A new depsipeptide,Rakicidin B1(1),together with two known rakicidin A(2)and rakicidin B(3),were isolated from the fermentation broth of marine Micromonospora sp.FIM02-523.The structures of all the compounds were dete...A new depsipeptide,Rakicidin B1(1),together with two known rakicidin A(2)and rakicidin B(3),were isolated from the fermentation broth of marine Micromonospora sp.FIM02-523.The structures of all the compounds were determined by extensive spectroscopic method such as 1D and 2D NMR,IR,UV,and HR-ESI-MS.All the compounds were tested for the antitumor activities against HCT-8,MGC803,A549,A375,HepG2 and CASKI human tumor cell lines.Results indicated that compound 1,2 and 3 exhibited significant cytotoxicities to these tumor cell lines(To these 5 tumor cell lines,the IC_(50)values of compound 1 were 0.341,0.121,0.394,0.066 and 2.516μg/mL,respectively;the IC_(50)values of compound 2 were 0.731,0.991,0.226,0.040 and 0.576μg/mL,respectively;the IC_(50)values of compound 3 were 0.347,0.104,0.216,0.041 and 2.239μg/mL,respectively).Compound 1 and 3 showed similar antitumor activities.展开更多
Grifolin,a secondary metabolite isolated from the fresh fruiting bodies of mushroom Albatrellus confluens,inhibits the growth of some cancer cell lines in vitro by induction of apoptosis in the previous studies of our...Grifolin,a secondary metabolite isolated from the fresh fruiting bodies of mushroom Albatrellus confluens,inhibits the growth of some cancer cell lines in vitro by induction of apoptosis in the previous studies of our group.However,the mechanisms are not completely understood.An expression profiling analysis of apoptosis-related gene provided a clue that death-associated protein kinase 1(dapk 1)gene was upregulated at least twofold in response to grifolin treatment in nasopharyngeal carcinoma cell CNE1.Here,we further investigated the role of DAPK1 in apoptotic effect induced by grifolin in nasopharyngeal carcinoma cells.展开更多
Systematic experiments about the antitumor effects of low energy laser irradiation combined with the traditional antitumor medicine of cyclophosphamide were conducted using the experimental model of mouse S180 ascite...Systematic experiments about the antitumor effects of low energy laser irradiation combined with the traditional antitumor medicine of cyclophosphamide were conducted using the experimental model of mouse S180 ascites sarcoma.The three groups of tumor bearing mice were irradiated upon the inner corners with the dosages of 11 00,14 67 and 22 00 J·cm -2 LELI respectively,and injected with CYT intraperitoneally to observe the changes of the survival time,the ascites growth speed,and the kinetic changes of immune functions.The survival times of the three groups of CYT/LELI combination were obviously longer than those of the tumor and CYT control groups.Correspondingly,the amounts of ascites,tumor cells densities and total tumor cells in CYT/LELI groups decreased significantly,while the death ratio of the tumor cells increased.Comparatively,the group of 22 00 J·cm -2 LELI combined with CYT showed the most ideal antitumor effects,and the life prolongation ratio was up to 53 20%.展开更多
The residual metal impurities in cisplatin, carboplatin and oxaliplatin were determined by ICP-AES. The samples were ignited and dissolved with HCl:HNO 3 (3:1). The method is simple and accurate. By the determination ...The residual metal impurities in cisplatin, carboplatin and oxaliplatin were determined by ICP-AES. The samples were ignited and dissolved with HCl:HNO 3 (3:1). The method is simple and accurate. By the determination of the metal residues in the samples, the calculated actual daily exposure and concentration of the metal Pd, Ir, Rh, Ru, Mo, Ni, Cr, V, Cu, Mn, Fe and Zn that were less than the permitted daily exposures (PDE) and the limited concentration permitted in the EMEA guideline on the specification limits for residues of metal catalysts or metal reagents [1] . The metal residues can de adequately removed from the active pharmaceutical ingredients and the corresponding drugs. The trace metal residues will not affect human health and lead to the safety hazard by the intravenous injection.展开更多
Here we report results of our investigations of new class of bioactive palladium compounds (AH n ) m [PdCl 4 ], which were discovered as a result of systematic study of correlations between composition, structure and ...Here we report results of our investigations of new class of bioactive palladium compounds (AH n ) m [PdCl 4 ], which were discovered as a result of systematic study of correlations between composition, structure and bioactivity of different types of platinum metals coordination compounds. For the first time we demonstrated in vivoa possibility of development of palladium compounds, which exceed cisplatin in antitumor activity and do not show immunosuppressive effects, and palladium compounds with immunostimulating and radioprotective activities. Combinations of cytostatic agents or radiation with palladium complexes lead to significant synergism of their activities and high therapeutic efficiency exceeded an efficiency of their separated use.展开更多
OBJECTIVE Hedyotis diffusa Willd and Scutellaria barbata D Don are most commonly used herb pair for cancer treatment in traditional Chinese medicine.This study aimed to evaluated the in vitro and in vivo antitumor eff...OBJECTIVE Hedyotis diffusa Willd and Scutellaria barbata D Don are most commonly used herb pair for cancer treatment in traditional Chinese medicine.This study aimed to evaluated the in vitro and in vivo antitumor effects and the compatibility mechanisms of Hedyotis diffusa-Sculellaria barbata herb pair.METHODS Hedyotic diffusa extract,Scutellariae Barbatae extract,and herb pair extract were prepared and the component were detected by UPLC-Q-TOF-MS.The effects of different concentrations of Hedyotic diffusa extract,Scutellariae Barbatae extract,and herb pair extract were detected using MTS assay.The in vivo antitumor effects were evaluated in Panc28 pancreatic cells bearing nude mice model.The compatibility mechanism of Hedyotis diffusa-Sculellaria barbata herb pair were evaluated based on the network pharmacology,using TCMSP,Cytoscape 3.6.1 software,and DAVID 6.8.The anticancer mechanism were further validated in vitro.RESULTS Both the MTS and in vivo results showed that herb pair extract showed more obvious inhibitory effects on cancer cells compared to each individual.A total of 37 active components were selected from Hedyotis diffusa and Sculellaria barbata,33 kinds of active ingredients are involved in their anti-tumor effects.58 cancer-related targets and 66 KEGG pathways were identified.The potential targets for the herb pair might be prostaglandin G/H synthase 2(PTGS2),HSP90,EGFR,72 ku typeⅣcollagenase,PPAR-γ,et al.In vitro validation result showed that compatibility mech⁃anisms was related with HSP90,EGFR related pathways.CONCLUSION The result of the study preliminarily verified the basic anti-tumor pharmacological effects of Hedyotis diffusa-Sculellaria barbata herb pair,and lays a solid foundation for further studies on the anti-tumor mechanism of the herbal pair.展开更多
HSV-TK/GCV system and CD/5FC system aretwo effective systems of cancer suicide gene therapy.We have demonstrated that adenovirus-mediated CD/5FC system could suppress the growth of subcutaneoushuman hepatocellular car...HSV-TK/GCV system and CD/5FC system aretwo effective systems of cancer suicide gene therapy.We have demonstrated that adenovirus-mediated CD/5FC system could suppress the growth of subcutaneoushuman hepatocellular carcinoma to some degree. Tofurther investigate whether the suicide gene therapyaffects the immune system or the immune systemaffects the effectiveness of suicide gene therapy, acolon adenocarcinoma of BALB/c mice, CT26,展开更多
Effects of fibroblast-mediated IL-2 and IL-3 genetherapy on recovery of bone marrow depression in tumor-bearing mice treated with cyclophosphamide (300 mg/kg) and syngeneic BMT were investigated in the presentreport. ...Effects of fibroblast-mediated IL-2 and IL-3 genetherapy on recovery of bone marrow depression in tumor-bearing mice treated with cyclophosphamide (300 mg/kg) and syngeneic BMT were investigated in the presentreport. BALB/c mice were inoculated with J558Lplasmacytoma cells s. c. and 3 days later IL-2 secretingNIH3T3-IL-2, IL-3 secreting NIH3T3-IL-3 fibroblastcells were implanted into the tumor-bearing mice展开更多
It’s well known that interleukin-2 (IL-2) plays animportant role in eliciting antitumor immunityparticularly mediated by T cells. In addition, theexpression of MHC can be enhanced by IL-2 genetransfection in tumor ce...It’s well known that interleukin-2 (IL-2) plays animportant role in eliciting antitumor immunityparticularly mediated by T cells. In addition, theexpression of MHC can be enhanced by IL-2 genetransfection in tumor cells. Recent studies have indicatedthat at least two signals are required for the activation ofnaive T cells by antigen-bearing target cells: an antigen-sopific signal and a crystimulatory signal. B7-l is展开更多
Interleukin-15 (IL-15) is a novel cytokine thatstimulates the proliferation of T cells, B cells and NKcells. Several biological activities of interleukin-15overlap those of IL-2. Here, we report that lung cancercells....Interleukin-15 (IL-15) is a novel cytokine thatstimulates the proliferation of T cells, B cells and NKcells. Several biological activities of interleukin-15overlap those of IL-2. Here, we report that lung cancercells. which were modified by IL-15 cDNA, may serve astumor vaccine that plays an antitumor role in murinemodel. IL-15 cDNA was amplified by RT-PCR withmRNA templates that were extracted from展开更多
Antitumor effects of combined transfer of suicidegene and cytokine gene were investigated in this report.Adenovirus harboring E.coli. cytosine deaminase (CD)gene (Ad-CD) and murine interleukin 2 (IL-2) gene(Ad-IL-2) w...Antitumor effects of combined transfer of suicidegene and cytokine gene were investigated in this report.Adenovirus harboring E.coli. cytosine deaminase (CD)gene (Ad-CD) and murine interleukin 2 (IL-2) gene(Ad-IL-2) were used for gene transfer in vitro and invivo. C57BL/6 mice were inoculated subcutaneously withB16F10 melanoma cells and three days later treated withadenovirus injection at the site of tumor inoculation.Significant inhibition of tumor growth was achieved展开更多
A new europium(Ⅲ)complex containing(4-Methyl-2-oxo-2 H-chromen-7-yloxy)-acetic acid moiety(CMMC)was synthesized,characterized,and confirmed as antitumor agent and fluorescent probe.The spectroscopic measurements of ...A new europium(Ⅲ)complex containing(4-Methyl-2-oxo-2 H-chromen-7-yloxy)-acetic acid moiety(CMMC)was synthesized,characterized,and confirmed as antitumor agent and fluorescent probe.The spectroscopic measurements of Eu(Ⅲ)in the presence of CMMC were obtained in different solvents.The results show that the strongest Eu(Ⅲ)emission bands were monitored in iso-propyl alcohol while the weakest Eu(Ⅲ)emission band was observed in acetonitrile.The interaction of Eu(Ⅲ)-(CMMC)2 complex with DNA was monitored using absorption and emission techniques.From fluorescence titration measurements,the binding constants of DNA with Eu(Ⅲ)-(CMMC)_2 complex were found to be 1.04×10~5 L·mol^(-1) in Tris-HCl and 1.17×10~7 L·mol^(-1) in DMSO-Tris-HCl buffer(9∶1 V/V).Hypochromism was observed from the absorption titration experiment which indicates the intercalation of Eu(Ⅲ)-complex between the base pair of DNA.This result further confirmed by fluorescent Ethidium bromide displacement assay.The fluorescence calibration curve was used for the determination of DNA with LOD of 1.2 ng in DMSO-Tris-HCl buffer(9∶1 V/V)and 5 ng in Tris-HCl buffer.The preliminary antitumor investigation shows promising cytotoxicity against MDA-MB-231,MCF-7(mammary cancer),and PC-3(prostate carcinoma)cell lines with IC50 values of 40.63,25.42 and 30.25μmol·L^(-1),respectively.展开更多
The aim of this study was to determine the chemical composition of Synsepalum dulcificum leaf essential oil obtained by steam distillation.The in vitro antibacterial activity and antitumoral activity of this essential...The aim of this study was to determine the chemical composition of Synsepalum dulcificum leaf essential oil obtained by steam distillation.The in vitro antibacterial activity and antitumoral activity of this essential oil was characterized.Sixty-eight compositions were separated.Among them 44 components were identified and represented 92.14%of the total detected constituents.The major chemical compounds of leaf essential oil were spathulenol(24.194%),limonene(15.805%),diisooctyl phthalate(12.402%),dibutyl phthalate(10.326%),palmitic acid(4.865%)and linalool(2.139%).The result of the antimicrobial assay showed that the essential oil displayed varying degrees of antibacterial activity against all tested bacterial except for Pseudomonas aeruginosa,along with minimum inhibition concentration(MIC)values from 39.06 to 252.15 mg/L.In addition,the antitumoral activity using MTY assay of the leaf essential oil exhibited this oil was effective against human K562 cancer cell line in a dose dependent manner.Its inhibition concentration 50%(IC50)value was 13.5 mg/L.展开更多
Two complexes[Cd(L)(CH_(3)O)(CH_(3)COO)]·CH_(3)OH·(CH_(3))_(2)NH(C1)and[Mn(L)Cl_(2)(CH_(3)OH)](C2)were synthesized by reacting a new imidazole-bearing ligand 4-(1H-imidazol-1-yl)-N'-(pyridin-2-ylmethylen...Two complexes[Cd(L)(CH_(3)O)(CH_(3)COO)]·CH_(3)OH·(CH_(3))_(2)NH(C1)and[Mn(L)Cl_(2)(CH_(3)OH)](C2)were synthesized by reacting a new imidazole-bearing ligand 4-(1H-imidazol-1-yl)-N'-(pyridin-2-ylmethylene)benzohydrazide(L)with cadmium and manganese salts,respectively.The ligand was characterized by ^(1)H NMR and ^(13)C NMR spectroscopy,while the complexes were analyzed by single-crystal X-ray diffraction,powder X-ray diffraction,thermogravimetric analyses,and UV-Vis spectroscopy.Complex C1 features a 1D zigzag chain structure formed by alternating connections of one ligand and one metal ion.In contrast,complex C2 exhibits a mononuclear molecular structure,where each unit consists of one ligand connected to one manganese ion.Both complexes further form a 3D structure through π-π interactions and intermolecular hydrogen bonds.Cell proliferation assays conducted on four tumor cell lines and one normal cell line revealed that both C1 and C2 exhibited significantly stronger inhibition of tumor cell growth compared to the ligand L.Notably,C1 demonstrated superior anti-proliferative activity against A549 and A2780 cells relative to cisplatin,while showing comparable cytotoxicity toward SMMC-7721 cells.Further mechanistic studies indicated that C1 induces apoptosis in both SMMC-7721 and A549 tumor cells,suppresses the invasion and migration of SMMC-7721 cells,and arrests the cell cycle at the G0/G1 phase.展开更多
The hydrated tricyclohexyltin theophylline-7-acetic acid(tpH)complex[Sn(C_(6)H_(11))_(3)(tp)(H_(2)O)]was synthesized via an ethanol solvothermal method using tricyclohexyltin hydroxide and tpH in a 1∶1 molar ratio.Th...The hydrated tricyclohexyltin theophylline-7-acetic acid(tpH)complex[Sn(C_(6)H_(11))_(3)(tp)(H_(2)O)]was synthesized via an ethanol solvothermal method using tricyclohexyltin hydroxide and tpH in a 1∶1 molar ratio.The complex was characterized by IR,^(1)H(^(13)C)NMR,elemental analysis,and powder X-ray diffraction,and the crystal structure was determined by single-crystal X-ray diffraction.The crystal belongs to the orthorhombic system with space group Iba2,and the central tin atom is in a five-coordinated trigonal bipyramidal configuration.Quantum chemistry ab initio calculations were performed to investigate the stability,molecular orbital energy,and frontier molecular orbital characteristics of the complex.Additionally,its thermal stability,electrochemical properties,and in vitro anticancer activity were evaluated.CCDC:2380308.展开更多
文摘A new depsipeptide,Rakicidin B1(1),together with two known rakicidin A(2)and rakicidin B(3),were isolated from the fermentation broth of marine Micromonospora sp.FIM02-523.The structures of all the compounds were determined by extensive spectroscopic method such as 1D and 2D NMR,IR,UV,and HR-ESI-MS.All the compounds were tested for the antitumor activities against HCT-8,MGC803,A549,A375,HepG2 and CASKI human tumor cell lines.Results indicated that compound 1,2 and 3 exhibited significant cytotoxicities to these tumor cell lines(To these 5 tumor cell lines,the IC_(50)values of compound 1 were 0.341,0.121,0.394,0.066 and 2.516μg/mL,respectively;the IC_(50)values of compound 2 were 0.731,0.991,0.226,0.040 and 0.576μg/mL,respectively;the IC_(50)values of compound 3 were 0.347,0.104,0.216,0.041 and 2.239μg/mL,respectively).Compound 1 and 3 showed similar antitumor activities.
文摘Grifolin,a secondary metabolite isolated from the fresh fruiting bodies of mushroom Albatrellus confluens,inhibits the growth of some cancer cell lines in vitro by induction of apoptosis in the previous studies of our group.However,the mechanisms are not completely understood.An expression profiling analysis of apoptosis-related gene provided a clue that death-associated protein kinase 1(dapk 1)gene was upregulated at least twofold in response to grifolin treatment in nasopharyngeal carcinoma cell CNE1.Here,we further investigated the role of DAPK1 in apoptotic effect induced by grifolin in nasopharyngeal carcinoma cells.
文摘Systematic experiments about the antitumor effects of low energy laser irradiation combined with the traditional antitumor medicine of cyclophosphamide were conducted using the experimental model of mouse S180 ascites sarcoma.The three groups of tumor bearing mice were irradiated upon the inner corners with the dosages of 11 00,14 67 and 22 00 J·cm -2 LELI respectively,and injected with CYT intraperitoneally to observe the changes of the survival time,the ascites growth speed,and the kinetic changes of immune functions.The survival times of the three groups of CYT/LELI combination were obviously longer than those of the tumor and CYT control groups.Correspondingly,the amounts of ascites,tumor cells densities and total tumor cells in CYT/LELI groups decreased significantly,while the death ratio of the tumor cells increased.Comparatively,the group of 22 00 J·cm -2 LELI combined with CYT showed the most ideal antitumor effects,and the life prolongation ratio was up to 53 20%.
基金The national SME technology innovation fund(11C26215305898)Kunming SME technology innovation fund(CJ2011040)
文摘The residual metal impurities in cisplatin, carboplatin and oxaliplatin were determined by ICP-AES. The samples were ignited and dissolved with HCl:HNO 3 (3:1). The method is simple and accurate. By the determination of the metal residues in the samples, the calculated actual daily exposure and concentration of the metal Pd, Ir, Rh, Ru, Mo, Ni, Cr, V, Cu, Mn, Fe and Zn that were less than the permitted daily exposures (PDE) and the limited concentration permitted in the EMEA guideline on the specification limits for residues of metal catalysts or metal reagents [1] . The metal residues can de adequately removed from the active pharmaceutical ingredients and the corresponding drugs. The trace metal residues will not affect human health and lead to the safety hazard by the intravenous injection.
文摘Here we report results of our investigations of new class of bioactive palladium compounds (AH n ) m [PdCl 4 ], which were discovered as a result of systematic study of correlations between composition, structure and bioactivity of different types of platinum metals coordination compounds. For the first time we demonstrated in vivoa possibility of development of palladium compounds, which exceed cisplatin in antitumor activity and do not show immunosuppressive effects, and palladium compounds with immunostimulating and radioprotective activities. Combinations of cytostatic agents or radiation with palladium complexes lead to significant synergism of their activities and high therapeutic efficiency exceeded an efficiency of their separated use.
文摘OBJECTIVE Hedyotis diffusa Willd and Scutellaria barbata D Don are most commonly used herb pair for cancer treatment in traditional Chinese medicine.This study aimed to evaluated the in vitro and in vivo antitumor effects and the compatibility mechanisms of Hedyotis diffusa-Sculellaria barbata herb pair.METHODS Hedyotic diffusa extract,Scutellariae Barbatae extract,and herb pair extract were prepared and the component were detected by UPLC-Q-TOF-MS.The effects of different concentrations of Hedyotic diffusa extract,Scutellariae Barbatae extract,and herb pair extract were detected using MTS assay.The in vivo antitumor effects were evaluated in Panc28 pancreatic cells bearing nude mice model.The compatibility mechanism of Hedyotis diffusa-Sculellaria barbata herb pair were evaluated based on the network pharmacology,using TCMSP,Cytoscape 3.6.1 software,and DAVID 6.8.The anticancer mechanism were further validated in vitro.RESULTS Both the MTS and in vivo results showed that herb pair extract showed more obvious inhibitory effects on cancer cells compared to each individual.A total of 37 active components were selected from Hedyotis diffusa and Sculellaria barbata,33 kinds of active ingredients are involved in their anti-tumor effects.58 cancer-related targets and 66 KEGG pathways were identified.The potential targets for the herb pair might be prostaglandin G/H synthase 2(PTGS2),HSP90,EGFR,72 ku typeⅣcollagenase,PPAR-γ,et al.In vitro validation result showed that compatibility mech⁃anisms was related with HSP90,EGFR related pathways.CONCLUSION The result of the study preliminarily verified the basic anti-tumor pharmacological effects of Hedyotis diffusa-Sculellaria barbata herb pair,and lays a solid foundation for further studies on the anti-tumor mechanism of the herbal pair.
文摘HSV-TK/GCV system and CD/5FC system aretwo effective systems of cancer suicide gene therapy.We have demonstrated that adenovirus-mediated CD/5FC system could suppress the growth of subcutaneoushuman hepatocellular carcinoma to some degree. Tofurther investigate whether the suicide gene therapyaffects the immune system or the immune systemaffects the effectiveness of suicide gene therapy, acolon adenocarcinoma of BALB/c mice, CT26,
文摘Effects of fibroblast-mediated IL-2 and IL-3 genetherapy on recovery of bone marrow depression in tumor-bearing mice treated with cyclophosphamide (300 mg/kg) and syngeneic BMT were investigated in the presentreport. BALB/c mice were inoculated with J558Lplasmacytoma cells s. c. and 3 days later IL-2 secretingNIH3T3-IL-2, IL-3 secreting NIH3T3-IL-3 fibroblastcells were implanted into the tumor-bearing mice
文摘It’s well known that interleukin-2 (IL-2) plays animportant role in eliciting antitumor immunityparticularly mediated by T cells. In addition, theexpression of MHC can be enhanced by IL-2 genetransfection in tumor cells. Recent studies have indicatedthat at least two signals are required for the activation ofnaive T cells by antigen-bearing target cells: an antigen-sopific signal and a crystimulatory signal. B7-l is
基金Sponsored by 863 Program for Young Scientists in China to Professor Wei He and National foundation of Natural Science to Professor Denian Ba
文摘Interleukin-15 (IL-15) is a novel cytokine thatstimulates the proliferation of T cells, B cells and NKcells. Several biological activities of interleukin-15overlap those of IL-2. Here, we report that lung cancercells. which were modified by IL-15 cDNA, may serve astumor vaccine that plays an antitumor role in murinemodel. IL-15 cDNA was amplified by RT-PCR withmRNA templates that were extracted from
文摘Antitumor effects of combined transfer of suicidegene and cytokine gene were investigated in this report.Adenovirus harboring E.coli. cytosine deaminase (CD)gene (Ad-CD) and murine interleukin 2 (IL-2) gene(Ad-IL-2) were used for gene transfer in vitro and invivo. C57BL/6 mice were inoculated subcutaneously withB16F10 melanoma cells and three days later treated withadenovirus injection at the site of tumor inoculation.Significant inhibition of tumor growth was achieved
基金supported by grants 4590/1434 by Deanship of Scientific Resea rch at Taibah University in Saudi Arabia for financial assistance
文摘A new europium(Ⅲ)complex containing(4-Methyl-2-oxo-2 H-chromen-7-yloxy)-acetic acid moiety(CMMC)was synthesized,characterized,and confirmed as antitumor agent and fluorescent probe.The spectroscopic measurements of Eu(Ⅲ)in the presence of CMMC were obtained in different solvents.The results show that the strongest Eu(Ⅲ)emission bands were monitored in iso-propyl alcohol while the weakest Eu(Ⅲ)emission band was observed in acetonitrile.The interaction of Eu(Ⅲ)-(CMMC)2 complex with DNA was monitored using absorption and emission techniques.From fluorescence titration measurements,the binding constants of DNA with Eu(Ⅲ)-(CMMC)_2 complex were found to be 1.04×10~5 L·mol^(-1) in Tris-HCl and 1.17×10~7 L·mol^(-1) in DMSO-Tris-HCl buffer(9∶1 V/V).Hypochromism was observed from the absorption titration experiment which indicates the intercalation of Eu(Ⅲ)-complex between the base pair of DNA.This result further confirmed by fluorescent Ethidium bromide displacement assay.The fluorescence calibration curve was used for the determination of DNA with LOD of 1.2 ng in DMSO-Tris-HCl buffer(9∶1 V/V)and 5 ng in Tris-HCl buffer.The preliminary antitumor investigation shows promising cytotoxicity against MDA-MB-231,MCF-7(mammary cancer),and PC-3(prostate carcinoma)cell lines with IC50 values of 40.63,25.42 and 30.25μmol·L^(-1),respectively.
文摘The aim of this study was to determine the chemical composition of Synsepalum dulcificum leaf essential oil obtained by steam distillation.The in vitro antibacterial activity and antitumoral activity of this essential oil was characterized.Sixty-eight compositions were separated.Among them 44 components were identified and represented 92.14%of the total detected constituents.The major chemical compounds of leaf essential oil were spathulenol(24.194%),limonene(15.805%),diisooctyl phthalate(12.402%),dibutyl phthalate(10.326%),palmitic acid(4.865%)and linalool(2.139%).The result of the antimicrobial assay showed that the essential oil displayed varying degrees of antibacterial activity against all tested bacterial except for Pseudomonas aeruginosa,along with minimum inhibition concentration(MIC)values from 39.06 to 252.15 mg/L.In addition,the antitumoral activity using MTY assay of the leaf essential oil exhibited this oil was effective against human K562 cancer cell line in a dose dependent manner.Its inhibition concentration 50%(IC50)value was 13.5 mg/L.
文摘Two complexes[Cd(L)(CH_(3)O)(CH_(3)COO)]·CH_(3)OH·(CH_(3))_(2)NH(C1)and[Mn(L)Cl_(2)(CH_(3)OH)](C2)were synthesized by reacting a new imidazole-bearing ligand 4-(1H-imidazol-1-yl)-N'-(pyridin-2-ylmethylene)benzohydrazide(L)with cadmium and manganese salts,respectively.The ligand was characterized by ^(1)H NMR and ^(13)C NMR spectroscopy,while the complexes were analyzed by single-crystal X-ray diffraction,powder X-ray diffraction,thermogravimetric analyses,and UV-Vis spectroscopy.Complex C1 features a 1D zigzag chain structure formed by alternating connections of one ligand and one metal ion.In contrast,complex C2 exhibits a mononuclear molecular structure,where each unit consists of one ligand connected to one manganese ion.Both complexes further form a 3D structure through π-π interactions and intermolecular hydrogen bonds.Cell proliferation assays conducted on four tumor cell lines and one normal cell line revealed that both C1 and C2 exhibited significantly stronger inhibition of tumor cell growth compared to the ligand L.Notably,C1 demonstrated superior anti-proliferative activity against A549 and A2780 cells relative to cisplatin,while showing comparable cytotoxicity toward SMMC-7721 cells.Further mechanistic studies indicated that C1 induces apoptosis in both SMMC-7721 and A549 tumor cells,suppresses the invasion and migration of SMMC-7721 cells,and arrests the cell cycle at the G0/G1 phase.
文摘The hydrated tricyclohexyltin theophylline-7-acetic acid(tpH)complex[Sn(C_(6)H_(11))_(3)(tp)(H_(2)O)]was synthesized via an ethanol solvothermal method using tricyclohexyltin hydroxide and tpH in a 1∶1 molar ratio.The complex was characterized by IR,^(1)H(^(13)C)NMR,elemental analysis,and powder X-ray diffraction,and the crystal structure was determined by single-crystal X-ray diffraction.The crystal belongs to the orthorhombic system with space group Iba2,and the central tin atom is in a five-coordinated trigonal bipyramidal configuration.Quantum chemistry ab initio calculations were performed to investigate the stability,molecular orbital energy,and frontier molecular orbital characteristics of the complex.Additionally,its thermal stability,electrochemical properties,and in vitro anticancer activity were evaluated.CCDC:2380308.
