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1. NGF contribute to acid-induced articular chondrocytes apoptosis by modulating ASIC1a/NLRP1/Caspase-1 signaling axis | |||
HU Wei | |||
Pharmacy 14 May 2018 | |||
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Abstract:Objective: Nerve growth factor (NGF) is key regulators in the pathogenesis of the rheumatoid arthritis (RA) diseases. However, the potential role of NGF in RA remains unclear. It has been shown that ASIC1a is an extracellular pH sensor in articular chondrocytes and RA. Moreover, NGF modulates the expression of ASICs in sensory neurons sensitization. In this study, we examined whether NGF contribute to ASIC1a expression could affect acid-induced apoptotic injury to articular chondrocytes. Methods: The primary rat articular chondrocytes were isolated from Sprague-Dawley rats. Apoptosis of chondrocytes was observed by the terminal deoxyribonucleotidyl transferase- mediated dUTP nick-end labeling method as well as propidium iodide labeling methods. Treatment of articular chondrocytes with NGF, ASIC1a-siRNA and acid, the expression levels of NGF, ASIC1a, NLRP1 and Caspase-1 were examined by qRT-PCR and western blotting, respectively. Results: We found that up-regulation of ASIC1a in acid-induced articular chondrocytes is associated with NGF treatment. Knockdown of ASIC1a inhibited NLRP-1 expression in acid-induced articular chondrocytes. Knockdown of ASIC1a suppressed acid-induced articular chondrocytes apoptosis. Moreover, we investigated the effect of ASIC1a on NLRP1/Caspase-1 pathway. Our results demonstrated that NGF contribute to acid-induced articular chondrocytes apoptosis by modulating ASIC1a/NLRP1/Caspase-1 signaling axis. Conclusion: Taken together, these results indicated that NGF promotes acid-induced articular chondrocytes apoptosis by up-regulation of ASIC1a/NLRP1/Caspase-1 signaling axis. | |||
TO cite this article:HU Wei. NGF contribute to acid-induced articular chondrocytes apoptosis by modulating ASIC1a/NLRP1/Caspase-1 signaling axis[OL].[14 May 2018] http://en.paper.edu.cn/en_releasepaper/content/4745087 |
2. Discovery of quercetin derivatives as metal ions chelators with potent anti-HCV activities | |||
ZHONG Dongwei,LIU Mingming,CAO Yang,ZHOU Lu,YE Deyong | |||
Pharmacy 08 May 2017 | |||
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Abstract:The α,γ-diketoacid (DKA) analogues or isosteres show potent inhibition of hepatitis C virus (HCV) NS5B polymerase through chelation of the two magnesium ions at the active site. The anti-HCV activity of flavonoid quercetin (2) could partly be attributed to its structural mimic of DKAs. In order to delineate the structural features required for the inhibitory effect and improve the anti-HCV potency, two novel quercetin analogues, 7-O-arylmethyl quercetin and quercetin-3-O-benzoic acid-ester, were designed, synthesized and evaluated for their anti-HCV properties in cell-based assays. Among the 38 newly synthesized compounds, 7-O-substituted derivative 3i and 3-O-substituted derivative 4f were found to be the most active in corresponding series (EC50 = 3.8 μM and 9.0 μΜ, respectively). Docking studies suggested that the quercetin analogues are capable of establishing key coordination with the two magnesium ions as well as interactions with residues at the active site of HCV NS5B. | |||
TO cite this article:ZHONG Dongwei,LIU Mingming,CAO Yang, et al. Discovery of quercetin derivatives as metal ions chelators with potent anti-HCV activities[OL].[ 8 May 2017] http://en.paper.edu.cn/en_releasepaper/content/4730625 |
3. Tetrazole and triazole as bioisosteres of carboxylic acid: discovery of diketo tetrazoles and diketo triazoles as anti-HCV agents | |||
SONG Wuhui,LIU Mingming,ZHONG Dongwei,YE Deyong,ZHOU Lu,YUAN Zhenghong | |||
Pharmacy 28 April 2017 | |||
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Abstract:In this paper, a series of diketo tetrazoles and diketo triazoles were designed and synthesized as bioisosteres of α, γ-diketo acid, the active site inhibitor of HCV (Hepatitis C virus) polymerase NS5B. Among the synthesized compounds, 4-(4-fluorobenzyloxy)phenyl diketo triazole (30) exhibited anti-HCV activity with an EC50 value of 3.9 μM and an SI value more than 128. The reduction of viral protein and mRNA levels were also validated, supportingthe anti-HCV activity of compound 30. These results provide convincing evidence that the diketo tetrazoles and diketo triazoles can be developed as bioisosteres of α,γ-diketo acid to exhibit potent inhibitory activity against HCV. | |||
TO cite this article:SONG Wuhui,LIU Mingming,ZHONG Dongwei, et al. Tetrazole and triazole as bioisosteres of carboxylic acid: discovery of diketo tetrazoles and diketo triazoles as anti-HCV agents[OL].[28 April 2017] http://en.paper.edu.cn/en_releasepaper/content/4730608 |
4. Acid-sensing ion channel 1a regulates matrix metabolism of rat | |||
weihu,Cheng Sun,shiming wang | |||
Pharmacy 25 April 2017 | |||
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Abstract:Objectives: ASIC1a has a wide range of biological functions, plays an important role in cell metabolic activity, Our research has shown that extracellular pH plays an important role in matrix synthesis and metabolism in articular chondrocytes by activated ASIC1a. However, little is kown about the underlying mechanism of ASIC1a on matrix synthesis and metabolism in articular chondrocytes. The present study was undertaken to investigate the mechanism of ASIC1a on matrix synthesis and metabolism in articular chondrocytes by acidosis. Down-regulation of GAG, HYP, MMP-2, MMP-9, TIMP-1 and TIMP-2 mRNA expression and production was abolished by inhibit acidosis- elicited increase in intracellular Ca2+ concentration. Pretreatment with BAPTA-AM (Ca2+ chelator) abolished acidosis induced ERK1/2, p38 MAPK, c-jun and c-fos activation. PD98059 (ERK1/2 inhibitor) attenuate c-jun activation and restored GAG, HYP, TIMP-1 and TIMP-2 mRNA expression and production. SB203580 (p38 MAPK inhibitor) inhibit c-fos activation and restored MMP-2 and MMP-9 mRNA expression and production. We founded that bolcking ASIC1a inhibit the effect of extracellular acidosis on GAG, HYP, MMP-2, MMP-9, TIMP-1 and TIMP-2 mRNA expression and production in articular chondrocytes. Taken together, our data indicate that blocking acid-sensing ion channel 1a inhibit abberant matrix synthesis and metabolism from acid-induced articular chondrocytes via Ca2+-mediated activation of p38 MAPK/c-jun and ERK/c-fos pathway. | |||
TO cite this article:weihu,Cheng Sun,shiming wang. Acid-sensing ion channel 1a regulates matrix metabolism of rat[OL].[25 April 2017] http://en.paper.edu.cn/en_releasepaper/content/4727034 |
5. Pharmacokinetics of membrane-moderated granulated pellet-containing tablets in beagles | |||
LI Lu,LIN Shiqi,HUANG Ying,ZHU Chune,QUAN Guilan,PAN Xin,WU Chuanbin | |||
Pharmacy 21 May 2016 | |||
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Abstract:Granulated pellet-containing tablets (GPCT) were prepared via a novel granulation technique, which laid the excipients on coated pellets and then compressed into GCPT after mixing with the cushioning fillers. The pharmacokinetics of doxycycline hydrochloride GPCT were evaluated to confirm the integrity of the coating film after compaction, with the coated pellets as a reference, containing equivalent doxycycline hydrochloride in the two formulations. The study was performed on six healthy beagles by a randomized-sequence, open-label, single-dose, two-period, crossover design with a 2-week washout period. Blood samples were collected and analyzed to calculate several pharmacokinetics parameters. The mean maximum plasma concentration (Cmax) for the test formulation and reference formulation were 2.73±0.22 mg/L and 2.94±0.47 mg/L, the mean time to reach Cmax (Tmax) were 6.67±0.47 h and 6.33±0.42 h, the AUC0-t were 68.42±6.94 mgoh/L and 72.87±12.51 mgoh/L, and the mean residence time (MRT) were 15.62±0.53 h and 15.26±0.79 h respectively. The pharmacokinetics analysis suggested that there was no significant difference regarding drug release properties, and the granulated pellet-containing tablets met the regulatory criteria for bioequivalence to the reference formulation of coated pellets in the healthy fasting beagles, from which the novel granulation technique might be proposed as an effective approach to prepare pellet-containing tablets without compromising the integrity of coating films. | |||
TO cite this article:LI Lu,LIN Shiqi,HUANG Ying, et al. Pharmacokinetics of membrane-moderated granulated pellet-containing tablets in beagles[OL].[21 May 2016] http://en.paper.edu.cn/en_releasepaper/content/4693621 |
6. Cardioprotective effects of a novel hydrogen sulfide donor in diabetes mellitus rat models with acute myocardial infarction | |||
Wei Guo,Zhijun Wang,Yizhun Zhu | |||
Pharmacy 10 May 2016 | |||
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Abstract:Although many studies have been performed to elucidate the molecular mechanisms of heart failure, an effective pharmacological therapy to protect cardiac tissues from severe loss of contractile function associated with heart failure after acute Myocardial Infarction(MI)has yet to be developed. We examined the cardioprotective effects of S-Propargyl-L-cysteine (SPRC, also named as ZYZ-802), a novel hydrogen sulfide donor with potent antioxidant and anti-apoptotic activities in diabetes mellitus (DM) rat models of heart failure.SPRC was systemically delivered to rats 7 days before MI and 6 weeks after MI at different doses (15, 30, 60mg/kg). Cardiac function was assessed by hemodynamic measurements. The expression of proinflammatory cytokines, apoptosis-related molecules and the markers of adverse ventricular remodeling were measured using RT-PCR and Western blot. Treatment with SPRC significantly improved cardiac function, in particular by increasing dP/dt. Simultaneously, the expression of the pro-inflammatory cytokines TNF-α and IL-1 was markedly reduced in the treatment group compared with the MI group. In addition, SPRC-treated tissues displayed decreased expression of Bax, caspase-3, and caspase-9 and increased expression of Bcl-2, which was in part due to the promotion of Akt phosphorylation. These data demonstrated that SPRC possesses potent cardioprotective effects against cardiac injury in DM rat modelsof heart failure, which is mediated, at least in part, by suppression of the inflammatory and cell apoptosis responses. | |||
TO cite this article:Wei Guo,Zhijun Wang,Yizhun Zhu. Cardioprotective effects of a novel hydrogen sulfide donor in diabetes mellitus rat models with acute myocardial infarction[OL].[10 May 2016] http://en.paper.edu.cn/en_releasepaper/content/4687929 |
7. The treatment effect of igf-1 rice capsule in mice with T1DM and T2DM and the relationship with its dosage | |||
ZHOU Yi,XIAO Yuling | |||
Pharmacy 29 February 2016 | |||
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Abstract:In the previous study,some high expression transgenic igf-1 rice was got and its treatment on diabetic mice had been tested. In order to improve the bioavailability of igf-1 and protect from being decomposed by the digestive enzyme, the rice power had been grinded into power and made into enteric capsule. The best recipe had been tested. Through the enzyme-linked immunosorbent assay (ELISA), the igf-1 content of the rice and the capsule were determined as well as the release rate of the capsule. Type 1 diabetes model and Type 2 diabetes model had been made to inspect the effects that igf-1 capsule has on diabetic mice. The main test contained the weight effect, water intake effect and the glucose effect of igf-1 in different dosage(1mg/g,0.5mg/g and 0.25mg/g). In this study, igf-1 had showed a better effect on mice with T2DM than T1DM,and the treatment effect was closely related with the doasge. | |||
TO cite this article:ZHOU Yi,XIAO Yuling. The treatment effect of igf-1 rice capsule in mice with T1DM and T2DM and the relationship with its dosage[OL].[29 February 2016] http://en.paper.edu.cn/en_releasepaper/content/4679229 |
8. Preparation, characterization and antitumor activity of six polysaccharides isolated from natural sources | |||
CEN Yihong,WU Huaping,YAN Xiaorong,Qi Wenwen,GUO Hui,WANG Xiaoqian,XIAO Yuling | |||
Pharmacy 24 February 2016 | |||
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Abstract:The carboxymethylated derivatives of six kinds of polysaccharides isolated from natural Angelica sinensis, Lentinus edodes, Ganoderma lucidum, Poria cocos, Astragalus membranaceus and Maitake were synthesized and characterized. In vitro anti-tumor activity results showed that derivatives of the six polysaccharides showed more effective anti-tumor activities than their original polysaccharides. Also, their water solubility was highly improved. Moreover, Angelica sinensis which showed the best antitumor effect were carboxymethylated with five different degree of carboxymethylation substitution in order to study the correlations between the antitumor activity, the water solubility and the degree of substitution (DS) of the polysaccharide. Experimental results showed that the water solubility of the carboxymethylated derivatives of Angelica sinensis (CASP) was highly improved with increasing of DS. However, the anti-tumor activity was not just enhanced with the increasing of water solubility. A relatively moderate DS (0.187) was found to have the best anti-tumor activities of CASP. Therefore, it can be concluded that carboxymethylation of polysaccharides can effectively enhance their water solubility and in vitro anti-tumor activity. | |||
TO cite this article:CEN Yihong,WU Huaping,YAN Xiaorong, et al. Preparation, characterization and antitumor activity of six polysaccharides isolated from natural sources[OL].[24 February 2016] http://en.paper.edu.cn/en_releasepaper/content/4678512 |
9. The synthesis and biological evaluation of Targeted Peptide conjugate of phthalocyanine | |||
Zhangyong Hong,Zhixiong Zeng,Fu Li | |||
Pharmacy 25 December 2015 | |||
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Abstract:In recent decades, photodynamic therapy has been rapid developed. In the process of photodynamic therapy, photosensitizer plays a vital role. Here we reported our synthestic studies and activitiy test of two new peptide conjugates zinc phthalocyanine photosensitizers for targeted cancer ohotodynamic therapy, Synthesis asymmetric phthalocyanine PCZN2 by introducing glycol structure and asymmetric phthalocyanine PCZN5 by introducing a hydrophilic group hydroxyl. By introducing hydrophilic functional groups, it can greatly increase the solubility of phthalocyanine. The two highly soluble phthalocyanine PCZN2 and phthalocyanine PCZN5By were conjugated to EGFR targeting peptide D4 on resin through solid phase synthesis, which solve the problem of separation and purification about phthalocyanine coupled. Optical experiments show the product has a high quantum yield and singlet oxygen yield. The maximum absorption wavelength is at 685nm with good penetration depth. Cytotoxicity test (MTT) showed targeting peptide conjugate phthalocyanine PCZN3 and PCZN6 are toxic selectively to tumor cells. Confocal microscopic experiments showsed they are able to be selectively recognized by tumor cells. In vivo imaging show both materials PCZN3 and PCZN6 are able to concentrate in tumors in mice with strong targeting. These new targeting photosensitizers show good potential for cancer photodynamic therapy. | |||
TO cite this article:Zhangyong Hong,Zhixiong Zeng,Fu Li. The synthesis and biological evaluation of Targeted Peptide conjugate of phthalocyanine[OL].[25 December 2015] http://en.paper.edu.cn/en_releasepaper/content/4669782 |
10. Fluorescent carbon dots derived from lactose for assaying folic acid | |||
CHEN Zhangbao,WANG Jing,MIAO Hong,WANG Lan,YANG Xiaoming | |||
Pharmacy 01 December 2015 | |||
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Abstract:The fluorescent carbon dots were successfully synthesized by simply heating the mixture of lactose and NaOH solution. The as-synthesized carbon dots had been systematically characterized by fluorescence, FTIR, HR-TEM and 13C-NMR. Since the fluorescence of the carbon dots were efficiently quenched by folic acid, the carbon dots were employed as selective fluorescence probes for detecting of folic acid, depending on the formation of hydrogen bond among the functional group of folic acid (-OH, -COOH and -NH2) and -OH and -COOH of the carbon dots. Moreover, the decrease of fluorescence intensity was capable of detecting folic acid in a linear range of 6×10-5 mol/L-8×10-8mol/L with a detection limit of 1.2×10-9 mol/L at a signal-to-noise ratio of 3, suggesting a promising assay for folic acid. Significantly, the practicability of this fluorescence probe to assay folic acid in human urine samples was further evaluated. | |||
TO cite this article:CHEN Zhangbao,WANG Jing,MIAO Hong, et al. Fluorescent carbon dots derived from lactose for assaying folic acid[OL].[ 1 December 2015] http://en.paper.edu.cn/en_releasepaper/content/4667768 |
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