Background: The search for natural anticancer agents is a worthy scientific research goal, driven by
the hope to lessen cancer's tremendous global burden.
Objective: This study aimed at evaluating the cytotoxic activity of Gardenia latifolia Ait. (Rubiaceae)
against lung (A549) and colon (HCT116) cancer cell lines. Cytotoxicity-guided isolation of the
bioactive phytochemicals was conducted, followed by various mechanistic validations of the appealing
cytotoxic metabolites.
Methods: The cytotoxic effects were determined using MTT assay. The two most cytotoxic compounds
were further evaluated for their effects on cell cycle progression and apoptotic capabilities using flow
cytometry approach. Additionally, we conducted a molecular docking analysis to reveal their potential
interactions with the human topoisomerase IIα.
Results: The phytochemical investigation led to isolation of nine compounds including a new one, (-)
1-acetyl 4,5-di-O-caffeoyl quinic acid. The latter compound was the most cytotoxic against the colon
cancer cell line (IC50 1.9 µg/ml) with a remarkable tumor-selectivity (SI ≈ 15). Moreover, the isolated
glycoside, 1-O-[6-O-(5-O-vanilloyl-β-ᴅ-apiofuranosyl)-β-ᴅ-glucopyranosyl]-3,4,5-trimethoxybenzene,
showed selective cytotoxicity towards A549 and HCT116 cells (IC50 values of 3.8 and 3.3 µg/ml,
respectively). Both compounds considerably affected the cell cycle distribution. They caused G2/M cell
cycle arrest, showed apoptotic capabilities, and displayed significant in silico topoisomerase IIα
inhibition.
Conclusion: Two cytotoxic and apoptotic compounds were reported from Gardenia latifolia.
Subsequent in vivo studies and clinical trials should be conducted to substantiate their anticipated
therapeutic values.
تاريخ البحث
قسم البحث
مجلة البحث
Current bioactive compounds
الناشر
Bentham Science
عدد البحث
18
موقع البحث
https://benthamscience.com/article/121314
سنة البحث
2022
المشارك في البحث
ملخص البحث