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Therapeutic Potential of Baicalein in Endometrial Cancer: Suppression of mTOR Signaling and Synergy with Metformin
Alison L Dumitriu1, Wei Wen1, Jin Yan1
1Division of Surgical Oncology, Department of Surgery, City of Hope National Medical Center, Duarte, CA 91010, USA.
Abstract:
Baicalein, a natural flavonoid derived from traditional medicinal herbs, has demonstrated anticancer activity in various malignancies, but its role in endometrial cancer remains largely unexplored. In this study, we investigated the therapeutic potential of baicalein, alone and in combination with metformin, in human endometrial cancer cells. Given that the mTOR signaling pathway is frequently dysregulated in endometrial cancer due to PTEN loss, we examined how baicalein affects this pathway. Our results demonstrated that baicalein significantly inhibited cell proliferation in a dose-dependent manner, which was associated with increased DDIT4 expression, activation of AMPK, and decreased phosphorylation of mTOR downstream targets S6K1 and S6. In vivo, baicalein treatment led to a reduction in tumor volume in HEC-1A xenograft female nude mice without affecting body weight. While metformin also reduced cell viability, baicalein achieved comparable effects at lower concentrations. The combination of baicalein and metformin produced a synergistic anti-tumor effect and more effectively inhibited the AMPK/PI3K/mTOR signaling pathway than either agent alone. These findings suggest that baicalein may represent a promising, non-toxic therapeutic option for endometrial cancer, particularly when used in combination with metformin. Further investigation is warranted to assess the clinical relevance of this strategy.
Insights
Baicalein, a natural flavonoid, effectively inhibits endometrial cancer cell growth by targeting the AMPK/PI3K/mTOR pathway. Combining baicalein with metformin shows synergistic anti-tumor effects, suggesting a promising therapeutic strategy.
Area of Science:
- Oncology
- Pharmacology
- Biochemistry
Background:
- Endometrial cancer (EC) is a common gynecologic malignancy.
- The mTOR signaling pathway is frequently dysregulated in EC, often due to PTEN loss.
- Baicalein, a flavonoid from medicinal herbs, shows anticancer potential but its role in EC is understudied.
Purpose of the Study:
- To investigate the therapeutic potential of baicalein in human endometrial cancer cells.
- To explore the effects of baicalein, alone and with metformin, on the AMPK/PI3K/mTOR pathway.
- To evaluate baicalein's efficacy in an in vivo endometrial cancer xenograft model.
Main Methods:
- Cell proliferation assays were performed on human endometrial cancer cells treated with baicalein and/or metformin.
- Western blotting was used to assess protein expression and phosphorylation related to the AMPK/PI3K/mTOR pathway (DDIT4, p-S6K1, p-S6).
- In vivo efficacy was evaluated using HEC-1A xenografts in female nude mice.
Main Results:
- Baicalein significantly inhibited endometrial cancer cell proliferation in a dose-dependent manner.
- Baicalein treatment increased DDIT4 expression and AMPK activation, while decreasing mTORC1 activity (p-S6K1, p-S6).
- Baicalein reduced tumor volume in vivo without affecting body weight; combination therapy with metformin demonstrated synergistic anti-tumor effects.
Conclusions:
- Baicalein exhibits potent anti-proliferative and anti-tumor effects in endometrial cancer models.
- Baicalein targets the AMPK/PI3K/mTOR pathway, offering a potential non-toxic therapeutic strategy.
- Combination therapy with metformin enhances baicalein's efficacy, warranting further clinical investigation.
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