Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.
Department of Pharmacognosy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.
Molecules. 2020 Feb 25;25(5):1023. doi: 10.3390/molecules25051023.
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.
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。