Jiangxi Key Laboratory of Natural Product and Functional Food, College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang, China.
J Sci Food Agric. 2021 Jul;101(9):3862-3869. doi: 10.1002/jsfa.11022. Epub 2020 Dec 31.
Dihydromyricetin (DMY) is a natural dihydroflavonol with many bioactive effects. However, the physicochemical properties of DMY related to its bioavailability, especially its stability, are unclear.
The effects of pH, temperature, metal ions and ascorbic acid (AA) on the stability of DMY were studied using high-performance liquid chromatography (HPLC). The bioavailability of DMY in the presence and absence of AA was compared. Dihydromyricetin was unstable in weak alkaline solutions, and the degradation was significantly accelerated in the presence of Cu and Fe . The degradation process followed the first-order kinetic model. The degradation rate constant (k) increased with increasing pH and temperature. The remaining DMY was only 49% of its initial concnentration after 4 h in simulated intestinal fluid (SIF) at 37 °C. However, by supplementing with AA, the degradation of DMY was rarely occured within 6 h. The solubility of DMY at pH 3-5 was about 750 μg mL , slightly increasing to 853 μg mL at pH 6. Pharmacokinetic studies showed that the bioavailability of DMY increased from 0.122% to 0.341% by supplementing with AA (10% of DMY).
The degradation of DMY is one reason for its poor bioavailability. The presence of AA could significantly improve the stability of DMY, and further improve its bioavailability in rats. © 2020 Society of Chemical Industry.
二氢杨梅素(DMY)是一种具有多种生物活性的天然二氢黄酮醇。然而,与其生物利用度相关的 DMY 的物理化学性质,尤其是其稳定性,尚不清楚。
采用高效液相色谱法(HPLC)研究了 pH 值、温度、金属离子和抗坏血酸(AA)对 DMY 稳定性的影响。比较了 DMY 在有/无 AA 存在下的生物利用度。DMY 在弱碱性溶液中不稳定,在 Cu 和 Fe 的存在下,其降解速度明显加快。降解过程遵循一级动力学模型。降解速率常数(k)随 pH 值和温度的升高而增加。在 37°C 模拟肠液(SIF)中,4 小时后,DMY 的剩余量仅为初始浓度的 49%。然而,通过补充 AA,DMY 的降解在 6 小时内很少发生。在 pH 3-5 时,DMY 的溶解度约为 750μg·mL-1,在 pH 6 时略微增加到 853μg·mL-1。药代动力学研究表明,通过补充 AA(DMY 的 10%),DMY 的生物利用度从 0.122%增加到 0.341%。
DMY 的降解是其生物利用度差的一个原因。AA 的存在可以显著提高 DMY 的稳定性,从而进一步提高其在大鼠体内的生物利用度。 © 2020 英国化学学会。