College of Food Science and Engineering, Ocean University of China, No. 5 Yushan Road, Qingdao 266003, P. R. China.
Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao 266237 Shandong Province, P. R. China.
J Agric Food Chem. 2022 Jan 19;70(2):480-487. doi: 10.1021/acs.jafc.1c04218. Epub 2021 Dec 22.
Sea cucumber-derived sulfated sterols exhibited more significant bioactivities compared to plant sterols due to the distinctive structure of the sulfate group at the C-3 position; however, their absorption, pharmacokinetics, tissue distribution, and excretion profiles are unknown, which limits the analysis of molecular mechanisms related to their unique activities. In this study, the absorption characteristics of sea cucumber sterols were determined by oral gavage administration, and their pharmacokinetics, excretion, and tissue distribution were studied by tail vein injection. The results showed that SS1 and SS2 reached the peak at 3 h (20.14 ± 1.2 μg/mL) and 4 h (13.32 ± 0.9 μg/mL) in serum, respectively, after oral gavage administration, suggesting the faster absorption rate of SS1 than SS2 due to the difference in the side-chain groups. Besides, lipid-containing food media improved the digestion and absorption rates of sea cucumber sterols. Moreover, SS1 exhibited a relatively longer duration of efficacy than SS2, and they were almost completely excreted within 9 h through urine. Additionally, sea cucumber sterols were found to be mainly accumulated in the liver ( < 0.05), followed by the kidney and spleen. These findings might provide a theoretical basis for the research and development of functional foods and nutraceuticals associated with sea cucumber sterols.
海参来源的硫酸甾醇由于 C-3 位硫酸基团的独特结构，与植物甾醇相比表现出更显著的生物活性；然而，其吸收、药代动力学、组织分布和排泄特征尚不清楚，这限制了对与其独特活性相关的分子机制的分析。在本研究中，通过灌胃给药确定了海参甾醇的吸收特征，并通过尾静脉注射研究了其药代动力学、排泄和组织分布。结果表明，SS1 和 SS2 在口服给药后分别在 3 小时（20.14 ± 1.2 μg/mL）和 4 小时（13.32 ± 0.9 μg/mL）达到血清峰值，表明 SS1 的吸收速度快于 SS2，这是由于侧链基团的差异。此外，含脂食物介质提高了海参甾醇的消化吸收速度。此外，SS1 表现出相对较长的疗效持续时间，并且它们几乎在 9 小时内通过尿液完全排泄。此外，海参甾醇主要积聚在肝脏（<0.05），其次是肾脏和脾脏。这些发现可能为与海参甾醇相关的功能性食品和营养保健品的研究和开发提供理论基础。
