荜茇中的类黄酮及其他哥伦比亚药用植物对淋球菌敏感和耐药株的抗菌活性。

Antimicrobial activity of flavonoids from Piper lanceaefolium and other Colombian medicinal plants against antibiotic susceptible and resistant strains of Neisseria gonorrhoeae.

机构信息

Departments of Biology, University of Ottawa, ON, Canada.

出版信息

Sex Transm Dis. 2011 Feb;38(2):82-8. doi: 10.1097/OLQ.0b013e3181f0bdbd.

DOI:10.1097/OLQ.0b013e3181f0bdbd

PMID:20921932

Abstract

BACKGROUND

The successful treatment of Neisseria gonorrhoeae (NG) infections is increasingly problematic because of the resistance of this pathogen to multiple antimicrobial agents. This development underscores the need for new antimicrobial sources. In the current study, 21 crude methanol extracts, from 19 plants used in Colombian traditional medicine for cutaneous infections, were screened for antimicrobial activity against NG.

METHODS

Extracts were screened by disc susceptibility assay. In addition, the minimum inhibitory concentrations of active compounds from P. lanceaefolium were assayed using a panel of 26 NG strains comprising 12 antibiotic-resistant phenotypes.

RESULTS

In all, 71% of the crude extracts exhibited antibacterial activity against the antibiotic susceptible NG strain WHO V, whereas 10% of the extracts inhibited penicillinase-producing NG strain GC1-182. The crude extract of Piper lanceaefolium was the only extract to show significant activity without ultraviolet (UV) light activation. Preliminary screening identified 3 compounds in this plant possessing antimicrobial activity: the flavonoids 5,7-dihydroxyflavanone (pinocembrin), 2',4',6'-trihydroxychalcone (pinocembrin chalcone), and the prenylated benzoic acid derivative cyclolanceaefolic acid methyl ester. Pinocembrin and pinocembrin chalcone inhibited 100% of the NG panel at 64 μg/mL and 128 μg/mL, respectively, whereas cyclolanceaefolic acid methyl ester inhibited 44% of the strains at 128 μg/mL.

CONCLUSIONS

This is the first report of the antibacterial activity of Columbian plants against NG. The activity of the 2 flavonoids, pinocembrin, and pinocembrin chalcone, toward both susceptible and resistant NG strains makes them promising candidates for further research.

摘要

背景

由于淋病奈瑟菌（NG）对多种抗菌药物的耐药性，成功治疗 NG 感染的问题日益严重。这一发展凸显了寻找新抗菌药物来源的必要性。在目前的研究中，从用于治疗哥伦比亚传统医学中皮肤感染的 19 种植物中提取了 21 种粗甲醇提取物，并对其进行了针对 NG 的抗菌活性筛选。

方法

采用药敏纸片法筛选提取物。此外，还采用包含 12 种抗生素耐药表型的 26 株 NG 菌株的药敏板，对来自 P. lanceaefolium 的活性化合物的最小抑菌浓度进行了测定。

结果

所有粗提取物中有 71%对敏感的 NG 菌株 WHO V 表现出抗菌活性，而有 10%的提取物对产青霉素酶的 NG 菌株 GC1-182 有抑制作用。只有 Piper lanceaefolium 的粗提取物在没有紫外线（UV）光激活的情况下表现出显著的活性。初步筛选发现该植物中有 3 种化合物具有抗菌活性：黄酮类化合物 5,7-二羟基黄烷酮（pinocembrin）、2'，4'，6'-三羟基查耳酮（pinocembrin chalcone）和异戊烯基苯甲酸衍生物环兰石脂酸甲酯。Pinocembrin 和 pinocembrin chalcone 分别在 64 μg/mL 和 128 μg/mL 时抑制了 100%的 NG 药敏板，而 cyclolanceaefolic acid methyl ester 在 128 μg/mL 时抑制了 44%的菌株。