首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >The effect of caffeic acid phenethyl ester (CAPE) on metabolic enzymes including acetylcholinesterase, butyrylcholinesterase, glutathione S-transferase, lactoperoxidase, and carbonic anhydrase isoenzymes I, II, IX, and XII
【24h】

The effect of caffeic acid phenethyl ester (CAPE) on metabolic enzymes including acetylcholinesterase, butyrylcholinesterase, glutathione S-transferase, lactoperoxidase, and carbonic anhydrase isoenzymes I, II, IX, and XII

机译:咖啡酸苯乙酯(CAPE)对包括乙酰胆碱酯酶,丁酰胆碱酯酶,谷胱甘肽S-转移酶,乳过氧化物酶和碳酸酐酶同工酶I,II,IX和XII在内的代谢酶的影响

获取原文
           

摘要

Abstract Caffeic acid phenethyl ester (CAPE) is an active component of honeybee propolis extracts. Carbonic anhydrases (CAs, EC 4.2.1.1) are widespread and intensively studied metalloenzymes present in higher vertebrates including humans as many diverse isoforms. Acetylcholinesterase (AChE) is responsible for acetyl choline (ACh) hydrolysis and plays a fundamental role in nerve impulse transmission by terminating the action of the ACh neurotransmitter at cholinergic synapses and neuromuscular junctions. Butyrylcholinesterase (BChE) is another enzyme abundantly present in the liver and released into blood in a soluble form. Lactoperoxidase (LPO) is an enzyme involved in fighting pathogenic microorganisms whereas glutathione S-transferases (GSTs) are dimeric proteins present both in prokaryotic and eukaryotic organisms and involved in cellular detoxification mechanisms. In the present study, the inhibition effect of CAPE on human carbonic anhydrase (hCA) isoforms I, II, IX, and XII, AChE, BChE, LPO, and GST was evaluated. CAPE inhibited these enzymes with Kis in the range between micromolar to picomolar. The best inhibitory effect was observed against AChE and BChE.
机译:摘要咖啡酸苯乙酯(CAPE)是蜜蜂蜂胶提取物中的活性成分。碳酸酐酶(CAs,EC 4.2.1.1)是一种广泛存在的,经过深入研究的金属酶,存在于包括人类在内的高级脊椎动物中,并具有多种多样的同工型。乙酰胆碱酯酶(AChE)负责乙酰胆碱(ACh)的水解,并通过终止ACh神经递质在胆碱能突触和神经肌肉接头处的作用,在神经冲动传递中起重要作用。丁酰胆碱酯酶(BChE)是另一种在肝脏中大量存在并以可溶形式释放到血液中的酶。乳过氧化物酶(LPO)是一种与病原微生物作斗争的酶,而谷胱甘肽S-转移酶(GSTs)是原核和真核生物中都存在的二聚体蛋白,并参与细胞排毒机制。在本研究中,评估了CAPE对人碳酸酐酶(hCA)亚型I,II,IX和XII,AChE,BChE,LPO和GST的抑制作用。 CAPE用微摩尔至皮摩尔的K i s抑制这些酶。观察到对AChE和BChE的最佳抑制作用。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号