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Idesia polycarpa var. vestita Diels is a perennial deciduous tree widely distributed throughout China. Four I. polycarpa fruit of different cultivars with different fruit issues during the growth process were compared, which were on the basis of morphological characteristics and chemical compositions. The influencing factors of oil accumulation in I. polycarpa fruit and the correlation between different components were investigated, and the results revealed a negative correlation between oil content and total sugar (r = -0.930), ash (r = -0.606), and crude fiber (r = -0.952). Except for oil, none of the chemical components changed substantially during the growing phase, and most cultivars showed higher oil content in the pulp portion (14.14-43.99 g/100 g). Linoleic acid was the most abundant fatty acid in I. polycarpa oil (IPO), with values ranging from 52.18% to 66.65% (fruit), 55.44% to 65.15% (pulp), and 68.99% to 78.76% (seed). Principal component analysis revealed that Hubei varieties are more advantageous. Besides, the lipid composition of IPO was identified by ultrahigh-performance liquid chromatography coupled with electrospray ionization Q-Exactive Focus mass spectrometry. The glyceride components of IPO were mostly composed of 22 triacylglycerols, 30 diacylglycerols, and 8 monoacyglycerols. Meanwhile, linoleic acid was mainly distributed in sn-2 and sn-3 positions. PRACTICAL APPLICATION: Morphologic characteristics, chemical compositions, oil fatty acid profiles, and oil correlation factors of I. polycarpa were analyzed. The comprehensive score of oil quality by PCA in Hb fruit was the highest. The glyceride components of I. polycarpa oil were mainly composed of 22 triacylglycerols, 30 diacylglycerols, and eight monoacyglycerols.

A new approach to the synthesis of Emitasvir (DAG181), a small molecule hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor, is described. Enantioselective enzymatic desymmetrization ...

Idesia polycarpa var. vestita Diels fruits oil (IPO) has the potential to broaden the availability of healthy vegetable oil and relieve pressure on the edible oil supply. In this study, we compared the physicochemical, bioactivity, and digestive properties of IPO, olive oil (OO), and soybean oil (SO) to comprehensively evaluate the edible potential of IPO. The results revealed no significant differences in relative density or refractive index among the three oils. IPO was rich in β-sitosterol (366.74 mg/100 g), β-tocopherol (8.42 mg/100 g), and α-tocopherol (37.10 mg/100 g). The digestive properties of IPO emulsion were investigated for the first time using in vitro simulated digestion. The IPO emulsion stood out regarding its free fatty acid release (88.03 %). Finally, the IPO emulsion released mainly unsaturated fatty acids and had a higher monoacylglycerol content. This study provides new insights into IPO as a high-quality edible vegetable oil.

The perceptible bitterness of Zanthoxylum schinifolium Sieb. et Zucc is an important factor limiting its consumption. Metabolomics was used to identify potentially bitter metabolites during the development of Z. schinifolium, and dynamic changes in 17 key bitter components were characterized. The key bitter components in Z. schinifolium at different developmental stages were mainly synthesized through the "phenylpropanoid biosynthesis", "flavonoid biosynthesis", and "flavone and flavonol biosynthesis" pathways. In combination with transcriptomic data, the expression of related genes regulates the accumulation process of these bitter components; based on this, a biosynthetic pathway of bitter components in Z. schinifolium was constructed. In addition, quercetin-3-galactoside, isoquercitin, quercitrin, kaempferol, and isorhamnetin were identified as the main sources of bitterness in mature Z. schinifolium based on an evaluation of taste activity value. These findings provide valuable information for understanding mechanisms underlying Z. schinifolium bitterness and promoting the further development of high-quality Z. schinifolium.

Bacterial leaf blight (BLB) caused by Xanthomonas oryzae pv oryzae (Xoo) is considered as the most destructive disease of rice. The use of bactericides is among the most widely used traditional met...

Xanthomonas oryzae pv. oryzae (Xoo) infection directly leads to a severe disease known as leaf blight, which is a major cause of yield loss of rice. Use of traditional bactericides has resulted in severe resistance in pathogenic bacteria. A new approach screening compounds that target the virulence factors rather than killing bacterial pathogens is imperative. In gram-negative bacteria, the type III secretion system (T3SS) is a conserved and significant virulence factor considered as a target for drug development. Therefore, we designed and synthesized a new series of 5-phenyl-2-furan carboxylic acid derivatives stitched with 2-mercapto-1,3,4-thiadiazole. Bioassays revealed that the title candidates attenuated the hypersensitive response through suppressing the promoter activity of a harpin gene hpa1 without affecting bacterial growth. Quantitative real time polymerase chain reaction (qRT-PCR) analysis demonstrated reduced the expression of several genes associated with T3SS, when title compounds were applied. Additionally, hrp gene cluster members, including hrpG and hrpX, had reduced mRNA levels. In vivo greenhouse tests showed that candidate compounds could alleviate the effects of Xoo infection in rice (Oryza sativa) and possess better protective activity against rice bacterial leaf blight than bismerthiazol and thiodiazole copper. All tested compounds were safe to rice. This work suggests there are new safe options for Xoo control in rice from these 1,3,4-thiadiazole derivatives.

In this present study, a series of 5-phenyl-2-furan and 4-phenyl-2-oxazole derivatives were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. In vitro results showed that the synthesized compounds exhibited considerable inhibitory activity against PDE4B and blockade of LPS-induced TNF-α release. Among the designed compounds, Compound 5j exhibited lower IC50 value (1.4 μM) against PDE4 than parent rolipram (2.0 μM) in in vitro enzyme assay, which also displayed good in vivo activity in animal models of asthma/COPD and sepsis induced by LPS. Docking results suggested that introduction of methoxy group at para-position of phenyl ring, demonstrated good interaction with metal binding pocket domain of PDE4B, which was helpful to enhance inhibitory activity.

Targeting virulence factors of bacterial without affecting their growth and survival, has been an initiative strategy for the development of novel anti-microbial agents. The type III secretion system (T3SS), one of essential and highly conserved virulence factors in most Gram-negative pathogenic bacteria, has been regarded as an effective target that developed new anti-microbial drugs. Xanthomonas oryzae pv. oryzae (Xoo) is one of the most Important bacterial pathogens on rice, which causes leaf blight disease. To discover potential anti-virulence agents against the pathogens, a new series of thiazolidin-2-cyanamide derivatives containing 5-phenyl-2-furan were designed and synthesized. Their structures were characterized by 1H NMR, 13C NMR, MS, and elemental analysis. All the title compounds inhibited the promoter activity of a harpin gene hpa1, significantly, that were further checked for the impact on bacterial growth and on the hypersensitive response (HR) caused by Xoo on non-host tobacco plants. The results indicated that treatment of Xoo with the title compounds II-2, II-3 and II-4 resulted in significantly attenuated HR without affecting bacterial growth or survival. Moreover, quantitative reverse transcription-polymerase chain reaction (qRT-PCR) analysis showed that the expression of the Xoo T3SS was suppressed by treatment with the three inhibitors. The mRNA levels of representative genes in the hrp (hypersensitive response and pathogenicity) cluster, as well as the regulatory genes hrpG and hrpX, were reduced. Finally, the in vivo test demonstrated that the compounds could reduce the disease symptoms of Xoo on the rice cultivar (Oryza sativa) IR24.

This study investigated the influence of inulins with different molecular weights (Mw) and added concentrations on the structure and thermal stability of gliadin and glutenin gels. All inulins reduced hydrophobicity index (H0) and hindered disulfide bond (S–S) formation of both glutenin and gliadin. The H0 of glutenin reduced by 72.6%, 64.8% and 77.1% after the addition of 400 g/kg low, middle and high molecular weight inulins (L-, M-, and H-inulin, respectively), whereas the H0 of gliadin decreased by 11.7%, 31.9% and 48.6%. Furthermore, inulin increased random coils and decreased α-helix and β-sheet prevalence for gliadin, while it increased α-helix and β-turn prevalence and decreased β-sheets and random coils for glutenin. Inulin also triggered S–S configuration of these two proteins to vary from g-g-g to t-g-g or t-g-t. H-inulin deepened gel electrophoresis bands of the 30–35 kDa gliadin molecules, and all inulins reduced band strength for the 30–35 kDa glutenin subunits. Inulin limited interactions between glutenin/gliadin and water, resulting in more fragile and open network structure. Moreover, the thermal stability of heat-induced inulin-gliadin gel was higher than that of inulin-glutenin gel. The impact of inulin on glutenin was stronger than on gliadin, and the effect was Mw-dependent (H-inulin > M-inulin > L-inulin).

A techno-economic analysis (TEA) was performed on glucosamine and lipid production from a marine diatom Cyclotella sp. in raceway open pond (RWP) and tubular photobioreactor (PBR) cultivation systems. Two PBR operating schemes were assessed: one to produce high lipid (HL) content, and another to produce high chitin (HC) content. In order to generate 1 kg of glucosamine, 9700 kg (RWP)/1050 kg (PBR HL) freshwater, 40 kg CO2, 0.70 kg nitrogen, 0.18 kg phosphorus, and 1.2 kg silicon nutrients are required for algae cultivation with water and nutrient recovery. With a price of $1.5 for lipid as coproduct, the projected selling price of glucosamine were $35/kg, $106/kg and $82/kg for RWP, PBR HL, and PBR HC systems, respectively. Currently, these prices are not competitive with industrial shellfish-derived glucosamine, but can be reduced by technology improvements such as producing food grade lipid, increasing algal productivity or chitin content.

Biofilm is a bacterial lifestyle ubiquitously in natural environments. Bacterial biofilm leads to drug resistance, a main reason why many infectious diseases are difficult to control. Due to the prominent points of biofilms implicated in infectious disease and the spread of multi-drug resistance, it is urgent to discover new antibacterial agents that can regulate biofilm formation and development. This review introduces chemical agents that could modulate bacterial biofilm formation and development.细菌的生物被膜是其在自然界中一种常见的生存状态。生物被膜的形成是细菌耐药性产生的主要机制之一，也是许多感染性疾病难以控制的重要原因。由于生物被膜在传染性疾病中的突出地位和细菌多重耐药性的蔓延，目前急需研制开发出能够调节生物被膜形成的新型抗菌药物。文中对调节生物被膜形成和发育的小分子抑制剂进行了详细的综述。.

The cyclic dinucleotide c-di-GMP is known as an important second messenger in bacteria, which controls various important cellular processes, such as cell differentiation, biofilm formation and virulence factors production. It is extremely vital for the development of new antibacterial agents by virtue of blocking c-di-GMP signal conduction. Current research indicates that there are three potential targets for discovering new antibacterial agents based on c-di-GMP regulated signal pathway, which are c-di-GMP synthases, c-di-GMP degrading enzymes and c-di-GMP receptors. Herein, we review small molecules that have been developed to inhibit c-di-GMP related enzymes and indicate perspectives of c-di-GMP inhibitors.环二鸟苷酸 (Bis-(3′-5′) cyclic diguanylic acid, c-di-GMP) 是细菌所特有的一类核酸类第二信使，参与并调节细菌多种生理功能，包括细胞分化、生物被膜的形成以及致病因子的产生等。阻断c-di-GMP 信号的传导对于发展新型抗菌药物具有重要的意义。现有研究结果表明，基于c-di-GMP 调控的信号通路开发新型抗菌药物具有3 类潜在的靶点，分别是c-di-GMP 合成酶 (DGCs)、c-di-GMP 降解酶 (PDEs) 以及c-di-GMP 受体。文中根据上述3 类关键靶点，介绍了相关小分子抑制剂的研究进展，并展望了c-di-GMP 信号分子抑制剂的发展方向。.

The initiative strategy for the development of novel anti-microbial agents usually uses the virulence factors of bacteria as a target, without affecting their growth and survival. The type III secretion system (T3SS), one of the essential virulence factors in most Gram-negative pathogenic bacteria because of its highly conserved construct, has been regarded as an effective target that developed new anti-microbial drugs. Xanthomonas oryzae pv. oryzae (Xoo) causes leaf blight diseases and is one of the most important pathogens on rice. To find potential anti-virulence agents against this pathogen, a number of natural compounds were screened for their effects on the T3SS of Xoo. Three of 34 compounds significantly inhibited the promoter activity of the harpin gene, hpa1, and were further checked for their impact on bacterial growth and on the hypersensitive response (HR) caused by Xoo on non-host tobacco plants. The results indicated that treatment of Xoo with CZ-1, CZ-4 and CZ-9 resulted in an obviously attenuated HR without affecting bacterial growth and survival. Moreover, quantitative reverse transcription-polymerase chain reaction (qRT-PCR) analysis showed that the expression of the Xoo T3SS was suppressed by treatment with the three inhibitors. The mRNA levels of representative genes in the hypersensitive response and pathogenicity (hrp) cluster, as well as the regulatory genes hrpG and hrpX, were reduced. Finally, the in vivo test demonstrated that the compounds could reduce the disease symptoms of Xoo on the rice cultivar (Oryza sativa) IR24.