Patel Neeraj K, Bhutani Kamlesh K
Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S Nagar, Mohali-160062, Punjab (India).
EXCLI J. 2014 Aug 29;13:1011-21. eCollection 2014.
The present study deals with the isolation of fourteen compounds from the active ethyl acetate (MPE) extract of M. pudica (L.) whole plant and their subsequent evaluation for the nitric oxide (NO), tumor necrosis factor alpha (TNF-α) and interleukin 1 beta (IL-1ß) inhibitory activities in lipopolysaccharide (LPS) stimulated RAW 264.7 and J774A.1 cells. Among the tested compounds, L-mimosine (12; IC50 = 19.23 to 21.15 µM), crocetin (4; IC50 = 23.45 to 25.57 µM), crocin (14; IC50 = 27.16 to 31.53 µM) and jasmonic acid (11; IC50 = 21.32 to 29.42 µM) were identified as potent NO inhibitor when tested on the macrophages. Similarly, towards TNF-α and IL-1ß inhibition, including these four compounds, and ethyl gallate (3), gallic acid (10) and caffeic acid (7) were found to be more active with half maximal concentration, 17.32 to 62.32 µM whereas the other compounds depicted moderate and mild effects (IC50 = 59.32 to 95.01 µM). Also, at a dose of 40 mg/Kg, L-mimosine (12), jasmonic acid (11), crocin (14) and its de-esterified form, crocetin (4) were found to significantly (p < 0.05 and 0.001) reduce 60.7 %, 48.9 %, 48.4 % and 43.6 % respectively of TNF-de-esterified production in female Sprague Dawley rats. However, in case of IL-1ß, with the same dose (40 mg/Kg), jasmonic acid (11) exhibited significant reduction with 54.2 % followed by crocin (14) (50.2 %) and crocetin (4) (39.8 %) while L-mimosine (12) was found to reduce only 16.3 %. Based on the results, it can be estimated that these compounds imparting greatly to anti-inflammatory effects of M. pudica in vitro as well as in vivo through reduction of LPS-induced pro-inflammatory mediators which affirm the ethno-pharmacological use of this plant for prevention of inflammatory-related disorders.
本研究从含羞草全株的活性乙酸乙酯提取物（MPE）中分离出14种化合物，并随后评估了它们在脂多糖（LPS）刺激的RAW 264.7和J774A.1细胞中对一氧化氮（NO）、肿瘤坏死因子α（TNF-α）和白细胞介素1β（IL-1β）的抑制活性。在测试的化合物中，左旋含羞草碱（12；IC50 = 19.23至21.15 μM）、藏红花酸（4；IC50 = 23.45至25.57 μM）、藏红花素（14；IC50 = 27.16至31.53 μM）和茉莉酸（11；IC50 = 21.32至29.42 μM）在巨噬细胞上测试时被鉴定为有效的NO抑制剂。同样，对于TNF-α和IL-1β的抑制，包括这四种化合物，以及没食子酸乙酯（3）、没食子酸（10）和咖啡酸（7）被发现更具活性，半数最大浓度为17.32至62.32 μM，而其他化合物表现出中度和轻度作用（IC50 = 59.32至95.01 μM）。此外，在40 mg/Kg的剂量下，发现左旋含羞草碱（12）、茉莉酸（11）、藏红花素（14）及其去酯形式藏红花酸（4）分别显著（p < 0.05和0.001）降低雌性Sprague Dawley大鼠中TNF去酯产物的60.7%、48.9%、48.4%和43.6%。然而，在IL-1β的情况下，在相同剂量（40 mg/Kg）下，茉莉酸（11）表现出显著降低，为54.2%，其次是藏红花素（14）（50.2%）和藏红花酸（4）（39.8%），而左旋含羞草碱（12）仅降低16.3%。基于这些结果，可以估计这些化合物通过减少LPS诱导的促炎介质，在体外和体内对含羞草的抗炎作用有很大贡献，这证实了该植物在预防炎症相关疾病方面的民族药理学用途。
