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|Title:||Interaction of Compounds Isolated from Boesenbergia rotunda with Human Renal Organic Anion and Cation Transporters|
|Keywords:||Boesenbergia rotunda;drug interaction;organic anion transporters;organic cation transporters;renal basolateral transporter|
|Publisher:||The Physiological Society of Thailand|
|Citation:||Journal of Physiological and Biomedical Sciences. 2017;30(2):52-56.|
|Abstract:||Boesenbergia rotunda extract (BPE) is used as a dietary supplement and therapeutic purposes, such as antioxidant activity, antibacterial, anticancer, and antiobesity. Therefore, co-use of this herb and therapeutic drug possibly causes herb-drug interaction and leads to altering drug efficiency and toxicity. Organic anion transporters (OAT1 and OAT3) and organic cation transporters (OCT2) play an importance role in renal excretion of anionic and cationic drugs. Inhibition of these transporters influences the plasma level of the drugs. Thus, the study was set up to determine the interaction of the extract and pure compounds isolated from B. rotunda with OAT1, OAT3 and OCT2 in human renal proximal tubular cells (RPTEC/TERT1) by measuring the uptake of 3 H-PAH, 3 H-ES and 3 H-MPP + which is a prototypical substrate of OAT1, OAT3 and OCT2, respectively. The results showed that BPE did not inhibit OAT1-mediated 3 H-PAH uptake and OAT3- mediated 3 H-ES uptake. BPE inhibited OCT2-mediated 3 H-MPP + uptake with a half maximal inhibitory concentration (IC 50 ) of 44.17 ± 0.09 μg/ml. The effect of major compounds isolated from B. rotunda, panduratin A, pinocembrin and pinostrobin, on OCT2 function was determined. Pinocembrin and pinostrobin but not panduratin A inhibited OCT2-mediated 3 H-MPP + uptake with an IC 50 of 33.50 ± 0.16 µM. These data suggest that the use of B. rotunda as dietary supplement or for therapeutic purposes may cause herb-drug interaction and subsequently alter renal cationic drug clearance.|
|Appears in Collections:||Physiology: National Journal Publications|
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