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  1. In vitro inhibitory mechanisms and molecular docking of 1'-S-1'-acetoxychavicol acetate on human cytochrome P450 enzymes
    Haque AKMM, Leong KH, Lo YL, Awang K, Nagoor NH
    Phytomedicine, 2017 Jul 15;31:1-9.
    PMID: 28606510 DOI: 10.1016/j.phymed.2017.05.002
    BACKGROUND: The compound, 1'-S-1'-acetoxychavicol acetate (ACA), isolated from the rhizomes of a Malaysian ethno-medicinal plant, Alpinia conchigera Griff. (Zingiberaceae), was previously shown to have potential in vivo antitumour activities. In the development of a new drug entity, potential interactions of the compound with the cytochrome P450 superfamily metabolizing enzymes need to be ascertain.

    PURPOSE: The concomitant use of therapeutic drugs may cause potential drug-drug interactions by decreasing or increasing plasma levels of the administered drugs, leading to a suboptimal clinical efficacy or a higher risk of toxicity. Thus, evaluating the inhibitory potential of a new chemical entity, and to clarify the mechanism of inhibition and kinetics in the various CYP enzymes is an important step to predict drug-drug interactions.

    STUDY DESIGN: This study was designed to assess the potential inhibitory effects of Alpinia conchigera Griff. rhizomes extract and its active constituent, ACA, on nine c-DNA expressed human cytochrome P450s (CYPs) enzymes using fluorescent CYP inhibition assay.

    METHODS/RESULTS: The half maximal inhibitory concentration (IC50) of Alpinia conchigera Griff. rhizomes extract and ACA was determined for CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C19, CYP2D6, CYP2E1, CYP3A4 and CYP3A5. A. conchigera extract only moderately inhibits on CYP3A4 (IC50 = 6.76 ± 1.88µg/ml) whereas ACA moderately inhibits the activities of CYP1A2 (IC50 = 4.50 ± 0.10µM), CYP2D6 (IC50 = 7.50 ± 0.17µM) and CYP3A4 (IC50 = 9.50 ± 0.57µM) while other isoenzymes are weakly inhibited. In addition, mechanism-based inhibition studies reveal that CYP1A2 and CYP3A4 exhibited non-mechanism based inhibition whereas CYP2D6 showed mechanism-based inhibition. Lineweaver-Burk plots depict that ACA competitively inhibited both CYP1A2 and CYP3A4, with a Ki values of 2.36 ± 0.03 µM and 5.55 ± 0.06µM, respectively, and mixed inhibition towards CYP2D6 with a Ki value of 4.50 ± 0.08µM. Further, molecular docking studies show that ACA is bound to a few key amino acid residues in the active sites of CYP1A2 and CYP3A4, while one amino residue of CYP2D6 through predominantly Pi-Pi interactions.

    CONCLUSION: Overall, ACA may demonstrate drug-drug interactions when co-administered with other therapeutic drugs that are metabolized by CYP1A2, CYP2D6 or CYP3A4 enzymes. Further in vivo studies, however, are needed to evaluate the clinical significance of these interactions.

  2. Fulltext Prospect of biobased antiviral face mask to limit the coronavirus outbreak
    Chowdhury MA, Shuvho MBA, Shahid MA, Haque AKMM, Kashem MA, Lam SS, et al.
    Environ Res, 2021 Jan;192:110294.
    PMID: 33022215 DOI: 10.1016/j.envres.2020.110294
    The rapid spread of COVID-19 has led to nationwide lockdowns in many countries. The COVID-19 pandemic has played serious havoc on economic activities throughout the world. Researchers are immensely curious about how to give the best protection to people before a vaccine becomes available. The coronavirus spreads principally through saliva droplets. Thus, it would be a great opportunity if the virus spread could be controlled at an early stage. The face mask can limit virus spread from both inside and outside the mask. This is the first study that has endeavoured to explore the design and fabrication of an antiviral face mask using licorice root extract, which has antimicrobial properties due to glycyrrhetinic acid (GA) and glycyrrhizin (GL). An electrospinning process was utilized to fabricate nanofibrous membrane and virus deactivation mechanisms discussed. The nanofiber mask material was characterized by SEM and airflow rate testing. SEM results indicated that the nanofibers from electrospinning are about 15-30 μm in diameter with random porosity and orientation which have the potential to capture and kill the virus. Theoretical estimation signifies that an 85 L/min rate of airflow through the face mask is possible which ensures good breathability over an extensive range of pressure drops and pore sizes. Finally, it can be concluded that licorice root membrane may be used to produce a biobased face mask to control COVID-19 spread.
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