地黄叶浸膏微波真空低温干燥工艺优化

为充分利用地黄叶资源,提高其经济附加值并为植物提取物干燥提供方法。采用单因素试验考察微波功率、干燥时间等因素对干燥产物含水率的影响,在单因素试验的基础上,选用L9(34)正交试验法和多指标综合评分法对工艺参数进行优化,确定地黄叶浸膏微波真空低温干燥的最佳工艺条件,并与真空烘箱干燥、真空带式干燥和冷冻干燥等方法进行比较研究。结果表明：地黄叶浸膏微波真空低温干燥的最佳工艺条件为浸膏初始含水率45%、微波功率2kW、干燥时间18min、装料盘转速90r/min、间歇比3:1、装载量110g;在此工艺条件下干燥产物含水率2.89%、毛蕊花糖苷保留率95.98%、地黄叶总苷保留率89.41%。与其他干燥方法相比,微波真空干燥具有干燥产品含水率低、有效成分损失少、干燥时间短且操作简便等优点,工艺稳定可靠,有较大的工业化应用价值。     

体外模拟消化对车前子来源毛蕊花苷抑制黄嘌呤氧化酶活性的影响

研究体外模拟消化各阶段的条件对车前子来源毛蕊花苷抑制黄嘌呤氧化酶活性的影响。结果发现毛蕊花苷含量在模拟消化作用4 h后降低,降低程度最高的是肠菌孵育样液,毛蕊花苷含量减少率为(71.26±0.96)%,其次是累加消化样液,达(28.46±0.50)%。模拟消化后各样液的黄嘌呤氧化酶抑制作用均有所增加,增加程度最大的为肠菌孵育样液(P0.05),其次为累加消化样液。经高效液相色谱-质谱联用分析发现,各消化样液中均能检出毛蕊花苷的代谢苷元咖啡酸和羟基酪醇,活性实验表明后两者对黄嘌呤氧化酶的体外抑制活性高于前体毛蕊花苷。毛蕊花苷降解成具有黄嘌呤氧化酶体外抑制活性的产物可能是其在体内表现生理活性的途径之一。     

Natural Compounds for Counteracting Nonalcoholic Fatty Liver Disease (NAFLD): Advantages and Limitations of the Suggested Candidates

The booming prevalence of nonalcoholic fatty liver disease (NAFLD) in adults and children will threaten the health system in the upcoming years. The “multiple hit” hypothesis is the currently accepted explanation of the complex etiology and pathophysiology of the disease. Some of the critical pathological events associated with the development of NAFLD are insulin resistance, steatosis, oxidative stress, inflammation, and fibrosis. Hence, attenuating these events may help prevent or delay the progression of NAFLD. Despite an increasing understanding of the mechanisms involved in NAFLD, no approved standard pharmacological treatment is available. The only currently recommended alternative relies on lifestyle modifications, including diet and physical activity. However, the lack of compliance is still hampering this approach. Thus, there is an evident need to characterize new therapeutic alternatives. Studies of food bioactive compounds became an attractive approach to overcome the reticence toward lifestyle changes. The present study aimed to review some of the reported compounds with beneficial properties in NAFLD; namely, coffee (and its components), tormentic acid, verbascoside, and silymarin. We provide details about their protective effects, their mechanism of action in ameliorating the critical pathological events involved in NAFLD, and their clinical applications.     

Quality attributes and their relations in fresh black ripe ‘Kalamon’ olives (Olea europaea L.) for table use – phenolic compounds and total antioxidant capacity

Quality attributes were investigated in fresh Greek black table ‘Kalamon’ olives prior to processing. Fruit weight, dimensions, respiration and ethylene production rates, firmness, peel colour, moisture, oil content, total antioxidant capacity (TAC), the concentration of total phenolics (TP) and phenolic compounds (hydroxytyrosol, oleuropein, tyrosol, verbascoside, luteolin‐7‐O‐glucoside, luteolin, rutin) were determined in olives from different orchards. There was a significant effect of orchard on most attributes, but not on fruit firmness. Verbascoside, oleuropein and hydroxytyrosol were the major phenolics, and the presence of verbascoside in ‘Kalamon’ olives is revealed for the first time. Positive correlations were found among fruit weight, dimensions, respiration and ethylene. TAC was positively related mainly to TP, hydroxytyrosol, verbascoside and rutin, but inversely to oleuropein. Luteolin was inversely related to luteolin‐7‐O‐glucoside. Colour darkening was directly related to TAC, while colour parameters were positively and moderately affected by oil and moisture.     

毛蕊花苷的稳定性、吸收特性和生物利用度 研究进展

毛蕊花苷作为自然界双子叶植物中具有丰富生理活性且普遍存在的重要苯乙醇苷类物质之一,受到研究者广泛关注。毛蕊花苷具有众多的中文名称和英文名称,为规范研究者的使用,本文首先对其诸多的名称一一进行了分析,建议依据首次从毛蕊花植物中发现将该物质命名为毛蕊花苷(对应英文名verbascoside)最为合理。然后本文阐述了毛蕊花苷的稳定性,其含量在原料处理、存在于中性和碱性环境、加热、模拟消化等过程中均会发生变化,原因可能与其结构中的酯键和糖苷键发生断裂有关,具体变化机理有待深入研究。最后,对不同实验模型下观测到的毛蕊花苷的吸收特性和生物利用度进行了总结,并联系其稳定性探讨其生理活性的可能影响因素,以期为全面深入研究开发毛蕊花苷这一天然活性物质提供一定理论基础。     

Suppression of IL‐8 Release by Sweet Olive Ethanolic Extract and Compounds in WiDr Colon Adenocarcinoma Cells

Oxidative stress can stimulate the secretion of pro‐inflammatory cytokines. Interleukin‐8 (IL‐8) has been implicated in the pathogenesis of inflammatory bowel disease and the metastatic spread of colorectal cancer. The flowers of Osmanthus fragrans (sweet olive) are used to alleviate dysentery with blood in the bowel, as well as stomach ache and diarrhea. However, the evidence of their therapeutic effects on these symptoms remains unclear. In the present study, the protective effects of sweet olive flower ethanolic extract (OFE) against oxidative stress in WiDr cells was assessed by evaluating its 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH) free radical scavenging activity. In addition, cellular IL‐8 secretion was evaluated. Notably, high‐performance liquid chromatography showed verbascoside to be the primary constituent in OFE; it exhibited a DPPH scavenging activity with an IC₅₀ of 8.23 μg/mL. Moreover, OFE (1 to 100 μg/mL) showed a potent, dose‐dependent inhibitory effect on H₂O₂‐induced IL‐8 secretion in WiDr cells. Nine compounds were isolated from OFE based on a protective effect‐guided purification process. Of these compounds, 5 phenolic compounds—verbascoside, phillygenin, tyrosol, methyl 4‐hydroxycinnamate, and eutigoside A—reduced IL‐8 secretion at 10 μg/mL treatment concentrations. Further analysis showed that the anti‐inflammatory effects of OFE likely occurred via nuclear factor‐κB pathway inhibition, which attenuates IL‐8 secretion in cells. Collectively, these data suggest that OFE could be developed as an agent that suppresses IL‐8 secretion to treat chronic inflammatory diseases.     

小包装中药饮片地黄中梓醇和毛蕊花糖苷质量稳定性研究

目的考察小包装中药饮片地黄中梓醇和毛蕊花糖苷的质量稳定性。方法用2015年版《中国药典》梓醇和毛蕊花糖苷的检测方法,先进行影响因素(高温、高湿、强光照射)实验的考察,再采用加速实验和长期实验考察其质量稳定性。结果小包装中药饮片地黄在高温条件下梓醇含量明显降低,真空包装小包装饮片地黄质量稳定性好于常规包装。在25℃、RH 60%条件下储存的小包装中药饮片地黄梓醇和毛蕊花糖苷稳定性超过6个月。结论该研究可为小包装中药饮片地黄的保存条件和有效期提供依据。     

Verbascosides from olive mill waste water: assessment of their bioaccessibility and intestinal uptake using an in vitro digestion/Caco-2 model system

Olive mill wastewater (OMWW) is an agricultural waste material produced in high quantities in the Mediterranean basin. OMWW may be an inexpensive source of health promoting phytochemicals with potential economic value including many low molecular weight compounds such as verbascosides. While promising as antioxidants in vitro, little information is available on the potential absorption of verbascosides by humans. The main objective of the present study was to characterize the verbascoside content and potential for their bioavailability from a partially purified phenolic fraction (IP) of OMWW. The IP was obtained after ultrafiltration step at 5000 Dalton and gel filtration low-pressure chromatography (LH20) of OMWW. RP-HPLC analysis identified several soluble phenolics compounds including verbascoside and isoverbascoside as major components of OMWW fractions. The potential for bioavailability of these polyphenols was estimated by using both in vitro digestion and Caco-2 human intestinal cell models. In vitro digestive recoveries (bioaccessibility) were found to be 35.5%± 0.55% for verbascoside and 9.2% ± 0.94% for isoverbascoside highlighting potential sensitivity of these phenolics to gastric and small intestinal digestive conditions. Accumulation of verbascosides by highly differentiated Caco-2 monolayers was linear between 10 and 100 μM of verbascoside and isoverbascoside from IP extract. Uptake of verbascoside and isoverbascoside was rapid with peak accumulation occurring after 30 min with total accumulation efficiency of 0.1% and 0.2% providing intracellular levels of 130 and 80 pmol/mg cell protein for verbascoside and isoverbascoside, respectively. Combined, these data suggest that verbascosides present in OMWW are bioaccessible and provides a rationale for subsequent in vivo studies on the bioavailability and bioactivity of OMWW components.