Objective To study the pharmacokinetics and distribution of mangiferin in brain tissue of mice after oral administration. Methods ICR mice were orally administered with mangiferin (50 mg/kg), and the concentration (content) in their serum and brain tissue was determined by high-performance liquid chromatography to calculate their pharmacokinetic parameters. The chromatographic conditions are: AQ C18 column (250mm×4.6mm, 5 μm); The mobile phase is acetonitrile 0.1% acetic acid (55∶45, v/v). The flow rate is 1 mL·min-1; The column temperature is 32℃; The detection wavelength is 248 nm. Results The pharmacokinetic data fit best matched the two -chambers model with time delay. The distribution half-life in the serum of male and female mice is 16.10 min, 15.72 min respectively, the elimination half-life is 395.51 min, 384.28 min, the peak concentrations are 893.53 ng/mL, 939.64 ng/mL, and the area under the curve (AUC) is 110 070.91 ng/mL·min, 112 157.66 ng/mL·min, respectively. The variation profile of drug concentration in the brain is similar to that in serum. The average brain/blood concentration ratio (CBrain/CBlood) is calculated based on the AUC ratio of the brain to serum, with a value of 1.13 for males and 1.19 for females, indicating that formononetin has good brain permeability both in male and females and the latter are slightly better than the former. It is almost undetectable in serum and brain tissue 8 hours after dosing. Conclusion Fomononetin can rapidly penetrate the brain after oral administration to mice, but the attenuation is also relatively fast. The brain penetration ability of formononetin is slightly stronger in female mice than in males.
Key words
formononetin /
brain /
high performance liquid chromatography
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References
[1] 白月, 王红芳, 黄怀鹏. 芒柄花素药理作用的研究进展[J]. 现代药物与临床, 2022, 37(2): 425-432.
[2] 丛亚婷, 翁宗琴, 张子昕, 等. 芒柄花素抗肿瘤的研究进展[J/OL]. 中药药理与临床, 1-14[2025-02-21].https://doi.org/10.13412/j.cnki.zyyl.20240912.002.
[3] DUTRA J M, ESPITIA P J P, BATISTA R A . Formononetin: Biological Effects and Uses - A review[J]. Food Chemistry, 2021, 359(5): 129975.
[4] 田亚静, 杨雪, 汪静, 等. 芒柄花素对妊娠期糖尿病大鼠氧化应激损伤的影响[J]. 天津医药, 2023, 51(7): 734-739.
[5] 林海, 易金容, 饶运帷. 芒柄花素对脂多糖诱导的肺泡上皮细胞凋亡及炎症反应的抑制作用[J]. 中国药房, 2023, 34(22): 2721-2726.
[6] 邹小蓉, 徐露. 刺芒柄花素对脑缺血再灌注损伤大鼠的保护作用及其机制研究[J]. 中国现代应用药学, 2018, 35(6): 855-858.
[7] 刘其羽, 邹一峰, 黎阳. 葛根中刺芒柄花素预防和改善阿尔兹海默病的机制[J]. 武汉轻工大学学报, 2024, 43(4): 23-32+48.
[8] 黄渊智, 刘红玲. 芒柄花素通过miR-1229/ZDHHC9分子轴对胶质瘤细胞增殖、活力及凋亡的影响[J]. 世界中医药, 2024, 19(3): 329-335+341.
[9] 张星, 陆兔林, 毛春芹, 等. 不同器具煎煮补阳还五汤的4种成分含量比较[J]. 中国医院药学杂志, 2013, 33(7): 533-536.
[10] 陈惠军, 刁秀敏, 冯黎明. 补阳还五汤加味(水蛭与鸡血藤)联合丹参川芎嗪治疗急性脑梗死的疗效及对凝血因子和血液黏度影响的临床研究[J]. 世界最新医学信息文摘, 2019, 19(26): 174-175.
[11] 李嘉雨. 天然冰片促进芒柄花素透过血脑屏障发挥抗脑缺血作用的研究[D]. 福州: 福建中医药大学, 2022.
[12] LIU Z, ZHENG X, LV J, et al.Pharmacokinetic synergy from the taxane extract of Taxus chinensis improves the bioavailability of paclitaxel[J]. Phytomedicine, 2015, 22(3): 573-578.
[13] ZHANG Y, HUO M, ZHOU J, et al.PKSolver: An add-in program for pharmacokinetic and pharmacodynamic data analysis in Microsoft Excel[J]. Comput Methods Programs Biomed, 2010, 99(3): 306-314.
[14] DI L, KERNS EH, CARTER GT.Strategies to assess blood-brain barrier penetration[J]. Expert Opin Drug Discov, 2008, 3(6): 677-687.
[15] WANG YH, GAO XH, LI X, et al.Design, synthesis and the evaluation of cholinesterase inhibition and blood-brain permeability of daidzein derivatives or analogs[J]. Chem Biol Drug Des, 2023, 102(4): 718-729.
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