非甾体抗炎镇痛药的研究和应用进展

抗炎镇痛药是一类具有抗炎、解热、镇痛及抗风湿作用的常用药物.由于此类药具有糖皮质激素类(甾体类)样抗炎、抗风湿作用,但又与甾体类化学结构不同,故此类药物又称非甾体类抗炎镇痛药(nonsteroidal antiinflammatory drugs,NSAIDs).     

来曲唑促排卵的应用进展

芳香化酶是细胞色素P450酶复合物,是CYP19基因产物,催化雄烯二酮和睾酮转化为雌酮和雌二醇,是雌激素合成的限速酶。芳香化酶抑制剂分为甾体类和非甾体类。来曲唑（letrozole,LE）是第三代非甾体类芳香化酶抑制剂,通常用于乳腺癌等雌激素依赖性肿瘤的治疗。1999年Mitwally等首次将LE用于不孕妇女的促排卵治疗。随着LE在辅助生殖临床上的逐渐应用,LE已有取代克罗米酚（clomepheneci-trate,CC）成为一线促排卵药物的趋势。     

天然资源型化合物甾体皂苷元的化学研究

甾体皂苷元是一类重要的天然资源型化合物，它们已经被作为合成甾体药物的基本原料之一。为了能够实现高效、洁净并以“原子经济性”方式利用这类化合物资源，作者课题组系统地研究了甾体皂苷元的氧化降解反应。通过研究提供了用30%双氧水作为氧化试剂分别氧化伪甾体皂苷元和甾体甾苷元成为相应的孕烯酮醇、孕甾三醇、甾体-22-酸内酯以及系列含甲基侧链的双官能团手性合成试剂的实用方法和技术，进一步还研究了甾体皂苷元氧化降解产物在甾体药物、天然甾体活性分子和非甾体功能手性分子合成中的应用。作者课题组研究了甾体皂苷元螺环缩酮的溴代开环、胺代开环、内酯化溴代等反应，为利用甾体皂苷元完整骨架高效合成一些具有胆固醇基本结构的中药活性成分和具有重要生物活性的天然甾体化合物提供了新的思路和方法。     

非甾体类抗炎药临床新进展

<正>非甾体类抗炎药是一类具有解热、镇痛,多数还有抗炎、抗风湿作用的药物,故也称为解热镇痛抗炎药。由于这一类药物其化学结构中缺乏糖皮质激素甾体抗炎药(SAIDS)所具有的甾环,故称为非甾体类抗炎药(NSAIDS)。它具有解热、镇痛和抗炎作用,是治疗风湿性疾病的一线药物。对于一些风湿性疾病,如早期类风湿关节炎、老年性关节炎及早期强直性脊柱炎等是首选药物。     

化妆品中性激素的分析方法研究进展

一、概述 性激素是由动物体的性腺以及胎盘,肾上腺皮质网状带等组织合成的甾体激素,具有促进性器官成熟,副性征发育及维持性功能等作用。根据生理功能,性激素分为雌激素、雄激素（包括蛋白同化激素）和孕激素三大类（表1）;根据化学特点分为游离体性激素和结合体性激素。另外目前还有很多人工合成的性激素,临床应用较多的比如己烯雌酚。     

持续无排卵与外周内分泌失调

生理情况下,有两条途径调节体循环中性甾体激素(雌激素、雄激素和孕激素)的浓度,一条是通过与特异性结合球蛋白结合而不起生物反应,另一条是甾体激素在腺外转换,二者起缓冲作用,共同调节有生物活性的甾体激素的种类和数量,对靶器官起作用,以维持下丘脑-垂体-卵巢系统的平衡. 某些病理情况下.雄激素在外周向雌激素转化增     

性激素的临床应用(一)

一、国内、外常用制剂 (一)雌激素制剂过去根据化学结构将雌激素分成两大类:一类属于天然雌激素,以雌二醇为代表;另一类属合成雌激素,以己烯雌酚为代表。近年来,对于雌激素的作用机理作了深入研究后,发现上述分类并不符合雌激素的药理性能。所以目前趋向将雌激素制剂按下述分成4类。事实上,现代的各种雌激素制剂多数是合成的,下述分类是根据药理性能划分的: 1.天然雌激素相当于卵巢所分泌的三种雌     

浅析消炎药与抗菌药

消炎药指的是解热镇痛抗炎药,它是一类具有解热、镇痛,多数还有抗炎、抗风湿作用的药物.由于其化学结构和抗炎机制与糖皮质激素甾体抗炎药(SAIDS)不同,故称为非甾体类抗炎药(NSAIDS).抗菌药是对细菌具有抑制或杀灭作用,包括抗生素和人工合成抗菌药(喹诺酮类、磺胺类等).抗生素指某些微生物(细菌、真菌等)产生的具有抗病原体作用和其他活性的一类物质.     

肝脏X受体与炎症反应

人类基因组分析发现在人体细胞核内存在一类具有基因调控作用的核受体(nuclear receptor).核受体家族包括48个成员,分为甾体类和非甾体类.前者有12种,包括雌激素和雄激素受体,以同源二聚体的形式与靶基因结合发挥作用.后者有36种,包括肝X受体(liver X receptors,LXRs)、过氧化物酶体增殖物激活受体(peroxisome proliferatoractivated receptors,PPARs)等,主要通过与类固醇X受体(retinoid X receptors,RXRs)形成异源二聚体调控靶基因的转录.     

阿司匹林哮喘的诊断治疗

由于服用以阿司匹林为代表的非甾体类抗炎药而引发的哮喘被统称为阿司匹林哮喘(aspirin-induced asthma,AIA),也有将其称为阿司匹林敏感性哮喘(aspirin-sensitive asthma)、阿司匹林不耐受性哮喘(aspirin-intolerant asthma)或非甾体类抗炎药性鼻炎和哮喘(NSAID-induced rhirdtis and asthma)等.     

Estrogen and its signaling pathway in non-small cell lung cancer(NSCLC)

Lung cancer is the most common cancer in the world. It is a highly lethal disease in women and men, and new treatments are urgently needed. Several studies have implicated a role of estrogens and estrogen receptors in lung cancer progression. This review will investigate the biological significance of estrogens in lung cancer cells, the expression and molecular mechanisms of estrogen receptors(ERαand ER β, elucidate the prognostic significance of estrogens and their receptors in lung carcinomas and provide ...     

Analysis of the ERalpha germline PvuII marker in breast cancer risk.

BACKGROUND: Prolonged exposure to estrogens was found to be a risk factor for breast cancer. The molecular mechanism has been suggested to be the binding of estrogen receptors in mammary tissue, which promotes the proliferation of breast tissue. Different biomarkers mapping estrogen receptor alpha (ESR1) have been associated with breast cancer risk, although the size of the effect is not consistent among different reports. Variation in the estrogen receptor gene PvuII has been associated with an increased risk of developing breast cancer. However, some studies suggest that its effect might be constrained to a definite subgroup of patients. MATERIAL/METHODS: In this study the involvement of PvuII in breast cancer was analyzed in an independent sample of 444 unrelated breast cancer cases and 704 controls of Spanish origin. A case-control comparison was performed and the genotype distributions examined according to different tumor and population parameters. RESULTS: A trend towards association was observed in adjusted case-control association analysis (p=0.07). PvuII was associated with the familial forms of breast cancer (OR=3.81, p=0.02). T allele frequency was higher among patients with highly differentiated tumors (p=0.02), positive for steroid receptors (p=0.06), and negative for p53 (p=0.02). However, the PvuII genetic background did not affect disease-free survival time (p=0.65). CONCLUSIONS: The PvuII T allele may be a germline risk factor for familial forms of breast cancer and is associated with a specific subset of immunohistochemical tumor phenotype.     

Combined collision-induced dissociation and photo-selected reaction monitoring mass spectrometry modes for simultaneous analysis of coagulation factors and estrogens

Oral estrogens are directly associated with changes in plasma levels of coagulation proteins. Thus, the detection of any variation in protein concentrations due to estrogen contraceptives, by a simultaneous analysis of both coagulation proteins and estrogens, would be a very informative tool. In the present study, the merit of photo-selected reaction monitoring (SRM), a new analytical tool, was evaluated towards estrogens detection in plasma. Then, SRM and photo-SRM detection modes were combined for the simultaneous analysis of estrogen molecules together with heparin co-factor and factor XIIa, two proteins involved in the coagulation cascade. This study shows that photo-SRM could open new multiplexed analytical routes.     

雌激素神经保护作用研究进展

近年来,雌激素的神经保护作用日益受到关注,大量研究数据表明雌激素在神经保护中的作用,然而,其调控的分子机制尚不清楚。本文综述了雌激素的神经保护作用及其可能发挥神经保护作用相关机制的资料,包括经典的雌激素受体介导途径,MAPK信号转导的激活途径,直接减弱谷氨酸受体活化,抗氧化活性机制,线粒体功能调节机制等。雌激素是调节多方面神经功能的多方位激素,尚未有单一的作用机制能够阐明雌激素的神经保护作用。     

The postmenopausal estrogen/breast cancer controversy.

OBJECTIVE--To provide an overview of the postmenopausal estrogen/breast cancer controversy emphasizing the sources of disagreement in the literature and their clinical and research implications. DATA SOURCE AND SELECTION--A MEDLINE search of the English-language literature and a review of bibliographies of meta-analyses describing the association between postmenopausal estrogen use and breast cancer risk. DATA EXTRACTION--Twenty-four original articles and three meta-analyses were reviewed. In addition, five studies that attempted to minimize detection bias were reviewed to assess the potential role of this bias on risk estimates. DATA SYNTHESIS--Among the original articles, risk estimates ranged from a protective to an adverse effect in women who ever used estrogens; no consistent quantitative effects of estrogens on breast cancer risk were found. In the meta-analyses, summary risk estimates were not significantly elevated in women who ever used estrogen. Findings from European-based studies may account for the increased risk associated with increasing duration of use reported in one meta-analysis. In studies that controlled for detection bias, risk estimates were 1 or less in the ever-used category; there was no consistent effect across other categories of use. CONCLUSION--These findings do not support an overall increased risk of breast cancer in women who ever used postmenopausal estrogens or a conclusive or consistent effect across other measures of use. Cross-national differences in estrogen use and inequalities in breast cancer detection between estrogen users and nonusers may account for the increased risk estimates reported in some studies. Newer estrogen and progestin-opposed regimens need to be evaluated further.     

重度宫腔黏连患者宫腔黏连分离术后雌激素的应用效果

目的:探讨重度宫腔黏连(IUA)患者行宫腔镜宫腔黏连分离术(TCRA)后应用雌激素的疗效。方法:95例行TCRA术的重度IUA患者,术后辅以不同剂量(0.625、1.250、1.975和2.500mg/d)及疗程(用药1～3个月经周期和≥4个月经周期)雌激素治疗为观察组,20例未服用任何雌激素患者为对照组。随访2组术后月经改善情况、宫腔再黏连情况、用药不良及妊娠情况。结果:观察组与对照组的月经改善率和宫腔再黏连率差异有统计学意义(χ2=14.446和4.876,P<0.05)。不同剂量和疗程雌激素应用的月经改善率、宫腔再黏连率和妊娠率差异无统计学意义(P>0.05)。剂量和疗程对重度IUA患者术后月经改善、宫腔再黏连和妊娠无影响(P>0.05)。结论:重度IUA患者TCRA术后应用雌激素是有效预防黏连的方法;不同剂量、疗程雌激素对TCRA术后预防IUA效果相同。     

Systemic absorption and sustained effects of vaginal estrogen creams.

Systemic absorption and sustained effects of two estrogen vaginal cream preparations (Premarin and Estrace) were measured in 29 postmenopausal women receiving daily applications. With both preparations, vaginal absorption of estrogens into the systemic circulation was rapid, efficient, and sustained. It is apparent that estrogen vaginal cream preparations, as widely used in clinical practice for their local effects on the vaginal mucosa, actually result in sustained high estrogen levels in the systemic circulation. The vaginal route shows promise when systemic estrogen therapy is indicated, but is dangerous when estrogen is contraindicated.     

Postmenopausal vaginal bleeding during estrogen therapy

Opinions on whether dilatation and curettage is justified in the case of vaginal bleeding in postmenopausal women taking estrogens are presented. Postmenopausal bleeding induced by estrogens usually stops after cessation of treatment, while bleeding due to endometrial cancer usually recurs or continues after cessation of estrogen therapy. Since endometrial cancer may become "silent" after initial bleeding, dilatation and curettage is indicated in all cases of postmenopausal vaginal bleeding, irregardless of estrogen therapy.     

Endometrial cancer in relation to patterns of menopausal estrogen use.

Female residents of King County, Washington, in whom endometrial cancer developed between January 1975 and April 1976 were interviewed concerning prior use of menopausal estrogens. Their responses were compared with those of a random sample of women from the same population. Among current estrogen users, endometrial cancer risk was strongly related to duration of use; although only a minimal elevation of risk was present during the first two years, there was a rapid rise to a 20-fold excess after about ten to 15 years. Cessation of estrogen use led to a decline in incidence of endometrial cancer within several years, but the risk remained higher than in nonusers through the first decade after administration of the drug was stopped. Risk was elevated whether or not the regimen was cyclic and whether conjugated or other types of estrogens had been used. Dosages of less than 0.625 mg/day of conjugated estrogens produced a smaller increase in risk than did other dosages.     

Modulation of uterine contractility and peristalsis by oxytocin in estrogen-primed non-pregnant swine uteri

Oxytocin is one of the most potent uterotonic agents and is known to fluctuate throughout the menstrual cycle, showing an increase during sexual stimulation and arousal, with a peak during orgasm in women. To date, limited data are available on the effects of oxytocin on the regulation of uterine contractility and transport mechanisms in human reproduction. The goal of this study was to evaluate the effects of oxytocin on uterine contractility and peristalsis in estrogen-primed non-pregnant uteri. In an extracorporeal perfusion model of the swine uterus the effect of dynamic changes in uterine contractility and peristalsis in response to oxytocin and estrogen administration was observed. Spontaneous uterine contractility and oxytocin-induced uterine contractility and peristalsis with and without estrogen perfusion were assessed using an intrauterine double-chip microcatheter. Spontaneous peristalsis and oxytocin induced contraction waves without estrogen perfusion resulted in a slightly higher intrauterine pressure in the isthmus uteri in comparison with the corpus uteri, while the peristaltic waves were seen to start mostly in the corpus uteri, moving in the direction of the cervix. While after estrogen perfusion oxytocin produced a significant increase in intrauterine pressure in the isthmus uteri compared to the corpus uteri, and 80% of the peristaltic waves started in the isthmus uteri, moving in the direction of the corpus uteri. This observation strengthens the view that oxytocin is able to support directed transport mechanism in the female genital tract only in the presence of estrogens. The biological role of oxytocin increase during sexual stimulation and arousal with a peak during orgasm for the mechanisms of reproduction may be to stimulate directed uterine transport mechanisms in the presence of estrogens.