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枳实降脂等效组合成分。

The antihyperlipidemic equivalent combinatorial components from peel of Citrus reticulata 'Chachi'.

机构信息

State Key Laboratory of Natural Medicines, China Pharmaceutical University, No. 24 Tongjia Lane, Nanjing, China.

Academy of Chinese Medical Sciences, Henan University of Chinese Medicine, Zhengzhou, 450046, China.

出版信息

J Food Drug Anal. 2022 Mar 15;30(1):77-87. doi: 10.38212/2224-6614.3388.

DOI:10.38212/2224-6614.3388
PMID:35647727
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9930996/
Abstract

Since the combinatorial components responsible for the antihyperlipidemic activity of Citrus reticulata 'Chachi' (CRC) peels remains unclear, we herein developed a bioactive equivalence oriented feedback screening method to discover the bioactive equivalent combinatorial components (BECCs) from CRC peels. Using palmitic acid (PA)-stimulated hepatocyte model, a combination of 5 polymethoxyflavones (PMFs) including tangeretin, sinensetin, nobiletin, 5,7,8,4'-tetramethoxyflavone and 3,5,6,7,8,3',4'-heptamethoxyflavone was identified to be responsible for the antihyperlipidemic effect of CRC peels. Via evaluation of combination effect by combination index (CI), these 5 PMFs were found to take effect via a synergistic mode. Our data indicated that the antihyperlipidemic mechanism of PMF combination was associated with the inhibition of fatty acid and cholesterol synthesis, and inflammation. Also, the PMF combination exhibited robust antihyperlipidemic effects in HFD-fed rats in vivo. Our study offers evidence-based data to uncover the pharmacological effect of CRC peels.

摘要

由于负责枳实降脂活性的组合成分尚不清楚，我们在此开发了一种基于生物等效性导向的反馈筛选方法，从枳实皮中发现生物等效组合成分（BECCs）。使用棕榈酸（PA）刺激的肝细胞模型，鉴定出包括桔皮素、川陈皮素、诺必灵、5,7,8,4'-四甲氧基黄酮和 3,5,6,7,8,3',4'-七甲氧基黄酮在内的 5 种多甲氧基黄酮（PMFs）组合对枳实皮的降脂作用负责。通过组合指数（CI）评估组合效果，发现这 5 种 PMFs 以协同模式发挥作用。我们的数据表明，PMF 组合的降脂机制与抑制脂肪酸和胆固醇合成以及炎症有关。此外，PMF 组合在体内高脂饮食喂养的大鼠中表现出强大的降脂作用。本研究为揭示枳实皮的药理作用提供了循证数据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/bd489b80f376/jfda-30-77f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/8475d5fbaea6/jfda-30-77f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/338ce30e8dca/jfda-30-77f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/18a7364527e7/jfda-30-77f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/ca91f5d9c274/jfda-30-77f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/207244d8c49b/jfda-30-77f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/bd489b80f376/jfda-30-77f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/8475d5fbaea6/jfda-30-77f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/338ce30e8dca/jfda-30-77f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/18a7364527e7/jfda-30-77f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/ca91f5d9c274/jfda-30-77f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/207244d8c49b/jfda-30-77f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8c2/9930996/bd489b80f376/jfda-30-77f6.jpg

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