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51.
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Tamer Nasr Samir Bondock Sameh Eid 《Journal of enzyme inhibition and medicinal chemistry》2016,31(2):236-246
Microbial resistance to the available drugs poses a serious threat in modern medicine. We report the design, synthesis and in vitro antimicrobial evaluation of new functionalized 2,3-dihydrothiazoles and 4-thiazolidinones tagged with sulfisoxazole moiety. Compound 8d was most active against Bacillis subtilis (MIC, 0.007?µg/mL). Moreover, compounds 7c–d and 8c displayed significant activities against B. subtilis and Streptococcus pneumoniae (MIC, 0.03–0.06?µg/mL and 0.06–0.12?µg/mL versus ampicillin 0.24?µg/mL and 0.12?µg/mL; respectively). Compounds 7a and 7c–d were highly potent against Escherichia coli (MIC, 0.49–0.98?µg/mL versus gentamycin 1.95?µg/mL). On the other hand, compounds 7e and 9c were fourfolds more active than amphotericin B against Syncephalastrum racemosum. Molecular docking studies showed that the synthesized compounds could act as inhibitors for the dihydropteroate synthase enzyme (DHPS). This study is a platform for the future design of more potent antimicrobial agents. 相似文献
53.
Huiming Xu Kam Sze Tsang Yonghui Wang Juliana CN Chan Gang Xu Wei-Qiang Gao 《The Journal of biological chemistry》2014,289(38):26290-26301
Tremendous efforts have been made to elucidate the molecular mechanisms that control the specification of definitive endoderm cell fate in gene knockout mouse models and ES cell (ESC) differentiation models. However, the impact of the unfolded protein response (UPR), because of the stress of the endoplasmic reticulum on endodermal specification, is not well addressed. We employed UPR-inducing agents, thapsigargin and tunicamycin, in vitro to induce endodermal differentiation of mouse ESCs. Apart from the endodermal specification of ESCs, Western blotting demonstrated the enhanced phosphorylation of Smad2 and nuclear translocation of β-catenin in ESC-derived cells. The inclusion of the endoplasmic reticulum stress inhibitor tauroursodeoxycholic acid to the induction cultures prevented the differentiation of ESCs into definitive endodermal cells even when Activin A was supplemented. Also, the addition of the TGF-β inhibitor SB431542 and the Wnt/β-catenin antagonist IWP-2 negated the endodermal differentiation of ESCs mediated by thapsigargin and tunicamycin. These data suggest that the activation of the UPR appears to orchestrate the induction of the definitive endodermal cell fate of ESCs via both the Smad2 and β-catenin signaling pathways. The prospective regulatory machinery may be helpful for directing ESCs to differentiate into definitive endodermal cells for cellular therapy in the future. 相似文献
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The presence of congenital skin abnormalities on the back may be associated with a serious underlying spinal anomaly, diastematomyelia. The significance of the progressive development of neurological deficits, due to the presence of a bony or cartilaginous spur in the spinal cord, is stressed. An awareness of this condition should lead to an early diagnosis with a neurological evaluation and, if necessary, prophylactic surgery before irreversible nerve damage develops. 相似文献
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Ahmed Eid Fazary Suryadi Ismadji Yi-Hsu Ju 《International journal of biological macromolecules》2009,44(3):240-248
Thermal stabilities of a native freeze dried Aspergillus awamori feruloyl esterase (FAE-II) enzyme and a cross-linked feruloyl esterase aggregate (CLEAs) at 25–85 °C were evaluated and discussed. Effects of some metal ions and some chemicals on the activity of both native freeze dried FAE-II enzyme and CLEAs were examined and explained. Differential scanning calorimetry, thermogravimetry, and derived thermogravimetry, were used to observe and explain the thermal denaturation processes. Structural analyses were made for native FAE-II and CLEAs using FT-IR and SEM techniques to investigate whether the cross-linking had any effect on the powder structure of native FAE-II enzyme. 相似文献
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The thermodynamics of the interactions of serum apotransferrin (T) and holotransferrin (TFe(2)) with ceruloplasmin (Cp), as well as those of human lactoferrin (Lf), were assessed by fluorescence emission spectroscopy. Cp interacts with two Lf molecules. The first interaction depends on pH and μ, whereas the second does not. Dissociation constants were as follows: K(11Lf) = 1.5 ± 0.2 μM, and K(12Lf) = 11 ± 2 μM. Two slightly different interactions of T or TFe(2) with Cp are detected for the first time. They are both independent of pH and μ and occur with 1:1 stoichiometry: K(1T) = 19 ± 7 μM, and K(1TFe2) = 12 ± 4 μM. These results can improve our understanding of the probable process of the transfer of iron from Cp to T in iron and copper transport and homeostasis. 相似文献
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Saleh Jaweesh Mayyas Hammadeh Mohamad Eid Dahadhah Fatina W. Al Zoubi Mazhar Salim Amor Houda 《Molecular biology reports》2022,49(5):3609-3616
Molecular Biology Reports - Idiopathic male infertility can be attributed to genetic predispositions that affect sperm performance and function. Genetic alterations in the mitochondrial DNA (mtDNA)... 相似文献
60.
Omneya Eid Wafaa M. Elkady Shahira Ezzat Abeer El Sayed Essam Abd elsattar 《化学与生物多样性》2023,20(3):e202200935
Barley (Hordeum vulgare L.) is one of the world's oldest cereal crops. There is considerable interest in barley's potential usage in human diets. Barley is rich in bioactive metabolites such as high content of β-glucan, fiber, and vitamin E. It is also well-known as a rich source of phytochemical derivatives, namely, phenolic acids, flavonols, chalcones, flavones, proanthocyanidins, and flavanones. Phenolic compounds are recognized as excellent dietary materials with antioxidant and anti-inflammatory activities. This review was written to give an overview of the main components that are separated from barley using different solvents. Even though there were numerous biological activities for barely, the antioxidant, as well as the anti-inflammatory, are the main focus of this review. 相似文献