摘要
通过磺酸化、卤化、酯化、乙酰化等途径对橘皮素进行结构改造后得到 8种新衍生物 :橘皮素磺酸取代物 - 1、橘皮素磺酸取代物 - 2、橘皮素溴取代物 - 1、橘皮素溴取代物 - 2、橘皮素碳酸酯、橘皮素甲基酮 - 1、橘皮素甲基酮 - 2、橘皮素乙酰酯。并对这 8种衍生物进行了离体兔耳痒螨药效筛选试验 ,结果除磺酸取代物 - 1无杀螨作用外 ,另 7种都具有较强的杀螨作用 ,其中橘皮素乙酰酯作用最强。将橘皮素乙酰酯制成乳浊液作药效试验 ,在 0 .1%、0 .0 5%和 0 .0 2 %浓度时 ,分别在 2～ 5min、3～ 6min和 8～ 10 min内将被试螨虫全部杀死 ,杀螨效力强于橘皮素 ,与螨净、双甲脒相近 ;将其制成 1%的擦剂 ,两次滴耳、涂擦治疗 2 5只耳痒螨感染病兔和 4 75只耳痒螨感染病狐 ,两周后治愈率达 96.5% ;将其制成 50 %的乳油 ,再稀释至 0 .0 5%和 0 .0 2 5%的浓度 ,间隔1周 ,药浴两次治疗 172只和 132只两群螨虫感染病羊 ,两周后 ,治愈率分别达到 99%和 98% ,优于同期药浴的辛硫磷对照组 ,且无任何异常现象发生。橘皮素乙酰酯毒性试验结果表明 :其小鼠腹腔注射 LD50 为 2 50 .0 3mg/kg,口服给药 L D50 分别为 182 1.2 8mg/kg(溶剂为玉米油时 )和 LD50 为 2 4 99.19mg/kg(溶剂为吐温 - 2 0时 ) ,对兔皮肤急性毒性大于
The chemical structure of Tangeretin were modified by sulfonylation, halogenation, acetylation and so on. Eight derivates of Tangeretin were obtained from above methods. Thus the pharmacodynamical screening test on rabbit ear itch mite in vitro was started The result showed that seven derivates of Tangeretin but sulforic acid derivates Tangeretin 2 had better action of killing itch mite. The best one was acetate derivate of Tangeretin. At concentration 0.1%, 0.05% and 0.02%, acetate derivate of Tangeretin could kill all rabbit ear itch mite in 2～5 min, 3～6 min and 8～10 min respectively in vitro. Its effect was superior to that of Tangeretin, and was similar to that of dimplate and amitraze. 1% linimentum of acetate derivate of Tangeretin had 96.5% per cent cure rate on 25 rabbits and 475 foxes suffered from ear itch mite by smearing ear two times. With 0.05% and 0.025% emulsion of acetate derivate of Tangeretin treating 172 and 132 sheep infected with itch mite separately by two times dipping, its cure rates were 99% and 98% respectively after 2 weeks, and abnormal reaction was not found.
出处
《中国兽医杂志》
CAS
北大核心
2000年第12期5-8,共4页
Chinese Journal of Veterinary Medicine
基金
"九五"国家科技攻关项目 !编号 :96 - 0 0 5 -0 2 - 0 4- 0 6
关键词
橘皮素
结构改造
橘皮素乙酰酯
杀螨药物
兽药
Tangeretin
structure modification
Tangeretin acetate
pharmacodynamic
