Wu Sydney, Wang Shang-Ta, Chen Guan-Yuan, Hsu Chen, Chen Yi-Hsin, Tsai Hsin-Ya, Weng Te-I, Chen Chien-Li, Wu Yi-Fang, Su Nan-Wei
Department of Agricultural Chemistry, National Taiwan University, Taipei 106, Taiwan.
Department of Food Science, National Taiwan Ocean University, Keelung 202, Taiwan.
Antioxidants (Basel). 2024 Dec 13;13(12):1530. doi: 10.3390/antiox13121530.
Luteolin (Lut) and apigenin (Apn), flavones present in various edible plants, exhibit diverse antioxidant and pharmacological activities but have limited in vivo efficacy due to low water solubility and poor bioavailability. Here, we generated luteolin and apigenin monophosphate derivatives (LutPs and ApnPs) individually via microbial biotransformation. We then characterized their physicochemical properties and evaluated their in vitro and in vivo pharmacokinetics and bioavailability. Both LutPs and ApnPs showed enhanced solubility and dissolution and remained stable in simulated gastrointestinal conditions. Additionally, they efficiently reverted to parental forms via alkaline phosphatase in Caco-2 cells. Following oral administration in rats, LutPs and ApnPs exhibited higher plasma exposure to both aglycone and conjugated forms compared to Lut and Apn. Notably, the in vivo biotransformation of Apn to Lut was observed in all apigenin-related groups. Our study suggests that flavone monophosphates are effective alternatives with enhanced bioavailability, providing insights for the potential application of emerging bioactive nutraceuticals.
木犀草素（Lut）和芹菜素（Apn）是存在于多种可食用植物中的黄酮类化合物，具有多种抗氧化和药理活性，但由于水溶性低和生物利用度差，其体内疗效有限。在此，我们通过微生物生物转化分别生成了木犀草素和芹菜素单磷酸酯衍生物（LutPs和ApnPs）。然后，我们对它们的物理化学性质进行了表征，并评估了它们的体外和体内药代动力学及生物利用度。LutPs和ApnPs均表现出增强的溶解度和溶出度，且在模拟胃肠道条件下保持稳定。此外，它们在Caco-2细胞中能通过碱性磷酸酶有效地还原为母体形式。在大鼠口服给药后，与Lut和Apn相比，LutPs和ApnPs对苷元和结合形式均表现出更高的血浆暴露量。值得注意的是，在所有与芹菜素相关的组中均观察到Apn在体内生物转化为Lut。我们的研究表明，黄酮单磷酸酯是具有增强生物利用度的有效替代品，为新兴生物活性营养保健品的潜在应用提供了见解。
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