In this study, ent-Kaurane-3β,16β,17-trioi （1） and ent-kaurane-2a,16β,17-triol （2）, were isolated from the leaves ofRubus corchorifolius L. f. Their structures were elucidated based on extensive spectroscopic a...In this study, ent-Kaurane-3β,16β,17-trioi （1） and ent-kaurane-2a,16β,17-triol （2）, were isolated from the leaves ofRubus corchorifolius L. f. Their structures were elucidated based on extensive spectroscopic analysis. NMR experiments identified the two compounds and X-ray crystallographic analysis confirmed their crystal structures. The crystal of 1 belongs to monoclinic with space group P21 and a = 10.7641（3）, b = 7.2789（3）, c = 11.7862（4） A, β = 95.275（3）°, V = 919.55（6） A3, Z = 2, C20H34O4, Mr = 322.49 g/mol, Dc = 1.230 g/m3, F（000） = 376, 2 = 1.54178 A,μ = 0.661 mm-1, R = 0.0319, and wR = 0.0811 for 10889 observed reflections （I〉 2σ（I））. The crystal of 2 is classified as orthorhombic with space group P212121 and a = 10.7641（3）, b = 12.72224（19）, c = 21.3929（3） A, V= 1748.94（4） A3, Z= 4, C20H3404, Mr = 322.47, De = 1.225 Mg/m3 F（000） = 712, λ = 1.54184 A,μ = 0.625 mm-1, R = 0.0303 and wR = 0.0759 for 10470 observed reflections （1〉 2σ（I））. Meanwhile, the compound revealed low inhibitory activities toward HepG2, MCF-7, and SCG-7901 cells.展开更多
The tender leaves of Rubus corchorifolius L.f.(R.corchorifolius)have been made into herbal tea for relieving coughs in East and Southeast Asia from ancient times.Herein,we obtained an ethyl acetate extract from R.corc...The tender leaves of Rubus corchorifolius L.f.(R.corchorifolius)have been made into herbal tea for relieving coughs in East and Southeast Asia from ancient times.Herein,we obtained an ethyl acetate extract from R.corchorifolius leaves and isolated a major bioactive compound within.Structural analysis of the isolated compound was performed by spectroscopic methods and the compound was identified as ethyl ferulate.Effect of ethyl ferulate on the growth and proliferation of human liver cancer HepG2 cells and normal human liver LO2 cells was determined by MTT assay.We found that ethyl ferulate significantly suppressed the cell proliferation of HepG2 cells(IC_(50)26.4μM),while it did not cause cytotoxicity on LO2 cells.In addition,flow cytometry analysis demonstrated that ethyl ferulate inhibited HepG2 cell growth via inducing cellular apoptosis.Specifically,ethyl ferulate reduced the electrical potential of the mitochondrial membrane and increased the concentration of calcium ions inside cells.Moreover,these changes were accompanied by increases in the expression of the pro-apoptotic proteins,such as cleaved caspase-3 and Bax.In contrast,cell morphology and growth of LO2 cells remained unaffected.In conclusion,for the first time,our observations demonstrated that ethyl ferulate possesses great potential as an effective and safe antitumor agent for cancer chemoprevention in humans.展开更多
Objective： To investigate the anti-leukemia effect of total saponins of Rubus parvifo/ius L. （TSRP） on K562 cell xenografts in nude mice and the mechanisms of action. Methods： The K562 cell xenografts in nude mice...Objective： To investigate the anti-leukemia effect of total saponins of Rubus parvifo/ius L. （TSRP） on K562 cell xenografts in nude mice and the mechanisms of action. Methods： The K562 cell xenografts in nude mice were established, and then randomly divided into 5 groups, the control group, the cytosine arabinoside group（Am-c） and 3 TSRP groups （20, 40 and 100 mg/kg）. The tumor volume and mass of each group of nude mice were measured and the anti-tumor rates of TSRP were calculated subsequently. The apoptosis status of tumor cells was detected by hematoxylin-eosin （HE） and terminal dexynucleotidyl transferase （TdT）-mediated dUTP nick end labeling （TUNEL） staining analysis. Finally, the activities of apoptosis related signaling of signal transducer and activator of transcription 3 （STAT3）, eukaryotic initiation factor 4E （eIF4E） and B-cell lymphoma-2 （bcl-2） were determined with immunohistochemistry tests. Results： Subcutaneous injection of K562 cells induced tumor formation in nude mice, and the TSRP treated group showed a significant inhibitory effect on tumor formation. The nude mice treated with TSRP showed a significant decrease in tumor growth rate and tumor weight in comparison to the control group （all P〈0.05）. The HE staining and TUNEL assay showed that TSRP induced cell death by apoptosis. The immunohistochemical assay showed down-regulation of the bcl-2 gene in the TSRP treated cells. The phosphorylation levels of elF4E and STAT3 were decreased obviously after the treatment of TSRP. Conclusion： TSRP had an excellent tumor-suppressing effect on K562 cells in the nude mice xenograft model, suggesting that TSPR can be developed as a promising anti-chronic myeloide leukemia drug.展开更多
基金financially supported by the National Science and Technology Pillar Program during the Twelfth Five-year Plan Period(2012BAK17B00)the Doctoral Program of Higher Education,China(No.20114404120022)the Agricultural Science and Technology Planned Projects of Guangzhou,China(No.2012A020602038)
文摘In this study, ent-Kaurane-3β,16β,17-trioi （1） and ent-kaurane-2a,16β,17-triol （2）, were isolated from the leaves ofRubus corchorifolius L. f. Their structures were elucidated based on extensive spectroscopic analysis. NMR experiments identified the two compounds and X-ray crystallographic analysis confirmed their crystal structures. The crystal of 1 belongs to monoclinic with space group P21 and a = 10.7641（3）, b = 7.2789（3）, c = 11.7862（4） A, β = 95.275（3）°, V = 919.55（6） A3, Z = 2, C20H34O4, Mr = 322.49 g/mol, Dc = 1.230 g/m3, F（000） = 376, 2 = 1.54178 A,μ = 0.661 mm-1, R = 0.0319, and wR = 0.0811 for 10889 observed reflections （I〉 2σ（I））. The crystal of 2 is classified as orthorhombic with space group P212121 and a = 10.7641（3）, b = 12.72224（19）, c = 21.3929（3） A, V= 1748.94（4） A3, Z= 4, C20H3404, Mr = 322.47, De = 1.225 Mg/m3 F（000） = 712, λ = 1.54184 A,μ = 0.625 mm-1, R = 0.0303 and wR = 0.0759 for 10470 observed reflections （1〉 2σ（I））. Meanwhile, the compound revealed low inhibitory activities toward HepG2, MCF-7, and SCG-7901 cells.
基金supported by Natural Science Foundation of Guangdong basic and applied basic research foundation([2018]105 to Xuexiang Chen)U.S.Department of Agriculture(MAS00450,MAS00492 to Hang Xiao)+3 种基金Natural Science Foundation of Guangdong basic and applied basic research foundation(2021A1515010965 to Xuexiang Chen)Laboratory opening project of Guangzhou Medical University(PX-1020423 to Xuexiang Chen)Guangdong Provincial Department of Education(S202010570042 to Changhui Du&Xuexiang Chen)Communist Youth League Committee of Guangzhou Medical University(2019A060 to Changhui Du&Xuexiang Chen).
文摘The tender leaves of Rubus corchorifolius L.f.(R.corchorifolius)have been made into herbal tea for relieving coughs in East and Southeast Asia from ancient times.Herein,we obtained an ethyl acetate extract from R.corchorifolius leaves and isolated a major bioactive compound within.Structural analysis of the isolated compound was performed by spectroscopic methods and the compound was identified as ethyl ferulate.Effect of ethyl ferulate on the growth and proliferation of human liver cancer HepG2 cells and normal human liver LO2 cells was determined by MTT assay.We found that ethyl ferulate significantly suppressed the cell proliferation of HepG2 cells(IC_(50)26.4μM),while it did not cause cytotoxicity on LO2 cells.In addition,flow cytometry analysis demonstrated that ethyl ferulate inhibited HepG2 cell growth via inducing cellular apoptosis.Specifically,ethyl ferulate reduced the electrical potential of the mitochondrial membrane and increased the concentration of calcium ions inside cells.Moreover,these changes were accompanied by increases in the expression of the pro-apoptotic proteins,such as cleaved caspase-3 and Bax.In contrast,cell morphology and growth of LO2 cells remained unaffected.In conclusion,for the first time,our observations demonstrated that ethyl ferulate possesses great potential as an effective and safe antitumor agent for cancer chemoprevention in humans.
基金Supported by grants from Zhejiang Provincial Administration of Traditional Chinese Medicine(No.2011ZA081,No.2012ZB120,No.2013ZB095 and No.2014ZB089)Hangzhou Medical Science and Technology Plan(No.2012A048)
文摘Objective： To investigate the anti-leukemia effect of total saponins of Rubus parvifo/ius L. （TSRP） on K562 cell xenografts in nude mice and the mechanisms of action. Methods： The K562 cell xenografts in nude mice were established, and then randomly divided into 5 groups, the control group, the cytosine arabinoside group（Am-c） and 3 TSRP groups （20, 40 and 100 mg/kg）. The tumor volume and mass of each group of nude mice were measured and the anti-tumor rates of TSRP were calculated subsequently. The apoptosis status of tumor cells was detected by hematoxylin-eosin （HE） and terminal dexynucleotidyl transferase （TdT）-mediated dUTP nick end labeling （TUNEL） staining analysis. Finally, the activities of apoptosis related signaling of signal transducer and activator of transcription 3 （STAT3）, eukaryotic initiation factor 4E （eIF4E） and B-cell lymphoma-2 （bcl-2） were determined with immunohistochemistry tests. Results： Subcutaneous injection of K562 cells induced tumor formation in nude mice, and the TSRP treated group showed a significant inhibitory effect on tumor formation. The nude mice treated with TSRP showed a significant decrease in tumor growth rate and tumor weight in comparison to the control group （all P〈0.05）. The HE staining and TUNEL assay showed that TSRP induced cell death by apoptosis. The immunohistochemical assay showed down-regulation of the bcl-2 gene in the TSRP treated cells. The phosphorylation levels of elF4E and STAT3 were decreased obviously after the treatment of TSRP. Conclusion： TSRP had an excellent tumor-suppressing effect on K562 cells in the nude mice xenograft model, suggesting that TSPR can be developed as a promising anti-chronic myeloide leukemia drug.
