title: Antifibrinolytic role of a bee venom serine protease inhibitor that acts as a plasmin inhibitor.
abstract: Bee venom is a rich source of pharmacologically active substances. In this study, we identified a bumblebee (Bombus ignitus) venom Kunitz-type serine protease inhibitor (Bi-KTI) that acts as a plasmin inhibitor. Bi-KTI showed no detectable inhibitory effect on factor Xa, thrombin, or tissue plasminogen activator. In contrast, Bi-KTI strongly inhibited plasmin, indicating that it acts as an antifibrinolytic agent; however, this inhibitory ability was two-fold weaker than that of aprotinin. The fibrin(ogen)olytic activities of B. ignitus venom serine protease (Bi-VSP) and plasmin in the presence of Bi-KTI indicate that Bi-KTI targets plasmin more specifically than Bi-VSP. These findings demonstrate a novel mechanism by which bumblebee venom affects the hemostatic system through the antifibrinolytic activity of Bi-KTI and through Bi-VSP-mediated fibrin(ogen)olytic activities, raising interest in Bi-KTI and Bi-VSP as potential clinical agents.
authors.affiliation: College of Natural Resources and Life Science, Dong-A University, Busan, Republic of Korea.
authors.forename: Young Moo
authors.initials: YM
authors.lastname: Choo
authors.forename: Kwang Sik
authors.initials: KS
authors.lastname: Lee
authors.forename: Hyung Joo
authors.initials: HJ
authors.lastname: Yoon
authors.forename: Yuling
authors.initials: Y
authors.lastname: Qiu
authors.forename: Hu
authors.initials: H
authors.lastname: Wan
authors.forename: Mi Ri
authors.initials: MR
authors.lastname: Sohn
authors.forename: Hung Dae
authors.initials: HD
authors.lastname: Sohn
authors.forename: Byung Rae
authors.initials: BR
authors.lastname: Jin
mesh_terms: D000818:Animals; D000933:Antifibrinolytic Agents / Q000302:isolation & purification*; D001514:Bee Venoms / Q000737:chemistry*; D001516:Bees / Q000737:chemistry*; D005341:Fibrinolysin / Q000037:antagonists & inhibitors*; D005343:Fibrinolytic Agents; D006487:Hemostasis; D006801:Humans; D015842:Serine Proteinase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D000933:Antifibrinolytic Agents; D001514:Bee Venoms; D005343:Fibrinolytic Agents; D015842:Serine Proteinase Inhibitors; D005341:Fibrinolysin