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Doan Minh Sang Ik Ho Na Dr. Duong Tien Anh Do Thi Mai Dung Nguyen Thi Thu Hang Nguyen T. Phuong-Anh Assoc. Prof. Dr. Pham-The Hai Assoc. Prof. Dr. Dao Thi Kim Oanh Dr. Truong Thanh Tung Soo Jung Lee Joo Hee Kwon Prof. Dr. Jong Soon Kang Prof. Dr. Sang-Bae Han Assoc. Prof. Dr. Dinh Thi Thanh Hai Prof. Dr. Nguyen-Hai Nam 《化学与生物多样性》2023,20(5):e202201030
Herein, we report the design, synthesis and evaluation of novel (E)-3-(3-oxo-4-substituted-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-N-hydroxypropenamides ( 4 a – i , 7 a – g ) targeting histone deacetylases. Three human cancer cell lines were used to test the cytotoxicity of the synthesized compounds (SW620, colon; PC-3, prostate; NCI−H23, lung cancer); inhibitory activity towards HDAC; anticancer activity; as well as their impact on the cell cycle and apoptosis. As a result, compounds 4 a – i bearing the alkyl substituents seemed to be less potent than the benzyl-containing compounds 7 a – g in all biological assays. Compounds 7 e – f were found to be the most active HDAC inhibitors with IC50 of 1.498±0.020 μM and 1.794±0.159 μM, respectively. In terms of cytotoxicity and anticancer assay, 7 e and 7 f also showed good activity with IC50 values in the micromolar range. In addition, the cell cycle and apoptosis of SW620 were affected by compound 7 f in almost a similar manner to that of reference compound SAHA. Docking assays were carried out for analysis the binding mode and selectivity of this compound toward 8 HDAC isoforms. Overall, our data confirmed that the inhibition of HDAC plays a pivotal role in their anticancer activity. 相似文献
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Era is a highly conserved GTPase essential for bacterial growth. The N-terminal part of Era contains a conserved GTPase domain, whereas the C-terminal part of the protein contains an RNA- and membrane-binding domain, the KH domain. To investigate whether the binding of Era to 16S rRNA and membrane requires its GTPase activity and whether the GTPase domain is essential for these activities, the N- and C-terminal parts of the Streptococcus pneumoniae Era - Era-N (amino acids 1-185) and Era-C (amino acids 141-299), respectively - were expressed and purified. Era-C, which had completely lost GTPase activity, bound to the cytoplasmic membrane and 16S rRNA. In contrast, Era-N, which retained GTPase activity, failed to bind to RNA or membrane. These results therefore indicate that the binding of Era to RNA and membrane does not require the GTPase activity of the protein and that the RNA-binding domain is an independent, functional domain. The physiological effects of the overexpression of Era-C were assessed. The Escherichia coli cells overexpressing Era and Era-N exhibited the same growth rate as wild-type E. coli cells. In contrast, the E. coli cells overexpressing Era-C exhibited a reduced growth rate, indicating that the overexpression of Era-C inhibits cell growth. Furthermore, overexpression of era-N and era-C resulted in morphological changes. Finally, purified Era and Era-C were able to bind to poly(U) RNA, and the binding of Era to poly(U) RNA was significantly inhibited by liposome, as the amount of Era bound to the RNA decreased proportionally with the increase of liposome in the assay. Therefore, this study provides the first biochemical evidence that both binding sites are overlapping. Together, these results indicate that the RNA- and membrane-binding domain of Era is a separate, functional entity and does not require the GTPase activity or the GTPase domain of the protein for activity. 相似文献
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本研究采用EBV-EA诱导抑制实验的方法,对40种蔬菜,60个品种,共150个样品的防癌抗促作用效果进行了筛选与比较,其中具有中等以上抑制活性的样品117个,占样品总数的78%,尤其以非洲野苋菜、辣椒、羽衣甘蓝、山药芋头、苦瓜及紫苏、罗勒等一些芳香莱的效果较好。不同品种、不同植株部位、不同提取方法以及不同产地,对蔬菜的抗促活性也有影响,值得进一步研究。 相似文献
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良种茶树芽叶中氨基酸研究 总被引:2,自引:0,他引:2
黄秋转 《氨基酸和生物资源》1996,18(1):13-15
本文报导利用日立-EG型氨基酸自动分析仪测定的六个茶树良种芽叶中十九种氨基酸组成情况,并以此为依据对良好的品质风格进行了探讨。 相似文献
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甜玉米籽实含糖量的配合力分析 总被引:2,自引:0,他引:2
乔春贵 王玉兰 禹航 马景勇 王思远 张连发QIAO Chun-Gui WANG Yu-Lan YU Hang MA Jing-Yong WANG Si-Yuan 《遗传》1995,17(4):25-27
采用不完全双列杂交设计研究了 6个母本3个父本甜玉米自交系籽实含糖量的配合力效应。结果表明,父母本一般配合力和特殊配合力效应均方都显著。根据各亲本的表现把亲本5033归为一般配合力高而特殊配合力方差大的最理想类型;亲本5012和5011属一般配合力高而特殊配合力方差小的类型;亲本5018、5034、5028和5024为一般配合力低,但特殊配合力方差高的类型; 亲本5023和5009属一般配合力效应和特殊配合力方差都低的类型,最缺少实用价值。 相似文献
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Baked-bean waste was found to be a favorable substrate for amylase production by Aspergillus foetidus NRRL 337. Under optimum conditions, the yields of α-amylase (EC 3.2.1.1) and glucoamylase (EC 3.2.1.3) were 47 and 226 U, respectively, per ml of the waste fermented. 相似文献