An artemisinin derivative of praziquantel as an orally active antischistosomal agent.
BACKGROUND
Schistosomiasis is a major health problem in tropical and sub-tropical areas caused by species of trematode belonging to the genus Schistosoma. The treatment and control of this disease has been relying on the use of a single drug praziquantel. However, the drug resistance concern urged the development of new drugs against schistosoma. Here, we report our systematic biological evaluation of DW-3-15, a new lead compound developed based on our conjugation design rationale as an effective anti-schistosomal agent.


RESULTS
The antischistosomal activity of DW-3-15 was systematically evaluated in S. japonicum infected mouse model for its stage-sensitivity and dose response. The results revealed that DW-3-15 exhibited 60-85% worm reduction rate against different development stage of worm. Scanning electron microscopy (SEM) observation indicated that DW-3-15 may damage to the tegument of male schistosomes.


CONCLUSIONS
Our results demonstrated that DW-3-15 showed potent anti-schistosomal activities in vivo. The results strongly support our conjugation design strategy of artemisinin analogs and further development of DW-3-15 as a new lead compound as anti-schistosomal agent.
College of Medical Science, Soochow University, Suzhou, China.
Lanlan
L
Dong
College of Medical Science, Soochow University, Suzhou, China.
Wenwen
W
Duan
College of Medical Science, Soochow University, Suzhou, China.
Jinglei
J
Chen
College of Medical Science, Soochow University, Suzhou, China.
Huan
H
Sun
College of Medical Science, Soochow University, Suzhou, China.
Chunhua
C
Qiao
College of Medical Science, Soochow University, Suzhou, China.
Chao-ming
CM
Xia
D000284:Administration, Oral; D000818:Animals; D037621:Artemisinins / Q000627:therapeutic use*; D004195:Disease Models, Animal; D005260:Female; D051379:Mice; D008813:Mice, Inbred ICR; D011223:Praziquantel / Q000627:therapeutic use*; D012554:Schistosomiasis japonica / Q000188:drug therapy*; D012556:Schistosomicides / Q000627:therapeutic use*
D037621:Artemisinins; D012556:Schistosomicides; D011223:Praziquantel; C031327:artemisinin