Inhibition of Bioactive compounds from entomogenous fungi on monoamine oxidase / 中国药理学通报

ABSTRACT

AIM To study the inhibitory effect of bioactive compounds from entomogenous fungi(BCEF0083) on monoamine oxidase. METHODS Spectrofluorometer was used to detect the activity of MAO in mouse and rat brain mitochondria; Dose effect and time effect relationship of BCEF in inhibition of MAO were studied in vivo and in vitro in mice and rats; Method of Lineweaver Burk was used to assay the Km of MAO. RESULTS The antagoning action of BCEF0083 on MAO( BCEF 500 mg?kg -1 , 0 5, 1, 2, 4, 8, 16, 24, 48, 72 h after ig; 500, 400, 200, 100, 50, 25 mg?kg -1 , 2 h after ig)showed some extent of dose effect and time effect relationship. BCEF0083 in vitro inhibited the activity of MAO A,B in a dose dependent manner with IC 50 (95% of confidence limits)of 128 88(82 70～200 86),184 14(156 17～217 11) ?g?ml -1 in rats. The antagonism type of BCEF0083 on MAOA, B were both mixed type, their Km were 11 97, 8 13 ?mol?L -1 . CONCLUSION The results suggest that BCEF0083 could obviously inhibite the activity of MAO on brain remitochondria in mice and rats.