title: Study of the efficacy of the new antischistosomal drug 10-[2-(diethylamino)ethyl]-9-acridanone-(thiazolidin-2-ylidene) hydrazone against an Egyptian strain of S. mansoni in mice.
abstract: The efficacy of 3 doses (10, 15 and 20 mg/kg) of the new antischistosomal drug Ro 15-5458 (10-[2-(diethylamino)ethyl]-9-acridanone-(thiazolidin-2-ylidene)hy drazone, CAS 092928-47-7) against an Egyptian strain of S. mansoni was studied in mice. The effect of duration of infection on the response of mice to treatment with 20 mg/kg was evaluated at 7 and 12 weeks after infection. The criteria used for the assessment of drug efficacy were: worn count and distribution in the liver and portomesenteric system, oogram changes in the small intestine, estimation of the number of ova/g stood, liver and intestine and histopathological examination of mice liver. Data revealed a dose dependent decrease in number of adult worms and number of ova/g stool, liver and intestine. A reduction of 83.6, 89.4 and 94.9% in mean number of schistosomes compared to control was recorded following treatment with 10, 15 and 20 mg/ kg of the drug, respectively. Oogram changes were more remarkable following treatment with 20 mg/kg as evidenced by complete disappearance of all immature stages. Treatment with Ro 15-5458 in a dose of 20 mg/kg resulted in complete disappearance of couples and 100% shift or worms to the live. Examination of mice liver 2 weeks post treatment revealed on changes in pathology following treatment with 10 mg/kg compared to control. Treatment with 20 mg/kg gave better results comparable to 15 mg/kg, a decreased number and size of granulomas with minimal areas of necrosis was observed. Parasitological cure was effectively achieved when treatment was initiated 7 or 12 weeks post infection. However, histopathological data revealed that the earlier the treatment the better the results.
authors.affiliation: Pharmacology Department, Theodor Bilharz Research Institute, Imbaba, Giza, Egypt.
authors.forename: A
authors.initials: A
authors.lastname: Metwally
authors.forename: A
authors.initials: A
authors.lastname: Abdel Hadi
authors.forename: E G
authors.initials: EG
authors.lastname: Mikhail
authors.forename: O
authors.initials: O
authors.lastname: Aboú Shadi
authors.forename: H
authors.initials: H
authors.lastname: Sabry
authors.forename: H
authors.initials: H
authors.lastname: el-Nahal
mesh_terms: D000166:Acridines / Q000627:therapeutic use*; D000818:Animals; D006099:Granuloma / Q000469:parasitology; D007422:Intestines / Q000469:parasitology; D008099:Liver / Q000469:parasitology; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D011169:Portal Vein / Q000469:parasitology; D012555:Schistosomiasis mansoni / Q000188:drug therapy* / Q000469:parasitology; D012556:Schistosomicides / Q000627:therapeutic use*
chemical_list: D000166:Acridines; D012556:Schistosomicides; C062730:Ro 15-5458