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17aα-D-高炔雌二醇-3-乙酯对辐射和化学损伤小鼠的防护作用及其雌活性的实验研究 被引量:1
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作者 周则卫 沈秀 +3 位作者 唐卫生 吴小霞 王月英 张良安 《辐射防护》 CAS CSCD 北大核心 2008年第4期221-225,共5页
采用我所自行合成的新型雌激素类化合物17aα-D-高炔雌二醇-3-乙酯,观察其对受致死剂量(8.0 Gy)137Csγ射线照射IRM-2小鼠30 d存活率的影响,以及药物对注射环磷酰胺(CY)所致的IRM-2小鼠造血系统损伤的保护作用,比较了其与炔雌二醇(EE2)... 采用我所自行合成的新型雌激素类化合物17aα-D-高炔雌二醇-3-乙酯,观察其对受致死剂量(8.0 Gy)137Csγ射线照射IRM-2小鼠30 d存活率的影响,以及药物对注射环磷酰胺(CY)所致的IRM-2小鼠造血系统损伤的保护作用,比较了其与炔雌二醇(EE2)对昆明种雌性小鼠的雌活性。结果表明,5 mg/kg7、.5 mg/kg、10 mg/kg三个不同剂量17aα-D-高炔雌二醇-3-乙酯药物注射组,30 d存活率分别比单纯照射对照组提高55%、85%、75%(p<0.01),保护指数分别为1.99、2.56、2.46;同时,药物可明显保护环磷酰胺所致的小鼠造血系统功能的损伤。与EE2相比,该药物雌活性约为其1/10000。因此,17aα-D-高炔雌二醇-3-乙酯对γ射线及化学药物损伤均有明显的保护作用,而且该药的雌活性低,毒副作用小。 展开更多
关键词 17aα-D-高炔二醇-3-乙酯 二醇 辐射损伤防护 药理活性 雌活性
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雌二醇衍生物分子结构与雌激素受体的亲和力及雌活性构效关系的分析
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作者 徐文富 汤仲明 王志清 《临床军医杂志》 CAS 1994年第1期1-3,共3页
雌激素和受体的相互作用表现出高度的亲和性特异性,可在离体简单体系中显示出来.为此利用标记雌二醇[<sup>3</sup>H]E<sub>2</sub>与家兔胞液受体结合的实验模型,研究了雌二醇衍生物对这种结合反应的竞争性抑... 雌激素和受体的相互作用表现出高度的亲和性特异性,可在离体简单体系中显示出来.为此利用标记雌二醇[<sup>3</sup>H]E<sub>2</sub>与家兔胞液受体结合的实验模型,研究了雌二醇衍生物对这种结合反应的竞争性抑制作用和对小鼠子宫增重雌活性作用,总结了40多种衍生物的构效关系. 展开更多
关键词 二醇衍生物 激素受体 雌活性构效关系
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Evaluation of Estrogenic Activity and Measurement of EDCs in Wastewater Treatment Plants 被引量:2
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作者 B. C. Lee J. Y. Jung H. K. Kim 《Journal of Ocean University of China》 SCIE CAS 2006年第4期351-356,共6页
Correlations between estrogenic activity and DOC/UV260 ratio in wastewater treatment processes were investigated to propose a simple, reliable and comprehensive indicator for the presence of estrogenic substances. Con... Correlations between estrogenic activity and DOC/UV260 ratio in wastewater treatment processes were investigated to propose a simple, reliable and comprehensive indicator for the presence of estrogenic substances. Contrary to this, when short-term bioassays such as the E-SCREEN, receptor binding and reporter gene expression assays are used for detecting estrogenic activity in the wastewater sample, they require a long time, at least a few days. The major factors contributing to the estrogenic activity were found to be 17β-estradiol (E2) and estrone (El). A good relationship between the DOC/ UV260 ratio and the concentration of estrogens (El and E2) in the effluent of the activated sludge process was found: the E2 concentration increased as the DOC/UV260 ratio increased while the E1 concentration decreased. The relative estrogenic activity and DOC/UV260 ratio showed a good correlation (R^2 = 0.84) for all sewage samples except the ozonized samples in the sewage treatment plants. This study shows that the estrogenic compounds are hard to be mineralized by the conventional biological processes. Advanced oxidation processes are required to further remove estrogenic substances in the secondary effluent. By analysis of DOC and UV260, the estrogenic activity in the wastewater can be rapidly estimated. 展开更多
关键词 activated sludge process estrogenic substances 17Β-ESTRADIOL ESTRONE DOC/UV260
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Dietary zinc and metallothionein on small intestinal disaccharidases activity in mice 被引量:2
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作者 Cuong D Tran Johanna Cool Cory J Xian 《World Journal of Gastroenterology》 SCIE CAS CSCD 2011年第3期354-360,共7页
AIM: To examine the effect of increasing dietary zinc (Zn) intake and the lack of metallothionein (MT) expression on activity of small intestinal disaccharidases. METHODS: MT-Ⅰ and Ⅱ knockout (MT-/-) and wild-type (... AIM: To examine the effect of increasing dietary zinc (Zn) intake and the lack of metallothionein (MT) expression on activity of small intestinal disaccharidases. METHODS: MT-Ⅰ and Ⅱ knockout (MT-/-) and wild-type (MT+/+) female mice at 3.5 wk of age were randomly fed with a diet containing 2 (2 Zn), 15 (15 Zn) or 50 (50 Zn) mg Zn/kg (n = 8/group/genotype) for 5 wk. Small intestinal segments (duodenum, jejunum and ileum) were collected and either fixed in 10% formalin for histological analysis or snap frozen in liquid nitrogen for sucrase, lactase and maltase activity analyses.RESULTS: Plasma Zn was significantly (P < 0.05) lower (33%) in MT-/- compared with MT+/+ mice fed the 2 Zn diet. Villus height and crypt depth were increased by approximately 15% in MT+/+ mice compared with MT-/- mice. Duodenal disaccharidase activities were significantly higher in MT+/+ compared with MT-/- mice particularly in those fed the 2 Zn diet. For the 50 Zn diet, jejunal sucrase and lactase activities were significantly higher in MT-/- (13 313 ± 2314; 4107 ± 364 μmol glucose/well/min/g tissue, respectively) compared with MT+/+ mice (7054 ± 608; 1818 ± 174). Similarly, ileal lactase activities were higher in MT-/- (1480 ± 192) compared with MT+/+ (629 ± 353) mice particularly those fed the 2 Zn diet. CONCLUSION: Increasing dietary Zn has little effect on disaccharidases activity in MT wild-type mice. The presence of MT may enhance morphological and functional development of the gut. 展开更多
关键词 LACTASE MALTASE SUCRASE METALLOTHIONEIN DIET ZINC
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In Vitro Biossay for Assessing Estrogenic Activity of Sewage Treatment Works
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作者 张海珍 陆光华 +2 位作者 计勇 宋文婷 李湘鸣 《Journal of Donghua University(English Edition)》 EI CAS 2009年第6期580-585,共6页
The estrogenic activity of influents and effluents of five municipal sewage treatment works (STWs) in Nanjing was investigated. The water samples were enriched by solid phase extraction, then eluted with different p... The estrogenic activity of influents and effluents of five municipal sewage treatment works (STWs) in Nanjing was investigated. The water samples were enriched by solid phase extraction, then eluted with different polar solvents, and f'mally three fractionated extracts were obtained. Estrogen receptor recombinant yeast screen was used to evaluate the estrogenic activity of individual fractionated extracts and their mixture. The results show that the influents and effluents of the two STWs mainly receiving industrial wastewater have no obvious estrogenic activity, and the water samples from the other three STWs mainly receiving domestic wastewater show different degrees of estrogenic activity. The total estrogenic concentration ranged from 171. 52 ng/L EEQ (E2 - equivalent concentration) to 1 008.37 ng/L EEQ in the influents, and from ND (not detected) to 36.3 ng/L EEQ in the effluents. By comparing the results of different fractionated extracts, the methanol and dichloromethane extracts of the water samples show higher estrogenic activity, while the hexane extracts very low. The (xeno)estrogens from domestic wastewater could be removed obviously by activated sludge treatment units. However, the effluents of STWs in Nanjing still have chemical contaminants capable of binding to estrogen receptors. 展开更多
关键词 sewage treatment works (xeno)estrogens yeast estrogen screening (YES) bioassay
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Effect of Phytoestrogen Activity on hFOB 1.19 Osteoblast Cells of Vanilla Siamensis
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作者 Phenphichar Wanachantararak Juraruk Thongpaeng +2 位作者 Fahsai Kantawong Chuenchit Boonchird Griangsak Chairote 《Journal of Chemistry and Chemical Engineering》 2012年第9期843-852,共10页
The unsaponifiable compounds derived from the fresh green beans of Vanilla siamens& Rol. ex. Dow were assayed for the first time to detect their estrogenic activity. We used a simple screening method using the yeast ... The unsaponifiable compounds derived from the fresh green beans of Vanilla siamens& Rol. ex. Dow were assayed for the first time to detect their estrogenic activity. We used a simple screening method using the yeast two hybrid system based on the binding of a ligand to estrogen receptors. Yeast cells carrying the hER (human estrogen receptor) gene, ERE (estrogen response elements) and lacZ (β-galactosidase gene) are very suitable for screening and sensitive analysis of estrogenic compound. Our results showed that V. siamensis plant extracts bind with relatively affinity to YES- hERa was 2.27-fold the relative potency ofestradiol (E2) in YES-hERa. The effects of phytoestrogen activity on the osteoblast cells were examined on the proliferation of hFOB 1.19 cells and the bone mineralization process. V. siamens& was a positive screening result and induced mineralization ofosteoblasts. This study indicated that V. siamensis plant extract exhibited the characteristic effects of a nature bone promoter compound as phytoestrogen. 展开更多
关键词 Vanilla siamensis PHYTOESTROGEN osteoblast cells.
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