| Acquired immunodeficiency syndrome caused by human immunodeficiency virus is a serious infectious disease. Since its discovery in 1981, AIDS continues to spread around the world. UNAIDS referred to AIDS as one of the worst crises that affects global health, economic development and social stability. Although HAART therapy prolongs life period of HIV-infected persons to some extent, and improves the quality of life of those infected, it still has many disadvantages such as high cost, high toxicity and drug resistance after long-term usage.Chinese traditional herbal medicine has been widely used in the prevention and treatment of viral infectious diseases, and it has been used for nearly 30 years in AIDS treatment because of the diverse components, low cost, comparatively low toxicity, good efficacy, and little drug resistance. Therefore, more and more patients have begun to accept it.The purpose of the study is to research anti-HIV-1 components isolated and extracted from traditional Chinese medicine KA-15. Using water and different concentrations of ethanol as solvents, permeating extraction as method, traditional Chinese medicine KA-15 from different areas were extracted and crude extracts were collected. Multi-target high-throughput screening were conducted with BIAcore SPR technology. Gp41 was found as target protein and three crude extracts has better binding capacity with the target protein. CCK-8 and MAGI test results of these three extracts showed that the extract 2 is the best one. A purification column was used to concentrate active parts of the best crude extracts of medicine KA-15 against the target protein gp41, and several elutes were obtained. With the BIAcore SPR technology and MAGI test, these enriched product was screened and six enriched product N1.4, N1.5, N2.4, N2.5, N3.4 and N4.4 showed better effects in those tests. Using HPLC-MS method, these six enrichment products were analyzed in order to get the molecular weight of the obtained compounds in the effective part. Comparing the molecular weights with the data in a few databases, 14 kinds of possible active compounds were found. These 14 compounds were docked with target protein by i GEMDOCK software, compounds 13, 10, 6, 8, 12, 11, 5, 7 got higher docking score than others which suggested their potential inhibitory effects to false HIV-1. Among those compounds, 13, 10, 6, 8 have the best effects. |
