Abstract
Stauntonia hexaphylla leaf extract (YRA-1909), which is widely used for the antirheumatic properties, has been under phase 2 clinical trials in patients with rheumatoid arthritis since April 2017. Liquid chromatography-tandem mass spectrometric method while using liquid–liquid extraction with ethyl acetate was validated for the simultaneous determination of the major active components of YRA-1909, including chlorogenic acid (CGA), neochlorogenic acid (NCGA), cryptochlorogenic acid (CCGA), and their metabolites (i.e., caffeic acid (CA), caffeic acid 3-O-glucuronide (CA-3-G), caffeic acid 4-O-glucuronide (CA-4-G), and ferulic acid (FA)) in rat plasma and applied to a pharmacokinetic study of YRA-1909 in rats. Seven analytes were separated on Halo C18 while using gradient elution of formic acid and methanol, and then quantified in selected reaction monitoring mode whle using negative electrospray ionization. Following oral administration of YRA-1909 at doses of 25, 50, and 100 mg/kg to male Sprague-Dawley rats, CGA, NCGA, and CCGA were rapidly absorbed and metabolized to CA, CA-3-G, and CA-4-G. The area under the plasma concentration-time curve (AUClast) of CGA, NCGA, CCGA, and three metabolites linearly increased as the YRA-1909 dose increased. Other pharmacokinetic parameters were comparable among three doses studied. AUClast values for CA, CA-3-G, and CA-4-G exceeded those for CGA, NCGA, and CCGA.
Highlights
Stauntonia hexaphylla (Lardizabalaceae) is widely distributed throughout Korea, Japan, andChina, and is a popular herbal supplement in Korean and Chinese folk medicine due to its analgesic, sedative, and diuretic properties [1,2]
We developed a sensitive and selective liquid chromatography-mass spectrometry (LC-MS)/MS method for evaluating the pharmacokinetics of the active constituents of YRA-1909 (i.e., chlorogenic acid (CGA), neochlorogenic acid (NCGA), and cryptochlorogenic acid (CCGA)) and their active metabolites (i.e., caffeic acid to (CA), CA-3-G, CA-4-G, and ferulic acid (FA)) after the oral administration of YRA-1909 at doses of 25, 50, and 100 mg/kg to the rats
For the simultaneous quantification of CGA, NCGA, CCGA, CA, CA-3-G, CA-4-G, and FA, MS/MS parameters for all analytes were optimized by the flow-injection method to achieve maximum sensitivity, and Selected reaction monitoring (SRM) transitions of the precursor ion ([M − H]− ) to the intense product ion were used for data acquisition owing to the high selectivity and sensitivity (Figure 2) [24,28,29,30,31]
Summary
Is a popular herbal supplement in Korean and Chinese folk medicine due to its analgesic, sedative, and diuretic properties [1,2]. It exhibits anti-osteoporosis [3], antidiabetic activity [4], and anti-inflammatory effects in carrageenan-induced paw edema rats [5]. Stauntonia hexaphylla leaf extract, YRA-1909, is associated with the antirheumatic activity [6] and has been. Stauntonia hexaphylla of leaf extract, YRA-1909, is associated with the antirheumatic activity [6] and has been undergoing in phase 2 clinical trials in the Republic ofthe.
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