products, as well as through extraction and refinement from metabolites in
microorganism, plant, and animal cell strains or through chemical synthesis.
The chief focus in natural substance bioactivity has been on antioxidation,
anti-inflammation, anticancer, antitumor, cytotoxic, antibacterial, antifungal, and
antiviral (e.g., HSV, HIV, cytomegalovirus) effects. Increasingly, however, attention is focusing on antimycotic activity and on bioactivity related to specific
mechanisms, including the inhibition of particular enzymes or active substances,
ion channel regulation, and signal transmission. More and more leading groups are
shifting away from general activity toward mechanism-centered activity.
Marine natural products exhibit clear characteristics according to organism type.
Over 90% of natural substances from corals and other coelenterates consist of
terpenoids or the mixed biomaterials that form their framework, while oxylipins
account for the remainder. Virtually no alkaloid content has been detected. In
contrast, alkaloids are the main components of natural substances from sea squirts,
while terpenoids are present only in trace amounts.
Most natural substances from mollusks are polypropionates, which are rarely
found in other marine plants or animals. Echinoderms such as starfish and sea
cucumbers are well known for their saponin content. While saponin is known to be
present in large quantities in ginseng and some other land-based life forms, it is
only rarely found in marine flora and fauna.
In contrast, substances from nearly every type of biosynthetic origin can be
found in sponges, which occupy a central place in new marine substance research.
The natural substance bioactivity that has been the driving force in pharmaceutical
development has been focused chiefly on anticancer and antimicrobial effects.
Indeed, over 40% of new substances reported have exhibited anticancer activity
such as cytotoxicity and angiogenic inhibition. Antibacterial activity consists largely of Gram-positive and Gram-negative bacteria inhibition and intractable
infectious diseases was infected with bacteria and fungus, tuberculosis, and malaria.
Research over the past 30 years has led to the discovery of new bioactive
substances and substances with outstanding bioactive properties that have been
isolated and refined from various forms of marine organisms, including sponges,
large algae, coral, plankton, actinomycetes, fungi, and other marine microbes. Some
of these have shown strong anticancer and anti-inflammatory properties and effects
against cardiovascular disease. Several achievements have also been made in
research on these components’ pharmacology, medicinal effects, and toxicity
(Hartmann et al. 2015).
Table 10.1 shows some of the approved marine organism-derived pharmaceuticals to date, as well as those undergoing clinical testing. Zinotide has already been
approved as a new pain reliever and trabectedin (ecteinocidein 743), x-3 unsaturated fatty acid (an EPA-DHA mixture), and eribulin mesylate (a halichondron
derivative) as anticancer agents. In Japan, EPA is currently being used as a treatment for arteriosclerosis. While it is not listed in the table, the seaweed-derived
polysaccharide carragelose has reportedly been approved as a cold medication in
Austria. Currently in their third stage of clinic testing are the Dolabella auriculariaderived Brentuximab vedotin (SGN-35) and depsipeptides (aurilide-antibody
10.3 Bioactive Substances from Marine Organisms
369
microorganism, plant, and animal cell strains or through chemical synthesis.
The chief focus in natural substance bioactivity has been on antioxidation,
anti-inflammation, anticancer, antitumor, cytotoxic, antibacterial, antifungal, and
antiviral (e.g., HSV, HIV, cytomegalovirus) effects. Increasingly, however, attention is focusing on antimycotic activity and on bioactivity related to specific
mechanisms, including the inhibition of particular enzymes or active substances,
ion channel regulation, and signal transmission. More and more leading groups are
shifting away from general activity toward mechanism-centered activity.
Marine natural products exhibit clear characteristics according to organism type.
Over 90% of natural substances from corals and other coelenterates consist of
terpenoids or the mixed biomaterials that form their framework, while oxylipins
account for the remainder. Virtually no alkaloid content has been detected. In
contrast, alkaloids are the main components of natural substances from sea squirts,
while terpenoids are present only in trace amounts.
Most natural substances from mollusks are polypropionates, which are rarely
found in other marine plants or animals. Echinoderms such as starfish and sea
cucumbers are well known for their saponin content. While saponin is known to be
present in large quantities in ginseng and some other land-based life forms, it is
only rarely found in marine flora and fauna.
In contrast, substances from nearly every type of biosynthetic origin can be
found in sponges, which occupy a central place in new marine substance research.
The natural substance bioactivity that has been the driving force in pharmaceutical
development has been focused chiefly on anticancer and antimicrobial effects.
Indeed, over 40% of new substances reported have exhibited anticancer activity
such as cytotoxicity and angiogenic inhibition. Antibacterial activity consists largely of Gram-positive and Gram-negative bacteria inhibition and intractable
infectious diseases was infected with bacteria and fungus, tuberculosis, and malaria.
Research over the past 30 years has led to the discovery of new bioactive
substances and substances with outstanding bioactive properties that have been
isolated and refined from various forms of marine organisms, including sponges,
large algae, coral, plankton, actinomycetes, fungi, and other marine microbes. Some
of these have shown strong anticancer and anti-inflammatory properties and effects
against cardiovascular disease. Several achievements have also been made in
research on these components’ pharmacology, medicinal effects, and toxicity
(Hartmann et al. 2015).
Table 10.1 shows some of the approved marine organism-derived pharmaceuticals to date, as well as those undergoing clinical testing. Zinotide has already been
approved as a new pain reliever and trabectedin (ecteinocidein 743), x-3 unsaturated fatty acid (an EPA-DHA mixture), and eribulin mesylate (a halichondron
derivative) as anticancer agents. In Japan, EPA is currently being used as a treatment for arteriosclerosis. While it is not listed in the table, the seaweed-derived
polysaccharide carragelose has reportedly been approved as a cold medication in
Austria. Currently in their third stage of clinic testing are the Dolabella auriculariaderived Brentuximab vedotin (SGN-35) and depsipeptides (aurilide-antibody
10.3 Bioactive Substances from Marine Organisms
369