紫花地丁全草化学成分研究

目的研究紫花地丁Viola yedoensis全草的化学成分。方法采用硅胶、ODS、Sephadex LH-20凝胶和半制备型高效液相等柱色谱方法进行分离纯化,通过理化性质结合NMR、MS等谱学数据分析鉴定化合物结构。结果从紫花地丁95%乙醇提取物中分离得到21个化合物,分别鉴定为秦皮乙素-6-O-β-D-呋喃芹糖基-(1→2)-β-D-吡喃葡萄糖苷(1)、吲哚-3-甲酸乙酯(2)、脱氢地芰普内酯(3)、滨蒿内酯(4)、蒲公英苦素(5)、水杨苷(6)、丁香苷(7)、4-羟基-4-[3′-(β-D-葡萄糖基)亚丁基]-3,5,5-三甲基-2-环己烯-1-醇(8)、柑橘苷A(9)、(7S,8R)-二氢去氢二松柏醇-9-O-β-D-吡喃葡萄糖苷(10)、山柰素-3-O-α-L-(4-O-乙酰基)鼠李糖基-7-O-α-L-鼠李糖苷(11)、山柰酚-7-O-α-L-鼠李糖苷(12)、山柰酚-3-O-α-L-鼠李糖苷(13)、山柰酚-3-O-α-L-鼠李糖基-7-O-α-L-鼠李糖苷(14)、山柰酚-3-O-β-D-葡萄糖苷(15)、芹菜素(16)、(+)-异地芰普内酯(17)、尿苷(18)、腺苷(19)、6-羟基-香豆素-7-O-α-L-鼠李糖基-(1→6)-O-β-D-葡萄糖苷(20)、(7S,8R)-二氢去氢二松柏醇-4-O-β-D-吡喃葡萄糖苷(21)。结论化合物1为新化合物,命名为紫丁葡芹苷,2为新天然产物,5~11和18为首次从堇菜属中分离得到,12和21为首次从紫花地丁中分离得到。     

Antifungal activity of steroidal glycosides from Yucca gloriosa L

The antifungal activity of a crude steroidal glycoside extract from Yucca gloriosa flowers, named alexin, was investigated in vitro against a panel of human pathogenic fungi, yeasts as well as dermatophytes and filamentous species. The minimal inhibitory concentration (MIC) was determined by an agar dilution method. Alexin had a broad spectrum of antifungal activity, found to reside entirely in the spirostanoid fraction. The major tigogenyl glycosides, yuccaloeside B and yuccaloeside C, exhibited MICs between 0.39 and 6.25 microg[sol ]mL for all the tested yeast strains except for two (C. lusitaniae and C. kefyr). They were also active against several clinical Candida isolates known to be resistant to the usual antifungal agents. The MICs for the dermatophytes were between 0.78 and 12.5 microg[sol ]mL. The most sensitive filamentous species was A. fumigatus (MIC = 1.56 microg[sol ]mL). For most of the strains, the MICs of both glycosides were similar to those of the reference antifungal agent.     

牛蒡根中黄酮苷类化学成分及其抗氧化活性构效关系的研究

目的研究牛蒡Arctium lappa根中的黄酮苷类化学成分及其抗氧化活性,分析构效关系。方法采用重结晶、硅胶柱色谱、RP18柱色谱、Sephadex LH-20柱色谱和PHPLC等多种分离手段,对黄酮苷类化合物进行分离纯化,通过现代波谱学方法(NMR、ESI-MS)鉴定其结构,并采用DPPH法、ABTS法和FRAP法对分离得到的化合物进行抗氧化活性测试。结果从牛蒡根55%乙醇提取物中分离得到8个黄酮苷类化合物,分别鉴定为柚皮素-7-芸香糖苷(1)、橙皮苷(2)、淫羊藿苷(3)、芒柄花苷(4)、异芒柄花苷(5)、新甘草苷(6)、新异甘草苷(7)、甘草苷(8);经3种不同方法测试,分析了这一类化合物的抗氧化活性构效关系。结论化合物3为首次从该植物中分离得到,其他化合物均为首次从该属植物中分离得到;化合物1和8显示出较强抗氧化活性;黄酮的B环上的3′-OH和4′-OCH3结构具有较高电子离域并且能形成氢键,很大程度提高了其结构的稳定性,增强了其抗氧化活性。     

青钱柳中一个新的酯苷类化合物

对青钱柳[Cyclocarya paliurus(Batalin)Iljinskaja]叶的乙醇提取物正丁醇萃取部位进行化学成分研究。综合应用硅胶、MCI、ODS、Sephadex LH-20柱色谱、半制备高效液相色谱等多种色谱技术进行分离纯化，从中分离得到8个糖苷类化合物。根据理化性质及光谱数据分别鉴定为3-乙基-4-甲基戊酯-O-β-D-呋喃芹糖-（1→6）-β-D-吡喃葡萄糖苷（1）、胡桃苷E(2)、（4S）-α-松油醇-8-O-α-L-呋喃阿拉伯糖-（1→6）-β-D-吡喃葡萄糖苷（3）、（4S）-α-松油醇-8-O-β-D-呋喃芹糖-（1→6）-β-D-吡喃葡萄糖苷（4）、丁子香酚-O-β-D-呋喃芹糖-（1→6）-O-β-D-吡喃葡萄糖苷（5）、山柰酚-3-O-β-D-吡喃葡萄糖醛酸甲酯（6）、山柰酚-3-O-β-D-吡喃葡萄醛酸苷（7）、槲皮素-3-O-β-D-吡喃葡萄醛酸苷（8）。其中化合物1为新化合物，化合物2～6为首次从青钱柳属中分离得到。     

葛根素糖苷生物合成及对乳腺癌细胞增殖抑制的影响

目的 研究约氏不动杆菌G2菌株对葛根素糖苷生物合成的最佳转化条件，以及葛根素糖苷对人乳腺癌细胞株MDA-MB-231的增殖抑制作用。方法 考察生物合成体系中转化温度、pH和蔗糖浓度对转化率的影响；并以四甲基偶氮唑盐微量酶反应比色法（MTT法）观察不同浓度的葛根素及葛根素糖苷对MDA-MB-231细胞生长的影响。结果 葛根素糖苷的最佳转化条件为温度30 ℃，pH 7.38，蔗糖浓度60 g/L，在此条件反应24 h，转化率为85%。MTT法显示，不同浓度的葛根素及其糖苷对MDA-MB-231细胞均有抑制作用，并随浓度升高而抑制作用增强;其中200 μmol/L浓度葛根素及葛根素糖苷作用MDA-MB-231细胞48h后，其抑制率分别为61.91%和59.42%。结论 约氏不动杆菌G2菌株可有效催化葛根素合成葛根素糖苷；葛根素及其糖苷均能明显抑制人乳腺癌细胞株MDA-MB-231的增殖。     

An overview of structure-based activity outcomes of pyran derivatives against Alzheimer’s disease

Pyran is a heterocyclic group containing oxygen that possesses a variety of pharmacological effects. Pyran is also one of the most prevalent structural subunits in natural products, such as xanthones, coumarins, flavonoids, benzopyrans, etc. Additionally demonstrating the neuroprotective properties of pyrans is the fact that this heterocycle has recently attracted the attention of scientists worldwide. Alzheimer's Disease (AD) treatment and diagnosis are two of the most critical research objectives worldwide. Increased amounts of extracellular senile plaques, intracellular neurofibrillary tangles, and a progressive shutdown of cholinergic basal forebrain neuron transmission are often related with cognitive impairment. This review highlights the various pyran scaffolds of natural and synthetic origin that are effective in the treatment of AD. For better understanding synthetic compounds are categorized as different types of pyran derivatives like chromene, flavone, xanthone, xanthene, etc. The discussion encompasses both the structure–activity correlations of these compounds as well as their activity against AD. Because of the intriguing actions that were uncovered by these pyran-based scaffolds, there is no question that they are at the forefront of the search for potential medication candidates that could treat Alzheimer's disease.     

基于HPLC指纹图谱和多成分定量的玄参质量评价研究

目的 建立玄参Scrophularia ningpoensis的HPLC指纹图谱及多成分定量测定方法。方法 采用HPLC法建立浙江、湖北、四川、安徽等9个省份116批玄参指纹图谱，进行相似度评价，结合聚类分析（hierarchical cluster analysis,HCA）、正交偏最小二乘法-判别分析（orthogonal partial least squares-discriminant analysis,OPLS-DA）对玄参进行化学模式识别分析。同时对8个活性成分（桃叶珊瑚苷、哈巴苷、咖啡酸、对香豆酸、阿魏酸、类叶升麻苷、安格洛苷C、哈巴俄苷）进行含量测定，分析其与生境因子的相关性。结果 建立了116批玄参的指纹图谱，相似度为0.746～0.997，共标定34个共有峰。聚类分析将116批玄参分为4类，OPLS-DA分析能有效地将3个传统道地产区玄参与非道地产区玄参进行区分（Q2>0.5）。不同产地玄参中化学成分含量存在差异，与海拔、经纬度存在相关性。结论 建立的玄参HPLC指纹图谱及多成分含量分析方法稳定、可靠，结合化学识别模式可为玄参药材的产地判别及质量评价提供参考...     

Therapeutic and cosmeceutical role of glycosylated natural products in dermatology

Natural products (NPs) remain the primary source of pharmacologically active candidates for drug discovery. Since time immemorial, NPs have attracted considerable attention because of their beneficial skin effects. Moreover, there has been a great interest in using such products for the cosmetics industry in the past few decades, bridging the gap between modern and traditional medicine. Terpenoids, Steroids, and Flavonoids having glycosidic attachment have proven biological effects with a positive impact on human health. NPs derived glycosides are mainly found in fruits, vegetables, and plants, and most of them have a special reverence in traditional and modern medicine for disease prevention and treatment. A literature review was performed using scientific journals, Google scholar, Scifinder, PubMED, and Google patents. These scientific articles, documents, and patents establish the significance of glycosidic NPs in the areas of dermatology. Considering the human inclination to the usage of NPs rather than synthetic or inorganic drugs (especially in the area of skin care), in the present review we have discussed the worth of NP glycosides in beauty care and skin-related therapeutics and the mechanistic pathways involved.     

金银花黄酮苷类化学成分研究

目的 研究金银花（忍冬Lonicerajaponica的干燥花蕾）的黄酮苷类成分。方法 采用溶剂提取法，结合硅胶、ODS、Sephadex LH-20等柱色谱和半制备高效液相法进行分离和纯化，并通过显色及NMR等波谱学方法进行鉴定。结果 从金银花中分离到了9个黄酮苷类化合物，分别鉴定为3,5-二羟基-3′-甲氧基黄酮-7-O-β-D-葡萄糖苷（1）、槲皮素-3-O-葡萄糖苷（2）、3,5,3′-三羟基黄酮-7-O-β-D-葡萄糖苷（3）、棉花苷（4）、烟花苷（5）、水仙苷（6）、芦丁（7）、槲皮素-5-O-葡萄糖苷（8）、木犀草素-7-O-新橙皮糖苷（9）。结论 化合物1和3为新化合物，分别命名为金银花黄酮F和金银花黄酮E；化合物2、4～6、8、9为首次从该属植物中分离得到。化合物1对人肝癌HuH7细胞的生长具有显著的抑制作用，其半数抑制浓度（median inhibitory concentration,IC50）为（43.4±1.1）μmol/L。