Anticardiovascular Disease Agent From Insects

Insects are the largest and most diverse group of organisms. They are evolutionarily distant relations with vertebrates, plants, and microbial origin. For this reasons, the study of insects promises to reveal novel bioactive compounds. Scores of insects' extracts have been screened in the five kinds' assay system. We select three kinds' insects in the ACAT assay system and one kind of insect in the Lp-PLAi assay system to isolate and purify. The activity guided of isolation methods as the new isolation methods was used.in this project. In order to isolate small molecular compounds (organic synthesis easily), molecular filter and sepadex column were used.As inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), compounds (1, 2, 4, 5, 6, 7, 8, and 9) and two new compounds (3, 10) were isolated and purified from the solvent extracts of three insects, M. phalerate, A. parki, and P. brevitarsis, and were elucidated by their spectroscopic data analysis. Compounds 3, 10, and 6 inhibit rat liver microsomal ACAT, hACATl, and hACAT2 with IC50 values of 281, 177, 131 umol/i for 3, of 78, 43, 32 (amol/1 for 10, and of 9.6, 6.6, 8.6 |amol/l for 6, respectively. Three Lp-PLAa inhibitors (11, 12, and 13) were isolated and purified from the solvent extracte of the insect, P. cavimamis, and were elucidated by their spectroscopic data analysis.Compounds 11, 12, and 13 inhibit Lp-PLA2 with ICso values of 151, 53, and 45 umol/1, respectively. Some of isolated compounds (1, 2, 4, 5, 6, 7, 8, 9, 11, 12, and 13) have been reported to show various biological activities, as potential inhibitors of human ACAT or human Lp-PLAz were first evaluated.