[The effect of gossypol, praziquantel and artemether on recombinant lactate dehydrogenase from Schistosoma japonicum].
OBJECTIVE
To detect the effect of gossypol, praziquantel and artemether on activity of the recombinant lactate dehydrogenase of Schistosoma japonicum (rSjLDH).


METHODS
Effect of gossypol (0-0.10 mmol/L), praziquantel (0-0.20mmol/L) and artemether (0-0.10 mmol/L) on the enzymatic activity of rSjLDH was detected by spectrophotometric method in standard reaction system established before, same solvent of each reagent was used as control. Results were analyzed by SPSS13.0 software.


RESULTS
Compared with the control, considerable inhibition for both reduction and oxidation reactions catalyzed by rSjLDH was observed at 0.04 mmol/L of gossypol (P < 0.01). The enzyme activities of rSjLDH for reduction and oxidation reactions were inhibited by 91.3% and 89.1% respectively at 0.1 mmol/L of gossypol, com-pared with the control (P < 0.01). To praziquantel, enzymatic activity inhibition was observed at 0.02 mmol/L for oxidation reaction and at 0.06 mmol/L for reduction reaction (P < 0.05). At 0.2 mmol/L of praziquantel, enzymatic activities were inhibited by 83.8% for reduction reaction and 72.2% for oxidation reaction respectively, than that of the control (P < 0.01). No inhibition for both reduction and oxidation reactions was observed at 0.1 mmol/L of artemether, compared with that of the control (P > 0.05).


CONCLUSIONS
Gossypol and praziquantel show a high inhibition on rSjLDH. SiLDH may be one of the molecular targets of praziquantel.
Lv
Gang
G
Department of Parasitology, Hainan Medical College, Haikou 571101, China.
Hu
Xu-chu
XC
Huang
Can
C
Xie
Hong-yan
HY
Xu
Jin
J
Chen
Shou-yi
SY
Wu
Zhong-dao
ZD
Yu
Xin-bing
XB
D000818:Animals; D000077549:Artemether; D037621:Artemisinins / Q000494:pharmacology*; D002384:Catalysis / Q000187:drug effects; D006072:Gossypol / Q000494:pharmacology*; D007770:L-Lactate Dehydrogenase / Q000235:genetics / Q000378:metabolism*; D010084:Oxidation-Reduction / Q000187:drug effects; D011223:Praziquantel / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000378:metabolism; D012549:Schistosoma japonicum / Q000201:enzymology*; D013053:Spectrophotometry
D037621:Artemisinins; D011994:Recombinant Proteins; D011223:Praziquantel; D000077549:Artemether; D007770:L-Lactate Dehydrogenase; D006072:Gossypol