COMPLEX-I AND COMPLEX-III OF MITOCHONDRIA HAVE COMMON INHIBITORS ACTING AS UBIQUINONE ANTAGONISTS
COMPLEX-I AND COMPLEX-III OF MITOCHONDRIA HAVE COMMON INHIBITORS ACTING AS UBIQUINONE ANTAGONISTS
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DOI：
10.1006/bbrc.1993.1161
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发表时间：
1993-02-15
影响因子：
3.1
通讯作者：
LENAZ, G
中科院分区：
文献类型：
--
作者：
ESPOSTI, MD;GHELLI, A;LENAZ, G
线粒体复合物I和复合物III具有泛醌样结构的共同抑制剂。十三烷基类似物的stigmatellin，抑制线粒体复合物III在纳摩尔浓度，也抑制NADH：泛醌还原酶活性的复合物I在微摩尔浓度。抑制剂滴度取决于线粒体颗粒的浓度，并在零颗粒浓度下外推至0.2 μM。该化合物与外源性泛醌、鱼藤酮和piericidin.Myxothiazol相比，具有更强的抑制作用，其效价与stigmatellin的十三烷基类似物相当。此外，piericidin，这是最强大的抑制剂的复合物I，抑制泛醇：细胞色素还原酶活性的复合物III在微摩尔浓度在线粒体颗粒和atsubmicromolar浓度在分离的酶复合物。
Mitochondrial complex I and complex III have common inhibitors with ubiquinone-like structure. The tridecyl analog of stigmatellin, which inhibits mitochondrial complex III at nanomolar concentrations, also inhibits the NADH: ubiquinone reductase activity of complex I at micromolar concentrations. The inhibitor titer depends upon the concentration of the mitochondrial particles and extrapolates to 0.2 μM at zero particle concentration. The stigmatellin analog is more powerful than its parent compound and is noncompetitive with exogenous ubiquinone, rotenone and piericidin.Myxothiazol, which is another potent inhibitor of complex III, is also found to inhibit the activity of complex I with a titer comparable to that of the tridecyl analog of stigmatellin. Additionally, piericidin, which is the most powerful inhibitor of complex I, inhibits the ubiquinol: cytochromecreductase activity of complex III at micromolar concentrations in mitochondrial particles and atsubmicromolar concentrations in the isolated enzyme complex.