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941.
The discovery of threosyl phosphonate nucleoside (PMDTA, EC50 = 2.53 μM) as a potent anti-HIV agent has led to the synthesis and biological evaluation of 5 ′-deoxyversions of threosyl phosphonate nucleosides from 1,4-dihydroxy-2-butene. The synthesized nucleoside phosphonic acid analogues 14 and 19 were tested for anti-HIV activity as well as cytotoxicity. The adenine analogue 14 exhibits moderate in vitro anti-HIV-1 activity (EC50 = 12.6 μM). 相似文献
942.
943.
Novel syntheses of 4′-modified cyclopentenyl pyrimidine C-nucleosides were performed via C-C bond formation using SN2 alkylation via the key intermediate mesylates 6 and 16, which were prepared from acyclic ketone derivatives. When antiviral evaluation of synthesized compound was performed against various viruses such as HIV-1, HSV-1 and HSV-2, isocytidine analogue 20 showed moderate anti-HIV activity in CEM cell line (EC50 = 13.1 μmol).7 相似文献
944.
X. Xu L. Zhao X. Hu P. Zhang J. Wessale R. Bache 《Nucleosides, nucleotides & nucleic acids》2013,32(4-6):306-313
The nonpurine selective xanthine oxidase (XO) inhibitor febuxostat attenuates development of left ventricular (LV) hypertrophy and dysfunction in mice when treatment is initiated within 1 hour of transverse aortic constriction (TAC). This study investigated whether a 7-day delay of treatment with the XO inhibitors febuxostat or allopurinol would reverse TAC-induced changes after onset of heart failure (HF). Neither treatment significantly affected TAC-induced LV hypertrophy; only febuxostat caused a modest improvement in LV function (~10% increase in LV ejection fraction). However, the purine analog allopurinol tended to increase mortality compared with vehicle or febuxostat in HF mice. 相似文献
945.
Chang Hyun Oh Jin Woo Kim Joon Hee Hong 《Nucleosides, nucleotides & nucleic acids》2013,32(8):871-878
Novel vinyl branched apiosyl nucleosides were synthesized in this study. Apiosyl sugar moiety was constructed by sequential ozonolysis and reductions. The bases (uracil and thymine) were efficiently coupled by glycosyl condensation procedure (persilyated base and TMSOTf). The antiviral activities of the synthesized compounds were evaluated against the HIV-1, HSV-1, HSV-2, and HCMV. Compound 10β displayed moderate anti-HIV activity (EC50 = 17.3 μg/mL) without exhibiting any cytotoxicity up to 100 μM. 相似文献
946.
Jian Su Kittisak Sripanidkulchai Ying Hu Rungsiri Chaiittianan Bungorn Sripanidkulchai 《AAPS PharmSciTech》2013,14(3):1055-1062
Curcuma comosa has long been used as a gynecological medicine. Several diarylheptanoids have been purified from this plant, and their pharmacological effects were proven. However, there is no information about the absorption of C. comosa components to support the formulation usage. In the present study, C. comosa hexane extract and the mixture of its two major compounds, (4E,6E)-1,7-diphenylhepta-4,6-dien-3-ol (DA1) and (6E)-1,7-diphenylhept-6-en-3-ol (DA2), were formulated into nanoemulsions. The physical properties of the nanoemulsions and the in situ intestinal absorptions of DA1 and DA2 were evaluated. The results demonstrated the mean particle sizes at 0.207 ± 0.001 and 0.408 ± 0.014 μm, and the zeta potential at −14.57 ± 0.85 and −10.47 ± 0.32 mV for C. comosa nanoemulsion (C.c-Nano) and mixture of diarlylheptanoid nanoemulsions (DA-Nano), respectively. The entrapments of DA1 and DA2 were 76.61% and 75.41%, and 71.91% and 71.63% for C.c-Nano and DA-Nano, respectively. The drug loading ratios of DA1 and DA2 were 351.47 and 614.53 μg/mg, and 59.48 and 126.72 μg/mg for C.c-Nano and DA-Nano. The intestinal absorption rates of DA1 and DA2 were 0.329 ± 0.015 and 0.519 ± 0.026 μg/min/cm2 in C.c-Nano, and 0.380 ± 0.006 and 0.428 ± 0.036 μg/min/cm2 in DA-Nano, which were five to ten times faster than those in oil. In conclusion, the formulation in nanoemulsion forms obviously increased the intestinal absorption rate of diarylheptanoids.KEY WORDS: Curcuma comosa, diarylheptanoids, intestinal absorption, nanoemulsion, phytoestrogen 相似文献
947.
Tam Dinh Le Vo Ji-seun Ko Seung Hwan Lee Si Jae Park Soon Ho Hong 《Biotechnology and Bioprocess Engineering》2013,18(6):1062-1066
This study investigated the effect of glutamate decarboxylase from Neurospora crassa OR74A on GABA production in Escherichia coli. GABA is one of the inhibitory neurotransmitters in the mammalian central nervous system, and can be used as a precursor of promising biopolymer Nylon 4. E. coli that overexpressed N. crassa glutamate decarboxylase was cultured at various pH levels and temperatures to determine optimum conditions for GABA production. When the recombinant E. coli strain was cultured at 30°C and pH 3, a final GABA concentration of 5.26 g/L was obtained from 10 g/L of monosodium glutamate (MSG), corresponding to a GABA yield of 86.23%. 相似文献
948.
Recovery of native protein from potato root water by expanded bed adsorption with amberlite XAD7HP 总被引:3,自引:0,他引:3
Fan-Kui Zeng Hong Liu Peng-Jun Ma Gang Liu 《Biotechnology and Bioprocess Engineering》2013,18(5):981-988
Potato root water (PRW) contains ~1.5% protein. In this study, expanded bed adsorption (EBA) chromatography with Amberlite XAD7HP resin adsorbent was used to isolate native protein from crude PRW. The optimal pH and ionic strength for potato protein binding onto Amberlite XAD7HP were 5.0 and 20 mmol/L. The EBA-refined proteins were dried by vacuum freeze drying and spray drying at varying outlet temperatures. Results indicated that low temperature spray drying was the most cost effective method with respect to retaining protease inhibitor activities. The dried protein concentrates appeared bright yellow or dark reddish brown, with a total glycoalkaloid content of ~170 μg/g. The protease inhibitor activity was ~400 mg/g and 11 ~ 12 mg/g for trypsin inhibition and chymotrypsin inhibition, respectively. The results presented here suggest that EBA using Amberlite XAD7HP as the adsorbent is a feasible strategy for the direct adsorption of native protein from crude PRW. 相似文献
949.
Hao Zhang Jing Sun Xianting Liu Chuan Hong Yuanbo Zhu Aiping Liu Siqi Li Huiyuan Guo Fazheng Ren 《Journal of microbiology (Seoul, Korea)》2013,51(6):777-782
Lactobacillus paracasei subsp. paracasei LC01 (LC01) can tolerate intestinal stresses and has antioxidant activity. To evaluate the effect of the bacterium on human intestinal microflora, a randomized, double-blind, placebo-controlled human trial was carried out. Fifty-two healthy adult volunteers were randomized equally to two groups. One group consumed 12% (wt/vol) skimmed milk supplemented with 1010 CFU of LC01 each day for the 4-week treatment period, and then consumed placebo in the next treatment period, separated by a 2-week washout. The other group followed the reverse order. Group-specific real-time PCR and biochemical analyses was used to determine the intestinal bacterial composition of fecal samples collected at the end of every period, and the concentration of short-chain fatty acids and ammonia. A significant inhibition in fecal Escherichia coli and increase in Lactobacillus, Bifidobacterium, and Roseburia intestinalis were observed after consumption of LC01. Acetic acid and butyric acid were significantly higher in the probiotic stage and fecal ammonia was significantly lower. The results indicated a modulation effect of LC01 on the intestinal microflora of young adults, suggesting a beneficial effect on bowel health. LC01 may have potential value as a probiotic. 相似文献
950.
Xiang-Jun?Jiang Yi?Hu Ling?Jiang Bin?Zou Ping?Song He?HuangEmail author 《Biotechnology and Bioprocess Engineering》2013,18(2):350-357
Statistical experimental designs combined with solvent engineering for optimization of enzymatic synthesis of L-ascorbyl palmitate were developed. First, the composition of the solvent for co-dissolving polar and apolar substrates was determined. The co-solvent mixture of tert-pentanol: DMSO at a ratio of 9:1 (v/v) and the optimal biocatalyst were obtained. Then, the Plackett-Burman design was implemented to screen the variables that significantly influence the conversion. The method of steepest ascent was used to approach the proximity of optimum. After determining the Plackett-Burman and steepest ascent designs, the optimum values were determined by central composite design under response surface methodology. The statistical analysis showed that the optimum reaction conditions (temperature 50°C, enzyme concentration 5.8 g/L, and substrate molar ratio 11:1, stirring rate 160 rpm, amount of molecular sieve 50 g/L, time 18 h) led to the maximum conversion (66.44%) and production concentration (20.63 g/L). A very satisfactory conversion (64.74%) and production concentration (20.13 g/L) could be achieved in short time (6 h). 相似文献