Monophosphoramide derivatives: synthesis and crystal structure, theoretical and experimental studies of their biological effects.

Synthesizing new chemical compounds and studying their biological applications have been important issues in scientific research. In this investigation, we synthesized and characterized ten new N-acetyl phosphoramidate compounds and explored the crystal structure of three others. Furthermore, not only were some kinetic inhibition parameters measured, like IC50, Ki, kp, KD for 7 compounds on human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), but also their hydrophobic parameter was determined by shake-flask technique. All compounds (number 1-10) were investigated for anti-bacterial activity against three Gram-positive and three Gram-negative bacteria, while chloramphenicol was used as a standard antibiotic. In order to find new insecticide, toxicities of 13 acephate (Ace)-derived compounds (number 20-32) were bioassayed on third larval instar of elm leaf beetle and Xanthogaleruca luteola. Additionally, screening in vivo tests revealed that two compounds had had the greatest insecticidal potential in comparison with others. It means these ones inhibited AChE (with mixed mechanisms) and general esterase more than the rest. According to ChE-QSAR models, the inhibitory potency for enzyme and bacteria is directly influenced by the electronic parameters versus structural descriptors. AChE-QSPR model of fluorescence assay indicated that the inhibitory power of AChE is primarily influenced by a set of electronic factors with the priority of: EHB > PL > δ(31P) versus structural descriptor (SA and Mv). Synthesizing new chemical compounds and studying their biological applications have been important issues in scientific research. Toxicities of 13 acephate (Ace)-derived compounds (number 20-32) were bioassayed on third larval instar of elm leaf beetle and Xanthogaleruca luteola. Insect-QSAR equations of these compounds, based on MLR and PCA, showed that non-descriptor net charge nitrogen atom (which was affected by the polarization of N-H group) had the greatest effect on insecticidal potential.

Effects of enzymatically hydrolyzed yeast supplementation on blood attributes, antioxidant status and gene expression of cytokines in vaccinated dairy cows.

This study was done to assess the effects of hydrolyzed yeast on blood cells counts, antioxidant status and gene expression of pro-inflammatory and anti-inflammatory cytokines of vaccinated dairy cows. Twenty Holstein lactating dairy cows were randomly divided into four groups received basal diet without (control) and with 10, 20 and 30 g/d/head of hydrolyzed yeast. Cows were vaccinated against foot and mouth disease virus at day 10 and blood samples were taken 10 days after. Cows received hydrolyzed yeast at doses of 20 and 30 g/d/head had the lowest and those in the control group had the highest malondialdehyde concentration. Cows received hydrolyzed yeast at dose of 20 g/d/head had the highest lymphocyte and the lowest neutrophil/lymphocyte ratio. IL-1ß and TNF-α downregulated and INF-γ up-regulated in cows received different doses of hydrolyzed yeast. The lowest expression of IL-1ß and TNF-α and the highest expression of INF-γ was for cows received hydrolyzed yeast at dose of 20 g/d/head. The highest titers against foot and mouth disease virus were for cows received hydrolyzed yeast at dose of 20 g/d/head and the lowest titer was for the control group. Supplementation of 20 g/d/head hydrolyzed yeast recommended in vaccinated cows.