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水飞蓟宾二半琥珀酸酯对大鼠肝脏脂肪酸合成的影响(作者译)

[Influence of Silybin-dihemisuccinate on fatty acid synthesis in rat liver (author's transl)].

作者信息

Schriewer H, Krämer U, Rutkowski G, Borgis K J

出版信息

Arzneimittelforschung. 1979;29(3):524-6.

PMID:39576
Abstract
  1. The influence of silybin-dihemisuccinate, a derivative of the flavonolignane silybin from silybum marianum L. Gaertn., on fatty acid biosynthesis of rat liver was studied measuring the radioactivity incorporation of [1-14C]-acetate and 3H2O in fatty acids of the postmitochondrial supernatant of liver homogenates and in fatty acids of liver slices as well as the activities of enzymes involved in do novo synthesis of fatty acids. 2. In the postmitochondrial supernatant of liver homogenates or in liver slices, prepared 30 or 60 min after i.v. injection of 150.6 mg/kg silybin-dihemisuccinate, radioactivity incorporation of 14C-acetate or 3H2O in fatty acids was lowered by about 25%. Adding silybin-dihemisuccinate to incubation mixture in vitro in the concentration of 0.45--0.6 mmol/l silybin the radioactivity incorporation was linearly diminished with increased concentration of silybin. 3. After in vitro addition of varying concentrations of silybin to incubation mixtures in the presence of 0.1 mmol/l silybin activities of acetyl-CoA-carboxylase, fatty-acid-synthetase and ATP-citrate-lyase were diminished by about 50%, while activity of NADP-malate-dehydrogenase was lowered by 20% in the presence of 1 mmol/l silybin. 4. Our results suggest that silybin caused an unspecific and, under in vivo conditions, transitory inhibition of fatty acid synthesis in rat liver.
摘要
  1. 研究了水飞蓟宾二半琥珀酸酯(水飞蓟宾的黄酮木脂素衍生物,水飞蓟宾来自水飞蓟)对大鼠肝脏脂肪酸生物合成的影响,通过测量[1-14C]-乙酸盐和3H2O在肝脏匀浆线粒体后上清液脂肪酸以及肝切片脂肪酸中的放射性掺入情况,以及参与脂肪酸从头合成的酶的活性。2. 在静脉注射150.6mg/kg水飞蓟宾二半琥珀酸酯30或60分钟后制备的肝脏匀浆线粒体后上清液或肝切片中,14C-乙酸盐或3H2O在脂肪酸中的放射性掺入降低了约25%。在体外孵育混合物中添加浓度为0.45--0.6mmol/l水飞蓟宾的水飞蓟宾二半琥珀酸酯,放射性掺入随水飞蓟宾浓度增加呈线性降低。3. 在体外向孵育混合物中添加不同浓度水飞蓟宾,在存在0.1mmol/l水飞蓟宾的情况下,乙酰辅酶A羧化酶、脂肪酸合成酶和ATP柠檬酸裂解酶的活性降低了约50%,而在存在1mmol/l水飞蓟宾的情况下,NADP苹果酸脱氢酶的活性降低了20%。4. 我们的结果表明,水飞蓟宾在体内条件下对大鼠肝脏脂肪酸合成造成了非特异性的、短暂的抑制。

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