Anti-tuberculosis neolignans from Piper regnellii
| Autor: | Vera Ld Siqueira, Maria Valdrinez Campana Lonardoni, Caroline Ortega Terra Lemos, Regiane Bertin de Lima Scodro, Arlene G. Corrêa, Claudia Terencio Agostinho Pires, Lúcio Cardozo-Filho, R. F. Cardoso, D. A. G. Cortez, V.A. Souza, Vanessa da Silva Carrara |
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| Rok vydání: | 2012 |
| Předmět: |
Tuberculosis
Magnetic Resonance Spectroscopy Stereochemistry Sulforhodamine B Antitubercular Agents Pharmaceutical Science Potential candidate Microbial Sensitivity Tests Piper regnellii Lignans Cell Line Mycobacterium tuberculosis chemistry.chemical_compound Mice Anti tuberculosis Phenols Drug Discovery Toxicity Tests medicine Animals Cytotoxicity Benzofurans Pharmacology Chromatography biology Molecular Structure Plant Extracts Macrophages Resazurin medicine.disease biology.organism_classification Complementary and alternative medicine chemistry Molecular Medicine Piper |
| Zdroj: | Phytomedicine : international journal of phytotherapy and phytopharmacology. 20(7) |
| ISSN: | 1618-095X |
| Popis: | The present study determined the anti-Mycobacterium tuberculosis activities of supercritical CO2 extracts, neolignans eupomatenoid-5 (1), conocarpan (4) and eupomatenoid-3 (7) and their derivatives (2, 3, 5, 6, and 8) from Piper regnellii, as well as their cytotoxicities. The supercritical CO2 extract from leaves was purified by chromatographic methods, yielding compounds (1), (4) and (7), which were identified by (1)H NMR and comparison with literature data. Anti-M. tuberculosis activity (H37Rv and clinical isolates) was evaluated using a resazurin microtiter assay plate (REMA) to determine the MIC. The cytotoxicity assay was carried out in macrophages J774G.8 by sulforhodamine B colorimetric assay. The supercritical CO2 extracts from leaves and stems, and compound (4) showed activity against M. tuberculosis (MIC 15.6 μg/ml). Compound (1) showed the best activity (MIC 1.9 μg/ml), with good SI. Compounds (7) and (8) showed low activity against M. tuberculosis H37Rv. The derivative compounds did not show increased anti-M. tuberculosis activity. This is the first report, to our knowledge, to describe neolignans from P. regnellii with activity against M. tuberculosis, and compound (1) is a potential candidate for future antituberculosis drugs. |
| Databáze: | OpenAIRE |
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