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1.
J Environ Sci Health B ; 55(4): 396-405, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31905102

RESUMO

Bentazone is one of the toxic insecticides used to control forest tent caterpillar moths, boll weevils, gypsy moths, and other types of moths in various field crops. We report the efficacy of biochar prepared from the Azardirachta Indica waste biomass as adsorbent for removal of Bentazone. Biochar material was prepared by pyrolysis process under limited oxygen conditions. Biochar material was characterized by proximate and ultimate analysis, SEM analysis, FTIR analysis and TG/DTA analyses. The Bentazone adsorption capacity by biochar from aqueous solutions was assessed. Effect of time, adsorbent dosage, insecticide concentration and pH on the adsorption characteristics of the biochar were evaluated. Adsorption parameters were obtained at equilibrium contact time of 150 min, with biochar dosage of 0.5 g at pH 8. From the optimization studies, desirability of 0.952 was obtained with response (adsorption uptake) of 79.40 mg/g, for initial concentration of insecticide (50 mg/L), adsorbent dosage (0.448 g), time 30.0 min and pH 2. The adsorption isotherm data for the removal of Bentazone fitted well with the Freundlich isotherm. This study indicates that the biochar produced from the bark of Azardirachta Indica biomass could be employed as a potential adsorbent for removal of synthetic organic pollutants from the water streams.


Assuntos
Benzotiadiazinas/isolamento & purificação , Carvão Vegetal/química , Poluentes Químicos da Água/isolamento & purificação , Adsorção , Azadirachta/química , Benzotiadiazinas/química , Biomassa , Concentração de Íons de Hidrogênio , Inseticidas/química , Inseticidas/isolamento & purificação , Cinética , Casca de Planta/química , Espectroscopia de Infravermelho com Transformada de Fourier , Poluentes Químicos da Água/química , Purificação da Água
2.
J Sci Food Agric ; 100(4): 1541-1546, 2020 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-31769025

RESUMO

BACKGROUND: Citrus sinensis, Allium sativum, Ocimum basilicum, Mentha spicata, Curcuma longa, Carica papaya, Andrographis paniculata, Azadirachta indica, Cymbopogon citratus and Acorus calamus were compared in the form of extracts of chloroform, hexane and aqueous media for their effectiveness in repelling Tribolium castaneum. Filter paper of 9 cm in diameter was cut into halves. Using a micro-pipette, each extract was applied to one half of the filter paper. The volume applied was kept constant at 0.6 mL per 30 cm2 . The filter paper was dried and reattached leaving a 0.5 cm gap between, in a Petri-plate. Ten adults of T. castaneum were introduced and the repellency was observed after 30, 60 and 180 min. RESULTS: The aqueous extract of C. papaya exhibited the highest repellency (82-97%) followed by that of garlic bulbs (aqueous extract) with 86.67% repellency. Further, gunny bags were sprayed separately using bottle sprayers with the two most effective extracts at a constant volume of 42 mL per 575 cm2 . These treated gunny bags were compared with malathion-treated gunny bags in the insect management unit. The observations were taken after 2, 8 and 24 h. Papaya leaf extract-treated gunny bags showed relative repellent activity similar to that of malathion-treated gunny bags after 24 h of treatment. Thus, gas chromatography-mass spectrometry analysis of aqueous extract of papaya leaves was performed. CONCLUSIONS: It can be concluded that extract of papaya leaves containing 2-methoxy-4-vinylphenol (8.47% peak area) can be used as a repellent biopesticide. © 2019 Society of Chemical Industry.


Assuntos
Repelentes de Insetos/farmacologia , Extratos Vegetais/farmacologia , Tribolium/efeitos dos fármacos , Andrographis/química , Animais , Azadirachta/química , Carica/química , Curcuma/química , Cymbopogon/química , Alho/química , Repelentes de Insetos/química , Repelentes de Insetos/isolamento & purificação , Mentha spicata/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Tribolium/fisiologia
3.
Pak J Pharm Sci ; 32(4): 1679-1686, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31608890

RESUMO

Four fungal isolates were identified in this study of which three were Aspergillus species with Aspergillus flavus having the highest frequency followed by A. parasiticus. The result of high frequency of Aspergillus flavus and Aspergillus parasiticus in the Zea mays sample revealed production of aflatoxins. Maize sample in Awka was found to contain aflatoxin B1 (9.60ppb) and B2 (13.3ppb). Inhibition of A. flavus and A. parasiticus with Azadirachta indica and Garcinia kola seed extracts showed that the test plant extracts were effective for reducing mycelial growth on the test organism. Methanolic extract of G. kola showed antifungal inhibitory activity on the test organisms and the highest at 10% concentration. With ethanol extracts of G. kola, the antifungal activity was effective i.e. for inhibition of A. flavus and A. parasiticus, with A. parasiticus having the higher percentage inhibition at 10%. Inhibiting growth of Aspergillus flavus and Aspergillus parasiticus using methanolic and ethanolic extracts of neem seeds was effective in the inhibition of the test organism at 10%. The methanolic and ethanolic extracts of combined Garcinia kola and neem seeds revealed effective inhibition of A. flavus and A. parasiticus with ethanolic extracts of the combined test plants exerting the highest inhibition against A. flavus (80.43±3.62). The extracts from this plant show the ability to suppress growth of toxigenic A. flavus and A. parasiticus. Phytochemical analysis showed that the methanolic and ethanolic extracts of G. kola and neem seeds showed the presence of secondary metabolites and this may be a reason for the inhibitory activity on A. flavus and A. parasiticus. Results from this study will be important in planning a management strategy against aflatoxin-producing fungi and other fungi associated with spoilage of stored food products.


Assuntos
Aflatoxinas/metabolismo , Antifúngicos/farmacologia , Aspergillus/metabolismo , Azadirachta/química , Garcinia kola/química , Zea mays/microbiologia , Aflatoxinas/análise , Antifúngicos/química , Aspergillus/efeitos dos fármacos , Aspergillus/isolamento & purificação , Aspergillus/patogenicidade , Etanol/química , Microbiologia de Alimentos , Armazenamento de Alimentos , Metanol/química , Testes de Sensibilidade Microbiana , Nigéria , Compostos Fitoquímicos/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Sementes/microbiologia
4.
Anticancer Res ; 39(10): 5473-5481, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31570441

RESUMO

BACKGROUND/AIM: Aerial parts and seeds of the neem tree (Azadirachta indica) have long been used in traditional medicine such as Ayurveda for health-related purposes. Our interest in neem bioactives lies in their potential use as standalone anticancer agents, or as adjuvants to standard therapy. The aim of the present study was to explore a supercritical CO2 extract (SCNE) of neem leaf and a prominent liminoid in neem leaf, nimbolide, for epigenetic activity. MATERIALS AND METHODS: Human colorectal cancer cell lines (HCT116 and HT29) were cultured for 48 h in the presence of neem extract or nimbolide and evaluated for growth inhibition and evidence of suppression of histone deacetylation and DNA methylation. RESULTS: Both SCNE and nimbolide suppressed the proliferation of colon cancer cells by inducing epigenetic modifications. CONCLUSION: Neem leaf contains bioactive constituents which modify epigenetic activity.


Assuntos
Azadirachta/química , Neoplasias Colorretais/tratamento farmacológico , Epigênese Genética/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Dióxido de Carbono/química , Dióxido de Carbono/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Metilação de DNA/efeitos dos fármacos , Células HCT116 , Células HT29 , Humanos , Limoninas/farmacologia
5.
J Colloid Interface Sci ; 555: 304-314, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31394317

RESUMO

The use of Azadirachta indica (A.I.) leaf extract to synthesize green photocatalysts for efficient separation of photogenerated charges has been a promising way to enhance the photocatalytic activity. Herein, we report the synthesis of green bismuth oxybromide/oxyiodide composites (G-BiOBrxI1-x) using A.I. leaf extract with effective size control, high specific surface area, and porosity. The A.I. leaf extract also acted as an excellent sensitizer that boosted the optical window of the G-BiOBrxI1-x photocatalysts. The as-prepared G-BiOBrxI1-x photocatalysts possessed three-dimensional (3-D) nanoplates like structure with successive modulation of the band gaps from 2.28 eV to 1.98 eV by varying the bromine/iodine (Br/I) ratio. Furthermore, the photocatalytic activity of the G-BiOBrxI1-x samples was measured and compared with the bismuth oxybromide/oxyiodide composite (C-BiOBr0.5I0.5) synthesized via conventional hydrolysis route (without the leaf extract). The G-BiOBrxI1-x photocatalysts degraded higher percentage of methyl orange (MO) and amoxicillin (AMX) than C-BiOBr0.5I0.5 under visible light irradiation. The superior photocatalytic efficiency was attributed to the multiple heterojunctions developed between BiOBr, BiOI, and electron-accepting π-conjugated system offered by leaf extract constituents, thereby facilitating the charge transfer process and effective separation of photogenerated charges.


Assuntos
Bismuto/química , Poluentes Ambientais/química , Iodetos/química , Extratos Vegetais/química , Folhas de Planta/química , Amoxicilina/química , Azadirachta/química , Compostos Azo/química , Catálise , Estrutura Molecular , Fenômenos Ópticos , Tamanho da Partícula , Processos Fotoquímicos , Propriedades de Superfície
6.
Environ Sci Pollut Res Int ; 26(26): 27043-27051, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31313228

RESUMO

Improving digestibility, fermentation characteristics, and reducing greenhouse biogases to protect the environment without the use of synthetic materials is an important goal of modern-day farming and nutritionist. Plant extracts are capable of solving these. This is due to the digestive enzymes and the bioactive components capable of performing antimicrobial functions inherent in these plants. This study was aimed to investigate the effect of standard maize substrate treated with selected herbs and spices extracts on ruminal environmental biogas production and pressure during fermentation via biogas production technique. Herbs (Azadirachta indica leaves (T1), Moringa oleifera leaves (T2), Ocimum gratissimum leaves (T3) and spices (Allium sativum bulb (T4), Zingiber officinale rhizome (T5)) were harvested, air dried, and milled using standard procedures. Methanolic extracts of the herbs and spices were prepared and used as additives at different concentrations (50, 100, and 150 µL) to the maize substrate for in vitro biogas production. Data were analyzed using regression analysis. There were significant (P < 0.05) differences across all the treatments on the volume and pressure of biogas. The pressure and volume of biogas when compared with the levels tested showed differences (P < 0.05) across all the treatments for the prediction of volume from pressure of biogas. The pressure and volume of gas produced in vitro increased (P < 0.05) and biogases decreased (P < 0.05) by the substrate treated with herbs and spices but for the drum stick leaves which was similar for the levels of concentration tested. This means that the level tested had a pronounced mitigation effect on pressure of biogas and volume of biogas produced. It was concluded that the herb and spice extracts have the potential to improve rumen fermentation and reduce the production of biogases in ruminant diet.


Assuntos
Ração Animal , Biocombustíveis , Extratos Vegetais/farmacologia , Rúmen/metabolismo , Animais , Azadirachta/química , Digestão/efeitos dos fármacos , Fermentação/efeitos dos fármacos , Alho/química , Gengibre/química , Metano/metabolismo , Moringa oleifera/química , Ocimum/química , Folhas de Planta/química , Pressão , Rúmen/efeitos dos fármacos , Ovinos , Especiarias , Zea mays/química
7.
Int J Biol Macromol ; 138: 13-20, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31279061

RESUMO

The present study suggests the formation of polyvinyl alcohol (PVA)-Azadirachta indica (neem)-chitosan blend nanofibrous mat (PNCNM) by bi-layered technique under optimum processing conditions. The antibacterial activity against Staphylococcus aureus (S. aureus) bacteria, morphology, bonding behavior, thermal stability, tensile behavior and moisture management properties of the developed sample had been investigated. The scanning electron microscopy (SEM) images revealed the homogeneous and smooth fibers produced having average diameter of 213.52nm (nm) with the minimum and maximum diameter of 152nm and 298nm respectively. Besides, it showed 91% porosity which is indicative of porous structure. The presence of PVA, neem constituents and chitosan was established by Fourier Transform Infrared Spectroscopy (FTIR) indicating the formation of hydrogen bonding among them. The addition of neem extracts led to enhanced thermal stability and moisture management properties. In addition, the developed mat showed a tensile strength of 18.78N corresponding to the elongation value of 4.98mm. Besides, the incorporation of neem extract into the nanofiber mat exhibited a significant synergistic antibacterial activity against bacterial cells through the formation of inhibition zone. Thus, the newly developed nanofibrous mat could turn out to be a suitable material for the wound dressing purpose.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Azadirachta/química , Quitosana/química , Nanofibras/química , Extratos Vegetais/química , Álcool de Polivinil/química , Testes de Sensibilidade Microbiana , Folhas de Planta/química , Porosidade , Staphylococcus aureus/efeitos dos fármacos , Resistência à Tração
8.
Int J Biol Macromol ; 137: 54-61, 2019 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-31226380

RESUMO

Azadirachta indica leaf is used by Indian population for the healing of various diseases including viral infection. Herein, we analyzed the antiherpetic (HSV-1) activity of two polysaccharides (P1 and P2) isolated from the leaf of A. indica and their chemically sulfated derivatives (P1S and P2S). The molecular weights of P1S and P2S are 41 and 11 kDa, respectively. Sulfate groups are located at positions C3 of the Araf and C6 of both Galp and Glcp residues of the most active polysaccharide (P1S). These compounds were not cytotoxic in HEp-2 cells, up to 1000 µg/mL. Both P1S and P2S exhibited antiviral activity when used simultaneously to HSV-1, with 50% inhibitory concentration/selectivity index, respectively, of 31.1 µg/mL/>51.4 and 80.5 µg/mL/>19.8. P1S showed better inhibitory effect (91.8%) compared to P1 (50%), P2 (71.1%) and P2S (70%) at 200 µg/mL. Synthesis of viral protein showed a dose-dependent response and the nucleic acid synthesis was inhibited up to 25 µg/mL, by P1 and P1S and up to 50 µg/mL, by P2 and P2S. The antiviral effect is probably due to the interference of polysaccharides at the early stages of HSV-1 replication, including adsorption. Further studies are under way to get insight into the mechanism of action of the substances.


Assuntos
Antivirais/química , Antivirais/farmacologia , Azadirachta/química , Herpesvirus Humano 1/efeitos dos fármacos , Polissacarídeos/química , Polissacarídeos/farmacologia , Sulfatos/química , Linhagem Celular Tumoral , Herpesvirus Humano 1/fisiologia , Humanos , Relação Estrutura-Atividade , Replicação Viral/efeitos dos fármacos
9.
Artif Cells Nanomed Biotechnol ; 47(1): 2107-2113, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31137983

RESUMO

In this study, latex of Azadirachta indica was used for the synthesis of silver nanoparticles (AgNP). UV-visible spectroscopy revealed the formation of AgNPs and the absorption band optimized at 442 nm. Fourier transform infrared (FTIR) spectroscopy shows different functional groups (carboxyl, amine and hydroxyl) of biomolecule which are responsible for reduction and capping process. X-ray diffraction (XRD) analysis confirms the nanoparticles are crystalline silver and cubic (AgCl) with face-centered cubic (Ag) types. Electron microscopics (SEM and TEM) were used to characterize the shape and size of the nanoparticles. The anticandidal and antibiofilm activity of AgNPs was using Fluconazole resistant clinical isolate of Candida tropicalis. The new approach of plant-mediated AgNPs synthesis appears to be cost-effective, eco-friendly and easy methods. The synthesized AgNPs considered as a novel and alternative agent to prevent C. tropicalis biofilms.


Assuntos
Azadirachta/química , Biofilmes/efeitos dos fármacos , Candida tropicalis/efeitos dos fármacos , Farmacorresistência Fúngica/efeitos dos fármacos , Fluconazol/farmacologia , Compostos de Prata/farmacologia , Prata/farmacologia , Antifúngicos/síntese química , Antifúngicos/química , Antifúngicos/farmacologia , Candida tropicalis/fisiologia , Técnicas de Química Sintética , Química Verde , Látex/química , Nanopartículas Metálicas/química , Prata/química , Compostos de Prata/síntese química , Compostos de Prata/química
10.
Fitoterapia ; 135: 73-78, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30999025

RESUMO

Four new limonoids, 7,12-dihydroxyvilasinone (1), vilasindione (2), 4-dehydroxynimbandiol (3) and azadiramide B (4), were isolated from extracts of Bacillus subtilis-fermented neem seeds. Their planar structures and relative configurations were elucidated by spectroscopic methods including UV, IR, MS and NMR, and the absolute stereochemistry was determined by comparing their experimental and calculated CD spectra. 4 is a rare salannin-class limonoid alkaloid. In cytotoxic assays, 3 showed inhibitory activity against MDA-MB-231, A375 and Hela cell lines with IC50 values of 21.45 ±â€¯5.41, 17.67 ±â€¯3.96 and 28.13 ±â€¯9.12 µM, respectively, while 4 selectively inhibited growth of MDA-MB-231 cell line with an IC50 value of 15.73 ±â€¯6.07 µM.


Assuntos
Azadirachta/química , Bacillus subtilis/fisiologia , Limoninas/farmacologia , Extratos Vegetais/química , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Azadirachta/microbiologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Fermentação , Humanos , Limoninas/química , Limoninas/isolamento & purificação , Estrutura Molecular , Sementes/química , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
11.
Pak J Biol Sci ; 22(3): 127-132, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30972982

RESUMO

BACKGROUND AND OBJECTIVE: Chemical insecticides have some limitations in vectors control such as the emergence of resistance in vector mosquitoes to conventional synthetic insecticides. It aimed to evaluate the larvicidal efficacy and phytochemical potential of Azadirachta indica, Cymbopogon citratus and Allium sativum L. against ulex quinquefasciatus fourth instar larvae. MATERIAL AND METHODS: The plants were screened and evaluated for their phytochemical composition and larvicidal effects on . quinquefasciatus larvae. RESULTS: The bioassay results showed that the effects were dependent on time and concentration of the extract used. Results showed the least lethal dose value for ethanolic extract of . citrates (72 h exposure) and the highest value for aqueous extract of A. indica (24 h exposure). Chi-square values were significant at p<0.05. Phytochemical analysis showed phytochemicals such as alkaloids, flavonoids, cardiac glycosides and resins in all the three plants. However, tannins were absent in A. indica and A. sativum, while balsam was only present in A. indica. Saponins, balsam and phenols were not found in A. sativum. Phenols were also absent in . citratus. Terpenes, steroids and resins were absent A. indica. CONCLUSION: Findings of this study revealed that these herbal extracts constitute an effective eco-friendly approach for the control of . quinquefasciatus larvae.


Assuntos
Culex , Inseticidas , Larva , Extratos Vegetais/química , Animais , Azadirachta/química , Cymbopogon/química , Alho/química , Dose Letal Mediana , Compostos Fitoquímicos/química , Folhas de Planta/química
12.
Vet Med Sci ; 5(3): 442-450, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-30828990

RESUMO

Because of speculated risk in generating antibiotic resistance in pathogenic microbiota, natural products from plant origin due to their diverse biological activities, have recently gained a great attention in animal nutrition. This study was designed to evaluate graded levels of neem seed oil on growth performance of broiler chickens. A total of 400-day-old chicks were randomly allocated to five experimental treatment groups. Experimental rations consisted of supplementing basal diet (R0- ) with 1 g antibiotic (R0 + ), 15, 20 and 25 g neem seed oil/kg of feed. Data were recorded on feed intake, weight gain, feed conversion ratio, and serum biochemical parameters. Result revealed that feeding broiler chicks with 25 g of neem oil/kg of feed resulted in a marked (P < 0.05) decreased in feed intake as compared to the other treatments in the starter phase. The average live body weight and the weight gain decreased with increasing level of neem oil in the ration. Supplementation of poultry feed with graded levels of neem oil has no marked (P > 0.05) effect on carcass yield and relative weight of organs except for liver weight which significantly (P < 0.05) increased with the highest dose of neem oil. Serum content in total proteins, total cholesterol, HDL-cholesterol, aspartate aminotransferase (AST), alanine aminotransferase (ALT) and creatinine were not significantly (P > 0.05) affected by the graded levels of neem oil. LDL-cholesterol significantly (P < 0.05) decreased with diets supplemented 20 g of neem oil/kg while triglycerides significantly increased with the highest doses of oil (20 and 25 g/kg) as compared to the negative and positive control rations. In conclusion, feeding broilers with Azadirachta indica seed oil has no beneficial effect on growth performance but may lead to the production of low-cholesterol chicken meat as demand by health-conscious consumers.


Assuntos
Azadirachta/química , Galinhas/crescimento & desenvolvimento , Suplementos Nutricionais/análise , Glicerídeos/farmacologia , Terpenos/farmacologia , Ração Animal/análise , Animais , Análise Química do Sangue/veterinária , Galinhas/fisiologia , Dieta/veterinária , Ingestão de Alimentos , Glicerídeos/química , Aves Domésticas , Distribuição Aleatória , Sementes/química , Terpenos/química , Ganho de Peso/efeitos dos fármacos
13.
Malar J ; 18(1): 35, 2019 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-30736813

RESUMO

BACKGROUND: Medicinal plant research may contribute to develop new pharmacological control tools for vector borne diseases, such as malaria. METHODS: The effects of methanol extracts (ME) obtained from seed kernel of ripe and unripe Azadirachta indica fruits were studied on erythrocytic proliferation of the rodent malaria parasite Plasmodium berghei strain ANKA and on mice pro-inflammatory response, as evaluated by measuring the matrix-metalloproteinase-9 (MMP-9) and tumour necrosis factor (TNF) plasma levels, in two mouse strains (C57BL/6 and BALB/c) which are considered as prototypical of Th1 and Th2 immune response, respectively. RESULTS: ME obtained from seed kernel of unripe Azadirachta indica fruits decreased by about 30% the proportion of erythrocytes infected with the malaria parasite in C57BL/6 mice in the 4 days suppressive test. In this treatment group, MMP-9 and TNF levels were notably higher than those measured in the same mouse strain treated with the anti-malarial drug artesunate, Azadirachta indica kernel extracts from ripe fruits or solvent. In BALB/c mice, treatment with kernel extracts did not influence parasitaemia. MMP-9 and TNF levels measured in this mouse strain were notably lower than those recorded in C57BL/6 mice and did not vary among treatment groups. CONCLUSIONS: The effects of the ME on the parasite-host interactions appeared to be mouse strain-dependent, but also related to the ripening stage of the neem fruits, as only the unripe fruit seed kernel extracts displayed appreciable bioactivity.


Assuntos
Antimaláricos/farmacologia , Azadirachta/química , Malária/tratamento farmacológico , Parasitemia/tratamento farmacológico , Extratos Vegetais/farmacologia , Plasmodium berghei/efeitos dos fármacos , Animais , Sistemas de Liberação de Medicamentos , Eritrócitos/parasitologia , Feminino , Inflamação/tratamento farmacológico , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Plantas Medicinais/química , Sementes/química
14.
Fitoterapia ; 134: 141-150, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30738093

RESUMO

Azadirachta indica A. Juss. (Neem) is an Indian tree recognized for its activity as pesticide, as well as several pharmacological properties. Among the various compounds already isolated and studied from Neem tree, azadirachtin (AZA) was identified as the main bioactive compound. Azadirachtin can be found at different parts of the Neem plant but assumes its maximum concentration at the seed level. This compound features a quite complex chemical structure, which justifies the 20-plus-year difficulty to identify the synthetic pathway that subsequently permitted to carry out its artificial synthesis. Azadirachtin is widely used as a basis for production of biopesticides; nevertheless, other properties have been recognized for this substance, among which the anticancer and antimalarial activity stand out. The methods available for azadirachtin extraction are diverse, including solid-liquid extraction and extraction with solvents at high or low temperatures. Alcohol based solvents are associated with higher extraction yields and are therefore preferred for the isolation of azadirachtin from plant parts. Clean-up of the extracts is generally required for further purification. The highest azadirachtin levels have been obtained from Neem seeds but concentration values present a large variation between batches. Therefore, in addition to extraction procedures, it is essential to establish routine methods for azadirachtin identification and quantification. Chromatography-based techniques are preferably selected for detection and quantification of azadirachtin in plant matrices. Overall, this process will guarantee a future reproducible, safe and effective use of the extracts in formulations for commercial applications.


Assuntos
Azadirachta/química , Limoninas/química , Limoninas/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/análise , Sementes/química , Solventes/química , Árvores/química
15.
J Mol Graph Model ; 87: 144-164, 2019 03.
Artigo em Inglês | MEDLINE | ID: mdl-30544005

RESUMO

Plasmodium falciparum heat shock protein 90 (PfHsp90) has been investigated as a potential target of antimalarial drug action using naturally occurring compounds. In this study, we performed in silico screening of 236 phytochemicals of Azadirachta indica, a plant known to possess antimalarial activity, and identified fourteen (14) potential non-carcinogenic, non-mutagenic, non-teratogenic and non-genotoxic phytochemicals. These phytochemicals were docked into the ATP-binding site of PfHsp90 using Autodock vina, and docked poses were rescored using PLANTS ChemPlp, X-Score version 1.2 and NNScore version 2.0. Consensus analysis of the scores using rank-by-rank and rank-by-number and receptor-ligand interaction assessment using LigPlot, led to the identification of margolone, margolonone, nimbinone, nimbione, nimosone and sugiol as best ranked potential interacting partners of PfHsp90. Molecular dynamic simulations of PfHsp90-ligand complexes for the six phytochemicals were performed using NAMD 2.9. The RMSD analysis of simulations trajectories, the ligand interaction analysis of receptor-ligand complex, and the free energy of binding with MMPBSA.py script and Bennett's acceptance ratio method (BAR) confirmed that these six phytochemicals may have potential to functionally interact with PfHsp90. However, though sharing several similar interacting residues with standard control binders yet the higher number of hydrogen bonds, higher level of sustained stability during molecular dynamics simulations and better free energy of binding suggest that margolonone, nimbinone and nimbione may have higher functional interaction potential with PfHsp90. Therefore, these phytochemicals may serve as potential leads in antimalarial drug design and development.


Assuntos
Antimaláricos/farmacologia , Azadirachta/química , Proteínas de Choque Térmico HSP90/química , Modelos Moleculares , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Proteínas de Protozoários/química , Sequência de Aminoácidos , Antimaláricos/química , Dose Letal Mediana , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Compostos Fitoquímicos/química , Extratos Vegetais/química , Plasmodium falciparum/metabolismo , Relação Quantitativa Estrutura-Atividade
16.
Drug Metab Lett ; 13(1): 19-24, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30398126

RESUMO

BACKGROUND: Polypharmacy, that is, two (or more) drugs administered together, may cause chemical or pharmacological interactions. Such interactions may alter the effect of either agent, leading to decrease or increase effectiveness of the drugs, which may cause adverse effects. The co-intake of complementary and alternative medicines with therapeutic medicine are supposed to influence pharmacodynamics or pharmacokinetics of the latter. OBJECTIVE: This study was conducted to determine the interaction of glipizide (GZ) with an aqueous extract of Azadirachta indica (AZI) leaves. METHOD: The pharmacokinetics and pharmacodynamics of glipizide was evaluated in High Fat diet (HFD) and streptozotocin induced diabetic Sprague-Dawley rats. Two doses of the AZI leaf extract (250 and 500 mg/kg) were administered alone or in combination with GZ (5 mg/kg) and serum glucose during oral glucose tolerance test, AST, ALT, and ALP levels were as estimated. In vitro CYP3A activity of AZI at 50 µg and 100 µg was assessed using liver microsomes. RESULTS: In the glucose tolerance test, AZI and GZ showed a hypoglycemic effect. However, the hypoglycemic effect was lower when AZI was administered in combination with GZ compared with GZ alone. AZI at 100 µg has shown significant potentiation of CYP3A activity. AZI (500 mg/kg) pretreatment significantly decreased AUC and increased Tmax to 8 h. CONCLUSION: This indicated that the pharmacokinetics and pharmacodynamics of GZ altered by AZI might be due to the induction of CYP3A activity. In conclusion, AZI can decrease the bioavailability of GZ, and hence, it should be cautiously used.


Assuntos
Azadirachta/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Glipizida/farmacologia , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Animais , Área Sob a Curva , Glicemia/análise , Glicemia/efeitos dos fármacos , Citocromo P-450 CYP3A/metabolismo , Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/etiologia , Dieta Hiperlipídica/efeitos adversos , Interações Ervas-Drogas , Humanos , Masculino , Folhas de Planta/química , Polimedicação , Ratos , Ratos Sprague-Dawley , Estreptozocina/toxicidade
17.
Nat Prod Res ; 33(10): 1491-1494, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-29258345

RESUMO

Azadirachta indica has long been used in traditional medicine. This study focused on isolation and characterisation of active ingredients in the extract, its fractions (NF-EA, NF-AQ, NF-G) and its effect on the cholesterol absorption activity. The NF-EA fraction was identified by marker compounds by LC-ESI-QTOF/MS. Cholesterol absorption activity was performed by measuring the solubility and size of cholesterol micelles. The intestinal motility was also examined by isolated rat's ileum to test the contraction. The extract and its fractions consist of flavonoids and phenolic compounds, like quercetin, kaempferol and myricetin. We found that A. indica extract and NF-EA increase cholesterol micelles size, while the extract, NF-AQ, myricetin and quercetin, reduced the solubility of cholesterol in micelles. The extract and quercetin inhibited the contraction induced by KCl up to 29 and 18%, respectively, and also decreased CaCl2-induced contraction. This finding is in support to traditional uses of A. indica as cholesterol-lowering agents and regulator of gastrointestinal motility.


Assuntos
Anticolesterolemiantes/farmacologia , Azadirachta/química , Colesterol/metabolismo , Motilidade Gastrointestinal/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Anticolesterolemiantes/química , Colesterol/farmacocinética , Avaliação Pré-Clínica de Medicamentos , Flavonoides/análise , Flavonoides/farmacologia , Flores/química , Masculino , Micelas , Fenóis/análise , Fenóis/farmacologia , Extratos Vegetais/análise , Extratos Vegetais/química , Plantas Medicinais/química , Quercetina/análise , Quercetina/farmacologia , Ratos Wistar
18.
Nat Prod Res ; 33(13): 1903-1908, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29806497

RESUMO

From an EtOAc-soluble fraction of the leaves of Azadirachta indica, one new lactam 28-norlimonoid named nimbandiolactam-21 (1), together with 2 known limonoids (2 and 3) were isolated. Their relative structures were elucidated based on NMR spectroscopic analysis. Nimbandiolactone-23 (2) showed the most potent α-glucosidase inhibitory activity, with an IC50 value of 38.7 µM. Compound 1 represents the first naturally occurring example of a 28-norlimonoid having the lactam moiety. The plausible biosynthetic pathway for the formation of lactam moiety in 1 was proposed.


Assuntos
Azadirachta/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Lactamas/farmacologia , Limoninas/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Concentração Inibidora 50 , Lactamas/química , Lactamas/isolamento & purificação , Limoninas/química , Limoninas/isolamento & purificação , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Folhas de Planta/química , Plantas Medicinais/química
19.
Nat Prod Res ; 33(14): 2060-2072, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29882423

RESUMO

Natural products with therapeutic nature are nowadays warmly welcomed in textiles. Current study is concerned with isolation of tannin from neem bark (Azadirachta indica) and its application onto silk fabric. For improvement in shades, chemical & bio-mordants have been employed at optimal dyeing conditions. It is found that methanolic extract of pH 5 obtained 8 g dye powder after US Treatment for 30 min has given high color strength if used to dye irradiated silk for 65 min at 75 °C. Bio-mordanting using herbal plants has improved the color characteristics as compared to chemical mordants used. ISO standards for color fastness reveal that herbal based bio-mordants have improved the rating from good to excellent as compared to chemical mordants used. It is concluded that US treatment has not only isolate the colorant for neem bark under mild condition but also given excellent characteristic using bio mordants onto silk fabrics.


Assuntos
Azadirachta/química , Corantes/química , Seda , Têxteis , Fracionamento Químico , Corantes/isolamento & purificação , Concentração de Íons de Hidrogênio , Casca de Planta/química , Taninos/química , Taninos/isolamento & purificação , Ultrassom/métodos
20.
Chem Commun (Camb) ; 55(4): 521-524, 2019 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-30556083

RESUMO

Biocompatible graphene quantum dots (GQDs), obtained from extracts of neem root, are found to be suitable for structured illumination microscopy and two-photon microscopy (TPM). Results of TPM and confocal luminescence microscopy ensure lysosome specificity in live cells and tissue-dependent localization in zebrafish, respectively, of GQDs.


Assuntos
Materiais Biocompatíveis/química , Grafite/química , Imagem Óptica , Fótons , Pontos Quânticos/química , Animais , Azadirachta/química , Materiais Biocompatíveis/isolamento & purificação , Grafite/isolamento & purificação , Humanos , Lisossomos/química , Células MCF-7 , Camundongos , Microscopia Confocal , Microscopia de Fluorescência , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/química , Células RAW 264.7 , Peixe-Zebra
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