Tri Widiandani, Arwinda M. Riszkiani, Delis Susilawati, Mohammad G. Oxa, A. Ma Suryadi, Siswandono Siswodihardjo, Bambang T. Purwanto
Breast cancer is the leading cause of cancer-related death among women worldwide. This disease is commonly treated with doxorubicin, a chemotherapeutic agent associated with cardiotoxic side effect. Recently, pinostrobin, a compound isolated from the rhizome of Boesenbergia pandurata Roxb., has also shown potential in inhibiting the growth of human breast cancer cells (T47D). To enhance the bioavailability, reduce toxicity, and increase selectivity, the compound has been modified through the Schotten–Baumann reaction to produce 5-O-Acetylpinostrobin. Therefore, this research aimed to evaluate the cytotoxic effect of 5-O-Acetylpinostrobin against T47D cells, selectivity toward Vero cells, and interaction with estrogen receptor alpha (ERα) (PDB ID: 5T1Z) through molecular docking. Cytotoxicity was assessed using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay against T47D and Vero cells. Molecular docking was performed using AutoDockTools software (v1.5.7) and docking interaction was visualized on BIOVIA Discovery Studio. The result showed that the 50% inhibitory concentration (IC₅₀) values of 5-O-Acetylpinostrobin and pinostrobin against T47D were 53 µM and 156 µM, respectively. Cytotoxic concentration 50 (CC₅₀) values against Vero cells were 1155 µM and 3303 µM for 5-O-Acetylpinostrobin and pinostrobin, respectively, while selectivity index (SI) was 22 and 21, respectively. Furthermore, molecular docking showed that 5-O-Acetylpinostrobin had a favorable interaction with ERα, with a binding affinity of –7.98 kcal/mol. These results suggested that 5-O-Acetylpinostrobin had potential as anti-breast cancer agent and could be further developed as a co-chemotherapeutic agent. © 2026 Widiandani et al.
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga, Surabaya, 60115, Indonesia; Master Program of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga, Surabaya, 60115, Indonesia; Research Group of Drug Development, Faculty of Pharmacy, Universitas Airlangga, Surabaya, 60115, Indonesia; Inter-University Center of Excellence (IUCoE) of Health Autonomy-Drug Discovery, Universitas Airlangga, Surabaya, 60115, Indonesia; Department of Pharmacy, Faculty of Sports and Health, Universitas Negeri Gorontalo, Gorontalo, 96128, Indonesia; Faculty of Pharmacy, Institut Ilmu Kesehatan Bhakti Wiyata, Kediri, 64114, Indonesia
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