中药糖肾方单体成分莫诺苷药理作用的研究进展

通过查阅近些年的国内外文献对中药糖肾方单体成分莫诺苷的药理作用及分子机制进行归纳、梳理、分析及总结。从分子机制角度阐述莫诺苷具有促进细胞生长、减轻炎性反应、抑制细胞内钙超载、抑制氧化应激、抗凋亡、抗凝等作用,以便为今后临床及实验研究提供更多科学依据。     

f_2相似因子法评价银杏酮酯缓释微丸大类成分总黄酮和各类成分的体外释放相关性研究

目的引入f_2相似因子法对银杏酮酯(GBE)缓释微丸的大类成分总黄酮和各类成分(包括黄酮类和萜内酯类)的释放曲线进行分析,以能较全面地评价其体外释放。方法运用紫外分光光度法、高效液相-质谱联用(HPLC-MS)测定GBE缓释微丸中大类成分(总黄酮)和各类成分(槲皮苷、异鼠李素、芦丁、槲皮素、银杏内酯A、银杏内酯B、银杏内酯C、白果内酯)的体外释放率,并进行f_2相似因子计算;采用扫描电镜法观察微丸释药前后的微观结构,结合方程拟合分别对微丸中总黄酮和各类成分的释药机制解析,以验证f_2相似因子法的可靠性。结果优化工艺的GBE微丸黄酮类和内酯类的各成分与大类成分总黄酮的f_2均大于50,说明大类成分总黄酮与各类成分体外释放曲线具有较好的相关性。释药机制解析进一步验证了该结果的可靠性。结论 f_2相似因子法可运用于多组分中药缓释制剂大类成分和各类成分的体外释放评价。     

野菊的化学成分及质量评价研究进展

野菊Chrysanthemum indicum在我国资源分布广泛,有良好的药用前景。目前研究发现野菊中主要含有黄酮类、苯丙素类以及萜类等主要化学成分,红外光谱法、高效液相色谱法、超高效液相色谱法、气相-质谱联用法、火焰原子吸收光谱法及相关分子生物技术等现代分析技术广泛应用于野菊的质量评价研究。针对野菊的化学成分及质量评价研究进展进行综述,为野菊的进一步开发利用提供科学依据。     

The nonmevalonate pathway supports both monoterpene and sesquiterpene formation in snapdragon flowers

Terpenoids, the largest class of plant secondary metabolites, play essential roles in both plant and human life. In higher plants, the five-carbon building blocks of all terpenoids, isopentenyl diphosphate (IPP) and dimethylallyl diphosphate, are derived from two independent pathways localized in different cellular compartments. The methylerythritol phosphate (MEP or nonmevalonate) pathway, localized in the plastids, is thought to provide IPP and dimethylallyl diphosphate for hemiterpene, monoterpene, and diterpene biosynthesis, whereas the cytosol-localized mevalonate pathway provides C5 units for sesquiterpene biosynthesis. Stable isotope-labeled, pathway-specific precursors (1-deoxy-[5,5-2H2]-D-xylulose and [2,2-2H2]-mevalolactone) were supplied to cut snapdragon flowers, which emit both monoterpenes and the sesquiterpene, nerolidol. We show that only one of the two pathways, the plastid-localized MEP pathway, is active in the formation of volatile terpenes. The MEP pathway provides IPP precursors for both plastidial monoterpene and cytosolic sesquiterpene biosynthesis in the epidermis of snapdragon petals. The trafficking of IPP occurs unidirectionally from the plastids to cytosol. The MEP pathway operates in a rhythmic manner controlled by the circadian clock, which determines the rhythmicity of terpenoid emission.     

Hepatotoxic slimming aids and other herbal hepatotoxins

Perceptions of safety and/or cultural mores prompt individuals to seek herbal slimming aids in preference to conventional dietary, physical activity and medication-based protocols. In recent years, terpenoid-containing dietary supplements have been implicated in causing severe and sometimes fatal hepatotoxicity. Teucrium polium (germander) was the first of these herbal products to be clearly linked to cases of acute liver failure. Subsequently, similar hepatotoxicity has been observed with other members of the Teucrium genus. While diterpenoid-derived reactive metabolites are central to germander hepatotoxicity, it may also be that the hepatic effects of compounds such as Sho-saiko-to, Centella asiatica and Black cohosh are linked to their triterpenoid content. Other non-terpenoid-containing herbal remedies marketed for weight reduction have been causally associated with significant liver injury. Important among these are preparations containing N-nitrosofenfluramine, usnic acid and ephedra alkaloids. Finally, we review recent data on known and emerging hepatotoxins such as Boh-Gol-Zhee, Kava, pyrrolizidine alkaloids and Shou-Wu-Pian. Better public and physician awareness through health education, early recognition and management of herbal toxicity and tighter regulation of complementary/alternative medicine systems are required to minimize the dangers of herbal product use.     

基于经典人群口尝法和电子舌法的中药饮片水煎液苦度叠加规律研究

目的探索苦味中药饮片水煎液(decoction of Chinese materia medica,DCMM)的苦度叠加规律。方法以生物碱类(黄连Coptidis Rhizoma、黄柏Phellodendron Chinensis Cortex、苦参Sophora Flavescens Radix)、萜类(穿心莲Andrographis Herba、野菊花Chrysanthemi Indici Flos、苦楝皮Melia Cortex)、糖苷类(龙胆Gentianae Radix et Rhizoma、黄芩Scutellariae Radix、连翘Forsythiae Fructus)9种苦味DCMM为研究载体,在单味载体呈味规律研究基础上,采用均匀设计法进行二元(6组)、三元(10组)叠加实验,通过经典人群口尝法(traditional human taste panel method,THTPM)及电子舌法(electrionic tongue,E-tongue)分别评价其苦度,建立二元、三元叠加时叠加苦度-质量浓度对数(IZ-ln C)、叠加苦度-叠加前分苦度(IZ-I)、口尝叠加苦度-电子舌叠加苦度(IZo-IZe)拟合模型,探索其苦度叠加规律。结果 THTPM法中,二元叠加IZ-ln C、IZ-I共12组,均拟合出有意义模型(Rc2≥0.868,P0.05,n=6),模型类型为二次多项式或近似结构的模型(下同);三元叠加IZ-ln C、IZ-I共20组,拟合出18组有意义模型(Rc2≥0.659,P0.05,n=6)。E-tongue法中,针对3类味觉信息进行分析,二元叠加IZ-ln C、IZ-I共36组,均拟合出有意义模型(Rc2≥0.689,P0.05,n=6);三元叠加IZ-ln C、IZ-I共60组,拟合出52组有意义模型(Rc2≥0.662,P0.05,n=6)。IZo-IZe中,二元叠加共18组,拟合出8组有意义线性模型(Rc2≥0.727,P0.05,n=6);三元叠加共30组,拟合出13组有意义的线性或对数模型(Rc2≥0.670,P0.05,n=6)。结论叠加后苦度随浓度增加呈上升趋势;叠加实验良好模型获取率为(二元100%,Rc2=0.936;三元87.5%,Rc2=0.906),而IZo-IZe中有意义的模型获取率较低,即以IZe预测IZo的方法目前尚不成熟;二元、三元叠加中原始苦度越高的饮片对IZ贡献度越大;黄连在同类型和不同类型叠加中苦度贡献度均最大;除黄连+黄柏+黄芩组存在因成分间可能发生沉淀反应等导致叠加后的苦度降低外,未发现更多因各成分交互作用而产生异常的苦度促进或拮抗现象;IZo-IZe相关性随组分增加而降低。     

HMG-CoA Reductase inhibitors: an updated review of patents of novel compounds and formulations (2011-2015)

Introduction: Statins are remarkably safe and efficient medications that are the mainstay of hypercholesterolemia treatment and have proven to be an invaluable tool to lower the risk of acute cardiovascular events. These compounds are inhibitors of 3-hydroxy-methylglutaryl CoA reductase (HMG-R), the rate-limiting enzyme in cholesterol biosynthesis. In spite of their success, they present undesirable side effects and are now loosing patent protection, which provides a great opportunity for the development of new and improved statins.

Areas covered: This review summarizes the new patents for HMG-R inhibitors for the 2011–2015 period. Combinations of existing statins with other drugs are also addressed, as well as novel applications of existing statins.

Expert opinion: Recent efforts for the discovery of HMG-CoA-R inhibitors has resulted in several new molecules. Most of these are based on commercially available statins, including sterol and terpenoid derivatives. A few peptides have also been patented. However, the origin of the side effects caused by previous statins continues to be, to a large extent, unknown. Although the patents published in the past 5 years are promising, and might result in new drugs, there is still no way to know if they will present reduced toxicity. Only future clinical trials will answer this question.