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1.
Arch Microbiol ; 206(2): 72, 2024 Jan 22.
Artigo em Inglês | MEDLINE | ID: mdl-38252323

RESUMO

Antimicrobial agents are used to treat microbial ailments, but increased use of antibiotics and exposure to infections in healthcare facilities and hospitals as well as the excessive and inappropriate use of antibiotics at the society level lead to the emergence of multidrug-resistant (MDR) bacteria. Antimicrobial resistance (AMR) is considered a public health concern and has rendered the treatment of different infections more challenging. The bacterial strains develop resistance against antimicrobial agents by limiting intracellular drug accumulation (increasing efflux or decreasing influx of antibiotics), modification and inactivation of drugs and its targets, enzymatic inhibition, and biofilm formation. However, the driving factors of AMR include the sociocultural and economic circumstances of a country, the use of falsified and substandard medicines, the use of antibiotics in farm animals, and food processing technologies. These factors make AMR one of the major menaces faced by mankind. In order to promote reciprocal learning, this article summarizes the current AMR situation in Pakistan and how it interacts with the health issues related to the COVID-19 pandemic. The COVID-19 pandemic aids in illuminating the possible long-term impacts of AMR, which are less immediate but not less severe since their measures and effects are equivalent. Impact on other sectors, including the health industry, the economy, and trade are also discussed. We conclude by summarizing the several approaches that could be used to address this issue.


Assuntos
Antibacterianos , COVID-19 , Animais , Humanos , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Farmacorresistência Bacteriana , Pandemias/prevenção & controle , Saúde Pública
2.
Crit Rev Food Sci Nutr ; : 1-19, 2023 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-36748791

RESUMO

Myrtaceae is one of the most important plants families, being regarded as the eighth largest flowering plant family. It includes many genera of utmost ecological and economical importance distributed all over the world. This review aimed to report the latest studies on this family focusing on certain widely used plants including Eucalyptus sp., Eugenia sp. (Eugenia uniflora, Eugenia sulcata), Syzygium sp. (Syzygium aromaticum and Syzygium cumini), Psidium sp., Pimenta dioica, Myrtus sp. (Myrtus communis), Myrciaria sp. and Melaleuca alternifolia. The extraction of bioactive compounds has been evolving through the optimization of conventional methods and the use of emerging technologies. Supercritical CO2 was applied for essential oils and ultrasound for polyphenols leading to extracts and essential oils rich in bioactive compounds. Advances in the field of encapsulation and delivery systems showed promising results in the production of stable essential oils nanoemulsions and liposomes and the production of plant extracts in the form of nanoparticles. Moreover, a significant increase in the number of patents was noticed especially the application of Myrtaceae extracts in the pharrmacuetucal field. The applications of ceratin plants (Pimenta dioica, Melaleuca alternifolia, Syzygium aromaticum essential oils or Myrciaria cauliflora peel extract) in food area (either as a free or encapsulated form) also showed interesting results in limiting microbial spoilage of fresh meat and fish, slowing oxidative degradation in meat products, and inhibiting aflatoxin production in maize. Despite the massive literature on Myrtaceae plants, advances are still necessary to optimize the extraction with environmentally friendly technologies and carry out risk assessment studies should be accomplished to harness the full potential in food, industrial and pharmaceutical applications.

3.
Chem Biodivers ; 20(4): e202200721, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36935351

RESUMO

Some issues, such as their obscure fate or low survival rate into the body during stem cell therapy, should be addressed to boost efficiency. Nanotechnology offers a suitable solution to combat such limitations. Carbon quantum dots (CQDs) are carbon-based nanomaterials and may be used as multi-purpose compounds in stem cell therapy. CQDs are excellent choices for stem cell labeling thanks to their special features such as optical properties and good biocompatibility. Besides, they can modulate the biological function of stem cells, such as their proliferation, homing ability, and differentiation properties. Considering the charismatic feature of CQDs and their broad unique effect on stem cells, the current review aims to summarize the advancements in this field. Hence, we first focused on CQDs synthesis and their applications. In the next section, the stem cell categories will be discussed, and the final part is dedicated to the recent research evaluating the impact of CQDs on stem cell therapy.


Assuntos
Pontos Quânticos , Carbono , Terapia Baseada em Transplante de Células e Tecidos
4.
Molecules ; 28(12)2023 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-37375137

RESUMO

A series of carbamothioyl-furan-2-carboxamide derivatives were synthesized using a one-pot strategy. Compounds were obtained in moderate to excellent yields (56-85%). Synthesized derivatives were evaluated for their anti-cancer (HepG2, Huh-7, and MCF-7 human cancer cell lines) and anti-microbial potential. Compound p-tolylcarbamothioyl)furan-2-carboxamide showed the highest anti-cancer activity at a concentration of 20 µg/mL against hepatocellular carcinoma, with a cell viability of 33.29%. All compounds showed significant anti-cancer activity against HepG2, Huh-7, and MCF-7, while indazole and 2,4-dinitrophenyl containing carboxamide derivatives were found to be less potent against all tested cell lines. Results were compared with the standard drug doxorubicin. Carboxamide derivatives possessing 2,4-dinitrophenyl showed significant inhibition against all bacterial and fungal strains with inhibition zones (I.Z) in the range of 9-17 and MICs were found to be 150.7-295 µg/mL. All carboxamide derivatives showed significant anti-fungal activity against all tested fungal strains. Gentamicin was used as the standard drug. The results showed that carbamothioyl-furan-2-carboxamide derivatives could be a potential source of anti-cancer and anti-microbial agents.


Assuntos
Anti-Infecciosos , Antineoplásicos , Humanos , Relação Estrutura-Atividade , Anti-Infecciosos/farmacologia , Células MCF-7 , Fungos , Furanos/farmacologia , Antineoplásicos/farmacologia , Estrutura Molecular , Proliferação de Células
5.
Crit Rev Food Sci Nutr ; 62(14): 3913-3929, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33427482

RESUMO

Naturally occurring plant-based gums and their engineered bio-nanostructures have gained an immense essence of excellence in several industrial, biotechnological, and biomedical sectors of the modern world. Gums derived from bio-renewable resources that follow green chemistry principles are considered green macromolecules with unique structural and functional attributes. For instance, gum mostly obtained as exudates are bio-renewable, bio-degradable, bio-compatible, sustainable, overall cost-effective, and nontoxic. Gum exudates also offer tunable attributes that play a crucial role in engineering bio-nanostructures of interest for several bio- and non-bio applications, e.g., food-related items, therapeutic molecules, sustained and controlled delivery cues, bio-sensing constructs, and so on. With particular reference to plant gum exudates, this review focuses on applied perspectives of various gums, i.e., gum Arabic, gum albizzia, gum karaya, gum tragacanth, and gum kondagogu. After a brief introduction with problem statement and opportunities, structural and physicochemical attributes of plant-based natural gums are presented. Following that, considerable stress is given to green synthesis and stabilization of gum-based bio-nanostructures. The final part of the review focuses on the bio- and non-bio related applications of various types of gums polysaccharides-oriented bio-nanostructures.


Assuntos
Nanoestruturas , Tragacanto , Goma Arábica/química , Gomas Vegetais , Polissacarídeos , Tragacanto/química
6.
Environ Res ; 215(Pt 3): 114398, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36174757

RESUMO

Industrial wastewater is causing serious health problems due to presence of large concentrations of toxic metals. Removal of these metals is still a big challenge using pristine natural biopolymers due to their low surface area, water solubility, and poor recovery. Developing biopolymeric composites with other materials has attained attention because they possess a high surface area and structural porosity, high reactivity, and less water solubility. In simple words, biopolymeric nanohybrids have great adsorption capacity for heavy metals. Biopolymeric materials are abundant, low cost, biodegradable, and possess different functional moieties (carboxyl, amine, hydroxyl, and carbonyl) which play a vital role to adsorb metal ions through various inter-linkages (i.e., electrostatic, hydrogen bonding, ion exchange, chelation, etc.). Biopolymeric nanohybrids have been proven a potent tool in environmental remediation such as the abatement of heavy metal ions from polluted water. Herein, we have reported the adsorption potential of various biopolymers (cellulose, chitosan, pectin, gelatin, and silk proteins) for the removal of heavy metals. This review discusses the suitability of biopolymeric nanohybrids as an adsorbent for heavy metals, their synthesis, modification, adsorption potential, and adsorption mechanism along with best fitted thermodynamic and kinetic models. The influence of pH, contact time, and adsorbent dose on adsorption potential has also been discussed in detail. Lastly, the challenges, research gaps and recommendations have been presented. This review concludes that biopolymers in combination with other materials such as metal-based nanoparticles, clay, and carbon-based materials are excellent materials to remove metallic ions from wastewater. Significant adsorption of heavy metals was obtained at a moderate pH (5-6). Contact time and adsorbent dose also affect the adsorption of heavy metals in certain ways. The Pseudo-first order model fits the data for the initial period of the first step of the reaction. Kinetic studies of different adsorption processes of various biopolymeric nanohybrids described that for majority of bionanohybrids, Pseudo-second order fitted the experimental data very well. Functionalized biopolymeric nanohybrids being biodegradable, environment friendly, cost-effective materials have great potential to adsorb heavy metal ions. These may be the future materials for environmental remediation.


Assuntos
Quitosana , Metais Pesados , Poluentes Químicos da Água , Adsorção , Aminas , Biopolímeros , Carbono , Celulose , Argila , Gelatina , Concentração de Íons de Hidrogênio , Íons , Cinética , Metais Pesados/análise , Pectinas , Seda , Águas Residuárias/química , Água , Poluentes Químicos da Água/análise
7.
J Basic Microbiol ; 62(9): 1143-1155, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34724237

RESUMO

Naphthamides have pharmacological potential as they express strong activities against microorganisms. The commercially available naphthoyl chloride and 4-bromoaniline were condensed in dry dichloromethane (DCM) in the presence of Et3 N to form N-(4-bromophenyl)-1-naphthamide (86%) (3). Using a Pd(0) catalyzed Suzuki-Miyaura Cross-Coupling reaction of (3) and various boronic acids, a series of N-([1,1'-biaryl]-4-yl)-1-naphthamide derivatives (4a-h) were synthesized in moderate to good yields. The synthesized derivatives were evaluated for cytotoxicity haemolytic assay and biofilm inhibition activity through in silico and in vitro studies. Molecular docking, ADME (absorption, distribution, metabolism, and excretion), toxicity risk, and other cheminformatics predict synthesized molecules as biologically active moieties, further validated through in vitro studies in which compounds (4c) and (4f) showed significant haemolytic activity whereas (4e) exhibited an efficient biofilm inhibition activity against Gram-negative bacteria Escherichia coli and Gram-positive bacteria Bacillus subtilis. When forming biofilms, bacteria become resistant to various antimicrobial treatments. Currently, research is focused on the development of agents that inhibit biofilm formation, thus the present work is valuable for preventing future drug resistance.


Assuntos
Biofilmes , Quimioinformática , Antibacterianos/farmacologia , Bactérias , Escherichia coli , Bactérias Gram-Positivas , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular
8.
Int J Mol Sci ; 22(14)2021 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-34299082

RESUMO

The Mimosa genus belongs to the Fabaceae family of legumes and consists of about 400 species distributed all over the world. The growth forms of plants belonging to the Mimosa genus range from herbs to trees. Several species of this genus play important roles in folk medicine. In this review, we aimed to present the current knowledge of the ethnogeographical distribution, ethnotraditional uses, nutritional values, pharmaceutical potential, and toxicity of the genus Mimosa to facilitate the exploitation of its therapeutic potential for the treatment of human ailments. The present paper consists of a systematic overview of the scientific literature relating to the genus Mimosa published between 1931 and 2020, which was achieved by consulting various databases (Science Direct, Francis and Taylor, Scopus, Google Scholar, PubMed, SciELO, Web of Science, SciFinder, Wiley, Springer, Google, The Plant Database). More than 160 research articles were included in this review regarding the Mimosa genus. Mimosa species are nutritionally very important and several species are used as feed for different varieties of chickens. Studies regarding their biological potential have shown that species of the Mimosa genus have promising pharmacological properties, including antimicrobial, antioxidant, anticancer, antidiabetic, wound-healing, hypolipidemic, anti-inflammatory, hepatoprotective, antinociceptive, antiepileptic, neuropharmacological, toxicological, antiallergic, antihyperurisemic, larvicidal, antiparasitic, molluscicidal, antimutagenic, genotoxic, teratogenic, antispasmolytic, antiviral, and antivenom activities. The findings regarding the genus Mimosa suggest that this genus could be the future of the medicinal industry for the treatment of various diseases, although in the future more research should be carried out to explore its ethnopharmacological, toxicological, and nutritional attributes.


Assuntos
Etnofarmacologia , Mimosa/química , Compostos Fitoquímicos/farmacologia , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Humanos
9.
Molecules ; 26(18)2021 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-34577076

RESUMO

A series of (E)-4-bromo-N-((3-bromothiophen-2-yl)methylene)-2-methylaniline analogs synthesized in considerable yields through Suzuki cross-coupling reactions. Various electron donating and withdrawing functional moieties were successfully incorporated under the employed reaction conditions. Reaction of 4-bromo-2-methylaniline (1) with 3-bromothiophene-2-carbaldehyde (2b) in the existence of glacial acetic acid, provided (E)-4-bromo-N-((3-bromothiophen-2-yl)methylene)-2-methylaniline (3b) in excellent yield (94%). Suzuki coupling of 3b with different boronic acids in the presence of Pd(PPh3)4/K3PO4 at 90 °C led to the synthesis of the monosubstituted and bisubstituted products 5a-5d and 6a-6d in moderate yields (33-40% and 31-46%, respectively). Density functional theory (DFT) investigations were performed on different synthesized analogues 5a-5d, 6a-6d to determine their structural characteristics. The calculations provide insight into the frontier molecular orbitals (FMOs) of the imine-based analogues and their molecular electrostatic potential (MESP). Reactivity descriptors like ionization energy (I), electron affinity (A), chemical hardness (ƞ) and index of nucleophilicity have been calculated for the first time for the synthesized molecules.

10.
Molecules ; 25(7)2020 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-32244456

RESUMO

Metal-organic frameworks (MOFs) are a fascinating class of porous crystalline materials constructed by organic ligands and inorganic connectors. Owing to their noteworthy catalytic chemistry, and matching or compatible coordination with numerous materials, MOFs offer potential applications in diverse fields such as catalysis, proton conduction, gas storage, drug delivery, sensing, separation and other related biotechnological and biomedical applications. Moreover, their designable structural topologies, high surface area, ultrahigh porosity, and tunable functionalities all make them excellent materials of interests for nanoscale applications. Herein, an effort has been to summarize the current advancement of MOF-based materials (i.e., pristine MOFs, MOF derivatives, or MOF composites) for electrocatalysis, photocatalysis, and biocatalysis. In the first part, we discussed the electrocatalytic behavior of various MOFs, such as oxidation and reduction candidates for different types of chemical reactions. The second section emphasizes on the photocatalytic performance of various MOFs as potential candidates for light-driven reactions, including photocatalytic degradation of various contaminants, CO2 reduction, and water splitting. Applications of MOFs-based porous materials in the biomedical sector, such as drug delivery, sensing and biosensing, antibacterial agents, and biomimetic systems for various biological species is discussed in the third part. Finally, the concluding points, challenges, and future prospects regarding MOFs or MOF-based materials for catalytic applications are also highlighted.


Assuntos
Estruturas Metalorgânicas/química , Bioengenharia , Catálise , Sinais (Psicologia) , Oxirredução , Processos Fotoquímicos , Porosidade , Relação Estrutura-Atividade
11.
Bioorg Chem ; 92: 103216, 2019 11.
Artigo em Inglês | MEDLINE | ID: mdl-31491567

RESUMO

In our current research, a diverse effect of acetylcholinesterase inhibitors was studied on BALB-C mice by using pentylenetetrazole (PTZ) seizure model. A series of carboxamide analogs (4a-4i) have been synthesized via Suzuki coupling reaction in moderate to good yields (35-84%). To study the efficacy of the synthesized compounds against AD, in-vitro inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) was performed. A number of compounds showed inhibition in low micromolar range. Subsequently, these compounds were evaluated for anticonvulsive effects in BALB-C mice by using pentylenetetrazole (PTZ) seizure model. The compound 4e displayed potential anticonvulsive effect and displayed 50% and 80% protection from mortality at the dose of 10 mg/kg, and 30 mg/kg respectively. The compound 4h showed some protection (33%) from mortality at 10 mg/kg and was not further explored based on non-significant delay in onset of myoclonic seizures. While, other compounds from the series did not show any anticonvulsive activity. To rationalize the observed biological activity, we performed docking studies against AChE and BChE targets. To explore the rationale of the mechanism of in-vivo anticonvulsant activity, docking studies were performed on GABAergic receptors. Moreover, in order to establish a relationship between physiochemical data of the synthesized compounds and their in-vivo performance, we employed in-silico pharmacokinetic predictions. Our in-silico predictions suggest that the plasma protein binding, low to moderate blood brain barrier penetration and low solubility are the main attributes of low in-vivo performance.


Assuntos
Anticonvulsivantes/farmacologia , Inibidores da Colinesterase/farmacologia , Convulsões/tratamento farmacológico , Tiofenos/farmacologia , Acetilcolinesterase/metabolismo , Animais , Anticonvulsivantes/síntese química , Anticonvulsivantes/química , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Diazepam , Relação Dose-Resposta a Droga , Electrophorus , Feminino , Cavalos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Estrutura Molecular , Pentilenotetrazol , Convulsões/induzido quimicamente , Relação Estrutura-Atividade , Tiofenos/síntese química , Tiofenos/química
12.
Molecules ; 24(14)2019 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-31319634

RESUMO

In the present study, 4-methylpyridin-2-amine was reacted with 3-bromothiophene-2-carbaldehyde and the Schiff base (E)-1-(3-bromothiophen-2-yl)-N-(4-methylpyridin-2-yl)methanimine was obtained in a 79% yield. Coupling of the Schiff base with aryl/het-aryl boronic acids under Suzuki coupling reaction conditions, using Pd(PPh3)4 as catalyst, yielded products with the hydrolysis of the imine linkages (5a-5k, 6a-6h) in good to moderate yields. To gain mechanistic insight into the transition metal-catalyzed hydrolysis of the compounds, density functional theory (DFT) calculations were performed. The theoretical calculations strongly supported the experiment and provided an insight into the transition metal-catalyzed hydrolysis of imines.


Assuntos
Iminas/química , Piridinas/química , Catálise , Hidrólise , Iminas/síntese química , Modelos Moleculares , Estrutura Molecular , Nitrogênio/química , Paládio/química , Piridinas/síntese química , Bases de Schiff/química
13.
Molecules ; 24(17)2019 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-31470508

RESUMO

Viola betonicifolia (Violaceae) is commonly recognized as "Banafsha" and widely distributed throughout the globe. This plant is of great interest because of its traditional, pharmacological uses. This review mainly emphases on morphology, nutritional composition, and several therapeutic uses, along with pharmacological properties of different parts of this multipurpose plant. Different vegetative parts of this plant (roots, leaves, petioles, and flowers) contained a good profile of essential micro- and macronutrients and are rich source of fat, protein, carbohydrates, and vitamin C. The plant is well known for its pharmacological properties, e.g., antioxidant, antihelminthic, antidepressant, anti-inflammatory, analgesic, and has been reported in the treatment of various neurological diseases. This plant is of high economic value. The plant has potential role in cosmetic industry. This review suggests that V. betonicifolia is a promising source of pharmaceutical agents. This plant is also of significance as ornamental plant, however further studies needed to explore its phytoconstituents and their pharmacological potential. Furthermore, clinical studies are needed to use this plant for benefits of human beings.


Assuntos
Analgésicos/química , Anti-Helmínticos/química , Anti-Inflamatórios/química , Antidepressivos/química , Antioxidantes/química , Fármacos Neuroprotetores/química , Viola/química , Analgésicos/isolamento & purificação , Analgésicos/farmacologia , Anti-Helmínticos/isolamento & purificação , Anti-Helmínticos/farmacologia , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antidepressivos/isolamento & purificação , Antidepressivos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Humanos , Micronutrientes/classificação , Micronutrientes/isolamento & purificação , Fármacos Neuroprotetores/isolamento & purificação , Fármacos Neuroprotetores/farmacologia , Nutrientes/classificação , Nutrientes/isolamento & purificação , Fitoterapia/métodos , Componentes Aéreos da Planta/anatomia & histologia , Componentes Aéreos da Planta/química , Extratos Vegetais/análise , Extratos Vegetais/química , Raízes de Plantas/anatomia & histologia , Raízes de Plantas/química , Plantas Medicinais , Viola/anatomia & histologia
14.
Microb Pathog ; 125: 366-384, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30287189

RESUMO

A novel approach was employed for the synthesis of un-doped tinoxide and Cobalt-doped tinoxide (Co-doped SnO2) nanoparticles (NAPs) by using aqueous extract of Clerodendrum inerme with the help of eco-friendly superficial solution combustion method. Synthesized NAPs were characterized by different spectroscopic techniques and results from XRD, TEM, SEM, EDX and UV-Vis examines confirmed the successful synthesis, crystalline nature and spherical structure of un-doped SnO2 and Co-doped SnO2 NAPs with the average grain size of 30 and 40 nm; and band gap energy of 3.68 and 2.76 eV respectively. Antimicrobial propensity of the synthesized NAPs was determined by agar well assay, SEM, TEM and confocal laser scanning microscopic analysis against various bacterial and fungal strains. Synthesized Co-doped SnO2 NAPs were unveiled the extraordinary antibacterial and antifungal activities against E. coli, B. subtilis, A. niger, A. flavus, and C. albicans with the zone of inhibitions of 30 ±â€¯0.08 mm and 26 ±â€¯0.06 mm, 17 ±â€¯0.04 mm, 23 ±â€¯0.08 mm and 26 ±â€¯0.06 respectively which were also evidenced from SEM, TEM and confocal laser scanning microscopy. In addition, green synthesized Co-doped SnO2 NAPs were demonstrated the substantial antioxidant activity by scavenging DPPH, significant in vitro anticancer and in vivo antitumor activity on breast carcinoma cells (MCF-7) and Ehrlich ascites tumor cell lines respectively than standard. The hemolytic activity disclosed low cytotoxicity of fabricated NAPs (0.89 ±â€¯0.05%) at 5 mg/mL, which was indicated their biocompatibility potential. Hence, the multi-purpose properties of synthesized NAPs presented in the current study can be further deliberated for pharmaceutical and nanomedicine applications.


Assuntos
Anti-Infecciosos/metabolismo , Antineoplásicos/metabolismo , Antioxidantes/metabolismo , Clerodendrum/metabolismo , Nanopartículas/metabolismo , Compostos de Estanho/metabolismo , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Compostos de Bifenilo/metabolismo , Neoplasias da Mama/tratamento farmacológico , Fungos/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Nanopartículas/química , Picratos/metabolismo , Análise Espectral , Compostos de Estanho/isolamento & purificação , Compostos de Estanho/farmacologia , Células Tumorais Cultivadas
15.
J Org Chem ; 81(16): 7308-13, 2016 08 19.
Artigo em Inglês | MEDLINE | ID: mdl-27336284

RESUMO

Iridium- and ruthenium-free approaches to protected allylic amines and alkyl nitriles under photoredox conditions are reported. An inexpensive organic dye, eosin Y, catalyzes coupling of Boc-protected potassium α-aminomethyltrifluoroborates with a variety of substituted alkenyl sulfones through an α-aminomethyl radical addition-elimination pathway. Allylic and homoallylic amines were formed in moderate yields with high E/Z selectivity. The mechanistic approach was extended using tosyl cyanide as a radical trap, enabling the conversion of alkyltrifluoroborates to nitriles via a Fukuzumi acridinium-catalyzed process.


Assuntos
Alcenos/química , Compostos de Boro/química , Cianetos/química , Luz , Compostos Orgânicos/química , Compostos de Potássio/química , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Catálise , Oxirredução , Espectroscopia de Prótons por Ressonância Magnética , Espectrometria de Massas por Ionização por Electrospray
16.
Tetrahedron Lett ; 56(49): 6839-6842, 2015 Dec 09.
Artigo em Inglês | MEDLINE | ID: mdl-26576065

RESUMO

A practical protocol for the synthesis of N-arylated methyl 2-aminothiophene-3-carboxylate has been developed via Chan-Lam cross-coupling. The desired products were synthesized by cross-coupling of methyl 2-aminothiophene-3-carboxylate with both arylboronic acids and potassium aryltrifluoroborate salts in moderate to good yields. A broad range of functional groups was well tolerated.

17.
Biol Res ; 47: 12, 2014 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-25052892

RESUMO

BACKGROUND: Current study has been designed to evaluate the chemical composition of essential and fixed oils from stem and leaves of Perovskia abrotanoides and antioxidant and antimicrobial activities of these oils. RESULTS: GC-MS analysis of essential oil identified 19 compounds with (E)-9-dodecenal being the major component in stem and hexadecanoic acid in leaves. In contrast, GC-MS analysis of fixed oil showed 40 constituents with α-amyrin the major component in stem and α-copaene in leaves. The antioxidant activity showed the highest value of 76.7% in essential oil from leaves in comparison with fixed oil from stem (45.9%) through inhibition of peroxidation in linoleic acid system. The antimicrobial assay tested on different microorganisms (e.g. E. coli, S. aureus, B. cereus, Nitrospira, S. epidermis, A. niger, A. flavus and C. albicans) showed the higher inhibition zone at essential oil from leaves (15.2 mm on B. cereus) as compared to fixed oil from stem (8.34 mm on S. aureus) and leaves (11.2 mm on S. aureus). CONCLUSIONS: The present study revealed the fact that essential oil analyzed from Perovskia abrotanoides stem and leaves could be a promising source of natural products with potential antioxidant and antimicrobial activities, as compared to fixed oil.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Lamiaceae/química , Folhas de Planta/química , Óleos de Plantas/farmacologia , Caules de Planta/química , Alcanos/análise , Alcanos/farmacologia , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Aspergillus/efeitos dos fármacos , Bacillus cereus/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Escherichia coli/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Peroxidação de Lipídeos/efeitos dos fármacos , Éteres Metílicos/análise , Éteres Metílicos/farmacologia , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/análise , Ácido Oleanólico/farmacologia , Ácido Palmítico/análise , Ácido Palmítico/farmacologia , Triterpenos Pentacíclicos/análise , Triterpenos Pentacíclicos/farmacologia , Óleos de Plantas/química , Substâncias Redutoras/análise , Sesquiterpenos/análise , Sesquiterpenos/farmacologia , Staphylococcus/efeitos dos fármacos , Ácidos Esteáricos/análise , Ácidos Esteáricos/farmacologia
18.
ScientificWorldJournal ; 2013: 489071, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23818824

RESUMO

The present study was designed to investigate the antioxidant potential and oil composition of Callistemon viminalis leaves. GC-MS analysis of the n-hexane extract revealed the presence of 40 compounds. Leaves contained appreciable levels of total phenolic contents (0.27-0.85 GAE mg/g) and total flavonoid contents (2.25-7.96 CE mg/g). DPPH radical scavenging IC50 and % inhibition of linoleic acid peroxidation were found to be in the ranges of 28.4-56.2 µg/ml and 40.1-70.2%, respectively. The haemolytic effect of the plant leaves was found in the range of 1.79-4.95%. The antioxidant activity of extracts was also studied using sunflower oil as an oxidative substrate and found that it stabilized the oil. The correlation between the results of different antioxidant assays and oxidation parameters of oil indicated that leaves' methanolic extract, exhibiting higher TPC and TFC and scavenging power, was also more potent for enhancing the oxidative stability of sunflower oil.


Assuntos
Antioxidantes/química , Myrtaceae/química , Extratos Vegetais/química , Folhas de Planta/química , Óleos de Plantas/análise , Óleos de Plantas/química , Extratos Vegetais/análise
19.
Molecules ; 18(3): 2663-82, 2013 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-23449066

RESUMO

Grewia asiatica L., is a species native to south Asia from Pakistan, east to Cambodia, cultivated primarily for its edible fruit and well-reputed for its diverse medicinal uses. Fruits are a rich source of nutrients such as proteins, amino acids, vitamins, and minerals and contain various bioactive compounds, like anthocyanins, tannins, phenolics and flavonoids. Different parts of this plant possess different pharmacological properties. Leaves have antimicrobial, anticancer, antiplatelet and antiemetic activities; fruit possess anticancer, antioxidant, radioprotective and antihyperglycemic properties; while stem bark possesses analgesic and anti-inflammatory activities. This review focuses on the botanical description, phytochemistry, nutritional studies and pharmacological properties of this plant.


Assuntos
Grewia/química , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/farmacologia , Análise de Alimentos , Frutas/química , Grewia/anatomia & histologia , Humanos , Fotoquímica , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia
20.
Int J Biol Macromol ; 230: 123161, 2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36610574

RESUMO

Cancer is a complicated, adaptable, and heterogeneous disease caused by a wide variety of genetic changes that might impair ability of cells to function normally. The majority of the tumors can only be shrunk using conventional oncology therapies like chemotherapy, radiation, and surgical resection, and the tumor often recurs. The inability of conventional cancer therapies to completely destroy the Cancer Stem Cells (CSCs) that otherwise lead to therapy resistance is thus addressed by therapeutic approaches that concentrate on targeting CSCs and their micro-environmental niche. In this review, we summarize approaches that are used for the development of fusion proteins and their therapeutic applications for treating cancer. The main purpose of making advancements towards the fusion technology instead of using conventional treatment methods is to achieve a prolonged half-life of the therapeutic drugs. The fusion of drugs to the immune response enhancing cytokines or the fusion of antibody and cytokines not only increases half-life but also increase the stability of the anti-tumor drug. Several molecules including different fragments of antibodies, cytokines, Human Serum Albumin, transferrin, XTEN polymers, Elastin-like polypeptides (ELPs) can be employed as a fusion partner and the resulting fusion proteins are reported to show enhanced anti-tumor response.


Assuntos
Antineoplásicos , Neoplasias , Humanos , Peptídeos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Antineoplásicos/química , Polímeros/química , Neoplasias/tratamento farmacológico , Tecnologia , Citocinas
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