Eight phenyl benzoate compounds were synthesized in one step, and then their antioxidant, anti-tyrosinase, and anti-pancreatic lipase activities were evaluated in the present study. The total yields ranged from 31% to...Eight phenyl benzoate compounds were synthesized in one step, and then their antioxidant, anti-tyrosinase, and anti-pancreatic lipase activities were evaluated in the present study. The total yields ranged from 31% to 85%. Compound 4 c exhibited a stronger antioxidant activity compared with Trolox, with half maximal inhibitory concentrations(IC50) of approximately 13.06 μM, and the antioxidant mechanism was further studied using computational chemistry. Compounds 1 c–5 c exhibited minimal anti-tyrosinase activity. Compounds 4 c, 5 d, 6 c and 6 d exhibited weak anti-pancreatic lipase activity, with an inhibition rate of 33.52%, 15.76%, 18.37% and 20.77%, respectively. These results demonstrated that all compounds had reference significance, especially compound 4 c.展开更多
In the present study, we evaluated the antitumor, anti-tyrosinase, anti-pancreatic lipase, antibacterial, antifungal, and anti-α-glycosidase activities for all or a subset of 20 known compounds. They included 8 pheny...In the present study, we evaluated the antitumor, anti-tyrosinase, anti-pancreatic lipase, antibacterial, antifungal, and anti-α-glycosidase activities for all or a subset of 20 known compounds. They included 8 phenyl benzoates, 10 benzophenones, and 2 xanthones. Phenyl benzoate compounds 1–8 did not exhibit evident antitumor activity, which was consistent with existing theories. Compounds 16, 17, and 18 exhibited moderate anti-tyrosinase activity. In addition, compounds 11 and 18 exhibited moderate inhibitory activity against Candida albicans, and compound 20 exhibited stronger anti-α-glycosidase activity than quercetin, with an IC_(50)of approximately 2.45 μM. These results demonstrated that compounds 11, 16–18, and 20 were promising leads for further structural modification.展开更多
Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11%to 36%.All of the compounds were first reported.Then,the antitumor,anti-tyrosinase,anti-pancreatic lipase,antif...Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11%to 36%.All of the compounds were first reported.Then,the antitumor,anti-tyrosinase,anti-pancreatic lipase,antifungal and antibacterial activities of all or part of compounds 1–9 were evaluated.Compound 9 exhibited clear antitumor activity,and its cytotoxicity against MCF-7 and MDA-MB-231 cells was stronger compared with cisplatin.Compounds 1–4 and 6–7 also exhibited certain activity other than the antitumor activity described above.These results demonstrated that compounds 1–4,6–7 and 9 were very promising leads for further structural modification.展开更多
基金Scientific Research Fund of the School of Pharmacy and Medical Technology of Putian University (Grant No.Z202102)。
文摘Eight phenyl benzoate compounds were synthesized in one step, and then their antioxidant, anti-tyrosinase, and anti-pancreatic lipase activities were evaluated in the present study. The total yields ranged from 31% to 85%. Compound 4 c exhibited a stronger antioxidant activity compared with Trolox, with half maximal inhibitory concentrations(IC50) of approximately 13.06 μM, and the antioxidant mechanism was further studied using computational chemistry. Compounds 1 c–5 c exhibited minimal anti-tyrosinase activity. Compounds 4 c, 5 d, 6 c and 6 d exhibited weak anti-pancreatic lipase activity, with an inhibition rate of 33.52%, 15.76%, 18.37% and 20.77%, respectively. These results demonstrated that all compounds had reference significance, especially compound 4 c.
基金Natural Science Foundation of Fujian Province (Grant No. 2022J011158)Putian City Science and Technology Plan Project (Grant No. 2021S2001-9)Fujian Provincial Key Laboratory of Innovative Drug Target Research (Grant No. FJ-YW-2021KF01)。
文摘In the present study, we evaluated the antitumor, anti-tyrosinase, anti-pancreatic lipase, antibacterial, antifungal, and anti-α-glycosidase activities for all or a subset of 20 known compounds. They included 8 phenyl benzoates, 10 benzophenones, and 2 xanthones. Phenyl benzoate compounds 1–8 did not exhibit evident antitumor activity, which was consistent with existing theories. Compounds 16, 17, and 18 exhibited moderate anti-tyrosinase activity. In addition, compounds 11 and 18 exhibited moderate inhibitory activity against Candida albicans, and compound 20 exhibited stronger anti-α-glycosidase activity than quercetin, with an IC_(50)of approximately 2.45 μM. These results demonstrated that compounds 11, 16–18, and 20 were promising leads for further structural modification.
基金Leading Project of Fujian Provincial Department of Science and Technology(Grant No.2018Y0072)。
文摘Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11%to 36%.All of the compounds were first reported.Then,the antitumor,anti-tyrosinase,anti-pancreatic lipase,antifungal and antibacterial activities of all or part of compounds 1–9 were evaluated.Compound 9 exhibited clear antitumor activity,and its cytotoxicity against MCF-7 and MDA-MB-231 cells was stronger compared with cisplatin.Compounds 1–4 and 6–7 also exhibited certain activity other than the antitumor activity described above.These results demonstrated that compounds 1–4,6–7 and 9 were very promising leads for further structural modification.
