SPF-32629 A and B, novel human chymase inhibitors produced by Penicillium sp.
Two new human chymase inhibitors, SPF-32629A and B, were isolated from the cultured broth of Penicillium sp. SPF-32629. These structures were determined by spectroscopic methods and identified as new pyridone compounds. SPF-32629B was the carboxylated derivative of SPF-32629A. SPF-32629A and B specifically inhibited human chymase among four serine proteases tested with the IC50 of 0.25 and 0.42 microg/ml, respectively.
Exploratory Research Group, Research Division, Sumitomo Pharmaceuticals Co., Ltd., 4-2-1 Takatsukasa, Takarazuka, Hyogo 665-0051, Japan. takuro-shimatani@ds-pharma.co.jp
Takuro
T
Shimatani
Nobuo
N
Hosotani
Masako
M
Ohnishi
Kazuo
K
Kumagai
Ikutaro
I
Saji
D000903:Antibiotics, Antineoplastic / Q000096:biosynthesis / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D053818:Chymases; D005285:Fermentation; D018922:HL-60 Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D009525:Niacin / Q000031:analogs & derivatives* / Q000737:chemistry; D010407:Penicillium / Q000145:classification / Q000378:metabolism*; D011480:Protease Inhibitors / Q000494:pharmacology*; D011728:Pyridones / Q000737:chemistry* / Q000494:pharmacology*; D012697:Serine Endopeptidases / Q000378:metabolism*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013056:Spectrophotometry, Ultraviolet
D000903:Antibiotics, Antineoplastic; D011480:Protease Inhibitors; D011728:Pyridones; C509636:SPF 32629 A; C509637:SPF 32629 B; D009525:Niacin; D012697:Serine Endopeptidases; D053818:Chymases