Studies on the mammary tumor-inhibiting effects of diethylstilbestrol and its mono- and diphosphate

Summary Diethylstilbestrol (DES), diethylstilbestrol monophosphate (DES-MP) and diethylstilbestrol diphosphate (DES-DP) were tested for their estrogen receptor affinity, estrogenic potency and mammary tumor-inhibiting activity in vitro and in vivo. DES had a much higher receptor binding affinity than its mono-or diphosphate. All three compounds inhibited the growth of the hormone-dependent MCF-7 and hormone-independent MDA-MB 231 breast cancer line only at relatively high concentrations. The estrogenic potency in the immature mouse uterine weight test decreased in the order DES>DES-MPDES-DP. The hormone-dependent MXT mammary tumor of the mouse was inhibited by all three compounds at a dosage of 1.0 mg/kg per week. At a dose of 0.01 mg/kg, DES, DES-MP, and DES-DP stimulated the tumor growth. Thus, for the first time, a biphasic effect on tumor growth was demonstrated in intact mature animals. As the effects of all three compounds were similar in this assay, a cleavage of the phosphate groups is likely. A decrease in estrogenic potency concomitant with a retained antitumor effect of DES-MP and DES-DP compared to DES was not demonstrable in the mature mouse using the MXT assay, only in the uterotrophic test in the immature mouse.Dedicated to Professor Dietrich Schmähl on occasion of his 60th birthdaySupported by the Deutsche Forschungsgemeinschaft and by the Verband der Chemischen Industrie, Fonds der Chemischen Industrie. The authors thank Dr. Weigert, Asta-Werke AG, Degussa Pharma Gruppe, Bielefeld, FRG, for the analysis of DES-MP and DP     

The effects of ethanol,estrogen, and hexachlorobenzene on the activities of hepatic δ-aminolevulinate synthetase, δ-aminolevulinate dehydratase,and uroporphyrinogen decarboxylase in male rats

To determine if clinically observed disorders in heme biosynthetic enzymes, known as sporadic porphyria cutanea tarda (PCT), could be reproduced in experimental animals, male Fischer rats were treated with ethanol, estrogen and hexachlorobenzene (HCB). A series of heme biosynthetic enzymes were assayed. In the rats given free access to 8% ethanol-drinking water for 15 weeks, -aminolevulinate (ALA) dehydratase was significantly reduced in erythrocytes. In the liver, ALA synthetase and uroporphyrinogen (UROgen) decarboxylase activities remained unchanged. In bone marrow cells, these activities did not change markedly. In the rats treated with estrogen (1 mg estrioltripropionate /rat/week, IM), no body weight gain was observed during the treatment for 15 weeks and urinary ALA excretion increased to 1.7 fold over normal level. In the liver, a significant increase was observed in the activity of ALA dehydratase, but other enzymes remained within the normal level. In bone marrow cells and erythrocytes, ALA dehydratase was also increased. ALA synthetase increased only in bone marrow cells to 2.1 times higher than the control level. In rats fed 0.3% HCB-diet for 8 weeks, urinary excretion of ALA, coproporphyrin and uroporphyrin increased to 2.4, 3.3 and 3.8 times higher than the controls, respectively. In the liver, an increase was observed in ALA synthetase, while a decrease was observed in ALA dehydratase and UROgen decarboxylase. In bone marrow cells and erythrocytes, ALA dehydratase was reduced and activities of other enzymes did not show any changes.These results indicate that alcohol, estrogen and HCB do not produce phenomena similar to those observed clinically in PCT.     

雌孕激素序贯用药治疗流产术后宫腔残留患者的临床价值分析

目的分析雌孕激素序贯用药治疗流产术后宫腔残留患者的临床价值。方法选取2017年1月至2019年12月我站收治的人工流产患者60例,按治疗方式不同分为对照组(28例)和观察组(32例)。对照组采用刮宫治疗,观察组于人工流产术后第7 d行B超检查,观察宫腔残留情况后采用药物治疗。比较两组的临床疗效、并发症。结果两组的总有效率比较无统计学差异(P>0.05)。观察组的腹痛发生率低于对照组,出血时间短于对照组(P <0.05)。结论雌孕激素序贯用药治疗能够有效清除宫腔残留,缩短出血时间,减轻腹痛,有利于重新建立正常的月经周期,促进子宫功能修复,避免再次刮宫对子宫内膜的损伤及手术对患者造成的不良身心应激,具有较高的临床推广价值。     

男性膀胱癌患者血清性激素水平的检测

目的　探讨性激素在膀胱癌发病中的意义。方法 :采用放射免疫法检测 31例男性膀胱癌患者及 2 7例同年龄正常人对照组血清中的雌二醇 (EstradiolE2 )、孕酮 (ProgesteroneP)及睾酮 (TestosteroneT)水平。结果 :男性膀胱癌患者血清E2 、P、T分别为 44.98± 2 0 .96pg ml( x±s) ,0 .37± 0 .18ng ml( x±s) ,6 .2 5± 2 .37ng ml( x±s) ,而正常对照组E2 、P、T分别为 5 6 .0 1± 13.5 0pg ml( x±s) ,1.14± 0 .37ng ml( x±s) ,5 .15± 1.37ng ml( x±s) ,两者比较膀胱癌组T明显高于对照组 (P <0 .0 5 ) ;而E2 、P明显低于对照组 (P <0 .0 5 )。结论 :膀胱癌的发生可能与性激素代谢失衡有一定的关系     

Estrogen and estrogen receptors in kidney diseases

Acute kidney injury (AKI) and chronic kidney disease (CKD) are posing great threats to global health within this century. Studies have suggested that estrogen and estrogen receptors (ERs) play important roles in many physiological processes in the kidney. For instance, they are crucial in maintaining mitochondrial homeostasis and modulating endothelin-1 (ET-1) system in the kidney. Estrogen takes part in the kidney repair and regeneration via its receptors. Estrogen also participates in the regulation of phosphorus homeostasis via its receptors in the proximal tubule. The ERα polymorphisms have been associated with the susceptibilities and outcomes of several renal diseases. As a consequence, the altered or dysregulated estrogen/ERs signaling pathways may contribute to a variety of kidney diseases, including various causes-induced AKI, diabetic kidney disease (DKD), lupus nephritis (LN), IgA nephropathy (IgAN), CKD complications, etc. Experimental and clinical studies have shown that targeting estrogen/ERs signaling pathways might have protective effects against certain renal disorders. However, many unsolved problems still exist in knowledge regarding the roles of estrogen and ERs in distinct kidney diseases. Further research is needed to shed light on this area and to enable the discovery of pathway-specific therapies for kidney diseases.     

胃癌及癌前病变组织中雌激素受体和P21ras的表达及意义

目的 探讨雌激素受体（ＥＲ）和ｒａｓ原癌基因蛋白－Ｐ２ｒａｓ的表达在胃癌发生、发展中的作用及与胃癌生物学行为的关系。方法 采用免疫组化ＳＰ法。结果 ＥＲ在慢性浅表性胃炎（２０例）、异型增生（２１例）中均为阴性,胃癌（４０例）的表达阳性率为４０％,三组比较有显著性差异（Ｉ〈０．０５）。Ｐ２１＾ｒａｓ在慢性浅表性胃炎、异型增生、胃癌的表达阳性率分别为１０％、２３．８％、４７．５％,三组比较差异有显著性     

雌素受体在胃癌细胞的表达和意义

目的 检测雌激素受体（ＥＲ）在胃癌的表达及其与胃癌生物学行为的关系。方法 应用免疫组化Ｓ－Ｐ法。结果 ＥＲ在慢浅表性胃炎、异型增生中表达均为阴性,在胃癌阳性率为４０％,三组 比较比较有显著性差异（Ｐ〈０．０５）。ＥＲ在进展期胃癌的阳性率显著高于早期胃癌（Ｐ〈０．０５）。胃癌有淋巴结转移组的阳性率显著高于无淋巴结转移组（Ｐ〈０．０５）。ＥＲ的表达在分化不良型胃癌高于分化型胃癌,但无统计学意义（Ｐ〉０     

乳腺癌ER,PR检测技术

目的：探讨ＥＲ、ＰＲ的最佳染色条件。方法：应用免疫组化Ｓ－Ｐ法,对乳腺癌进行ＥＲ和ＰＲ检查。结果：实验组：“１”的阳性率高于对照组“２”。结论：成功地显示ＥＲ和ＰＲ关键在于微波修复抗原及组织的固定时间和一抗的作用时间。     

Effects of Mifepristone Compound on the Receptors of Estrogen and Progesterone in Early Pregnancy Deciduas

Mifeprlstone,a norethindrone, is the first synthetic effective steroid which canbind to the progesterone receptor with greater affinity than progesterone, but lacksthe agonistic effect. Its anti--progestin action results in the withdrawal of progesterone at cellular level to interrupt its biological action and can terminate early pregnancy['j. At present, the dose of mifepristone in combination with the analogue ofprostaglandin in terminating early pregnancy is 150 mg-- 200 mg and the complete…