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Repurposing Bacopa monnieri extracts containing Aquaporin-1 blockers to improve systemic oxidative stress: The BacOxy_I study
(en) OBJECTIVES: To evaluate the efficacy of Bacopa monnieri (BM) containing Bacopaside II, a specific Aquaporin 1 (AQP1)-blocker, on systemic oxidative stress. Background: AQP1, is a peroxiporin which facilitates hydrogen peroxide transmembrane passage. It is predominantly expressed in endothelial cells and erythrocytes. METHODS: BM extract was administered orally for 6 weeks to 20 healthy volunteers (Group A/B: 400/800 mg/day). Assessments occurred at baseline (V0), after 6 weeks of treatment (V4), and 4 weeks post-treatment (V6). Primary endpoint: ROS levels in erythrocytes post-H2O2 exposure (DCFDA fluorescence). Secondary endpoints: Oxidative stress and safety biomarkers, blood pressure monitoring. Bacopaside II metabolites in plasma were identified using liquid chromatography-mass spectrometry (LC-MS). RESULTS: BM intake reduced ROS levels in RBCs in Group B (T40 min: Mean Fluorescence Intensity of DCF V0=381 ± 43 a.u vs V4= 187 ± 69 a.u, p<0.01). Methemoglobin and oxidized Methionine 148 of Apolipoprotein A-1 levels decreased (Methemoglobin group B: V0= 0.900 ± 0.105 a.u vs V4= 0.233 ± 0.047 a.u; p<0.001, M148-ox/M148 ratio group B: V0= 0.06 ± 0.01 a.u. vs V4= 0.02 ± 0.00 a.u.; p<0.05). A reduction in blood pressure was observed in Group B (Systolic Blood Pressure V0=131 ± 15 mmHg vs SBP V4=116 ± 7 mmHg; p < 0.05). Two potential Bacopaside II metabolites with putative binding pockets on AQP1 were identified during the treatment. CONCLUSION: A six-week oral intake of BM reduced systemic oxidative stress in healthy volunteers in a dose-dependent manner. Pharmacological blocking of AQP1 may help restore redox balance in the vasculature.
Boughaleb, H., Verdoy, R., Pochet, A., Fabian, N., Bella, R., Muruganandam, G., Frédérick, R., Boudjeltia, K. Z., Bourez, A., Delporte, C., Van Antwerpen, P., Robert, A., Haufroid, V., Dewulf, J., Balligand, J.-L., & Montiel, V. (2025). Repurposing Bacopa monnieri extracts containing Aquaporin-1 blockers to improve systemic oxidative stress: The BacOxy_I study. Advances in redox research, 15, 100126 [1-21]. https://doi.org/10.1016/j.arres.2025.100126 (Original work published 2025)