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1.
ACS Omega ; 6(18): 12318-12330, 2021 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-34056384

RESUMO

Two types of NiO-based composites (NiO@diatomite and Ni/NiO@diatomite) were synthesized as modified products of enhanced catalytic performances during the transesterification reactions of waste cooking oil. The influence of the diatomite substrate and the integration of metallic Ni0 in inducing the catalytic activity were evaluated in a series of transesterification reactions. The experimental conditions were adjusted according to the response surface methodology and the central composite statistical design. Experimentally, the diatomite substrate and the Ni0 metal induced the efficiency of the reaction to achieve a yield of 73.4% (NiO@diatomite) and 91% (Ni/NiO@diatomite), respectively, as compared to 66% for the pure phase (NiO). This was obtained under experimental conditions of 80 °C temperature, 100 min time, 12:1 methanol/oil molar ratio, and 3.75 wt % loading. The theoretical optimization functions of the designs suggested enhancement to the experimental conditions to achieve a yield of 76.3% by NiO@diatomite and 93.2% by Ni/NiO@diatomite. This reflected the role of the diatomite substrate in enhancing the surface area, the adsorption of fatty acids, and the exposure of the catalytic sites in addition to the effect of the Ni0 metal in enhancing the catalytic reactivity of the final product. Finally, the biodiesel produced over Ni/NiO@diatomite as the best product was of acceptable properties according to the international standards.

2.
Mitochondrial DNA B Resour ; 5(1): 754-755, 2020 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-33366735

RESUMO

The complete chloroplast genome sequences of vulnerable medicinal plant Saraca asoca (Roxb.) Willd. (Fabaceae) was sequenced. A total of 5,206,216,851 paired-end filtered reads of 151 bp were obtained. The plastome length (including LSC, SSC, IRa, and IRb) was 137,743 bp (GC content: 35.26%). A total of 126 coding genes which includes 97 CDS, 24 tRNA, and five rRNA genes were annotated. The phylogenetic analysis attempts to establish molecular signature in order to differentiate genuine sample of S. asoca from its adulterants easily.

3.
Curr Pharm Biotechnol ; 21(9): 842-851, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31995002

RESUMO

BACKGROUND: Estrogen Receptors (ER) are members of the nuclear intracellular receptors family. ER once activated by estrogen, it binds to DNA via translocating into the nucleus and regulates the activity of various genes. Withaferin A (WA) - an active compound of a medicinal plant Withania somnifera was reported to be a very effective anti-cancer agent and some of the recent studies has demonstrated that WA is capable of arresting the development of breast cancer via targeting estrogen receptor. OBJECTIVE: The present study is aimed at understanding the molecular level interactions of ER and Tamoxifen in comparison to Withaferin A using In-silico approaches with emphasis on Withaferin A binding capability with ER in presence of point mutations which are causing de novo drug resistance to existing drugs like Tamoxifen. METHODS: Molecular modeling and docking studies were performed for the Tamoxifen and Withaferin A with the Estrogen receptor. Molecular docking simulations of estrogen receptor in complex with Tamoxifen and Withaferin A were also performed. RESULTS: Amino acid residues, Glu353, Arg394 and Leu387 was observed as crucial for binding and stabilizing the protein-ligand complex in case of Tamoxifen and Withaferin-A. The potential of Withaferin A to overcome the drug resistance caused by the mutations in estrogen receptor to the existing drugs such as Tamoxifen was demonstrated. CONCLUSION: In-silico analysis has elucidated the binding mode and molecular level interactions which are expected to be of great help in further optimizing Withaferin A or design / discovery of future breast cancer inhibitors targeting estrogen receptor.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias da Mama/metabolismo , Receptores de Estrogênio/antagonistas & inibidores , Withania/química , Vitanolídeos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Simulação por Computador , Humanos , Ligantes , Simulação de Acoplamento Molecular , Plantas Medicinais , Mutação Puntual , Ligação Proteica , Receptores de Estrogênio/genética , Vitanolídeos/isolamento & purificação
4.
Drug Chem Toxicol ; 43(2): 158-164, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30203996

RESUMO

The present study was conducted to demonstrate cytotoxicity, apoptosis and hepatic damage induced by gemcitabine in laboratory mice. Animals were treated with a single dose of gemcitabine (415 mg/kg body wt), equivalent to a human therapeutic dose, and sacrificed after 1, 2 and 3 weeks. A significant decrease in mean body weight and absolute liver weight was registered. The levels of alkaline phosphatase (ALP), aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were increased as a result of this induced stress. Various structural changes were observed in the liver tissue of treated mice, as evident in the histological sections. Specifically, gemcitabine exposure was able to induce apoptosis in liver cells, and the incidence of TUNEL positive liver cells was increased compared to the control group. DNA fragmentation appeared on agarose gel and flow cytometry analysis confirmed the induction of apoptosis. These findings in gemcitabine-treated animal tissues suggest that inhibition or disruption of cells' DNA synthesis may be the mechanism by which this drug induces toxicity in the animal body.


Assuntos
Antimetabólitos Antineoplásicos/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Dano ao DNA/efeitos dos fármacos , Desoxicitidina/análogos & derivados , Animais , Apoptose/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/fisiopatologia , Fragmentação do DNA/efeitos dos fármacos , Desoxicitidina/toxicidade , Marcação In Situ das Extremidades Cortadas , Fígado/efeitos dos fármacos , Fígado/enzimologia , Fígado/patologia , Masculino , Camundongos , Fatores de Tempo , Gencitabina
5.
Saudi J Biol Sci ; 26(3): 547-553, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30899170

RESUMO

The extracts prepared from various areal parts of the Adenium obesum (Forssk.) Roem. & Schult. (Family: Apocynaceae) including leaves, fruit and seeds ethanolic extracts and seed aqueous extract were evaluated against MCF-7 cells in order to investigate its potential of cytogenotoxicity and induction of apoptosis. The ethanolic seeds extract had comparatively higher cytotoxicity (IC50 ∼ 337 µg/ml). Further, apoptosis and DNA damaging potential of seeds ethanolic extract was analyzed by applying multiple sub-lethal concentrations and durations. Flow cytometry results revealed that maximum percentage of early apoptosis (37%) and late apoptosis (35%) were observed after 12 h exposure in concentrations 200 µg/ml and 300 µg/ml, respectively. Similarly, the higher effect of extract in terms of DNA damage by alkaline comet assay was registered after 12 h treatment at concentrations 200 and 300 µg/mL. The calculated total damage score (TDS) for these concentrations were 614 and 617, respectively. The above findings indicate that A. obesum ethanolic seeds extracts has cytogenotoxic properties that could be further explored for the potential source of chemotherapeutic lead against cancer.

6.
Biomed Pharmacother ; 106: 499-509, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29990838

RESUMO

Commiphora molmol possesses multiple therapeutic benefits against various diseases; however, its protective role against methotrexate (MTX) renal toxicity has not been previously investigated. MTX is a dihydrofolate reductase inhibitor that can induce acute kidney injury (AKI). This study evaluated the in vitro antioxidant activity and the protective effect of C. molmol resin extract against MTX-induced oxidative stress, inflammation and renal injury. Male Wistar rats received 125 and 250 mg/kg C. molmol resin extract for 15 days and a single injection of MTX at day 16. C. molmol showed a radical scavenging activity against DPPH, superoxide and nitric oxide (NO) radicals. Rats received MTX showed renal injury evidenced by the significantly elevated serum creatinine and urea, and the histological alterations. The kidney of MTX-induced rats exhibited increased lipid peroxidation, NO, NF-κB and pro-inflammatory cytokines. Pre-treatment with C. molmol prevented MTX-induced kidney injury and attenuated oxidative stress and inflammation. C. molmol down-regulated Bax and enhanced the activity and expression of the antioxidant defenses. Furthermore, the expression of Bcl-2, Nrf2, NQO-1 and HO-1 was down-regulated in the kidney of MTX-induced rats. Pre-treatment with C. molmol resin up-regulated Bcl-2 and activated Nrf2/HO-1 signaling in the kidney of MTX-induced rats. In conclusion, C. molmol resin provided protection against MTX-induced AKI via activation of Nrf2 signaling and mitigation of oxidative stress.


Assuntos
Injúria Renal Aguda/prevenção & controle , Anti-Inflamatórios/farmacologia , Elementos de Resposta Antioxidante , Commiphora , Sequestradores de Radicais Livres/farmacologia , Heme Oxigenase (Desciclizante)/metabolismo , Rim/efeitos dos fármacos , Metotrexato , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Resinas Vegetais/farmacologia , Injúria Renal Aguda/induzido quimicamente , Injúria Renal Aguda/enzimologia , Injúria Renal Aguda/patologia , Animais , Anti-Inflamatórios/isolamento & purificação , Commiphora/química , Citoproteção , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Sequestradores de Radicais Livres/isolamento & purificação , Regulação Enzimológica da Expressão Gênica , Heme Oxigenase (Desciclizante)/genética , Mediadores da Inflamação/metabolismo , Rim/enzimologia , Rim/patologia , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Fator 2 Relacionado a NF-E2/genética , Fitoterapia , Plantas Medicinais , Ratos Wistar , Resinas Vegetais/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos
7.
Asian-Australas J Anim Sci ; 30(2): 154-159, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27492350

RESUMO

OBJECTIVE: This study was designed to characterize the DNA polymorphisms of the melanocortin-1 receptor (MC1R) gene in indigenous Saudi Arabian sheep breeds exhibiting different color coats, along with individuals of the Sawaknee breed, an exotic sheep imported from Sudan. METHODS: The complete coding region of MC1R gene including parts of 3' and 5' untranslated regions was amplified and sequenced from three the indigenous Saudi sheep; Najdi (generally black, n = 41), Naeimi (generally white with brown faces, n = 36) and Herri (generally white, n = 18), in addition to 13 Sawaknee sheep. RESULTS: Five single nucleotide polymorphisms (SNPs) were detected in the MC1R gene: two led to nonsynonymous mutations (c.218 T>A, p.73 Met>Lys and c.361 G>A, p.121 Asp>Asn) and three led to synonymous mutations (c.429 C>T, p.143 Tyr>Tyr; c.600 T>G, p.200 Leu>Leu, and c.735 C>T, p.245 Ile>Ile). Based on these five SNPs, eight haplotypes representing MC1R Ed and E+ alleles were identified among the studied sheep breeds. The most common haplotype (H3) of the dominant Ed allele was associated with either black or brown coat color in Najdi and Sawaknee sheep, respectively. Two other haplotypes (H6 and H7) of Ed allele, with only the nonsynonymous mutation A218T, were detected for the first time in Saudi indigenous sheep. CONCLUSION: In addition to investigating the MC1R allelic variation in Saudi indigenous sheep populations, the present study supports the assumption that the two independent nonsynonymous Met73Lys and Asp121Asn mutations in MC1R gene are associated with black or red coat colors in sheep breeds.

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