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RISS 인기검색어
- 검색키워드
- 저자 : Mansour S. Al-Said (검색결과 3 건)
- 무료
- 기관 내 무료
- 유료
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Antitumor Activity of Novel Pyridine, Thiophene and Thiazole Derivatives
Mostafa M. Ghorab,Mansour S. Al-Said 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.6
2-Cyano-N'-[1-(2,5-dimethoxyphenyl)]ethylideneacetohydrazide 1 was obtained via reaction of cyanoacetic acid hydrazide with 2,5-dimethoxyacetophenone. A number of novel pyridines 2aj, 3, 4, thiophenes 5-9 and thiazoles 10-12 were prepared by using the hydrazide-hydrazone derivative 1 as a starting material. The structure of the newly synthesized compounds was characterized by elemental analyses, IR, 1H-NMR, 13C-NMR and mass spectral data. All the target compounds were subjected to in vitro antitumor activity against Ehrlich Ascites Carcinoma (EAC) cells. Compounds 2j and 6 showed a higher activity with IC50 values (54.54, 61.57 μM), 8 when compared with a reference drug IC50 value (68.99 μM), while compound 5 is nearly as active as Doxorubicin (CAS 23214-92-8).
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Anticancer Activity of Novel Indenopyridine Derivatives
Mostafa M. Ghorab,Mansour S. Al-Said 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.6
Eighteen new 4-[2-amino-3-cyano-5-oxo-4-substitutedaryl-4H-indeno[1,2-b]pyridin-1-(5H)-yl]benzenesulfonamide derivatives 6a-q were synthesized via a reaction of aromatic aldehydes, enaminone 3 and malononitrile in one-pot reaction. Also, compounds 6a-q were obtained, via another route by reaction of enaminone 3 with arylidenemalononitriles 4a-q. The structure of the synthesized compounds was characterized by microanalysis, IR, 1H-NMR, 13C-NMR and mass spectral data. All the target compounds were subjected to in vitro anticancer activity against breast cancer cell line (MCF7). Compound 6d showed a higher potency with IC50 value (4.34 μM) than that of the Doxorubicin (5.40 μM), as the reference drug, while compound 6n with IC50 value (6.84 μM) is nearly as active as Doxorubicin. Also, compounds 6a-c, 6e, 6f, 6h and 6p exhibited a moderate activity, while compounds 3, 6g, 6i-m, 6o and 6q showed weak activity.
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Proanthocyanidin-Rich Date Seed Extract Protects Against Chemically Induced Hepatorenal Toxicity
Atallah F. Ahmed,Jawaher H. Al-Qahtani,Hanan M. Al-Yousef,Mansour S. Al-Said,AbdelKader E. Ashour,Mohammed Al-Sohaibani,Syed Rafatullah 한국식품영양과학회 2015 Journal of medicinal food Vol.18 No.3
A hydroacetone extract was prepared from seeds of Phoenix dactylifera L. var. Khalas, which is an industrial by-product of date processing. The proanthocyanidin nature of the extract (coded as DTX) was characterized by phytochemical and nuclear magnetic resonance (NMR) analyses. The total phenol/proanthocyanidin content and antioxidant activity of DTX were estimated by Folin–Ciocalteu, vanillin-sulfuric acid, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays, respectively. The hepatorenal protective activity of DTX was evaluated using CCl4-induced toxicity model in rats, in comparison with silymarin (SYL). Results of the histopathological examination and measurements of various hepatorenal serum indices and tissue biochemical markers demonstrated that DTX displayed marked protective potential against CCl4-induced liver and kidney injury at 100 mg/kg/rat. Relative to the control CCl4-intoxicated group, pretreatment with DTX significantly (P<.001) suppressed the elevated serum levels of alanine aminotransferase and aspartate aminotransferase (ALT and AST), alkaline phosphatase (ALP), γ-glutamyl transferase (GGT), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), bilirubin, creatinine, and calcium, whereas it significantly (P<.001) increased the diminished serum levels of high-density lipoprotein cholesterol (HDL-C) and total protein (TP). Moreover, DTX significantly decreased malondialdehyde (MDA) formation and increased TP synthesis in hepatorenal tissues compared with the intoxicated control. The improvement in biochemical parameters by DTX was observed in a dose-dependent manner and confirmed by restoration of normal histological features. The acute toxicity test of DTX in rats revealed safety of the extract. This study reveals that DTX enhances the recovery from xenobiotics-induced toxicity initiated by free radicals.
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