Publication: A novel curcumin-mycophenolic acid conjugate inhibited hyperproliferation of tumor necrosis factor-alpha-induced human keratinocyte cells
Issued Date
2021-07-01
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ISSN
19994923
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2-s2.0-85109143672
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Mahidol University
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SCOPUS
Bibliographic Citation
Pharmaceutics. Vol.13, No.7 (2021)
Suggested Citation
Yonelian Yuyun, Pahweenvaj Ratnatilaka Na Bhuket, Wiwat Supasena, Piyapan Suwattananuruk, Kemika Praengam, Opa Vajragupta, Chawanphat Muangnoi, Pornchai Rojsitthisak A novel curcumin-mycophenolic acid conjugate inhibited hyperproliferation of tumor necrosis factor-alpha-induced human keratinocyte cells. Pharmaceutics. Vol.13, No.7 (2021). doi:10.3390/pharmaceutics13070956 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/78953
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Title
A novel curcumin-mycophenolic acid conjugate inhibited hyperproliferation of tumor necrosis factor-alpha-induced human keratinocyte cells
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Abstract
Curcumin (CUR) has been used as adjuvant therapy for therapeutic application in the treatment of psoriasis through several mechanisms of action. Due to the poor oral bioavailability of CUR, several approaches have been developed to overcome the limitations of CUR, including the prodrug strategy. In this study, CUR was esterified with mycophenolic acid (MPA) as a novel conjugate prodrug. The MPA-CUR conjugate was structurally elucidated using FT-IR,1H-NMR,13C-NMR, and MS techniques. Bioavailable fractions (BFs) across Caco-2 cells of CUR, MPA, and MPA-CUR were collected for further biological activity evaluation representing an in vitro cellu-lar transport model for oral administration. The antipsoriatic effect of the BFs was determined using antiproliferation and anti-inflammation assays against hyperproliferation of tumor necrosis factor-alpha (TNF-α)-induced human keratinocytes (HaCaT). The BF of MPA-CUR provided better antiproliferation than that of CUR (p < 0.001). The enhanced hyperproliferation suppression of the BF of MPA-CUR resulted from the reduction of several inflammatory cytokines, including IL-6, IL-8, and IL-1β. The molecular mechanisms of anti-inflammatory activity were mediated by an attenuated signaling cascade of MAPKs protein, i.e., p38, ERK, and JNK. Our results present evidence for the MPA-CUR conjugate as a promising therapeutic agent for treating psoriasis by antiproliferative and anti-inflammatory actions.
