Inhibition of adipocyte lipolysis by papaverine: papaverine can inhibit the redistribution of hormone-sensitive lipase.
Inhibition of adipocyte lipolysis by papaverine: papaverine can inhibit the redistribution of hormone-sensitive lipase.
复制标题
罂粟碱抑制脂肪细胞脂肪分解：罂粟碱可抑制激素敏感脂肪酶的再分布。
DOI：
10.1016/s0024-3205(00)80012-0
复制
发表时间：
2000
期刊：
影响因子：
6.1
通讯作者：
Hideki Ohno
中科院分区：
文献类型：
--
作者：
Tetsuya Izawa;Sachiko Nomura;T. Kizaki;S. Oh;T. Ookawara;Hideki Ohno
罂粟碱，尽管是一种有效的磷酸二酯酶抑制剂，实际上阻止脂肪细胞脂解。本研究旨在阐明罂粟碱抑制脂肪分解的作用机制。罂粟碱（100 μM及以上）显著抑制10 μM异丙肾上腺素或5 mM双丁酰cAMP刺激的脂解。罂粟碱，但是，不影响异丙肾上腺素诱导的蛋白激酶A（A-激酶）活性比的增加。在非刺激的脂肪细胞的无细胞提取物中，cAMP刺激的A-激酶活性几乎完全被H-89（一种有效的A-激酶抑制剂）阻断，但不被罂粟碱阻断。因此，罂粟碱对脂解的抑制作用可能是导致A-激酶活性远端步骤缺陷的原因。激素敏感的脂肪酶活性的infranatant部分的离心匀浆的细胞，这是最大限度地刺激异丙肾上腺素，显着减少。这一结果表明，在脂解刺激的细胞中，对脂肪酸敏感的脂肪酶从胞质溶胶重新分配到其底物。罂粟碱完全阻断了异丙肾上腺素诱导的脂肪酶活性下降的infranatant馏分。这些结果表明，罂粟碱阻断脂解通过其抑制作用的再分配的酶敏感的脂肪酶。
Papaverine, despite being a potent phosodiesterase inhibitor, actually blocks adipocyte lipolysis. The present study was designed to clarify the mechanism of the inhibitory effect of papaverine on lipolysis. Lipolysis, stimulated by either 10 μM isoproterenol or 5 mM dibutyryl cAMP, was significantly inhibited by papaverine (100 μM and above). Papaverine, however, did not affect the isoproterenol-induced increase in the protein kinase A (A-kinase) activity ratio. In cell-free extract from non-stimulated adipocytes, cAMP-stimulated A-kinase activities were almost completely blocked by H-89, a potent inhibitor of A-kinase, but not by papaverine. Thus, the inhibitory effect of papaverine on lipolysis could be responsible for a deficit in step(s) distal to A-kinase activity. Hormone-sensitive lipase activities in the infranatant fraction of centrifuged homogenates of cells, which were maximally stimulated with isoproterenol, were significantly reduced. This result indicates that hormone-sensitive lipase redistributes from cytosol to its substrate in lipolytically stimulated cells. Papaverine completely blocked the isoproterenol-induced decrease in lipase activity in the infranatant fraction. These results suggest that papaverine blocks lipolysis through its inhibitory effect on the redistribution of hormone-sensitive lipase.
脂肪分解刺激调节 3T3-L1 细胞中激素敏感性脂肪酶的亚细胞分布。
影响因子：
6.5
作者：
Hirsch,AH;Rosen,OM
通讯作者：
Rosen,OM