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1.
Environ Res ; 216(Pt 2): 114465, 2023 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-36241075

RESUMO

Atmospheric Aerosol Optical Depth (AOD), derived from polar-orbiting satellites, has shown potential in PM2.5 predictions. However, this important source of data suffers from low temporal resolution. Recently, geostationary satellites provide AOD data in high temporal and spatial resolution. However, the feasibility of these data in PM2.5 prediction needs further study. In this paper, we analyzed the impact of AOD derived from Himawari-8 in PM2.5 predictions. Moreover, by combining wavelet, machine learning techniques, and minimum redundancy maximum relevance (mRMR), a novel hybrid model was proposed. The results showed that AOD missing rate over Yangtze River Delta region is the highest in Nanjing, Hefei, and Maanshan. In addition, missing rates are the lowest in winter and summer (∼80%). Moreover, we found that considering AOD, as an auxiliary variable in the model, could not improve the accuracy of PM2.5 predictions, and in some cases decreased it slightly. In comparison with other models, our proposed hybrid model showed higher prediction accuracy, R2 is improved by 11.64% on average, and root mean square error, mean absolute error, and mean absolute percentage error is reduced by 26.82%, 27.24%, and 29.88% respectively. This research provides a general overview of the availability of Himawari-8 AOD data and its feasibility in PM2.5 predictions. In addition, it evaluates different machine learning approaches in PM2.5 predictions. Our proposed framework can be used in other regions to predict different air pollutants concentrations and can be used as an aid for air pollution controlling programs.


Assuntos
Poluentes Atmosféricos , Poluição do Ar , Material Particulado/análise , Monitoramento Ambiental/métodos , Aerossóis/análise , Poluentes Atmosféricos/análise , Poluição do Ar/análise , Aprendizado de Máquina
2.
J Asian Nat Prod Res ; 22(5): 474-488, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-30945944

RESUMO

One new indole alkaloid, reflexin A (1), and two known indoles, macusine B (2) and vinorine (3), were isolated from the bark of Rauvolfia reflexa. Their structures were elucidated by 1D and 2D NMR, UV, IR, and MS spectroscopic analyses. Compound 1 displayed anticancer activity against HCT-116 colon cancer cells with an IC50 value of 30.24 ± 0.75 µM. The results implied that the newly isolated 1 induced apoptosis in HCT-116 cells, suggesting its possible role as an anticancer agent. In vivo acute toxicity study was performed on compound 1 to evaluate its safety profile.


Assuntos
Neoplasias do Colo , Rauwolfia , Apoptose , Flavanonas , Humanos , Alcaloides Indólicos , Estrutura Molecular
3.
Int J Hyperthermia ; 36(1): 104-114, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30428737

RESUMO

PURPOSE: Although magnetite nanoparticles (MNPs) are promising agents for hyperthermia therapy, insufficient drug encapsulation efficacies inhibit their application as nanocarriers in the targeted drug delivery systems. In this study, porous magnetite nanoparticles (PMNPs) were synthesized and coated with a thermosensitive polymeric shell to obtain a synergistic effect of hyperthermia and chemotherapy. MATERIALS AND METHODS: PMNPs were produced using cetyltrimethyl ammonium bromide template and then coated by a polyethylene glycol layer with molecular weight of 1500 Da (PEG1500) and phase transition temperature of 48 ± 2 °C to endow a thermosensitive behavior. The profile of drug release from the nanostructure was studied at various hyperthermia conditions generated by waterbath, magnetic resonance-guided focused ultrasound (MRgFUS), and alternating magnetic field (AMF). The in vitro cytotoxicity and hyperthermia efficacy of the doxorubicin-loaded nanoparticles (DOX-PEG1500-PMNPs) were assessed using human lung adenocarcinoma (A549) cells. RESULTS: Heat treatment of DOX-PEG1500-PMNPs containing 235 ± 26 mg·g-1 DOX at 48 °C by waterbath, MRgFUS, and AMF, respectively led to 71 ± 4%, 48 ± 3%, and 74 ± 5% drug release. Hyperthermia treatment of the A549 cells using DOX-PEG1500-PMNPs led to 77% decrease in the cell viability due to the synergistic effects of magnetic hyperthermia and chemotherapy. CONCLUSION: The large pores generated in the PMNPs structure could provide a sufficient space for encapsulation of the chemotherapeutics as well as fast drug encapsulation and release kinetics, which together with thermosensitive characteristics of the PEG1500 shell, make DOX-PEG1500-PMNPs promising adjuvants to the magnetic hyperthermia modality.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Hipertermia Induzida/métodos , Nanopartículas de Magnetita/química , Polietilenoglicóis/química , Humanos , Campos Magnéticos
5.
Molecules ; 23(2)2018 Jan 28.
Artigo em Inglês | MEDLINE | ID: mdl-29382104

RESUMO

Diabetes is associated with obesity, generally accompanied by a chronic state of oxidative stress and redox imbalances which are implicated in the progression of micro- and macro-complications like heart disease, stroke, dementia, cancer, kidney failure and blindness. All these complications rise primarily due to consistent high blood glucose levels. Insulin and glucagon help to maintain the homeostasis of glucose and lipids through signaling cascades. Pancreatic hormones stimulate translocation of the glucose transporter isoform 4 (GLUT4) from an intracellular location to the cell surface and facilitate the rapid insulin-dependent storage of glucose in muscle and fat cells. Malfunction in glucose uptake mechanisms, primarily contribute to insulin resistance in type 2 diabetes. Plant secondary metabolites, commonly known as phytochemicals, are reported to have great benefits in the management of type 2 diabetes. The role of phytochemicals and their action on insulin signaling pathways through stimulation of GLUT4 translocation is crucial to understand the pathogenesis of this disease in the management process. This review will summarize the effects of phytochemicals and their action on insulin signaling pathways accelerating GLUT4 translocation based on the current literature.


Assuntos
Diabetes Mellitus Tipo 2/metabolismo , Transportador de Glucose Tipo 4/metabolismo , Resistência à Insulina , Obesidade/metabolismo , Compostos Fitoquímicos/farmacologia , Transdução de Sinais/efeitos dos fármacos , Animais , Diabetes Mellitus Tipo 2/patologia , Humanos , Insulina , Obesidade/patologia , Transporte Proteico/efeitos dos fármacos
6.
Tumour Biol ; 39(11): 1010428317731451, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29110583

RESUMO

Xanthones are phytochemical compounds found in a number of fruits and vegetables. Characteristically, they are noted to be made of diverse properties based on their biological, biochemical, and pharmacological actions. Accordingly, the apoptosis mechanisms induced by beta-mangostin, a xanthone compound isolated from Cratoxylum arborescens in the human promyelocytic leukemia cell line (HL60) in vitro, were examined in this study. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was done to estimate the cytotoxicity effect of ß-mangostin on the HL60 cell line. Acridine orange/propidium iodide and Hoechst 33342 dyes and Annexin V tests were conducted to detect the apoptosis features. Caspase-3 and caspase-9 activities; reactive oxygen species; real-time polymerase chain reaction for Bcl-2, Bax, caspase-3, and caspase-9 Hsp70 genes; and western blot for p53, cytochrome c, and pro- and cleavage-caspase-3 and caspase-9 were assessed to examine the apoptosis mechanism. Cell-cycle analysis conducted revealed that ß-mangostin inhibited the growth of HL60 at 58 µM in 24 h. The administration of ß-mangostin with HL60 caused cell morphological changes related to apoptosis which increased the number of early and late apoptotic cells. The ß-mangostin-catalyzed apoptosis action through caspase-3, caspase-7, and caspase-9 activation overproduced reactive oxygen species which downregulated the expression of antiapoptotic genes Bcl-2 and HSP70. Conversely, the expression of the apoptotic genes Bax, caspase-3, and caspase-9 were upregulated. Meanwhile, at the protein level, ß-mangostin activated the formation of cleaved caspase-3 and caspase-9 and also upregulated the p53. ß-mangostin arrested the cell cycle at the G0/G1 phase. Overall, the results for ß-mangostin showed an antiproliferative effect in HL60 via stopping the cell cycle at the G0/G1 phase and prompted the intrinsic apoptosis pathway.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Proteínas de Choque Térmico HSP70/efeitos dos fármacos , Leucemia Promielocítica Aguda , Xantonas/farmacologia , Clusiaceae , Regulação para Baixo , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Células HL-60 , Proteínas de Choque Térmico HSP70/biossíntese , Humanos , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio
7.
BMC Vet Res ; 13(1): 27, 2017 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-28103938

RESUMO

BACKGROUND: Cibotium barometz is a medical herb used traditionally in the Malaysian peninsula for several ailments, including gastric ulcer. The aim of this study was assessment the anti-ulcer effects of C. barometz hair on ethanol-induced stomach hemorrhagic abrasions in animals. Seven groups of Sprague Dawley (SD) rats were administered 10% Tween 20 in the normal control and ulcer control groups, and omeprazole 20 mg/kg and 62.5, 125, 250, and 500 mg/kg of C. barometz hair extract in the experimental groups. After 60 min, the normal control group of rats was orally administered 10% Tween 20, while absolute ethanol was orally administered to the groups of ulcer control, omeprazole and experimental groups. Stomachs of the rats were examined macroscopically and histologically. Homogenates of stomachs were used to evaluate endogenous antioxidant enzyme activities. RESULTS: Rats pre-fed with plant extract presented a significant decrease in the sore area, increased pH of gastric contents and preserved stomach wall mucus compared to the ulcer group. Histologically, rats pre-fed with C. barometz hair extract showed mild to moderate disruptions of the surface epithelium while animals pre-fed with absolute ethanol showed severe disruptions of the stomach epithelium with edema and leucocyte penetration of the submucosal layer. A Periodic acid Schiff (PAS) staining revealed that each rat pre-treated with the plant extract displayed an intense uptake of stomach epithelial glycoprotein magenta color compared to the ulcer control group. Immunohistochemical analysis revealed that rats pre-fed with the plant extract showed an up-regulation of the heat shock protein 70 (HSP70) and down-regulation of Bax proteins compared to ulcer control rats. Homogenates of the stomach tissue demonstrated significant increases in the endogenous antioxidant enzymatic activity and decreased lipid peroxidation (MDA) in rats pre-treated with C. barometz hair extract compared with the ulcer control rats. In acute toxicity, the liver and kidney revealed no hepatotoxic or nephrotoxic effects histologically. CONCLUSIONS: The gastric cytoprotective action of C. barometz hair extract might be attributed to antioxidants, an increase in gastric pH, stomach mucus preservation, increased endogenous antioxidant enzymes, decreased lipid peroxidation, up-regulation of HSP70 and down-regulation of Bax proteins.


Assuntos
Etanol/toxicidade , Gleiquênias/química , Extratos Vegetais/farmacologia , Úlcera Gástrica/induzido quimicamente , Animais , Antioxidantes/farmacologia , Compostos de Bifenilo , Relação Dose-Resposta a Droga , Masculino , Medicina Tradicional Chinesa , Fitoterapia , Picratos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley , Estômago/efeitos dos fármacos , Estômago/patologia , Úlcera Gástrica/prevenção & controle , Testes de Toxicidade
8.
BMC Complement Altern Med ; 17(1): 366, 2017 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-28716025

RESUMO

BACKGROUND: Beta-mangostin (BM) is a xanthone-type of natural compound isolated from Cratoxylum arborescens. This study aimed to examine the apoptosis mechanisms induced by BM in a murine monomyelocytic cell line (WEHI-3) in vitro and in vivo. METHODS: A WEHI-3 cell line was used to evaluate the cytotoxicity of BM by MTT. AO/PI and Hoechst 33342 dyes, Annexin V, multiparametric cytotoxicity 3 by high content screening (HCS); cell cycle tests were used to estimate the features of apoptosis and BM effects. Caspase 3 and 9 activities, ROS, western blot for Bcl2, and Bax were detected to study the mechanism of apoptosis. BALB/c mice injected with WEHI-3 cells were used to assess the apoptotic effect of BM in vivo. RESULTS: BM suppressed the growth of WEHI-3 cells at an IC50value of 14 ± 3 µg/mL in 24 h. The ROS production was increased inside the cells in the treated doses. Both caspases (9 and 3) were activated in treating WEHI-3 cells at 24, 48 and 72 h. Different signs of apoptosis were detected, such as cell membrane blebbing, DNA segmentation and changes in the asymmetry of the cell membrane. Another action by which BM could inhibit WEHI-3 cells is to restrain the cell cycle at the G1/G0 phase. In the in vivo study, BM reduced the destructive effects of leukaemia on the spleen and liver by inducing apoptosis in leukaemic cells. CONCLUSION: BM exerts anti-leukaemic properties in vitro and in vivo.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose , Clusiaceae/química , Leucemia/tratamento farmacológico , Fitoterapia , Extratos Vegetais/farmacologia , Xantonas/farmacologia , Animais , Antineoplásicos Fitogênicos/uso terapêutico , Caspase 3/metabolismo , Caspase 9/metabolismo , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células , Fígado/efeitos dos fármacos , Fígado/patologia , Camundongos Endogâmicos BALB C , Extratos Vegetais/uso terapêutico , Espécies Reativas de Oxigênio/metabolismo , Baço/efeitos dos fármacos , Baço/patologia , Xantonas/uso terapêutico
9.
Cell Physiol Biochem ; 37(5): 1997-2011, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26584298

RESUMO

BACKGROUND/AIMS: Rauvolfia reflexa is a member of the Apocynaceae family. Plants from the Apocynaceae family have been traditionally used in the treatment of age-related brain disorders Methods and Results: Two new indole alkaloids, rauvolfine C (1) and 3-methyl-10,11-dimethoxy-6-methoxycarbonyl-ß-carboline (2), along with five known, macusine B (3), vinorine (4), undulifoline (5), isoresrpiline (6) and rescinnamine (7) were isolated from the bark of Rauvolfia reflexa. Cholinesterase inhibitory assay and molecular docking were performed to get insight of the inhibitory activity and molecular interactions of the compounds. The compounds showed good to moderate cholinesterase inhibitory activity with IC50 values in the range of 8.06 to 73.23 µM. Compound 7 was found to be the most potent inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Compounds 1, 2, 5 and 6 were found to be selective towards BChE, while compounds 3, 4 and 7 were dual inhibitors, having almost equal inhibitory activity on both AChE and BChE. Molecular docking revealed that compounds 6 and 7 interacted differently on AChE and BChE, by means of hydrophobic interactions and hydrogen bonding. In AChE, the indole moiety of both compounds interacted with the residues lining the peripheral anionic site, whereas in BChE, their methoxy groups are primarily responsible for the strong inhibitory activity via interactions with residues at the active site of the enzyme. CONCLUSION: Two new and five known indole alkaloids were isolated from R. reflexa. Among the compounds, 7 and 6 showed the most potent and promising cholinesterase inhibitory activity, worthy for further investigations.


Assuntos
Acetilcolinesterase/química , Butirilcolinesterase/química , Alcaloides Indólicos/química , Rauwolfia/química , Acetilcolinesterase/metabolismo , Sítios de Ligação , Butirilcolinesterase/metabolismo , Carbolinas , Alcaloides Indólicos/isolamento & purificação , Alcaloides Indólicos/metabolismo , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Simulação de Acoplamento Molecular , Casca de Planta/química , Casca de Planta/metabolismo , Estrutura Terciária de Proteína , Rauwolfia/metabolismo
10.
Cell Physiol Biochem ; 36(3): 988-1003, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26087920

RESUMO

BACKGROUND: Tanacetum polycephalum L. Schultz-Bip is a member of the Asteraceae family. This study evaluated the chemopreventive effect of a T. polycephalum hexane extract (TPHE) using in in vivo and in vitro models. METHODS AND RESULTS: Five groups of rats: normal control, cancer control, TPHE low dose, TPHE high dose and positive control (tamoxifen) were used for the in vivo study. Histopathological examination showed that TPHE significantly suppressed the carcinogenic effect of LA7 tumour cells. The tumour sections from TPHE-treated rats demonstrated significantly reduced expression of Ki67 and PCNA compared to the cancer control group. Using a bioassay-guided approach, the cytotoxic compound of TPHE was identified as a tricyclic sesquiterpene lactone, namely, 8ß- hydroxyl- 4ß, 15- dihydrozaluzanin C (HDZC). Signs of early and late apoptosis were observed in MCF7 cells treated with HDZC and were attributed to the mitochondrial intrinsic pathway based on the up-regulation of Bax and the down-regulation of Bcl-2. HDZC induced cell cycle arrest in MCF7 cells and increased the expression of p21 and p27 at the mRNA and protein levels. CONCLUSION: This results of this study substantiate the anticancer effect of TPHE and highlight the involvement of HDZC as one of the contributing compounds that act by initiating mitochondrial-mediated apoptosis.


Assuntos
Anticarcinógenos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Regulação Neoplásica da Expressão Gênica , Lactonas/farmacologia , Neoplasias Mamárias Experimentais/tratamento farmacológico , Sesquiterpenos/farmacologia , Tanacetum/química , Animais , Anticarcinógenos/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Inibidor de Quinase Dependente de Ciclina p21/agonistas , Inibidor de Quinase Dependente de Ciclina p21/genética , Inibidor de Quinase Dependente de Ciclina p21/metabolismo , Inibidor de Quinase Dependente de Ciclina p27/agonistas , Inibidor de Quinase Dependente de Ciclina p27/genética , Inibidor de Quinase Dependente de Ciclina p27/metabolismo , Feminino , Humanos , Lactonas/isolamento & purificação , Células MCF-7 , Neoplasias Mamárias Experimentais/genética , Neoplasias Mamárias Experimentais/metabolismo , Neoplasias Mamárias Experimentais/patologia , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Transplante de Neoplasias , Extratos Vegetais/química , Proteínas Proto-Oncogênicas c-bcl-2/antagonistas & inibidores , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Ratos , Ratos Sprague-Dawley , Sesquiterpenos/isolamento & purificação , Transdução de Sinais , Proteína X Associada a bcl-2/agonistas , Proteína X Associada a bcl-2/genética , Proteína X Associada a bcl-2/metabolismo
11.
BMC Complement Altern Med ; 14: 299, 2014 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-25127718

RESUMO

BACKGROUND: Annona muricata leaves have been reported to have antiproliferative effects against various cancer cell lines. However, the detailed mechanism has yet to be defined. The current study was designed to evaluate the molecular mechanisms of A. muricata leaves ethyl acetate extract (AMEAE) against lung cancer A549 cells. METHODS: The effect of AMEAE on cell proliferation of different cell lines was analyzed by MTT assay. High content screening (HCS) was applied to investigate the suppression of NF-κB translocation, cell membrane permeability, mitochondrial membrane potential (MMP) and cytochrome c translocation from mitochondria to cytosol. Reactive oxygen species (ROS) formation, lactate dehydrogenase (LDH) release and activation of caspase-3/7, -8 and -9 were measured while treatment. The western blot analysis also carried out to determine the protein expression of cleaved caspase-3 and -9. Flow cytometry analysis was used to determine the cell cycle distribution and phosphatidylserine externalization. Quantitative PCR analysis was performed to measure the gene expression of Bax and Bcl-2 proteins. RESULTS: Cell viability analysis revealed the selective cytotoxic effect of AMEAE towards lung cancer cells, A549, with an IC50 value of 5.09 ± 0.41 µg/mL after 72 h of treatment. Significant LDH leakage and phosphatidylserine externalization were observed in AMEAE treated cells by fluorescence analysis. Treatment of A549 cells with AMEAE significantly elevated ROS formation, followed by attenuation of MMP via upregulation of Bax and downregulation of Bcl-2, accompanied by cytochrome c release to the cytosol. The incubation of A549 cells with superoxide dismutase and catalase significantly attenuated the cytotoxicity caused by AMEAE, indicating that intracellular ROS plays a pivotal role in cell death. The released cytochrome c triggered the activation of caspase-9 followed by caspase-3. In addition, AMEAE-induced apoptosis was accompanied by cell cycle arrest at G0/G1 phase. Moreover, AMEAE suppressed the induced translocation of NF-κB from cytoplasm to nucleus. CONCLUSIONS: Our data showed for the first time that the ethyl acetate extract of Annona muricata inhibited the proliferation of A549 cells, leading to cell cycle arrest and programmed cell death through activation of the mitochondrial-mediated signaling pathway with the involvement of the NF-kB signalling pathway.


Assuntos
Annona/química , Apoptose/efeitos dos fármacos , Neoplasias Pulmonares/metabolismo , Mitocôndrias/metabolismo , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Caspase 3/metabolismo , Caspase 9/metabolismo , Ciclo Celular/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citocromos c/metabolismo , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/genética , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Folhas de Planta/química , Espécies Reativas de Oxigênio/metabolismo , Proteína X Associada a bcl-2/metabolismo
12.
ScientificWorldJournal ; 2014: 768323, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24526922

RESUMO

Seaweed is one of the largest producers of biomass in marine environment and is a rich arsenal of active metabolites and functional ingredients with valuable beneficial health effects. Being a staple part of Asian cuisine, investigations on the crude extracts of Phaeophyceae or brown algae revealed marked antitumor activity, eliciting a variety of research to determine the active ingredients involved in this potential. The sulfated polysaccharide of fucoidan and carotenoid of fucoxanthin were found to be the most important active metabolites of brown algae as potential chemotherapeutic or chemopreventive agents. This review strives to provide detailed account of all current knowledge on the anticancer and antitumor activity of fucoidan and fucoxanthin as the two major metabolites isolated from brown algae.


Assuntos
Antineoplásicos/metabolismo , Phaeophyceae/metabolismo , Polissacarídeos/metabolismo , Xantofilas/metabolismo , Animais , Antineoplásicos/isolamento & purificação , Antineoplásicos/uso terapêutico , Linfoma de Burkitt/tratamento farmacológico , Linfoma de Burkitt/patologia , Humanos , Células Jurkat , Células K562 , Polissacarídeos/isolamento & purificação , Polissacarídeos/uso terapêutico , Xantofilas/isolamento & purificação , Xantofilas/uso terapêutico
13.
ScientificWorldJournal ; 2014: 540463, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24737979

RESUMO

Metal-based drugs with extensive clinical applications hold great promise for the development of cancer chemotherapeutic agents. In the last few decades, Schiff bases and their complexes have become well known for their extensive biological potential. In the present study, we examined the antiproliferative effect of a copper (II) complex on HT-29 colon cancer cells. The Cu(BrHAP)2 Schiff base compound demonstrated a potent antiproliferative effect in HT-29 cells, with an IC50 value of 2.87 µg/ml after 72 h of treatment. HT-29 cells treated with Cu (II) complexes underwent apoptosis death, as exhibited by a progressive elevation in the proportion of the G1 cell population. At a concentration of 6.25 µg/ml, the Cu(BrHAP)2 compound caused significant elevation in ROS production following perturbation of mitochondrial membrane potential and cytochrome c release, as assessed by the measurement of fluorescence intensity in stained cells. Furthermore, the activation of caspases 3/7 and 9 was part of the Cu (II) complex-induced apoptosis, which confirmed the involvement of mitochondrial-mediated apoptosis. Meanwhile, there was no significant activation of caspase-8. Taken together, these results imply that the Cu(BrHAP)2 compound is a potential candidate for further in vivo and clinical colon cancer studies to develop novel chemotherapeutic agents derived from metal-based agents.


Assuntos
Neoplasias do Colo/metabolismo , Cobre/química , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Caspase 7/metabolismo , Caspase 9/metabolismo , Proliferação de Células/efeitos dos fármacos , Citocromos c/metabolismo , Células HT29 , Humanos , Concentração Inibidora 50 , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Compostos Organometálicos/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos
14.
Molecules ; 19(9): 13909-31, 2014 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-25197930

RESUMO

The gastroretentive dosage form of famotidine was modified using tamarind seed powders to prolong the gastric retention time. Tamarind seeds were used in two different forms having different swelling and gelling properties: with husk (TSP) or without husk (TKP). TKP (TKP1 to TKP 6) and TSP (TSP1 to TSP 6) series were prepared using tamarind powder:xanthan in the ratios of 5:0, 4:1, 3:2, 2:3, 1:4, 0:5, respectively. The matrix tablets were prepared by the wet granulation method and evaluated for pharmacopoeial requirements. TKP2 was the optimum formulation as it had a short floating lag time (FLT<30 s) and more than 98.5% drug release in 12 h. The dissolution data were fitted to popular mathematical models to assess the mechanism of drug release, and the optimum formulation showed a predominant first order release and diffusion mechanism. It was concluded that the TKP2 prepared using tamarind kernel powder:xanthan (4:1) was the optimum formulation with shortest floating lag time and more than 90% release in the determined period of time.


Assuntos
Famotidina/química , Hidrogéis/química , Polissacarídeos Bacterianos/química , Tamarindus/química , Varredura Diferencial de Calorimetria , Preparações de Ação Retardada/química , Concentração de Íons de Hidrogênio , Cinética , Preparações de Plantas/química , Espectroscopia de Infravermelho com Transformada de Fourier , Viscosidade , Difração de Raios X
15.
Molecules ; 19(7): 9478-501, 2014 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-24995928

RESUMO

Tanacetum polycephalum (L.) Schultz-Bip (Mokhaleseh) has been traditionally used in the treatment of headaches, migraines, hyperlipidemia and diabetes. The present study aimed to evaluate its anticancer properties and possible mechanism of action using MCF7 as an in vitro model. T. polycephalum leaves were extracted using hexane, chloroform and methanol solvents and the cytotoxicity was evaluated using the MTT assay. Detection of the early apoptotic cells was investigated using acridine orange/propidium iodide staining. An Annexin-V-FITC assay was carried out to observe the phosphatidylserine externalization as a marker for apoptotic cells. High content screening was applied to analyze the cell membrane permeability, nuclear condensation, mitochondrial membrane potential (MMP) and cytochrome c release. Apoptosis was confirmed by using caspase-8, caspase-9 and DNA laddering assays. In addition, Bax/Bcl-2 expressions and cell cycle arrest also have been investigated. MTT assay revealed significant cytotoxicity of T. Polycephalum hexane extract (TPHE) on MCF7 cells with the IC50 value of 6.42±0.35 µg/mL. Significant increase in chromatin condensation was also observed via fluorescence analysis. Treatment of MCF7 cells with TPHE encouraged apoptosis through reduction of MMP by down-regulation of Bcl-2 and up-regulation of Bax, triggering the cytochrome c leakage from mitochondria to the cytosol. The treated MCF7 cells significantly arrested at G1 phase. The chromatographic analysis elicited that the major active compound in this extract is 8ß-hydroxy-4ß,15-dihydrozaluzanin C. Taken together, the results presented in this study demonstrated that the hexane extract of T. Polycephalum inhibits the proliferation of MCF7 cells, resulting in the cell cycle arrest and apoptosis, which was explained to be through the mitochondrial pathway.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose , Movimento Celular/efeitos dos fármacos , Tanacetum/química , Proteínas Reguladoras de Apoptose/genética , Proteínas Reguladoras de Apoptose/metabolismo , Permeabilidade da Membrana Celular , Proliferação de Células , Sobrevivência Celular , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Células MCF-7 , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Invasividade Neoplásica , Regulação para Cima
16.
Environ Sci Pollut Res Int ; 30(12): 34306-34318, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36509958

RESUMO

In the twenty-first century, mobile phones have become one of the most indispensable electronic products in the international community. The pollution of wasted mobile phones has become an urgent problem worldwide and needs special attention. In this paper, we applied the consumption and usage method to calculate the high-tech mineral elements in China from 2001 to 2019. To analyze the spatial distribution of per capita high-tech minerals in China, we proposed a model (3D GHM) through which a 3D grid of high-tech minerals in wasted mobile phones can be obtained in 1 km resolution. The results showed that the total amount of wasted mobile phones in China from 2001 to 2019 was 8.6 billion, with a growth rate of 1026.7% in 2019 compared with 2001. Moreover, the spatiotemporal distribution of wasted mobile phones is characterized by more in the east and less in the west. The total amount of cobalt, palladium, antimony, beryllium, neodymium, praseodymium, and platinum in wasted mobile phones from 2001 to 2019 reached 42,422.4 tons. Based on our results, we proposed a system for efficient collecting and recycling of wasted mobile phones in China.


Assuntos
Telefone Celular , Resíduo Eletrônico , China , Reciclagem/métodos , Minerais
17.
Chemosphere ; 335: 139065, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37247670

RESUMO

This study explores the dynamic transmission of infectious particles due to COVID-19 in the environment using a spatiotemporal epidemiological approach. We proposed a novel multi-agent model to simulate the spread of COVID-19 by considering several influencing factors. The model divides the population into susceptible and infected and analyzes the impact of different prevention and control measures, such as limiting the number of people and wearing masks on the spread of COVID-19. The findings suggest that reducing population density and wearing masks can significantly reduce the likelihood of virus transmission. Specifically, the research shows that if the population moves within a fixed range, almost everyone will eventually be infected within 1 h. When the population density is 50%, the infection rate is as high as 96%. If everyone does not wear a mask, nearly 72.33% of the people will be infected after 1 h. However, when people wear masks, the infection rate is consistently lower than when they do not wear masks. Even if only 25% of people wear masks, the infection rate with masks is 27.67% lower than without masks, which is strong evidence of the importance of wearing a mask. As people's daily activities are mostly carried out indoors, and many super-spreading events of the new crown epidemic also originated from indoor gatherings, the research on indoor epidemic prevention and control is essential. This study provides decision-making support for epidemic preventions and controls and the proposed methodology can be used in other regions and future epidemics.


Assuntos
COVID-19 , Epidemias , Humanos , COVID-19/epidemiologia , Densidade Demográfica , Probabilidade
18.
Environ Sci Pollut Res Int ; 30(32): 79402-79422, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37286829

RESUMO

Eutrophication happens when water bodies are enriched by minerals and nutrients. Dense blooms of noxious are the most obvious effect of eutrophication that harms water quality, and by increasing toxic substances damage the water ecosystem. Therefore, it is critical to monitor and investigate the development process of eutrophication. The concentration of chlorophyll-a (chl-a) in water bodies is an essential indicator of eutrophication in them. Previous studies in predicting chlorophyll-a concentrations suffered from low spatial resolution and discrepancies between predicted and observed values. In this paper, we used various remote sensing and ground observation data and proposed a novel machine learning-based framework, a random forest inversion model, to provide the spatial distribution of chl-a in 2 m spatial resolution. The results showed our model outperformed other base models, and the goodness of fit improved by over 36.6% while MSE and MAE decreased by over 15.17% and over 21.26% respectively. Moreover, we compared the feasibility of GF-1 and Sentinel-2 remote sensing data in chl-a concentration prediction. We found that better prediction results can be obtained by using GF-1 data, with the goodness of fit reaching 93.1% and MSE only 3.589. The proposed method and findings of this study can be used in future water management studies and as an aid for decision-makers in this field.


Assuntos
Big Data , Ecossistema , Clorofila A , Monitoramento Ambiental/métodos , Clorofila/análise , Algoritmos , Aprendizado de Máquina , Eutrofização , Lagos
19.
Environ Sci Pollut Res Int ; 29(36): 54150-54166, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35294690

RESUMO

Exposure to fine particulate matter can easily lead to health issues. PM2.5 concentrations are associated with various spatiotemporal factors, which makes the prediction of PM2.5 concentrations still a challenging task. One of the reasons that makes the accurate prediction by statistical learning method difficult is severe fluctuations in input data. In addition, the abstraction method of space will also affect the prediction results. To address these important issues, a novel hybrid decomposing-ensemble and spatiotemporal attention (DESA) model is proposed to improve the prediction accuracy by decomposing the mode-mixed time series into single-mode series and automatically assign weights to the spatiotemporal factors. In our proposed framework, raw PM2.5 series are firstly decomposed into simple sub-series via the complete ensemble empirical mode decomposition (CEEMD) method. Then, to keep the results independent of the spatial abstraction method, a data-driven approach called multiscale spatiotemporal attention network is employed to extract spatiotemporal features from the sub-series. Finally, the predictions of each sub-series are processed separately and combined to obtain the final prediction results. The experimental results indicate that the proposed model achieved the better performance with RMSE of 11.15, 17.49, 24.84, and 26.93 for 6-, 12-, 24-, and 36-h forecasting, respectively. The proposed method is expected to be applied in fine prediction of air pollution and controlling programs and therefore provide decision support or useful guidance.


Assuntos
Poluentes Atmosféricos , Poluição do Ar , Poluentes Atmosféricos/análise , Poluição do Ar/análise , Monitoramento Ambiental/métodos , Previsões , Material Particulado/análise , Fatores de Tempo
20.
Chemosphere ; 308(Pt 2): 136301, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36064028

RESUMO

The AOD derived from the MODIS deep blue(DB) algorithm and AQI were used to investigate the correlation between AOD and AQI in seven major cities of Yangtze River Delta (YRD) from January to December 2019. The accuracy of MODIS AOD was validated by AERONET. Moreover, the AOD and AQI were studied to explore the annual and seasonal distribution characteristics, and the correlation analysis was carried out using five regression models. It was found: Ⅰ) There was a significant correlation between AOD and AERONET data (R2 ˃ 0.80, RMSE = 0.106, and MAE = 0.089). Ⅱ) The highest AQI was observed in winter (83), followed by spring (76), autumn (74), and summer (72). Ⅲ) The monthly average AOD showed noticeable seasonal variations, which reached the highest in summer (0.91) and the lowest in winter (0.69), followed by spring and autumn. Ⅳ) Among the five models, the cubic model obtained the best results with R2 ˃ 0.55. In the sub-seasonal regression model, the cubic model outperformed other models in spring (R2 ˃ 0.57), summer (R2 ˃ 0.76) and autumn (R2 ˃ 0.38). However, in winter the composite model outperformed others (R2 ˃ 0.68). Ⅴ) Considering annual data, the AOD can predict over 70% of the variations in AQI (0.41<R2 <0.81). These results demonstrate the feasibility of AOD derived from the MODIS DB algorithm in AQI prediction. The method used in this study can be applied as an aid for air pollution control programs in different regions.


Assuntos
Poluentes Atmosféricos , Poluição do Ar , Aerossóis/análise , Poluentes Atmosféricos/análise , Poluição do Ar/análise , Cidades , Monitoramento Ambiental/métodos , Material Particulado/análise , Rios
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