Primula macrocalyx Bunge (Primulaceae) is a perennial herbaceous plant, which has been widely used as an expectorant, diuretic, sedative, spasmolytic, in folk medicine to treat vitamin deficiencies, colds, fever, insomnia, paralysis, scurvy, heart disease, rheumatism, and kidney diseases.1
The organic anion transporters (OATs) play key roles in the distribution and excretion of drugs. Specifically, OAT1 and OAT3, which are highly expressed in the kidney, play important parts in the renal elimination of a range of substrate molecules.2 Apparently, the development of several above diseases is closely related to OATs.
As part of an ongoing program exploring the interaction of dietary phytochemicals with the OATs, a bioactivity guided fractionation was performed on the methanol extract of P. macrocalyx collected in Armenia, followed by structure determination of the isolated compounds based on LC-MS and NMR data, leading to the elucidation of twelve flavones, including one previously unreported compound.
To our knowledge, this study is the first to evaluate these compounds as inhibitors of the OATs, and may allow an initial elucidation of the structure activity relationships within this group. These data may also provide a rational basis for the therapeutic applications of P. macrocalyx in traditional medicine.
1. Kosenkova, Y. S.; Polovinka, M. P.; Komarova, N. I.; Korchagina, D. V.; Kurochkina, N. Y.; Cheremushkina, V. A.; Salakhutdinov, N. F., Chemistry of Natural Compounds 2007, 43 (6), 712-713.
2. Hagos, Y.; Wolff, N. A., Toxins 2010, 2, 2055-2082.