Background:To study the effects of the main diterpene esters in Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)on the transcriptional activity and protein expression of liver X receptor(LXR).Methods:The effe...Background:To study the effects of the main diterpene esters in Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)on the transcriptional activity and protein expression of liver X receptor(LXR).Methods:The effect of the main diterpene ester components in Semen Euphorbiae on the viability of HEK293 cells were studied by MTT assay.The LXR-Luc plasmid vector was transfected into HEK293 cells and treated with Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)for 24 h.The effect of the main diterpene ester components of Semen Euphorbiae on LXR-Luc luciferase activity was investigated by dual luciferase reporter gene system,and the expression of LXRαprotein was detected by Western Blot.Results:Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)could significantly reduce the relative luciferase activity(RLU)of LXRα,and the expression level of LXRαprotein was significantly down-regulated.Conclusion:Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)can inhibit the expression of LXR protein level,which may be achieved by inhibiting the transcriptional activity of LXR.展开更多
Two novel diterpenes, Euphorprolitherin A (1) and Euphorprolitherin B (2), were isolated from the roots of Euphorbia prolifera. Their structures were elucidated on the basis of spectroscopic methods.
Two new diterpenes, 15-ethyl-18-methyl pinifolate （1） and 18-hydroxy-labda-8（17）, 13E-dien-15-acetate （2）, were isolated from the needles of Pinus sylvestris. Their structures were elucidated by spectroscopic me...Two new diterpenes, 15-ethyl-18-methyl pinifolate （1） and 18-hydroxy-labda-8（17）, 13E-dien-15-acetate （2）, were isolated from the needles of Pinus sylvestris. Their structures were elucidated by spectroscopic methods, including 2D-NMR spectra. Compound 1 exhibited the significant cytotoxic activity against the human carcinoma cell lines Hela, SK-N-SH and BEL-7402 in vitro.展开更多
Euphorbia ebracteolata Hayata （E. ebracteolata） is a Chinese herbal medicine used for the treatment of tumor diseases. An ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry （UPLC-Q-...Euphorbia ebracteolata Hayata （E. ebracteolata） is a Chinese herbal medicine used for the treatment of tumor diseases. An ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry （UPLC-Q-TOF/MS） based chemical profiling approach was established for the rapid separation and characterization on phloroglucinol derivatives and diterpenes in E. ebracteolata. Three phloroglucinol derivatives and nine diterpenes were identified by exact mass measurement and were further confirmed by Ms2 data. In addition, the chemical profiles of six compounds were acquired by reference standards. Furthermore, the fragmentation rules of phloroglucinol derivatives and diterpenes of E. ebracteolata were analyzed, and each chromatographic peak was classified.展开更多
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
Five new diterpenes were isolated from Euphorbia sieboldiana and identified as atis-16-en-13(S)-hydroxy-3,14-dione(Ⅰ),atis-16-en- 14-oxo-13(S),3 β-diol(Ⅱ),atisane-3-oxo-16α,17-diol(Ⅳ),atisane-3β ,16α,17-triol(...Five new diterpenes were isolated from Euphorbia sieboldiana and identified as atis-16-en-13(S)-hydroxy-3,14-dione(Ⅰ),atis-16-en- 14-oxo-13(S),3 β-diol(Ⅱ),atisane-3-oxo-16α,17-diol(Ⅳ),atisane-3β ,16α,17-triol(Ⅴ)and atisane-3β-acetyl-16α,17-diol(Ⅵ)based on the chemical,spectral evidences and X-ray diffraction.展开更多
Two new brominated diterpenes, namely, laurendecumtriol and 11-deacetylpinnaterpene C, were isolated and identified from the marine red alga Laurencia decumbens. Their structures were established on the basis of vario...Two new brominated diterpenes, namely, laurendecumtriol and 11-deacetylpinnaterpene C, were isolated and identified from the marine red alga Laurencia decumbens. Their structures were established on the basis of various NMR spectroscopic techniques and HR-ESI-MS analyses.展开更多
Two new labdane diterpenoids named heteronone A （1） and heteronone B （2） were isolated from the aerial parts of Leonurus heterophyllus Sweet. Their structures were established by various spectroscopic means, and t...Two new labdane diterpenoids named heteronone A （1） and heteronone B （2） were isolated from the aerial parts of Leonurus heterophyllus Sweet. Their structures were established by various spectroscopic means, and the structure of heteronone A is confn-med by X-ray diffraction analysis.展开更多
Three new jatropholane-type diterpenoids,jatropholones C-E(1-3),along with seven other known compounds,including sikkimenoid B(4),jatrophaldehyde(5),epi-jatrophaldehyde(6),epi-jatrophol(7),jatrophol(8),jatropholone A(...Three new jatropholane-type diterpenoids,jatropholones C-E(1-3),along with seven other known compounds,including sikkimenoid B(4),jatrophaldehyde(5),epi-jatrophaldehyde(6),epi-jatrophol(7),jatrophol(8),jatropholone A(9),and jatropholone B(10),were isolated from the roots of a natural cultivar of Jatropha curcas(J.curcas cv.Multiflorum CY Yang).The structural elucidations of 1-3 were accomplished by extensive NMR analysis.Compounds 4,6,and 8 demonstrated inhibition activity against the microorganisms with the MIC values from 0.10 to 0.18 mg/mL.展开更多
Five new guanacastane-type diterpenes,named guanacastepenes P–T(1–5),were isolated from cultures of the fungus Psathyrella candolleana.Their structures were elucidated on the basis of extensive spectroscopic methods...Five new guanacastane-type diterpenes,named guanacastepenes P–T(1–5),were isolated from cultures of the fungus Psathyrella candolleana.Their structures were elucidated on the basis of extensive spectroscopic methods.All of the compounds were tested for their 11b-hydroxysteroid dehydrogenase(11b-HSD1)inhibitory activity.Compound 3 exhibited inhibitory activity against both human and mouse isozymes of 11b-HSD1 with IC50 values of 6.2 and 13.9 lM,respectively.展开更多
基金supported by National Natural Science Foundation of China(Grant No.82074021).
文摘Background:To study the effects of the main diterpene esters in Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)on the transcriptional activity and protein expression of liver X receptor(LXR).Methods:The effect of the main diterpene ester components in Semen Euphorbiae on the viability of HEK293 cells were studied by MTT assay.The LXR-Luc plasmid vector was transfected into HEK293 cells and treated with Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)for 24 h.The effect of the main diterpene ester components of Semen Euphorbiae on LXR-Luc luciferase activity was investigated by dual luciferase reporter gene system,and the expression of LXRαprotein was detected by Western Blot.Results:Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)could significantly reduce the relative luciferase activity(RLU)of LXRα,and the expression level of LXRαprotein was significantly down-regulated.Conclusion:Euphorbia factor L_(1),L_(2),L_(3),L_(7a),L_(7b)and L_(8)can inhibit the expression of LXR protein level,which may be achieved by inhibiting the transcriptional activity of LXR.
基金We wish to thank the Teaching and Research Award Program for Outstanding Young Teachers in Higher Education Institutions of the Ministry of Education and the Med-X Foundation from Fudan University.
文摘Two novel diterpenes, Euphorprolitherin A (1) and Euphorprolitherin B (2), were isolated from the roots of Euphorbia prolifera. Their structures were elucidated on the basis of spectroscopic methods.
文摘Two new diterpenes, 15-ethyl-18-methyl pinifolate （1） and 18-hydroxy-labda-8（17）, 13E-dien-15-acetate （2）, were isolated from the needles of Pinus sylvestris. Their structures were elucidated by spectroscopic methods, including 2D-NMR spectra. Compound 1 exhibited the significant cytotoxic activity against the human carcinoma cell lines Hela, SK-N-SH and BEL-7402 in vitro.
基金supported by National Science and Technology Support Program and Drug Safety Critical Technology (2006BAI14B00)funding subject-Common and Important Drug Safety Standards(2006BAI14B01)
文摘Euphorbia ebracteolata Hayata （E. ebracteolata） is a Chinese herbal medicine used for the treatment of tumor diseases. An ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry （UPLC-Q-TOF/MS） based chemical profiling approach was established for the rapid separation and characterization on phloroglucinol derivatives and diterpenes in E. ebracteolata. Three phloroglucinol derivatives and nine diterpenes were identified by exact mass measurement and were further confirmed by Ms2 data. In addition, the chemical profiles of six compounds were acquired by reference standards. Furthermore, the fragmentation rules of phloroglucinol derivatives and diterpenes of E. ebracteolata were analyzed, and each chromatographic peak was classified.
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.
文摘Five new diterpenes were isolated from Euphorbia sieboldiana and identified as atis-16-en-13(S)-hydroxy-3,14-dione(Ⅰ),atis-16-en- 14-oxo-13(S),3 β-diol(Ⅱ),atisane-3-oxo-16α,17-diol(Ⅳ),atisane-3β ,16α,17-triol(Ⅴ)and atisane-3β-acetyl-16α,17-diol(Ⅵ)based on the chemical,spectral evidences and X-ray diffraction.
基金the National Natural Science Foundation of China.
文摘vinyl-8,11,13-podocatriene 8, which is a model of Carnosic acid type diterpenes, has been synthesized by an expeditious convergent synthetic approach.
基金financially supported by the National Natural Science Foundation of China(No.30530080)by the Department of Science and Technology of Shandong Province(No.2006GG2205023).
文摘Two new brominated diterpenes, namely, laurendecumtriol and 11-deacetylpinnaterpene C, were isolated and identified from the marine red alga Laurencia decumbens. Their structures were established on the basis of various NMR spectroscopic techniques and HR-ESI-MS analyses.
文摘Two new labdane diterpenoids named heteronone A （1） and heteronone B （2） were isolated from the aerial parts of Leonurus heterophyllus Sweet. Their structures were established by various spectroscopic means, and the structure of heteronone A is confn-med by X-ray diffraction analysis.
基金This work was financially supported by the Key Projects of the Chinese Ministry of Science and Technology(2007BAD32B01-03 and SB2007FY400)the National Natural Science Foundation of China(81202437)the National Knowledge Innovation Program of Chinese Academy of Sciences(KSCX2-YW-G-038).
文摘Three new jatropholane-type diterpenoids,jatropholones C-E(1-3),along with seven other known compounds,including sikkimenoid B(4),jatrophaldehyde(5),epi-jatrophaldehyde(6),epi-jatrophol(7),jatrophol(8),jatropholone A(9),and jatropholone B(10),were isolated from the roots of a natural cultivar of Jatropha curcas(J.curcas cv.Multiflorum CY Yang).The structural elucidations of 1-3 were accomplished by extensive NMR analysis.Compounds 4,6,and 8 demonstrated inhibition activity against the microorganisms with the MIC values from 0.10 to 0.18 mg/mL.
基金the National Natural Sciences Foundation of China(U1132607,81373289).
文摘Five new guanacastane-type diterpenes,named guanacastepenes P–T(1–5),were isolated from cultures of the fungus Psathyrella candolleana.Their structures were elucidated on the basis of extensive spectroscopic methods.All of the compounds were tested for their 11b-hydroxysteroid dehydrogenase(11b-HSD1)inhibitory activity.Compound 3 exhibited inhibitory activity against both human and mouse isozymes of 11b-HSD1 with IC50 values of 6.2 and 13.9 lM,respectively.
