Cardiovascular diseases(CVDs)are the leading global cause of mortality and disease burden.Statins are the most prescribed lipid-lowering drugs to treat hypercholesterolemia and prevent CVDs.The biochemical mechanism o...Cardiovascular diseases(CVDs)are the leading global cause of mortality and disease burden.Statins are the most prescribed lipid-lowering drugs to treat hypercholesterolemia and prevent CVDs.The biochemical mechanism of statins consists of competitive inhibition of the 3-hydroxy-3-methylglutaryl-coenzyme A reductase enzyme(HMG-CoAR),the limiting enzyme in cholesterol biosynthesis.Due to statin intolerance in some patient groups,the search for new inhibitors is a field of great interest.This review focusses on the studies reporting the inhibitory effect of protein hydrolysates and biopeptides on the HMG-CoAR enzyme activity.The analysis of the action mechanism and physicochemical characteristics of the HMG-CoAR inhibitory peptides revealed that the molecular weight,amino acid composition,charge,and polarity are key aspects of the interaction with the HMG-CoAR enzyme.In conclusion,this review reveals the potential of using food peptides as new cholesterol-lowering agents and opens a new interesting field of research.However,clinical approaches are mandatory to confirm their therapeutic hypercholesterolemic effect.展开更多
基金funded by Consejería de Salud,Junta de Andalucía(PC-0111-2016-0111)and PEMP-0085-2020(cofinanciado con fondos FEDER,convocatoria Resolución de 7 de julio de 2021 de la Secretaría General de Investigación,Desarrollo e Innovación en Salud,que convoca subvenciones para financiar la investigación,el desarrollo y la innovación en Biomedicina y Ciencias de la Salud en Andalucía,para 2021),and the Programa PAIDI from the Junta de Andalucía(CTS160).G.S.S.was supported by a FPU grant from the Spanish Ministerio de Educación,Cultura y Deporte(FPU16/02339).I.C.C.was supported by the VI Program of Inner Initiative for Research and Transfer of the University of Seville(VIPPIT-2020-II.4)and by a postdoctoral fellowship from the Andalusian Government Ministry of Economy,Knowledge,Business,and University(DOC_00587/2020).A.I.A.L.was funded by Andalusian Government Ministry of Health(PI-0136-2019).E.P.E.was supported by the VI Program of Inner Initiative for Research and Transfer of University of Seville.
文摘Cardiovascular diseases(CVDs)are the leading global cause of mortality and disease burden.Statins are the most prescribed lipid-lowering drugs to treat hypercholesterolemia and prevent CVDs.The biochemical mechanism of statins consists of competitive inhibition of the 3-hydroxy-3-methylglutaryl-coenzyme A reductase enzyme(HMG-CoAR),the limiting enzyme in cholesterol biosynthesis.Due to statin intolerance in some patient groups,the search for new inhibitors is a field of great interest.This review focusses on the studies reporting the inhibitory effect of protein hydrolysates and biopeptides on the HMG-CoAR enzyme activity.The analysis of the action mechanism and physicochemical characteristics of the HMG-CoAR inhibitory peptides revealed that the molecular weight,amino acid composition,charge,and polarity are key aspects of the interaction with the HMG-CoAR enzyme.In conclusion,this review reveals the potential of using food peptides as new cholesterol-lowering agents and opens a new interesting field of research.However,clinical approaches are mandatory to confirm their therapeutic hypercholesterolemic effect.