ABSTRACT
AIM: To observe the anti-inflammatory effect of CQMUH-011 and to explore its mechanism.METHODS: Three kinds of animal models, mouse ear swelling induced by xylene, rat granuloma induced by cotton ball and rat rheumatoid arthritis induced by Freund's complete adjuvant, were established to study the anti-inflammatory effect of CQMUH-011.The ear swelling degree, dry weight of cotton ball granuloma, arthritis index, paw swelling and ankle joint pathological changes were measured to reflect the severity of inflammation.The anti-inflammatory mechanisms of CQMUH-011 were investigated by detecting the serum levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) by ELISA.Malondialdehyde (MDA), myeloperoxidase (MPO) and nitric oxide (NO) were determined by corresponding kits.RESULTS: Treatment with CQMUH-011 significantly decreased TNF-α, IL-6 and NO concentrations, MDA contents and MPO activity in the serum.Meanwhile, Ear swelling degree, dry weight of cotton ball granuloma, arthritis index, paw swelling and ankle joint pathological damage were attenuated.CONCLUSION: CQMUH-011 has an anti-inflammatory effect, which may be related to inhibiting the production of inflammatory factors and attenuating lipid peroxidation.
ABSTRACT
Saxagliptin,a novel antihyperglycemic agent belonging to dipeptidyl peptidase-4(DPP-4)inhibitor,was devel?oped by Bristol-Myers Squibb and AstraZeneca. It has the merit of obvious hypoglycemic activity,less side effect,good treatment com?pliance and remarkably high safety,and is widely applied to treatment of type 2 diabetes. In this paper,we review the synthetic meth?ods of the key intermediate(S)-N-Boc-3-hydroxyadamantylglycine(compound 3)as well as its two important compounds 3-hydroxy-1-acetyladamantane(1)and 2-(3-hydroxy-1-adamant-yl)-2-oxoacetic acid(2)and briefly discuss their advantages and disadvantages.
ABSTRACT
Pimavanserin(Nuplazid) is a drug of selective targeting 5-HT2A receptor,developed by Acadia Pharmaceuticals. In April 29,2016,it was approved by FDA for the treatment of Parkinson′s disease(PD)patients experiencing mental symptoms such as hallucinations and delusions. In this paper,we summarize the synthetic methods of pimavanserin published in literature in re?cent years and their advantages and disadvantages.
ABSTRACT
Objective To study the molecular epidemiology of C.albicans isolates in infectious disease patients and to explore biofilm phenotypic characterization responsible for biofilm formation in clinical strains.Methods A total of 104 hospital-acquired C.alibcans clinical isolates collected from sterile sites and mucosal lesions of 92 infectious disease patients ( viral hepatitis, tuberculosis and AIDS) in Shanghai Public Health Clinical Center were analyzed.MLST analysis was performed to identify their phylogenetic status.The capability of biofilm formation was measured by [2,3-bis-(2-methoxy-4-nitro-5-sulphenyl)-2H-tetrazolium-5-carboxanilide] XTT assay.The results were compared using Kruskal-Wallis test.Results MLST analysis identified 63 DSTs with a decentralized phylogeny among 104 C.albicans isolates, of which 41 DSTs (65.1%) had not been reported in the online MLST database.The Single Locus Sequence Query from the C.albicans database identified new alleles.MEGA6 analysis of the MLST data assigned the 104 isolates within 14 of the 18 known clades; among them the clade 1 contained the greatest proportion of isolates (26.9%).Of the 43 novel DSTs isolates, 37 ( 86.0%) clustered within 11 of the 18 known clades.16 high biofilm formers were found from a total of 104 clinical isolates.The biofilm formation capabilities differed in strains isolated from different anatomical sites (H =18.23,P=0.0326).Biofilm formation by blood-originated isolates was lower than that of catheter-originated isolates ( Z=-72.20,P<0.001).Genotypes also affected the biofilm formation capability of the C.albicans isolates (H=10.01,P=0.0185).Conclusions A high level of diversity within C.albicans isolates.Microevlution clearly influences C.albicans genetic alterations upon environmental selection.The site of isolation and genotype associates with the biofilm formation capability.
ABSTRACT
ObjectiveTo analyze the characterstics of phenotype and genotype of multidrug resistant tuberculosis (MDR-TB) and extensively drug resistant tuberculosis (XDR-TB) by molecular line probe assay and liquid culture with MGIT960.MethodsGenoType MTBDR Kits were used for identifying the types of the first-line and second-line antituberculosis drug resistant genes partly and BD MGIT960 was used for detecting the chug susceptibility.Results( 1 ) Out of 94 MDR-TB strains,the rate of drug resistant to EMB,AMK,OFX and MFX by BD MGIT960 assay were 36.2%,17.0%,54.3% and 55.3%,respectively.Among these isolates,13 were extensively drug resistant tuberculosis (XDR-TB).(2) Compared with MGIT960,the concordance rate of GenoType MTBDRplus was 86.2% and 95.7% respectively.Taking MGIT960 results as reference,the sensitivity of GenoType MTBDRsl detecting the susceptibility of EMB,AMK,OFX and MFX to 94 isolates were 47.1%,81.3%,94.1%,94.2%,respectively.The specificity were 75.0%,98.7%,90.7%,92.9%,respectively.(3) Among the rpoB mutation categories,S531L accounts for most.MTB resistant to IFN caused by the mutation of katG chiefly and the S315T1 was in the majority.The gyrA mutation sites located at the ninety-fourth codon most.Out of 94 strains,23 were mixed with 2 kindsof Mycobacterium tuberculosis at least and 7 were undetectable mutations.Conclusion Among the M/XDR-TB,the strains resistant to INH,RFP,AMK,OFX and MFX were caused most by the mutation of katG,rpoB,rrs and gyrA,respectively.The relationship between EMB and embB was not so clear relatively.As a fast detecting drug susceptibility test kit,GenoType MTBDR possess good sensitivity and specificity.So,it could be as an assistant method to guide the therapy on clinic.
ABSTRACT
Through the research training of undergraduate students of pharmacy utilizing medicinal chemistry research platform, not only the undergraduate teaching can be facilitated, but also the creative ability, communications skills, ability to work independently and team spirit of students can be developed,which will be helpful to cultivating high quality pharmacy talents, so as to meet the requirement of today's pharmaceutical companies and research institutes.
ABSTRACT
This article summarizes some methods in teaching physical chemistry,such as inspiring students’ interests and improving teacher’s teaching level. Then,how to enhance the teaching quality of physical chemistry is discussed.
ABSTRACT
The authors have made an investigation on the conditions of the internet access,the platform for network-aided teaching,the teaching resource and the teaching effect for physical chemistry among 127 pharmacy students of 2008 enrollment.Based on the results of the investigation,an analysis on the current situation and problems of network-aided teaching for this course was performed and recommendations were put forward accordingly.
ABSTRACT
Objective To determine the affinities of five oligopeptides specifically binding with DNA binding domain of NF-?B p65 subunit and identify their inhibiting effect on DNA binding activity of NF-?B. Methods By using biosensor the affinities were measured by means of kinetic analysis, and the inhibiting effects were determined by competitive ELISA. Results The results of biosensor showed that all of five oligopeptides really possessed the capability of specific interacting with NF-?B p65 subunit. The affinity constants of these oligopeptides were 2.67?10~ -7 mol/L, 9.02?10~ -6 mol/L, 1.07?10~ -6 mol/L, 8.03?10~ -6 mol/L, 9.83?10~ -7 mol/L respectively. The results of competitive ELISA indicated that five oligopeptides could inhibit NF-?B from binding with ?B motif, and their inhibiting effect depended on their concentration. Conclusion Five oligopeptides that were screened by yeast two-hybrid system method can really interact with p65, and possess the inhibiting effect on DNA binding activity of NF-?B. So it will be possible that these oligopeptides are regarded as model to design and develop novel anti-inflammatory peptide drug targeting NF-?B.
ABSTRACT
OBJECTIVE:To determine the oil-water partition coefficients (logP) of rosiglitazone at different pH values by two kinds of methods.METHODS:A shake flask-ultraviolet spectrophotometry method was used to determine plasma concentration of rosiglitazone in water phase and organic phase at variable pH values (0.95,2.0,3.0,4.0,5.07,5.7,6.55,7.06,7.5,8.15,9.21) to calculate logP by using with n-caprylic alcohol-water as simulation system.Above logP values were compared with that calculated by Pallas software.RESULTS:The logP value was lower than 1 when pH value was lower than 4;the logP value was higher than 1 when pH value was ranged from 5 to 9.Measured logP values were in good agreement with that calculated by Pallas software.CONCLUSION:Rosiglitazone exists in the form of hydrochloride salt with good water solubility (pH
ABSTRACT
OBJECTIVE:To establish a method for determination of ionization equilibrium constant of sildenafil using ultraviolet spectrophotometry.METHODS:Methanol solutions of sildenafil with pH values of 2.26,8.56,9.31,9.83 and 12.38 were respectively scanned at the wavelength within the range of 200nm～400nm.The absorbability and pKa value of sildenafil were determined at the selected wavelength of 280,287,290,295 and 297nm respectively.RESULTS:The pKa value of sildenafil was 9.35?0.02.CONCLUSION:The present method is convenient and practicable.