Browsing by Author "Hafez, Ahmed M"

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    Development of Semisynthetic Apoptosis-Inducing Agents Based on Natural Phenolic Acids Scaffold: Design, Synthesis and In-Vitro Biological Evaluation
    (Multidisciplinary Digital Publishing Institute (MDPI), 2022-10) Ezzat, Shahira M; Teba, Heba El Sayed; Shahin, Inas G; Hafez, Ahmed M; Kamal, Aliaa M; Aborehab, Nora M
    : A crucial target in drug research is magnifying efficacy and decreasing toxicity. Therefore, using natural active constituents as precursors will enhance both safety and biological activities. Despite having many pharmacological activities, caffeic and ferulic acids showed limited clinical usage due to their poor bioavailability and fast elimination. Therefore, semisynthetic compounds from these two acids were prepared and screened as anticancer agents. In this study, CA and FA showed very potent anticancer activity against Caco-2 cells. Consequently, eighteen derivatives were tested against the same cell line. Four potent candidates were selected for determination of the selectivity index, where compound 10 revealed a high safety margin. Compound 10 represented a new scaffold and showed significant cytotoxic activity against Caco-2. Cell-cycle analysis and eval- uation of apoptosis showed that derivatives 10, 7, 11, 15 and 14 showed the highest proportion of cells in a late apoptotic stage. :
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    The medicinal activity of lyophilized aqueous seed extract of Lepidium sativum L. in an androgenic alopecia model
    (Nature Publishing Group, 2023-05) Albalawi, Marzough Aziz; Hafez, Ahmed M; Elhawary, Seham S; Sedky, Nada K; Hassan, Omnia F; Bakeer, Rofanda M; Abd El Hadi, Soha; El‑Desoky, Ahmed H; Mahgoub, Sebaey; Mokhtar, Fatma A
    This study evaluated the topical efect of Lepidium sativum lyophilized seed extract (LSLE) towards Sustanon-induced alopecia in male adult Wistar albino rats in vivo, compared to minoxidil topical reference standard drug (MRD). LC–MS/MS together with molecular networking was used to profle the metabolites of LSLE. LSLE treated group revealed signifcant changes in alopecia related biomarkers, perturbation of androgenic markers; decline in testosterone level and elevation in 5α-reductase (5-AR); decline in the cholesterol level. On the other hand, LSLE treated group showed improvement in vascular markers; CTGF, FGF and VEGF. Groups treated topically with minoxidil and LSLE showed signifcant improvement in hair length. LC–MS/MS profle of LSLE tentatively identifed 17 constituents: mainly glucosinolates, favonoid glycosides, alkaloids and phenolic acids. The results point to the potential role of LSLE in the treatment of alopecia through decreasing 5(alpha)- dihydrotestosterone levels. Molecular docking was attempted to evaluate the probable binding mode of identifed compounds to androgen receptor (PDB code: 4K7A).