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991.
Beata Morak-Młodawska Krystian Pluta Małgorzata Latocha Małgorzata Jeleń 《Journal of enzyme inhibition and medicinal chemistry》2016,31(6):1132-1138
New derivatives of two isomeric types of azaphenothiazines, 1,8- and 2,7-diazaphenothiazine, containing the triple bond substituents and additionally tertiary cyclic and acyclic amine groups, were synthesized and tested for their anticancer activity. The compounds exhibited differential inhibitory activities. Better results were obtained when the acetylenic group was transformed via the Mannich reaction to the dialkylaminobutynyl groups. The most active was 2,7-diazaphenothiazine with the N-methylpiperazine-2-butynyl substituent against the human ductal breast epithelial tumor cell line T47D, more potent than cisplatin. The 2,7-diazaphenothiazine system turned out to be more active than isomeric 1,8-diaza one. For the most active compound, the expression of TP53, CDKN1A, BCL-2 and BAX genes was detected by the RT-QPCR method. The gene expression ratio BACL-2/BAX suggests the mitochondrial apoptosis in T47D cells. The synthesis makes possible to obtain many new bioactive phenothiazines with the dialkylaminoalkynyl substituents inserting various tertiary cyclic and acyclic amine moieties to the substituents. 相似文献
992.
Deletion of amino acids 1641-2437 from the foot region of skeletal muscle ryanodine receptor alters the conduction properties of the Ca release channel. 总被引:2,自引:0,他引:2 下载免费PDF全文
The ryanodine receptor (RyR) of skeletal muscle contains two functional domains: a carboxyl-terminal hydrophobic domain that forms the putative conduction pore of the calcium release channel, and a large cytoplasmic domain that corresponds to the "foot structure." To understand the contribution of the foot structure to the function of the calcium release channel, we studied a RyR deletion mutant, delta(1641-2437)-RyR, in which a region that is rich in glutamate and aspartate residues (a.a. 1641-2437) was removed. The wild-type and delta(1641-2437)-RyR proteins were expressed in a Chinese hamster ovary (CHO) cell line, and functions of single calcium release channels were measured in the lipid bilayer membrane. The wild-type RyR forms functional calcium release channels with a linear current-voltage relationship similar to that of the native channel identified in the sarcoplasmic reticulum membrane of skeletal muscle, whereas the channels formed by delta(1641-2437)-RyR exhibit significant inward rectification, i.e., currents moving from cytoplasm into SR lumen were approximately 20% less than that in the opposite direction. As in to the wt-RyR channel, opening of the delta(1641-2437)-RyR channel has a bell-shaped dependence on the cytoplasmic calcium, but the calcium-dependent activation and inactivation processes of the delta(1641-2437)-RyR channel are shifted to higher calcium concentrations. Our data show that deletion of a.a. 1641-2437 from the foot region of the skeletal muscle RyR results in changes in both ion conduction and calcium-dependent regulation of the calcium release channel. 相似文献
993.
汞对小麦种子活力和萌发代谢的影响 总被引:8,自引:1,他引:8
研究Hg^2+对小麦种子活力、幼苗生长、呼吸及淀粉酶、脂肪酶和转氨酶活力的影响。结果表明,Hg^2+能抑制种子萌发过程中淀粉酶、脂肪酶和转氨酶活性,抑制幼苗生长和呼吸代谢,降低种子活力,但浓度低时,在萌发初期有短暂促进作用。 相似文献
994.
东亚大都市学生头型的比较研究 总被引:1,自引:1,他引:1
为了研讨居住区域的气候条件和社会经济环境对头型的影响,采用国际通用的人体测量法,调查测量了东亚三个国家四个集团3472名6-17岁学生的头长和头宽,经统计学处理求得其平均值、头指数,回归方程,并作性差和地区差检验,其结果表明:中国大连学生为特圆头型,菲律宾马尼拉学生为圆头型,地理位置在大连和马尼拉之间的日本东京的学生的头型也位于二者之间,生活富裕集团的头长和头宽明显大于生活贫穷集团的学生,但头型二 相似文献
995.
Influence of supplemental ultraviolet-B on indoleacetic acid and calmodulin in the leaves of rice (Oryza sativa L.) 总被引:9,自引:0,他引:9
Shaobai Huang Qiujie Dai Shaobing Peng Arlene Q. Chavez Ma. Lourdes L. Miranda Romeo M. Visperas Benito S. Vergara 《Plant Growth Regulation》1997,21(1):59-64
IR68 and Dular rice cultivars were grown under ambient, 13.0 (simulating 20% ozone depletion) and 19.1 (simulating 40% ozone depletion) kJ m-2 day-1 of biologically effective ultraviolet-B (UV-BBE) for 4 weeks. Plant height and leaf area were significantly reduced by supplemental UV-BBE radiation. Greater reduction in leaf area than of plant height was observed. A decrease in indole-3-acetic acid (IAA) content and increase in peroxidase and IAA oxidase activities of UV-B treated plants in both cultivars were observed compared with ambient control. Calmodulin content also decreased after plants were treated with high supplemental UV-B for two weeks and medium UV-B treatment for four weeks. The results indicated that peroxidase and IAA oxidase activities in rice leaves were stimulated by supplemental UV-B, resulting in the destruction of IAA which in turn may cause inhibition of rice leaf growth. Although the mechanism is unclear, calmodulin is most likely involved in leaf growth. 相似文献
996.
Allelopathy of diterpenoids extracted from plants of the genus Robdosia on three common species of soil ciliates, Colpoda inflata, Colpoda cucullus and Euplotes muscicola, was studied by acute toxicity test, sub-lethal effect test and morphological observation. Acute toxicity test showed that there was remarkable toxicity of the diterpenoids on the individuals of the three soil ciliate species, and there was close correlation between toxicity and concentration of the diterpenoids. 12 h-LC50 values of the diterpenoids on the individuals of C. inflata, C. cucullus and E. muscicola were 161.40 mg L?1, 94.80 mg L?1 and 83.70 mg L?1 respectively, and 24 h-LC50 values were 114.90 mg L?1, 92.30 mg L?1and 65.80 mg L?1 separately. Sub-lethal effect test of soil ciliates suggested that there existed significant inhibition of the diterpenoids on population growth of the three ciliates with dose-dependant relationships, population density and growth rate of the test group was obviously lower than that of the control group. Morphological observation indicated that diterpenoids affected the body shapes of the three ciliates and made them shorter and thicker, and the higher the concentration of diterpenoids, the greater the affection. The results are of great significance for understanding the functions of ciliates and their relationships to other organisms, and for the application of allelopathy in biological pest control in the soil ecosystems. 相似文献
997.
998.
基于图像几何变换映射的色盲矫正方法 总被引:1,自引:0,他引:1
为了提高色盲患者分辨色彩的能力,提出了基于图像几何变换映射的色盲矫正方法。首先根据图像中颜色面两侧的颜色比例对颜色空间各个平面进行相应的几何变换,进而划分不同的颜色映射区域,通过颜色变换,生成色盲患者较易分辨颜色的图像。实验表明,该方法可以改善色盲患者对原本难以区分的颜色的分辨能力,同时计算速度快,有望满足实时处理的需要,性能上优于已有的方法。 相似文献
999.
1000.