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Amir Assadieskandar Amirali Amirhamzeh Marjan Salehi Keriman Ozadali Seyed Nasser Ostad Abbas Shafiee Mohsen Amini 《Bioorganic & medicinal chemistry》2013,21(8):2355-2362
A series of 4-aryl-5-(4-(methylsulfonyl)phenyl)-2-alkylthio and 2-alkylsulfonyl-1H-imidazole derivatives were synthesized. All compounds were tested in human blood assay to determine COX-1 and COX-2 inhibitory potency and selectivity. Among the synthesized compounds, 2-alkylthio series were more potent and selective than 2-sulfonylalkyl derivatives. In molecular modeling, interaction of 2-sulfonylalkyl moiety with Arg120 in COX-1 and an extra hydrogen bond with Tyr341 in COX-2 increased the residence time of ligands in the active site in 2-sulfonylalkyl and 2-alkylthio analogs, respectively. 相似文献
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Maryam Mansourpour Reza Mahjub Mohsen Amini Seyed Naser Ostad Elnaz Sadat Shamsa Morteza Rafiee- Tehrani Farid Abedin Dorkoosh 《AAPS PharmSciTech》2015,16(4):952-962
In this study, the use of trimethylchitosan (TMC), by higher solubility in comparison with chitosan, in alginate/chitosan nanoparticles containing cationic β-cyclodextrin polymers (CPβCDs) has been studied, with the aim of increasing insulin uptake by nanoparticles. Firstly, TMCs were synthesized by iodomethane, and CPβCDs were synthesized within a one-step polycondensation reaction using choline chloride (CC) and epichlorohydrine (EP). Insulin–CβCDPs complex was prepared by mixing 1:1 portion of insulin and CPβCDs solutions. Then, nanoparticles prepared in a three-step procedure based on the iono-tropic pregelation method. Nanoparticles screened using experimental design and Placket Burman methodology to obtain minimum size and polydispercity index (pdI) and the highest entrapment efficiency (EE). CPβCDs and TMC solution concentration and pH and alginate and calcium chloride solution concentrations are found as the significant parameters on size, PdI, and EE. The nanoparticles with proper physicochemical properties were obtained; the size, PdI, and EE% of optimized nanoparticles were reported as 150.82 ± 21 nm, 0.362 ± 0.036, and 93.2% ± 4.1, respectively. The cumulative insulin release in intestinal condition achieved was 50.2% during 6 h. By SEM imaging, separate, spherical, and nonaggregated nanoparticles were found. In the cytotoxicity studies on Caco-2 cell culture, no significant cytotoxicity was observed in 5 h of incubation, but after 24 h of incubation, viability was decreased to 50% in 0.5 mμ of TMC concentration. Permeability studies across Caco-2 cells had been carried out, and permeability achieved in 240 min was 8.41 ± 0.39%, which shows noticeable increase in comparison with chitosan nanoparticles. Thus, according to the results, the optimized nanoparticles can be used as a new insulin oral delivery system.KEY WORDS: alginate, cationic β-cyclodextrin, insulin nanoparticle, oral delivery, trimethyl chitosan 相似文献
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Polyana C Tizioto Jeremy F Taylor Jared E Decker Caio F Gromboni Mauricio A Mudadu Robert D Schnabel Luiz L Coutinho Gerson B Mour?o Priscila SN Oliveira Marcela M Souza James M Reecy Renata T Nassu Flavia A Bressani Patricia Tholon Tad S Sonstegard Mauricio M Alencar Rymer R Tullio Ana RA Nogueira Luciana CA Regitano 《遗传、选种与进化》2015,47(1)
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Recombinant human Factor IX (rFIX) was cloned in a mammalian expression vector and transfected into CHO and HEK-293. Treatment
with 10−9 M methyl testosterone increased rFIX production by 30–50% in CHO and HEK clones. However, 10−9 M 17β-oestradiol increased production of rFIX by ~50% in CHO-F7 clone and decreased production by 48% and 37% in CHO-F8 and
HEK-F2-6, respectively. Progesterone treatment inhibited rFIX production in both cell lines. Production of rFIX can thus be
increased by sex hormone treatment and therefore used to enhance biotechnological production in mammalian cells. 相似文献
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The aim of this study was to determine the first effect of lead on microbial activity in soil. The study was carried out in the soil samples from four different radish (Raphanus sativus L. var. radicula, Brassicaceae) fields along the highway in a district (Kadirli, Osmaniye) of the Eastern Mediterranean Region, Turkey. After the calculation of Pb contents, the Pb amounts of the soil samples were brought up to 50 and 100 mg Pb kg?1 by treatment with Pb(NO 3 ) 2 , and the samples for the carbon and the nitrogen mineralization were incubated under controlled conditions (28°C, constant moist). The carbon mineralization was determined by a CO 2 respiration method for 30 days. The nitrogen mineralization was observed in vitro for 6 weeks. The untreated group was statistically different from the 50 and 100 mg Pb kg?1 treatments in the aspect of the C(CO 2 ) outlet during mineralization (P ≤ 0.05), but difference between the 50 and 100 mg Pb kg?1 treatments was not significant. NH 4 -N and NO 3 -N contents of each soil were shown differences between across treatments. Based on these results, it is possible to conclude that the addition of 50 and 100 mg Pb kg?1 provided a toxic effect threshold for the microbial activity into 30 days. 相似文献
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Twelve fungi namelyAlternaria alternata, Aspergillus flavus, A niger, A ochraceus, Actinomucor repens, Capnodoium spp., Curvularia lunata, Fusarium
pallidoroseum, F solani, F verticillioides, Penicillium citrinum and Rhizopus stolonifer were recorded from samples ofAegle marmelos, Aesculus indica, Buchanania lanzan andPinus gerardiana. In case ofPrunus amygdalus only Rstolonifer was recorded. A significant variation in pattern of mycoflora incidence was observed in terms of source and season. Fungal
infestation in most of the substrates was found to be highest during monsoon. Aflatoxins were the most common mycotoxins elaborated
by different isolates ofA flavus obtained fromA marmelos, B lanzan andP gerardiana. The amount of aflatoxins produced by the toxigenic isolates ofA flavus was in the range of traces to 0.9–26.0 μg/ml inA marmelos, 0.8–17.5 μg/ml inP gerardiana and 0.65–13.2 μg/ml inB lanzan. The percentage toxigenicity was comparatively lower in the isolates of other mycotoxigenic fungi. Aflatoxins were detected
almost in all the samples analyzed for mycotoxin contamination. However, traces of zearalenone were detected inA marmelos. The concentration of aflatoxin B1 was in the range of 0.13–0.75 μg/g inA marmelos, 0.09–0.60 μg/g inP gerardiana and 0.01–0.20 ug/g inB lanzan. Mycotoxins were not detected inAesculus indica andPrunus amygdalus. 相似文献
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Mousa Abkhezr Ali Reza Keramati Seyed Nasser Ostad Jamshid Davoodi Mohammad H. Ghahremani 《Molecular biology reports》2010,37(4):2037-2042
The cell growth is controlled by the interaction of survival and cell growth arrest pathways as well as apoptosis mechanisms
which determine the outcome of cell faith as proliferation or apoptosis. In this study, we have studied the activity of survival
pathways, i.e., Akt and ERK1/2 with regard to XIAP (inhibitor of apoptosis) in serum starved and stimulated conditions. The
HEK-293 cells were cultured in RPMI + 10% FBS. The cells were serum starved by switching to medium with 1% FBS for 24 h and
serum stimulated by changing the medium to 10% FBS following serum starvation. The expression of p-Akt, p-ERK, Akt, ERK and
XIAP was studied in various time points using western blot. The apoptosis was evaluated by DNA condensation using Hoechst
33258 and Caspase-3 assay. In serum starved condition expression of p-Akt and XIAP is very low. Serum stimulation increases
p-Akt and p-ERK within 5 min and sustains a high level for 30 min. The expression of total Akt and ERK1/2 has not changed
significantly for 24 h. XIAP expression starts at 6 h after serum stimulation, reaches to maximum level at 12 h and decreases
to baseline within 24 h. Furthermore, serum starvation for 24 h does not induced apoptosis and DNA condensation. Taken together,
the results indicate that serum activates Akt and ERK pathways earlier than XIAP expression. Furthermore, XIAP expression
is low in serum starvation unlike p-ERK which suggests a survival role for ERK in serums starvation. The expression pattern
of XIAP indicates induction by Akt and/or ERK activation which requires further studies. 相似文献