排序方式: 共有57条查询结果,搜索用时 15 毫秒
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Xinxian Deng Jian Shen Hui Zhu Jia Xiao Ran Sun Fangzhou Xie Celine Lam Juntao Wang Yixue Qiao Mojdeh S. Tavallaie Yang Hu Yi Du Jianqi Li Lei Fu Faqin Jiang 《Bioorganic & medicinal chemistry》2018,26(4):903-912
The initial focus on characterizing novel pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as DPP-4 inhibitors, led to a potent and selective inhibitor compound b2. This ligand exhibits potent in vitro DPP-4 inhibitory activity (IC50: 80?nM), while maintaining other key cellular parameters such as high selectivity, low cytotoxicity and good cell viability. Subsequent optimization of b2 based on docking analysis and structure-based drug design knowledge resulted in d1. Compound d1 has nearly 2-fold increase of inhibitory activity (IC50: 49?nM) and over 1000-fold selectivity against DPP-8 and DPP-9. Further in vivo IPGTT assays showed that compound b2 effectively reduce glucose excursion by 34% at the dose of 10?mg/kg in diabetic mice. Herein we report the optimization and design of a potent and highly selective series of pyrazolo[1,5-a]pyrimidin-7(4H)-one DPP-4 inhibitors. 相似文献
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Mojdeh Salehnia 《Experimental Animals》2002,51(5):509-512
Ovaries from 8 to 10-week-old N MRI mice were vitrified using RPMI solution containing 30% (W/V) ficoll 70, 0.5 M sucrose, 10.7% (V/V) acetamide and 40% (V/V) ethylene glycol (EGFS40%), and were stored in liquid nitrogen. After warming at 25 degrees C in 1 M sucrose solution and equilibration with RPMI medium, the vitrified and fresh ovarian tissues were autografted intraperitoneally. After one and two estrus cycles the animals were sacrificed and the recovered grafts were examined histologically. Five days after transplantation the vitrified ovaries they were invaded by fat and fibrous cells and the large preantral and antral follicles were degenerated. At 11 days postgrafting the stroma was devoid of necrotic cells and contained normal primordial and primary follicles, suggesting that the vitrification is a simple, useful and efficient procedure for cryopreservation of murine ovarian tissues. 相似文献
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Mojdeh Khosravi Hanieh Mohammad Rahimi Abdoreza Nazari Kaveh Baghaei Hamid Asadzadeh Aghdaei Shabnam Shahrokh Meysam Sharifdini Ana Claudia Torrecilhas Fatemeh Mehryab Hamed Mirjalali Faezeh Shekari Mohammad Reza Zali 《Journal of cellular and molecular medicine》2023,27(17):2614-2625
Hydatidosis is a disease caused by the larval stage of Echinococcus granulosus, which involves several organs of intermediate hosts. Evidence suggests a communication between hydatid cyst (HC) and hosts via extracellular vesicles. However, a little is known about the communication between EVs derived from HC fluid (HCF) and host cells. In the current study, EVs were isolated using differential centrifugation from sheep HCF and characterized by western blot, electron microscope and size distribution analysis. The uptake of EVs by human monocyte cell line (THP-1) was evaluated. The effects of EVs on the expression levels of pro- and anti-inflammatory cytokines were investigated using quantitative real-time PCR (RT-PCR), 3 and 24 h after incubation. Moreover, the cytokine level of IL-10 was evaluated in supernatant of THP-1 cell line at 3 and 24 h. EVs were successfully isolated and showed spherical shape with size distribution at 130.6 nm. After 3 h, the expression levels of pro-inflammatory cytokine genes (IL1Β, IL15 and IL8) were upregulated, while after 24 h, the expression levels of pro-inflammatory cytokines were decreased and IL13 gene expression showed upregulation. A statistically significant increase was seen in the levels of IL-10 after 24 h. The main mechanism of the communication between EVs derived from HCF and their host remains unclear; however, time-dependent anti-inflammatory effects in our study suggest that HC may modulate the immune responses via EVs. 相似文献
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Mousavi Seyedeh Zahra Rahmanian Mojdeh Sami Ashkan 《Functional & integrative genomics》2022,22(3):429-433
Functional & Integrative Genomics - Although extrapulmonary manifestations of coronavirus disease 2019 (COVID-19) are increasingly reported, no effective therapeutic strategy for these... 相似文献
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