title: Local anesthetics inhibit tissue factor expression in activated monocytes via inhibition of tissue factor mRNA synthesis.
abstract: Local anesthetics have been reported to have anticoagulant properties, but the mechanisms responsible for this action are poorly understood. Here, we evaluated the in vitro effects of 3 local anesthetics--lidocaine, ropivacaine, and bupivacaine--on the tissue factor expression by monocytes. Monocytes from peripheral blood were stimulated with lipopolysaccharide (LPS) in the presence or absence of local anesthetics. All 3 local anesthetics inhibited the expression of tissue factor antigen and tissue factor activity in LPS-stimulated monocytes in a dose- and time-dependent manner and reduced tissue factor messenger RNA (mRNA) expression in endothelial cells and a monocytic cell line. None of the 3 drugs induced apoptosis or affected the viability of monocytes. Our findings that local anesthetics inhibited the tissue factor induction in activated monocytes by inhibiting tissue factor mRNA level may demonstrate the feasibility of using local anesthetics in hypercoagulable and inflammatory conditions.
authors.affiliation: Department of Laboratory Medicine and Cancer Research Institute, Seoul National University College of Medicine, Jongnogu, Seoul, Korea.
authors.forename: Ji-Eun
authors.initials: JE
authors.lastname: Kim
authors.forename: Ki Jun
authors.initials: KJ
authors.lastname: Kim
authors.forename: Wonsik
authors.initials: W
authors.lastname: Ahn
authors.forename: Kyou-Sup
authors.initials: KS
authors.lastname: Han
authors.forename: Hyun Kyung
authors.initials: HK
authors.lastname: Kim
mesh_terms: D000779:Anesthetics, Local / Q000494:pharmacology; D017209:Apoptosis; D002045:Bupivacaine / Q000494:pharmacology; D002478:Cells, Cultured; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D008012:Lidocaine / Q000494:pharmacology; D008070:Lipopolysaccharides / Q000494:pharmacology; D009000:Monocytes / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D012333:RNA, Messenger / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000097:blood / Q000235:genetics; D013925:Thromboplastin / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000235:genetics
chemical_list: D000779:Anesthetics, Local; D008070:Lipopolysaccharides; D012333:RNA, Messenger; D013925:Thromboplastin; D008012:Lidocaine; D002045:Bupivacaine