Guo Lina, Qiao Shanshan, Hu Junhong, Li Deli, Zheng Shiqi, Shi Duozhi, Liu Junxiu, Wang Rufeng
a School of Life Sciences , Beijing University of Chinese Medicine , Beijing , China.
b Department of Nephrology , Binzhou People's Hospital , Binzhou , China.
Pharm Biol. 2017 Dec;55(1):1747-1758. doi: 10.1080/13880209.2017.1321023.
The flowers of Trollius chinensis Bunge (Ranunculaceae), used for respiratory tract infections, mainly contain flavonoids, phenolic acids, and alkaloids; however, the effective components are debatable because of their unclear in vivo activities.
This study investigates the effective components from the perspectives of biotransformation and absorption.
Both single person derived- and multiple people-derived intestinal florae were used to investigate the biotransformation of aqueous extract of the flowers of T. chinensis (AEOF) at the concentrations of 15.0, 30.0, and 60.0 mg/mL, respectively, for 72 h. Both human colon adenocarcinoma cell line (Caco-2) monolayers and everted gut sacs were employed to evaluate the intestinal absorption of the intestinal bacterial transformed AEOF at the concentrations of 10, 20, and 30 mg/mL, respectively, for 180 min.
2″-O-β-l-Galactopyranosylorientin, orientin, vitexin, quercetin, veratric acid, proglobeflowery acid, and trolline in AEOF were not transformed by intestinal bacteria, while isoquercetin and trollioside were completely transformed. The P values of 2″-O-β-l-galactopyranosylorientin, orientin, and vitexin calculated based on the experimental data of intestinal absorption were at the levels of 10, whereas those of veratric acid, proglobeflowery acid, and trolline were at 10. The mass ratio of flavonoids to phenolic acids to alkaloids changed from 16:10:7 to 9:12:8 before and after absorption.
The dominant position of flavonoids was replaced by phenolic acids after absorption. In addition to flavonoids which are usually considered as the dominant effective ones, phenolic acids and alkaloids should be also very important for the efficacy of these flowers.
金莲花(毛茛科)花用于治疗呼吸道感染,主要含有黄酮类、酚酸类和生物碱类;然而,由于其体内活性不明确,有效成分存在争议。
本研究从生物转化和吸收的角度研究其有效成分。
分别采用单人来源和多人来源的肠道菌群,研究金莲花水提取物(AEOF)在浓度为15.0、30.0和60.0mg/mL时的生物转化,作用72小时。采用人结肠腺癌细胞系(Caco-2)单层和外翻肠囊,分别评价肠道细菌转化后的AEOF在浓度为10、20和30mg/mL时的肠道吸收,作用180分钟。
AEOF中的2″-O-β-L-吡喃半乳糖基荭草素、荭草素、牡荆素、槲皮素、藜芦酸、原球花酸和金莲花碱未被肠道细菌转化,而异槲皮素和金莲花苷被完全转化。根据肠道吸收实验数据计算,2″-O-β-L-吡喃半乳糖基荭草素、荭草素和牡荆素的P值处于10的水平,而藜芦酸、原球花酸和金莲花碱的P值处于10的水平。吸收前后黄酮类、酚酸类和生物碱类的质量比从16:10:7变为9:12:8。
吸收后黄酮类的主导地位被酚酸类取代。除了通常被认为是主要有效成分的黄酮类外,酚酸类和生物碱类对这些花的功效也应该非常重要。