Browsing by Author "Khalil W.K.B."

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Antitumor activity of Cuphea ignea extract against benzo(a)pyrene-induced lung tumorigenesis in Swiss Albino mice
(Taylor and Francis Ltd., 2019) Hassan S.K.; Mousa A.M.; El-Sammad N.M.; Abdel-Halim A.H.; Khalil W.K.B.; Elsayed E.A.; Anwar N.; Linscheid M.W.; Moustafa E.S.; Hashim A.N.; Nawwar M.; Department of Biochemistry; National Research Centre; Dokki; Cairo; Egypt; Department of Cell Biology; National Research Centre; Dokki; Cairo; Egypt; Bioproducts Research Chair; Zoology Department; College of Science; King Saud University; Riyadh; Saudi Arabia; Department of Chemistry of Natural and Microbial Products; National Research Centre; Dokki; Cairo; Egypt; Department of Pathology; National Cancer Institute; Cairo University; Cairo; Egypt; Laboratory of Applied Analytical and Environmental Chemistry; Humboldt-University; Berlin; Germany; October University of Modern Sciences and Arts; 6th October City; Egypt; Department of Phytochemistry and Plant Systematics; National Research Centre; Cairo; Egypt
Lung cancer has one of the highest mortality rates among various types of cancer and is the most frequent cancer in the world. The incidence of lung cancer is increasing rapidly, in parallel with an increased incidence of smoking. Effective chemoprevention may be an alternative strategy to control the incidence of lung cancer. Thus, the objective of current work was to ascertain the possible preventive and therapeutic efficacies of Cuphea ignea extract in a mouse model of lung tumorigenesis and its cytotoxicity toward the A549 human lung cancer cell line. Lung tumorigenesis was induced by the oral administration of benzo(a)pyrene (50 mg/kg b.w.) twice per week to Swiss albino mice for 4 weeks. Benzo(a)pyrene-treated mice were orally administered C. ignea (300 mg/kg body weight, 5 days/week) for 2 weeks before or 9 weeks after the first benzo(a)pyrene dose, for a total of 21 weeks. At the end of the administration period, various parameters were measured in the serum and lung tissues. The results revealed that the oral administration of benzo(a)pyrene resulted in increases in relative lung weight, serum levels of tumor markers (ADA, AHH, and LDH), and the inflammatory marker NF-?B, and a decreased total antioxidant capacity compared with the control. In addition, decreased levels of enzymatic and non-enzymatic antioxidants, with a concomitant increase in lipid peroxidation, metalloproteinases (MMP-2 and MMP-12), and the angiogenic marker VEGF were detected in lung tissues. Moreover, benzo(a)pyrene administration induced the upregulation of PKC?, COX-2, and Bcl-2 expression, with the downregulation of BAX and caspase-3 expression. C. ignea treatment alleviated all alterations in these parameters, which was further confirmed by the histopathological analysis of lung tissues. The findings of the current work provide the first verification of the preventive and therapeutic potentials of C. ignea extract against benzo(a)pyrene-induced lung tumorigenesis in mice. � 2019 The Authors
Cytotoxicity and gene expression profiles of novel synthesized steroid derivatives as chemotherapeutic anti-breast cancer agents
(2011) Elmegeed G.A.; Khalil W.K.B.; Mohareb R.M.; Ahmed H.H.; Abd-Elhalim M.M.; Elsayed G.H.; Hormones Department; National Research Centre; 12622 Dokki; Giza; Egypt; Cell Biology Department; National Research Centre; Dokki; Giza; Egypt; Organic Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); October City; Egypt; Chemistry Department; Faculty of Science; Cairo University; Cario; Egypt
Anti-cancer agents which combine two biologically active compounds in one such as steroidal heterocyclic derivatives attain both hormone and cytotoxic effects on cancer cells. The aim of the present study is to synthesize and evaluate new potential chemotherapeutic anti-breast cancer agents. Several pyridazino-, pyrimido-, quinazolo-, oxirano- and thiazolo-steroid derivatives were synthesized. The structure of the novel steroid derivatives was confirmed using the analytical and spectral data. The most structurally promising of the novel synthesized steroid derivatives, compounds 8, 12, 17, 20, 22c, 24c, 30a and 30b, were investigated individually as anti-breast cancer agents against human breast cancer cells (MCF-7) using sulforhodamine B (SRB) assay. The tested compounds 17, 20, 22c and 8 showed potent broad spectrum cytotoxic activity in vitro after 48 h incubation. Compound 17 (IC 50 = 2.5 ?M) exhibited more inhibitory influence on MCF-7 growth than the reference drug doxorubicin (Dox) (IC 50 = 4.5 ?M) after 48 h incubation. Also, the present study showed that all the tested steroid derivatives exhibited significant depletion with various intensities in gene expression of breast cancer related genes (VEGF, CYP19 and hAP-2?). Noteworthy, compounds 17, 20 and 22c showed the most pronounced effect in this respect. � 2011 Elsevier Ltd. All rights reserved.