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1.
Enferm Clin ; 32: S30-S34, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35935729

RESUMO

COVID-19 pandemic is a threat to public health caused by Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). Significant increases in cases occurred worldwide, including in Indonesia and Aceh Province. Pregnant women as a vulnerable group need to equip themselves with knowledge, attitudes, and practices to prevent themselves from being infected with the virus. This study aimed to determine the knowledge, attitude, and practice factors among pregnant women undergoing pregnancy in the COVID-19 pandemic. A cross-sectional online survey in Aceh was carried out among 148 pregnant women between May 3rd and May 14th, 2020. This study was conducted using a knowledge, attitude, and practice questionnaire adapted to pregnancy conditions during the COVID-19 pandemic. Responses were analyzed and categorized by using univariate analysis. The study identified that most pregnant women aged 31-35 years old (41.2%) and had higher education as their latest education (59.5%). This study found 94.6% of participants were knowledgeable on pregnancies carried out during the COVID-19 pandemic. Furthermore, 60.1% had a positive attitude, and 60.8% of pregnant women had good practice in carrying pregnancy during the COVID-19 pandemic. In conclusion, the knowledge, attitude, and practice factors of pregnant women were quite adequate. However, antenatal education is still needed to reduce anxiety in pregnant women and their family.


Assuntos
COVID-19 , Adulto , Feminino , Humanos , Gravidez , Acetona/análogos & derivados , Estudos Transversais , Conhecimentos, Atitudes e Prática em Saúde , Pandemias/prevenção & controle , Gestantes , SARS-CoV-2 , Inquéritos e Questionários
2.
Molecules ; 27(16)2022 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-36014547

RESUMO

Herein, we report our success synthesizing silver nanoparticles (AgNPs) using aqueous extracts from the leaves and flowers of Calotropis gigantea growing in the geothermal manifestation Ie Seu-Um, Aceh Besar, Indonesia. C. gigantea aqueous extract can be used as a bio-reductant for Ag+→Ag0 conversion, obtained by 48h incubation of Ag+, and the extract mixture in a dark condition. UV-Vis characterization showed that the surface plasmon resonance (SPR) peaks of AgNPs-leaf C. gigantea (AgNPs-LCg) and AgNPs-flower C. gigantea (AgNPs-FCg) appeared in the wavelength range of 410-460 nm. Scanning electron microscopy energy-dispersive X-ray spectrometry (SEM-EDS) revealed the agglomeration and spherical shapes of AgNPs-LCg and AgNPs-FCg with diameters ranging from 87.85 to 256.7 nm. Zeta potentials were observed in the range of -41.8 to -25.1 mV. The Kirby-Bauer disc diffusion assay revealed AgNPs-FCg as the most potent antimicrobial agent with inhibition zones of 12.05 ± 0.58, 11.29 ± 0.45, and 9.02 ± 0.10 mm for Escherichia coli, Staphylococcus aureus, and Candida albicans, respectively. In conclusion, aqueous extract from the leaves or flowers of Calotropis gigantea may be used in the green synthesis of AgNPs with broad-spectrum antimicrobial activities.


Assuntos
Anti-Infecciosos , Calotropis , Nanopartículas Metálicas , Acetona/análogos & derivados , Antibacterianos/química , Anti-Infecciosos/química , Escherichia coli , Química Verde , Indonésia , Nanopartículas Metálicas/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Prata/química
3.
Psychopharmacology (Berl) ; 239(9): 2875-2884, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35716192

RESUMO

RATIONALE: Following the emergence of methylone as one of the most popular synthetic cathinones, this group of novel psychoactive substance with names ending in "-lone," such as dibutylone, ethylone, and N-ethylpentylone, appeared on the recreational drug market. The pharmacological mechanisms of dibutylone, ethylone, and N-ethylpentylone are well understood; however, to date, the reinforcing effects of dibutylone, ethylone, and N-ethylpentylone are still unclear. OBJECTIVES: This study aimed to examine the self-administration of dibutylone, ethylone, and N-ethylpentylone relative to methamphetamine (METH) and to quantify their relative reinforcing effectiveness using behavioral economic analysis. METHODS: Male Sprague-Dawley rats were trained to self-administer METH (0.05 mg/kg) under a fixed-ratio 1 (FR1) schedule. Following the training, dose substitution was used to generate full dose-response curves for METH and the three synthetic cathinones. According to the first doses on the descending limb of the dose-response curves, rats were trained to self-administer METH (0.05 mg/kg), dibutylone (0.1 mg·kg-1·infusion-1), ethylone (0.4 mg·kg-1·infusion-1), or N-ethylpentylone (0.1 mg·kg-1·infusion-1) under an FR1 schedule, and a behavioral economic evaluation of their reinforcing effectiveness was then performed. RESULTS: Dibutylone, ethylone, and N-ethylpentylone functioned as reinforcers, and the inverted U-shaped dose-response curves were obtained. The rank order of reinforcing potency in this procedure was METH > N-ethylpentylone ≈ dibutylone > ethylone. In the economic analysis, the comparisons of the essential value (EV) transformed from demand elasticity (α) indicated that the rank order of efficacy as reinforcers was METH (EV = 7.93) ≈ dibutylone (EV = 7.81) > N-ethylpentylone (EV = 5.21) ≈ ethylone (EV = 4.19). CONCLUSIONS: These findings demonstrated that dibutylone, ethylone, and N-ethylpentylone function as reinforcers and have addictive potential, suggesting that the modification of α-alkyl and N-alkyl side chains may affect their reinforcing efficacy.


Assuntos
Estimulantes do Sistema Nervoso Central , Metanfetamina , Acetona/análogos & derivados , Animais , Benzodioxóis , Butilaminas , Relação Dose-Resposta a Droga , Economia Comportamental , Etilaminas , Masculino , Metanfetamina/farmacologia , N-Metil-3,4-Metilenodioxianfetamina/análogos & derivados , Ratos , Ratos Sprague-Dawley , Autoadministração
4.
Bioorg Chem ; 125: 105867, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35576739

RESUMO

Baeyer-Villiger monooxygenase (BVMO) mediated sulfoxidation is a sustainable approach for the synthesis of esomeprazole. In this work, a novel phenylacetone monooxygenase from Limnobacter sp. (LnPAMO) was found to have trace activity for synthesis of enantiopure esomeprazole. Through engineering in the substrate tunnel using a mutagenesis strategy called "nonpolarity paving" and some modifications in cofactor binding domains, a mutant harboring 15 mutations (LnPAMO Mu15) was obtained with 6.6 × 103-fold higher activity to convert omeprazole sulfide into esomeprazole. The activities of the mutant for synthesis of (S)-methyl phenyl sulfoxide and (S)-pantoprazole also increased much, indicating the versatility of the mutant for sulfoxide synthesis. Importantly, no over-oxidation byproduct omeprazole sulfone was detected in the sulfoxidation products by both mass spectrometry and HPLC analysis. Then NADP-dependent Burkholderia stabili formate dehydrogenase was ligated behind Mu15 along with a ribosome binding site sequence in pET-28a for co-expression. By single whole-cell of recombinant Escherichia coli BL21 coexpressing Mu15 and formate dehydrogenase, omeprazole sulfide was efficiently converted into esomeprazole without production of sulfone (16 g/L substrate, enantiomeric excess > 99.9% (S) and > 99% conversion) and the space-time-yield reached 1.67 g product/L/h.


Assuntos
Esomeprazol , Oxigenases de Função Mista , Acetona/análogos & derivados , Acetona/metabolismo , Escherichia coli/genética , Esomeprazol/metabolismo , Formiato Desidrogenases/metabolismo , Oxigenases de Função Mista/genética , Oxigenases de Função Mista/metabolismo , Oxirredução , Especificidade por Substrato
5.
Sci Total Environ ; 833: 155044, 2022 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-35413341

RESUMO

Acetol as one of the major constituent derived from biomass pyrolysis has shown high potential as feedstock to produce chemicals but remains challenging due to the unsatisfied productivity. We here developed a novel technology (Sn(IV)-Cu(II) system), achieving acetol transformation towards lactic acid (LaA) production with an unprecedented yield (91.8 C-mol%), the highest value among the state-of-the-art strategies. The results of experiment and DFT study revealed that [Cu(H2O)4]2+ and [Sn(OH)3(H2O)3]+ were the possible active species, which showed an outstanding synergetic effect. [Cu(H2O)4]2+ exhibited better ability for acetol activation, and gave more contribution to promote the dehydrogenation oxidation in the terminal carbon and hydroxyl of acetol yielding pyruvaldehyde (PRA). Subsequently, the combination of [Sn(OH)3(H2O)3]+ with PRA raised the electrophilicity capacity of terminal C in PRA, thereby facilitating the hydration reaction of PRA so that CH bond energy in the terminal carbon was sharply reduced. This greatly favored the next H-shift from the terminal carbon of hydrated-PRA to adjacent one, allowing LaA synthesis in high productivity. This work might give some important insights for designing new approach to meet the huge demand of LaA in the current market.


Assuntos
Acetona , Ácido Láctico , Acetona/análogos & derivados , Biomassa , Carbono
6.
Rev Bras Parasitol Vet ; 31(1): e020421, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35293430

RESUMO

Betta rubra is an ornamental freshwater fish endemic to northern Sumatra, Indonesia. The B. rubra population has decreased in recent decades, and is classified as an endangered species in the IUCN Red List. This study aims to report for the first time infection by L. cyprinacea in B. rubra harvested from the Aceh Besar region of Indonesia. The fish samples were obtained from the Cot Bira tributaries, Aceh Besar District, Indonesia from January to December 2020. The results showed that the parasite infected 6 out of 499 samples in August and September, with a prevalence and intensity rate of 1% and 2 parasites/fish, respectively. The eyes and pectoral fins were the common infection sites. Despite B. rubra is not an optimal host (small size) for the parasite, this parasite might serve as additional threatening factors for the endangered B. rubra fish population.


Assuntos
Copépodes , Animais , Acetona/análogos & derivados , Peixes/parasitologia , Água Doce , Indonésia/epidemiologia
7.
Drug Test Anal ; 14(3): 496-504, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33185037

RESUMO

Stable isotope ratio mass spectrometry (IRMS) can be used to determine the precursor and precursor origin of methylamphetamine drug samples. Previous work has shown that methylamphetamine samples can be distinguished as derived from different sources of (pseudo)ephedrine or phenyl-2-propanone (P2P) through the use of IRMS alongside conventional chemical profiling techniques. To date, limited research has been conducted to investigate whether methylamphetamine samples of differing P2P origins can be distinguished through drug profiling. This was investigated by synthesising methylamphetamine in-house in a three-step process. Two 'preprecursors' were used in this study, phenylacetic acid (PAA) and α-phenylacetoacetonitrile (α-PAAN). Using a combination of profiling techniques, it was found that methylamphetamine samples of PAA preprecursor origin and methylamphetamine samples of α-PAAN preprecursor origin can be distinguished.


Assuntos
Drogas Ilícitas , Metanfetamina , Acetona/análogos & derivados , Isótopos de Carbono/análise , Drogas Ilícitas/análise , Metanfetamina/análise , Isótopos de Nitrogênio/análise
8.
Drug Test Anal ; 14(3): 439-449, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34597469

RESUMO

Methyl 3-oxo-2-phenylbutyrate (MAPA) is a recently circulating precursor of phenylacetone (P2P), a precursor of amphetamine and methamphetamine. MAPA has a hybrid chemical structure of acetoacetic acid ester and P2P. Acetoacetic acid ester is de-esterified and decarboxylated to give the ketone by heating under acidic conditions; therefore, MAPA is presumed to be converted to P2P by such treatment. Considering that ethyl 3-oxo-2-phenylbutyrate (EAPA), methyl 3-oxo-4-phenylbutyrate (MGPA), and ethyl 3-oxo-4-phenylbutyrate (EGPA) have the same chemical features as MAPA, these three compounds are potential P2P precursors. The authors examined the analysis of these compounds by gas chromatography-mass spectrometry (GC-MS) and their conversion to P2P by heating under acidic and basic conditions. These compounds were remarkably decomposed into P2P during GC-MS analysis regardless of the injection method and injector temperature. EAPA and EGPA also caused ester exchange to methyl ester by injection of methanol solution. P2P production and transesterification were almost prevented by methoxime derivatization. These compounds were converted to P2P by heating under acidic conditions. The reaction of MGPA and EGPA proceeded quicker than that of EAPA. The important by-product associated with the reaction was phenylacetylcarbinol (formed from EAPA and MGPA), which will be converted to (pseudo)ephedrine, important methamphetamine impurities. By heating under basic conditions, MGPA and EGPA were converted to P2P but EAPA was mainly converted to phenylacetic acid. In the future, when these compounds are in circulation, our study will be useful for identifying and elucidating the synthetic method of P2P.


Assuntos
Anfetamina , Fenilbutiratos , Acetona/análogos & derivados , Cromatografia Gasosa-Espectrometria de Massas
9.
Rev. bras. parasitol. vet ; 31(1): e020421, 2022. tab, graf
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1365762

RESUMO

Abstract Betta rubra is an ornamental freshwater fish endemic to northern Sumatra, Indonesia. The B. rubra population has decreased in recent decades, and is classified as an endangered species in the IUCN Red List. This study aims to report for the first time infection by L. cyprinacea in B. rubra harvested from the Aceh Besar region of Indonesia. The fish samples were obtained from the Cot Bira tributaries, Aceh Besar District, Indonesia from January to December 2020. The results showed that the parasite infected 6 out of 499 samples in August and September, with a prevalence and intensity rate of 1% and 2 parasites/fish, respectively. The eyes and pectoral fins were the common infection sites. Despite B. rubra is not an optimal host (small size) for the parasite, this parasite might serve as additional threatening factors for the endangered B. rubra fish population.


Resumo Betta rubra é um peixe de água doce ornamental endemico da região norte Sumatra, Indonesia. A população de Betta rubra diminuiu ao longo dos anos, sendo classificada como espécie em extinção na Lista Vermelha da IUCN. Este estudo tem como objetivo relatar pela primeira vez infecção por L. cyprinacea em B. rubra coletados na região de Aceh Besar na Indonésia. As amostras de peixes foram obtidas nos afluentes Cot Bira, distrito de Aceh Besar, Indonésia de janeiro a dezembro de 2020. Os resultados mostraram que o parasito infectou 6 das 499 amostras em agosto e setembro, com uma prevalência e taxa de intensidade de 1% e 2 parasitas/peixes, respectivamente. Os olhos e as nadadeiras peitorais foram os sítios de infecção mais comuns. Apesar de B. rubra não ser um hospedeiro ideal (pequeno tamanho) para o parasita, este parasita pode servir como fator de ameaça adicional para a população de peixes B. rubra, ameaçada de extinção.


Assuntos
Animais , Copépodes , Acetona/análogos & derivados , Peixes/parasitologia , Água Doce , Hidrazonas , Indonésia/epidemiologia
10.
Gac Sanit ; 35 Suppl 2: S334-S336, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34929846

RESUMO

OBJECTIVE: To find out the relationship of energy intake, carbohydrate intake, protein intake, fat intake, and physical activity with the incidents of fatness in venerable. METHODS: Quantitative approach with cross-sectional design was applied and analyzed using chi square. Subjects in this research were venerable people aged 45-59 years old, who have the inclusion criteria were 88 people using Nutri survey technique through questionnaire. RESULT: The result showed a significant relationship between protein intake, fat, and activity of physic among fatness cases on venerable with p-value=0.023 (OR=0.164), p-value=0.028 (OR=1.529) and p-value=0.016 (OR=1.474). On the other hand, the research found not a significant relationship between energy intake and carbohydrate intake with the incidents of fatness in venerable with p-value =0.308 (OR=1.474) and p-value=1.000 (OR=1.450). CONCLUSION: Excessive protein intake and fat intake with light activity can be a risk factor for fatness, especially in the venerable. It is suggested to venerable people to keep their daily food intake and do physical activity to reduce the risk of fatness.


Assuntos
Gorduras na Dieta , Ingestão de Energia , Humanos , Pessoa de Meia-Idade , Acetona/análogos & derivados , Tecido Adiposo , Estudos Transversais
11.
Artigo em Inglês | MEDLINE | ID: mdl-34501804

RESUMO

Indonesian universal health coverage was implemented in 2013 and hemodialysis services became universally accessible, yet few studies have examined patient adherence to hemodialysis schedules. We examined the rates of missed in-center hemodialysis sessions in Banda Aceh and the factors associated with non-attendance. This cross-sectional questionnaire survey included 193 patients receiving in-center hemodialysis. Approximately 28% of the patients missed ≥ 1 hemodialysis session in the month prior to the questionnaire's administration. About 65% reported attending religious activities as the reason for missing hemodialysis. The level of health literacy was generally low with a mean score of 14.38 out of 26 (55.3%). Multivariate logistic regression analyses showed that patients with educational levels higher than elementary school were less likely to miss hemodialysis sessions. Participants who performed more self-care behaviors had lower odds of missing hemodialysis sessions. Every unit increase in the health literacy score was associated with increased odds of missing hemodialysis sessions. Emphasizing the importance of attending hemodialysis sessions and modifying hemodialysis schedules based on patients' needs is essential. Patients who miss hemodialysis sessions should be reminded of all self-care behaviors. Health literacy among hemodialysis patients should be improved, with emphasis on patient safety, advanced knowledge, and critical health literacy.


Assuntos
Falência Renal Crônica , Humanos , Acetona/análogos & derivados , Estudos Transversais , Indonésia/epidemiologia , Falência Renal Crônica/epidemiologia , Falência Renal Crônica/terapia , Diálise Renal
12.
Free Radic Biol Med ; 166: 178-186, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33636334

RESUMO

Aminoacetone (1-aminopropan-2-one), a putative minor biological source of methylglyoxal, reacts like other α-aminoketones such as 6-aminolevulinic acid (first heme precursor) and 1,4-diaminobutanone (a microbicide) yielding electrophilic α-oxoaldehydes, ammonium ion and reactive oxygen species by metal- and hemeprotein-catalyzed aerobic oxidation. A plethora of recent reports implicates triose phosphate-generated methylglyoxal in protein crosslinking and DNA addition, leading to age-related disorders, including diabetes. Importantly, methylglyoxal-treated hemoglobin adds four water-exposed arginine residues, which may compromise its physiological role and potentially serve as biomarkers for diabetes. This paper reports on the co-oxidation of aminoacetone and oxyhemoglobin in normally aerated phosphate buffer, leading to structural changes in hemoglobin, which can be attributed to the addition of aminoacetone-produced methylglyoxal to the protein. Hydroxyl radical-promoted chemical damage to hemoglobin may also occur in parallel, which is suggested by EPR-spin trapping studies with 5,5-dimethyl-1-pyrroline-N-oxide and ethanol. Concomitantly, oxyhemoglobin is oxidized to methemoglobin, as indicated by characteristic CD spectral changes in the Soret and visible regions. Overall, these findings may contribute to elucidate the molecular mechanisms underlying human diseases associated with hemoglobin dysfunctions and with aminoacetone in metabolic alterations related to excess glycine and threonine.


Assuntos
Hemoglobinas , Aldeído Pirúvico , Acetona/análogos & derivados , Espectroscopia de Ressonância de Spin Eletrônica , Humanos , Oxirredução , Espécies Reativas de Oxigênio
13.
Biosens Bioelectron ; 172: 112773, 2021 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-33161291

RESUMO

Highly selective molecularly imprinted polymers (MIPs) towards benzyl methyl ketone (BMK) were synthesized for application as recognition elements in a capacitive sensor. A computational approach was employed to select the most appropriate monomers and cross-linkers. Using the selected compounds, different polymerization techniques and protocols were compared in order to study the effect on the MIP performance and characteristics. MIPs synthesized by bulk polymerization using itaconic acid and 1-vinylimidazole as monomers and p-divinylbenzene as cross-linker possess the highest affinity towards the target analyte. Prior to capacitive analysis, the developed particles were immobilized on the surface of gold transducers using tyramine as a linker. The validity of the developed sensor was checked by the BMK detection in spiked tap water and real water samples. A linear working range from 50 to 1000 µM was found while the limit of detection (LOD) was determined to be 1 µM in tap water. To the best of our knowledge, both the developed MIPs towards BMK and the electrochemical sensor for its detection have not been published or marketed to date.


Assuntos
Técnicas Biossensoriais , Impressão Molecular , Pró-Fármacos , Acetona/análogos & derivados , Anfetamina , Técnicas Eletroquímicas , Polímeros Molecularmente Impressos , Polímeros , Água
14.
Photochem Photobiol ; 97(2): 327-334, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33296511

RESUMO

Triplet carbonyls generated by chemiexcitation are involved in typical photobiochemical processes in the absence of light. Due to their biradical nature, ultraweak light emission and long lifetime, electronically excited triplet species display typical radical reactions such as isomerization, fragmentation, cycloaddition and hydrogen abstraction. In this paper, we report chemical reactions in a set of amino acid residues induced by the isobutanal/horseradish peroxidase (IBAL/HRP) system, a well-known source of excited triplet acetone (Ac3* ). Accordingly, quenching of Ac3* by tryptophan (Trp) unveiled parallel enzyme damage and inactivation, likely explained by scavenging of IBAL tertiary radical reaction intermediate and Ac3* -derived 2-hydroxy-i-propyl radical. Quenching constants were calculated from Stern-Volmer plots, and the structure of radical adducts was revealed by mass spectrometry. As expected, a concurrent Schiff-type adduct was found to be one of the reaction by-products. These findings draw attention to potential structural and functional changes in enzymes involved in the electronic chemiexcitation of their products.


Assuntos
Acetona/análogos & derivados , Peroxidase do Rábano Silvestre/química , Triptofano/química , Acetona/química , Catálise , Eletroforese em Gel de Poliacrilamida , Cinética , Oxirredução
15.
Gac. sanit. (Barc., Ed. impr.) ; 35(supl. 2): S334-S336, 2021. tab
Artigo em Inglês | IBECS | ID: ibc-220974

RESUMO

Objective: To find out the relationship of energy intake, carbohydrate intake, protein intake, fat intake, and physical activity with the incidents of fatness in venerable. Methods: Quantitative approach with cross-sectional design was applied and analyzed using chi square. Subjects in this research were venerable people aged 45–59 years old, who have the inclusion criteria were 88 people using Nutri survey technique through questionnaire. Result: The result showed a significant relationship between protein intake, fat, and activity of physic among fatness cases on venerable with p-value = 0.023 (OR = 0.164), p-value = 0.028 (OR = 1.529) and p-value = 0.016 (OR = 1.474). On the other hand, the research found not a significant relationship between energy intake and carbohydrate intake with the incidents of fatness in venerable with p-value = 0.308 (OR = 1.474) and p-value = 1.000 (OR = 1.450). Conclusion: Excessive protein intake and fat intake with light activity can be a risk factor for fatness, especially in the venerable. It is suggested to venerable people to keep their daily food intake and do physical activity to reduce the risk of fatness. (AU)


Assuntos
Humanos , Masculino , Feminino , Adulto , Pessoa de Meia-Idade , Consumo de Energia , Gorduras na Dieta , Estudos Transversais , Inquéritos e Questionários , Acetona/análogos & derivados , Tecido Adiposo
16.
Biochemistry (Mosc) ; 85(5): 575-582, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32571187

RESUMO

Phenylacetone monooxygenase (EC 1.14.13.92, PAMО) catalyzes oxidation of ketones with molecular oxygen and NADPH with the formation of esters. PAMО is a promising enzyme for biotechnological processes. In this work, we generated genetic constructs coding for PAMO from Thermobifida fusca, containing N- or C-terminal His6-tags (PAMO N and PAMO C, respectively), as well as PAMO L with the His6-tag attached to the enzyme C-terminus via a 19-a.a. spacer. All PAMO variants were expressed as catalytically active proteins in Escherichia coli BL21(DE3) cells; however, the expression level of PAMO N was 3 to 5 times higher than for the other two enzymes. The catalytic constants (kcat) of PAMO C and PAMO L were similar to that published for PAMO L produced in a different expression system; the catalytic constant for PAMO N was slightly lower (by 15%). The values of Michaelis constants with NADPH for all PAMО variants were in agreement within the published data for PAMO L (within the experimental error); however, the KM for benzylacetone was several times higher. Thermal inactivation studies and differential scanning calorimetry demonstrated that the thermal stability of PAMO N was 3 to 4 times higher compared to that of the enzymes with the C-terminal His6-tag.


Assuntos
Acetona/análogos & derivados , Histidina/química , Oxigenases de Função Mista/química , Oxigenases de Função Mista/metabolismo , Oligopeptídeos/química , Proteínas Recombinantes/metabolismo , Acetona/metabolismo , Cinética , Relação Estrutura-Atividade , Especificidade por Substrato , Thermobifida/enzimologia
17.
J Econ Entomol ; 113(3): 1419-1425, 2020 06 06.
Artigo em Inglês | MEDLINE | ID: mdl-32173761

RESUMO

The diamondback moth, Plutella xylostella (L.), is a worldwide insect pest of cruciferous crops. Although insecticides have long been used for its control, diamondback moth rapidly evolves resistance to almost any insecticide. In insects, juvenile hormone (JH) is critically involved in almost all biological processes. The correct activity of JH depends on the precise regulation of its titer, and juvenile hormone esterase (JHE) is the key regulator. Thus, JH and JHE have become important targets for new insecticide development. Trifluoromethyl ketones are specific JHE inhibitors, among which 3-octylthio-1,1,1-trifluoropropan-2-one (OTFP) has the highest activity. The interaction effects between pretreatment with or combination of OTFP and the insecticides diafenthiuron, indoxacarb, and Bacillus thuringiensis (Bt) were investigated in diamondback moth larvae to determine OTFP's potential as an insecticide synergist. In third-instar larvae, both pretreatment and combination treatment with OTFP decreased or antagonized the toxicities of diafenthiuron, indoxacarb, and Bt at all set concentrations. In fourth-instar larvae, combination treatment with OTFP decreased or antagonized the toxicities of diafenthiuron and indoxacarb at all set concentrations. However, it increased or synergized the toxicity of Bt at lower concentrations despite the limited effect at higher concentrations. Our results indicated that the effect of OTFP on the toxicities of insecticides varied with the type and concentration, larval stage, and treatment method. These findings contribute to the better use of OTFP in diamondback moth control.


Assuntos
Bacillus thuringiensis , Inseticidas , Mariposas , Acetona/análogos & derivados , Animais , Resistência a Inseticidas , Inseticidas/farmacologia , Larva , Oxazinas , Feniltioureia/análogos & derivados
18.
Nano Lett ; 20(4): 2558-2568, 2020 04 08.
Artigo em Inglês | MEDLINE | ID: mdl-32167768

RESUMO

Given the physically encapsulated payloads with drug burst release and/or low drug loading, it is critical to initiate an innovative prodrug strategy to optimize the design of modular nanomedicines. Here, we designed modular pH-sensitive acetone-based ketal-linked prodrugs of dexamethasone (AKP-dexs) and formulated them as nanoparticles. We comprehensively studied the relationships between AKP-dex structure and properties, and we selected two types of AKP-dex-loaded nanoparticles for in vivo studies on the basis of their size, drug loading, and colloidal stability. In a collagen-induced arthritis rat model, these AKP-dex-loaded nanoparticles showed higher accumulation in inflamed joints and better therapeutic efficacy than free dexamethasone phosphate with less-severe side effects. AKP-dex-loaded nanoparticles may be useful for treating other inflammatory diseases and thus have great translational potential. Our findings represent an important step toward the development of practical applications for acetone-based ketal-linked prodrugs and are useful in the design of modular nanomedicines.


Assuntos
Acetona/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Artrite Reumatoide/tratamento farmacológico , Dexametasona/uso terapêutico , Nanopartículas/uso terapêutico , Pró-Fármacos/uso terapêutico , Acetona/análogos & derivados , Acetona/farmacocinética , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacocinética , Artrite Reumatoide/patologia , Dexametasona/análogos & derivados , Dexametasona/farmacocinética , Camundongos , Nanomedicina , Nanopartículas/análise , Nanopartículas/química , Pró-Fármacos/química , Pró-Fármacos/farmacocinética , Células RAW 264.7 , Ratos
19.
J Agric Food Chem ; 68(11): 3558-3567, 2020 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-32065523

RESUMO

2-Ethyl-3,5(3,6)-dimethylpyrazines (EDMPs) have a pleasant aroma of roasted cocoa or nuts with an extreme low odor threshold that have potential in industrial applications as food fragrances. The food fermentation process can accumulate EDMPs, and this might be the chance to study the biosynthesis mechanism of EDMPs under mild conditions for "natural" EDMPs' production. In this study, an EDMP-producing strain was isolated from baijiu fermentation. This strain was identified as Bacillus subtilis, a generally regarded as safe organism. After reasonable assumption and substrate addition and isotope-labeled experiments, we found that EDMPs are produced from l-threonine and d-glucose at environmental temperature and pressure. In addition, aminoacetone, the metabolite of l-threonine, and 2,3-pentanedione, the metabolite of l-threonine and d-glucose, are intermediates for the production of EDMPs. This study proposed and confirmed the biosynthesis pathway of EDMPs. It will be helpful for the industrial production of EDMPs and provides reference for the biosynthetic mechanism analysis of other valuable pyrazines.


Assuntos
Bacillus subtilis , Acetona/análogos & derivados , Fermentação , Pentanonas , Feromônios , Pirazinas
20.
Molecules ; 25(3)2020 Feb 03.
Artigo em Inglês | MEDLINE | ID: mdl-32028657

RESUMO

A highly efficient quinine-derived primary-amine-catalyzed asymmetric aldol addition of hydroxyacetone to arylglyoxals is described. Structurally diverse anti-2,3-dihydroxy-1,4-diones were generated in high yields, with good diastereoselectivities and enantioselectivities.


Assuntos
Acetona/análogos & derivados , Aldeídos/química , Glioxilatos/química , Acetona/química , Catálise , Técnicas de Química Sintética , Estrutura Molecular
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