Protective Effect of High-bioavailability Curcumin on a Model of Tumor Necrosis Factor-α-induced Inflammatory Injury in Human Umbilical Vein Endothelial Cells
Objective To investigate the in vivo pharmacokinetics and in vitro anti-inflammatory effect of nano-formulatedcur-cumin(PURCUMIN®)versus ordinary curcumin(Curcumin 95％).Methods Sprague-Dawley rats were given PURCUMIN® or Curcumin 95％by gavage at a dose of 200 mg/kg to observe their pharmacokinetic parameters in vivo,and relative bioavail-ability was calculated to evaluate the advantages of PURCUMIN®.Human umbilical vein endothelial cells(HUVECs)were stimulated with tumor necrosis factor-α(TNF-α)to establish a model of inflammation-induced endothelial cell injury.The two curcumin preparations were compared in terms of their protective effect on endothelial cells at different concentrations and dura-tions of action based on the levels of key inflammatory factors and the expression levels of the key proteins in the inhibitor of nuclear factor-κB(IκB)/nuclear factor-kappa B(NF-κB)signaling pathway.Results At the same dose of 200 mg/kg,the ex-posure of PURCUMIN® in rats was significantly increased by 17.5 times compared with that of Curcumin 95％.Curcumin ef-fectively inhibited the inflammation of endothelial cells induced by TNF-α,and PURCUMIN® had a significantly better anti-in-flammatory effect.Under the same duration of intervention,low-concentration PURCUMIN® significantly reduced the levels of prostaglandin E2,interleukin-1β,interleukin-6,and monocyte chemoattractant protein-1(MCP-1)(P＜0.05)and inhibited the mRNA expression of cyclooxygenase-2 and MCP-1(P＜0.05)and the activation of the IκB/NF-κB signaling pathway(P＜0.05),with a comparable pharmacological action to high-concentration Curcumin 95％(10 μmol/L).Under the same con-centration of intervention,PURCUMIN® significantly reduced the levels of the above inflammatory factors and inhibited the ac-tivation of the IκB/NF-κB signaling pathway within 2 hours(P＜0.05),with a comparable pharmacological action to Curcumin 95％intervention for 4 hours.Conclusion PURCUMIN® can exert a good anti-inflammatory effect at a relatively low concen-tration and within a short period of time,which might be associated with its significantly improved bioavailability.
BioavailabilityCurcuminInflammationHuman umbilical vein endothelial cellsNuclear factor-kappa B
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