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Chem Biol Drug Des. 2019 Sep;94(3):1672-1679. doi: 10.1111/cbdd.13570. Epub 2019 Jun 12.

The inhibitory effect of tachyplesin I on thrombosis and its mechanisms.

Author information

1
Department of Biochemistry and Molecular Biology, Guangdong Medical University, Zhanjiang, China.
2
Guangdong Key Laboratory for Research and Development of Natural Drugs, Guangdong Medical University, Zhanjiang, China.
3
Affiliated Hospital of Guangdong Medical University, Zhanjiang, Guangdong, China.

Abstract

Thrombotic diseases are major cause of cardiovascular diseases. This study was designed to investigate the effect of tachyplesin I on platelet aggregation and thrombosis. Platelet aggregation was analysed with a whole blood aggregometer. The mice were employed to investigate the effect of tachyplesin I on thrombosis in vivo. Tachyplesin I inhibited thrombin-induced platelet aggregation in a dose-dependent manner. Furthermore, tachyplesin I significantly reduced thrombosis in carrageenan-induced tail thrombosis model by intraperitoneal injection (0.1, 0.2 or 0.4 mg/kg) or intragastric administration (15, 30 or 60 mg/kg). Tachyplesin I also prolonged the bleeding time (BT) and clotting time (CT). The results revealed that tachyplesin I inhibited platelet aggregation and thrombosis by interfering the PI3K/AKT pathway. Tachyplesin I did not show significantly toxicity to mice under 300 mg/kg via intravenous injection. The results show that tachyplesin I inhibits thrombosis and has low toxicity. It is suggested that tachyplesin I has the potential to develop a new anti-thrombotic drug.

KEYWORDS:

PI3K/Akt; anti-thrombosis; platelet aggregation; tachyplesin I

PMID:
31108023
DOI:
10.1111/cbdd.13570

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