Govindaraju, Kayatri and Mak, Yin Ying and Lee, Fong Kai and Bauer, Claudia C. and Lim, Kuan Hon and Bon, Robin S. and Kong, Cin and Then, Sue Mian and Ting, Kang Nee (2024) Vasorelaxant effect of a phenylethylamine analogue based on schwarzinicine A an alkaloid isolated from the leaves of Ficus schwarzii. Phytochemistry Letters, 59. pp. 24-35. ISSN 1874-3900, DOI https://doi.org/10.1016/j.phytol.2023.11.007.
Full text not available from this repository.Abstract
N-Phenethyl-1-phenyl-pentan-3-amine (1) is a new compound synthesised as a simplified analogue of schwarzinicine A (2), a natural compound extracted from Ficus schwarzii. Compound 1 differs from compound 2 due to its structural simplification, featuring two phenyl rings without methoxy substitution, as opposed to compound 2, which possesses three 3,4-dimethoxy aromatic rings. Our previous research findings highlighted the calciuminhibitory effects of compound 2, but the mechanism of action for compound 1 remains unexplored, serving as the primary focus of this study. Building upon our earlier research, this study aimed to elucidate compound 1's calcium-modulating potential by using rat-isolated aortae in an organ bath set-up and HEK cells expressing hTRPC channels with the fluorometric assay to measure calcium influx. Compound 1 elicited a vasorelaxation response (Emax 111.4%) similar to its parent compound 2 (Emax 123.1%), and inhibited hTRPC3-, hTRPC4-, hTRPC5-, and hTRPC6-mediated calcium influx into HEK cells with IC50 values of 6, 2, 2, 5 mu M, respectively. Compound 1 has a similar pharmacological profile as its parent compound 2, whereby it exerts a vasorelaxant effect by attenuating calcium influx and inhibits multiple TRPC channels.
| Item Type: | Article |
|---|---|
| Funders: | Malaysia Toray Science Foundation - Ministry of Higher Education Malaysia [TML-CA/17.195 (17/G62)], Schachter award from the British Pharmacological Society |
| Uncontrolled Keywords: | Schwarzinicine A; Phenylethylamine; Vascular smooth muscle; Vasodilator; TRPC cation channels |
| Subjects: | R Medicine R Medicine > RS Pharmacy and materia medica |
| Divisions: | Faculty of Pharmacy |
| Depositing User: | Ms. Juhaida Abd Rahim |
| Date Deposited: | 27 Jun 2024 05:14 |
| Last Modified: | 27 Jun 2024 05:14 |
| URI: | http://eprints.um.edu.my/id/eprint/44247 |
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