Search Results (3)

Glutathione transferases (GSTs; EC 2.5.1.18) form a group of multifunctional enzymes that are involved in phase II of the cellular detoxification mechanism and are associated with increased susceptibility to cancer development and resistance to anticancer drugs. The present study aims to evaluate the ligandability of the human GSTM1-1 isoenzyme (hGSTM1-1) using a broad range of structurally diverse pesticides as probes. The results revealed that hGSTM1-1, compared to other classes of GSTs, displays limited ligandability and ligand-binding promiscuity, as revealed by kinetic inhibition studies. Among all tested pesticides, the carbamate insecticide pirimicarb was identified as the strongest inhibitor towards hGSTM1-1. Kinetic inhibition analysis showed that pirimicarb behaved as a mixed-type inhibitor toward glutathione (GSH) and 1-chloro-2,4-dinitrobenzene (CDNB). To shine a light on the restricted hGSTM1-1 ligand-binding promiscuity, the ligand-free crystal structure of hGSTM1-1 was determined by X-ray crystallography at 1.59 Å-resolution. Comparative analysis of ligand-free structure with the available ligand-bound structures allowed for the study of the enzyme’s plasticity and the induced-fit mechanism operated by hGSTM1-1. The results revealed important structural features of the H-site that contribute to xenobiotic-ligand binding and specificity. It was concluded that hGSTM1-1 interacts preferentially with one-ring aromatic compounds that bind at a discrete site which partially overlaps with the xenobiotic substrate binding site (H-site). The results of the study form a basis for the rational design of new drugs targeting hGSTM1-1. Full article

Being in a confined environment causes chronic stress in gestating sows, which is detrimental for sow health, welfare and, consequently, offspring physiology. This study assessed the health and welfare of gestating sows housed in a group housing system compared to individual gestation stalls. After pregnancy was confirmed, experimental sows were divided randomly into two groups: the group housing system (GS), with the electronic sow feeding (ESF) system; or individual stall (IS). The behavior of sows housed in the GS or IS was then compared; throughout pregnancy, GS sows displayed more exploratory behavior, less vacuum chewing, and less sitting behavior (p < 0.05). IS sows showed higher stress hormone levels than GS sows. In particular, at 41 days of gestation, the concentration of the adrenocorticotropic hormone (ACTH) and adrenaline (A) in IS sows was significantly higher than that of GS sows, and the A level of IS sows remained significantly higher at 71 days of gestation (p < 0.01). The lipopolysaccharide (LPS) test was carried out in the weaned piglets of the studied sows. Compared with the offspring of gestating sows housed in GS (PG) or IS (PS), PG experienced a shorter period of high temperature and showed a quicker return to the normal state (p < 0.05). Additionally, their lower levels of stress hormone (p < 0.01) suggest that PG did not suffer from as much stress as PS. These findings suggested that gestating sows housed in GS were more able to carry out their natural behaviors and, therefore, had lower levels of stress and improved welfare. In addition, PG also showed better disease resistance and resilience. These results will provide a research basis for the welfare and breeding of gestating sows. Full article

This study was conducted to provide commercial pig farms with information about group housing systems for sows in accordance with the amendment of the prohibition law for individual stalls for sows in South Korea. Therefore, this experiment was performed to compare the effects of individual stalls (IS) and group housing systems (GS) on the productivity of sows to investigate the feasibility of replacing individual stalls with group housing systems in commercial sow units. Forty primiparous sows (Landrace × Yorkshire; 210.67 ± 2.22 kg average initial body weight) were randomly assigned to four treatments with restricted feeding after 8 weeks from artificial insemination. The four treatments were (i) individual stalls (IS; housed in pen stalls), (ii) short stalls (SS; sows housed in pens with non-gated feeding stalls), (iii) free access stalls (FAS; a non-competitive housing system), and (iv) electronic sow feeders (ESF; used with radio frequency identification technology to allow individual sow management without individual confinement). All sows were transferred to farrowing crates at 110 days of gestation. There were no differences in sow productive performance, reproductive performance, and colostrum composition between IS and GS and among GS. The considered GS did not negatively affect any productivity parameters of primiparous sows compared with IS; the GS could replace IS in commercial sow units. Full article