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印度南方黑姜(Curcuma caesia Roxb.)植物化学成分的药理学评价及其对癌症细胞凋亡的作用。

Pharmacological evaluation of phytochemicals from South Indian Black Turmeric (Curcuma caesia Roxb.) to target cancer apoptosis.

机构信息

Department of Biotechnology, Manipal Institute of Technology, Manipal University, Manipal, Karnataka 576104, India.

Parikshan, C-53, T.V.K. Industrial Estate, Guindy, Chennai, Tamil Nadu, India.

出版信息

J Ethnopharmacol. 2017 Sep 14;209:82-90. doi: 10.1016/j.jep.2017.07.021. Epub 2017 Jul 19.

Abstract

Curcuma caesia Roxb. (Black turmeric), a perennial herb of the family Zingiberaceae is indigenous to India. C. caesia is used as a spice, food preservative and coloring agent commonly in the Indian subcontinent. Functional parametric pharmacological evaluations like drug ability and toxicity profile of this endangered species is poorly documented. In our present study, among all the extracts of dried C. caesia rhizome viz- hexane, ethyl acetate, methanol and water tested for free radical scavenging capacity by total antioxidant activity (TAO) method, Hexane Rhizome Extract (HRE) was found to possess remarkable activity (1200mg ascorbic acid equivalent/100g). In MTT assay across three cancer cell lines and a control cell line, HRE exhibited a dose-dependent inhibition only in cancer cells, with notable activity in HepG2 cell lines (IC50: 0976µg/mL). Further, western blotting and flow cytometry experiments proved that HRE induces cell arrest at G2/M phase along with cellular apoptosis as suggestive by multiple-point mitochondrial mediated intrinsic pathway of Programmed Cell Death (PCD). Gas Chromatography-Mass Spectrophotometry (GC-MS) analysis of HRE suggested twenty compounds that when docked in silico with Tubulin (1SA0) and Epidermal Growth Factor Receptor/ EGFR (1XKK) showed very intimate binding with the original ligands. Our results provided significant evidence of the toxicity mechanisms of HRE that may be beneficial for more rational applications of drug discovery for slowing down cancer progression.

摘要

莪术(黑姜),姜科姜黄属的多年生草本植物,原产于印度。莪术在印度次大陆被用作香料、食品防腐剂和着色剂。这种濒危物种的功能参数药理学评价,如药物能力和毒性特征,记录很少。在我们目前的研究中,在对干燥莪术根茎的所有提取物(正己烷、乙酸乙酯、甲醇和水)进行总抗氧化活性(TAO)法测定自由基清除能力的测试中,发现正己烷根茎提取物(HRE)具有显著的活性(1200mg 抗坏血酸当量/100g)。在 MTT 测定中,在三种癌细胞系和一种对照细胞系中,HRE 仅在癌细胞中表现出剂量依赖性抑制,在 HepG2 细胞系中表现出显著的活性(IC50:0976µg/mL)。此外,Western blot 和流式细胞术实验证明,HRE 诱导细胞在 G2/M 期停滞,并通过程序性细胞死亡(PCD)的多点线粒体内在途径诱导细胞凋亡。HRE 的气相色谱-质谱分析(GC-MS)表明,有二十种化合物,当在计算机中与微管蛋白(1SA0)和表皮生长因子受体/EGFR(1XKK)对接时,与原始配体表现出非常密切的结合。我们的结果提供了 HRE 毒性机制的重要证据,这可能有助于更合理地应用药物发现来减缓癌症的进展。

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