Neferine methylIt is a dibenzyl isoquinoline alkaloid derived from the embryo of the mature seed of lotus in the family Nymphaeaceae. Many experiments have proved that neferine is an effective calcium antagonist. It can antagonize calmodulin, inhibit calcium ion and magnesium ion ATPase, and have significant cardiovascular effects such as anti arrhythmia, anti hypertension, anti platelet aggregation, etc. It was found that neferine could react with phosphorylated cholinesterase to reactivate phosphorylated cholinesterase inhibited by organophosphorus. Anticholinergic drugs and phosphorylated cholinesterase reactivators are effective drugs for the treatment of organophosphorus pesticide poisoning and organophosphorus nerve agent poisoning. Atropine had no effect on the nicotine like symptoms caused by organophosphorus poisoning, and could not be the reactivation of phosphatidylcholinesterase. Phosphated cholinesterase reactivators can alleviate nicotine like symptoms and restore the original structure and activity of cholinesterase.
Before the complete "aging" of phosphorylated esterase, neferine may have a stronger force than chlorphosphine to pull down the phosphoryl group from the toxic enzyme and enable it to recover its energy. Moreover, the inhibitory effect of neferine on phosphatidyl cholinesterase reactivation by organophosphorus is incomparable to atropine, which shows the difference in the mechanism of their anti organophosphorus pesticide poisoning. The existing phosphating cholinesterase reactivators are mainly pyridine aldoxime compounds, such as chlorphosphine, phosphine and so on. However, phosphine cholinesterase reactivators still have problems that can not be solved, such as sufficient use may inhibit respiration. Even the optimal dose of atropine and chlorophosphamide can only increase the LD50 of organophosphorus poisoned mice by 45%. Therefore, it is necessary to try to find new drugs to introduce new mechanisms of action. When we reduce the effective dose by half, the combined application of lotus base and atropine, its protective effect is particularly prominent. Therefore, it is necessary to further study that neferine has a strong central effect and rapidly restore the activity of phosphatidylcholinesterase.
As a kind of effective antidote for organophosphate poisoning, neferine has obvious effect, and its phosphating cholinesterase reactivation is even higher than that of chlorphenidine. However, atropine is still an important drug in the treatment of organophosphorus poisoning. If neferine, etc. are reasonably combined with neferine, give play to their respective characteristics and complement each other, it is possible to provide a more effective combination antidote for the rescue of this kind of poison poisoning.