Dynamics of the Cellular Metabolism of Leptosperin Found in Manuka Honey
Dynamics of the Cellular Metabolism of Leptosperin Found in Manuka Honey
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DOI：
10.1021/acs.jafc.9b03894
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发表时间：
2019-10-02
影响因子：
6.1
通讯作者：
Ikushiro, Shinichi
中科院分区：
文献类型：
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作者：
Kato, Yoji;Kawai, Masaki;Ikushiro, Shinichi
麦卢卡蜂蜜中含有丰富的龙胆苦苷(丁香酸甲酯β-D-龙胆糖苷)，因其具有抗菌和可能的抗炎活性而被广泛使用。本研究的目的是研究钩端螺旋体代谢的分子机制。将5种植物化学物质(钩端螺旋体、丁香酸甲酯、葡萄糖醛酸偶联物、S磺酸偶联物和丁香酸)分别与肝癌细胞和Caco-2细胞孵育。培养后发现，菌体内的胞外激素浓度降低，而SyR、胞外激素GA和胞外激素-S的浓度升高。通过抑制剂和羧酸酯酶(CES1，2)的分析，我们发现从MSYR到SyR的转换是由CES1介导的。脂多糖刺激的RAW264.7细胞可能通过分泌β-葡萄糖醛酸酶将MSYR-GA恢复为MSYR。所有服用钩端螺旋体、MSYR或麦卢卡蜂蜜的小鼠血浆MSYR(13.84+/-11.51、14.29+/-9.19或6.66+/-2.30 nM)和SyR(1.85+/-0.66、6.01+/-1.20或8.16+/-3.10 nM)水平均高于赋形剂对照组(3.33+/-1.45(MSYR)和1.85+/-0.66(SyR)nM)。我们的研究结果表明，这些化合物独特的代谢途径可能解释了麦卢卡蜂蜜可能的功能。
Leptosperin (methyl syringate beta-D-gentiobioside) is abundantly found in manuka honey, which is widely used because of its antibacterial and possible anti-inflammatory activities. The aim of this study was to examine the molecular mechanism underlying the metabolism of leptosperin. Five phytochemicals (leptosperin, methyl syringate (MSYR), glucuronate conjugate of MSYR (MSYR-GA), sulfonate conjugate of MSYR (MSYR-S), and syringic acid (SYR)) were separately incubated with HepG2 and Caco-2 cells. After incubation, we found that the concentration of MSYR decreased, whereas the concentrations of SYR, MSYR-GA, and MSYR-S increased. By profiling with inhibitors and carboxylesterases (CES1, 2), we found that the conversion from MSYR to SYR was mediated by CES1. Lipopolysaccharide-stimulated RAW264.7 cells restored MSYR-GA to MSYR possibly by the secreted beta-glucuronidase. All of the mice administered with leptosperin, MSYR, or manuka honey showed higher MSYR (13.84 +/- 11.51, 14.29 +/- 9.19, or 6.66 +/- 2.30 nM) and SYR (1.85 +/- 0.66, 6.01 +/- 1.20, or 8.16 +/- 3.10 nM) levels in the plasma compared with that of the vehicle controls (3.33 +/- 1.45 (MSYR) and 1.85 +/- 0.66 (SYR) nM). The findings of our study indicate that the unique metabolic pathways of these compounds may account for possible functionalities of manuka honey.