新合成的罗氏酮曼尼希碱的体内镇痛及体外抗氧化活性

Gulam Muheyuddeen, Sarwar Husain Rayini, P. Yadav, Sujeet Kumar Gupta
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引用次数: 0

摘要

1,4 -萘醌(Lawsone)广泛分布于自然界,自古以来就被用于传统医学。Lawsone已被用作染料,其天然形式和合成衍生物均具有抗真菌、抗菌、抗肿瘤、抗疟疾、杀软体动物和抗氧化活性。采用pH梯度法(搅拌法)和浸渍法从刺槐叶中分离得到1,4 -萘醌(Lawsone)。以分离的1,4 -萘醌为原料,在乙醇存在下与取代苯胺反应合成了2-取代氨基萘- 1,4 -二酮(3a-o),并采用DPPH模型,用吗啡诱导白化小鼠热板法评价了其抗氧化活性和体内镇痛活性。在元素分析、红外光谱、核磁共振氢谱和质谱的基础上,确定了最终类似物的结构。元素调查、红外光谱、核磁共振氢谱、质谱等各项标准被提出。结果表明,合成的化合物3d的IC50为75.39±4.12mg/ml,其抗氧化活性与标准抗坏血酸(IC50为45.54±3.06mg/ml)相当。3c、3m和30显示出与标准尼美舒利相当的强效镇痛活性(50mg/kg b.w时100%)。这一研究结果表明,刺槐叶具有生物活性化合物,可用于创新抗氧化和镇痛药物的开发。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In vivo Analgesics and in vitro Antioxidants Activity of Newly Synthesized Mannich Bases of Lawsone
1, 4- naphthoquinone (Lawsone) is widely distributed in nature and has been used since ancient times in traditional medicine. Lawsone has been used as a dye, and both its natural form and synthetic derivatives exhibit antifungal, antibacterial, antitumor, Antimalarial, molluscicidal, and antioxidant activity. 1, 4- naphthoquinone (Lawsone) was isolated from the leaves of Lawsonia inermis by using the pH gradient (agitation) and maceration method. A convenient synthesis of 2-substituted amino naphthalene-1, 4-dione (3a-o) has been achieved by reaction of isolated 1, 4- naphthoquinone with substituted aniline in the presence of ethanol and DPPH model is used for the evaluation of the antioxidant activities and in vivo analgesic activity using albino mice morphine-induced hot plate method. The structure of the ultimate analogs has been inveterate on the basis of elemental analysis, IR, 1H NMR, and mass spectra. All the standards of elemental investigation, IR, 1H NMR, and mass spectra were initiate to be prominent. The results indicate that synthesized compound 3d having IC50 75.39 ± 4.12mg/ml showed potent antioxidant activity comparable to standard ascorbic acid (IC50 45.54 ± 3.06mg/ml). 3c, 3m, and 3o showed potent analgesic activity comparable to standard nimesulide (100% at 50mg/kg b.w). This reading suggests that leaves of Lawsonia inermis have bioactive compounds for innovative antioxidant and analgesic remedy development.
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