Synthesis,telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety

Based on previous studies, 66 2-phenyl-4H-chromone derivatives containing amide and 1,3,4-oxadiazole moieties were prepared as potential telomerase inhibitors. The results showed most of the title compounds exhibited significantly inhibitory activity on telomerase. Among them, some compounds demonstrated the most potent telomerase inhibitory activity (IC₅₀ < 1 µM), which was significantly superior to the staurosporine (IC₅₀ = 6.41 µM). In addition, clear structure–activity relationships were summarised, indicating that the substitution of the methoxy group and the position, type and number of the substituents on the phenyl ring had significant effects on telomerase activity. Among them, compound A33 showed considerable inhibition against telomerase. Flow cytometric analysis showed that compound A33 could arrest MGC-803 cell cycle at G2/M phase and induce apoptosis in a concentration-dependent way. Meanwhile, Western blotting revealed that this compound could reduce the expression of dyskerin, which is a fragment of telomerase.     

Hybrid Anticancer Peptides DN1 and DN4 Exert Selective Cytotoxicity Against Hepatocellular Carcinoma Cells by Inducing Both Intrinsic and Extrinsic Apoptotic Pathways

International Journal of Peptide Research and Therapeutics - Bioactive peptides have emerged as promising therapeutic alternatives in pharmaceutical industry, especially to fight cancer. Here we...     

Poly(ADP-ribose) polymerase inhibitor PJ34 protects against UVA-induced oxidative damage in corneal endothelium

Apoptosis - Fuchs endothelial corneal dystrophy (FECD) is one of the main causes for corneal endothelial blindness, which is characterized by the progressive decline of corneal endothelial cells....     

Seasonal changes in cuticular hydrocarbons in response to polyphenism in the host-alternating aphid Prociphilus oriens

In most terrestrial arthropods, cuticular hydrocarbons (CHCs) function to assist in desiccation tolerance and chemical communications. However, few studies have clarified whether CHC profiles change among developmental stages or among different morphs in non-social insects. In the present study, we evaluated how CHC profiles change in accordance with polyphenism in the host-alternating aphid Prociphilus oriens, which exhibits a complex life cycle and five distinct morphs. These morphs are sexual or asexual and adapt to different host plants. We found that all generations of P. oriens shared high proportions of n-alkanes, but its composition varied among morphs. Three morphs that are attended by ants were characterized by relatively high proportions of n-C25 to n-C27, whereas two morphs that are not attended by ants had higher proportions of longer-chain n-alkanes, such as n-C27 and n-C29. The CHC profiles of sexual females were largely different from those of males. Considering that sexual females of Prociphilus spp. lack organs that secrete sex pheromones (scent plaques), the CHCs of sexual females are likely to function as a sex attractant. High proportions of methyl-branched alkanes were detected in the long and flocculent waxy substances of autumnal migrants. These methyl-branched alkanes are considered a cue to recognize conspecifics. We concluded that the functions and components of CHCs differ among morphs, and that those of sexual females differ from those of males and asexual generations because of their function in sexual communication.     

Assembly of the Non-Canonical Myo9a-RhoGAP and RhoA·GDP Transition State Complex in the Presence of MgF3−

The Protein Journal - Myo9a is an actin-based molecular motor with a RhoGAP domain in its C-terminal tail. It plays a role in a variety of biological processes, such as in regulating the immune...     

基于流式细胞术和K-mer分析的银缕梅属(Parrotia C.A.Mey.)植物基因组大小测定

金缕梅科(Hamamelidaceae)银缕梅属(Parrotia C.A.Mey.)仅包含银缕梅(Parrotia subaequalis(H.T.Chang)R.M.Hao&H.T.Wei)和波斯铁木(Parrotia persica(DC.)C.A.Mey.)两种落叶阔叶乔木,其中银缕梅是我国华东地区特有的Ⅰ级濒危珍稀保护植物,属东亚第三纪孑遗成分;其姊妹种波斯铁木则间断分布于伊朗北部,属北极第三纪孑遗植物类群。本研究首次利用流式细胞术和K-mer分析方法对银缕梅属两姊妹种的基因组大小进行了测定,建立和优化了以萝卜(Raphanus sativus L.‘Saxa’)为内标、WPB(Woody plant buffer)为细胞核解离液的两种植物单倍体基因组的DNA含量(DNA C值)流式测定的适宜体系,旨在为金缕梅科银缕梅属植物的全基因组测序、基因组学研究、种质资源开发和利用以及物种保育等提供前期基础数据参考;同时也可为金缕梅科其他属、种的基因组大小测定提供借鉴。主要研究结果如下:(1)通过流式测定银缕梅基因组大小约为971.45±13.91 Mb,波斯铁木基因组大小约为890.52±24.69 Mb;(2)K-mer分析估测银缕梅基因组大小为951.70 Mb,杂合率为1.740%,重复序列比例为77.50%;波斯铁木基因组大小为858.50 Mb,杂合率为0.695%,重复序列占74.30%;(3)银缕梅属于高杂合和高重复基因组,波斯铁木则属于微杂合和高重复基因组。本研究的结果为银缕梅属植物后续基于DNA三代高通量测序技术的全基因组测序、组装及去冗余处理等工作提供了重要的数据参考。     

采自西藏和新疆的7种中国新记录植物

本文报道了6个中国被子植物新记录种及1个新记录亚种, 分别是采自西藏的灰滨藜(Atriplex pallida)、类球花藜(Blitum litwinowii)、滨藜状藜(Chenopodium atripliciforme)、土耳其针茅(Stipa turkestanica)、扁果岩蓼(Polygonum cognatum subsp. chitralicum)及新疆的宝格达黄芪(Astragalus baitagensis)和神香草叶千屈菜(Lythrum hyssopifolia), 观察了部分类群的微形态特征并提供了生境或形态图。凭证标本均存放于内蒙古大学植物标本馆(HIMC)。     

树冠结构对典型阔叶红松林生产力的影响

阔叶红松(Pinus koraiensis)林是东北东部山区的地带性森林植被, 阐明其生产力的影响因素, 对于理解温带森林生产力维持机制具有重要意义。该研究依托小兴安岭典型阔叶红松林9 hm²动态监测样地, 基于2005和2015年的30 m × 30 m样方内所有胸径>6.5 cm的木本植物的调查数据, 计算各样方的树冠结构复杂性、物种多样性和林分胸高断面积, 结合各样方的地形和土壤理化性质数据, 拟合结构方程模型, 定量分析影响典型阔叶红松林生产力的直接和间接因素。研究结果显示: 树冠结构复杂性和物种多样性与生产力显著正相关, 且树冠结构复杂性对生产力的影响显著高于物种多样性; 树冠结构复杂性对生产力的作用分为树冠垂直分层和树冠可塑性, 其中树冠垂直分层是树冠结构复杂性影响阔叶红松林生产力的主要因素, 而树冠可塑性无显著影响; 林分胸高断面积与生产力显著正相关, 其解释权重仅次于树冠结构复杂性, 树冠结构复杂性与物种多样性均通过影响林分胸高断面积对阔叶红松林生产力产生间接影响; 考虑不同树冠结构复杂性时, 坡度和土壤全磷含量代表的环境因素在调节生产力上发挥的作用存在差异, 移除树冠垂直分层的作用后两者与生产力呈显著的负相关关系。综上可知, 在典型阔叶红松林中, 树冠结构复杂性比物种多样性更有效地解释了生产力的变化, 同时不可忽视其他生物和非生物因素对生产力的作用。     

草地土壤有机质不同组分氮库对长期氮添加的响应

土壤氮库对生态系统的养分循环至关重要。目前多数研究主要关注氮沉降对土壤总氮的影响, 而对土壤不同有机质组分的氮库对氮沉降响应的研究较为缺乏。该研究基于内蒙古典型草地的长期多水平施氮(0、8、32、64 g·m^-2·a^-1)实验平台, 利用土壤密度分级方法, 探究氮添加处理13年后典型草地中两种土壤有机质组分(颗粒态有机质(POM), 矿质结合态有机质(MAOM))氮含量的变化及调控机制。结果显示: 土壤总碳含量、POM和MAOM的碳含量在施氮处理间均没有显著差异。土壤总氮含量则随着施氮水平增加呈显著增加的趋势, 同时施氮处理下POM的氮含量显著上升, 而MAOM的氮含量没有变化。进一步分析发现, 施氮促进植物地上生物量积累, 增加了凋落物量及其氮含量, 从而导致POM的氮含量增加。由于MAOM主要通过黏土矿物等吸附土壤中小分子有机质形成, 其氮含量受土壤中黏粒与粉粒含量影响, 而与氮添加水平无显著相关关系。该研究结果表明长期氮添加促进土壤氮库积累, 但增加的氮主要分布在稳定性较低的POM中, 受干扰后容易从生态系统中流失。为了更准确地评估和预测氮沉降对陆地生态系统的氮循环过程的影响, 应考虑土壤中不同有机质组分的差异响应。