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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Biological evaluation of synthetic chalcone and flavone derivatives as anti-inflammatory agents
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Biological evaluation of synthetic chalcone and flavone derivatives as anti-inflammatory agents

机译：合成查尔酮和黄酮衍生物作为抗炎药的生物学评价

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摘要

Flavonoids and chalcones are natural plant derived compounds with inherent therapeutic value for a range of human pathologies. In this study, a series of 24 substituted chalcones and flavones were synthesized and subsequently screened for anti-inflammatory effects on lipopolysaccharide (1 A mu g/ml)-activated BV-2 microglial cells by assessing initial production/release of nitric oxide (NO). The data obtained eliminate the majority of compounds as weak or non-effective, whereas 2'-hydroxy-3,4,5,3',4'-pentamethoxychalcone (1) and 2'-hydroxy-3,4,5-trimethoxychalcone (2) were potent, having an IC50 of 1.10 and 2.26 mu M, respectively; with greater potency than L-N6-(1-iminoethyl)lysine selective iNOS inhibitor (IC50 = 3.1 mu M) but less than steroidal dexamethasone (IC50 < 200 nM). The most potent compound (chalcone 1) attenuated NO parallel to reducing iNOS protein expression, events also corresponding to reduction of IL-1 alpha, IL-10 and IL-6 pro-inflammatory cytokines. These findings suggest that the presence of electron donating groups OH and OCH3 on both A and B rings of synthetic compounds correlate to stronger anti-inflammatory potency.
机译：类黄酮和查耳酮是天然植物衍生的化合物，对多种人类病理都有固有的治疗价值。在这项研究中，合成了一系列24个取代的查耳酮和黄酮，随后通过评估一氧化氮的最初产生/释放，筛选了对脂多糖（1 Aμg / ml）激活的BV-2小胶质细胞的抗炎作用。 ）。获得的数据消除了大多数化合物的弱或无效效果，而2'-羟基-3,4,5,3'，4'-五甲氧基查尔酮（1）和2'-羟基-3,4,5-三甲氧基查尔酮（2）是有效的，IC50分别为1.10和2.26μM;具有比L-N6-（1-亚氨基乙基）赖氨酸选择性iNOS抑制剂（IC50 = 3.1μM）更高的效力，但低于甾体地塞米松（IC50 <200 nM）。最有效的化合物（查耳酮1）与减少iNOS蛋白表达平行地减弱NO，其事件也对应于IL-1α，IL-10和IL-6促炎细胞因子的减少。这些发现表明，合成化合物的A和B环上均存在供电子基团OH和OCH3，与更强的抗炎能力相关。

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