Functional zones in cities constitute the most conspicuous components of newly developed urban areas, and have been a hot spot for domestic and foreign investors in China, which not only show the expanse of urban spac...Functional zones in cities constitute the most conspicuous components of newly developed urban areas, and have been a hot spot for domestic and foreign investors in China, which not only show the expanse of urban space accompanied by the shifts both in landscape (from rural to urban) and land use(from less extensive to extensive), but also display the transformation of regional ecological functions. By using the theories and methods of landscape ecology, the structure of landscapes and landscape ecological planning can be analyzed and evaluated for studying the urban functional zones' layout. In 1990, the Central Government of China declared to develop and open up Pudong New Area so as to promote economic development in Shanghai. Benefited from the advantages of Shanghai's location and economy, the government of Pudong New Area has successively built up 7 different functional zones over the past decade according to their functions and strategic goals. Based on the multi-spectral satellite imageries taken in 1990, 1997 and 2000, a landscape ecology analysis was carried out for Pudong New Area of Shanghai, supported by GIS technology. Green space (including croplands) and built-up areas are the major factors considered in developing urban landscape. This paper was mainly concerned with the different spatial patterns and dynamics of green space, built-up areas and new buildings in different functional zones, as influenced by different functional layouts and development strategies. The rapid urbanization in Pudong New Area resulted in a more homogeneous landscape. Agricultural landscape and suburban landscape were gradually replaced by urban landscape as the degree of urbanization increased. As a consequence of urbanization in Pudong, not only built-up patches, but also newly-built patches and green patches merged into one large patch, which should be attributed to the construction policy of extensive green space as the urban development process in Pudong New Area. The shape of green area of 7 functional zones became more and more regular because of the horticultural needs in Shanghai urban planning. Some suggestions were finally made for the study of future urban planning and layout.展开更多
Our previous study showed that up-regulating hippocampal peroxisome proliferator-activated receptorδ(PPARδ)displays an antidepressive effect and enhanc-es hippocampal neurogenesis in the context of chronic stress.He...Our previous study showed that up-regulating hippocampal peroxisome proliferator-activated receptorδ(PPARδ)displays an antidepressive effect and enhanc-es hippocampal neurogenesis in the context of chronic stress.Here,the changes in depressive behaviors and hippocampal neurogenesis were investigated after PPARδknockdown by microinfusion of the lentiviral vector,expressing short hairpin RNA(sh RNA)complementary to the coding exon of PPARδ,into the bilateral dentate gyri of the hippocampus or PPARδblockade by repeated systemic administration of PPARδantagonist,GSK0660(1 or 3mg·kg-1,ip,for 21 d).We found that hippocampal PPARδknockdown or blockade induced depressive-like behaviors and increased vulnerability to stress,which is involved in decreased hippocampal neurogenesis and neuronal differentiation.Down-regulating hippocampal PPARδalso induced significant decreases in phosphorylation c AMP response element-binding protein(CREB)and BDNF level in the hippocampus.The in vitro study that PPARδknockdown or blockade inhibited proliferation and differentiation of neural stem cells.Taken together,our results suggest that PPARδcould be a novel and promising target for developing new PPARδagonists for the treatment of depressive disorders.展开更多
The present study aimed at identifying potential lead compounds for diabetes mellitus drug discovery. We developed a novel method involving centrifugal ultrafiltration separation subsequent liquid chromatography with ...The present study aimed at identifying potential lead compounds for diabetes mellitus drug discovery. We developed a novel method involving centrifugal ultrafiltration separation subsequent liquid chromatography with quadrupole time of flight tandem mass spectrometry(LC-Q/TOF-MS/MS) determination to screen α-glucosidase inhibitors in complex Scutellaria baicalensis Georgi(SBG) extract. By adding a second filter to the screening process, the level of non-specific binding of Compounds 1, 3, 10 and 11 was significantly decreased, and the level of non-specific binding of Compounds 5 and 15 also was reduced. As a result, five flavonoids identified as baicalein, baicalein, wogonin, chrysin, and oroxylin A, were rapidly found to interact with α-glucosidase and possess potent anti-α-glucosidase activity in vitro. Specific binding of ligands to α-glucosidase was demonstrated though the proposed method and the ligands could be ranked in order of affinity for α-glucosidase, which were corresponded to the order of inhibitory activity in vitro. In conclusion, our results indicated that the developed method is a rapid and effective screening method for rat intestinal α-glucosidase inhibitors from complex herbal medicines such as SBG.展开更多
AIM: To study the chemical constituents of the roots and stem bark of Kadsura coccinea. METHOD: Compounds were isolated by column chromatography on silica gel and Sephadex LH-20, and finally purified by prep-HPLC. The...AIM: To study the chemical constituents of the roots and stem bark of Kadsura coccinea. METHOD: Compounds were isolated by column chromatography on silica gel and Sephadex LH-20, and finally purified by prep-HPLC. Their structures were elucidated by extensive spectroscopic methods, including 1D- and 2D-NMR, and HR-ESI-MS. RESULTS: Two compounds were determined as(7′S,8′S,8R)-(8β,8′α)- dimethyl-4,4′-dihydroxy-5,3′-dimethoxy-5′-cyclolignan glucoside(1) and micrandiactone H(2), respectively. CONCLUSION: Compunds 1 and 2 are new and neither showed inhibitory effects on nitric oxide(NO) production in lipopolysaccharide-induced RAW264.7 macrophages.展开更多
Polyphyllin I(PPI)purified from Polyphylla rhizomes displays puissant cytotoxicity in many kinds of cancers.Several researches investigated its anti-cancer activity.But novel mechanisms are still worth investigation.T...Polyphyllin I(PPI)purified from Polyphylla rhizomes displays puissant cytotoxicity in many kinds of cancers.Several researches investigated its anti-cancer activity.But novel mechanisms are still worth investigation.This study aimed to explore PPI-induced endoplasmic reticulum(ER)stress as well as the underlying mechanism in non-small cell lung cancer(NSCLC).Cell viability or colony-forming was detected by MTT or crystal violet respectively.Cell cycle,apoptosis,reactive oxygen species(ROS)and mitochondrial membrane potential were assessed by flow cytometry.Gene and protein levels were evaluated by q RT-PCR and immunoblotting respectively.Protein interaction was determined by immunoprecipitation or immunofluorescence assay.Gene overexpression or silencing was carried out by transient transfection with plasmids or small interfering RNAs.The Cancer Genome Atlas(TCGA)database was used for Gene Set Enrichment Analysis(GSEA),survival analysis,gene expression statistics or pathway enrichment assay.PPI inhibited the propagation of NSCLC cells,increased non-viable apoptotic cells,arrested cell cycle at G2/M phase,induced ROS levels but failed to decrease mitochondrial membrane potential.High levels of GRP78 indicates poor prognosis in NSCLC patients.PPI selectively suppressed unfolded protein response(UPR)-induced GRP78 expression,subsequently protected CHOP from GRP78-mediated ubiquitination and degradation.We demonstrated that the natural product PPI,obtained from traditional herbal medicine,deserves for further study as a valuable candidate for lead compound in the chemotherapy of NSCLC.展开更多
Multidrug resistance(MDR) is one of the major obstacles in cancer chemotherapy. Our previous study has shown that icariin could reverse MDR in MG-63 doxorubicin-resistant(MG-63/DOX) cells. It is reported that icariin ...Multidrug resistance(MDR) is one of the major obstacles in cancer chemotherapy. Our previous study has shown that icariin could reverse MDR in MG-63 doxorubicin-resistant(MG-63/DOX) cells. It is reported that icariin is usually metabolized to icariside II and icaritin. Herein, we investigated the effects of icariin, icariside Ⅱ, and icaritin(ICT) on reversing MDR in MG-63/DOX cells. Among these compounds, ICT exhibited strongest effect and showed no obvious cytotoxicity effect on both MG-63 and MG-63/DOX cells ranging from 1 to 10 μmol·L^(-1). Furthermore, ICT increased accumulation of rhodamine 123 and 6-carboxyfluorescein diacetate and enhanced DOX-induced apoptosis in MG-63/DOX cells in a dose-dependent manner. Further studies demonstrated that ICT decreased the m RNA and protein levels of multidrug resistance protein 1(MDR1) and multidrug resistance-associated protein 1(MRP1). We also verified that blockade of STAT3 phosphorylation was involved in the reversal effect of multidrug resistance in MG-63/DOX cells. Taken together, these results indicated that ICT may be a potential candidate in chemotherapy for osteosarcoma.展开更多
Two new phenolic glycosides, 7S, 8R-urolignoside-9′-O-β-D-glucoside(1) and scrophenoside G(2), were isolated and identified from the seeds of Ginkgo biloba L., a famous traditional medicine and functional food aroun...Two new phenolic glycosides, 7S, 8R-urolignoside-9′-O-β-D-glucoside(1) and scrophenoside G(2), were isolated and identified from the seeds of Ginkgo biloba L., a famous traditional medicine and functional food around the world. Their structures were elucidated by spectroscopic methods(1D and 2D NMR, HR-ESI-MS, and CD), and the comparisons of spectroscopic data with the reported values in the literature.展开更多
Two new type B polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2)and a known biogenetic precursor hyperbeanol Q(3)were isolated from the root extract of Hypericum beanii,a medicinal plant widespread in sout...Two new type B polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2)and a known biogenetic precursor hyperbeanol Q(3)were isolated from the root extract of Hypericum beanii,a medicinal plant widespread in southwest China.Their chemical structures were elucidated by 1 D/2 D NMR and HRESIMS data analysis,and absolute configurations were determined through detailed electric circular dichroism(ECD)analysis including ECD exciton chirality,Mo2(OAc)4-induced ECD,and ECD comparison.Of these compounds,hyperbeone A(1)is a typical[3.3.1]-type B PPAP with an unusual C-1 geranyl side chain,and hyperberin C(2)possesses a rare bicyclo[5.3.1]hendecane core.Taking compound 3 as a starting point,a plausible biosynthetic pathway to the bicyclic type B frameworks of 1 and 2 was proposed.展开更多
Two new phragmalin-type limonoids orthoesters, encandollens A and B(1 and 2), were isolated from the stem barks of Entandrophragma candollei collected in Ghana. The structures of these compounds were elucidated on the...Two new phragmalin-type limonoids orthoesters, encandollens A and B(1 and 2), were isolated from the stem barks of Entandrophragma candollei collected in Ghana. The structures of these compounds were elucidated on the basis of HR-ESI-MS, ~1 H and ^(13) C NMR, HSQC, HMBC, and ROESY data. Compound 1 was a rare C-15 enolic acyl phragmalin-type limonoid orthoester. Compounds 1 and 2 exhibited weak inhibitory effects on NO production in lipopolysaccharide(LPS)-induced RAW 264.7 cells.展开更多
AIM: To study the chemical constituents and bioactivity of the stem bark of Mitragyna diversifolia. METHOD: Compounds were isolated by various chromatographic methods. Their structures were elucidated on the basis of ...AIM: To study the chemical constituents and bioactivity of the stem bark of Mitragyna diversifolia. METHOD: Compounds were isolated by various chromatographic methods. Their structures were elucidated on the basis of spectroscopic techniques(IR, UV, MS, and NMR), and they were evaluated for their cytotoxic activities by the MTT method. RESULTS: Eight triterpenes were isolated and identified as 3α, 6β, 19α-trihydroxy-urs-12-en-28-oic acid(1), 3β, 6β, 19α- trihydroxy-urs-12-en-28-oic acid(2), 3-oxo-6β-19α-dihydroxy-urs-12-en-28-oic acid(3), 3β, 6β, 19α-trihydroxy-urs-12-en-24, 28-dioic acid 24-methyl ester(4), 3β, 6β, 19α, 24-tetrahydroxy-urs-12-en-28-oic acid(5), rotundic acid(6), 23-nor-24-exomethylene- 3β, 6β, 19α-trihydroxy-urs-12-en-28-oic acid(7), and pololic acid(8), respectively. All of the isolates were tested against two human tumor cell lines, MCF-7(breast) and HT-29(colon). CONCLUSION: Compound 1 was a new triterpene. Compounds 5-7 exhibited potent inhibitory effects on the growth of MCF-7 and HT-29 cells, and the others showed no cytotoxicity.展开更多
AIM: To investigate the chemical constituents from the whole plants of Phlegmariurus fargesii. METHOD: Compounds were isolated by repeated silica gel column chromatography. Their structures were elucidated by spectros...AIM: To investigate the chemical constituents from the whole plants of Phlegmariurus fargesii. METHOD: Compounds were isolated by repeated silica gel column chromatography. Their structures were elucidated by spectroscopic methods and chemical correlation. The acetylcholinesterase(AChE) inhibitory activity of the isolated compounds was evaluated. RESULTS: A new Lycopodium alkaloid, lycopodine N-oxide(1), along with lycopodine(2), 8,15-dehydrolycopodine(3), 6α-hydroxylycopodine(4), deacetyllycoclavine(5), N-methylhuperzine B(6), lycodine(7), and phlegmarine(8), was isolated. CONCLUSION: Compound 1 is a new Lycopodium alkaloid, and compound 3 was obtained from nature for the first time. Other alkaloids are isolated from this plant for the first time.展开更多
Wuzi-Yanzong-Wan(WZYZW)is a classic prescription for male infertility.Our previous investigation has demon-strated that it can inhibit sperm apoplosis via afecting mitochondria,but the underlying mechanisms are unclea...Wuzi-Yanzong-Wan(WZYZW)is a classic prescription for male infertility.Our previous investigation has demon-strated that it can inhibit sperm apoplosis via afecting mitochondria,but the underlying mechanisms are unclear.The purpose of the present study was to explore the actions of WZYZW on mitochondrial permeability transition pore(mPTP)in mouse spermatocyte cell line(GC-2 cells)opened by atractyloside(ATR).At first,WZYZW-mediated serum was prepared from rats following oral adminis-tration of WZYZW for 7 days.GC-2 cells were divided into control group,model group,positive group,as well as 5%,10%,15%WZYZW-medicated serum group.Cyclosporine A(CsA)was used as a positive control.50 μmol·L^(-1) ATR was added afer drugs in-cubation.Cell viability was asessed using CCK-8.Apoptosis was detected using flow cytometry and TUNEL method.The opening of mPTP and mitochondrial membrane potential(MMP)were dected by Calcein AM and JC-1 fuorescent probe respectively.The mRNA and protein levels of voltage-dependent anion channel I(VDACI),cyelophilin D(CypD),adenine nucleide translocator(ANT),cytochrome C(Cyt C),caspase 3,9 were dected by RT-PCR(real time quantity PCR)and Western blotting respectively.The results demonstrated that mPTP of GC-2 cells was opened alpter 24 hours of ATR treatment,resulting in decreased MMP and increased apoptosis.Pre-protection with WZYZ-medicated serum and CsA inhibited the opening of mPTP of GC-2 cells induced by ATR associ ated with increased MMP and decreased apoptosis.Morcover,the results of RT-qPCR and WB suggested that WZYZW-medicated serum could significantly reduce the mRNA and protein levels of VDACI and CypD,Caspase-3,9 and CylC,as well as a increased ra-tio of BclBax.However,ANT was not significantly ffected.Therefore,these findings indicated that WZYZW inhibited mitochondri-al mediated apoptosis by atenuating the opening of mPTP in GC-2 cells.WZYZW-medicated serum inhibited the expressions of VDACI and CypD and increased the expression of Bcl-2,which afected the opening of mPTP and exerted protective and anti-apop-totic ffects on GC-2 cell induced by ATR.展开更多
Sarglanoids A-F,six new sesquiterpenoids belonging to eudesmane(1-5)and eremophilane(6)types,were isolated from the leaves of Sarcandra glabra,a famous traditional Chinese medicine(TCM).Their structures including abso...Sarglanoids A-F,six new sesquiterpenoids belonging to eudesmane(1-5)and eremophilane(6)types,were isolated from the leaves of Sarcandra glabra,a famous traditional Chinese medicine(TCM).Their structures including absolute configurations were elucidated through extensive spectroscopic analysis and electronic circular dichroism(ECD)calculations.Compounds 1-2 were rare N-containing eudesmane-type sesquiterpenoids.Compound 3 exhibited inhibitory activity against nitric oxide(NO)production in lipopolysaccharides(LPS)-induced RAW 264.7 cells with IC_(50) values at 20.00±1.30μmol·L^(-1).These findings provide scientific evidence for sesquiterpenoids as the material foundation of S.glabra.展开更多
Six new trichilin-type limonoids(1-6)with C-19/29 lactol or acetal bridge and a new ring intact limonoid(7)were isolated from the desiccative ripe fruits of Trichilia sinensis.Their structures were determined by exten...Six new trichilin-type limonoids(1-6)with C-19/29 lactol or acetal bridge and a new ring intact limonoid(7)were isolated from the desiccative ripe fruits of Trichilia sinensis.Their structures were determined by extensive spectroscopic methods including 1 H NMR,13 C NMR,HSQC,HMBC,ROESY experiments as well as HRESI-MS data.All isolated compounds were evaluated for toxicities against human pulmonary carcinoma A549 and Hela cell lines by sulforhodamine B(SRB)method.Compound 7 showed weak inhibitory activity in Hela cell line at 40μmol·L^-1.展开更多
文摘Functional zones in cities constitute the most conspicuous components of newly developed urban areas, and have been a hot spot for domestic and foreign investors in China, which not only show the expanse of urban space accompanied by the shifts both in landscape (from rural to urban) and land use(from less extensive to extensive), but also display the transformation of regional ecological functions. By using the theories and methods of landscape ecology, the structure of landscapes and landscape ecological planning can be analyzed and evaluated for studying the urban functional zones' layout. In 1990, the Central Government of China declared to develop and open up Pudong New Area so as to promote economic development in Shanghai. Benefited from the advantages of Shanghai's location and economy, the government of Pudong New Area has successively built up 7 different functional zones over the past decade according to their functions and strategic goals. Based on the multi-spectral satellite imageries taken in 1990, 1997 and 2000, a landscape ecology analysis was carried out for Pudong New Area of Shanghai, supported by GIS technology. Green space (including croplands) and built-up areas are the major factors considered in developing urban landscape. This paper was mainly concerned with the different spatial patterns and dynamics of green space, built-up areas and new buildings in different functional zones, as influenced by different functional layouts and development strategies. The rapid urbanization in Pudong New Area resulted in a more homogeneous landscape. Agricultural landscape and suburban landscape were gradually replaced by urban landscape as the degree of urbanization increased. As a consequence of urbanization in Pudong, not only built-up patches, but also newly-built patches and green patches merged into one large patch, which should be attributed to the construction policy of extensive green space as the urban development process in Pudong New Area. The shape of green area of 7 functional zones became more and more regular because of the horticultural needs in Shanghai urban planning. Some suggestions were finally made for the study of future urban planning and layout.
基金The project supported Natural Science Foundation of Jiangsu Province(SBK201320969)National Natural Science Foundation of China(81573413 and 81273497)
文摘Our previous study showed that up-regulating hippocampal peroxisome proliferator-activated receptorδ(PPARδ)displays an antidepressive effect and enhanc-es hippocampal neurogenesis in the context of chronic stress.Here,the changes in depressive behaviors and hippocampal neurogenesis were investigated after PPARδknockdown by microinfusion of the lentiviral vector,expressing short hairpin RNA(sh RNA)complementary to the coding exon of PPARδ,into the bilateral dentate gyri of the hippocampus or PPARδblockade by repeated systemic administration of PPARδantagonist,GSK0660(1 or 3mg·kg-1,ip,for 21 d).We found that hippocampal PPARδknockdown or blockade induced depressive-like behaviors and increased vulnerability to stress,which is involved in decreased hippocampal neurogenesis and neuronal differentiation.Down-regulating hippocampal PPARδalso induced significant decreases in phosphorylation c AMP response element-binding protein(CREB)and BDNF level in the hippocampus.The in vitro study that PPARδknockdown or blockade inhibited proliferation and differentiation of neural stem cells.Taken together,our results suggest that PPARδcould be a novel and promising target for developing new PPARδagonists for the treatment of depressive disorders.
基金supported by the National Key Scientific and Technological Special Projects(2012ZX09103-101-007)the Program for Changjiang Scholars and Innovative Research Team in University(PCSIRT-IRT1193)the Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)
文摘The present study aimed at identifying potential lead compounds for diabetes mellitus drug discovery. We developed a novel method involving centrifugal ultrafiltration separation subsequent liquid chromatography with quadrupole time of flight tandem mass spectrometry(LC-Q/TOF-MS/MS) determination to screen α-glucosidase inhibitors in complex Scutellaria baicalensis Georgi(SBG) extract. By adding a second filter to the screening process, the level of non-specific binding of Compounds 1, 3, 10 and 11 was significantly decreased, and the level of non-specific binding of Compounds 5 and 15 also was reduced. As a result, five flavonoids identified as baicalein, baicalein, wogonin, chrysin, and oroxylin A, were rapidly found to interact with α-glucosidase and possess potent anti-α-glucosidase activity in vitro. Specific binding of ligands to α-glucosidase was demonstrated though the proposed method and the ligands could be ranked in order of affinity for α-glucosidase, which were corresponded to the order of inhibitory activity in vitro. In conclusion, our results indicated that the developed method is a rapid and effective screening method for rat intestinal α-glucosidase inhibitors from complex herbal medicines such as SBG.
基金supported by the Program for New Century Excellent Talents in University(NCET-12-0977)the National New Drug Innovation Great Project of China(2011ZX09307-002-02)+1 种基金the Program for Changjiang Scholars and Innovative Research Team in a University(PCSIRT-IRT1193)the Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)
文摘AIM: To study the chemical constituents of the roots and stem bark of Kadsura coccinea. METHOD: Compounds were isolated by column chromatography on silica gel and Sephadex LH-20, and finally purified by prep-HPLC. Their structures were elucidated by extensive spectroscopic methods, including 1D- and 2D-NMR, and HR-ESI-MS. RESULTS: Two compounds were determined as(7′S,8′S,8R)-(8β,8′α)- dimethyl-4,4′-dihydroxy-5,3′-dimethoxy-5′-cyclolignan glucoside(1) and micrandiactone H(2), respectively. CONCLUSION: Compunds 1 and 2 are new and neither showed inhibitory effects on nitric oxide(NO) production in lipopolysaccharide-induced RAW264.7 macrophages.
基金the National Natural Science Foundation of China(Nos.81973524 and 81703754)the 111 Project from Ministry of Education of China and the State Administration of Foreign Export Affairs of China(B18056)+2 种基金the Drug Innovation Major Project(Nos.2018ZX09711-001-007and 2018ZX09735002-003)the“Double First-Class”University Project(CPU2018GF03)the special funds for Science and Technology Development under the Guidance of the Central Government(ZY20198020)。
文摘Polyphyllin I(PPI)purified from Polyphylla rhizomes displays puissant cytotoxicity in many kinds of cancers.Several researches investigated its anti-cancer activity.But novel mechanisms are still worth investigation.This study aimed to explore PPI-induced endoplasmic reticulum(ER)stress as well as the underlying mechanism in non-small cell lung cancer(NSCLC).Cell viability or colony-forming was detected by MTT or crystal violet respectively.Cell cycle,apoptosis,reactive oxygen species(ROS)and mitochondrial membrane potential were assessed by flow cytometry.Gene and protein levels were evaluated by q RT-PCR and immunoblotting respectively.Protein interaction was determined by immunoprecipitation or immunofluorescence assay.Gene overexpression or silencing was carried out by transient transfection with plasmids or small interfering RNAs.The Cancer Genome Atlas(TCGA)database was used for Gene Set Enrichment Analysis(GSEA),survival analysis,gene expression statistics or pathway enrichment assay.PPI inhibited the propagation of NSCLC cells,increased non-viable apoptotic cells,arrested cell cycle at G2/M phase,induced ROS levels but failed to decrease mitochondrial membrane potential.High levels of GRP78 indicates poor prognosis in NSCLC patients.PPI selectively suppressed unfolded protein response(UPR)-induced GRP78 expression,subsequently protected CHOP from GRP78-mediated ubiquitination and degradation.We demonstrated that the natural product PPI,obtained from traditional herbal medicine,deserves for further study as a valuable candidate for lead compound in the chemotherapy of NSCLC.
基金supported by the National Natural Science Foundation of China(Nos.81673554 and 81503211)Natural Science Foundation of Jiangsu Province(No.BK20160763)+1 种基金the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)the Program for Changjiang Scholars and Innovative Research Team in University(No.IRT_15R63)
文摘Multidrug resistance(MDR) is one of the major obstacles in cancer chemotherapy. Our previous study has shown that icariin could reverse MDR in MG-63 doxorubicin-resistant(MG-63/DOX) cells. It is reported that icariin is usually metabolized to icariside II and icaritin. Herein, we investigated the effects of icariin, icariside Ⅱ, and icaritin(ICT) on reversing MDR in MG-63/DOX cells. Among these compounds, ICT exhibited strongest effect and showed no obvious cytotoxicity effect on both MG-63 and MG-63/DOX cells ranging from 1 to 10 μmol·L^(-1). Furthermore, ICT increased accumulation of rhodamine 123 and 6-carboxyfluorescein diacetate and enhanced DOX-induced apoptosis in MG-63/DOX cells in a dose-dependent manner. Further studies demonstrated that ICT decreased the m RNA and protein levels of multidrug resistance protein 1(MDR1) and multidrug resistance-associated protein 1(MRP1). We also verified that blockade of STAT3 phosphorylation was involved in the reversal effect of multidrug resistance in MG-63/DOX cells. Taken together, these results indicated that ICT may be a potential candidate in chemotherapy for osteosarcoma.
基金supported by the National Natural Sciences Foundation of China(No.81430092)the Outstanding Youth Fund of the Basic Research Program of Jiangsu Province(No.BK20160077)+1 种基金the project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)the Program for Changjiang Scholars and Innovative Research Team in University(No.IRT_15R63)
文摘Two new phenolic glycosides, 7S, 8R-urolignoside-9′-O-β-D-glucoside(1) and scrophenoside G(2), were isolated and identified from the seeds of Ginkgo biloba L., a famous traditional medicine and functional food around the world. Their structures were elucidated by spectroscopic methods(1D and 2D NMR, HR-ESI-MS, and CD), and the comparisons of spectroscopic data with the reported values in the literature.
基金the National Natural Science Foundation of China(No.31900287)the Drug Innovation Major Project(2018ZX09711-001-007)the China Postdoctoral Science Foundation(2017M621889)。
文摘Two new type B polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2)and a known biogenetic precursor hyperbeanol Q(3)were isolated from the root extract of Hypericum beanii,a medicinal plant widespread in southwest China.Their chemical structures were elucidated by 1 D/2 D NMR and HRESIMS data analysis,and absolute configurations were determined through detailed electric circular dichroism(ECD)analysis including ECD exciton chirality,Mo2(OAc)4-induced ECD,and ECD comparison.Of these compounds,hyperbeone A(1)is a typical[3.3.1]-type B PPAP with an unusual C-1 geranyl side chain,and hyperberin C(2)possesses a rare bicyclo[5.3.1]hendecane core.Taking compound 3 as a starting point,a plausible biosynthetic pathway to the bicyclic type B frameworks of 1 and 2 was proposed.
基金supported by the National Natural Science Foundation of China(Nos.31470416 and 81430092)the Program for New Century Excellent Talents in University(No.NCET-2013-1035)+1 种基金the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)the Program for Changjiang Scholars and Innovative Research Team in University(IRT_15R63)
文摘Two new phragmalin-type limonoids orthoesters, encandollens A and B(1 and 2), were isolated from the stem barks of Entandrophragma candollei collected in Ghana. The structures of these compounds were elucidated on the basis of HR-ESI-MS, ~1 H and ^(13) C NMR, HSQC, HMBC, and ROESY data. Compound 1 was a rare C-15 enolic acyl phragmalin-type limonoid orthoester. Compounds 1 and 2 exhibited weak inhibitory effects on NO production in lipopolysaccharide(LPS)-induced RAW 264.7 cells.
基金supported by the National Science Foundation of China(No.21272275)the Program for Changjiang Scholars and Innovative Research Team in University(No.PCSIRT-IRT1193)
文摘AIM: To study the chemical constituents and bioactivity of the stem bark of Mitragyna diversifolia. METHOD: Compounds were isolated by various chromatographic methods. Their structures were elucidated on the basis of spectroscopic techniques(IR, UV, MS, and NMR), and they were evaluated for their cytotoxic activities by the MTT method. RESULTS: Eight triterpenes were isolated and identified as 3α, 6β, 19α-trihydroxy-urs-12-en-28-oic acid(1), 3β, 6β, 19α- trihydroxy-urs-12-en-28-oic acid(2), 3-oxo-6β-19α-dihydroxy-urs-12-en-28-oic acid(3), 3β, 6β, 19α-trihydroxy-urs-12-en-24, 28-dioic acid 24-methyl ester(4), 3β, 6β, 19α, 24-tetrahydroxy-urs-12-en-28-oic acid(5), rotundic acid(6), 23-nor-24-exomethylene- 3β, 6β, 19α-trihydroxy-urs-12-en-28-oic acid(7), and pololic acid(8), respectively. All of the isolates were tested against two human tumor cell lines, MCF-7(breast) and HT-29(colon). CONCLUSION: Compound 1 was a new triterpene. Compounds 5-7 exhibited potent inhibitory effects on the growth of MCF-7 and HT-29 cells, and the others showed no cytotoxicity.
基金supported by the National Natural Science Foundation of China(No.81073009)the Cultivation Fund of the Key Scientific and Technical Innovation Project,Ministry of Education of China(No.707033)+1 种基金the Scaling Project for Innovation Scholars,Natural Science Foundation of Jiangsu Province,China(BK2008039)a project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions
文摘AIM: To investigate the chemical constituents from the whole plants of Phlegmariurus fargesii. METHOD: Compounds were isolated by repeated silica gel column chromatography. Their structures were elucidated by spectroscopic methods and chemical correlation. The acetylcholinesterase(AChE) inhibitory activity of the isolated compounds was evaluated. RESULTS: A new Lycopodium alkaloid, lycopodine N-oxide(1), along with lycopodine(2), 8,15-dehydrolycopodine(3), 6α-hydroxylycopodine(4), deacetyllycoclavine(5), N-methylhuperzine B(6), lycodine(7), and phlegmarine(8), was isolated. CONCLUSION: Compound 1 is a new Lycopodium alkaloid, and compound 3 was obtained from nature for the first time. Other alkaloids are isolated from this plant for the first time.
基金This work was supported by the National Natural Science Foundation of China(No.81473674)and Natural Science Foundation of Anhui Provincial Department of Education(No.KJ2020A0386).
文摘Wuzi-Yanzong-Wan(WZYZW)is a classic prescription for male infertility.Our previous investigation has demon-strated that it can inhibit sperm apoplosis via afecting mitochondria,but the underlying mechanisms are unclear.The purpose of the present study was to explore the actions of WZYZW on mitochondrial permeability transition pore(mPTP)in mouse spermatocyte cell line(GC-2 cells)opened by atractyloside(ATR).At first,WZYZW-mediated serum was prepared from rats following oral adminis-tration of WZYZW for 7 days.GC-2 cells were divided into control group,model group,positive group,as well as 5%,10%,15%WZYZW-medicated serum group.Cyclosporine A(CsA)was used as a positive control.50 μmol·L^(-1) ATR was added afer drugs in-cubation.Cell viability was asessed using CCK-8.Apoptosis was detected using flow cytometry and TUNEL method.The opening of mPTP and mitochondrial membrane potential(MMP)were dected by Calcein AM and JC-1 fuorescent probe respectively.The mRNA and protein levels of voltage-dependent anion channel I(VDACI),cyelophilin D(CypD),adenine nucleide translocator(ANT),cytochrome C(Cyt C),caspase 3,9 were dected by RT-PCR(real time quantity PCR)and Western blotting respectively.The results demonstrated that mPTP of GC-2 cells was opened alpter 24 hours of ATR treatment,resulting in decreased MMP and increased apoptosis.Pre-protection with WZYZ-medicated serum and CsA inhibited the opening of mPTP of GC-2 cells induced by ATR associ ated with increased MMP and decreased apoptosis.Morcover,the results of RT-qPCR and WB suggested that WZYZW-medicated serum could significantly reduce the mRNA and protein levels of VDACI and CypD,Caspase-3,9 and CylC,as well as a increased ra-tio of BclBax.However,ANT was not significantly ffected.Therefore,these findings indicated that WZYZW inhibited mitochondri-al mediated apoptosis by atenuating the opening of mPTP in GC-2 cells.WZYZW-medicated serum inhibited the expressions of VDACI and CypD and increased the expression of Bcl-2,which afected the opening of mPTP and exerted protective and anti-apop-totic ffects on GC-2 cell induced by ATR.
基金supported in part by the National Natural Science Foundation of China(No.320703S9)the 111 Project from Ministry of Education of China and the State Administration of Foreign Export Affairs of China(No.B18056)the Drug Innovation Major Project(No.2018ZX09735002-003).
文摘Sarglanoids A-F,six new sesquiterpenoids belonging to eudesmane(1-5)and eremophilane(6)types,were isolated from the leaves of Sarcandra glabra,a famous traditional Chinese medicine(TCM).Their structures including absolute configurations were elucidated through extensive spectroscopic analysis and electronic circular dichroism(ECD)calculations.Compounds 1-2 were rare N-containing eudesmane-type sesquiterpenoids.Compound 3 exhibited inhibitory activity against nitric oxide(NO)production in lipopolysaccharides(LPS)-induced RAW 264.7 cells with IC_(50) values at 20.00±1.30μmol·L^(-1).These findings provide scientific evidence for sesquiterpenoids as the material foundation of S.glabra.
基金supported by the National Natural Science Foundation of China(No.31470416)the Outstanding Youth Fund of the Basic Research Program of Jiangsu Province(No.BK20160077)the Program for Changjiang Scholars and Innovative Research Team in University(No.IRT_15R63)
文摘Six new trichilin-type limonoids(1-6)with C-19/29 lactol or acetal bridge and a new ring intact limonoid(7)were isolated from the desiccative ripe fruits of Trichilia sinensis.Their structures were determined by extensive spectroscopic methods including 1 H NMR,13 C NMR,HSQC,HMBC,ROESY experiments as well as HRESI-MS data.All isolated compounds were evaluated for toxicities against human pulmonary carcinoma A549 and Hela cell lines by sulforhodamine B(SRB)method.Compound 7 showed weak inhibitory activity in Hela cell line at 40μmol·L^-1.