Doc:Bioactives
From Metabolomics.JP
Bioactive Metabolites
Bioactivity refers to antimicrobial, antitumor, antiviral, pharmacological, and similar activities. Such functions are generally not associated with structures or producer species or pathways.
| Bioactivity types of discovered microbial metabolites [1] | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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The number of bioactive natural products is estimated around 200000 to 250000.
Approximate number of known natural products[1]
| Source | All known compounds | “Bioactives” | Antibiotics |
|---|---|---|---|
| Natural Products | over one million | 200000 to 250000 | 25000 to 30000 |
| Plant Kingdom | 600000 to 700000 | 150000 to 200000 | ca. 25000 |
| Microbes | over 50000 | 22000 to 23000 | ca. 17000 |
| Algae, Lichens | 3000 to 5000 | 1500 to 2000 | ca. 1000 |
| Higher Plants | 500000 to 600000 | ca. 100000 | 10000 to 12000 |
| Animal Kingdom | 300000 to 400000 | 50000 to 100000 | ca. 5000 |
| Protozoa | several hundreds | 100 to 200 | ca. 50 |
| Invertebrates: | ca. 100000 | ? | ca. 500 |
| Marine animals | 20000 to 25000 | 7000 to 8000 | 3000 to 4000 |
| Insects/worms/etc. | 8000 to 10000 | 800 to 1000 | 150 to 200 |
| Vertebrates (mammals, fishes, amphibians, etc.) |
200000 to 250000 | 50000 to 70000 | ca. 1000 |
In microbes, most bioactive natural products are found in Actinomycetales and fungi.
Approximate number of bioactive microbial natural products (2002). According to their producers[1]
| Source | Antibiotics | “Other bioactive” metabolites |
Total bioactive metabolites |
Practically used (in human therapy) |
Inactive metabolites |
|---|---|---|---|---|---|
| Bacteria | 2900 | 900 | 3800 | 10 to 12 (8 to 10) | 3000 to 5000 |
| Actinomycetales | 8700 | 1400 | 10100 | 100 to 120 (70 to 75) | 5000 to 10000 |
| Fungi | 4900 | 3700 | 8600 | 30 to 35 (13 to 15) | 2000 to 15 000 |
| Total | 16500 | 6000 | 22500 | 140 to 160 (ca. 100) | 20000 to 25000 |
In higher forms of life, most natural products are found in plants and sponges.
Approximate numbers of bioactive natural products (2002). Derived from higher forms of life[1]
| Source | Antibiotics | “Other bioactive” | Total | |
|---|---|---|---|---|
| Lichens | 160 | ? | 160 | Plant products 13210 |
| Algae | 620 | 730 | 1350 | |
| Lower Plants (Bryophyta)* | 200 | ? | 200 | |
| Higher Plants* | 11500 | ? | 11500 | |
| Invertebrates* | 480 | ? | 480 | Animal products 7280 |
| Insects* | 320 | 320 | ||
| Worms, others (crustaceans)* | 160 | 160 | ||
| Marine Animals (total) | 3400 | 2700 | 6100 | |
| Sponges | 1850 | 1500 | 3350 | |
| Coelenterates | 630 | 570 | 1100 | |
| Tunicates | 420 | 230 | 650 | |
| Molluscs | 300 | 350 | 650 | |
| Echinoderms | 220 | 60 | 280 | |
| Bryozoa | 70 | 50 | 120 | |
| Fishes* | 50 | ? | 50 | |
| Amphibians, reptils* | 240 | ? | 240 | |
| Terrestrial vertebrates* (total) | 410 | ? | 410 | |
| Mammals* | 340 | 340 | ||
| Others (birds, etc.)* | 50 | 50 | ||
| Total | 16985 | 20540 | ||
| * ... Only antibiotic compounds, but no "other bioactive" compounds are covered. | ||||
Most frequent producers are relatively limited.
- Exclusively fungi
- All peptaibols (300-400), grisan and scirpene derivatives, cytochalasins (>100 each) are produced exclusively by fungi.
- Microscopic fungi frequently produce small (8-10) membered lactone ring compounds (-200), dilactones or condensed macrolactones, macrodiolides, azaphilones, diketothiapiperazines, small terpenoids and simple benzene derivatives, alpha-pyrones, xanthone derivatives, simple benzo- or naphthoquinones.
More than half of all bacterial metabolites are amino acid derivatives (e.g. peptides, peptolides, polypeptides).
- Exclusively bacteria
- cyclolipopeptides (polymyxins) and lantibiotics (nisin type) are exclusively produced by bacteria.
Approximate number of bioactive microbial metabolites according to their producers and bioactivities[1]
| Bioactive secondary microbial metabolites | |||||
| Source | Antibiotics | Bioactive metabolites | Total bioactive metabolites | ||
| Total | (with other activity) | no antibiotic activity | (antibiotics plus “other bioactives”) | ||
| Bacteria | 2900 | (780) | 900 | (1680) | 3800 |
|---|---|---|---|---|---|
| Eubacteriales | 2170 | (570) | 580 | (1150) | 2750 |
| Bacillus sp. | 795 | (235) | 65 | (300) | 860 |
| Pseudomonas sp. | 610 | (185) | 185 | (370) | 795 |
| Myxobacter | 400 | (130) | 10 | (140) | 410 |
| Cyanobacter | 300 | (80) | 340 | (420) | 640 |
| Actinomycetales | 8700 | (2400) | 1400 | (3800) | 10100 |
| Streptomyces sp. | 6550 | (1920) | 1080 | (3000) | 7630 |
| Rare actinos | 2250 | (580) | 220 | (800) | 2470 |
| Fungi | 4900 | (2300) | 3700 | (6000) | 8600 |
| Microscopic fungi | 3770 | (2070) | 2680 | (4750) | 6450 |
| Penicillium/Aspergillus | 1000 | (450) | 950 | (1400) | 1950 |
| Basidiomycetes | 1050 | (200) | 950 | (1150) | 2000 |
| Yeasts | 105 | (35) | 35 | (70) | 140 |
| Slime moulds | 30 | (5) | 20 | (25) | 60 |
| Total Microbial | 16500 | (5500) | 6000 | (11500) | 22500 |
| Protozoa | 35 | (10) | 5 | (45) | 50 |
In actinomycetales, the rare actinos produce most diverse and unique compounds.
- Exclusively rare actinos
- All known glycopeptide antibiotics (about 120) and most orthosomycins are produced exclusively by rare actinos.
- Exclusively actinomycetales
- All known macrolides, polyene antibiotics, aminoglycosides, anthracyclines are produced exclusively by actinomycetales.
- Known small categories such as:
- polyether antibiotics (-250),
- novobiocin related glycosidic antibiotics, streptothricins, actinomycins, echinomycin-like quinoxalin peptides (80-120 each),
- elfamycins, glutarimides, orthosomycins (50-60 each)
Number of actinomycetales species producing bioactive microbial metabolites[1]
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