CHINESE JOURNAL OF CHEMISTRY
·
2025
·
IF 5.5
Meng Li,Yu-Na Jiang,Zheng Li,Zhaobo Liu,Zehua Chen,Yufei Mao,Kang Yuan,Jiting Cui,Haiming Zhu,Shu Xing,Ming Wang,Bing Wang
Comprehensive Summary Aromatic ketones, such as 9-fluorenone (9-FO), are known for their high intersystem crossing quantum yields ( Φ ISC ≈ 1), rendering them highly valuable for photochemical reactions and dye-sensitized solar cells. However, their use as photosensitizers in biological contexts has been hindered by their low extinction coefficients, high excitation energies, and weak fluorescence. To address these limitations, we conjugated 9-FO with a fused-ring electron donor, resulting in an acceptor-donor-acceptor derivative IDT-9F. This strategy has successfully redshifted the absorption peak of 9-FO (380 nm) into the visible light range (498 nm) and significantly enhanced its light absorption capability (~310-fold) and fluorescence quantum yield (~100-fold). Furthermore, IDT-9F was encapsulated within pH-responsive nanoparticles using an acid-induced charge-reversal polymer as the amphiphilic matrix, and enabled fluorescence imaging-guided photodynamic inactivation of Gram-positive bacteria in acidic environment with a remarkable bacterial inhibition rate exceeding 99.9%.
研究领域:
光化学
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生物光子学
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纳米医学
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有机化学
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抗菌治疗
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产品关联
DOI
高影响因子
ORGANIC & BIOMOLECULAR CHEMISTRY
·
2022
·Vol. 20
·期 15
·3201-3210
·
IF 3.89
Lin Chen,Wei Liang
Michael/ammonolysis cascade reactions between cyclohexane-1,3-dione-derived enaminones and olefinic azlactones via phase-transfer catalysis have been developed. This method provides rapid access to a suite of architecturally complex and diverse quinoline-2,5-diones bearing a secondary amide group at the C-3 position in moderate to excellent yields (53–94%) and with excellent diastereoselectivities (>99 : 1 dr in most cases). The achievement of a preparative-scale reaction and the diverse product derivatization that can be obtained highlight the application potential of this protocol both in academic and industrial settings. An investigation of the reaction mechanism implies that tetrabutylammonium hydroxide may be the actual catalyst during this cascade reaction.
研究领域:
有机化学
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药物化学
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DOI
高影响因子
LANGMUIR
·
2024
·
IF 3.7
Satish Gudala,Miao Dong,Xinrui Lin,Ruotong Liu,Annadurai Vinothkanna,Anubhuti Jha,Archi Sharma,Dazhuang Wang,Xinghua Liu,Jianxin Yang
A series of 1,2,4-triazolo-quinazolinones and 1,2-benzisothiazolone derivatives (S1–S12) were successfully synthesized as environmentally friendly alternatives to copper-based antifouling paints using N-alkylation, cyclocondensation, and one-pot three-component and amide coupling reactions. The monoclinic structure of single-crystal 1,2,4-triazolo-quinazolin-acetic acid (S8) was confirmed by single-crystal X-ray diffraction analysis. All the synthesized molecules were studied for their in silico molecular docking interactions with three target proteins, namely, RbmA, ToxR, and Bap. Following that, the antialgal activity was assessed against two types of marine algae: Chlorella sp. and Chaetoceros curvisetus. The minimal inhibitory concentration and zone of inhibition have been used to evaluate the antibacterial activities of S1–S12 against both marine Gram-positive (Staphylococcus aureus) and Gram-negative (Vibrio parahemolyticus and Vibrio vulnificus) bacteria. Additionally, antifouling studies have been done on all the compounds, and among them, 1,2,4-triazolo-quinazolinyl-acetate (S7), 1,2,4-triazolo-quinazolinyl-acetic acid (S8), 1,2,4-triazolo-quinazolinyl-oxobutanoate (S9), benzo[d]isothiazolyl butanoate (S10), benzo[d]isothiazolyl-acetic acid (S11), and 1,2,4-triazolo-quinazolinyl-acetyl-benzo[d]isothiazolone (S12) exhibited good antialgal, antibacterial, and antifouling activities.
研究领域:
海洋生物学
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药物化学
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环境科学
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产品关联
DOI
PubMed
高影响因子
Phytochemistry Letters
·
2018
·
IF 1.575
Dai Ren,Fan-Cheng Meng,Hui Liu,Tong Xiao,Jin-Jian Lu,Li-Gen Lin,Xiu-Ping Chen,Qing-Wen Zhang
Three new biflavonoids, umcephabiflovin A ( 1 ), umcephabiflovin B ( 2 ), and S -taiwanhomoflavone-B ( 3 ), together with seven known flavonoids ( 4–10 ) and seven known alkaloids ( 11 – 17 ), were isolated from the twigs of Cephalotaxus oliveri Mast. The flavonoids were found to inhibit α-glucosidase activity.
研究领域:
植物化学
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药理学
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天然产物研究
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产品关联
DOI
高影响因子
Journal of Ovarian Research
·
2019
·Vol. 12
·期 1
·1-7
·
IF 2.469
Wu Gengxiang,Hu Xue,Ding Jinli,Yang Jing
Background The mechanism of the pathological change of polycystic ovary syndrome (PCOS) is still unclear. Previous studies have shown that PCOS is a chronic nonspecific low-grade inflammatory condition, and that heat shock protein (HSP)70 has a potent anti-inflammatory property. So the aim of this study is to investigate the correlation between HSP70 and the hormones and inflammatory factors and to find out the role of HSP70 in the pathogenesis of PCOS.Methods Twenty female Sprague–Dawley (SD) rats (aged 23 days and weighted 80-90 g) were randomly divided into two groups (n = 10 per group), PCOS group and control group. PCOS group were subcutaneously injected with 6 mg/100 g dehydro-epiandrosterone (DHEA) for 20 consecutive days, the control group were subcutaneously injected with a solvent of equivalent amount. All the samples were collected in the morning fasting state, 12 h after the last administration. Histological examinations of ovarian tissues were analyzed. Hormone levels and inflammatory factors levels were measured by enzyme-linked immunosorbent assay (ELISA) kits.Results Serum concentrations of testosterone (T) and luteinizing hormone (LH) were significantly higher in the PCOS group than the control group (P < 0.001), but the concentrations of estradiol (E2), follicle stimulating hormone (FSH) and insulin didn’t show significant difference between these two groups. All the concentrations of inflammatory factors including C-reactive protein (CRP), interleukin (IL)-6, IL-18, and tumor necrosis factor (TNF)-α. were significantly higher in PCOS group than the control group (P < 0.001). The expressions of HSP70 were significantly lower in serum but higher in ovarian tissues in the PCOS group than the control group. Spearman rank correlation analysis showed strong negative correlation of serum HSP70 levels with T, LH and all the detected inflammatory factors.Conclusion The abnormal expression of HSP70 correlated with testosterone and inflammatory factors, which indicates that HSP70 may play an important role in PCOS pathology.
研究领域:
内分泌学
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生殖生物学
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炎症
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2021
·
IF 6.953
Yanan Zhang,Xue Li,Di Xu,Mengyun Wu,Yinghui Dai,Mingyu Xia,Dong Wang
Bufadienolides are the main active ingredients of Venenum Bufonis, which is a widely used traditional Chinese medicine secreted from parotoid gland and skin glands of Bufo bufo gargarizans . According to the transcriptome analysis, “cholesterol-bile acid-bufadienolidies pathway” was proposed as animal-derived bufadienolides biosynthesis pathway by us previously. In this pathway 3 β -hydroxysteroid dehydrogenase (3 β HSD) and steroid 5 β -reductase (SRD5 β ) might be the key enzymes to convert the A/B ring to cis -configuration. Therefore, as the second report of our group, here we report the cloning of the full length of SRD5 β cDNA of B. bufo gargarizans ( Bbg - SRD5β ) from the parotoid gland of B. bufo gargarizans for the first time, and site-directed mutagenesis was used to explored the character of Bbg -SRD5 β . Bbg -SRD5 β had an open reading frame of 981 bp and encoded 326 amino acids residues. The expression conditions of the recombinant Bbg -SRD5 β in E. coli BL21 (DE3) harbored with pCold- Bbg -SRD5 β was optimized as induction for 10 h at 15 °C with 0.1 mM IPTG. With NADPH as a cofactor, Bbg -SRD5 β can reduce the Δ 4,5 double bonds of progesterone to generate dihydroprogesterone õwithout substrate inhibition effect. The catalytic rate of mutant type Bbg -SRD5 β -Y132G was 1.8 times higher than that of wild type Bbg -SRD5 β . Although Bbg -SRD5 β was almost unable to reduce the progesterone to dihydroprogesterone after mutation of V309, the affinity of enzyme with NADPH changed significantly. Bbg -SRD5 β is the key enzymes to convert the A/B ring of steroid to cis -configuration, and V309 is a key site affecting the binding affinity of enzyme with NADPH, and the mutation of Y132 can adjust the catalytic rate of Bbg -SRD5 β .
研究领域:
生物化学
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分子生物学
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中医药学
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药理学
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DOI
PubMed
高影响因子
BIOORGANIC CHEMISTRY
·
2021
·
IF 5.275
Shiyang Zhou,Huiying Zou,Gangliang Huang,Guangying Chen,Xueming Zhou,Shuheng Huang
Four series of double-ring conjugated enones were designed, synthesized and studied for the inhibition of synovial cell activity through the modification of Dysodensiol K core structure, double-ring, double-bond and double-carbonyl groups. For in vitro synovial cell assay of rats, compound 151 and 168 exhibited good inhibitory activities, with IC 50 values of 2.71 ± 0.18 and 2.68 ± 0.16 μM respectively. At the same time, the LDH release and LD 50 test results revealed that the target compounds were low cytotoxicity and acute toxicity. For in vivo CIA model test through the oral administration, compounds 151 and 168 were exhibited similar effect to positive control group methotrexate.
研究领域:
药物化学
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药理学
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风湿病学
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DOI
PubMed
高影响因子
CHEMICAL ENGINEERING SCIENCE
·
2021
·
IF 4.311
Xiaoyan Chen,Fan Wang,Qiang Yu,Shijie Liu,Wen Wang,Yu Zhang,Zhongming Wang,Zhenhong Yuan
One pot cascade of enzymatic catalysis was applied for d -allulose synthesis from d -glucose by the combination of d -glucose isomerase (GI) from Escherichia coli MG1655 and d -allulose 3-epimerase (DAE) from Agrobacterium tumefaciens C58. The synthesis process was investigated by characterizing the initial substrate concentration, molar ratios of GI and DAE, the enzyme loading, and contents of cobalt and magnesium ions. The increase of enzyme loading and the molar ratios of GI vs DAE caused the raising of d -allulose yield from 4% to 9%, verifying that the generation rate of d -fructose was an essential factor for rare sugar conversion improvement. The optimal enzyme loadings required for reactions with substrate concentrations of 100 g L −1 and 200 g L −1 were 60 U and 200 U. Kinetics stimulation was conducted to reveal the underlying relationship within the three sugars converted by dual-enzyme, with the fitting curve validated the reliability of the model.
研究领域:
生物化学
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酶工程
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食品科学
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产品关联
DOI
高影响因子
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2023
·
IF 6.7
Yong-Jun Huang,Xiao-Lin Zhong,Yi-Peng Zang,Ming-Han Yang,Jing Lin,Wei-Min Chen
The natural prenylated chalcone isobavachalcone ( IBC ) shows good antibacterial activity against Gram-positive bacteria but is ineffective against Gram-negative bacteria, most likely due to the outer membrane barrier of Gram-negative bacteria. The Trojan horse strategy has been shown to be an effective strategy to overcome the reduction in the permeability of the outer membrane of Gram-negative bacteria. In this study, eight different 3-hydroxy-pyridin-4(1 H )-one-isobavachalcone conjugates were designed and synthesized based on the siderophore Trojan horse strategy. The conjugates exhibited 8- to 32-fold lower minimum inhibitory concentrations (MICs) and 32- to 177-fold lower half-inhibitory concentrations (IC 50 s) against Pseudomonas aeruginosa PAO1 as well as clinical multidrug-resistant (MDR) strains compared to the parent IBC under iron limitation. Further studies showed that the antibacterial activity of the conjugates was regulated by the bacterial iron uptake pathway under different iron concentration conditions . Studies on the antibacterial mechanism of conjugate 1b showed that it exerts antibacterial activity by disrupting cytoplasmic membrane integrity and inhibiting cell metabolism. Finally, conjugate 1b showed a lower cytotoxic effects on Vero cells than IBC and a positive therapeutic effect in the treatment of bacterial infections caused by Gram-negative bacteria PAO1. Overall, this work demonstrates that IBC can be delivered to Gram-negative bacteria when combined with 3-hydroxy-pyridin-4(1H)-ones as siderophores and provides a scientific basis for the development of effective antibacterial agents against Gram-negative bacteria.
研究领域:
微生物学
·
药物化学
·
感染病学
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产品关联
DOI
PubMed
高影响因子
MICROBIAL PATHOGENESIS
·
2024
·
IF 3.3
Xiaoye Cheng,Yijin Jiang,Xu Zhao,Nana Ma,Xiangzhen Shen
Lactate has been increasingly recognized for its role in diseases progression, necessitating a deeper understanding of its metabolic processes and regulatory mechanisms. This study aimed to evaluate the impact of lipopolysaccharide (LPS) on lactate accumulation in bovine mammary epithelial cells (BMECs) and to elucidate the underlying regulatory mechanisms. Further optimization of LPS treatment points was achieved by assessing the content of key glycolytic enzymes-hexokinases (HK), pyruvate kinase (PK) and pyruvate dehydrogenase (PDH)-as well as the expression levels of HK2, pyruvate dehydrogenase kinase4 (PDK4) and lactate dehydrogenase (LDHA). Our results indicate that LPS can promote intracellular glycolysis and inhibits pyruvate synthesis, thereby increasing lactate content. BMECs were cultured and divided into a control group (CON) and an LPS-stimulated group (10 μg/mL for 6 h, LPS group). LPS was found to upregulate expression levels of HIF-1α and MCT1, suggesting a role for HIF-1α and MCT1 in cellular glucose metabolism. To explore the effect of HIF-1α on lactate accumulation, BMECs were stimulated with a HIF-1α inducer (COCL 2 ) and HIF-1α inhibitor (DMBPA). COCL 2 was observed to promote lactate accumulation, while DMBPA inhibited it. Additionally, modulation of HIF-1α expression influenced the expression of MCT1, which is a crucial transporter for extracellular lactate influx. To investigate the specific impact of MCT1 on intracellular lactate, we utilized overexpression plasmids and small interfering RNA to modulate MCT1 expression. The findings indicate that while MCT1 expression alone does not affect intracellular lactate levels, it does modulate the changes induced by LPS. In conclusion, our study suggests that LPS regulates lactate accumulation in BMECs through the HIF-1α/MCT1 pathway, providing insights into the metabolic dysregulation associated with LPS-induced stress in dairy cattle.
研究领域:
动物科学
·
细胞生物学
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代谢学
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乳品科学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2024
·
IF 3.1
Yufang Huang,Xikang Ren,Yonghui Li,Junqing Zhang,Na Wei,Hailong Li,Yinfeng Tan
The Liangfu formula, as described in 'Liangfang Jiye', is well-known for its efficacy in treating stomach pain, abdominal pain, and dysmenorrhea. This research aimed to investigate the pharmacokinetics and tissue distribution of 5-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenyl-3-heptanone (DPHA), Galangin, Kaempferide, 5-Hydroxy-1,7-diphenyl-3-heptanone (DPHC), α-Cyperone, and Nootkatone in vivo using an LC-MS/MS method. The method successfully separated the six active components and internal standards (Chrysin and Yakuchinone-A) on an XB-C18 column with a mobile phase of 0.2 ‰ formic acid water-acetonitrile. It demonstrated good linearity with a correlation coefficient (r 2 ) ≥ 0.9911 and a lower limit of quantification (LLOQ) of 5–80 ng/mL for the different components. Precision, accuracy, matrix effects, and recovery rates were within acceptable ranges. Pharmacokinetic analysis revealed significant differences in parameters between primary dysmenorrhea (PD) and normal rats (especially AUC, T max, and CL z /F). Tissue distribution showed that the six active components of the herbal pair Alpinia officinarum Hance- Cyperus rotundus L. (HPAC) extract was primarily distributed in the liver, lung, and kidney. This study offers valuable insights into the potential mechanisms of action and drug development for treating PD.
研究领域:
药理学
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中医
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分析化学
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药物动力学
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产品关联
DOI
PubMed
高影响因子
Food Bioscience
·
2022
·
IF 5.318
Qi Mei,Zhaona Xu,Quanye Wu,Likang Qin,Haiying Zeng,Yi Zhu
In this study, an untargeted metabolomics method based on LC-MS was used to investigate the differential metabolites of coix seed after fermentation by Monascus purpureus . The compounds with highly correlated variable importance in projection (VIP) values of orthogonal partial least squares discriminant analysis (OPLS-DA) were selected as the important metabolites of coix seed samples. Coix seed was fermented by M. purpureus for 9 d. The color value units (CVU) of pigment in fermented coix seed reached 157.47 CVU/g, and the contents of total phenols and total flavonoids were 0.32 mg/g and 1.2 mg/g, respectively. A total of 270 differential metabolites were detected, including amino acids, peptides, fatty acids, phenols, steroids, and their derivatives, of which the relative contents of 187 metabolites showed a significant upward trend (p < 0.05). Amino acids, peptides and analogues accounted for the largest proportion at 26%, among which most metabolites were enriched. For example, N-alpha-acetyllysine, l -tryptophan and l -arginine exhibited a fold change (FC) of 6200.87, 330.29, and 35.59, respectively. In particular, the detected steroid metabolites accounted for 3% of the total metabolites, and they all participated in the same pathway, in which androsterone, 2-methoxyestrone and etiocholanolone were upregulated. The synthesis of these steroids was related to the precursors and enzymes in the pathway, such as dehydroepiandrosterone, androstenedione, and 3beta-hydroxy-delta5-steroid dehydrogenase (HSD3B). The results of this study reveal M. purpureus fermentation can successfully transform coix seed, improving the functional activities of metabolites. Thus, this process has high development value with important applications in the food industry.
研究领域:
食品科学
·
代谢组学
·
微生物学
·
药理学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）