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毛茛科鸡屎藤中黄烷醇 C-糖苷的生物利用度和吸收:采用模拟消化、Caco-2 细胞和原位单次通过灌流模型。

Bioaccessibility and Absorption of Flavonoid C-glycosides from Abrus mollis Using Simulated Digestion, Caco-2 Cell, and In Situ Single-pass Perfusion Models.

机构信息

State Key Laboratory of Natural Medicines, Department of TCMs Pharmaceuticals, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, People's Republic of China.

出版信息

Planta Med. 2021 Jun;87(7):570-580. doi: 10.1055/a-1363-2088. Epub 2021 Feb 5.

Abstract

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.

摘要

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。

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