河南省桐柏-大别山旅游区发展战略研究

在分析河南省桐柏-大别山旅游区发展条件的基础上,提出了该区"红绿结合,跨区整合"、"政府主导,市场运作"、"加速升级,打造精品"的旅游发展战略和一些重要发展措施,确立了"一心、两带、四区"的旅游空间格局和"完善一个中心、力推三个组团、优先发展主轴、积极培育山前"的空间发展思路,旨在指导该区旅游业的科学有序发展.     

重金属联合毒性对蚤类与鱼类敏感性的影响及预测模型研究进展

通过阅读文献了解各类重金属在联合作用情况下对水生生物产生的毒性效应并讨论了联合毒性的作用机制.研究了水环境中重金属污染对水生生物的敏感性影响,介绍了联合毒性作用的具体表现形式,总结了包括蚤类、鱼类等常见水生生物的收集与培养、联合毒性实验的具体步骤与结果讨论,对联合毒性的两种基本模型原理与预测结果进行了阐述.结果表明,水...     

In Vitro Antineoplastic and Antiviral Activity and In Vivo Toxicity of Geum urbanum L. Extracts

This study evaluated the in vitro antineoplastic and antiviral potential and in vivo toxicity of twelve extracts with different polarity obtained from the herbaceous perennial plant Geum urbanum L. (Rosaceae). In vitro cytotoxicity was determined by ISO 10993-5/2009 on bladder cancer, (T-24 and BC-3C), liver carcinoma (HEP-G2) and normal embryonic kidney (HEK-293) cell lines. The antineoplastic activity was elucidated through assays of cell clonogenicity, apoptosis induction, nuclear factor kappa B p65 (NFκB p65) activation and total glutathione levels. Neutral red uptake study was applied for antiviral activity. The most promising G. urbanum extract was analyzed by UHPLC–HRMS. The acute in vivo toxicity analysis was carried out following OEDC 423. The ethyl acetate extract of aerial parts (EtOAc-AP) exhibited the strongest antineoplastic activity on bladder cancer cell lines (IC₅₀ = 21.33–25.28 µg/mL) by inducing apoptosis and inhibiting NFκB p65 and cell clonogenicity. EtOAc and n-butanol extracts showed moderate antiviral activity against human adenovirus type 5 and human simplex virus type I. Seventy four secondary metabolites (gallic and ellagic acid derivatives, phenolic acids, flavonoids, etc.) were identified in EtOAc-AP by UHPLC–HRMS. This extract induced no signs of acute toxicity in liver and kidney specimens of H-albino mice in doses up to 210 mg/kg. In conclusion, our study contributes substantially to the detailed pharmacological characterization of G. urbanum, thus helping the development of health-promoting phytopreparations.     

南宁市城市森林发展现状与对策

介绍南宁市城市森林的发展及城市空间格局的变迁,指出南宁市城市森林发展中存在缺乏长期全面合理的规划、城市森林体系尚未形成,大量使用草坪、绿化模式单一,城市森林的经营管理水平较低、缺乏高层次的管理人才等问题.建议南宁市城市森林建设要与城市空间格局、环境格局相结合,完善城市森林体系建设;要因地制宜,突出地方城市森林特色;要将城市森林纳入生态网络,促进生物多样性和景观多样性;要保护城市生态环境,提高全民城市森林建设意识.     

Musa sp. Leaves Extract Ameliorates the Hepato-Renal Toxicities Induced by Cadmium in Mice

Heavy metals intoxication causes several health problems that necessitate finding new protective and therapeutic approaches. This study aimed to evaluate the impact of Musa sp. leaves extract (MLE) on hepato-renal toxicities induced by cadmium (Cd) in male mice. The phytochemical screening, metal chelating activity (MCA), and the median lethal dose (LD₅₀) of MLE were determined. Fifty CD-1 male mice were used and intraperitoneally (i.p.) injected with MLE (1000 to 5000 mg/kg b.wt) for MLE LD₅₀ determination. Another 50 mice were used for evaluating the effect of MLE on Cd toxicity. Blood samples were collected for hematological, liver, and kidney functions assessments. Liver tissue homogenates were used for determination of oxidant/antioxidant parameters. Liver and kidney tissues were harvested for histopathological and molecular investigations. MLE showed potent in vitro antioxidant activities. The MCA and LD₅₀ of the MLE were 75 µg/mL and 3000 mg/kg b.wt, respectively. MLE showed beneficial therapeutic activity against hepato-renal toxicities in Cd-intoxicated mice, evidenced by improving the hematological, biochemical, histopathological, and molecular alterations.     

芦荟毒理作用研究

观察芦荟毒性作用.采用最大给药量及长期毒性测定芦荟毒性作用.芦荟最大给药量为临床成人1 d(4.5 g)口服量的1 400倍,长期毒性实验对血液学、血液生化学及重要组织形态学观察未见病理学改变.芦荟毒性低微长期用药安全.     

邻苯二甲酸丁基苄酯对雄性大鼠生殖系统影响

研究邻苯二甲酸丁基苄酯(BBP)对雄性生殖内分泌系统的损害作用及其机制．将不同剂量的BBP(0、0．45、0．9、1．8 mL/kg),每日对Wistar雄性大鼠连续灌胃,染毒30 d、60 d,测定大鼠血清中FSH、LH、T和睾丸匀浆中T的水平及睾丸标志酶ACP、γ-GT的活性．随着BBP染毒剂量的增加及时间的延长血清中及睾丸匀浆中T的水平显著下降(P＜0．01),血清中LH、FSH呈上升趋势(P＜0．05),睾丸中ACP水平先升后降,γ-GT的活性则明显下降(P＜0．01)．BBP对雄性失鼠有明显的生殖毒性,影响其血清及睾丸性激素水平和酶活性,这可能与BBP对支持细胞和生精上皮的损害有关．     

Identification of the New Metabolite of Nebivolol Using Liquid Chromatography Coupled with High-Resolution Mass Spectrometry and Chemometrics

In this study, the phase I hepatic metabolism pathway of a cardiovascular drug nebivolol was proposed on the basis of a human liver microsomes assay with the use of LC-HR-MS coupled with the chemometric method. Six biotransformation products were found with the assistance of chemometric analysis. Five of them were identified as the previously reported products of alicyclic hydroxylation and dihydroxylation, aromatic hydroxylation, as well as alicyclic oxidation of the parent compound. Moreover, one metabolite, not reported so far, was found to be a product of N-dealkylation of nebivolol—2-amino-1-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)ethan-1-ol. The novel metabolite was submitted to an in silico toxicity analysis to assess its biological properties. The applied computational methods indicated a significantly elevated risk of its mutagenic activity, compared to the parent molecule. Several metabolites of the nebivolol described in the literature were not detected in this study, indicating their non-hepatic origin.     

全球性环境污染物多氯联苯的结构-活性相关性研究进展*

本文对全球性典型污染物--多氯联苯(PCBs) 的结构-活性相关性研究的最新成果进行了综述。给出了该类环境污染物的分组归类、结构特征与活性、毒性当量因子的应用和利用有关结构模型阐述毒性机理的研究进展, 并对将来的有关研究方向做了展望。     

Computational design of rasagiline derivatives: Searching for enhanced antioxidant capability

A set of new rasagiline derivatives is presented. They were designed to be antioxidant compounds with the potential to be used for treating neurodegenerative disorders. They are expected to be multifunctional molecules that can help reduce oxidative stress, which is thought to contribute to neurodegenerative disorders. The CADMA-Chem computational protocol was used to produce rasagiline derivatives and to evaluate their likeliness as oral drugs and antioxidants. Three of them were identified as the most promising ones. They are proposed to be better free radical scavengers than rasagiline. In addition, they are expected to keep the parent's molecule neuroprotective capability. Hopefully, the results presented here would promote further experimental and theoretical investigations on these compounds.