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1.
Clin Respir J ; 18(5): e13756, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38725310

RESUMO

INTRODUCTION: This meta-analysis sought to investigate the effect of neoadjuvant chemotherapy (NACT) combined with surgery in patients with nonsmall cell lung cancer (NSCLC). METHODS: With time span from January 2010 to December 2022, PubMed, Web of Science and Embase, China National Knowledge Infrastructure, and WanFang databases were searched for randomized controlled trials on comparison between NACT combined with surgery and surgery alone in patients with NSCLC. Then a meta-analysis was performed in accordance with Preferred Reporting Items for Systematic reviews and Meta-Analyses (PRISMA) guidelines. RESULTS: A total of 1511 studies were retrieved and 12 were finally included. Meta-analysis results showed that compared with surgery alone, a combination of NACT and surgery was associated with higher treatment response rate (odds ratio, OR = 2.459, 95% confidence interval, CI [1.785, 3.388], P < 0.001), 1-year survival rate (OR = 2.185, 95% CI [1.608, 2.970], P < 0.001), and 3-year survival rate (OR = 2.195, 95% CI [1.568, 3.073], P < 0.001) and lower levels of intraoperative blood loss (standardized mean difference, SMD = -0.932, 95% CI [-1.588, -0.275], P = 0.005) and length of hospital stay (SMD = -0.481, 95% CI [-0.933, -0.028], P = 0.037). CONCLUSION: NACT combined with surgery is superior to surgery alone in the treatment of NSCLC and can promote postoperative recovery. Collectively, such combination is a safe and effective treatment for patients with NSCLC.


Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Terapia Neoadjuvante , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Carcinoma Pulmonar de Células não Pequenas/cirurgia , Carcinoma Pulmonar de Células não Pequenas/patologia , Carcinoma Pulmonar de Células não Pequenas/mortalidade , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/cirurgia , Neoplasias Pulmonares/patologia , Neoplasias Pulmonares/mortalidade , Neoplasias Pulmonares/terapia , Terapia Neoadjuvante/métodos , Pneumonectomia/métodos , Taxa de Sobrevida , Resultado do Tratamento , Quimioterapia Adjuvante/métodos , Ensaios Clínicos Controlados Aleatórios como Assunto , Tempo de Internação/estatística & dados numéricos , Feminino , Terapia Combinada
2.
Adipocyte ; 12(1): 2266147, 2023 12.
Artigo em Inglês | MEDLINE | ID: mdl-37795948

RESUMO

Exercise is a universally acknowledged and healthy way to reducing body weight. However, the roles and mechanisms of exercise on metabolism of adipose tissue remain largely unclear. Adipose tissues include white adipose tissue (WAT), brown adipose tissue (BAT) and beige adipose tissue (BeAT). The main function of WAT is to store energy, while the BAT and BeAT can generate heat and consume energy. Therefore, promotion of BAT activation and WAT browning contributes to body weight loss. To date, many studies have suggested that exercise exerts the potential regulatory effects on BAT activation and WAT browning. In the present review, we compile the evidence for the regulatory effects of exercise on BAT activation and WAT browning and summarize the possible mechanisms whereby exercise modulates BAT activation and WAT browning, including activating sympathetic nervous system (SNS) and promoting the secretion of exerkines, with special focus on exerkines. These data might provide reference for prevention or treatment of obesity and the related metabolic disease through exercise.


Assuntos
Tecido Adiposo Marrom , Termogênese , Humanos , Tecido Adiposo Marrom/metabolismo , Tecido Adiposo Branco/metabolismo , Obesidade/metabolismo , Peso Corporal
3.
Front Psychol ; 14: 1199285, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38274673

RESUMO

Introduction: Parenting and peer victimization (PV) are crucial for adolescent drinking. To further explore the cause of adolescent drinking, the present study investigated the role of PV and personal growth initiative (PGI) in the relationship between parental corporal punishment (PCP) and adolescent drinking. Methods: Present study build moderated mediation models to test the hypothesis, and detailed analysis of gender differences was conducted on the models. The data were collected in a cross-sectional questionnaire study with n = 1,007 adolescents (mean age = 13.16 years, 51.84% girls, n = 522). Results: Model analysis showed that: (1) PV totally mediated the relationship between PCP and adolescent girls' drinking behavior; (2) The positive association between PV and drinking was only significant for girls with low PGI. Discussion: These findings underscore the importance of the protective effect of a personality trait characterized by spontaneous self-promotion on adolescent girls' drinking.

4.
J Cardiothorac Surg ; 17(1): 324, 2022 Dec 19.
Artigo em Inglês | MEDLINE | ID: mdl-36536456

RESUMO

BACKGROUND: Multiple ground-glass nodules (mGGNs) in the lung has been defined as synchronous multiple primary lung cancer (SMPLC), it is has been very difficult challenging to differentiate SMPLC from intrapulmonary metastases, and its treatment remains controversial. CASE PRESENTATION: We report a case simultaneously involving mGGNs and lung adenocarcinoma harboring primary EGFR-T790M mutation, in which the patient underwent the radical resection of lesions in the left upper lung, and continued the osimertinib treatment for the residual mGGNs in all lobes of the right lung. These mGGNs displayed different responses to osimertinib. CONCLUSIONS: We reported a successful strategy on the postoperative treatment for mGGNs. For those that cannot be completely resected, the chemotherapy, radiotherapy, stereotactic body radiation therapy, immunotherapy and targeted therapy have been performed instead. The EGFR-TKI therapy strategy showed significant advantages, but how to achieve even better therapeutic effect needs more researches.


Assuntos
Adenocarcinoma de Pulmão , Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Humanos , Neoplasias Pulmonares/patologia , Carcinoma Pulmonar de Células não Pequenas/patologia , Receptores ErbB/genética , Pneumonectomia , Mutação , Inibidores de Proteínas Quinases/uso terapêutico , Compostos de Anilina/uso terapêutico
5.
Artigo em Inglês | MEDLINE | ID: mdl-36276870

RESUMO

Background: Molecular categorization of lung cancer in medical care is becoming increasingly important on a regular basis. One of the molecular classifications of NSCLC (early-stage NSCLC) supports that tumors of different biological varieties differ in terms of their genomes and clinical characteristics. Methods: Based on published immune cell signatures and early-stage NSCLC gene expression data including cancer genome maps, we used consensus cluster analysis to identify immune molecular subtypes associated with early-stage NSCLC expression subtypes. These subtypes were correlated with early-stage NSCLC expression subtypes. Next, applying a wide range of statistical techniques, we evaluated the link between molecular subtypes and clinical features, immunological microenvironment, and immunotherapy reactivity. Molecular subtypes were defined as a classification of cancerous cells. Results: Multiple RNAseq cross-platform datasets of immune genes were used to identify two molecular subtypes (C1 and C2) of NSCLC, with C1 showing a more favorable prognosis than C2. The results were validated on the CSE datasets. In terms of clinical characteristics, C2 subtype samples with a worse prognosis showed a more advanced tumor stage and higher mortality. C2 showed immuno-infiltrative characteristics but had depletion of T-cells. Biological functions such as EMT were enriched on C2. A low TIDE score in C1 indicated that C1 samples could benefit from taking immunotherapy. C2 were more susceptible to standard chemotherapeutic treatments such paclitaxel, cisplatin, sorafenib, crizotinib, and erlotinib. Conclusion: According to our findings, early-stage NSCLC patients may benefit from receiving treatment with immune checkpoint blockade therapy.

6.
Sci Data ; 9(1): 465, 2022 08 02.
Artigo em Inglês | MEDLINE | ID: mdl-35918334

RESUMO

The dataset of simultaneous 64-channel electroencephalography (EEG) and high-speed eye-tracking (ET) recordings was collected from 31 professional athletes and 43 college students during alertness behavior task (ABT) and concentration cognitive task (CCT). The CCT experiment lasting 1-2 hours included five sessions for groups of the Shooting, Archery and Modern Pentathlon elite athletes and the controls. Concentration targets included shooting target and combination target with or without 24 different directions of visual distractors and 2 types of music distractors. Meditation and Schulte Grid trainings were done as interventions. Analysis of the dataset aimed to extract effective biological markers of eye movement and EEG that can assess the concentration level of talented athletes compared with same-aged controls. Moreover, this dataset is useful for the research of related visual brain-computer interfaces.


Assuntos
Eletroencefalografia , Tecnologia de Rastreamento Ocular , Atletas , Atenção , Movimentos Oculares , Humanos
7.
Xenobiotica ; 51(12): 1389-1399, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34806938

RESUMO

1. 8-methylene-tert-butylamine-3',5,7-trihydroxy-4'-methoxyflavanone (MTBH), a novel hesperidin derivative, has potential in the prevention of hepatic disease, however, its effects on cytochrome P450 isoforms (CYP450s) remains unexplored. The purpose was to investigate the effects of MTBH on the mRNA, protein levels, and activities of six CYP450s (1A2, 2C11/9, 2D2/6, 3A1/4, 2C13/19, and 2E1) in vitro and in vivo.2. In vitro study, rat and human liver microsomes were adopted to elucidate the inhibitory effect of MTBH on six CYP450s using probe drugs. In vivo study, Sprague-Dawley male rats were treated with MTBH (25, 50, or 100 mg/kg for 28 consecutive days), phenobarbital (80 mg/kg for 12 consecutive days), or 0.5% CMC-Na solution (control group) by intragastric administration, then, the mRNA, protein levels and activities of liver CYP450s were analysed by real-time PCR, western blotting and probe-drug incubation systems, respectively.3. The in vitro study indicated that MTBH inhibits the activities of CYP3A1/4 and CYP2E1 in rat and human liver microsomes. In vivo data showed that MTBH inhibits mRNA, protein levels, and activities of CYP3A1 and CYP2E1 in medium- and high-dose MTBH groups.4. MTBH has the potential to cause drug-drug interactions when co-administered with drugs that are metabolised by CYP3A1/4 and CYP2E1.


Assuntos
Hesperidina , Animais , Cromatografia Líquida de Alta Pressão , Sistema Enzimático do Citocromo P-450 , Hesperidina/farmacologia , Fígado , Masculino , Microssomos Hepáticos , Isoformas de Proteínas , Ratos , Ratos Sprague-Dawley , Espectrometria de Massas em Tandem
8.
Oncol Rep ; 45(5)2021 05.
Artigo em Inglês | MEDLINE | ID: mdl-33864661

RESUMO

The present study aimed to investigate the role of partner of NOB1 homolog (PNO1) in esophageal cancer (EC). The expression levels of PNO1 in EC were primarily analyzed using data obtained from databases. PNO1 expression was also knocked down in EC cells (Eca­109 and TE1) to determine the biological effects of PNO1 on tumorigenesis in vitro and in vivo. In addition, possible downstream targets of PNO1 in EC were identified. The expression levels of PNO1 were upregulated in the tumor tissues compared with that noted in normal tissues. Moreover, the knockdown (KD) of PNO1 suppressed cell proliferation, migration and invasion, and promoted cell apoptosis (P < 0.05). Furthermore, the protein expression levels of AKT1, Twist, Myc, mTOR, matrix metalloproteinase 2 (MMP2), nuclear factor (NF)­κB p65 and ß­catenin 1 (CTNNB1) were downregulated following the KD of PNO1 in Eca­109 cells (P < 0.05). In addition, the overexpression of CTNNB1 reversed the effects of PNO1 KD in Eca­109 cells (P < 0.05). In conclusion, the findings of the present study suggest that PNO1 promotes EC progression by regulating AKT1, Twist, Myc, mTOR, MMP2, NF­κB p65 and CTNNB1 expression.


Assuntos
Carcinogênese/genética , Neoplasias Esofágicas/genética , Regulação Neoplásica da Expressão Gênica , Proteínas de Ligação a RNA/metabolismo , Animais , Apoptose/genética , Carcinogênese/patologia , Linhagem Celular Tumoral , Proliferação de Células/genética , Conjuntos de Dados como Assunto , Progressão da Doença , Neoplasias Esofágicas/diagnóstico , Neoplasias Esofágicas/patologia , Esôfago/patologia , Feminino , Humanos , Camundongos , Estadiamento de Neoplasias , Proteínas de Ligação a RNA/genética , RNA-Seq , Regulação para Cima , Ensaios Antitumorais Modelo de Xenoenxerto
9.
J Thorac Dis ; 11(10): 4159-4168, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31737299

RESUMO

BACKGROUND: To investigate the feasibility and indications of video-assisted thoracic surgery (VATS) in thymoma resection. METHODS: The clinical data of 103 patients undergoing thymoma resection via different approaches [including conventional lateral thoracotomy approach (LTA) in 41 cases, median sternotomy approach (MSA) in 40 cases, and right-sided VATS in 22 cases] were analyzed. Among them, 59, 13, 25, and 6 patients were in Masaoka stage I, II, III, and IV, respectively. Myasthenia gravis (MG) was also found in 54 cases. The patients were followed up for postoperative survival and the improvement in MG. The prognostic indicators of patients undergoing thymoma resection via different surgical approaches (i.e., LTA, MSA, and VATS) were statistically analyzed. RESULTS: Eight of 103 patients died. Six patients underwent unilateral sacral nerve resection, among whom 4 patients developed respiratory dysfunction, and 3 died. Two patients died of MG after surgery, 1 patient died of tumor recurrence and metastasis, 1 patient died of heart disease, and the cause of death was unknown in the remaining patient. The drainage time was shorter in VATS group than in open groups, along with smaller tumor size. The VATS group also had shorter hospital stay in the whole series and the subgroup without accompanying MG. The improvement in MG showed no significant difference among the three surgical groups. Both 5- and 10-year survival rates were 91% in the entire cohort. CONCLUSIONS: VATS is like a conventional surgeries for improving MG in thymoma patients with accompanying MG. VATS resection can still be considered for thymoma that only invades the mediastinal pleura. For thymomas that have intact capsules and have not invaded mediastinal pleura, MSA surgery shall be performed to ensure patient safety if the anteroposterior diameters of the tumors are large and the masses have produced severe compression of the innominate vein, even if the tumors are still in the Masaoka stage II. For thymomas with large left-to-right diameters and with most parts of the tumors located in the left thoracic cavity, a left-sided approach (either VATS or an open approach) may be used in the absence of MG; if MG accompanies the condition, an MT approach or a bilateral VATS may be considered. In patients with unilateral pericardial phrenic nerve and/or local pericardial involvement, right-sided VATS thymectomy may be considered for thymomas located at the right side and bilateral VATS surgery can be performed for tumors located at the left side. In summary, VATS is feasible for the treatment of thymoma complicated by MG. VATS can be performed in patients with Masaoka stage I, II and (a certain portion of) III thymoma; for some patients with Masaoka stage II thymoma, especially those with compression of the innominate vein, the use of VATS should be cautious.

10.
Zhonghua Nan Ke Xue ; 25(3): 248-256, 2019 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-32216244

RESUMO

OBJECTIVE: To compare the differentially expressed proteins in mice with kidney-yang deficiency and those with kidney-yin deficiency induced by hydrocortisone, and explore the similar and different material bases of male infertility caused by the two types of kidney deficiency. METHODS: Thirty Kunming mice were equally randomized into a normal control, a kidney-yang deficiency and a kidney-yin deficiency group. The animals of the normal control group were injected intraperitoneally with normal saline at 0.2 ml qd for 7 days, while those of the latter two groups with hydrocortisone at 25 mg/kg/d for 10 days and 50 mg/kg/d for 7 days, respectively, for establishment of kidney-yang deficiency and kidney-yin deficiency models. Then the pathological changes in the testicular tissue of the mice were observed by HE staining and the differentially expressed proteins were compared among different groups using isobaric tags for relative and absolute quantitation (iTRAQ) and the bioinformatics method. RESULTS: Sod1 was found to be a reproduction-related node protein differentially expressed in the testis tissues of the two types of kidney-deficiency mice, more highly expressed in the kidney-yin than in the kidney-yang deficiency group (P < 0.05). Five reproduction-associated node proteins were co-expressed in the testes of the two groups of kidney-deficiency mice, with significantly up-regulated expression of Rps28 and down-regulated expressions of Rpl11, Rplp2, Svs2 and Svs3a (P < 0.01). CONCLUSIONS: Sod1 may be one of the key material bases for the differentiation of male infertility caused by kidney-yang deficiency from that induced by kidney-yin deficiency, while Rps28, Rpl11, Rplp2, Svs2 and Svs3a may be the common material bases of male infertility caused by the two types of kidney deficiency.


Assuntos
Rim/fisiopatologia , Proteínas Secretadas pela Vesícula Seminal/metabolismo , Testículo/metabolismo , Deficiência da Energia Yang , Deficiência da Energia Yin , Animais , Hidrocortisona , Rim/metabolismo , Masculino , Medicina Tradicional Chinesa , Camundongos , Distribuição Aleatória , Reprodução , Superóxido Dismutase-1 , Testículo/patologia
11.
Zhonghua Nan Ke Xue ; 24(2): 156-162, 2018 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-30156077

RESUMO

OBJECTIVE: To investigate the expression of the G-protein coupled estrogen receptor (GPER) in the testis of the male mouse with kidney yin or kidney yang deficiency and its influence on the reproductive function of the mouse. METHODS: We randomized 30 six-week-old male Kunming mice into three groups of equal number: kidney yang deficiency, kidney yin deficiency, and normal control, and established the models of kidney yang deficiency and kidney yin deficiency by peritoneal injection of hydrocortisone at 50 mg/kg for 5 days and 25 mg/kg for 10 days, respectively. We observed the behavioral changes of the mice using the elevated plus-maze, exhaustive swimming and field experiment, examined the semen quality with the automatic sperm quality analyzer, calculated the average number of the offspring, measured the serum testosterone (T) and estradiol (E2) levels and T/E2 ratio by Roche electrochemiluminescence assay, and determined the localization and expression of GPER in the testis by immunohistochemistry and immunofluorescence staining. RESULTS: Compared with the mice with kidney yin deficiency, those with kidney yang deficiency showed remarkably fewer entries into the open arm and central area (P <0.05) and shorter time of exhaustive swimming (P <0.05), but no statistically significant difference in the time spent in the open arm or the central area (P >0.05); the latter group also exhibited significant decreases in the epididymal sperm count (ï¼»7.27 ± 1.30ï¼½ vs ï¼»3.05 ± 1.06ï¼½ ×108/g, P <0.01), sperm motility (ï¼»54.15 ± 13.52ï¼½ vs ï¼»51.57 ± 8.75ï¼½ %, P <0.01) and average number of the offspring (6.46 vs 4.33, P <0.05), a slight increase in the rate of morphologically abnormal sperm (ï¼»13.42 ± 2.32ï¼½ vs ï¼»15.39 ± 2.48ï¼½ %, P >0.05), and markedly reduced serum T (ï¼»24.96 ± 6.18ï¼½ vs ï¼»16.72 ± 5.92ï¼½ ng/dl,P <0.05), E2 (ï¼»19.81 ± 4.01ï¼½ vs ï¼»15.24 ± 1.11ï¼½ pg/ml,P <0.05) and T/E2 ratio (1.41 vs 1.25, P <0.05). The expression of GPER was found in the cytoplasm of the Leydig cells, negative in the nuclei and cell membrane, significantly higher in the kidney yang than in the kidney yin deficiency group (P <0.05). CONCLUSIONS: The numbers of sperm and offspring decreased while the percentage of morphologically abnormal sperm increased in both the kidney yang and kidney yin deficiency mice, even more significantly in the former, which might be associated with the up-regulated expression of GPER in the testis of the mouse with kidney yang deficiency and consequently the reduced serum T level and T/E2 ratio.


Assuntos
Nefropatias/metabolismo , Receptores Acoplados a Proteínas G/metabolismo , Reprodução/fisiologia , Testículo/metabolismo , Deficiência da Energia Yang/metabolismo , Deficiência da Energia Yin/metabolismo , Animais , Medicamentos de Ervas Chinesas , Masculino , Camundongos , Distribuição Aleatória , Receptores de Estrogênio/metabolismo , Análise do Sêmen
12.
In Vitro Cell Dev Biol Anim ; 53(8): 744-751, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28707224

RESUMO

Several studies have indicated that microgravity can influence cellular progression, proliferation, and apoptosis in tumor cell lines. In this study, we observed that simulated microgravity inhibited proliferation and induced apoptosis in U251 malignant glioma (U251MG) cells. Furthermore, expression of the apoptosis-associated proteins, p21 and insulin-like growth factor binding protein-2 (IGFBP-2), was upregulated and downregulated, respectively, following exposure to simulated microgravity. These findings indicate that simulated microgravity inhibits proliferation while inducing apoptosis of U251MG cells. The associated effects appear to be mediated by inhibition of IGFBP-2 expression and stimulation of p21 expression. This suggests that simulated microgravity might represent a promising method to discover new targets for glioma therapeutic strategy.


Assuntos
Inibidor de Quinase Dependente de Ciclina p21/genética , Glioma/genética , Proteína 2 de Ligação a Fator de Crescimento Semelhante à Insulina/genética , Simulação de Ausência de Peso , Apoptose/genética , Linhagem Celular Tumoral , Proliferação de Células/genética , Regulação Neoplásica da Expressão Gênica , Glioma/patologia , Humanos
13.
Zhonghua Nan Ke Xue ; 22(10): 867-871, 2016 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-29278465

RESUMO

OBJECTIVE: To study the effect of Icariin on rat Leydig cells with TGF-ß1-induced injury. METHODS: We determined the optimal concentration of Icariin for protecting primarily cultured Leydig cells against TGF-ß1-induced injury by methyl thiazolyl tetrazolium assay. We detected the effects of Icariin on the secretion of estradiol (E2) and activity of aromatase in the injured Leydig cells by radioimmunoassay and Tritium water release experiment and its effect on the gap junctional intercellular communication (GJIC) between the Leydig cells by fluorescence distribution after photobleaching. RESULTS: Different concentrations of Icariin showed different degrees of protective effect on the TGF-ß1-treated Leydig cells, the effect observed at 20 µg/ml and at its optimum at 160 µg/ml. After treatment of the injured Leydig cells with Icariin at 160 µg/ml, significant improvement was observed in the E2 secretion and aromatase activity (P<0.01) as well as in the GJIC between the Leydig cells (P<0.01). CONCLUSIONS: Icariin can effectively protect rat Leydig cells against TGF-ß1-induced injury, which is largely attributed to its effects of increasing E2 synthesis, enhancing aromatase activity, and improving GJIC between Leydig cells.


Assuntos
Flavonoides/farmacologia , Junções Comunicantes , Células Intersticiais do Testículo/efeitos dos fármacos , Fator de Crescimento Transformador beta1/efeitos adversos , Animais , Aromatase/metabolismo , Comunicação Celular , Linhagem Celular , Células Cultivadas , Estradiol/metabolismo , Masculino , Ratos , Fator de Crescimento Transformador beta1/farmacologia
14.
Biol Reprod ; 92(1): 24, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25429088

RESUMO

Sertoli cells (SCs) function as "nurse cells," which play crucial roles in supporting spermatogenesis through establishing a unique and essential environment in the male reproductive tract. Given the important roles of SCs in male fertility, this study was designed to evaluate the effect of diosgenin, an aglycone of the steroidal saponin, on TM4 cell proliferation and to elucidate the possible mechanisms. We showed that diosgenin increased the proliferation of TM4 cell and primary SCs in a time- and concentration-dependent manner. Diosgenin increased cyclins D1 and E as well as CDK4/6 and CDK2 expression but inhibited P27 expression, with no significant alterations of cyclin B and cdc2 (cell division cycle 2), resulting in cell-cycle G1/S transition. Diosgenin significantly inhibited apoptosis, as reflected by decreased percentage of TUNEL-positive cells; decreased expression of Bax (Bcl-2-associated X protein), AIF (apoptosis-inducing factor), and cleaved caspases 3 and 9; and increased expression of Bcl-2 (B-cell lymphoma 2). Diosgenin induced an immediate and transient plasma membrane translocation of ESR1 and ESR2 from the nucleus, which was inhibited by the antiestrogen ICI 182 780 and PP2, an inhibitor of SRC. Moreover, ICI 182 780 and PP2 significantly inhibited diosgenin-induced cell-cycle transition and inhibition of apoptosis. Activation of extracellular regulated protein kinase (ERK)/Akt signaling was also involved in diosgenin-induced TM4 cell proliferation, which was SRC- and ESR-dependent. Furthermore, diosgenin induced late activation of nuclear ESR transcriptional activity, which in turn directly regulated cell cycle and apoptosis-related factors, such as cyclin D and Bcl-2. Taken together, the results show that diosgenin activated SRC-ESR translocation-ERK/Akt-ESR transcriptional activity, leading to cell-cycle transition and inhibition of apoptosis and thus final cell proliferation. These findings may better our understanding of the pharmacological actions of diosgenin and advance therapeutic approaches to male infertility.


Assuntos
Proliferação de Células/efeitos dos fármacos , Diosgenina/farmacologia , Receptores de Estrogênio/metabolismo , Receptores de Estrogênio/fisiologia , Células de Sertoli/efeitos dos fármacos , Ativação Transcricional/efeitos dos fármacos , Animais , Apoptose/efeitos dos fármacos , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Masculino , Transporte Proteico/efeitos dos fármacos , Ratos , Células de Sertoli/fisiologia , Regulação para Cima/efeitos dos fármacos
15.
Org Biomol Chem ; 9(23): 8195-201, 2011 Dec 07.
Artigo em Inglês | MEDLINE | ID: mdl-22027929

RESUMO

A novel chemosensor based on unsymmetrical squaraine dye (USQ-1) for the selective detection of Hg(2+) in aqueous media is described. USQ-1 in combination with metal ions shows dual chromogenic and "turn-on" fluorogenic response selectivity toward Hg(2+) as compared to Li(+), Na(+), K(+), Mg(2+), Ca(2+), Ba(2+), Al(3+), Cu(2+), Cd(2+), Mn(2+), Fe(3+), Ag(+), Pb(2+), Zn(2+), Ni(2+) and Co(2+) due to the Hg(2+)-induced deaggregation of the dye molecule. A recognition mechanism based on the binding mode is proposed based on the absorption and fluorescence changes, (1)H NMR titration experiments, ESI-MS study, and theoretical calculations.


Assuntos
Ciclobutanos/química , Mercúrio/química , Fenóis/química , Cátions Bivalentes/química , Modelos Moleculares , Estrutura Molecular
16.
Org Lett ; 13(5): 1162-5, 2011 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-21306133

RESUMO

A novel squaraine-based chemosensor SQ-1 has been synthesized, and its sensing behavior toward various metal ions was investigated by UV-vis and fluorescence spectroscopies. In AcOH-H(2)O (40:60, v/v) solution, Hg(2+) ions coordinate with SQ-1 causing a deaggregation which induces a visual color and absorption spectral changes as well as strong fluorescence. In contrast, the addition of other metals (e.g., Pb(2+), Cd(2+), Cu(2+), Zn(2+), Al(3+), Ni(2+), Co(2+), Fe(3+), Ca(2+), K(+), Mg(2+), Na(+), and Ag(+)) does not induce these changes at all. Thus SQ-1 is a specific Hg(2+) sensing agent due to the inducing deaggregation of the dye molecule by Hg(2+).


Assuntos
Ciclobutanos , Corantes Fluorescentes , Mercúrio/análise , Fenóis , Colorimetria/métodos , Íons , Metais/análise , Água
17.
Pharmazie ; 65(9): 670-8, 2010 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21038844

RESUMO

A simple and rapid LC-MS/MS method was established for the determination of dihydroartemisinin (DHA) in plasma and tissues of rats. Sample preparation was achieved by liquid-liquid extraction with aether and analysis was performed on LC-MS/MS in positive ion mode using electrospray ionization (ESI) as an interface. Target compounds were quantified in a single ion-monitoring (SIM) mode. DHA was monitored at m/z 267.1 and the internal standard finasteride at m/z 305.2. Chromatography was carried out using a Synergi fusion RP 80 column with a mixture of ethanol and 0.1% formic acid mixture (75:25) as the mobile phase. The pharmacokinetics and tissue distribution after intravenous administration of DHA in nanostructured lipid carrier (NLC) and in solution were then compared. The mean residence times (MRT) of the DHA-NLC was much longer than that of the DHA solution. In the tested organs, the AUC values of the DHA-NLC were higher than that of the DHA solution in liver, spleen, lung, brain and muscle, and lower than the DHA solution in heart and kidney. DHA-NLC prepared in this study is a promising sustained-release and drug-targeting system for antitumor drugs. It may also allow a reduction in dosage and a decrease in systemic toxicity.


Assuntos
Antimaláricos/química , Antimaláricos/farmacocinética , Artemisininas/química , Artemisininas/farmacocinética , Animais , Antimaláricos/administração & dosagem , Área Sob a Curva , Artemisininas/administração & dosagem , Cromatografia Líquida de Alta Pressão , Portadores de Fármacos , Estabilidade de Medicamentos , Meia-Vida , Injeções Intravenosas , Lipídeos/química , Masculino , Espectrometria de Massas , Nanopartículas , Controle de Qualidade , Ratos , Ratos Wistar , Padrões de Referência , Reprodutibilidade dos Testes , Espectrometria de Massas por Ionização por Electrospray , Distribuição Tecidual
18.
Acta Crystallogr Sect E Struct Rep Online ; 66(Pt 9): o2330, 2010 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-21588676

RESUMO

In the title compound, C(11)H(18)N(4)O(2)S(2), the dithiol-ane ring displays an envelope conformation, the tetra-hydro-pyrimidine ring has a conformation that is between half-chair and screw-boat, and the imidazole ring is essentially planar (r.m.s. deviation = 0.0017 Å). No significant directional inter-molecular inter-actions are present in the structure.

19.
Acta Crystallogr Sect E Struct Rep Online ; 66(Pt 9): o2359, 2010 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-21588701

RESUMO

In the title compound, C(9)H(15)N(3)O(4), the 1,3-dioxane ring displays a chair conformation and the five-membered ring is close to planar (r.m.s. deviation = 0.054 Å). An intra-molecular N-H⋯O hydrogen bond to one of the nitro-group O atoms generates an S(6) ring. In the crystal, inter-molecular N-H⋯O hydrogen bonds link the mol-ecules into C(6) chains propagating in [010] and a C-H⋯O link also occurs.

20.
Acta Crystallogr Sect E Struct Rep Online ; 66(Pt 9): o2416, 2010 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-21588742

RESUMO

In the title compound, C(13)H(22)N(4)O(2)S(2), the six-membered ring displays a half-chair conformation. The olefin amine unit is close to being coplanar with the imidazolidine ring (r.m.s. deviation = 0.059 Å). The dithiol-ane ring adopts a twisted conformation. In the crystal, mol-ecules are linked by weak C-H⋯O inter-actions.

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