从用于治疗炎症的药用植物中发现环氧化酶抑制剂。
Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation.
机构信息
Department of Medicinal Chemistry and Pharmacognosy, University of Illinois College of Pharmacy, 833 S. Wood Street, Chicago, IL, USA.
出版信息
Pharmacol Res. 2010 Jun;61(6):519-24. doi: 10.1016/j.phrs.2010.02.007. Epub 2010 Feb 24.
Abstract
Eleven authenticated botanicals used in the traditional Chinese medicine Huo-Luo-Xiao-Ling Dan were screened for ligands to cyclooxygenase (COX) using pulsed ultrafiltration liquid chromatography-mass spectrometry, and a mass spectrometry-based enzyme assay was used to determine the concentration of each of 17 ligands that inhibited COX-1 or COX-2 by 50% (IC(50)). Acetyl-11-keto-beta-boswellic acid, beta-boswellic acid, acetyl-alpha-boswellic acid, acetyl-beta-boswellic acid, and betulinic acid were COX-1 selective inhibitors with IC(50) values of approximately 10 microM. Senkyunolide O and cryptotanshinone were COX-2 selective inhibitors with IC(50) values of 5 microM and 22 microM, respectively. Roburic acid and phenethyl-trans-ferulate inhibited COX-1 and COX-2 equally. COX inhibition and the IC(50) values of most of these natural product ligands have not been reported previously.
摘要
采用脉冲超滤液相色谱-质谱联用技术，对用于中药活洛消癥丹的 11 种已鉴定的植物药进行了能与环氧化酶（COX）结合的配体筛选，同时还采用基于质谱的酶检测法，测定了能使 COX-1 或 COX-2 的抑制率达 50%时的各配体浓度（IC50）。11-酮基乙酰基-β-乳香酸、β-乳香酸、乙酰-α-乳香酸、乙酰-β-乳香酸和桦木酸对 COX-1 有选择性抑制作用，IC50 值约为 10μM。升麻醇 O 和隐丹参酮对 COX-2 有选择性抑制作用，IC50 值分别为 5μM 和 22μM。罗布麻酸和对香豆酸乙酯对 COX-1 和 COX-2 的抑制作用相当。这些天然产物配体的 COX 抑制作用及其 IC50 值此前尚未有报道。
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