Objective: To evaluate the cytotoxic activity of wood extracts of Lunasia amara Blanco(L. amara) and to perform further phytochemical standardization.Methods: The wood extracts of L. amara were assessed for cytotoxic ...Objective: To evaluate the cytotoxic activity of wood extracts of Lunasia amara Blanco(L. amara) and to perform further phytochemical standardization.Methods: The wood extracts of L. amara were assessed for cytotoxic activity by in vitro tetrazolium bromide(MTT) method against two human cancer cell lines, cervical cancer cells(He La) and breast cancer cells(T47D). Thin layer chromatography, Dragendorf,acetic anhydride-sulfuric acid and ferric chloride were used to detect alkaloids, steroids and polyphenols, respectively. Furthermore, quantitative determination of total alkaloid by ultra fast liquid chromatography-photodiode array detection using lunacrine as a marker compound was performed as well.Results: The ethyl acetate extract exhibited higher cell-growth inhibition than methanol and n-hexane extracts on He La and T47 D cancer line cells with the IC50 of 71.15 and79.04 mg/m L, respectively. Total alkaloid in ethyl acetate extract was counted as(10.46 ± 0.28)%(w/w), while lunacrine determined by ultra fast liquid chromatographyphotodiode array detection method was found to be(3.55 ± 0.26)%(w/w).Conclusions: The high total alkaloid and lunacrine concentration on the extract confirm the potential cytotoxic property of ethyl acetate wood extract of L. amara.展开更多
Lunasia amara Blanco is a famous plant in South Sulawesi. It was used largely by local people as antibacteria and aphrodisiac. Quinoline alkaloid lunacridine was known as the active principle from Lunasia amara Blanco...Lunasia amara Blanco is a famous plant in South Sulawesi. It was used largely by local people as antibacteria and aphrodisiac. Quinoline alkaloid lunacridine was known as the active principle from Lunasia amara Blanco. Its activity was reported as a DNA Intercalating Topoisomerase II inhibitor. In this study, we have isolated and assayed the cytotoxic activity of lunacridine on P388 murine leukemia cells by MTT colorimetric assay （in vitro）. Lunacridine showed the less cytotoxic activity with the IC50 of 39.52 μg/mL. With the aim to explore the structural determinants responsible for this activity, molecular docking study have been carried out with DNA model using AutoDock 4.0 software with various total of energy evaluations （in silico）. The best docking reached at the total energy evaluations of 2.5 × 107 with the binding free energy of-6.63 kcal/mol. Analysis of the docking results was in accordance with the ability of lunacridine to intercalate between base pairs of DNA. Cytotoxic activity of lunacridine is less probably due to low affinity and molecular interaction. Therefore this study suggests to design and to develop lunacridine as a lead compound for anticancer drug.展开更多
基金Supported by the Ministry of Research,Technology and Higher Education,Republic of Indonesia through Hibah Bersaing grant(Grant No.2851/UN28/DT/2014)
文摘Objective: To evaluate the cytotoxic activity of wood extracts of Lunasia amara Blanco(L. amara) and to perform further phytochemical standardization.Methods: The wood extracts of L. amara were assessed for cytotoxic activity by in vitro tetrazolium bromide(MTT) method against two human cancer cell lines, cervical cancer cells(He La) and breast cancer cells(T47D). Thin layer chromatography, Dragendorf,acetic anhydride-sulfuric acid and ferric chloride were used to detect alkaloids, steroids and polyphenols, respectively. Furthermore, quantitative determination of total alkaloid by ultra fast liquid chromatography-photodiode array detection using lunacrine as a marker compound was performed as well.Results: The ethyl acetate extract exhibited higher cell-growth inhibition than methanol and n-hexane extracts on He La and T47 D cancer line cells with the IC50 of 71.15 and79.04 mg/m L, respectively. Total alkaloid in ethyl acetate extract was counted as(10.46 ± 0.28)%(w/w), while lunacrine determined by ultra fast liquid chromatographyphotodiode array detection method was found to be(3.55 ± 0.26)%(w/w).Conclusions: The high total alkaloid and lunacrine concentration on the extract confirm the potential cytotoxic property of ethyl acetate wood extract of L. amara.
文摘Lunasia amara Blanco is a famous plant in South Sulawesi. It was used largely by local people as antibacteria and aphrodisiac. Quinoline alkaloid lunacridine was known as the active principle from Lunasia amara Blanco. Its activity was reported as a DNA Intercalating Topoisomerase II inhibitor. In this study, we have isolated and assayed the cytotoxic activity of lunacridine on P388 murine leukemia cells by MTT colorimetric assay （in vitro）. Lunacridine showed the less cytotoxic activity with the IC50 of 39.52 μg/mL. With the aim to explore the structural determinants responsible for this activity, molecular docking study have been carried out with DNA model using AutoDock 4.0 software with various total of energy evaluations （in silico）. The best docking reached at the total energy evaluations of 2.5 × 107 with the binding free energy of-6.63 kcal/mol. Analysis of the docking results was in accordance with the ability of lunacridine to intercalate between base pairs of DNA. Cytotoxic activity of lunacridine is less probably due to low affinity and molecular interaction. Therefore this study suggests to design and to develop lunacridine as a lead compound for anticancer drug.
