胡萝卜籽中化合物对环氧化酶（COX）的抑制作用。

Inhibition of cyclooxygenase (COX) enzymes by compounds from Daucus carota L. Seeds.

作者信息

Momin Rafikali A, De Witt David L, Nair Muraleedharan G

机构信息

Bioactive Natural Products and Phytoceuticals, Department of Horticulture and National Food Safety and Toxicology Center, Michigan State University, East Lansing, Michigan 48824, USA.

出版信息

Phytother Res. 2003 Sep;17(8):976-9. doi: 10.1002/ptr.1296.

DOI:10.1002/ptr.1296

PMID:13680840

Abstract

Cyclooxygenase (COX) enzymes inhibitory assay directed investigation of Daucus carota seed extracts resulted in the isolation and characterization of compounds, 2,4,5-trimethoxybenzaldehyde (1), oleic acid (2), trans-asarone (3) and geraniol (4). Compounds 1-4 showed 3.32, 45.32, 46.15, and 3.15% of prostaglandin H endoperoxide synthase-I (COX-I) inhibitory activity and 52.69, 68.41, 64.39 and 0% prostaglandin H endoperoxide synthase-II (COX-II) inhibitory activity, respectively at 100 mg mL(-1). Compound 1 showed selectivity towards COX-II enzyme inhibition at 100 microg mL(-1). The COX-II/COX-I ratio for compound 1 was 17.68 at 100 microg mL(-1) compared to solvent control. Ibuprofen, Naproxen, Aspirin, Celebrex and Vioxx at concentrations of 2.06, 2.52, 180, 1.67 and 1.67 microg mL(-1), respectively, gave COX-II/COX-I ratios of 1.13, 0.92, 0.24, 16 and 75, respectively. The inhibition of COX-II enzymes by compounds 1 at 100 microg mL(-1) was significant when compared to Aspirin, Ibuprofen, Naproxen and Celebrex at concentrations studied.

摘要

对胡萝卜籽提取物进行环氧化酶（COX）酶抑制试验的研究，结果分离并鉴定出了化合物2,4,5 -三甲氧基苯甲醛（1）、油酸（2）、反式细辛脑（3）和香叶醇（4）。化合物1 - 4在100 mg mL⁻¹浓度下，分别表现出3.32%、45.32%、46.15%和3.15%的前列腺素H内过氧化物合酶 - I（COX - I）抑制活性，以及52.69%、68.41%、64.39%和0%的前列腺素H内过氧化物合酶 - II（COX - II）抑制活性。化合物1在100 μg mL⁻¹时对COX - II酶表现出选择性抑制。与溶剂对照相比，化合物1在100 μg mL⁻¹时的COX - II/COX - I比值为17.68。布洛芬、萘普生、阿司匹林、塞来昔布和万络在浓度分别为2.06、2.52、180、1.67和1.67 μg mL⁻¹时，COX - II/COX - I比值分别为1.13、0.92、0.24、16和75。在研究的浓度下，与阿司匹林、布洛芬、萘普生和塞来昔布相比，化合物1在100 μg mL⁻¹时对COX - II酶的抑制作用显著。