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从非洲豆蔻中分离出的二萜类化合物对大肠杆菌、单核细胞增生李斯特菌和金黄色葡萄球菌的体外杀菌活性。

In vitro bactericidal activity of diterpenoids isolated from Aframomum melegueta K.Schum against strains of Escherichia coli, Listeria monocytogenes and Staphylococcus aureus.

机构信息

Institute for Global Food Security, Queen's University Belfast, Belfast, United Kingdom.

Institute for Global Food Security, Queen's University Belfast, Belfast, United Kingdom.

出版信息

J Ethnopharmacol. 2014 Feb 12;151(3):1147-1154. doi: 10.1016/j.jep.2013.12.035. Epub 2013 Dec 27.

DOI:10.1016/j.jep.2013.12.035
PMID:24378352
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The ethnobotanical use of Aframomum melegueta in the treatment of urinary tract and soft tissue infection suggested that the plant has antimicrobial activity.

MATERIALS AND METHODS

To substantiate the folkloric claims, an acetone, 50:50 acetone:methanol and 2:1 chloroform:methanol extracts were tested against Escherichia coli K12; acetone extract and the fractions of acetone extracts were tested against Listeria monocytogenes. Bioassay-guided fractionation was performed on the extract using L. monocytogenes as the test organism to isolate the bioactive compounds which were then tested against all the other organisms.

RESULTS

Four known labdane diterpenes (G3 and G5) were isolated for the first time from the rhizomes of A. melegueta and purified. These were tested against E. coli, L. monocytogenes, methicillin resistant Staphylococus aureus (MRSA) and S. aureus to determine antibacterial activity. The result showed that two compounds G3 and G5 exhibited more potent antibacterial activity compared to the current clinically used antibiotics ampicillin, gentamicin and vancomycin and can be potential antibacterial lead compounds. The structure of the labdane diterpenes were elucidated using nuclear magnetic resonance (NMR) spectroscopy and Mass spectrometry. A possible mode of action of the isolated compound G3 and its potential cytotoxicity towards mammalian cells were also discussed.

CONCLUSION

The results confirmed the presence of antibacterial compounds in the rhizomes of A. melegueta with a favourable toxicity profile which could be further optimized as antibacterial lead compounds.

摘要

民族药理学相关性

阿福花科植物 Amomum melegueta 在治疗尿路感染和软组织感染方面的民间应用表明,该植物具有抗菌活性。

材料和方法

为了证实民间传说,我们测试了丙酮、50:50 丙酮:甲醇和 2:1 氯仿:甲醇提取物对大肠杆菌 K12 的抗菌活性;测试了丙酮提取物和丙酮提取物的馏分对单核细胞增生李斯特菌的抗菌活性。使用单核细胞增生李斯特菌作为测试生物,对提取物进行生物活性导向分离,以分离出活性化合物,然后对所有其他生物进行测试。

结果

首次从阿福花科植物的根茎中分离出四种已知的贝壳杉烷二萜(G3 和 G5)并进行了纯化。这些化合物被测试了对大肠杆菌、单核细胞增生李斯特菌、耐甲氧西林金黄色葡萄球菌(MRSA)和金黄色葡萄球菌的抗菌活性。结果表明,两种化合物 G3 和 G5 的抗菌活性比目前临床上使用的抗生素氨苄西林、庆大霉素和万古霉素更强,可能是潜在的抗菌先导化合物。利用核磁共振(NMR)光谱和质谱法阐明了贝壳杉烷二萜的结构。还讨论了分离化合物 G3 的可能作用机制及其对哺乳动物细胞的潜在细胞毒性。

结论

研究结果证实了阿福花科植物根茎中存在具有良好毒性特征的抗菌化合物,可进一步优化为抗菌先导化合物。

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