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1.
Bioorg Med Chem Lett ; 47: 128206, 2021 09 01.
Artigo em Inglês | MEDLINE | ID: mdl-34146704

RESUMO

Acetylcholinesterase (AChEis) inhibitors are used to treat neurodegenerative diseases like Alzheimer's disease (AD). l-Hypaphorine (l-HYP) is a natural indole alkaloid that has been shown to have effects on the central nervous system (CNS). The goal of this research was to synthesize l-HYP and d-HYP and test their anticholinesterasic properties in rat brain regions. l-HYP suppressed acetylcholinesterase (AChE) activity only in the cerebellum, whereas d-HYP inhibited AChE activity in all CNS regions studied. No cytotoxic effect on normal human cells (HaCaT) was observed in the case of l-HYP and d-HYP although an increase in cell proliferation. Molecular modeling studies revealed that d-HYP and l-HYP have significant differences in their binding mode positions and interact stereospecifically with AChE's amino acid residues.


Assuntos
Acetilcolinesterase/metabolismo , Encéfalo/enzimologia , Inibidores da Colinesterase/farmacologia , Indóis/farmacologia , Animais , Encéfalo/patologia , Inibidores da Colinesterase/química , Relação Dose-Resposta a Droga , Indóis/química , Estrutura Molecular , Ratos , Relação Estrutura-Atividade
2.
J Surg Oncol ; 121(5): 840-847, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32003476

RESUMO

INTRODUCTION: Multivisceral resection (MVR) is potentially curative for selected gastric cancer patients, supposedly at the cost of increased complications. However, current data comparing MVR to standard gastrectomy (SG) is lacking. OBJECTIVES: Compare complications and survival after MVR and SG. METHODS: In a retrospective cohort of 1015 patients with gastric adenocarcinoma, 58 underwent MVR and 466 SG. Groups were compared concerning their characteristics, complications, and survival. RESULTS: One hundred seventy-six patients had postoperative complications. Major complications were more frequent after MVR (P = .002). Surgical mortality was 8.6% and 4.9% for MVR and SG (P = .221). Older age, higher morbidities, and MVR were independent risk factors for major complications. The odds ratio for major complications was 5.89 for MVR with one or two organs and 38.01 for MVR with three or more organs. The pancreas was the most commonly removed organ and pT4b disease were confirmed in 34 (58.6%) of the MVR cases. Disease-free survival (DFS) was lower in MVR patients (51% vs 77.8%; P < .001), being worse according to the number of organs resected. In pN+ patients, DFS was worse after MVR. DFS was equivalent to pT4b and non-pT4b in the MVR group. CONCLUSIONS: Increased morbidity and lower survival are expected for gastric cancer patients undergoing MVR.


Assuntos
Gastrectomia , Neoplasias Gástricas/terapia , Adenocarcinoma/mortalidade , Adenocarcinoma/patologia , Adenocarcinoma/terapia , Fatores Etários , Quimioterapia Adjuvante , Estudos de Coortes , Colo/cirurgia , Intervalo Livre de Doença , Feminino , Humanos , Tempo de Internação/estatística & dados numéricos , Fígado/cirurgia , Masculino , Pessoa de Meia-Idade , Multimorbidade , Terapia Neoadjuvante , Pâncreas/cirurgia , Complicações Pós-Operatórias , Estudos Retrospectivos , Fatores de Risco , Esplenectomia , Neoplasias Gástricas/mortalidade , Neoplasias Gástricas/patologia
3.
Regul Toxicol Pharmacol ; 117: 104762, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32805323

RESUMO

In the state of Mato Grosso do Sul, Brazil, Piper glabratum leaves are used as a popular medicine for pain and inflammation. We performed a phytochemical analysis and evaluated the effects of ethanolic extract (EEPG) obtained from leaves of P. glabratum on toxicity as well as the effects of application of the hexanic fraction (HXPG) and the hydroalcoholic fraction (HAPG) obtained from the EEPG on inflammatory parameters and pain in mice. Swiss mice were treated with EEPG (30-300 mg/kg body weight (b.w.)), HXPG (19.5 mg/kg b.w.) or HAPG (83.37 mg/kg b.w.) and then subjected to carrageenan-induced pleurisy and paw oedema tests, the spontaneous pain, and zymosan-induced intra-articular inflammation. Wistar rats were treated with EEPG to assess acute toxicity. Phytochemical analysis of the fractions demonstrated the presence of phytol and mixture of stigmasterol and ß-sitosterol in the fractions. In the acute toxicity test, LD50 above 2000 mg/kg b.w. was observed. The treatments reduced oedema, cold and mechanical hyperalgesia, leukocyte migration and protein exudation. The antihyperalgesic and anti-inflammatory properties of EEPG and fractions were demonstrated in the present study. These results from EEPG and HXPG may be related, at least in part, to modulation of the inflammatory mediators by phytol, stigmasterol and ß-sitosterol.


Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Etanol/uso terapêutico , Piper , Extratos Vegetais/uso terapêutico , Folhas de Planta , Analgésicos/química , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Chondrus , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/tratamento farmacológico , Edema/patologia , Etanol/química , Feminino , Hiperalgesia/induzido quimicamente , Hiperalgesia/tratamento farmacológico , Hiperalgesia/patologia , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Ratos , Ratos Wistar , Testes de Toxicidade Aguda/métodos
4.
Int Wound J ; 16(2): 316-324, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30467979

RESUMO

To examine the influence of carboxytherapy on wound healing under venous insufficiency, full-thickness excisional wounds were created on Wistar rats. We used three groups with 32 rats each: Group (I): daily cleaning with 0.9% saline solution; Group Sulfadiazine (II): 1% silver sulfadiazine; and Carboxytherapy (III): subcutaneous application of 0.3 mL of carbon dioxide. The predetermined periods of analysis were the 3rd, 7th, 14th, and 30th day. The slides were stained with haematoxylin and eosin and Picrosirius red and submitted for immunohistochemistry. Groups II and III presented a statistically significant decrease in relation to the presence of neutrophilic and lymphocytic infiltrates. The presence of collagen significant increased in groups II and III. However, group III presented better organisation. Only group I maintained the neovascularisation until the 30th day. The new epithelium statistically significantly increased in groups II and III. On immunohistochemistry, regarding fibronectin expression, only group III demonstrated a statistically significant increase since the beginning of the healing process. Thus, the use of carboxytherapy promotes the formation of a tissue better structured and that may be an important resource for the treatment of wounds under venous insufficiency, especially those of recurrent re-openings.


Assuntos
Dióxido de Carbono/uso terapêutico , Fibronectinas/efeitos dos fármacos , Inflamação/tratamento farmacológico , Sulfadiazina de Prata/uso terapêutico , Insuficiência Venosa/tratamento farmacológico , Cicatrização/efeitos dos fármacos , Animais , Masculino , Ratos , Ratos Wistar
6.
Int J Pharm ; 644: 123323, 2023 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-37597596

RESUMO

Herein we report the synthesis of transition-metal-free potassium borophosphate glasses and their application as bactericidal and bacteriostatic material. The antimicrobial activity was achieved through a simple change in the molar ratio of boron and phosphorus atoms, making borophosphate glass soluble in water. The glasses were analyzed by X-ray powder diffraction, Raman spectroscopy, laser-induced breakdown spectroscopy, and water absorption. The addition of a boron compound is required to obtain potassium-based phosphate glasses. Moreover, the change in the phosphorus and boron molar ratio (P/B), 2, 1 or 0.5 affects the glass solubilization in water, which increases with the phosphorus content. The glass materials were submitted to tests of biological activity against the bacteria Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. These water-soluble borophosphate glasses were employed in the development of hydrogel formulations using Carbopol®. Phosphorous-rich samples at a concentration of 15 % (w/w) in hydrogel showed better antimicrobial activity against S. aureus and E. coli, when compared to other samples, including commercial alcohol hand sanitizer gel, with an average size of the inhibition halo of 24.02±1.43 and 19.24±1.63mm, respectively.


Assuntos
Anti-Infecciosos , Boro , Escherichia coli , Staphylococcus aureus , Hidrogéis , Fósforo , Potássio
7.
Langmuir ; 27(15): 9277-84, 2011 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-21739956

RESUMO

A new class of photoreactive surfactants (PRSs) is presented here, consisting of amphiphiles that can also act as reagents in photochemical reactions. An example PRS is cobalt 2-ethylhexanoate (Co(EH)(2)), which forms reverse micelles (RMs) in a hydrocarbon solvent, as well as mixed reversed micelles with the standard surfactant Aerosol-OT (AOT). Small-angle neutron scattering (SANS) data show that mixed AOT/PRS RMs have a spherical structure and size similar to that of pure AOT micelles. Excitation of the ligand-to-metal charge transfer (LMCT) band in the PRSs promotes electron transfer from PRS to associated metal counterions, leading to the generation of metal and metal-oxide nanoparticles inside the RMs. This work presents proof of concept for employing PRSs as precursors to obtain nearly monodisperse inorganic nanoparticles: here both Co(3)O(4) and Bi nanoparticles have been synthesized at high metal concentration (10(-2) M) by simply irradiating the RMs. These results point toward a new approach of photoreactive self-assembly, which represents a clean and straightforward route to the generation of nanomaterials.

8.
Life Sci ; 264: 118697, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-33130084

RESUMO

AIM: To evaluate the influence of intermittent fasting and high-intensity interval training (HIIT) on myocardial apoptosis signaling and cardiac morphological characteristics in healthy rats. METHODS: Male Wistar rats (n = 60) were divided into four groups: sedentary control (SED-C), intermittent fasting (SED-IF), high-intensity interval training (HIIT-C), and high-intensity interval training plus intermittent fasting (HIIT-IF). SED-C and HIIT-C groups were treated daily with ad libitum chow; SED-IF and HIIT-IF received the same standard chow every other day. HIIT-C and HIIT-IF rats were submitted to an HIIT protocol five times a week for 12 weeks. At the end of the experiment, functional capacity, cardiac morphology, and expression of apoptosis signaling pathways-related proteins were analyzed. KEY FINDINGS: HIIT increased cardiomyocyte cross-sectional area, collagen interstitial fraction, and the pro-apoptotic proteins AIF and caspase-3 expression, and reduced pro-apoptotic protein CYTC expression and the cleaved-to-non-cleaved PARP-1 ratio in myocardium. Intermittent fasting reduced cardiomyocyte cross-sectional area, collagen interstitial fraction, and expression of Bax, CYTC and cleaved PARP-1, and increased expression of the anti-apoptotic protein BCL-2. SMAC, ARC, and caspase-8 expression was not changed by HIIT or intermittent fasting. SIGNIFICANCE: HIIT promotes cardiomyocyte hypertrophy and interstitial fibrosis, and modulates the apoptosis signaling pathway in healthy rat myocardium. Intermittent fasting reduces pro-apoptotic and increases antiapoptotic signaling, besides attenuating HIIT-induced cardiomyocyte hypertrophy and myocardial interstitial fibrosis.


Assuntos
Apoptose , Jejum , Treinamento Intervalado de Alta Intensidade , Miocárdio/patologia , Condicionamento Físico Animal , Animais , Masculino , Modelos Biológicos , Miócitos Cardíacos/metabolismo , Miócitos Cardíacos/patologia , Ratos Wistar , Transdução de Sinais
9.
Int J Burns Trauma ; 10(6): 296-306, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33500841

RESUMO

Overall, major burn wounds may require special care and long-term hospitalization as they not only bring complications from the wound itself, but may also compromise the immune system, or even other organs. Previous studies have indicated that topical insulin cream shortened wound closure time in second-degree burns in rats. Transplanted adipose-derived stem cells (AD-MSCs) have been developed as an alternative to treat burns and to accelerate the healing process. The aim of the present study is to investigate the effect of topical insulin gel, associated with AD-MSCs intradermal administration to heal second-degree burn wounds in rat models who were subjected to second-degree dorsal burns. The models were divided into four groups (n = 10 per group): placebo gel (C), topical insulin gel (TI), topical insulin gel and adipose-derived mesenchymal stem cells (TIMSCs) and placebo gel and adipose-derived mesenchymal stem cells (CMSCs). Wounds were assessed on a daily basis and histological evaluations were made on 5 animals from each group on the seventh and fourteenth day. There was a significant macroscopic decrease in burn wound areas in the Control (P = 0.0083), TIMSCs and CMSCs (P = 0.042) groups between the seventh and fourteenth days. The TI treatment did not show any significant change (P > 0.05) throughout this same period. The histological analysis showed significant granulation tissue formation in CMSCs and TIMSCs (P = 0.02235) treatments during the experimental period. According to the results, intradermal administration of allogenic AD-MSCs in experimental second-degree burns for short periods of time in the rat model has contributed to reducing the inflammatory phase duration, improving wound re-epithelialization, tissue granulation and wound contraction, as well as increasing collagen deposition.

10.
ChemMedChem ; 15(5): 449-458, 2020 03 05.
Artigo em Inglês | MEDLINE | ID: mdl-31834975

RESUMO

Organosulfur compounds show cytotoxic potential towards many tumor cell lines. Disulfides and thiosulfonates act through apoptotic processes, inducing proteins associated with apoptosis, endoplasmic reticulum stress, and the unfolded protein response. Three p-substituted symmetric diaryl disulfides and three diaryl thiosulfonates were synthesized and analyzed for inhibition of tubulin polymerization and for human cancer cell cytotoxic activity against seven tumor cell lines and a non-tumor cell line. S-(4-methoxyphenyl)-4-methoxybenzenesulfonothioate (6) exhibited inhibition of tubulin polymerization and showed the best antiproliferative potential, especially against the 786-0 cell line, being six times more selective as compared with the non-tumor cell line. In addition, compound 6 was able to activate caspase-3 after 24 and 48 h treatments of the 786-0 cell line and induced cell-cycle arrest in the G2/M stage at the highest concentration evaluated at 24 and 48 h. Compound 6 was able to cause complete inhibition of proliferation, inducing the death of 786-0 cells, by increasing the number of cells at G2/M and greater activation of caspase-3.


Assuntos
Antineoplásicos/farmacologia , Carcinoma de Células Renais/tratamento farmacológico , Neoplasias Renais/tratamento farmacológico , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Carcinoma de Células Renais/metabolismo , Carcinoma de Células Renais/patologia , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Neoplasias Renais/metabolismo , Neoplasias Renais/patologia , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Polimerização/efeitos dos fármacos , Tubulina (Proteína)/metabolismo
11.
J Colloid Interface Sci ; 533: 216-226, 2019 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-30165299

RESUMO

The development of self-healing materials opens perspectives to fabricate devices with unprecedented lifetimes and recyclability that can be integrated with flexible electronics. However, the timescale at which these materials operate remains an important challenge to overcome. This article describes the fast self-healing behavior of aluminum/iron polyphosphate metallo-gels and their hybrids with polyaniline and gives a detailed investigation of their electrical behaviors. The samples can be cut, molded and healed by manual handling. The rebuilding process is mediated by water uptake and was directly observed by environmental scanning electron microscopy. Metallo-gels with and without polyaniline can be mixed to give homogeneous samples, where the conducting polymer is uniformly distributed within the inorganic matrix. Cyclic voltammetry experiments showed that polyaniline behaves within the metallo-gel in the same manner as it does in aqueous electrolytes. Furthermore, polyaniline adds electronic conductivity to the originally ion-conducting polyphosphate metallo-gel, as demonstrated by impedance spectroscopy. The ionic and electronic conductivities are 1.3-1.7 × 10-2 S·cm-1 and 5.2 × 10-4 S·cm-1, respectively. Such properties result from the "free" and "bound" water within the hydrogel network and the dynamic nature of the aluminum-phosphate interactions within the supramolecular network. The features presented here make these materials good candidates to be used as moldable electroactive binders in carbon-based electrodes and in all-solid-state flexible separators for repairable electrochemical capacitors and batteries.

12.
Mutat Res ; 658(3): 154-61, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-17827055

RESUMO

The polysaccharides beta-glucans occur as a principal component of the cellular walls. Some microorganisms, such as yeast and mushrooms, and also cereals such as oats and barley, are of economic interest because they contain large amounts of beta-glucans. These substances stimulate the immune system, modulating humoral and cellular immunity, and thereby have beneficial effect in fighting infections (bacterial, viral, fungal and parasitic). beta-Glucans also exhibit hypocholesterolemic and anticoagulant properties. Recently, they have been demonstrated to be anti-cytotoxic, antimutagenic and anti-tumorogenic, making them promising candidate as pharmacological promoters of health.


Assuntos
Mutação/efeitos dos fármacos , Neoplasias/prevenção & controle , beta-Glucanas/uso terapêutico , Animais , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Infecciosos/uso terapêutico , Antimutagênicos/química , Antimutagênicos/isolamento & purificação , Antimutagênicos/farmacologia , Antimutagênicos/uso terapêutico , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Citoproteção/efeitos dos fármacos , Citoproteção/genética , Promoção da Saúde/métodos , Humanos , Modelos Biológicos , Neoplasias/genética , beta-Glucanas/química , beta-Glucanas/isolamento & purificação , beta-Glucanas/farmacologia
13.
ACS Appl Mater Interfaces ; 10(9): 8077-8085, 2018 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-29462559

RESUMO

Plastic debris is a major environmental concern, and to find effective ways to reuse polystyrene (PS) presents major challenges. Here, it is demonstrated that polystyrene foams impregnated with SnO2 are easily generated from plastic debris and can be applied to photocatalytic degradation of dyes. SnO2 nanoparticles were synthesized by a polymeric precursor method, yielding specific surface areas of 15 m2/g after heat treatment to 700 °C. Crystallinity, size, and shape of the SnO2 particles were assessed by X-ray diffraction (XRD) and transmission electron microscopy (TEM), demonstrating the preparation of crystalline spherical nanoparticles with sizes around 20 nm. When incorporated into PS foams, which were generated using a thermally induced phase separation (TIPS) process, the specific surface area increased to 48 m2/g. These PS/SnO2 nanofoams showed very good efficiency for photodegradation of rhodamine B, under UV irradiation, achieving up to 98.2% removal. In addition the PS/SnO2 nanofoams are shown to retain photocatalytic activity for up to five reuse cycles.

14.
Chem Commun (Camb) ; 49(27): 2765-7, 2013 Apr 07.
Artigo em Inglês | MEDLINE | ID: mdl-23443740

RESUMO

Dicationic magnetic ionic liquids with heteroanionic anions allow for tunability of physicochemical properties while retaining magnetic susceptibility.

15.
Rev. bras. farmacogn ; 24(5): 565-575, Sep-Oct/2014. tab, graf
Artigo em Inglês | LILACS | ID: lil-730563

RESUMO

Inflammatory and genetic alterations are related to the development of chronic diseases such as cancer. Schinus terebinthifolius Raddi, Anacardiaceae, is used in folk medicine to treat inflammation, wounds and tumors. This study evaluated the anti-inflammatory, immunomodulatory, chemopreventive, and wound healing potentials of the methanolic extract from the leaves of Schinus terebinthifolius. The chemical composition of the extract was characterized using preliminary analytical LC methods. The results showed that the anti-inflammatory activity of the methanolic extract was similar to that of dexamethasone for edema reduction. Also, it inhibited the leukocyte migration into the air pouch and decreased plasma extravasation. In addition, the methanolic extract showed a healing action similar to that observed with collagenase. The methanolic extract is not genotoxic nor mutagenic, and in contrast it has chemopreventive activity, which elicits a high percentage of damage reduction by comet and micronucleus assay, preferably by bioantimutagenic action. The methanolic extract induced apoptosis and enhanced splenic phagocytosis in animals treated with cyclophosphamide. The methanolic extract contents, resolved by LC, include phenolic acid and flavonoids. Our results suggest a therapeutic potential for the methanolic extract.

16.
Rev. bras. toxicol ; v.18(1): 57-61, jul. 2005. ilus, tab
Artigo em Português | LILACS | ID: lil-417099

RESUMO

O arsênio é um poluente ambiental que influência a função reprodutiva masculina, afetando o processo espermatogênico. O objetivo deste trabalho foi avaliar a eficiência reprodutiva de ratos adultos expostos ao arsênio e as possíveis malformações externas em sua prole. Foram utilizados 42 ratos (Wistar) distribuídos em 6 grupos de 7 animais cada. O grupo controle (G1) recebeu solução salina 2 vêzes por semana (i.p). Os grupos 2 a 6 receberam, 2 vezes por semana, 3,6 mg/Kg de arsenato de sódio (i.p), por 15, 30, 45, 60 e 75 dias, respectivamente. A taxa de prenhez apresentou diminuição significativa, associada à redução no potencial de fertilidade e o aumento na taxa de perdas pré-implantação; e as médias dos pesos fetais foram reduzidas. A taxa de perdas pós-implantação, reabsorção e malformação mostraram estatisticamente significativas. Os resultados mostram que a exposição crônica ao arsênio pode provocar redução na fertilidade de ratos. Estudos futuros são necessários para esclarecer os efeitos do arsênio no sistema reprodutor masculino e na prole destes machos...


Assuntos
Animais , Masculino , Ratos , Arsênio/toxicidade , Esterilizantes Químicos , Fertilidade , Poluentes Ambientais/efeitos adversos , Ratos Wistar
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