Flavonoids: Nutraceuticals for Rheumatic Diseases via Targeting of Inflammasome Activation

Inflammation, an innate immune response that prevents cellular damage caused by pathogens, consists of two successive mechanisms, namely priming and triggering. While priming is an inflammation-preparation step, triggering is an inflammation-activation step, and the central feature of triggering is the activation of inflammasomes and intracellular inflammatory protein complexes. Flavonoids are natural phenolic compounds predominantly present in plants, fruits, and vegetables and are known to possess strong anti-inflammatory activities. The anti-inflammatory activity of flavonoids has long been demonstrated, with the main focus on the priming mechanisms, while increasing numbers of recent studies have redirected the research focus on the triggering step, and studies have reported that flavonoids inhibit inflammatory responses and diseases by targeting inflammasome activation. Rheumatic diseases are systemic inflammatory and autoimmune diseases that primarily affect joints and connective tissues, and they are associated with numerous deleterious effects. Here, we discuss the emerging literature on the ameliorative role of flavonoids targeting inflammasome activation in inflammatory rheumatic diseases.     

发芽条件对西兰花芽苗菜总黄酮富集的影响

为富集西兰花芽苗菜总黄酮,研究不同消毒方法(物理消毒、物理化学联合法)对西兰花种子消毒效果的影响以及不同培养条件下总黄酮含量的变化。以西兰花种子为试材,通过单因素试验(浸泡温度、浸泡时间、发芽温度、发芽时间)与正交试验对发芽条件进行优化。结果表明,紫外消毒10 min联合1%食品级奥克泰士D10消毒效果好,发芽率最高;西兰花富集总黄酮的最适发芽条件为:浸泡温度25℃、浸泡时间6 h、发芽温度20℃、发芽时间4 d。在最佳工艺条件下,西兰花芽苗总黄酮含量为11.33 mg/g。     

体外模拟消化过程中核桃花提取物抗氧化活性的变化

为研究体外模拟消化过程中核桃花提取物抗氧化活性的变化，对核桃花提取物依次进行模拟口腔消化、胃消化和小肠消化，分别采用福林酚法和亚硝酸钠-硝酸铝法测定核桃花提取物在不同消化阶段的总酚和总黄酮含量，以DPPH自由基、ABTS自由基清除能力和铁还原能力为指标，考察核桃花提取物抗氧化活性的变化情况。结果表明：在口腔消化、胃消化和小肠消化过程中，核桃花提取物的总酚、总黄酮含量以及抗氧化活性均呈下降趋势。其中总酚含量从消化前的3.30 mg/mL降至消化后的0.62 mg/mL，降低了81.21%；总黄酮含量从2.88 mg/mL降至0.02 mg/mL，降低了99.31%；核桃花提取物清除DPPH自由基的IC50值从211.02 μg/mL上升到424.45 μg/mL，清除ABTS自由基的IC50值从220.63 μg/mL上升至421.82 μg/mL，铁还原能力从106.13 μg/mL下降为40.47 μg/mL。在模拟胃消化和小肠消化阶段，酸碱环境和消化酶的作用破坏了核桃花提取物中的抗氧化成分，使其抗氧化活性发生了显著下降。     

Bioactive compounds from Cudrania tricuspidata: A natural anticancer source

Abstract

The tumor is becoming a critical threat to our lives in these years. Searching for antitumor substances from natural products is a great interest of scientists. Cudrania tricuspidata (C. tricuspidata) is a regional plant containing 158 flavonoids and 99 xanthones, and others ingredients with favorable bioactivity. This review comprehensively analyzes the antitumor compounds from C. tricuspidata against different tumors, and 78 flavonoids plus xanthones are considered as underlying antineoplastic. Importantly, the structure of preylation groups is the primary source of antitumor activity among 45 flavonoids plus xanthones, which could be a direction of structural modification for a better antitumor ability. Additionally, the fruits are also preferable sources of antitumor compounds compared to the roots and barks due to the abundant isoflavones and sustainability. However, many studies only focused on the cells viability inhibition of the compounds, the underlying molecular mechanisms, and the intracellular targets remain ambiguous. In conclusion, C. tricuspidata has a great potential for anti-tumor prevention or therapy, but more attention should be paid to deeper research in vitro and in vivo models.     

Box-Behnken设计响应面法优化黑果枸杞总黄酮纯化工艺

目的应用Box-Behnken设计响应面法优化黑果枸杞总黄酮纯化工艺条件及相关参数。方法考察6种大孔吸附树脂静态、动态吸附和解吸性能,用单因素试验分别对上样浓度、上样体积、上样pH、洗脱液浓度、洗脱液体积和洗脱流速进行考察,以黑果枸杞总黄酮纯化后含量为指标,再从6个单因素中选出对解吸附试验影响最显著的3个因素进行三因素三水平Box-Behnken设计响应面实验。结果 NKA-9型大孔树脂为纯化黑果枸杞总黄酮的最佳树脂,最佳纯化工艺条件为总黄酮提取液浓度为4mg/mL,pH为4.0,按5BV进行上样,再用3VB的80%乙醇在2mL/min流速下进行洗脱,黑果枸杞总黄酮含量可以从4.54%提高到43.19%。结论此工艺对黑果枸杞总黄酮的纯化效果较好,工艺简单且稳定性良好,适用于工业化生产。     

煮制加工对不同绿豆中黄酮含量的影响及抗氧化活性研究

在绿豆加工过程中,煮制对黄酮类物质相对含量影响较大,所以本实验分别考察了乙醇浓度、煮制温度、煮制时间和pH对绿丰2号和5号两种绿豆煮制液中黄酮含量的影响,在单因素试验基础上通过正交试验对影响黄酮含量的因素进行了优化研究,并对提取出的两种黄酮进行抗氧化活性测定。结果表明:乙醇浓度和pH对煮制液黄酮含量影响显著。最佳的煮制工艺参数为:pH为7.5,煮制温度80℃,煮制时间1.6 h,乙醇浓度为70%。在此提取参数下,绿丰2号绿豆的黄酮类化合物提取量为1.82 mg/g,绿丰5号绿豆的黄酮类化合物提取量为1.77 mg/g;而两种绿豆黄酮类化合物对DPPH自由基、羟基自由基、超氧阴离子自由基均有清除能力,同时,该研究也将为下一步绿豆饮料的开发中黄酮类物质的抗氧化活性提供数据依据。     

板栗壳黄酮结构分析及其对胰脂肪酶活力的抑制作用

在分析板栗壳黄酮结构的基础上，研究其对胰脂肪酶的抑制作用及类型。采用醇提法提取板栗壳中的黄酮，并用AB-8大孔吸附树脂进行纯化，冻干后得到的黄酮含量为（107.50±1.00）mg/g，提取得率为（5.66±0.05）%。利用超高效液相色谱-四极杆/静电场轨道阱质谱联用技术对板栗壳黄酮进行结构分析，鉴定出8 种黄酮类化合物。采用对硝基苯酚法测定胰脂肪酶活力，分别考察板栗壳黄酮对胰脂肪酶的抑制效果及不同反应条件下板栗壳黄酮对胰脂肪酶活性的影响，结果表明，板栗壳黄酮对胰脂肪酶有较好的抑制作用，半抑制浓度（half maximal inhibitory concentration，IC50）为0.074 mg/mL，且使胰脂肪酶最适pH值向碱性偏移。通过Lineweaver-Burk双倒数作图法确定其抑制类型为非竞争性抑制，抑制常数Ki＝53.19 mg/mL。由此可见，板栗壳黄酮是一种效果良好的胰脂肪酶抑制剂。