In order to evaluate the moUuseicidal effect of 50% wettable power of niclosamide ethanolamine salt(WPN)combined with urea against Oncomelania snails in the field,4 g/m~2 WPN,4 g/m~2 WPN+20 g/m2 urea and 4 g/m~2 WPN+30 g/m~2 urea were used for mollusciciding with the spraying method.The results showed after 7 days,the mortality rates of snail were 74.43% for 4 g/m~2 WPN,90.32% for 4 g/m~2 WPN+20 g/m~2 urea and 94.83% for 4 g/m~2 WPN+30 g/m~2 urea,respectively.It is indicated that WPN combined with urea can improve the molluscieidal effect significantly.

OBJECTIVETo study the anti-inflammatory and analgesic activities of diethyl 1,3-dicyclohexyl-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (ZL-5010) in vivo and in vitro.

METHODSThe analgesic effect of ZL-5010 was evaluated by acetic acid-induced writhing response in mice, and the anti-inflammatory effects was assessed in mice with xylene-induced ear edema and in rats with carrageenan-induced paw edema. Mouse peritoneal exudate cells activated by bacterial lipopolysaccharides (LPS) were used to evaluate the anti-inflammatory effect of ZL-5010 in vitro. The levels of interleukin-1β (IL -1β) and tumor necrosis factor-α (TNF-α) in the cell culture supernatant were measured using enzyme-linked immunosorbent assay (ELISA).

RESULTSAt the doses of 0.25 and 0.5 mmol/kg, ZL-5010 administered by gavage once daily for 3 days significantly reduced acetic acid-induced writhing frequency and suppressed xylene-induced ear edema in mice, and alleviated paw edema induced by carrageenan in rats (P<0.05). The agent also inhibited the production of the pro-inflammatory cytokines IL-1β and TNF-α by LPS-induced mouse peritoneal exudate cells in vitro, with the statistically significant minimum effective concentrations of 10 and 20 µmol/L, respectively (P<0.05).

CONCLUSIONZL-5010 administered by gavage has anti-inflammatory and analgesic effects in mice and rats, and in mouse peritoneal exudate cell cultures, the agent also inhibits the production of the pro-inflammatory cytokines IL-1β and TNF-α.

Amino Acids, Diamino ; pharmacology ; therapeutic use ; Analgesics ; pharmacology ; therapeutic use ; Animals ; Anti-Inflammatory Agents ; pharmacology ; therapeutic use ; Cyclohexanes ; pharmacology ; therapeutic use ; Female ; Interleukin-1beta ; metabolism ; Male ; Mice ; Mice, Inbred Strains ; Pyrimidines ; pharmacology ; therapeutic use ; Rats ; Rats, Sprague-Dawley ; Tumor Necrosis Factor-alpha ; metabolism