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药用植物橄榄(Canarium patentinervium Miq.,橄榄科Kunth.)是一种具有抗炎作用的生物资源,其含有环氧化酶(COX)和5-脂氧合酶(5-LOX)的双重抑制剂。

The Medicinal Timber Canarium patentinervium Miq. (Burseraceae Kunth.) Is an Anti-Inflammatory Bioresource of Dual Inhibitors of Cyclooxygenase (COX) and 5-Lipoxygenase (5-LOX).

作者信息

Mogana R, Teng-Jin K, Wiart C

机构信息

Center for Natural and Medicinal Products Research, School of Pharmacy, Faculty of Science, University of Nottingham (Malaysia Campus), Jln Broga, 43500 Semenyih, Selangor Darul Ehsan, Malaysia.

出版信息

ISRN Biotechnol. 2013 Oct 1;2013:986361. doi: 10.5402/2013/986361. eCollection 2013.

DOI:10.5402/2013/986361
PMID:25937987
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4393036/
Abstract

The barks and leaves extracts of Canarium patentinervium Miq. (Burseraceae Kunth.) were investigated for cyclooxygenase (COX) and 5-lipoxygenase (LOX) inhibition via in vitro models. The corresponding antioxidative power of the plant extract was also tested via nonenzyme and enzyme in vitro assays. The ethanolic extract of leaves inhibited the enzymatic activity of 5-LOX, COX-1, and COX-2 with IC50 equal to 49.66 ± 0.02 μg/mL, 0.60 ± 0.01 μg/mL, and 1.07 ± 0.01 μg/mL, respectively, with selective COX-2 activity noted in ethanolic extract of barks with COX-1/COX-2 ratio of 1.22. The ethanol extract of barks confronted oxidation in the ABTS, DPPH, and FRAP assay with EC50 values equal to 0.93 ± 0.01 μg/mL, 2.33 ± 0.02 μg/mL, and 67.00 ± 0.32 μg/mL, respectively, while the ethanol extract of leaves confronted oxidation in β-carotene bleaching assay and superoxide dismutase (SOD) assay with EC50 value of 6.04 ± 0.02 μg/mL and IC50 value of 3.05 ± 0.01 μg/mL. The ethanol extract acts as a dual inhibitor of LOX and COX enzymes with potent antioxidant capacity. The clinical significance of these data is quite clear that they support a role for Canarium patentinervium Miq. (Burseraceae Kunth.) as a source of lead compounds in the management of inflammatory diseases.

摘要

通过体外模型研究了毛叶橄榄(橄榄科)的树皮和树叶提取物对环氧化酶(COX)和5-脂氧合酶(LOX)的抑制作用。还通过非酶和酶体外试验测试了植物提取物相应的抗氧化能力。树叶乙醇提取物对5-LOX、COX-1和COX-2的酶活性具有抑制作用,IC50分别为49.66±0.02μg/mL、0.60±0.01μg/mL和1.07±0.01μg/mL,树皮乙醇提取物表现出对COX-2的选择性活性,COX-1/COX-2比值为1.22。树皮乙醇提取物在ABTS、DPPH和FRAP试验中对抗氧化,EC50值分别为0.93±0.01μg/mL、2.33±0.02μg/mL和67.00±0.32μg/mL,而树叶乙醇提取物在β-胡萝卜素漂白试验和超氧化物歧化酶(SOD)试验中对抗氧化,EC50值为6.04±0.02μg/mL,IC50值为3.05±0.01μg/mL。乙醇提取物作为LOX和COX酶的双重抑制剂,具有强大的抗氧化能力。这些数据的临床意义非常明确,即支持毛叶橄榄(橄榄科)作为炎症性疾病治疗中先导化合物来源的作用。

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