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991.
花椒属植物生物碱研究进展 总被引:3,自引:0,他引:3
花椒属植物全世界约有250种,我国约有39种14变种。近年来研究发现花椒属植物生物碱具有多种药理作用与临床功能,现就近20年来花椒属生物碱和花椒生物碱的提取、分离、测定方法以及其药理作用等研究作一综述。 相似文献
992.
993.
Hongbo Shen ;Yanping Yang ;Feifei Wang ;Ying Zhang ;Naihao Ye ;Shengfeng Xu ;Honghai Wang 《Acta biochimica et biophysica Sinica》2009,(5):379-388
The increasing emergence of drug-resistant tuberculosis (TB) poses a serious threat to the control of this disease. It is in urgent need to develop new TB drugs. Tryptophan biosynthetic pathway plays an important role in the growth and replication of Mycobacterium tuberculosis (Mtb). The β-subunit of tryptophan synthase (TrpB) catalyzes the last step of the tryptophan biosynthetic pathway, and it might be a potential target for TB drug design. In this study, we overexpressed, purified, and characterized the putative TrpB-encoding gene Rv1612 in Mtb H37Rv. Results showed that Mtb His-TrpB optimal enzymatic activity is at pH 7.8 with 0.15 M Na^+ or 0.18 M Mg^2+ at 37℃. Structure analysis indicated that Mtb TrpB exhibited a typical β/α barrel structure. The amino acid residues believed to interact with the enzyme cofactor pyridoxal-5'-phosphate were predicted by homology modeling and structure alignment. The role of these residues in catalytic activity of the Mtb His-TrpB was confirmed by site-directed mutagenesis. These results provided reassuring structural information for drug design based on TrpB. 相似文献
994.
Independence of stem and leaf hydraulic traits in six Euphorbiaceae tree species with contrasting leaf phenology 总被引:1,自引:0,他引:1
Hydraulic traits and hydraulic-related structural properties were examined in three deciduous (Hevea brasiliensis, Macaranga denticulate, and Bischofia javanica) and three evergreen (Drypetes indica, Aleurites moluccana, and Codiaeum variegatum) Euphorbiaceae tree species from a seasonally tropical forest in south-western China. Xylem water potential at 50% loss of
stem hydraulic conductivity (P50stem) was more negative in the evergreen tree, but leaf water potential at 50% loss of leaf hydraulic conductivity (P50leaf) did not function as P50stem did. Furthermore, P50stem was more negative than P50leaf in the evergreen tree; contrarily, this pattern was not observed in the deciduous tree. Leaf hydraulic conductivity overlapped
considerably, but stem hydraulic conductivity diverged between the evergreen and deciduous tree. Correspondingly, structural
properties of leaves overlapped substantially; however, structural properties of stem diverged markedly. Consequently, leaf
and stem hydraulic traits were closely correlated with leaf and stem structural properties, respectively. Additionally, stem
hydraulic efficiency was significantly correlated with stem hydraulic resistance to embolism; nevertheless, such a hydraulic
pattern was not found in leaf hydraulics. Thus, these results suggest: (1) that the evergreen and deciduous tree mainly diverge
in stem hydraulics, but not in leaf hydraulics, (2) that regardless of leaf or stem, their hydraulic traits result primarily
from structural properties, and not from leaf phenology, (3) that leaves are more vulnerable to drought-induced embolism than
stem in the evergreen tree, but not always in the deciduous tree and (4) that there exists a trade-off between hydraulic efficiency
and safety for stem hydraulics, but not for leaf hydraulics. 相似文献
995.
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents
Saleem Ahmad Khehyong Ngu Keith J. Miller Ginger Wu Chen-pin Hung Sarah Malmstrom Ge Zhang Eva O’Tanyi William J. Keim Mary Jane Cullen Kenneth W. Rohrbach Michael Thomas Thao Ung Qinling Qu Jinping Gan Rangaraj Narayanan Mary Ann Pelleymounter Jeffrey A. Robl 《Bioorganic & medicinal chemistry letters》2010,20(3):1128-1133
Agonists of the 5-HT2C receptor have been shown to suppress appetite and reduce body weight in animal models as well as in humans. However, agonism of the related 5-HT2B receptor has been associated with valvular heart disease. Synthesis and biological evaluation of a series of novel and highly selective dihydroquinazolinone-derived 5-HT2C agonists with no detectable agonism of the 5-HT2B receptor is described. Among these, compounds (+)-2a and (+)-3c were identified as potent and highly selective agonists which exhibited weight loss in a rat model upon oral dosing. 相似文献
996.
Jared Cumming Suresh Babu Ying Huang Carolyn Carrol Xia Chen Leonard Favreau William Greenlee Tao Guo Matthew Kennedy Reshma Kuvelkar Thuy Le Guoqing Li Nansie McHugh Peter Orth Lynne Ozgur Eric Parker Kurt Saionz Andrew Stamford Corey Strickland Dawit Tadesse Qi Zhang 《Bioorganic & medicinal chemistry letters》2010,20(9):2837-2842
With collaboration between chemistry, X-ray crystallography, and molecular modeling, we designed and synthesized a series of novel piperazine sulfonamide BACE1 inhibitors. Iterative exploration of the non-prime side and S2′ sub-pocket of the enzyme culminated in identification of an analog that potently lowers peripheral Aβ40 in transgenic mice with a single subcutaneous dose. 相似文献
997.
Yong Ling Xiaolei Ye Hui Ji Yihua Zhang Yisheng Lai Sixun Peng Jide Tian 《Bioorganic & medicinal chemistry》2010,18(10):3448-3456
Novel furoxan-based nitric oxide (NO)-releasing derivatives (11a–p) of farnesylthiosalicylic acid (FTA) were synthesized. Compounds 11d, 11f, 11k, and 11m–o displayed anti-tumor activities superior to FTA and sorafenib in most cancer cells tested. Analysis of six compounds revealed that 11d, 11f, 11n, 11o, and 11p, but not 11a that had low anti-tumor activity, produced high levels of NO, associated with their strong anti-tumor activity. Furthermore, the anti-tumor activity of 11f was partially mimicked by the furoxan moiety, but reduced by pre-treatment with hemoglobin. Importantly, treatment with 11f inhibited Ras-related signaling in cancer cells. Apparently, the high anti-tumor activity of 11f was attributed to the synergic effect of high levels of NO production and inhibition of Ras-related signaling in cancer cells. Our findings suggest that the furoxan/FTA hybrids may hold greater promise as therapeutic agents for the intervention of human cancers. 相似文献
998.
生长激素受体(growth hormone receptor,GHR)是细胞因子/造血因子受体超级家族的一员。它通过二聚体的形式和生长激素(growth hormone,GH)相结合,然后诱发Janus激酶2(Janus kinase 2,JAK2)等细胞因子酪氨酸磷酸化并通过4条不同的途径将信号传入细胞内从而产生一系列的生理效应。现在了解GHR的结构特征、组织分布的基础上,对其介导的信号转导途径作进一步的阐明。 相似文献
999.
一种利用STO饲养层细胞制备拟胚体的新方法 总被引:2,自引:0,他引:2
建立了一种利用STO饲养层细胞制备拟胚体的新方法。该方法选用生长至80%饱和密度的STO细胞,经丝裂霉素C(10 mg/ml)处理4 h后以8×104 cm-2的密度接种培养12 h,制备饲养层,再将ES-D3细胞以1×104 cm-2的密度接种其上,首先用含mLIF的DMEM培养液培养24 h,再更换拟胚体诱导培养液,5~9天后获得了各成熟阶段的拟胚体。形态结构和分化潜能等研究表明,该方法制备的拟胚体结构典型,具有产生3个胚层谱系来源的功能细胞的潜能。与传统拟胚体制作方法如悬滴培养法相比,具有操作简便,拟胚体形成率高,重复性好等优点,是开展哺乳动物早期胚胎发育和干细胞分化研究的理想工具。 相似文献
1000.
非点源污染物在沟渠湿地中的累积和植物吸收净化 总被引:21,自引:0,他引:21
对有机质和总氮在沟渠湿地底泥中的垂直分布和水平分布的研究表明,40 cm以下深度的芦苇(Phragmites communis)和茭草(Zizania latifolia)湿地底泥对有机质和总氮有显著的持留和累积作用;但表层底泥中含量随季节变化大,最高与最低值相差近2倍以上.有机质和总氮之间有极显著的相关关系,在芦苇和茭草湿地底泥中的相关系数分别为0.9876和0.9335.水体中总氮与NH4+-N和NO3-N也显著相关,表明总氮的主要成分是有机氮,其矿化作用是无机氮的重要来源.每年秋季芦苇收割以后,可带走氮818 kg·hm-2和磷103.6 kg·hm-2,茭草可带走氮131 kg·hm-2和磷28.9 kg·hm-2.茭白对氮的吸收能力高,试验表明,利用茭白取代野生植物,既能取得很好的净化效果,又可被农民主动回收,解决植物的二次污染问题. 相似文献