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姜科生药中PGC-1α激活成分的鉴定

Identification of PGC-1α activating constituents in Zingiberaceous crude drugs.

作者信息

Nishidono Yuto, Fujita Takashi, Kawanami Akira, Nishizawa Mikio, Tanaka Ken

机构信息

College of Pharmaceutical Science, Ritsumeikan University, 1-1-1 Noji-Higashi, Kusatsu, Shiga 525-8577, Japan.

Sumitomo Chemical Asia PTE Ltd., 150 Beach Road, #17-07 Gateway West, 189720, Singapore.

出版信息

Fitoterapia. 2017 Oct;122:40-44. doi: 10.1016/j.fitote.2017.08.007. Epub 2017 Aug 18.

Abstract

The activity of Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α) as an index of thermogenesis induced by four Indonesian Zingiberaceous crude drugs, Boesenbergia rotunda, Curcuma longa, Kaempferia galanga, Zingiber montanum, was examined, and GC-MS analyses of extracts of these drugs were performed. The results showed that activation of PGC-1α by K. galanga was high, whereas no activation was shown for the other drugs. Ethyl p-methoxycinnamate and ethyl cinnamate were identified as the PGC-1α activating compounds of K. galanga. Furthermore, study on the structure-activity relationship revealed that ethyl p-methoxycinnamate has the strongest activity among the cinnamic acid derivatives. This suggests that the ester structure and the methoxy group are important factors responsible for the PGC-1α activity.

摘要

研究了四种印度尼西亚姜科生药莪术、姜黄、山奈、高良姜诱导产热作用的指标——过氧化物酶体增殖物激活受体γ共激活因子1α(PGC-1α)的活性,并对这些药物的提取物进行了气相色谱-质谱(GC-MS)分析。结果表明,山奈对PGC-1α的激活作用较高,而其他药物未显示出激活作用。对甲氧基肉桂酸乙酯和肉桂酸乙酯被鉴定为山奈的PGC-1α激活化合物。此外,构效关系研究表明,对甲氧基肉桂酸乙酯在肉桂酸衍生物中具有最强的活性。这表明酯结构和甲氧基是影响PGC-1α活性的重要因素。

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