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Anti-inflammatory mechanisms of compounds from Curcuma mangga rhizomes using RAW264.7 macrophage cells

机译:RAW264.7巨噬细胞对姜黄根茎化合物的抗炎作用

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Curcuma mangga extract and its compounds were investigated for their anti-inflammatory mechanisms against nitric oxide (NO) and prostaglandin E _2 (PGE_2) release using RAW 264.7 cells. From bioassay-guided fractionation, demethoxycurcumin (1) was isolated from the chloroform fraction, whereas 15,16 bisnorlabda-8(17), 11-dien-13-one (2) and (E)-15,15-diethoxylabda-8(17),12-dien-16-al (3) were from the n-hexane fraction. Bisdemethoxycurcumin (4), the structure of which is similar to that of 1, was also tested. Of the tested compounds, 3 exhibited the highest activity against NO release with an IC_(50) value of 9.4 μM, followed by 1 (IC _(50) = 12.1 μM), 4 (IC_(50) = 16.9 μM) and 2 (IC _(50) = 30.3 μM). For the effect on PGE_2 release, 1 possessed the highest activity (IC_(50) = 4.5 μM, followed by 4 (IC_(50) = 5.6 μM), 3 (IC_(50) = 35.3 μM) and 2 (IC _(50) = 42.5 μM). The mechanism at transcriptional level revealed that 1, 3 and 4 down-regulated the mRNA expressions of iNOS and COX-2 in a dose-dependent manner, whereas 2 had an effect only on iNOS mRNA. These results indicate that C. mangga and its compounds do exert anti-inflammatory activity. Moreover, this is the first report of the isolation of 3 from C. mangga rhizomes.
机译:使用RAW 264.7细胞研究了姜黄提取物及其化合物抗一氧化氮(NO)和前列腺素E _2(PGE_2)释放的抗炎机制。从生物测定指导的分级分离中,从氯仿级分中分离了脱甲氧基姜黄素(1),而15,16 bisnorlabda-8(17),11-dien-13-one(2)和(E)-15,15-dithoxylabda-8 (17),12-dien-16-al(3)来自正己烷馏分。还测试了双去甲氧基姜黄素(4),其结构类似于1。在测试的化合物中,有3种化合物具有最高的NO释放活性,其IC_(50)值为9.4μM,其次是1(IC _(50)= 12.1μM),4(IC_(50)= 16.9μM)和2 (IC _(50)= 30.3μM)。对于PGE_2释放的影响,1具有最高活性(IC_(50)= 4.5μM,其次是4(IC_(50)= 5.6μM),3(IC_(50)= 35.3μM)和2(IC_( 50)= 42.5μM)。在转录水平上的机制揭示了1、3和4以剂量依赖性方式下调了iNOS和COX-2的mRNA表达,而2仅对iNOS mRNA起作用。这表明芒果樟脑及其化合物确实具有抗炎活性,这是从芒果樟脑根中分离出3种化合物的首次报道。

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