Abstract
To investigate the transport mechanism of isorhynchophylline (IRN) by using the specific inhibitors of organic cation transporters (OCTs) and organic anion transporting polypeptides (OATPs) and attempt illustrate the metabolic mechanism of IRN in the liver. All animals were randomly divided into three groups: control group (only inject IRN), RIF group (inject IRN and rifampicin), and ADR group (inject IRN and adrenalone). The control group was injected with IRN via the caudal vein. The RIF group was injected with rifampicin (RIF) by gavage, and after 1 h, IRN was injected into the caudal vein. Similarly, the ADR group received adrenalone by the caudal vein, and after 0.5 h, IRN was injected into the caudal vein. Thereafter, blood samples were obtained by the heart punctures at 90 min, 180 min, and 300 min following drug administration. Rats were sacrificed at 300 min after drug administration; then, the liver tissue was harvested. The level of IRN was measured by using high-performance liquid chromatography (HPLC), and the Kp values were calculated. After RIF administration (OATPs inhibitors), the Kp value of IRN was slightly decreased when compared with that of the control group. Meanwhile, the Kp value of IRN was dramatically reduced compared to that of the control group following ADR administration (OCTs inhibitors). The results suggested that OCTs have mainly participated in the hepatic uptake process of IRN.
Highlights
Traditional Chinese medicine (TCM), as a system of theories and therapeutic strategies, is usually used to prevent, diagnose, treat, and regulate the function of the human body [1]
Accumulating evidence revealed that IRN is a promising herb for disease treatment including asthma, cancer, cirrhosis, diabetes, hypertension, stroke, and rheumatism [9]
Some studies indicated that organic cation transporters (OCTs) are critical for the uptake and transport of drugs [19, 20], and the membrane transport proteins are obviously expressed in certain target tissues like liver, muscle, and adipose tissue [18, 21]
Summary
Traditional Chinese medicine (TCM), as a system of theories and therapeutic strategies, is usually used to prevent, diagnose, treat, and regulate the function of the human body [1]. Throughout the world and importantly in China, TCM is a leading complementary and alternative medicine manner and plays an increasingly indispensable role in the remedy of plentiful diseases in international medical practice [4]. In addition to being used directly as therapeutic agents for the prevention and treatment of disorders or diseases, medicinal plants are used as influential resources for pharmacological research [5]. Consistent with the pharmacological activities, IRN could block the activity of calcium release from intracellular stores, exert protective roles against the ischemia, glutamate, or dopamine-induced damage or death [7], and lowered blood pressure against ischemia-induced neuronal damage [8]. Lee H found that IRN could extensively downregulate the expression level of antiapoptotic, proliferative, metastatic, and angiogenic genes and bring
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
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 call
