Polyprenylated Benzoylphloroglucinols with DNA Polymerase Inhibitory Activity from the Fruits of Garcinia schomburgkiana
| Autor: | Katsumi Nishimura, Yoshiyuki Mizushina, Takao Tanahashi, Duy Hoang Le, Yukiko Takenaka |
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| Rok vydání: | 2016 |
| Předmět: |
DNA polymerase
Stereochemistry Phloroglucinol Pharmaceutical Science 01 natural sciences Analytical Chemistry HeLa chemistry.chemical_compound Inhibitory Concentration 50 Drug Discovery Humans Garcinia Pharmacology Biflavonoids biology Bicyclic molecule Molecular Structure 010405 organic chemistry Organic Chemistry Absolute configuration biology.organism_classification DNA Polymerase I Antineoplastic Agents Phytogenic 0104 chemical sciences 010404 medicinal & biomolecular chemistry Complementary and alternative medicine chemistry Vietnam Fruit biology.protein Proton NMR Molecular Medicine Drug Screening Assays Antitumor Drugs Chinese Herbal HeLa Cells |
| Zdroj: | Journal of natural products. 79(7) |
| ISSN: | 1520-6025 |
| Popis: | Chemical investigation of the fruits of Garcinia schomburgkiana collected in Vietnam led to the isolation of eight new schomburgkianones, A-H (1-8), four known (9-12) polyprenylated benzoylphloroglucinols, and four known biflavonoids. The structures of these compounds were elucidated by spectroscopic and chemical means. The absolute configuration at C-40 of 1 and 2 was determined by (1)H NMR analyses of their MPA esters. The configuration of the bicyclo[3.3.1]nonane core of the polyprenylated benzoylphloroglucinols was assigned by comparison of their experimental ECD spectra with those of related compounds. The polyprenylated benzoylphloroglucinols exhibited inhibitory activities against mammalian DNA polymerases α and λ, with IC50 values ranging from 5.0 to 8.8 μM. Compounds 1, 2, 4, 5, and 9-11 showed cytotoxic effects against HeLa human cervical cancer cells with median lethal dose values lower than 10 μM. |
| Databáze: | OpenAIRE |
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