Mahendran Sekar, Badami Shrishailappa, Ravi Subban, Thippeswamy Boreddy Shivanandappa, Veerapur Veeresh Prabhakar
Department of Pharmaceutical Chemistry, J.S.S. College of Pharmacy, Rocklands, Ootacamund, TN, India.
Chem Pharm Bull (Tokyo). 2011;59(8):913-9. doi: 10.1248/cpb.59.913.
Antioxidant and related properties of the plant Embelia ribes and embelin are well known. In the present study embelin was condensed with various aromatic substituted primary amines to yield ten new and one reported derivatives along with monomethyl embelin. All these compounds along with embelin were evaluated for in vitro antioxidant activity using 2,2'-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) diammonium salt (ABTS) and 2,2'-diphenyl-1-picryl hydrazyl (DPPH) methods. Two para-substituted embelin derivatives showed potent antioxidant activity. These compounds along with embelin were studied for analgesic and anti-inflammatory activities at 10 and 20 mg/kg doses by standard methods. Potent analgesic activity higher than the standard pentazocine was observed. Embelin and both of its derivatives almost completely abolished the acetic acid induced writhing. p-Sulfonylamine phenylamino derivative showed better anti-inflammatory activity than embelin.
植物酸藤子和紫金牛醌的抗氧化及相关特性广为人知。在本研究中，紫金牛醌与各种芳香取代的伯胺缩合，得到了10种新的衍生物和1种已报道的衍生物以及单甲基紫金牛醌。使用2,2'-联氮-双-(3-乙基苯并噻唑啉-6-磺酸)二铵盐（ABTS）和2,2'-二苯基-1-苦基肼（DPPH）方法对所有这些化合物以及紫金牛醌进行了体外抗氧化活性评估。两种对位取代的紫金牛醌衍生物表现出较强的抗氧化活性。通过标准方法研究了这些化合物以及紫金牛醌在10和20 mg/kg剂量下的镇痛和抗炎活性。观察到其镇痛活性强于标准喷他佐辛。紫金牛醌及其两种衍生物几乎完全消除了乙酸诱导的扭体反应。对磺酰胺苯氨基衍生物显示出比紫金牛醌更好的抗炎活性。
