A series of β-carboline oxadiazoles were synthesized, and their fungicidal activities and mechanism of action against rice sheath blight caused by Rhizoctonia solani was evaluated. The results showed that all of these compounds exhibited significant in vitro fungicidal activity. Significantly, compound 5i (EC = 4.2 μg/mL) displayed the best efficacy and superior fungicidal activity compared to validamycin A (EC = 197.6 μg/mL). Moreover, the in vivo test also demonstrated that compound 5i could effectively control rice sheath blight and showed higher in vivo protective and curative activities against R. solani than validamycin A. Preliminary mechanism studies revealed that compound 5i caused the loss of mitochondrial membrane potential, reactive oxygen species accumulation, cell membrane destruction, and DNA synthesis interference. These findings indicated that compound 5i displayed superior fungicidal activities against R. solani and could be a potential fungicidal candidate against rice sheath blight.

Dietary zinc oxide (ZnO) at pharmacological level has been widely used to prevent and treat diarrhea in weaning piglets. Despite its importance for promoting animal health and performance, the influence of microbiome profiles in intestinal tracts by ZnO needs to be comprehensively investigated. In this study, we conducted a comparative microbial community analysis in the ileum and colon of piglets fed by either control diet, high ZnO (3,000 mg/kg) supplement or antibiotics (300 mg/kg chlortetracycline and 60 mg/kg colistin sulfate) supplement. Our results showed that both high dietary ZnO and in-feed antibiotics supplementations significantly increased 5 phyla of Spirochaetes, Tenericutes, Euryarchaeota, Verrucomicrobia, TM7, and reduced 1 phyla of Chlamydiae in ileal digesta. The relative abundance of opportunistic pathogens Campylobacterales were decreased while Enterobacteriales were increased in ZnO or antibiotics-supplemented group when compared to the control. In the colon, the phyla Euryarchaeota, the genus Methanobrevibacter, and the species Methanobrevibacter smithii were drastically increased by high dietary ZnO supplementation when compared with other groups. The microbial functional prediction analysis showed that high dietary ZnO and in-feed antibiotics had a higher abundance of transporter pathway enrichment in the ileum when compared with the control. While in the colon high dietary ZnO had a higher abundant enrichment of methane metabolism involving energy supply when compared with other groups. Both high dietary ZnO and antibiotics increased the microbiota diversity of ileal digesta while they decreased the microbiota diversity of the colonic digesta. Collectively, these results suggested that dietary ZnO and in-feed antibiotics supplementations presented similar effect on ileal microbiota, and mainly affected the non-predominant microbiota.

Based on the bioassay result and quantitative structure-activity relationship (QSAR) information, structure modification in β-carboline warrants further investigation and its benzoylurea derivative 17c, which showed the best fungicidal activities, could emerge as a potential fungicide against rice sheath blight. © 2018 Society of Chemical Industry.

The objective of the present study was to investigate the effects of dietary supplementation with glycitein, a major soy isoflavone, during late pregnancy (starting on d 85) and lactation on antioxidative indices and performance in primiparous sows. A total of 227 gilts (Yorkshire × Landrace) were used, and after parturition, piglets were cross-fostered within treatment so that each sow suckled 10 piglets. Gilts were randomly divided into 4 groups on d 85 of pregnancy and thereafter fed the basal diets of gestation or lactation (controls) or those supplemented with 15, 30, or 45 mg/kg diet glycitein. Reproductive performance of the sows, growth of litters, concentration of plasma glycitein, milk composition, and antioxidative indices in sows' plasma and milk, such as the activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GSH-Px), total antioxidant capacity (T-AOC), and the content of malondialdehyde (MDA), were measured. Supplementation of the dam's diets with glycitein increased ADG of piglets (linear, P = 0.003) and weaned BW of litters (linear, P = 0.01) and both variables were approximately 10% greater than controls with the 45 mg/kg treatment. The percentage of milk protein was linearly (P < 0.05) increased on d 1 and 7 of lactation, and milk fat content increased on d 7 and 14 (linear, P< 0.05). All other measured indices of performance were unaffected by supplementation with glycitein (P > 0.05). The glycitein concentration in sow's plasma was linearly (P < 0.0001) elevated. During lactation, linear increases occurred in plasma activities of SOD (P < 0.001) and T-AOC (P < 0.05 to P< 0.001), CAT (d 7 to 18 of lactation, P < 0.05) and GSH-Px (d 7 of lactation, P < 0.05), whereas the content of plasma MDA decreased (linear, P < 0.05) throughout lactation with glycitein supplementation. Activities of CAT and T-AOC in milk were not affected by maternal supplementation with glycitein, but increases in SOD on d 18 of lactation (P< 0.001) and GSH-Px in colostrum (P < 0.05) were observed. The content of MDA in milk was decreased (linear, P< 0.05) at all stages of lactation except d 14. Collectively, the results of this study indicate that dietary supplementation with glycitein in sows during late pregnancy and lactation elevated the antioxidative indices, decreased the content of MDA in sow's plasma and milk, improved milk composition, and enhanced the growth performance of the sucking piglets.

Forty-eight Duroc x Landrace x Large White gilts were used to determine the relationship between proteome changes of longissimus muscle and intramuscular fat (IMF) content in arginine-supplemented pigs. Beginning at 60 kg BW, pigs were fed a corn- and soybean meal-based diet supplemented or not with 1% L-arginine until they reached a BW of 100 kg. Supplementation with 1% L-arginine did not affect the growth performance or carcass traits, while it increased IMF content by 32% (P < 0.01), it also decreased the drip loss at 48 h post-mortem and the b* meat color value at 24 h post-mortem; supplementation with 1% dietary L-arginine did not change the proportion of SFA and MUFA in muscle lipids. The proteome changes in longissimus muscle between the control and supplemented pigs showed that L-arginine significantly influenced the abundance of proteins related to energy metabolism, fiber type and structure. The increase in IMF content was positively correlated with the increased abundance of slow twitch troponin I (TNNI1) protein and negatively correlated with myosin heavy chain IIb (MyHC IIb) protein content. It is suggested that the proteome changes in longissimus muscle contributed to the greater IMF content in L-arginine supplemented pigs.