Doc:Bioactives

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=={{Bilingual|生理活性物質|Bioactive Metabolites}}==
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==={{Bilingual|生理活性とは|On Bioactivity}}===
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=={{Bilingual|生理活性物質|Bioactive Metabolites}}==
 
{{Twocolumn|
 
{{Twocolumn|
 
Bioactivity refers to antimicrobial, antitumor, antiviral, pharmacological, and similar activities. Such functions are generally not associated with structures or producer species or pathways.
 
Bioactivity refers to antimicrobial, antitumor, antiviral, pharmacological, and similar activities. Such functions are generally not associated with structures or producer species or pathways.
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==={{Bilingual|生理活性物質は自然界に20～25万程度存在すると予想される。|The number of bioactive natural products is estimated around 200000 to 250000.}}===
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=={{Bilingual|生理活性物質は自然界に20～25万程度存在すると予想される。|The number of bioactive natural products is estimated around 200000 to 250000.}}==
 
Approximate number of known natural products<ref name="Berdy"/>
 
Approximate number of known natural products<ref name="Berdy"/>
 
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==={{Bilingual|微生物の中では、放線菌とカビ類が生理活性物質を生産する。|In microbes, most bioactive natural products are found in Actinomycetales and fungi.}}===
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=={{Bilingual|微生物の中では、放線菌とカビ類が生理活性物質を生産する。|In microbes, most bioactive natural products are found in Actinomycetales and fungi.}}==
 
Approximate number of bioactive microbial natural products (2002). According to their producers<ref name="Berdy"/>
 
Approximate number of bioactive microbial natural products (2002). According to their producers<ref name="Berdy"/>
 
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==={{Bilingual|高等生物の中では、植物と海綿類が生理活性物質を生産する。|In higher forms of life, most natural products are found in plants and sponges.}}===
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=={{Bilingual|高等生物の中では、植物と海綿類が生理活性物質を生産する。|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<ref name="Berdy"/>
 
Approximate numbers of bioactive natural products (2002). Derived from higher forms of life<ref name="Berdy"/>
 
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==={{Bilingual|微生物の中でも、生理活性物質を生産する種は限られる。|Most frequent producers are relatively limited.}}===
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=={{Bilingual|微生物の中でも、生理活性物質を生産する種は限られる。|Most frequent producers are relatively limited.}}==
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{{Twocolumn|
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;Exclusively fungi
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* All peptaibols (300-400), grisan and scirpene derivatives, cytochalasins (>100 each) are produced exclusively by fungi.
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* 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.
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|
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; 真菌類特有
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* 全てのペプタイボール (300-400), グリサンとシルペンの誘導体, シトカラシン (各 >100) は真菌由来。
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* 微小真菌類はしばしば、環の少ない(8-10)ラクトン環化合物 (-200), ジラクトンまたは縮合型マクロラクトン, マクロジオライド, アザフィロン, ジケトチアピペラジン, 小さいテルペノイドやベンゼン誘導体, α-ピロン, キサントン誘導体, 単純なベンゾキノン, ナフトキノンを合成する。
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}}
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{{Twocolumn|
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More than half of all bacterial metabolites are amino acid derivatives (e.g. peptides, peptolides, polypeptides).
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;Exclusively bacteria
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* cyclolipopeptides (polymyxins) and lantibiotics (nisin type) are exclusively produced by bacteria.
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|
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バクテリア由来の代謝物の半数以上が、アミノ酸誘導体である。
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; バクテリア特有
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* シクロリポペプチド (ポリミキシン)はバチラス等。
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* ランチ抗生物質はグラム陽性菌(Streptococcus and Streptomyces)由来。
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}}
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Approximate number of bioactive microbial metabolites according to their producers and bioactivities<ref name="Berdy"/>
 
Approximate number of bioactive microbial metabolites according to their producers and bioactivities<ref name="Berdy"/>
 
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==={{Bilingual|アクチノミセス目では、珍しい種が多くの変わった物質を生産する。|In actinomycetales, the rare actinos produce most diverse and unique compounds.}}===
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=={{Bilingual|放線菌類では、珍しい種が多くの変わった物質を生産する。|In actinomycetales, the rare actinos produce most diverse and unique compounds.}}==
  
 
{{Twocolumn|
 
{{Twocolumn|
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:: elfamycins, glutarimides, orthosomycins (50-60 each)
 
:: elfamycins, glutarimides, orthosomycins (50-60 each)
 
are produced exclusively by actinomycetales.
 
are produced exclusively by actinomycetales.
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|
 
|
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; 希少アクチノマイセス属特有
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; 希少アクチノマイセス（放線菌類）属特有
 
* 知られる全ての糖ペプチド抗生物質（およそ120)とほぼ全てのオルトソマイシンは、希少アクチノマイセス属由来。
 
* 知られる全ての糖ペプチド抗生物質（およそ120)とほぼ全てのオルトソマイシンは、希少アクチノマイセス属由来。
 
; アクチノマイセス目特有
 
; アクチノマイセス目特有

Latest revision as of 14:45, 6 June 2011


Contents

[edit] 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]
Antibiotic Activity (16500 compounds)
Antimicrobial activity
Antibacterial Gram-positive 11000-12000
Gram-negative 5000-5500
Mycobacteria 800-1000
Antifungal Yeasts 3000-3500
Phytopathogenic fungi 1600-1800
Other fungi 3800-4000
Antiprotozoal -1000
Chemotherapeutic activity
Antitumor (cytotoxic) 5000-5500
Antiviral 1500-1600
Other Bioactivities (11500 compounds)
Pharmacological activity
enzyme inhibitor 3000-3200
immunological activity (suppressive, modulatory) -800
biochemical activity (DNS, tubulin, mitotic etc.) -1000
2000-2500
Agricultural activity
pesticide (antiparasitic, algicide, amoebicide, etc.) 900-1000
herbicide (phytotoxic, plant growth regulatory, etc.) 1800-1900
insecticide/miticide/larvicide/deterrent 1100-1200
food additive, preservative 1100-1200
Other activities
microbial regulators (growth factors, microbial hormones, morphogens) -500
biophysical effects (surfactants, etc.) -300

[edit] 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

[edit] 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

[edit] 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.

[edit] 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

[edit] 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)
are produced exclusively by actinomycetales.

Number of actinomycetales species producing bioactive microbial metabolites[1]

Streptomycetaceae:
Streptomyces ca. 8000
Streptoverticillium 258
Kitasatosporia 37
Chainia 30
Microellobosporia 11
Nocardioides 9
Micromonosporaceae:
(Actinoplanetes)
Micromonospora 740
Actinoplanes 248
Dactylosporangium 58
Ampullariella 9
Glycomyces 2
Catenuloplanes 3
Catellatospora 1
Pseudonocardiaceae:
Saccharopolyspora 131
Amycalotopsis/Nocardia 120/357
Kibdellosporangium 34
Pseudonocardia 27
Amycolata 12
Saccharomonospora 2
Actinopolyspora 1
Streptosporangiaceae:
(Maduromycetes)
Streptosporangium 79
Streptoalloteichus 48
Spirillospora 11
Planobispora 10
Kutzneria 4
Planomonospora 2
Thermomonosporaceae:
Actinomadura 345
Saccharothrix 68
Microbispora 54
Actinosynnema 51
Nocardiopsis 41
Microtetraspora/Nonomuria 26/21
Thermomonospora 19
Micropolyspora/Faenia 13/3
Thermoactinomyces 14
Thermopolyspora 1
Thermoactinopolyspora 1
Mycobacteriaceae:
(Actinobacteria)
Nocardia (357)
Mycobacterium 57
Arthrobacter 25
Brevibacterium 17
Proactinomyces 14
Rhodococcus 13
Other (unclassified) species:
Actinosporangium 30
Microellobosporia 11
Frankia 7
Westerdykella 6
Kitasatoa 5
Synnenomyces 4
Sebekia 3
Elaktomyces 3
Excelsospora 3
Waksmania 3
Alkalomyces 1
Catellatospora 1
Erythrosporangium 1
Streptoplanospora 1
Microechinospora 1
Salinospora 1
  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 Berdy J (2005) "Bioactive Microbial Metabolites" J Antibiot 58(1):1-26
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