International Journal of Chemical and Biochemical Sciences (ISSN 2226-9614)[/vc_column_text][/vc_column][/vc_row]
VOLUME 28(22) (2025)
Aromatase Inhibition by Polyphenolic Extracts and Isolated Compounds from Seeds and Shoots of Georgian Grapevine (Vitis vinifera L.) Varieties
Mariam Tatanashvili1*, Malkhaz Jokhadze2, Koba Sivsivadze1, Natia Bokuchava1, Ia Pantsulaia3, Tamaz Murtazashvili1, Tamar Masiukovichi1
1Department of Pharmaceutical, Toxicological and Medical Chemistry, Faculty of Pharmacy, Tbilisi State Medical University, Tbilisi, Georgia
2Department of Pharmaceutical Botany, Faculty of Pharmacy, Tbilisi State Medical University, Tbilisi, Georgia
3Vladimer Bakhutashvili Institute of Medical Biotechnology, Tbilisi State Medical University, Tbilisi, Georgia
Abstract
Breast cancer remains a significant global health challenge, with estrogen-dependent subtypes accounting for the majority of postmenopausal cases. Aromatase inhibitors (AIs) are central to current therapeutic strategies, yet synthetic AIs are associated with adverse effects and resistance, necessitating the search for safer alternatives. This study investigates the in vitro aromatase inhibitory activity of crude extracts and isolated polyphenolic compounds from grapevine (Vitis vinifera L.) by-products, specifically seeds and shoots from various Georgian cultivars. Polyphenol-enriched extracts were obtained using ultrasound-assisted extraction, and individual compounds were isolated via chromatographic techniques and identified by nuclear magnetic resonance spectroscopy. Aromatase inhibition was assessed using a cell-free fluorometric assay. Results demonstrated that seed extracts, particularly from the Kisi and Saperavi cultivars, exhibited the highest inhibitory activity (up to 41.9% inhibition; IC₅₀ ≈ 452 µg/mL), while shoot extracts showed comparatively lower activity. Among isolated compounds, resveratrol displayed the most potent inhibition (43.0%), followed by kaempferol (26.1%), whereas quercetin showed lower but measurable activity under the applied assay conditions. These findings highlight grape seeds as a promising source of natural aromatase inhibitors, with resveratrol contributing significantly to the observed activity. The study supports valorization of viticultural by-products as potential agents for prevention and adjunctive treatment of estrogen-dependent breast cancer, warranting further in vivo and mechanistic investigations.
Keywords: Breast cancer, Aromatase inhibition, cell-free assay, Grape by-products, Polyphenols
Full length article *Corresponding Author, e-mail: m.tatanashvili@tsmu.edu, Doi # https://doi.org/10.62877/1-IJCBS-25-28-22-1,
Submitted: 22-10-2025; Accepted: 16-12-2025; Published: 22-12-2025