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从褐蜂胶中提取的标准化多酚混合物的生物利用度和体内抗氧化活性。

Bioavailability and In Vivo Antioxidant Activity of a Standardized Polyphenol Mixture Extracted from Brown Propolis.

机构信息

Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section, Pavia University, Viale Taramelli 12, 27100 Pavia, Italy.

Department of Pharmacy, University of Napoli Federico II, Via D. Montesano 49, 80131 Naples, Italy.

出版信息

Int J Mol Sci. 2019 Mar 12;20(5):1250. doi: 10.3390/ijms20051250.

Abstract

Several lines of evidence demonstrate the antioxidant, anti-inflammatory and antimicrobial activities of propolis, mostly ascribed to its polyphenol content. However, little is known regarding the bioavailability of propolis in acute and prolonged settings of oral administration. In this study, we first determined the content of the main polyphenols in a brown propolis extract obtained using a patented extraction method (Multi Dinamic Extraction-M.E.D.) by RP-HPLC-UV-PDA-MSn analysis, followed by the bioavailability of galangin and chrysin, the most abundant polyphenols in the mixture (7.8% and 7.5% respectively), following acute (single bolus of 500 mg/kg containing about 3.65 mg of the polyphenol mixture) and prolonged (100, 250 and 500 mg/kg body for 30 days) oral administration in 30 male 8 weeks old C57BL/6 wild-type mice. In the acute setting, blood was taken at 30 s and 5, 10, 15, 20, 25, 30, 45, 60 and 120 min following the oral bolus. In the prolonged setting, blood samples were obtained after 10, 20 or 30 days of administration. At the end of treatment, expression of antioxidant enzymes (superoxyde dismutase, SOD-1; catalase, CAT; glutathione peroxidase, GSS) was evaluated in liver tissue. Following both acute and prolonged administration, neither galangin nor chrysin were detectable in the plasma of mice, whereas the glucuronide metabolite of galangine was detectable 5 min after acute administration. At the end of the prolonged treatment SOD-1 was found to have increased significantly, unlike CAT and GSS. Overall, these data suggest that oral administration of whole brown propolis extract is followed by rapid absorption and metabolization of galangin followed by adaptations of the antioxidant first line defense system.

摘要

有几条证据表明,蜂胶具有抗氧化、抗炎和抗菌活性,这主要归因于其多酚含量。然而,对于蜂胶在急性和长期口服给药情况下的生物利用度知之甚少。在这项研究中,我们首先通过反相高效液相色谱-紫外-光电二极管-串联质谱分析(RP-HPLC-UV-PDA-MSn)确定了一种使用专利提取方法(多动态提取-MED)获得的棕色蜂胶提取物中主要多酚的含量,然后确定了混合物中含量最丰富的两种多酚(白杨素和白杨素,分别为 7.8%和 7.5%)在急性(单次口服 500mg/kg 剂量,含有约 3.65mg 多酚混合物)和长期(30 天内口服 100、250 和 500mg/kg 体重)条件下的生物利用度。在急性条件下,口服后 30 秒和 5、10、15、20、25、30、45、60 和 120 分钟取血。在长期给药条件下,给药 10、20 或 30 天后取血样。治疗结束时,评估肝脏组织中抗氧化酶(超氧化物歧化酶 1,SOD-1;过氧化氢酶,CAT;谷胱甘肽过氧化物酶,GSS)的表达。在急性和长期给药后,两种多酚均未在小鼠血浆中检测到,而白杨素的葡萄糖醛酸代谢物在急性给药后 5 分钟即可检测到。在长期治疗结束时,SOD-1 发现显著增加,而 CAT 和 GSS 则不然。总的来说,这些数据表明,口服全棕色蜂胶提取物后,白杨素迅速吸收和代谢,然后适应抗氧化第一线防御系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/64fa/6429100/ab875b221487/ijms-20-01250-g001.jpg

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