Ahmed Iftekhar, Leach David N, Wohlmuth Hans, De Voss James J, Blanchfield Joanne T
School of Chemistry and Molecular Biosciences, The University of Queensland, St. Lucia, QLD 4072, Australia.
Integria Healthcare Limited, 2728 Logan Road, Eight Mile Plains, QLD 4113, Australia.
ACS Omega. 2020 Aug 20;5(34):21561-21569. doi: 10.1021/acsomega.0c02180. eCollection 2020 Sep 1.
(the immortal herb) has been an important component of Chinese Traditional Medicine for millennia. Recent clinical studies have revealed that the plant exhibits numerous beneficial biological activities, making it of interest to the pharmaceutical industry. An extract of the herb contains over 200 individual secondary metabolites including flavonol glycosides and dammarane saponins. To focus attention on the compounds most likely to be responsible for the biological activities, this study predicts the potential oral bioavailability of nine dammarane saponins and five flavonol glycosides from using the Caco-2 cell monolayer permeability model. Two flavonoids, and , and four saponins, , , , and , exhibited high permeability across the monolayers. The results indicated that a higher degree of glycosylation-facilitated permeability, suggestive of active transport. This study demonstrates the utility of the Caco-2 permeability assay as a method of identifying possible bioavailable compounds from medicinal herbal extracts.
(这种仙草)数千年来一直是中药的重要组成部分。最近的临床研究表明,这种植物具有多种有益的生物活性,这使其受到制药行业的关注。该草药的提取物含有200多种单一的次生代谢产物,包括黄酮醇苷和达玛烷皂苷。为了关注最有可能对生物活性负责的化合物,本研究使用Caco-2细胞单层通透性模型预测了9种达玛烷皂苷和5种黄酮醇苷的潜在口服生物利用度。两种黄酮类化合物, 和 ,以及四种皂苷, 、 、 和 ,在单层中表现出高通透性。结果表明,较高程度的糖基化促进了通透性,提示存在主动转运。本研究证明了Caco-2通透性测定法作为一种从药草提取物中鉴定可能具有生物利用度的化合物的方法的实用性。