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Indole alkaloids from Ochreinauclea maingayi (Rubiaceae) as butyrylcholinesterase inhibitors and their paralysis effect in transgenic Caenorhabditis elegans.
Osman, Norfaizah; Awang, Khalijah; Khaw, Kooi Yeong; Qi Mak, Wen; Tiamas, Shelly Gapil; Maulana, Saipul; Zubair, Muhammad Sulaiman; Pudjiastuti, Pratiwi; Hazni, Hazrina; Liew, Sook Yee; Zahari, Azeana.
Afiliación
  • Osman N; Department of Chemistry, Faculty of Science, Universiti Malaya, Kuala Lumpur, Malaysia.
  • Awang K; Department of Chemistry, Faculty of Science, Universiti Malaya, Kuala Lumpur, Malaysia.
  • Khaw KY; Centre for Natural Products Research and Drug Discovery (CENAR), Universiti Malaya, Kuala Lumpur, Malaysia.
  • Qi Mak W; School of Pharmacy, Monash University Malaysia, Subang Jaya, Selangor, Malaysia.
  • Tiamas SG; School of Pharmacy, Monash University Malaysia, Subang Jaya, Selangor, Malaysia.
  • Maulana S; Department of Chemistry, Faculty of Science, Universiti Malaya, Kuala Lumpur, Malaysia.
  • Zubair MS; Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Tadulako University, Palu, Indonesia.
  • Pudjiastuti P; Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Tadulako University, Palu, Indonesia.
  • Hazni H; Department of Pharmaceutical Science, Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia.
  • Liew SY; Centre for Natural Products Research and Drug Discovery (CENAR), Universiti Malaya, Kuala Lumpur, Malaysia.
  • Zahari A; Centre for Natural Products Research and Drug Discovery (CENAR), Universiti Malaya, Kuala Lumpur, Malaysia.
Nat Prod Res ; : 1-8, 2024 Aug 21.
Article en En | MEDLINE | ID: mdl-39165195
ABSTRACT
This study investigated the butyrylcholinesterase (BChE) inhibitory activity of harmane (1), naucledine (2), and dihydrodeglycocadambine (3) isolated from fractions F7 and F9 of Ochreinauclea maingayi. Both fractions demonstrated significant inhibition, exceeding 80%, against BChE at 100 µg/mL. Compound 2, is the most potent inhibitor, exhibiting an IC50 value of 22.08 µM, followed by 1 and 3 (IC50 23.96 and 30.32 µM, respectively). Docking studies revealed that 1 and 2 effectively bind to BChE, with binding energies of -51.24 and -57.17 kcal/mol, respectively. Kinetic analysis of 2 indicated mixed-mode inhibition of BChE, with a Ki of 6.08 µM. In the paralysis assay, 1 showed a weak delay in paralysis and reduced the paralysis ratio from 72.59 ± 4.7% to 60.00 ± 7.0% (12.59% reduction) followed by 2 with 70.00 ± 1.7% (2.59% reduction) compared with negative standard (DMSO 0.1%) on human amyloid ß-protein in a transgenic Caenorhabditis elegans (CL4176) model.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Nat Prod Res Año: 2024 Tipo del documento: Article País de afiliación: Malasia Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Nat Prod Res Año: 2024 Tipo del documento: Article País de afiliación: Malasia Pais de publicación: Reino Unido