不同采收期陈皮中脂肪酶抑制活性与生物活性类黄酮的评价
Evaluation of anti-lipase activity and bioactive flavonoids in the Citri Reticulatae Pericarpium from different harvest time.
机构信息
State Key Laboratory of Natural Medicines, China Pharmaceutical University, No. 24 Tongjia Lane, Nanjing 210009, PR China.
National Resource Center for Chinese Materia Medica, China Academy of Chinese Medical Sciences, State Key Laboratory Breeding Base of Dao-di Herbs, Beijing, 100700, PR China.
出版信息
Phytomedicine. 2018 Apr 1;43:103-109. doi: 10.1016/j.phymed.2018.04.008. Epub 2018 Apr 7.
BACKGROUND
Inhibition of pancreatic lipase is an attractive approach to the treatment of obesity and other metabolic disorders. Naturally occurring phytochemicals are promising sources of lipase inhibitors.
PURPOSE
In the present study, the anti-lipase activity of Citri Reticulatae Pericarpium (CRP) extracts was firstly evaluated in vitro. Moreover, the dynamic alteration of bioactive flavonoids in CRP collected at different time and its correlation with anti-lipase activities was investigated.
STUDY DESIGN/METHODS: Quantitative analysis of multi-components by a single-marker (QAMS) method was developed and validated for simultaneous determination of six flavonoids including narirutin, hesperidin, didymin, nobiletin, 3,5,6,7,8,3',4'-heptamethoxyflavone and tangeretin. Anti-lipase activity evaluation and docking studies of the flavonoids was also carried out to screen out the candidate lipase inhibitors.
RESULTS
The QAMS method validation results exhibited that the developed method had desirable specificity, linearity, precision and accuracy. CRP collected in early months contained higher concentrations of bioactive flavonoids, and exhibited more potent anti-lipase activity.
CONCLUSION
Harvest timing had a significant impact on the amounts of bioactive flavonoids and the anti-lipase activities of CRP extracts. The contents of total flavonoids were positively correlated with the anti-lipase activities of CRP, and polymethoxyflavones played a significant role in the hypolipidemic effect of CRP. Nobiletin might be the most potential lipase inhibitor in CRP.
背景
抑制胰脂肪酶是治疗肥胖症和其他代谢紊乱的一种有吸引力的方法。天然存在的植物化学物质是潜在的脂肪酶抑制剂来源。
目的
本研究首次评估了陈皮提取物（CRP）的抗脂肪酶活性。此外，还研究了不同时间采集的 CRP 中生物活性类黄酮的动态变化及其与抗脂肪酶活性的相关性。
研究设计/方法：建立并验证了一种基于单标志物的多成分定量分析（QAMS）方法，用于同时测定包括柚皮苷、橙皮苷、二氢川陈皮素、诺必林、3,5,6,7,8,3',4'-七甲氧基黄酮和橘红素在内的六种黄酮类化合物。还进行了抗脂肪酶活性评价和黄酮类化合物的对接研究，以筛选出候选的脂肪酶抑制剂。
结果
QAMS 方法验证结果表明，所建立的方法具有良好的专属性、线性、精密度和准确度。早期月份采集的 CRP 含有更高浓度的生物活性类黄酮，表现出更强的抗脂肪酶活性。
结论
收获时间对 CRP 中生物活性类黄酮的含量和抗脂肪酶活性有显著影响。总黄酮含量与 CRP 的抗脂肪酶活性呈正相关，多甲氧基黄酮在 CRP 的降血脂作用中起重要作用。诺必林可能是 CRP 中最有潜力的脂肪酶抑制剂。
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