Two new steroidal glycosides named Lm-4 （1） and Lm-5 （2） were isolated from the tubers of Liriope muscari. Their structures were elucidated by 1D and 2D NMR, ESI/MALDIMS techniques, and chemical methods.
The present study was designed to investigate the chemical constituents and bioactivities of the roots of Liriope muscari(Decne.) L.H. Bailey. The compounds were isolated through various chromatography techniques, inc...The present study was designed to investigate the chemical constituents and bioactivities of the roots of Liriope muscari(Decne.) L.H. Bailey. The compounds were isolated through various chromatography techniques, including silica gel, Sephadex LH-20, and semi-preparative HPLC. The structures were elucidated by infrared(IR), mass spectrometric(MS), 1D- and 2D-NMR analyses in comparison with reference data. In addition, the cytotoxicity of these compounds against human breast cancer MDA-MB-435 cells was evaluated by the MTT assay. Two new steroidal glycosides, 25(R, S)-ruscogenin-1-O-[β-D-fucopyranosyl(1→2)]-[ β-D-xylopyranosyl(1→3)]-β-D-glucopyranoside(Liriopem I, 1) and 25(R, S)- ruscogenin-1-O-[β-D-fucopyranosyl(1→2)]-[β-D-xylopyranosyl(1→4)]-β-D-fucopyranoside(Liriopem II, 2) and two known compounds LM-S6(3) and DT-13(4) were isolated and identified. Liriopem I(1), liriopem II(2) and DT-13(4) showed remarkable cytotoxicity with IC50 values being(0.58 ± 0.08),(0.05 ± 0.10), and(0.15 ± 0.09) μg·m L-1, respectively. In summary, compounds 1 and 2 identified in the present study exerted cytotoxicity against breast cancer cells, providing a basis for future development of these compounds as novel anticancer agents.展开更多
AIM: To investigate the effect of DT-13 on gastric cancer cell migration, and to explore the possible mechanisms underlying the anti-metastasis activity of DT-13. METHODS: Growth inhibition of DT-13 was analyzed by th...AIM: To investigate the effect of DT-13 on gastric cancer cell migration, and to explore the possible mechanisms underlying the anti-metastasis activity of DT-13. METHODS: Growth inhibition of DT-13 was analyzed by the MTT assay. Cell migration was measured by the scratch-wound assay and transwell double chamber assay. To investigate the possible mechanisms underlying the anti-metastasis activity of DT-13, chemokine receptors that are involved in cancer metastasis(CCR2, CCR5, CCR7, CXCR4, and CXCR6) were detected by conventional PCR. The effect of DT-13 on CCR5 and CXCR4 expression was further evaluated by quantitative PCR and Western blot, respectively. The secretion of CCL5(ligand of CCR5) and SDF-1(ligand of CXCR4) were detected by enzyme-linked immunosorbent assay(ELISA). RESULTS: DT-13 inhibited BGC-823 and HGC-27 cell growth in a dose dependent manner, and the estimated IC50 value for 24 h treatment was 23.5 ± 5.1 μmol·L-1 for BGC-823 cells and 35.6 ± 7.6 μmol·L-1 for HGC-27 cells. DT-13 also significantly decreased gastric cancer cell migration. DT-13 significantly decreased the gene expression of CCR5 in both BGC-823 and HGC-27 gastric cancer cells, and moderately reduced the expression of CXCR4. Similar to the results of gene expression, significant down-regulation of CCR5 protein was observed, but CXCR4 protein levels were much less affected. CCL5 secretion, but not SDF-1 production, was inhibited by DT-13. CONCLUSION: DT-13 inhibited gastric cancer cell migration by down-regulation of the CCR5-CCL5 axis.展开更多
文摘Two new steroidal glycosides named Lm-4 （1） and Lm-5 （2） were isolated from the tubers of Liriope muscari. Their structures were elucidated by 1D and 2D NMR, ESI/MALDIMS techniques, and chemical methods.
基金supported by the Major National Science and Technology Project of China for Significant New Drugs Development(No.2012ZX09102201-015)the National Natural Science Foundation of China(No.81274004)+2 种基金the Priority Academic Program Development of Jiangsu Higher Education Institutionsthe 2011’Program for Excellent Scientific and Technological Innovation Team of Jiangsu Higher Educationthe Major Project Program of State Key Laboratory of Natural Medicines,China Pharmaceutical University(No.SKLNMZZ201203)
文摘The present study was designed to investigate the chemical constituents and bioactivities of the roots of Liriope muscari(Decne.) L.H. Bailey. The compounds were isolated through various chromatography techniques, including silica gel, Sephadex LH-20, and semi-preparative HPLC. The structures were elucidated by infrared(IR), mass spectrometric(MS), 1D- and 2D-NMR analyses in comparison with reference data. In addition, the cytotoxicity of these compounds against human breast cancer MDA-MB-435 cells was evaluated by the MTT assay. Two new steroidal glycosides, 25(R, S)-ruscogenin-1-O-[β-D-fucopyranosyl(1→2)]-[ β-D-xylopyranosyl(1→3)]-β-D-glucopyranoside(Liriopem I, 1) and 25(R, S)- ruscogenin-1-O-[β-D-fucopyranosyl(1→2)]-[β-D-xylopyranosyl(1→4)]-β-D-fucopyranoside(Liriopem II, 2) and two known compounds LM-S6(3) and DT-13(4) were isolated and identified. Liriopem I(1), liriopem II(2) and DT-13(4) showed remarkable cytotoxicity with IC50 values being(0.58 ± 0.08),(0.05 ± 0.10), and(0.15 ± 0.09) μg·m L-1, respectively. In summary, compounds 1 and 2 identified in the present study exerted cytotoxicity against breast cancer cells, providing a basis for future development of these compounds as novel anticancer agents.
基金supported by the Natural Science Foundation of Jiangsu Province(No.2012353)the Specialized Research Fund for the Doctoral Program of Higher Education of China(No.20120096120012)the National Natural Science Foundation of China(No.81071841)
文摘AIM: To investigate the effect of DT-13 on gastric cancer cell migration, and to explore the possible mechanisms underlying the anti-metastasis activity of DT-13. METHODS: Growth inhibition of DT-13 was analyzed by the MTT assay. Cell migration was measured by the scratch-wound assay and transwell double chamber assay. To investigate the possible mechanisms underlying the anti-metastasis activity of DT-13, chemokine receptors that are involved in cancer metastasis(CCR2, CCR5, CCR7, CXCR4, and CXCR6) were detected by conventional PCR. The effect of DT-13 on CCR5 and CXCR4 expression was further evaluated by quantitative PCR and Western blot, respectively. The secretion of CCL5(ligand of CCR5) and SDF-1(ligand of CXCR4) were detected by enzyme-linked immunosorbent assay(ELISA). RESULTS: DT-13 inhibited BGC-823 and HGC-27 cell growth in a dose dependent manner, and the estimated IC50 value for 24 h treatment was 23.5 ± 5.1 μmol·L-1 for BGC-823 cells and 35.6 ± 7.6 μmol·L-1 for HGC-27 cells. DT-13 also significantly decreased gastric cancer cell migration. DT-13 significantly decreased the gene expression of CCR5 in both BGC-823 and HGC-27 gastric cancer cells, and moderately reduced the expression of CXCR4. Similar to the results of gene expression, significant down-regulation of CCR5 protein was observed, but CXCR4 protein levels were much less affected. CCL5 secretion, but not SDF-1 production, was inhibited by DT-13. CONCLUSION: DT-13 inhibited gastric cancer cell migration by down-regulation of the CCR5-CCL5 axis.
