Planta Med 2016; 82(S 01): S1-S381
DOI: 10.1055/s-0036-1596881
Abstracts
Georg Thieme Verlag KG Stuttgart · New York

Preparation of epimagnolin A, a tetrahydrofurofuranoid lignan from Magnolia sp., and evaluation of anti-drug-resistance activity

Y Mitani
1   Department of Applied Biological Chemistry, College of Bioscience and Biotechnology, Chubu University, 1200 Matsumoto-cho, Kasugai 487 – 8501, Japan
,
K Satake
1   Department of Applied Biological Chemistry, College of Bioscience and Biotechnology, Chubu University, 1200 Matsumoto-cho, Kasugai 487 – 8501, Japan
,
M Tsukamoto
1   Department of Applied Biological Chemistry, College of Bioscience and Biotechnology, Chubu University, 1200 Matsumoto-cho, Kasugai 487 – 8501, Japan
,
T Teruya
2   Faculty of Education, University of the Ryukyus, 1 Senbaru, Nishihara-cho, Nakagami-gun, Okinawa 903 – 0129, Japan
,
BY Cha
3   Research Institute for Biological Functions, Chubu University, 1200 Matsumoto-cho, Kasugai, Aichi 487 – 8501, Japan
,
JT Woo
3   Research Institute for Biological Functions, Chubu University, 1200 Matsumoto-cho, Kasugai, Aichi 487 – 8501, Japan
,
H Nakagawa
1   Department of Applied Biological Chemistry, College of Bioscience and Biotechnology, Chubu University, 1200 Matsumoto-cho, Kasugai 487 – 8501, Japan
› Author Affiliations
Further Information

Publication History

Publication Date:
14 December 2016 (online)

Also available at
 

Herbal products have been used to treat or prevent health problems for a long time. Although the biological effects of these products have been reported, their safety still remains to be elucidated. Therefore, studies are required to ensure their safe use. Among the herbal products listed in the Korean, Chinese, and Japanese Pharmacopoeias, Shin-i (Xin-yi/Flos magnoliae), dried flower buds of Magnolia fargesii or M. flos are one of the most commonly used traditional herbs for the treatment of allergic rhinitis, emphysema, headache, nasal congestion, and sinusitis. Tetrahydrofurofuranoid lignans, such as aschantin, dimethoxyaschantin, dimethylliroresinol, dimethylpinoresinol, epimagnolin A, fargesin, and magnolin extracted from Shin-i have effects, such as anti-angiogenic, anti-allergic, anti-diabetic, anti-inflammatory, anti-microbial, and anti-rheumatoid arthritis. Among them, the pharmacokinetics of epimagnolin A and magnolin have been reported, but not their molecular mechanisms. We examined the possibility of interaction between epimagnolin A and human multidrug resistance protein ABCB1, a major transmembrane efflux pump belonging to the ABC transporter superfamily. In the calcein and ATPase assay [1], epimagnolin A inhibited the extrusion of calcein by Flp-In-293/ABCB1 cells and stimulated the ATPase activity of ABCB1, respectively, in a concentration-dependent manner. It showed saturation kinetics between compound-stimulated ATPase activity and compound concentration, suggesting Michaelis-Menten kinetics similar to control drug, verapamil. The Km and Vmax values were calculated from Hanes-Woolf plots; epimagnolin, Km = 42.9 ± 7.53µM and Vmax = 156 ± 15.0µM and verapamil, Km = 12.3 ± 4.79µM and Vmax = 109 ± 3.18µM. In the MTT assay, the sensitivities of the Flp-In-293/ABCB1 cells to anti-cancer drugs were enhanced in the presence of 10µM epimagnolin A. The present study results indicate that epimagnolin A affects the transport activity of ABCB1.

Acknowledgements: This study was supported by Grant-in-Aid for Scientific Research (C) (JSPS KAKENHI Grant Number 24592822) from the Ministry of Education, Culture, and MEXT-Supported Program for the Strategic Research Foundation at Private Universities (S1201007).

Keywords: Epimagnolin A, ABCB1, drug-resistance.

References:

[1] Tajima Y, Nakagawa H, Tamura A, Kadioglu O, Satake K, Mitani Y, Murase H, Regasini LO, Bolzani Vda S, Ishikawa T, Fricker G, Efferth T. Nitensidine A, a guanidine alkaloid from Pterogyne nitens, is a novel substrate for human ABC transporter ABCB1. Phytomedicine 2014; 21: 323 – 332