Biological Activities Study On4-Arylcoumarins And4-Aryl-3,4-Dihydrocoumarins

Many novel biological activities were discovered from old compounds,4-arylcoumarins.4-Arylcoumarin is also named neoflavoniod and classified in flavone family, for its structural similar with flavoniod. As the physiological action of a substance was linked to its chemical composition,4-arylcoumarins with variable structural would have abundant biological activities. Since being first found in1950s, natural as well as synthetic4-arylcoumarins have drawn more attention for its broad pharmacological activities after it was first found in1950s. Such as, antimicrobial, anti-HIV, anticancer, antiprotozoal, antioxidant, anti-inflammatory etc. Twelve3,4-dihydro-4-arylcoumarins and six4-arylcoumarins numbered from a to r were tested in our studies for the purpose of finding the potential antimicrobial, anticancer, and antioxidant activities in them. The main findings are the following three aspects.The results of antimicrobial tests showed that4-arylcoumarins exhibited moderate and potent activities in Bacillus subtilis, Staphylococcus aureus and Candida albicans growth inhibition, and relatively weaker antibacterial activity in Escherichia coli. Samples n and p had a significant activity against B. subtilis, with the MIC7.3μg.mL-1and14.4μg.mL-1, respectively. Compound m (with MIC29μg.mL-1) and n (with MIC58.5μg.mL-1) earned better activity against C. albicans. While compound n and h showed strong activity on inhibiting the growth of S. aureus, MICs of them were39μg.mL-1.4-Arylcoumarins that possess two hydroxyl groups ortho to each other in the benzonoid ring, such as, e, f, g, n and p, had excellent radical scavenging properties in DPPH assay and ABTS+assay. All the reaction can reached endpoint in one minute, which similar with ascorbic acid (Vc). SNP assay was employed to evaluate the antioxidant property of4-arylcoumarins under investigation against NO. The result indicated that4-arylcoumarins with4-(3’-hydroxyl-4’-methylphenly) structural show more efficient activity than others. The EC50of o compound in NO scavenging was26.4μg.mL-1, which was better than Vc (EC50is121.9μg.mL-1) and Resveratrol (ECs0is54.6μg.mL-1).The MTT assay was used to find the cytotoxicity activity in4-arylcoumarins. The results indicated that compound i, j, n, o, p,1and r had an potential anticancer effect, for them inhibitied the proliferation of BGC-823cell line (an human stomach cancer cell). n (IC50is29.1±1.3μg.mL-1) wined the most efficient cytotoxicity activity from those compounds and it almost completely killed cells in62.5mg.L"1. In our final work, we have used injection=and oral toxicity tests to detecting the potential toxicity of4-arylcoumarins in the larvae of greater wax moth. The results showed that none of the tested4-arylcoumarins significantly affect the larvae viability. No significant mortality and antifeedant effect were indicated in the tested larvae. Base on our findings, those4-arylcoumarins may be considered as potential medicine candidates for treat cancer and some pathological conditions that were caused by free radical overproduction.