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补充微囊化二十二碳六烯酸的志愿者的药代动力学和氧化参数

Pharmacokinetics and Oxidation Parameters in Volunteers Supplemented with Microencapsulated Docosahexaenoic Acid.

作者信息

Petyaev Ivan M, Chalyk Natalya E, Klochkov Victor A, Pristensky Dmitry V, Chernyshova Marina P, Kyle Nigel H, Bashmakov Yuriy K

机构信息

Lycotec Limited, Granta Park Campus, Cambridgeshire, UK.

Department of Clinical Cardiology, Institute of Cardiology, Saratov, Russia.

出版信息

Int J Appl Basic Med Res. 2018 Jul-Sep;8(3):148-154. doi: 10.4103/ijabmr.IJABMR_367_17.

Abstract

CONTEXT

Docosahexaenoic acid (DHA) is an omega-3 fatty acid essential for cardiovascular health, brain development, and reproductive function. Due to hydrophobicity and low DHA bioavailability, new microencapsulated DHA formulations are under development.

AIM

This study aims to evaluate DHA pharmacokinetics (PKs) and biological oxidation parameters in volunteers ingesting a newly developed lutein-containing lycosomal formulation of DHA (LF-DHA).

MATERIALS AND METHODS

A total of 32 healthy volunteers (40-65 years old) with signs of oxidative stress (OS) and subclinical hypoxia were orally supplemented for a month with 250 mg of regular DHA (1 group) or a combination of lutein (7.0 mg) and zeaxanthin (1.4 mg) (2 group). The third group received regular DHA (250 mg) co-ingested with lutein/zeaxanthin (7.0/1.4 mg), whereas the 4 group was given LF-DHA containing lutein/zeaxanthin (7.0/1.4 mg). PK, OS, and oxygenation parameters were analyzed.

RESULTS

LF-DHA improved the PKs of DHA enhancing its serum concentrations time dependently by 34.6% and 94.1% after 2 and 4 weeks, respectively. DHA and lutein ingested either alone or simultaneously as two separate formulations reduced the levels of OS markers. However, LF-DHA inhibited the malonicdialdehyde (MDA) and oxidized low-density lipoprotein values were better than other formulations. LF-DHA also enhanced the plasma oxygen and tissue oxygen saturation. This effect was significantly higher than in other groups.

CONCLUSION

LF-DHA eliminates the need in high-dose DHA supplementation protocols and confers a higher DHA bioavailability, thereby improving the parameters of biological oxidation and tissue respiration in affected individuals.

摘要

背景

二十二碳六烯酸(DHA)是一种对心血管健康、大脑发育和生殖功能至关重要的ω-3脂肪酸。由于其疏水性和较低的DHA生物利用度,新型微囊化DHA制剂正在研发中。

目的

本研究旨在评估摄入新开发的含叶黄素的DHA脂质体制剂(LF-DHA)的志愿者体内DHA的药代动力学(PKs)和生物氧化参数。

材料与方法

共有32名年龄在40至65岁之间、有氧化应激(OS)和亚临床缺氧迹象的健康志愿者,口服补充250毫克普通DHA(第1组)或叶黄素(7.0毫克)和玉米黄质(1.4毫克)的组合(第2组),为期一个月。第三组摄入普通DHA(250毫克)并同时摄入叶黄素/玉米黄质(7.0/1.4毫克),而第四组摄入含叶黄素/玉米黄质(7.0/1.4毫克)的LF-DHA。分析PK、OS和氧合参数。

结果

LF-DHA改善了DHA的药代动力学,使血清浓度在2周和4周后分别随时间依赖性提高了34.6%和94.1%。单独或同时作为两种不同制剂摄入的DHA和叶黄素降低了OS标志物的水平。然而,LF-DHA对丙二醛(MDA)的抑制作用以及氧化型低密度脂蛋白值优于其他制剂。LF-DHA还提高了血浆氧和组织氧饱和度。这种效果明显高于其他组。

结论

LF-DHA无需采用高剂量DHA补充方案,具有更高的DHA生物利用度,从而改善了受影响个体的生物氧化和组织呼吸参数。

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1
Omega-3 Fatty Acids and Cardiovascular Disease: Are There Benefits?欧米伽-3脂肪酸与心血管疾病:有益处吗?
Curr Treat Options Cardiovasc Med. 2016 Nov;18(11):69. doi: 10.1007/s11936-016-0487-1.

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