Inhibitory effects of clotrimazole on TNF-α-induced adhesion molecule expression and angiogenesis

Cell adhesion molecules play a pivotal role in chronic inflammation and pathological angiogenesis. In the present study, we investigated the inhibitory effects of clotrimazole (CLT) on tumor necrosis factor (TNF)-α-induced changes in adhesion molecule expression. CLT dose-dependently inhibited monocyte chemoattractant protein-1 (MCP-1), intercellular cell adhesion molecule-1 (ICAM-1), and vascular cell adhesion molecule-1 (VCAM-1) expressions in TNF-α-stimulated HT29 colonic epithelial cells. This inhibitory action of CLT correlated with a significant reduction in TNF-α-induced adhesion of monocytes to HT29 cells, which was comparable to the inhibitory effects of anti-ICAM-1 and VCAM-1 monoclonal antibodies on monocyte-epithelial adhesion. These inhibitory actions of CLT were, at least in part, attributable to the inhibition of redox sensitive NF-κB activation, as CLT inhibited TNF-α-induced ROS generation as well as NF-κB nuclear translocation and activation in HT29 cells. Furthermore, the inhibition of TNF-α-induced monocyte adhesion was also mimicked by the specific NF-κB inhibitor, pyrrolidine dithiocarbamate (PDTC). Inflammatory mediators including TNF-α have known to promote angiogenesis, which in turn further contributes to inflammatory pathology. Therefore, we additionally evaluated whether CLT modulates TNF-α-induced angiogenesis using in vivo chick chorioallantoic membrane (CAM) assay. The CAM assay showed that CLT dose-dependently attenuated TNF-α-induced angiogenesis, and the effect was correlated with decreased inflammation of the CAM tissue. In conclusion, our results suggest that CLT can inhibit TNF-α-triggered expression of adhesion molecules, ICAM-1 and VCAM-1, and angiogenesis during inflammation.     

Basic experiments with clotrimazole administered orally

Summary

A series of experiments was carried out with the antimycotic agent clotrimazole to establish MICs against a number of different yeasts and to estimate its blood levels following oral administration. Marked differences were notedbetween the MIC against A and B serotypes of Candida albicans in its yeast-like cell form, that against Type B being nearly 10-times higher than against Type A. Against the mycelial form, however, the MIC was much lower and there was little difference between the levels for the two serotypes. Clotrimazole administered in oraltabletform appearedtobepoorly absorbed, little being transferred to the blood. Urinary levels were low and large amounts of the drug were detected in the faeces. Serum levels were below MIC levels in all cases examined. Blood levels 3-times as great as those after the same dosage in tablet form were produced when clotrimazole was given in oil solution and even with 250?mg, effective blood levels were achieved and maintained.     

复方洛美沙星栓的研制与临床应用

目的 探讨洛美沙星栓研制方法和临床疗效。方法 利用稳定、刺激性等实验方法,结合药物性质和药物具体用途,确定制剂制备工艺,采用双波长法测定该栓剂的含量,并进行105例临床试验。结果 临床试验有效率达96．2％。结论 本制剂设计合理,稳定性好,可满足临床需要。     

替勃龙片联合双唑泰泡腾片治疗老年性阴道炎疗效观察

目的探讨替勃龙片联合双唑泰泡腾片治疗老年性阴道炎的临床疗效。方法选取2016年1月—2016年7月在信阳市第四人民医院接受诊治的老年性阴道炎患者90例,所有患者根据用药方案的不同分为对照组和治疗组,每组各45例。对照组每晚清洁外阴后于阴道深处置入双唑泰泡腾片,1片/次,1次/d。治疗组在对照组基础上口服替勃龙片,1片/次,1次/d。两组患者均连续治疗3个月。观察两组的临床疗效,比较两组的临床症状消失时间和生活质量。结果治疗后,对照组和治疗组的总有效率分别为77.78%、95.56%,两组比较差异有统计学意义(P0.05)。治疗后,治疗组外阴瘙痒、阴道黏膜充血和阴道分泌物消失时间明显短于对照组,两组比较差异具有统计学意义(P0.05)。治疗后,两组躯体功能、心理功能、社会功能和物质生活评分均明显升高,同组治疗前后比较差异有统计学意义(P0.05);且治疗组这些观察指标的升高程度明显优于对照组,两组比较差异具有统计学意义(P0.05)。结论替勃龙片联合双唑泰泡腾片治疗老年性阴道炎具有较好的临床疗效,可缩短临床症状消失时间,改善生活质量,具有一定的临床推广应用价值。     

乳酸杆菌制剂联合克霉唑阴道片对外阴阴道假丝酵母菌病患者的有效性分析

目的:探讨乳酸杆菌制剂联合克霉唑阴道片对外阴阴道假丝酵母菌病(VVC)患者的临床治疗效果。方法:以2017年12月至2018年12月在我院接受治疗的60例VVC患者为研究对象,按照治疗方法的不同进行分类:对照组(n=30,采用克霉唑阴道片治疗),观察组(n=30,采用克霉唑阴道片+乳酸杆菌剂),对比两组最终的治疗效果。结果:观察组症状缓解时间较对照组显著缩短(P<0.05);治疗总有效率观察组显著高于对照组(96.67%vs 66.67%)、复发率观察组显著低于对照组(3.33%vs 20.00%)(P<0.05)。结论:VVC采用乳酸杆菌制剂、克霉唑阴道片联合治疗效果显著,快速缓解了症状,降低复发率,可在临床中推广、应用。     

维生素AD滴剂联合克霉唑治疗婴儿尿布性皮炎

目的 观察应用维生素AD滴剂联合克霉唑治疗婴儿尿布性皮炎的临床疗效。方法 将我院98例婴儿尿布性皮炎患儿随机分为两组，治疗组49例，除进行一般尿布性皮炎常规处理外，用维生素AD滴剂加1％克霉唑霜外涂患处；对照组49例，保持臀部皮肤清洁干燥，皮损局部外涂氧化锌油软膏。观察两组治疗效果。结果 治疗组婴儿尿布性皮炎痊愈率、总有效率明显高于对照组（Х^2分别为27．60、12．17，P均〈0．01），两组比较差异有统计学意义。结论 应用维生素AD滴剂联合克霉唑治疗婴儿尿布性皮炎有良好效果，并无明显不良反应。     

萆薢渗湿汤联合克霉唑栓治疗复发性外阴阴道假丝酵母菌病的疗效观察

目的探讨萆薢渗湿汤联合克霉唑栓治疗复发性外阴阴道假丝酵母菌病的疗效。方法 80例外阴阴道假丝酵母菌病随机分为中西医组和西医组。两组均予以克霉唑栓放入阴道,每晚1粒,连用7d。中西医组加用中药萆薢渗湿汤口服,连用7d。结果中西医组临床总有效率为92.5%,明显优于西医组的75.0%。西医组和中西医组分别出现不良反应4例和6例,较轻,两组比较差异无统计学意义(P>0.05)。随访3个月,中西医组总复发率12.5%,明显低于西医组的32.5%(P<0.05)。结论萆薢渗湿汤联合克霉唑栓治疗复发性外阴阴道假丝酵母菌病明显优于单纯克霉唑栓,安全性较好,并能降低其复发率。