葎草黄酮凝胶的制备及其对湿疹小鼠的初步药效学评价
Preparation of Humulus scandens flavonoids gel and its preliminary pharmacodynamics in eczema mice
刘艳 1陈杨南 1伍丹情 1龙艳秋 1何宁2
作者信息
- 1. 安徽中医药大学药学院药剂系,合肥 230012
- 2. 安徽中医药大学药学院药剂系,合肥 230012;安徽省中医药科学院药物制剂研究所
- 折叠
摘要
目的 制备一种律草黄酮外用凝胶,探讨其对湿疹的治疗作用.方法 采用溶剂提取法提取葎草中的黄酮,以卡波姆940作为凝胶基质,葎草黄酮水溶液作为分散介质,甘油作为保湿剂和增稠剂,制备葎草黄酮凝胶,对凝胶的酸碱度以及体外释放率进行质量评价.采用2,4-二硝基氯苯在小鼠背后建立特异性湿疹模型,造模成功后,连续10 d小鼠背部涂抹律草黄酮凝胶.观察记录湿疹小鼠30 min内瘙痒次数和瘙痒持续时间,免疫组织化学方法检测湿疹小鼠背部皮损处PAR-2的表达,酶联免疫吸附法测定血浆白细胞介素(IL)-2和IL4的含量以及皮损组织中白三烯B4(LTB4)和白三烯C4(LTC4)的含量.结果 葎草黄酮最优提取条件为液料比20∶1,提取温度70 ℃,提取时间90 min,提取剂浓度60％乙醇,葎草黄酮得率为1.780 3％;葎草黄酮凝胶最优制备条件为卡波姆940含量为4.72％,甘油含量为15.75％,粗黄酮含量为0.79％.制备的葎草黄酮凝胶外观呈棕黄色,均匀细腻,pH范围在6～7之间,葎草黄酮凝胶中黄酮含量为3.20 mg/g,葎草黄酮凝胶48 h的体外释放率为68％.葎草黄酮凝胶显著降低了湿疹小鼠30 min内瘙痒次数与瘙痒持续时间(P＜0.01),抑制湿疹小鼠皮损中PAR-2的表达(P＜0.01),上调湿疹小鼠血浆中IL-2的表达(P＜0.01),下调血浆中IL4的表达(P＜0.01),减少皮损组织中LTB4和LTC4的表达水平(P＜0.01).结论 成功制备葎草黄酮凝胶.葎草黄酮凝胶可以通过调节机体Th1/Th2平衡、抗炎和止痒对湿疹小鼠发挥治疗作用.
Abstract
Objective To prepare a kind of Humulus scandens flavonoids gel,and explore its therapeutic effect on eczema in mice.Methods Humulus scandens flavonoids were extracted by solvent extraction method,and Humulus scandens flavonoids gel was pre-pared with carbomer 940 as gel base,Humulus scandens flavonoids aqueous solution as dispersing medium,glycerin as moisturizing agent and thickening agent.The pH and the release rate of flavonoids gel were evaluated.The atopic eczema mouse model was induced by 2,4-dinitrochlorobenzene.After the modeling,the mice were treated with Humulus scandens flavonoids gel for 10 consecutive days.Then the itching times and the duration of eczema mice within 30 min were observed and recorded,the expression of PAR-2 in the dorsal lesions of eczema mice was detected by immunohistochemical method,the contents of interleukin-2(1L-2)and IL-4 in plasma and the contents of leukotriene B4(LTB4)and leukotriene C4(LTC4)in the lesions were determined by enzyme-related immunosorbent assay.Results The optimal extraction condition of Humulus scandens flavonoids was as follows:the liquid-solid ratio of 20:1,the extraction temperature of 70 ℃,the extraction time of 90 min,and 60％ethanol,and the yield of Humulus scandens flavonoids was 1.780 3％.The optimum preparation conditions of Humulus scandens flavonoids gel were 4.72％carbomer 940,15.75％glycerin and 0.79％crude flavonoids.The prepared Humulus scandens flavonoids gel was brown in appearance,uniform and delicate,its pH was 6-7,the content of flavonoids in the gel was 3.20 mg/g,and the release rate in vitro was 68％in 48 h after gel treatment.Humulus scandens flavonoids gel significantly reduced the number and the duration of pruritus in eczema mice within 30 min(P＜0.01),inhibited the expression of PAR-2 in skin lesions of eczema mice(P＜0.01),upregulated the expression of IL-2 and downregulated the expression of IL-4 in plasma of eczema mice(P＜0.01),and decreased the expression levels of LTB4 and LTC4 in skin lesions(P＜0.01).Conclusion Humulus scandens flavonoids gel is successfully prepared and play a good therapeutic effect on eczema mice by the regulation of Th1/Th2 balance,anti-inflammatory and antipruritus.
关键词
葎草黄酮凝胶/抗炎/止痒/特应性湿疹Key words
Humulus scandens flavonoids gel/anti-inflammatory/antipruritus/atopic eczema引用本文复制引用
基金项目
安徽省研究生教育质量工程项目(省级研究生创新创业实践项目)(2022cxcysj132)
出版年
2024
国家科技期刊平台
NSTL
万方数据