Scyphostatin, a neutral sphingomyelinase inhibitor from a discomycete, Trichopeziza mollissima: taxonomy of the producing organism, fermentation, isolation, and physico-chemical properties.
We performed experiments to screen for neutral sphingomyelinase inhibitors using rat brain microsomes as an enzyme source. Among more than 10,000 microbial extracts tested, a mycelial extract of Trichopeziza mollissima SANK 13892 exhibited potent inhibitory activity. The active compound, scyphostatin, was purified by a series of chromatographies. Scyphostatin inhibited the enzyme with an IC50 value of 1.0 microM.
Nara
F
F
Biological Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Tanaka
M
M
Hosoya
T
T
Suzuki-Konagai
K
K
Ogita
T
T
D000577:Amides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D000818:Animals; D001203:Ascomycota / Q000145:classification / Q000378:metabolism*; D001921:Brain / Q000648:ultrastructure; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D005285:Fermentation; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008861:Microsomes / Q000201:enzymology; D011753:Pyrones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013108:Sphingomyelin Phosphodiesterase / Q000037:antagonists & inhibitors*
D000577:Amides; D004791:Enzyme Inhibitors; D011753:Pyrones; C121123:scyphostatin; D013108:Sphingomyelin Phosphodiesterase