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STX0119 Ameliorates Arthritis in SKG Mice via Inhibiting T Helper 17
Hayat Faisal,이승훈,이은정,김석중,정경아,이순규,윤지희,민준기,조미라,신동윤 한국조직공학과 재생의학회 2016 조직공학과 재생의학 Vol.13 No.1
Rheumatoid arthritis (RA) is an autoimmune disease with chronic and excessive inflammation. Upregulation of interleukin (IL)-17 is involved in the pathogenesis of RA. STX0119 is a specific inhibitor of signal transducer and activator of transcription 3 (STAT3) as a potential target for the treatment of RA. STAT3 is a member of DNA-binding molecules that regulates the expression of proinflammatory cytokines involved in the pathogenesis of RA. The objective of this study was to determine whether STX0119 could inhibit STAT3 and IL-17. We demonstrated that STX0119 decreased T helper (Th) 17 differentiation and IL-17 expression in vitro. STX0119 also improved the severity of zymosan induced arthritis and reduced joint inflammation. STX0119 reduced the proliferation of Th17 and phosphorylated STAT3 expression while increasing Treg differentiation and phosphorylated STAT5 expression. Moreover, STX0119 decreased the expression of IL-6 and -17 but not IL-10. These findings suggest that STX0119 can be used to treat autoimmune RA through inhibiting the activation of STAT3.
Synthesis and Inhibition Effects on 5-HT<sub>6</sub> Receptor of Benzothiazole Derivatives
Hayat, Faisal,Yoo, Euna,Rhim, Hyewhon,ParkChoo, Hea-Young Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.2
A novel series of aryl sulfonylpiperazine derivatives (5-15) were synthesized as 5-$HT_6$ ligands. In vitro assay was evaluated by measuring the 5-HT-induced $Ca^{2+}$ increases using HeLa cell line expressing the cloned human 5-$HT_6$ receptor, and the compound 13 showed potent 5-$HT_6$ receptor antagonistic effect with $IC_{50}$ value of 3.9 ${\mu}M$. Compound 13 also showed good selectivity on the 5-$HT_6$ over 5-$HT_4$ and 5-$HT_7$ receptors.
Synthesis and Inhibition Effects on 5-HT6 Receptor of Benzothiazole Derivatives
Faisal Hayat,Euna Yoo,Hyewhon Rhim,박혜영 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.2
A novel series of aryl sulfonylpiperazine derivatives (5-15) were synthesized as 5-HT6 ligands. In vitro assay was evaluated by measuring the 5-HT-induced Ca2+ increases using HeLa cell line expressing the cloned human 5-HT6 receptor, and the compound 13 showed potent 5-HT6 receptor antagonistic effect with IC50 value of 3.9 μM. Compound 13 also showed good selectivity on the 5-HT6 over 5-HT4 and 5-HT7 receptors.
Novel aryl carbamate derivatives of metronidazole as potential antiamoebic agents
Hayat Faisal,HUSSAIN MUSTATAB WAHEDI,Seonghyeok Park,Saba Tariq,Amir Azam,신동윤 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.1
A series of novel aryl carbamate derivatives of metronidazole (MNZ) were designed, synthesized, and screened for antiamoebic activity. As compared to MNZ, most of the derivatives exhibited moderate to excellent activity against the HM1:IMSS strain of Entamoeba histolytica. Compounds 7, 14, 16, 19, and 21 exhibited the most promising antiamoebic activity with IC50 values of 0.24, 0.08, 0.26, 0.26, and 0.15 lM, respectively, compared to that of MNZ (1.78 lM). Moreover, from the toxicological studies of these compounds on human melanocytes, the melan-a cell line revealed that the potent compounds are nontoxic at concentrations ranging from 2.5 to 50 lM.
Hayat Faisal,Bai Yang,Iqbal Shahid,Ma Chengdong,Ali Muhammad Moaaz,Shahid Muhammad Adnan,Hasan Mahmood Ul,Mosa Walid F. A.,Khan Ummara,Xiao Huang,Gao Zhihong 한국원예학회 2023 Horticulture, Environment, and Biotechnology Vol.64 No.5
Indole-3-acetic acid (IAA) is an important plant hormone required for various plant growth and developmental activities. YUCCA proteins are the enzymes for IAA synthesis that catalyze the rate-limiting step. However, the YUCCA gene family in Japanese apricot has not been thoroughly characterized. Here, we investigated the eff ect of rootstocks on scion growth of Japanease apricot and genes involved in auxin biosynthesis ( YUCCA ). Growth characteristics revealed that the height of ‘Longyan’ [ Prunus mume Sieb. et Zucc] plants with P. mume rootstock were signifi cantly shorter than ‘Longyan’ plants with P. persica rootstock. This study isolated 13 PmYUCCA genes from the Japanese apricot genome. Bioinformatics and expression studies were undertaken to investigate the functions and characteristics of YUCCA genes. The physicochemical properties, gene structure, conserved domains, conserved motif, and phylogenetic relationships of YUCCA genes were determined using bioinformatics analysis. Likewise, we analyzed the expression of PmYUCCA genes in Japanese apricot’s leaf and stem-bark (scion). The expression levels of PmYUCCA3 and PmYUCCA5 genes were noticeably lower in the leaves of ‘Longyan’/ P. mume graft combination than that of the ‘Longyan’/ P. persica graft combinations, suggesting their distinct roles in regulating growth vigor. This research explores the genome-wide identifi cation, characterization, and possible relationship between growth vigor and expression profi le analysis of the YUCCA gene family in Japanese apricot.