Fera Kurniadewi, Lutfia Miftah Palah, Irma Ratna Kartika, Muktiningsih Nurjayadi, Elvira Hermawati, Ade Danova
Xanthone derivatives, known for their bioactive properties, have garnered significant attention in recent years owing to their potential therapeutic applications. In this study, we isolated three xanthone derivatives, α-mangostin (1), β-mangostin (2), and 2,8-diisoprenyl-1,3-dihydroxy-6,7-dimethoxyxanthone (3), from the ethyl acetate fraction of Garcinia mangostana twigs. Structural identification of these compounds was confirmed by UV, IR, NMR, and MS analyses. Notably, compound 3 was isolated from twigs of G. mangostana for the first time. The inhibitory activity of the isolated compounds was evaluated against several receptor tyrosine kinases (RTKs), including the Epidermal Growth Factor Receptor (EGFR), HER2, HER4, IGFR, InsR, KDR, PDGFRα, and PDGFRβ. Compounds 1-3 exhibited moderate EGFR inhibition, with inhibitory effects ranging from 29-30%. Molecular docking studies revealed that these compounds interacted with EGFR through hydrogen bonding and hydrophobic interactions, with binding energies of-8.4,-8.2, and-8.2 kcal/mol, respectively. This study highlights the potential of xanthone derivatives as selective inhibitors of specific RTKs, offering insights for developing targeted cancer therapies. In particular, the selective activity of compound 2 against EGFR suggests promising therapeutic applications for EGFR-related conditions, including certain cancers and provides a foundation for future research on drug development. © 2025, Sami Publishing Company. All rights reserved.
Chemistry Study Program, Universitas Negeri Jakarta, Jakarta, 13220, Indonesia; Organic Chemistry Division, Department of Chemistry, Faculty of Mathematics and Natural Sciences, Institut Teknologi Bandung, Jl. Ganesha no.10, Bandung, 40132, Indonesia
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