Department of Medicinal Chemistry and Pharmacognosy, University of Illinois College of Pharmacy, 833 S. Wood Street, Chicago, IL, USA.
Pharmacol Res. 2010 Jun;61(6):519-24. doi: 10.1016/j.phrs.2010.02.007. Epub 2010 Feb 24.
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.
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。
