Planta Med 2020; 86(05): 312-318
DOI: 10.1055/a-1106-6785
Biological and Pharmacological Activity
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Pharmacokinetics, Tissue Distribution, and Excretion Study of Cajanonic Acid A in Rats by UPLC-MS/MS

Li Zhang
1   State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang, China
,
Rui Chen
2   Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang, China
,
Yujuan Ban
1   State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang, China
,
Jin Cai
1   State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang, China
,
Jingang Peng
1   State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang, China
,
Jing Huang
1   State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang, China
,
Jianta Wang
1   State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang, China
2   Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang, China
,
Wenzhang Chen
2   Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang, China
,
Xiuli Gao
1   State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang, China
,
Xunrong Zhou
3   The Second Affiliated Hospital of Guizhou Chinese Traditional Medicine University, Guiyang, China
,
Lei Tang
1   State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang, China
2   Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang, China
› Author Affiliations
Supported by: Guizhou innovative talent foundation 2016-4015
Supported by: first-class discipline construction project in Guizhou Province-Public Health and Preventive Medicine 2017[85]
Supported by: the Science Fundation of Guiyang [2017]30-28
Supported by: Foundation of Guizhou Educational Committee KY[2017]072
Supported by: National natural science foundation of China 81660573
Supported by: The Social Development of Technical Supporting Foundation of Guizhou Province [2017]2842
Further Information

Publication History

received 11 September 2019
revised 17 January 2020

accepted 23 January 2020

Publication Date:
11 February 2020 (online)

Abstract

Cajanonic acid A (CAA), a prenylated stilbene derivative extracted from the leaves of pigeon pea (Cajanus cajan), has been reported to possess inhibitory activity on the peroxisome proliferator-activated receptor gamma (PPARγ) and protein tyrosine phosphatase 1B (PTP1B). Its hypoglycemic activity in rats is comparable to that of the approved antidiabetic agent rosiglitazone. Therefore, CAA is a potential candidate for the treatment of type 2 diabetes and a lead compound for the discovery of novel hypoglycemic drugs. To achieve a thorough understanding of the biological behavior of CAA in vivo, our current study was designed to investigate the pharmacokinetics, bioavailability, distribution, and excretion of CAA in rats by UPLC-MS/MS. Chromatographic separation was performed on BEHC18 column (2.1 mm × 50 mm, 1.7 µm). Quantification was performed under the negative ion mode by using single reaction monitoring (SRM) of the transitions of m/z 353.14 → 309.11 for CAA and m/z 269.86 → 224.11 for genistein, respectively. Standard calibration curve showed excellent linearity (r2 > 0.99) within the range of 2 – 800 ng/mL. The accuracies and precisions were within the acceptance limits (all < 20%). CAA was quickly absorbed into bloodstream and distributed rapidly and widely to various tissues. The excretion ratio of CAA in the 3 main pathways via bile, feces, and urine was only 5.17%. These results indicate that CAA was quickly and thoroughly metabolized in vivo and excreted mainly as metabolites.

Supporting Information