University Department of Biochemistry, L.I.T. Premises, R.T.M. Nagpur University, Nagpur 440 033, Maharashtra, India.
J Ethnopharmacol. 2012 Jun 14;141(3):989-96. doi: 10.1016/j.jep.2012.03.044. Epub 2012 Mar 30.
Cissus quadrangularis is an ancient medicinal plant. It is an active ingredient of one Ayurvedic formula called "Laksha Gogglu". Its stem is used in food preparation in India. Traditionally it is used to treat various diseases like asthma, indigestion, ear diseases, irregular menstruation, skin diseases, piles, fractured bones, etc.
This study aimed to evaluate the ability of the plant extracts to inhibit cycloxygenase (COX-1), cycloxygenase (COX-2), and 5-lipoxygenase (5-LOX) enzyme activity. Western blot analysis was also carried out in the quest to determine the effect of active acetone fraction of Cissus quadrangularis (AFCQ) on proinflammatory mediators as acetone extract is found to be the most effective in this study.
The differential extract of the stem were tested for enzyme inhibition of COX and 5-LOX using spectroscopic and polarigraphic method. Effective acetone extract was partially purified by silica column, one of the active fraction showed dual inhibition against COX and 5-LOX. Western blotting shows downregulation of proinflammatory mediators as well as upregulation of phase-II enzymes.
AFCQ extract showed COX and 5-LOX inhibition with IC(50) values of 7 μg/ml, 0.4 μg/ml, and 20 μg/ml for COX-1, COX-2 and 5-LOX respectively. It also showed anti-inflammatory activity on RAW 264.7 cell line with IC(50) value 65 μg/ml. In addition to this it is showing inhibition of proinflammatory mediators like iNOS and TNFα, along with translocation of Nrf-2 and upregulation of HO-1.
AFCQ is a COX and 5-LOX inhibitor isolated from the stems of Cissus quadrangularis. It is also effectively downregulate the iNOS, TNFα, and upregulation of HO-1.
菱叶崖爬藤是一种古老的药用植物。它是一种被称为“Laksha Gogglu”的阿育吠陀配方的活性成分。其茎在印度用于食品制备。传统上，它用于治疗各种疾病，如哮喘、消化不良、耳部疾病、月经不调、皮肤病、痔疮、骨折等。
本研究旨在评估该植物提取物抑制环氧化酶（COX-1）、环氧化酶（COX-2）和 5-脂氧合酶（5-LOX）酶活性的能力。还进行了 Western blot 分析，以确定活性丙酮提取物（AFCQ）对促炎介质的影响，因为在这项研究中，丙酮提取物被发现是最有效的。
用分光光度法和极谱法对茎的差异提取物进行 COX 和 5-LOX 的酶抑制测试。有效的丙酮提取物通过硅胶柱进行部分纯化，其中一个活性部分对 COX 和 5-LOX 表现出双重抑制作用。Western blot 显示促炎介质下调以及 II 相酶上调。
AFCQ 提取物对 COX-1、COX-2 和 5-LOX 的 IC50 值分别为 7 μg/ml、0.4 μg/ml 和 20 μg/ml，对 COX 和 5-LOX 均有抑制作用。它对 RAW 264.7 细胞系也表现出抗炎活性，IC50 值为 65 μg/ml。除此之外，它还显示出对 iNOS 和 TNFα 等促炎介质的抑制作用，以及 Nrf-2 的易位和 HO-1 的上调。
AFCQ 是从菱叶崖爬藤茎中分离得到的 COX 和 5-LOX 抑制剂。它还能有效下调 iNOS、TNFα，并上调 HO-1。
