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Antiproliferative Effect of 24-Deoxysericoside From Terminalia macroptera Guill. & Perr. (Combretaceae) Against
Romeo Toko Feunaing1, Alfred Ngenge Tamfu2, Abel Joel Yaya Gbaweng1
1Department of Chemistry, Faculty of Sciences, University of Ngaoundere, Ngaoundere, Cameroon.
Background:
Terminalia macroptera (Combretaceae) is an important medicinal plant in the traditional pharmacopeia in most tropical areas, where its different parts are used in treating illnesses including cancer.
Aims:
In this study, two oleanane-type triterpenoids: terminolic acid (TM32) and arjungenin (TM34), together with three saponins: arjunglucoside I (TM35), 24-deoxysericoside (TM36) and chebuloside II (TM37) from T. macroptera, were screened for their cytotoxic effects against breast cancer cell lines.
Methods And Results:
The compounds were isolated using column chromatography and characterized from their NMR data. Their cytotoxic and antiproliferative effects against estrogen non-sensitive (MDA-MB 231) and estrogen sensitive (MCF-7) breast cancer cell lines were evaluated. Against estrogen non-sensitive (MDA-MB 231) cancer cell lines, deoxysericoside (TM36) was profoundly active compared to the control. Terminolic acid (TM32), arjungenin (TM34), and arjunglucoside I (TM35) were also active. Against estrogen sensitive (MCF-7) breast cancer cell lines, deoxysericoside (TM36) exhibited significant activity (p < 0.05) compared to control experiments. The most active compound had an optimum concentration of 30 μg/mL. Deoxysericoside (TM36) showed concentration-dependent inhibition percentages at 15 and 30 μg/mL, and MDA-MB 231 breast carcinoma cells were more susceptible. MDA-MB 231 treated with 15 and 30 μg/mL of deoxysericoside (TM36) showed significant reduction (p < 0.05) in clone formation after 48 h when compared to untreated controls, suggesting that it can restrict cancer to a preliminary stage. The deoxysericoside (TM36) reduced cell migration with dose-dependent improvement in wound healing at 15 and 30 μg/mL, revealed by the micrographs. Molecular docking indicated that the compounds fit well into hERα and PI3Kα receptor binding sites, forming stable complexes with binding energies in ranges of -9.04 to -5.02 kcal mol-1 (hERα receptor) and -8.84 to -5.97 kcal mol-1 (PI3Kα receptor). The compounds exhibited appreciable drug likeness predicted using SwissADME.
Conclusion:
The studies showed that the isolated compounds could be used for the development of anticancer therapies.

