School of Pharmaceutical Science and Technology , Tianjin University , Tianjin , China.
Beijing Key Laboratory of Analysis and Evaluation on Chinese Medicine , Beijing Institute of Drug Control , Beijing 102206 , China.
J Agric Food Chem. 2018 Mar 21;66(11):2917-2924. doi: 10.1021/acs.jafc.8b00035. Epub 2018 Mar 12.
Formononetin and its glycoside ononin are bioactive isoflavones widely present in legumes. The present study investigated the pharmacokinetics, bioavailability, and in vitro absorption of formononetin and ononin. After an oral administration to rats, formononetin showed a higher systemic exposure over ononin. The oral bioavailability of formononetin and ononin were 21.8% and 7.3%, respectively. Ononin was more bioavailable than perceived, and its bioavailability reached 21.7% when its metabolite formononetin was taken into account. Both formononetin and ononin exhibited better absorption in large intestine segments than that in small intestine segments. Formononetin displayed a better permeability in all intestinal segments over ononin. Transport of formononetin across Caco-2 cell monolayer was mainly through passive diffusion, while ononin was actively pumped out by MRP2 but not P-gp. The results provide evidence for better understanding of the pharmacological actions of formononetin and ononin, which advocates more in vivo evaluations or human trials.
芒柄花素及其糖苷大豆苷元是广泛存在于豆类植物中的生物活性异黄酮。本研究考察了芒柄花素和大豆苷元的药代动力学、生物利用度和体外吸收。在大鼠口服给药后，芒柄花素的全身暴露水平高于大豆苷元。芒柄花素和大豆苷元的口服生物利用度分别为 21.8%和 7.3%。大豆苷元比预期更具生物利用度，当将其代谢产物芒柄花素考虑在内时，其生物利用度达到 21.7%。芒柄花素和大豆苷元在大肠段的吸收均优于小肠段。芒柄花素在所有肠段的通透性均优于大豆苷元。芒柄花素在 Caco-2 细胞单层中的转运主要通过被动扩散，而大豆苷元则被 MRP2 主动泵出，但不受 P-糖蛋白的影响。这些结果为更好地理解芒柄花素和大豆苷元的药理作用提供了证据，这需要更多的体内评价或人体试验。
