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含有熊果酸和对苯二酚的茵陈蒿甲醇植物提取物对结核分枝杆菌的抗分枝杆菌活性。

Antimycobacterial activity of methanolic plant extract of Artemisia capillaris containing ursolic acid and hydroquinone against Mycobacterium tuberculosis.

作者信息

Jyoti Md Anirban, Nam Kung-Woo, Jang Woong Sik, Kim Young-Hee, Kim Su-Kyung, Lee Byung-Eui, Song Ho-Yeon

机构信息

Department of Microbiology and Immunology, Soonchunhyang University, 8 Soonchuhyang 2-gil, Cheonan si 330-721, Republic of Korea; Department of Chemistry, Soonchunhyang University, 22 Soonchunhyang-ro, Sinchangmyeon, Asan si, Chungcheonam 336-745, Republic of Korea.

Department of Chemistry, Soonchunhyang University, 22 Soonchunhyang-ro, Sinchangmyeon, Asan si, Chungcheonam 336-745, Republic of Korea.

出版信息

J Infect Chemother. 2016 Apr;22(4):200-8. doi: 10.1016/j.jiac.2015.11.014. Epub 2016 Feb 8.

Abstract

OBJECTIVE

In order to protect against Mycobacterium tuberculosis (MTB) infection, novel drugs and new targets should be screened from the vast source of plants. We investigated the potentiality of the herbal plant of Artemisia capillaris extract (AC) against Mycobacterium tuberculosis.

DESIGN

In this study, we isolated ursolic acid and hydroquinone by bio-activity guided fractionation from the methanol extracts of AC, and tested the inhibitory effects against several strains of MTB. Anti-mycobacterial evaluation of these compounds was carried out using the MGIT™ 960 and resazurin assay. Mycobacterial morphological changes due to the treatment of these compounds were further evaluated by Transmission electron microscopy (TEM).

RESULTS

Ursolic acid (UA) and hydroquinone (HQ) inhibited the growth of both susceptible and resistant strains of M. tuberculosis. The MIC (minimum inhibitory concentration) values of both UA and HQ were 12.5 μg/ml against the susceptible strains of M. tuberculosis. Also both UA and HQ showed 12.5-25 μg/ml of MIC values against MDR/XDR MTB strains. However, against clinical strains of MTB, UA was found sensitive against those strains that are sensitive against both INH and RFP but resistant against those strains that are resistant to INH. On the other hand HQ was sensitive against all clinical strains. TEM image-analysis of the strain H37Ra after treatment with UA revealed cell wall lysis, whereas HQ-treated cells showed deformed cytoplasmic morphology.

CONCLUSION

All these results indicate that AC extracts containing UA and HQ possess promising chemotherapeutic potency against MTB for future use.

摘要

目的

为了预防结核分枝杆菌(MTB)感染,应从大量植物资源中筛选新型药物和新靶点。我们研究了茵陈蒿提取物(AC)对结核分枝杆菌的潜在作用。

设计

在本研究中,我们通过生物活性导向分级分离从AC的甲醇提取物中分离出熊果酸和对苯二酚,并测试了它们对几种MTB菌株的抑制作用。使用MGIT™ 960和刃天青测定法对这些化合物进行抗分枝杆菌评价。通过透射电子显微镜(TEM)进一步评估这些化合物处理后分枝杆菌的形态变化。

结果

熊果酸(UA)和对苯二酚(HQ)均抑制结核分枝杆菌敏感菌株和耐药菌株的生长。UA和HQ对结核分枝杆菌敏感菌株的最低抑菌浓度(MIC)值均为12.5μg/ml。此外,UA和HQ对多药耐药/广泛耐药MTB菌株的MIC值均为12.5 - 25μg/ml。然而,对于MTB临床菌株,发现UA对那些对异烟肼(INH)和利福平(RFP)均敏感的菌株敏感,但对那些对INH耐药的菌株耐药。另一方面,HQ对所有临床菌株均敏感。用UA处理后H37Ra菌株的TEM图像分析显示细胞壁裂解,而用HQ处理的细胞显示细胞质形态变形。

结论

所有这些结果表明,含有UA和HQ的AC提取物对MTB具有有前景的化疗潜力,可供未来使用。

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