左旋吡喹酮、右旋吡喹酮和消旋吡喹酮的体外与体内抗不同发育期日本血吸虫的作用（英文）

中国寄生虫学与寄生虫病杂志 ›› 1998, Vol. 16 ›› Issue (5): 335-341.

左旋吡喹酮、右旋吡喹酮和消旋吡喹酮的体外与体内抗不同发育期日本血吸虫的作用（英文）

肖树华¹; 尤纪青¹; 梅静艳¹; 胡玉琴¹; 周德涵¹; Brian A. Catto ²

中国预防医学科学院寄生虫病研究所

收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:1998-10-31 发布日期:1998-10-31

IN VITRO AND IN VIVO EFFECT OF LEVOPRAZIQUANTEL, DEXTROPRAZIQUANTEL VERSUS RACEMIC PRAZIQUANTEL ON DIFFERENT DEVELOPMENTAL STAGES OF SCHISTOSOMA JAPONICUM

Xiao Shuhua ¹; You Jiqing ¹; Mei Jinyan¹; Hu Yuqin ¹; Zhou Dehan ¹; Brian A.
Catto ²

1 Institute of Parasitic Diseases; Chinese Academy of Preventive Medicine; WHO Collaborating Center for Malaria; Schistosomiasis and Filariasis; Shanghai 200025, China 2　Hospital Epidemiology/Infectious Diseases Section, Veterans Administration Medical Center/Medical College of Georgia, Augusta, Georgia 30912

Received:1900-01-01 Revised:1900-01-01 Online:1998-10-31 Published:1998-10-31

摘要/Abstract

摘要： 目的：测定消旋吡喹酮（Ｐｒａ）、左旋吡喹酮（Ｌ－Ｐｒａ）和右旋吡喹酮（Ｄ－Ｐｒａ）对不同发育期日本血吸虫的作用。方法：用含２０％小牛血清的ＰＲＭＩ１６４０培养不同发育期的血吸虫，测定上述三种药物的体外抗血吸虫作用。体内试验系于小鼠感染血吸虫尾蚴后不同时间灌服（ｉｇ）Ｐｒａ、Ｌ－Ｐｒａ或Ｄ－Ｐｒａ，根据残留平均虫数评估药效。结果：依据药物引起虫的皮层损害程度，虫龄为２８ｄ（ｄ２８）和３５ｄ（ｄ３５）的成虫对Ｌ－Ｐｒａ最敏感，而１４ｄ（ｄ１４）童虫则最不敏感。在药物浓度为０．１－１μｇ／ｍｌ时，Ｌ－Ｐｒａ的抗血吸虫作用较Ｐｒａ的为强，即使Ｌ－Ｐｒａ的浓度减至Ｐｒａ最低有效药浓度的１／２亦有效。在体外，上述浓度的Ｄ－Ｐｒａ对不同发育期血吸虫无明显作用。感染小鼠ｉｇ单剂量的Ｌ－Ｐｒａ，Ｐｒａ或Ｄ－Ｐｒａ３００ｍｇ／ｋｇ或５００ｍｇ／ｋｇ，仅前２种药物对３ｈ（ｄｏ）、２１ｄ（ｄ２１）童虫和ｄ２８及ｄ３５成虫有较明显的疗效，而对３ｄ（ｄ３）、７ｄ（ｄ７）和ｄ１４童虫的疗效甚差或无效。与Ｌ－Ｐｒａ和Ｐｒａ相比，Ｄ－Ｐｒａ仅对ｄ３５成虫有较差的疗效。感染ｄ３５血吸虫成虫的小鼠用Ｌ－Ｐｒａ１５０ｍｇ／ｋｇｉｇ治疗，其疗效与用Pra 300mg/kg 治疗的相仿。D-Pra 的总剂量增至L -Pra 的2—6 倍时亦仅示很差的疗效。结论: 在消旋Pra 中,L-Pra 是抗血吸虫的活性成分。

关键词: 日本血吸虫, 对映体, 吡喹酮, 左旋吡喹酮, 右旋吡喹酮, 疗效

Abstract: AIM: To compare the antischistosomal effect of racemic praziquantel (Pra) and its
enantiomers, levopraziquantel (L Pra) and dextropraziquantel (D Pra), on different developmental
stages of Schistosoma japonicum. METHODS: The in vitro effects of the drugs were determined in
different stages of schistosomes maintained in RPMI 1640 supplemented with 20% calf serum. In
vivo study mice infected with schistosome cercariae were treated intragastrically (ig) with Pra,
L-Pra or D-Pra at different intervals after infection. The efficacy of the drugs was evaluated by residualmean worm number. RESULTS: Based on the degree of tegument damage induced by L-Pra, d28 and d35 schistosomes were most susceptible to L-Pra, while d14 schistosomules being least susceptible. At comparable concentrations of 0.1- 1 g/ml, L-Pra was more active than Pra even when the concentration of L-Pra was reduced to one-half of the minimum effective concentration Of Pra. At above-mentioned concentrations D-Pra exhibited no apparent in vitro effect on different stages of schistosomes. When infected mice were treated ig with L-Pra, Pra or D-Pra at a single dose of 300mg/kg or 500 mg/kg, only the former two drugs showed apparent effect on d0, d21, d28 and d35 schistosomes and less or much less effect on d3, d7 and d14 schistosomules. D-Pra only exhibited a negligible effect on d35 adult schistosomes as compared with L-Pra and Pra. When mice infected with d35 adult schistosmes were treated ig with L-Pra 150 mg/kg, the efficacy was similar to that of mice treated with Pra 300 mg/kg. CONCLUSION: L-Pra is the principal active component against schistosomes in racemic Pra.

Key words: Schistosoma japonicum, enantiomer, praziquantel, levopraziquantel, dextropraziquantel, therapeutic effect

肖树华;尤纪青;梅静艳;胡玉琴;周德涵;BrianA.Catto. 左旋吡喹酮、右旋吡喹酮和消旋吡喹酮的体外与体内抗不同发育期日本血吸虫的作用（英文）[J]. 中国寄生虫学与寄生虫病杂志, 1998, 16(5): 335-341.

XiaoShuhua;YouJiqing;MeiJinyan;HuYuqin;ZhouDehan;BrianA.Catto. IN VITRO AND IN VIVO EFFECT OF LEVOPRAZIQUANTEL, DEXTROPRAZIQUANTEL VERSUS RACEMIC PRAZIQUANTEL ON DIFFERENT DEVELOPMENTAL STAGES OF SCHISTOSOMA JAPONICUM[J]. Chinese Journal of Parasitology and Parasitic Diseases, 1998, 16(5): 335-341.

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