Poor permeability and absorption affect the activity of four alkaloids from Coptis

Molecular Medicine Reports
Han-Ming CuiXiao-Lin Tong

Abstract

Coptidis rhizoma (Coptis) and its alkaloids exert various pharmacological functions in cells and tissues; however, the oral absorption of these alkaloids requires further elucidation. The present study aimed to examine the mechanism underlying the poor absorption of alkaloids, including berberine (BER), coptisine (COP), palmatine (PAL) and jatrorrhizine (JAT). An ultra‑performance liquid chromatography (UPLC) method was validated for the determination of BER, COP, PAL and JAT in the above experimental medium. In addition, the apparent oil‑water partition coefficient (Po/w); apparent permeability coefficient (Papp), determined using a parallel artificial membrane permeability assay (PAMPA) plate; membrane retention coefficient (R %); and effect of P‑glycoprotein (P‑gp) inhibitor on the Papp of the four alkaloids were investigated. The intestinal absorption rate constant (Ka) and absorption percentage (A %) of the four alkaloids were also determined. The results of the present study demonstrated that the Po/w of the four alkaloids in 0.1 mol·l‑1 HCl medium was significantly higher (P<0.01), compared with those of the alkaloids in phosphate buffer (pH 7.4). The Papp of BER was 1.0‑1.2x10‑6 cm·s‑1, determined using a PAMPA plate, a...Continue Reading

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Citations

Sep 10, 2019·Phytotherapy Research : PTR·Dominik Tarabasz, Wirginia Kukula-Koch
Mar 16, 2017·Drug Metabolism Reviews·Kun WangFeng Qiu
Jun 8, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Chi-Yu HeJian-Dong Jiang
Apr 5, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Solomon Habtemariam

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