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1.
J Ethnopharmacol ; 334: 118521, 2024 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-38969152

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Sangju Cold Granule (SJCG) is a classical traditional Chinese medicine (TCM) prescription described in "Item Differentiation of Warm Febrile Diseases". Historically, SJCG was employed to treat respiratory illnesses. Despite its popular usage, the alleviating effect of SJCG on influenza A virus infection and its mechanisms have not been fully elucidated. AIM OF THE STUDY: Influenza is a severe respiratory disease that threatens human health. This study aims to assess the therapeutic potential of SJCG and the possible molecular mechanism underlying its activity against influenza A virus in vitro and in vivo. MATERIALS AND METHODS: Ultrahigh-performance liquid chromatography (UPLC)-Q-Exactive was used to identify the components of SJCG. The 50% cytotoxic concentration of SJCG in MDCK and A549 cells were determined using the CCK-8 assay. The activity of SJCG against influenza A virus H1N1 was evaluated in vitro using plaque reduction and progeny virus titer reduction assays. RT-qPCR was performed to obtain the expression levels of inflammatory mediators and the transcriptional regulation of RIG-I and MDA5 in H1N1-infected A549 cells. Then, the mechanism of SJCG effect on viral replication and inflammation was further explored by measuring the expressions of proteins of the RIG-I/NF-kB/IFN(I/III) signaling pathway by Western blot. The impact of SJCG was explored in vivo in an intranasally H1N1-infected BALB/c mouse pneumonia model treated with varying doses of SJCG. The protective role of SJCG in this model was evaluated by survival, body weight monitoring, lung viral titers, lung index, lung histological changes, lung inflammatory mediators, and peripheral blood leukocyte count. RESULTS: The main SJCG chemical constituents were flavonoids, carbohydrates and glycosides, amino acids, peptides, and derivatives, organic acids and derivatives, alkaloids, fatty acyls, and terpenes. The CC50 of SJCG were 24.43 mg/mL on MDCK cells and 20.54 mg/mL on A549 cells, respectively. In vitro, SJCG significantly inhibited H1N1 replication and reduced the production of TNF-α, IFN-ß, IL-6, IL-8, IL-13, IP-10, RANTES, TRAIL, and SOCS1 in infected A549 cells. Intracellularly, SJCG reduced the expression of RIG-I, MDA5, P-NF-κB P65 (P-P65), P-IκBα, P-STAT1, P-STAT2, and IRF9. In vivo, SJCG enhanced the survival rate and decreased body weight loss in H1N1-infected mice. Mice with H1N1-induced pneumonia treated with SJCG showed a lower lung viral load and lung index than untreated mice. SJCG effectively alleviated lung damage and reduced the levels of TNF-α, IFN-ß, IL-6, IP-10, RANTES, and SOCS1 in lung tissue. Moreover, SJCG significantly ameliorated H1N1-induced leukocyte changes in peripheral blood. CONCLUSIONS: SJCG significantly reduced influenza A virus and virus-mediated inflammation through inhibiting the RIG-I/NF-kB/IFN(I/III) signaling pathway. Thus, SJCG could provide an effective TCM for influenza treatment.


Assuntos
Anti-Inflamatórios , Antivirais , Medicamentos de Ervas Chinesas , Vírus da Influenza A Subtipo H1N1 , Camundongos Endogâmicos BALB C , Infecções por Orthomyxoviridae , Animais , Antivirais/farmacologia , Cães , Humanos , Células A549 , Anti-Inflamatórios/farmacologia , Células Madin Darby de Rim Canino , Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Infecções por Orthomyxoviridae/tratamento farmacológico , Infecções por Orthomyxoviridae/virologia , Camundongos , Replicação Viral/efeitos dos fármacos , Feminino , Pulmão/efeitos dos fármacos , Pulmão/patologia , Pulmão/virologia
2.
Genes (Basel) ; 15(6)2024 Jun 02.
Artigo em Inglês | MEDLINE | ID: mdl-38927667

RESUMO

The Cucumber mosaic virus (CMV) presents a significant threat to pepper cultivation worldwide, leading to substantial yield losses. We conducted a transcriptional comparative study between CMV-resistant (PBC688) and -susceptible (G29) pepper accessions to understand the mechanisms of CMV resistance. PBC688 effectively suppressed CMV proliferation and spread, while G29 exhibited higher viral accumulation. A transcriptome analysis revealed substantial differences in gene expressions between the two genotypes, particularly in pathways related to plant-pathogen interactions, MAP kinase, ribosomes, and photosynthesis. In G29, the resistance to CMV involved key genes associated with calcium-binding proteins, pathogenesis-related proteins, and disease resistance. However, in PBC688, the crucial genes contributing to CMV resistance were ribosomal and chlorophyll a-b binding proteins. Hormone signal transduction pathways, such as ethylene (ET) and abscisic acid (ABA), displayed distinct expression patterns, suggesting that CMV resistance in peppers is associated with ET and ABA. These findings deepen our understanding of CMV resistance in peppers, facilitating future research and variety improvement.


Assuntos
Capsicum , Cucumovirus , Resistência à Doença , Regulação da Expressão Gênica de Plantas , Doenças das Plantas , Cucumovirus/genética , Cucumovirus/patogenicidade , Resistência à Doença/genética , Doenças das Plantas/virologia , Doenças das Plantas/genética , Capsicum/virologia , Capsicum/genética , Ácido Abscísico/metabolismo , Ácido Abscísico/farmacologia , Etilenos/metabolismo , Transcriptoma , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Perfilação da Expressão Gênica/métodos , Interações Hospedeiro-Patógeno/genética , Reguladores de Crescimento de Plantas/genética , Reguladores de Crescimento de Plantas/farmacologia
3.
Sci Rep ; 13(1): 4058, 2023 03 11.
Artigo em Inglês | MEDLINE | ID: mdl-36906685

RESUMO

Based on 22 qualitative traits, 13 quantitative traits, and 27 molecular markers (26 SSR and 1 InDel), in the current study we compared the diversity and population structure of 94 local landraces and 85 current breeding lines of pepper in China. The results showed that the Shannon Diversity indices of 9 qualitative traits and 8 quantitative traits in current breeding lines were greater than those of landraces, of which 11 were fruit organ-related traits. Compared with current breeding lines, the mean values of Gene Diversity index and Polymorphism Information content of local landraces were higher by 0.08 and 0.09, respectively. Population structure and phylogenetic tree analysis showed that the 179 germplasm resources could be divided into two taxa, dominated by local landraces and current breeding lines, respectively. The above results indicated that the diversity of quantitative traits of current breeding lines were higher than that of local landraces, especially traits related to fruit organs, but the genetic diversity based on molecular markers was lower than that of local landraces. Therefore, in the future breeding process, we should not only focus on the selection of target traits, but also strengthen the background selection based on molecular markers. Moreover, the genetic information of other domesticated species and wild species will be transferred to the breeding lines through interspecific crosses to expand the genetic background of the breeding material.


Assuntos
Variação Genética , Melhoramento Vegetal , Genótipo , Filogenia , Frutas
4.
Front Oncol ; 13: 1086963, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36816913

RESUMO

Lip verrucous carcinoma is a rare low-grade neoplasm, with an unsightly appearance and locally aggressive nature. Treatment of verrucous carcinoma is as yet challenging, no well-defined guidelines for effective and safe management of this disease are available. A case of a patient with a huge verrucous carcinoma of the lower lip successfully treated by surgical excision and double Abbe flap reconstruction technique is presented, and striking features of lip locations of this tumor as well as their management are discussed.

5.
Med Chem ; 18(8): 895-902, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35142271

RESUMO

BACKGROUND: In recent years, the anticancer effects of biguanide drugs have received considerable attention. However, the effective concentration of biguanide drugs to kill cancer cells is relatively high. Thus, we focus on structural modification of biguanides to obtain better antitumor candidates. A previous study in our laboratory has found that a biguanide compound containing the n-heptyl group has potent anticancer activity. However, the effect of different substituents on the benzene ringside of the biguanides on the anti-proliferative activity is unknown. OBJECTIVE: A series of n-heptyl-containing biguanide derivatives whose benzene rings were modified by halogen substitution based on the intermediate derivatization method were further synthesized to find new compounds with improved antiproliferative activities. METHODS: Ten n-heptyl-containing biguanide derivatives were synthesized via established chemical procedures. The activities of these derivatives were explored by MTT assay, clonogenic assay, and scratch assay. The protein levels were detected via Western blotting to explore the underlying mechanisms. RESULTS: The optimal biguanide derivatives 10a-10c, 11d exhibited IC50 values of 2.21-9.59 µΜ for five human cancer cell lines, significantly better than the control drug proguanil. The results of clonogenic and scratch wound healing assays also confirmed the inhibitory effects of derivatives 10a- 10c, 11d on the proliferation and migration of human cancer cell lines. Western blot results demonstrated that one representative derivative, 10c upregulates the AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. CONCLUSION: All biguanide derivatives containing n-heptyl groups are more active than proguanil, indicating that the modification of n-heptyl-containing biguanide derivatives provides a novel approach for the development of novel high efficient antitumor drugs.


Assuntos
Antineoplásicos , Neoplasias , Antineoplásicos/química , Benzeno , Biguanidas/química , Biguanidas/farmacologia , Biguanidas/uso terapêutico , Linhagem Celular Tumoral , Proliferação de Células , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Neoplasias/tratamento farmacológico , Proguanil/farmacologia , Proguanil/uso terapêutico , Relação Estrutura-Atividade
6.
J Contam Hydrol ; 241: 103815, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-33964551

RESUMO

In the contaminant remediation of groundwater, the release history of contaminant sources and hydraulic conductivity field are two key parameters that need to know, but their actual values are difficult to obtain and can only be inversely identified by limited measured data. However, the process of solving the inverse problem needs to repeatedly call the forward model of contaminant transport, which is very time-consuming, especially for the high-dimensional inverse problems. In this study, based on the training data generated from a prior range of parameters (the release strength of contaminant sources and hydraulic conductivity at pilot points), the self-organizing maps (SOM) algorithm was employed to construct the surrogate model for the numerical model of contaminant transport in a simplified hypothetical aquifer, then the surrogate model was used to retrieve jointly the contaminant strength of sources and the hydraulic conductivity at pilot points, and the Kriging method of geostatistics was further used to process the estimated K-values at pilot points to obtain the hydraulic conductivity field. Also, to investigate the ability of the SOM-based surrogate model for retrieving both contaminant source strengths and hydraulic conductivity, we gradually expanded the prior range and increased the number of inversion terms in each prior range. Moreover, the robustness of the SOM-based surrogate model for inversion was illustrated by proposing the scarcity of data and different degrees of measurement error in the limited actual observation data. When the actual observation data is reduced by 2/3, the Root Mean Square Error (RMSE) of retrieving source strengths and hydraulic conductivity at pilot points are 1.07 and 0.09, respectively. The results indicated the SOM-based surrogate model shows remarkable inversion precision and robustness, and an accurate estimation of the actual hydraulic conductivity field could be obtained by the Kriging method based on that.


Assuntos
Água Subterrânea , Algoritmos , Condutividade Elétrica , Modelos Teóricos , Análise Espacial , Movimentos da Água
7.
Sci Rep ; 9(1): 3691, 2019 03 06.
Artigo em Inglês | MEDLINE | ID: mdl-30842649

RESUMO

Genome-wide identification of Insertion/Deletion polymorphisms (InDels) in Capsicum spp. was performed through comparing whole-genome re-sequencing data from two Capsicum accessions, C. annuum cv. G29 and C. frutescens cv. PBC688, with the reference genome sequence of C. annuum cv. CM334. In total, we identified 1,664,770 InDels between CM334 and PBC688, 533,523 between CM334 and G29, and 1,651,856 between PBC688 and G29. From these InDels, 1605 markers of 3-49 bp in length difference between PBC688 and G29 were selected for experimental validation: 1262 (78.6%) showed polymorphisms, 90 (5.6%) failed to amplify, and 298 (18.6%) were monomorphic. For further validation of these InDels, 288 markers were screened across five accessions representing five domesticated species. Of these assayed markers, 194 (67.4%) were polymorphic, 87 (30.2%) monomorphic and 7 (2.4%) failed. We developed three interspecific InDels, which associated with three genes and showed specific amplification in five domesticated species and clearly differentiated the interspecific hybrids. Thus, our novel PCR-based InDel markers provide high application value in germplasm classification, genetic research and marker-assisted breeding in Capsicum species.


Assuntos
Capsicum/genética , Marcadores Genéticos , Mutação INDEL , Sequenciamento Completo do Genoma/métodos , Cromossomos de Plantas , Filogenia , Polimorfismo Genético , Reprodutibilidade dos Testes , Sintenia
8.
Int J Mol Sci ; 19(4)2018 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-29596349

RESUMO

The NAM, ATAF1/2, and CUC2 (NAC) transcription factors form a large plant-specific gene family, which is involved in the regulation of tissue development in response to biotic and abiotic stress. To date, there have been no comprehensive studies investigating chromosomal location, gene structure, gene phylogeny, conserved motifs, or gene expression of NAC in pepper (Capsicum annuum L.). The recent release of the complete genome sequence of pepper allowed us to perform a genome-wide investigation of Capsicum annuum L. NAC (CaNAC) proteins. In the present study, a comprehensive analysis of the CaNAC gene family in pepper was performed, and a total of 104 CaNAC genes were identified. Genome mapping analysis revealed that CaNAC genes were enriched on four chromosomes (chromosomes 1, 2, 3, and 6). In addition, phylogenetic analysis of the NAC domains from pepper, potato, Arabidopsis, and rice showed that CaNAC genes could be clustered into three groups (I, II, and III). Group III, which contained 24 CaNAC genes, was exclusive to the Solanaceae plant family. Gene structure and protein motif analyses showed that these genes were relatively conserved within each subgroup. The number of introns in CaNAC genes varied from 0 to 8, with 83 (78.9%) of CaNAC genes containing two or less introns. Promoter analysis confirmed that CaNAC genes are involved in pepper growth, development, and biotic or abiotic stress responses. Further, the expression of 22 selected CaNAC genes in response to seven different biotic and abiotic stresses [salt, heat shock, drought, Phytophthora capsici, abscisic acid, salicylic acid (SA), and methyl jasmonate (MeJA)] was evaluated by quantitative RT-PCR to determine their stress-related expression patterns. Several putative stress-responsive CaNAC genes, including CaNAC72 and CaNAC27, which are orthologs of the known stress-responsive Arabidopsis gene ANAC055 and potato gene StNAC30, respectively, were highly regulated by treatment with different types of stress. Our results also showed that CaNAC36 plays an important role in the interaction network, interacting with 48 genes. Most of these genes are in the mitogen-activated protein kinase (MAPK) family. Taken together, our results provide a platform for further studies to identify the biological functions of CaNAC genes.


Assuntos
Capsicum , Cromossomos de Plantas , Regulação da Expressão Gênica de Plantas/fisiologia , Redes Reguladoras de Genes , Filogenia , Proteínas de Plantas , Regiões Promotoras Genéticas , Proteínas Repressoras , Capsicum/genética , Capsicum/metabolismo , Cromossomos de Plantas/genética , Cromossomos de Plantas/metabolismo , Estudo de Associação Genômica Ampla , Proteínas de Plantas/biossíntese , Proteínas de Plantas/genética , Proteínas Repressoras/biossíntese , Proteínas Repressoras/genética
9.
Theor Appl Genet ; 130(1): 41-52, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27650192

RESUMO

KEY MESSAGE: Next-generation sequencing enabled a fast discovery of QTLs controlling CMV resistant in pepper. The gene CA02g19570 as a possible candidate gene of qCmr2.1 was identified for resistance to CMV in pepper. Cucumber mosaic virus (CMV) is one of the most important viruses infecting pepper, but the genetic basis of CMV resistance in pepper is elusive. In this study, we identified a candidate gene for CMV resistance QTL, qCmr2.1 through SLAF-seq. Segregation analysis in F2, BC1 and F2:3 populations derived from a cross between two inbred lines 'PBC688' (CMV-resistant) and 'G29' (CMV-susceptible) suggested quantitative inheritance of resistance to CMV in pepper. Genome-wide comparison of SNP profiles between the CMV-resistant and CMV-susceptible bulks constructed from an F2 population identified two QTLs, designated as qCmr2.1 on chromosome 2 and qCmr11.1 on chromosome 11 for resistance to CMV in PBC688, which were confirmed by InDel marker-based classical QTL mapping in the F2 population. As a major QTL, joint SLAF-seq and traditional QTL analysis delimited qCmr2.1 to a 330 kb genomic region. Two pepper genes, CA02g19570 and CA02g19600, were identified in this region, which are homologous with the genes LOC104113703, LOC104248995, LOC102603934 and LOC101248357, which were predicted to encode N-like protein associated with TMV-resistant in Solanum crops. Quantitative RT-PCR revealed higher expression levels of CA02g19570 in CMV resistance genotypes. The CA02g19600 did not exhibit obvious regularity in expression patterns. Higher relative expression levels of CA02g19570 in PBC688 and F1 were compared with those in G29 during days after inoculation. These results provide support for CA02g19570 as a possible candidate gene of qCmr2.1 for resistance to CMV in pepper.


Assuntos
Capsicum/genética , Cucumovirus , Resistência à Doença/genética , Doenças das Plantas/genética , Locos de Características Quantitativas , Capsicum/virologia , Mapeamento Cromossômico , DNA de Plantas/genética , Genes de Plantas , Marcadores Genéticos , Genótipo , Mutação INDEL , Padrões de Herança , Doenças das Plantas/virologia , Polimorfismo de Nucleotídeo Único , Análise de Sequência de DNA/métodos
10.
Bioorg Chem ; 69: 29-36, 2016 12.
Artigo em Inglês | MEDLINE | ID: mdl-27669118

RESUMO

1,3,4-Thiadiazole derivatives bearing Schiff base moieties were designed, synthesized, and their tyrosinase inhibitory activities were evaluated. Some compounds displayed potent tyrosinase inhibitory activities, especially, 4-(((5-mercapto-1,3,4-thiadiazol-2-yl)-imino)methyl)-2-methoxy-phenol (14) exhibited superior inhibitory effect to the other compounds with an IC50 value of 0.036µM. The structure-activity relationships (SARs) were preliminarily discussed and docking studies showed compound 14 had strong binding affinity to mushroom tyrosinase. Hydroxy might be the active groups. The inhibition kinetics study revealed that compounds (13 and 14) inhibited tyrosinase by acting as uncompetitive inhibitors. The LD50 value of the compound 14 was 5000mg/kg.


Assuntos
Inibidores Enzimáticos/farmacologia , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Tiadiazóis/farmacologia , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Estrutura Molecular , Monofenol Mono-Oxigenase/metabolismo , Bases de Schiff/síntese química , Bases de Schiff/química , Bases de Schiff/farmacologia , Relação Estrutura-Atividade , Tiadiazóis/síntese química , Tiadiazóis/química
11.
Eur J Med Chem ; 118: 266-75, 2016 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-27132164

RESUMO

G-quadruplex ligands have been touted as potential anticancer agents, however, none of the reported G-quadruplex-interactive small molecules have gone past phase II clinical trials. Recently it was revealed that diminazene (berenil, DMZ) actually binds to G-quadruplexes 1000 times better than DNA duplexes, with dissociation constants approaching 1 nM. DMZ however does not have strong anticancer activities. In this paper, using a panel of biophysical tools, including NMR, FRET melting assay and FRET competition assay, we discovered that monoamidine analogues of DMZ bearing alkyne substitutes selectively bind to G-quadruplexes. The lead DMZ analogues were shown to be able to target c-MYC G-quadruplex both in vitro and in vivo. Alkyne DMZ analogues display respectable anticancer activities (single digit micromolar GI50) against ovarian (OVCAR-3), prostate (PC-3) and triple negative breast (MDA-MB-231) cancer cell lines and represent interesting new leads to develop anticancer agents.


Assuntos
Alcinos/química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Diminazena/metabolismo , Diminazena/farmacologia , Quadruplex G , Antineoplásicos/química , Sequência de Bases , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Diminazena/química , Humanos , Proteínas Proto-Oncogênicas c-myc/genética , Proteínas Proto-Oncogênicas c-myc/metabolismo , Telomerase/antagonistas & inibidores
12.
Front Plant Sci ; 7: 211, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26941768

RESUMO

The WRKY family of transcription factors is one of the most important families of plant transcriptional regulators with members regulating multiple biological processes, especially in regulating defense against biotic and abiotic stresses. However, little information is available about WRKYs in pepper (Capsicum annuum L.). The recent release of completely assembled genome sequences of pepper allowed us to perform a genome-wide investigation for pepper WRKY proteins. In the present study, a total of 71 WRKY genes were identified in the pepper genome. According to structural features of their encoded proteins, the pepper WRKY genes (CaWRKY) were classified into three main groups, with the second group further divided into five subgroups. Genome mapping analysis revealed that CaWRKY were enriched on four chromosomes, especially on chromosome 1, and 15.5% of the family members were tandemly duplicated genes. A phylogenetic tree was constructed depending on WRKY domain' sequences derived from pepper and Arabidopsis. The expression of 21 selected CaWRKY genes in response to seven different biotic and abiotic stresses (salt, heat shock, drought, Phytophtora capsici, SA, MeJA, and ABA) was evaluated by quantitative RT-PCR; Some CaWRKYs were highly expressed and up-regulated by stress treatment. Our results will provide a platform for functional identification and molecular breeding studies of WRKY genes in pepper.

13.
Bioorg Med Chem Lett ; 26(7): 1715-9, 2016 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-26920798

RESUMO

Anisodamine was isolated from the medicinal herb, it was used in the treatment of gastrointestinal smooth muscle spasm, infective toxic shock and organophosphorus intoxication. But there is no report about anisodamine with α-glucosidase inhibitory activity. In order to find novel α-glucosidase inhibitors, a series of α-substituted arylacetates derivatives have been synthesized based on the active unit of anisodamine. In α-glucosidase assay, compound 9 in Schiff base form and compound 22 in ester form show strong inhibition against α-glucosidase with IC50 value of 46.81µM and 83.76µM, respectively. Compounds 9 and 22 exhibit comparable good antidiabetic activities as commercial drug Glimepiride. In addition, Schiff bases of α-substituted arylacetates show antitumor activities against human cancer cell lines, where compound 9 with thiourea moiety performs the best antitumor activity. We anticipate that our research will provide potential candidate scaffolds for antidiabetic drug design.


Assuntos
Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Alcaloides de Solanáceas/química , Alcaloides de Solanáceas/farmacologia , Acetatos/síntese química , Acetatos/química , Acetatos/farmacologia , Acetatos/uso terapêutico , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Linhagem Celular Tumoral , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/uso terapêutico , Humanos , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Neoplasias/tratamento farmacológico , Ratos , Alcaloides de Solanáceas/síntese química , Alcaloides de Solanáceas/uso terapêutico , Relação Estrutura-Atividade , alfa-Glucosidases/metabolismo
14.
Bioorg Med Chem Lett ; 25(22): 5142-6, 2015 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-26471089

RESUMO

Twenty aloe-emodin derivatives were designed, synthesized, and their biological activities were evaluated. Some compounds displayed potent tyrosinase inhibitory activities, especially, compounds with thiosemicarbazide moiety showed more potent inhibitory effects than the other compounds. The structure-activity relationships (SARs) were preliminarily discussed. The inhibition mechanism of selected compounds 1 and 13 were investigated. The results showed compound 1 was reversible inhibitor, however, compound 13 was irreversible. Kinetic analysis indicated that compound 1 was competitive tyrosinase inhibitor. Furthermore, the antibacterial activities and anti-inflammatory activities of some selected compounds were also screened. The results showed that compound 3 exhibited more potent antibacterial activity than the aloe-emodin, compounds 5 and 6 possessed more potent anti-inflammatory activities than the diacerein.


Assuntos
Antibacterianos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Emodina/análogos & derivados , Emodina/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Agaricales , Animais , Antraquinonas/farmacologia , Antibacterianos/síntese química , Anti-Inflamatórios não Esteroides/síntese química , Emodina/síntese química , Camundongos , Monofenol Mono-Oxigenase/química , Pironas/farmacologia , Relação Estrutura-Atividade
15.
Hua Xi Kou Qiang Yi Xue Za Zhi ; 33(3): 281-5, 2015 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-26281258

RESUMO

OBJECTIVE: To examine the benefits of anterolateral thigh myocutaneous flaps in reconstruction of oral and maxillofacial defects. METHODS: Patients were recruited from February 2002 to June 2013 in the Department of Oral and Maxillofacial Surgery of Central South University. All patients (1,185 patients, 1,212 transferred flaps) underwent reconstructive surgery employing anterolateral thigh myocutaneous flaps. Basic information for all patients including defect side, flap size and type, recipient vessel processing method, donor complications, and postoperative quality of life were recorded and statistically analyzed. RESULTS: Among the 1 212 transferred flaps, 1 176 survived and 36 showed necrosis, for a survival rate of about 97.0%. No cases presented with local serious complications, and 90% of patients achieved good functional recovery and aesthetically acceptable results after reconstruction of oral and maxillofacial defects at various locations using anterolateral thigh myocutaneous flaps. The time for anastomosis of one vein was significantly less than that for two veins (P=-0.000 3), which indicated one vein anastomosis could significantly reduce the operating time. The incidence of venous crisis, the survival rate after treatment, and the rate of venous crisis resulting in flap necrosis were comparable between the groups (P>0.05). CONCLUSION: Anterolateral thigh myocutaneous flaps can be easily obtained and provide a good amount of muscle for filling dead space and fascia lata. These flaps can meet the various requirements of oral and maxillofacial defects. Therefore, the anterolateral thigh myocutaneous free flaps are more suitable for oral and maxillofacial defects than other flaps.


Assuntos
Anormalidades Maxilofaciais/cirurgia , Retalho Miocutâneo , Procedimentos de Cirurgia Plástica/métodos , Coxa da Perna , Retalhos de Tecido Biológico , Humanos , Necrose , Qualidade de Vida , Procedimentos de Cirurgia Plástica/estatística & dados numéricos , Cirurgia Bucal , Cicatrização
16.
Curr Pharm Des ; 21(16): 2136-46, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25578891

RESUMO

Molecular imaging enables noninvasive characterization, quantification and visualization of biological and pathological processes in vivo at cellular and molecular level. It plays an important role in drug discovery and development. The skillful use of molecular imaging can provide unique insights into disease processes, which greatly aid in identifications of target. Importantly, molecular imaging is widely applied in the pharmacodynamics study to provide earlier endpoints during the preclinical drug development process, since it can be applied to monitor the effects of treatment in vivo with the use of biomarkers. Herein, we reviewed the application of molecular imaging technologies in antitumor drug development process ranging from identification of targets to evaluation of therapeutic effect.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/uso terapêutico , Descoberta de Drogas/métodos , Imagem Molecular/métodos , Neoplasias/tratamento farmacológico , Animais , Apoptose/efeitos dos fármacos , Descoberta de Drogas/tendências , Avaliação Pré-Clínica de Medicamentos/métodos , Avaliação Pré-Clínica de Medicamentos/tendências , Humanos , Imagem Molecular/tendências , Neoplasias/diagnóstico
17.
Shanghai Kou Qiang Yi Xue ; 24(6): 743-7, 2015 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-27063131

RESUMO

PURPOSE: To investigate the characteristics of cervical lymph node metastasis in oral squamous cell carcinoma (OSCC), and the relationship between clinicopathologic factors of OSCC and cervical lymph node metastasis (CLNM). METHODS: Clinicopathologic data of 708 patients with OSCC who underwent neck dissection were retrospectively analyzed. The relationship between clinicopathologic factors of OSCC and CLNM was analyzed with univariate analysis and multivariate analysis using SPPPSS19.0 software package. RESULTS: The incidence of CLNM of OSCC was 35.6%(252/708), and the incidence of CLNM at each level was:levelⅠ30.7%(149/485), level II33.8% (164/485), level III22.5% (109/485), level Ⅳ8.0% (39/485), and levelⅤ4.9% (24/485), respectively. From univariate analysis of the results, age, differentiation degree, depth of invasion, pathological T stage were significantly correlated with CLNM (P<0.05); while gender, location were not significantly correlated with CLNM (P>0.05). From multivariate analysis of the results, only differentiation degree, depth of invasion and pathological T stage were significantly correlated with CLNM (P<0.05). Depth of invasion was probably the most important influential factor for CLNM of OSCC (OR=2.191). CONCLUSIONS: There was positive relationship between CLNM and pathological T stage , depth of invasion; while there was negative relationship between CLNM and differentiation degree. Depth of invasion was probably the first influential factor for CLNM of OSCC.


Assuntos
Carcinoma de Células Escamosas/patologia , Metástase Linfática , Neoplasias Bucais/patologia , Carcinoma de Células Escamosas/diagnóstico , Humanos , Linfonodos , Neoplasias Bucais/diagnóstico , Análise Multivariada , Pescoço , Esvaziamento Cervical , Estudos Retrospectivos
18.
Br J Oral Maxillofac Surg ; 53(2): 148-52, 2015 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-25497587

RESUMO

Reconstruction of through-and-through oral and maxillofacial defects has always been difficult. We have evaluated the feasibility and reconstructive efficacy of chimeric flaps pedicled with the lateral circumflex femoral artery in the reconstruction of 41 through-and-through oral and maxillofacial defects after resections for cancer. There were 29 chimeric anterolateral thigh and anterolateral thigh flaps and 12 chimeric anterolateral thigh and anteromedial thigh flaps, the sizes of which ranged from 5×8 to 9×11 cm. The chimeric flaps provided separate flaps to reconstruct the intraoral mucosa and extraoral skin defects, and 40/41 of them survived. The appearance and function were satisfactory in all patients after the reconstruction. Chimeric flaps pedicled with the lateral circumflex femoral artery are a good choice for the reconstruction of through-and-through oral and maxillofacial defects.


Assuntos
Neoplasias Faciais/cirurgia , Artéria Femoral/transplante , Neoplasias Bucais/cirurgia , Procedimentos de Cirurgia Plástica/métodos , Transplante de Pele/métodos , Retalhos Cirúrgicos/classificação , Tecido Adiposo/transplante , Adulto , Idoso , Carcinoma de Células Escamosas/cirurgia , Estética , Estudos de Viabilidade , Feminino , Seguimentos , Sobrevivência de Enxerto , Humanos , Masculino , Pessoa de Meia-Idade , Músculo Esquelético/transplante , Estadiamento de Neoplasias , Complicações Pós-Operatórias , Estudos Retrospectivos , Neoplasias Cutâneas/cirurgia , Retalhos Cirúrgicos/irrigação sanguínea , Retalhos Cirúrgicos/transplante , Coxa da Perna/cirurgia , Sítio Doador de Transplante/cirurgia , Resultado do Tratamento
19.
Hua Xi Kou Qiang Yi Xue Za Zhi ; 32(5): 476-9, 2014 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-25490826

RESUMO

OBJECTIVE: To seek a new method for reconstructing bilateral intemrnal jugular vein invaded by metastasis lymph node in advanced oral cancer patients. METHODS: A combination of microvascular anastomosis and longitudinal constriction suture venoplasty was performed to reconstruct internal jugular vein. We resected the part of the bilateral internal jugular vein of advanced oral cancer patients invaded by metastasis lymph node and used the external carotid vein to reconstruct the internal jugular vein. A part of the vessel wall of the internal jugular vein could also be resected to reconstruct the vein. Longitudinal constriction suture venoplasty could slowly narrow the lumen diameter of the internal jugular vein. Thus, difference in anastomosis diameter should be avoided because it generates eddy currents and subsequently causes blood clots. A total of five advanced cases of oral squamous cell carcinoma were involved in this study. We performed bilateral radical neck dissection on all patients to reconstruct the internal jugular vein and observed their postoperative conditions. RESULTS: Postopera-tive follow-up of 5 months to 19 months was performed on all patients. Doppler or CT angiography and related tests showed no internal jugular vein thrombosis. No patient with facial edema, throat swelling, cerebral edema, and high intracranial pressure or other serious complications caused by blocked venous blood was observed. The one-year survival rate of five patients was 60% (3/5). CONCLUSION: Microvascular anastomosis combined with longitudinal constriction suture venoplasty is a new method for reconstructing internal jugular vein. This method was proved successful and clinically feasible.


Assuntos
Carcinoma de Células Escamosas , Veias Jugulares , Neoplasias Bucais , Procedimentos de Cirurgia Plástica , Constrição , Humanos , Metástase Linfática , Esvaziamento Cervical , Período Pós-Operatório , Suturas
20.
Sensors (Basel) ; 14(7): 11805-24, 2014 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-24999715

RESUMO

Laser scan matching with grid-based maps is a promising tool for real-time indoor positioning of mobile Unmanned Ground Vehicles (UGVs). While there are critical implementation problems, such as the ability to estimate the position by sensing the unknown indoor environment with sufficient accuracy and low enough latency for stable vehicle control, further development work is necessary. Unfortunately, most of the existing methods employ heuristics for quick positioning in which numerous accumulated errors easily lead to loss of positioning accuracy. This severely restricts its applications in large areas and over lengthy periods of time. This paper introduces an efficient real-time mobile UGV indoor positioning system for large-area applications using laser scan matching with an improved probabilistically-motivated Maximum Likelihood Estimation (IMLE) algorithm, which is based on a multi-resolution patch-divided grid likelihood map. Compared with traditional methods, the improvements embodied in IMLE include: (a) Iterative Closed Point (ICP) preprocessing, which adaptively decreases the search scope; (b) a totally brute search matching method on multi-resolution map layers, based on the likelihood value between current laser scan and the grid map within refined search scope, adopted to obtain the global optimum position at each scan matching; and (c) a patch-divided likelihood map supporting a large indoor area. A UGV platform called NAVIS was designed, manufactured, and tested based on a low-cost robot integrating a LiDAR and an odometer sensor to verify the IMLE algorithm. A series of experiments based on simulated data and field tests with NAVIS proved that the proposed IMEL algorithm is a better way to perform local scan matching that can offer a quick and stable positioning solution with high accuracy so it can be part of a large area localization/mapping, application. The NAVIS platform can reach an updating rate of 12 Hz in a feature-rich environment and 2 Hz even in a feature-poor environment, respectively. Therefore, it can be utilized in a real-time application.

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