Anticancer activity of Hedyotis corymbosa nanoliposomes targeting estrogen receptor-alpha in breast cancer cells: In silico and in vitro studies

Sofy Permana, Laili Nurzaidah, Edwin Widodo, Kenty W. Anita, Raditya W. Nugraheni,Yoshiyuki Kawamoto, Heni Endrawati, Agustina T. Endharti

JOURNAL OF PHARMACY & PHARMACOGNOSY RESEARCH(2024)

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摘要
Context: Breast cancer expresses high levels of the estrogen receptor alpha (ER-alpha).Aims: To investigate the potential anticancer activity of nanoliposome Hedyotis corymbosa in breast cancer cells by specifically targeting the ER-alpha through a combination of in silico and in vitro studies.Methods: This study used molecular docking to analyze the interaction between ER-alpha and active compounds from H. corymbosa. In vitro studies, the H. corymbosa extract was converted into nanoliposomes. The nanoliposomes' characteristics were examined, combined with tamoxifen, and applied to breast cancer cell cultures. Viability, proliferation, and ER-alpha expression were assessed, and statistical analysis was performed (p<0.05).Results: The findings show that H. corymbosa compounds, especially rutin, inhibit ER-alpha binding and act as a substrate for P-glycoprotein. Extract H. corymbosa selectively decreases viability in breast cancer cells (T47D) compared to non-cancerous cells (NIH3T3). Combining extracts with tamoxifen at 10 mg/mL enhances treatment efficacy. The combined treatment is effective for up to 72 h, reducing T47D breast cancer cell proliferation. Nanoliposomes derived from extract exhibit favorable characteristics, including a spherical shape, uniform size distribution, and stability. Using these nanoliposomes at 100 mu g/mL with tamoxifen significantly reduces ER-alpha expression (p<0.05) without affecting cell viability.Conclusions: Compounds from H. corymbosa, especially rutin, inhibit ER-alpha binding. H. corymbosa nanoliposomes are stable for drug delivery. Combining tamoxifen with nanoliposomes at 100 mu g/mL reduces ER-alpha expression. This shows potential for breast cancer treatment, but validation through further research and clinical trials is necessary.
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关键词
breast cancer,estrogen receptor alpha,Hedyotis,liposomes,rutin
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