Abstract
Puerarin (PUR) and gastrodin (GAS) are often used in combined way for treating diseases caused by microcirculation disorders. The current study aimed to investigate the absorption and transportation mechanism of PUR and GAS and their interaction via Caco-2 monolayer cell model. In this work, the concentration in Caco-2 cell of PUR and GAS was determined by HPLC method. The bidirectional transport of PUR and GAS and the inhibition of drug efflux including verapamil and cyclosporine on the transport of these two components were studied. The mutual influence between PUR and GAS, especially the effect of the latter on the former of the bidirectional transport were also investigated. The transport of 50 μg·mL−1 PUR in Caco-2 cells has no obvious directionality. While the transport of 100 and 200 μg·mL−1 PUR presents a strong directionality, and this directionality can be inhibited by verapamil and cyclosporine. When PUR and GAS were used in combination, GAS could increase the absorption of PUR while PUR had no obvious influence on GAS. Therefore, the compatibility of PUR and GAS is reasonable, and GAS can promote the transmembrane transport of PUR, the effect of which is similar to that of verapamil.
Highlights
Puerarin (Figure 1A, PUR), chemically known as 8-β-D-glucopyranose-4,7-dihydroxy isoflavone, is an important bioactive isoflavone glycoside, and it was isolated from several leguminous plants of the genus Pueraria, including Pueraria tuberosa (Willd.), Pueraria lobata (Willd.) Ohwi (Gegen in Chinese), and Pueraria thomsonii Benth [1,2,3]
The results showed that (1) GAS can increase the solubility of PUR, (2) anticoagulation and anti-platelet aggregation effects of PUR and GAS can be enhanced when used in combination in a certain range of dosage, and (3) the combined use of GAS can promote the absorption, decrease the elimination rate, and prolong the mean residence time of PUR in rats
Caco-2 cells were maintained under humidity with 5% CO2 at 37 ◦C in Dulbecco’s modified Eagle’s medium (DMEM) supplemented 10% (v/v) heat-inactivated fetal bovine serum (FBS), 1% non-essential amino acids, 1% L-glutamine, and penicillin (100 IU·mL−1)-streptomycin (100 μg·mL−1) double antidotic solution
Summary
Puerarin (Figure 1A, PUR), chemically known as 8-β-D-glucopyranose-4 ,7-dihydroxy isoflavone, is an important bioactive isoflavone glycoside, and it was isolated from several leguminous plants of the genus Pueraria, including Pueraria tuberosa (Willd.), Pueraria lobata (Willd.) Ohwi (Gegen in Chinese), and Pueraria thomsonii Benth [1,2,3]. PUR has the effects of dilating coronary arteries and cerebral blood vessels, improving microcirculation, anti-platelet aggregation, lowering blood pressure, and anti-oxidation [4]. It is mainly used to treat hypertension, coronary heart disease, angina pectoris, myocardial infarction, cerebral ischemia, migraine, sudden deafness and diabetes [5,6,7]. There is widespread interest in how to improve the oral absorption of PUR. Gas has a variety of pharmacological effects such as sedation and sleeping, promoting intelligence, protecting neurons, lowering blood pressure, antioxidant, and improving microcirculation, etc. It is extensively used to treat dizziness, migraine, high blood pressure, stroke and epilepsy [11,12,13,14,15]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
