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- Title
Inhibitory activities of Aruncus dioicus alkaloidal glycosides against protein tyrosine phosphatase 1B and α-glucosidase: A methodical theory-experiment investigation.
- Authors
Phi-Hung Nguyen; Bui, Thanh Q.; Thi-Tuyen Tran; Thi-Thuc Bui; Thi-Thuy Do; Dao-Cuong To; Manh Hung Tran; Phan Tu Quy; Nguyen Quang Co; Nguyen Vinh Phu; Nguyen Thi Ai Nhung
- Abstract
Objective: Aruncus dioicus has been known by the scientific literature and folk experiences for its diverse biological activities, including anti-hyperglycemic effects. Methodology: The aerial parts of the plant collected from Quan Lan Island (Vietnam) were subjected to a methodical theory-experiment investigation for its chemical composition and biological potentials. Results: Firstly, experimental isolation and spectroscopic characterization identified the compositional compounds, ie sambunigrin (1), prunasin (2), uridine (3), and adenosine (4). Secondly, their elucidated structures were predicted with promising bio-chemo-pharmacological potentiality by different computational platforms, ie: docking simulation (docking scores < 10 kcal.mol−1); quantum calculation (dipole moments < 3 Debye); QSARIS model (satisfying Lipinski's rule of five); SwissADME model (satisfying Pires’ interpretations). Finally, the compounds (1-4) were under accumulative purification and in vitro tests against diabetes-related enzymes, ie: protein tyrosine phosphatase 1B (1 with lowest IC50 value 0.39 ± 0.26 μM, 2 with no activity) and α-glucosidase (1 with lowest IC50 value 44.89 ± 0.93 μM, 2 with no activity); also, the inhibitory kinetics based on Lineweaver-Burk and Dixon plot experiments revealed the competitive inhibition mode of 1 against PTP1B (Ki value 0.49 μM). Conclusions: Altogether, the results obtained suggest that A. dioicus and its bioactive compounds, especially sambunigrin (1), uridine (3), and adenosine (4), could be considered as a natural source for further research and development of anti-diabetic agents.
- Subjects
SCIENTIFIC literature; PROTEIN-tyrosine phosphatase; PHOSPHOPROTEIN phosphatases; FOLK literature; HYPOGLYCEMIC agents; ALPHA-glucosidases
- Publication
Natural Product Communications, 2024, Vol 19, Issue 8, p1
- ISSN
1934-578X
- Publication type
Article
- DOI
10.1177/1934578X241271648