title: Puerarin Inhibits oxLDL-Induced Macrophage Activation and Foam Cell Formation in Human THP1 Macrophage.
abstract: Puerarin, an isoflavone derived from Kudzu roots, has been widely used for treatment of cardiovascular and cerebral vascular diseases in China and other Asian countries. However, the underlying mechanisms are largely unknown. The present study investigated whether puerarin inhibited atherogenic lipid oxLDL-mediated macrophage activation and foam cell formation in human THP1 macrophage. Treatment with oxLDL significantly increased the mRNA expression of proinflammatory cytokines tumor necrosis factor α (TNFα, 160%) and interleukin (IL) 1β (13 fold) accompanied by upregulation of toll-like receptor 4 (TLR4, 165%) and the ratio of phospho-IκBα/IκBα in THP1 macrophage. Puerarin dose-dependently prevented an increase in oxLDL-induced proinflammatory gene expression with downregulation of TLR4 and the ratio of phospho-IκBα/IκBα. Furthermore, puerarin prevented oxLDL-mediated lipid deposition and foam cell formation associated with downregulation of scavenger receptor CD36. Flow cytometry analysis showed that puerarin reduced the number of early apoptotic cells of macrophages induced by oxLDL. Our results show that puerarin has anti-inflammatory and antiatherogenic effects in vitro; the underlying mechanisms may involve the inhibition of TLR4/NFκB pathway and downregulation of CD36 expression. The results from the present study provide scientific evidence and may expand our armamentarium to use puerarin for prevention and treatment of cardiovascular and atherosclerotic diseases.
authors.affiliation: Department of Physiology, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
authors.forename: Heng
authors.initials: H
authors.lastname: Zhang
authors.affiliation: Department of Oncology, Cancer Center, Turmounesis and Microenvironment Laboratory, The First Affiliated Hospital, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
authors.forename: Zhenhua
authors.initials: Z
authors.lastname: Zhai
authors.affiliation: Vagelos Scholars Program of the Molecular Life Sciences, University of Pennsylvania, Philadelphia, PA 19104, USA.
authors.forename: Hongyu
authors.initials: H
authors.lastname: Zhou
authors.affiliation: Department of Physiology, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
authors.forename: Yao
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Physiology, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
authors.forename: Xiaojie
authors.initials: X
authors.lastname: Li
authors.affiliation: Department of Physiology, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
authors.forename: Yuhan
authors.initials: Y
authors.lastname: Lin
authors.affiliation: Department of Physiology, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
authors.forename: Weihong
authors.initials: W
authors.lastname: Li
authors.affiliation: Department of Chinese Medicine, The First Affiliated Hospital, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
authors.forename: Yueping
authors.initials: Y
authors.lastname: Shi
authors.affiliation: Department of Physiology, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
authors.forename: Ming-Sheng
authors.initials: MS
authors.lastname: Zhou
mesh_terms: D002460:Cell Line; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D005487:Foam Cells / Q000166:cytology / Q000187:drug effects / Q000276:immunology*; D006801:Humans; D018836:Inflammation Mediators / Q000276:immunology*; D007529:Isoflavones / Q000008:administration & dosage*; D008077:Lipoproteins, LDL / Q000008:administration & dosage*; D008262:Macrophage Activation / Q000187:drug effects / Q000276:immunology*; D008264:Macrophages / Q000166:cytology / Q000187:drug effects / Q000276:immunology*
chemical_list: D018836:Inflammation Mediators; D007529:Isoflavones; D008077:Lipoproteins, LDL; C099252:oxidized low density lipoprotein; C033607:puerarin