中药化学融入中医类专业的三维教学实践——以大黄为例

随着现代医药技术的迅速发展,人们对于疾病原因和药物作用机理认识日益深刻,单纯宏观思维模式已难以适应新时代下中医的教学与发展需求,亟须引入新的教学方法或模式。中医药防治疾病有赖于其药效物质基础——中药化学成分,本文在中医药理论指导下,以大黄为例,围绕蒽醌类化学成分,将化学引入中医的教学实践。通过理论、实践及拓展这三个维度的课堂教学,有效提升了学生对中医药的认知和应用能力,为中医复合型人才培养提供了参考。

羟基化合物的催化转化研究:酚类与醇类化合物转化为醚与酯

在当前经济快速发展的背景下,高附加值化学品的高效绿色合成备受关注,而羟基化合物的催化转化产物醚与酯是近年来受到国内外广泛关注的环保型绿色化工产品。然而,苛刻的反应条件限制了其在催化有机合成领域的发展。基于此,本文概述了酚烷基化制备醚与醇氧化酯化制备酯的研究进展,重点总结了对催化体系改性的策略以及催化机理。主要对非均相催化体系及其机理进行讨论与概述,发现酸碱位协同催化以及金属与载体间的协同催化有利于实现醚与酯的低温、绿色合成。此外,光催化被认为是一种富有潜力的绿色合成方法,本文还介绍了光催化在醇氧化酯化反应中的应用。最后,对羟基化合物催化转化的研究工作进行了总结,并对其在催化技术中面临的挑战及未来的发展进行了展望,我们认为新型催化剂的合成与改性及其催化机理的探索仍是前景广阔的研究领域。

Interacting with α7 nAChR is a new mechanism for AChE to enhance the inflammatory response in macrophages

Acetylcholine(ACh)regulates inflammation viaα7 nicotinic acetylcholine receptor(α7 nAChR).Acetylcholinesterase(AChE),an enzyme hydrolyzing ACh,is expressed in immune cells suggesting non-classical function in inflammatory responses.Here,the expression of PRiMA-linked G4 AChE was identified on the surface of macrophages.In lipopolysaccharide-induced inflammatory processes,AChE was upregulated by the binding of NF-κB onto the ACHE promotor.Conversely,the overexpression of G4 AChE inhibited ACh-suppressed cytokine release and cell migration,which was in contrast to that of applied AChE inhibitors.AChEmt,a DNA construct without enzymatic activity,was adopted to identify the protein role of AChE in immune system.Overexpression of G4 AChEmt induced cell migration and inhibited ACh-suppressed cell migration.The co-localization ofα7 nAChR and AChE was found in macrophases,suggesting the potential interaction ofα7 nAChR and AChE.Besides,immunoprecipitation showed a close association ofα7 nAChR and AChE protein in cell membrane.Hence,the novel function of AChE in macrophage by interacting withα7 nAChR was determined.Together with hydrolysis of ACh,AChE plays a direct role in the regulation of inflammatory response.As such,AChE could serve as a novel target to treat age-related diseases by antiinflammatory responses.

Upregulation of Spinal Voltage-Dependent Anion Channel 1 Contributes to Bone Cancer Pain Hypersensitivity in Rats

Voltage-dependent anion channel 1（VDAC1） is thought to contribute to the progression of tumor development. However, whether VDAC1 contributes to bone cancer pain remains unknown. In this study, we found that the expression of VDAC1 was upregulated in the L2–5 segments of the spinal dorsal horn at 2 and 3 weeks after injection of tumor cells into the tibial cavity. Intrathecal injection of a VDAC1 inhibitor significantly reversed the pain hypersensitivity and reduced the over-expression of Toll-like receptor 4（TLR4）. Intrathecal injection of minocycline, an inhibitor of microglia, also attenuated the pain hypersensitivity of rat models of bone cancer pain.These results suggest that VDAC1 plays a significant role in the development of complicated cancer pain, possibly by regulating the expression of TLR4.

An optimization of ultra-sonication-assisted extraction from flowers of Apocynum venetum in targeting to amount of free amino acids determined by UPLC-MS/MS

Amino acids are naturally occurring compounds in many edible or medicinal plants,which possess a variety of nutraceutical effects in human.Here,a method of ultrasound-assisted extraction was optimized using Box-Behnken design of response surface methodology in maximizing the yield of free amino acids deriving from flowers of Apocynum venetum L.Under the optimal condition of ultrasound-assisted extraction,i.e.187.5 W of ultrasonic power,31.93 min of extraction time,and 0.47 mg/ml of solid-liquid ratio,the experimental yield of extractive was 287.17±0.205 mg/g,which was in close agreement with the value,as predicted by the established model.In addition,a hydrophilic interaction ultra-high performance liquid chromatography coupled with QqQ-MS/MS method was developed and validated for simultaneous quantification of 20 types of amino acids without derivatization contained in A.venetum flowers.The analytical method was validated by matrix effect,linearity,limit of detection,limit of quantification,precision,repeatability,stability,and recovery.The analysis results showed that A.venetum flower was rich in free amino acids of~3%of total dried weight,and which contained leucine(13.7 g/mg),isoleucine(7.9 g/mg),and lysine(2.2 g/mg)as the most abundant amino acids.Thus,A.venetum flower could provide beneficial nutrient values for human health,e.g.adult weight maintenance or glucose homeostasis.