Synthesis and screening of anti-cancer, antioxidant, and anti-inflammatory activities of novel galloyl pyrazoline derivatives

被引:10
|
作者
Abdel-Aziz, Mohamed [2 ]
Gamal-Eldeen, Amira M. [1 ]
机构
[1] Natl Res Ctr, Ctr Excellence Adv Sci, Canc Biol Lab, Cairo 12622, Egypt
[2] Menia Univ, Fac Pharm, Dept Med Chem, Al Minya, Egypt
关键词
2-Pyrazoline; galloyl derivatives; anti-cancer; anti-inflammatory; antioxidant; IN-VITRO; FLAVONOIDS; TANNINS;
D O I
10.1080/13880200902946452
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
A novel series of galloyl-2-pyrazoline derivatives were synthesized and screened for their cytotoxic effect against hepatocellular carcinoma (Hep-G2) and colon carcinoma (HCT-116) cells using the MTT assay, proliferative effect on the immune cells RAW macrophage 264.7 using the MTT assay, anti-inflammatory activity through measurement of the accumulation of nitrites using Griess reagent, and for their antioxidant activity through scavenging of the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. Most of the tested compounds had a concomitant weak cytotoxic effect against both Hep-G2 and HCT-116 cells, except 5-(2-furyl)-4,5-dihydro-1-(3,4,5-trihydroxybenzoyl)-3-(3,4-dimethoxyphenyl)-1H-pyrazole (IC50 8.4 mu g/mL and 18.6 mu g/mL) and 5-(4-cyanophenyl)-4,5-dihydro-1-(3,4,5-trihydroxybenzoyl)-3-(3,4-dimethoxy-phenyl)-1H-pyrazole (IC50 15.2 mu g/mL, 31.5 mu g/mL), which exhibited a cytotoxic effect against Hep-G2 and HCT-116 cells, respectively, while only 5-(2,6-dichlorophenyl)-4,5-dihydro-1-(3,4,5-trihydroxybenzoyl)-3-(3,4-dimethoxyphenyl)-1H-pyrazole was a significant dose-dependent inducer of macrophage proliferation. On the other hand, all of the tested compounds were significant inhibitors of LPS-stimulated NO generation and potential scavengers of the DPPH radical, except 1-(3,4,5-trihydroxybenzoyl)-4,5-dihydro-5-(4-methoxyphenyl)-3(3,4-dimethoxyphenyl)-1H-pyrazole.
引用
收藏
页码:854 / 863
页数:10
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