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Rongliflozin L -pyroglutamic acid, a highly active SGLT-2 inhibitor cocrystal discovered and developed by our group, is currently undergoing clinical trials for the treatment of diabetes. Here, we report and design a simple and robust process to obtain a single and pure crystalline form I (1) of the cocrystal, containing Rongliflozin (2) with L -pyroglutamic acid (L -PA), based on coformer-induced purification (CoIP). Extensive experiments showed that the addition of L -pyroglutamic acid in the eluent was key to suppression of the dissociation equilibrium of the cocrystal during lessivation, with high efficiency. Importantly, based in this profile, this process exhibited strong robustness and margin of safety at multigram and multikilogram scales. [ABSTRACT FROM AUTHOR]

Simple Summary: This study found that moringa (Moringa oleifera) leaves' water extract triggered phenoloxidase activity, phagocytic rate, and superoxide anion production in whiteleg shrimp (Penaeus vannamei) hemocytes by an in vitro assay. By an in vivo assay, a dietary moringa extract enhanced the total hemocyte count, phenoloxidase activity, phagocytic rate, immune-related gene expressions, and growth performance of the whiteleg shrimp. The administration of dietary moringa extract increased the survival rate after challenging the whiteleg shrimp with Vibrio alginolyticus. Moringa is widely known as a plant with high medicinal properties. Therefore, moringa has a high potential for use as an immunostimulant in shrimp. This study investigated the effect of a moringa water extract on the immune response, resistance against V. alginolyticus, and growth performance of whiteleg shrimp. To perform the in vitro assay, hemocytes were incubated with different concentrations of the moringa extract. Furthermore, the moringa extract was incorporated at 0 (control), 1.25 g (ME1.25), 2.5 g (ME2.5), and 5.0 g (ME5.0) per kg of diet for the in vivo assay. During the rearing period, immune responses, namely the total hemocyte count (THC), phenoloxidase (PO) activity, phagocytosis activity, superoxide anion production, and immune-related gene expression were examined on days 0, 1, 2, 4, 7, 14, 21, and 28. Growth performance was measured 60 days after the feeding period. Furthermore, the shrimp were challenged with V. alginolyticus after being fed for different feeding durations. The results of the in vitro assay revealed that 100–250 ppm of the moringa extract enhanced the PO activity, phagocytic rate (PR), and superoxide anion production. The findings of the in vivo assay demonstrated that the THC, PO activity, PR, and immune-related gene expression, including alpha-2-macroglobulin, prophenoloxidase II, penaeidin2, penaeidin3, anti-lipopolysaccharide factor, crustin, lysozyme, superoxide dismutase, and clotting protein, were higher in the group of ME.25 and ME5.0 than in the control and ME1.25 at several time points. Growth performance was significantly increased (p < 0.05) in the ME2.5 group compared to the control group. Furthermore, the dietary ME2.5 resulted in a higher survival rate compared to that of the control group after challenging with V. alginolyticus, especially at ME2.5 administered for 4 and 7 days. This study indicated that the incorporation of the moringa extract at 2.5 g per kg of diet enhanced the immune response, the growth performance of the whiteleg shrimp, and the resistance against V. alginolyticus infection. [ABSTRACT FROM AUTHOR]

Sarcodia suieae acetyl-xylogalactan was reported to induce macrophage polarisation, and could positively regulate macrophage activation. In this study, we evaluated the effect of Sarcodia suieae acetyl-xylogalactan on the Nile tilapia. First, we assessed the influence of acetyl-xylogalactan on the survival, glucose uptake, and phagocytic activity of tilapia head kidney (THK) melanomacrophage, and observed increased proliferation of these cells in the MTT assay after 12 and 24 h of treatment. Glucose uptake increased in THK melanomacrophage treated with 20 and 30 μg acetyl-xylogalactan for 24 h. Their phagocytic activity was positively enhanced following exposure to acetyl-xylogalactan. Nile tilapia were fed with acetyl-xylogalactan for 4 weeks. At the end of the experiment, Nile tilapia were sacrificed, and the lipopolysaccharide-induced liver and head-kidney apoptosis was examined under reducing conditions in comparison with controls. The phagocytic activities of liver and head-kidney cells were enhanced after 4 weeks of feeding. Blood biochemical analysis revealed a reduction in glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT) levels after 4 weeks of feeding. Combined with in vitro and in vivo experiments results, the extracted S. suieae acetyl-xylogalactan could directly induce THK melanomacrophage proliferation, glucose uptake, and phagocytic activity. Acetyl-xylogalactan was able to induce Nile tilapia liver and head-kidney resident macrophage activity, and reduced LPS-induced liver and head-kidney cell apoptosis. S. suieae acetyl-xylogalactan may modulate Nile tilapia macrophage activation by polarising them into M1 macrophages to improve the Nile tilapia nonspecific immune response. [ABSTRACT FROM AUTHOR]

Reported herein is a practical, economical, and efficient construction of 3-alkylated quinoxalin-2(1 H )-ones with alkyl carboxylic acids and alkyl iodides by quinoxalin-2(1 H )-one excitation and cobaloxime catalysis. Primary, secondary, and tertiary alkyl iodides and carboxylic acids all could be efficiently transferred into target products with excellent functional group tolerance. Mechanism studies reveal that the quinoxalin-2(1 H )-one derivatives could be directly excited and yield alkyl carbon radicals from alkyl carboxylic acids and alkyl iodides with the aid of the cobaloxime complex.

In order to understand the occurrence characteristics and ecological risks of pharmaceuticals and personal care products (PPCPs) in surface water and sediments of Hongze Lake and Gaoyou Lake in the lower reaches of the Huaihe River, 43 surface water and sediment samples from 23 sampling sites were collected, and 61 PPCPs were detected in the samples. The concentration level and spatial distribution of target PPCPs in Hongze Lake and Gaoyou Lake were analyzed, the distribution coefficient of typical PPCPs in the water/sediment system in the study area was calculated, and the ecological risk of target PPCPs was evaluated using the entropy method. The results showed that the PPCPs in surface water of Hongze Lake and Gaoyou Lake were 1.56-2534.44 ng·L -1 and 3.32-1027.47 ng·L -1 , respectively, and those in sediment were 1.7-926.7 ng·g -1 and 1.02-289.37 ng·g -1 , respectively. The concentrations of lincomycin (LIN) in surface water and doxycycline (DOX) in sediment were the highest, and antibiotics were the main components. The spatial distribution of PPCPs was higher in Hongze Lake and lower in Gaoyou Lake. The distribution characteristics of typical PPCPs in the study area showed that typical PPCPs tended to stay in the water phase, and there was a significant correlation between lg K oc and lg K d , indicating that total organic carbon (TOC) played an important role in the distribution of typical PPCPs in the water/sediment system. The ecological risk assessment results showed that the ecological risk of PPCPs to algae in surface water and sediment was significantly higher than that of fleas and fish, the ecological risk value of PPCPs in surface water was higher than that in sediment, and the ecological risk of Hongze Lake was higher than that of Gaoyou Lake.

In this study, we separately collected rainwater sewer sediments from typical samples in Suzhou city, such as the urban commercial district, historical and cultural protection area, cultural and educational area, and living area, and analyzed the particle size distribution of the sediments and the characteristics of carbon, nitrogen, phosphorus content, and pollution load distribution under each graded particle size. The median particle size D 50 of each sample point was 16.55-327.50 μm, and the particle size trend was as follows:commercial area > living area > historical and cultural protection area > cultural and educational area. D 50 was related to the total organic carbon (TOC). The total nitrogen (TN), total phosphorus (TP), and ammonia nitrogen (NH 4 + -N) were significantly positively correlated, as were the pollutants. The spatial difference of ω (TOC), ω (TN), ω (TP), and ω (NH 4 + -N) in rainwater sewer sediments from different regions was as follows:commercial area > historical and cultural protection area > living area > cultural and educational area, in which ω (TOC) was 0.84%-6.76%, and ω (TN), ω (TP), and ω (NH 4 + -N) were 917.5-12707.1, 196.1-2524.8, and 9.3-156.8 mg·kg -1 , respectively. TOC, TP, and NH 4 + -N pollution loads were mainly concentrated on particles ≤ 75 μm and 250-1000 μm. Street dust pollutants highly differed spatially, with a high content of attached pollutants on street dust particles with a particle size of ≤ 75 μm. Various pollutants migrated into the street dust-pipes, and TP and TN showed certain enrichment characteristics in the sewer. Controlling the transportation of street dust and the accumulation of sediments in the sewer can reduce the pollution of sediment into the rivers during the rainy season.