Citric Acid Enhances the Activities of Astilbin on Psoriasis via Down-Regulation of P-Glycoprotein

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Abstract
Astilbin (AS) has been confirmed to be an attractive candidate drug for psoriasis; however, the low oral absorption limits its further development and utilization. Herein, a simple method was discovered to solve this problem, which was combined with citric acid (CA). The efficiency was estimated by imiquimod (IMQ)-induced psoriasis-like mice, and the absorption was predicted by the Ussing chamber model, HEK293-P-gp cells were used to validate the target. Compared with the AS group, the combination with CA significantly reduced the PASI score and down-regulated the protein expression of IL-6 and IL-22, which showed that the combination of CA enhanced the anti-psoriasis effect of AS. Moreover, AS concentration in psoriasis-like mice plasma was significantly increased (3.90-fold) in the CA combined group, and the mRNA and protein levels of P-gp in the small intestine of the combined group were decreased by 77.95 and 30.00%, respectively. In addition, when combined with CA, AS absorption significantly increased while the efflux ratio decreased in vitro. Furthermore, CA significantly elevated the uptake of AS by 153.37% and decreased the protein expression of P-gp by 31.70% in HEK293-P-gp cells. These results indicated that CA enhanced the therapeutic efficacy of AS by improving its absorption via down-regulation of P-gp.
Funding Information
  • State Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine (SZ2021ZZ51)
  • Guangdong Provincial Bureau of Traditional Chinese Medicine (20201130)
  • Guangdong Province Hospital of Traditional Chinese Medicine (YN2019MJ06, YN2019QJ11)

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