【作者】 李秀义；

【导师】 王玲；

【作者基本信息】 昆明医学院 ， 病原生物学， 2007， 硕士

【摘要】 目的：探讨几种植物多糖衍生物和镧系化合物在体外抗HIV和其它性传播疾病病原体活性的研究。方法：我们采用了三种体外抗HIV-1活性的研究方法（合包体形成抑制试验、MTT比色法和定量p24抗原ELISA检测）对几种天然多糖的衍生物和镧系化合物进行了较为系统的研究；同时采用空斑形成法对抗HSV活性和改良的MTT比色法对抗白色念珠菌活性进行了研究。结果：植物多糖衍生物821A和821B对HIV-1X₄(HIV-1_ⅢB)株有较高的活性，50％的有效抑制浓度(IC₅₀)分别为1.88±0.18μg／ml和2.10±0.28μg／ml，SI值为＞1340.84和＞1203.37；抗HIV-1R₅株(HIV-1_BaL)的IC₅₀值分别为5.90μg／ml和7.40μg／ml，SI值分别为＞678.00和＞540.50；对HSV-1的IC₅₀各为21.41±3.38μg／ml和23.74±3.81μg／ml，SI值各为＞237.21和＞214.67；对HSV-2的IC₅₀各为26.42±1.59μg／ml和18.98±6.79μg／ml，SI值各为＞189.74和＞284.23。多糖衍生物LD对HIV-1 X₄(HIV-1_ⅢB)的IC₅₀为1.91±0.13μM，SI值为313.19；对HIV-1R₅(HIV-1_BaL)株的IC₅₀为578.90μg／ml，SI值为2.20。镧系化合物LCI、LNI、LCH和LSU对HIV-1 X₄株(HIV-1_ⅢB)的IC₅₀各为13.83±1.36μg／ml、11.13±1.88μg／ml、19.03±4.16μg／ml和14.95±1.17μg／ml，SI值各为＞279.86、233.69、127.69和45.52。为了进一步了解化合物的作用机制，我们进行了化合物阻止病毒进入细胞试验，821A、821B、LCI、LNI、LCH和LSU的抗病毒进入的IC₅₀值各为2.03±0.44μg／ml、1.81±0.86μg／ml、10.12±0.93μg／ml、20.49±7.18μg／ml、12.64±3.09μg／ml和17.09±1.50μg／ml。结论：821A、821B、LD和镧系化合物均显示较高的抗HIV活性，且821A和821B显示了较强的抗HSV的活性，是具有良好开发前景的杀微生物剂的候选化合物，值得进一步的研究。更多还原

【Abstract】 ObjectionTo study anti-HIV and -other STD pathogen activities of several polysaccharides isolatedfrom plant and lanthanides in vitro.MethodsAnti-HIV activity were detected by syncytial formation inhibition assay and quantitativeenzyme-linked immunsorbent assay（ELISA）, cytotoxicity tests were detected by MTTassay, anti-HSV activity were detected by plaque reduction assay and anti-Candidaalbicans activity analysis use an improved MT-F test.ResultsThe antimicrobial activities of several polysaccharides and lanthanides was evaluated.Polysaccharide derivatives, 821A and 821B, had high anti-HIV-1 (HIV-1_ⅢB) activities andtheir 50% inhibition concentration (IC₅₀) were 1.88±0.18μg/ml and 2.10±0.28μg/ml,and their selective index （SI） were more than 1340. 84 and 1203.37, respectively; IC₅₀ oftheir anti-HIV-1 (HIV-1_BaL) activities were 5.90μg/ml and 7. 40μg/ml and their SI weremore than 678.00 and 540.50, respectively; IC₅₀ of their anti-HSV-1 activities were21.41±3.38μg/ml and 23.74±3.81μg/ml and their SI were more than 237.21 and214.67,respectively; IC₅₀ were 26.42±1.59μg/ml and 18.98±6.79μg/ml for theiranti-HSV-2 activities and their SI were more then 189.74 and 284.23, respectively. IC₅₀of LD anti-HIV-1 (HIV-1_ⅢB) activity was 1.91±0.13μM.and its SI was 313.19; IC₅₀ was13.83±1.36μg/ml for LD anti-HIV-1(HIV-1_BaL) activity and its SI was 2.20. EC₅₀ oflanthanides （including : LCI、LNI、LCH and LSU） anti-HIV-1 (HIV-1_ⅢB) activities were 13.83±1.36μg/ml、11.13±1.88μg/ml、19.03±4.16μg/ml and 14.95±1.17μg/ml,respectively. Further more, the activities of compounds that prevent virus entry into cellwere evaluated, IC₅₀ of 821A、821B、LCI、LNI、LCH and LSU were2.03±0.44μg/ml、1.81±0.86μg/ml、10.12±0.93μg/ml、20.49±7.18μg/ml、12.64±3.09μg/ml and 17.09±1.50μg/ml, respectively.ConclusionSeveral plant polysaccharide derivatives and lanthanides showed anti-HIV-1 (HIV-1_ⅢB)activity strongly; 821A and 821B showed stronger anti-HIV-1R₅ strain and anti-HSVactivity. Lanthanides showed certainly anti-Candida albicans activity. These resultssuggest that several polysaccharides isolated from plant and lanthanides may be potentialcandidates for microbicides development.更多还原