Department of Animal Biology, School of Life Sciences, University of Hyderabad, Hyderabad 500046, India.
Department of Animal Biology, School of Life Sciences, University of Hyderabad, Hyderabad 500046, India..
Fitoterapia. 2018 Nov;131:189-199. doi: 10.1016/j.fitote.2018.10.016. Epub 2018 Oct 16.
Premna integrifolia (Agnimantha brihat) is a traditional medicinal plant with a prominent place in Ayurveda, Siddha and Unani systems of medicine. In this study we have evaluated the anti-inflammatory and immunomodulatory properties of the Premna integrifolia root extracts employing cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), and 5-lipoxygenase (5-LOX) enzyme-based assays, lymphocyte proliferation assay, pro-and anti-inflammatory cytokines measurement. Petroleum ether extract (PEE) of Premna integrifolia showed potent inhibition of COX-2 and 5-LOX with IC values of 6.15 μg/mL and 11.33 μg/mL respectively. In in vitro studies on RAW 264.7 cell line, PEE showed inhibition in the formation of nitric oxide (NO), pro-inflammatory cytokines (IL-1β, IL-6), prostaglandin E (PGE) production, induction of anti-inflammatory cytokine (IL-2) and down-regulation of expression of COX-2, 5-LOX, TNF-α, IL-1β and iNOS. PEE also significantly reduced carrageenan-induced paw edema in mouse model of inflammation. Further, attempts in isolating the active principle(s) involved in these anti-inflammatory effects of PEE by separation on RP-HPLC resulted in the isolation of four active peaks, H1, H2, H3 and H5, inhibiting COX-1, COX-2 and 5-LOX, out of which H3 was identified as 6- hydroxy salvinolone (6-HS). Present findings reveal that PEE of roots of Premna integrifolia exhibits potent anti-inflammatory and immunomodulatory activities, which could form a potential source for development of anti-inflammatory drugs. 6-HS, a COX-2/5-LOX dual inhibitor along with other lead molecules isolated from PEE of Premna integrifolia may form lead molecules for the development of COX-LOX dual inhibitors.
水麻（Agnimantha brihat）是一种传统药用植物，在阿育吠陀、悉达和顺势疗法医学体系中占有重要地位。在这项研究中，我们评估了水麻根提取物的抗炎和免疫调节特性，采用环加氧酶-1（COX-1）、环加氧酶-2（COX-2）和 5-脂氧合酶（5-LOX）酶基测定法、淋巴细胞增殖测定法、促炎和抗炎细胞因子测定法。水麻的石油醚提取物（PEE）对 COX-2 和 5-LOX 表现出很强的抑制作用，IC 值分别为 6.15μg/mL 和 11.33μg/mL。在 RAW 264.7 细胞系的体外研究中，PEE 抑制了一氧化氮（NO）、促炎细胞因子（IL-1β、IL-6）、前列腺素 E（PGE）的产生，诱导抗炎细胞因子（IL-2）的产生，并下调 COX-2、5-LOX、TNF-α、IL-1β 和 iNOS 的表达。PEE 还显著降低了角叉菜胶诱导的小鼠炎症模型的足肿胀。此外，通过反相高效液相色谱（RP-HPLC）对 PEE 中涉及这些抗炎作用的活性成分进行分离的尝试导致分离出四个活性峰 H1、H2、H3 和 H5，它们抑制 COX-1、COX-2 和 5-LOX，其中 H3 被鉴定为 6-羟基血根碱（6-HS）。目前的研究结果表明，水麻根的 PEE 表现出很强的抗炎和免疫调节活性，这可能成为开发抗炎药物的潜在来源。6-HS 是一种 COX-2/5-LOX 双重抑制剂，以及从水麻 PEE 中分离出的其他先导分子，可能成为 COX-LOX 双重抑制剂的先导分子。
