Synthesis Of Matrine Oxime Esters Derivatives And Their Activities

Matrine is a kind of natural alkaloid extracted from active medicine plants, it has a variety of pharmacological effects in medicine, such as anti-inflammatory, anti-viral, anti-infective and anti-tumor. Since matrine exists in most Chinese herbs plants and extraction technology means are mature, so its as a quality natural alkaloid were used widely. Furthermore, matrine is also a natural botanical pesticide that its prevention and eradication of pests are multiple points, not harmful to the natural environment and not worried about residues. Therefore, matrine is a precursor compound and its structural modification has very important significance.In order to enhance the activity of matrine, bioavailability and reduce the toxicity, matrine used as the parent compound. Based on the principle of drug split, the intermediate oxime matrine was obtained by introducing tert-butyl nitrite, and its structure was modified. We designed and synthesized 23 novel structure of matrine derivatives and were identified by MS, IR,1H NMR,13C NMR.The synthesized 23 matrine derivatives were tested pesticidal and anti-tumor activity. When the concentration of matrine oxime ester derivative as 200 ppm, the spider mite has a good contact toxicity. There are 10 target compounds activity reached more than 90% and 9 target compounds closed to the control group avermectin. Aphids contact toxicity test indicated nine target compounds activity reached more than 90% which the active of the compound were quite with the control group avermectin. Discovered LHW-03、LHW-08、LHW-11、 LHW-13、LHW-16、LHW-17、LHW-18、LHW-19、LHW-22 and LHW-23 were less than 50μM by IC50, which LHW-03, LHW-17 and LHW-22 were less than 10μM,matrine activity has been significantly improved.