A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots o...A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots of Stellera chamaejasme L. together with known chamaechromone. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.展开更多
The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L.(Thymelaeaceae) that is used in traditional Chinese medicine(TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isoch...The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L.(Thymelaeaceae) that is used in traditional Chinese medicine(TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isochamaejasmin was found to show similar bioactivity against Bcl-2 family proteins to the reference Bcl-2 ligand(–)-gossypol through 3D similarity search. It selectively bound to Bcl-xL and Mcl-1 with Ki values being 1.93 ± 0.13 μmol·L-1 and 9.98 ± 0.21 μmol·L-1, respectively. In addition, isochamaejasmin showed slight growth inhibitory activity against HL-60 with IC50 value being 50.40 ± 1.21 μmol·L-1 and moderate growth inhibitory activity against K562 cells with IC50 value being 24.51 ± 1.62 μmol·L-1. Furthermore, isochamaejasmin induced apoptosis of K562 cells by increasing the intracellular expression levels of proteins of the cleavage of caspase-9, caspase-3, and PARP which involved in the Bcl-2-induced apoptosis pathway. These results indicated that isochamaejasmin induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. chamaejasme L..展开更多
A new biflavonoid, stelleranol, was isolated from the roots of Stellera chamaejasme L.. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.
OBJECTIVE:To investigate the inhibitory and pro-apoptotic effect of Stellera Chamaejasme L extract(ESC) in vitro.METHODS:ESC was first extracted with ethanol,and then washed using a polyamide column with 60% ethanol.E...OBJECTIVE:To investigate the inhibitory and pro-apoptotic effect of Stellera Chamaejasme L extract(ESC) in vitro.METHODS:ESC was first extracted with ethanol,and then washed using a polyamide column with 60% ethanol.ESC was then decompressively recycled and vacuum dried at room temperature to obtain active fractions.Subsequently,the cytotoxic and apoptotic effects of ESC on NCI-H157 human lung cancer cells were determined.RESULTS:The results showed that ESC was rich in isomers of Chamaejasminor,neochamaejasmine and Sikokianin.ESC had significant cytotoxicity against NCI-H157 cells,with an IC 50 of approximately 18.50 μg.mL-1.ESC caused significant increase in total apoptotic rate,the activity of caspase 3 and 8,and Fas protein expression(P<0.05).CONCLUSION:The inhibitory effect of ESC on NCI-H157 tumor cells might partly be attributed to its apoptotic induction through activation of the Fas death receptor pathway.展开更多
Methanol extract of Stellera chamaejasme L wasassessed for antitumor activity by an antitumor activebioassay against murine leukemia P388 in vivo. Thebioassay-directed separation of the extract furnishedseven diterpen...Methanol extract of Stellera chamaejasme L wasassessed for antitumor activity by an antitumor activebioassay against murine leukemia P388 in vivo. Thebioassay-directed separation of the extract furnishedseven diterpene compounds (stellerarin, stelleramacrin,gnidimacrin, pimelea factor P2, subtoxin, huratoxin,simplexin ) and two biflavanone compounds (neochemae-jasmin A and B). Among them, gnidimacrin, stellerarinand stelleramacrin (a novel compound) were found tohave high antitumor and cytotoxic activities against P388,L1210 and K562 in vivo and in vitro. The results suggestedthat the diterpene compounds were the potent anti-tumor principles of Stellera chamaejame L展开更多
Steller chamaejasme L. （S. chamaejasme for short） is one of the most noxious unpalatable weeds in China, which has been frequently reported its negative interaction （i.e. competition and allelopathy） with other he...Steller chamaejasme L. （S. chamaejasme for short） is one of the most noxious unpalatable weeds in China, which has been frequently reported its negative interaction （i.e. competition and allelopathy） with other herbaceous species in grasslands. This study compared species diversity, biomass and sexual reproduction of herbaceous plants in meadows with S. chamaejasme and in open meadows without S. ehamaejasme in overgrazing meadows on the Tibetan Plateau in China to determine whether positive facilitation exist between S. chamaejasme and other herbaceous species under livestock＇s overgrazing. The results showed that there are more herbaceous species in meadows with S. chamaejasme than those in open meadows （35s and30s, respectively）. Diversity index and above-ground biomass were also significantly higher in meadows with S. charnaejasme. There were 39% （11/28） of all species with sexual reproduction found in meadows with S. charnaejasme, which was 7 times more than those in open meadows. Our study showed that S. charnaejasme could provide biotic refuge for neighboring plants and preserve plant diversity from livestock＇s overgrazing in alpine meadows on the Tibetan Plateau. It also suggested that inter-specific facilitation between S. charnaejasme and other herbaceous species may play a key role in overgrazing alpine meadows.展开更多
Gnidimacrin, a diterpene compound, isolated from the methanol extract of Stellera, chamaejasme L., showed significant antitumor activities against mouse leukemia P-388 and L-1210 in vivo, such as Lewis lung carcinoma,...Gnidimacrin, a diterpene compound, isolated from the methanol extract of Stellera, chamaejasme L., showed significant antitumor activities against mouse leukemia P-388 and L-1210 in vivo, such as Lewis lung carcinoma, B-16 melanoma and Colon cancer 26. It showed ILSs of 40%.49% and 41% at the dosages of 0.01-0.02 mg/kg ip,respectively. Gnidimacrin strongly inhibited cell Proliferation of human cancer cell lines such as leukemia K562, stomach cancers Kato-III, MKN-28, MKN-45, and mouse leukemia L-1210 by the MTT assay and colony forming assay in vitro. The IC50 of gnidimacrin was 0.007-0.00012 μg/ml. It is concluded that gnidimacrin is the principal antitumor element in Stellera chemaejasme L. with strong antitumor activities.展开更多
The mountains of Southwest China comprise a significant large mountain range and biodiversity hotspot imperiled by global climate change.The high species diversity in this mountain system has long been attributed to a...The mountains of Southwest China comprise a significant large mountain range and biodiversity hotspot imperiled by global climate change.The high species diversity in this mountain system has long been attributed to a complex set of factors,and recent large-scale macroevolutionary investigations have placed a broad timeline on plant diversification that stretches from 10 million years ago(Mya)to the present.Despite our increasing understanding of the temporal mode of speciation,finer-scale populationlevel investigations are lacking to better refine these temporal trends and illuminate the abiotic and biotic influences of cryptic speciation.This is largely due to the dearth of organismal sampling among closely related species and populations,spanning the incredible size and topological heterogeneity of this region.Our study dives into these evolutionary dynamics of speciation using genomic and ecomorphological data of Stellera chamaejasme L.We identified four previously unrecognized cryptic species having indistinct morphological traits and large metapopulation of evolving lineages,suggesting a more recent diversification(~2.67-0.90 Mya),largely influenced by Pleistocene glaciation and biotic factors.These factors likely influenced allopatric speciation and advocated cyclical warming–cooling episodes along elevational gradients during the Pleistocene.The study refines the evolutionary timeline to be much younger than previously implicated and raises the concern that projected future warming may influence the alpine species diversity,necessitating increased conservation efforts.展开更多
The present study investigated the chemical constituents of the roots of Stellera chamaejasme(Thymelaeaceae).One new biflavone glucoside(1),along with other thirteen known compounds(2–14),was isolated by repeated col...The present study investigated the chemical constituents of the roots of Stellera chamaejasme(Thymelaeaceae).One new biflavone glucoside(1),along with other thirteen known compounds(2–14),was isolated by repeated column chromatographic methods and their structures were elucidated on the basis of spectral analyses.The cytotoxic activities of selected compounds were evaluated against four human cancer cell lines(A549,BEL-7402,HCT-116,and MDA-MB-231) by the SRB assay method.Compound 9 showed remarkable cytotoxicity against BEL-7402 with IC50 value being 0.65 μg·mL-1; compounds 7,8,and 12 exhibited significant cytotoxic activity against A549 with IC50 values being 2.38,1.57,and 2.35 μg·m L-1,respectively.展开更多
Three series of novel 1,5-diphenyl-l-pentanone derivatives were designed and synthesized. Their structures were characterized by IR, IH NMR techniques, and elemental analysis. The insecticidal activities of the new co...Three series of novel 1,5-diphenyl-l-pentanone derivatives were designed and synthesized. Their structures were characterized by IR, IH NMR techniques, and elemental analysis. The insecticidal activities of the new compounds were preliminarily evaluated. The bioassay results indicated that the compounds Xll--X30 displayed better aphicidal activity against Aphis gossypii than compounds X1--X10 and the lead compound （E）-l,5-diphenyl-1- penten-1-one （A）. The inhibitory rates of compounds X6 and X29 were 100% against Plutella xylostella （L.） at 600 mgoL 1. Compounds X12, X13, X19, X24, X25, X26 and X27 showed higher insecticidal activity against Tetranychus cinnabarinus （Boisduval） at 600 mgoL 1 than the lead compound （A）. Keywords Stellera chamaejasme L, （E）-l,5-diphenyl-l-penten-l-one, analogue, synthesis, design, insecticidal activity展开更多
The activation effect of boric acid as an activator is good,and we investigate the best activation conditions for the boric acid impregnation method.To represent the structural characteristics and adsorption performan...The activation effect of boric acid as an activator is good,and we investigate the best activation conditions for the boric acid impregnation method.To represent the structural characteristics and adsorption performance of the Stellera Chamaejasme based carbon molecular sieves,we use Brunner-Emmet-Teller(BET)measurements,scan-ning electron microscope(SEM),Raman spectra(Raman),X-ray diffraction(XRD),and adsorption property measurement.When the loading ratio was 0.68:1,the specific surface area was 532.21 m^(2)/g,the total pore volume was 0.24 cm 3/g,the average pore size was 1.81 nm,the adsorption value of methylene blue was 145.28 mg/g,and the adsorption value of iodine was 713.33 mg/g,the results showed that boric acid had better activation effect.The carbon molecular sieves made from Stellera Chamaejasme and activated with boric acid produce two peaks on the aperture distribution graph that are densely distributed in the micropore range.This indicates that boric acid’s pore-forming tendency is primarily micropore.展开更多
Objective: The aim of this study was to investigate the effect on Akt and PTEN expression and the mechanism of proliferation and apoptosis of melanoma B16 cells treated with chamaejasme extract. Methods: The expressio...Objective: The aim of this study was to investigate the effect on Akt and PTEN expression and the mechanism of proliferation and apoptosis of melanoma B16 cells treated with chamaejasme extract. Methods: The expressions of Akt and PTEN of B16 cells treated with different concentrations of chamaejasme extract were detected with immunohistochemical method, cell apoptosis index(AI) was calculated with in situ labeling method. Results: Akt expressions of B16 cells treated with different concentrations of chamaejasme extract were significantly lower than the control group, while the PTEN expressions significantly up-regulated, and the effects appeared to be dose-related(P < 0.05). The Akt/AI of B16 cells treated with different concentrations of chamaejasme extract was significantly lower than the control group, all the parameters had extremely difference(F = 24.58, P < 0.05). Conclusion: Chamaejasme extract can inhibit proliferation and induce apoptosis of malignant melanoma B16 cells by down-regulating the expression of Akt and up-regulating the expression of PTEN.展开更多
A series of novel daphneolone analogs was designed and synthesized on the basis of natural product 1,5-diphenyl-2-penten-1-one（I） from Stellera chamaejasme L. as lead compound, whereby 2,6-dimethylmorpholine moiety ...A series of novel daphneolone analogs was designed and synthesized on the basis of natural product 1,5-diphenyl-2-penten-1-one（I） from Stellera chamaejasme L. as lead compound, whereby 2,6-dimethylmorpholine moiety was introduced to replace 1-phenyl group. Their structures were confirmed by IR,1H NMR, and HRMS（ESI） or elemental analysis,13 C NMR for some representative compounds. The two isomers of target compounds were separated and identified by NOESY technique and chemical method.All of the synthesized compounds have been evaluated for anti-plant pathogenic fungi activities. The results showed that some compounds exhibited moderate to good antifungal activities against tested fungi at the concentration of 50 mg/L. Among them, compound 7d, with a 4-bromine-substituted phenyl group and cis-2,6-dimethylmorpholine moiety, displayed best activity with an EC50 of 23.87 mmol/L against Valsa mali, superior to lead compound I. In addition, preliminary structure–activity relationship analysis indicated that, between two isomers of target compounds, the antifungal activities of the isomer with cis-2,6-dimethylmorpholine were better than the trans-isomer.展开更多
文摘A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots of Stellera chamaejasme L. together with known chamaechromone. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.
基金supported by the National Natural Science Foundation of China(Nos.81302651,81230090,and 81222046)the Fundamental Research Funds for the Central Universities(No.222201314041)+3 种基金the Global Research Network for Medicinal Plants(GRNMP)King Saud University,the Shanghai Leading Academic Discipline Project(No.B906)the Key Laboratory of Drug Research for Special Environments,PLA,the Shanghai Engineering Research Center for the Preparation of Bioactive Natural Products(No.10DZ2251300)the Scientific Foundation of Shanghai China(Nos.12401900801,09DZ1975700,09DZ1971500,and 10DZ1971700)
文摘The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L.(Thymelaeaceae) that is used in traditional Chinese medicine(TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isochamaejasmin was found to show similar bioactivity against Bcl-2 family proteins to the reference Bcl-2 ligand(–)-gossypol through 3D similarity search. It selectively bound to Bcl-xL and Mcl-1 with Ki values being 1.93 ± 0.13 μmol·L-1 and 9.98 ± 0.21 μmol·L-1, respectively. In addition, isochamaejasmin showed slight growth inhibitory activity against HL-60 with IC50 value being 50.40 ± 1.21 μmol·L-1 and moderate growth inhibitory activity against K562 cells with IC50 value being 24.51 ± 1.62 μmol·L-1. Furthermore, isochamaejasmin induced apoptosis of K562 cells by increasing the intracellular expression levels of proteins of the cleavage of caspase-9, caspase-3, and PARP which involved in the Bcl-2-induced apoptosis pathway. These results indicated that isochamaejasmin induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. chamaejasme L..
文摘A new biflavonoid, stelleranol, was isolated from the roots of Stellera chamaejasme L.. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.
基金Supported by China Postdoctoral Foundation, No.20090450550Optional research project sponsored by China Academy of Chinese Medical Science,No.Z02065
文摘OBJECTIVE:To investigate the inhibitory and pro-apoptotic effect of Stellera Chamaejasme L extract(ESC) in vitro.METHODS:ESC was first extracted with ethanol,and then washed using a polyamide column with 60% ethanol.ESC was then decompressively recycled and vacuum dried at room temperature to obtain active fractions.Subsequently,the cytotoxic and apoptotic effects of ESC on NCI-H157 human lung cancer cells were determined.RESULTS:The results showed that ESC was rich in isomers of Chamaejasminor,neochamaejasmine and Sikokianin.ESC had significant cytotoxicity against NCI-H157 cells,with an IC 50 of approximately 18.50 μg.mL-1.ESC caused significant increase in total apoptotic rate,the activity of caspase 3 and 8,and Fas protein expression(P<0.05).CONCLUSION:The inhibitory effect of ESC on NCI-H157 tumor cells might partly be attributed to its apoptotic induction through activation of the Fas death receptor pathway.
文摘Methanol extract of Stellera chamaejasme L wasassessed for antitumor activity by an antitumor activebioassay against murine leukemia P388 in vivo. Thebioassay-directed separation of the extract furnishedseven diterpene compounds (stellerarin, stelleramacrin,gnidimacrin, pimelea factor P2, subtoxin, huratoxin,simplexin ) and two biflavanone compounds (neochemae-jasmin A and B). Among them, gnidimacrin, stellerarinand stelleramacrin (a novel compound) were found tohave high antitumor and cytotoxic activities against P388,L1210 and K562 in vivo and in vitro. The results suggestedthat the diterpene compounds were the potent anti-tumor principles of Stellera chamaejame L
基金funded by the National Natural Science Foundation of China (Grant Nos. 31100360, 31200378, 31000233)
文摘Steller chamaejasme L. （S. chamaejasme for short） is one of the most noxious unpalatable weeds in China, which has been frequently reported its negative interaction （i.e. competition and allelopathy） with other herbaceous species in grasslands. This study compared species diversity, biomass and sexual reproduction of herbaceous plants in meadows with S. chamaejasme and in open meadows without S. ehamaejasme in overgrazing meadows on the Tibetan Plateau in China to determine whether positive facilitation exist between S. chamaejasme and other herbaceous species under livestock＇s overgrazing. The results showed that there are more herbaceous species in meadows with S. chamaejasme than those in open meadows （35s and30s, respectively）. Diversity index and above-ground biomass were also significantly higher in meadows with S. charnaejasme. There were 39% （11/28） of all species with sexual reproduction found in meadows with S. charnaejasme, which was 7 times more than those in open meadows. Our study showed that S. charnaejasme could provide biotic refuge for neighboring plants and preserve plant diversity from livestock＇s overgrazing in alpine meadows on the Tibetan Plateau. It also suggested that inter-specific facilitation between S. charnaejasme and other herbaceous species may play a key role in overgrazing alpine meadows.
文摘Gnidimacrin, a diterpene compound, isolated from the methanol extract of Stellera, chamaejasme L., showed significant antitumor activities against mouse leukemia P-388 and L-1210 in vivo, such as Lewis lung carcinoma, B-16 melanoma and Colon cancer 26. It showed ILSs of 40%.49% and 41% at the dosages of 0.01-0.02 mg/kg ip,respectively. Gnidimacrin strongly inhibited cell Proliferation of human cancer cell lines such as leukemia K562, stomach cancers Kato-III, MKN-28, MKN-45, and mouse leukemia L-1210 by the MTT assay and colony forming assay in vitro. The IC50 of gnidimacrin was 0.007-0.00012 μg/ml. It is concluded that gnidimacrin is the principal antitumor element in Stellera chemaejasme L. with strong antitumor activities.
基金funded by the Second Tibetan Plateau Scientific Expedition and Research(STEP)program(2019QZKK0502)the Key Projects of the Joint Fund of the National Natural Science Foundation of China(U23A20149)+4 种基金the Research Fund for International Young Scientists of the National Natural Science Foundation of China(32150410356)National Natural Science Foundation of China(32322006)the Young Academic and Technical Leader Raising Foundation of Yunnan Province(2019HB039)the International Association for Plant Taxonomy(IAPT)Research grant(421064806)supported by the“CAS President's International Fellowship Initiative”(PIFI)postdoctoral fel owship(2021PB0034)。
文摘The mountains of Southwest China comprise a significant large mountain range and biodiversity hotspot imperiled by global climate change.The high species diversity in this mountain system has long been attributed to a complex set of factors,and recent large-scale macroevolutionary investigations have placed a broad timeline on plant diversification that stretches from 10 million years ago(Mya)to the present.Despite our increasing understanding of the temporal mode of speciation,finer-scale populationlevel investigations are lacking to better refine these temporal trends and illuminate the abiotic and biotic influences of cryptic speciation.This is largely due to the dearth of organismal sampling among closely related species and populations,spanning the incredible size and topological heterogeneity of this region.Our study dives into these evolutionary dynamics of speciation using genomic and ecomorphological data of Stellera chamaejasme L.We identified four previously unrecognized cryptic species having indistinct morphological traits and large metapopulation of evolving lineages,suggesting a more recent diversification(~2.67-0.90 Mya),largely influenced by Pleistocene glaciation and biotic factors.These factors likely influenced allopatric speciation and advocated cyclical warming–cooling episodes along elevational gradients during the Pleistocene.The study refines the evolutionary timeline to be much younger than previously implicated and raises the concern that projected future warming may influence the alpine species diversity,necessitating increased conservation efforts.
基金supported by the National Natural Science Foundation of China(Nos.81001369 and 31170327)the Fundamental Research Funds for the Central Universities(No.2000219078)of China
文摘The present study investigated the chemical constituents of the roots of Stellera chamaejasme(Thymelaeaceae).One new biflavone glucoside(1),along with other thirteen known compounds(2–14),was isolated by repeated column chromatographic methods and their structures were elucidated on the basis of spectral analyses.The cytotoxic activities of selected compounds were evaluated against four human cancer cell lines(A549,BEL-7402,HCT-116,and MDA-MB-231) by the SRB assay method.Compound 9 showed remarkable cytotoxicity against BEL-7402 with IC50 value being 0.65 μg·mL-1; compounds 7,8,and 12 exhibited significant cytotoxic activity against A549 with IC50 values being 2.38,1.57,and 2.35 μg·m L-1,respectively.
文摘Three series of novel 1,5-diphenyl-l-pentanone derivatives were designed and synthesized. Their structures were characterized by IR, IH NMR techniques, and elemental analysis. The insecticidal activities of the new compounds were preliminarily evaluated. The bioassay results indicated that the compounds Xll--X30 displayed better aphicidal activity against Aphis gossypii than compounds X1--X10 and the lead compound （E）-l,5-diphenyl-1- penten-1-one （A）. The inhibitory rates of compounds X6 and X29 were 100% against Plutella xylostella （L.） at 600 mgoL 1. Compounds X12, X13, X19, X24, X25, X26 and X27 showed higher insecticidal activity against Tetranychus cinnabarinus （Boisduval） at 600 mgoL 1 than the lead compound （A）. Keywords Stellera chamaejasme L, （E）-l,5-diphenyl-l-penten-l-one, analogue, synthesis, design, insecticidal activity
基金Graduate Innovation Project of Qinghai University for Nationalities(2021XJXS12)Graduate Innovation Project of Qinghai University for Nationalities(12M2021018).
文摘The activation effect of boric acid as an activator is good,and we investigate the best activation conditions for the boric acid impregnation method.To represent the structural characteristics and adsorption performance of the Stellera Chamaejasme based carbon molecular sieves,we use Brunner-Emmet-Teller(BET)measurements,scan-ning electron microscope(SEM),Raman spectra(Raman),X-ray diffraction(XRD),and adsorption property measurement.When the loading ratio was 0.68:1,the specific surface area was 532.21 m^(2)/g,the total pore volume was 0.24 cm 3/g,the average pore size was 1.81 nm,the adsorption value of methylene blue was 145.28 mg/g,and the adsorption value of iodine was 713.33 mg/g,the results showed that boric acid had better activation effect.The carbon molecular sieves made from Stellera Chamaejasme and activated with boric acid produce two peaks on the aperture distribution graph that are densely distributed in the micropore range.This indicates that boric acid’s pore-forming tendency is primarily micropore.
基金Supported by grants from the Shandong Province Natural Science Fund Project(No.ZR2013HL004)Binzhou Medical College Students of Science and Technology Innovation Fund Project(No.BY2013DKCX003)
文摘Objective: The aim of this study was to investigate the effect on Akt and PTEN expression and the mechanism of proliferation and apoptosis of melanoma B16 cells treated with chamaejasme extract. Methods: The expressions of Akt and PTEN of B16 cells treated with different concentrations of chamaejasme extract were detected with immunohistochemical method, cell apoptosis index(AI) was calculated with in situ labeling method. Results: Akt expressions of B16 cells treated with different concentrations of chamaejasme extract were significantly lower than the control group, while the PTEN expressions significantly up-regulated, and the effects appeared to be dose-related(P < 0.05). The Akt/AI of B16 cells treated with different concentrations of chamaejasme extract was significantly lower than the control group, all the parameters had extremely difference(F = 24.58, P < 0.05). Conclusion: Chamaejasme extract can inhibit proliferation and induce apoptosis of malignant melanoma B16 cells by down-regulating the expression of Akt and up-regulating the expression of PTEN.
基金supported by the National Natural Science Foundation of China (No. 21272266)the National High Technology Research and Development Program of China (No. 2011AA10A202)
文摘A series of novel daphneolone analogs was designed and synthesized on the basis of natural product 1,5-diphenyl-2-penten-1-one（I） from Stellera chamaejasme L. as lead compound, whereby 2,6-dimethylmorpholine moiety was introduced to replace 1-phenyl group. Their structures were confirmed by IR,1H NMR, and HRMS（ESI） or elemental analysis,13 C NMR for some representative compounds. The two isomers of target compounds were separated and identified by NOESY technique and chemical method.All of the synthesized compounds have been evaluated for anti-plant pathogenic fungi activities. The results showed that some compounds exhibited moderate to good antifungal activities against tested fungi at the concentration of 50 mg/L. Among them, compound 7d, with a 4-bromine-substituted phenyl group and cis-2,6-dimethylmorpholine moiety, displayed best activity with an EC50 of 23.87 mmol/L against Valsa mali, superior to lead compound I. In addition, preliminary structure–activity relationship analysis indicated that, between two isomers of target compounds, the antifungal activities of the isomer with cis-2,6-dimethylmorpholine were better than the trans-isomer.
