SF2809 compounds, novel chymase inhibitors from Dactylosporangium sp. 1. Taxonomy, fermentation, isolation and biological properties.
Six novel chymase inhibitors, SF2809-I, SF2809-II, SF2809-III, SF2809-IV, SF2809-V and SF2809-VI, were isolated from the fermentation broth of an actinomycete strain SF2809. The strain was identified as Dactylosporangium sp. by morphological, chemotaxonomical and phylogenetic studies. These six novel compounds inhibited recombinant human chymase in the range between IC50 of 0.014 and 7.3 microM. However, they showed little or no inhibitory activity against chymotrypsin or cathepsin G, even though these two and chymase belong to the chymotryptic serine protease family. This result indicates that these compounds work as specific chymase inhibitors.
Tani
Masato
M
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd. Morooka-Cho 760, Kohoku-Ku, Yokohama 222-8567, Japan. masato_tani@meiji.co.jp
Gyobu
Yasuhiro
Y
Sasaki
Toru
T
Takenouchi
Osami
O
Kawamura
Takashi
T
Kamimura
Takashi
T
Harada
Toshiaki
T
D039903:Actinobacteria / Q000737:chemistry* / Q000145:classification / Q000378:metabolism; D050260:Carbohydrate Metabolism; D053818:Chymases; D005285:Fermentation; D006801:Humans; D007211:Indoles / Q000302:isolation & purification / Q000494:pharmacology*; D008855:Microscopy, Electron, Scanning; D010802:Phylogeny; D015363:Quinolones / Q000302:isolation & purification / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000494:pharmacology*
D007211:Indoles; D015363:Quinolones; D011994:Recombinant Proteins; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053818:Chymases