Synthesis of Novel Diselenide‐Linked Porphyrin Dimers under Phase‐Transfer Catalysis Condition and Their Interactions with DNA

Novel diselenide‐linked porphyrin dimers were synthesized under phase‐transfer catalysis conditions. The targeted compounds were characterized by ¹H‐NMR, high‐resolution mass spectrometry, UV/VIS and fluorescence spectroscopies, redox‐potential measurements, and elemental analysis. The interaction of the title compounds with DNA was studied using UV/VIS, fluorescence, and circular dichroism (CD) spectroscopies. The relative rates of singlet‐oxygen production from the diselenide‐linked porphyrin dimers upon photoirradiation were also measured.     

城市群生态安全格局构建:概念辨析与理论思考

城市群是城市发展到一定阶段通过城市间物流、人流和能流高度融合而形成的区域性复合生态系统，如何保障城市群生态安全与健康发展成为当前关注的热点问题。本研究系统分析了生态安全、城市生态安全与城市群生态安全的内涵。认为狭义上城市群生态安全侧重于城市群内部生态空间优化和生态系统服务功能提升，重点关注城市群地区生态用地空间优化与"三生空间"（生态、生活及生产空间）的合理布局。广义上的城市群生态安全不仅需要考虑城市群内部生态系统结构和功能协调及其生态系统服务的供需平衡，也需要从区域尺度考虑城市群与其他区域之间的协调关系。城市群生态安全格局构建的目的则是保障城市群内部区域一体化协调发展，满足人们日常生活的基本需求，实现城市群与区域之间物流、能流和人流的有序流通。在城市群生态安全格局构建时，除了遵循生态安全一般性原则外，还需要遵循以下原则：①生态系统服务供需平衡尺度效应；②生态安全保障的阈值效应；③生态安全格局的空间联动效应。最后文章提出了城市群生态安全格局构建的基本思路和技术路径。     

Three new species of the leafhopper genus Tambocerus Zhang & Webb (Hemiptera,Cicadellidae) from southern China

Three new species, Tambocerus dentatus, T. longicaudatus and T. robustispinus spp. n. from southern China, are described and illustrated. A checklist and distribution to the Tambocerus species from China is provided together with a key for their separation.     

山岳型乡村旅游地“三生”空间演变及优化——德庆金林水乡的案例实证

以德庆县金林水乡为例,采用参与式观察和空间统计法,选取2000、2008年和2018年3个时段分析旅游发展对山岳型乡村旅游地"三生"空间的影响,并探讨了金林水乡"三生"空间的发展瓶颈及优化路径。研究发现:(1)旅游开发前,金林水乡土地结构与用地功能单一且呈片状分布;村落呈现传统乡村风貌,基础设施不健全;空间形态变化稳定,扩张缓慢。(2)旅游开发后,土地利用类型多样化,出现新型复合用地;土地功能利用复杂化,以服务旅游业为主;村庄景观风貌现代化,生活空间更加宜居。(3)旅游开发前后对比可得,土地平面占地规模化,空间用地以居民点为核心,呈圈层状向外围扩张;生产-生活-生态空间相互转化,乡村聚落重构特征较为显著;村落景观风貌的变化较大,呈现城镇化趋势。(4)金林水乡"三生"空间演化与旅游发展存在的问题表现在生产用地效率不高,生活用地质量较低,生态空间不断萎缩,在旅游产业发展上表现为旅游产品单一且缺乏创新,旅游服务功能不完善等。为此从生活空间的提质、生产空间增效、生态空间保护、旅游产业创新以及土地利用五方面提出优化建议。     

Design,synthesis, biological evaluation,and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors

A series of novel chalcone-rivastigmine hybrids were designed, synthesized, and tested in vitro for their ability to inhibit human acetylcholinesterase and butyrylcholinesterase. Most of the target compounds showed hBChE selective activity in the micro- and submicromolar ranges. The most potent compound 3 exhibited comparable IC₅₀ to the commercially available drug (rivastigmine). To better understand their structure activity relationships (SAR) and mechanisms of enzyme-inhibitor interactions, kinetic and molecular modeling studies including molecular docking and molecular dynamics (MD) simulations were carried out. Furthermore, compound 3 blocks the formation of reactive oxygen species (ROS) in SH-SY5Y cells and shows the required druggability and low cytotoxicity, suggesting this hybrid is a promising multifunctional drug candidate for Alzheimer’s disease (AD) treatment.     

Comparison Study of Bone Defect Healing Effect of Raw and Processed Pyritum in Rats

To evaluate and compare the effect of raw and processed pyritum on tibial defect healing, 32 male Sprague Dawley rats were randomly divided into four groups. After tibial defect, animals were produced and grouped: sham and control group were orally administrated with distilled water (1 mL/100 g), while treatment groups were given aqueous extracts of raw and processed pyritum (1.5 g/kg) for successive 42 days. Radiographic examination showed that bone defect healing effect of the treatment groups was obviously superior compared to that of the control group. Bone mineral density of whole tibia was increased significantly after treating with pyritum. Inductively coupled plasma-optical emission spectrometry showed that the contents of Ca, P, and Mg in callus significantly increased in the treatment groups comparing with the control. Moreover, serological analysis showed that the concentration of serum phosphorus of the treatment groups significantly increased compared with that of the control group. By in vitro study, we have evaluated the effects of drug-containing serum of raw and processed pyritum on osteoblasts. It was manifested that both the drug-containing sera of raw and processed pyritum significantly increased the mRNA levels of alkaline phosphatase and collagen type I. Protein levels of phosphorylated Smad2/3 also increased. The mRNA levels of osteocalcin and transforming growth factor β (TGF-β) type I and II receptors, as well as the protein levels of TGF-β1 in the processed groups, were higher than those in the control. In summary, both raw and processed pyritum-containing sera exhibited positive effects on osteoblasts, which maybe via the TGF-β1/Smad signaling pathway. Notably, the tibia defect healing effect of pyritum was significantly enhanced after processing.