A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring Nε-thioacetyl-lysine

Past few years have seen an active pursuit of the inhibitors for the deacylation catalyzed by the seven human sirtuins (i.e. SIRT1-7) as valuable chemical biological/pharmacological probes of this enzymatic deacylation and lead compounds for developing novel therapeutics for human diseases. In the current study, we prepared eight monocyclic and one bicyclic analogs of a linear pentapeptide-based potent (sub-μM IC₅₀’s) pan-SIRT1/2/3 inhibitor Zheng laboratory discovered recently that harbors the catalytic mechanism-based SIRT1/2/3 inhibitory warhead N^ε-thioacetyl-lysine at its central position. We found that the bicyclic analog exhibited largely comparable SIRT1/2/3 inhibitory potencies to those of the parent linear pentapeptide, however, the former is proteolytically much more stable than the latter. Moreover, the bicyclic analog displayed very weak inhibition against SIRT5/6/7, was cell permeable, and exhibited an anti-proliferative effect on the human SK-MEL-2 melanoma cells. This bicyclic analog could be a lead for the future development of more potent and still selective pan-SIRT1/2/3 inhibitors whose use in studies on human sirtuin biology, pharmacology, and medicinal chemistry could complement with the use of the potent inhibitors selective for a single human sirtuin.     

市县级限制开发区环境功能区划研究——以河北省张家口市为例

限制开发地区是我国主体功能区划中划定的提供重要生态功能和农产品的地区,对其进行环境功能区划对于推动环境功能区划制度落地与实施,以及限制开发区的保护与发展有着重要意义。当前国家及省级的环境功能区划研究已经相对成熟,而市县尺度的限制开发地区环境功能区划相关研究较少。在总结现有环境功能区划研究方法的基础上,以河北省张家口市为例,探讨了市县级限制开发地区环境功能区划体系设计和技术方法,提出了以公里格网作为分析单元,结合县域行政边界,基于环境功能综合评价的结果,从自然生态安全、维护人群健康和区域环境支撑能力等3个方面,开展环境功能区划。基于该方法,将张家口市分为自然生态保留区、生态功能保持区、生态功能恢复区、农产品安全保障区、环境开发准入区、聚居发展维护区6类环境功能区,并根据各环境功能区的主要功能及生态环境特点提出相应的发展建议,以期为该区域管理提供可行的操作手段。本文提出的方法也可为其他限制开发地区的环境功能区划提供参考。     

火干扰强度对亚热带四种森林类型土壤理化性质的影响

火干扰是通过改变土壤理化性质而影响土壤生态系统功能的重要因素之一。探讨火干扰强度对不同森林类型下土壤理化性质的影响,为利用火干扰促进林分更新及经营提供理论指导。2014年在湖南省株洲市和湘潭市4种次生林(枫香次生林、马尾松-木荷混交林、杉木-木荷混交林及檫木-杉木混交林)内设置16块20 m×20 m样地进行试验,研究了火干扰强度(对照、低强度、中强度、高强度火烧)和林分类型对土壤容重(BD)、土壤斥水性(SWR)、有机质(SOM)、pH、全氮(TN)、全磷(TP)和全钾(TK)的影响。通过描述性统计分析、单因素方差分析和Fisher LSD检验研究各土壤性质在同一林分不同火干扰间,以及同一火干扰下不同林分间的显著性差异和变化趋势(P0.05)。研究发现BD、SWR、pH、TK都随火强度的增大呈上升的趋势,而SOM、TP随火强度增大而减少,TN则随火强度增大没有规律性变化。在同一林分内与对照组相比,低强度火烧对BD、SWR、pH和SOM的影响不显著,中强度有一定影响,而高强度火烧影响显著;而TN、TP、TK在火烧前后均无显著性差异。火干扰后,TN和TP在同一火强度下不同林分间均存在显著性差异(P0.05),而BD、pH值和TP在同一林分内不同火强度间均存在显著性差异(P0.05)。BD、SOM、pH、TK在枫香次生林内普遍显著大于其他林分。结果说明火干扰强度和林分类型在影响土壤理化性质方面起着重要作用。高强度火干扰对土壤性质影响最大,枫香次生林中土壤理化性质与其他混交林相比普遍存在显著性差异。BD、pH和TP受火强度影响显著,BD、SOM、pH、TN、TK和TP受林分类型影响显著。     

基于生态系统服务和生态系统健康的生态风险评价——以长株潭城市群为例

基于生态系统服务和生态系统健康的生态风险评估框架为城市群生态风险管理和国土生态修复提供新的视角。以生态风险评估框架为基础,综合运用生态系统服务、生态系统健康评估模型以及相关分析法对长株潭城市群展开生态风险评价,并对风险程度进行分类。结果表明:(1)城市群的城市化水平提升,区域生态风险也随之增加。生态系统服务价值、生态系统组织、生态系统活力、生态系统弹性等生态指数呈现下降趋势。(2)人工表面比率和生态指数之间的Pearson相关系数表明,人工表面比率与生态指数之间存在负相关关系,人工表面比率是生态风险提升的关键因素。(3)城市群人工表面比率要控制在36%以下,以进行生态风险管理和国土生态修复。总的来说,评价框架可以作为区域生态风险的评价终点。     

巴氏芽孢杆菌矿化作用机理及应用研究进展

本文介绍了具有诱导碳酸钙矿化功能的巴氏芽孢杆菌及其矿化核心酶脲酶的结构与功能,较为系统地综述了巴氏芽孢杆菌矿化作用的生物机制,简要介绍了国内外多领域关于巴氏芽孢杆菌矿化应用的研究现状及典型应用案例,并探讨了相应微生物矿化技术在特定环境下的应用前景及在未来应用中可能存在的不足之处,相关分析论述对进一步推进微生物矿化技术的应用具有较为重要的意义.     

不同缓释过氧化钙对潜育环境下水稻土微生物特性的影响

为了解不同缓释过氧化钙对潜育化稻田土壤微生物特性的影响,于网室内进行潜育化稻田环境模拟试验,以不施过氧化钙为对照,探究过氧化钙粉末、过氧化钙颗粒与4种不同释氧效果的包膜过氧化钙在早稻分蘖期同等时期对潜育化稻田土壤活性有机碳、有效养分及微生物特性的影响。结果表明: 施用过氧化钙均能提高土壤活性有机碳、有效养分、微生物生物量及可培养微生物数量和酶活性,包膜过氧化钙对土壤微生物和酶活性的改善效果较好,其次依次为过氧化钙颗粒和过氧化钙粉末。包膜过氧化钙处理中,以乙基纤维素包膜效果最好,与不施过氧化钙处理相比,其土壤活性有机碳、微生物生物量碳、微生物生物量氮、微生物生物量磷分别显著提高19.4%、11.4%、121.5%、127.2%,土壤碱解氮和有效磷分别提高4.0%和45.5%;土壤可培养细菌和可培养微生物总量分别显著提高137.3%和113.7%,真菌和放线菌数量分别提高33.6%和44.7%;蔗糖酶、磷酸酶和脲酶活性分别显著提高92.4%、91.8%和112.5%,过氧化氢酶活性提高17.1%。研究结果可为包膜过氧化钙对潜育化稻田改良提供参考。     

Phenotypic and genetic dissection of cadmium accumulation in roots,nodes and grains of rice hybrids

Plant and Soil - Rice accumulates higher levels of cadmium (Cd) in grain than other cereals, and hybrid rice varieties cover around half of the total rice area in China. Therefore, understanding...     

Anatomy and lignin deposition of stone cell in Camellia oleifera shell during the young stage

Protoplasma - As the by-products of edible oil production with rich lignin, the reserves of Camellia oleifera shell were abundant and had a great economic value. Lignin was the most important...     

Screening of immunosuppressive cells from colorectal adenocarcinoma and identification of prognostic markers

Background: Colorectal cancer (CRC) is the most common type of gastrointestinal malignant tumour. Colorectal adenocarcinoma (COAD) – the most common type of CRC – is particularly dangerous. The role of the immune system in the development of tumour-associated inflammation and cancer has received increasing attention recently.Methods: In the present study, we compiled the expression profiles of 262 patients with complete follow-up data from The Cancer Genome Atlas (TCGA) database as an experimental group and selected 65 samples from the Gene Expression Omnibus (GEO) dataset (of which 46 samples were with M0) as a verification group. First, we screened the immune T helper 17 (Th17) cells related to the prognosis of COAD. Subsequently, we identified Th17 cells-related hub genes by utilising Weighted Gene Co-expression Network Analysis (WGCNA) and Least Absolute Shrinkage and Selector Operation (LASSO) regression analysis. Six genes associated with the prognosis in patients with COAD were identified, including: KRT23, ULBP2, ASRGL1, SERPINA1, SCIN, and SLC28A2. We constructed a clinical prediction model and analysed its predictive power.Results: The identified hub genes are involved in developing many diseases and closely linked to digestive disorders. Our results suggested that the hub genes could influence the prognosis of COAD by regulating Th17 cells’ infiltration.Conclusions: These newly discovered hub genes contribute to clarifying the mechanisms of COAD development and metastasis. Given that they promote COAD development, they may become new therapeutic targets and biomarkers of COAD.