Schistosomicides

Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica
Author(s): 
Tu, Z. G.
Quan, Y. Z.
Publication Title: 
Antimicrobial Agents and Chemotherapy

To determine whether artemether, a derivative of the antimalarial agent qinghaosu, is therapeutically active against Schistosoma mansoni, we determined the in vitro, in vivo, and histopathologic effects of the drug on S. mansoni worms. In vitro, toxic effects of artemether on S. mansoni were not seen at concentrations of less than 100 micrograms/ml. However, in vivo, 30 and 50% reductions in the lengths of male and female worms, respectively, were observed 14 days after treatment. By 56 days worm dimensions had returned to control values.

Author(s): 
Xiao, S. H.
Catto, B. A.
Publication Title: 
Memórias Do Instituto Oswaldo Cruz

The action of the ether of artemisinin (artemether) on Schistosoma mansoni in mice and hamsters experimentally infected with the LE strain was studied. In mice, the drug showed high schistosomicidal activity using a single intramuscular dose of 100 mg/kg/day. By the oral route, this dose showed a low activity. Mice treated with a single intramuscular dose of 200 mg/kg/day, and examined 15 days after treatment, presented 100% alteration of the oogram; when examined 45 days after treatment, the oogram was normal.

Author(s): 
Araújo, N.
Kohn, A.
Katz, N.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

Mice infected with 100 and 50 Schistosoma japonicum cercariae for 7 and 35 d respectively were treated with im artemether 100 mg.kg-1.d-1 or arteether 100 and 300 mg.kg-1.d-1 for 2 d. The mice were killed at different intervals within 28 d after medication and the livers were sectioned for histological and histochemical observations. The results showed that both artemether and arteether caused degeneration in the tegument, intestine and genital gland of the hepatic-shifted worms.

Author(s): 
Yin, J. W.
Yang, Y. Q.
Xiao, S. H.
Li, Y.
Jiang, H. J.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

Artemether (beta-methyl ether of artemisinin) first synthesized by Shanghai Institute of Materia Medica, Chinese Academy of Sciences(1), appears in colorless crystal and is more lipid-soluble than artemisinin. When artemether was given ig or im to mice infected with Schistosoma japonicum for 32-35 d at the dosage of 1/10-1/2 LD50. Its effects in the two administration routes were similar.

Author(s): 
You, J. Q.
Mei, J. Y.
Xiao, S. H.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

The first single dose of praziquantel (Pra) was given ig to mice on the day of infection with Schistosoma japonicum cercariae, or 7 d, 14 d, and 21 d after infection. Afterwards, the same dose of Pra was given once at 1-3 wk intervals for 2-3 times. The prophylactic effect was estimated by the reduction of average number of total and female worms, the number of mice without female worm, and the gross change of the liver.

Author(s): 
Xiao, S. H.
You, J. Q.
Mei, J. Y.
Jiao, P. Y.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

Artemether (Art, beta-methyl ether of artemisinin) first synthesized by Shanghai Institute of Materia Medica, Chinese Academy of Sciences, is effective against not only malaria but also schistosomiasis. When rabbits infected with Schistosoma japonicum cercariae for 7 d were treated ig with Art 10 mg.kg-1, the total worm reduction rates were 74.6-76.7%. If Art (10 mg.kg-1) was given once weekly after the first treatment for 3-4 times, the total worm reduction rate was > 98%, and most of the rabbits were free from female worms.

Author(s): 
Xiao, S. H.
You, J. Q.
Mei, J. Y.
Jiao, P. Y.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

To study the histopathological change of the liver of the hosts treated with artemether (Art) or praziquantel (Pra) in early stage after infection with Schistosoma japonicum cercariae. METHODS: Dogs infected once with schistosome cercariae were treated ig with Art 10 mg.kg-1 or Art capsule (ArtC) 15 mg.kg-1 on d 7, or praziquantel (Pra) 30-40 mg.kg-1 on d 21 after infection, followed by the repeated dosing once every 1 or 2 wk for 2-4 times.

Author(s): 
Xiao, S. H.
Yang, Y. Q.
Zhang, C. W.
You, J. Q.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

AIM: To study the effect of artemether (Art) on the tegument of schistosomes. METHODS: Mice infected with S japonicum cercariae for 7 and 35 d, or with S mansoni cercariae for 49 d were treated intragastrically with Art 200-300 mg.kg-1.d-1 for 2 d. Schistosomes were collected in groups of 2 mice at various intervals after medication for scanning electron microscopic observation. RESULTS: The tegumental changes induced by Art appeared to be similar in S japonicum and S mansoni: swelling and fusion of tegumental surfaces, vesicle formation and collapse of discoid-like sensory structures.

Author(s): 
Xiao, S. H.
Shen, B. G.
Horner, J.
Catto, B. A.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

AIM: To study the effect of artemether (Art) on the thio proteinase ("hemoglobinase", Hem) of Schistosoma japonicum. METHODS: Hem was extracted from S japonicum adults. The inhibitory effect of Art on the activity of Hem to degrade human hemoglobin (Hgb) was examined with UV-photometer at 280 nm, SDS-PAGE and scanning at 600 nm on a chromoscanner. RESULTS: Human Hgb was degraded at pH 4.0 by the Hem. The activities of Hem preincubated at 37 degrees C with Art 0.14, 1.4, and 14 mmol.L-1, were inhibited by 30.2%, 39.8%, and 45.0%, respectively.

Author(s): 
Gong, P. L.
Li, Y. L.
Feng, Y. R.

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