Fakhrudin, Nanang;
Pertiwi, Krisna Kharisma;
Takubessi, Marce Inggrita;
Susiani, Eka Fitri;
Nurrochmad, Arief;
Widyarini, Sitarina;
Sudarmanto, Ari;
... Wahyuono, Subagus; + view all
(2020)
A geranylated chalcone with antiplatelet activity from the leaves of breadfruit (Artocarpus altilis).
Pharmacia
, 67
(4)
pp. 173-180.
10.3897/pharmacia.67.e56788.
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Abstract
Platelet plays a crucial role in cardiovascular diseases (CVDs) development. Abnormalities in platelet aggregation provokes thromboembolism, eventually leading to death. In Indonesia, breadfruit (Artocarpus altilis) leaf is traditionally used to treat CVDs. This study aimed to evaluate the antiplatelet activity of A. altilis leaf extract (AAE) and to identify its active compound. A. altilis leaves were extracted with ethanol, and the antiplatelet activity was assessed using ADP-induced platelet aggregation. The major compound was isolated with column chromatography followed by preparative TLC, and the structure was determined on the basis of UV, MS, IR, and NMR spectra. The binding mode of the active compound to platelet receptors was characterized in in silico study. AAE exhibited an antiplatelet activity (IC50 of 252.23 µg/mL). A geranylated chalcone, 2-geranyl-2ʹ,3,3,4ʹ-tetrahydroxydihydrochalcone (GTDC) was identified as the antiplatelet compound (IC50 of 9.09 µM). GTDC actions with P2Y12 platelet receptor involving three amino acid residues.
| Type: | Article |
|---|---|
| Title: | A geranylated chalcone with antiplatelet activity from the leaves of breadfruit (Artocarpus altilis) |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.3897/pharmacia.67.e56788 |
| Publisher version: | http://dx.doi.org/10.3897/pharmacia.67.e56788 |
| Language: | English |
| Additional information: | Copyright Fakhrudin N et al. This is an open access article distributed under the terms of the Creative Commons Attribution License (CC-BY 4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
| Keywords: | Artocarpus communis, 2-geranyl-2ʹ,3,3,4ʹ-tetrahydroxydihydrochalcone, thrombosis, P2Y12, P2Y1 |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10193544 |
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