首页> 外国专利> A NON STEROIDAL ANTI INFLAMMATORY COMPUOUND FROM TREE: ANOGEISSUS PENDULA EDGEW

A NON STEROIDAL ANTI INFLAMMATORY COMPUOUND FROM TREE: ANOGEISSUS PENDULA EDGEW

机译:一种来自树的非甾体抗炎复合物:无齿天牛缘

摘要

The invention relates to a process for isolation and purification of bioactive proanthocynidins possessing anti-inflammatory activity by virtue of its inhibitory action on cylooxygenase -1 and 2 (COX-1 and COX-2).The relief from pain and inflammation Anti-inflammatory Drugs is achieved by blocking production of enzymes cylooxygenase -1 and 2 (COX-1 and COX-2). Under the normal conditions, COX-2 expression is highly restricted; but COX-2 is dramatically unregulated during inflammation and in the rheumatoid arthritis (RA). Hence the inhibition of COX-2 and COX-1 consequently decline of formation of prostaglandins with relief from pain and inflammation. The proanthocyanidins under patent was isolated from the leaves of Anogeissus pendula, a very common tree in deciduous forest of Bundelkhand region of Uttar Pradesh and nearby states and is much popular for fuel wood and fodder in lean periods. It was isolated by simple process of extraction with aqueous acetone and purified by paper chromatography using water as eluting solvent avoiding expensive organic solvents and costly techniques like High Performance Liquid Chromatography (HPLC), Centrifugal partition chromatography (CPC) and gel-permeable chromatography (GPC)etc. The final purification was done by paper chromatography enhancing the economic viabilityof the process. The proanthocyanidins exhibited excellent anti inflammatory activity by inhibiting cox-2 and Cox-1 enzyme with IC50 35.0µgm and 96.0ngm showing cox-2/cox-l ratio 2.74 very much similar to Diclofen, a popular NSAID on OTC which has COX-2/ COX-1 ratio 2.2. Keeping in view the economic viability of process and potentiality of proanthocyanidin as anti-inflammatory activity it possesses all merits to get patent under IPR.
机译:本发明涉及一种由于对环加氧酶-1和2(COX-1和COX-2)具有抑制作用而具有抗炎活性的生物活性原花青素的分离和纯化方法。减轻疼痛和炎症的作用抗炎药通过阻断环氧化酶-1和2(COX-1和COX-2)的生产来实现这一目标。在正常情况下,COX-2的表达受到高度限制。但在炎症和类风湿关节炎(RA)期间,COX-2的表达明显失调。因此,对COX-2和COX-1的抑制作用从而减少了前列腺素的形成,减轻了疼痛和炎症。受专利保护的原花青素是从蓬蒿的叶子中分离出来的。蓬蒿是北方邦和邻州邦德尔坎德地区落叶林中非常常见的一棵树,在贫瘠的时期广泛用作薪柴和饲料。它可以通过简单的丙酮水溶液萃取工艺进行分离,然后通过纸色谱法纯化,使用水作为洗脱溶剂,避免使用昂贵的有机溶剂,并采用高效液相色谱(HPLC),离心分配色谱(CPC)和凝胶渗透色谱(GPC)等昂贵的技术)等等。通过纸色谱法进行最终纯化,以提高该方法的经济可行性。原花青素通过抑制cox-2和Cox-1酶表现出优异的抗炎活性,IC50为35.0µgm和96.0ngm,显示cox-2 / cox-1比例为2.74,非常类似于Diclofen,后者是OTC上流行的NSAID,具有COX-2 / COX-1比值2.2。考虑到该方法的经济可行性以及原花青素作为抗炎活性的潜力,它具有在IPR下获得专利的所有优点。

著录项

  • 公开/公告号IN2009DE01484A

    专利类型

  • 公开/公告日2011-01-28

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN1484/DEL/2009

  • 发明设计人 SUMAN LATA;DR S K TANDAN;DR B K BHADORIA;

    申请日2009-07-21

  • 分类号A61K36/18;

  • 国家 IN

  • 入库时间 2022-08-21 18:05:54

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