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1.
J Chem Ecol ; 2024 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-38372833

RESUMO

The melon fly, Zeugodacus cucurbitae (Coquillett), is a major invasive pest, widely distributed in the Asia-Pacific region and some parts of Africa. Melon fly attractants could improve the effectiveness of current pest management measures. Previous studies have shown that some host fruits are attractive to melon flies but few have investigated the chemical compounds responsible for their attraction. In this study, we aimed to identify the volatile compounds from Luffa acutangula L that attract Z. cucurbitae. In headspace trapping, chemical profiling identified 19 compounds from ridge gourds, with 1-pentadecene being the major component. EAG results revealed that seven compounds elicited antennal responses in Z. cucurbitae, and significant differences in antennal responses between male and female Z. cucurbitae adults were recorded to p-xylene, alpha-pinene, and 1-octadecene. Behavioral experiments demonstrated that the EAG-active compounds methyl isovalerate and methyl myristate had either attractive or repellent effects on Z. cucurbitae at different concentrations, and 1-octadecene attracted Z. cucurbitae. Our findings provide a theoretical basis producing repellents or attractants for effective Integrated Pest Management of Z. cucurbitae.

3.
Int J Mol Sci ; 24(23)2023 Dec 02.
Artigo em Inglês | MEDLINE | ID: mdl-38069395

RESUMO

Zn2+-dependent histone deacetylases (HDACs) are enzymes that regulate gene expression by removing acetyl groups from histone proteins. These enzymes are essential in all living systems, playing key roles in cancer treatment and as potential pesticide targets. Previous phylogenetic analyses of HDAC in certain species have been published. However, their classification and evolutionary origins across biological kingdoms remain unclear, which limits our understanding of them. In this study, we collected the HDAC sequences from 1451 organisms and performed analyses. The HDACs are found to diverge into three classes and seven subclasses under divergent selection pressure. Most subclasses show species specificity, indicating that HDACs have evolved with high plasticity and diversification to adapt to different environmental conditions in different species. In contrast, HDAC1 and HDAC3, belonging to the oldest class, are conserved and crucial in major kingdoms of life, especially HDAC1. These findings lay the groundwork for the future application of HDACs.


Assuntos
Histonas , Zinco , Filogenia , Zinco/metabolismo , Histona Desacetilase 1/genética , Histona Desacetilase 1/metabolismo
4.
Sci Data ; 10(1): 848, 2023 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-38040744

RESUMO

The fruit fly Zeugodacus tau (Diptera: Tephritidae) is a major pest of melons and other cucurbits in Southeast Asia. In this study, we used Illumina, Nanopore, and Hi-C sequencing technologies to assemble a reference genome of Z. tau at the chromosomal level. The assembled genome was 421.79 Mb and consisted of six chromosomes (one X-chromosome + five autosomes). The contig N50 was 4.23 Mb. We identified 20,922 protein-coding genes, of which 17,251 (82.45%) were functionally annotated. Additionally, we found 247 rRNAs, 435 tRNAs, 67 small nuclear RNAs, and 829 small RNAs in the genome. Repetitive elements accounted for 55.30 Mb (13.15%) of the genome. This high-quality genome assembly is valuable for evolutionary and genetic studies of Z. tau and its relative species.


Assuntos
Genoma de Inseto , Tephritidae , Animais , Cromossomos , Anotação de Sequência Molecular , Filogenia , Sequências Repetitivas de Ácido Nucleico , Tephritidae/genética
5.
Drug Des Devel Ther ; 17: 3151-3167, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37876500

RESUMO

Objective: Traditional Chinese medicine Polygonum cuspidatum (PC) has significant effects on reducing pain. In this study, we investigated the analgesic effects of the alcohol extract of PC on three types of inflammatory pain and explored its mechanism. Methods: Potential targets for the analgesic effects of the main active components of PC alcohol extract were screened by network pharmacology and molecular docking. Three different inflammatory pain mouse models (acetic acid twisting, formalin foot swelling, and xylene ear swelling) were used to study the analgesic effects of PC. The expression of latent signaling pathways in L4-6 spinal cord tissues in formalin foot swelling mice was evaluated using real-time qPCR (RT-qPCR), Western blot (WB), and immunohistochemistry (IHC) analyses. Results: Network pharmacology analysis shows that PC analgesic mechanism is related to the MAPK/ERK signaling pathway. The five main active components of PC have good docking ability with JNK and p38. PC alcohol extract significantly reduced the pain behavior and alleviated inflammatory reactions in three mouse models, inhibited the mRNA and protein phosphorylation levels of JNK, ERK, p38, and CREB in spinal cord tissues. Conclusion: PC alcohol extract can inhibit inflammation and alleviate pain, which is related to its inhibition of the MAPK/ERK signaling pathway in spinal cord. Thus, PC alcohol extract is a promising candidate for pain treatment.


Assuntos
Fallopia japonica , Ratos , Camundongos , Animais , Fallopia japonica/química , Ratos Sprague-Dawley , Simulação de Acoplamento Molecular , Dor/tratamento farmacológico , Transdução de Sinais , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Etanol , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Modelos Animais de Doenças , Formaldeído/farmacologia
6.
Cell Death Dis ; 14(4): 234, 2023 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-37005437

RESUMO

The 5-year survival rate of non-small cell lung cancer (NSCLC) patients is very low. MicroRNAs (miRNAs) are involved in the occurrence of NSCLC. miR-122-5p interacts with wild-type p53 (wtp53), and wtp53 affects tumor growth by inhibiting the mevalonate (MVA) pathway. Therefore, this study aimed to evaluate the role of these factors in NSCLC. The role of miR-122-5p and p53 was established in samples from NSCLC patients, and human NSCLC cells A549 using the miR-122-5p inhibitor, miR-122-5p mimic, and si-p53. Our results showed that inhibiting miR-122-5p expression led to the activation of p53. This inhibited the progression of the MVA pathway in the NSCLC cells A549, hindered cell proliferation and migration, and promoted apoptosis. miR-122-5p was negatively correlated with p53 expression in p53 wild-type NSCLC patients. The expression of key genes in the MVA pathway in tumors of p53 wild-type NSCLC patients was not always higher than the corresponding normal tissues. The malignancy of NSCLC was positively correlated with the high expression of the key genes in the MVA pathway. Therefore, miR-122-5p regulated NSCLC by targeting p53, providing potential molecular targets for developing targeted drugs.


Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , MicroRNAs , Humanos , Carcinoma Pulmonar de Células não Pequenas/patologia , Neoplasias Pulmonares/patologia , Ácido Mevalônico , Proteína Supressora de Tumor p53/genética , Proteína Supressora de Tumor p53/metabolismo , MicroRNAs/genética , MicroRNAs/metabolismo , Proliferação de Células/genética , Regulação Neoplásica da Expressão Gênica , Movimento Celular/genética , Linhagem Celular Tumoral
7.
Drug Discov Today ; 28(5): 103546, 2023 05.
Artigo em Inglês | MEDLINE | ID: mdl-36871844

RESUMO

As major forces for modulating protein folding and molecular recognition, cation and π interactions are extensively identified in protein structures. They are even more competitive than hydrogen bonds in molecular recognition, thus, are vital in numerous biological processes. In this review, we introduce the methods for the identification and quantification of cation and π interactions, provide insights into the characteristics of cation and π interactions in the natural state, and reveal their biological function together with our developed database (Cation and π Interaction in Protein Data Bank; CIPDB; http://chemyang.ccnu.edu.cn/ccb/database/CIPDB). This review lays the foundation for the in-depth study of cation and π interactions and will guide the use of molecular design for drug discovery.


Assuntos
Descoberta de Drogas , Proteínas , Modelos Moleculares , Proteínas/metabolismo , Cátions/química
8.
Insects ; 14(2)2023 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-36835759

RESUMO

The olfactory system plays a key role in various insect behaviors, and odorant-binding proteins participate in the first step of the olfactory process. Ophraella communa Lesage is an oligophagous phytophagous insect that is a specific biological control agent for Ambrosia artemisiifolia L. The leaf beetle must identify and locate A. artemisiifolia through olfaction; however, its odorant-binding protein (OBP) function has not yet been reported. In this study, OcomOBP7 was cloned, and its tissue expression profile and binding ability were analyzed using RT-qPCR and fluorescence binding assays, respectively. Sequence analysis demonstrated that OcomOBP7 belongs to the classical OBP family. The RT-qPCR results showed that OcomOBP7 was specifically expressed in the antennae, indicating that OcomOBP7 may be involved in chemical communication. The fluorescence binding assay showed that OcomOBP7 has an extensive binding ability to alkenes. The electroantennography experiments showed that O. communa antennal response to α-pinene and ocimene decreased significantly after interference because the two odors specifically bound to OcomOBP7. In summary, α-pinene and ocimene are odorant ligands corresponding to OcomOBP7, indicating that OcomOBP7 is involved in the chemical recognition of A. artemisiifolia. Our study lays a theoretical foundation for research into O. communa attractants, which is helpful for the better biological control of A. artemisiifolia by O. communa.

9.
Insects ; 13(2)2022 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-35206756

RESUMO

Ophraella communa is an efficient biocontrol agent used against the invasive weed Ambrosia artemisiifolia. It is an herbivorous insect that feeds on specific plants; the olfactory functions of this insects plays an important role in their search for host plants. There are no reports on O. communa sensilla types, morphology, or chemosensory protein (CSP) genes. In this study, we observed the external structure and distribution of antennal sensilla in adult O. communa antennae by scanning electron microscopy; moreover, we cloned 11 CSPs (CSP1-CSP11) and elucidated their tissue-expression profiles using quantitative real-time polymerase chain reaction. Six types of sensilla were identified: sensilla trichodea (including two subtypes), sensilla chaetica, sensilla basiconica (including two subtypes), sensilla styloconica, sensilla coeloconica, and Böhm bristles. Both male and female antennae had all six types of sensilla, and no sexual dimorphism was noted in sensillar types or distribution. We also found that the expression levels of CSP2, CSP3, CSP4, CSP6, and CSP7 in male and female antennae were higher than those in other tissues, which suggests that these five CSPs may be related to olfactory function in O. communa. Ultimately, our results lay the foundation for interpreting the olfactory functions of adult O. communa.

10.
Front Physiol ; 11: 518876, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33324230

RESUMO

Glucose metabolism is a biologically important metabolic process. Glycogen synthase kinase (GSK-3) is a key enzyme located in the middle of the sugar metabolism pathway that can regulate the energy metabolism process in the body through insulin signaling. This paper mainly explores the regulatory effect of glycogen synthase kinase on the metabolism of glycogen and trehalose in the brown planthopper (Nilaparvata lugens) by RNA interference. In this paper, microinjection of the target double-stranded GSK-3 (dsGSK-3) effectively inhibited the expression of target genes in N. lugens. GSK-3 gene silencing can effectively inhibit the expression of target genes (glycogen phosphorylase gene, glycogen synthase gene, trehalose-6-phosphate synthase 1 gene, and trehalose-6-phosphate synthase 2 gene) in N. lugens and trehalase activity, thereby reducing glycogen and glucose content, increasing trehalose content, and regulating insect trehalose balance. GSK-3 can regulate the genes chitin synthase gene and glucose-6-phosphate isomerase gene involved in the chitin biosynthetic pathway of N. lugens. GSK-3 gene silencing can inhibit the synthesis of chitin N. lugens, resulting in abnormal phenotypes and increased mortality. These results indicated that a low expression of GSK-3 in N. lugens can regulate the metabolism of glycogen and trehalose through the insulin signal pathway and energy metabolism pathway, and can regulate the biosynthesis of chitin, which affects molting and wing formation. The relevant research results will help us to more comprehensively explore the molecular mechanism of the regulation of energy and chitin metabolism of insect glycogen synthase kinases in species such as N. lugens.

11.
Arch Insect Biochem Physiol ; 105(1): e21721, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32557787

RESUMO

The alligator weed flea beetle, Agasicles hygrophila is a monophagous natural enemy of the invasive alligator weed Alternanthera philoxeroides. Oogenesis plays a vital role in the process of individual development and population continuation of oviparous insects. Sox is an ancient and ubiquitous metazoan gene family that plays a key regulatory role in various physiological processes, including oogenesis, which is closely related to fecundity. In this study, two Sox genes AhDichaete and AhSox3 were cloned and characterized, and then the expression profiles of AhDichaete and AhSox3 were qualified by a quantitative reverse transcription-polymerase chain reaction. The result showed that these two Sox genes were expressed significantly higher in ovary, especially in the adult developmental stage. Furthermore, the functions of AhDichaete and AhSox3 in A. hygrophila females were studied using RNA interference (RNAi). Fewer offsprings were produced when AhDichaete and AhSox3 RNAi females mated with wild-type males. Moreover, dsAhSox3 injection reduced the hatching rate of eggs but injection with dsAhDichaete did not. Further study of the reproductive system of AhDichaete and AhSox3 RNAi females showed that yolk protein deposition reduction in the ovarioles, then the expression of vitellogenin gene AhVg2 in ovaries was decreased. These results indicate that AhDichaete and AhSox3 play an important regulatory role in the process of ovarian development and oogenesis by affecting yolk synthesis in the ovary of A. hygrophila.


Assuntos
Besouros/genética , Proteínas de Insetos/genética , Oogênese/genética , Fatores de Transcrição SOX/genética , Animais , Besouros/crescimento & desenvolvimento , Feminino , Proteínas de Insetos/metabolismo , Ovário/crescimento & desenvolvimento , Fatores de Transcrição SOX/metabolismo , Análise de Sequência de DNA
12.
J Insect Sci ; 19(5)2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31557289

RESUMO

Glucose-6-phosphatase (G6Pase) and hexokinase (HK) are two key enzymes in the glycolysis and gluconeogenesis pathways, which catalyze the synthesis and degradation of glucose in insects, respectively. G6Pase and HK play an important role in insect growth by regulating the metabolism of glucose, leading to the efficient metabolism of other macromolecules. However, it is unclear whether these genes could be investigated for pest control through their actions on chitin metabolism. We studied the potential functions of G6Pase and HK genes in the regulation of chitin metabolism pathways by RNAi technology. Interference with G6Pase expression did not affect trehalose and chitin metabolism pathways in brown planthopper, Nilaparvata lugens (Stål). However, knockdown of the HK gene resulted in a significant decrease of expression of genes associated with the trehalose metabolic pathway but had no significant effect on trehalase activity, trehalose content, or glucogen content. Additionally, HK knockdown resulting in downregulation of the genes involved in chitin metabolism in the brown planthopper. These insects also showed wing deformities and difficulty in molting to varying degrees. We suggest that the silencing of HK expression directly inhibited the decomposition of glucose, leading to impaired chitin synthesis.


Assuntos
Quitina/biossíntese , Glucose/metabolismo , Hemípteros/metabolismo , Animais , Glucose-6-Fosfatase/genética , Hemípteros/enzimologia , Hemípteros/genética , Hexoquinase/genética , Proteínas de Insetos/genética , Interferência de RNA , Trealose/metabolismo
13.
Int J Biol Macromol ; 121: 1135-1144, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30352227

RESUMO

The cotton mealybug, Phenacoccus solenopsis Tinsley (Hemipeta: Pseudoccoccidae), is an aggressively invasive pest causing huge economic losses of crops around the world. In this study, we developed genome-wide microsatellites for population genetic analysis of P. solenopsis. We obtained a random genome of P. solenopsis with a size of 267.07 Mb and scaffold N50 of 14.12 Kb. In total 115,639 microsatellites were isolated from the genome, of which those with trinucleotide motifs were the most abundant. Forty-two polymorphic loci were selected for primer validation based on three populations. Allele numbers varied from 2 to 5 with an average value of 2.5 per locus, and allelic richness ranged from 1.00 to 4.48. The observed heterozygosity (H0) and expected heterozygosity (HE) ranged from 0.00 to 0.92 and 0.00 to 0.73, respectively. Population genetic structure analysis based on the developed markers revealed strong differentiation between three populations of P. solenopsis collected from its invasive range in China. The microsatellites developed in our study should provide efficient genetic markers for population level studies of P. solenopsis to reveal invasion history and patterns of dispersal.


Assuntos
Genômica , Hemípteros/genética , Repetições de Microssatélites/genética , Animais , Genética Populacional , Espécies Introduzidas , Análise de Sequência de DNA
14.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-666570

RESUMO

OBJECTIVE To investigate the effect of phosphotyrosine interaction domain containing 1 (PID1, NYGGF4) on promotion of IR and HCC, and explore its underlying mechanisms. METHODS Lentivirus were used to mediate the knockdown of PID1 in HFD induced IR mouse model as well as ob/ob mice. Intraperitoneal glucose and insulin tolerance were performed 4 weeks after lentivirus injection. Hydrodynamics-based transfection was applied to inducethe liver specific overexpression of PID1. Flow cytometry was exerted to detect the proportion and function of immune cells. qRT-PCR and Western blot were used to detect the expression of downstream pathways of PID1.Immunoprecipitation was used to determine the receptor of PID1. Chromatin immunoprecipitation (ChIP) was operated to measure the modification of H3K4me3 of PID1 promoter. RESULTS PID1 restriction improved insulin resistance, hyperglycemia and fatty liver. Conversely, hepatic knockdown of PID1 attenuated liver xenografted tumor growth. Moreover, PID1 liver- specific protooncogenes via hydrodynamics- based transfection established a primary hepatocellular carcinoma mouse model, induced an immunosuppressive environment, with the reduction of CD3 +, CD4 +, CD8 +T cells, retarded maturation of dendritic cells (DCs), pronounced differentiation of regulatory T cells (Tregs), and recruitment of MDSC. In addition, PID1 overexpression activated proliferation related genes, promoted anti- inflammatory genes, suppressed pro-inflammatory genes, induced glycolysis and lipid metabolism genes to facilitate tumorigenesis in liver. Importantly, PID1 exerted its tumor-promoting function through binding to epidermal growth factor receptor (EGFR) and activation of downstream MAPK pathway. As such, PID1 exist trimethylation of histone H3 at lysine 4 (H3K4me3) modification and IR up-regulated the expression of PID1 by activation the H3K4me3 modification. CONCLUSION PID1 is a new gene that exerts both liver cancer-promoting and insulin resistance inducing function. IR accelerates liver cancer development and progression partially dependent on the activation of PID1.

15.
J Econ Entomol ; 109(4): 1586-94, 2016 08.
Artigo em Inglês | MEDLINE | ID: mdl-27270575

RESUMO

Insect development occurs within a specific temperature range. Constant temperature studies may produce misleading information on the eco-physiological impacts of temperature on the population dynamics of an insect species, as in most natural environments, temperature usually undergoes daily variation. In China, field surveys showed that the decline in the Agasicles hygrophila (Selman & Vogt) (Coleoptera: Chrysomelidae) population from early August to late September in summer resulted in difficulties in effectively controlling the population of Alternanthera philoxeroides (Mart.) Griseb (Amaranthaceae). Previous studies have largely ignored more natural, fluctuating conditions. In our study, we first investigated the impacts of different temperature conditions (25°C constant temperature for 20 h with a 4-h period of a high temperature of either 30°C, 33°C, 36°C, or 39°C) on adult reproduction and longevity, egg development time, egg hatch rate, female ovarian development, and oogenesis of A. hygrophila. Our results indicated that high temperatures of 30°C and 33°C did not affect the female ovarian development and oogenesis of A. hygrophila Contrarily, high temperatures of 36°C and 39°C negatively affected the population development of A. hygrophila. At 36°C and 39°C, the egg hatch rates were very low, and the egg development times significantly lengthened. The frequency of abnormal ovaries significantly rose at 39°C. We concluded that the decline in the A. hygrophila population during August and September may be related to the extreme high temperatures that frequently occur in summer. These results help provide a better understanding of A. hygrophila population dynamics under natural conditions.


Assuntos
Besouros/fisiologia , Temperatura Alta/efeitos adversos , Animais , Besouros/crescimento & desenvolvimento , Feminino , Longevidade , Masculino , Ovário/crescimento & desenvolvimento , Periodicidade , Dinâmica Populacional , Reprodução
16.
Yao Xue Xue Bao ; 51(2): 174-81, 2016 02.
Artigo em Chinês | MEDLINE | ID: mdl-29856196

RESUMO

Pancreatic cancer is one of the most lethal and intractable human malignancies with poor prognosis. Chronic pancreatitis is the independent risk factor for pancreatic cancer. Smoking, obesity and family history are the risk factors for chronic inflammation-associated pancreatic carcinogenesis. Recent studies of signal pathways have made a significant progress in our understanding of chronic pancreatitis in pancreatic cancer. This review summarizes recent development in the important signal pathways involved in pancreatic carcinogenesis from chronic pancreatitis.


Assuntos
Carcinogênese , Inflamação/complicações , Neoplasias Pancreáticas/complicações , Transdução de Sinais , Humanos , Inflamação/patologia , Obesidade , Pâncreas/fisiopatologia , Neoplasias Pancreáticas/patologia , Fatores de Risco , Fumar
17.
Sci Rep ; 5: 15691, 2015 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-26503138

RESUMO

Mutualistic ants can protect their partners from natural enemies in nature. Aenasius bambawalei is an important parasitoid of the the invasive mealybug Phenacoccus solenopsis. We hypothesized that mutualism between native ants and mealybugs would favor survival of mealybugs. To test this, we examined effects of tending by the native mutualistic ant Tapinoma melanocephalum on growth of P. solenopsis colonies on Chinese hibiscus, Hibiscus rosa-sinensis, in a field setting. Ant workers with access to honeydew of mealybugs lived much longer than those provisioned only with water in the laboratory, and number of ant workers foraging increased significantly with growth of mealybug colonies in the field. In later observations, there were significant differences in densities of mealybugs between ant-tended and -excluded treatments. Survival rate of mealybugs experiencing parasitoid attack was significantly higher on ant-tended plants than on ant-excluded plants. When the parasitoid was excluded, there was no difference in survival rate of mealybugs between ant-tended and -excluded plants. In most cases, ants directly attacked the parasitoid, causing the parasitoid to take evasive action. We conclude that native ants such as T. melanocephalum have the potential to facilitate invasion and spread of P. solenopsis in China by providing them with protection from parasitoids.


Assuntos
Formigas/fisiologia , Hemípteros/parasitologia , Simbiose , Animais , Comportamento Animal , Comportamento Alimentar , Hemípteros/crescimento & desenvolvimento , Longevidade , Plantas/parasitologia
18.
Arch Pharm Res ; 38(10): 1761-73, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-25724284

RESUMO

To identify novel therapeutic agents to treat cancer, we synthesized a series of diaryl ether derivatives. Structure-activity relationship studies revealed that the presence of a chlorine or hydroxyl at the para-position on the phenyl ring (5h or 5k) significantly enhanced antitumor activity. Compound 5h had stronger growth inhibitory activity in HepG2, A549, and HT-29 cells than compound 5k, with IC50 values of 2.57, 5.48, and 30.04 µM, respectively. Compound 5h also inhibited the growth of other cells lines, including Hep3B, PLC/PRF5, SMMC-7721, HeLa, and A375, with IC50 values of 2.76, 4.26, 29.66, 18.86, and 10.21 µM, respectively. The antitumor activity of compound 5h was confirmed by a colony forming assay. Further, our results indicated that the antitumor activity of compound 5h may be mediated by enhancing expression of p21 and cl-caspase3, and leading to apoptosis of cancer cells.


Assuntos
Antineoplásicos/farmacologia , Éteres/farmacologia , Neoplasias/tratamento farmacológico , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Caspase 3/genética , Linhagem Celular Tumoral , Inibidor de Quinase Dependente de Ciclina p21/genética , Éteres/síntese química , Éteres/química , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Células HT29 , Células HeLa , Humanos , Concentração Inibidora 50 , Neoplasias/patologia , Relação Estrutura-Atividade
19.
Chem Biol Drug Des ; 86(2): 223-31, 2015 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25430863

RESUMO

In this study, a series of novel N-(piperidine-4-yl)benzamide derivatives was designed, synthesized, and evaluated for antitumor activity. Some compounds were found to have potent antitumor activity. In particular, compound 47 showed the most potent biological activity against HepG2 cells, with an IC50 value of 0.25 µm. Western blot analysis demonstrated that compound 47 inhibited the expression of cyclin B1 and p-Rb and enhanced the expression of p21, p53, Rb, and phospho-adenosine monophosphate-activated protein kinase (p-AMPK). Further, cell cycle arrest was observed by flow cytometry (FCM). In summary, compound 47 was screened to have potential activity for the treatment of hepatocarcinoma via the induction of cell cycle arrest by a p53/p21-dependent pathway.


Assuntos
Antineoplásicos/farmacologia , Benzamidas/síntese química , Benzamidas/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Piperidinas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Benzamidas/química , Carcinoma Hepatocelular/patologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Inibidor de Quinase Dependente de Ciclina p21/metabolismo , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Concentração Inibidora 50 , Neoplasias Hepáticas/patologia , Piperidinas/síntese química , Piperidinas/química , Proteína Supressora de Tumor p53/metabolismo
20.
Environ Entomol ; 43(5): 1435-42, 2014 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-25203359

RESUMO

Ophraella communa LeSage (Coleoptera: Chrysomelidae) is an important biological control agent of the common ragweed, Ambrosia artemisiifolia L., in China. Development and fecundity of O. communa, and hatch rate of progeny eggs were studied at five photoperiods (8:16, 10:14, 12:12, 14:10, and 16:8 [L:D] h). The highest survival rate of eggs was 92% at the photoperiod of 16:8 (L:D) h, and those of both larvae and pupae were observed at the photoperiod of 14:10 (L:D) h (85 and 96%). The shortest developmental durations of larvae and pupae were observed at photoperiods of 14:10 and 16:8 (L:D) h. Fecundity was 1,159-1,976 eggs per female from photoperiods of 8:16 to 16:8 (L:D) h. The hatch rates of progeny eggs were 67-92% from photoperiods of 8:16 to 16:8 (L:D) h, and photoperiods did not affect developmental duration of progeny eggs. The intrinsic rate for increase (r), the net reproductive rate (r0), and the finite rate of increase (λ) reached the maximum values at 16:8 (L:D) h (0.2219 d(-1), 721 hatched eggs and 1.2484 d(-1), respectively) and 14:10 (L:D) h (0.2133 d(-1), 605.6 hatched eggs and 1.2378 d(-1), respectively). Their minimum values were observed at the photoperiod of 8:16 (L:D) h, which were 0.1731 d(-1), 212.2 hatched eggs and 0.1890 d(-1), respectively. The shortest T value was 29.7 d at a photoperiod of 16:8 (L:D) h and the longest was 31.4 d at a photoperiod of 12:12 (L:D) h. Our study shows that O. communa could survive and reproduce successfully at different photoperiods, thus may expand its distribution to regions with different photoperiods.


Assuntos
Agentes de Controle Biológico , Besouros/fisiologia , Aptidão Genética , Fotoperíodo , Ambrosia/crescimento & desenvolvimento , Animais , Besouros/genética , Besouros/crescimento & desenvolvimento , Feminino , Fertilidade , Larva/crescimento & desenvolvimento , Larva/fisiologia , Masculino , Óvulo/crescimento & desenvolvimento , Óvulo/fisiologia , Dinâmica Populacional , Pupa/crescimento & desenvolvimento , Pupa/fisiologia
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