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海桐花多靶点潜力研究:HPLC-ESI-MS 分析、计算机对接、DNA 保护、抗菌、酶抑制、抗癌和凋亡活性。

Multi-targeted potential of Pittosporum senacia Putt.: HPLC-ESI-MS analysis, in silico docking, DNA protection, antimicrobial, enzyme inhibition, anti-cancer and apoptotic activity.

机构信息

Department of Health Sciences, Faculty of Science, University of Mauritius, 230 Réduit, Mauritius.

Department of Economics and Statistics, Faculty of Social Studies & Humanities, University of Mauritius, Réduit, Mauritius.

出版信息

Comput Biol Chem. 2019 Dec;83:107114. doi: 10.1016/j.compbiolchem.2019.107114. Epub 2019 Aug 29.

Abstract

Pittosporum senacia (PS) Putt. (Pittosporaceae), indigenous to the Mascarene Islands, is a common ingredient in traditional medicines. However, there is currently a dearth of studies to validate some of these traditional claims. Given the broad traditional uses of PS against several diseases, we aimed to provide a comprehensive insight into the biological and chemical profile of P. senacia. The antioxidant, enzyme inhibitory activity, anticancer, and phytochemical composition of the methanolic extract of P. senacia leaf extracts were studied. The possible interaction and binding mode of the most abundant phytochemicals were studied via in silico docking experiments on tyrosinase and α-glucosidase. The mechanism behind the cytotoxic property of P. senacia extract for MDA-MB-231 was also examined using different methods including 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cell viability test checking apoptosis-associated genes, and wound healing assays. Twenty-six compounds were identified, of which caffeoylquinic acid derivatives, ferulic acid derivative, cinnamoylquinic acid derivative and two other polyphenols (oleuropeine and isoramnetin glucoside) being abundant, have been tested using in silico studies, against α-glucosidase and tyrosinase. The extract (IC = 118.8 μg/ml) exhibited time and dose dependent anti-proliferative effect on human breast cancer cell line, MDA-MB-231. According to the expression profile of apoptosis inhibitors and apoptosis promoters genes, expression of Bax and Bak genes were significantly increased compared to Bcl-2 and Birc5 genes. Based on wound healing analysis, cell migration was inhibited after the application of the plant extract. The present findings suggested that PS might be a good candidate as sources of bioactive compounds for designing functional applications.

摘要

马岛相思树(PS)Putt.(海桐科)原产于马斯克林群岛,是传统药物中的常见成分。然而,目前缺乏一些传统说法的验证研究。鉴于 PS 在多种疾病方面的广泛传统用途,我们旨在全面了解马岛相思树的生物和化学成分概况。研究了马岛相思树叶提取物的甲醇提取物的抗氧化、酶抑制活性、抗癌和植物化学成分。通过对酪氨酸酶和α-葡萄糖苷酶进行计算机对接实验,研究了最丰富的植物化学成分的可能相互作用和结合模式。还使用不同的方法,包括 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴盐 (MTT) 细胞活力试验检查与细胞凋亡相关的基因,以及划痕愈合试验,研究了马岛相思树提取物对 MDA-MB-231 的细胞毒性作用的机制。鉴定出了 26 种化合物,其中含有丰富的绿原酸衍生物、阿魏酸衍生物、肉桂酰奎宁酸衍生物和另外两种多酚(橄榄苦苷和异槲皮苷),这些化合物已通过计算机研究进行了测试,针对α-葡萄糖苷酶和酪氨酸酶。提取物(IC=118.8μg/ml)对人乳腺癌细胞系 MDA-MB-231 表现出时间和剂量依赖性的抗增殖作用。根据凋亡抑制剂和凋亡促进剂基因的表达谱,与 Bcl-2 和 Birc5 基因相比,Bax 和 Bak 基因的表达明显增加。基于划痕愈合分析,在应用植物提取物后,细胞迁移受到抑制。研究结果表明,PS 可能是设计功能性应用的生物活性化合物的良好候选物。

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