Cytotoxic cardenolides from the latex of Calotropis procera
| Autor: | Gamal Badr, Lixin Zhang, Huanqin Dai, Ahmed A. M. Shoreit, Xueting Liu, Lamya H. Alwahibi, Ronald J. Quinn, Miaomiao Liu, Nadia H. Mohamed, Wael M. Abdel-Mageed, Mady A. Ismail |
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| Rok vydání: | 2015 |
| Předmět: |
Antifungal Agents
Latex Stereochemistry Clinical Biochemistry Ethyl acetate Pharmaceutical Science Microbial Sensitivity Tests Biochemistry HeLa Structure-Activity Relationship chemistry.chemical_compound Calotropis procera Cell Line Tumor Drug Discovery Humans Structure–activity relationship Molecular Biology Cell Proliferation Chloroform Chromatography Bacteria Dose-Response Relationship Drug Molecular Structure biology Organic Chemistry Broth microdilution Fungi Calotropis biology.organism_classification Antimicrobial Antineoplastic Agents Phytogenic Anti-Bacterial Agents Cardenolides chemistry Molecular Medicine Drug Screening Assays Antitumor HeLa Cells |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 25:4615-4620 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2015.08.044 |
| Popis: | Three new cardenolides (3, 9 and 10), along with eight known ones, were isolated from the latex of Calotropis procera. The structural determination was accomplished by the 1D- and 2D-NMR spectra as well as HRESIMS analysis. The growth inhibitory activity of the latex and its sub-fractions as well as isolated compounds was evaluated against human A549 and Hela cell lines. The results exhibited that latex had strong growth inhibitory activity with IC50s of (3.37 μM, A-549) and (6.45 μM, Hela). Among the four extracts (hexane, chloroform, ethyl acetate and aqueous), chloroform extract displayed the highest potential cytotoxic activity, with IC50s of (0.985 μM, A-549) and (1.471 μM, Hela). All the isolated compounds displayed various degrees of cytotoxic activity and the highest activity was observed by calactin (1) with IC50s values of (0.036 μM, A-549) and (0.083 μM, Hela). None of these isolated compounds exhibited good antimicrobial activity evaluated by determination of their MICs using the broth microdilution method against various infectious pathogens. The structure-activity relationships for cytotoxic activity were also discussed. |
| Databáze: | OpenAIRE |
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