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1.
Micron ; 140: 102976, 2021 01.
Artigo em Inglês | MEDLINE | ID: mdl-33221524

RESUMO

The Asian larch bark beetle, Ips subelongatus, is a severe pest of larches in Northeastern China. The gustatory and olfactory systems of I. subelongatus play important roles in host location, mating, and feeding. In this study, we examined the types, distributions, and abundances of various sensilla associated with the mouthparts and antennae of I. subelongatus using scanning electron microscopy (SEM). On the mouthparts, five types of sensilla are present: sensilla trichodea (S.t.1-3), sensilla chaetica (S.c.1-3), sensilla basiconica (S.b.1-2), sensilla twig basiconica (S.tb.1-3), and sensilla placodea (S.p). S.t.3 are the most abundant sensilla subtype on the mouthparts in both sexes, while S.b.1 are the least abundant. Most sensilla on the mouthparts are located on the maxillae and labium, and the apex of each maxillary and labial palp carry the same sensilla subtypes (S.b.2 and S.tb.1-3). However, the total number of sensilla on the apex of each maxillary palp is higher than that on the labial palp. On the antennae, five types of sensilla are present: sensilla trichodea (S.t.1-3), sensilla chaetica (S.c.1-2), sensilla basiconica (S.b.1-3), Böhm bristles (B.b), and sensilla coeloconica (S.co). Antennal sensilla are mostly situated on the anterior surface of the antennal club, particularly on the two dense sensory bands. S.b.1 are the most abundant sensilla subtype on the antennae in both sexes, while S.t.1 are the least abundant. No sexual dimorphism in sensilla type or distribution on the mouthparts or antennae is observed between the sexes of I. subelongatus. However, S.t.3 (on mouthparts) and S.c.1 (on antennae) were significantly more abundant in males than in females, while more S.t.1 (on mouthparts) were observed in females than in males. Finally, the putative functions of each kind of sensilla with respect to their fine structures, distributions, and abundances on the mouthparts and antennae are discussed.

2.
Pharmacol Res ; 161: 105109, 2020 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-32738494

RESUMO

Protocatechuic acid is a natural phenolic acid, which widely exists in our daily diet and herbs. It is also one of the main metabolites of complex polyphenols, such as anthocyanins and proanthocyanins. In recent years, a large number of studies on the pharmacological activities of protocatechuic acid have emerged. Protocatechuic acid has a wide range of pharmacological activities including antioxidant, anti-inflammatory, neuroprotective, antibacterial, antiviral, anticancer, antiosteoporotic, analgesia, antiaging activties; protection from metabolic syndrome; and preservation of liver, kidneys, and reproductive functions. Pharmacokinetic studies showed that the absorption and elimination rate of protocatechuic acid are faster, with glucuronidation and sulfation being the major metabolic pathways. However, protocatechuic acid displays a dual-directional regulatory effect on some pharmacological activities. When the concentration is very high, it can inhibit cell proliferation and reduce survival rate. This review aims to comprehensively summarize the pharmacology, pharmacokinetics, and toxicity of protocatechuic acid with emphasis on its pharmacological activities discovered in recent 5 years, so as to provide more up-to-date and thorough information for the preclinical and clinical research of protocatechuic acid in the future. Moreover, it is hoped that the clinical application of protocatechuic acid can be broadened, giving full play to its characteristics of rich sources, low toxicity and wide pharmacological activites.

3.
Preprint | medRxiv | ID: ppmedrxiv-20156810

RESUMO

Knowledge of the host immune response after natural SARS-CoV-2 infection is essential for informing directions of vaccination and epidemiological control strategies against COVID-19. In this study, thirty-four COVID-19 patients were enrolled with 244 serial blood specimens (38.1% after hospital discharge) collected to explore the chronological evolution of neutralizing (NAb), total (TAb), IgM, IgG and IgA antibody in parallel. IgG titers reached a peak later (approximately 35 days postonset) than those of Nab, Ab, IgM and IgA (20[~]25 days postonset). After peaking, IgM levels declined with an estimated average half-life of 10.36 days, which was more rapid than those of IgA (51.25 days) and IgG (177.39 days). Based on these half-life data, we estimate that the median times for IgM, IgA and IgG to become seronegative are 4.59 (IQR 4.12-5.03), 7.78 (IQR 6.71-9.16) and 42.72 (IQR 33.75-47.96) months post disease onset. The relative contribution of IgM to NAb was higher than that of IgG (standardized {beta} regression coefficient: 0.53 vs 0.48), so the rapid decline in NAb may be attributed to the rapid decay of IgM in acute phase. However, the relative contribution of IgG to NAb increased and that of IgM further decreased after 6 weeks postonset. Its assumed that the decline rate of NAb might slow down to the same level as that of IgG over time. This study suggests that SARS-CoV-2 infection induces robust neutralizing and binding antibody responses in patients and that humoral immunity against SARS-CoV-2 acquired by infection may persist for a relatively long time.

4.
Cancer Chemother Pharmacol ; 85(3): 593-604, 2020 03.
Artigo em Inglês | MEDLINE | ID: mdl-32008115

RESUMO

PURPOSE: This Phase I study evaluated the safety, tolerability, food effects, pharmacodynamics, and pharmacokinetics of donafenib in patients with advanced solid tumours. METHODS: Eligible patients received a single dose of donafenib (50 mg, 100 mg, 200 mg, 300 mg, or 400 mg) and were then observed over a 7-day period; thereafter, each patient received the corresponding dose of donafenib twice daily for at least 4 weeks. Safety assessment and pharmacokinetic sampling were performed for all patients at the given time points; preliminary tumour response was also assessed. RESULTS: Twenty-five patients were enrolled in this study. Gastrointestinal reactions were the most common treatment-related adverse event, followed by skin toxicity. The maximum tolerated dose (MTD) was 300 mg bid. The dose-limiting toxicities (DLTs) were grade 3 diarrhoea and fatigue at 300 mg bid and grade 3 skin toxicity at 400 mg bid. In the dose range of 100 ~ 400 mg, T1/2 and AUC0-t after multiple doses were 26.9 ~ 30.2 h and 189 ~ 356 h*µg/mL, respectively. Food did not have a significant effect on the pharmacokinetics of donafenib. Twenty-one patients were assessed for efficacy, and two patients achieved a partial response according to Response Evaluation Criteria in Solid Tumors (RECIST), with a disease control rate of 57.1%. CONCLUSION: Oral donafenib was generally well tolerated and appeared to provide some clinical benefits; adverse events were manageable. Based on the results of this study, oral donafenib at 200 mg ~ 300 mg twice daily is recommended for further studies.


Assuntos
Antineoplásicos/administração & dosagem , Antineoplásicos/farmacocinética , Interações Alimento-Droga/fisiologia , Neoplasias/tratamento farmacológico , Piridinas/administração & dosagem , Piridinas/farmacocinética , Administração Oral , Adulto , Idoso , Antineoplásicos/efeitos adversos , Fadiga/induzido quimicamente , Feminino , Humanos , Masculino , Dose Máxima Tolerável , Pessoa de Meia-Idade , Neoplasias/metabolismo , Piridinas/efeitos adversos , Critérios de Avaliação de Resposta em Tumores Sólidos , Pele/efeitos dos fármacos , Adulto Jovem
5.
Zhongguo Zhong Yao Za Zhi ; 44(22): 4786-4792, 2019 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-31872583

RESUMO

The consistency of drug quality is related to the clinical efficacy and safety,which is highly valued by the government and relevant industries. Compared with chemical medicine,traditional Chinese medicine originates from the nature,and is greatly influenced by natural factors,such as the place of origin,cultivation and processing technology,climate. The quality consistency of traditional Chinese medicine is poor. The quality consistency has become the pain point and difficulty of the development of the traditional Chinese medicine industry,which seriously affects the stability and controllability of clinical efficacy and the reproducibility or recognition of modern research results. It is also a bottleneck for Chinese patent medicine to enter the international market. Mixed batch blending technology is an effective method for the scientific guarantee of the quality consistency in other industries and disciplines,and widely applied in liquor making industry,tobacco industry and perfume industry. Overseas,mixed batch blending technology has been successfully applied in guaranteeing the quality consistency of Ginkgo biloba preparations Jinnado. It has been used in the production of Chinese formulations in Japan for more than 30 years. In recent years,mixed batch blending technology has been introduced into the pharmaceutical field to ensure the quality consistency of traditional Chinese medicine,and relevant research has gradually increased.This manuscript reviews the application of blending technology in other disciplines,summarizes the algorithm principles and software systems of mixed batch blending in traditional Chinese medicine or natural medicine,explains the specific implementation process of mixed batch blending technology,and looks forward to the application prospects of artificial intelligence and other new technologies,in the hope of providing new ideas and technologies for breaking through the problem of quality consistency,and boosting the high-quality and high-level development of Chinese medicine industry in the new era.


Assuntos
Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , Algoritmos , Indústria Farmacêutica , Reprodutibilidade dos Testes , Tecnologia
6.
Front Pharmacol ; 10: 1060, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31619999

RESUMO

Triphala is a famous herbal formula originated in Asia and is popular in America. Due to the high abundance of polyphenols, its oral liquid is unstable and easy to cause precipitate, which results in the loss of activities. However, complex composition and unclear precipitation mechanism hinders the improvement of stability. In this study, the accumulation of precipitation in the storage and its effect on activity were investigated. Then, an integrated chain of evidence was proposed based on the physical phase, chemical profile, and sediment elements. The results showed that antioxidant activity decreased from IC50 115 to 146 µl before and after 90 days of storage, and the anti-fatigue activity decreased from 30.54 to 28.47 min. Turbiscan Lab Expert observed that particle size increased from 106 to 122 nm, and the turbiscan stability index increased from 0 to 14, which indicated that its stability is continuously decreasing. High performance liquid chromatography (HPLC) fingerprint coupled with multivariate statistical analysis identified that these chemical markers changed significantly, such as gallic acid, catechins, and ellagic acid. Loss of catechins tends to be involved in the formation of phlobaphene precipitation. The fact that the new-born ellagic acid in precipitation (0.47 mg/ml) is significantly higher than that reduced in solution (0.25 mg/ml) indicates that it is not only derived from colloid aging. Microscopic observation combined with energy spectrum analysis further confirmed the existence of the multi-precipitates. The crystalline precipitate is ellagic acid, and the other is phlobaphene. In conclusion, based on the evidence chain analysis, this study revealed a systematic change of the whole polyphenol solution system. It provides a novel perspective to understand the sedimentation formation of polyphenol solution, which is an important theoretical contribution to the preparation of polyphenol solutions.

7.
BMB Rep ; 52(9): 566-571, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31401980

RESUMO

Lymphoma is one of the most curable types of cancer. However, drug resistance is the main challenge faced in lymphoma treatment. Peroxisomal acyl-CoA oxidase 1 (ACOX1) is the rate-limiting enzyme in fatty acid ß-oxidation. Deregulation of ACOX1 has been linked to peroxisomal disorders and carcinogenesis in the liver. Currently, there is no information about the function of ACOX1 in lymphoma. In this study, we found that upregulation of ACOX1 promoted proliferation in lymphoma cells, while downregulation of ACOX1 inhibited proliferation and induced apoptosis. Additionally, overexpression of ACOX1 increased resistance to doxorubicin, while suppression of ACOX1 expression markedly potentiated doxorubicin-induced apoptosis. Interestingly, downregulation of ACOX1 promoted mitochondrial location of Bad, reduced mitochondrial membrane potential and provoked apoptosis by activating caspase-9 and caspase-3 related apoptotic pathway. Overexpression of ACOX1 alleviated doxorubicin-induced activation of caspase-9 and caspase-3 and decrease of mitochondrial membrane potential. Importantly, downregulation of ACOX1 increased p73, but not p53, expression. p73 expression was critical for apoptosis induction induced by ACOX1 downregulation. Also, overexpression of ACOX1 significantly reduced stability of p73 protein thereby reducing p73 expression. Thus, our study indicated that suppression of ACOX1 could be a novel and effective approach for treatment of lymphoma. [BMB Reports 2019; 52(9): 566-571].


Assuntos
Acil-CoA Oxidase/metabolismo , Doxorrubicina/farmacologia , Linfoma/metabolismo , Proteína Tumoral p73/metabolismo , Acil-CoA Oxidase/genética , Apoptose/efeitos dos fármacos , Apoptose/fisiologia , Western Blotting , Caspase 3/metabolismo , Caspase 9/metabolismo , Células HEK293 , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Proteína Tumoral p73/genética
8.
Molecules ; 24(17)2019 Aug 24.
Artigo em Inglês | MEDLINE | ID: mdl-31450584

RESUMO

For the treatment of diseases, especially chronic diseases, traditional natural drugs have more effective therapeutic advantages because of their multi-target and multi-channel characteristics. Among many traditional natural medicines, resins frankincense and myrrh have been proven to be effective in the treatment of inflammation and cancer. In the West, frankincense and myrrh have been used as incense in religious and cultural ceremonies since ancient times; in traditional Chinese and Ayurvedic medicine, they are used mainly for the treatment of chronic diseases. The main chemical constituents of frankincense and myrrh are terpenoids and essential oils. Their common pharmacological effects are anti-inflammatory and anticancer. More interestingly, in traditional Chinese medicine, frankincense and myrrh have been combined as drug pairs in the same prescription for thousands of years, and their combination has a better therapeutic effect on diseases than a single drug. After the combination of frankincense and myrrh forms a blend, a series of changes take place in their chemical composition, such as the increase or decrease of the main active ingredients, the disappearance of native chemical components, and the emergence of new chemical components. At the same time, the pharmacological effects of the combination seem magically powerful, such as synergistic anti-inflammation, synergistic anticancer, synergistic analgesic, synergistic antibacterial, synergistic blood-activation, and so on. In this review, we summarize the latest research on the main chemical constituents and pharmacological activities of these two natural resins, along with chemical and pharmacological studies on the combination of the two.


Assuntos
Franquincenso/química , Resinas Vegetais/química , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Franquincenso/farmacologia , Humanos , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Resinas Vegetais/farmacologia
9.
Sci Rep ; 8(1): 10319, 2018 07 09.
Artigo em Inglês | MEDLINE | ID: mdl-29985460

RESUMO

Slow disintegration and poor solubility are common problems facing the dispersible tablets of Traditional Chinese Medicine (TCM). In an early study, the research group found that co-grinding of extracts and silica could achieve a rapid disintegration effect, though the mechanism of this effect was not thoroughly elucidated. In this study, Yuanhu Zhitong dispersible tablets (YZDT) were selected as a model drug to explore the mechanism of rapid disintegration and dissolution. First, eight types of silica were used to prepare modified YZDT, and their disintegration time and amount of dissolution within 5 min were measured. Next, the powder properties of eight types of silica were investigated. By correlation analysis, it was found that the average pore size and density of silica were closely related to the effect of promoting disintegration. It was determined that the co-grinding of silica and extracts provided high porosity for the raw material drug, and its abundant narrow channels provided a strong static pressure for water penetration to achieve a rapid disintegration effect. Meanwhile, it was found that the addition of silica had a certain effect on promoting dissolution. Our results provide a highly operational approach for improving the disintegration and dissolution of TCM dispersible tablets. Meanwhile, this approach is also beneficial for establishing a high-quality evaluation index for silica.


Assuntos
Composição de Medicamentos/métodos , Medicamentos de Ervas Chinesas/química , Medicina Tradicional Chinesa , Comprimidos/química , Adsorção , Medicina Tradicional Chinesa/normas , Porosidade , Pós/química , Controle de Qualidade , Dióxido de Silício/química , Comprimidos/normas , Água/química
10.
Sci Rep ; 8(1): 7454, 2018 05 10.
Artigo em Inglês | MEDLINE | ID: mdl-29748583

RESUMO

Nowadays, breast disorders seriously affect women's health in an increasing number. In China, Xiaojin Pills are commonly used in the treatment of breast diseases. Doctors have concluded that the combined use of Xiaojin Pills with conventional therapy can significantly improve the efficacy with fewer side effects. However, the prescription of Xiaojin Pills is complicated and their quality control methods cannot completely ensure the quality of Xiaojin Pills. On the basis of its mechanism, our study combined chemical evaluation and biological evaluation to identify the anti-inflammatory markers of Xiaojin Pills. In this manuscript, 13 compounds in Xiaojin Pills were quantified. At the same time, the cyclooxygenase-2 inhibition rates of different Xiaojin Pills were measured and the possible markers were screened by spectrum-effect relationship. Further, anti-inflammatory activities of markers were verified and protein interaction network was analyzed, identifying the components of Protocatechuate, Beta-Boswellic acid and Levistilide A as the anti-inflammatory quality markers of Xiaojin Pills. We hope our studies can provide a scientific theoretical basis for accurately quality control of Xiaojin Pills and reasonable suggestions for pharmaceutical companies and new ideas for the quality control of other medicines.


Assuntos
Anti-Inflamatórios/farmacologia , Inibidores de Ciclo-Oxigenase 2/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Mapas de Interação de Proteínas/efeitos dos fármacos , Anti-Inflamatórios/química , Doenças Mamárias/tratamento farmacológico , Cromatografia Líquida de Alta Pressão , Análise por Conglomerados , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/química , Medicamentos de Ervas Chinesas/química , Feminino , Humanos , Modelos Moleculares , Controle de Qualidade , Espectrometria de Massas em Tandem
11.
Zhongguo Zhong Yao Za Zhi ; 43(24): 4801-4807, 2018 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-30717523

RESUMO

Xiaojin Pill, was firstly recorded in Life-saving Manual of Diagnosis and Treatment of External Diseases, with its primitive name of "Xiaojin Dan". Xiaojin Pill is a classic prescription for treating carbuncle and it is the first choice for Chinese medicine in the clinical treatment of hyperplasia of mammary glands. In this paper, the literature reports on Xiaojin Pills were summarized and the historical evolution, material basis, pharmacological action, quality control and other problems were systematically discussed to explore the potential problems in every aspect of the development status, and put forward the development countermeasures, providing reference for the modernization research and development of Xiaojin Pills.


Assuntos
Medicamentos de Ervas Chinesas , Cápsulas , Controle de Qualidade , Pesquisa
12.
Pain Med ; 18(1): 14-24, 2017 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-27516366

RESUMO

Objective: To assess the efficacy and safety of tapentadol IR for moderate to severe pain compared to oxycodone IR. Methods: A search was carried out up to July 2015 for randomized controlled trials (RCTs) of tapentadol IR compared to placebo or oxycodone HCL IR 10 mg for moderate to severe pain. Studies were pooled by risk ratio (RR) and weighted mean differences (WMD) with 95% confidence interval (CI). Results: Nine RCTs (n = 3,961) were analyzed. In this meta-analysis, tapentadol IR (50-, 75-, and 100-mg doses) showed significant improvements in moderate to severe pain relief on the sum of pain intensity difference over 48 hours (SPID 48 ) scores ( P < 0.00001 or P = 0.01). No statistically significant difference among all three doses of tapentadol IR and oxycodone HCL IR 10 mg on both SPID 48 and total pain relief over 48 hours (TOTPAR 48 ) scores (all P > 0.05) was found. Compared with tapentadol IR 50 mg, tapentadol IR 75 mg demonstrated significant improvement in moderate to severe pain relief based on both SPID 48 and TOTPAR 48 scores (all P < 0.05). For total adverse events (AEs) incidence, tapentadol IR 50 and 75 mg were significantly lower than oxycodone HCL IR 10 mg. Incidence of nausea and constipation were significantly lower with either tapentadol IR 50 or 75 mg compared with oxycodone HCL IR 10 mg (all P < 0.05). Conclusions: Tapentadol IR 75 mg might be an optimal dose for moderate to severe pain control with fewer side effects. All three doses of tapentadol IR could provide comparable efficacy to oxycodone HCL IR 10 mg.


Assuntos
Analgésicos/uso terapêutico , Dor/tratamento farmacológico , Fenóis/uso terapêutico , Humanos , Ensaios Clínicos Controlados Aleatórios como Assunto , Tapentadol
13.
Oncotarget ; 7(52): 87136-87146, 2016 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-27888624

RESUMO

Colorectal cancer (CRC) is a major cause of mortality and morbidity worldwide. While surgery remains the mainstay of treatment in early stage CRC, chemotherapy is usually given to prolong the overall survival and improve the quality of life for metastatic colorectal cancer (mCRC). But drug resistance is one of the major hurdles of mCRC treatment, and the underlying mechanisms are still largely unknown. In this study, we show that, compared with parental cells, RhoA is up-regulated in irinotecan (CPT-11)-resistant CRC cells. Furthermore, inhibition of RhoA in drug resistant cells, at least partially, rescues the resistance against irinotecan and increases the sensitivity to other chemotherapeutic drug by inhibiting expression of MDR1, MRP1and GSTP1, promotes apoptosis by suppressing the expression of BCL-XL and Bcl-2 and increasing Bax expression, and significantly decreases side population cells. Our results suggest that, in addition to survival, proliferation, migration, adhesion, cell cycle and gene transcription, RhoA is also involved in chemoresistance by regulating the expression of membrane transporter and apoptosis protein in colorectal cancer. They raise an interesting possibility that the expression of RhoA may indicate a poor prognosis due to the high probability to therapy resistance and, on the other hand, inhibition of RhoA activity and function may overcome chemoresistance and improve the effectiveness of clinical treatment of CRC.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Camptotecina/análogos & derivados , Neoplasias Colorretais/tratamento farmacológico , Proteínas de Membrana Transportadoras/genética , Proteína rhoA de Ligação ao GTP/fisiologia , Camptotecina/farmacologia , Linhagem Celular Tumoral , Neoplasias Colorretais/metabolismo , Neoplasias Colorretais/patologia , Resistencia a Medicamentos Antineoplásicos , Regulação Neoplásica da Expressão Gênica , Humanos , Irinotecano , Proteínas Proto-Oncogênicas c-bcl-2/análise , Transdução de Sinais/efeitos dos fármacos , Proteína bcl-X/análise , Proteína rhoA de Ligação ao GTP/antagonistas & inibidores , Proteína rhoA de Ligação ao GTP/genética
14.
J Exp Bot ; 67(8): 2263-75, 2016 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-26889012

RESUMO

The DNA binding with one finger (Dof) proteins, a family of plant-specific transcription factors, are involved in a variety of plant biological processes. However, little information is available on their involvement in fruit ripening. We have characterized 25 MaDof genes from banana fruit (Musa acuminata), designated as MaDof1-MaDof25 Gene expression analysis in fruit subjected to different ripening conditions revealed that MaDofs were differentially expressed during different stages of ripening. MaDof10, 23, 24, and 25 were ethylene-inducible and nuclear-localized, and their transcript levels increased during fruit ripening. Moreover, yeast two-hybrid and bimolecular fluorescence complementation analyses demonstrated a physical interaction between MaDof23 and MaERF9, a potential regulator of fruit ripening reported in a previous study. We determined that MaDof23 is a transcriptional repressor, whereas MaERF9 is a transcriptional activator. We suggest that they might act antagonistically in regulating 10 ripening-related genes, including MaEXP1/2/3/5, MaXET7, MaPG1, MaPME3, MaPL2, MaCAT, and MaPDC, which are associated with cell wall degradation and aroma formation. Taken together, our findings provide new insight into the transcriptional regulation network controlling banana fruit ripening.


Assuntos
Frutas/crescimento & desenvolvimento , Frutas/genética , Genes de Plantas , Musa/genética , Proteínas de Plantas/metabolismo , Proteínas Repressoras/metabolismo , Fatores de Transcrição/metabolismo , Sequência de Aminoácidos , Núcleo Celular/metabolismo , Regulação da Expressão Gênica de Plantas , Musa/crescimento & desenvolvimento , Proteínas de Plantas/química , Proteínas de Plantas/genética , Plantas Geneticamente Modificadas , Ligação Proteica , Transporte Proteico , Saccharomyces cerevisiae/metabolismo , Alinhamento de Sequência , Análise de Sequência de DNA , Frações Subcelulares/metabolismo , Tabaco/genética , Fatores de Transcrição/química , Fatores de Transcrição/genética , Ativação Transcricional/genética
15.
J Obstet Gynaecol Res ; 40(7): 1925-30, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-25056472

RESUMO

AIM: It has been shown that glycolytic metabolism is increased in malignant cells. Cancer cell growth is an energy-related process supported by an increased glucose metabolism. In addition, p63, a known homolog of p53, is expressed predominantly in basal cell and squamous cell carcinomas. The purpose of this study was to evaluate the expression of glucose transporter protein 1 (GLUT1) and p63 in patients with serous ovarian tumor (benign, borderline and malignant) and study their close relationship with the malignant transformation of serous ovarian tumors. METHODS: Two hundred formalin-fixed, paraffin-embedded sections were immunostained with rabbit anti-GLUT1 polyclonal antibody and mouse anti-p63 monoclonal antibody using the streptavidin-biotin method. The samples were as follows: 40 normal ovarian tissues, 40 serous cystadenomas, 40 borderline serous cystadenomas and 80 serous cystadenocarcinomas were stained. RESULT: Normal ovarian tissues showed completely negative staining for GLUT1 and p63. However, from benign serious cystadenomas, borderline cystadenomas to cystadenocarcinomas, the expression of GLUT1 and p63 grew stronger (P < 0.05). Moreover, the intensity staining of GLUT1 maintained a significant association with the expression of p63 (P < 0.05). In χ²-test analysis, expression of borderline cystadenomas and cystadenocarcinomas, intraperitoneal implants, ascites, lymph node status and International Federation of Gynecology and Obstetrics (FIGO) stage and GLUT1 expression levels have an appalling significance (P < 0.05), while FIGO stage, intraperitoneal implants and lymph node status except patient age and ascites have a statistical significance with the expression of p63 levels (P < 0.05). CONCLUSION: Our findings show a progressive increase in the expression of GLUT1 and p63 from the benign serous cystadenomas, borderline cystadenomas to cystadenocarcinomas. Overexpression of GLUT1 and p63 are associated with the histology FIGO stage and metastasis of the tumors. These data suggested that the expression of GLUT1 and p63 may be closely related to the malignant transformation of serous ovarian tumors. However, the relative importance of GLUT1 and p63 in ovarian serous tumor development and tumorigenesis remains mostly unclear and awaits further investigation.


Assuntos
Cistadenocarcinoma Seroso/metabolismo , Cistadenoma Seroso/metabolismo , Transportador de Glucose Tipo 1/metabolismo , Neoplasias Ovarianas/metabolismo , Ovário/metabolismo , Fatores de Transcrição/metabolismo , Proteínas Supressoras de Tumor/metabolismo , Regulação para Cima , Adulto , Biomarcadores Tumorais/metabolismo , Cistadenocarcinoma Seroso/patologia , Cistadenoma Seroso/patologia , Feminino , Humanos , Pessoa de Meia-Idade , Proteínas de Neoplasias/metabolismo , Estadiamento de Neoplasias , Neoplasias Ovarianas/patologia , Ovário/patologia
16.
J Chromatogr Sci ; 52(8): 766-72, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23888003

RESUMO

Photocyanine, a novel amphoteric phthalocyanine drug, showed favorable anticancer activity in vivo. Pharmacokinetic study in cancer patients is an important component in dose administration choice. In this study, a rapid, sensitive analytical method based on high-performance liquid chromatography with ultraviolet detection was developed and validated for the determination of four isomers of photocyanine (FD1-4) in cancer patients. Sample preparation involved liquid-liquid extraction with a combination of ultrasound and N,N-dimethyl formamide. Calibration curves (1/x(2)) offered satisfactory linearity for the four isomers of photocyanine. The lower limit of quantification (LLOQ) for FD1-3 isomers was 30 ng/mL, and LLOQ for FD-4 was 5 ng/mL. Inter- and intra-day accuracies for four isomers ranged from 96.6 to 105.5%, and 95.0 to 103.6%, respectively. Inter- and intra-day precision ranged from 4.8 to 8.9%, and 3.6 to 12.2%, respectively. Stability studies showed that photocyanine was stable. This method was successfully used to quantify photocyanine in a pharmacokinetic study in which a single-dose of photocyanine (0.1 mg/kg) was intravenously administered to patients with cancer. On the basis of the discovery that photocyanine has a half-life of 57.5 h in vivo, we suggest that avoiding light for a longer period is essential for patients undergoing photocyanine therapy.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Indóis/sangue , Indóis/farmacocinética , Adulto , Feminino , Humanos , Masculino , Neoplasias/sangue , Neoplasias/tratamento farmacológico , Reprodutibilidade dos Testes
17.
Yi Chuan ; 35(8): 1030-9, 2013 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-23956092

RESUMO

Serine/Threonine-specific calcineurin (CN) is highly conserved in eukaryotes, which plays an important role in transcriptional regulation. In Schizosaccharomyces pombe, CN exists as a heterodimer composed by catalytic subunit Ppb1 and regulatory subunit Cnb1. Deletion of cnb1+ reduced the growth rate of cells, and caused a chained phenotype, and had delay in cytokinesis. In cytokinesis, Cnb1 could form CN complex with Ppb1 and could colocalize and constrict with the contractile ring at division plane. Tubulin could cross the septum in cnb1Δ strain, suggesting that the septum is not fully matured. These results suggest Cnb1 might be involved in maturation of septum. The signals of septins in cnb1Δ strain were also analyzed. Septins include Spn1, Spn2, Spn3, and Spn4. Septins help to guide hydrolytic enzymes for septum degrada-tion. Eighty percent of cnb1Δ cells lacked the signals of Spn2 or Spn3 at septum, and twenty percent of cnb1Δ cells lacked the signals of Spn1 or Spn4 at septum. The reduction of the septin signals was not due to impaired transcription of septins, since the protein levels of septins in the cnb1Δ cells were not decreased. These results imply that Cnb1 might regulate the stability of septin ring in a transcription-independent manner. In general, our study showed that Cnb1 contributes to the maturation of septum and the stability of septin ring and is important in the cytokinesis.


Assuntos
Citocinese , Schizosaccharomyces , Divisão Celular , Fenótipo , Proteínas de Saccharomyces cerevisiae/genética , Schizosaccharomyces/genética , Proteínas de Schizosaccharomyces pombe/genética , Septinas
18.
Clin Exp Obstet Gynecol ; 40(4): 574-8, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24597260

RESUMO

OBJECTIVE: To explore the effect of patient-controlled lumbar epidural combined anesthesia with Doula for labor analgesia with ropivacaine and sufentanil, and its influence on the progress of labor, and outcomes of mother and infant. MATERIALS AND METHODS: Two hundred parturients that requested labor analgesia were randomly selected by patient-controlled lumbar epidural combined anesthesia with Doula as the observation group, meanwhile another 200 parturients were selected as the control group without any analgesic measurements. Labor pain score, labor duration, blood gas analysis results, the incidence of cesarean section, neonatal asphyxia, and postpartum hemorrhage were compared between the two groups. RESULTS: Compared with the control group, labor analgesic effect was remarkable, the cesarean section rate was significantly reduced in observation group, and the difference was statistically significant (p < 0.05), but with respect to the duration of labor, maternal, postpartum hemorrhage, and neonatal asphyxia, there was no statistical significance between the two groups (p > 0.5). In the observation group regarding maternal and neonatal blood gas analysis results, PO2 was higher and PCO2 was lower than those in the control group. The differences were statistically significant (p < 0.05). CONCLUSION: Labor analgesia by patient-controlled lumbar epidural combined anesthesia accompanied with Doula with ropivacaine and sufentanil is effective, safe, reliable, has no adverse effects, and reduces cesarean section rate.


Assuntos
Analgesia Obstétrica/métodos , Anestesia Epidural , Anestesia Obstétrica/métodos , Parto Obstétrico/métodos , Doulas , Adulto , Amidas , Analgésicos Opioides , Anestésicos Locais , Feminino , Humanos , Dor do Parto/fisiopatologia , Medição da Dor , Paridade , Gravidez , Ropivacaina , Sufentanil , Adulto Jovem
19.
J Inorg Biochem ; 116: 19-25, 2012 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23010325

RESUMO

Ferrocene (Fc) and its conjugates have attracted considerable attention in recent years due to their unique electrochemical behavior and significant biological activities such as antitumor, antimalarial, and antifungal. Arg-Gly-Asp (RGD)-containing peptides, because of their selective binding to integrins which are highly expressed in tumor-induced angiogenesis, play a key role in cancer targeted therapy. In this study, Fc-RGD and Fc-Am-RGD (Fc: ferrocenoyl; Am: 6-aminohexanoic acid) conjugates were synthesized, and the antitumor activities in vitro were investigated. The cell uptake of the conjugates by B16 murine melanoma cells was measured using HPLC-electrochemical method. The antitumor activities of the conjugates were also evaluated by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and flow cytometric measurements. The experimental results revealed that Fc-RGD and Fc-Am-RGD exhibit more effective antitumor activities than their parent compounds RGD and Fc-COOH. Moreover, it is found that Fc-Am-RGD yields the lowest IC(50) values of 5.2 ± 1.4 µM toward B16 cells. The HPLC-electrochemical studies confirmed that the insertion of flexible alkyl spacer Am between Fc and RGD significantly increases the cell uptake toward B16 cells and consequently improves the antitumor activity. Our results suggest that Fc-RGD and Fc-Am-RGD conjugates are potential candidates for cancer treatment.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Compostos Ferrosos/química , Oligopeptídeos/química , Animais , Linhagem Celular Tumoral , Citometria de Fluxo , Corantes Fluorescentes , Técnicas In Vitro , Espectroscopia de Ressonância Magnética , Metalocenos , Camundongos , Oligopeptídeos/farmacologia , Espectrometria de Massas por Ionização por Electrospray
20.
Plant Physiol Biochem ; 55: 33-42, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22522578

RESUMO

Polar auxin transport (PAT) plays an important role in the adventitious root formation of mango cotyledon segments, but the molecular mechanism remains unclear. In this study, we cloned a gene encoding an auxin efflux carrier (designated as MiPIN1), and we cloned four genes encoding auxin influx carriers (designated as MiAUX1, MiAUX2, MiAUX3 and MiAUX4). The results of a phylogenetic tree analysis indicated that MiPIN1 and the MiAUXs belong to plant PIN and AUXs/LAXs groups. Quantitative real-time PCR indicated that the expression of MiPIN1 and the MiAUXs was lowest at 0 days but sharply increased on and after day 4. During the root formation in the mango cotyledon segments, the MiPIN1 expression in the distal cut surface (DCS) was always higher than the expression in the proximal cut surface (PCS) whereas the expression of the MiAUXs in the PCS was usually higher than in the DCS. This expression pattern might be result in the PAT from the DCS to the PCS, which is essential for the adventitious root formation in the PCS. Our previous study indicated that a pre-treatment of embryos with indole-3-butyric acid (IBA) significantly promoted adventitious rooting in PCS whereas a pre-treatment with 2,3,5-triiodobenzoic acid (TIBA) completely inhibited this rooting. In this study, however, IBA and TIBA pre-treatments slightly changed the expression of MiPIN1. In contrast, while the MiAUX3 and MiAUX4 expression levels were significantly up-regulated by the IBA pre-treatment, the expression levels were down-regulated by the TIBA pre-treatment. These findings imply that MiAUX3 and MiAUX4 are more sensitive to the IBA and TIBA treatments and that they might play important roles during adventitious root formation in mango cotyledon segments.


Assuntos
Cotilédone/genética , Ácidos Indolacéticos/metabolismo , Mangifera/genética , Proteínas de Plantas/genética , Raízes de Plantas/genética , Sequência de Aminoácidos , Sequência de Bases , Transporte Biológico , Clonagem Molecular , Cotilédone/crescimento & desenvolvimento , Cotilédone/metabolismo , DNA Complementar/química , DNA Complementar/genética , Regulação da Expressão Gênica no Desenvolvimento , Regulação da Expressão Gênica de Plantas , Mangifera/crescimento & desenvolvimento , Mangifera/metabolismo , Dados de Sequência Molecular , Filogenia , Proteínas de Plantas/classificação , Proteínas de Plantas/metabolismo , Raízes de Plantas/crescimento & desenvolvimento , Raízes de Plantas/metabolismo , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Análise de Sequência de DNA , Homologia de Sequência de Aminoácidos
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