In this paper,the anti-tumor,anti-inflammatory,antibacterial and anti-asthma effects of isobavachalcone and their molecular mechanisms were reviewed to provide theoretical support for further research of isobavachalco...In this paper,the anti-tumor,anti-inflammatory,antibacterial and anti-asthma effects of isobavachalcone and their molecular mechanisms were reviewed to provide theoretical support for further research of isobavachalcone and development of new drugs.展开更多
Isobavachalcone （IBC） or （E）-l-[2,4-dihydroxy-3-（3-methyl-2-butenyl）-phenyl]-3-（4- hydroxyphenyl）-2-propen-1-one or （E）-4,2＇,4＇-trihydroxy-3＇-prenylchalcone; 2＇,4,4＇-trihydroxy-3＇-prenyl-trans- chalcon...Isobavachalcone （IBC） or （E）-l-[2,4-dihydroxy-3-（3-methyl-2-butenyl）-phenyl]-3-（4- hydroxyphenyl）-2-propen-1-one or （E）-4,2＇,4＇-trihydroxy-3＇-prenylchalcone; 2＇,4,4＇-trihydroxy-3＇-prenyl-trans- chalcone, is a prenylated chalcone of the class flavonoid, firstly isolated from Psoralea corylifolia in 1968. IBC is known to possess a wide spectrum of biological activities, antibacterial, antifungal, anticancer, anti-reverse transcriptase, antitubercular and antioxidant. The compound was isolated from plant families, mostly Moraceae and Fabaceae. This review brings out together the knowledge on IBC, and can serve as the start point for future research and valorization accomplishments.展开更多
Pancreatic lipase(PL), a crucial enzyme in the digestive system of mammals, has been proven as a therapeutic target to prevent and treat obesity. The purpose of this study is to evaluate and characterize the PL inhibi...Pancreatic lipase(PL), a crucial enzyme in the digestive system of mammals, has been proven as a therapeutic target to prevent and treat obesity. The purpose of this study is to evaluate and characterize the PL inhibition activities of the major constituents from Fructus Psoraleae(FP), one of the most frequently used Chinese herbs with lipid-lowering activity. To this end, a total of eleven major constituents isolated from Fructus Psoraleae have been obtained and their inhibition potentials against PL have been assayed by a fluorescence-based assay. Among all tested compounds, isobavachalcone, bavachalcone and corylifol A displayed strong inhibition on PL(IC50 < 10 μmol·L-1). Inhibition kinetic analyses demonstrated that isobavachalcone, bavachalcone and corylifol A acted as mixed inhibitors against PL-mediated 4-methylumbelliferyl oleate(4-MUO) hydrolysis, with the Ki values of 1.61, 3.77 and 10.16μmol·L-1, respectively. Furthermore, docking simulations indicated that two chalcones(isobavachalcone and bavachalcone) could interact with the key residues located in the catalytic cavity of PL via hydrogen binding and hydrophobic interactions. Collectively, these finding provided solid evidence to support that Fructus Psoraleae contained bioactive compounds with lipid-lowering effects via targeting PL, and also suggested that the chalcones in Fructus Psoraleae could be used as ideal leading compounds to develop novel PL inhibitors.展开更多
基金Supported by the Key Research and Development Plan Guidance Project of Heilongjiang Province(GZ20220039)Central Support for Local Universities Reform and Development Fund Talent Training Project(2020GSP16).
文摘In this paper,the anti-tumor,anti-inflammatory,antibacterial and anti-asthma effects of isobavachalcone and their molecular mechanisms were reviewed to provide theoretical support for further research of isobavachalcone and development of new drugs.
文摘Isobavachalcone （IBC） or （E）-l-[2,4-dihydroxy-3-（3-methyl-2-butenyl）-phenyl]-3-（4- hydroxyphenyl）-2-propen-1-one or （E）-4,2＇,4＇-trihydroxy-3＇-prenylchalcone; 2＇,4,4＇-trihydroxy-3＇-prenyl-trans- chalcone, is a prenylated chalcone of the class flavonoid, firstly isolated from Psoralea corylifolia in 1968. IBC is known to possess a wide spectrum of biological activities, antibacterial, antifungal, anticancer, anti-reverse transcriptase, antitubercular and antioxidant. The compound was isolated from plant families, mostly Moraceae and Fabaceae. This review brings out together the knowledge on IBC, and can serve as the start point for future research and valorization accomplishments.
基金the National Key Research and Development Program of China (Nos.2017YFC1700200,2017YFC1702000)NSF of China (Nos.81922070, 81973286, 81973393, 81773687)+4 种基金Natural Science Foundation of Liaoning Province (No.20180530025)Program of Shanghai Academic/Technology Research Leader (No. 18XD1403600)Shuguang Program (No. 18SG40) supported by Shanghai Education Development Foundation and Shanghai Municipal Education CommissionInnovative Entrepreneurship Program of High-level Talents in Dalian (No. 2017RQ121)Undergraduate Training Program for Innovation and Entrepreneurship from Shanghai University of Traditional Chinese Medicine (No. 2017101419803010904)。
文摘Pancreatic lipase(PL), a crucial enzyme in the digestive system of mammals, has been proven as a therapeutic target to prevent and treat obesity. The purpose of this study is to evaluate and characterize the PL inhibition activities of the major constituents from Fructus Psoraleae(FP), one of the most frequently used Chinese herbs with lipid-lowering activity. To this end, a total of eleven major constituents isolated from Fructus Psoraleae have been obtained and their inhibition potentials against PL have been assayed by a fluorescence-based assay. Among all tested compounds, isobavachalcone, bavachalcone and corylifol A displayed strong inhibition on PL(IC50 < 10 μmol·L-1). Inhibition kinetic analyses demonstrated that isobavachalcone, bavachalcone and corylifol A acted as mixed inhibitors against PL-mediated 4-methylumbelliferyl oleate(4-MUO) hydrolysis, with the Ki values of 1.61, 3.77 and 10.16μmol·L-1, respectively. Furthermore, docking simulations indicated that two chalcones(isobavachalcone and bavachalcone) could interact with the key residues located in the catalytic cavity of PL via hydrogen binding and hydrophobic interactions. Collectively, these finding provided solid evidence to support that Fructus Psoraleae contained bioactive compounds with lipid-lowering effects via targeting PL, and also suggested that the chalcones in Fructus Psoraleae could be used as ideal leading compounds to develop novel PL inhibitors.
