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1.
Probiotics Antimicrob Proteins ; 12(2): 451-460, 2020 06.
Article in English | MEDLINE | ID: mdl-31111440

ABSTRACT

The probiotic effect of Enterococcus faecalis-1 (isolated from healthy chickens) on growth performance, immune response, and modulation of the intestinal microbiota of broilers was assessed with a total of 100-day-old commercial Cobb chicks. The chicks were randomly divided into two equal groups. The control group received a basal diet, while the test group received a basal diet and was orally supplied with E. faecalis at a dose of 108 CFU/bird/day. Results showed that E. faecalis-1 supplement significantly (P < 0.05) improved the body weight and feed conversion ratio of treated broilers compared with the control ones. The mortality percentage was reduced in E. faecalis-1-supplemented group. The total IgY serum level was significantly (P < 0.05) increased in broilers receiving E. faecalis-1 supplement (7.1 ± 0.39) compared with the control group (5.8 ± 0.3), while the serum avidin level was significantly (P < 0.05) decreased in E. faecalis-1-supplemented broilers (76 ± 11.1). There was no significant change in the immune response towards avian influenza and Newcastle vaccines in both groups. The total Lactobacillus and Enterococcus counts were significantly (P < 0.05) higher in the cecal contents of broilers given E. faecalis-1 than those that received the control treatment. E. faecalis-1 supplement enhanced the enzyme activities, antioxidant system, and liver functions of treated broilers compared with those in the control group. Collectively, these results showed that E. faecalis-1 could promote growth performance and immunological status and convey beneficial modulation of the cecal microbiota in broilers.


Subject(s)
Animal Nutritional Physiological Phenomena , Chickens , Enterococcus faecalis , Gastrointestinal Microbiome , Immunity , Probiotics/administration & dosage , Animals , Chickens/growth & development , Chickens/immunology
2.
Arzneimittelforschung ; 62(12): 554-60, 2012 Dec.
Article in English | MEDLINE | ID: mdl-23023518

ABSTRACT

VEGFR-2 tyrosine kinase inhibitors are currently receiving high interest in drug discovery process as anticancer agents. We have used virtual screening techniques in order to discover new scaffolds that can be used for developing new VEGFR-2 kinase inhibitors.Similarity ensemble approach was used to reduce the chemical space of ZINC database to select a subset of compounds. A validated structure-based pharmacophore was developed and adopted to screen the selected subset. Initial hits mapped to the pharmacophore were filtered using docking and scoring. Selected compounds were synthesized and biologically tested. Compound 9 showed very good cytotoxicity profile against the NCI 60 cancer cell lines, while compound 8 showed reasonable inhibition of VEGFR-2 tyrosine kinase.Stepwise virtual screening of databases such as ZINC may result in new scaffolds for developing VEGFR-2 kinase inhibitors.


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors , Algorithms , Cell Line, Tumor , Cell Survival/drug effects , Computer Simulation , Databases, Factual , Drug Screening Assays, Antitumor , Humans , Ligands , Models, Molecular , Molecular Conformation , Protein Kinase Inhibitors/pharmacology , User-Computer Interface
4.
Arch Pharm Res ; 22(2): 194-201, 1999 Apr.
Article in English | MEDLINE | ID: mdl-10230512

ABSTRACT

The reaction of thiocyanoacetamide (1) with alpha,beta-unsaturated ketones 2a,b resulted in the formation of the corresponding newly synthesized 1(H)-pyridinethione derivatives 3a,b. Compounds 3a,b were used as synthons for the preparation of 2-S-alkyl-, 2-S-aryl-, 2-S-acetamidopyridine, thieno[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives via a wide range of reactions with different reagents. The antimicrobial activity of some of the newly synthesized compounds was tested. Compounds 3a, 11a, 15a, and 19a,b were found to be the most active ones.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Pyrazoles/chemical synthesis , Pyridines/chemical synthesis , Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Pyrazoles/pharmacology , Pyridines/pharmacology
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