Medicina oral, patologia oral y cirugia bucal · 2017
Relationship between -889 C/T polymorphism in interleukin-1A gene and risk of chronic periodontitis: Evidence from a meta-analysis with new published findings.
СтатьяМетаанализОбзорНазвание и аннотация: Перевод пока не подготовлен
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da Silva F-R-P, Guimarães-Vasconcelos A-C-C, de-Carvalho-França L-F, di-Lenardo D, Rodrigues L-S, Barreto-do-Nascimento M-L-L, Vasconcelos D-F-P
Аннотация
BACKGROUND: Scopoletin, a compound abundant in Rubiaceae such as Lasianthus lucidus and Morinda citrifolia, has demonstrated various activities, including antimicrobial activity, antinociceptive properties or pain relief and effects on cancer cell lines. Accordingly, it has significant potential as a precursor for synthetic bioactive agents for reducing pain such its derivative includes benzene ring. However, very little has been reported regarding normal cellular effects or human skin irritation of such synthetic compounds, knowledge which is necessary if they are to be further developed. Thus, the aim of this study was to isolate scopoletin from Thai Rubiaceae, synthesize a derivative, and test its cytotoxicity.
MATERIALS AND METHODS: Stem bark of L. lucidus and fruits of M. citrifolia were extracted and the extract partitioned into hydrophilic and lipophilic fractions. Lipophilic extracts were further fractionated by column chromatography and analysed by High-Performance Liquid Chromatography with Diode Array Detection (HPLC-DAD). Purified scopoletin was used for the synthesis of its benzoate derivative and their structures were confirmed with the help of Nuclear Magnetic Resonance (NMR) spectroscopy. The cytotoxicity of the derivative compound was tested in the immortalized human keratinocyte HaCaT cell line.
RESULTS: The lipophilic extracts displayed scopoletin contents of 16.14% and 13.94%, respectively. Scopoletin was completely converted to a target derivative, 6-methoxy-2-oxo-4a,8a-dihydro-2H-chromen-7-yl benzoate. This compound exhibited an IC50 value of 182.95 ± 6.15 µg/mL, with cell viability increased at concentrations less than 15.63 µg/mL but decreased at concentrations of 31.25 to 500 µg/mL.
CONCLUSIONS: We completely actualized both isolation and synthesis to achieve a high yield of the target scopoletin and benzoylscopoletin. The cytotoxicity evidence obtained from this study supports the establishment of safe dosage limits, which have not been previously reported. This finding provides a scientific basis for further drug development. The analyses demonstrate reproducible isolation of scopoletin and synthesis of the derivative.
MATERIALS AND METHODS: Stem bark of L. lucidus and fruits of M. citrifolia were extracted and the extract partitioned into hydrophilic and lipophilic fractions. Lipophilic extracts were further fractionated by column chromatography and analysed by High-Performance Liquid Chromatography with Diode Array Detection (HPLC-DAD). Purified scopoletin was used for the synthesis of its benzoate derivative and their structures were confirmed with the help of Nuclear Magnetic Resonance (NMR) spectroscopy. The cytotoxicity of the derivative compound was tested in the immortalized human keratinocyte HaCaT cell line.
RESULTS: The lipophilic extracts displayed scopoletin contents of 16.14% and 13.94%, respectively. Scopoletin was completely converted to a target derivative, 6-methoxy-2-oxo-4a,8a-dihydro-2H-chromen-7-yl benzoate. This compound exhibited an IC50 value of 182.95 ± 6.15 µg/mL, with cell viability increased at concentrations less than 15.63 µg/mL but decreased at concentrations of 31.25 to 500 µg/mL.
CONCLUSIONS: We completely actualized both isolation and synthesis to achieve a high yield of the target scopoletin and benzoylscopoletin. The cytotoxicity evidence obtained from this study supports the establishment of safe dosage limits, which have not been previously reported. This finding provides a scientific basis for further drug development. The analyses demonstrate reproducible isolation of scopoletin and synthesis of the derivative.