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11.
A new phenolic glucoside, acremonoside (1), along with two known compounds, F-11334 A2 and 2,2-dimethyl-2H-chromen-6-ol, were isolated from the sea fan-derived fungus Acremonium polychromum PSU-F125. The structure of 1 was elucidated by spectroscopic techniques, acid hydrolysis and X-ray crystallographic analysis. The isolated compounds were tested for antibacterial, antimalarial, antimycobacterial and cytotoxic activities.  相似文献   
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Plants resist infection through an innate immune response, which is usually associated with slowing of growth. The molecular mechanisms underlying the trade-off between plant growth and defense remain unclear. The present study reveals that growth/defense trade-offs mediated by gibberellin (GA) and salicylic acid (SA) signaling pathways are uncoupled during constitutive overexpression of transgenic AtRAN1 and AtRAN1Q72L (active, GTP-locked form) Arabidopsis plants. It is well known that the small GTP-binding protein Ran (a Ras-related nuclear protein) functions in the nucleus–cytoplasmic transport of proteins. Although there is considerable evidence indicating that nuclear–cytoplasmic partitioning of specific proteins can participate in hormone signaling, the role of Ran-dependent nuclear transport in hormone signaling is not yet fully understood. In this report, we used a combination of genetic and molecular methods to reveal whether AtRAN1 is involved in both GA and SA signaling pathways. Constitutively overexpressed AtRAN1 promoted both elongation growth and the disease resistance response, whereas overexpression of AtRAN1Q72L in the atran2atran3 double mutant background clearly inhibited elongation growth and the defense response. Furthermore, we found that AtRAN1 coordinated plant growth and defense by promoting the stability of the DELLA protein RGA in the nucleus and by modulating NPR1 nuclear localization. Interestingly, genetically modified rice (Oryza sativa) overexpressing AtRAN1 exhibited increased plant height and yield per plant. Altogether, the ability to achieve growth/defense trade-offs through AtRAN1 overexpression provides an approach to maximizing crop yield to meet rising global food demands.  相似文献   
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Seven previously undescribed metabolites, designated as tricycloalternarenes Q–W (17), were isolated and identified from the fermented rice substrate of fungus Alternaria brassicicola. The planar and absolute structures of all new compounds were determined on the basis of extensive NMR spectroscopic data, a modified Mosher’s method, X-ray crystallographic analysis, and electronic circular dichroism (ECD) spectral analyses. All the isolates were evaluated for in vitro cytotoxicity against five human tumor MM231, MM468, HeLa, SW1990, and SW480 cell lines, and compounds 1, 2, 5, and 7 showed selective cytotoxicity against certain human tumor cell lines with IC50 values ranging from 12.83 to 32.87 μM, with no obvious cytotoxicity to the normal LO2 cell.  相似文献   
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Three new pseudo-disesquiterpenoids, vernodalidimer F – H (13), which are formed by esterification of two sesquiterpenoids, along with a new sesquiterpenoid (4) and two known sesquiterpeonids (5, 6) were isolated from the seeds of Vernonia anthelmintica. Their structures were elucidated by NMR data. The absolute configurations of 1–3 and 5 were determined by comparison of the experimental and calculated electronic circular dichroism spectra. Cytotoxicity of the isolated compounds against four human tumor cell lines were assayed. 5 exhibited strong cytotoxicity against HCT-15, PC-3, A549 and Hela cells lines with IC50 values of 5.3, 5.6, 6.2, and 8.2 μM, respectively. 2 showed non-concentration dependent cytotoxicity against HCT-15, PC-3, and A549 cells lines with inhibition rate of 56.1%, 55.3%, and 50.1%, respectively. 1 and 3 showed moderate cytotoxicity against four cell lines with IC50 values ranging from 12.2 ± 5.1 to 28.6 ± 2.5 μM. The influence of melanin content in B16 melanoma cells of 1, 5, and 6 were tested, and they increased melanin content by 43.6%, 28.1%, and 37.0% higher than positive control 8-methoxypsoralen.  相似文献   
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The mechanisms that underlie metal carcinogenesis are the subject of intense investigation; however, data from in vitro and in vivo studies are starting to piece together a story that implicates epigenetics as a key player. Data from our lab has shown that nickel compounds inhibit dioxygenase enzymes by displacing iron in the active site. Arsenic is hypothesized to inhibit these enzymes by diminishing ascorbate levels – an important co-factor for dioxygenases. Inhibition of histone demethylase dioxygenases can increase histone methylation levels, which also may affect gene expression. Recently, our lab conducted a series of investigations in human subjects exposed to high levels of nickel or arsenic compounds. Global levels of histone modifications in peripheral blood mononuclear cells (PBMCs) from exposed subjects were compared to low environmentally exposed controls. Results showed that nickel increased H3K4me3 and decreased H3K9me2 globally. Arsenic increased H3K9me2 and decreased H3K9ac globally. Other histone modifications affected by arsenic were sex-dependent. Nickel affected the expression of 2756 genes in human PBMCs and many of the genes were involved in immune and carcinogenic pathways. This review will describe data from our lab that demonstrates for the first time that nickel and arsenic compounds affect global levels of histone modifications and gene expression in exposed human populations.  相似文献   
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目的:研究自拟柴芍护膜汤联合莫沙必利治疗反流性食管炎的临床效果和可能机制。方法:选择2015年12月~2018年12月我院内科杂病门诊治疗的70例反流性食管炎患者,将其随机分为两组。对照组服用莫沙必利,每次5 mg,每天3次;观察组联合服用自拟柴芍护膜汤以及莫沙必利。比较两组患者治疗后的临床治疗效果,治疗前后泛酸、烧心、脘腹胀满、嗳气、呃逆、情志抑郁、善太息、食欲不振以及嘈杂等症状的严重程度、血浆胃动素和血清胃泌素水平的变化。结果:治疗后,观察组的有效率为91.43%,明显高于对照组(71.43%,P0.05)。两组治疗后的泛酸、烧心、脘腹胀满、嗳气、呃逆、情志抑郁、善太息、食欲不振以及嘈杂评分均较治疗前明显降低(P0.05),且观察组的上述症状评分明显低于对照组(P0.05);两组治疗后的血浆胃动素和血清胃泌素水平均较治疗前明显升高(P0.05),且观察组以上指标均明显高于对照组(P0.05)。结论:自拟柴芍护膜汤联合莫沙必利能有效改善反流性食管炎的临床症状,其作用机制可能与提高血浆胃动素和血清胃泌素水平有关。  相似文献   
17.
目的:探究血府逐瘀汤联合四联疗法治疗幽门螺旋杆菌(Hp)阳性慢性萎缩性胃炎的效果。方法:回顾性分析2014年5月-2017年12月在我院进行诊治的80例Hp阳性慢性萎缩性胃炎患者的临床资料,按照其入院顺序经随机数字表分为研究组和对照组,每组各40例患者。其中,对照组患者采用四联疗法,研究组患者在对照组基础上联合血府逐瘀汤进行治疗,对比两组患者的Hp转阴率、治疗前后胃黏膜病理积分的变化情况、临床症状积分的变化情况和不良反应发生率。结果:治疗后,研究组患者的Hp转阴率[85.0%(34/40)]显著高于对照组[62.5%(25/40)](P0.05)。两组上腹痛、纳差、上腹胀、反酸、嗳气等临床症状积分以及胃黏膜萎缩、肠化、不典型增生等病理积分均显著低于治疗前(P0.05),且研究组以上指标均明显低于对照组(P0.05)。研究组患者的不良反应发生率[5.0%(2/40)]与对照组[12.5%(5/40)]无显著性差异(P0.05)。结论:血府逐瘀汤联合四联疗法治疗Hp阳性慢性萎缩性胃炎的效果显著优于单用四联疗法,其可有效改善患者的病变程度和临床症状,且无明显不良反应产生。  相似文献   
18.
目的:利用X线衍射技术解析孕烷X受体(PXR)配体结合结构域(LBD)蛋白晶体的3维结构。方法:对PXR蛋白LBD(130~434氨基酸残基)序列进行密码子优化并化学合成后克隆至pRSFDuet-1表达载体,再将载体导入大肠杆菌BL21(DE3),对PXR-LBD蛋白进行原核表达与分离纯化;采用晶体筛选试剂盒筛选蛋白结晶条件,采用悬滴法获得目标蛋白的晶体;对获得的蛋白晶体进行X线晶体衍射检测,并收集相关数据建立PXR-LBD的三维结构。结果:获得了PXR-LBD的高质量晶体并利用X线衍射解析了该蛋白质晶体的结构数据,使用Phenix.refine软件和COOT软件等对结构进行修正,最终获得了高分辨率的3维结构数据。结论:完成了孕烷X受体配体结合结构域蛋白晶体的X线衍射结构解析,为研究和开发PXR相关药物奠定了基础。  相似文献   
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