title: SF2809 compounds, novel chymase inhibitors from Dactylosporangium sp. 1. Taxonomy, fermentation, isolation and biological properties.
abstract: 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.
authors.affiliation: Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd. Morooka-Cho 760, Kohoku-Ku, Yokohama 222-8567, Japan. masato_tani@meiji.co.jp
authors.forename: Masato
authors.initials: M
authors.lastname: Tani
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Gyobu
authors.forename: Toru
authors.initials: T
authors.lastname: Sasaki
authors.forename: Osami
authors.initials: O
authors.lastname: Takenouchi
authors.forename: Takashi
authors.initials: T
authors.lastname: Kawamura
authors.forename: Takashi
authors.initials: T
authors.lastname: Kamimura
authors.forename: Toshiaki
authors.initials: T
authors.lastname: Harada
mesh_terms: 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*
chemical_list: D007211:Indoles; D015363:Quinolones; D011994:Recombinant Proteins; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053818:Chymases