BCEF0083抗单胺氧化酶作用的研究

目的　研究一种白僵菌代谢产物提取物 (BCEF0 0 83)对单胺氧化酶 (MAO)的抑制作用。方法　提取动物脑组织重线粒体应用荧光分光光度计法检测MAO活性 ;采用大、小鼠体内外给药研究BCEF抗MAO作用的量效、时效关系 ,应用林 -贝氏法测定MAOKm值。结果　小鼠BCEF 50 0mg·kg- 1 ,ig给药后 0 5hMAO活性已有抑制 ,2～ 8h活性抑制明显 ,一次给药后 72h抑制作用基本消失 ;小鼠BCEF50 0、40 0、2 0 0、1 0 0、50、2 5mg·kg- 1 ,ig后 2h取脑组织测MAO活性 ,BCEF对MAO活性的抑制呈现一定的量效关系。BCEF体外给药对大鼠脑组织MAO活性的抑制随药物浓度增加而增强 ,BCEF体外给药对MAO A、MAO B抑制的IC50 (95 %可信限 )分别为 1 2 8 88(82 70～ 2 0 0 86)mg·L- 1 、1 84 1 4 (1 56 1 7～ 2 1 7 1 1 )mg·L- 1 ;BCEF对MAO A ,B抑制呈混合型抑制作用 ,Km值分别为 1 1 97、 8 1 3μmol·L- 1 。结论　BCEF0 0 83体内外给药对大、小鼠脑组织MAO活性具有抑制作用

Inhibition of Bioactive compounds from entomogenous fungi on monoamine oxidase

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) μg·ml -1 in rats. The antagonism type of BCEF0083 on MAOA, B were both mixed type, their Km were 11 97, 8 13 μmol·L -1 . CONCLUSION The results suggest that BCEF0083 could obviously inhibite the activity of MAO on brain remitochondria in mice and rats.