The Developmental Process of TGP-Pae-CP-25 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). Meanwhile a series of further studies has demonstrated that TG... See full list on Arthritis The anti-inflammatory and immunoregulatory effects of Pae on mesenteric lymph node (MLN) lymphocytes and the underlying mechanisms were investigated in an adjuvant arthritis (AA) rat model. Pae greatly reduced arthritis scores and secondary hind paw swelling, pro-inflammatory cytokine production and the proliferation of MLN lymphocytes. Pae induced the expression of β2-adrenergic receptor (ADRB2) and decreased that of β-arrestin1/2 in MLN lymphocytes. In addition, Pae reversed the pro-inflamm... Liver Diseases Pae treatment showed protective effect for several liver diseases. Ma et al. (2016) demonstrated that the Pae repressed serum alanine transferase (ALT), aspartate transferase (AST) and total levels of cholesterol (TC), low-density lipoprotein (LDL), and TNF-α, from a non-alcoholic steatohepatitis (NASH) rat model via inhibiting Rho kinase (ROCK) and NF-κB pathway. Zhao et al. (Zhao et al., 2017) evaluated the effect of Pae on α-naphthylisothiocyanate (ANIT)-induced cholestasis rat model. Pae... Kidney Diseases High glucose activated macrophages mainly through TLR2-dependent pathway which aggravated the severity of renal inflammation and eventually contributed to diabetic nephropathy (DN). Pae might be used as a potential therapeutic agent against progressive DN (Shao et al., 2016). In vivo, Pae reduced the urinary albumin excretion rate and inhibit macrophage infiltration and activation through inhibition of the TLR2/4 pathway. In vitro, Pae reduced the advanced glycation end products (AGEs)-induce... See full list on Recombit human interleukin-1b (rhIL-1β) was used to treat primary monocytes to imitate inflammatory condition in vitro. Pae showed low cytotoxi on rhIL-1β-treated monocytes. Pae significantly suppressed phagocytic function of rhIL-1β-induced monocytes, and decreased the levels of TNF-α and PGE2 production. Administration of Pae significantly inhibited the HLA-DR and CD80 with rhIL-1β-stimulated monocytes. These results indicated that Pae could inhibit activation and normal function of monocytes in human peripheral blood (Wang D. et al., 2012). Another similar study focused on the effect of Pae on rhIL-1β-stimulated human peripheral blood mononuclear cells (PBMCs). Pae inhibited the proliferation of rhIL-1β-treated PBMCs and production of IL-17 and IL-10. rhIL-1β-induced down-regulation of PBMCs CD4+CD25+Foxp3+ subpopulation numbers was also repressed by Pae. Therefore, Pae exerts its anti-inflammatory effects via regulating IL-17/IL-10 secretion (Dai et al., 2015). Topical ap... See full list on Arthritis By using a T cell and FLS co-culture system, CP-25 repressed the proliferation and production of pro-inflammatory cytokines of FLS via inhibiting BAFF-R in CD4+ T cells, suggesting that CP-25 could interfere in the crosstalk between T cells and FLS in vitro (Jia et al., 2016). The AA model was used to investigate the anti-arthritic activity of CP-25. In general, CP-25 repressed both the clinical and the histopathological scores of arthritis. The levels ouding... Other Chronic Inflammatory Diseases Bone marrow dendritic cells (DCs) were isolated from BALB/c mice and stimulated by PGE2 and TNF-α, respectively, which induced CD40, CD80, CD83, CD86, and MHC-II and suppressed the antigen uptake by DCs. Additionally, the proliferation of T cells was induced using a co-culture system. The expression of surface markers, DC antigen uptake and DC-mediated proliferation of T cells were inhibited by CP-25 treatment. Moreover, CP-25 decreased PGE2-induced EP4 and NF-κB and induced PGE2-suppressed i... Absorption and Excretion As a bioavailable derivative of Pae, CP-25 improves the absorption of Pae. This has been attributed to both the lipid solubility enhancement and its resistance to P-gp-mediated efflux (Yang et al., 2016). With regard to tissue distribution, CP-25 concentration was higher in most tissues when compared to Pae via an oral route with the highest concentration in the liver at 3 h after ouding intestine, synovium, muscle, lung, and brain in both male and female rat... See full list on The mixture of glycosides Pae has been shown to be anti-inflammatory, anti-neoplastic, anti-hyperglycemia, and neuroprotective. To improve oral bioavailability of Pae. Paeoniflorin-6′-O-benzene sulfonate (CP-25) was developed which enhanced eases could be shown in animal experiments. Current basic and preclinical studies imply that these natural compounds with their strong anti-inflammatory properties should be considered in the clinic. As shown in various preclinical studies, Pae and its derivative CP-25 demonstrated positive effects on chronic inflammatory diseases, such as arthritis, and in different models of liver injury and kidney injury. The use in therapy modulated inflammatory mediators such as cytokines (IL-1β, IL-6, TNF-α), chemokines (CCL8), pattern recognition receptors and their relevant transcription factors (STAT, NF-κB). Although the effectiveness of Pae and CP-25 has been demonstrated, aspects such as pharmacokinetics and product s... See full list on This study was supported by the National Natural Science Foundation of China and), Natural Sc for Young Scholars (1708085QH200), and Grants for Scientific Research of BSKY from Medical University ). See full list on The authors declare that the research was conducted in the absence of any commercial or ficial relationships that could be construed as a potential conflict of interest. See full list on
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