Abstract
Paeoniflorin (PF) is one of the main bioactive components of total glucosides of paeony (TGP) extracted from the root of Paeonia lactiflora Pall. TGP exhibit various biological activities such as improvement in memory, hepatoprotection, antimutagenic properties and platelet aggregation inhibition. The aim of this paper is to review the pharmacokinetics (PK) of PF as a pure compound and in single or multiple herb(s) of traditional Chinese medicine (TCM) prescriptions. The distribution of PF or PF in TCM fitted one or two compartmental model after oral administration or intravenous injection, respectively. However, PF has a low bioavailability (BA) in rabbit (7.24%) and rat (3.24%) after oral administration. The PK profiles and BA of PF were remarkably improved when co-administered with sinomenine or glycyrrhizin acid. The PK profiles and BA of PF in Radix Paeonia Rubra (RP-R) and Jing-zhi guan-xin were improved, but in co-administration of RP-R with Radix Angelicae Sinensis, the BA was significantly reduced. PK profiles and BA of PF in Shan yao gan-cao tang or Danggui-Shaoyao-San was either remarkably improved or not. However, neither the PK profiles nor the BA of PF in Radix paeonia alba, Huangqin-tang Si ni san or Tang-Min-Ling-Wan was improved. Metabolism in the liver did not play any role in the low oral BA of PF. The low BA was thus attributed to poor permeation due to low lipophilicity, P-glycoprotein mediated efflux, intestinal bacteria and hydrolytic degradation in the intestine by the intestinal brush border lactase phlorizin hydrolase (LPH) and certain esterases. These findings show the in vivo course of PF and provide information on the maximum biological actions of PF that may help traditional Chinese herbal medicinal practitioners.
Highlights
Paeonia lactiflora Pall is a Chinese herb commonly known as Baishao or white peony (Figure 1) from the Ranunculaceae family
Radix paeonia rubra (RP-R) and radix paeonia alba (RP-A) are two independent traditional Chinese herbal medicines, both of which are obtained from the root of P. lactiflora Pall. (Figure 1(b)) and have different pharmacological actions
Different methods to determine the cause of its low bioavailability have shown that PF is poorly absorbed due to low lipophilicity, efflux through P-glycoproteins, hydrolytic degradation in the intestine by intestinal brush border lactase phlorizin hydrolase (LPH) and certain esterases, as well as intestinal bacteria and without hepatic metabolism
Summary
Paeonia lactiflora Pall is a Chinese herb commonly known as Baishao or white peony (Figure 1) from the Ranunculaceae family. Paeoniflorin (PF) (Figure 2(a)), the major bioactive monoterpene glucoside from P. lactiflora is characterised as a neutral compound (MW 428.47) with good solubility (log P = 2.88) indicating low lipophilicity Advance in Pre-Clinical Pharmacokinetics of Paeoniflorin, a Major Monoterpene Glucoside from the. One major active ingredient is selected as the indicative compound and the interactions of ingredients in the herb or prescription are clarified based on the pharmacokinetic behaviour of the selected compound. The development of pharmacokinetic study on PF, the major bioactive monoterpene glucoside of P. lactiflora, as a pure compound and in single or multiple herb(s) of TCM Prescriptions was reviewed in this paper
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