雷公藤内酯醇和缬沙坦对高糖诱导小鼠足细胞活性的影响

目的观察不同浓度高糖对小鼠足细胞活性的抑制作用,以及不同浓度雷公藤内酯醇（TP）和缬沙坦（Val）对高糖抑制后小鼠足细胞活性的影响,探讨高糖对足细胞的损伤作用,以及有效的药物干预浓度范围。方法将培养成熟的小鼠足细胞随机分为对照组（11.1mmol/L葡萄糖）和不同浓度高糖组（16.1、21.1、26.1、31.1、36.1mmol/L）,以上述浓度培养48h后采用CCK-8检测足细胞活性的变化。取活性变化最大的浓度为高糖诱导浓度,在此基础上随机分为不同浓度的TP组（4、8、16、32、64ng/ml）和Val组（2×10-8、2×10-7、2×10-6、2×10-5、2×10-4mol/L）,以上述浓度干预48h后,采用CCK-8检测足细胞活性的变化。结果（1）与对照组相比,除16.1mmol/L高糖组外,其余各高糖组的足细胞活性显著减少,其中以26.1mmol/L葡萄糖组减少最为明显（P＜0.01）。（2）与26.1mmol/L葡萄糖组相比,TP组（除4ng/ml组外）和Val组（除2×10-8mol/L组外）足细胞活性部分恢复,其中以16ng/mlTP组和2×10-5mol/LVal组足细胞活性恢复最为明显（P＜0.01）。结论一定浓度范围的TP和Val可部分恢复受高糖抑制的小鼠足细胞活性。     

Synthesis of Lithium Boracarbonate Ion Pairs by Copper‐Catalyzed Multi‐Component Coupling of Carbon Dioxide,Diboron, and Aldehydes

The catalytic selective multi‐component coupling of CO₂, bis(pinacolato)diboron, LiOtBu, and a wide range of aldehydes has been achieved for the first time by using an NHC‐copper catalyst. This transformation has efficiently afforded a series of novel lithium cyclic boracarbonate ion pair compounds in high yields from readily available starting materials. This protocol has not only provided a new catalytic process for the utilization of CO₂, but it has also constituted a novel route for the efficient synthesis of a new class of lithium borate compounds that might be of interest as potential electrolyte candidates for lithium ion batteries.     

Electrochemical C−H/N−H Functionalization for the Synthesis of Highly Functionalized (Aza)indoles

Indoles and azaindoles are among the most important heterocycles because of their prevalence in nature and their broad utility in pharmaceutical industry. Reported herein is an unprecedented noble‐metal‐ and oxidant‐free electrochemical method for the coupling of (hetero)arylamines with tethered alkynes to synthesize highly functionalized indoles, as well as the more challenging azaindoles.     

Design,synthesis, and antimicrobial activities of new tanshinone IIA esters

Sixteen new ester derivatives with various partition coefficient (ClogP) values of tanshinone IIA (TSIIA), a major lipophilic component of Salvia miltiorrhiza, were designed and synthesised, including six aliphatic esters (3a–e, 5a), one phosphate ester (4c) and nine aromatic esters (5b–j). Their antimicrobial activities against three Gram-positive bacteria strains, Staphylococcus aureus, Bacillus subtilis, and Bacillus amyloliquefaciens, and two Gram-negative bacteria strains, Pseudomonas aeruginosa and Escherichia coli, as well as two fungi species, Candida albicans and Saccharomyces cerevisiae, were evaluated in vitro by broth microdilution susceptibility tests. The results showed that keeping ClogP values in a certain range is necessary for their antimicrobial activities. For those compounds with ClogP values between 5 and 10, their MIC values showed positive correlations with ClogP values. In particular, compound 3e exhibited fourfold and twofold higher potency than the standard drug amphotericin B against fungi C. albicans and S. cerevisiae with MIC values of 1.95 and 7.81 μg/mL, respectively.     

Chemical constituents from Agrimonia pilosa Ledeb. and their chemotaxonomic significance

Phytochemical investigation of the ethanol extract from the whole plant of Agrimonia pilosa led to the isolation of 31 compounds, including 16 flavonoids (1–16), 5 triterpenes (17–21), 1 isocoumarin (22), 5 phenolic acids (23–27), 1 ceramide (28), 2 agrimols (29–30) and 1 fatty acid (31). Their structures were determined by various spectroscopic analyses. Compounds 5, 7 and 20 were firstly isolated from the genus Agrimonia, and compounds 6, 10–11, 15, 26, 28 and 31 were isolated from the family Rosaceae for the first time. Moreover, the chemotaxonomic significance of these compounds was summarised.     

Synthesis and crystal structures of C24‐epimeric 20(R)‐ocotillol‐type saponins

Ocotillol‐type saponins have a wide spectrum of biological activities. Previous studies indicated that the configuration at the C24 position may be responsible for their stereoselectivity in pharmacological action and pharmacokinetics. Natural ocotillol‐type saponins share a 20(S)‐form but it has been found that the 20(R)‐stereoisomers have different pharmacological effects. The semisynthesis of 20(R)‐ocotillol‐type saponins has not been reported and it is therefore worthwhile clarifying their crystal structures. Two C24 epimeric 20(R)‐ocotillol‐type saponins, namely (20R,24S)‐20,24‐epoxydammarane‐3β,12β,25‐triol, C₃₀H₅₂O₄, (III), and (20R,24R)‐20,24‐epoxydammarane‐3β,12β,25‐triol monohydrate, C₃₀H₅₂O₄·H₂O, (IV), were synthesized, and their structures were elucidated by spectral studies and finally confirmed by single‐crystal X‐ray diffraction. The (Me)C—O—C—C(OH) torsion angle of (III) is 146.41 (14)°, whereas the corresponding torsion angle of (IV) is −146.4 (7)°, indicating a different conformation at the C24 position. The crystal stacking in (III) generates an R₄⁴(8) motif, through which the molecules are linked into a one‐dimensional double chain. The chains are linked via nonclassical C—H…O hydrogen bonds into a two‐dimensional network, and further stacked into a three‐dimensional structure. In contrast to (III), epimer (IV) crystallizes as a hydrate, in which the water molecules act as hydrogen‐bond donors linking one‐dimensional chains into a two‐dimensional network through intermolecular O—H…O hydrogen bonds. The hydrogen‐bonded chains extend helically along the crystallographic a axis and generate a C₄⁴(8) motif.     

通道调制型偏振成像系统的波段宽度限制判据

通道调制型偏振成像技术是一种体积紧凑、空间分辨率高且能够实时获取全偏振信息的新型偏振成像探测技术. 但该技术目前只能实现准单色光的全偏振探测, 严重制约了其实用化. 本文首先对宽带光通道调制型偏振成像出现混叠现象的原因进行了分析, 得出载波频率是限制波段宽度的主要因素. 据此在空间频谱域上分析并推导了通道调制型偏振成像系统的光谱宽度限制判据公式, 同时通过模型仿真得到了系统的极限有效光谱范围, 与理论推导公式结果进行了对比分析, 验证了判据的准确性. 基于该判据可预测给定通道调制型偏振成像系统的有效工作波段, 同时还可为扩展系统波段宽度提供理论支撑.