ARCHIV DER PHARMAZIE
·
2022
·Vol. 355
·期 7
·2100465
·
IF 4.613
Yating Guo,Xiaoding Jiang,Qi Chang,Zhihong Xiao,Zhuo Chen,Dejian Jiang,Gaoyun Hu,Qianbin Li
A series of novel pyrazolo[3,4- b ]pyridine derivatives were designed, synthesized, and biologically evaluated for anti-lung cancer activity. Structure–activity relationship and AutoGPA models were constructed based on the in vitro antiproliferative potency of the compounds against a human lung adenocarcinoma cell line (A549). Compound 9d exhibits improved potency for A549 cell growth inhibition (3.06 ± 0.05 μM) compared with A-769662 (45.29 ± 2.14 μM). Compound 9d can elevate the phosphorylation levels of adenosine monophosphate-activated protein kinase (AMPK) and its substrate acetyl-CoA carboxylase and reduce the level of phosphorylated ribosomal S6 kinase (p-70S6K) at 1 μM, which is comparable to the activity of A-769662 at 20 μM. 9d induced G2/M cell cycle arrest, which was rescued when co-incubated with “Compound C,” a potent AMPK inhibitor. Taken together, compound 9d showed potential anti-lung cancer activity via inducing cell cycle arrest by regulation of the AMPK/70S6K pathway in A549 cells, which could provide a new lead for the discovery of anti-lung cancer agents.
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PubMed
高影响因子
Aging-US
·
2021
·
IF 5.682
Longlong Gong,Zhengzhi Zou,Lei Liu,Shuang Guo,Da Xing
Ameliorating hyperglycemia and insulin resistance are major therapeutic strategies for type 2 diabetes. Previous studies have indicated that photobiomodulation therapy (PBMT) attenuates metabolic abnormalities in insulin-resistant adipose cells and tissues. However, it remains unclear whether PBMT ameliorates glucose metabolism in skeletal muscle in type 2 diabetes models. Here we showed that PBMT reduced blood glucose and insulin resistance, and reversed metabolic abnormalities in skeletal muscle in two diabetic mouse models. PBMT accelerated adenosine triphosphate (ATP) and reactive oxygen species (ROS) generation by elevating cytochrome c oxidase (C c O) activity. ROS-induced activation of phosphatase and tensin homolog (PTEN)/ protein kinase B (AKT) signaling after PBMT promoted glucose transporter GLUT4 translocation and glycogen synthase (GS) activation, accelerating glucose uptake and glycogen synthesis in skeletal muscle. C c O subunit III deficiency, ROS elimination, and AKT inhibition suppressed the PBMT effects of glucose metabolism in skeletal muscle. This study indicated amelioration of glucose metabolism after PBMT in diabetic mouse models and revealed the metabolic regulatory effects and mechanisms of PBMT on skeletal muscle.
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高影响因子
BIOMATERIALS
·
2021
·
IF 12.479
Rui Chen,Chenqi Zhu,Liu Xu,Yi Gu,Shujing Ren,Hua Bai,Qin Zhou,Xin Liu,Shengfeng Lu,Xiaolin Bi,Weidong Li,Xiaobin Jia,Zhipeng Chen
Drug-loaded hydrogels can improve blood supply and inhibit extracellular matrix degradation after myocardial infarction. However, due to the continual dynamic motion of cardiac tissue , the hydrogel structure cannot be reconstructed in time, causing accelerated degradation and drug burst release. Here, a novel, superior, self-healing elastin-mimic peptide hydrogel (EMH) was fabricated for the local delivery of salvianolic acid B (SaB). The self-healing ability of EMH is enhanced by SaB-loaded polydopamine nanoparticles (SaB-PDA). In vitro, the pre-hydrogel (SaB-PDA/pre-EMH) is endowed with excellent biocompatibility and a low viscosity, making it suitable for intramyocardial injection. Once injected into the myocardial infarction (MI) region, SaB-PDA/pre-EMH can form SaB-PDA/EMH with great mechanical strength under the action of upregulated transglutaminase (TGase) in heart tissue post-MI. The superior self-healing ability of SaB-PDA/EMH allows for an increase in retention time in the beating ventricular wall. Therefore, with long-term release of SaB, SaB-PDA/EMH can inhibit ventricular remodeling and promote angiogenesis for MI treatment.
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高影响因子
PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS
·
2012
·Vol. 81
·期 4
·613-621
·
IF 3.392
Biao Cheng,Hao Gong,Xiaochao Li,Yue Sun,Hong Chen,Xin Zhang,Qian Wu,Ling Zheng,Kun Huang
The misfolding of human islet amyloid polypeptide (hIAPP) is regarded as one of the causative factors of type 2 diabetes mellitus (T2DM). Salvia miltiorrhiza (Danshen), one of the most commonly used of traditional Chinese medicines, is often used in Compound Recipes for treating diabetes, however with unclear mechanisms. Since salvianolic acid B (SalB) is the most abundant bioactive ingredient of salvia miltiorrhiza water-extract. In this study, we tested whether SalB has any effect on the amyloidogenicity of hIAPP. Our results clearly suggest that SalB can significantly inhibit the formation of hIAPP amyloid and disaggregate hIAPP fibrils. Furthermore, photo-crosslinking based oligomerization studies suggest SalB significantly suppresses the toxic oligomerization of hIAPP monomers. Cytotoxicity protection effects on pancreatic INS-1 cells by SalB were also observed using MTT-based assays, potentially due to the inhibition on the membrane disruption effects and attenuated mitochondria impairment induced by hIAPP. These results provide evidence that SalB may further be studied on the possible pharmacological treatment for T2DM. Proteins 2013. © 2012 Wiley Periodicals, Inc.
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高影响因子
JOURNAL OF POWER SOURCES
·
2022
·
IF 9.794
Yang Tao,Qing Liu,Yujiao Guo,Mingwu Xiang,Xiaofang Liu,Wei Bai,Junming Guo,Shulei Chou
Electrochemical properties of spinel LiMn 2 O 4 cathode material have been always suffered from Mn dissolution and Jahn-Teller distortion. Herein, various Ni/B dual-doped LiNi 0.08 B x Mn 1.92- x O 4 ( x = 0–0.15) with a truncated octahedral morphology are synthesized via a facile solid-state combustion. The effects of Ni/B co-doping on the morphology, crystal structure, Mn dissolution, Li + diffusion coefficient and activation energy are investigated. Due to the relatively high Ni–O and B–O bond energy than that of Mn–O bond, the structure stability of the LiMn 2 O 4 is enhanced, whilst restraining the Jahn-Teller distortion. The LiNi 0.08 Mn 1.92 O 4 shows (111), (110) and (100) facets. In comparison, the B-doping endows the LiNi 0.08 B x Mn 1.92- x O 4 ( x ≥ 0.02) with (111) and (100) facets. This morphology evolution without (110) facets effectively inhibits the Mn dissolution. Owing to the synergistic merits of Ni/B dual-doping and unique truncated octahedron , the optimized LiNi 0.08 B 0.06 Mn 1.86 O 4 delivers an initial discharge capacity of 113.9 mAh∙g −1 at 1C and maintains a durable cycling life up to 2000 cycles at 5C. Even at 20C, a capacity retention of 86.3% is still obtained after 2000 cycles. Furthermore, a capacity retention of 70.6% can be retained after 500 cycles at 5C and 55 °C. The truncated octahedral LiNi 0.08 B x Mn 1.92- x O 4 with excellent electrochemical performance will be a good candidate for developing long-life lithium-ion batteries.
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高影响因子
JOURNAL OF PHYSICS AND CHEMISTRY OF SOLIDS
·
2019
·
IF 2.752
Wen Cui,Xiaoli Kang,Xiaoying Zhang,Xudong Cui
A highly efficient Rhodamine B (RhB) adsorbent based on a gel-like ZnO/Zr-metal-organic framework (ZnO/Zr-MOF) composite was prepared by reacting ZnO nanoparticles with glacial-acetic-acid-modulated Zr-MOF(bpy) via a sample solvothermal method. Introduction of ZnO greatly improved the texture properties of the parent Zr-MOF(bpy), and the resulting material exhibited an agglomerate morphology consisting of numerous quadrate nanoparticles, which is quite different from the cubo-polyhedron morphology of Zr-MOF(bpy). In this way, this composite showed a considerable RhB absorption capacity from aqueous solution in a wide pH range. The adsorption kinetics , isotherms and thermodynamics of the RhB adsorption by ZnO/Zr-MOF(bpy) were discussed and confirmed that this adsorption process satisfied pseudo-second-order kinetics and the Langmuir model, and was a spontaneous exothermic process. Moreover, the excellent adsorption performance is likely related to the synergism of hydrogen bonding , electrostatic interactions and π–π interactions between the ZnO/Zr-MOF(bpy) nanocomposite and RhB. The excellent texture properties of ZnO/Zr-MOF(bpy) promote the adsorption and diffusion of RhB on it, which is also crucial during the adsorption process.
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高影响因子
CHINESE JOURNAL OF CHEMICAL ENGINEERING
·
2015
·
IF 1.098
Jianguo Yang,Shuo Liu,Huanan Hu,Shibin Ren,Anguo Ying
A simple and efficient method is proposed for the synthesis of tetrahydrobenzo[b]pyrans with aromatic aldehydes, active methylene compounds, and dimedone using basic ionic liquid catalyst in water. The procedure offers several advantages including short reaction time, good yield, easy procedure, and good recyclability of catalysts, which may be a practical alternative to conventional processes for preparation of 4-hpyrans.
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高影响因子
HELVETICA CHIMICA ACTA
·
2012
·Vol. 95
·期 2
·320-326
·
IF 1.478
Lianbao Ye,Yuanxin Tian,Zhonghuang Li,Jiajie Zhang,Shuguang Wu
Since deregulation of the tyrosine-kinase receptor c-Met is implicated in several human cancers and is an attractive target for small-molecule-drug discovery, we report herein the synthesis of 2,3,4,5-tetrahydro-8-[1-(quinolin-6-ylmethyl)-1 H -1,2,3-triazolo[4,5- b ]pyrazin-6-yl]-1 H -pyrido[4,3- b ]indoles 4a – 4c and 2,3,4,5-tetrahydro-8-[3-(quinolin-6-ylmethyl)-1,2,4-triazolo[4,3- b ]pyridazin-6-yl]-1 H -pyrido[4,3-b]indoles 5a – 5c . These indole derivatives demonstrated inhibition of c-Met kinase activity. Concurrently, five key intermediates were synthesized. These compounds could be prepared in good yields.
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高影响因子
MICROCHEMICAL JOURNAL
·
2020
·
IF 3.594
Bokai Ma,Fujian Xu,Mian He,Yuqing Lin,Guanghui Hu,Mei Zhang,Xinying Zhao,Weili Liu
Rhodamine B hydrazide (RBH) was prepared as a new derivatizing reagent for residual formaldehyde in a drug such as N-butyl-2-cyanoacrylate (NBCA). RBH reacted with formaldehyde rapidly at room temperature, and the resulting derivative can be detected sensitively at 238 nm. After optimizing the derivatization and chromatographic separation conditions, RBH as a pre-column derivatizing reagent has been successfully used for the analysis of formaldehyde in real NBCA samples by high-performance liquid chromatography (HPLC). The detection limit of the method is 0.004 μg/mL for formaldehyde, and the recovery is 94.0%-96.6%. Most notably, compared with the previous HPLC methods, the developed method has the advantages of mild derivatization temperature, short derivatization time and high sensitivity.
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高影响因子
Journal of Energy Chemistry
·
2022
·
IF 13.599
Yang Ding,Soumyajit Maitra,Chunhua Wang,Runtian Zheng,Meiyu Zhang,Tarek Barakat,Subhasis Roy,Jing Liu,Yu Li,Tawfique Hasan,Bao-Lian Su
Graphitic carbon nitride (g-C 3 N 4 ) has attracted great interest in photocatalysis and photoelectrocatalysis. However, their poor hydrophilicity poses a great challenge for their applications in aqueous environment . Here, we demonstrate synthesis of a hydrophilic bi-functional hierarchical architecture by the assembly of B-doped g-C 3 N 4 nanoplatelets . Such hierarchical B-doped g-C 3 N 4 material enables full utilization of their highly enhanced visible light absorption and photogenerated carrier separation in aqueous medium , leading to an excellent photocatalytic H 2 O 2 production rate of 4240.3 μM g −1 h −1 , 2.84, 2.64 and 2.13 times higher than that of the bulk g-C 3 N 4 , g-C 3 N 4 nanoplatelets and bulk B doped g-C 3 N 4 , respectively. Photoanodes based on these hierarchical architectures can generate an unprecedented photocurrent density of 1.72 mA cm −2 at 1.23 V under AM 1.5 G illumination for photoelectrochemical water splitting. This work makes a fundamental improvement towards large-scale exploitation of highly active, hydrophilic and stable metal-free g-C 3 N 4 photocatalysts for various practical applications.
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高影响因子
MOLECULES
·
2018
·Vol. 23
·期 12
·3083
·
IF 3.098
Xiaojian Ouyang,Xican Li,Wenbiao Lu,Xiaojun Zhao,Dongfeng Chen
To clarify the role of theB-ring in antioxidant flavonols, we performed a comparative study between galangin with a nullB-ring and 3,5,7-trihydroxychromone without aB-ring using five spectrophotometric assays, namely,•O2−-scavenging, 1,1-diphenyl-2-picrylhydrazyl radical (DPPH•)-scavenging, 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide radical-scavenging, 2,2′-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) radical-scavenging, and Fe3+-reducing activity. The DPPH•-scavenging reaction products of these assays were further analyzed by ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC-ESI-Q-TOF-MS/MS) technology. In the five spectrophotometric assays, galangin and 3,5,7-trihydroxychromone dose-dependently increased their radical-scavenging (or Fe3+-reducing) percentages. However, galangin always gave lower IC50values than those of 3,5,7-trihydroxychromone. In the UPLC-ESI-Q-TOF-MS/MS analysis, galangin yielded galangin-DPPH adduct MS peaks (m/z662, 434, 301, 227,196, and 151) and galangin-galangin dimer MS peaks (m/z538, 385, 268, 239, 211, 195, and 151). 3,5,7-Trihydroxychromone, however, only generatedm/z3,5,7-trihydroxychromone-DPPH adduct MS peaks (m/z586, 539, 227, 196, and 136). In conclusion, both galangin and 3,5,7-trihydroxychromone could similarly undergo multiple antioxidant pathways, including redox-dependent pathways (such as electron transfer (ET) and ETplusproton transfer (PT)) and a non-redox-dependent radical adduct formation (RAF) pathway; thus, the nullB-ring could hardly change their antioxidant pathways. However, it did improve their antioxidant levels in these pathways. Such improvement of theB-ring toward an antioxidant flavonol is associated with its π-π conjugation, which can provide more resonance forms and bonding sites.Keywords:antioxidant;galangin;3,5,7-trihydroxychromone;flavonol;structure–activity;B-ring
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高影响因子
JOURNAL OF POWER SOURCES
·
2016
·
IF 6.333
Xing Qian,Rucai Yan,Chong Xu,Li Shao,Hongmei Li,Linxi Hou
A new series of organic dyes based on indeno[1,2- b ]indole have been synthesized and applied in dye-sensitized solar cells (DSSCs) for the first time. These four dyes QX11 – 14 are constructed to a D–π–A type structure consisting of an indeno[1,2- b ]indole donor and a cyanoacrylic acid acceptor/anchoring group. Different π-bridges (thiophene and furan) and different alkyl groups (ethyl and hexyl) are involved to tune the photoelectric properties . Their optical, electrochemical, and photovoltaic properties, as well as the density functional theory calculations have been systematically investigated, indicating these four dyes are all capable as photosensitizers . The four dyes all show good DSSC performances and a highest power conversion efficiency up to 7.64% with a J sc of 15.8 mA cm −2 and a V oc of 763 mV has been achieved by the dye QX12 with a furan π-bridge and a pair of ethyl groups, which reaches 95% of the commercial N719 dye (8.07%) under AM 1.5G illumination. This result reveals indeno[1,2- b ]indole is a promising electron donor to construct efficient organic dyes for DSSCs.
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