The Anti-insecta Effect Of Statins And Pharmacokinetics In Plasma

The biosynthetic pathway of Juvenile hormones (JHs) is divided conventionally into two steps, the early step and the late step. The early step is the classical mevalonate(MVA) pathway. Mevalonic acid is an important intermediate in the biosynthesis of cholesterol and other bioactive terpenoids. 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, an important regulatory enzyme in the classical MVA pathway, catalyzes the formation of MVA from HMG-CoA. Once the bioactivity of the enzyme was inhibited, the MVA pathway would be blocked effectively. Statins is an inhibitor of HMG-CoA reductase. This inhibitor and HMG-CoA are a pair of competitive substrates to HMG-CoA reductase, and the former's inhibition is more than 10,000 times stronger than the latter's combination. According to this, Statins can block the MVA pathway, also it can obstruct The biosynthetic pathway of Juvenile hormones. So we have the new idea of inhibiting the development of insects with statins, then to prevent and control insects. The feasibility of this idea has been obtatined by a series of trails. The trails were carried on Drosophile and Hypodermosis in yaks. The results have indicated that the dose of 1μg/mL statin had an obvious effect on the growth of Drosophile and taking one dose of 100mg statin orally decreased the Hypodermosis infection ratio in yaks from 80% to 40% and infection intensity dropped from 6.8 to 2.4. These tests have shown that few doses of statins can inhibit insects' development obviously, so it can exploit as a new concept drug to anti-pests in stockbreeding, which is an independent intellectual property right and innovation. Meanwhile, a liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) method for determining Lovastatin in Beagle plasma has been developed. The calibration curve showing a direct ratio between the concentration and the peak area were obtained;coefficient of relation (r) was 0.9993,the detection limits were 0.1ng/mL;the recovery percent were between 89.87% and 106.50%.The high sensitivity and speciality are satisfied to determination of low Lovastatin concentration. The datas of preparatory plasma pharmacokinetics in beagle are important references to determine the dosage and formulation of statins as a new concept anti-pests agent. This drug will creat a new bio-technique route to control pests in livestock and poultry set.