Tetracyclic Endiandric Acids Isolated from Endiandra kingiana Gamble (Lauraceae) with In vitro and Molecular Docking Studies of β-Glucuronidase Activity.
6 affiliations
- 1Natural Products and Synthesis Organic Research Laboratory (NPSO), School of Chemical Sciences, School of Chemical Sciences, Universiti Sains Malaysia, 11800 USM Pulau Pinang, Malaysia.
- 2Faculty of Science and Marine Environment, Universiti Malaysia Terengganu, 21030, Terengganu, Malaysia.
- 3H.E.J Research Intitute of Chemistry, International Centre for Chemical and BIological Sciences, University of Karachi, Karachi-75270, Pakistan.
- 4Department of Chemistry, Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia.
- 5Biological Section, School of Distance Education, Universiti Sains Malaysia, 11800 USM, Pulau Pinang, Malaysia.
- 6Institute de Chimie des Substances Naturelles, CNRS, UPR 2301, Université Paris-Saclay, 91108 Gif-Sur-Yvette, France.
Abstract
β-glucuronidase is a lysosomal enzyme that hydrolyses of glucuronide conjugates, playing a significant role in drug and xenobiotic metabolism as well as various disease processes. Elevated activity of this enzyme reactivates glucuronidated carcinogens, promoting tumorigenesis and inflammation. Thus, inhibiting β-glucuronidase has emerged as a promising therapeutic strategy, particularly for the prevention of colonic carcinogenesis. In this study, three endiandric acid derivatives named kingianic acid A (1), tsangibeilin B (2), and endiandric acid M (3) that isolated from Endiandra kingiana bark, were evaluated for their β-glucuronidase inhibitory activity. Their chemical structures were identified using spectroscopic data and by comparison with published reports. In vitro enzyme inhibition assays revealed that compound 2 (IC50 value of 7.5 ± 2.77 μM) exhibited the most potent inhibition compared to compound 1 (IC50 value of 292 ± 5.40 μM) and the positive control, D-saccharic acid-1,4-lactone (IC50 value of 45.75 ± 2.16 μM). In addition, molecular docking studies further supported these findings, demonstrating that compound 2 exhibited stronger binding affinity to β-glucuronidase (-9.9 ± 0.1 kcal/mol) than compound 1 (IC50 value of 292 ± 5.40 μM) and D-saccharic acid-1,4-lactone (-7.0 ± 0.1 kcal/mol). These results highlight the potential of compound 2 as a lead scaffold for the development of β-glucuronidase inhibitors and contribute to the growing interest in plant-derived compounds for therapeutic applications.
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BibTeX
@article{tanazi2026tetracyclic,
title = {{Tetracyclic Endiandric Acids Isolated from Endiandra kingiana Gamble (Lauraceae) with In vitro and Molecular Docking Studies of β-Glucuronidase Activity.}},
author = {Nurul Najihah Husna Tanazi and Ahmad Nazif Aziz and M Iqbal Choudhary and Sadia Siddiq and Muhamad Aqmal Othman and Mohammad Tasyriq Che Omar and Cécile Apel and Mohamad Nurul Azmi},
journal = {Tropical life sciences research},
year = {2026},
month = oct,
doi = {10.21315/tlsr2026.37.3.15},
url = {https://europepmc.org/article/MED/42997703},
note = {CC BY},
}
RIS
TY - JOUR
TI - Tetracyclic Endiandric Acids Isolated from Endiandra kingiana Gamble (Lauraceae) with In vitro and Molecular Docking Studies of β-Glucuronidase Activity.
AU - Nurul Najihah Husna Tanazi
AU - Ahmad Nazif Aziz
AU - M Iqbal Choudhary
AU - Sadia Siddiq
AU - Muhamad Aqmal Othman
AU - Mohammad Tasyriq Che Omar
AU - Cécile Apel
AU - Mohamad Nurul Azmi
PY - 2026
DA - 2026/10/15
JO - Tropical life sciences research
DO - 10.21315/tlsr2026.37.3.15
UR - https://europepmc.org/article/MED/42997703
AB - β-glucuronidase is a lysosomal enzyme that hydrolyses of glucuronide conjugates, playing a significant role in drug and xenobiotic metabolism as well as various disease processes. Elevated activity of this enzyme reactivates glucuronidated carcinogens, promoting tumorigenesis and inflammation. Thus, inhibiting β-glucuronidase has emerged as a promising therapeutic strategy, particularly for the prevention of colonic carcinogenesis. In this study, three endiandric acid derivatives named kingianic acid A (1), tsangibeilin B (2), and endiandric acid M (3) that isolated from Endiandra kingiana bark, were evaluated for their β-glucuronidase inhibitory activity. Their chemical structures were identified using spectroscopic data and by comparison with published reports. In vitro enzyme inhibition assays revealed that compound 2 (IC50 value of 7.5 ± 2.77 μM) exhibited the most potent inhibition compared to compound 1 (IC50 value of 292 ± 5.40 μM) and the positive control, D-saccharic acid-1,4-lactone (IC50 value of 45.75 ± 2.16 μM). In addition, molecular docking studies further supported these findings, demonstrating that compound 2 exhibited stronger binding affinity to β-glucuronidase (-9.9 ± 0.1 kcal/mol) than compound 1 (IC50 value of 292 ± 5.40 μM) and D-saccharic acid-1,4-lactone (-7.0 ± 0.1 kcal/mol). These results highlight the potential of compound 2 as a lead scaffold for the development of β-glucuronidase inhibitors and contribute to the growing interest in plant-derived compounds for therapeutic applications.
SN - 1985-3718
SN - 2180-4249
ER -