Open AccessInhibition of platelet aggregation and thrombosis by indole alkaloids isolated from the edible insect Protaetia brevitarsis seulensis (Kolbe)
Author(s) -
Lee JungIn,
Lee Wonhwa,
Kim MiAe,
Hwang Jae Sam,
Na MinKyun,
Bae JongSup
Publication year - 2017
Publication title -
journal of cellular and molecular medicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.44
H-Index - 130
eISSN - 1582-4934
pISSN - 1582-1838
DOI - 10.1111/jcmm.13055
Subject(s) - antithrombotic , chemistry , indole test , carboxylic acid , pharmacology , traditional medicine , biochemistry , biology , medicine , cardiology
Protaetia brevitarsis seulensis (Kolbe) has been temporarily registered as a food material by the Ministry of Food and Drug Safety of Korea ( MFDS ). The current study aimed to discover small antithrombotic molecules from this edible insect. Five indole alkaloids, 5‐hydroxyindolin‐2‐one ( 1 ), (1 R ,3 S )‐1‐methyl‐1,2,3,4‐tetrahydro‐β‐carboline‐3‐carboxylic acid ( 2 ), (1 S ,3 S )‐1‐methyl‐1,2,3,4‐tetrahydro‐β‐carboline‐3‐carboxylic acid ( 3 ), (3 S )‐1,2,3,4‐tetrahydro‐β‐carboline‐3‐carboxylic acid ( 4 ) and L‐tryptophan ( 5 ), were isolated from the insect. Among them, compounds 1 and 2 prolonged aPTT and PT and impaired thrombin and FXa generation on HUVEC surface. Moreover, these compounds inhibited platelet aggregation. Antithrombotic effects of compounds 1 and 2 were further confirmed in pre‐clinical models of pulmonary embolism and arterial thrombosis. Collectively, these results demonstrated that compounds 1 and 2 could be effective antithrombotic agents and serve as new scaffolds for the development of antithrombotic drug.