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从加拿大药用植物杜松中提取的抗分枝杆菌天然产物。

Anti-mycobacterial natural products from the Canadian medicinal plant Juniperus communis.

机构信息

Department of Biology, University of New Brunswick, Saint John, New Brunswick, Canada E2L 4L5.

出版信息

J Ethnopharmacol. 2012 Sep 28;143(2):695-700. doi: 10.1016/j.jep.2012.07.035. Epub 2012 Aug 1.

DOI:10.1016/j.jep.2012.07.035
PMID:22877928
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Common juniper, Juniperus communis, is amongst the plants most frequently used by the indigenous peoples of North America for medicinal purposes. The First Nations of the Canadian Maritimes use infusions of juniper primarily as a tonic and for the treatment of tuberculosis. Previous investigations of extracts derived from the aerial parts of J. communis have shown it to possess anti-mycobacterial activity. The aim of the study is to isolate and identify anti-mycobacterial constituents from the aerial parts of J. communis.

MATERIALS AND METHODS

Methanolic extracts of J. communis needles and branches were subjected to bioassay guided fractionation using the microplate resazurin assay (MRA) to assess inhibitory activity against Mycobacterium tuberculosis strain H37Ra. The anti-mycobacterial constituents were identified by NMR, MS and polarimetry.

RESULTS

The diterpenes isocupressic acid and communic acid and the aryltetralin lignan deoxypodophyllotoxin were isolated from the J. communis extract. Isocupressic acid and communic acid (isolated as an inseparable 3:2 mixture of cis and trans isomers) displayed MICs of 78 μM and 31 μM and IC(50)s of 46 μM and 15 μM against M. tuberculosis H37Ra respectively. Deoxypodophyllotoxin was less active, with a MIC of 1004 μM and an IC(50) of 287 μM.

CONCLUSIONS

Isocupressic acid, communic acid and deoxypodophyllotoxin were identified as the principal constituents responsible for the anti-mycobacterial activity of the aerial parts of J. communis. Although further research will be required to evaluate the relative activities of the two communic acid isomers, this work validates an ethnopharmacological use of this plant by Canadian First Nations and Native American communities.

摘要

民族药理学相关性

在北美原住民用于药用的植物中,最为常见的植物之一是刺柏,刺柏属。加拿大沿海地区的第一民族主要使用刺柏的浸剂作为滋补品和治疗肺结核的药物。此前对刺柏地上部分提取的研究表明,其具有抗分枝杆菌活性。本研究的目的是从刺柏地上部分中分离和鉴定具有抗分枝杆菌活性的成分。

材料与方法

采用微量板-resazurin assay(MRA)法对刺柏针和枝的甲醇提取物进行生物活性导向分离,以评估其对结核分枝杆菌 H37Ra 株的抑制活性。通过 NMR、MS 和旋光法鉴定抗分枝杆菌成分。

结果

从刺柏提取物中分离得到二萜化合物异土木香酸和土木香酸以及芳基四氢萘木脂素脱氧鬼臼毒素。异土木香酸和土木香酸(以顺式和反式不可分离混合物的形式分离)对 M. tuberculosis H37Ra 的 MIC 分别为 78 μM 和 31 μM,IC50 分别为 46 μM 和 15 μM。脱氧鬼臼毒素的活性较低,MIC 为 1004 μM,IC50 为 287 μM。

结论

异土木香酸、土木香酸和脱氧鬼臼毒素被鉴定为刺柏地上部分具有抗分枝杆菌活性的主要成分。尽管还需要进一步研究来评估两种土木香酸异构体的相对活性,但这项工作验证了加拿大第一民族和美洲原住民社区对这种植物的民族药理学用途。

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