RESUMO
The apoptosis of mono-hepatocellular induced by the active ingredients of the Zanthoxyli Radix was investigated using laser Raman spectroscopy. Hepatoma cells (BEL-7404) were treated with 10 mgâ¢L⻹ nitidine chloride and 3 gâ¢L⻹ the extracts of Zanthoxyli Radix, respectively, then were divided into two parts, one for fluorescence staining, the other for determination of Raman spectroscopy. The acquired spectra were then processed by background elimination, smoothing, and normalization. Fluorescence staining results showed that the nucleuses from untreated group were uniformly stained, while those from the group treated for 48 hours were densely stained and broken. The spectra results revealed that the intensity of peaks associated with nucleic acid and protein decreased after the cells were incubated with the extracts of Zanthoxyli Radix for 12, 24, 36 and 48 hours. The intensity of peaks at 785,1 002,1 175,1 660 cm⻹ was decreased with the time of the cells were incubated by the extracts of Zanthoxyli Radix. The results indicated that the extracts of Zanthoxyli Radix could induce the apoptosis of hepatoma cells and reduce the amount of nucleic acid and protein in the cells. There is a certain relevance between the drug treatment time and the efficacy. The above results suggest that Raman spectra can provide abundant information about the changes in biological macromolecules within the cells after incubated by the extracts of Zanthoxyli Radix and serve as an effective method for the real time measurement of apoptosis.
Assuntos
Apoptose , Carcinoma Hepatocelular/patologia , Medicamentos de Ervas Chinesas/farmacologia , Neoplasias Hepáticas/patologia , Zanthoxylum/química , Linhagem Celular Tumoral , Humanos , Raízes de Plantas/química , Análise Espectral RamanRESUMO
Chemical examination of the fermentation broth of a sponge-associated fungus Trichoderma harzinum HMS-15-3 led to the isolation of four pairs of new C13 lipid enantiomers namely harzianumols A-H (1a-4b). Their structures were elucidated on the basis of extensive spectroscopic (IR, MS, 1D, and 2D NMR) data analysis, including the modified Mosher's method for the assignment of their absolute configurations. The new compounds were evaluated for antihyperlipidemic effects in HepG2 cells.
Assuntos
Lipídeos/isolamento & purificação , Trichoderma/química , Animais , Lipídeos/química , Lipídeos/farmacologia , Biologia Marinha , Testes de Sensibilidade Microbiana , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Poríferos/microbiologiaRESUMO
A high performance liquid chromatography coupled with diode array and evaporative light scattering detection (HPLC-DAD-ELSD) method for simultaneous determination of eight major bioactive compounds including two flavonoids (rutin and eriodictyol-7-O-ß-D-glucopyranoside), two isochlorogenic acids (isochlorogenic acid A and isochlorogenic acid C) and four triterpenoids (ilexhainanoside D, ilexsaponin A1, ilexgenin A and ursolic acid) in Ilex hainanensis has been developed for the first time. The 283 nm wavelength was chosen for determination of two flavonoids and two isochlorogenic acids. ELSD was applied to determine four triterpenoids. The analysis was performed on an Agilent Zorbax SB-C18 column (250 × 4.6 mm i.d., 5 µm) with gradient elution of 0.2% formic acid in water and acetonitrile. The method was validated for linearity, limit of detection, limit of quantification, precision, repeatability and accuracy. The proposed method has been successfully applied for simultaneous quantification of the analytes in four samples of Ilex hainanensis, which is helpful for quality control of this plant.
Assuntos
Ácido Clorogênico/análogos & derivados , Flavonoides/química , Ilex/química , Triterpenos/química , Ácido Clorogênico/análise , Ácido Clorogênico/química , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Lasers Semicondutores , Luz , Extratos Vegetais/análise , Extratos Vegetais/química , Reprodutibilidade dos Testes , Espalhamento de Radiação , Sensibilidade e Especificidade , Triterpenos/análiseRESUMO
OBJECTIVE: To analyze the essential oil from the rhizome of Curcuma aromatica of different growth periods, and to provide the scientific reference for reasonable cultivation and quality control of this plant. METHODS: The essential oil was extracted by hydrodistillation and analyzed with GC-MS. The relative contents were determined with area normalization method. RESULTS: The main volatile constituents in the rhizome of Curcuma aromatica were basically the same. Among these volatile constituents, curdione was the major. The relative content of curdione was 16.35% in the rhizome of wild plant in Hengxian county, and 15.81% in the rhizome of one-year-old plant in Mingyang farm, Nanning city. The relative content of eucalyptol in the 2-year-old cultivated rhizome in Hengxian county was 15.40%, and 14.59% in the rhizome of wild plant in Hengxian county. beta-Elemene, beta-caryophyllene,eugenol and germacrone were also the main constituents in the rhizome essential oil. CONCLUSION: Volatile constituents in the rhizome of Curcuma aromatica are similar to each other,but the relative content of each component is different. This result can provide the scientific foundation for the cultivation of Curcuma aromatica.
Assuntos
Curcuma/química , Óleos Voláteis/análise , Óleos de Plantas/análise , Rizoma/química , Sesquiterpenos de Germacrano/análise , Curcuma/crescimento & desenvolvimento , Cicloexanóis/análise , Eucaliptol , Cromatografia Gasosa-Espectrometria de Massas , Monoterpenos/análise , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Óleos de Plantas/química , Óleos de Plantas/isolamento & purificação , Controle de Qualidade , Rizoma/crescimento & desenvolvimento , Sesquiterpenos/análise , Fatores de TempoRESUMO
OBJECTIVE: To investigate the chemical constituents from Ilex hainanensis. METHODS: The compounds were isolated and purified by various chromatographic techniques. The structures were identified by mass and NMR spectral data. RESULTS: Ten compounds were isolated and identified as Ilexgenin A (1), 3beta, 19alpha-dihydroxyolean-12-ene-24,28-Dioicacid-28-O-beta-D-glucopyranoside (2), Ilexsaponin A1 (3), 2-(Caffeoyloxy) methyl-3-hydroxy-1-butane-4-O-beta-D-glucopyranoside (4), Dibutyl phthalate (5), Rutin (6), Eriodictyol-7-O-beta-D-glucopyranoside (7), Syringaresinol-4-O-beta-D-glucopyranoside (8), (2E) -2-methyl-2-butene-1, 4-diol-4-O-beta-D-(6"-O- caffeoyl) -glucopyranoside (9), 1-O-caffeoyl-(2E) -2-methyl-2-butene-1, 4-diol-4-O-beta-D- glucopyranoside (10), respectively. CONCLUSION: Compound 4, 7 - 10 are obtained from this plant for the first time.
Assuntos
Flavonoides/isolamento & purificação , Glucosídeos/isolamento & purificação , Ilex/química , Lignanas/isolamento & purificação , Folhas de Planta/química , Flavonoides/química , Glucosídeos/química , Lignanas/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Saponinas/química , Saponinas/isolamento & purificaçãoRESUMO
OBJECTIVE: To observe the effect of Jinhuang Fuzheng powder on cytokines of immunosuppressive mice by using protein antibody micro-array. METHOD: The immunosuppressive mice model was established by subcutaneously injecting cyclophosphamide. Rats were orally administered with low, middle and high dose of Huangjin Fuzheng powder for 10 days, and fasted for 12 hours after the final administration. 1 mL blood was drawn from caudal veins and isolated hearts of rats of each group. A quantitative test was conducted for cytokines with cytokine antibody array. RESULT: Compared with the control group, IFN-gamma and RANTES of the CTX group decreased significantly (P<0.05). After the administration, IFN-gamma of low, middle and high-dose groups, and RANTES of the high-dose group increased significantly (P<0.05). Compared with the control group, IL-5, IL-6, IL-9, IL-13 and MCP-1 of the CTX group increased remarkably (P<0.01, P<0.05). After the administration, IL-5, IL-6, IL-9, IL-13 and MCP-1 of low, middle and high-dose groups decreased to varying degrees. GM-CSF, IL-1alpha, IL-1beta, IL-2, IL-3, IL-4, IL-10, IL-12, IL-17, M-CSF, TNF-alpha, KC and VEGF of the 13 types of cytokines showed no significant change. CONCLUSION: Jinhuang Fuzheng powder shows effect on 20 types of cytokines of immunosuppressive mice to varying degrees, which may be related to the regulatory immunosuppression of Th1/Th2 subgroup in mice.
Assuntos
Anticorpos/imunologia , Citocinas/imunologia , Medicamentos de Ervas Chinesas/administração & dosagem , Hospedeiro Imunocomprometido/efeitos dos fármacos , Imunossupressores/administração & dosagem , Inflamação/tratamento farmacológico , Animais , Citocinas/genética , Feminino , Humanos , Hospedeiro Imunocomprometido/genética , Hospedeiro Imunocomprometido/imunologia , Inflamação/genética , Inflamação/imunologia , Masculino , Camundongos , Análise Serial de ProteínasRESUMO
In the present work, the authors explored a rapid method of the Zanthoxylum nitidum geographical origins determination. Based on Fourier transform infrared spectroscopy (FTIR) technology, the band of 1 800-400 cm(-1) which is the IR fingerprint of Zanthoxylum nitidum, the Fisher ratio and the soft independent modeling of class analogies (SIMCA) were used to build a classification model. Respectively, four kinds of Zanthoxylum nitidum in the Guangxi region were detected by the model, and the model was verified by calculating their recognition rate and rejection rate. The results show that the authors can accurately extract the overall information of Chinese herbal medicines by using the FTIR, also established a pattern recognition model to predict unknown samples, and obtained satisfactory recognition rate and rejection rate, indicating that the model has stronger ability of identification. The detection on real time was carried out rapidly with the Fisher model, suggesting that the model has more practical value.
Assuntos
Espectroscopia de Infravermelho com Transformada de Fourier , Zanthoxylum/classificação , China , Medicamentos de Ervas Chinesas/análise , Geografia , Modelos TeóricosRESUMO
OBJECTIVE: To study the hypoglycemic effect and mechanism of the extracts of cactus pear fruit polysaccharide (CPFP) in diabetic rats induced by streptozotocin (STZ). METHODS: The diabetic rats were induced by STZ in SD rats, and randomly divided into model group, insulin group,cactus pear juice group, high dose CPFP group,low dose CPFP group. The experimental rats were administrated for 8 weeks. During the experiment, the contents of blood glucose and blood limit of the rats were detected and body weight were recorded. The pathology of beta cell and alpha cell in pancreas of experimental rats were observed by immunohistochemistry. RESULTS: Compared with model group, the contents of blood glucose, total cholesterol and triglyceride were remarkably decreased in high and low dose CPFP groups. At the same time the body weight was significantly increased in high dose and low dose CPFP groups. The results of immunohistochemical stain demonstrated that the number of islet beta cells was increased and that of islet alpha cells was unchanged in the treatment groups. CONCLUSION: CPFP can markedly decrease blood glucose and blood limit in STZ-induced diabetic rats. Its mechanism may be related to stimulating the secretion of insulin from beta cells.
Assuntos
Glicemia/efeitos dos fármacos , Cactaceae/química , Diabetes Mellitus Experimental/patologia , Frutas/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Animais , Peso Corporal/efeitos dos fármacos , Colesterol/sangue , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/tratamento farmacológico , Relação Dose-Resposta a Droga , Feminino , Hipoglicemiantes/administração & dosagem , Insulina/biossíntese , Células Secretoras de Insulina/efeitos dos fármacos , Masculino , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Polissacarídeos/administração & dosagem , Polissacarídeos/uso terapêutico , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Estreptozocina , Triglicerídeos/sangueRESUMO
OBJECTIVE: To provide the scientific basis for the reasonable development and use of the leaves of Rhizoma Curcumae. METHODS: To extract the volatile oil from roots and leaves of three species Rhizoma Curcumae by steam distillation and isolate these products with the method of gas chromatography-mass spectrum. Taking Nist98 standard mass spectrometer database and contrast as control, the structure of the mass spectrogram was identified, and the relative contents of the components were determined with area normalization method. RESULTS: The anti-tumor active constituents such as curdione and germacrone in the leaves had the greater content than in its rhizome. CONCLUSION: The varieties of volatile components in different parts of three species of Rhizoma Curcumae are similar, but their contents are obviously various. We can make the leaves of Rhizoma Curcumae for recycling use.
Assuntos
Curcuma/química , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Plantas Medicinais/química , Sesquiterpenos/análise , Curcuma/classificação , Cromatografia Gasosa-Espectrometria de Massas , Folhas de Planta/química , Rizoma/química , Sesquiterpenos de Germacrano/análiseRESUMO
OBJECTIVE: To observe the protective effect of Jinhuang-1 (JH-1) on oleic acid-induced acute respiratory distress syndrome (ARDS) in rats and provide a basis to clinical application. METHOD: Oleic acid was injected into the tail vein of rats and JH-1 were administered to rats. After four days, their blood were collected for the blood gas analysis. The superoxide dismutase (SOD), the malondialdehyde (MDA), nitic oxide (NO) content and the positive expression ratio of tumor necrosis factor-alpha (TNF-alpha) were determined. The pathological changes of microstructure of lung were observed. RESULT: The results demonstrated that JH-1 could significantly increase PO2, reduce PCO2 of oleic acid-induced ARDS rats, increase the superoxide dismutase, decrease the malondialdehyde, nitic oxide content and the positive expression ratio of TNF-alpha, and improve the histological destruction on lung. CONCLUSION: JH-1 plays a protective role for ARDS rats induced by oleic acid. The mechanism is probably related to attenuating lipid peroxidation and decreasing NO content and the expression of TNF-alpha in lung.
Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Pneumopatias/prevenção & controle , Pulmão/efeitos dos fármacos , Substâncias Protetoras/farmacologia , Fator de Necrose Tumoral alfa/metabolismo , Doença Aguda , Animais , Astragalus propinquus/química , Gasometria , Combinação de Medicamentos , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/uso terapêutico , Feminino , Lonicera/química , Pulmão/metabolismo , Pulmão/patologia , Pneumopatias/sangue , Pneumopatias/induzido quimicamente , Masculino , Malondialdeído/metabolismo , Óxido Nítrico/metabolismo , Ácido Oleico , Fitoterapia , Plantas Medicinais/química , Substâncias Protetoras/uso terapêutico , Distribuição Aleatória , Ratos , Ratos Wistar , Superóxido Dismutase/metabolismo , Síndrome , Ziziphus/químicaRESUMO
This article summarized the progresses of pharmacokinetic about traditional Chinese medicine (TCM) in recent 10 years. Reports indicated that the studies of pharmacokinetic about TCM were in the stage of exploratory. Many factors restricted the progresses of pharmacokinetic such as complexity of medicine components, multi-target of drug effect and imperfect of evaluation methods. With the developing of modern analytical techniques and indication of TCM theories, we believe that the pharmacokinetic study will be constantly updated and improved.
Assuntos
Medicamentos de Ervas Chinesas/farmacocinética , Medicina Tradicional Chinesa , Plantas Medicinais/química , Animais , Área Sob a Curva , Combinação de Medicamentos , Medicamentos de Ervas Chinesas/isolamento & purificação , Distribuição TecidualRESUMO
Nitidine chloride (NC), a bioactive alkaloid isolated from Zanthoxylum nitidum, has been used as a herbal ingredient in toothpaste that prevents cavities for decades. It also displays potential antitumor and anti-inflammation properties. However, its anticatabolic effect on bone is not known. We investigated the effect of NC on osteoclastogenesis, bone resorption and RANKL-induced NF-κB and NFATc1 signalling. In mouse-derived bone marrow monocytes (BMMs), NC suppressed RANKL-induced multinucleated tartrate-resistant acid phosphatase (TRAP)-positive osteoclast formation and bone resorption in a dose dependent manner. NC attenuated the expression of osteoclast marker genes including cathepsin K, D2, calcitonin receptor, NFATc1, and TRAP. Further, NC inhibited RANKL-activated NF-κB and NFATc1 signalling pathways. In vivo study revealed that NC abrogated oestrogen deficiency-induced bone loss in ovariectomized mice. Histological analysis showed that the number of osteoclasts was significantly lower in NC-treated groups. Collectively, our data demonstrate that NC suppressed osteoclastogenesis and prevented OVX-induced bone loss by inhibiting RANKL-induced NF-κB and NFATc1 signalling pathways. NC may be a natural and novel treatment for osteoclast-related bone lytic diseases.
Assuntos
Benzofenantridinas/farmacologia , Reabsorção Óssea/prevenção & controle , Diferenciação Celular/efeitos dos fármacos , Fatores de Transcrição NFATC/metabolismo , Osteoclastos/metabolismo , Transdução de Sinais/efeitos dos fármacos , Animais , Reabsorção Óssea/metabolismo , Reabsorção Óssea/patologia , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Feminino , Camundongos , Osteoclastos/patologia , Fosfatase Ácida Resistente a Tartarato/biossínteseRESUMO
BACKGROUND: Atrial fibrosis causes abnormal conduction through the atria, creating a substrate for atrial fibrillation (AF). In a rabbit model, rapid atrial pacing produces significant atrial fibrosis and the substrate for AF maintenance. This atrial remodeling is a potential therapeutic target. OBJECTIVE: To evaluate the effects of the losartan on atrial fibrosis. METHODS: Thirty rabbit AF models were produced by rapid atrial stimulation. They were randomly divided into three groups: sham group, rapid atrial pacing group, and rapid atrial pacing with losartan group. We performed AF vulnerability studies, atrial histologic, and molecular analyses after 4 weeks. RESULTS: Only rabbits in the rapid atrial pacing group developed sustained AF (30 min, 4of 10 rabbits). Treatment with losartan resulted in a significant reduction in left atrial fibrosis and AF duration (P<.01). real-time polymerase chain reaction analyses demonstrated the drug's effects on the expression of Collagen I, Collagen III, and TGF-ß/Smads signaling pathway. CONCLUSIONS: The treatment of losartan results in significantly reduced atrial fibrosis and AF vulnerability. Pharmacological therapy targeted at the fibrotic substrate itself may play an important role in the management of AF.
Assuntos
Bloqueadores do Receptor Tipo 1 de Angiotensina II/farmacologia , Fibrilação Atrial/tratamento farmacológico , Losartan/farmacologia , Animais , Fibrilação Atrial/patologia , Fibrilação Atrial/fisiopatologia , Estimulação Cardíaca Artificial , Colágeno/genética , Colágeno/metabolismo , Modelos Animais de Doenças , Eletrocardiografia , Feminino , Fibrose , Átrios do Coração/efeitos dos fármacos , Átrios do Coração/patologia , Átrios do Coração/fisiopatologia , Masculino , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Coelhos , Taquicardia/complicaçõesRESUMO
Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone, H-PLN) was isolated from Plumbago zeylanica, the anticancer traditional Chinese medicine (TCM). Five new lanthanide(III) complexes of deprotonated plumbagin: [Y(PLN)(3)(H(2)O)(2)] (1), [La(PLN)(3)(H(2)O)(2)] (2), [Sm(PLN)(3)(H(2)O)(2)]â H(2)O (3), [Gd(PLN)(3)(H(2)O)(2)] (4), and [Dy(PLN)(3)(H(2)O)(2)] (5) were synthesized by the reaction of plumbagin with the corresponding lanthanide salts, in amounts equal to ligand/metal molar ratio of 3:1. The PLN-lanthanide(III) complexes were characterized by different physicochemical methods: elemental analyses, UV-visible, IR and (1)H NMR and ESI-MS (electrospray ionization mass spectrum) as well as TGA (thermogravimetric analysis). The plumbagin and its lanthanide(III) complexes 1-5, were tested for their in vitro cytotoxicity against BEL7404 (liver cancer) cell lines by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The five PLN-lanthanide (III) complexes 1-5 effectively inhibited BEL7404 cell lines growth with IC(50) values of 11.0±3.5, 5.1±1.3, 6.1±1.1, 6.4±1.3, and 9.8±1.5 µM, respectively, and exhibited a significantly enhanced cytotoxicity compared to plumbagin and the corresponding lanthanide salts, suggesting a synergistic effect upon plumbagin coordination to the Ln(III) ion. The lanthanide complexes under investigation also exerted dose- and time-dependent cytotoxic activity. [La(PLN)(3)(H(2)O)(2)] (2) and plumbagin interact with calf thymus DNA (ct-DNA) mainly via intercalation mode, but for [La(PLN)(3)(H(2)O)(2)] (2), the electrostatic interaction should not be excluded; the binding affinity of [La(PLN)(3)(H(2)O)(2)] (2) to DNA is stronger than that of free plumbagin, which may correlate with the enhanced cytotoxicity of the PLN-lanthanide(III) complexes.
Assuntos
Antineoplásicos/farmacologia , Elementos da Série dos Lantanídeos/química , Naftoquinonas/química , Compostos Organometálicos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Cátions , Linhagem Celular Tumoral , DNA/metabolismo , Humanos , Concentração Inibidora 50 , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Compostos Organometálicos/síntese química , Compostos Organometálicos/química , Projetos Piloto , Análise Espectral , TermogravimetriaRESUMO
Three new compounds of Ga(III), Au(III), Sn(IV) with matrine (MT), [H-MT][GaCl(4)] (1), [H-MT][AuCl(4)] (2) and [Sn(H-MT)Cl(5)] (3), have been synthesized and characterized by elemental analysis, IR, ESI-MS and single crystal X-ray diffraction methods. The crystal structural analyses indicate that 1 and 2 are ionic compounds, whereas 3 is a tin(IV) complex formed by the monodentate MT via its carbonyl oxygen atom of MT coordinating to Sn(IV). Their in vitro cytotoxicity towards eight selected tumour cell lines has been evaluated by MTT (3-[4,5-Dimentylthiazole-2-yl]-2,5-diphenpyltetra-zolium bromide) method, and compounds 1 and 2 exhibit enhanced activity, such as 1 to SW480, 2 to HeLa, HepG2 and MCF-7, which exceeds matrine and cisplatin, and display synergistic contribution of their components. The cell cycle analyses show that compounds 1, 3 and MT exhibit cell cycle arrest at the G(2)/M phase. Interactions of these compounds with calf thymus DNA (ct-DNA) have been investigated by spectroscopic analyses. The planar extension of the intercalative metal-matrine compounds increases the interaction of the metal-matrine with DNA, indicating that the cationic metal ions and configuration of the intercalated metal-matrine will affect the extent of interaction. Compound 2, [H-MT][AuCl(4)], exhibits more intensive binding ability to DNA, which may correlate with intercalation and other action mode. The circular dichroism spectra of the ct-DNA bound with metal-MT compounds also suggest that ct-DNA interacted with 1, 2, 3 does not influence its secondary structure. Furthermore, both compounds 1 and 2 exhibit effective inhibition ability to topoisomerase (TOPO I) at concentration of 50 µM, while matrine and compound 3 do not.
Assuntos
Alcaloides/farmacologia , Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , DNA/química , Gálio , Ouro , Quinolizinas/farmacologia , Estanho , Alcaloides/química , Antineoplásicos/síntese química , Antineoplásicos/química , Ciclo Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Cristalografia por Raios X , DNA Topoisomerases Tipo I/química , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Modelos Moleculares , Estrutura Molecular , Quinolizinas/química , Relação Estrutura-Atividade , Inibidores da Topoisomerase/síntese química , Inibidores da Topoisomerase/química , Inibidores da Topoisomerase/farmacologia , Células Tumorais Cultivadas , MatrinasRESUMO
Liriodenine (L), a natural alkaloid, was isolated as an active component from the anticancer traditional Chinese medicine (TCM), Zanthoxylum nitidum. It reacted with Mn(II), Fe(II), Co(II) and Zn(II) to afford four metal complexes: [MnCl(2)(L)(2)] (1), [FeCl(2)(L)(2)] (2), [Co(L)(2)(H(2)O)(2).Co(L)(2)(CH(3)CH(2)OH)(2)](ClO(4))(4) (3), and [Zn(2)(L)(2)(mu(2)-Cl)(2)Cl(2)] (4), which were characterized by elemental analysis, IR, ESI-MS. Their crystal structures were determined by the single crystal X-ray diffraction method. The in vitro cytotoxicity of L and complexes 1-4 against 10 human tumour cell lines was assayed. Some of these metal-based compounds exhibited enhanced cytotoxicity vs. free L to selected tumour cell lines. The binding properties of L and its complexes 1-4 to ct-DNA were investigated by spectroscopic methods and viscosity measurements. Agarose gel electrophoresis experiments were also carried out to evaluate their unwinding ability towards plasmid DNA and their inhibition towards Topoisomerase I. All the results indicate that complexes 1-4 may bind more intensively to the DNA helix than does L, and intercalative binding for complexes 1-4 and electrostatic interactions for complexes 3-4 to DNA should be considered. For complex 4, covalent binding to DNA may exist. Of special note, all these metal complexes effectively inhibit Topoisomerase I even at low concentration (< or = 10 microM).
Assuntos
Antineoplásicos Fitogênicos/química , Aporfinas/química , Complexos de Coordenação/química , DNA/metabolismo , Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/toxicidade , Aporfinas/isolamento & purificação , Aporfinas/toxicidade , Linhagem Celular Tumoral , Complexos de Coordenação/síntese química , Complexos de Coordenação/toxicidade , Cristalografia por Raios X , DNA/química , DNA Topoisomerases Tipo I/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Medicina Tradicional Chinesa , Conformação Molecular , Inibidores da Topoisomerase I , Zanthoxylum/químicaRESUMO
Liriodenine (), an active component of the anticancer traditional Chinese medicine (TCM), was isolated from Zanthoxylum nitidum. Its reactions with Pt(II) and Ru(II) afforded three metal complexes: cis-[PtCl2(L)] (), cis-[PtCl2(L)(DMSO)] (), and cis-[RuCl2(L)(DMSO)2].1.5H2O (), the crystal structures of , and were determined by single-crystal X-ray diffraction methods. These complexes were fully characterized by elemental analysis, IR spectrophotometry, 1H and 13C NMR spectroscopies, and ES mass spectrometry. The in vitro cytotoxicity of and complexes against 11 human tumour cell lines was assayed. The metal-based compounds exhibit enhanced cytotoxicity vs. free , suggesting that these compounds display synergy in the combination of metal ions and liriodenine. The binding properties of and its complexes to ct-DNA were investigated through UV-vis, fluorescence, CD spectra, viscosity and agarose gels electrophoretic measurements.
Assuntos
Antineoplásicos/farmacologia , Aporfinas/farmacologia , DNA/metabolismo , Medicina Tradicional Chinesa , Compostos de Platina/química , Compostos de Rutênio/química , Zanthoxylum/química , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Aporfinas/química , Aporfinas/isolamento & purificação , Linhagem Celular Tumoral , Dicroísmo Circular , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Raízes de Plantas/química , Caules de Planta/química , Compostos de Platina/farmacologia , Compostos de Rutênio/farmacologiaRESUMO
The anticancer traditional Chinese medicine (TCM), plumbagin (PLN), was isolated from Plumbago Zeylanica. Reaction of plumbagin with Cu(II) salt, afforded [Cu(PLN)(2)].2H(2)O (1). With 2,2'-bipyridine (bipy) as a co-ligand, PLN reacts with Cu(II) to give [Cu(PLN)(bipy)(H(2)O)](2)(NO(3))(2).4H(2)O (2). 1 and 2 were characterized by elemental analysis, IR, ESI-MS spectra. Their crystal structures were determined by single crystal X-ray diffraction methods. The in vitro cytotoxicity of PLN, 1 and 2 against seven human tumour cell lines was assayed. The metal-based compounds exhibit enhanced cytotoxicity vs. that of free PLN, suggesting that these compounds display synergy in the combination of metal ions with PLN. The binding properties of PLN, 1 and 2 to DNA were investigated through UV-vis, fluorescence, CD spectra, and gel mobility shift assay, which indicated that 1 and 2 were non-covalent binding and mainly intercalated the neighboring base pairs of DNA. PLN, 1 and 2 exhibit inhibition activity to topoisomerase I (TOPO I), but 1 and 2 were more effective than PLN.
Assuntos
Antineoplásicos Fitogênicos/toxicidade , Complexos de Coordenação/toxicidade , Cobre/química , Naftoquinonas/toxicidade , 2,2'-Dipiridil/química , Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Cristalografia por Raios X , DNA/química , DNA/metabolismo , DNA Topoisomerases Tipo I/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Medicina Tradicional Chinesa , Conformação Molecular , Naftoquinonas/química , Naftoquinonas/isolamento & purificação , Raízes de Plantas/química , Plumbaginaceae/química , Inibidores da Topoisomerase IRESUMO
BACKGROUND & OBJECTIVE: Polysaccharide components of some traditional Chinese medicine have certain antitumor effects and can promote immune responses. Extractions from cactus pear fruit can inhibit the proliferation of cervical cancer, ovary cancer and bladder cancer cells, and suppress the growth of ovarian cancer in mice. This study was to observe the antitumor effect of polysaccharides extracted from cactus pear fruit in S180-bearing mice. METHODS: S180-bearing mice were established and divided into five groups: normal saline (NS) group, cyclophosphamide (CTX) group, high, middle and low dose of polysaccharide groups. Tumor inhibition rates, values of thymus index, spleen index, superoxide dismutase (SOD), maleic dialdehyde (MDA) and nitrogen monoxidum (NO) were recorded. Changes in ultra-structures of tumor cells under transmission electron microscopy were observed. RESULTS: The tumor inhibition rates in CTX group, high, middle and low dose groups were 7.78%, 31.13%%, 49.70%, 61.07%, respectively. The thymus index was significantly higher in middle and high dose groups than in NS group [(2.61+/-0.43) mg x g(-1) and (2.65+/-0.73) mg x g(-1) vs. (2.22+/-0.24) mg x g(-1), P<0.05]. The spleen index of high dose group was higher than that of NS group [(6.45+/-0.97) mg x g(-1) vs. (5.42+/-1.13) mg x g(-1),P<0.05]. SOD of middle and high dose groups [(303.12+/-13.03) U/mL and (310.03+/-18.02) U/mL] were higher than that of NS group [(280.12+/-10.01) U/mL](P<0.05). MDA was lower in low, middle and high dose groups [(6.56+/-0.75) nmol/mL, (6.24+/-1.03) nmol/mL and (5.78+/-0.90) nmol/mL, respectively] than that in NS group [(7.39+/-0.51) nmol/mL] (P<0.05). NO was lower in low, middle and high dose groups [(56.12+/-8.60) micromol/L, (50.12+/-10.05) micromol/L, (48.06+/-8.45) micromol/L respectively] than in NS group [(64.14+/-1.25) micromol/L](P<0.05). Under electron microscopy, polysaccharide or CTX treated tumor cells showed typical morphology of early apoptosis with condensed chromatin at the margins of nuclei, disintegrated nucleolus and vacuoles in the cytoplasm. CONCLUSION: Polysaccharides extracted from cactus pear fruit possess certain antitumor effects, which can induce apoptosis, increase antioxidation and promote immune responses.
Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Cactaceae/química , Polissacarídeos/uso terapêutico , Sarcoma 180/tratamento farmacológico , Animais , Feminino , Masculino , Camundongos , Óxido Nítrico/biossíntese , Tamanho do Órgão/efeitos dos fármacos , Sarcoma 180/metabolismo , Sarcoma 180/patologia , Sarcoma 180/ultraestruturaRESUMO
OBJECTIVE: To evaluate the effect of octacostyl alcohol preparation on the motor function, blood free radical metabolism and cardiac endocrine function of rats. METHODS: A rat model of exercise fatigue was used for this study. The rats were made to perform continuous exhaustive exercise, and the total exercise time of the rats till exhaustion was recorded followed by examination of the serum superoxide dismutase (SOD), malonaldehyde (MDA), plasma endothelin (ET), calcitonin gene-related peptide (CGRP), and atrial natriuretic peptide (ANP). RESULTS: Compared with rats without interventions for exercise fatigue, the rats receiving octacostyl alcohol preparation had significant prolonged exercise time till exhaustion (P<0.05), with also significantly enhanced serum SOD activity (P<0.05), significantly decreased MDA level and plasma ET (P<0.05) and increased CGRP and ANP levels (P<0.05). Octacostyl alcohol preparation produced more favorable effect on all the indices measured than pyruvic acid-creatine (P<0.05). CONCLUSION: The octacostyl alcohol preparation can promote the motor function, increases blood antioxidase activity, suppressed lipid peroxidation in rats engaged in exhaustive exercise. The preparation also produces favorable effect on cardiac endocrine function for heart protection during exercise.