Pharmacodynamic Evaluation And Material Basis Study Of Anti-tumor Activity Of Miao Medicine-prionobelum Qianensis

Prionobelum qianensis,a dry whole insect of the genus Prionobelum of the genus zema family?Zephroniidae?,perched on the wet side of the hillside,under withered branches,saprophytes or stones,mainly distributed in Guizhou,Yunnan and Sichuan provinces.It is recorded in books such as Chinese Herbal-Herbal Medicine Volume and Guizhou Miao Medicine Research and Development.P.qianensis is medicinal insect,with the effect of dispelling wind and activating blood,dispersing blood stasis and relieving pain,mainly used to treat rheumatism arthralgia,vein clonus,falling injury and fracture swelling and so on.P.qianensis are more effective in anti-tumor,especially in the Miao area of Guizhou province.In the past,it have not been reported on fundamental studies of pharmacology and efficacy in anti-tumor on the substance of P.qianensis around the world.Therefore,the activities of the acute toxicity,material basis and anti-tumor in vitro/vivo were studied in this paper.The main results are as follows:1. Study on anti-tumor activity of P.qianensis in vitroWe conducted drug activity screening on three cancer cell lines?NCI-H1650,OVCAR3,MKN45?,using the MTT method and found that PQ-T3 had the best anticancer activity;On this basis,we extracted the PQ-T3 drug to obtain the ethyl acetate part?PQ-EA?,n-butanol part?PQ-NB?and jelly liquid?PQ-PW?.Using the MTT method,we found that PQ-EA has better anti-tumor activity;Based on this result,we calculated the IC₅₀ values of the PQ-EA drugs on the three cancer cell lines,which were 276.41,235.75,and 48.79?g·m L^-1respectively,and the drug concentration showed a dose-dependent inhibition of the proliferation to the three cancer cell lines.2. Study on anti-tumor activity of P.qianensis in vivoWe established a nude mouse model of human gastric cancer cell line MKN45 invivo,and selected PQ-EA as the test drug for the experiment,and investigated the relative tumor volume and relative tumor inhibition rate of nude mice in each group.The results showed that the drug-administration group had a good effect on inhibiting tumor growth.The inhibition rates of the high,medium,and low-dose groups were45.86%,40.80%,and 35.74%,respectively,and the drug concentration showed an obvious inhibition trend from low to high-dose groups.3. Acute toxicity test of P.qianensisPre-experiment:We investigated the acute toxicity of the drugs PQ-T3 and PQ-EA,and gave a single gavage to observe the changes in the signs of mice in each group within 14 days after administration.The results showed that none of the mice in the drug group died,and the maximum tolerance test was conducted.Maximum Tolerance Test:We conducted toxicity evaluation through investigate the mice blood routine,biochemical indexes,organ index,pathological morphology sections of main organs,etc.The results showed that the P.qianensis have low toxicity because of the drugs PQ-T3 and PQ-EA are less toxic to mice.4. Basic research on the material of P.qianensisWe carried out the separation and purification of the ethyl acetate active site?PQ-EA?of P.qianensis,which is based on the previous work?in vitro/in vivo antitumor activity?.In the end,10 pure compounds were obtained,but only the structure of PQ-1 monomer was analyzed because of instrument conditions and time constraints,the remaining compounds could not be further purified and structured.