Two new phenylpropanoid glycosides from Sanguisorba officinalis

Two new phenylpropanoid glycosides,9-O-[6-O-acetyl-β-D-glucopyranosyl]-4-hydroxycinnamic acid(1) and 8-O-β-D-glucopyranosyl -(R)-(+)-3,4,8-trihydroxy methyl phenylpropionate(2) were isolated from the 80%EtOH extract of the roots of Sanguisorba officinalis.Their structures were characterized by spectroscopic analysis and chemical method,including 1D NMR,2D NMR,and HR-ESI-MS.Compounds 1 and 2 exhibited the moderate antimicrobial activities against all Gram-positive and Gram-negative bacteria tested.     

与Pi—2（t）基因连锁的栽培稻BAC克隆在药用野生稻和栽培稻中的比较物理定位

用栽培稻遗传图第6连锁群中与Pi-2(t)紧密连锁的RFLP标记RG64及其筛选出来的BAC克隆38D17作为探针,对药用野生稻和栽培稻进行荧光原位杂交(FISH),供试探针RG64及BAC克隆38D17均被定位于药用野生稻和栽培稻第6染色体.药用野生稻杂交信号的百分距离分别为44.87士5.33和46.50士4.57,而栽培稻则为35.85士3.06和36.05±2.44,信号检出率相应地为7.14%、42.53%、8.09%和40.78%.BAC克隆和RFLP探针杂交位置几乎一致,由此推知,与抗性基因Pi-2(t)连锁的BAC克隆在药用野生稻中的同源顺序就在第6染色体杂交信号出现的相应位置.在未封阻的情况下,药用野生稻多个染色体上具有信号,这表明它和栽培稻的Cot-IDNA重复序列在一定的程度上具有同源性.文中讨论了栽培稻BAC克隆对药用野生稻原位杂交物理作图的可行性和Cot-IDNA的制备所涉及的一些技术问题.     

Antiviral Activities of Officinaloside C against Herpes Simplex Virus-1

The iridoid compounds in traditional Chinese medicine play a prominent role in their antiviral effects. We previously reported the anti-inflammatory effect of new iridoids from the aerial parts of Morinda officinalis. Nevertheless, several open questions remain to explore the other biological functions of these new iridoid compounds. Herpes simplex virus-1 (HSV-1) is one of the most prevalent pathogens in human beings worldwide and due to limited therapies, mainly with the guanosine analog aciclovir (ACV) and other analogs, the search for new drugs with different modes of action and low toxicity becomes particularly urgent for public health. This study aimed to explore the anti-HSV-1 effects of iridoids from the aerial parts of Morinda officinalis. The dried aerial parts of Morinda officinalis were extracted with 95% ethanol and systematic separation and purification were then carried out by modern column chromatography methods such as silica gel column, RP-ODS column, Sephadex LH-20 gel column, and semi-preparative liquid phase, and the structure of these compounds were identified through the physical and chemical properties and a variety of spectral techniques. The obtained seven new iridoid compounds were screened for antiviral activity on HSV-1 through CCK8 and the cytopathic effect, and then the plaque reduction assay, the anti-fluorescence reporter virus strain replication, and RT-qPCR experiments were carried out to further evaluate the antiviral effect. Seven new iridoid compounds (officinaloside A–G) were identified from the aerial parts of Morinda officinalis, and officinaloside C showed anti-HSV-1 activity. Further functional experiments confirmed that officinaloside C has a significant inhibiting effect on HSV-1 virus plaque formation, viral gene, and protein expression, and fluorescent virus replication. Our findings suggest that officinaloside C has significant inhibitory effects on viral plaque formation, genome replication, and viral protein expression of HSV-1 which implies that officinaloside C exhibits viral activity and may be a promising treatment for HSV-1 infection.     

Rosmarinus officinalis L. Leaf Extracts and Their Metabolites Inhibit the Aryl Hydrocarbon Receptor (AhR) Activation In Vitro and in Human Keratinocytes: Potential Impact on Inflammatory Skin Diseases and Skin Cancer

Aryl hydrocarbon receptor (AhR) activation by environmental agents and microbial metabolites is potentially implicated in a series of skin diseases. Hence, it would be very important to identify natural compounds that could inhibit the AhR activation by ligands of microbial origin as 6-formylindolo[3,2-b]carbazole (FICZ), indirubin (IND) and pityriazepin (PZ) or the prototype ligand 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). Five different dry Rosmarinus officinalis L. extracts (ROEs) were assayed for their activities as antagonists of AhR ligand binding with guinea pig cytosol in the presence of [³H]TCDD. The methanolic ROE was further assayed towards CYP1A1 mRNA induction using RT-PCR in human keratinocytes against TCDD, FICZ, PZ, and IND. The isolated metabolites, carnosic acid, carnosol, 7-O-methyl-epi-rosmanol, 4′,7-O-dimethylapigenin, and betulinic acid, were assayed for their agonist and antagonist activity in the presence and absence of TCDD using the gel retardation assay (GRA). All assayed ROE extracts showed similar dose-dependent activities with almost complete inhibition of AhR activation by TCDD at 100 ppm. The methanol ROE at 10 ppm showed 99%, 50%, 90%, and 85% inhibition against TCDD, FICZ, IND, and PZ, respectively, in human keratinocytes. Most assayed metabolites exhibited dose-dependent antagonist activity. ROEs inhibit AhR activation by TCDD and by the Malassezia metabolites FICZ, PZ, and IND. Hence, ROE could be useful for the prevention or treatment of skin diseases mediated by activation of AhR.     

三维荧光光谱结合二阶校正算法测定人体血浆和厚朴药材中的厚朴酚及和厚朴酚

利用三维荧光光谱与化学计量学二阶校正算法相结合, 直接测定人体血浆中和厚朴药材中的厚朴酚及和厚朴酚. 采用平行因子分析(PARAFAC)算法解析所得两种物质的回收率分别为(99.5±2.6)%和(90.2±1.8)%. 采用交替三线性分解(ATLD)算法解析, 当组分数N取3时, 回收率分别为(104.2±3.2)%和(98.7±4.0)%; 当N取4时, 回收率分别为(102.7±2.9)%和(99.0±4.6)%. 同时用该方法对厚朴药材中的厚朴酚及和厚朴酚进行快速定量测定, 结果令人满意. 实验结果表明, 此法可用于复杂试样中未知干扰共存下厚朴酚及和厚朴酚的同时测定.     

溶剂浮选-紫外分光光度法测定厚朴中总厚朴酚

建立了一种测定厚朴中总厚朴酚的新方法,即采用溶剂浮选法分离富集厚朴中的总厚朴酚,用紫外分光光度法测定其含量。考察了浮选溶剂、试液pH、氮气流速、浮选时间及电解质NaCl等因素对浮选效果的影响,优选出最佳浮选条件。采用所述方法对不同产地厚朴样品中总厚朴酚含量进行测定,样品加标回收率为94.9%-100.8%,RSD为2.8-4.1%。     

紫外光辐射山茱萸水提液制备纳米银及生物活性

利用254 nm紫外光照射山茱萸水提液在室温下制备了纳米银,并通过UV-Vis光谱检测其在410 nm附近的等离子体共振峰;研究了溶液p H值、料液比以及反应时间对还原反应的影响,确定了纳米银的最优合成条件:p H=7. 0,料液比1∶1,反应时间1 h.通过X射线晶体衍射、透射电子显微镜和激光粒度仪对纳米银的晶体结构、粒径、表面性质和形貌等进行表征发现,在最优反应条件下制得的纳米银为面心立方结构,呈近球形,平均粒径(55. 4±0. 9) nm,分散均匀,表面带负电(-10. 2 m V),具有较高的稳定性.生物活性研究结果表明,制得的纳米银具有良好的抗氧化、抗菌及抗癌活性.当纳米银浓度为62. 5μg/m L时,对DPPH自由基的清除率为70. 0%;对S. aureus和E. coli最低抑菌浓度分别为3. 9和7. 8μg/m L;对结直肠癌细胞HCT116和SW620的IC₅₀值分别为23. 1和35. 1μg/m L.     

云南蕊木茎中的抗炎吲哚生物碱

应用多种色谱和波谱学方法,从云南蕊木(Kopsia officinalis)茎中分离鉴定了27个单萜吲哚生物碱,包括7个新化合物kopsiofficines A～G和20个已知化合物.此外,建立脂多糖(LPS)诱导的小鼠巨噬细胞RAW 264.7炎症模型,通过测定IL-1β, PGE2和TNF-α炎症因子释放评价生物碱的抗炎活性.结果表明, kopsiofficines A (1), kopsiofficines B (2),kopsiofficines D(4),kopsiofficines F(6),kopsiofficines G(7), 12-methoxykopsine(11),kopsinoline(15),(-)-N-methoxy-carbonyl-11,12-methylenedioxykopsinaline(16),kopsinine(18)和kopsinic acid(20)表现出显著的抗炎活性,与阳性对照(地塞米松)基本相当.研究发现C-5位丙酮基取代的单萜吲哚生物碱的抗炎活性明显强于原型生物碱,推测丙酮基可能是抗炎活性的药效促进基团,研究结果为进一步的结构修饰...     

薰衣草挥发油化学成分的GC-MS分析

彩和毛细管气质联用法薰衣草挥发油化学成分进行了研究，共确认了其中21种成分，占精油总含量的96．55％，其主要化学成分为芳樟醇（Linalool），乙醇芳樟酯（Linalyl acetate），4－甲基－1－（1－异丙基）－3－环已烯－1－醇（3－Cclohexen-1-o1,4-mthey1-1-1(1-methylethyl)－），乙酸薰衣草酯（Lavandal acetate）等。     

卡宾活性中间体在有机合成中的应用——Ⅱ.马鞭草烯醇类似物的合成

本文以α-蒎烯与二氯卡宾的加成物3为原料,合成了马鞭草烯醇的类似物2,7,7-三甲基三环[4.1.1.0~(2,4)]-5-辛醇及其酯类和醚类衍生物。