Andrographis Paniculata And Curcuma Xanthorrhiza Extracts And Active Constituents Inhibit Morphine Glucuronidation

Husni, Zulhilmi (2016) Andrographis Paniculata And Curcuma Xanthorrhiza Extracts And Active Constituents Inhibit Morphine Glucuronidation. Masters thesis, Universiti Sains Malaysia.

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    Abstract

    Baru-baru ini, fenomena interaksi herba-drug telah mendapat perhatian hampir seantero dunia atas sebab tersebarnya populariti penggunaan produk herba dalam bentuk suplemen tambahan. Dalam kajian ini kesan perencatan herba Malaysia yang telah disenaraikan iaitu: hempedu bumi (Andrographis paniculata) dan temulawak (Curcuma xanthorrhiza) terhadap proses glukuronidasi morfina akan diuji menggunakan model protein rekombinan UGT2B7 dan mikrosom hepar bersumberkan dari manusia. Kesemua ekstrak etanol dan akueus bagi herba hempedu bumi serta andrografolida telah merencatkan aktiviti glukuronidasi morfina kecuali neoandrografolida. Ekstrak akueus merencatkan glukuronidasi morfina secara sederhana jika dibandingkan dengan ekstrak etanol dan andrografolida. Andrografolida adalah fito-konstituen yang dipercayai telah menyumbang besar terhadap trend perencatan yang ditunjukkan oleh ekstrak etanol dan analisis kinetik menunjukkan bahawa kedua-dua ekstrak etanol dan andrografolida merencatkan proses glukuronidasi morfina secara kompetitif (bukan tulen) dengan julat pemalar-perencatan, Kic dari 3.22 hingga 17.94 μg/mL bagi ekstrak etanol dan juga dari 1.35 hingga 15.06 μM bagi andrografolida yang mana kesemuanya dikaji di dalam protein rekombinan dan mikrosom hepar. A resurgence in the widespread popularity of herbal product in its supplement forms has recently attracted global attention concerning to herb-drug interaction. The inhibitory effects of selected Malaysian medicinal plant herbs namely Andrographis paniculata and Curcuma xanthorrhiza on morphine glucuronidation were evaluated on recombinant UGT2B7 protein and human liver microsomes. Ethanolic and aqueous extracts of Andrographis paniculata as well as andrographolide inhibited morphine glucuronidation at various degrees except for neoandrographolide. Aqueous extract moderately inhibited morphine glucuronidation compared to andrographolide and ethanolic extract. Andrographolide is the main perpetrator that contributes to the potent inhibitory action of ethanolic extract and kinetic analysis has suggested that andrographolide and Andrographis paniculata ethanolic extract competitively (mixed competitive) inhibited morphine glucuronidation featuring competitive inhibition constant, Kic values ranging from 1.35 to 15.06 μM for andrographolide and 3.22 to 17.94 μg/mL for Andrographis paniculata ethanolic extract on both recombinant UGT2B7 protein and human liver microsomes.

    Item Type: Thesis (Masters)
    Subjects: R Medicine > RM Therapeutics. Pharmacology > RM300-666 Drugs and their actions
    Divisions: Pusat Penyelidikan Dadah dan Ubat-ubatan (Centre for Drug Research)
    Depositing User: Mr Noorazilan Noordin
    Date Deposited: 09 Mar 2017 08:38
    Last Modified: 09 Mar 2017 08:38
    URI: http://eprints.usm.my/id/eprint/32348

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