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排序方式: 共有188条查询结果,搜索用时 281 毫秒
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C.Z. DONG H. DE ROCQUIGNY E. RMY S. MELLAC M.C. FOURNI-ZALUSKI B.P. ROQUES 《Chemical biology & drug design》1997,50(4):269-278
Specific interactions between the 72-amino acid nucleocapsid protein NCp7 of the human immunodeficiency virus, type 1 and the genomic RNA are essential for virus replication. Studies on the mechanism of action of NCp7 require a direct visualization of its complexes with nucleic acids and the determination of binding affinities. To facilitate these investigations, fluorescent NCp7 derivatives were developed by introduction in the NCp7 sequence of a non-natural amino acid, (S)-β-(9-acridinyl)alanine (Aca) obtained by a chiral synthetic method. Three fluorescent NCp7 derivatives were obtained by introducing this amino acid at different positions. As shown by NMR, the three-dimensional structure of NCp7 is not altered by introduction of Aca. The fluorescent peptides were found to be as potent as their precursors in interacting with nucleic acids and in promoting HIV-1 genomic RNA dimerization. Moreover, because of their fluorescent properties, these NCp7s can be used at submicromolar concentrations to directly visualize and quantify protein-nucleic acid interactions in solution or after gel electrophoresis. This could facilitate the development of new antiviral agents aimed at inhibiting the functions of NCp7 and studies on the intracellular traffic of NCp7 within the preintegration complex. 相似文献
23.
The paper reports results of an analysis based on face-to-face interviews with two samples of Prague women aged 20-49: (1) a probabilistic sample (h = 718) of the Prague female population; and (2) a sample of 152 inpatients treated for substance dependence/abuse. Of the inpatients, 79% were diagnosed as alcohol dependent only, 15% as both alcohol dependent and drug dependent/abusers, 6% as drug dependent only. With very few exceptions, those with drug problems among the inpatients abused analgesics, hypnotics, or anxiolytics. With data obtained from the general population sample, two-stage hierarchical logistic regression was run with each of the eleven differently defined substance uses as dependent variables. Four demographic variables were entered as predictors into the regression equations in the first stage. From the seven potential risk factors of substance use statistically significant predictors were entered stepwise in stage two. The major result of the study is the specificity of the pattern of predictors related to each of the eleven considered substance uses. It is also found that in the general population the use of a particular substance is generally uncorrelated with the use of other substances. Alcohol use (even heavy alcohol use) has no relation to smoking, to the use of analgesics, hypnotics, anxiolytics-and is connected with a specific pattern of predictors. 相似文献
24.
Navid Mosallaei Mahmoud Reza Jaafari Mohammad Yahya Hanafi-Bojd Shiva Golmohammadzadeh Bizhan Malaekeh-Nikouei 《Journal of pharmaceutical sciences》2013,102(6):1994-2004
The aim of the present study was to prepare, characterize, and evaluate solid lipid nanoparticles (SLNs) containing docetaxel (DTX) to improve the efficacy of this chemotherapeutic agent. SLNs containing DTX (SLN-DTX) were prepared by microemulsion and probe sonication techniques. In vitro cytotoxicity of SLN-DTX compared with Taxotere® (TXT) was evaluated on colorectal (C-26) and malignant melanoma (A-375) cell lines. Cellular uptake experiment was also carried out on C-26 cells. In in vivo tests, tumor inhibitory efficacy and survival were compared with TXT on C-26-implanted BALB/c mice. SLN-DTX particle size was 180 nm and PDI of 0.2 with spherical shape. Encapsulation efficacy was more than 98%. SLN-DTX at concentration of 100 μM caused 100% and 99.9% viability reduction in C-26 and A-375 after 48 and 72 h, respectively. The half maximal inhibitory concentration (IC50) of SLN-DTX on C-26 and A-375 was respectively 0.769 and 28.132 μM after 24 h. DTX cell uptake from SLN-DTX was remarkably higher than TXT. SLN-DTX showed better tumor inhibitory efficacy and survival at a dose of 10 mg/kg versus 10 and 20 mg/kg TXT. In conclusion, the results of the present study showed that the efficacy of SLN-DTX was better than TXT in cell-uptake and in vivo experiments. 相似文献
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Babak Shiravand Ahmad Ali Hanafi-Bojd Abbas Ali Dehghani Tafti Mohammad Reza Abai Ali Almodarresi Masoud Mirzaei 《Asian Pacific journal of tropical medicine》2019,(5)
Objective: To investigate and predict the effects of climate change on the potential distribution of the main vector and reservoir hosts of the disease in Yazd province in the future.Methods: Distribution data for vector and reservoir hosts of zoonotic cutaneous leishmaniasis in Yazd province were obtained from earlier studies conducted in the area.MaxEnt ecological niche modeling was used to predict environmental suitability.BCC-CSM1-1(m) model and two climate change scenarios, RCP 4.5 and RCP 8.5 were used for horizons 2030 and 2050 climate projections.Future projections were based on data of a regional climate change model.Results: With both scenarios in 2030 and 2050, the results of jackknife test indicated that the mean temperature of wettest quarter and temperature annual range had the greatest effect on the model for the vector and the reservoir hosts, respectively.Conclusions: The climate conditions are the major determinants of zoonotic cutaneous leishmaniasis incidence rate in Yazd Province.These climate conditions provide favorable habitats for ease transmission of zoonotic cutaneous leishmaniasis in this endemic area.Habitats suitability for the vector and reservoir will be expanding in the coming years compared with the current conditions, such that, in horizon 2030 2050, the probability of the presence of the vector and reservoir within 38 580 and 37 949 km~2, respectively, from Yazd province is above 60%.Moreover, an increase is predicted in the presence of the vector in the western parts and the reservoir in the northern and central parts of the province in the future.Understanding the role of environmental and bioclimatic factors in zoonotic cutaneous leishmaniasis occurrence can provide a guide for policy-makers in the creation and implementation of more effective policies for prevention and control. 相似文献
28.
Madineh Abbasi Ahmad Ali Hanafi-Bojd Mohammad Reza Yaghoobi-Ershadi Hassan Vatandoost Mohammad Ali Oshaghi Teimour Hazratian Mohammad Mehdi Sedaghat Sajjad Fekri Reza Safari Abdol Rasoul Mojahedi Yousef Salari 《Asian Pacific journal of tropical medicine》2019,(1)
Objective: To evaluate the susceptibility of Anopheles stephensi(An. stephensi) Liston, the main malaria vector in southern Iran, to WHO recommended insecticides. Methods: Larvae of An. stephensi were collected from three different larval habitats in both urban and rural area of Bandar Abbas city and one rural area in Rudan county southern Iran. WHO standard method was used for evaluation of adult and larval mosquito susceptibility. Bendiocarb, permethrin, lambda-cyhalothrin, deltamethrin as insecticide and temephos and chlorpyriphos as larvicide were used at the diagnostic dosages recommended by WHO. Results: Findings of this study showed all larval populations of An. stephensi were completely susceptible to temephos and candidate for resistance to chlorpyriphos. Adult mosquitoes in rural areas of Bandar Abbas city were resistant to pyrethroid and carbamate insecticides. Conclusion: Comparison of the results of this survey with previous studies indicates that the resistance to pyrethroids and carbamates in this malaria endemic region is increasing. Wide use of pesticides in agriculture is certainly effective in increasing resistance. The inter-sectoral coordination and collaboration in health and agriculture seem to be necessary to manage insecticide resistance in malaria vectors. 相似文献
29.
Hon YY; Fessing MY; Pui CH; Relling MV; Krynetski EY; Evans WE 《Human molecular genetics》1999,8(2):371-376
The molecular basis for the genetic polymorphism of thiopurine S -
methyltransferase (TPMT) has been estab-lished for Caucasians, but it
remains to be elucidated in African populations. In the current study, we
determined TPMT genotypes in a population of 248 African-Americans and
compared it with allele frequencies in 282 Caucasian Americans. TPMT
genotype was determined in all individuals with TPMT activity indicative of
a heterozygous genotype (</=10.1 U/ml pRBC, n = 23African- Americans, n
= 21 Caucasians) and a control group with TPMT activity indicative of a
homozygous wild-type genotype (>10.2 U/ml pRBC, n = 23
African-Americans, n = 21 Caucasians). No mutant alleles were found in the
high activity control groups. The overall mutant allele frequencies were
similar in African-Americans and Caucasians (4.6 and 3.7% of alleles,
respectively). However, while TPMT*3C was the most prevalent mutant allele
in African-Americans (52.2% of mutant alleles), it represented only 4.8% of
mutant alleles in Caucasians ( P < 0.001). In contrast, TPMT*3A and
TPMT*2 were less common in African-Americans (17.4 and 8.7% of mutant
alleles), whereas TPMT*3A was the most prevalent mutant allele in
Caucasians (85.7% of mutant alleles). A novel allele ( TPMT*8 ), containing
a single nucleotide transition (G644A), leading to an amino acid change at
codon 215 (Arg-->His), was found in one African-American with
intermediate activity. These data indicate that the same TPMT mutant
alleles are found in American black and white populations, but that the
predominant mutant alleles differ in these two ethnic groups.
相似文献
30.
目的 :研究硝苯吡啶以及硝苯吡啶与格列本脲合用对空腹大鼠和肾上腺素诱发高血糖大鼠血糖水平的影响。方法 :本实验采用葡萄糖氧化酶法测定血糖含量。结果 :硝苯吡啶 2 .5mg/kgig使空腹大鼠血糖水平显著升高(P <0 .0 1 ) ,并加重肾上腺素诱发的高血糖反应。而硝苯吡啶与降糖药格列本脲 0 .9mg/kg合用时不影响空腹大鼠的血糖水平 ,硝苯吡啶对肾上腺素诱发高血糖大鼠灌胃格列本脲后的降血糖作用亦无明显影响。结论 :尽管硝苯吡啶对空腹大鼠以及肾上腺素诱发高血糖大鼠有显著升高血糖的作用 ,但对格列本脲的降血糖作用无明显不良影响 相似文献