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1.
PLoS One ; 17(4): e0266678, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35404969

RESUMO

OBJECTIVES: Adjuvant radiotherapy is the standard of care in locally advanced head and neck cancers. The radiation field is correlated with the surgical field in the adjuvant radiotherapy setting; therefore, tailoring the irradiation field is reasonable. MATERIALS AND METHODS: We retrospectively analyzed patients with oral cavity and oropharyngeal cancers included in the cancer registry between 2015 and 2019 in the study hospital. Patients who underwent whole-neck irradiation (WNI) were compared with those who underwent lower-neck-sparing (LNS) irradiation. RESULTS: A total of 167 patients with oral cavity and oropharyngeal cancers were included in the study. Cancer recurrence was recorded in 33% of the patients. The rate of recurrence of oral cavity and oropharyngeal cancer at neck level IV was 8%. The 2-year incidence of level IV recurrence was lower in the WNI group than in the LNS group (2% vs. 10%; p = 0.04). The 2-year disease-free survival rates were 75% and 63% in the WNI and LNS groups, respectively (p = 0.08). CONCLUSION: The rate of level IV recurrence was higher in the LNS group than in the WNI group. Trends of improvement in disease-free survival with lower-neck irradiation suggested that it is premature to consider LNS irradiation as daily practice in patients with oral cavity and oropharyngeal cancer.


Assuntos
Neoplasias Bucais , Neoplasias Orofaríngeas , Estudos de Viabilidade , Humanos , Neoplasias Bucais/radioterapia , Neoplasias Bucais/cirurgia , Recidiva Local de Neoplasia/radioterapia , Neoplasias Orofaríngeas/radioterapia , Neoplasias Orofaríngeas/cirurgia , Radioterapia Adjuvante , Estudos Retrospectivos
2.
Nat Prod Res ; 36(4): 891-895, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33146019

RESUMO

A new phenolic glycoside, chinenside A (1), and a new megastigmane glycoside, chinenionside A (2), together with twelve known compounds (3-14), were isolated from the roots of Alangium chinense. Their structures were deduced on the basis of extensive spectroscopic analyses and comparison with data reported in the literature. The anti-inflammatory activity in vitro of all 13 phenolic glycosides was evaluated against lipopolysaccharide-induced mouse macrophage RAW264.7 cells. The compounds 1, 9, and 10 potentially inhibited the productions of nitric oxide (NO), prostaglandin (PEG2), tumor necrosis factor alpha (TNF-α), interleukin 1 beta (IL-1ß) and interleukin 6 (IL-6). Compound 1 (50 µM) showed stronger anti-inflammatory activity than Triptolide (TPL, 20 nm).


Assuntos
Alangiaceae , Alangiaceae/química , Animais , Anti-Inflamatórios/farmacologia , Glicosídeos/química , Lipopolissacarídeos/farmacologia , Camundongos , Óxido Nítrico , Células RAW 264.7 , Fator de Necrose Tumoral alfa
3.
Planta Med ; 88(11): 881-890, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34359084

RESUMO

The root Rhynchosia volubilis was widely used for contraception in folk medicine, although its molecular mechanism on antifertility has not yet been revealed. In human sperm, it was reported that the cation channel of sperm, an indispensable cation channel for the fertilization process, could be regulated by various steroid-like compounds in plants. Interestingly, these nonphysiological ligands would also disturb the activation of the cation channel of sperm induced by progesterone. Therefore, this study aimed to explore whether the compounds in R. volubilis affect the physiological regulation of the cation channel of sperm. The bioguided isolation of the whole herb of R. volubilis has resulted in the novel discovery of five new prenylated isoflavonoids, rhynchones A - E (1:  - 5: ), a new natural product, 5'-O-methylphaseolinisoflavan (6: ) (1H and 13C NMR data, Supporting Information), together with twelve known compounds (7:  - 18: ). Their structures were established by extensive spectroscopic analyses and drawing a comparison with literature data, while their absolute configurations were determined by electronic circular dichroism calculations. The experiments of intracellular Ca2+ signals and patch clamping recordings showed that rhynchone A (1: ) significantly reduced cation channel of sperm activation by competing with progesterone. In conclusion, our findings indicat that rhynchone A might act as a contraceptive compound by impairing the activation of the cation channel of sperm and thus prevent fertilization.


Assuntos
Progesterona , Motilidade dos Espermatozoides , Cálcio/metabolismo , Canais de Cálcio/metabolismo , Sinalização do Cálcio , Humanos , Masculino , Progesterona/análise , Progesterona/metabolismo , Progesterona/farmacologia , Sementes , Espermatozoides/química , Espermatozoides/metabolismo
4.
J Asian Nat Prod Res ; 24(11): 1071-1077, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34951327

RESUMO

The phytochemical investigation of the methanol extract of Ixeris sonchifolia led to the isolation and identification of nine analogs, including one new guaiane-type sesquiterpenoid, named ixerinoid A (1). The structure of 1 was determined by extensive analysis of the 1 D and 2 D nuclear magnetic resonance spectroscopic data, as well as quantum chemical calculations. Additionally, all the isolates were tested for their neuroprotective activity using the oxygen-glucose deprivation/reperfusion-induced SH-SY5Y cell injury model. Compounds 3, 5, 6, 8, and 9 displayed remarkable protective effects at concentrations of 1, 5, and 10 µM, respectively.


Assuntos
Asteraceae , Neuroblastoma , Fármacos Neuroprotetores , Traumatismo por Reperfusão , Sesquiterpenos , Humanos , Estrutura Molecular , Asteraceae/química , Sesquiterpenos/farmacologia , Sesquiterpenos/química , Fármacos Neuroprotetores/farmacologia
5.
Bioorg Chem ; 115: 105251, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34390969

RESUMO

Thirteen previously undescribed guaiane-type sesquiterpenoids based on [5,7] bicyclic system, stelleranoids A-M (1-13), along with six known analogues (14-20), were isolated from the roots of Stellera chamaejasme with chromatographic techniques. Their structures including absolute configurations were determined by HRESIMS and spectroscopic data, quantum chemical calculations, as well as X-ray crystallographic analysis. Cytotoxicity test in three cell lines indicated that compound 14 had relatively stronger cytotoxic effect against MKN-45, SKOV3, and Du145 cell lines with IC50 of 9.8, 17.4 and 7.3 µM, respectively; compounds 3 and 8 displayed moderate cytotoxic effect against MKN-45 and Du145 cell lines with IC50 ranged from 14.5 to 18.8 µM, comparable to those of the positive control. As determined by fluorescent microscopy and flow cytometry in Du145 cell line, compound 14 could promote cell apoptosis and cause cell cycle arrest at the G0/G1 phase, leading to the inhibition of cell proliferation. Further Western blot analysis revealed that this inhibitory effect was accompanied by upregulating pro-apoptosis proteins cleaved-PARP, cleaved-Caspase-9 and tumor suppressor protein p53 while downregulating anti-apoptotic protein Bcl-2 in 14-treated Du145 cells.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Sesquiterpenos/farmacologia , Thymelaeaceae/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Modelos Moleculares , Estrutura Molecular , Raízes de Plantas/química , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Relação Estrutura-Atividade
6.
Artigo em Inglês | MEDLINE | ID: mdl-31583009

RESUMO

Xiao Ke Yin Shui (XKYS) formula is a traditional Chinese medicine formula treating type 2 diabetes mellitus (T2DM). XKYS formula consists of four herbs, i.e., Coptidis rhizoma, Liriopes radix, bitter melon, and Cassiae semen. Herein, the chemical profiles of four herb extracts were investigated, and further analysis of the underlying mechanism of XKYS formula treating T2DM was performed using network pharmacology. The main components were selected for our network-based research. Targets of XKYS formula were mainly collected from two databases, SwissTargetPrediction and Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), and the text-mining method was also implemented. T2DM relating genes and therapeutic targets were collected from five databases. Subsequently, STRING and Cytoscape were employed for the analysis of protein-protein interaction (PPI) networks. Functional annotation and pathway analysis were conducted to investigate the functions and relating pathways of target genes. The content of 12 compounds in the herb extracts was determined. With the analysis of PPI networks, a total of 76 genes were found to be important nodes and could be defined as the main target genes regulated by XKYS formula in the treatment of T2DM and its complications. Components in XKYS formula mainly regulate proteins including protein kinase B (Akt), phosphatidylinositol 3-kinase (PI3K), insulin receptor substrate (IRS), and tumor necrosis factor (TNF). XKYS formula exerts therapeutic effects in a synergetic manner and exhibits antidiabetic effect mainly via reducing insulin resistance. These findings could be guidelines in the further investigation of this formula.

7.
J Ethnopharmacol ; 225: 359-366, 2018 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-29753098

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Circaea mollis Sieb. & Zucc., a genus of Circaea that follows Onagraceae, has been used for centuries as a folk herb in traditional Chinese medicine (TCM) and Hani Ethnopharmacy for the treatment of joint swelling and pain in rheumatoid arthritis. AIM OF THE STUDY: This study was designed to confirm anti-arthritic effects and its underlying mechanism of ethanol extracts of Circaea mollis Sieb. & Zucc. (EEC), which may contribute to provide the pharmacological basis in the treatment of rheumatoid disease. MATERIALS AND METHODS: Dimethylbenzene (DMB)-induced inflammatory swelling model, hot-plate pain model in mice and Freund's complete adjuvant (FCA)-induced arthritis model in rats were used to evaluate the anti-arthritis effect of EEC. Arthritis severity was done by measuring inflammatory swelling, pain threshol, paw swelling, arthritis index, body weight, spleen index and thymus index. The levels of TNF-α, IL-1ß and IL-10 in sera were measured using ELISA. The pathological change of the ankle joint was also done. Phenolic composition of EEC was analyzed. RESULTS: EEC inhibited inflammatory swelling and increased heat-induced pain threshold in mice. Furthermore, EEC significantly alleviated paw swelling and arthritis index, decreasing the spleen index and thymus index. Besides, EEC down-regulated the serum TNF-α and IL-1ß, and increased the production of serum IL-10 in FCA-induced rats. Histopathological examination demonstrated that EEC can effectively relieve synovial hyperplasia, control the infiltration of the inflammatory and protect cartilage from destruction. CONCLUSION: Our work demonstrated that EEC possessed the potential therapeutic effect against arthritis in rodents which was attributed to modulating proinflammatory cytokines TNF-α, IL-1ß and anti-inflammatory factors IL-10. Flavonoids and polyphenols may contribute to the therapeutic effect of EEC on arthritis.


Assuntos
Anti-Inflamatórios/uso terapêutico , Artrite Experimental/tratamento farmacológico , Onagraceae , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/análise , Anti-Inflamatórios/farmacologia , Artrite Experimental/sangue , Artrite Experimental/induzido quimicamente , Artrite Experimental/patologia , Citocinas/sangue , Edema/induzido quimicamente , Edema/tratamento farmacológico , Etanol/química , Feminino , Adjuvante de Freund , Temperatura Alta/efeitos adversos , Articulações/efeitos dos fármacos , Articulações/patologia , Masculino , Camundongos , Dor/tratamento farmacológico , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Fitoterapia , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Ratos Sprague-Dawley , Solventes/química , Xilenos
8.
Carbohydr Polym ; 173: 215-222, 2017 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-28732860

RESUMO

Structures and in vitro hypoglycemic activities of polysaccharides from different species of Maidong were studied. The primary structures of polysaccharides were elucidated on the basis of GC, GC-MS, infrared, NMR and periodate oxidation-Smith degradation. Liriope spicata polysaccharide (LSP), Ophiopogon japonicus polysaccharide (OJP) and Liriope muscari polysaccharide (LMP) were composed of ß-fructose and α-glucose. The average molecular weights of LSP, OJP and LMP were 4742, 4925 and 4138Da with polydispersity indexes of 1.1, 1.2 and 1.1, respectively. The backbones of polysaccharides were formed by Fruf-(2→, →2)-Fruf-(6→, →6)-Glcp-(1→ and →1, 2)-Fruf-(6→ with a molar ratio of 5.0:18.2:1.0:5.3 (LSP), 6.8:15.8:1.0:5.8 (OJP), 8.3:12.3:1.0:3.9 (LMP), respectively. The RT-PCR and western blot analysis indicated that LSP, LMP and OJP increased the expression of PI3K, AKT, InsR, PPARγ and decreased the expression of PTP1B in mRNA level and protein level in IR HepG2 cells. Furthermore, glucose consumption was increased after treated with polysaccharides. These results revealed that LSP, OJP and LMP had potential anti-diabetic effects.


Assuntos
Hipoglicemiantes/farmacologia , Liriope (Planta)/química , Ophiopogon/química , Polissacarídeos/farmacologia , Células Hep G2 , Humanos
9.
Sci Rep ; 7: 43556, 2017 04 03.
Artigo em Inglês | MEDLINE | ID: mdl-28368001

RESUMO

Snake gallbladder, a traditional Chinese medicine, has been believed in various Asian countries to improve visual acuity and alleviate rheumatism. Bile acids, a major component of the gallbladder, are toxic to the liver and kidney in humans and animals due to its detergent effects, while also exhibiting therapeutic effects due to an increase in the gallbladder contractions of muscle strips in patients with cholesterol gallstones. Secretion of bile acids in human and mammals depends on the bile salt export pump (BSEP), a liver-specific adenosine triphosphate (ATP)-binding cassette transporter encoded by ABCB11. However, the presence of BSEP in snakes has not been thoroughly explored. Here we confirm the existence of BSEP and its coding DNA sequence in snakes on both the proteomic and genetic level. This work provides information on the snake ABCB11 sequence and helps further potential genetic manipulation to affect bile salt metabolism. Our study provides the foundation for research on bile acid production from snakes by using modern genetic and proteomic methodologies.


Assuntos
Membro 11 da Subfamília B de Transportadores de Cassetes de Ligação de ATP/genética , Membro 11 da Subfamília B de Transportadores de Cassetes de Ligação de ATP/metabolismo , Genômica , Fígado/metabolismo , Proteômica , Serpentes/genética , Serpentes/metabolismo , Animais , Genômica/métodos , Filogenia , Proteômica/métodos , Análise de Sequência de DNA , Serpentes/classificação
10.
Sci Rep ; 7: 44681, 2017 03 20.
Artigo em Inglês | MEDLINE | ID: mdl-28317897
11.
J Ethnopharmacol ; 194: 1078-1086, 2016 Dec 24.
Artigo em Inglês | MEDLINE | ID: mdl-27840082

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Schisandra glaucescens Diels (SGD) is used in a subclass of traditional Chinese medicine known as "Tujia drugs". It has been long used for the treatment of rheumatoid arthritis (RA), cough with dyspnea, spontaneous sweating, night sweating, chronic diarrhea, and neurasthenia. As a woody liana growing in mountain jungles at the altitudes of 750-1800m, it is mainly distributed in Sichuan and Hubei Provinces of China. AIM OF THE STUDY: To evaluate the antiarthritic activity of acetate (EA) and n-butanol (Bu) fractions of SGD extract on a collagen-induced arthritis mice model. MATERIALS AND METHODS: Acute toxicity of EA and Bu fractions of SGD extract was evaluated by gavage on normal mice. Pharmacological investigations were conducted on arthritis male Balb/c mice. The animal model was induced by immunization with type II bovine collagen (CII) on the 1st and the 14th day of the experimental schedule. EA fraction (104, 312, 936mg/kg), Bu fraction (156, 469, 1407mg/kg) of SGD extract was orally administered every two days since the 15th day for 3 weeks. Progression of edema in the paws was measured using a vernier caliper every 3 days since the 10th day. At the end of the experiment, the spleen index and histological changes of the hind knee joints were investigated. Additionally, to explore the possible antirheumatic mechanisms of the EA and Bu fractions, ELISA was carried out to analyze TNF-α, IL-10, IL-6 and IL-1ß in the serum. RESULTS: The half lethal doses of both EA and Bu fractions were much higher than the dose administered in the pharmacological investigations. Oral administration of EA fraction and Bu fraction of SGD extract significantly and does-dependently inhibited type ІІ collagen induced arthritis (CIA) in mice, as indicated by the effects on paws swelling and spleen index. Histopathological examinations demonstrated that SGD effectively protected the bones and cartilages of knee joints from erosion, lesion and deformation. Besides, the serum concentrations of cytokines TNF-α, IL-1ß and IL-6 were significantly lower than the ones from the vehicle control group. Respectively, while cytokine IL-10 was remarkably higher compare with the vehicle control group. CONCLUSIONS: SGD might be a safe and effective candidate for the treatment of RA, and deserves further investigation on the chemical components in both EA and Bu fractions of SGD extract.


Assuntos
Artrite Experimental/tratamento farmacológico , Artrite Reumatoide/tratamento farmacológico , Colágeno Tipo II/farmacologia , Extratos Vegetais/farmacologia , Caules de Planta/química , Schisandra/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antirreumáticos/química , Antirreumáticos/farmacologia , Artrite Experimental/induzido quimicamente , Artrite Experimental/metabolismo , Artrite Reumatoide/induzido quimicamente , Modelos Animais de Doenças , Edema/induzido quimicamente , Edema/tratamento farmacológico , Edema/metabolismo , Feminino , Interleucina-10/metabolismo , Interleucina-6/metabolismo , Masculino , Medicina Tradicional Chinesa/métodos , Camundongos , Camundongos Endogâmicos BALB C , Fitoterapia/métodos , Extratos Vegetais/química , Baço/efeitos dos fármacos , Baço/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
12.
J Ethnopharmacol ; 150(2): 536-44, 2013 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-24055468

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Swertia macrosperma is a traditional folk medicine used for its anti-hepatitis, antipyretic and antidotal effects as "Dida" or "Zangyinchen" in Tibet, Yunnan and Guizhou province for a long time, and it has been reported for its anti-diabetic effects in a Chinese patent. Swertia macrosperma was reported rich in xanthones, iridoids, seco-iridoids and their glycosides, several of which had been documented as potential antidiabetic agents. The objective of this study was to investigate the antidiabetic effect of Swertia macrosperma in diabetic rats. MATERIALS AND METHODS: This study was designed firstly to evaluate the effect of Swertia macrosperma on glucose consumption in HepG2 cells. Based on the result in HepG2 cells, the antidiabetic effect of ethanol extract (EE) and n-butanol extract (BE) were investigated in diabetic rats induced by high fat fed and streptozotocin. The effects of EE and BE on fasting blood glucose, oral glucose tolerance test, serum insulin, glycosylated hemoglobin, serum lipid level, serum antioxidant parameters, glucokinase, glucose-6-phosphatase activities and glycogen content in liver tissue were measured, histology examination of pancreatic tissue was also carried out. RESULTS: After 4 weeks treatment with EE and BE, apparently decreased fasting blood glucose concentrations were observed in these treated groups, compared with the diabetic control groups. Additionally, improvement in serum antioxidant parameters and lipid profile were evidenced clearly. Moreover, EE and BE had effects of protecting the pancreatic ß-cells and stimulating insulin secretion from the remaining pancreatic ß-cells, evidenced by pancreatic histology examination. Increased glucokinase activity and decreased glucose-6-phosphatase activity were observed in liver. CONCLUSION: The results of in vivo and in vitro experiment suggested that EE and BE of Swertia macrosperma had excellent effects on controlling the hyperglycemia and hyperlipidemia in diabetic rats.


Assuntos
Antioxidantes/uso terapêutico , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Swertia , Animais , Antioxidantes/farmacologia , Catalase/sangue , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/patologia , Glucoquinase/metabolismo , Glucose/metabolismo , Glucose-6-Fosfatase/metabolismo , Glutationa Peroxidase/sangue , Hemoglobinas Glicadas/análise , Glicogênio/metabolismo , Células Hep G2 , Humanos , Hipoglicemiantes/farmacologia , Insulina/sangue , Lipídeos/sangue , Fígado/efeitos dos fármacos , Fígado/enzimologia , Masculino , Malondialdeído/sangue , Pâncreas/efeitos dos fármacos , Pâncreas/patologia , Fitoterapia , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Superóxido Dismutase/sangue
13.
Ecotoxicol Environ Saf ; 93: 163-70, 2013 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23680394

RESUMO

There is little information on the organochlorine pesticides (OCPs) residues in agricultural soils of Wuhan, the largest city in central China. Surface soil samples were collected from agricultural soils in Wuhan and analyzed to determine twenty-one OCPs. According to the measured concentrations and detection frequencies, dichlorodiphenyltrichloroethanes (DDTs), hexachlorocyclohexanes (HCHs), heptachlor (HEPT), hexachlorobenzene (HCB) and aldrin were the predominant compounds in soil. DDTs accounted for 77.10% of total OCPs, followed by HCHs (7.83%), aldrin (4.21%), HEPTs (2.82%) and HCB (1.53%). The total DDT concentrations ranged from nd to 1198.0ngg(-1) and the main contaminated areas were distributed in Hannan and Xinzhou districts of Wuhan. The total HCH concentrations ranged from nd to 100.58ngg(-1) in soil and relatively higher levels were observed in soil samples from Huangpi and Hannan districts. Source analysis showed that OCPs residues except heptachlor originated mainly from historical application, besides slight recent introduction at some sites. Based on the China National Soil Quality Standard, DDT pollution in most samples of Wuhan agricultural soils could be considered as no and low contamination, while the level of HCHs was classified as no pollution. Our study indicated that there existed potential exposure risk of OCPs in Wuhan agricultural soils although the use of OCPs has been banned.


Assuntos
Hidrocarbonetos Clorados/análise , Praguicidas/análise , Poluentes do Solo/análise , Solo/química , Agricultura/estatística & dados numéricos , China , Monitoramento Ambiental , Poluição Ambiental/estatística & dados numéricos , Hexaclorobenzeno/análise , Hexaclorocicloexano/análise
14.
J Asian Nat Prod Res ; 15(5): 466-72, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23614827

RESUMO

One new lignan (7S,8R,7'R,8'R)-7-(3,4-methylenedioxyphenyl)-8,8'-dimethyl-8'-hydroxyl-7'-methoxyl-7'-(3',4'-methylenedioxyphenyl)-tetrahydrofuran (1), one new sesquiterpene 2-hydroxy-11,12-dehydrocalamenene (2), one new natural product erythro-1-(3,4-dimethoxyphenyl)-4-(3,4-methylenedioxyphenyl)-2,3-dimethyl-butane (3), and two known lignans (+)-anwulignan(erythro-1-(4-hydroxy-3-methoxyphenyl)-4-(3,4-methylenedioxyphenyl)-2,3-dimethyl-butane) (4) and ( - )-zuonin-A (5) were isolated from the stems of Schisandra glaucescens Diels. Their structures were elucidated by spectroscopic methods. The cytotoxicity of compounds 1 and 2 was assayed.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Lignanas/isolamento & purificação , Schisandra/química , Sesquiterpenos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Furanos , Células HCT116 , Humanos , Lignanas/química , Lignanas/farmacologia , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Caules de Planta/química , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Estereoisomerismo
15.
J Ethnopharmacol ; 147(3): 622-30, 2013 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-23567032

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Swertia kouitchensis has long been used as a folk medicine to treat hepatitis and diabetes in central-western China. Therefore, this study was aimed to evaluate the anti-diabetic activity of the plant ethanol extract. MATERIALS AND METHODS: Firstly, the extract was tested for its inhibitory activity on α-amylase and α-glucosidase in vitro. Following that, insulin secretion test in NIT-1 cell was performed. Then, oral sucrose or starch tolerance test of the extract were carried out in normal mice. After that, acute effect of the extract was executed in normal and streptozotocin-induced (60 mg/kg) diabetic mice. Eventually, long term effect of the extract was performed in diabetic mice for 4 weeks. Oral glucose tolerance test and biochemical parameters were estimated at the end of the study. RESULTS: Swertia kouitchensis extract could remarkably inhibit the activity of α-amylase and α-glucosidase and stimulate insulin secretion in vitro. And also the extract displayed anti-hyperglycemic activity, improved antioxidant capacity, ameliorated the hyperlipidemia and carbohydrate metabolism in diabetic mice. CONCLUSIONS: Swertia kouitchensis exhibits considerable anti-diabetic activity and metabolic alterations in diabetic mice. These results provide a rationale for the use of Swertia kouitchensis to treat diabetes mellitus.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Fitoterapia , Extratos Vegetais/uso terapêutico , Swertia , Animais , Glicemia/análise , Linhagem Celular Tumoral , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/metabolismo , Feminino , Glucoquinase/metabolismo , Teste de Tolerância a Glucose , Glucose-6-Fosfatase/metabolismo , Glicogênio/metabolismo , Hipoglicemiantes/farmacologia , Insulina/metabolismo , Secreção de Insulina , Lipídeos/sangue , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Malondialdeído/sangue , Camundongos , Camundongos Endogâmicos BALB C , Extratos Vegetais/farmacologia , Superóxido Dismutase/sangue , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
16.
J Asian Nat Prod Res ; 12(5): 355-9, 2010 May.
Artigo em Inglês | MEDLINE | ID: mdl-20496192

RESUMO

Two new flavan-4-ol glycosides, (2R,4S)-6,8-dimethyl-7-hydroxy-4'-methoxy-4,2''-oxidoflavan-5-O-beta-D-6''-O-acetyl-glucopyranoside (1) and (2R,4S)-5,7-O-beta-D-di-glucopyranosyloxy-4'-methoxy-6,8-dimethyl-4,2''-oxidoflavane (2), were isolated from the rhizomes of Abacopteris penangiana. Their structures were elucidated by spectroscopic methods. Compounds 1 and 2 showed significant anticancer activities against HeLa and L929 cell lines in vitro.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Gleiquênias/química , Flavonoides/isolamento & purificação , Glicosídeos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Glicosídeos/química , Glicosídeos/farmacologia , Células HeLa , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Rizoma/química , Estereoisomerismo
18.
Zhongguo Zhong Yao Za Zhi ; 34(19): 2473-6, 2009 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-20067016

RESUMO

OBJECTIVE: To investigate antitumor constituents from n-butyl alcohol extract of Alternanthera philoxeroides. METHOD: The constituents were isolated with silica gel, gel permeation chromatography, and purified by HPLC. Their structures were elucidated by spectroscopy and acid hydrolysis. The antitumor effects of extracts and isolated compounds were tested by MTH method in vitro. RESULT: Seven compounds were isolated and elucidated as followings: oleanolic acid 3-O-beta-D-glucuronopyranoside (1), oleanolic acid 28-O-beta-D-glucopyranoside (2), oleanolic acid 3-O-beta-D-glucuronopyranoside-6'-O-methyl ester (3), chikusetsusaponin IV a methyl ester (4), hederagenin 3-O-beta-D-glucuronopyranoside-6'-O-methyl ester (5), 4,5-dihydroblumenol (6), 6S,7E,9R-6,9-di-hydroxymegastigma-4,7-dien-3-one-9-O-beta-D-glucopyranoside (7). Compound 1 showed significant inhibitory effect against Hela and L929 with inhibitive ratios 91.3% and 92.9% at 30 mg x L(-1), respectively. CONCLUSION: Compounds 4, 5 and 7 were isolated from this genus for the first time. Compound 1 showed significant inhibitory effect against Hela and L929 at 30 mg x L(-1).


Assuntos
Amaranthaceae/química , Antineoplásicos/química , Medicamentos de Ervas Chinesas/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Hidrólise
19.
Artigo em Inglês | MEDLINE | ID: mdl-17357494

RESUMO

To investigate the effects of anti-sense peptide nucleic acids (PNAs) targeting Ki-67 gene on modulation of the proliferation and apoptosis of human renal carcinoma cell lines, human renal carcinoma cell line 786-0 cells were treated with anti-sense PNAs at different concentrations (1.0 micromol/L, 2.0 micromol/L, 10.0 micromol/L). The Ki-67 expression of 786-0 cells was detected by immunohistochemical technique and Western blot method respectively. The proliferation of 786-0 cells was studied by cell growth curves and 3H-thymidine incorporation. The apoptosis of 786-0 cells was detected by TUNEL assay. The control groups were treated with anti-sense oligonucleotide (ASODNs) targeting Ki-67 gene. Our results showed that the Ki-67 expression of 786-0 cells treated with anti-sense PNAs (16.9+/-0.7) was significantly inhibited as compared with that of the control groups (28.6+/-0.4) (P<0.01). The Ki-67 protein rate of 786-0 cells treated with anti-sense PNAs (42.1 +/-2.2) was significantly reduced when compared with that of the control groups (83.6+/- 1.4) (P<0.01). Proliferation of 786-0 cells treated with anti-sense PNAs (20.7+/- 1.5) was significantly inhibited as compared with that of the control groups (58.6+/- 1.4) (P<0.01). The apoptosis rate of 786-0 cells treated with anti-sense PNAs (28.7+/- 2.3) was significantly increased higher compared with that of the control groups (13.8 +/- 1.0) (P<0.01). From these finds we are led to conclude that anti-sense PNAs targeting Ki-67 gene have stronger effects on the inhibition of the proliferation and induction of apoptosis of human renal carcinoma cells than ASODNs targeting Ki-67 gene. The strategies using anti-sense PNAs targeting Ki-67 gene may be a promising approach for the treatment of renal cell carcinoma.


Assuntos
Carcinoma de Células Renais/patologia , Antígeno Ki-67/genética , Neoplasias Renais/patologia , Ácidos Nucleicos Peptídicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos
20.
Life Sci ; 76(16): 1873-81, 2005 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-15698864

RESUMO

We treated in vitro human renal carcinoma cells (cell line 786-0) with the lipid-delivered peptide nucleic acids (PNAs) against Ki-67 gene. Corresponding control groups were treated with the antisense oligonucleotides (ASOs) of the same nucleobase sequence, and with mismatched PNAs. In cells treated by anti-Ki-67 PNAs, the Ki-67 expression rate, Ki-67 protein level, cell growth and the DNA synthesis-indicative 3H-thymidine incorporation rate were lower than in the ASO-treated groups, and reduced significantly compared to untreated controls, whereas the rate of apoptosis was markedly increased by PNA treatment. We conclude that anti-Ki-67 PNA has more strong (than ASO) and dose-dependent effects on the proliferation and apoptosis of human renal carcinoma cells. Our results indicate that the strategy of using PNA against the Ki-67 gene might be a promising approach in renal carcinoma therapy.


Assuntos
Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Antígeno Ki-67/biossíntese , Ácidos Nucleicos Peptídicos/farmacologia , Western Blotting , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Humanos , Imuno-Histoquímica , Marcação In Situ das Extremidades Cortadas , Neoplasias Renais/metabolismo , Neoplasias Renais/patologia
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