Browsing by Author "Sedky, Nada K"
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Item 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 AThis 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).Item New proapoptotic chemotherapeutic agents based on the quinolone‑3‑carboxamide scafold acting byVEGFR‑2 inhibition(Springer, 2023-06) El‑Fakharany, Zeinab S; Nissan, Yassin M; Sedky, Nada K; Arafa, Reem K.; Abou‑Seri, Sahar M.In the current study, we designed and synthesized a series of new quinoline derivatives 10a-p as antiproliferative agents targeting cancer through inhibition of VEGFR-2. Preliminary molecular docking to assess the interactions of the designed derivatives with the binding site of VEGFR-2 (PDB code: 4ASD) displayed binding poses and interactions comparable to sorafenib. The synthesized compounds exhibited VEGFR-2 inhibitory activity with IC50 ranging from 36 nM to 2.23 μM compared to sorafenib (IC50 = 45 nM), where derivative 10i was the most potent. Additionally, the synthesized derivatives were evaluated in vitro for their cytotoxic activity against HepG2 cancer cell line. Seven compounds 10a, 10c, 10d, 10e, 10i, 10n and 10o (IC50 = 4.60, 4.14, 1.07, 0.88, 1.60, 2.88 and 2.76 μM respectively) displayed better antiproliferative activity than sorafenib (IC50 = 8.38 μM). Compound 10i was tested against Transformed Human Liver Epithelial-2 normal cell line (THLE-2) to evaluate its selective cytotoxicity. Furthermore, 10i, as a potent representative of the series, was assayed for its apoptotic activity and cell cycle kinetics’ infuence on HepG2, its efects on the gene expression of VEGFR-2, and protein expression of the apoptotic markers Caspase-7 and Bax. Compound 10i proved to have a potential role in apoptosis by causing signifcant increase in the early and late apoptotic quartiles, a remarkable activity in elevating the relative protein expression of Bax and Caspase-7 and a signifcant reduction of VEGFR-2 gene expression. Collectively, the obtained results indicate that compound 10i has a promising potential as a lead compound for the development of new anticancer agents