Molluscicidal activity and physiological toxicity of quaternary benzo[c]phenanthridine alkaloids (QBAs) from Macleaya cordata fruits on Oncomelania hupensis.

Schistosomiasis is a serious worldwide parasitic disease. One of the best ways to control schistosomiasis is to control the population of Oncomelania hupensis snails. We sought to identify a high-efficiency biogenic molluscicide against Oncomelania with low toxicity, to avoid chemical molluscicide contamination and toxicity in aquatic organisms. We extracted quaternary benzo[c]phenanthridine alkaloids (QBAs) from Macleaya cordata fruits. Molluscicidal activity of the QBAs against Oncomelania was determined using bioassay. Our results showed that the extracted QBAs had a strong molluscicidal effect. In treatment of O. hupensis with QBAs for 48 h and 72 h, the lethal concentration (LC50) was 2.89 mg/L and 1.29 mg/L, respectively. The molluscicidal activity of QBAs was close to that of niclosamide (ethanolamine salt), indicating that QBAs have potential development value as novel biogenic molluscicides. We also analyzed physiological toxicity mechanisms by examining the activity of several important detoxification enzymes. We measured the effect of the extracted QBAs on the activities of glutathione S-transferase (GST), carboxylesterase (CarE), acid phosphatase (ACP), and alkaline phosphatase (AKP) in the liver of O. hupensis. We found that the effects of QBAs on detoxification metabolism in O. hupensis were time and concentration dependent. The activities of GST, CarE, AKP, and ACP in the liver of snails increased significantly in the early stage of treatment (24 h), but decreased sharply in later stages (120 h), compared with these activities in controls. GST, CarE, AKP, and ACP activity in the liver of snails treated with LC50 QBAs for 120 h decreased by 62.3%, 78.1%, 59.2%, and 68.6%, respectively. Our results indicate that these enzymes were seriously inhibited by the extracted QBAs and the detoxification and metabolic functions of the liver gradually weakened, leading to poisoning, which could be the main cause of death in O. hupensis snails.

Molluscicidal activity and physiological toxicity of Macleaya cordata alkaloids components on snail Oncomelania hupensis.

In order to search new local plant molluscicides for the control of the vectors of schistosomiasis, leaves of Macleaya cordata (Willd) R. Br. were used to extract and separate alkaloid components by thinner acid method and column chromatography, and the molluscicidal effect of alkaloid components against snail Oncomelania hupensis was determined by bioassay. The results showed that 7 alkaloid components (AN1-7) were obtained after extracting and separating alkaloids from the leaves of M. cordata, where AN2 was found being the most toxic against snail O. hupensis with 48h LC50 and LC90 values of AN2 of 6.35mg/L and 121.23mg/L, respectively. Responses of some critical enzymes to AN2, including activities of Alkaline phosphatase (ALP), Alanine aminotransferase (ALT), Aspartate transaminase (AST), Malic dehydrogenase (MDH) and Succinate dehydrogenase (SDH) in both cephalopodium and liver, were also detected through experiments, which also explored esterase isozyme (EST) exposed to AN2 in liver tissue. The results showed that AN2 significantly inhibited the activities of SDH, MDH and esterase isozyme, as AN2 significantly stimulated the activities of ALP, ALT and AST to increase at a low concentration (e.g. 25mg/L), while significantly inhibited the activities of these enzymes at a high concentration (100mg/L). These results indicated that AN2 not only inhibited protein synthesis, and respiratory chain oxidative phosphorylation, but also caused hepatocellular injury and reduced the detoxification ability of liver.