ACS Infectious Diseases
·
2025
·
IF 3.8
Feifei Zhao,Yizhen Zhu,Lingxiang Mao,Honghao Huang,Wei Wei,Qiangcheng Deng,Youzhi Tang,Ning Han,Zhenling Zeng
Staphylococcus aureus poses a global threat to livestock health and public health security, necessitating a novel antibiotic. Pleuromutilin, a natural antibiotic, has served as a promising foundation for developing new antibacterial agents through structural modification. This study aims to evaluate the antibacterial potential, safety, and pharmacokinetic profile of a novel pleuromutilin derivative 2-3 (22-[2-(L-prolylamino)phenylsulfanyl]-22-deoxypleuromutilin). The compound 2–3 exhibited potent antibacterial activity (MIC = 0.25 μg/mL), concentration-dependent bactericidal effects, and prolonged post-antibiotic effects (PAEs). Safety assessments revealed low cytotoxicity (CC50 = 62.63 μg/mL) and no observable hemolytic activity. In vitro metabolic studies indicated species-dependent clearance, primarily mediated by CYP3A4. Pharmacokinetic in rats showed rapid absorption and elimination, with oral and intramuscular bioavailability of 16.03% ± 8.82% and 53.36% ± 12.27%, respectively. Notably, 2–3 demonstrated superior efficacy over tiamulin in a neutropenic murine thigh infection model. Molecular docking revealed a stronger binding free energy between 2–3 and the 50S ribosomal subunit compared to tiamulin. Collectively, these results highlight 2–3 as a promising clinical candidate against S. aureus infections, characterized by enhanced efficacy and a favorable safety profile.
研究领域:
抗生素研发
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药理学
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微生物学
·
药物化学
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药物代谢
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产品关联
DOI
PubMed
高影响因子
MOLECULAR CELL
·
2024
·
IF 14.5
Wei Luo,Yunyuan Xu,Jie Cao,Xiaoyu Guo,Jingdan Han,Yuanyuan Zhang,Yuda Niu,Meiling Zhang,Yi Wang,Guohua Liang,Qian Qian,Song Ge,Kang Chong
While it is known that temperature sensors trigger calcium (Ca 2+ ) signaling to confer cold tolerance in cells, less is known about sensors that couple with other secondary messengers. Here, we identify a cold sensor complex of CHILLING-TOLERANCE DIVERGENCE 6 (COLD6) and osmotin-like 1 (OSM1), which triggers 2′,3′-cyclic adenosine monophosphate (2′,3′-cAMP) production to enhance cold tolerance in rice. COLD6, which is encoded by a major quantitative trait locus (QTL) gene, interacts with the rice G protein α subunit (RGA1) at the plasma membrane under normal conditions. Upon exposure to chilling, cold-induced OSM1 binds to COLD6, kicking out RGA1 from interaction. This triggers an elevation of 2′,3′-cAMP levels for enhancing chilling tolerance. Genetic data show that COLD6 negatively regulates cold tolerance and functionally depends on OSM1 in chilling stress. COLD6 alleles were selected during rice domestication. Knockout and natural variation of COLD6 in hybrid rice enhanced chilling tolerance, hinting design potential for breeding. This highlighted a module triggering 2′,3′-cAMP to improve chilling tolerance in crops.
研究领域:
植物学
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遗传学
·
分子生物学
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DOI
PubMed
高影响因子
NEW PHYTOLOGIST
·
2026
·
IF 8.7
Lele Chu,Xiangming Shang,Bachar Dahro,Xi Zeng,Wenqiang Hu,Chunlong Li,Ji-Hong Liu
Summary Ethylene exerts a divergent role in modulating plant organ abscission. Spermidine (Spd) shares a common precursor for de novo biosynthesis with ethylene, but the antagonistic role between them in the regulation of plant organ abscission remains largely elusive. Here, RNA-sequencing of abscission zones from ethylene-treated sweet orange ( Citrus sinensis L.) fruit led to the identification of two ethylene-responsive factors (ERFs), CsERF113 and CsERF7. CsERF113 functioned in promoting fruit abscission and suppressed Spd accumulation, whereas CsERF7 exhibited an opposite trend. CsERF113 and CsERF7 were verified to act as a transcriptional repressor or an activator of CsSAMDC1 / 2 / 3 encoding S -adenosylmethionine decarboxylase (SAMDC), an enzyme responsible for Spd biosynthesis, by binding directly to their promoters in an ethylene-dependent manner. Moreover, CsSAMDC1 / 2 / 3 functioned to inhibit fruit abscission by promoting Spd synthesis. Interestingly, CsERF7 and CsERF113 transcriptionally repressed each other to modulate the ethylene-mediated downregulation of CsSAMDC1 / 2 / 3 , forming an antagonistic regulatory circuit that could be negatively orchestrated by exogenous Spd. Taken together, our results uncover that CsERF113 and CsERF7 integrate the ethylene signal to antagonistically regulate CsSAMDC1 / 2 / 3 -mediated synthesis of Spd and fruit abscission. This study provides important insights into understanding the molecular mechanisms by which ethylene and Spd antagonize to modulate fruit abscission.
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DOI
PubMed
高影响因子
JOURNAL OF POLYMER RESEARCH
·
2019
·Vol. 26
·期 12
·1-12
·
IF 1.53
Jiao Yang,Chen Guofei,Zhou Haijun,Zhang Feng,Chen Xiaoqi,Li Yantao,Xiao Xueshan,Fang Xingzhong
A series of poly(benzimidazole-imide)s (PBIPIs) derived from different dianhydrides and 2-(3-aminophenyl)-5-aminobenzimidazole ( m -BIA) were synthesized via thermal imidization to form flexible films. This series of PBIPIs showed great T g s ranging from 296 to 484 °C, excellent thermal stability performed in 5% weight loss temperatures ( T d5% s) of 502–529 °C in N 2 and good mechanical properties (tensile strengths of 89–127 MPa, tensile moduli of 2.9–4.1 GPa and elongations at break of 3.9–6.9%). Compared with PIs derived from 6-amino-2-(4-(4-aminophenoxy)phenyl)-1H-benzimidazole ( p -BIODA), m -BIA based PBIPI films exhibited higher T g , and better solubility. Besides, the thermoplastic PBIPI resin (PI-6-PA) derived from 2,2-bis[4-(3,4-dicarboxyphenoxy)phenyl]propane dianhydride (BPADA) and m -BIA exhibited good melt processability with high T g of 273 °C, melt flow index (MFI) of 7.76 g/10 min, minimum complex viscosity of 11.9 × 10 3 Pa·s at 402 °C and low melt viscosity ratio of 2.46 at 400 °C.
研究领域:
高分子化学
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材料科学
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产品关联
DOI
高影响因子
BIORESOURCE TECHNOLOGY
·
2022
·
IF 11.889
Yue Wang,Bowen Wu,Tian Ma,Yaozu Mi,Hanyi Jiang,Haohao Yan,Peichao Zhao,Shuo Zhang,Linxuan Wu,Lei Chen,Hailian Zang,Chunyan Li
Low-temperature biorefineries inhibit the multiplication of undesired microorganisms, improve product purity and reduce economic costs. Herein, to improve the 2,3-butanediol (2,3-BD) bioconversion efficiency from hemicellulose, a psychrotrophic hemicellulose-degrading strain Raoultella terrigena HC6 with high β-xylosidase activity 1520 U/mL was isolated and genetically modified. Xylan (hemicellulose replacement) was depolymerized into xylooligosaccharides (XOS) and xylose by HC6, which were further converted into 2,3-BD. Transcriptomic analysis revealed that β-xylosidase gene ( xynB ) and xylose isomerase gene ( xylA ), which are beneficial for increasing the carbon flux from xylan to 2,3-BD, were significantly upregulated 56.9-fold and 234-fold, respectively. A recombinant strain was constructed by overexpressing xynB in HC6, which obtained 0.389 g/g yield of 2,3-BD from hemicellulose extracted from corn straw at 15 °C. This study proposed a promised strategy for the bioconversion of agricultural waste into 2,3-BD at low temperatures and provides a basis for future efforts in the achievement of carbon neutrality.
研究领域:
生物技术
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微生物学
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代谢工程
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环境科学
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产品关联
DOI
PubMed
高影响因子
ORGANIC & BIOMOLECULAR CHEMISTRY
·
2014
·Vol. 12
·期 27
·4885-4889
·
IF 3.487
Jiaxing Hu,Zhihong Deng,Xueqiong Zhang,Fanglin Zhang,Hua Zheng
A convenient one-pot reaction was conducted by mixing bromoacetophenone, a functionalized α,β-unsaturated ketone and potassium hydroxide in tetrahydrofuran at room temperature, ammonium acetate was added and heated to reflux, resulting in four chemical bonds forming from easily accessible substrates. This process provides a flexible and rapid synthetic route for the construction of polysubstituted benzofuro[2,3-c]pyridines in moderate to good yields.
研究领域:
有机化学
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药物化学
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DOI
PubMed
高影响因子
Chemistry-An Asian Journal
·
2015
·Vol. 10
·期 5
·1177-1183
·
IF 4.587
Shuai Zhao,Haining Wang,Lanxia Xin,Jian Cui,Yehai Yan
Graphical Easy as 2, 3, 4 : 2-(3,4-Dihydroxyphenyl) pyrrolidine grafted graphene was developed as a competent platform for covalent functionalization of graphene, from which four typical but not exclusive graphene-derived materials of magnetic graphene-FeCl 3 complex, phenolic-, epoxide-, and methacryloyl-functionalized graphenes were successfully prepared. Covalent functionalization has proven an effective solution for graphene to realize its revolutionary potential in real applications, whereas the platform strategy (a reactive graphene-based material acting as the platform to undergo post-reactions for generation of various graphene-derived materials) is an attractive option to execute efficiently such a task. This contribution demonstrates that 2-(3,4-dihydroxyphenyl) pyrrolidine (DHPP) grafted graphene, G-OH, is a competent platform. Four typical but not exclusive graphene-derived materials have been prepared from G-OH by using the chemical virtue of each DHPP unit having three categories totaling six reactive sites. The controlled feature of 1,3-dipolar cycloaddition for the synthesis of G-OH ensures that the electronic structure and properties of pristine graphene are succeeded largely by G-OH and thus its derivatives. A promising alternative to graphene oxide, which has been widely used as a platform to prepare the graphene-derived materials but suffers from some intrinsic disadvantages, is thus developed.
研究领域:
材料科学
·
化学
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产品关联
DOI
PubMed
高影响因子
Polymer Chemistry
·
2020
·Vol. 11
·期 11
·1937-1946
·
IF 5.342
Yang Jiao,Guofei Chen,Nafeesa Mushtaq,Haijun Zhou,Xiaoqi Chen,Yantao Li,Xingzhong Fang
Two isomeric diamine monomers, 2-(3-aminophenyl)benzo[d]oxazol-5-amine (2a) and 2-(3-aminophenyl)benzo[d]oxazol-6-amine (2b), were designed and synthesized. The corresponding novel series of poly(benzoxazole imide)s (PBOPIs) were prepared with commercial tetracarboxylic dianhydrides via thermal imidization. These series of PBOPIs showed great Tgs ranging from 285 to 363 °C, excellent thermal stability when performed at 5% weight loss temperatures (Td5%s) of 510–564 °C in N2 and good mechanical properties (tensile strengths of 103–126 MPa, tensile moduli of 2.9–3.7 GPa and elongations at break of 3.0–6.5%). Furthermore, controlled molecular weight (Mw) polymers PI-3a-PA and PI-3b-PA derived from 4,4′-oxydiphthalic anhydride (ODPA) with 2a and 2b demonstrated good melt processability with minimum complex viscosities of 2258 and 3444 Pa·s at 420 °C and low melt viscosity ratios of 1.29 and 1.93 at 400 °C, respectively. The PI-b series showed higher Tg & Td5% and lower transparency compared with the PI-a series due to the isomeric effect.
研究领域:
高分子科学
·
材料科学
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产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2024
·
IF 4
Meng Ye,Hongying Hou,Xianxi Liu,Zhaowei Sun,Xiaohua Yu,Ju Rong
With the development of the consumer society, low cost and high performance supercapacitors are being pursued. To realize the practical supercapacitors, developing the cheap and highly capacitive electrode is the most essential. However, it is a harsh challenge to achieve this target based on single-component electrode. Herein, a series of inexpensive ternary-metal-sulfides, 2MnS/Cu 2 S/ x ZnS/C ( x = 0, 0.5, 1, 2, 3) are synthesized by hydrothermal reaction and the subsequent calcination with expired manganese/copper gluconates as the raw materials for the electrode in the pseudocapacitors. Furthermore, the effect of ZnS's content on the electrochemical properties of the ternary composites is also investigated. Specially, the optimal 2MnS/Cu 2 S/xZnS/C( x = 1) can output a specific capacitance of 1608 F/g at 1 A/g in the three-electrode system, while the 2MnS/Cu 2 S/xZnS/C||AC( x = 1) asymmetric supercapacitor can deliver a specific capacitance of 194 F/g at 1 A/g with the desirable energy density (800 W/kg) and power density (70.9 Wh/kg), higher than those of other samples. Especially, even after 2000 cycles at 5.0 A/g, the 2MnS/Cu 2 S/xZnS/C||AC( x = 1) asymmetric supercapacitor also delivers the reversible specific capacitance of 103 F/g with high capacitance retention of 97.0 %, indicating high cycling stability. The outstanding performances of the optimal 2MnS/Cu 2 S/xZnS/C( x = 1) may be attributed to the bridge-effect of ZnS component, which makes up for the low conductivity of MnS component and the low capacitance of Cu 2 S component, thus achieving the best synergistic effect of ternary metal sulfide 2MnS/Cu 2 S/xZnS/C( x = 1) .
研究领域:
材料科学
·
电化学
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产品关联
DOI
高影响因子
ACS Applied Polymer Materials
·
2024
·
IF 4.4
Haifeng Yu,Yanting Du,Jiayu Li,Songhao Zhao,Cheng Wang,Shuhong Wang,Haiyang Chang
Donor–acceptor (D–A) conjugated polymers have exhibited their utility in the fabrication of memory devices with high information storage capacity. The device performance can be effectively regulated through the appropriate pairing of the acceptor and donor moieties. Six different D–A conjugated polymers, featuring varied structures, were synthesized by using the Suzuki coupling reaction. Donor molecules such as fluorene, carbazole, and 4′-methoxytriphenylamine, as well as the acceptor molecule dipyrido[3,2-a:2′,3′-c]phenazine (dppz), were employed in this process. Interestingly, it was observed that simply increasing the ratio of donor groups did not yield improvements in device performance. On the other hand, the memory devices fabricated using these polymers as the active layers exhibited favorable ternary resistance memory behavior. Specifically, the first and second threshold voltages were impressively low, at −0.40 and −0.75 V, respectively. The OFF: ON1: ON2 current ratio reached an outstanding ratio of 1:102.90:105.47. Moreover, these devices demonstrated excellent stability with a retention time of 104 s and an endurance of 103 cycles. In conclusion, this study successfully synthesized D–A conjugated polymer with dppz as an acceptor and proved the great potential of constructing ternary memory devices using the dppz structure.
研究领域:
材料科学
·
电子工程
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DOI
高影响因子
ANALYTICA CHIMICA ACTA
·
2019
·
IF 5.256
Feng Zhang,Mengke Wang,Lili Zhang,Xingguang Su
Herein, we developed a novel and sensitive ratiometric fluorescence strategy for pH sensing and urea detection based on MoS 2 quantum dots (MQDs) and 2, 3-diaminophenazine (DAP). The DAP was pH-sensitive and can be used as pH indicator while MQDs was pH-insensitive and acted as a reference fluorescent signal. The fluorescence intensity of DAP at 568 nm exhibited increases gradually while the fluorescence intensity of MQDs at 420 nm kept unchanged as the pH changed from 3.0 to 9.0. So the ratio of the two fluorescence intensities at 568 nm and 420 nm can be used to monitor the change of pH. The pH-sensing system showed a linear and reversible respond to pH in the range of 3.8–6.0 with an interval of 0.2 pH unit. Furthermore, the enzymatic reaction of urea in the presence of urease can lead to the pH increase of the solution, which can be used to detect urea by using the above-mentioned pH-sensing system. There exhibited a good linear relationship between the ratiometric fluorescence intensity of I 568 /I 420 and urea concentrations ranging from 5 to 700 μM. And a low detection limit of 1.8 μM was obtained. The proposed strategy exhibited excellent selectivity and sensitivity. Additionally, the developed ratiometric fluorescence strategy was successfully applied to detect urea in water samples.
研究领域:
生物化学
·
分析化学
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产品关联
DOI
PubMed
高影响因子
CHEMICO-BIOLOGICAL INTERACTIONS
·
2021
·
IF 5.194
Min Wang,Longji Fang,Tongtong Liu,Xuejie Chen,Yan Zheng,Yilong Zhang,Shiming Chen,Zeng Li
The development of multi-target-directed ligands (MTDLs) may improve complex central nervous system diseases such as Alzheimer's disease (AD). Here, a series of 7-O-1, 2, 3-triazole hesperetin derivatives was evaluated for their inhibition of cholinesterase , anti-neuroinflammatory, and neuroprotective activity. Among the hesperetin derivatives, compound a8 (7-O-((1-(3-chlorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)hesperetin) possessed excellent anti-butyrylcholinesterase activity (IC 50 = 3.08 ± 0.29 μM) and exhibited good anti-neuroinflammatory activity (IC 50 = 2.91 ± 0.47 μM) against NO production through remarkably blocking the NF-κB signaling pathway and inhibiting the phosphorylation of P65. In addition, a8 showed a remarkable neuroprotective effect and lacked neurotoxicity up to 50 μM concentration. Furthermore, possessing significant self-mediated Aβ 1-42 aggregation inhibitory activity, chelated biometals and reduced ROS production were found in compound a8 . In the bi-directional transport assay, a8 exhibited a blood–brain barrier penetrating ability. In this study, the Morris water maze task showed that compound a8 significantly improved the learning and memory impairment of the scopolamine-induced AD mice model. Results highlighted the potential of compound a8 to be a potential MTDL for the development of anti-AD agents.
研究领域:
神经科学
·
药理学
·
药物发现
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）