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1.
Angew Chem Int Ed Engl ; 59(9): 3491-3494, 2020 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-31901005

RESUMO

We have developed a highly efficient and practical approach for palladium-catalyzed trifluoroacetate-promoted N-quinolylcarboxamide-directed glycosylation of inert ß-C(sp3 )-H bonds of N-phthaloyl α-amino acids with glycals under mild conditions. For the first time, C(sp3 )-H activation for glycosylation was achieved to build C-alkyl glycosides. This method facilitates the synthesis of various ß-substituted C-alkyl glycoamino acids and offers a tool for glycopeptide synthesis.

3.
Endocrine ; 2019 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-31845180

RESUMO

PURPOSE: Fatty acid binding protein 4 (FABP4) has been demonstrated to be secreted from adipocytes in an unconventional pathway associated with lipolysis. Circulating FABP4 is elevated in metabolic disorders and has been shown to affect various peripheral cells such as pancreatic ß-cells, hepatocytes and macrophages, but its effects on adipocytes remains unclear. The aim of this study was to investigate the effects of exogenous FABP4 (eFABP4) on adipocyte differentiation and function. METHODS: 3T3-L1 pre-adipocytes or mature adipocytes were treated with recombinant FABP4 in the absence or presence of FABP4 inhibitor I-9/p38 MAPK inhibitor SB203580; Meanwhile male C57BL/6J mice were subcutaneously injected twice a day with recombinant FABP4 (0.35 mg/kg) with or without I-9 (50 mg/kg) for 2 weeks. The effects of eFABP4 on differentiation, lipolysis and inflammation were determined by triglyceride measurement or lipolysis assay, western blotting, or RT-qPCR analysis. RESULTS: eFABP4 treatment significantly reduced intracellular triglyceride content and decreased expression of adipogenic markers peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT/enhancer binding protein alpha (C/EBPα), intracellular FABP4, and adiponectin in 3T3-L1 cells. Besides, eFABP4 promoted lipolysis and inflammation in differentiated 3T3-L1 adipocytes as well as in adipose tissue of eFABP4-treated C57BL/6J mice, with elevated gene expression of monocyte chemoattractant protein (MCP)-1, tumor necrosis factor (TNF)-α, and elevated protein expression of adipose triglyceride lipase (ATGL), phosphorylation of hormone-sensitive lipase (HSL) (Ser-660), p38, and nuclear factor-kappa B (NF-κB). The pro-inflammatory and pro-lipolytic effects of eFABP4 could be reversed by SB203580/I-9. CONCLUSIONS: These findings indicate that eFABP4 interferes with adipocyte differentiation, induces p38/HSL mediated lipolysis and p38/NF-κB mediated inflammation in adipocytes in vitro and in vivo.

4.
Int J Biol Macromol ; 2019 Nov 19.
Artigo em Inglês | MEDLINE | ID: mdl-31756487

RESUMO

OBJECTIVE: Fas is a positive regulator of Th17 cells differentiation in experimental autoimmune encephalomyelitis (EAE). However, its upstream regulators are still not fully determined. This study was designed to explore the upstream regulators of Fas in regulating Th17 cells differentiation in EAE. METHODS: The mouse model of EAE was established by myelin oligodendrocyte glycoprotein injection. Th17 cells differentiation was induced by IL-23, IL-6 and TGF-ß. RESULTS: Down-regulated Hsp70 and miR-374c and up-regulated Fas were observed in the spleen and brain of EAE mice. Hsp70 overexpression evidently reduced Fas protein level, but not mRNA level. The luciferase reporter assay indicated that miR-374c targets Fas. Overexpression of miR-374c down-regulated the mRNA and protein level of Fas. The concentration of IL-17A in CD4+ T-cells was reduced by miR-374c or Hsp70 overexpression, and Fas overexpression altered this trend. Hsp70 did not regulate the expression of miR-374c, and likewise, miR-374c did not regulate the expression of Hsp70. Further results suggested that Hsp70 and miR-374c regulated Fas expression through different ways to affect Th17 cells differentiation in EAE. CONCLUSIONS: This study suggested that down-regulated miR-374c and Hsp70 promote Th17 cell differentiation by inducing Fas expression in EAE.

5.
Medicine (Baltimore) ; 98(44): e17381, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31689744

RESUMO

BACKGROUND: This study will assess the effectiveness of electroacupuncture (EA) for pain in patients with osteosarcoma post surgery (OSPS). METHODS: In this study, we will comprehensively search the following electronic databases from inception to the present without language restrictions: Cochrane Library, EMBASE, MEDLINE, the Cumulative Index to Nursing and Allied Health Literature, the Allied and Complementary Medicine Database, and Chinese Biomedical Literature Database. Two authors will independently carry out study selection, data extraction, and methodological assessments. RevMan 5.3 software will be used for statistical analysis. RESULTS: The primary outcome is pain intensity. The secondary outcomes consist of event-free survival, overall survival, quality of life, and adverse events. CONCLUSION: The findings of this study will provide helpful evidence of EA treatment for patients with OSPS. PROSPERO REGISTRATION NUMBER: PROSPERO CRD42019146696.


Assuntos
Dor do Câncer/terapia , Eletroacupuntura/métodos , Osteossarcoma/terapia , Intervalo Livre de Doença , Eletroacupuntura/efeitos adversos , Humanos , Osteossarcoma/cirurgia , Qualidade de Vida , Ensaios Clínicos Controlados Aleatórios como Assunto , Projetos de Pesquisa
6.
Cancer Nurs ; 2019 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-31714266

RESUMO

BACKGROUND: Non-small cell lung cancer is the most common type of lung cancer. Lung resection is proven to be the most effective curative treatment for early-stage non-small cell lung cancer (stages I-IIIA). Studies show evidence-based pulmonary rehabilitation is critical for improving exercise capacity and pulmonary function, reducing burden of cancer-related symptoms, and facilitating quality of life following a lung resection. OBJECTIVE: To explore the effectiveness of an animation education program to promote respiratory rehabilitation outcomes for postsurgical lung cancer patients. INTERVENTIONS/METHODS: Eighty lung cancer patients who had undergone lung resection were equally randomized to 2 groups with 40 participants in each group. The intervention group received animation education. The control group received traditional face-to-face education. The training-related knowledge and exercise compliance were evaluated at baseline, 3 days after education, and the day of discharge, along with related pulmonary functional indicators. RESULTS: Eighty of 99 eligible participants were enrolled (80.8%). Mean scores of training-related knowledge and exercise compliance in the intervention group were higher than those of the control group. Occurrences of postoperative pulmonary complications and the indwelling time of thoracic drainage tube were lower, and 6-minute walk distance was longer compared with the control group. No statistical differences in other pulmonary functional indicators were found. CONCLUSIONS: Educational animation is effective for promoting training-related knowledge and exercise compliance with active respiratory rehabilitation in postsurgical lung cancer patients. IMPLICATIONS FOR PRACTICE: Oncology nurses can implement animation as an innovative educational method for improving cancer patients' uptake and compliance on health education.

7.
Bioorg Med Chem Lett ; 29(22): 126685, 2019 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-31607606

RESUMO

C14 alkyl benzoate ABG001, derived from naturally occurring gentisides, was reported to exhibit neurotrophic activity which is similar to NGF (Nerve Growth Factor). In this research, ABG001 was modified by the strategy of isosteric replacement and conformational restriction with the purpose of improving the bioactivity. The cellular neurotrophic activity of those ABG001 derivatives were evaluated, among which 3-hydroxyquinolin-2-(1H)-one A3 and 4-decylphenol ester B7 displayed much better neurotrophic activity compared with ABG001, which highlights the potential of those novel scaffolds for future neurotrophic agent development.

8.
Bioorg Med Chem ; 27(19): 115015, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31420256

RESUMO

Fatty acid binding protein 4 (FABP4) and fatty acid binding protein 5 (FABP5) are mainly expressed in adipocytes and/or macrophages and play essential roles in energy metabolism and inflammation. When FABP4 function is diminished, FABP5 expression is highly increased possibly as a functional compensation. Dual FABP4/5 inhibitors are expected to provide beneficial synergistic effect on treating diabetes, atherosclerosis, and inflammation-related diseases. Starting from our previously reported selective FABP4 inhibitor 8, structural biology information was used to modulate the selectivity profile and to design potent dual FABP4/5 inhibitors with good selectivity against FABP3. Two compounds A16 and B8 were identified to show inhibitory activities against both FABP4/5 and good selectivity over FABP3, which could also reduce the level of forskolin-stimulated lipolysis in mature 3T3-L1 adipocytes. Compared with compound 8, these two compounds exhibited better anti-inflammatory effects in lipopolysaccharide-stimulated RAW264.7 murine macrophages, with decreased levels of pro-inflammatory cytokines TNFα and MCP-1 and apparently inhibited IKK/NF-κB pathway.

9.
FEBS Open Bio ; 9(10): 1734-1743, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31376210

RESUMO

Lysophosphatidylcholine acyltransferase 3 (LPCAT3) is an important enzyme in phospholipid remodeling, a process that influences the biophysical properties of cell membranes and thus cell function. Multiple lines of evidence suggest that LPCAT3 is involved in several diseases, including atherosclerosis, non-alcoholic steatohepatitis, and carcinoma. Thus, LPCAT3 may have potential as a therapeutic target for these diseases. In the present study, we devised an assay based on reversed-phase HPLC to measure LPCAT3 activity, which may facilitate the identification of LPCAT3 inhibitors and activators. We found that optimal pH and temperature of recombinant human LPCAT3 are 6.0 and 30 °C, respectively. The enzyme Km values for substrates NBD-labelled lysophosphatidylcholine and arachidonoyl CoA were 266.84 ± 3.65 and 11.03 ± 0.51 µmol·L-1 , respectively, and the Vmax was 39.76 ± 1.86 pmol·min-1 ·U-1 . Moreover, we used our new method to determine the IC50 of a known LPCAT inhibitor, TSI-10. In conclusion, this novel assay can be used to measure the effects of compounds on LPCAT3 activity.

10.
Curr Med Chem ; 2019 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-31364510

RESUMO

CBP and p300 are two closely related histone acetyltransferases (HATs) that interact with numerous transcription factors and act to increase the expression of their target genes. Both proteins contain a bromodomain flanking the HAT catalytic domain that is important in binding of CBP/p300 to chromatin and which offers an opportunity to develop protein-protein interaction inhibitors. Since their discovery in 2006, CBP/p300 bromodomains have attracted much interest as promising new epigenetic targets for diverse human diseases, including inflammation, cancer, autoimmune disorders, and cardiovascular disease. Herein, we present a comprehensive review of the structure, function, and inhibitors of CBP/p300 bromodomains developed in the last several years, which is expected to be beneficial to relevant studies.

11.
Life Sci ; 232: 116649, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31301415

RESUMO

AIMS: To investigate the potential biological role of E2F6 and its underlying molecular mechanism in gastric carcinoma (GC) progression. MAIN METHODS: The expressions of cancer susceptibility candidate 2 (CASC2), E2F6 and matrix metalloprotein-2 (MMP-2) were measured by quantitative real-time polymerase chain reaction and western blotting. The inhibitory effect of E2F6 on CASC2 was evaluated using luciferase reporter assay. Cell growth was assessed by colony formation assay and cell counting kit-8. Cell invasion and apoptosis were measured by transwell assay and flow cytometry assay, respectively. In vivo tumorigenicity was assessed by tumor xenografts in nude mice. KEY FINDINGS: Our data revealed that CASC2 was downregulated while E2F6 was upregulated in GC tissues and cell lines. Remarkably, lower expression of CASC2 was associated with poor survival in GC patients. E2F6 inhibited the expression of CASC2. Subsequently, reliable data showed that downregulation of E2F6 suppressed the proliferation and invasion, and promoted the apoptosis of GC cells. Furthermore, downregulation of E2F6 decreased the expression of MMP-2 and increased the activity of caspase-3. However, these changes triggered by E2F6 knockdown could be reversed by inhibition of CASC2. Moreover, we also proved that downregulation of CASC2 reverses the effect of E2F6 knockdown on tumor growth in vivo. SIGNIFICANCE: Our data demonstrated that E2F6 could regulate the proliferation, invasion and apoptosis of GC cells via inhibiting the expression of CASC2, suggesting that E2F6/CASC2 axis is another regulator of GC progression.


Assuntos
Regulação para Baixo/fisiologia , Fator de Transcrição E2F6/fisiologia , RNA Longo não Codificante/genética , Neoplasias Gástricas/genética , Neoplasias Gástricas/patologia , Proteínas Supressoras de Tumor/genética , Animais , Western Blotting , Linhagem Celular Tumoral , Progressão da Doença , Xenoenxertos , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Prognóstico , Reação em Cadeia da Polimerase em Tempo Real , Regulação para Cima
12.
Eur J Med Chem ; 180: 171-190, 2019 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-31306905

RESUMO

p300 is an important histone acetyltransferase in epigenetics, and its overexpression is closely related to various diseases such as cancers. C646 is one of the most representative p300 inhibitors and used in various studies of p300. However, its intrinsic drawbacks such as containing potentially toxic groups prevent it from further development. In order to find potent p300 inhibitors with good drug-like properties, C646 was chosen as the lead compound and a series of new p300 inhibitors were designed based on the principle of bioisosterism and reasonable scaffold hopping, and the structure-activity relationship was systematically explored. Ten of them were found to show comparable inhibitory activity as C646. The most potent compound, 1r (IC50 = 0.16 µM), showed better p300 inhibitory activity than C646 with improved drug-like properties. Western blotting experiment confirmed that 1r could reduce the level of H3K27 acetylation more significantly than C646. Further cellular assay indicated that it could inhibit the proliferation of human breast ductal carcinoma cell T47D and human breast cancer cell MCF7 with the IC50 values of 5.08 µM and 22.54 µM, respectively. Docking study of 1r with p300 protein showed the possible reasons for its higher inhibition activity. Thus, compound 1r might be with potential for development as a novel epigenetic agent targeting p300.


Assuntos
Antineoplásicos/farmacologia , Inibidores Enzimáticos/farmacologia , Pirazolonas/farmacologia , Fatores de Transcrição de p300-CBP/antagonistas & inibidores , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Células MCF-7 , Simulação de Acoplamento Molecular , Estrutura Molecular , Pirazolonas/síntese química , Pirazolonas/química , Relação Estrutura-Atividade , Fatores de Transcrição de p300-CBP/metabolismo
13.
Mar Drugs ; 17(7)2019 Jun 26.
Artigo em Inglês | MEDLINE | ID: mdl-31248044

RESUMO

Two new dimeric 1,4-benzoquinone derivatives, peniquinone A (1) and peniquinone B (2), a new dibenzofuran penizofuran A (3), and a new pyrazinoquinazoline derivative quinadoline D (4), together with 13 known compounds (5-17), were isolated from a marine-derived fungus Penicillium sp. L129. Their structures, including absolute configurations, were elucidated by extensive spectroscopic data and electronic circular dichroism calculations. Compound 1 exhibited cytotoxicity against the MCF-7, U87 and PC3 cell lines with IC50 values of 12.39 µM, 9.01 µM and 14.59 µM, respectively, while compound 2 displayed relatively weak cytotoxicity activities against MCF-7, U87 and PC3 cell lines with IC50 values of 25.32 µM, 13.45 µM and 19.93 µM, respectively. Furthermore, compound 2 showed weak quorum sensing inhibitory activity against Chromobacterium violaceum CV026 with an MIC value of 20 µg/well.


Assuntos
Antineoplásicos/farmacologia , Organismos Aquáticos/química , Benzoquinonas/farmacologia , Penicillium/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Benzoquinonas/química , Benzoquinonas/isolamento & purificação , Linhagem Celular Tumoral , Chromobacterium/efeitos dos fármacos , Chromobacterium/fisiologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Percepção de Quorum/efeitos dos fármacos
14.
Bioorg Med Chem ; 27(13): 2784-2800, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31101493

RESUMO

Toll-like receptor 2 (TLR2) is a bridge between innate immunity and adaptive immunity. TLR2 agonists have been exploited as potential vaccine adjuvants and antitumor agents. However, no TLR2 agonists have been approved by FDA up to now. To discover drug-like TLR2 selective agonists, a novel series of Pam3CSK4 derivatives were designed based on the crystal structure of hTLR2-hTLR1-Pam3CSK4 complex, synthesized and evaluated for their immune-stimulatory activities. Among them, 35c was identified as a murine-specific TLR2 agonist, while 35f was a human-specific TLR2 agonist. Besides, 35d (human and murine TLR2 agonist) showed TLR2 agonistic activity comparable to Pam3CSK4, which included: elevated IL-6 expression level (EC50 = 83.08 ±â€¯5.94 nM), up-regulated TNF-α and IL-6 mRNA expression and promoted maturation of DCs through activating the NF-κB signaling pathway. TLRs antibodies test showed that 35a and 35d were TLR2/1 agonists, while 35f was a TLR2/6 agonist.

16.
Nat Prod Res ; : 1-6, 2019 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-30663360

RESUMO

A new γ-pyrone derivative, acrepyrone A (1), and three known sorbicillinoids, trichodimerol (2), dihydrotrichodimerol (3) and tetrahydrotrichodimerol (4) were isolated from an endophytic fungus, Acremonium citrinum SS-g13, harboured in the roots of the Chinese medicinal plant Fructus mori. Their structures were determined by analysing MS, NMR, and ECD data. Compound 1 was evaluated for its cytotoxic effect, antibacterial activity and quorum sensing inhibitory potential.

17.
J Phycol ; 55(2): 343-351, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-30516826

RESUMO

Saccharina japonica undergoes an alternating life cycle during which the diploid sporophyte generation alternates with the happloid gametophyte generation. Saccharina japonica uses the UV sex determination system to determine the sex of its haploid gametophytes. However, the sex-determining genes and the sex-determining mechanisms of kelp gametophytes have not been thoroughly elucidated to date. In this study, a kelp HMG-box-containing gene (SjHMG), which is located within the sex determination region of S. japonica, was isolated and characterized. SjHMG contained an open reading frame of 1,266 bp in length and encoded a deduced protein of 421 amino acid residues with two HMG-box domains. Phylogenetic analysis showed the strongest relationship between SjHMG and its orthologs in brown algae. An alternatively spliced transcript (SjHMG isoform-2) encoding a protein of 256 amino acid residues was also identified. The two isoforms were specific for male gametophytes. A real-time quantitative PCR analysis showed significantly higher abundances of two isoforms in immature male gametophytes than in mature ones. These findings suggested that the SjHMG gene is a candidate male gametophyte determination gene of kelp. In addition, the abundance of SjHMG isoform-2 transcripts was significantly lower than that of SjHMG isoform-1 transcripts, and only an HMG-box domain was conserved among species in the order Laminariales, which indicated that the gene is specifically involved in sex regulation in some species of the order Laminariales by alternative splicing.

18.
Hepatology ; 70(2): 496-510, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30516845

RESUMO

In nonalcoholic fatty liver disease (NAFLD), triglycerides accumulate within the liver because the rates of fatty acid accrual by uptake from plasma and de novo synthesis exceed elimination by mitochondrial oxidation and secretion as very low-density lipoprotein (VLDL) triglycerides. Thioesterase superfamily member 2 (Them2) is an acyl-coenzyme A (CoA) thioesterase that catalyzes the hydrolysis of fatty acyl-CoAs into free fatty acids plus CoASH. Them2 is highly expressed in the liver, as well as other oxidative tissues. Mice globally lacking Them2 are resistant to diet-induced obesity and hepatic steatosis, and exhibit improved glucose homeostasis. These phenotypes are attributable, at least in part, to roles of Them2 in the suppression of thermogenesis in brown adipose tissue and insulin signaling in skeletal muscle. To elucidate the hepatic function of Them2, we created mice with liver-specific deletion of Them2 (L-Them2-/- ). Although L-Them2-/- mice were not protected against excess weight gain, hepatic steatosis or glucose intolerance, they exhibited marked decreases in plasma triglyceride and apolipoprotein B100 concentrations. These were attributable to reduced rates of VLDL secretion owing to decreased incorporation of plasma-derived fatty acids into triglycerides. The absence of hepatic steatosis in L-Them2-/- mice fed chow was explained by compensatory increases in rates of fatty acid oxidation and by decreased de novo lipogenesis in high fat-fed mice. Consistent with a role for Them2 in hepatic VLDL secretion, THEM2 levels were increased in livers of obese patients with NAFLD characterized by simple steatosis. Conclusion: Them2 functions in the liver to direct fatty acids toward triglyceride synthesis for incorporation into VLDL particles. When taken together with its functions in brown adipose and muscle, these findings suggest that Them2 is a target for the management of NAFLD and dyslipidemia.

19.
Bioorg Med Chem Lett ; 29(2): 225-229, 2019 01 15.
Artigo em Inglês | MEDLINE | ID: mdl-30522954

RESUMO

A new series of 1-substituted pyrazolopyrimidine derivatives were synthesized as potent BTK inhibitors and they were evaluated by enzyme-based assay and anti-proliferation against multiple B-cell lymphoma cell lines in vitro. Among these compounds, 9h exhibited the highest potency against BTK enzyme, with IC50 value of 4.2 nM. In particular, 8 and 9f performed better inhibition against the proliferation of B lymphoma cell lines DOHH2 and WSU-DLCL2 than the clinical drug ibrutinb. In addition, the test toward the normal PBMC cells showed that 8 possessed low cell cytotoxicity. All these explorations indicated that 8 could serve as a valuable anti-tumor agent for B-cell lymphoblastic leukemia treatment.


Assuntos
Tirosina Quinase da Agamaglobulinemia/antagonistas & inibidores , Antineoplásicos/farmacologia , Leucemia de Células B/tratamento farmacológico , Pirimidinas/farmacologia , Tirosina Quinase da Agamaglobulinemia/metabolismo , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Leucemia de Células B/metabolismo , Leucemia de Células B/patologia , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/metabolismo , Estrutura Molecular , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/farmacologia , Pirimidinas/síntese química , Pirimidinas/química , Relação Estrutura-Atividade
20.
Sci Total Environ ; 651(Pt 1): 114-121, 2019 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-30227281

RESUMO

Accurate modelling of particulates build-up process is essential for designing effective stormwater management strategies. However, current modelling practice relies on the classical 'power model' which has limitations in accounting for the variability in the build-up process. This research study investigated the relationships between influential factors of the build-up process and coefficients in the power model. The outcomes showed that the coefficient, which determines the build-up rate, is predominantly influenced by land use factors (pervious area, road area, commercial area and residential area), such that land use factors exerted 23 times more influence than the site characteristics (distance to pervious area and road surface texture depth). The coefficient, which determines how quickly build-up reaches equilibrium, was found to be equally influenced by anthropogenic activities (sweeping frequency and traffic volume) and site characteristics. Further, site characteristics were found to play a major role in generating build-up process variability with three times more influence than that of anthropogenic activities. It was found that the power model satisfactorily replicates the build-up of particles <74 µm. For the build-up of particles >74 µm, a new coefficient, namely, 'coefficient of variability' was introduced in order to improve the prediction performance (up to 17% compared to original power model). The study outcomes provide a deeper understanding into particulates build-up modelling, and can contribute to the formulation of effective stormwater treatment strategies.

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