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1.
Molecules ; 27(6)2022 Mar 16.
Artigo em Inglês | MEDLINE | ID: mdl-35335292

RESUMO

The genus Bidens a member of family Compositae, is widely documented as an ethno-medicinally important genus of plants. In the present study, anticancer potential of three ethno-medicinally important species i.e., B. bipinnata, B. biternata and B. pilosa were tested. For in-vitro evaluation, an MTT (Thiazolyl blue tetrazolium bromide) assay was performed against cervical cancer cells (HeLa), hepatocellular carcinoma (HepG), and adenocarcinoma human alveolar basal epithelial cells (A549). For in vivo evaluation, Artemia salina, Danio rerio, and Caenorhabditis elegans were used. Among all the tested extracts, the ethanol extract of B. biternata appeared to have highest anticancer activity, and the compounds responsible for this activity were identified to be Tris (2,4-di-tert-butylphenyl), 4-hydroxy-2,4'-dimethoxychalcone, and 2,4-di-tert-butylphenol. This is the first report of the isolation of Tris (2,4-di-tert-butylphenyl) phosphate from the genus Bidens and the first report of 4-hydroxy-2,4'-dimethoxychalcone and 2,4-di-tert-butylphenol from B. biternata. Among the isolated compounds, 4-hydroxy-2,4'-dimethoxychalcone showed the highest anticancer activity with an LD50 value of 236.7 µg/mL. Therefore, this compound carries promising potential for being established as a pharmaceutical for chemoprevention and chemotherapy.


Assuntos
Extratos Vegetais , Plantas , Cromatografia Líquida de Alta Pressão , Cromatografia Gasosa-Espectrometria de Massas , Células HeLa , Humanos
2.
Molecules ; 27(22)2022 Nov 16.
Artigo em Inglês | MEDLINE | ID: mdl-36432033

RESUMO

Medicinal plants play important role in the public health sector worldwide. Natural products from medicinal plants are sources of unlimited opportunities for new drug leads because of their unique chemical diversity. Researchers have focused on exploring herbal products as potential sources for the treatment of cancer, cardiac and infectious diseases. Arisaema flavum (Forssk.) is an important medicinal plant found in the northwest Himalayan regions of Pakistan. It is a poisonous plant and is used as a remedy against snake bites and scorpion stings. In this study, two bioactive compounds were isolated from Arisaema flavum (Forssk.) and their anticancer activity was evaluated against human breast cancer cell line MCF-7 using an MTT assay. The crude extract of Arisaema flavum (Forssk.) was subjected to fractionation using different organic solvents in increasing order of polarity. The fraction indicating maximum activity was then taken for isolation of bioactive compounds using various chromatographic and spectroscopic techniques such as column chromatography, thin-layer chromatography (TLC), gas chromatography−mass spectrometry (GC-MS), Fourier transform infrared spectroscopy (FTIR) and nuclear magnetic resonance spectroscopy (NMR). Crude extract of Arisaema flavum (Forssk.), as well as various fractions extracted in different solvents such as n-hexane, chloroform and ethyl acetate, were tested against human breast cancer cell line MCF-7 using an MTT assay. The crude extract exhibited significant dose-dependent anticancer activity with a maximum activity of 78.6% at 500 µg/mL concentration. Two compounds, hexadecanoic acid ethyl ester with molecular formula C18H36O7 and molar mass 284 and 5-Oxo-19 propyl-docosanoic acid methyl ester with molecular formula C26H50O3 and molecular mass 410, were isolated from chloroform fraction. These compounds were tested against the MCF-7cell line for cytotoxic activity and exhibited a significant (p < 0.00l) decrease in cell numbers for MCF-7 cells with IC50 of 25 µM after 48 h of treatment. Results indicated that Arisaema flavum (Forssk.) possesses compounds with cytotoxic activity that can further be exploited to develop anticancer formulations.


Assuntos
Antineoplásicos , Arisaema , Neoplasias da Mama , Plantas Medicinais , Humanos , Feminino , Extratos Vegetais/química , Clorofórmio , Plantas Medicinais/química , Cromatografia em Camada Fina , Antineoplásicos/farmacologia , Solventes , Ésteres
3.
Molecules ; 26(19)2021 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-34641363

RESUMO

Gui Zhen Cao is an herbal formulation that has been documented in Chinese traditional medicine as a remedy for diarrhea, dysentery, inflammation, and toxicity. The sources of this formulation (Bidens pilosa L., Bidens biternata (Lour.) Merr. & Sherff, Bidens bipinnata L.) are also listed in ethnomedicinal reports all over the world. In this study, all these plants are tested for in vitro anticandida activity. A quantitative evaluation of the phytochemicals in all these plants indicated that their vegetative parts are rich in tannins, saponins, oxalates, cyanogenic glycoside and lipids; moreover, the roots have high percentages of alkaloids, flavonoids, and phenols. The results indicated significant anticandida activity, especially for the hexane extract of B. bipinnata leaves which inhibited C. albicans (42.54%), C. glabrata (46.98%), C. tropicalis (50.89%), C. krusei (40.56%), and C. orthopsilosis (50.24%). The extract was subjected to silica gel chromatography and 220 fractions were obtained. Purification by High Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD) and Gas Chromatography tandem Mass Spectrometry (GC-MS/MS) analysis led to the identification of two anticandida compounds: dehydroabietic and linoleic acid having an inhibition of 85 and 92%, respectively.


Assuntos
Bidens/química , Candida/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Flavonoides/farmacologia , Cromatografia Gasosa-Espectrometria de Massas/métodos , Extratos Vegetais/farmacologia , Candida/crescimento & desenvolvimento , Espectrometria de Massas em Tandem/métodos
4.
Pak J Pharm Sci ; 32(4): 1687-1695, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31608891

RESUMO

Peel, pulp and kernel extracts of seven mango fruit (varieties) were analyzedsubjected for antibacterial and antioxidative potential. Langra peel showed good activity against B. subtilis, S. aureus and E. aerogenes. Good zone of inhibition by chaunsa kernel (28mm) and pulp (22mm) against Streptomyces stipulate its potential as anticarcinogencancerous. Dosehri and almashil pulp and sindhri peel asserted free radical scavenger (upto 79%) determined through DPPH assay. The peel and kernel of almashil contained maximum (total) flavonoids contents (58 & 43µgQE/100mg, respectively) while; total phenolics were higher in kernel of sindhri, chaunsa, langra and hujra and almashil pulp. Reducing power potential demonstrated variation from 300 to 554µgAAE/100mg. Total antioxidant potential was maximum in hujra pulp (512µg AAE/100mg). Concluded This study concludes that mango has vast beneficial potential for prone to human health and may also be used for isolation of antioxidative and antimicrobial as well as a protein kinase inhibition agent.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Mangifera/química , Inibidores de Proteínas Quinases/farmacologia , Antibacterianos/química , Antioxidantes/química , Compostos de Bifenilo , Avaliação Pré-Clínica de Medicamentos , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Frutas/química , Testes de Sensibilidade Microbiana , Paquistão , Fenóis/análise , Picratos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Inibidores de Proteínas Quinases/química , Sementes/química , Especificidade da Espécie , Streptomyces/efeitos dos fármacos
5.
Nanomedicine (Lond) ; 19(10): 875-893, 2024 04.
Artigo em Inglês | MEDLINE | ID: mdl-38530883

RESUMO

Aim: To develop a biocompatible conjugated ciprofloxacin-PEG-FeO nanodelivery system with increased efficacy of available therapeutics in a controlled manner. Materials & methods: FeO nanoparticles were synthesized by chemical and biological methods and modified as ciprofloxacin-PEG-FeO nanoformulations. After initial antibacterial and cytotoxicity studies, the effective and biocompatible nanoformulations was further fabricated as nanotherapeutics for in vivo studies in mouse models. Results: Chemically synthesized ciprofloxacin-PEG-FeO nanoformulations demonstrated boosted antibacterial activity against clinically isolated bacterial strains. Nanoformulations were also found to be compatible with baby hamster kidney 21 cells and red blood cells. In in vivo studies, nanotherapeutic showed wound-healing effects with eradication of Staphylococcus aureus infection. Conclusion: The investigations indicate that the developed nanotherapeutic can eradicate localized infections and enhance wound healing with controlled cytotoxicity.


Assuntos
Antineoplásicos , Nanopartículas , Infecções Estafilocócicas , Cricetinae , Animais , Camundongos , Ciprofloxacina/farmacologia , Ciprofloxacina/uso terapêutico , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Infecções Estafilocócicas/tratamento farmacológico , Antineoplásicos/uso terapêutico
6.
Sci Rep ; 14(1): 4689, 2024 02 26.
Artigo em Inglês | MEDLINE | ID: mdl-38409460

RESUMO

Antimicrobial resistance is a worldwide health problem that demands alternative antibacterial strategies. Modified nano-composites can be an effective strategy as compared to traditional medicine. The current study was designed to develop a biocompatible nano-drug delivery system with increased efficacy of current therapeutics for biomedical applications. Zinc oxide nanoparticles (ZnO-NPs) were synthesized by chemical and green methods by mediating with Moringa olifera root extract. The ZnO-NPs were further modified by drug conjugation and coating with PEG (CIP-PEG-ZnO-NPs) to enhance their therapeutic potential. PEGylated ZnO-ciprofloxacin nano-conjugates were characterized by Fourier Transform Infrared spectroscopy, X-ray diffractometry, and Scanning Electron Microscopy. During antibacterial screenings chemically and green synthesized CIP-PEG-ZnO-NPs revealed significant activity against clinically isolated Gram-positive and Gram-negative bacterial strains. The sustainable and prolonged release of antibiotics was noted from the CIP-PEG conjugated ZnO-NPs. The synthesized nanoparticles were found compatible with RBCs and Baby hamster kidney cell lines (BHK21) during hemolytic and MTT assays respectively. Based on initial findings a broad-spectrum nano-material was developed and tested for biomedical applications that eradicated Staphylococcus aureus from the infectious site and showed wound-healing effects during in vivo applications. ZnO-based nano-drug carrier can offer targeted drug delivery, and improved drug stability and efficacy resulting in better drug penetration.


Assuntos
Nanopartículas Metálicas , Nanopartículas , Óxido de Zinco , Ciprofloxacina/farmacologia , Óxido de Zinco/química , Nanopartículas Metálicas/química , Antibacterianos/farmacologia , Antibacterianos/química , Nanopartículas/química , Microscopia Eletrônica de Varredura , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Espectroscopia de Infravermelho com Transformada de Fourier , Testes de Sensibilidade Microbiana
7.
PLoS One ; 19(8): e0308761, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39133684

RESUMO

This study was conducted to investigate the effects of selenium nanoparticle (Se-NP) supplementation on the growth performance, carcass composition, antioxidant status, hepatic enzyme activities, and immunity of Cirrhinus mrigala. For this purpose, fish with an average initial weight of 7.44 ± 0.04 g were fed five experimental diets containing 0 (control), 0.25, 0.5, 1, and 2 mg kg-1 Se-NPs diets for 90 days. The analysed selenium (Se) contents of the diets were 0.35, 0.64, 0.92, 1.43, and 2.39 mg kg-1. Twenty five fish were randomly distributed in each of 5 aquarium (36 × 23.7 × 24.3 inches) in triplicate. The results showed that supplementation with Se up to 0.92 mg/kg significantly increased (p<0.05) weight gain, weight gain% (WG%), and specific growth rate (SGR) by 34%, 33%, and 16%, respectively, compared to the control diet. Dietary Se concentrations up to 0.92 mg/kg significantly increased the crude protein and crude fat and reduced (p<0.05) the moisture content as compared to the control group. Fish fed 0.92 mg kg-1 Se had significantly lower malondialdehyde (MDA) contents and higher activities of catalase, superoxide dismutase, and glutathione peroxidase in liver and serum as compared to other experimental diets. Moreover, a significant increase (p<0.05) in the level of serum immunoglobulin and lysozyme (LYZ) activity was recorded in fish fed 0.92 mg/kg Se diet. Moreover, the highest (p<0.05) values of aspartate transaminase (AST) and alanine transaminase (ALT) were recorded in fish fed 2.39 mg/kg Se level. However, serum alkaline phosphatase (ALP) activity remained unaffected by dietary treatment. Broken-line regression analysis indicated that 0.83 mg/kg Se is required for the optimum growth performance of C. mrigala.


Assuntos
Antioxidantes , Suplementos Nutricionais , Fígado , Selênio , Animais , Selênio/farmacologia , Fígado/efeitos dos fármacos , Fígado/metabolismo , Antioxidantes/metabolismo , Nanopartículas , Ração Animal/análise , Dieta/veterinária , Carpas/crescimento & desenvolvimento , Carpas/metabolismo , Carpas/imunologia
8.
Sci Rep ; 14(1): 21246, 2024 09 11.
Artigo em Inglês | MEDLINE | ID: mdl-39261712

RESUMO

Antibacterial resistance requires an advanced strategy to increase the efficacy of current therapeutics in addition to the synthesis of new generations of antibiotics. In this study, copper oxide nanoparticles (CuO-NPs) were green synthesized using Moringa oleifera root extract. CuO-NPs fabricated into a form of aspartic acid-ciprofloxacin-polyethylene glycol coated copper oxide-nanotherapeutics (CIP-PEG-CuO) to improve the antibacterial activity of NPs and the efficacy of the drug with controlled cytotoxicity. These NPs were charachterized by Fourier transform infrared spectroscopy (FTIR), x-rays diffraction spectroscopy (XRD), scanning electron microscopy (SEM) and energy-dispersive spectroscopy (EDS). Antibacterial screening and bacterial chemotaxis investigations demonstrated that CIP-PEG-CuO NPs show enhanced antibacterial potential against Gram-positive and Gram-negative clinically isolated pathogenic bacterial strains as compared to CuO-NPs. In ex-vivo cytotoxicity CIP-PEG-CuO-nano-formulates revealed 88% viability of Baby Hamster Kidney 21 cell lines and 90% RBCs remained intact with nano-formulations during hemolysis assay. An in-vivo studies on animal models show that Staphylococcus aureus were eradicated by this newly developed formulate from the infected skin and showed wound-healing properties. By using specially designed nanoparticles that are engineered to precisely transport antimicrobial agents, these efficient nano-drug delivery systems can target localized infections, ensure targeted delivery, enhance efficacy through increased drug penetration through physical barriers, and reduce systemic side effects for more effective treatment.


Assuntos
Antibacterianos , Ciprofloxacina , Cobre , Polietilenoglicóis , Staphylococcus aureus , Cobre/química , Cobre/farmacologia , Polietilenoglicóis/química , Antibacterianos/farmacologia , Antibacterianos/química , Staphylococcus aureus/efeitos dos fármacos , Animais , Ciprofloxacina/farmacologia , Ciprofloxacina/química , Química Verde , Testes de Sensibilidade Microbiana , Nanopartículas Metálicas/química , Linhagem Celular , Infecções Estafilocócicas/tratamento farmacológico , Moringa oleifera/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Nanopartículas/química , Cricetinae
9.
J Microbiol Biotechnol ; 34(7): 1452-1463, 2024 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-38858094

RESUMO

Fungi generate different metabolites some of which are intrinsically bioactive and could therefore serve as templates for drug development. In the current study, six endophytic fungi namely Aspergillus flavus, Aspergillus tubigenesis, Aspergillus oryzae, Penicillium oxalicum, Aspergillus niger, and Aspergillus brasiliensis were isolated and identified from the medicinal plant, Silybum marianum. These endophytic fungi were identified through intra transcribed sequence (ITS) gene sequencing. The bioactive potentials of fungal extracts were investigated using several bioassays such as antibacterial activity by well-diffusion, MIC, MBC, anti-biofilm, antioxidant, and haemolysis. The Pseudomonas aeruginosa PAO1 was used to determine the antibiofilm activity. The ethyl acetate extract of Aspergillus flavus showed strong to moderate efficacy against Staphylococcus aureus, Escherichia coli, P. aeruginosa, and Bacillus spizizenii. Aspergillus flavus and Aspergillus brasiliensis exhibited significant antibiofilm activity with IC50 at 4.02 and 3.63 mg/ml, while A. flavus exhibited maximum antioxidant activity of 50.8%. Based on HPLC, LC-MS, and NMR experiments kojic acid (1) and carbamic acid (methylene-4, 1-phenylene) bis-dimethyl ester (2) were identified from A. flavus. Kojic acid exhibited DPPH free radical scavenging activity with an IC50 value of 99.3 µg/ml and moderate activity against ovarian teratocarcinoma (CH1), colon carcinoma (SW480), and non-small cell lung cancer (A549) cell lines. These findings suggest that endophytic fungi are able to produce promising bioactive compounds which deserve further investigation.


Assuntos
Antibacterianos , Antineoplásicos , Antioxidantes , Aspergillus , Endófitos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Endófitos/química , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antineoplásicos/farmacologia , Antineoplásicos/química , Humanos , Cromatografia Líquida de Alta Pressão , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Aspergillus/química , Linhagem Celular Tumoral , Biofilmes/efeitos dos fármacos , Fungos/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Aspergillus flavus/efeitos dos fármacos
10.
Pak J Pharm Sci ; 26(5): 1009-12, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24035960

RESUMO

This study was aimed to determine the effectiveness of two ethnobotanically important plant species Carissa opaca and Toona ciliata against cancer cells. Antiproliferative activity of the plant extracts and their fractions was tested against MCF-7 breast cancer cell line using MTT assay. A concentration dependent inhibition was observed for both crude extracts. C. opaca crude extract showed 78.5% inhibition while T. ciliata showed 57% activity against cancer cells at 500 µg/mL. Fractions were tested at 200 µg/mL concentration and were more active than crude extracts. Chloroform fraction of C. opaca showed maximum inhibition 99% followed by ethyl acetate and methanol fraction of C. opaca exhibiting 96% and 94% inhibition, respectively. Ethyl acetate fraction of T. ciliata showed 78% inhibition of cancer cells at the same concentration. Preliminary phytochemical screening revealed the chemical composition of C. opaca extract containing alkaloids, flavonoids, tannins and saponins while T. ciliata had tannins and coumarins. Present investigation suggests that tested plant species possess potent anticancer compounds specially chloroform, ethyl acetate and methanol fractions of C. opaca and ethyl acetate fraction of T. ciliata can be an important source of anticancer drugs.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apocynaceae , Neoplasias da Mama/patologia , Proliferação de Células/efeitos dos fármacos , Meliaceae , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Apocynaceae/química , Relação Dose-Resposta a Droga , Feminino , Humanos , Células MCF-7 , Meliaceae/química , Fitoterapia , Plantas Medicinais , Solventes/química
11.
PLoS One ; 18(4): e0284285, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37104295

RESUMO

The aim of the current study was to evaluate the toxic effect of silver nanoparticles (Ag-NPs) on biochemical biomarkers, immune responses, and the curative potential effects of vitamin C and E on grass carp. Fish (n = 420) with an average initial body weight of 8.045 ± 0.13 g were shifted to glass aquaria (36 x 18 x 18 inches, filled with 160-L tap water) in triplicates. Aquaria were randomly designated as A, B, C, D with alone Ag-NPs (Control (0), 0.25, 0.50, 0.75 mg/L) and E, F, G with Ag-NPs + Vit. C + Vit. E (0.25+0.25+0.25, 0.50+0.50+0.50, 0.75+0.75+0.75 mg/L). NPs particles were administrated viz, oral and intravenous routes for 7 days. The results indicated that both routes had non-significant effect, but levels of Ag-NPs had significant effect. Treatments C, D and G showed significant decrease in levels of RBC, HGB and HCT except for WBC and NEUT levels, which significantly increased. ALT, ALP, AST, urea, and creatinine showed significant increase in activity in the C, D, and G groups. CAT, SOD decreased significantly in all Ag-NPs alone groups, while significantly increased with vitamin E and C. LYZ, TP, ALB, GLB showed significant low activity in the B, C, and D groups while significantly high activity in the E, F, and G groups. Cortisol, glucose and triglycerides showed significant increase in the B, C, and D groups, while E, F, and G groups showed significant low levels of triglycerides, COR, and GLU. Cholesterol level was same across all treatment groups. In conclusion, vitamin E and C as powerful antioxidants protect the fish against Ag-NPs except high dose level of 0.75mg/L, while 0.25mg/L of Ag-NPs was presumably safe for C. idella.


Assuntos
Carpas , Nanopartículas Metálicas , Animais , Antioxidantes , Nanopartículas Metálicas/toxicidade , Prata/toxicidade , Vitamina E/farmacologia
12.
Pak J Pharm Sci ; 25(1): 183-7, 2012 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-22186328

RESUMO

Aesculus indica (Linn.) (Sapindaceae) is an ethanobotanically important plant specie traditionally used against rheumatism, skin and vein complaints. Cytotoxic potential of Aesculus indica crude leaf extract and its fractions was investigated against MCF-7 cell line. Crude extract of Aesculus indica was prepared in methanol by maceration technique. Crude extract was fractionated into four organic and one aqueous fraction on polarity basis. MTT assay was used to evaluate the reduction of viability of MCF-7 breast cancer cell line. Cell viability was inhibited by Aesculus indica crude extract in a dose dependent manner ranging from 34.2% at 10 µg/ml to 94% at 500µg/ml. Activity was found in an ascending order from hexane showing 29.8% inhibition to aqueous fraction indicating maximum inhibition, 60%. Phytochemical analysis of crude and fractionated extracts revealed presence of flavonoids, saponins, coumarins and tannins upto varying degrees. Methanol and aqueous fraction of methanol extract of Aesculus indica can be good source of cytotoxic compounds.


Assuntos
Adenocarcinoma/tratamento farmacológico , Aesculus/química , Neoplasias da Mama/tratamento farmacológico , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Fracionamento Químico/métodos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Ensaios de Seleção de Medicamentos Antitumorais/estatística & dados numéricos , Feminino , Humanos , Extratos Vegetais/farmacologia , Folhas de Planta/química
13.
J Biomol Struct Dyn ; 40(13): 5748-5758, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-33446058

RESUMO

The COVID-19 being a preconized global pandemic by the World Health Organization needs persuasive immediate research for possible medications. The present study was carried out with a specific aim to computationally evaluate and identify compounds derived from Bacillus species as the plausible inhibitors against 3-chymotrypsin-like main protease (3CLpro) or main protease (MPro), which is a key enzyme in the life-cycle of coronavirus. The compounds were isolated from the crude extracts of Bacillus species. Among the isolated compounds, novel inhibitory leads were identified using in silico techniques. Molecular docking revealed that stigmasterol (-8.3 kcal/mol), chondrillasterol (-7.9 kcal/mol) and hexadecnoic acid (-6.9 kcal/mol)) among others bind in the substrate-binding pocket and also interacted with the catalytic dyad of the 3-CLpro. Further evaluation using 50 ns molecular dynamic simulation and MMPB-GBSA indicated that among the top three docking hits, hexadecanoic acid was found to be the most promising anti-COVID-19 lead against the main protease. Hexadecanoic acid might serve as a potent anti-SARS-CoV-2 compound to combat COVID-19, however, in vitro and in vivo validation and optimization is needed.Communicated by Ramaswamy H. Sarma.


Assuntos
Bacillus , Tratamento Farmacológico da COVID-19 , Bacillus/metabolismo , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Ácido Palmítico , Inibidores de Proteases/química , Inibidores de Proteases/farmacologia
14.
Saudi J Biol Sci ; 29(2): 1191-1196, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35197786

RESUMO

Xanthones C-glycosides are plants secondary metabolites with diverse biological activities. Among the C-glycoside xanthones, the mangiferin (MF) is of widespread occurrence in plants while isomangiferin (IsoMF) is not very common. For the present study mangiferin (MF) and isomangiferin (IsoMF) were isolated from Dryopteris ramosa. The antibacterial potential of MF and IsoMF was evaluated by using agar well diffusion method while cytotoxic properties of MF and IsoMF were assessed by brine shrimp lethality test (BSLT). The antibacterial potential of MF and IsoMF increases in dose dependent manner. The minimum inhibitory concentration (MIC) indicated strong antibacterial potential of MF against Salmonella setubal (125 µg/mL) and Bacillus subtilis (125 µg/mL) while MF showed weak antibacterial potential against Escherichia coli (500 µg/mL). On the other hand the IsoMF showed better antibacterial potential against all the tested strain including Escherichia coli (MIC = 250 µg/mL). The MF and IsoMF showed poor cytotoxicity towards Brine shrimp nauplii as indicated by their LD50 (969.77 ± 0.67 and 768.92 ± 0.81 µg/mL respectively). The present study has highlighted the antibacterial potential of MF and IsoMF. Further evaluation of these two isomeric compounds may prove to be the future remedies for various bacterial infections and other human ailments.

15.
Antibiotics (Basel) ; 11(3)2022 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-35326886

RESUMO

At the request of Dr. Markus Bacher, Dr. Johann Schinnerl, and Dr. Karin Valant-Vetschera, they have been removed as authors of the paper [...].

16.
Sci Rep ; 12(1): 4061, 2022 03 08.
Artigo em Inglês | MEDLINE | ID: mdl-35260726

RESUMO

Porous silica particles were prepared by sol-gel method with some modification to get wide-pore particles. These particles were derivatized with N-phenylmaleimide-methylvinylisocyanate (PMI) and styrene by reversible addition fragmentation chain transfer (RAFT) polymerization to prepare N-phenylmaleimide embedded polystyrene (PMP) stationary phases. Narrow bore stainless steel column (100 × 1.8 mm i.d) was packed by slurry packing method. The chromatographic performance of PMP column was evaluated for the separation of synthetic peptides mixture composed of five peptides (Gly-Tyr, Gly-Leu-Tyr, Gly-Gly-Tyr-Arg, Tyr-Ile-Gly-Ser-Arg, Leucine enkephalin) and tryptic digest of human serum albumin (HAS) respectively. Number of theoretical plates as high as 280,000 plates/m were obtained for peptides mixture at optimum elution condition. Separation performance of the developed column was compared with commercial Ascentis Express RP-Amide column and it was observed that separation performance of PMP column was better than commercial column in terms of separation efficiency and resolution.


Assuntos
Peptídeos , Proteínas , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Peptídeos/química , Poliestirenos/química , Dióxido de Silício/química
17.
Saudi J Biol Sci ; 29(2): 1185-1190, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35197785

RESUMO

Medicinal plants have significant contribution in pharmaceutical industries being producers of compounds utilized as precursors for drug development. A plant of Lamiaceae family; Pseudocaryopteris foetida had not been investigated for its biomedical potential. Current research was aimed to investigate phytochemical analysis, cytotoxic potential and antioxidant activity of crude methanolic extract and fractions of Pseudocaryopteris foetida (leaves). The preliminary phytochemical analysis of crude methanolic extracts and fractions of Pseudocaryopteris foetida revealed that plant is rich in phenolic and flavonoid classes of secondary metabolites while presence of tannin was observed only in crude methanolic extract. The cytotoxicity was determined using brine shrimp lethality test. Different concentrations (25, 50, 100, 150, 200 and 250 µg/mL) of crude methanolic extract and fractions exhibited dose dependent cytotoxicity. However, The LD50 for all the extracts was more than 200 µg/mL indicating weak cytotoxic potential of Pseudocaryopteris foetida. The antioxidant capabilities of crude methanolic extract and fraction of Pseudocaryopteris foetida were analyzed by in vitro bio assays including DPPH, ABTS, Reducing power and phosphomolybdate antioxidant assays using ascorbic acid as standard. The crude methanolic extract showed IC50 (256.38 ± 0.6 and 314.95 ± 1.1 µg/mL) for DPPH and ABTS respectively, while total antioxidant capacity was calculated as 55.79 ± 0.5 µg/mL for crude methanolic extract of Pseudocaryopteris foetida while ascorbic acid indicated total antioxidant capacity of 71.89 ± 2.3 µg/mL. Study concluded that leaves of Pseudocaryopteris foetida were the rich source of antioxidant phytochemicals. Based on preliminary investigations further research should be focused to isolate bioactive phytochemicals as leading source of clinical medicines in future.

18.
Saudi J Biol Sci ; 29(1): 88-95, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-35002397

RESUMO

Citrus black rot disease being caused by Alternaria citri is a major disease of citrus plants with 30-35% economic loss annually. Fungicides had not been effective in the control of this disease during last few decades. In the present study, antifungal role of green synthesized zinc oxide (ZnO) and copper oxide (CuO) nanoparticles (NPs) were studied against Alternaria citri. Alternaria citri was isolated from disease fruits samples and was identified by staining with lacto phenol cotton blue. Furthermore, CuO and ZnO NPs were synthesized by utilizing the lemon peels extract as the reducing and capping agent. Nanoparticles were characterized by X-ray diffraction (XRD) and scanning electron microscopy (SEM) techniques. From the XRD data, the calculated size of CuO NPs was to be 18 nm and ZnO NPs was16.8 nm using Scherrer equation. The SEM analyses revealed the surface morphology of all the metal oxide NPs synthesized were rounded, elongated and or spherical in the shape. The zone of inhibition was observed to be 50 ± 0.5 mm by CuO NPs, followed by 51.5 ± 0.5 mm by ZnO NPs and maximum zone of antifungal inhibition was observed to be 53 ± 0.6 mm by mix metal oxide NPs. The results of minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of the synthesized nanoparticles showed that at the certain concentrations (80 mg ml-1), these NPs were capable of inhibiting the fungal growth, whereas above that specified concentrations (100 mg ml-1), NPs completely inhibited the fungal growth. Based on these findings, the green synthesized NPs can be used as alternative to fungicide in order to control the citrus black rot disease.

19.
Saudi J Biol Sci ; 29(1): 287-295, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-35002421

RESUMO

Endophytes are microorganisms residing within plant tissues. Bacterial endophytes are important sources for production of pharmaceutically important metabolites. Berberis lycium is an important medicinal plant and there exist no report regarding isolation and determination of bioactive potential of its bacterial endophytes. Therefore the present study was aimed to isolate and identify bacterial endophytes from Berberis lycium. The study resulted in isolation of 20 strains of bacterial endophytes. Based on their antibacterial activity three strains were identified as Bacillus cereus (LBL6), Bacillus thuringiensis (SBL3) and Bacillus anthracis (SBL4) on basis of 16SrRNA gene using universal primers. Crude ethyl acetate extracts of LBL6, SBL3 and SBL4 were further evaluated for antioxidant and antifungal activities. Moderate antioxidant activity (56 %) at a concentration of 1000 µg/mL was observed for LBL6 followed by 45 and 43 % activity by SBL4 and SBL3 respectively. Significant antifungal activity was observed against Aspergillus niger (60 %) and Aspergillus flavus (56 %) at concentration of 4 mg/mL of SBL3 and SBL4 respectively. GCMS analysis of extract (LBL6) exhibited presence of 12 bioactive secondary metabolites corresponding to antimicrobial, antifungal, antioxidant, antitumor and anticancer activities. In conclusion, present study highlighted the importance of Berberis lycium to host diverse bacterial endophytes of pharmaceutical importance.

20.
Saudi J Biol Sci ; 29(2): 941-954, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35197762

RESUMO

Salmonella enterica serovar Typhi is Gram negative, rod shaped, facultative anaerobic bacterium, belongs to enterobacteriaceae family that causes typhoid fever in humans. This bacterium has become a super bug due to acquisition of multi drug resistance. Bacteria is transmitted through food and water contaminated with human feaces. Present study reports the screening of Adhatoda vasica, Amaranthus hybridus and Aloe barbadensis and their evaluation against multi-drug resistant Salmonella enterica serovar Typhi. Qualitative analysis of ten phytochemicals was conducted using chemical method and Gas Chromatography-Mass Spectrometry (GCMS). Antibacterial activity of plants was carried out by agar well diffusion method on Mueller Hinton agar. Total tannins, total alkaloids and total flavonoids of different parts of three plants were estimated through spectrophotometer. Total tannins content in different parts of plants was present in the given order Amaranthus hybridus leaf > Aloe barbadensis leaf > Adhatoda vasica leaf > Adhatoda vasica flower > Adhatoda vasica stem. Whereas, the order of total flavonoid concentration was Amaranthus hybridus leaf > Aloe barbadensis leaf > Adhatoda vasica leaf > Amaranthus hybridus seed. Total alkaloids have order, Adhatoda vasica leaf > Amaranthus hybridus leaf > Adhatoda vasica flower > Amaranthus hybridus seed > Aloe barbadensis leaf. Results of phytochemical analysis suggested that plants have strong profile of antioxidants, total phenolic contents and various enzymes proposing them best alternate to cure bacterial infections. GC-MS analysis further confirmed stronger phytochemical profile that can be utilized as antagonists to Salmonella enterica serovar Typhi.

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