title: A potent anti-thrombosis peptide (vasotab TY) from horsefly salivary glands.
abstract: Vasotab TY is a KGD (Lys-Gly-Asp)-containing peptide identified from salivary glands of the horsefly of Tabanus yao. We have previously reported that vasotab TY showed a strong vasodilator activity. In the present study, vasotab TY was found to inhibit platelet aggregation effectively. It completely inhibited platelet aggregation induced by adenosine diphosphate (ADP) at the concentration of 9.6μg/ml. Vasotab TY significantly reduced thrombus weight in rat arteriovenous shunt model and inhibited thrombosis in carrageenan-induced mouse tail thrombosis model in vivo. Vasotab TY competitively bound to glycoprotein IIb/IIIa (GPIIb/IIIa) with eptifibatide, a well-known KGD-containing cyclic heptapeptide containing high specificity and high affinity for GPIIb/IIIa, suggesting that it is an antagonist of the fibrinogen receptor GPIIb/IIIa on the surface of platelet. The KGD motif in vasotab TY may facilitate the binding of it to GPIIb/IIIa. Vasotab TY showed a half-life of more than 1h in vivo. It showed little side effects including little bleeding, no hemolytic activity on human blood red cells and no cytotoxicity on human keratinocyte and THP-1 cells. Combined its vasodilator and platelet inhibitory functions, vasotab TY might be an excellent candidate for the development of clinical anti-thrombosis medicines.
authors.affiliation: Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Kunming 650223, Yunnan, China; University of Chinese Academy of Sciences, Beijing 100009, China.
authors.forename: Zhiye
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: Life Sciences College of Nanjing Agricultural University, 1st Weigang, Nanjing, Jiangsu 210095, China.
authors.forename: Lan
authors.initials: L
authors.lastname: Gao
authors.affiliation: Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Kunming 650223, Yunnan, China; University of Chinese Academy of Sciences, Beijing 100009, China.
authors.forename: Chuanbin
authors.initials: C
authors.lastname: Shen
authors.affiliation: Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Kunming 650223, Yunnan, China.
authors.forename: Mingqiang
authors.initials: M
authors.lastname: Rong
authors.affiliation: Life Sciences College of Nanjing Agricultural University, 1st Weigang, Nanjing, Jiangsu 210095, China.
authors.forename: Xiuwen
authors.initials: X
authors.lastname: Yan
authors.affiliation: Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Kunming 650223, Yunnan, China; Life Sciences College of Nanjing Agricultural University, 1st Weigang, Nanjing, Jiangsu 210095, China. Electronic address: rlai@mail.kiz.ac.cn.
authors.forename: Ren
authors.initials: R
authors.lastname: Lai
mesh_terms: D000818:Animals; D000911:Antibodies, Monoclonal / Q000276:immunology; D004175:Diptera / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism; D004591:Electrophoresis, Polyacrylamide Gel; D004912:Erythrocytes / Q000187:drug effects / Q000378:metabolism; D005260:Female; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010446:Peptide Fragments / Q000276:immunology / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects*; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D012469:Salivary Glands / Q000187:drug effects* / Q000378:metabolism; D013927:Thrombosis / Q000188:drug therapy* / Q000378:metabolism
chemical_list: D000911:Antibodies, Monoclonal; D010446:Peptide Fragments; D019039:Platelet Glycoprotein GPIIb-IIIa Complex
keywords: Anti-thrombosis; Glycoprotein IIb/IIIa; Horsefly; Platelet inhibitor; Vasodilator