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1.
Fitoterapia ; 140: 104431, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31759031

RESUMO

Two novel heptanornemoralisin-type diterpenoids nornemoralisins A (1) and B (2), together with two known compounds nemoralisin (3) and nemoralisin A (4), were isolated from the stem bark and leaves of Aphanamixis polystachya (Wall.) R. Parker. Their structures were established through comprehensive analyses of NMR spectroscopic data and high resolution mass spectrometric (HR-ESI-MS) data. The absolute configurations of carbon stereocenters were elucidated by circular dichroism (CD) analyses. The four compounds were tested for their potential cytotoxic effects against ACHN, HeLa, SMMC-7721, and MCF-7 cell lines. Nornemoralisins A (1) and B (2) exhibited significant cytotoxicity on ACHN with an IC50 value of 13.9 ± 0.8 and 10.3 ± 0.4 µM, respectively, and other compounds failed to reveal obvious cytotoxicity on the tested cell lines, compared to positive control vinblastine (IC50, 28.0 ± 0.9 µM).


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Diterpenos/farmacologia , Meliaceae/química , Antineoplásicos Fitogênicos/isolamento & purificação , China , Diterpenos/isolamento & purificação , Humanos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Casca de Planta/química , Folhas de Planta/química
2.
Nat Prod Res ; : 1-5, 2019 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-30990080

RESUMO

A new isopimarane-type diterpenoid, crolaevinoid A, along with four known analogues was isolated from the twigs and leaves of Croton laevigatus. The structures of the isolated compounds were established on the basis of NMR and MS spectroscopic analyses. The isolated compounds were examined the antibacterial activities. Unfortunately, the compounds showed no antibacterial activity against Micrococcus luteus, Methicillin-resistant Staphylococcus aureus, Aeromonas hydrophila, Klebsiella pneumoniae ssp pneumoniae, Acinetobacter Baumanii, and Escherichia coli.

3.
Org Lett ; 20(4): 1158-1161, 2018 02 16.
Artigo em Inglês | MEDLINE | ID: mdl-29420039

RESUMO

A bifunctional squaramide-catalyzed reaction of pyrazolin-5-ones with o-quinone methides in situ generated from 2-(1-tosylalkyl)phenols has been successfully developed, providing a facile access to chiral pyrazolones with high enantioselectivities. In addition, the chiral spiropyrazolones with adjacent tertiary and quaternary stereogenic centers can also be obtained through cascade chlorination/cyclization of the chiral pyrazolones.

4.
Oncotarget ; 8(59): 100045-100055, 2017 Nov 21.
Artigo em Inglês | MEDLINE | ID: mdl-29245959

RESUMO

A low dose of formononetin accelerates the proliferation of nasopharyngeal carcinoma cells in vitro; however, the underlying mechanism remains unknown. Here, we investigated the molecular mechanism of formononetin in CNE2 cell proliferation. CNE2 cells were treated with 0 to 1 µM formononetin. To inhibit mitogen activated protein kinase / extracellular regulate kinase (MAPK/ERK) kinase (MEK) and microRNA (miR)-375, cells were pretreated with either PD98059 or a miR-375 inhibitor, respectively, followed by co-treatment with formononetin (0.3 µM) plus an inhibitor. Female rats were ovariectomized (OVX), and some OVX rats received formononetin or estrogen (E2) injections. Sham operated animals were used as controls. Compared to control, 0.3 µM formononetin accelerated proliferation and decreased late apoptosis of CNE2 cells. However, formononetin-induced pro-growth and anti-apoptosis activity was abolished by PD98059 and the miR-375 inhibitor. In addition, 0.1 and 0.3 µM formononetin significantly increased estrogen receptor-α (ERα) and bcl-2, but decreased protein-phosphatase and tensin homologue (PTEN) protein expression, all of which was reversed by the miR-375 inhibitor. Additionally, formononetin treatment resulted in a transient upregulation of phosphorylated (p)-ERK1/2. In vivo studies indicated that formononetin significantly increased endometrium thickness and down-regulated ERα expression in OVX rats. Taken together, our study demonstrates that a low concentration of formononetin can promote growth of CNE2 cells and uterine tissues, possibly through regulating the ERα-miR-375-PTEN-ERK1/2-bcl-2 signaling pathway.

5.
Cancer Med ; 6(3): 631-639, 2017 03.
Artigo em Inglês | MEDLINE | ID: mdl-28181425

RESUMO

Pyropheophorbide-α methyl ester (MPPa) was a promising photosensitizer with stable chemical structure, strong absorption, higher tissue selectivity and longer activation wavelengths. The present study investigated the effect of MPPa-mediated photodynamic treatment on lung cancer A549 cells as well as the underlying mechanisms. Cell Counting Kit-8 was employed for cell viability assessment. Reactive oxygen species levels were determined by fluorescence microscopy and flow cytometry. Cell morphology was evaluated by Hoechst staining and transmission electron microscopy. Mitochondrial membrane potential, cellular apoptosis and cell cycle distribution were evaluated flow-cytometrically. The protein levels of apoptotic effectors were examined by Western blot. We found that the photocytotoxicity of MPPa showed both drug- and light- dose dependent characteristics in A549 cells. Additionally, MPPa-PDT caused cell apoptosis by reducing mitochondrial membrane potential, increasing reactive oxygen species (ROS) production, inducing caspase-9/caspase-3 signaling activation as well as cell cycle arrest at G0 /G1 phase. These results suggested that MPPa-PDT mainly kills cells by apoptotic mechanisms, with overt curative effects, indicating that MPPa should be considered a potent photosensitizer for lung carcinoma treatment.


Assuntos
Caspase 3/metabolismo , Caspase 9/metabolismo , Neoplasias Pulmonares/metabolismo , Fármacos Fotossensibilizantes/farmacologia , Porfirinas/farmacologia , Células A549 , Ciclo Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Fotoquimioterapia , Espécies Reativas de Oxigênio/metabolismo
6.
Apoptosis ; 22(5): 639-646, 2017 05.
Artigo em Inglês | MEDLINE | ID: mdl-28176145

RESUMO

Previous studies have shown that propofol, an intravenous anesthetic commonly used in clinical practice, protects the myocardium from injury. Mitochondria- and endoplasmic reticulum (ER)-mediated oxidative stress and apoptosis are two important signaling pathways involved in myocardial injury and protection. The present study aimed to test the hypothesis that propofol could exert a cardio-protective effect via the above two pathways. Cultured neonatal rat cardiomyocytes were treated with culture medium (control group), H2O2 at 500 µM (H2O2 group), propofol at 50 µM (propofol group), and H2O2 plus propofol (H2O2 + propofol group), respectively. The oxidative stress, mitochondrial membrane potential (ΔΨm) and apoptosis of the cardiomyocytes were evaluated by a series of assays including ELISA, flow cytometry, immunofluorescence microscopy and Western blotting. Propofol significantly suppressed the H2O2-induced elevations in the activities of caspases 3, 8, 9 and 12, the ratio of Bax/Bcl-2, and cell apoptosis. Propofol also inhibited the H2O2-induced reactive oxygen species (ROS) generation, lactic dehydrogenase (LDH) release and mitochondrial transmembrane potential (ΔΨm) depolarization, and restored the H2O2-induced reductions of glutathione (GSH) and superoxide dismutase (SOD). In addition, propofol decreased the expressions of glucose-regulated protein 78 kDa (Grp78) and inositol-requiring enzyme 1α (IRE1α), two important signaling molecules in the ER-mediated apoptosis pathway. Propofol protects cardiomyocytes from H2O2-induced injury by inhibiting the mitochondria- and ER-mediated apoptosis signaling pathways.


Assuntos
Apoptose/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Propofol/administração & dosagem , Animais , Animais Recém-Nascidos , Caspases/genética , Sobrevivência Celular/efeitos dos fármacos , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Regulação da Expressão Gênica/efeitos dos fármacos , Glutationa/genética , Humanos , Peróxido de Hidrogênio/toxicidade , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/genética , Ratos , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos , Superóxido Dismutase/genética
7.
Comput Assist Surg (Abingdon) ; 21(1): 160-165, 2016 12.
Artigo em Inglês | MEDLINE | ID: mdl-27973962

RESUMO

Acetabular fractures have always been very challenging for orthopedic surgeons; therefore, appropriate preoperative evaluation and planning are particularly important. This study aimed to explore the application methods and clinical value of preoperative computer simulation (PCS) in treating pelvic and acetabular fractures. Spiral computed tomography (CT) was performed on 13 patients with pelvic and acetabular fractures, and Digital Imaging and Communications in Medicine (DICOM) data were then input into Mimics software to reconstruct three-dimensional (3D) models of actual pelvic and acetabular fractures for preoperative simulative reduction and fixation, and to simulate each surgical procedure. The times needed for virtual surgical modeling and reduction and fixation were also recorded. The average fracture-modeling time was 45 min (30-70 min), and the average time for bone reduction and fixation was 28 min (16-45 min). Among the surgical approaches planned for these 13 patients, 12 were finally adopted; 12 cases used the simulated surgical fixation, and only 1 case used a partial planned fixation method. PCS can provide accurate surgical plans and data support for actual surgeries.


Assuntos
Acetábulo/diagnóstico por imagem , Acetábulo/lesões , Acetábulo/cirurgia , Fixação Interna de Fraturas/métodos , Fraturas do Quadril/diagnóstico por imagem , Fraturas do Quadril/cirurgia , Ortopedia , Planejamento de Assistência ao Paciente , Ossos Pélvicos/diagnóstico por imagem , Ossos Pélvicos/lesões , Ossos Pélvicos/cirurgia , Cirurgia Assistida por Computador/métodos , Tomografia Computadorizada por Raios X , Simulação por Computador , Humanos , Software
8.
Orthop Surg ; 8(3): 405-10, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27627726

RESUMO

A rare case of atlantoaxial lateral mass joint interlocking secondary to traumatic posterolateral C1,2 complete dislocation associated with type II odontoid fracture is herein reported and the impact of atlantoaxial joint interlocking on fracture reduction discussed. A 72-year-old man presented with traumatic atlantoaxial lateral mass joint interlocking without spinal cord signal change, the diagnosis being confirmed by radiography and 3-D reconstruction digital anatomy. Posterior internal fixation was performed after failure to achieve closed reduction by skull traction. After many surgical attempts at setting had failed because of interlocking of the lateral mass joints, reduction was achieved by compressing the posterior parts of the atlantal and axial screws. Odontoid bone union and C1,2 posterior bone graft fusion were eventually obtained by the 12-month follow-up. The patient had a complete neurological recovery with no residual neck pain or radiculopathy.


Assuntos
Articulação Atlantoaxial/cirurgia , Fixação Interna de Fraturas/métodos , Luxações Articulares/complicações , Processo Odontoide/lesões , Fraturas da Coluna Vertebral/cirurgia , Idoso , Articulação Atlantoaxial/diagnóstico por imagem , Humanos , Luxações Articulares/diagnóstico por imagem , Masculino , Processo Odontoide/diagnóstico por imagem , Processo Odontoide/cirurgia , Fraturas da Coluna Vertebral/diagnóstico por imagem , Fraturas da Coluna Vertebral/etiologia
9.
Pharm Biol ; 54(1): 74-9, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-25880142

RESUMO

CONTEXT: Genistein inhibits the proliferation and induces apoptosis of colorectal cancer cells; however, the underling molecular mechanisms remain to be determined. AIM: The aim of this study was to investigate whether genistein reduces cell viability by suppressing the phosphorylation of AKT and activating the mitochondrial apoptosis pathway in colorectal cancer cells. MATERIALS AND METHODS: The anti-proliferative effects of genistein (0, 25, 50, and 100 µM) on HCT-116 and LoVo cells were assessed using MTT assay. Genistein-induced apoptosis was measured by Hoechst 33258 staining and flow cytometry. The mRNA level of Bax was detected by real-time PCR. The protein levels of Bax, total Akt, and phosphorylated Akt were assessed by western blot. RESULTS: The IC50 values of genistein were 690, 135, and 61 µM in HCT-116 cells and 204, 135, and 93 µM in LoVo cells after treatment for 24, 48, and 72 h, respectively. After treatment with different concentrations of genistein (0, 25, 50, and 100 µM) for 48 h, the early apoptotic cells in HCT-116 increased from 1.99% ± 0.55% to 6.78% ± 2.12%, 23.16% ± 3.87%, and 36.99% ± 3.76%, respectively. The same concentrations of genistein increased the early apoptotic cells in LoVo from 2.56% ± 1.42% to 3.21% ± 1.52%, 18.22% ± 3.56%, and 23.56% ± 3.02%, respectively. Moreover, genistein increased the mRNA and protein levels of Bax, while it inhibited the phosphorylation of Akt in HCT-116 cells. CONCLUSION: Genistein inhibited cell proliferation and induced apoptosis of colorectal cancer cells. Genistein induced the mitochondrial pathway of apoptosis in HCT-116 cells by inhibiting phosphorylation of Akt.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Neoplasias Colorretais/tratamento farmacológico , Genisteína/farmacologia , Mitocôndrias/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Neoplasias Colorretais/enzimologia , Neoplasias Colorretais/genética , Neoplasias Colorretais/patologia , Relação Dose-Resposta a Droga , Células HCT116 , Humanos , Concentração Inibidora 50 , Mitocôndrias/enzimologia , Mitocôndrias/patologia , Fosforilação , Transdução de Sinais/efeitos dos fármacos , Fatores de Tempo , Regulação para Cima , Proteína X Associada a bcl-2/genética , Proteína X Associada a bcl-2/metabolismo
10.
Zhongguo Ying Yong Sheng Li Xue Za Zhi ; 32(3): 279-282, 2016 Mar 08.
Artigo em Chinês | MEDLINE | ID: mdl-29931892

RESUMO

OBJECTIVE: This study aimed to construct a large conductance calcium activated potassium channel α (BKCa) subunit plasmid with two tags by the overlapping PCR technique to set up a steady base for future ion channel study. METHODS: Based on the existing coding BKCa channel α subunit expression plasmid pcDNA3.1-hSlo, we constructed a double-tag expression plasmid, namely, pcDNA3.1-Flag-hSlo-GFP (Flag-hSlo-GFP). RESULTS: Flag tag was inserted into the S1-S2 extracellular loop of BKCa channel α subunit, and GFP tag was connected to the C-terminus of BKCa channel α subunit. Sequence of the constructed plasmid was confirmed successful. CONCLUSIONS: The expression plasmid Flag-hSlo-GFP was constructed successfully with overlapping PCR. Overlapping PCR is a valuable method for amplifying long size genes.


Assuntos
Subunidades alfa do Canal de Potássio Ativado por Cálcio de Condutância Alta/genética , Plasmídeos , Reação em Cadeia da Polimerase
11.
Artigo em Chinês | MEDLINE | ID: mdl-30146863

RESUMO

Objective: To evaluate the molluscicidal effect of the chlorosalicylicamide sustained-release granules (LDS-SRG) on Oncomelania hupensis. Methods: Seven effective concentrations or dosages of LDS-SRG, 0.1, 0.2, 0.4, 0.8, 1.6, 3.2 and 6.4 mg/L (for immersion test) or g/m2(for spraying test), were prepared from the original 5% and 10% concentrations or dosages in the laboratory. In the immersion test, each concentration of LDS-SRG was incubated with 3 packs of snails(30 snails in each pack), and each pack was taken for snail counting at 24, 48 and 72 h respectively. In the spraying test, each dosage of LDS-SRG was applied to 200 snails, and the snail mortality was calculated in 50 randmoly collected snails on days 3 and 7, and in the whole on day 14 after administration. In the field immersion test, LDS-SRG at concentrations of 0.4, 0.8 and 1.6 g/m3 was incubated with 6 packs of snails (30 snails in each pack), and each 2 packs were taken at 24, 48, and 72 h to calculate the snail mortality. In the field spraying test, 0.8, 1.6 and 3.2 g/m2 LDS-SRG was sprayed in 3 snail-positive ditches (~100 m2), and 10 boxes of snails were selected in each ditch on days 3, 7 and 14 to calculate the snail mortality. The 50% wettable powder of niclosamide ethanolamine salt (WPN) with effective concentrations or dosages of 1.0 mg/L (or g/m2 and g/m3) was used as the positive control. Fresh water served as the blank control. Results: In the labratory immersion test using the original concentration of 5%, both 0.1-6.4 mg/L LDS-SRG for 72 h and 1.6-6.4 mg/L LDS-SRG for 48 h caused 100% mortality; and the concentration lethal to 50% (LC50) at 24, 48 and 72 h was 0.70, 0.01 and 0.01 mg/L respectively. When using the original concentration of 10%, both 0.1-6.4 mg/L LDS-SRG for 72 h and 0.2-6.4 mg/L LDS-SRG for 48 h caused 100% mortality; and the LC50 at 24, 48 and 72 h was 0.15, 0.01 and 0.01 mg/L respectively. The labratory spraying test showed that 7-day administration of 1.6 and 6.4 g/m2 LDS-SRG as well as 14-day administration of 3.2 and 6.4 g/m2 LDS-SRG prepared from 5% dosage, resulted in a snail mortality>95%, with the LD50 on days 3, 7 and 14 being 0.06, 0.16, and 0.18 g/m2; 14-day administration of 1.6 g/m2 LDS-SRG as well as 7-day administration of 6.4 g/m2 LDS-SRG prepared from 10% dosage, resulted in a snail mortality>95%, with the LD50 on days 3, 7 and 14 being 3.29, 0.75, and 0.16 g/m2. The mortality by various dosages of LDS-SRG prepared from 5% dosage was significantly higher than that of the control group (P<0.05). In the field immersion test, the snail mortality by 1.6 g/m3 LDS-SRG prepared from 5% and 10% concentrations for 72 h was 96.43% and 98.21% respectively (P>0.05 versus the control group). In the field spraying test, the snail mortality by 3.2 g/m2 LDS-SRG prepared from 5% dosage for 3, 7 and 14 days was 93.99%, 91.18% and 86.48% respectively, and that from 10% dosage was 94.95%, 93.50% and 85.43%, all significantly higher than that of the control group (82.83%, 72.38% and 48.38%)(P<0.05); the snail mortality by 0.8 g/m2 LDS-SRG prepared from 5% dosage for 14 days(66.51%) and that by 1.6 g/m2 LDS-SRG prepared from 5% dosage for 3 days(84.61%) were both significantly higher than that by 10% LDS-SRG(20.13% and 43.06%) (P<0.05). Conclusion: The 5% and 10% LDS-SRG used separately in the immersion test and the spraying test both meet the requirements of the national standard of Efficacy Test Methods and Evaluation of Molluscicide for Pesticide Registration.


Assuntos
Preparações de Ação Retardada , Moluscocidas , Animais , Água Doce , Niclosamida , Caramujos
12.
J Asian Nat Prod Res ; 17(12): 1213-9, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26654567

RESUMO

Euphorpekone A (1) and euphorpekone B (2), two new diterpenoids, 3ß-hydroxy-25-methyloxylanosta-8,23-diene, a new triterpenoid (3), together with a known triterpenoid, 3ß,25-dihydroxylanosta-8,23-diene (4), were isolated from Euphorbia pekinensis Rupr. Their structures were elucidated on the basis of UV, IR, 1D ((1)H, (13)C, NOE) and 2D ((1)H-(1)H COSY, HSQC, HMBC) NMR, HR-ESI-MS, X-ray diffraction analysis, and CD method.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Diterpenos/isolamento & purificação , Euphorbia/química , Triterpenos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Diterpenos/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Triterpenos/química , Triterpenos/farmacologia
13.
Pharm Biol ; 2013 Dec 20.
Artigo em Inglês | MEDLINE | ID: mdl-24359236

RESUMO

Abstract Context: Formononetin, an isoflavone, can inhibit the proliferation of cancer cells, including those of the prostate. However, its antitumor mechanism remains unclear. Aim: To investigate whether the insulin-like growth factor 1 (IGF-1)/insulin-like growth factor 1 receptor (IGF-1 R) signaling pathway mediates the formononetin antitumor effect on prostate cancer cells. Materials and methods: The viability of PC-3 cells was measured by MTT assay 48 h after formononetin treatment (25, 50 and 100 µM). Formononetin-induced cell apoptosis was measured by Hoechst 33258 staining and flow cytometry. Expression of Bax mRNA was detected by real-time PCR, and the expression levels of Bax and IGF-1 R proteins were detected by western blots. Results: At concentrations >12.5 µM, formononetin significantly inhibited the proliferation of human prostate cancer cells. Formononetin increased Bax mRNA and protein expression levels and decreased the expression levels of pIGF-1 R protein in a dose-dependent manner. Conclusion: High concentrations of formononetin-induced apoptosis in androgen-independent prostate cancer cells through inhibition of the IGF-1/IGF-1 R pathway.

14.
Zhonghua Xin Xue Guan Bing Za Zhi ; 41(8): 683-6, 2013 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-24225241

RESUMO

OBJECTIVE: To investigate the relationship between blood pressure variability (BPV) and left ventricular diastolic function in patients with essential hypertension. METHODS: Left ventricular diastolic function of 252 hypertensive patients were assessed by early (E) diastolic transmitral flows to early diastolic mitral annular velocity (Ea) (E/Ea) ratio derived from Doppler echocardiography. Patients were divided into two groups according to normal left ventricular diastolic function group (E/Ea<15, n = 168) and left ventricular diastolic dysfunction group (E/Ea ≥ 15, n = 84). All patients were monitored by ambulatory blood pressure. Standard deviation (SD) and coefficient of variation (CV) of blood pressure were calculated as the BPV. Relationship between BPV and left ventricular diastolic function were analyzed by multivariate logistic regression analysis. RESULTS: All-day average diastolic blood pressure(DBP), the day systolic blood pressure (SBP), night SBP, night DBP, SBPSD, DBPSD and DBPCV in the left ventricular diastolic dysfunction group were significantly higher than in the normal diastolic function group (all P < 0.05). Multivariate logistic regression analysis showed that left ventricular diastolic dysfunction was associated with SBPSD (OR:1.126, 95%CI:1.054-1.203, P < 0.01), SBPCV (OR:1.127, 95%CI:1.036-1.225, P < 0.01) in this patient cohort. CONCLUSION: High variability of SBP is correlated with left ventricular diastolic dysfunction in hypertensive patients.


Assuntos
Pressão Sanguínea/fisiologia , Hipertensão/fisiopatologia , Função Ventricular Esquerda/fisiologia , Adulto , Idoso , Diástole/fisiologia , Hipertensão Essencial , Feminino , Humanos , Modelos Logísticos , Masculino , Pessoa de Meia-Idade
15.
Zhonghua Nan Ke Xue ; 19(5): 398-402, 2013 May.
Artigo em Chinês | MEDLINE | ID: mdl-23757959

RESUMO

OBJECTIVE: To study the changes in the activities of carbon monoxide (CO) and heme oxygenase 2 (HO-2) in ED rats with hyperhomocysteinemia (HHcy). METHODS: This study included 40 male Wistar rats weighing 280 - 310 g, 10 as normal controls (group A). HHcy models were made in the other 30 by giving 3% methionine for 4 weeks, and then divided into groups B, C and D. The rats in group B continued to be fed with 3% methionine, those in group C were treated with betaine hydrochloride, and those in group D were given zinc porphyrin IX at 45 micromol per kg per d. Penile erections of the rats were recorded, and 4 weeks later, all were killed for determination of the levels of homocysteine (Hcy) in the blood plasma and the activities of CO and HO-2 in the corpus cavernosum of the penis. RESULTS: The level of plasma Hcy, penile erection frequency and the content of CO in the corpus cavernosum were (12.55 +/- 0.82) micromol/L, (1.88 +/- 0.05) times and (10.55 +/- 1.73) micromol/L in group A, the Hcy level significantly higher while the penile erection frequency and CO content remarkably lower than in group B ([25.01 +/- 0.94] micromol/L, [0.70 +/- 0.05] times and [9.51 +/- 1.52] micromol/L, P < 0.05 or P < 0.01), with a negative correlation between the level of Hcy and that of CO and HO-2 (P < 0.01). Compared with group B, the three parameters were all significantly increased in C ([14.37 +/- 0.47] micromol/L, [1.18 +/- 0.08] times and [10.36 +/- 1.56] micromol/L, all P < 0.05 or P < 0.01). CONCLUSION: Decreased expressions of CO and HO-2 in the corpus cavernosum of the penis may result in ED in HHcy rats. Betaine can reduce the Hcy level in the blood plasma and CO content in the corpus cavernosum, which might be one of the mechanisms of its action on ED with HHcy.


Assuntos
Disfunção Erétil/sangue , Heme Oxigenase (Desciclizante)/sangue , Homocisteína/sangue , Hiper-Homocisteinemia/metabolismo , Pênis/metabolismo , Animais , Monóxido de Carbono/sangue , Disfunção Erétil/metabolismo , Hiper-Homocisteinemia/sangue , Masculino , Ratos , Ratos Wistar
16.
Asian Pac J Cancer Prev ; 13(8): 4037-43, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23098513

RESUMO

Despite progress in elucidating mechanisms associated with colorectal cancer and improvement of treatment methods, it remains a frequent cause of death worldwide. New and more effective therapies are therefore urgently needed. Recent studies have shown that immunogenicity of whole ovarian tumor cells and subsequent T cell response were potentiated by oxidation modification with hypochlorous acid (HOCl) in vitro and ex vivo. These results prompted us to investigate the protective antitumor response with an HOCl treated CT26 colorectal cancer cell vaccine in an in vivo mouse model. Administration of HOCl modified vaccine triggered robust antitumor immunity to autologous tumor cells in mice and prolonged survival period significantly. In addition, increased necrosis and apoptosis were found in tumor tissue from the oxidation group. Interestingly, ELISPOT assays showed that specific T cell responses were not elicited in response to the immunizing cellular antigen, in contrast to raising sera antibody titer and antibody binding activity shown by ELISA assay and flow cytometry. Further evaluation of the mechanisms underlying HOCl modified vaccine mediated humoral immunity highlighted the role of antibody-dependent cell-mediated cytotoxicity. These results combined with previous studies suggest that HOCl oxidation modified whole cell vaccine has wide applicability as a cancer vaccine because it can target both T cell- and B cell-specific responses. It may thus represent a promising approach for the immunotherapy of colorectal cancer.


Assuntos
Adenocarcinoma/prevenção & controle , Vacinas Anticâncer/uso terapêutico , Neoplasias do Colo/prevenção & controle , Citotoxicidade Imunológica/imunologia , Modelos Animais de Doenças , Ácido Hipocloroso/farmacologia , Imunoterapia , Adenocarcinoma/imunologia , Adenocarcinoma/patologia , Animais , Citotoxicidade Celular Dependente de Anticorpos , Apoptose , Western Blotting , Linhagem Celular Tumoral , Proliferação de Células , Neoplasias do Colo/imunologia , Neoplasias do Colo/patologia , Feminino , Citometria de Fluxo , Técnicas Imunoenzimáticas , Camundongos , Camundongos Endogâmicos BALB C , Oxidantes/farmacologia , RNA Mensageiro/genética
17.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 43(2): 210-3, 225, 2012 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-22650033

RESUMO

OBJECTIVE: To investigate the prevalence of four common neuropsychiatric disorders in Tibet, with an aim to providing information support to health planning. METHODS: The survey was carried out in four regions of Tibet. The sampling strategy was adapted from that of a national psychiatric epidemiological survey in China in 1982 and 1993. The Neurosis Screening Inventory, Screening Inventory for Alcohol Dependence and Related Problems, Child Intelligence Screening Inventory, and a questionnaire for the Detection of Epileptic Seizures were administered to the respondents through face to face interview. Those with a positive response and 10% of those with a negative response were further interviewed with the Structured Clinical Interview for DSM-IV Axis I Disorders (research version) (SCID-I ). Anxiety disorders and alcohol used disorders were diagnosed according to the American Psychiatric Association: Diagnostic and Statistical Manual of Mental Disorders (4th edition) (DSM-IV). Hysteria and mental retardation were diagnosed according to the International Classification of Diseases, 10th edition (ICD-10), and the Chinese Classification of Mental Disorders, 3rd edition (CCMD-3). RESULTS: The point prevalence of neuroses, alcohol-related disorders, mental retardation and epilepsy was 2. 56%, 4. 06%, 0. 28% and 0. 68%, respectively. The lifetime prevalence of neuroses, alcohol-related disorders, mental retardation and epilepsy was 2. 62%, 4. 24%, 0. 28% and 0.72%, respectively. CONCLUSION: Alcohol-related disorders and neuroses are the two common mental health problems in Tibet. Mental retardation and epilepsy are the two serious neuropsychiatric disorders affecting Tibetan children and adolescence. These disorders should be identified as priorities in the reginonal health planning in Tibet.


Assuntos
Transtornos Relacionados ao Uso de Álcool/epidemiologia , Epilepsia/epidemiologia , Deficiência Intelectual/epidemiologia , Transtornos Neuróticos/epidemiologia , Adolescente , Adulto , Feminino , Inquéritos Epidemiológicos , Humanos , Masculino , Pessoa de Meia-Idade , Prevalência , Amostragem , Inquéritos e Questionários , Tibet/epidemiologia , Adulto Jovem
18.
Oncol Rep ; 28(1): 225-31, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22552608

RESUMO

Despite progress made in the treatment of hepatocellular carcinoma (HCC), there is no curable treatment. Novel therapies are therefore needed. In our previous study on the design and synthesis of a small molecular inhibitor targeting Aurora kinase, we discovered a novel thienopyridine derivative compound (1g, TP58) which displayed the most potent and relatively specific inhibition of the proliferation of HepG2 human hepatoma cells in vitro. However, the molecular mechanism remains to be elucidated. Herein, in vitro and in vivo studies were conducted to further verify its antitumor activity against HCC. cDNA microarray and two-dimensional protein gel electrophoresis technology were utilized to elucidate the mechanism of HCC-specific inhibition of TP58. Flow cytometry analysis displayed that TP58 can significantly induce G0/G1 arrest in HepG2 cells. Sixteen genes involved in cell cycle regulation were found to be dysregulated following TP58 treatment using microarray technology. Nine proteins whose expression was altered (corresponding to 10 spots identified as differentially expressed) were identified by proteomic analysis. Further study showed that TP58 can modulate the expression of some liver-enriched transcription factors (LETFs) and liver-specific marker genes, such as hepatic nuclear factor (HNF-4) and α-fetoprotein (AFP). These findings may help explain the mechanism of HCC-specific antitumor activity of TP58 and provide some useful insight for anti-HCC drug design and future use of thienopyridine derivatives in HCC therapy.


Assuntos
Antineoplásicos/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Piridinas/farmacologia , Tiofenos/farmacologia , Animais , Antineoplásicos/uso terapêutico , Apoptose , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Proliferação de Células/efeitos dos fármacos , Eletroforese em Gel Bidimensional , Feminino , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Proteínas de Choque Térmico HSP27/genética , Proteínas de Choque Térmico HSP27/metabolismo , Células Hep G2 , Humanos , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Camundongos , Camundongos Nus , Piridinas/uso terapêutico , Tiofenos/uso terapêutico , Fatores de Transcrição/metabolismo , Carga Tumoral/efeitos dos fármacos , Ensaios Antitumorais Modelo de Xenoenxerto
19.
Artigo em Chinês | MEDLINE | ID: mdl-22164500

RESUMO

A total of 80 cases of advanced schistosomiasis were selected and divided into an experiment group and a control group, 40 cases each group, by the random sampling method. The patients in the experiment group were administered with Jian-gan-le, and the patients in the control group received compound purple granules. In the experiment group, the curative rate was 25.0%, the improving rate was 70.0%, the inefficacy rate was 5%, and the efficiency rate was 95.0%. In the control group, the curative rate was 12.5%, the improving rate was 75%, the inefficacy rate was 12.5%. There was no statistic difference between the 2 groups (P all > 0.05). The expense was cheaper in the experiment group than in the control group.


Assuntos
Medicamentos de Ervas Chinesas/administração & dosagem , Esquistossomose/tratamento farmacológico , Efeitos Psicossociais da Doença , Medicamentos de Ervas Chinesas/economia , Feminino , Humanos , Masculino , Fitoterapia/economia , Esquistossomose/economia , Resultado do Tratamento
20.
Artigo em Chinês | MEDLINE | ID: mdl-22164847

RESUMO

OBJECTIVE: To explore the causes of infected Oncomelania snails and the sources of infection of schistosomiasis in marshland and lake regions of Jingzhou City, so as to provide the evidence for the establishment of control strategy. METHODS: The snail environments in villages with or without cattle in Gong'an and Jianli counties, Hubei Province were selected, the snail status, infection status of people and livestock and wildlife reservoir host (mice), as well as the contamination status of wild faeces were surveyed, and the infectivity of water in investigated villages without cattle were detected by sentinel mice. The correlation between the densities of infected snails and positive faeces were tested by the rank correlation method. RESULTS: In villages without cattle, there were no positive faeces and infected sentinel mice discovered, while in the villages with cattle, 374 pieces of wild faeces were collected, the densities of wild faeces were 0.02 - 0.29 pieces/100 m2, and those of the positive ones were 0 - 0.01 pieces/100 m2, and the densities of infected snails were 0.001 - 0.040 snails /0.1 m2. The distribution of infected snails was consistent with that of the positive faeces, but the correlation coefficient between their densities had no statistical significance (r(s) = 0.123 5, P > 0.05). The average infection rates of human in villages with cattle inside embankment of Gong'an and Jianli counties were 2.87% and 1.37%, respectively, while that of the villages outside embankment of Gong'an County was 1.23%, and all the infection rates of cattle were 0. No infected wild mice were discovered. CONCLUSIONS: Human and cattle are the main sources of schistosome infection in the local areas, the possibility of wild mice as source of infection is low, and cattle is an important cause of infected snails in marshland and lake regions in Jingzhou City.


Assuntos
Doenças dos Bovinos/parasitologia , Reservatórios de Doenças/parasitologia , Lagos/parasitologia , Doenças dos Roedores/parasitologia , Esquistossomose/parasitologia , Esquistossomose/veterinária , Caramujos/parasitologia , Animais , Bovinos , Doenças dos Bovinos/epidemiologia , China/epidemiologia , Fezes/parasitologia , Humanos , Camundongos , Doenças dos Roedores/epidemiologia , Saúde da População Rural , Esquistossomose/epidemiologia , Áreas Alagadas
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