| 引用本文： |
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李子达,张月华,黄健军,蒋才武.6种中药单体脂肪酶抑制活性及其作用机制[J].广西科学,2019,26(5):555-559. [点击复制]
- LI Zida,ZHANG Yuehua,HUANG Jianjun,JIANG Caiwu.Study on lipase inhibitory activity and mechanisms of six kinds of Chinese medicine monomers[J].Guangxi Sciences,2019,26(5):555-559. [点击复制]
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| 摘要: |
| 筛选具有胰脂肪酶抑制活性的中药有效成分，明确其作用机制。以文献报道的有减肥降脂作用的6种中药单体化合物（熊果酸、齐墩果酸、姜黄素、大黄酸、芒果苷和二氢杨梅素）为筛选对象，以市售减肥样品奥利司他为阳性对照品，采用对硝基苯酚法通过测定反应体系在405 nm下的吸光度数值来测算出其对胰脂肪酶的抑制率。同时测定抑制作用最强姜黄素的3种主要分解产物（反式阿魏酸、香草酸、香草醛）对胰脂肪酶的抑制率。结果显示：奥利司他、黄素和熊果酸的半数抑制浓度（IC50）依次是0.95 μmol/L、27 μmol/L和100 μmol/L，黄素和熊果酸的抑制作用机理都是通过抑制剂和酶的相互作用，阻碍酶和底物的作用，属于非竞争性抑制。齐墩果酸和双氢杨梅素的最大抑制率是（27.45±0.04）%和23.76%，其余样品的最大抑制率均少于10%；姜黄素和熊果酸具有显著的胰脂肪酶抑制作用，其抑制作用机理属于非竞争性抑制，齐墩果酸和双氢杨梅素有一定脂肪酶抑制作用，其余单体及姜黄素分解产物均无明显脂肪酶抑制作用。 |
| 关键词: 熊果酸 姜黄素 脂肪酶 奥利司他 对硝基苯酚法 半数抑制浓度 |
| DOI：10.13656/j.cnki.gxkx.20191024.008 |
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| 基金项目:省部共建药用资源化学与药物分子工程国家重点实验室课题（CMEMR2017-B18）和广西人文社科重点研究基地-特色养老与养生产业发展研究中心项目（05J1402703）资助。 |
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| Study on lipase inhibitory activity and mechanisms of six kinds of Chinese medicine monomers |
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LI Zida, ZHANG Yuehua, HUANG Jianjun, JIANG Caiwu
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| (Pharmaceutical College, Guangxi University of Traditional Chinese Medicine, Nanning, Guangxi, 530200, China) |
| Abstract: |
| The effective components of traditional Chinese medicine with pancreatic lipase inhibitory activity were screened,and the mechanism of action was clarified and confirmed.Six kinds of traditional Chinese medicine monomer compounds (ursolic acid,oleanolic acid,curcumin,rhein,mangiferin and dihydromyricetin) with weight loss and lipid-lowering effects reported in the literature were selected as objects,and the commercially available weight-loss drug orlistat was been selected as positive control,the inhibition rate of pancreatic lipase was determined by measuring the absorbance of the reaction system at 405 nm by the p-nitrophenol method.At the same time,the inhibition rate of pancreatic lipase was determined by the three major decomposition products of curcumin (trans-ferulic acid,vanillic acid,vanillin).The half-inhibitory concentration (IC50) of orlistat,curcumin and ursolic acid was 0.95 μmol/L,27 μmol/L and 100 μmol/L,respectively.The inhibition mechanisms of curcumin and ursolic acidare were mainly through the interaction of inhibitors and enzymes,blocking the action of enzymes and substrate,which was non-competitive inhibition.The maximum inhibition rates of oleanolic acid and dihydromyricetin were (27.45±0.04)% and 23.76%,and the maximum inhibition rates of other samples were all less than 10%.Curcumin and ursolic acid had significant inhibition of pancreatic lipase.The mechanism of inhibition was non-competitive inhibition.Oleanolic acid and dihydromyricetin had certain lipase inhibition effects,and the other monomers and curcumin decomposition products had no obvious lipase inhibition. |
| Key words: ursolic acid curcumin lipase orlistat p-nitrophenol method half-inhibitory concentration |
