Gülçin İlhami, Scozzafava Andrea, Supuran Claudiu T, Koksal Zeynep, Turkan Fikret, Çetinkaya Songül, Bingöl Zeynebe, Huyut Zübeyir, Alwasel Saleh H
a Department of Chemistry , Ataturk University , Erzurum , Turkey .
b Department of Zoology , College of Science, King Saud University , Riyadh , Saudi Arabia .
J Enzyme Inhib Med Chem. 2016 Dec;31(6):1698-702. doi: 10.3109/14756366.2015.1135914. Epub 2016 Feb 10.
Rosmarinic acid (RA) is a natural polyphenol contained in many aromatic plants with promising biological activities. Carbonic anhydrases (CAs, EC 4.2.1.1) are widespread and intensively studied metalloenzymes present in higher vertebrates. Acetylcholinesterase (AChE, E.C. 3.1.1.7) is intimately associated with the normal neurotransmission by catalysing the hydrolysis of acetylcholine to acetate and choline and acts in combination with butyrylcholinesterase (BChE) to remove acetylcholine from the synaptic cleft. Lactoperoxidase (LPO) is an enzyme involved in fighting pathogenic microorganisms, whereas glutathione S-transferases (GSTs) are dimeric proteins present both in prokaryotic and in eukaryotic organisms and involved in cellular detoxification mechanisms. In the present study, the inhibition effects of rosmarinic acid on tumour-associated carbonic anhydrase IX and XII isoenzymes, AChE, BChE, LPO and GST enzymes were evaluated. Rosmarinic acid inhibited these enzymes with Kis in the range between micromolar to picomolar. The best inhibitory effect of rosmarinic acid was observed against both AChE and BChE.
迷迭香酸(RA)是一种存在于许多具有潜在生物活性的芳香植物中的天然多酚。碳酸酐酶(CAs,EC 4.2.1.1)是广泛存在且经过深入研究的金属酶,存在于高等脊椎动物中。乙酰胆碱酯酶(AChE,E.C. 3.1.1.7)通过催化乙酰胆碱水解为乙酸盐和胆碱,与正常神经传递密切相关,并与丁酰胆碱酯酶(BChE)共同作用,从突触间隙清除乙酰胆碱。乳过氧化物酶(LPO)是一种参与对抗病原微生物的酶,而谷胱甘肽S-转移酶(GSTs)是存在于原核生物和真核生物中的二聚体蛋白质,参与细胞解毒机制。在本研究中,评估了迷迭香酸对肿瘤相关碳酸酐酶IX和XII同工酶、AChE、BChE、LPO和GST酶的抑制作用。迷迭香酸以微摩尔至皮摩尔范围内的抑制常数(Ki)抑制这些酶。迷迭香酸对AChE和BChE均表现出最佳抑制效果。