基于聚类分析和主成分分析的叶下珠多酚部位HPLC指纹图谱研究

目的：建立基于聚类分析和主成分分析的不同产地叶下珠多酚部位高效液相色谱（HPLC）指纹图谱分析方法。方法：采用HPLC法测定9个不同产地叶下珠多酚部位指纹图谱,对其进行相似度分析、聚类分析和主成分分析,高效液相色谱-质谱（HPLC-MS）指认主要成分。结果：叶下珠多酚部位指纹图谱检出7个共有峰,指认了其中5个共有峰,9个不同产地叶下珠多酚部位相似度达到0.972-0.998,聚类分析和主成分分析从化学成分上说明了9批样品的相似性及差异性。结论：以指纹图谱数据为基础,将聚类分析与主成分分析结合起来进行识别,为叶下珠药材的资源利用提供依据。     

厚朴总酚固体分散体不同制备方法的比较研究

比较研究厚朴总酚固体分散体不同制备方法之间的差异。分别使用热熔挤出法、溶剂蒸发法、熔融冷却法制备厚朴总酚Plastone S-630及HPC 2种辅料固体分散体。采用DSC,X-射线衍射评价所制备固体分散体中药物的分散状态;通过FT-IR分析药物与辅料之间可能存在的连接方式;最后通过加速稳定性-溶出试验比较3种工艺的稳定性差异。DSC及X-射线衍射结果显示3种工艺制备的固体分散体中药物均能以无定形态存在;FT-IR结果也无法区别3种工艺间的差异;加速稳定性-溶出试验表明HPC所制备的固体分散体稳定性明显优于Plastone S-630,同种辅料间热熔挤出技术制备的固体分散体稳定性要好于其他2种工艺。     

基于Nrf2/HO-1通路探讨二十五味鬼臼丸对宫颈炎大鼠的治疗作用及机制

目的 研究藏药二十五味鬼臼丸对苯酚胶浆致宫颈炎模型大鼠的治疗作用及机制。方法 将雌性SD大鼠48只随机分为对照组、模型组及二十五味鬼臼丸低、中、高剂量（0.2、0.4、0.8 g·^kg-1）组和抗宫炎片（0.47 g·^kg-1）组,每组8只。除对照组外,其余5组建立25%苯酚胶浆致宫颈炎大鼠模型,各药物组分别以相应药物ig给药,每日1次,连续给药12 d后取材。观察大鼠外阴炎症程度评分、子宫指数、子宫解剖形态学改变;采用苏木精-伊红（HE）染色观察大鼠子宫组织病理学改变;采用酶联免疫吸附测定（ELISA）法检测子宫组织中超氧化物歧化酶（SOD）、丙二醛（MDA）含量变化;采用实时荧光定量PCR（qRT-PCR）法和蛋白免疫印迹（Western blotting）法检测子宫组织中核因子E2相关因子（Nrf2）、血红素氧合酶-1（HO-1）、NADPH氧化酶4（Nox4）的mRNA和蛋白表达情况。结果 与对照组比较,模型组大鼠外阴炎症评分、子宫指数、子宫组织中MDA水平、Nox4的mRNA和蛋白表达均显著升高（P＜0.01）,体质量、SOD活性、Nrf2、HO-1的mRNA和蛋白表达均显著降低（P＜0.01）,子宫组织出现不同程度的病理变化;与模型组比较,二十五味鬼臼丸能明显降低外阴炎症评分、子宫指数、子宫组织中MDA水平、Nox4的mRNA和蛋白表达（P＜0.05、0.01）,升高体质量及子宫组织中SOD活性和Nrf2、HO-1的mRNA和蛋白表达（P＜0.05、0.01）,减轻子宫颈炎症损伤程度。结论 二十五味鬼臼丸可能通过抑制Nox4的表达,激活Nrf2/HO-1通路,发挥抗氧化作用,减轻炎症反应,从而抑制宫颈炎发展。     

The use of tetrabutylammonium fluoride to promote N‐ and O‐11C‐methylation reactions with iodo[11C]methane in dimethyl sulfoxide

The N‐ or O‐methylation reactions of compounds bearing amide, aniline, or phenol moieties using iodo[¹¹C]methane (1) with the aid of a base are frequently applied to the preparation of ¹¹C‐labeled radiopharmaceuticals. Although sodium hydride and alkaline metal hydroxides are commonly employed as bases in these reactions, their poor solubility properties in organic solvents and hydrolytic activities have sometimes limited their application and made the associated ¹¹C‐methylation reactions difficult. In contrast to these bases, tetrabutylammonium fluoride (TBAF) is moderately basic, highly soluble in organic solvents, and weakly nucleophilic. Although it was envisaged that TBAF could be used as the preferred base for ¹¹C‐methylation reactions using 1, studies concerning the use of TBAF to promote ¹¹C‐methylation reactions are scarce. Herein, we have evaluated the efficiency of the ¹¹C‐methylation reactions of 13 model compounds using TBAF and 1. In most cases, the N‐¹¹C‐methylations were efficiently promoted by TBAF in dimethyl sulfoxide at ambient temperature, whereas the O‐¹¹C‐methylations required heating in some cases. Comparison studies revealed that the efficiencies of the ¹¹C‐methylation reactions with TBAF were comparable or sometimes greater than those conducted with sodium hydride. Based on these results, TBAF should be considered as the preferred base for ¹¹C‐methylation reactions using 1.     

Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists

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Iron(III) reducing and antiradical activities of three Sideritis from Turkey

Context: Sideritis species (Lamiaceae) are widely used as herbal tea and have been used in folk medicine for their anti-inflammatory, anti-rheumatic, digestive, and antimicrobial activities in Turkey. Sideritis dichotoma Huter., Sideritis erythrantha Boiss. var. cedrotorum, and Sideritis vuralii H. Duman et Ba?er are available as commercial products in Turkey.

Objective: The antiradical activities of the various solvent extracts of Sideritis species are investigated here for the first time.

Materials and methods: Plant samples were sequentially extracted with n-hexane, dichloromethane, methanol, and aqueous methanol (50%, v/v) in Soxhlet apparatus. The extracts of Camellia sinensis (L.) Kuntze (Theaceae) were also prepared for use as a positive control. Total phenolics, iron(III) reductive effects, and 1,1-diphenyl-2-picrylhydrazyl (DPPH^?) radical scavenging activities of the all extracts were measured colorimetrically.

Results: The aqueous MeOH and MeOH extracts contained the highest amount of total phenols, whereas the n-hexane extract contained the lowest amounts. The polar extracts of C. sinensis showed higher antiradical activity and also iron(III) reductive effects than the Sideritis species; however, the non-polar extracts of Sideritis species were found to be more active than those from C. sinensis in the iron(III) reductive assay and in the DPPH^? assay as well. But none of the extracts was found to be as active as with positive controls, viz., ascorbic acid, butylated hydroxyanisole (BHA), and Trolox.

Discussion and conclusion: These results can be shown to have antioxidant activities of these Sideritis species and support the ethnopharmacological use of these Sideritis plants.     

Six compounds from marine fungus Y26-02

Two new compounds, together with four known compounds, have been isolated from the ethyl acetate extract of the fermentation broth of the marine fungus Y26-02. Their structures were elucidated, respectively, as 5-(ethynyloxy)-3-hydroxy-3,6-dihydro-2H-pyran-2-one (1), 4-(butoxymethyl)benzene-1,2-diol (2), 4-(methoxymethyl)benzene-1,2-diol (3), 2-acetoxymethylphenol (4), N-(2-phenylethyl)acetamide (5), and 4-hydroxyphenethyl acetate (6) on the basis of their spectroscopic and physico-chemical properties.     

武汉市枯水期某水厂取水口污染状况

[目的]了解挥发酚类、锰、氨氮污染物在取水沟槽中自净进程的变化规律,为受污染水的处理提供科学依据。[方法]不我市某水厂水源水污染连续监测数据,对挥发酚类、锰、氨氮污染物在水厂取水沟槽内浓度变化进行了动态观察,按环境质量指数评价方法进行分析。[结果]挥发酚类指标变化迅速,11天达地表水环境质量标准Ⅱ级,氨氮次之达16天,锰污染指标变化迟缓达19天。3种污染物分指数与污染物衰减天数均呈直线回归,回归系数t检验差异均有极显著性（P＜0．01）。[结论]3种污染物自净进程都非常缓慢。且水位变化对水体中锰污染浓度影响最明显,环境挥发因素对取水沟槽挥发酚类和氨氮污染物的自净有重要影响。     

Influence of harvest season on chemical composition and bioactivity of wild rue plant hydroalcoholic extracts

The rue (Ruta graveolens) copiousness in rural areas of the Campania Region based a thorough chemical and biological investigation aimed at exploring the seasonal variability of phenol constituents in rue leaves and its influence on their antioxidant, cytotoxic and anti-inflammatory capabilities. To this purpose, hydroalcoholic extracts were prepared from plant samples seasonally collected. LC-ESI-MS/MS techniques were employed to analyze qualitatively and quantitatively the seasonal rue phenol content, whereas different chemical antioxidant assays (by DPPH, ABTS, Fe³⁺ RP, ORAC, and FCR methods) and XTT redox metabolic activity assay were performed to screen the seasonal phenol complex-related antioxidant and cytotoxic power. The ability of the rue leaf extracts to counteract cyclooxygenase-2 (COX-2) expression was also evaluated. Data obtained highlighted that the adopted extraction procedure markedly pauperized the furanocoumarin content in all the prepared rue extracts. Flavonol glycosides, along with the flavone acacetin and two sinapic acid derivatives were the main constituents of the spring harvest-derived extract, which exerted the highest antioxidant capability in cell-free systems and was capable to inhibit COX-2 synthesis by 44% comparably to dexamethasone, used as positive control. Data provide new insights for developing a proper management of rue plants for new safe industrial purposes in herbal medicine field.     

Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat

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