• 【腹内侧下丘脑核病变破坏了雌性雪貂的嗅觉伴侣识别和接受能力。】 复制标题 收藏 收藏
    DOI:10.1016/j.yhbeh.2006.08.009 复制DOI
    作者列表:Robarts DW,Baum MJ
    BACKGROUND & AIMS: :Previous research showed that ferrets of both sexes rely on the perception of conspecifics' body odors to identify and motivate approach towards opposite-sex mating partners, and exposure to male body odors stimulated Fos expression in an olfactory projection circuit of female, but not male, ferrets that terminates in the ventromedial hypothalamic nucleus (VMH). We asked whether the female-typical preference of ferrets to approach male as opposed to female body odors in Y-maze tests would be disrupted by VMH lesions. Sexually experienced female ferrets were ovo-hysterectomized prior to receiving bilateral electrolytic lesions of the VMH, the preoptic area/anterior hypothalamus (POA/AH) or a sham operation. Subsequently, while receiving estradiol benzoate, females that received either complete or partial bilateral lesions of the VMH approached volatile odors from an anesthetized male on significantly fewer trials than females given POA/AH lesions or a sham operation. Both groups of ferrets with VMH lesion damage reliably discriminated between volatile anal scents as well as urinary odors from the 2 sexes in home cage habituation/dishabituation tests, suggesting that their odor-based sex discrimination remained intact. Females with complete bilateral VMH lesions showed significantly lower acceptance of neck gripping from a stimulus male (receptivity) and more aggression towards the male than all other groups of female subjects. Estrogen-sensitive neurons in the VMH appear to play a central role in female-typical neural processing of odor inputs leading to a preference to seek out a male sex partner, in addition to facilitating females' sexual receptivity.
    背景与目标: : 先前的研究表明,男女雪貂都依赖于对个体体味的感知来识别和激励对异性交配伴侣的态度,暴露于男性体味会刺激女性而不是男性的嗅觉投射回路中的Fos表达,终止于腹内侧下丘脑核 (VMH) 的雪貂。我们询问,在Y迷宫测试中,雪貂对女性典型的偏爱接近男性而不是女性的体味是否会被VMH病变破坏。在接受VMH,视前区/下丘脑前部 (POA/AH) 或假手术的双侧电解病变之前,对有性经验的雌性雪貂进行了子宫切除。随后,在接受苯甲酸雌二醇的同时,接受了VMH完全或部分双侧病变的女性在麻醉的男性中获得的挥发性气味明显少于接受POA/AH病变或假手术的女性。两组患有VMH病变的雪貂在家庭笼子适应/不适应测试中可靠地区分了挥发性肛门气味以及来自2个性别的尿液气味,这表明它们基于气味的性别歧视仍然完好无损。与所有其他女性受试者相比,具有完全双侧VMH病变的女性对刺激男性的颈部抓握的接受度明显降低 (接受),并且对男性攻击更高。VMH中的雌激素敏感神经元似乎在女性典型的气味输入的神经处理中起着核心作用,除了促进女性的性接受外,还倾向于寻找男性性伴侣。
  • 【印度城市女性性工作者的健康寻求策略和性健康: 对研究和服务提供的影响。】 复制标题 收藏 收藏
    DOI:10.1016/s0277-9536(96)00288-2 复制DOI
    作者列表:Evans C,Lambert H
    BACKGROUND & AIMS: This paper presents and discusses selected findings from a study of health-seeking strategies in relation to sexual health among a group of female sex workers in Calcutta, India. Background information on sex work and sexually transmitted disease in Calcutta is followed by the presentation of findings pertaining to women's understandings of (sexual) health, treatment-seeking and service utilisation. In the urban context where health services are readily available, patterns of initial treatment-seeking are shown to be generally (biomedically) appropriate, but subsequent "non-compliant" therapeutic practices give cause for concern. Conventional approaches to the study of "health-seeking behaviour" are reviewed in the light of these findings and questions raised about the appropriateness of approaches that focus on initial choice of treatment type and/or assume processes of health-seeking to be determined primarily by cultural "beliefs" about illness. Inherent biomedical and culturalist biases in the orientation of such research are shown to produce an analytic neglect of the dual influences of material life conditions and people's perceptions of health, rather than illness, upon health-related strategies. Recommendations are made for operational research and policy formulation on the provision of effective sexual health services, and implications are drawn for the scope of interventions and applied research directed at improving sexual health.

    背景与目标: 本文介绍并讨论了印度加尔各答一群女性性工作者与性健康有关的寻求健康策略研究的部分发现。关于加尔各答性工作和性传播疾病的背景信息之后,介绍了与妇女对 (性) 健康,寻求治疗和服务利用的理解有关的发现。在容易获得医疗服务的城市环境中,最初寻求治疗的方式通常 (在生物医学上) 是适当的,但是随后的 “不合规” 治疗方法引起了人们的关注。根据这些发现和提出的有关方法的适当性的问题,对 “寻求健康行为” 研究的常规方法进行了审查,这些方法侧重于治疗类型的初始选择和/或假设寻求健康的过程主要由关于疾病的文化 “信仰” 决定。这种研究方向上固有的生物医学和文化主义偏见被证明是对物质生活条件和人们对健康而不是疾病的看法对健康相关策略的双重影响的分析忽略。提出了有关提供有效性健康服务的业务研究和政策制定的建议,并对旨在改善性健康的干预措施和应用研究的范围提出了影响。
  • 【欧洲男性和非洲女性对非裔美国人基因组的贡献增加。】 复制标题 收藏 收藏
    DOI:10.1007/s00439-006-0261-7 复制DOI
    作者列表:Lind JM,Hutcheson-Dilks HB,Williams SM,Moore JH,Essex M,Ruiz-Pesini E,Wallace DC,Tishkoff SA,O'Brien SJ,Smith MW
    BACKGROUND & AIMS: :The differential relative contribution of males and females from Africa and Europe to individual African American genomes is relevant to mapping genes utilizing admixture analysis. The assessment of ancestral population contributions to the four types of genomic DNA (autosomes, X and Y chromosomes, and mitochondrial) with their differing modes of inheritance is most easily addressed in males. A thorough evaluation of 93 African American males for 2,018 autosomal single nucleotide polymorphic (SNP) markers, 121 X chromosome SNPs, 10 Y chromosome haplogroups specified by SNPs, and six haplogroup defining mtDNA SNPs is presented. A distinct lack of correlation observed between the X chromosome and the autosomal admixture fractions supports separate treatment of these chromosomes in admixture-based gene mapping applications. The European genetic contributions were highest (and African lowest) for the Y chromosome (28.46%), followed by the autosomes (19.99%), then the X chromosome (12.11%), and the mtDNA (8.51%). The relative order of admixture fractions in the genomic compartments validates previous studies that suggested sex-biased gene flow with elevated European male and African female contributions. There is a threefold higher European male contribution compared with European females (Y chromosome vs. mtDNA) to the genomes of African American individuals meaning that admixture-based gene discovery will have the most power for the autosomes and will be more limited for X chromosome analysis.
    背景与目标: : 非洲和欧洲的男性和女性对非裔美国人单个基因组的不同相对贡献与利用混合分析定位基因有关。在男性中,最容易解决祖先种群对四种类型的基因组DNA (常染色体,X和Y染色体以及线粒体) 及其不同遗传方式的贡献的评估。提出了对93名非洲裔美国男性的2,018个常染色体单核苷酸多态性 (SNP) 标记,121个X染色体SNP,10个由SNP指定的Y染色体单倍群以及6个定义mtDNA SNP的单倍群的全面评估。在X染色体和常染色体混合组分之间观察到的明显缺乏相关性支持在基于混合的基因作图应用中对这些染色体进行单独处理。欧洲对Y染色体的遗传贡献最高 (非洲最低) (28.46%),其次是常染色体 (19.99%),然后是X染色体 (12.11%) 和mtDNA (8.51%)。基因组区室中混合组分的相对顺序验证了先前的研究,这些研究表明,性别偏向的基因流具有较高的欧洲男性和非洲女性贡献。与欧洲女性相比,欧洲男性对非裔美国人个体基因组的贡献高出三倍 (Y染色体与mtDNA),这意味着基于混合物的基因发现将对常染色体具有最大的力量,并且对X染色体分析。
  • 【雌性大鼠母体行为期间表达Fos的纹状体终末神经元的内侧视前区和腹床核的投影位点。】 复制标题 收藏 收藏
    DOI:10.1046/j.1365-2826.1997.t01-1-00597.x 复制DOI
    作者列表:Numan M,Numan MJ
    BACKGROUND & AIMS: :Medial preoptic area (MPOA) and ventral bed nucleus of the stria terminalis (VBST) neurons are involved in maternal behavior, but the neural sites to which the maternally relevant neurons project have not been determined. Since MPOA and VBST neurons express Fos during maternal behavior, we used a double-labeling immunocytochemical procedure to detect both Fos and a retrograde tracer, wheat germ agglutinin (WGA), in order to determine where these Fos neurons project. On Day 4 postpartum, fully maternal females were separated from their litters. On Day 5, WGA was iontophoretically injected into one of the following regions known to receive MPOA and/or VBST input: Lateral septum, medial hypothalamus at the level of the ventromedial nucleus, lateral habenula, ventral tegmental area, retrorubral field, or periaqueductal gray. On Day 7, females received a 2-h test with either pups or candy, after which they were perfused and their brains were processed for the detection of Fos and WGA. As expected, females tested with pups had more Fos-containing neurons in the MPOA and VBST than did females tested with candy. After WGA injections into several brain sites, the number of double-labeled cells observed in the MPOA and VBST was greater for the maternal females when compared to the non-maternal females. Therefore, these results pinpointed neural circuits that were activated during maternal behavior. For the maternal females, Fos-containing neurons in the MPOA projected most strongly to the medial hypothalamus at the level of the ventromedial nucleus and to the lateral septum, while Fos-containing neurons in the VBST projected most strongly to the retrorubral field, ventral tegmental area, and medial hypothalamus. Although relatively few MPOA and VBST neurons which expressed Fos during maternal behavior projected to the periaqueductal gray, these Fos-expressing neurons made up a relatively large proportion of the MPOA and VBST projection to the periaqueductal gray. This study suggests that MPOA and VBST efferents project to a variety of regions to promote full maternal responsiveness.
    背景与目标: : 视前区 (MPOA) 和纹状体 (VBST) 神经元的腹床核参与母体行为,但尚未确定与母系相关的神经元投射到的神经部位。由于MPOA和VBST神经元在母体行为中表达Fos,因此我们使用双标记免疫细胞化学程序来检测Fos和逆行示踪剂小麦胚芽凝集素 (WGA),以确定这些Fos神经元的投射位置。产后第4天,将完全的产妇与产仔分开。在第5天,将WGA离子电渗注射到以下已知接受MPOA和/或VBST输入的区域之一: 外侧隔膜,腹内侧核水平的下丘脑内侧,外侧habenula,腹侧被盖区,脑后野,或导水管周围灰色。在第7天,雌性接受了2小时的幼崽或糖果测试,然后对其进行灌注,并对其大脑进行处理以检测Fos和WGA。正如预期的那样,与用糖果测试的雌性相比,用幼崽测试的雌性在MPOA和VBST中具有更多的含Fos的神经元。在将WGA注射到多个大脑部位后,与非母体女性相比,在MPOA和VBST中观察到的双标记细胞数量更多。因此,这些结果确定了在母体行为期间激活的神经回路。对于母体女性,MPOA中含Fos的神经元最强烈地投射到腹内侧核水平的下丘脑内侧和外侧隔,而VBST中含Fos的神经元最强烈地投射到脑后野,腹侧被盖区和下丘脑内侧。尽管在投射到导水管周围灰色的母体行为中表达Fos的MPOA和VBST神经元相对较少,但这些表达Fos的神经元在MPOA和VBST投射到导水管周围灰色的比例相对较大。这项研究表明,MPOA和VBST传出剂投射到各个地区,以促进孕产妇的全面反应。
  • 【居住在西西里岛东部卡塔尼亚的哥伦比亚和多米尼加女性性工作者中艾滋病毒和其他性传播疾病的流行。】 复制标题 收藏 收藏
    DOI:10.1007/s10903-006-9002-1 复制DOI
    作者列表:Nigro L,Larocca L,Celesia BM,Montineri A,Sjoberg J,Caltabiano E,Fatuzzo F,Unit Operators Group.
    BACKGROUND & AIMS: INTRODUCTION:STDs are a significant cause of illness throughout the world. Female sex workers (FSWs) are commonly perceived as belonging to a social group which may engage in high-risk behaviour for acquiring or transmitting HIV and other STDs. The number of immigrant women engaged in sex work has increased in Catania, Sicily, over the last 10 years. This study aims to estimate the prevalence of HIV, HBV, HCV and syphilis among Colombian and Dominican FSWs. METHODS:In total 118 (63.78%) of the FSWs contacted in the course of the project agreed to participate in the study. All women enrolled were counselled on STDs/HIV, safer sex practices and the use of condoms. Blood samples were taken and tested for HIV, HBV, HCV and syphilis. RESULTS:Of the 118 FSWs enrolled, all were negative for both HIV and HCV infection. Two women (1.6%) were positive for hepatitis B (HbsAg). Syphilis testing by VDRL showed three positive results (2.5%), which was confirmed by TPHA. DISCUSSION:This study showed that HIV, HBV, HCV and syphilis seroprevalence among Colombian and Dominican FSWs remains low or very rare. It also indicates that these women were healthy when they arrived in Italy and that condom use with clients is high.
    背景与目标:
  • 【在台湾,替加环素与其他抗菌剂对肺炎链球菌,流感嗜血杆菌和卡他莫拉菌的体外活性比较。】 复制标题 收藏 收藏
    DOI:10.1089/mdr.2006.12.130 复制DOI
    作者列表:Lau YJ,Hsueh PR,Liu YC,Shyr JM,Huang WK,Teng LJ,Liu CY,Luh KT
    BACKGROUND & AIMS: :We compared the in vitro activities of tigecycline to those of other agents against 300 nonduplicate isolates of Streptococcus pneumoniae (194 isolates), Haemophilus influenzae (60 isolates), and Moraxella catarrhalis (46 isolates) recovered from patients treated in three major hospitals in Taiwan from August through December, 2003. All of these isolates were inhibited at 0.5 mg/L of tigecycline. For S. pneumoniae isolates, 72% were not susceptible to penicillin (69% intermediate and 3% resistant) and 96% were not susceptible to azithromycin. Among the 178 isolates resistant to azithromycin, 53 isolates (30%) had the M phenotype and 70% had the cMLSB phenotype. The rate of nonsusceptibility to ertapenem, telithromycin, moxifloxacin, and quinupristindalfopristin in S. pneumoniae was 3%, 2%, 1%, and 57%, respectively. For H. influenzae, 36 (60%) were not susceptible to ampicillin, among which 31 possessed beta-lactamase. A high rate (8.3%) of H. influenzae isolates with beta-lactamase-negative and ampicillin-resistant phenotype was found. All H. influenzae isolates were susceptible to azithromycin, but 40% of them were not susceptible to clarithromycin. Ninety-eight percent (44 isolates) of M. catarrhalis possessed beta-lactamase. All three fluoroquinolones tested were highly active (MIC90 < or =0.12 mg/L) against H. influenzae and M. catarrhalis.
    背景与目标: : 我们比较了替加环素与其他药物对300种非重复肺炎链球菌分离株 (194株),流感嗜血杆菌 (60株) 和卡他莫拉菌 (46株) 的体外活性,这些分离株是从8月到2003年12月在台湾的三家主要医院中康复的。在0.5 mg/L替加环素的浓度下,所有这些分离株均被抑制。对于肺炎链球菌分离株,72% 对青霉素不敏感 (69% 中间体和3% 耐药),96% 对阿奇霉素不敏感。在对阿奇霉素耐药的178株中,53株 (30% 株) 具有M表型,70% 株具有cMLSB表型。肺炎链球菌对厄他培南,泰利霉素,莫西沙星和奎奴普汀的不敏感性分别为3%,2%,1% 和57%。对于流感嗜血杆菌,36 (60%) 对氨苄青霉素不敏感,其中31具有 β-内酰胺酶。发现具有 β-内酰胺酶阴性和氨苄青霉素抗性表型的流感嗜血杆菌分离株率高 (8.3%)。所有流感嗜血杆菌分离株对阿奇霉素敏感,但其中40% 对克拉霉素不敏感。卡他氏杆菌的百分之九十八 (44个分离株) 具有 β-内酰胺酶。测试的所有三种氟喹诺酮类药物对流感嗜血杆菌和卡他氏杆菌具有高度活性 (MIC90 <或 = 0.12 mg/L)。
  • 【关系质量,激素避孕选择和青少年妇女不使用避孕套的发展关联。】 复制标题 收藏 收藏
    DOI:10.1016/j.jadohealth.2005.12.027 复制DOI
    作者列表:Sayegh MA,Fortenberry JD,Shew M,Orr DP
    BACKGROUND & AIMS: PURPOSE:Consistent condom use is critical to efforts to prevent sexually transmitted infections among adolescents, but condom use may decline as relationships and contraceptive needs change. The purpose of this research is to assess changes in condom non-use longitudinally in the context of changes in relationship quality, coital frequency and hormonal contraceptive choice. METHODS:Participants were women (aged 14-17 years at enrollment) recruited from three urban adolescent medicine clinics. Data were collected at three-month intervals using a face-to-face structured interview. Participants were able to contribute up to 10 interviews, but on average contributed 4.2 interviews over the 27-month period. Independent variables assessed partner-specific relationship quality (five items; scale range 5-25; alpha = .92, e.g., this partner is a very important person to me); and, number of coital events with a specific partner. Additional items assessed experience with oral contraceptive pills (OCP) use and injected depo medroxy-progesterone acetate (DMPA). The outcome variable was number of coital events without condom use during the past three months. Analyses were conducted as a three-level hierarchical linear growth curve model using HLM 6. The Level 1 predictor was time, to test the hypothesis that condom non-use increases over time. Level 2 predictors assessed relationship quality and coital frequency across all partners to assess hypotheses that participants' condom non-use increases over time as a function of relationship quality and coital frequency. Level 3 predictors assessed the participant-level influence of OCP or DMPA experience on time-related changes in condom non-use. RESULTS:A total of 176 women reported 279 sex partners and contributed 478 visits. Both average coital frequency and average condom non-use linearly increased during the 27-month follow-up. At any given follow-up, about 35% reported recent OCP use, and 65% reported DMPA use. HLM analyses showed that condom non-use increased as a function of time (beta = .12; p = .03, Level 1 analysis). Increased condom non-use over time was primarily a function of increased coital frequency (beta = .01; p = .00), although higher levels of relationship quality were associated with increased condom non-use at enrollment (beta = .44; p = .00, Level 2 analysis). The temporal rise in condom non-use significantly increased among DMPA users (beta = .06; p = .00) but not OCP users (Level 3 analysis) (beta = -.04; p = .06). CONCLUSIONS:Developmentally, relationship characteristics and coital frequency appear to have increasing weight in decisions about condom use. Hormonal contraceptive methods are not equivalently associated with the overall temporal decline in condom use. Future research associated with dual contraceptive/condom use should address differential factors associated condom use in combination with different hormonal methods.
    背景与目标:
  • 【氟化分子作为中枢神经系统中的药物和显像剂。】 复制标题 收藏 收藏
    DOI:10.2174/156802606777951046 复制DOI
    作者列表:Sun S,Adejare A
    BACKGROUND & AIMS: :The strategic use of fluorine substitution in drug discovery and drug development is well documented. The small size and high electronegativity of fluorine are among properties of this element that lend special advantages. Applications in drugs targeted to the central nervous system (CNS) have been particularly fruitful in addition to favorable properties seen in many peripherally acting drugs. Fluorine substitution can be used to solve problems unique to the CNS, such as blood brain barrier (BBB) penetration. Likewise, use of the positron emitting isotope, (18)F, provides a unique tool for non-invasive imaging and diagnoses in the CNS. In this review, fluorine in CNS drugs and drug discovery are discussed.
    背景与目标: : 氟替代在药物发现和药物开发中的战略用途已得到充分证明。氟的小尺寸和高电负性是该元素的特殊优点之一。除了在许多外周作用药物中看到的有利特性外,针对中枢神经系统 (CNS) 的药物中的应用特别富有成效。氟替代可用于解决CNS特有的问题,例如血脑屏障 (BBB) 渗透。同样,使用正电子发射同位素 (18)F为CNS中的非侵入性成像和诊断提供了独特的工具。本文对中枢神经系统药物中的氟和药物发现进行了讨论。
  • 【向雌性大鼠施用合成代谢雄激素类固醇癸酸诺龙会导致其子宫形态发生变化,并降低生殖能力。】 复制标题 收藏 收藏
    DOI:10.1016/j.ejogrb.2006.07.037 复制DOI
    作者列表:Mobini Far HR,Agren G,Lindqvist AS,Marmendal M,Fahlke C,Thiblin I
    BACKGROUND & AIMS: OBJECTIVE:The aim of the present investigation was to characterize the effects of supraphysiological doses of the anabolic androgenic steroid nandrolone decanoate (ND) on the fertility of female rats, as well as on the morphology of their uterus. STUDY DESIGN:Female Wistar rats (n=15) received a subcutaneous injection of ND (15 mg/kg) once daily during a 2-week period, while the control animals (n=10) were administered vehicle alone (arachidis oleum) in the same manner. Estrus behavior was evaluated 4 weeks after termination of this treatment and in cases where signs of receptivity were present, the female rat was given the opportunity to copulate with a male. After breeding, the female animals were sacrificed and their uteri examined histomorphologically. RESULTS:All ND-treated animals exhibited abnormal vaginal smears, whereas all of the control smears were normal. Most (73%) of the treated females demonstrated normal estrus behavior (i.e., willingness) on the day of mating, but none got pregnant; whereas all of the control rats became pregnant. The female rats receiving the ND showed an enhanced rate of weight gain and the myometrium thickness of their uteri was significantly increased, while the endometrium was significantly thinner. Furthermore, ND caused a significant proportion of the treated animals to display tortuous and irregularly branching endometrial glands, as well as a lack of the physiologically normal infiltration of eosinophilic leukocytes into the endometrium (endometrial eosinophilic homing), a finding that has not been reported previously. CONCLUSION:The present findings indicate that high doses of ND cause morphological and physiological alterations in the uterus of female rats that are associated with a suppression of their reproductive capacity.
    背景与目标:
  • 【缺碘雌性大鼠甲状腺和组织中的脱碘酶活性。】 复制标题 收藏 收藏
    DOI:10.1210/en.2012-1727 复制DOI
    作者列表:Lavado-Autric R,Calvo RM,de Mena RM,de Escobar GM,Obregon MJ
    BACKGROUND & AIMS: :Severe iodine deficiency is characterized by goiter, preferential synthesis, and secretion of T(3) in thyroids, hypothyroxinemia in plasma and tissues, normal or low plasma T(3), and slightly increased plasma TSH. We studied changes in deiodinase activities and mRNA in several tissues of rats maintained on low-iodine diets (LIDs) or LIDs supplemented with iodine (LID+I). T(4) and T(3) concentrations decreased in plasma, tissues, and thyroids of LID rats, and T(4) decreased more than T(3) (50%). The highest type 1 iodothyronine deiodinase (D1) activities were found in the thyroid, kidney, and the liver; pituitary, lung, and ovary had lower D1 activities; but the lowest levels were found in the heart and skeletal muscle. D1 activity decreased in all tissues of LID rats (10-40% of LID+I rats), except for ovary and thyroids, which D1 activity increased 2.5-fold. Maximal type 2 iodothyronine deiodinase (D2) activities were found in thyroid, brown adipose tissue, and pituitary, increasing 6.5-fold in thyroids of LID rats and about 20-fold in the whole gland. D2 always increased in response to LID, and maximal increases were found in the cerebral cortex (19-fold), thyroid, brown adipose tissue, and pituitary (6-fold). Lower D2 activities were found in the ovary, heart, and adrenal gland, which increased in LID. Type 3 iodothyronine deiodinase activity was undetectable. Thyroidal Dio1 and Dio2 mRNA increased in the LID rats, and Dio1 decreased in the lung, with no changes in mRNA expression in other tissues. Our data indicate that LID induces changes in deiodinase activities, especially in the thyroid, to counteract the low T(4) synthesis and secretion, contributing to maintain the local T(3) concentrations in the tissues with D2 activity.
    背景与目标: : 严重缺碘的特征是甲状腺肿大,甲状腺优先合成和分泌T(3),血浆和组织中的低甲状腺素血症,正常或低血浆T(3) 和血浆TSH略有升高。我们研究了低碘饮食 (LID) 或补充碘的LID (LID I) 维持的大鼠几个组织中脱碘酶活性和mRNA的变化。LID大鼠血浆,组织和甲状腺中T(4) 和T(3) 的浓度降低,T(4) 的降低幅度大于T(3) (50%)。在甲状腺,肾脏和肝脏中发现最高的1型碘甲状腺原氨酸脱碘酶 (D1) 活性; 垂体,肺和卵巢的D1活性较低; 但在心脏和骨骼肌中发现最低水平。除卵巢和甲状腺外,LID大鼠的所有组织 (LID I大鼠的10-40%) 中的D1活性均降低,D1活性增加了2.5倍。在甲状腺,棕色脂肪组织和垂体中发现最大的2型碘甲状腺原氨酸脱碘酶 (D2) 活性,在LID大鼠的甲状腺中增加6.5倍,在整个腺体中约增加20倍。D2总是响应LID而增加,并且在大脑皮层 (19倍),甲状腺,棕色脂肪组织和垂体 (6倍) 中发现最大增加。在卵巢,心脏和肾上腺中发现较低的D2活性,在LID中增加。无法检测到3型碘甲状腺原氨酸脱碘酶活性。LID大鼠甲状腺Dio1和Dio2 mRNA增加,肺中Dio1降低,其他组织中mRNA表达无变化。我们的数据表明,LID诱导脱碘酶活性的变化,尤其是在甲状腺中,以抵消低T(4) 的合成和分泌,有助于维持具有D2活性的组织中的局部T(3) 浓度。
  • 【一些腙衍生物作为新型抗癌剂和抗癌剂的合成和生物学评价。】 复制标题 收藏 收藏
    DOI:10.1016/j.ejmech.2012.10.011 复制DOI
    作者列表:Altıntop MD,Özdemir A,Turan-Zitouni G,Ilgın S,Atlı Ö,İşcan G,Kaplancıklı ZA
    BACKGROUND & AIMS: :New hydrazone derivatives were synthesized via the nucleophilic addition-elimination reaction of 2-[(1-methyl-1H-tetrazol-5-yl)thio)]acetohydrazide with aromatic aldehydes/ketones. The compounds were tested in vitro against various Candida species and compared with ketoconazole. Genotoxicity of the most effective anticandidal compounds was evaluated by umuC and Ames assays. All compounds were also investigated for their cytotoxic effects on NIH3T3 and A549 cell lines. Compound 8 was the most effective antifungal derivative against C. albicans (ATCC-90028) with a MIC value of 0.05 mg/mL. Compound 5 can be identified as the most promising anticancer agent against A549 cancer cell lines due to its inhibitory effect on A549 cell lines and low toxicity to NIH3T3 cells.
    背景与目标: : 通过2-[(1-甲基-1h-四唑-5-基) 硫代)] 乙酰酰肼与芳族醛/酮的亲核加成消除反应合成了新的腙衍生物。对化合物进行了针对各种念珠菌的体外测试,并与酮康唑进行了比较。通过umuC和Ames分析评估了最有效的抗癌症化合物的遗传毒性。还研究了所有化合物对NIH3T3和A549细胞系的细胞毒性作用。化合物8是对白色念珠菌 (ATCC-90028) 最有效的抗真菌衍生物,MIC值为0.05 mg/ml。化合物5由于对A549细胞系的抑制作用和对NIH3T3细胞的低毒性,可被确定为最有前途的抗A549癌细胞系的抗癌剂。
  • 【中国昆明女性青少年性工作者的脆弱性,健康需求和高风险性行为的预测因素。】 复制标题 收藏 收藏
    DOI:10.1136/sextrans-2012-050690 复制DOI
    作者列表:Zhang XD,Temmerman M,Li Y,Luo W,Luchters S
    BACKGROUND & AIMS: OBJECTIVES:This study assessed social and behavioural predictors for sexual risk taking and sexually transmitted infections (STIs) including HIV among adolescent female sex workers (FSWs) from Kunming, China. Additionally, health services needs and use were assessed. METHODS:A cross-sectional survey was conducted in 2010. Using snowball and convenience sampling, self-identified FSWs were recruited from four urban areas in Kunming. Women consenting to participate were administered a semi-structured questionnaire by trained interviewers identified from local peer-support organisations. Following interview, a gynaecological examination and biological sampling to identify potential STIs were undertaken. Descriptive and multivariable logistic regression analyses were performed. RESULTS:Adolescent FSWs had a mean age of 18.2 years and reported numerous non-paying sexual partners with very low rate of consistent condom use (22.2%). Half (50.3%) the respondents had sex while feeling drunk at least once in the past week, of whom 56.4% did not use condom protection. STI prevalence was high overall (30.4%) among this group. Younger age, early sexual debut, being isolated from schools and family, short duration in sex work, and use of illicit drugs were found to be strong predictors for unprotected sex and presence of an STI. Conversely, having access to condom promotion, free HIV counselling and testing, and peer education were associated with less unprotected sex. The majority reported a need for health knowledge, free condoms and low-cost STI diagnosis and treatment. CONCLUSIONS:There is an urgent need to improve coverage, accessibility and efficiency of existing interventions targeting adolescent FSWs.
    背景与目标:
  • 【发现链烯基硼酸作为神经保护剂,影响与阿尔茨海默氏病有关的多个生物靶标。】 复制标题 收藏 收藏
    DOI:10.1016/j.bmcl.2012.11.068 复制DOI
    作者列表:Jiménez-Aligaga K,Bermejo-Bescós P,Martín-Aragón S,Csákÿ AG
    BACKGROUND & AIMS: :Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.
    背景与目标: : 烯基硼酸显示出重要的生物活性,有助于神经保护。我们已经确定了它们对 β-淀粉样蛋白 (β a) 聚集过程,β-分泌酶和乙胆碱酯酶在无细胞系统上的活性,对氧化还原和脂质过氧化状态以及对APPswe神经母细胞瘤细胞凋亡死亡的脆弱性的影响过氧化氢治疗之前和之后。我们发现2-芳基乙烯基硼酸及其某些酯具有一系列特性,这使它们作为影响AD中涉及的多个生物靶标的神经保护剂非常有用。这些性质与相关的2-芳基硼酸不平行。
  • 【白藜芦醇衍生物的设计,合成和评估,如a ß (派-) 聚集抑制剂,抗氧化剂和神经保护剂。】 复制标题 收藏 收藏
    DOI:10.1016/j.bmcl.2012.09.105 复制DOI
    作者列表:Lu C,Guo Y,Li J,Yao M,Liao Q,Xie Z,Li X
    BACKGROUND & AIMS: :A series of novel resveratrol derivatives were designed, synthesised and evaluated as potential therapeutic agents for the treatment of Alzheimer's disease. Among these compounds, compound 7l, (E)-5-(4-(isopropylamino)styryl)benzene-1,3-diol, exhibited potent ß-amyloid aggregation inhibition activity, which was confirmed by a ThT fluorescence assay (71.65% at 20 μM) and transmission electron microscopy (TEM). Compound 7l also exhibited good antioxidant activity (4.12 Trolox equivalents in an oxygen radical absorbance capacity assay and a 37% reduction in reactive oxygen species in cells at 10 μM). The cytotoxicity analysis of compounds 7f, 7i, 7j and 7l indicated that these compounds have lower toxicities than resveratrol at 60 μM.
    背景与目标: : 设计,合成和评估了一系列新型白藜芦醇衍生物,可作为治疗阿尔茨海默氏病的潜在治疗剂。在这些化合物中,化合物7l,(E)-5-(4-(异丙基氨基) 苯乙烯基) 苯-1,3-二醇表现出有效的 β-淀粉样蛋白聚集抑制活性,通过ThT荧光分析 (71.65% 在20μm) 和透射电子显微镜 (TEM) 证实了这一点。化合物7l也显示出良好的抗氧化活性 (在氧自由基吸收能力分析中4.12的Trolox当量和10μm细胞中活性氧的37% 减少)。化合物的细胞毒性分析7f,7i,7j和7l表明这些化合物在60μm时的毒性比白藜芦醇低。
  • 【八氢吡嗪 [2,1-a:5,4-a '] 二异喹啉衍生物作为有效抗癌剂的生物学评价。】 复制标题 收藏 收藏
    DOI:10.1177/1010428317701641 复制DOI
    作者列表:Gornowicz A,Pawłowska N,Czajkowska A,Czarnomysy R,Bielawska A,Bielawski K,Michalak O,Staszewska-Krajewska O,Kałuża Z
    BACKGROUND & AIMS: :In this study, we evaluated the cytotoxic activity and antiproliferative potency of novel octahydropyrazin[2,1-a:5,4-a']diisoquinoline derivatives (1-7) in MCF-7 and MDA-MB-231 breast cancer cell lines. Annexin V binding assay and disruption of the mitochondrial potential were performed to determine apoptosis. The activity of caspases 3, 8, 9, and 10 was measured after 24 h of incubation with tested compounds to explain detailed molecular mechanism of induction of apoptosis. The results from experiments were compared with effects obtained after incubation in the presence of camptothecin and etoposide. Our study demonstrated that the most active compounds in both analyzed breast cancer cell lines were compounds 3 and 4. We also observed that all compounds induced apoptosis. We demonstrated the higher activity of caspases 3, 8, 9, and 10, which confirmed that induction of apoptosis is associated with external and internal cell death pathway. Our study revealed that the novel compounds in group of diisoquinoline derivatives are promising candidates in anticancer treatment by activation of both extrinsic and intrinsic apoptotic pathways.
    背景与目标: : 在这项研究中,我们评估了新型八氢吡嗪 [2,1-a:5,4-a '] 二异喹啉衍生物 (1-7) 在MCF-7和MDA-MB-231乳腺癌细胞系中的细胞毒性和抗增殖能力。进行膜联蛋白V结合测定和线粒体电位破坏以确定细胞凋亡。与测试化合物孵育24小时后,测量了胱天蛋白酶3、8、9和10的活性,以解释诱导凋亡的详细分子机制。将实验结果与在喜树碱和依托泊苷存在下孵育后获得的效果进行了比较。我们的研究表明,在两种分析的乳腺癌细胞系中最具活性的化合物是化合物3和4。我们还观察到所有化合物均诱导细胞凋亡。我们证明了caspases 3、8、9和10的较高活性,这证实了凋亡的诱导与外部和内部细胞死亡途径有关。我们的研究表明,二异喹啉衍生物组中的新型化合物通过激活外在和内在凋亡途径在抗癌治疗中是有希望的候选者。

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