不同药用辅料对人α防御素5抗菌活性影响的单因素实验研究  

Single factor experiments of different excipients on antibacterial effect of human α-defensin 5

作　　者：周小林[1,2] 王成[1] 申明强[1] 陈默[1] 贺赐安[1] 王军平[1] 

机构地区：[1]第三军医大学军事预防医学院防原医学教研室,全军复合伤研究所,创伤,烧伤与复合伤国家重点实验室 [2]第三军医大学基础部外科应用解剖与手术学教研室,重庆400038

出　　处：《局解手术学杂志》2013年第4期345-348,共4页Journal of Regional Anatomy and Operative Surgery

基　　金：国家自然科学基金资助项目(30771892;81271898);全军"十二"后勤科研重点项目(NO.BWS11J009)

摘　　要：目的探索单种药用辅料不同浓度条件下对人α防御素5(HD5)抗菌活性的影响,为后期新药制剂配方的研制提供实验依据。方法采用抗菌实验平板计数法,分析不同浓度HD5的抗菌活性,然后选择不同浓度甘油、蔗糖、NaCl、吐温80、羟丙基-β-环糊精(HP-β-CD)、尼泊金甲酯钠作为候选辅料,以含有各浓度不同辅料添加HD5多肽作为实验组,以各浓度辅料的未添加HD5作为对照组,其中将未添加HD5和辅料的对照组称为空白对照组。计数平板菌落数,以抑菌率作为响应值,从而选择适宜的辅料种类和浓度范围。结果与单纯HD5多肽相比,分别单独加入浓度大于0.29%的NaCl和10%以上的(HP-β-CD),HD5的抑菌率明显下降(P<0.05),而单独加入设定浓度的甘油、蔗糖、吐温80、HP-β-CD和尼泊金甲酯钠均不会显著影响HD5的抑菌率,但是由于较高浓度的甘油、吐温80和尼泊金甲酯钠本身具有显著抑菌活性,所以在较高浓度时无法判断它们是否影响了HD5的抗菌活性,因此在选取浓度时要注意区分抑菌活性的主次关系。分别单独加入浓度低于10%的甘油、12%的蔗糖、0.5%的吐温80、5%的HP-β-CD和0.5%的尼泊金甲酯钠均不会显著影响HD5的抗菌活性。结论在一定浓度范围内,甘油、蔗糖、吐温80、HP-β-CD和尼泊金甲酯钠不会影响HD5的抗菌活性,可作为HD5的备选辅料。Objective To explore the effect of antibacterial activity of single medicinal materials under different concentrations on hu- man a-defensin 5 （ HD5）, and to provide the experimental basis for the development of new drug formulations. Methods Antibacterial activity of different concentrations of HD5 was analyzed with plate colony-counting method. Different concentrations of glycerol, sucrose, NaC1, Tween 80,hydroxypropyl-β-cyclodextrin（ HP-β-CD）, methyl paraben sodium combined different concentration of excipients with HD5 polypeptides were regarded as experiment group,while the control group was with no HD5. Number of bacteria colonies was counted with plate colony-counting methods. According to the inhibitory rate, the suitable type and dosage of the excipients and range of concentration were selected. Results Compared with HD5 polypeptide,the inhibitory rate HD5 was significantly decreased with more than 0.29% of NaC1 and more than 10% HP-β-CD（P 〈 0.05）. The overall inhibitory rate did not change obviously with set concentration of HD5. However, the antimicrobial activity of high concentrations of glycerol, sucrose,Tween 80, HP-β-CD and methyl paraben sodium was unable to determine that if antimicrobial activity of HD5 had changed or not. The concentration with less than 10% of glycerin,less than 12% of sucrose,less than 0.5% of Tween 80, less than 5% of HP-β-CD and less than 0.5% of methyl paraben sodium may not affect the antibacterial activity of HD5. Conclusion In the certain concentration range, glycerin, sucrose, Tween 80, HP-β-CD and methyl paraben sodium may not affect the antibacterial activity of HD5, those can be alternative excipients.

关 键 词：人α防御素5 辅料 抗菌活性 单因素实验 

分 类 号：R945[医药卫生—微生物与生化药学] R978.16[医药卫生—药剂学]