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水果的化学标准化和抗增殖活性对 HCT116 人结肠癌细胞系的影响。

Chemical Standardization and Anti-Proliferative Activity of Fruit against the HCT116 Human Colon Cancer Cell Line.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.

Department of Pharmacognosy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.

出版信息

Molecules. 2020 Feb 25;25(5):1023. doi: 10.3390/molecules25051023.

Abstract

The present study is intended to carry out the chemical standardization and evaluation of the anti-proliferative activity of fruit extract. fruit powder was extracted with ethanol. The obtained extract was assessed for total phenolic content using the Folin-Ciocalteu method. Moreover, a simple, accurate, and precise reversed phase high-performance liquid chromatographic method was developed and validated to determine the embelin content of fruit extract. Then, the extract and embelin were investigated for their anti-proliferative effect against HCT-116 cells. Finally, the mechanisms of inhibition of the extract and embelin on the mRNA expression of pro-apoptotic genes Bad, Bax, and Caspase-8 and anti-apoptotic genes c-IAP1, Mcl-1, and XIAP were determined by real-time qRT-PCR. The phenolic content and embelin content of the extract were 5.20 ± 0.01 g of gallic acid equivalent per 100 g of dried fruit (g% GAE) and 5.57 ± 0.56 mg/g of extract, respectively. The extract and embelin showed strong anti-proliferative effects on HCT-116 cells with 50% inhibition concentration (IC) values of 19.16 ± 1.09 µg/mL and 25.93 ± 1.75 µg/mL, respectively. The extract exhibited a significant increase in the mRNA level of Bad, Bax, and Caspase-8 and a significant decrease in c-IAP1, Mcl-1, and XIAP. Embelin showed a significant decrease in Mcl-1 and XIAP.

摘要

本研究旨在对 果实提取物进行化学标准化和抗增殖活性评价。采用乙醇提取 果实粉末。采用福林-肖卡法测定提取物总酚含量。此外,还开发并验证了一种简单、准确、精密的反相高效液相色谱法,用于测定 果实提取物中埃贝利宁的含量。然后,研究了提取物和埃贝利宁对 HCT-116 细胞的抗增殖作用。最后,通过实时 qRT-PCR 确定了提取物和埃贝利宁对促凋亡基因 Bad、Bax 和 Caspase-8 及抗凋亡基因 c-IAP1、Mcl-1 和 XIAP 的 mRNA 表达的抑制机制。提取物的酚含量和埃贝利宁含量分别为 5.20 ± 0.01 g 没食子酸当量/100 g 干果实(g% GAE)和 5.57 ± 0.56 mg/g 提取物。提取物和埃贝利宁对 HCT-116 细胞均表现出较强的抗增殖作用,其 50%抑制浓度(IC)值分别为 19.16 ± 1.09 µg/mL 和 25.93 ± 1.75 µg/mL。提取物显著增加了 Bad、Bax 和 Caspase-8 的 mRNA 水平,同时显著降低了 c-IAP1、Mcl-1 和 XIAP。埃贝利宁显著降低了 Mcl-1 和 XIAP。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1165/7179138/6e2e0b257430/molecules-25-01023-g001.jpg

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