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乌干达大姆皮吉地区的抗炎药用植物在COX-2/PGH途径中作为强效抑制剂发挥作用。

Antiinflammatory Medicinal Plants from the Ugandan Greater Mpigi Region Act as Potent Inhibitors in the COX-2/PGH Pathway.

作者信息

Schultz Fabien, Osuji Ogechi Favour, Wack Barbara, Anywar Godwin, Garbe Leif-Alexander

机构信息

Institute of Biotechnology, Faculty III-Process Sciences, Technical University of Berlin, Gustav-Meyer-Allee 25, 13355 Berlin, Germany.

Department of Agriculture and Food Sciences, Neubrandenburg University of Applied Sciences, Brodaer Str. 2, 17033 Neubrandenburg, Germany.

出版信息

Plants (Basel). 2021 Feb 12;10(2):351. doi: 10.3390/plants10020351.

DOI:10.3390/plants10020351
PMID:33673238
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7918315/
Abstract

Our study investigates 16 medicinal plants via assessment of inhibition of proinflammatory enzymes such as cyclooxygenases (COX). The plants are used by traditional healers in the Greater Mpigi region in Uganda to treat inflammation and related disorders. We present results of diverse in vitro experiments performed with 76 different plant extracts, namely, (1) selective COX-2 and COX-1 inhibitor screening; (2) 15-LOX inhibition screening; (3) antibacterial resazurin assay against multidrug-resistant , , , and K12; (4) DPPH assay for antioxidant activity; and (5) determination of the total phenolic content (TPC). Results showed a high correlation between traditional use and pharmacological activity, e.g., extracts of 15 out of the 16 plant species displayed significant selective COX-2 inhibition activity in the PGH pathway. The most active COX-2 inhibitors (IC < 20 µg/mL) were nine extracts from , subsp. , , , , and . There was no counteractivity between COX-2 and 15-LOX inhibition in these nine extracts. The ethyl acetate extract of showed the lowest IC value with 0.66 µg/mL (COX-2), as well as the most promising selectivity ratio with 0.1 (COX-2/COX-1). The TPCs and the EC values for DPPH radical scavenging activity showed no correlation with COX-2 inhibitory activity. This led to the assumption that the mechanisms of action are most likely not based on scavenging of reactive oxygen species and antioxidant activities. The diethyl ether extract of stem bark displayed the highest growth inhibition activity against (MIC value: 13 µg/mL), (MIC value: 40 µg/mL), and (MIC value: 150 µg/mL). This study provides further evidence for the therapeutic use of the previously identified plants used medicinally in the Greater Mpigi region.

摘要

我们的研究通过评估对环氧化酶(COX)等促炎酶的抑制作用,对16种药用植物进行了调查。这些植物被乌干达大姆皮吉地区的传统治疗师用于治疗炎症及相关疾病。我们展示了用76种不同植物提取物进行的多种体外实验结果,即:(1)选择性COX - 2和COX - 1抑制剂筛选;(2)15 - 脂氧合酶(15 - LOX)抑制筛选;(3)针对多重耐药的大肠杆菌、金黄色葡萄球菌、粪肠球菌和肺炎克雷伯菌K12的抗菌刃天青试验;(4)用于抗氧化活性的DPPH试验;以及(5)总酚含量(TPC)的测定。结果表明传统用途与药理活性之间存在高度相关性,例如,16种植物中的15种植物提取物在PGH途径中表现出显著的选择性COX - 2抑制活性。活性最强的COX - 2抑制剂(IC<20μg/mL)是来自非洲马铃果、光叶马铃果亚种、钝叶马铃果、椭圆叶马铃果、长叶马铃果、线叶马铃果和狭叶马铃果的9种提取物。这9种提取物中COX - 2和15 - LOX抑制之间没有拮抗作用。非洲马铃果的乙酸乙酯提取物显示出最低的IC值,为0.66μg/mL(COX - 2),以及最有前景的选择性比率,为0.1(COX - 2/COX - 1)。TPC值和DPPH自由基清除活性的EC值与COX - 2抑制活性没有相关性。这导致人们推测其作用机制很可能不是基于清除活性氧和抗氧化活性。非洲马铃果茎皮的二乙醚提取物对大肠杆菌(MIC值:13μg/mL)、金黄色葡萄球菌(MIC值:40μg/mL)和粪肠球菌(MIC值:150μg/mL)表现出最高的生长抑制活性。本研究为大姆皮吉地区先前鉴定的药用植物的治疗用途提供了进一步的证据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/253514904031/plants-10-00351-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/9c9941c5ace1/plants-10-00351-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/f62dec02172f/plants-10-00351-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/bee6d8326e6c/plants-10-00351-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/ff42ba5b3cfc/plants-10-00351-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/95f53b65d486/plants-10-00351-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/772aa816ac38/plants-10-00351-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/253514904031/plants-10-00351-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/9c9941c5ace1/plants-10-00351-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/f62dec02172f/plants-10-00351-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/bee6d8326e6c/plants-10-00351-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/ff42ba5b3cfc/plants-10-00351-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/95f53b65d486/plants-10-00351-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/772aa816ac38/plants-10-00351-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf67/7918315/253514904031/plants-10-00351-g007.jpg

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