Chiral resolution and anticancer effect of xanthones from Garcinia paucinervis
| Autor: | Dahong Li, Hui-Ming Hua, Chi Gong, Jingjing Xue, Cui-Cui Jia, Xin-Yu Li, Zhan-Lin Li |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Stereochemistry
Xanthones HL-60 Cells Fractionation 01 natural sciences Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Xanthone Ic50 values Humans Garcinia paucinervis Pharmacology Molecular Structure Plant Stems biology 010405 organic chemistry Cytotoxic potency General Medicine biology.organism_classification Antineoplastic Agents Phytogenic Chiral resolution 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry Caco-2 Cells Enantiomer Antiproliferative effect Garcinia |
| Zdroj: | Fitoterapia. 127:220-225 |
| ISSN: | 0367-326X |
| DOI: | 10.1016/j.fitote.2018.02.023 |
| Popis: | Bioassay-guided fractionation of the dichloromethane-soluble portion of the stems of Garcinia paucinervis led to the isolation of eight new xanthones, including three pairs of enantiomers, (+) and (−) paucinervins L-N (1a-3a, and 1b-3b), one optically pure compound, (−) paucinervin O (4), and one new analogue, paucinervin P (5), as well as thirteen known xanthones (6–18). Their structures were established by detailed analysis of extensive spectroscopic data. The absolute configurations of 1–4 were confirmed by ECD calculations. All the isolates 1–18 displayed antiproliferative effect against HL-60 with IC50 values ranging from 0.87 to 29.14 μM, of which compound 5 was the most active. Compounds 6, and 14 exhibited potential inhibitory activity against PC-3 cells, while compounds 5–7, 14, and 16–17 displayed cytotoxic potency against Caco-2 cells. A preliminary structure-activity relationship was also discussed. |
| Databáze: | OpenAIRE |
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