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Bioactivity-Guided Isolation of Ethyl-p-methoxycinnamate an Anti-inflammatory Constituent from Kaempferia galanga L. Extracts

机译:生物活性指导下的高辛Kaempferia galanga L.提取物的抗炎成分对-甲氧基肉桂酸乙酯的分离。

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摘要

This study evaluated the anti-inflammatory effect of Kaempferia galanga (KG) using an activity-guided approach. KG rhizomes were serially extracted with petroleum ether, chloroform, methanol and water. These extracts (2 g/kg each) were tested for their ability to inhibit carrageenan-induced rat paw edema. The chloroform extract was found to exert the highest inhibition (42.9%) compared to control (p < 0.001), hence it was further fractionated by washing serially with hexane, hexane-chloroform (1:1) and chloroform. The chloroform fraction (1 g/kg) showed the highest inhibitory effect (51.9%, p < 0.001) on carrageenan-induced edema. This chloroform fraction was further fractionated with hexane-chloroform (1:3) and chloroform, and of the two fractions, the hexane-chloroform sub-fraction was the most effective in inhibiting edema (53.7%, p < 0.001). GC-MS analysis of the active sub-fraction identified ethyl-p-methoxycinnamate (EPMC) as the major component, which was re-crystallized. EPMC dose-dependently inhibited carrageenan-induced edema with an MIC of 100 mg/kg. Moreover, in an in vitro study, EPMC non-selectively inhibited the activities of cyclooxygenases 1 and 2, with IC50 values of 1.12 µM and 0.83 µM respectively. These results validate the anti-inflammatory activity of KG which may be exerted by the inhibition of cyclooxygenases 1 and 2. EPMC isolated from this plant may be the active anti-inflammatory agent.
机译:这项研究使用活性指导方法评估了Kaempferia galanga(KG)的抗炎作用。用石油醚,氯仿,甲醇和水连续提取KG根茎。测试这些提取物(每种2 g / kg)抑制角叉菜胶诱导的大鼠爪水肿的能力。与对照(p <0.001)相比,发现氯仿提取物具有最高的抑制作用(42.9%),因此通过依次用己烷,己烷-氯仿(1:1)和氯仿洗涤来进一步分离。氯仿组分(1 g / kg)对角叉菜胶诱导的水肿表现出最高的抑制作用(51.9%,p <0.001)。将该氯仿馏分进一步用己烷-氯仿(1:3)和氯仿分馏,在这两个馏分中,己烷-氯仿亚馏分最有效地抑制水肿(53.7%,p <0.001)。活性成分的GC-MS分析确定对-甲氧基肉桂酸乙酯(EPMC)为主要成分,将其重结晶。 EPMC剂量依赖性抑制角叉菜胶诱发的水肿,MIC为100 mg / kg。此外,在体外研究中,EPMC非选择性抑制环氧合酶1和2的活性,IC50值分别为1.12 µM和0.83 µM。这些结果证实了KG的抗炎活性,其可以通过抑制环氧合酶1和2而发挥作用。从该植物中分离出的EPMC可能是活性抗炎剂。

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