Romanian Society of Pharmaceutical Sciences

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ISOLATION OF ANTI-PROLIFERATIVE BIOACTIVE COMPOUNDS FROM GYPSOPHILA ERIOCALYX PLANT EXTRACTS BY ACTIVITY – GUIDED APPROACH

BUSRA GUNDOGDU 1,2,3, UMMUHAN DEMIR 1,4, HUSEYIN SERVI 5*, TIMUR HAKAN BARAK ⁶

¹ Science and Advanced Technologies Research Centre (BILTAM), Istanbul Medeniyet University, İstanbul, Türkiye
2 Department of Molecular Biology and Genetics, Faculty of Arts and Sciences, Yıldız Technical University, İstanbul, Türkiye
3 Faculty of Engineering and Natural Sciences, Sabancı University, İstanbul, Türkiye
4 Department of Molecular Biology and Genetics, Faculty of Engineering and Natural Sciences, Istanbul Medeniyet University, İstanbul, Türkiye
5 Department of Pharmacognosy, Faculty of Pharmacy, Istanbul Yeni Yuzyil University, İstanbul, Türkiye
6 Department of Pharmacognosy, Faculty of Pharmacy, Acibadem Mehmet Ali Aydinlar University, İstanbul, Türkiye

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Endemic Gypsophila eriocalyx species have been traditionally used for several purposes. The aim of this study was to isolate anti-cancer compounds from G. eriocalyx. The aerial parts of G. eriocalyx were dried in the laboratory, and hexane, ethyl acetate, methanol, and methanol:water (70:30) extracts were obtained by maceration. The ethyl acetate extract exhibited the highest antiproliferative activity and was separated into subfractions by chromatographic methods. The chemical structure of the bioactive compound was elucidated by nuclear magnetic resonance (NMR) and Gas Chromatography-Mass Spectroscopy (GC/MS). Monolayer colony assay and 3D spheroid formation were applied to test the anti-cancer effect of subfraction 3.2 in prostate cancer cell PC3. As subfractionation of the ethyl acetate extract progressed to 3 and 3.2, the IC50 values decreased. Subfraction 3.2 showed a significant anti-proliferative effect in both 2D cells and spheroid cultures of PC3 cells. Spectral analyses revealed that the active compound isolated through step-wise fractionation of G. eriocalyx was 2,4-di-tert-butylphenol. 2,4-di-tert-butylphenol compound was obtained from the 3.2.2.2.2 coded fraction of the G. eriocalyx plant.