Abstract

The plant extract “total glucosides of peony” (TGP) constitutes a mixture of glycosides that is isolated from the roots of the well-known traditional Chinese herb Paeonia lactiflora Pall. Paeoniflorin (Pae) is the most abundant component and the main biologically active ingredient of TGP. Pharmacologically, Pae exhibits powerful anti-inflammatory and immune regulatory effects in some animal models of autoimmune diseases including Rheumatoid Arthritis (RA) and Systemic Lupus Erythematosus (SLE). Recently, we modified Pae with an addition of benzene sulfonate to achieve better bioavailability and higher anti-inflammatory immune regulatory effects. This review summarizes the pharmacological activities of Pae and the novel anti-inflammatory and immunomodulatory agent Paeoniflorin-6′-O-benzenesulfonate (CP-25) in various chronic inflammatory and autoimmune disorders. The regulatory effects of Pae and CP-25 make them promising agents for other related diseases, which require extensive investigation in the future.

Highlights

  • The Developmental Process of total glucosides of peony” (TGP)-Pae-CP-25The glycoside mixture TGP is an active plant extract that is isolated from the roots of Paeonia lactiflora Pall, a traditional Chinese medicine (TCM)

  • We summarize the recent progress in the use of Pae in immunoregulatory and anti-inflammatory activities, including the regulation of Rheumatoid Arthritis (RA), kidney/liver injury and other immune-related diseases

  • Pae pretreatment could inhibit the Toll-like receptor (TLR) 4 and nuclear factor-κB (NF-κB) pathway in Concanavalin A (Con A)-induced liver. These results suggested that Pae pretreatment protects mice against Con A-induced liver damage via suppression of several inflammatory factors and infiltration of CD4+, CD8+ and NKT cells in liver, and Pae might exert this therapeutical effect through inhibition of TLR4 and NF-κB pathway (Chen et al, 2014)

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Summary

INTRODUCTION

The glycoside mixture TGP is an active plant extract that is isolated from the roots of Paeonia lactiflora Pall, a traditional Chinese medicine (TCM). In 1998, TGP was approved by the National Medical Products Administration (NMPA) for anti-inflammatory and immunomodulatory therapy in China It has been used in the treatment of Rheumatoid Arthritis (RA) and Systemic Lupus Erythematosus (SLE) (Chen et al, 2013; Wang et al, 2014). Modification of acetylation improves the absorption and lipophilicity of Pae in vitro (Yang et al, 2013) and the bioavailability of benzoylpaeoniflorin sulfonate was increased and tested in a mouse model (Cheng et al, 2010). Based on this principle, we prepared paeoniflorin-6 -O-benzene sulfonate (CP-25). We review the pharmaceutical effects of CP-25 on inflammation and immuneassociated diseases to highlight the use of Pae and its derivative CP-25 as potential agents for subsequent research and clinical application (Figure 1)

THE PHARMACOLOGICAL EFFECT OF PAE IN INFLAMMATORY PATHOLOGIES
Liver Diseases
Kidney Diseases
OTHER INFLAMMATORY RELATED CONDITIONS
Related target of pathway
Other Chronic Inflammatory Diseases
Absorption and Excretion
Related target or pathway
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