
first five years of the 1990s, which subsequently maintained a flat trend. However, the discovery of NMNP
from Cnidaria increased over the decades with a noticeable increase in the last 20 years. The class Anthozoa
generally comprise 99% of NMNP, which belongs to
the phylum Cnidaria. Further, most scleractinian corals
are representative of this class. The discovery of new
natural products from the Anthozoa class increased by
72% from the 1990s to the 2000s.
The investigation of natural products as novel human therapeutics reached its peak in the western pharmaceutical industry during 19701980 : It was reported
that between 1981 and 2002, a total of 877 small
molecules, new chemical entities (NCEs), were introduced and interestingly, approximately half of these
were derived from natural products, semisynthetic natural product analogs, or synthetic compounds based on
natural product pharmacophores [21.2].
Recently, Cheng et al. [21.3] discovered three new
diterpenoids designed as gyrosanols A–C from the soft
coral Sinularia gyrosa. An in vitro cytotoxicity study
with these compounds revealed activity against human
lung carcinoma (A-459), human colon adenocarcinoma
(HT-29), and mouse lymphocytic leukemia (P-388)
cancer cell lines. It also showed antiviral activity against
the human cytomegalovirus and antibacterial activity
against five pathogenic bacterial strains, Enterobacter
aerogenes, Salmonella enteritidis, Serratia marcescens,
Shigella sonnei, and Yersinia enterocolitica.
Initially, studies on another species, S. crassa,
yielded sphingosine and steroids possessing antiinflammatory activity. A further study by Cheo
et al. [21.4] confirmed isolation of eight new cembranoids showing bioactivity against selected human
carcinoma cells.
In a recent study, five new polyoxygenated steroids
were derived from the bamboo coral Isis hippuris, with
anti-HCMV (HCMV) activity as well as cytotoxicity
against selected cell lines. One of these compounds
showed inhibitory activity against HCMV, with an
EC 50 value of 6:0 g=ml [21.5].
Nematocyst venom of fire warm Millepora platyphylla (Mp-TX) was extracted and simultaneous biological and biochemical assays were performed to monitor the hemolytic, using washed human red blood cells
(RBC) and phospholipase A2 (using radio labeled sn2 C14-arachidonyl phosphatidylcholine as a substrate)
active venom fractions. The magnitude of both hemolysis and phospholipase A2 activity was found in a fraction rich in proteins of molecular masses of approximately 30 00034 000 Da. The former fraction was
purified by ion exchange chromatography, and a major bioactive protein factor (approximately 32 500 Da,
here named milleporin-1) was recovered. Milleporin1 enzymatic activity showed a significant contribution
to the overall hemolysis of human RBCs [21.6]. Su
and Wen [21.7] recently isolated five membrane-based
diterpenoids from the Taiwanese soft coral Sinularia
triangular. Among them, triangulenes A and B were
reported to be new metabolites and 3 and 5 exhibited moderate cytotoxicity to human tumor cell line
(CCRF-CEM) and DLD-1 (dihydrolipoamide dehydrogenase). Metabolites 4 and 5 also effectively reduced the expression of the COX-2 protein of the
macrophages.
Pharmaceutical research, especially the development of different antibiotics based on the screening of
different microbes expanded rapidly following the discovery of penicillin just after the Second World War.
By 1990, about 80% of drugs were either natural products or analogs inspired by them. Antibiotics (e.g.,
penicillin, tetracycline, erythromycin), antiparasitics
(e.g., avermectin), antimalarials (e.g., quinine), lipid
control agents (e.g., lovastatin and analogs), immune
suppressants for organ transplants (e.g., cyclosporine,
rapamycin), and anticancer drugs (e.g., taxol) revolutionized the pharmaceutical industry.
Bryozoans are an independent group of animals
closely related to corals and are the source of many
potent bioactive compounds. A common bryozoan
species, Bugula neritina, is a potent source of the protein kinase C inhibitor called bryostatin. Bryostatin-1
has been granted orphan drug status by the Food and
Drug Administration (FDA) and has been designated as
an orphan medicinal product in Europe for oesophageal
cancer in combination with paclitaxel [21.8].
532 Part C Marine Genomics
of the ocean, which prevails over the diversity of land,
shows a huge promise as a source of potential natural
products in future. In a recent study, Leal et al. [21.1]
compiled yearly reviews from 1990 to 1999 and 2000 to
2009 on marine natural products, which were published
in the journal Natural Products Reports. The reviews
pointed out that there was a noticeable increase in the
discovery of new natural products from porifera in the
first five years of the 1990s, which subsequently maintained a flat trend. However, the discovery of NMNP
from Cnidaria increased over the decades with a noticeable increase in the last 20 years. The class Anthozoa
generally comprise 99% of NMNP, which belongs to
the phylum Cnidaria. Further, most scleractinian corals
are representative of this class. The discovery of new
natural products from the Anthozoa class increased by
72% from the 1990s to the 2000s.
The investigation of natural products as novel human therapeutics reached its peak in the western pharmaceutical industry during 19701980 : It was reported
that between 1981 and 2002, a total of 877 small
molecules, new chemical entities (NCEs), were introduced and interestingly, approximately half of these
were derived from natural products, semisynthetic natural product analogs, or synthetic compounds based on
natural product pharmacophores [21.2].
Recently, Cheng et al. [21.3] discovered three new
diterpenoids designed as gyrosanols A–C from the soft
coral Sinularia gyrosa. An in vitro cytotoxicity study
with these compounds revealed activity against human
lung carcinoma (A-459), human colon adenocarcinoma
(HT-29), and mouse lymphocytic leukemia (P-388)
cancer cell lines. It also showed antiviral activity against
the human cytomegalovirus and antibacterial activity
against five pathogenic bacterial strains, Enterobacter
aerogenes, Salmonella enteritidis, Serratia marcescens,
Shigella sonnei, and Yersinia enterocolitica.
Initially, studies on another species, S. crassa,
yielded sphingosine and steroids possessing antiinflammatory activity. A further study by Cheo
et al. [21.4] confirmed isolation of eight new cembranoids showing bioactivity against selected human
carcinoma cells.
In a recent study, five new polyoxygenated steroids
were derived from the bamboo coral Isis hippuris, with
anti-HCMV (HCMV) activity as well as cytotoxicity
against selected cell lines. One of these compounds
showed inhibitory activity against HCMV, with an
EC 50 value of 6:0 g=ml [21.5].
Nematocyst venom of fire warm Millepora platyphylla (Mp-TX) was extracted and simultaneous biological and biochemical assays were performed to monitor the hemolytic, using washed human red blood cells
(RBC) and phospholipase A2 (using radio labeled sn2 C14-arachidonyl phosphatidylcholine as a substrate)
active venom fractions. The magnitude of both hemolysis and phospholipase A2 activity was found in a fraction rich in proteins of molecular masses of approximately 30 00034 000 Da. The former fraction was
purified by ion exchange chromatography, and a major bioactive protein factor (approximately 32 500 Da,
here named milleporin-1) was recovered. Milleporin1 enzymatic activity showed a significant contribution
to the overall hemolysis of human RBCs [21.6]. Su
and Wen [21.7] recently isolated five membrane-based
diterpenoids from the Taiwanese soft coral Sinularia
triangular. Among them, triangulenes A and B were
reported to be new metabolites and 3 and 5 exhibited moderate cytotoxicity to human tumor cell line
(CCRF-CEM) and DLD-1 (dihydrolipoamide dehydrogenase). Metabolites 4 and 5 also effectively reduced the expression of the COX-2 protein of the
macrophages.
Pharmaceutical research, especially the development of different antibiotics based on the screening of
different microbes expanded rapidly following the discovery of penicillin just after the Second World War.
By 1990, about 80% of drugs were either natural products or analogs inspired by them. Antibiotics (e.g.,
penicillin, tetracycline, erythromycin), antiparasitics
(e.g., avermectin), antimalarials (e.g., quinine), lipid
control agents (e.g., lovastatin and analogs), immune
suppressants for organ transplants (e.g., cyclosporine,
rapamycin), and anticancer drugs (e.g., taxol) revolutionized the pharmaceutical industry.
Bryozoans are an independent group of animals
closely related to corals and are the source of many
potent bioactive compounds. A common bryozoan
species, Bugula neritina, is a potent source of the protein kinase C inhibitor called bryostatin. Bryostatin-1
has been granted orphan drug status by the Food and
Drug Administration (FDA) and has been designated as
an orphan medicinal product in Europe for oesophageal
cancer in combination with paclitaxel [21.8].