Comparative pharmacokinetics study of orientin in rat plasma
by UHPLC‐MS/MS after intravenous administration of single
orientin and Trollius chinensis Bunge extract
College of Pharmacy, China Medical
University, Shenyang, People's Republic of
Fanhao Meng, College of Pharmacy, China
Medical University, Shenyang, People's
Republic of China.
Natural Science Foundation of Liaoning Prov-
ince, Grant/Award Number: 201602880;
National Natural Science Foundation of China,
Grant/Award Numbers: 31600278, 81274182
Orientin showed a broad array of biological activities, and it is the major bioactive compound in
the Trollius chinensis Bunge. The aim of this study was to investigate the comparative pharmaco-
kinetics of orientin after intravenous administration of single orientin and T. chinensis Bunge
extract. Sample preparation involved a simple one‐step deproteinization procedure with acetoni-
trile. Chromatographic separation was achieved on a Waters BEH C
column with a mobile
phase consisting of acetonitrile and water containing 0.1% formic acid in an isocratic elution
way. The detection was accomplished in multiple reaction monitoring mode with positive
electrospray ionization. The pharmacokinetic properties of orientin were compared after intrave-
nous administrations of pure orientin and T. chinensis Bunge extract to rats with approximately
the same dosage of 10mg/kg. The results of the study indicate that the pharmacokinetics of
orientin in rat plasma show significant differences between two groups. This is useful for the
clinical uses of therapeutic dosing of orientin and T. chinensis Bunge.
comparative pharmacokinetics, orientin, rat plasma, Trollius chinensis Bunge, UHPLC‐MS/MS
Trollius chinensis Bunge. belongs to the Ranunculaceae family and is
widely distributed in northern China (L. Q. Li, 1995; Z. L. Li, Li, Hua,
Chen, & Kim, 2009). It is listed in the medical literature in Zhong Hua's
Herbal Classic and has been used in China as both a medicinal and an
edible material, such as prescription medicine and in tea and wine (Edi-
torial Committee of State Administration of Traditional Chinese Medi-
cine, 1998). The flowers of this plant, as a traditional Chinese medicine,
have been employed to treat respiratory infections, tonsillitis, pharyn-
gitis, bronchitis, fever and aphtha (Chinese Pharmacopoeia Commis-
sion, 2015). Modern pharmacological studies have shown that T.
chinensis Bunge. possess various pharmacological activities such as
anti‐inflammatory, antiviral, antibacterial and antioxidative effects (J.
Lu, Qin, Han, Wang, & Li, 2015; Wang, Wu, Liu, & An, 2014; Zhao &
Orientin is one of the main flavone C‐glycosides of the purified
herbal extract from the flower of T. chinensis Bunge (Sun et al., 2013;
H. P. Li, Zhang, & Ma, 2011; J. Y. Liu, Li, et al., 2013; Wang, Geng,
Wu, & An, 2012). Recent pharmacological studies reported that
orientin has a diverse range of bioactivities including antioxidant and
anti‐aging activities (Praveena, Sadasivam, Deepha, & Sivakumar,
2014; An et al., 2012), antimicrobial activity (Huma & Savita, 2012),
anti‐inflammatory (Hayoung, Sae‐Kwang, Taeho, & Jong‐Sup, 2014;
Sae‐Kwang, Soyoung, & Jong‐Sup, 2014; Wonhwa, Sae‐Kwang, &
Jong‐Sup, 2014), cardioprotective (L. Y. Liu, Ma, et al., 2013; N. Lu,
Sun, & Zheng, 2011) and neuroprotective effects (Benjamin, Anna,
Rhun, Soi, & Ying, 2014; Yu et al., 2015). Modern pharmacological
studies have shown that orientin also has antitumor activity (An, Wang,
Tian, & Zhu, 2015; Guo et al., 2014).
Despite the fact that a number of pharmacological studiees have
been performed, there is no report of a comparative pharmacokinetic
study on orientin after the intravenous administration of pure orientin
and T. chinensis Bunge extract to rats by UHPLC‐MS methods.
Therefore, in the present paper, we developed a better sensitive and
selective UHPLC‐MS/MS method to determine orientin in rat plasma.
Meanwhile, we applied the method to the pharmacokinetic study of
orientin when given to rats in two different dosage forms: one the
single orientin, and the other an effective fraction of T. chinensis
Abbreviations: ESI, electrospray ionization; MRM, multiple reaction monitoring;
NBUE, n‐BuOH extract.
Received: 13 August 2017 Revised: 17 October 2017 Accepted: 7 November 2017
Biomedical Chromatography. 2018;32:e4142.
Copyright © 2017 John Wiley & Sons, Ltd.wileyonlinelibrary.com/journal/bmc 1of7