Brazilian Journal of Pharmaceutical Sciences
·
2023
·
IF 1.3
Mei Xuejiao,Lu Dingqiang,Yan Xiangping
L-Malic acid is the Active Pharmaceutical Ingredient of the latest generation of compound electrolyte injection (STEROFUNDIN ISO, Germany) and plays a very important role in the rescue of critically ill patients. The optical purity of L-malic acid is a Critical Quality Attributes. A new reversed-phase high performance liquid chromatography (RP-HPLC) method for pre-column derivatization of D-malic acid enantiomer impurity in L-malic acid bulk drug was established. The derivatization reaction was carried out using (R)-1-(1-naphthyl)ethylamine ((R)-NEA) as a chiral derivatization reagent. The Kromasil C18 column was used with a detection wavelength of 225 nm, a flow rate of 1.0 mL·min-1, and a column temperature of 30 °C. The mobile phase was acetonitrile-0.01 mol·L-1 potassium dihydrogen phosphate solution (containing 20 mmol·L-1 sodium heptanesulfonate, adjusted to pH 2.80 with phosphoric acid) (at a ratio of 45:55) and the resolution of D-malic acid and L-malic acid derivatization products reached 1.7. The proposed method possesses the advantages of simple operation, mild conditions, stable derivatization products and low cost. Also it gave better separation and was more accurate than previous methods.
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高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2022
·
IF 3.841
Qian Liu,Jia Wang,Yao Chong,Jinyan Liu
The corrosion inhibition efficiency of Betaine , 3-(N, N-dimethyldodecylammonio) propanesulfonate (SB3–12) and 2-(DodecyldiMethylaMMonio) acetate (BS-12) on Q235 steel in 1 mol⋅L −1 hydrochloric acid (HCl) solution were studied at various inhibitor concentration and temperature by means of the weight loss method (WLM), electrochemical impedance spectroscopy (EIS), potential polarization curve, atomic force microscope (AFM), X-ray photoelectron spectroscopy (XPS), Raman spectra , scanning electron microscopy (SEM) and electronic energy spectrum analyzer (EDS). The weight loss results showed that the increase of inhibition efficiency mainly attributed to its high concentration. While Betaine had almost no protective effect for metals, SB3–12 and BS-12 were powerful inhibitors with the inhibition efficiency of 89.06% and 95.98%, respectively at 1 × 10 −1 mol⋅L −1 at 30 °C. The blocking effect of BS-12 for metal corrosion that induced by HCl was stronger than SB3–12. The potential polarization curve potential demonstrated that SB3–12 and BS-12 were both mixed type corrosion inhibitors . The surface analysis results revealed that SB3–12 or BS-12 could be well adsorbed on the Q235 surface to form a compact membrane that is responsible for the protection of Q235 steel from corrosion. The theoretical calculations including quantum chemical calculations and molecular dynamics simulations , which based on density functional theory provided strong evidence for the close relationship between the molecular structure of inhibitor and its inhibition efficiency. Our study of corrosion inhibition efficiency of green betaine type surfactants laid a theoretical foundation for the application of betaine derivatives in metal anti-corrosion.
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CHEMISTRY & BIODIVERSITY
·
2021
·Vol. 18
·期 4
·e2001007
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IF 2.408
Yan Zhao,Yu Wang,Min Zhang,Yugang Gao,Zhaowei Yan
Ginsenosides (20 S )-Rg3 and (20 R )-Rg3 are famous rare ginsenosides from red ginseng, and their configurations in C-20 are different. This study aimed to investigate the protective mechanism of ginsenosides (20 S )-Rg3 and (20 R )-Rg3 on H 2 O 2 -induced H9C2 cells and compare their activity. The results showed that the ginsenosides (20 S )-Rg3 and (20 R )-Rg3 could increase the cell activity and the levels of GSH-Px, SOD and CAT, and decrease activities of LDH, MDA and ROS. Further studies showed that ginsenosides (20 S )-Rg3 and (20 R )-Rg3 could prevent oxidative stress injury of H9C2 cells by H 2 O 2 through the Keap-1/Nrf2/HO-1 pathway. But the ML385 counteracts these effects. Interestingly, among these results, ginsenoside (20 R )-Rg3 was superior to (20 S )-Rg3, indicating that ginsenoside (20 R )-Rg3 have a stronger effect of antioxidative stress. This study reflected that ginsenoside (20 R )-Rg3 could be used as a potential Nrf2 activator and a safe effective Chinese herbal monomer in the treatment of cardiovascular disease.
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高影响因子
MEDICAL SCIENCE MONITOR
·
2020
·
IF 1.918
Ying Lei,Tianxiao Yang,Aijing Shan,Wei Di,Mengyao Dai,Jingminjie Nan,Dongxue Liu,Yanan Cao,Xiuli Jiang
Background Interleukin-1 receptor-associated kinases (IRAKs) are crucial mediators in the signaling pathways of Toll-like receptors (TLRs)/IL1Rs. Targeting the IRAK4/IRAK1/TRAF6 axis and its associated pathway has therapeutic benefits in liver fibrosis. However, the function of IRAK1 itself in the development of liver fibrosis remains unknown. Material/Methods Irak1 global knockout (KO) mice were generated to study the functional role of Irak1 in liver fibrosis. Male Irak1 knockout and control mice were challenged with chronic carbon tetrachloride (CCl 4 ) or fed a methionine- and choline-deficient diet (MCDD) to generate models of nonalcoholic steatohepatitis (NASH). Liver inflammation and collagen deposition were assessed by histological examination, quantitative real-time PCR (qRT-PCR), and western blotting of hepatic tissues. Results The mRNA expression of the downstream inflammatory gene Il1 β was significantly lower in Irak1 -KO than in control mice. Irak1 ablation had little effect on inflammatory cell infiltration into livers of mice with NASH. Collagen deposition and the expression of genes related to fibrogenesis were similar in the livers of Irak1 -KO and control mice exposed to CCl 4 and MCDD. The loss of Irak1 did not affect lipid or glucose metabolism in these experimental models of steatohepatitis. Conclusions Irak1 knockout reduced the expression of inflammatory genes but had no effect on hepatic fibrogenesis. The Irak1 -related pathway may regulate liver fibrosis via other pathways or be compensated for by other factors.
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ELECTROCHIMICA ACTA
·
2018
·
IF 5.116
Li Zheng,Wei He,Kai Zhu,Chong Wang,Shouxu Wang,Yan Hong,Yuanming Chen,Guoyun Zhou,Hua Miao,Jinqun Zhou
A leveler containing quaternary ammonium cations, namely poly (1-vinyl imidazole co 1, 4-butanediol diglycidyl ether) (VIBDGE) was synthesized and studied in this work. Quantum chemical calculations and molecular dynamics simulation of VIBDGE were employed to get insight to the adsorption model by assessing the molecular configuration and electronic orbital parameters. The simulation results reveal that VIBDGE will spontaneously absorb on the copper surface because of its tiling way, the generated nitrogen ions and the large molecular volume of VIBDGE. Galvanostatic measurements (GMs) and cyclic voltammetry (CV) tests were performed to investigate the electrochemical behaviors of VIBDGE and its synergistic mechanism with other additives. The results of GMs demonstrate VIBDGE exhibits good inhibiting performance in copper deposition. However, the reactant, namely 1-vinyl imidazole and 1, 4-butanediol diglycidyl ether, have no inhibition effect. Additionally, GMs results show that adsorption competition between bis-(sodium sulfopropyl)-disulfide (SPS) and VIBDGE is kinetically controlled and a steady state can be achieved regardless of the injection order of additives. The steady potential at lower rpm is less polarized and thus very beneficial for achieving uniform plating of through-hole (TH). The CV testes show that VIBDGE is capable of inhibiting copper deposition in the absence of chloride ions and chloride ions have a synergistic effect with VIBDGE. In addition, VIBDGE and PEG have competitive adsorption in copper deposition process . Consistent with the results of the GMs, the CV results illustrate that in the VIBDGE-SPS-PEG-Cl - system, the amount of copper deposited in the center of TH is more than that of the surface. Through the results of electroplating, it is confirmed that VIBDGE-SPS-PEG-Cl - system significantly improves the throwing power which is in accordance with simulation and electrochemical experiments.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2024
·
IF 4.5
Yaru Li,Qian Yang,Lanlan Fan,Fang Liu,Yaqi Shang,Baoxin Zhang,Zheng Wang,Yanjun Zhao
Ovarian cancers (OC) often resist current standard chemotherapy because of the cancer heterogeneity and over-expression of an anti-apoptotic protein, myeloid cell leukemia-1 (MCL-1). The heterogeneous OC shows impaired redox homeostasis and relies heavily on glutathione peroxidase 4 to eliminate toxic lipid peroxides. Therefore, integrated apoptosis and ferroptosis therapy is promising for OC management. The current work reports a liposomal nanosystem for apoptotic and ferroptotic OC therapy. Simvastatin (Sim) and vorinostat (Saha) were selected as the pleiotropic model drugs. The successive release of Saha and Sim from liposomes enabled the sequential amplification of MCL-1 by Saha, and then MCL-1 inhibition by Sim. Such a strategy could potently induce apoptosis in a human OC cell line (SKOV3), as indicated by increased intracellular cytochrome c concentration, caspase 3/9 activity, and the extent of apoptosis. Besides, Saha played multiple roles in cell death. It could induce cell cycle arrest at the G 2 /M phase and apoptosis. Saha also inhibited the glutamate-cystine transporter (SLC7A11) and provoked ferroptosis, which was corroborated by the depletion of glutathione, reduced nicotinamide adenine dinucleotide phosphate, and boost of lipid peroxides and malondialdehyde in SKOV3 cells. The current work integrated the “sequential amplification and inhibition of MCL-1 target” concept with combinational apoptosis and ferroptosis OC therapy, which might offer a new approach for managing resistant OC and other malignant diseases.
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MedComm
·
2024
·Vol. 5
·期 5
·e555
·
IF 10.7
Heng Liang,Jiani Zhan,Yunqiu Chen,Zikang Xing,Zhen Ning Tony He,Yuying Liu,Xuewen Li,Yijia Chen,Zhiyao Li,Chunxiang Kuang,Dan Yang,Qing Yang
Indoleamine 2,3-dioxygenase 1 (IDO1), the key enzyme in the catabolism of the essential amino acid tryptophan (Trp) through kynurenine pathway, induces immune tolerance and is considered as a critical immune checkpoint, but its impacts as a metabolism enzyme on glucose and lipid metabolism are overlooked. We aim to clarify the potential role of IDO1 in aerobic glycolysis in pancreatic cancer (PC). Analysis of database revealed the positive correlation in PC between the expressions of IDO1 and genes encoding important glycolytic enzyme hexokinase 2 (HK2) , pyruvate kinase (PK) , lactate dehydrogenase A (LDHA) and glucose transporter 1 (GLUT1) . It was found that IDO1 could modulate glycolysis and glucose uptake in PC cells, Trp deficiency caused by IDO1 overexpression enhanced glucose uptake by stimulating GLUT1 translocation to the plasma membrane of PC cells. Besides, Trp deficiency caused by IDO1 overexpression suppressed the apoptosis of PC cells via promoting glycolysis, which reveals the presence of IDO1–glycolysis–apoptosis axis in PC. IDO1 inhibitors could inhibit glycolysis, promote apoptosis, and exhibit robust therapeutic efficacy when combined with GLUT1 inhibitor in PC mice. Our study reveals the function of IDO1 in the glucose metabolism of PC and provides new insights into the therapeutic strategy for PC.
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高影响因子
MOLECULES
·
2022
·Vol. 27
·期 15
·4996
·
IF 4.927
Guang-Xi Yu,Ying Hu,Wei-Xin Zhang,Xin-Yi Tian,Sai-Yang Zhang,Yan Zhang,Shuo Yuan,Jian Song
[1,2,4]Triazolo[1,5-a]pyrimidine and indole skeletons are widely used to design anticancer agents. Therefore, in this work, a series of [1,2,4]triazolo[1,5-a]pyrimidine indole derivatives were designed and synthesized by the molecular hybridization strategy. The antiproliferative activities of the target compoundsH1–H18against three human cancer cell lines, MGC-803, HCT-116 and MCF-7, were tested. Among them, compoundH12exhibited the most active antiproliferative activities against MGC-803, HCT-116 and MCF-7 cells, with IC50values of 9.47, 9.58 and 13.1 μM, respectively, which were more potent than that of the positive drug5-Fu. In addition, compoundH12could dose-dependently inhibit the growth and colony formation of MGC-803 cells. CompoundH12exhibited significant inhibitory effects on the ERK signaling pathway, resulting in the decreased phosphorylation levels of ERK1/2, c-Raf, MEK1/2 and AKT. Furthermore, compound12induced cell apoptosis and G2/M phase arrest, and regulated cell cycle-related and apoptosis-related proteins in MGC-803 cells. Taken together, we report here that [1,2,4]triazolo[1,5-a]pyrimidine indole derivatives, used as anticancer agents via the suppression of ERK signaling pathway and the most active compound,H12, might be a valuable hit compound for the development of anticancer agents.Keywords:[1,2,4]triazolo[1,5-a]pyrimidine;indole;antiproliferative activities;ERK signaling pathway
研究领域:
药物化学
·
肿瘤学
·
药理学
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JOURNAL OF PINEAL RESEARCH
·
2019
·Vol. 67
·期 2
·e12582
·
IF 15.221
Zixin Zhang,Qian Hu,Yanan Liu,Peilei Cheng,Hua Cheng,Weixin Liu,Xiaojuan Xing,Zhiyong Guan,Weimin Fang,Sumei Chen,Jiafu Jiang,Fadi Chen
The transition from vegetative to reproductive growth is a key developmental event in a plant's life cycle. The process is mediated by a combination of phytohormones, including melatonin (MT) and strigolactone (SL). Here, the Arabidopsis mutants, d14-1 and max4-1 , which are compromised with respect to either SL synthesis or signaling, were shown to flower earlier than wild types. The tissue MT content in both mutants was higher than in wild types, as a result of the up-regulation of various genes encoding enzymes involved in MT synthesis. The abundance in the mutants of transcripts derived from each of the genes SPLs , AP1 , and SOC1 was reduced with exogenously supplied MT, while FLC was induced. Plants exposed to a high concentration of MT did not flower earlier than wild types. The tissue MT content of a mutant unable to synthesize caffeic acid O -methyltransferase was less than that of wild type and flowered earlier than did wild types. The suggestion is that the flowering time of Arabidopsis is altered if the tissue content of MT is either higher than ~ 8 ng/g F.W, or lower than ~ 0.9 ng/g. Within this range, SL acts to determine flowering time by its regulation of SPL gene s . The application of exogenous SL reduces tissue MT content. The flowering time of the flc-3 mutant was unaffected by exogenously supplying either MT or/and SL. It is proposed that MT acts downstream of SL to activate FLC , inducing a delay to flowering if its concentration lies outside a certain range.
研究领域:
植物生物学
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激素调控
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发育遗传学
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高影响因子
IMMUNITY
·
2025
·Vol. 58
·期 7
·1811-1829
·
IF 26.3
Ding Qiu,Shuishen Zhang,Chanyan Huang,Xinying Wang,Jianping Deng,Haiyang Sun,Bingbing Feng,Ying Tan,Kaile Ji,Shaoting Xu,Xiaoqi Ye,Chao Cheng,Shigeru Kakuta,Yoshiyuki Adachi,Yoichiro Iwakura,Shuai Wang,Shaowei Dong,Ce Tang
Dectin-1 ( Clec7a ), a C-type lectin receptor for β-glucans, is critical in host defense against fungal infections and has been implicated in allergic responses, yet its role in pulmonary fibrosis remains unclear. In this study, we reveal that bleomycin-induced pulmonary fibrosis was suppressed in Dectin-1-deficient mice, mediated by interactions with the commensal lung fungus Engyodontium . Dectin-1 was predominantly expressed on alveolar macrophages (AMs), correlating with fibrosis severity in both humans and mice. Dectin-1 deficiency reduced Arginase-1 and TGF-β-producing AMs and profibrotic factor expression. Mechanistically, Dectin-1 signaling promoted quiescent AM differentiation into profibrotic AMs via the Raf1-dependent pathway, bypassing CARD9 signaling and mono-macrophage chemotactic recruitment. Therapeutic targeting of Dectin-1 with laminarin or Raf1 inhibitors attenuated fibrosis in mice and reduced profibrotic factors in human AMs and fibroblasts. These findings highlight the Dectin-1-Raf1 axis as a key regulator of pulmonary fibrosis and a promising therapeutic target for fibrotic diseases.
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Canadian Journal of Chemistry
·
2021
·Vol. 99
·期 11
·
IF 1.118
Ying Liu,Mengyu Zhu,Yadong Hu,Yijun Zhao,Chengzhu Zhu
The photochemical reactions between 1-naphthol (1-NP) and the superoxide anion radical (O2•–) were investigated in detail by using 365 nm UV irradiation. The results showed that the conversion rate of 1-NP decreased with the increase of the initial concentration of 1-NP, whereas by increasing the pH and riboflavin concentration, the photochemical reaction was accelerated. The second-order reaction rate constant was estimated to be (3.64 ± 0.17) × 108 L mol−1 s−1. The major photolysis products identified by using gas chromatography – mass spectrometry (GC–MS) were 1,4-naphquinone and 2,3-epoxyresin-2,3-dihydro-1,4-naphquinone, and their reaction pathways were also discussed. An atmospheric model showed that both the bulk water reaction and the heterogeneous surface reaction deserve attention in atmospheric aqueous chemistry.
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Frontiers in Chemistry
·
2022
·
IF 5.545
Zhang Changsheng,Chu Shaoqi,Jiang Jie,Zhao Jinchong,Wen Song,Sun Bing,Xu Wei
Synthesis of zeolites in more efficient and greener methods is of great significance in both industrial and academic fields. However, the relative long time for zeolite crystallization and much consumption of water solvent make the target challengeable. Herein, a route for ultrafast synthesis of nano Silicalite-1 zeolites in 10 min with much less water consumption has been developed. Comprehensive characterizations, i.e., X-ray powder diffraction, N2 sorption, scanning electron microscope, and NMR, confirm the high quality of such obtained Silicalite-1 zeolites. In the catalytic deoxygenation of O2-containing ethylene (mixture of O2 and ethylene), these reported Silicalite-1 zeolite samples show the comparable performance with the conventional Silicalite-1 zeolites synthesized under hydrothermal conditions. This research therefore provides a new trial toward the ultrafast synthesis of zeolite materials in an environment-friendly route.
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