Isolation and biological activity of thielocins: novel phospholipase A2 inhibitors produced by Thielavia terricola RF-143.
Thielocins A2 alpha, A2 beta, A3, B1, B2 and B3 were isolated as a novel family of phospholipase A2 inhibitors from the fermentation broth of Thielavia terricola RF-143 together with thielavins and thielocins A1 alpha and A1 beta. The most potent inhibitory activity (IC50 = 0.0033 microM) against rat group II phospholipase A2 was shown by thielocin A1 beta. Against human group II phospholipase A2, thielocin B3 (IC50 = 0.076 microM) was the most potent.
Matsumoto
K
K
Shinogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan.
Tanaka
K
K
Matsutani
S
S
Sakazaki
R
R
Hinoo
H
H
Uotani
N
N
Tanimoto
T
T
Kawamura
Y
Y
Nakamoto
S
S
Yoshida
T
T
D000818:Animals; D001203:Ascomycota / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D002852:Chromatography, Ion Exchange; D005285:Fermentation; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010741:Phospholipases A / Q000037:antagonists & inhibitors*; D054467:Phospholipases A2; D051381:Rats; D014966:Xanthenes / Q000302:isolation & purification* / Q000494:pharmacology
D014966:Xanthenes; D010741:Phospholipases A; D054467:Phospholipases A2