靛蓝叶猪屎豆中的紫檀素靛蓝果紫檀的抗氧化和抗增殖活性。

Antioxidant and antiproliferative activity of indigocarpan, a pterocarpan from Indigofera aspalathoides.

作者信息

Mahajan Pravin, Gnana Oli Rajaraman, Jachak Sanjay M, Bharate Sandip B, Chaudhuri Bhabatosh

机构信息

Leicester School of Pharmacy, De Montfort University, Leicester, UK.

Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Mohali, India.

出版信息

J Pharm Pharmacol. 2016 Oct;68(10):1331-9. doi: 10.1111/jphp.12609. Epub 2016 Jul 27.

DOI:10.1111/jphp.12609

PMID:27464528

Abstract

OBJECTIVES

This study aimed to investigate the anticancer potential of indigocarpan (1), a pterocarpan isolated from Indigofera aspalathoides, a plant found in India which has been used in Ayurveda for centuries for the treatment of oedematous tumours.

METHODS

The antiproliferative activity in a panel of four human cancer cell lines was studied. The mechanism of its antiproliferative activity in human colorectal adenocarcinoma LS174T cells was investigated in detail.

KEY FINDINGS

Indigocarpan (1) showed antiproliferative activity in a panel of four human cancer cell lines with IC50 s ranging from 180 to 250 μm. Indigocarpan induces p53-dependent p21 upregulation and apoptosis in LS174T cells, upregulates p53 and p21(WAF1) protein levels, enhances cleavage of caspase-3 and downregulates cyclin D1, cyclin B1 and PCNA protein levels, indicating its role in modulating cell cycle progression. Indigocarpan also exhibited a strong antioxidative effect in LS174T cells.

CONCLUSIONS

Along with the antiproliferative capacity, the strong antioxidative property of the compound makes it a promising candidate for further development as an anticancer and chemopreventive compound.

摘要

目的

本研究旨在探究靛紫檀（1）的抗癌潜力。靛紫檀是从印度发现的植物阿斯巴甜木蓝中分离得到的一种紫檀素，几个世纪以来，印度阿育吠陀医学一直使用该植物治疗水肿性肿瘤。

方法

研究了其在四种人类癌细胞系中的抗增殖活性。详细研究了其在人结肠腺癌LS174T细胞中抗增殖活性的机制。

主要发现

靛紫檀（1）在四种人类癌细胞系中显示出抗增殖活性，IC50范围为180至250μm。靛紫檀在LS174T细胞中诱导p53依赖性p21上调和凋亡，上调p53和p21（WAF1）蛋白水平，增强caspase-3的裂解，并下调细胞周期蛋白D1、细胞周期蛋白B1和PCNA蛋白水平，表明其在调节细胞周期进程中的作用。靛紫檀在LS174T细胞中也表现出很强的抗氧化作用。