Evaluation of bioactive saponins and triterpenoidal aglycons for their binding properties on human endothelin ETA and angiotensin AT1 receptors
| Autor: | Catherina Caballero-George, A. Vlietinck, Georges Vauquelin, Sandra Apers, Y. Okamoto, Zakaria H. Mbwambo, Patrick Vanderheyden, Luc Pieters, Mahabir P. Gupta, T. Masaki |
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| Přispěvatelé: | Molecular and Biochemical Pharmacology, Vrije Universiteit Brussel |
| Jazyk: | angličtina |
| Rok vydání: | 2004 |
| Předmět: |
Saponin
CHO Cells Binding Competitive complex mixtures Receptor Angiotensin Type 1 chemistry.chemical_compound Radioligand Assay Cricetulus Triterpene Betulinic acid Cricetinae parasitic diseases Animals Humans Receptor Oleanolic acid Pharmacology chemistry.chemical_classification Angiotensin II receptor type 1 Plants Medicinal Chemistry Plant Extracts Saponins Receptor Endothelin A Angiotensin II Triterpenes carbohydrates (lipids) Biochemistry cardiovascular system Female Endothelin receptor Phytotherapy |
| Zdroj: | Phytotherapy research |
| ISSN: | 0951-418X |
| Popis: | Different types of triterpenes including saponins and aglycons were evaluated for their ability to inhibit [3H] BQ-123 and [3H] angiotensin II binding to the human endothelin 1 ETA and angiotensin II AT1 receptors, respectively. Selectivity for only one of the two receptors was exhibited by asiatic acid and its saponins (ETA) and oleanolic acid (AT1). To a lesser extent betulinic acid, β-amyrin and friedelin also showed selectivity for the ETA receptor. To address the question whether the effect of saponins on cell membranes might interfere with the normal binding of specific radioligands to their receptors, the activity of saponins with different haemolytic properties were compared. Highly haemolytic saponins such as α-hederin and β-escine showed partial (60%) inhibition of radioligand-binding to the ETA receptor and complete inhibition (100%) to the AT1 receptor. Moreover, the haemolytically inactive kryptoescine, at the same concentration, caused complete inhibiton of radioligand-binding to both receptors, indicating that inhibition of receptor binding was not related to the membrane-interacting properties of saponins. Copyright © 2004 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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