Waterlogging has negative effects on crop yield. Physiological and transcriptome data of two peanut cultivars [Zhongkaihua 1 (ZKH 1) and Huayu 39 (HY 39)] were studied under normal water supply and waterlogging stress for 5 or 10 days at the flowering stage. The results showed that the main stem height, the number of lateral branches, lateral branch length, and the stem diameter increased under waterlogging stress, followed by an increase in dry matter accumulation, which was correlated with the increase in the soil and plant analysis development (SPAD) and net photosynthetic rate (Pn) and the upregulation of genes related to porphyrin and chlorophyll metabolism and photosynthesis. However, the imbalance of the source–sink relationship under waterlogging was the main cause of yield loss, and waterlogging caused an increase in the sucrose and soluble sugar contents and a decrease in the starch content; it also decreased the activities of sucrose synthetase (SS) and sucrose phosphate synthetase (SPS), which may be due to the changes in the expression of genes related to starch and sucrose metabolism. However, the imbalance of the source–sink relationship led to the accumulation of photosynthate in the stems and leaves, which resulted in the decrease of the ratio of pod dry weight to total dry weight (PDW/TDW) and yield. Compared with ZKH 1, the PDW of HY 39 decreased more probably because more photosynthate accumulated in the stem and leaves of HY 39 and could not be effectively transported to the pod.

Waterlogging has a negative effect on peanut production, but few studies have focused on the relationship between the geographical origin and waterlogging tolerance of peanut varieties. To explore this problem, three different peanut ecotypes (Zhanhong 2, Zhongkaihua 1, and Huayu 39) were waterlogged for 5, 10, and 15 days at seedling stage (S), flowering and pegging stage (F), and pod-filling stage (P), respectively. The relationship between the ecotype and waterlogging tolerance was determined by analyzing the effects of waterlogging on dry matter accumulation, photosynthetic characteristics, yield, and the yield components of peanut. The soil and plant analysis development (SPAD), net photosynthetic rate (Pn), stomatal conductance (Gs), transpiration rate (Tr), and intercellular CO2 concentration (Ci) values in leaves decreased under waterlogging stress, which led to a significant decrease in yield and yield components. The most noticeable effect of waterlogging stress appeared at the P stage and deleterious effects increased with an extension of the duration of waterlogging, where the yield loss was mainly attributed to the decrease in the number of total pods (TP) and the number of full pods (FP). Significant relationships were found between total dry weight (TDW), leaf dry weight (LDW), pod dry weight (PDW), TP, and FP, and the waterlogging stress tolerance index (WTI). Additionally, the waterlogging tolerance of peanut ecotypes is closely related to their geographic origin, where the most waterlogging-resistant ecotype was Zhanhong 2, followed by Zhongkaihua 1 and Huayu 39. Finally, breeding backgrounds and screening indices (SPAD, Pn, dry matter accumulation, and pod characteristics) beneficial to waterlogging tolerance breeding are suggested.

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Abstract:In the search for prodrug analogs of clopidogrel with improved metabolic characteristics and antiplatelet bioactivity, a group of clopidogrel and vicagrel analogs selectively deuterated at the benzylic methyl ester group were synthesized, characterized, and evaluated. The compounds included clopidogrel-d 3 (8), 2-oxoclopidogrel-d 3 (9), vicagrel-d 3 (10a), and 12 vicagrel-d 3 analogs (10b-10m) with different alkyl groups in the thiophene ester moiety. The D 3 C-O bond length in 10a was shown by X-ray single crystal diffraction to be shorter than the H 3 C-O bond length in clopidogrel, consistent with the slower rate of hydrolysis of 8 than of clopidogrel in rat whole blood in vitro. A study of the ability of the compounds to inhibit ADP-induced platelet aggregation in fresh rat whole blood collected 2 h after oral dosing of rats with the compounds (7.8 µmol/kg) showed that deuteration increased the activity of clopidogrel and that increasing the size of the alkyl group in the thiophene ester moiety reduced activity. A preliminary pharmacokinetic study comparing 10a with vicagrel administered simultaneously as single oral doses (72 µmol/kg of each drug) to male Wistar rats showed 10a generated more of its active metabolite than vicagrel. These results suggest that 10a is a potentially superior antiplatelet agent with improved metabolic characteristics and bioactivity, and less dose-related toxicity.

Alzheimer’s disease (AD) is a chronic progressive neurodegenerative disorder that is associated with learning, memory, and cognitive deficits. Neuroinflammation and synapse loss are involved in the pathology of AD. Diverse measures have been applied to treat AD, but currently, there is no effective treatment. Celastrol (CEL) is a pentacyclic triterpene isolated from Tripterygium wilfordii Hook F that has been shown to enhance cell viability and inhibit amyloid-β production induced by lipopolysaccharides in vitro. In the present study, the protective effect of CEL on Aβ25-35-induced rat model of AD was assessed. Our results showed that CEL administration at a dose of 2 mg/kg/day improved spatial memory in the Morris water maze. Further biochemical analysis showed that CEL treatment of intrahippocampal Aβ25-35-microinjected rats attenuated hippocampal NF-κB activity; inhibited proinflammatory markers, namely, IL-1β, IL-6, and TNF-α; and upregulated anti-inflammatory factors, such as IL-4 and IL-10. Furthermore, CEL upregulated hippocampal neurexin-1β, neuroligin-1, CA1, and PSD95 expression levels, which may improve synaptic function. Simultaneously, CEL also increased glucose metabolism in Aβ25-35-microinjected rats. In conclusion, CEL could exert protective effects against learning and memory decline induced by intrahippocampal Aβ25-35 through anti-inflammation, promote synaptic development, and maintain hippocampal energy metabolism.