白术的化学成分与药理作用及复方临床应用进展

白术作为一味传统中药,在历代本草著作中广泛记载,其功效有一定演变。现代研究发现,其主要化学成分有挥发油、多糖、内酯类等,具有抗肿瘤、抗炎、调节消化系统等药理作用。临床以中药复方的形式应用于胃肠道疾病、心血管疾病、免疫系统疾病、肝脏疾病等治疗。对近5年SCI收录的白术相关文章进行分析,简述其化学成分,重点围绕着药理作用以及复方的临床应用展开论述,为其进一步开发利用提供参考。     

重楼多指标UPLC定量分析及其化学品质综合评价

目的探讨10种重楼药材中7种有效成分含量,并进行化学成分整合评控,为其资源评价提供了科学依据。方法收集不同产地55批重楼药材,采用UPLC法测定重楼皂苷Ⅰ、重楼皂苷Ⅱ、重楼皂苷Ⅵ、重楼皂苷Ⅶ、薯蓣皂苷、重楼皂苷H、纤细薯蓣皂苷的含量,进一步采用TOPSIS数学模型对含量结果进行归一化与多指标数据集成化,获得重楼中7种指标的化学品质综合指数。结果 10种重楼药材的综合评价排名由高到低依次为长柱重楼(Ci=0.275 5)多叶重楼(Ci=0.273 2)大理重楼(Ci=0.269 8)滇重楼(Ci=0.244 5)南重楼(Ci=0.234 5)狭叶重楼(Ci=0.159 1)黑籽重楼(Ci=0.141 6)矮重楼(Ci=0.117 8)七叶一枝花(Ci=0.115 1)毛重楼(Ci=0.114 9),表明不同种重楼化学综合质量差异较大,其长柱重楼、多叶重楼和大理重楼的化学综合质量优于滇重楼,南重楼与滇重楼的结果较为接近,可作为滇重楼资源扩充的优势品种。结论通过TOPSIS整合评控对重楼类中药材的质量评价有一定的参考依据。     

Discovery of nitazoxanide-based derivatives as autophagy activators for the treatment of Alzheimer's disease

Drug repurposing is an efficient strategy for new drug discovery. Our latest study found that nitazoxanide (NTZ), an approved anti-parasite drug, was an autophagy activator and could alleviate the symptom of Alzheimer's disease (AD). In order to further improve the efficacy and discover new chemical entities, a series of NTZ-based derivatives were designed, synthesized, and evaluated as autophagy activator against AD. All compounds were screened by the inhibition of phosphorylation of p70S6K, which was the direct substrate of mammalian target of rapamycin (mTOR) and its phosphorylation level could reflect the mTOR-dependent autophagy level. Among these analogs, compound 22 exhibited excellent potency in promoting β-amyloid (Aβ) clearance, inhibiting tau phosphorylation, as well as stimulating autophagy both in vitro and in vivo. What's more, 22 could effectively improve the memory and cognitive impairments in APP/PS1 transgenic AD model mice. These results demonstrated that 22 was a potential candidate for the treatment of AD.     

不同干燥方法对桂枝药材中苯丙素类成分的影响及评价

目的:研究不同干燥方法对桂枝药材中苯丙素类(香豆素、肉桂醇、肉桂酸、桂皮醛、邻甲氧基肉桂醛)化学成分的影响,为桂枝适宜干燥方法的确定提供依据。方法:以苯丙素类化学成分含量为评价指标,分别对晒干、阴干及3种现代加工干燥方法后桂枝的质量进行评价,通过SPSS软件进行主成分分析,利用主成分得分进行综合评价。结果:不同干燥处理方法后有效成分含量差异较大,其中微波干燥使有效成分损失最多,阴干、晒干、低温热风干燥有利于桂枝有效成分的保留。结论:以干燥时间、化学成分含量、外观性状、气味等为评价指标,确定热风干燥50℃为桂枝药材较为适宜的现代干燥加工方法。     

HPLC法同时测定外感风寒颗粒中10种成分

目的建立HPLC法同时测定外感风寒颗粒(桂枝、防风、葛根等)中苦杏仁苷、3’-羟基葛根素、葛根素、3’-甲氧基葛根素、升麻素苷、升麻素、5-O-甲基维斯阿米醇苷、亥茅酚苷、肉桂酸、桂皮醛的含有量。方法该药物甲醇提取液的分析采用Agilent ZORBAX Eclipse XDB-C18色谱柱(4.6 mm×250 mm,5μm);流动相乙腈-0.1%磷酸,梯度洗脱;体积流量1.0 m L/min;柱温25℃;检测波长207、254、280 nm。结果 10种成分在各自范围内线性关系良好(r≥0.999 1),平均加样回收率为96.97%~100.08%,RSD为0.80%~1.45%。结论该方法简便、重复性好,可用于外感风寒颗粒的质量控制。     

一测多评法同时测定九味沉香胶囊中9种成分

目的 建立一测多评法同时测定九味沉香胶囊(沉香、广枣、黄芪等)中沉香四醇、毛蕊异黄酮葡萄糖苷、芒柄花苷、毛蕊异黄酮、芒柄花素、木香羟内酯、去氢木香内酯、肉豆蔻木脂素、去氢二异丁香酚的含有量.方法 该药物甲醇提取液的分析采用Agilent Zorbax SB-C18色谱柱(250 mm×4.6 mm,5μm);流动相[乙腈-甲醇(9∶1)]-0.1%甲酸,梯度洗脱;体积流量1.0 mL/min;柱温30℃;检测波长225、254、270 nm.以木香羟内酯为内标,计算其他8种成分的相对校正因子,测定含有量.结果 9种成分在各自范围内线性关系良好(r>0.999 0),平均加样回收率96.95%~ 100.12%,RSD 0.73%~ 1.51%.一测多评法所得结果与外标法接近.结论 该方法简便准确,重复性好,可用于九味沉香胶囊的质量控制.     

骨碎补化学成分和生物活性研究进展＊

骨碎补是历代临床常用中药，具有疗伤止痛、补肾强骨、消风祛斑等功效。其主要含黄酮、苯丙素、三萜、酚酸及其苷等类化学成分，现代研究表明骨碎补具有抗骨质疏松、促进骨折愈合、促软骨再生、护牙健齿、保护肾功能、抗炎、防治中毒性耳聋、降血脂等多种生物活性，开发前景广阔。本文对近年来骨碎补的化学成分、药理作用及临床应用研究进行综述，以期为骨碎补的进一步深入系统的研究和开发利用提供依据。     

Phytochemical and pharmacological progress on Syringa oblata, a traditional Mongolian medicine

Syringa oblata is a traditional Mongolian medicine mainly distributed in the Helan Mountains (the boundaries of Inner Mongolia and Ningxia, China) and the north of Yan Mountains (Aohan Qi, Inner Mongolia, China). It is clinically used to treat diseases caused by Heyi, such as heartache and heat pathogen in the heart. Phytochemical studies on S. oblata revealed the presence of iridoids, lignans, triterpenes, phenylpropanoids, phenylethanoids, and volatile components. Pharmacological investigations revealed a broad spectrum of bioactivities, such as antimicrobial, antioxidant, antiproliferative, and hepatoprotective effects. This article summarized the chemical components and pharmacological activities of S. oblata, providing a scientific rationale for its bioactive constituents, quality control, and utilization as an important medicine.     

Potential applications and human biosafety of nanomaterials used in nanomedicine

With the rapid development of nanotechnology, potential applications of nanomaterials in medicine have been widely researched in recent years. Nanomaterials themselves can be used as image agents or therapeutic drugs, and for drug and gene delivery, biological devices, nanoelectronic biosensors or molecular nanotechnology. As the composition, morphology, chemical properties, implant sites as well as potential applications become more and more complex, human biosafety of nanomaterials for clinical use has become a major concern. If nanoparticles accumulate in the human body or interact with the body molecules or chemical components, health risks may also occur. Accordingly, the unique chemical and physical properties, potential applications in medical fields, as well as human biosafety in clinical trials are reviewed in this study. Finally, this article tries to give some suggestions for future work in nanomedicine research. Copyright © 2017 John Wiley & Sons, Ltd.