Screening for bioactive natural products from a 67-compound library of Glycyrrhiza inflata

Autor: Wei Song, Yan Lin, Yi Kuang, Xue Qiao, Gulnar Sabir, Shuang Wang, Kai Li, Min Ye
Rok vydání: 2017
Předmět:
Glycyrrhiza inflata
Lipopolysaccharides
Stereochemistry
Tyrosinase
Clinical Biochemistry
Anti-Inflammatory Agents
Pharmaceutical Science
Apoptosis
01 natural sciences
Biochemistry
Plant Roots
Small Molecule Libraries
chemistry.chemical_compound
Mice
Cell Line
Tumor
Drug Discovery
Glycyrrhiza
Bioassay
Animals
Humans
Molecular Biology
IC50
chemistry.chemical_classification
Protein Tyrosine Phosphatase
Non-Receptor Type 1
Biological Products
Traditional medicine
biology
010405 organic chemistry
Monophenol Monooxygenase
Macrophages
Organic Chemistry
NF-kappa B
Hep G2 Cells
biology.organism_classification
0104 chemical sciences
010404 medicinal & biomolecular chemistry
Enzyme
HEK293 Cells
RAW 264.7 Cells
chemistry
Cell culture
Toxicity
MCF-7 Cells
Molecular Medicine
Drug Screening Assays
Antitumor
Glabridin
Zdroj: Bioorganicmedicinal chemistry. 25(14)
ISSN: 1464-3391
Popis: Licorice shows a variety of pharmacological activities. This work aims to discover bioactive natural products from one botanical source of licorice, Glycyrrhiza inflata. A total of 67 free phenolics were isolated to form a compound library. Based on the bioactivities of licorice, these compounds were screened using cell- or enzyme-based bioassay methods. A total of 11 compounds exhibited potent cytotoxic activities against three human cancer cell lines (HepG2, SW480 and MCF7), while showed little toxicity on human normal cell lines LO2 and HEK293T. A number of chalcones showed remarkable anti-inflammatory activities. Among them, 2 (licochalcone B, IC50 8.78μM), 10 (licoagrochalcone C, IC50 9.35μM) and 13 (licochalcone E, IC50 9.09μM) exhibited the most potent inhibitory activities on LPS-induced NO production, whereas 1, 8, 10, 12 and 13 (IC50 13.9, 7.27, 2.44, 6.67 and 3.83μM) showed potent inhibitory activities on NF-κB transcription. Nine prenylated phenolics were found to be PTP1B inhibitors. Particularly, licoagrochalcone A (4), kanzonol C (7), 2'-hydroxyisolupalbigenin (35), gancaonin Q (45), glisoflavanone (50) and glabrol (53) showed IC50 values of 0.31-0.97μM. Compounds 24 (semilicoisoflavone B, IC50 0.25μM), 26 (allolicoisoflavone B, IC50 0.80μM) and 64 (glabridin, IC50 0.10μM) showed noticeable tyrosinase inhibitory activities. Most of the above bioactive compounds were reported for the first time.
Databáze: OpenAIRE
Externí odkaz: