<i>Boesenbergia rotunda</i> and Its Pinostrobin for Atopic Dermatitis: Dual 5-Lipoxygenase and Cyclooxygenase-2 Inhibitor and Its Mechanistic Study through Steady-State Kinetics and Molecular Modeling

Human 5-lipoxygenase (5-LOX) and cyclooxygenase-2 (COX-2) are potential targets for suppressing pruritic skin inflammation in atopic dermatitis (AD). In addition, <i>Staphylococcus aureus</i> colonization and oxidative stress worsen AD skin conditions. We aimed to investigate anti-inflam...

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Main Authors: Desy Liana (Author), Chatchakorn Eurtivong (Author), Anuchit Phanumartwiwath (Author)
Format: Book
Published: MDPI AG, 2024-01-01T00:00:00Z.
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Summary:Human 5-lipoxygenase (5-LOX) and cyclooxygenase-2 (COX-2) are potential targets for suppressing pruritic skin inflammation in atopic dermatitis (AD). In addition, <i>Staphylococcus aureus</i> colonization and oxidative stress worsen AD skin conditions. We aimed to investigate anti-inflammatory activity, using 5-LOX and COX-2 inhibitions, and the anti-staphylococcal, and antioxidant potentials of several medicinal plants bio-prospected from traditional medicine related to AD pathogenesis. Essential oils and hexane fractions were prepared and analyzed using gas chromatography-mass spectrometry. <i>Boesenbergia rotunda</i> hexane extract displayed anti-<i>Staphylococcus aureus</i> (MIC = 10 µg/mL) and antioxidant activities (IC<sub>50</sub> = 557.97 and 2651.67 µg/mL against DPPH and NO radicals, respectively). A major flavonoid, pinostrobin, was further nonchromatographically isolated. Pinostrobin was shown to be a potent 5-LOX inhibitor (IC<sub>50</sub> = 0.499 µM) compared to nordihydroguaiaretic acid (NDGA; IC<sub>50</sub> = 5.020 µM) and betamethasone dipropionate (BD; IC<sub>50</sub> = 2.077 µM) as the first-line of AD treatment. Additionally, pinostrobin inhibited COX-2 (IC<sub>50</sub> = 285.67 µM), which was as effective as diclofenac sodium (IC<sub>50</sub> = 290.35 µM) and BD (IC<sub>50</sub> = 240.09 µM). This kinetic study and molecular modeling showed the mixed-type inhibition of NDGA and pinostrobin against 5-LOX. This study suggests that <i>B. rotunda</i> and its bioactive pinostrobin have promising properties for AD therapy.
Item Description:10.3390/antiox13010074
2076-3921