Oligonol is a low-molecular-weight form of polyphenol that is derived from lychee fruit extract and contains catechin-type monomers and oligomers of proanthocyanidins. This study investigates the anti-diabetic activities of oligonol via α-glucosidase and human recombinant protein tyrosine phosphatase 1B (PTP1B) assays, as well as its anti-Alzheimer activities by evaluating the ability of this compound to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Oligonol exhibited potent concentration-dependent anti-diabetic activities by inhibiting α-glucosidase and PTP1B with IC50 values of 23.14 µg/mL and 1.02 µg/mL, respectively. Moreover, a kinetics study revealed that oligonol inhibited α-glucosidase (K i = 22.36) and PTP1B (K i = 8.51) with characteristics typical of a mixed inhibitor. Oligonol also displayed potent concentration-dependent inhibitory activity against AChE and BChE with IC50 values of 4.34 µg/mL and 2.07 µg/mL, respectively. However, oligonol exhibited only marginal concentration-dependent BACE1 inhibitory activity with an IC50 value of 130.45 µg/mL. A kinetics study revealed mixed-type inhibition against AChE (K i = 4.65) and BACE1 (K i = 58.80), and noncompetitive-type inhibition against BChE (K i = 9.80). Furthermore, oligonol exhibited dose-dependent inhibitory activity against peroxynitrite (ONOO(-))-mediated protein tyrosine nitration. These results indicate that oligonol has strong preventative potential in diabetes mellitus and in Alzheimer's disease.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/s12272-015-0682-8 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Anti-cancer effect of midazolam via downregulating YWHAH in papillary thyroid cancer cells.
Discov Oncol
January 2025
Department of Anesthesiology, The First Affiliated Hospital, Zhejiang University School of Medicine, No.1367 Wenyi West Road, Yuhang District, Hangzhou, 311100, People's Republic of China.
The work is aimed to investigate whether midazolam functions in thyroid cancer and reveal the potential mechanism of action. Cell viability was detected by CCK-8 method when treated by varying doses of midazolam to detect the cytotoxicity of midazolam on human thyroid follicular epithelial cell line and thyroid cancer cell lines. In thyroid cancer cells, EDU staining, wound healing and transwell assays were respectively used to detect cell proliferation, migration and invasion.
View Article and Find Full Text PDFThe efficacy and safety of tyrosine kinase inhibitors in the treatment of advanced or metastatic chordoma: a single-arm meta-analysis.
Neurosurg Rev
January 2025
Department of Neurosurgery, Xuanwu Hospital, Capital Medical University, 45# Changchun Street, Xicheng District, Beijing, China.
Chordoma is a rare malignant tumor with a higher incidence in males than in females. There is an increasing number of clinical studies related to tyrosine kinase inhibitors (TKIs), yet the efficacy and safety of different drugs vary. In this single-arm meta-analysis evaluating the efficacy and safety of TKIs for chordoma treatment, 12 studies involving 365 patients were analyzed.
View Article and Find Full Text PDFSelf-sufficient biocatalytic cascade for the continuous synthesis of danshensu in flow.
Appl Microbiol Biotechnol
January 2025
Department of Chemistry, Biochemistry and Pharmaceutical Sciences, University of Bern, Freiestrasse 3, 3012, Bern, Switzerland.
A new strategy has been developed to successfully produce the active component danshensu ex vivo. For this purpose, phenylalanine dehydrogenase from Bacillus sphaericus was combined with the novel hydroxyphenylpyruvate reductase from Mentha x piperita, thereby providing an in situ cofactor regeneration throughout the conversion process. The purified enzymes were co-immobilized and subsequently employed in batch biotransformation, resulting in 60% conversion of 10 mM L-dopa within 24 h, with a catalytic amount of NAD as cofactor.
View Article and Find Full Text PDFThe Melanocyte and Nerve Fiber Cross-Talk, Facilitated Also by Semaphorin-4A, Enhances UV-B-Induced Melanogenesis.
Pigment Cell Melanoma Res
January 2025
QIMA Life Sciences, QIMA Monasterium GmbH, Münster, Germany.
Epidermal melanocytes form synaptic-like contacts with cutaneous nerve fibers, but the functional outcome of these connections remains elusive. In this pilot study we used our fully humanized re-innervated skin organ culture model to investigate melanocyte-nerve fiber interactions in UV-B-induced melanogenesis. UV-B-irradiation significantly enhanced melanin content and tyrosinase activity in re-innervated skin compared to non-innervated controls, indicating that neuronal presence is essential for exacerbating pigmentation upon UV-B irradiation in long-term culture.
View Article and Find Full Text PDFUnleashing the Power of Covalent Drugs for Protein Degradation.
Med Res Rev
January 2025
Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan, China.
Targeted protein degradation (TPD) has emerged as a significant therapeutic approach for a variety of diseases, including cancer. Advances in TPD techniques, such as molecular glue (MG) and lysosome-dependent strategies, have shown substantial progress since the inception of the first PROTAC in 2001. The PROTAC methodology represents the forefront of TPD technology, with ongoing evaluation in more than 20 clinical trials for the treatment of diverse medical conditions.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!