Two new compounds,badounoids A(1)and B(2),together with 13 known norsesquiterpenes,were isolated from the leaves of Croton tiglium L.The structures of the new compounds were established by means of spectroscopic metho...Two new compounds,badounoids A(1)and B(2),together with 13 known norsesquiterpenes,were isolated from the leaves of Croton tiglium L.The structures of the new compounds were established by means of spectroscopic methods.The absolute configuration of badounoid B was determined by single-crystal X-ray diffraction analysis.All the known compounds were isolated from Croton plants for the first time which added a new chemical facet for this genus.The selected compounds were evaluated for their cytostatic activity against several cancer cell lines.None of them was found to be active.展开更多
Objective of the study:We used fluorescence imaging methods of apoptosis and necrosis in human renal carcinoma A498 tumor cells in vitro to reveal the indicated forms of cell death under the combined effect of flavono...Objective of the study:We used fluorescence imaging methods of apoptosis and necrosis in human renal carcinoma A498 tumor cells in vitro to reveal the indicated forms of cell death under the combined effect of flavonoid-containing extract of Gratiola officinalis and cytostatic(cyclo-phosphamide).Materials and methods:The dyes were propidium iodide and acridine orange,which were used in the"alive and dead"test.This test helped us to identify the total number of dead cells in the forms of necrosis and apoptosis and the number of cells in which apoptosis had started,it was characterized by the appearance of apoptotic bodies or nucleus pyknosis.Results:We found the most pronounced cytotoxic activity at the ratio of extract of Gratiola officinalis and cyclophosphamide concentrations of 1∶1.The number of living cells decreased when exposed to the ratio of extract and cytostatic concentrations of 2∶1.When the ratio of concentration of the extract relative to the cytostatic increased to 3∶1,the cytostatic activity of the extract began to appear,the total number of tumor cells decreased.The number of cells with nucleus pyknosis and the number of cells with apoptosis signs significantly increased at a 3∶1 ratio of extract and cytostatic concentrations,which confirms the presence of pro-apoptotic activity of the studied combination.This trend indicates the dependence of a certain form of cell death(apoptosis,necrosis)on the ratio of extract and cytostatic doses,and it also demon-strates the cytostatic and cytotoxic effects of this combination.Conclusion:Fluorescence methods of investigation in the"alive and dead"test allowed us to visualize the forms of cell death of human kidney carcinoma A498 by combined exposure to the fiavonoid-containing extract of Gratiola officinalis and cytostatic(cyclophosphamide)24 h after exposure.We found that the combination with a concentration ratio of the extract and cyclophosphamide of 3:1 has the greatest effectiveness due to stimulation of the cytostatic effect and cytotoxic effect.展开更多
New complexes of coumarin-3-carboxylic acid(HCCA) with Ho(Ⅲ) and Pr(Ⅲ) were synthesized and their structures and spectral properties were investigated by elemental analysis,IR,Raman and NMR measurements.According to...New complexes of coumarin-3-carboxylic acid(HCCA) with Ho(Ⅲ) and Pr(Ⅲ) were synthesized and their structures and spectral properties were investigated by elemental analysis,IR,Raman and NMR measurements.According to the experimental data the complexes’ formula and geometries were suggested.Vibrational frequencies,IR intensities and Raman activities as well as 1H NMR chemical shifts of HCCA and its Ho(Ⅲ) and Pr(Ⅲ) complexes were presented.The comparative experimental vibrational and NMR analyses of both the ligand and the Ln(Ⅲ) complexes predicted the bidentate binding to Ho(Ⅲ) and Pr(Ⅲ) through the deprotonated carboxylic oxygen and the carbonylic oxygen of the ligand.The cytotoxic/cytostatic properties of the ligand and the newly synthesized complexes of coumarin-3-carboxylic acid with Ho(Ⅲ) and Pr(Ⅲ) were tested by MTT reduction assay against two mouse tumor cell lines:melanoma B16 and fibrosarcoma L929.They were also tested for cytotoxicity against normal mouse peritoneal macrophages.The proliferation inhibitory effect of the complexes compared to that of the ligand proved their cytotoxic/cytostatic properties against both the tumor cell lines.In addition,the complexes were less cytotoxic against normal mouse macrophages and were able to modulate NO release by activated macrophages.The obtained results were in accordance with our previously published data concerning the activity of lanthanide(Ⅲ) complexes with other coumarin derivatives.展开更多
基金This work was financially supported by the Project of Natural Compound Library Construction from Chinese Academy of Sciences(KSCX2-EW-R-15).
文摘Two new compounds,badounoids A(1)and B(2),together with 13 known norsesquiterpenes,were isolated from the leaves of Croton tiglium L.The structures of the new compounds were established by means of spectroscopic methods.The absolute configuration of badounoid B was determined by single-crystal X-ray diffraction analysis.All the known compounds were isolated from Croton plants for the first time which added a new chemical facet for this genus.The selected compounds were evaluated for their cytostatic activity against several cancer cell lines.None of them was found to be active.
基金The work was supported by State Assignment No.121032600197-2 of the Health Ministry of Russia.
文摘Objective of the study:We used fluorescence imaging methods of apoptosis and necrosis in human renal carcinoma A498 tumor cells in vitro to reveal the indicated forms of cell death under the combined effect of flavonoid-containing extract of Gratiola officinalis and cytostatic(cyclo-phosphamide).Materials and methods:The dyes were propidium iodide and acridine orange,which were used in the"alive and dead"test.This test helped us to identify the total number of dead cells in the forms of necrosis and apoptosis and the number of cells in which apoptosis had started,it was characterized by the appearance of apoptotic bodies or nucleus pyknosis.Results:We found the most pronounced cytotoxic activity at the ratio of extract of Gratiola officinalis and cyclophosphamide concentrations of 1∶1.The number of living cells decreased when exposed to the ratio of extract and cytostatic concentrations of 2∶1.When the ratio of concentration of the extract relative to the cytostatic increased to 3∶1,the cytostatic activity of the extract began to appear,the total number of tumor cells decreased.The number of cells with nucleus pyknosis and the number of cells with apoptosis signs significantly increased at a 3∶1 ratio of extract and cytostatic concentrations,which confirms the presence of pro-apoptotic activity of the studied combination.This trend indicates the dependence of a certain form of cell death(apoptosis,necrosis)on the ratio of extract and cytostatic doses,and it also demon-strates the cytostatic and cytotoxic effects of this combination.Conclusion:Fluorescence methods of investigation in the"alive and dead"test allowed us to visualize the forms of cell death of human kidney carcinoma A498 by combined exposure to the fiavonoid-containing extract of Gratiola officinalis and cytostatic(cyclophosphamide)24 h after exposure.We found that the combination with a concentration ratio of the extract and cyclophosphamide of 3:1 has the greatest effectiveness due to stimulation of the cytostatic effect and cytotoxic effect.
基金Project supported by the Bulgarian Ministry of Education and Science
文摘New complexes of coumarin-3-carboxylic acid(HCCA) with Ho(Ⅲ) and Pr(Ⅲ) were synthesized and their structures and spectral properties were investigated by elemental analysis,IR,Raman and NMR measurements.According to the experimental data the complexes’ formula and geometries were suggested.Vibrational frequencies,IR intensities and Raman activities as well as 1H NMR chemical shifts of HCCA and its Ho(Ⅲ) and Pr(Ⅲ) complexes were presented.The comparative experimental vibrational and NMR analyses of both the ligand and the Ln(Ⅲ) complexes predicted the bidentate binding to Ho(Ⅲ) and Pr(Ⅲ) through the deprotonated carboxylic oxygen and the carbonylic oxygen of the ligand.The cytotoxic/cytostatic properties of the ligand and the newly synthesized complexes of coumarin-3-carboxylic acid with Ho(Ⅲ) and Pr(Ⅲ) were tested by MTT reduction assay against two mouse tumor cell lines:melanoma B16 and fibrosarcoma L929.They were also tested for cytotoxicity against normal mouse peritoneal macrophages.The proliferation inhibitory effect of the complexes compared to that of the ligand proved their cytotoxic/cytostatic properties against both the tumor cell lines.In addition,the complexes were less cytotoxic against normal mouse macrophages and were able to modulate NO release by activated macrophages.The obtained results were in accordance with our previously published data concerning the activity of lanthanide(Ⅲ) complexes with other coumarin derivatives.
