新型抗结核多肽N22肽衍生物的稳定性和体外抑菌活性研究

摘要/Abstract

摘要： 目的研究多肽N22肽衍生物的稳定性以及体外抑菌活性，证实这种新型抗结核多肽的抑菌作用并且为进一步的药代动力学研究提供参考依据。方法通过高效液相色谱分析N22肽衍生物和异烟肼在37℃培养基中（PH7.2）0～6d的含量变化。采用试管二倍稀释法以及AlamarBlue法考察N22肽衍生物的体外抑菌活性。结果HPLC的实验结果表明N22肽衍生物稳定性较异烟肼差。体外抑菌实验证实N22肽衍生物对结核分枝杆菌有明显的抑制作用，最低抑菌浓度（MIC）为50μg/ml，小于异烟肼的最低抑菌浓度。同时该多肽对大肠杆菌也有抑制作用，其MIC为130μg/ml。结论N22肽衍生物在热、酸碱条件下不稳定、易降解，与对照药物异烟肼相比，N22肽衍生物体外抑菌效果较好、MIC较低，而且该多肽不仅对结核分枝杆菌有抑制作用，对大肠杆菌同样具有抑制作用。

关键词: 肽类, 抗结核药, 分枝杆菌, 结核

Abstract: Objective To study the stability and anti-microbial activity in vitro of a new polypeptide-peptide derivative N22. MethodsThe content change of the peptide derivative N22 and isoniazid(INH) in the neutral solution from 0 to 6 days at 37℃ was analyzed by HPLC. The anti-bacterial activity in vitro was detected by the 2-fold dilution assay and the AlamarBlue assay. ResultsThe Results of HPLC showed that peptide derivative N22 was more unstable than INH in the media. In vitro experiments, the peptide derivative N22 can inhibit M. tuberculosis better than INH, its minimum inhibitory concentration(MIC) was 50μg/ml. It had also the effect against E.coli, and the MIC for E.coli was 130μg/ml. ConclusionsThe peptide derivative N22 had better effect against M. tuberculosis and E.coli.

Key words: peptides, antitubercular agents, Mycobacterium tuberculosis

顾昊,徐佳佳,王鹤尧. 新型抗结核多肽N22肽衍生物的稳定性和体外抑菌活性研究[J]. 中国防痨杂志, 2009, 31(5): 287-290.

Gu Hao, Xu Jiajia, Wang Heyao. The stability and anti-mycobacterium activity of peptide derivative N22[J]. Chinese Journal of Antituberculosis, 2009, 31(5): 287-290.

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