Inhibition of platelet aggregation and thrombosis by indole alkaloids isolated from the edible insect Protaetia brevitarsis seulensis (Kolbe). Issue 6 (20th December 2016)

• Record Type: Journal Article
• Authors: Lee, JungIn; Lee, Wonhwa; Kim, Mi‐Ae; Hwang, Jae Sam; Na, MinKyun; Bae, Jong‐Sup
• Is Part Of: Journal of cellular and molecular medicine. Volume 21:Issue 6(2017)
• Page Start: 1217
• Page End: 1227
• Publication Date: 2016-12-20
• Subjects: Protaetia brevitarsis seulensis (Kolbe) -- indole alkaloids -- coagulation cascade -- fibrinolysis; Cytology; Medicine; Molecular Biology; Cytologie -- Périodiques; Médecine -- Périodiques; Biologie moléculaire -- Périodiques; Cytology -- Periodicals; Medicine -- Periodicals; Molecular biology -- Periodicals; 611.01805
• DOI: 10.1111/jcmm.13055
• Languages: English
• ISSNs: 1582-1838

Abstract

Abstract: 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, compounds1 and2 prolonged aPTT and PT and impaired thrombin and FXa generation on HUVEC surface. Moreover, these compounds inhibited platelet aggregation. Antithrombotic effects of compounds1 and2 were further confirmed in pre‐clinical models of pulmonary embolism and arterial thrombosis. Collectively, these results demonstrated that compounds1 and2 could be effective antithrombotic agents and serve as new scaffolds for the development of antithrombotic drug.