首页> 外国专利> USE OF FICUS VIRENS AIT EXTRACT AND NOVEL COMPOUND ISOLATED THEREFOM AGAINST -HYDROXY--METHYLGLUTARYL-COA REDUCTASE INHIBITORY ACTIVITY, HYPERLIPIDEMIA AND OXIDATIVE STRESS.

USE OF FICUS VIRENS AIT EXTRACT AND NOVEL COMPOUND ISOLATED THEREFOM AGAINST -HYDROXY--METHYLGLUTARYL-COA REDUCTASE INHIBITORY ACTIVITY, HYPERLIPIDEMIA AND OXIDATIVE STRESS.

机译:FICUS VIRENS AIT提取物的使用和新型复合物对羟基-甲基-谷氨酰胺-COA还原酶抑制活性,高脂血症和氧化应激的抵抗作用。

摘要

The present study was done to evaluate the most potent antioxidant and -hydroxy-Pmethylglutaryl-CoA reductase (HMGR) inhibitor from sequentially extracted fraction of Ficus virens Ait., as well as to isolate and purify the bioactive compound responsible for these activity. Our results shows that of all the sequentially extracted fraction of F. virens bark and leaves extract, F. virens bark methanol extract exhibits strong radical scavenging and antioxidant activity. In addition, F. virens bark methanol extract, which is non- cytotoxic, significantly and most potently inhibit the HMGR activity (IC50=3.45+-0.45 ug/ml) in comparison to other extracts. Further, the most potent bioactive fraction F18 was isolated from Ficus virens bark methanolic extract as a reddish brown crystal and subjected to IR, 1H NMR, 13C NMR and mass spectroscopy analysis to identify this compound. Our data showed it as a novel compound, n- Octadecanyl-0- a-D-glucopyranosyl (6+1) -0- a-D-glucopyranoside with a molecular weight of 594, that exhibits significant HMGR inhibitory activity in vitro (98.5%) at 5pg/ml and demonstrated uncompetitive mode of inhibition against HMGCoA reductase. Moreover, the in vivo hypolipidemic activity of FVBM extract and compound isolated therefrom were also evaluated against Tyloxapol induced hyperlipidemia in rats. The inventor for the first time reported a significant reduction in TC, TG and LDL-C with a increase in HDL-C level in FVBM extract (500 mglkg & 1000 mgkg) and pure bioactive compound (10mgkg) treated rats when compared to Tyloxapol induced hyperlipidemic control rats. These findings suggest that the extract or the bioactive compound isolated therefrom could be used in the treatment of risk factor induced hperlipidemia.
机译:本研究旨在评估顺序提取的榕榕中最有效的抗氧化剂和-羟基-P甲基戊二酰辅酶A还原酶(HMGR)抑制剂,以及分离和纯化负责这些活性的生物活性化合物。我们的结果表明,在按顺序提取的黄连木树皮和叶片提取物中,黄连木树皮甲醇提取物均具有较强的自由基清除和抗氧化活性。另外,与其他提取物相比,无细胞毒性的金黄色葡萄球菌树皮甲醇提取物显着且最有效地抑制HMGR活性(IC50 = 3.45 + -0.45 ug / ml)。此外,从榕榕树皮甲醇提取物中分离出最强的生物活性级分F18,为红棕色晶体,并进行IR,1 H NMR,13 C NMR和质谱分析以鉴定该化合物。我们的数据显示它是一种新颖的化合物,分子量为594的n-十八烷基-0- aD-吡喃葡萄糖基(6 + 1)-0-aD-吡喃葡糖苷,在5pg时表现出显着的HMGR抑制活性(98.5%) / ml,并且显示出对HMGCoA还原酶的非竞争性抑制方式。此外,还评价了FVBM提取物和从其分离的化合物的体内降血脂活性对泰洛沙泊诱导的大鼠高血脂症。发明人首次报道,与替洛沙泊诱导的大鼠相比,FVBM提取物(500 mglkg和1000 mgkg)和纯生物活性化合物(10mgkg)处理的大鼠的TC,TG和LDL-C显着降低,HDL-C水平升高高脂血症对照组。这些发现表明,提取物或从中分离的生物活性化合物可用于治疗危险因素引起的高脂血症。

著录项

  • 公开/公告号IN2014DE00308A

    专利类型

  • 公开/公告日2014-06-20

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN308/DEL/2014

  • 申请日2014-02-03

  • 分类号C07C33/14;A61K31/365;

  • 国家 IN

  • 入库时间 2022-08-21 15:57:21

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