栀子金花丸化学成分的UPLC-Q-TOF-MS/MS快速鉴定与分析

目的:采用超高效液相色谱串联四极杆飞行时间高分辨率质谱技术(UPLC-Q-TOF-MS/MS)对栀子金花丸整方的化学成分进行定性分析。方法:采用Waters ACQUITY BEH C_(18)超高效液相色谱柱(2.1 mm×100 mm,1.7μm),流动相0.1%甲酸乙腈溶液-0.1%甲酸水溶液梯度洗脱,流速0.4 m L·min~(-1),以正、负离子模式扫描的一级和二级质谱信息,结合文献报道,对栀子金花丸的主要色谱峰进行归属鉴别。结果:根据质谱裂解规律、保留时间及参考文献等信息,初步推测鉴定出65个化学成分,其中,20个黄酮类成分,9个环烯醚萜类成分,8个有机酸类成分,6个生物碱类成分,6个蒽醌类成分,4个甾体皂苷类成分,3个鞣质类成分,3个二萜色素类成分,3个双苯吡酮类成分,1个单萜类成分,1个二蒽酮类成分和1个柠檬苷素类成分。结论:建立的方法分离度好、灵敏度高,可同时对栀子金花丸不同类型化合物进行快速分析,有助于开展进一步的活性成分和质量控制研究。     

石榴皮鞣质对肾小球硬化大鼠内源性物质代谢的影响及代谢通路分析

目的利用高效液相色谱串联质谱(HPLC-MS)的尿液代谢组学研究方法,考察石榴皮鞣质对肾小球硬化大鼠内源性物质代谢的影响,寻找潜在的生物标志物并分析其代谢途径,为研究石榴皮鞣质对肾小球硬化大鼠的改善作用及其机制提供理论依据。方法将48只SD大鼠随机分为假手术组,模型组,贝那普利组,石榴皮鞣质高、中、低剂量组,采用单侧肾切除结合2次尾iv盐酸多柔比星的方法制备肾小球硬化大鼠模型,ig给药8周,每周收集大鼠24 h尿液,用HPLC-MS对其检测分析;采用主成分分析(PCA)、偏最小二乘法判别分析(PLS-DA)及正交偏最小二乘法判别分析(OPLS-DA)等方法对各组大鼠尿液代谢物进行聚类分析,筛选出潜在的生物标志物并构建相应的代谢通路。结果代谢组学分析发现给药后第8周各组大鼠尿液有明显的聚类现象,通过对重要变量的分析鉴定,筛选出10个潜在的生物标志物;涉及的代谢通路包括色氨酸、丙氨酸、天冬氨酸和谷氨酸等多种氨基酸的代谢通路。结论石榴皮鞣质干预下的肾小球硬化大鼠内源性代谢物聚类性趋近正常水平,为进一步阐明石榴皮鞣质对肾小球硬化大鼠的作用机制提供依据。     

In vitro activity of a partially purified and characterized bark extract of Castanea sativa Mill. (ENC®) against Chlamydia spp

Castanea sativa Mill (ENC®), containing tannins against 33 Chlamydia strains, was compared to SMAP-29 with inhibitory effect against C. trachomatis and C. pneumoniae. The ENC® activity against Chlamydia spp. was evaluated determining the lowest concentration to achieve more than half reduction of intact chlamydial inclusions versus controls. ENC® reduced all Chlamydia strains tested at 1 µg/mL, while SMAP-29 induced reductions of C. trachomatis and C. pneumoniae infectivity at 10 µg/mL. A great reduction of C. trachomatis, C. pneumoniae, and C. abortus infectivity was achieved with a 10 µg/mL ENC® concentration, whereas their infectivity was almost inhibited at 100 µg/mL ENC® concentration.     

玫瑰花鞣质提取物体外抗氧化的活性研究

目的：研究玫瑰花鞣质提取物体外抗氧化活性的能力。方法：采用Fenton体系和邻苯三酚自氧化法评价了玫瑰花鞣质的体外抗氧化能力,采用多元线性回归对鞣质浓度与抗氧化活性相关性进行了分析。结果：玫瑰花鞣质提取物浓度在0.05~4.00μg/mL范围内与对—OH和O2-清除能力呈量效关系,其最大清除率分别为62.85%和72.67%;浓度对抗氧化能力的线性回归方程为Y=-0.517＋1.732X1-0.903X2。结论：玫瑰花鞣质具有较强的抗氧化能力,是1种天然有效的抗氧化剂。     

磨盘草不同部位中鞣质含量测定

目的建立磨盘草不同部位中鞣质含量测定方法。方法以没食子酸为对照品,采用磷钼钨酸-干酪素比色法测定鞣质含量。结果没食子酸浓度在2～10mg/L范围内与吸光度呈良好线性关系,平均加样回收率为99.63%,RSD=1.08%,磨盘草叶、茎、根中鞣质含量分别为0.34%、0.16%、0.27%。结论本方法灵敏,准确性强,精密度高,重复性好,适用于磨盘草中鞣质含量的测定。     

Proanthocyanidins and Flavan-3-ols in the Prevention and Treatment of Periodontitis—Immunomodulatory Effects,Animal and Clinical Studies

This paper continues the systematic review on proanthocyanidins and flavan-3-ols in the prevention and treatment of periodontal disease and covers the immunomodulatory effects, and animal- and clinical studies, while the other part discussed the direct antibacterial properties. Inflammation as a major response of the periodontal tissues attacked by pathogenic microbes can significantly exacerbate the condition. However, the bidirectional activity of phytochemicals that simultaneously inhibit bacterial proliferation and proinflammatory signaling can provide a substantial alleviation of both cause and symptoms. The modulatory effects on various aspects of inflammatory and overall immune response are covered, including confirmed and postulated mechanisms of action, structure activity relationships and molecular targets. Further, the clinical relevance of flavan-3-ols and available outcomes from clinical studies is analyzed and discussed. Among the numerous natural sources of flavan-3-ols and proanthocyanidins the most promising are, similarly to antibacterial properties, constituents of various foods, such as fruits of Vaccinium species, tea leaves, grape seeds, and tannin-rich medicinal herbs. Despite a vast amount of in vitro and cell-based evidence of immunomodulatory there are still only a few animal and clinical studies. Most of the reports, regardless of the used model, indicated the efficiency of these phytochemicals from cranberries and other Vaccinium species and tea extracts (green or black). Other sources such as grape seeds and traditional medicinal plants, were seldom. In conclusion, the potential of flavan-3-ols and their derivatives in prevention and alleviation of periodontal disease is remarkable but clinical evidence is urgently needed for issuing credible dietary recommendation and complementary treatments.     

Prooxidant Activity of Polyphenols,Flavonoids, Anthocyanins and Carotenoids: Updated Review of Mechanisms and Catalyzing Metals

Natural antioxidants, including polyphenols, flavonoids, anthocyanins and carotenoids, play an important role in the treatment and prevention of a large number of diseases. However, studies indicate that natural antioxidants can act as prooxidants, which produce free radicals and cause DNA damage and mutagenesis. The prooxidant activity is typically catalyzed by metals, particularly transition metals such as Fe and Cu, present in biological systems. In this article, we aim to review new in vitro and in vivo evidence of the prooxidant activity of phenolics, flavonoids, anthocyanins and carotenoids. We highlight the role of catalyzing metals, including transition metals, non‐transition metals and metalloids, in the prooxidant activity of natural antioxidants. Prooxidant structure–activity relationships of simple phenolics, flavonoids and anthocyanins and the role of cellular antioxidant defense, including endogenous antioxidant compounds and antioxidant enzymes, are also addressed in this review. In addition, we discuss the question, With respect to in vitro evidence of the prooxidant activity of antioxidants, can we translate this activity into biological systems and the human body? Copyright © 2016 John Wiley & Sons, Ltd.     

基于Hermia模型的中药鞣质模拟体系的膜过程污染机制研究

目的分析中药鞣质模拟体系的膜过程污染机制。方法以中药水提液中的鞣质和小分子药效物质(小檗碱、栀子苷)组成的模拟溶液为研究对象,考察不同模拟溶液的膜过程通量、共性高分子物质去除率、小分子药效物质透过率等指标,借助Hermia数学模型进行分析。结果对于鞣质模拟溶液、鞣质+小檗碱+栀子苷模拟溶液,其膜通量变化和滤饼过滤模型拟合程度较高。滤饼层的形成是其通量降低和膜污染的主要原因。滤饼层的存在使得小檗碱和栀子苷透过率(分别为67.63%和87.55%)并不理想。结论 Hermia数学模型可以作为研究中药提取液膜污染机制的重要手段,滤饼层的形成和存在可能是中药提取液膜污染严重的原因之一。     

肠道菌群对石榴皮鞣质的分解代谢作用研究

目的考察肠道菌群对石榴皮鞣质的分解代谢作用,阐明石榴皮鞣质在肠道的代谢途径。方法将石榴皮鞣质与大鼠肠道菌液共同孵育4、6、8、12、24、48 h后,检测不同时间点溶液中的代谢成分。结果通过LC-MS/MS从石榴皮鞣质肠道菌群孵育液中共鉴别出了10个代谢产物,分别为尿石素B、没食子酸、焦性没食子酸、3-O-甲基没食子酸、尿石素A、甲基化尿石素A、尿石素C、尿石素-M6、葡萄糖醛酸化尿石素A、葡萄糖醛酸化尿石素C。结论石榴皮鞣质在肠道菌群中主要通过代谢酶的水解、还原等作用将其代谢成具有生理活性的小分子化合物,这些化合物有可能是石榴皮鞣质在机体内发挥药理活性的物质基础。     

Seasonal,gender and regional variations in total phenolic,flavonoid, and condensed tannins contents and in antioxidant properties from Pistacia atlantica ssp. leaves

Context: The widespread use of Pistacia atlantica Desf. ssp. (Anacardiaceae) in traditional medicine can be partly attributed to the content of its secondary metabolites, in particular, the phenolic compounds.

Objective: The effects of harvest period, growing region and gender on the phenolic compounds, flavonoids and condensed tannins contents were studied, as well as on the antioxidant activities of P. atlantica leaves in order to provide a scientific basis for optimal collection.

Materials and methods: Leaves were collected monthly from April to October 2010 in two Algerian sites. The powdered leaves were used for preparing the ethyl acetate extract. Contents of total phenolics (TPC), flavonoids (FC) and condensed tannins (CTC) were determined spectrophotometrically. Antioxidant activity was evaluated through radical scavenging activity (RSA) of 2,2-diphenyl-1-picrylhydrazyl (250?μM) and the reducing power capacity (RPC) determination by K₃Fe(CN)₆ (1%).

Results: The TPC was found to vary from 79?±?13 to 259?±?8?mg gallic acid equivalents/g of dry weight (DW) during the study period. The RSA and RPC varied between 262?±?18 and 675?±?21?mg Ascorbic Acid Equivalent (AAE)/g DW, and from 259?±?16 to 983?±?20?mg AAE/g DW, respectively. A seasonal pattern was observed consisting of a decrease in TPC content and RPC from spring to autumn. The FC, CTC and RSA did not show a seasonal pattern.

Discussion and conclusion: Our findings showed that secondary metabolite content and antioxidant activities of P. atlantica leaves were more influenced by harvest time and growing region than by gender.