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Membrane stabilisation: a possible anti-inflammatory mechanism for the extracts and compounds from Spathodea campanulata

机译:膜稳定:喜树(Spathodea campanulata)的提取物和化合物的可能的抗炎机制

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摘要

This study was undertaken to evaluate the efficiency of extract, fractions and pure molecules from Spathodea campanulata (SC) towards inflammation. Polarity-based extracts of SC were found active in stabilising red blood cell (RBC) membrane indicating anti-inflammatory potential. Bioactivity-guided isolation of SC produced 1-O-(E)-caffeoyl-beta-gentiobiose and (2S)-1,2-di-O-[(9Z, 12Z, 15Z)-octadeca-9,12,15-trienoyl]-3-O-[alpha-D-galctopyranosyl-(1" -> 6')-O-beta-D-galactopyranosyl] glycerol as the active constituents with 65.91% and 67.41% of membrane stability, respectively. Activity of the third compound (verminoside) could not be ascertained owing to extremely low recoverability. Furthermore, the isolated compounds were subjected to in silico studies. The compounds showed good binding affinity towards cyclooxygenase-2. Absorption, distribution, metabolism & excretion (ADME)-toxicity studies illustrated that the isolated compounds are free of toxicity. These observations help us to conclude that SC might exert its anti-inflammatory activity by soothing the RBC membrane as it is the case for non-steroidal anti-inflammatory drugs towards lysozomal membranes. Therefore, SC might be considered as a potential candidate for development of anti-inflammatory drugs.
机译:进行这项研究以评估来自桔梗(SC)的提取物,级分和纯分子对炎症的功效。发现基于极性的SC提取物在稳定红细胞(RBC)膜中具有活性,表明具有抗炎潜力。生物活性指导下的SC分离产生了1-O-(E)-咖啡酰-β-龙胆二糖和(2S)-1,2-di-O-[(9Z,12Z,15Z)-octadeca-9,12,15-三烯酰基] -3-O- [α-D-吡喃半乳糖基-(1“-> 6')-O-β-D-吡喃半乳糖基]甘油为有效成分,分别具有65.91%和67.41%的膜稳定性。由于回收率极低,无法确定第三种化合物(维米诺糖苷),此外,对分离出的化合物进行了计算机分析,发现它们对环氧合酶-2具有良好的结合亲和力,吸收,分布,代谢和排泄(ADME)-毒性研究表明分离出的化合物无毒,这些观察结果有助于我们得出结论,SC可能通过舒缓RBC膜发挥其抗炎活性,就像非甾体类抗炎药对溶酶体膜一样。 ,SC可能被认为是抗炎药开发的潜在候选者。

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