Rapid Identification of α-Glucosidase Inhibitors from Phlomis tuberosa by Sepbox Chromatography and Thin-Layer Chromatography Bioautography
Open Access
- 6 February 2015
- journal article
- research article
- Published by Public Library of Science (PLoS) in PLOS ONE
- Vol. 10 (2), e0116922
- https://doi.org/10.1371/journal.pone.0116922
Abstract
Alpha-glucosidase inhibitors currently form an important basis for developing novel drugs for diabetes treatment. In our preliminary tests, the ethyl acetate fraction of Phlomis tuberosa extracts showed significant α-glucosidase inhibitory activity (IC₅₀ = 100 μg/mL). In the present study, a combined method using Sepbox chromatography and thin-layer chromatography (TLC) bioautography was developed to probe α-glucosidase inhibitors further. The ethyl acetate fraction of P. tuberosa extracts was separated into 150 individual subfractions within 20 h using Sepbox chromatography. Then, under the guidance of TLC bioautography, 20 compounds were successfully isolated from these fractions, including four new diterpenoids [14-hydroxyabieta-8,11,13-triene-11-carbaldehyde-18-oic-12-carboxy-13-(1-hydroxy-1-methylethyl)-lactone (1), 14-hydroxyabieta-8,11,13-triene-17-oic-12-carboxy-13-(1-hydroxy-1-methylethyl)-lactone (2), 14,16-dihydroxyabieta-8,11,13-triene-15,17-dioic acid (3), and phlomisol (15,16-eposy-8,13(16),14-labdatrien-19-ol) (4)], and 16 known compounds. Activity estimation indicated that 15 compounds showed more potent α-glucosidase inhibitory effects (with IC50 values in the range 0.067–1.203 mM) than the positive control, acarbose (IC50 = 3.72 ± 0.113 mM). This is the first report of separation of α-glucosidase inhibitors from P. tuberosa.This publication has 25 references indexed in Scilit:
- Antimicrobial, anti-inflammatory activities and toxicology of phenylethanoid glycosides from Monochasma savatieri Franch. ex MaximJournal of Ethnopharmacology, 2013
- Antidiabetic and antioxidant properties of Ficus deltoidea fruit extracts and fractionsBMC Complementary and Alternative Medicine, 2013
- Alpha-glucosidase inhibitors 2012 – cardiovascular considerations and trial evaluationDiabetes and Vascular Disease Research, 2012
- Sepbox Technique in Natural ProductsJournal of Young Pharmacists, 2011
- Benzyl Derivatives with in Vitro Binding Affinity for Human Opioid and Cannabinoid Receptors from the Fungus Eurotium repensJournal of Natural Products, 2011
- A new biflavonoid from Daphniphyllum angustifolium HutchFitoterapia, 2009
- Drug Discovery and Natural Products: End of an Era or an Endless Frontier?Science, 2009
- Flavonoids and a New Polyacetylene from Bidens parviflora WilldMolecules, 2008
- Toxicological Evaluation of Polyphenol Extract from Acerola (Malpighia emarginata DC.) FruitJournal of Food Science, 2008
- Cardiovascular benefits and safety profile of acarbose therapy in prediabetes and established type 2 diabetesCardiovascular Diabetology, 2007