State Key Laboratory of Natural Medicines, Department of TCMs Pharmaceuticals, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, People's Republic of China.
Planta Med. 2021 Jun;87(7):570-580. doi: 10.1055/a-1363-2088. Epub 2021 Feb 5.
is commonly used as a traditional Chinese medicine for the treatment of liver diseases due to its hepatoprotection and anti-inflammation, but the absorption properties of its main bioactive ingredients remain unclear. Our previous studies verified that the flavonoid -glycosides, including vicenin-2 (1: ), isoschaftoside (2: ), and schaftoside (3: ), were the major active components in for hepatic protection against nonalcoholic fatty liver disease, hepatitis, and hepatic fibrosis. This study investigated the bioaccessibility and transport mechanisms of total flavonoid -glycoside, as well as vicenin-2 (1: ), isoschaftoside (2: ), and schaftoside (3: ), in by simulated digestion and use of the Caco-2 cell model. Moreover, this study attempted to verify their absorption properties by gastrointestinal perfusion in rats. Total flavonoid -glycoside and 1, 2: , and 3: exhibited similar bioaccessibility of 84.58%, 85.13%, 83.05%, and 81.65% respectively after simulated digestion. The transport of total flavonoid -glycoside in the Caco-2 cell model increased with the concentration, and the transport showed saturation characteristics with the time and concentration of total flavonoid -glycoside to a certain degree. The Papp values of total flavonoid -glycoside and the 3 flavonoid -glycosides were significantly improved by verapamil, probenecid, and EDTA-Na. Their absorption properties in the gastrointestinal tract were consistent with that found in Caco-2 cells, and superior absorption rates were observed in the duodenum and jejunum. The absorption pattern of total flavonoid -glycoside may involve multiple transport pathways, including active transport, passive diffusion, and the paracellular pathway. TFC was actively pumped out by P-glycoprotein and multidrug resistance-associated protein. These results revealed that the bioaccessibility and intestinal absorption characteristic of total flavonoid -glycoside were consistent with the 3 major flavonoids.
作为一种传统的中药,常用于治疗肝脏疾病,因为它具有保肝和抗炎作用,但它的主要生物活性成分的吸收特性仍不清楚。我们之前的研究证实,类黄酮 - 糖苷,包括 vicenin-2(1: )、异 schaftoside(2: )和 schaftoside(3: ),是 的主要活性成分,可保护肝脏免受非酒精性脂肪性肝病、肝炎和肝纤维化的侵害。本研究通过模拟消化和使用 Caco-2 细胞模型,研究了总类黄酮 - 糖苷以及 vicenin-2(1: )、异 schaftoside(2: )和 schaftoside(3: )的生物可利用性和转运机制。此外,本研究还试图通过大鼠胃肠道灌流来验证它们的吸收特性。总类黄酮 - 糖苷和 1、2: 和 3:在模拟消化后分别表现出 84.58%、85.13%、83.05%和 81.65%的相似生物可利用性。在 Caco-2 细胞模型中,总类黄酮 - 糖苷的转运随着浓度的增加而增加,并且转运在一定程度上表现出对总类黄酮 - 糖苷的时间和浓度的饱和特征。总类黄酮 - 糖苷和 3 种类黄酮 - 糖苷的 Papp 值均显著提高了维拉帕米、丙磺舒和 EDTA-Na。它们在胃肠道中的吸收特性与在 Caco-2 细胞中发现的吸收特性一致,并且在十二指肠和空肠中观察到了较高的吸收速率。总类黄酮 - 糖苷的吸收模式可能涉及多种转运途径,包括主动转运、被动扩散和细胞旁途径。TFC 被 P-糖蛋白和多药耐药相关蛋白主动泵出。这些结果表明,总类黄酮 - 糖苷的生物可利用性和肠道吸收特性与 3 种主要类黄酮一致。