Search

Revealing genomic variation of representative and diverse germplasm is the cornerstone of deploying genomics information into genetic improvement programs of species of agricultural importance. Here we report the re-sequencing of 239 japonica rice elites representing the genetic diversity of japonica germplasm in China, Japan and Korea. A total of 4.8 million SNPs and PAV of 35,634 genes were identified. The elites from Japan and Korea are closely related and relatively less diverse than those from China. A japonica rice pan-genome was constructed, and 35 Mb non-redundant novel sequences were identified, from which 1131 novel genes were predicted. Strong selection signals of genomic regions were detected on most of the chromosomes. The heading date genes Hd1 and Hd3a have been artificially selected during the breeding process. The results from this study lay the foundation for future whole genome sequences-enabled breeding in rice and provide a paradigm for other species.

Microplastics (MPs) are widely present in global oceans, and can pose a threat to marine organisms. This study examined the abundance and characteristics of MPs in seawater, sediment, and organism samples collected from Hangzhou Bay. Abundance of MPs in seawater (n = 26) and sediment (n = 26) were 0.77-9.6 items/m

Finding novel anti-diabetic compounds with effective suppression activities against hepatic glucagon response is urgently required for the development of new drugs against diabetes. Fungi are well known for their ability to produce new bioactive secondary metabolites. As part of our ongoing research, five new indole-terpenoids (

Four new indole-terpenoids (1–4) named encindolene A, 18-O-methyl-encindolene A, encindolene B, and encindolene C, as well as three known analogs (5–7), were isolated from the fungus Penicillium sp. HFF16 from the rhizosphere soil of Cynanchum bungei Decne. The structures of compounds including absolute configurations were elucidated by spectroscopic data and electronic circular dichroism (ECD) analysis. Anti-inflammatory activity evaluation revealed that compounds 1–7 inhibit the production of nitric oxide with IC50 values of 79.4, 49.7, 81.3, 40.2, 86.7, 90.1, and 54.4 μM, respectively, and decrease the levels of tumor necrosis factor-α, interleukin-6 contents in lipopolysaccharide-induced RAW264.7 macrophages.

The improvement of cold adaptation has contributed to the increased growing area of rice. Standing variation and de novo mutation are distinct natural sources of beneficial alleles in plant adaptation. However, the genetic mechanisms and evolutionary patterns underlying these sources in a single population during crop domestication remain elusive. Here we cloned the CTB2 gene, encoding a UDP-glucose sterol glucosyltransferase, for cold tolerance in rice at the booting stage. A single standing variation (I408V) in the conserved UDPGT domain of CTB2 originated from Chinese Oryza rufipogon and contributed to the cold adaptation of Oryza sativa ssp. japonica. CTB2 is located in a 56.8 kb region, including the previously reported gene CTB4a in which de novo mutation arose c. 3200 yr BP in Yunnan province, China, conferring cold tolerance. Standing variation of CTB2 and de novo mutation of CTB4a underwent stepwise selection to facilitate cold adaptation to expand rice cultivation from high-altitude to high-latitude regions. These results provide an example of stepwise selection on two kinds of variation and describe a new molecular mechanism of cold adaptation in japonica rice.

Rice in cold region is threatened by cold stress frequently, resulting in severe losses of rice production. In the present study, two rice varieties with contrast cold tolerance in the reproductive stage (Longjing25, cold tolerant; Longjing11 cold sensitive) were compared using RNA-seq technique. A total of 14,861 and 12,148 differentially expressed genes (DEGs) were obtained by comparison of LJ25 and LJ11 after 2 days and 4 days of cold stress challenge. Subsequent Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis revealed that five significant pathways were specifically enriched in LJ11. Starch and sucrose metabolism was the only one significant pathway (containing 47 DEGs) annotated in both of varieties during two cold treatment periods. By weighted gene co-expression network analysis (WGCNA), 14 co-expression gene modules were calculated, among which turquoise, cyan, and dark green were the most concerned modules, containing 4807, 2682, and 1174 DEGs, respectively. Finally, we analyzed the transcriptional factors (TFs), and TF families of MYB, zinc finger, AP2/ERF-AP2, bHLH, NAC, bZIP, and WRKY were the biggest seven subfamilies. Collectively, our findings provided valuable insights into the molecular and genetic mechanisms responsible for rice’s response to cold stress.

Two new thio-compounds named aspergerthinol A and B (1 and 2) and two new monoterpenes named aspergerthinacids A and B (3 and 4) were isolated from the fungus Aspergillus sp. CYH26 from the rhizosphere soil of Cynanchum bungei Decne. The structures of compounds were elucidated by spectroscopic data and quantum NMR and ECD calculations. Compounds 1 and 2 represented a new family of sulfur containing natural products with a 3-methyl-4H-cyclopenta[b]thiophen-4-one skeleton. Compounds 1–4 showed inhibitory activities against nitric oxide (NO) with IC50 values of 38.0, 19.8, 46.3, and 56.6 μM, respectively.

Objective: This study was designed to demonstrate the predictive value of Pulse indicate Contour Cardiac Output (PiCCO) monitoring technique combined with troponin I (cTnI) detection in septic myocardial dysfunction (SMD) of the elderly. Methods: One hundred and nineteen elderly patients with SMD treated in our hospital from March 2016 to September 2019 were enrolled and allocated into the joint group (JG; 64 cases) for capacity management of fluid resuscitation under the guidance of PiCCO monitoring technique and cTnI detection, and the control group (CG; 55 cases) for conventional capacity management. Clinical indicators, hemodynamics, improvement of myocardial injury markers and inflammatory factors 6 h and 36 h post intervention, fluid balance 6 h, 12 h and 36 h post intervention, drug consumption (norepinephrine), treatment effect and 28-day hospitalization mortality were compared between the two groups. Results: After resuscitation, the urine volume per hour and the fluid resuscitation volume were higher while the blood lactic acid (BLA) expression was lower in JG as compared to CG. JG presented a remarkably lower central venous pressure (CVP) than CG after resuscitation, with notably higher mean arterial pressure (MAP) and central venous oxygen saturation (ScvO2). In comparison with CG, JG displayed dramatically lower cTnI and N-terminal pro-brain natriuretic peptide (NT-ProBNP) 6 h and 36 h post intervention, as well as evidently reduced interleukin-6 (IL-6), procalcitonin (PCT) and high-sensitivity C-reactive protein (hs-CRP). After 36 h of intervention, the fluid balance was evidently lower in JG than in CG. JG showed statistically less use of norepinephrine, less time of mechanical ventilation and ICU stay, and noticeably lower incidence of multiple organ dysfunction syndrome (MODS), as well as dramatically lower 28-day hospitalization mortality than CG post intervention. Conclusions: PiCCO monitoring technique combined with cTnI detection is high-performing in fluid resuscitation of elderly patients with SMD, which can meliorate the myocardial function of patients, reduce medication and facilitate disease recovery.

The objective of this study was to explore the diagnosis of severe sepsis complicated with acute kidney injury (AKI) by ultrasonic image information based on the artificial intelligence pulse coupled neural network (PCNN) algorithm. In this study, an algorithm of ultrasonic image information enhancement based on the artificial intelligence PCNN was constructed and compared with the histogram equalization algorithm and linear transformation algorithm. After that, it was applied to the ultrasonic image diagnosis of 20 cases of severe sepsis combined with AKI in hospital. The condition of each patient was diagnosed by ultrasound image performance, change of renal resistance index (RRI), ultrasound score, and receiver operator characteristic curve (ROC) analysis. It was found that the histogram distribution of this algorithm was relatively uniform, and the information of each gray level was obviously retained and enhanced, which had the best effect in this algorithm; there was a marked individual difference in the values of RRI. Overall, the values of RRI showed a slight upward trend after admission to the intensive care unit (ICU). The RRI was taken as the dependent variable, time as the fixed-effect model, and patients as the random effect; the parameter value of time was between 0.012 and 0.015, p = 0.000 < 0.05 . Besides, there was no huge difference in the ultrasonic score among different time measurements (t = 1.348 and p = 0.128 > 0.05 ). The area under the ROC curve of the RRI for the diagnosis of AKI at the 2nd day, 4th day, and 6th day was 0.758, 0.841, and 0.856, respectively, which was all greater than 0.5 ( p < 0.05 ). In conclusion, the proposed algorithm in this study could significantly enhance the amount of information in ultrasound images. In addition, the change of RRI values measured by ultrasound images based on the artificial intelligence PCNN was associated with AKI.

International audience; A concise and practical method for the metal-free synthesis of 1,8-naphthyridones is described using a two-step approach involving regioselective amination of pyridine N-oxides and acid-mediated cyclization. This is the first synthesis of 1,8-naphthyridones utilizing easily accessible pyridine N-oxides as substrates. Compared to previous reports, this method benefits from simple operation, easy access to starting materials, and a wide substrate scope, providing a variety of novel 1,8-naphthyridones.

As one of the abiotic stresses, low temperature severely threatens rice production during its entire growth period, especially during the booting stage. In the present study, transcriptome analysis was performed comparing Longjing (LJ) 25 (chilling-tolerant) and LJ 11 (chilling-sensitive) rice varieties to identify genes associated with chilling tolerance in rice spikelets. A total of 23 845 expressed genes and 13 205 differentially expressed genes (DEGs) were identified, respectively. Gene ontology (GO) enrichment analyses revealed ‘response to cold’ (containing 180 DEGs) as the only category enriched in both varieties during the entire cold treatment period. Through M ap M an analysis, we identified nine and six DEGs related to the Calvin cycle and antioxidant enzymes, respectively, including OsRBCS3 , OsRBCS2 , OsRBCS4 , OsAPX2 and OsCATC , that under chilling stress were markedly downregulated in LJ11 compared with LJ25. Furthermore, we predicted their protein–protein interaction (PPI) network and identified nine hub genes (the threshold of co-expressed gene number ≥ 11) in Cytoscape, including three RuBisCO-related genes with 14 co-expressed genes. Under chilling stress, antioxidant enzyme activities (peroxidase (POD) and catalase (CAT)) were downregulated in LJ11 compared with LJ25. However, the content of malondialdehyde (MDA) was higher in LJ11 compared with LJ25. Collectively, our findings identify low temperature responsive genes that can be effectively used as candidate genes for molecular breeding programmes to increase the chilling tolerance of rice.

Anastatins A and B, two flavonoid compounds isolated from desert plant

Rice is sensitive to low temperatures, specifically at the booting stage. Chilling tolerance of rice is a quantitative trait loci that is governed by multiple genes, and thus, its precise identification through the conventional methods is an arduous task. In this study, we investigated the candidate genes related to chilling tolerance at the booting stage of rice. The F2 population was derived from Longjing25 (chilling-tolerant) and Longjing11 (chilling-sensitive) cross. Two bulked segregant analysis pools were constructed. A 0.82 Mb region containing 98 annotated genes on chromosomes 6 and 9 was recognized as the candidate region associated with chilling tolerance of rice at the booting stage. Transcriptomic analysis of Longjing25 and Longjing11 revealed 50 differentially expressed genes (DEGs) on the candidate intervals. KEGG pathway enrichment analysis of DEGs was performed. Nine pathways were found to be enriched, which contained 10 DEGs. A total of four genes had different expression patterns or levels between Longjing25 and Longjing11. Four out of the 10 DEGs were considered as potential candidate genes for chilling tolerance. This study will assist in the cloning of the candidate genes responsible for chilling tolerance and molecular breeding of rice for the development of chilling-tolerant rice varieties.

Excessive accumulation of free radicals in the body can cause liver damage, aging, cancer, stroke, and myocardial infarction. Anastatin B, a skeletal flavonoid, was reported to have antioxidant and hepatoprotective effects. Anastatin B derivatives, compound 1 and 2, were synthesized by our group previously. In this study, their antioxidant activity and hepatoprotective mechanism were studied using chemical evaluation methods, a cellular model of hydrogen peroxide (H2O2)-induced oxidative damage, and a mouse model of carbon tetrachloride (CCl4)-induced liver injury. Results from the chemical evaluation suggested that both compounds had good antioxidant power and radical scavenging ability in vitro. MTT assay showed that both compounds had cytoprotective activity in H2O2-treated PC12 cells. Moreover, their hepatoprotective activities evaluated using a mouse model of CCl4-induced liver injury that compared with the model group, pretreatment with compound 1 and 2 significantly decreased alanine transaminase (ALT), aspartate transaminase (AST), lactate dehydrogenase (LDH), and malondialdehyde (MDA) levels; reduced the liver tissue damage; and increased glutathione content. However, compound 2 was a more effective hepatoprotectant than compound 1 was. Finally, the amount of TNF-α and cytochrome P450 2E1 (CYP2E1) were significantly downregulated in compound 1 and 2 pretreatment groups. Collectively, our findings demonstrate that both compounds have potential antioxidant activity and hepatoprotective effect in vitro and in vivo. Further chemo-biological study and investigation of the compounds' enzymatic targets are ongoing.

The first total synthesis of I3,II8-biapigenin and ridiculuflavone A via the key steps of regioselective iodination, Sonogashira reaction, and rhodium-catalyzed oxidative coupling with the overall yields of 31% and 22%, respectively, was reported. The structures of the key intermediates for the two natural products were confirmed by single-crystal X-ray analysis.

The naturally occurring flavone 8-(6″-umbelliferyl)apigenin, a hybrid structure of apigenin and coumarin, as well as seven of its analogues were synthesized for the first time by using iodination and Suzuki coupling reactions as key steps. The synthesis of 8-(6″-umbelliferyl)-apigenin was achieved in seven linear steps from the commercially available 1-(2,4,6-trihydroxyphenyl)ethan-1-one and 7-hydroxyl coumarine with 31% overall yield. Effects of these compounds on glucose disposal were investigated in adipocytes. All of the flavonoid and coumarin hydrids were found to have better bioactivities than their corresponding flavonoid cores. The most potent compound 15 (10 μΜ) could promote glucose consumption by 57% which exhibited similar effect as the positive control metformin at 1 mM. Moreover, fluorescence microscopy showed that four 8-(6″-umbelliferyl)apigenin analogues 2, 15, 30 and 31 could promote the 2-NBDG uptake into 3T3-L1 cells, which consist with those observed in the regulation of glucose.

Non-metallic organic tanning agents were used during the leather processing, most of them will be combined with the collagen converted it into leather. But there still some of its components were discarded into the wastewater and caused serious environmental problems. In this study, the structure character of microbial communities in leather wastewater containing non-metallic organic tanning agents and the effect of the leather wastewater on the ecology of the microorganisms were studied with the high-throughput sequencing. The results show that the presence of 1,657, 49 bacterial and fungal OTUs (Operational Taxonomic Unit), at 97% similarity level. Significant differences on microbial community composition in wastewater were observed in systems containing different non-metallic organic tanning agents. The Firmicutes and proteobacteria were dominated bacteria in T1, T3, T8, KB and T6. Ascomycota and Basidiomycota were the most richness fungi in T1, T3, T6, T8 and KB. The relative abundance of dominant bacteria pseudodomonas was significantly positively correlated with TN, NH3, and TOC (0.01

Aim: The research of novel and potent antidiabetic agents is urgently needed for the control of the exploding diabetic population. We previously reported the synthesis and antidiabetic activity of natural 8-(6”-umbelliferyl)-apigenin (1), but its antidiabetic targets are not known. Therefore, four series of derivatives were synthesized and evaluated for their antidiabetic activities. Results & methodology: Compounds (5a) and (14a) were identified as new α-glucosidase and α-amylase dual inhibitors. The kinetic analysis of the most potent α-glucosidase inhibitor of each series of compounds revealed that they inhibited α-glucosidase in irreversible modes. In addition, compounds (5a) and (14a) showed potent glucose consumption-promoting activity. Conclusion: Compounds (5a) and (14a) could be regarded as promising starting points for the development of antidiabetic candidates.

Excessive accumulation of free radicals in the body can cause liver damage, aging, cancer, stroke, and myocardial infarction. Anastatin B, a skeletal flavonoid, was reported to have antioxidant and hepatoprotective effects. Anastatin B derivatives, compound 1 and 2, were synthesized by our group previously. In this study, their antioxidant activity and hepatoprotective mechanism were studied using chemical evaluation methods, a cellular model of hydrogen peroxide (H

Two novel flavones (±)-Anastatins A and B, each containing a benzofuran moiety, were synthesized for the first time by using bromination, Suzuki coupling reaction, and an oxidation/Oxa-Michael reaction cascade as the key steps. The syntheses of (±)-Anastatins A and B were achieved in eight steps from the commercially available phloroglucinol with 9% and 10% overall yield, respectively.

C-6 and C-8 monobromo flavonoids are important building blocks for the synthesis of flavonoid natural products and their derivatives. Bromination of suitably alkylated flavonoids with N-bromosuccinimide in dichloromethane (DCM), followed by deprotection with BCl3 , gives either a C-6 or a C-8 monobromo flavonoid in high yield and with high regioselectivity, depending on the protection pattern of the C-5 and C-7 OH groups. The mild and neutral conditions are particularly useful for the regioselective bromination of acid-labile substrates.

Two novel flavonoids (±)-Anastatins A and B as well as 14 analogs, which containing a benzofuran moiety, were synthesized by using halogenation, Suzuki coupling reaction and an oxidation/Oxa-Michael reaction cascade as the key steps. The structures of the new flavonoids were confirmed by 1 H NMR, 13 C NMR and HRMS. The antioxidant activities of them as well as the key intermediates were evaluated by ferric reducing antioxidant power (FRAP) assay and the active compounds were evaluated in the PC12 cell model of hydrogen peroxide (H 2 O 2 )-induced oxidative damage. SAR studies suggested that, for in vitro antioxidant activity, aurone derivatives showed better bioactivity than flavone counterparts. However, cyclization to benzofuran and connecting the two conjugated parts as a whole conjugated system by a double bond diminished the in vitro antioxidant activity. Among them, the most potent compound 24c was significantly decreased H 2 O 2 -caused cell injury. The apoptotic rate (Annexin V + ) of H 2 O 2 -damaged PC12 cells was 60.7% while that of the compound 24c -treated cells decreased to 5.9% and 4.1% at 10 μM and 100 μM respectively.

Quercetin, luteolin, and epigallocatechin gallate are flavonoids abundant in edible and medicinal plants with beneficial effects on glucose homeostasis. This study explored the action of these flavonoids on glucose disposal in adipocytes. Quercetin, luteolin, and epigallocatechin gallate enhanced glucose consumption with the positive regulation of AMP-activated kinase phosphorylation, and the AMP-activated kinase inhibitor compound C abolished their effects on glucose consumption. Luteolin and epigallocatechin gallate, but not quercetin, increased sirtuin 1 abundance, and their regulation of glucose consumption was also attenuated by co-treatment with sirtuin 1 inhibitor nicotinamide. Quercetin, luteolin, and epigallocatechin gallate suppressed nuclear factor-κB activation by inhibition of p65 phosphorylation with beneficial regulation of adipokine expression, whereas these actions were diminished by coincubation with compound C. The sirtuin 1 inhibitor nicotinamide attenuated the effects of luteolin and EGCG on p65 phosphorylation and adipokine expression without any influence on the activity of quercetin. Results of Western blot and fluorescence microscopy also showed that quercetin, luteolin, and epigallocatechin gallate increased Akt substrate of 160 kDa phosphorylation and promoted 2-deoxy-D-glucose uptake by adipocytes under basal and inflammatory conditions. These findings suggested that quercetin, luteolin, and epigallocatechin gallate inhibited inflammation and promoted glucose disposal in adipocytes with the regulation of AMP-activated kinase and/or sirtuin 1.

This paper describes the selective syntheses of two cis-isomer-enriched cyclopentanone fragrances: ( Z )-3-(2-oxopropyl)-2-(pent-2-en-1-yl)cyclopentanone (four steps, 62% overall yield, 67% cis) and Magnolione ® (five steps, 60% overall yield, 55% cis). In addition, the asymmetric synthesis of (3a R ,7a S )-5-methyl-2,3,3a,4,7,7a-hexahydro-1 H -inden-1-one as well as (3a′ R ,7a′ S )-5′-methyl-2′,3′,3a′,4′,7′,7a′-hexahydrospiro[[1,3]dioxolane-2,1′-indene] has been realized by an efficient kinetic resolution, which enables the selective synthesis of the 2 S ,3 R -isomer-enriched 3 and 4 .

Two novel flavones anastatins A (I) and B (II) are prepared from commercially available phloroglucinol in eight steps with 9% and 10% overall yield, respectively.

The resonant characteristic of hydraulic system has not been described yet because it is necessarily restricted by linear assumptions in classical fluid theory. A way of the resonance analysis is presented for an electrohydraulic exciter controlled by 2D valve. The block diagram of this excitation system is established by extracting nonlinear parts from the traditional linearization analysis; as a result the resonant frequency is obtained. According to input energy from oil source which is equal to the reverse energy to oil source, load pressure and load flow are solved analytically as the working frequency reaches the natural frequency. The analytical expression of resonant peak is also derived without damping. Finally, the experimental system is built to verify the theoretical analysis. The initial research on resonant characteristic will lay theoretical foundation and make useful complement for resonance phenomena of classical fluid theory in hydraulic system.

The asymmetric synthesis of an intermediate which enables the asymmetric syntheses of (I) and (II) is also presented.

This paper describes the selective syntheses of two cis-isomer enriched cyclopentanone fragrances: (Z)-3-(2-oxopropyl)-2-(pent-2-en-1-yl)cyclopentanone (4 steps, 62% overall yield, 67% cis) and Magnolione® (5 steps, 60% overall yield, 55% cis). In addition, the asymmetric synthesis of (3aR,7aS)-5-methyl-2,3,3a,4,7,7a-hexahydro-1H-inden-1-one as well as (3a'R,7a'S)-5'-methyl-2',3',3a',4',7',7a'-hexahydrospiro[[1,3]dioxolane-2,1'-indene]) has been realized by an efficient kinetic resolution, which enables the selective synthesis of the 2S,3R-isomer-enriched 3 and 4.

Indolinone displays promising antitumor properties by inhibiting various kinase families. In this paper, we’d like to report the design, synthesis, and primary biological evaluation of the novel indoline-3-one and its derivatives. All the newly synthesized compounds including the novel compound 2-(4-(trifluoromethyl)benzylidene)indolin-3-one (5f) were characterized by 1H NMR and their antitumor activities were evaluated by using MTT method in HT-29, K562, and HepG2 cell lines. 2-(2-nitrobenzylidene)indolin-3-one (5d) demonstrated good antitumor activity against HT-29, K562, and HepG2 with an IC50 of 2.04 μM, 2.33 μM, 2.24 μM, respectively. 2-(4-(trifluoromethyl)benzylidene)indolin-3-one(5f) demonstrated good antitumor activity against K562 and HepG2 with an IC50 of 2.27 μM, 3.47 μM.

The total syntheses of the lycopodium alkaloids fawcettimine, fawcettidine, lycoflexine, and lycoposerramine B have been accomplished through an efficient, unified, and stereocontrolled strategy that relies on a Diels–Alder reaction to construct the cis-fused 6,5-carbocycles with one all-carbon quaternary center. Access to the enantioselective syntheses of both antipodes of those alkaloids can be achieved by kinetic resolution of the earliest intermediate via a Sharpless asymmetric dihydroxylation (Sharpless AD). Compared to existing approaches to these alkaloids, our synthetic route possesses superior stereocontrol over the C-4 and C-15 stereogenic centers as well as allowing for more functional variation on the 6-membered ring.