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1.
Food Chem ; 464(Pt 1): 141612, 2024 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-39423522

RESUMO

Postharvest processing plays a crucial role in harnessing the benefits of prickly pear fruit by utilizing betalain as natural colorants to replace artificial colors in model food systems. Prickly pear betalain-enriched gummies were developed using various sugar substitutes, including table sugar, xylitol, stevia, and fructo-oligosaccharides (FOS). These gummies were analyzed for in vitro enzymatic inhibition, anti-inflammatory effects and molecular docking studies for decoding diabetes type-II and skin resilience. FTIR and HPLC confirmed the presence of betalain and isorhamnetin across all gummies. FOS and stevia incorporated gummies exhibited the highest polyphenolics and antioxidant activity. Betalain extract combined with stevia and FOS showed significant in vitro enzyme inhibition compared to other studied gummies. Specifically, FOS gummies showed the highest inhibition rates for α-amylase (23.58 %), α-glucosidase (24.12 %), tyrosinase (54.68 %), and collagenase (2.38 %). Additionally, all samples were non-toxic to RAW cell lines and exhibited anti-inflammatory effects. Molecular docking studies corroborated the in vitro results, and pharmacokinetics profiling confirmed the gummies' suitability for oral consumption and skin safety. The developed prickly pear betalain-enriched gummies, particularly those formulated with fructo-oligosaccharides and stevia, demonstrate significant potential as functional supplements for managing diabetes type-II and skin-related conditions.

3.
Crit Rev Food Sci Nutr ; 63(18): 3130-3149, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-34606382

RESUMO

Tea manufactured from the cultivated shoots of Camellia sinensis (L.) O. Kuntze is the most commonly consumed nonalcoholic drink around the world. Tea is an agro-based, environmentally sustainable, labor-intensive, job-generating, and export-oriented industry in many countries. Tea includes phenolic compounds, flavonoids, alkaloids, vitamins, enzymes, crude fibers, protein, lipids, and carbohydrates, among other biochemical constituents. This review described the nature of tea metabolites, their biosynthesis and accumulation with response to various factors. The therapeutic application of various metabolites of tea against microbial diseases, cancer, neurological, and other metabolic disorders was also discussed in detail. The seasonal variation, cultivation practices and genetic variability influence tea metabolite synthesis. Tea biochemical constituents, especially polyphenols and its integral part catechin metabolites, are broadly focused on potential applicability for their action against various diseases. In addition to this, tea also contains bioactive flavonoids that possess health-beneficial effects. The catechin fractions, epigallocatechin 3-gallate and epicatechin 3-gallate, are the main components of tea that has strong antioxidant and medicinal properties. The synergistic function of natural tea metabolites with synthetic drugs provides effective protection against various diseases. Furthermore, the application of nanotechnologies enhanced bioavailability, enhancing the therapeutic potential of natural metabolites against numerous diseases and pathogens.


Assuntos
Camellia sinensis , Catequina , Catequina/farmacologia , Flavonoides/farmacologia , Flavonoides/metabolismo , Polifenóis/análise , Camellia sinensis/química , Chá/química
4.
Front Pharmacol ; 13: 937484, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36188553

RESUMO

Ethnopharmacological relevance: Pien-Tze-Huang (PZH)-a traditional Chinese medicine (TCM) compound-has been employed to treat various liver inflammation and tumors for over 10 decades. Interestingly, most of the pharmacological effects had been validated and explored toward liver ailment along with pro-inflammatory conditions and cancer at the cellular and molecular level to date. Aim of the study: The present study aimed to investigate the therapeutic effect of PZH on autophagy and TGF-ß1 signaling pathways in rats with liver fibrosis and hepatic stellate cell line (HSC). Materials and methods: Male SD rats with carbon tetrachloride (CCl4)-induced liver fibrosis were used as the animal model. Next, PZH treatment was given for 8 weeks. Afterward, the therapeutic effects of PZH were analyzed through a hepatic tissue structure by hematoxylin-eosin (H&E), Van Gieson (VG) staining, and transmission electron microscopy (TEM), activity of ALT and AST by enzyme-associated immunosorbent assay as well. Subsequently, mRNA and protein expression were examined by quantitative polymerase chain reaction (qPCR), Western blotting, and immunohistochemistry (IHC). Then, the cell vitality of PZH-treated HSC and the expression of key molecules prevailing to autophagy were studied in vitro. Meanwhile, SM16 (a novel small molecular inhibitor which inhibits TGFß-induced Smad2 phosphorylation) was employed to confirm PZH's effects on the proliferation and autophagy of HSC. Results: PZH pharmacologically exerted anti-hepatic fibrosis effects as demonstrated by protecting hepatocytes and improving hepatic function. The results revealed the reduced production of extracellular collagen by adjusting the balance of matrix metalloproteinase (MMP) 2, MMP9, and tissue inhibitor of matrix metalloproteinase 1 (TIMP1) in PZH-treated CCl4-induced liver fibrosis. Interestingly, PZH inhibited the activation of HSC by down-regulating TGF-ß1 and phosphorylating Smad2. Furthermore, PZH down-regulated yeast Atg6 (Beclin-1) and microtubule-associated protein light chain 3 (LC3) toward suppressing HSC autophagy, and PZH exhibited similar effects to that of SM16. Conclusion: To conclude, PZH alleviated CCl4-induced liver fibrosis to reduce the production of extracellular collagen and inhibiting the activation of HSC. In addition, their pharmacological mechanisms related to autophagy and TGF-ß1/Smad2 signaling pathways were revealed for the first time.

5.
Oxid Med Cell Longev ; 2022: 9671594, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35795854

RESUMO

In this study, we report the green synthesis of silver nanoparticles (AgNPs) using the aqueous leaf extract of Tridax procumbens (TNP), which acts as the source of the reducing and capping agent. The distinctive absorption at 370 nm suggested synthesis of TNPs, which was confirmed by TEM, with a size in the range of 11.1 nm to 45.4 nm and a spherical shape, having a face-centered cubic structure, analyzed by XRD, and a Zeta potential of -20.7 mV, which indicated a moderate stability of TNP. The FTIR analysis revealed the presence of amines and hydroxyl groups with fluoro compounds over the TNPs. The HRLC-MS analysis of TNPs suggested the presence of a major capping agent such as fosinopril and reducing agents such as peptides (Gln Gly Ala, Ser Pro Asn, and Leu Met), terpenoids (lupanyl acid, tiamulin), polyphenol (peucenin), and alkaloids (8',10'-dihydroxydihydroergotamine, carteolol). The synthesized silver nanoparticles exhibited antimicrobial activity against multidrug-resistant (MDR) clinical isolates (Escherichia coli, Shigella spp., Aeromonas spp., Pseudomonas aeruginosa, and Candida tropicalis) and had anticancer activity against A459 (IC50 42.70 µg/ml). The extraction of partially purified aqueous leaf extracts by silica gel column chromatography followed by HPLC to synthesize silver nanoparticles (TNP11) and analyzed by HRLC-MS suggested that dipeptides were involved in the reduction of Ag+ to Ag0. Overall, the results showed that the green silver nanoparticles of T. procumbens could be safe, as they are endowed with potential antimicrobial activity against MDR clinical isolates and human lung carcinoma cells.


Assuntos
Anti-Infecciosos , Asteraceae , Nanopartículas Metálicas , Antibacterianos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Escherichia coli , Humanos , Nanopartículas Metálicas/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Prata/química
6.
Int J Mol Sci ; 22(19)2021 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-34639090

RESUMO

Cervical cancer is a life-threatening disease and the fourth most common cancer among women worldwide. Apple pomace is a multifunctional phenolic compound possessing effective biological activity against cervical cancer cells. This study aimed to investigate the anticancer effects of quercetin-3-glucoside (Q3G) extracted from apple pomace in HeLa cell lines and analyze its molecular mechanisms. High-performance liquid chromatography revealed that Q3G, coumaric acid, phloridzin, quercetin, and phloretin are the major polyphenolic compounds constituting apple pomace. Among them, Q3G possessed the greatest antioxidant and anti-inflammatory effects in vitro and exhibited significant cytotoxic effects in HeLa cells in a dose-and time-dependent manner. Flow cytometric analysis indicated that Q3G induced cell cycle arrest at the S phase in a time-dependent manner by altering cyclin-dependent kinase 2. Moreover, it induced apoptosis via chromosomal DNA degradation and increased reactive oxygen species generation. Furthermore, Q3G treatment altered the apoptosis-associated protein expression in the cells by activating caspase-9/-3, downregulating anti-apoptosis protein B-cell lymphoma (Bcl)-2 expressions and up regulating the pro-apoptotic Bcl-2-associated X protein. BH3-interacting domain death agonist cleavage occurred prior to the degradation of an anti-apoptotic Mu-2-related death-inducing gene involved in cell death signaling. Consequently, apple pomace Q3G holds promise as an anti-inflammatory and anticancer agent for treating cervical cancer.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Malus/química , Quercetina/análogos & derivados , Espécies Reativas de Oxigênio/metabolismo , Neoplasias do Colo do Útero/tratamento farmacológico , Apoptose , Proliferação de Células , Feminino , Humanos , Quercetina/farmacologia , Células Tumorais Cultivadas , Neoplasias do Colo do Útero/patologia
7.
Food Chem Toxicol ; 156: 112483, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34375721

RESUMO

Metabolic variations, antioxidant potential and cytotoxic effects were investigated in the different plant parts like the leaf, stem, flower, pod, and root of C. majus L. using spectroscopic and chromatographic methods. Total phenolics and flavonoids were studied in the different parts of C. majus L., leaf showed higher flavonoid content (137.43 mg/g), while the pod showed the highest phenolic (23.67 mg/g) content, when compared with the stem, flower and root. In the ABTS antioxidant assay, the flower extract showed 57.94% effect, while the leaf, pod and root extract exhibited 39.10%, 36.08% and 28.88% activity, respectively. The pod and leaf extracts demonstrated the potential effect, exhibiting 45.46 and 41.61% activity, respectively, for the DPPH assay. Similar to the phosphomolybdenum assay, the flower revealed higher antioxidant activity (46.82%) than the other plant parts. The in vitro SRB assay facilitated evaluation of the cytotoxic effect against the HeLa and CaSki human cervical cancerous cells. The extract displayed dose-dependent inhibitory effect on both the cell lines. The highest cytotoxic effect was observed in the pod and flower extracts post 48 h of exposure at 1000 µg/mL. The results of C. majus L. offered new insights in the preliminary steps regarding the development of a high value product for phytomedicine applications though promising metabolic variations with antioxidant and anticancer potentials.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Chelidonium/metabolismo , Flavonoides/análise , Células HeLa , Humanos , Polifenóis/análise
8.
Food Chem Toxicol ; 154: 112327, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34116102

RESUMO

Red onion skin waste (ROSW) was analyzed for extraction of naturally occurring 4'-O-glucoside of quercetin, spiraeoside (SPI) with promising biological activities. Reversed-phase high-performance liquid chromatography was used to determine the SPI content in three different solvent extracts of ROSW: water (12.2 mg/g), methanol (27.6 mg/g), and ethanol (32.5 mg/g). The ethanol extract and SPI showed significant radical-scavenging and anti-inflammatory activities. In addition, the anti-cancer effects of SPI on a HeLa cells was investigated. The results indicated that SPI treatment significantly inhibited cell growth, and the dose of 50 µg/mL exhibited the highest anti-cancer activity. SPI inhibited the expression of B-cell lymphoma 2 and BH3-interacting domain-death agonist and promoted apoptosis by activating caspase-9/-3 expression. Notably, SPI inhibited the expression of mu-2-related death-inducing gene, a molecule involved in death receptor-mediated apoptotic signaling. Cyclin-dependent kinase 2-cyclin-E expression was also inhibited after SPI treatment, particularly at the G2/M checkpoint. Our findings provide novel insights into the apoptotic potential with promising anticancer and enzyme inhibitory effects of ROSW SPI.


Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Inibidores Enzimáticos/farmacologia , Sequestradores de Radicais Livres/farmacologia , Cebolas/química , Quercetina/análogos & derivados , Antineoplásicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/isolamento & purificação , Sequestradores de Radicais Livres/isolamento & purificação , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Células HeLa , Humanos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Quercetina/isolamento & purificação , Quercetina/farmacologia
9.
Food Chem Toxicol ; 153: 112289, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34029669

RESUMO

Fritillaria thunbergii Miq. (Zhe beimu) ranked as oldest known homeopathic traditional folk medicine in China. The bulbs are medicinally important curing cough, inflammation, gastric ulcers, hypertension, diarrhea, and bronchitis. The aim of this review is to enlighten the deeper knowledge about F. thunbergii giving a comprehensive overview on its traditional uses, phytochemistry and pharmacology for future investigation of plant-based drugs and therapeutic applications. Total 48 medicinally important species of Fritillaria were described; total 122 compounds have been identified as results only 72 chemical constituents were described with proper chemical and biological details. F. thunbergii and its bulbs mainly constitute alkaloids, essential oils, diterpenoids, carbohydrates, sterols, amino acids, nucleosides, fatty acids, and lignans. The pharmacological studies demonstrate that F. thunbergii and its bulbs displays a wide range of bioactivities e.g., anti-inflammatory, anticancer, antitussive, expectorant, anti-ulcer, antimicrobial, antioxidant, anti-thyroid, regulation of blood rheology, anti-diarrhea, neuroprotection, and analgesic effects. Although promising reports on the various chemical bioactive constituents and biological properties of F. thunbergii have been published, very few reviews are related specifically to the traditional uses, phytochemistry and pharmacological applications. Further, various other studies on these plants should deserve our more attention for future investigation for drug development and its therapeutic applications.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Fritillaria/química , Animais , Medicamentos de Ervas Chinesas/química , Etnofarmacologia , Humanos , Raízes de Plantas/química
10.
Food Chem ; 334: 127508, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-32711265

RESUMO

Quercetin, a potential polyphenolic which possesses several biological effects. The influenza virus polymerase basic 2 (PB2) subunit of RNA polymerase responsible for replication, degree of virus conservation and active target site for designing specific antivirals. The quercetin derivatives downloaded from PubChem were screened using PyRX software configured with Vina Wizard, targeted on cap-binding site of the PB2 of influenza viral RNA polymerase. Among the PubChem library (total 97,585,747 compounds), 410 quercetin derivatives were screened using molecular docking (affinity: <-9.0 kcal) for their drug-likeness and in vitro cytopathic effect by Sulforhodamine B (SRB) assay. Among all quercetin derivatives, quercetin 3'-glucuronide (Q3G) showed strongest binding affinity towards cap-binding site of the PB2 subunit with -9.6 kcal of binding affinity and 0.00054 mM of Ki value, while quercetin 3'-glucuronide (Q7G) was presented highest anti-influenza activity with 2.10 ± 0.05 of IC50 on influenza A/PR/8/34 virus and non-cytotoxic effect as CC50 > 100 µg/mL.


Assuntos
Antivirais/farmacologia , Vírus da Influenza A/efeitos dos fármacos , Quercetina/análogos & derivados , Animais , Antivirais/química , Antivirais/metabolismo , Sítios de Ligação , Sobrevivência Celular/efeitos dos fármacos , RNA Polimerases Dirigidas por DNA/química , RNA Polimerases Dirigidas por DNA/metabolismo , Cães , Humanos , Vírus da Influenza A/enzimologia , Betainfluenzavirus/efeitos dos fármacos , Células Madin Darby de Rim Canino , Simulação de Acoplamento Molecular , Estrutura Terciária de Proteína , Subunidades Proteicas/química , Subunidades Proteicas/metabolismo , Quercetina/química , Quercetina/metabolismo , Quercetina/farmacologia , Termodinâmica
11.
Trends Biotechnol ; 39(2): 137-149, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-32690221

RESUMO

Medicinal plants produce valuable secondary metabolites with anticancer, analgesic, anticholinergic or other activities, but low metabolite levels and limited available tissue restrict metabolite yields. Transformed root cultures, also called hairy roots, provide a feasible approach for producing valuable secondary metabolites. Various strategies have been used to enhance secondary metabolite production in hairy roots, including increasing substrate availability, regulating key biosynthetic genes, multigene engineering, combining genetic engineering and elicitation, using transcription factors (TFs), and introducing new genes. In this review, we focus on recent developments in hairy roots from medicinal plants, techniques to boost production of desired secondary metabolites, and the development of new technologies to study these metabolites. We also discuss recent trends, emerging applications, and future perspectives.


Assuntos
Biotecnologia , Raízes de Plantas , Plantas Medicinais , Técnicas de Cultura de Células , Engenharia Genética , Raízes de Plantas/química , Raízes de Plantas/citologia , Raízes de Plantas/genética , Raízes de Plantas/metabolismo , Plantas Medicinais/química , Plantas Medicinais/citologia , Plantas Medicinais/genética , Plantas Medicinais/metabolismo
12.
J Agric Food Chem ; 68(39): 10685-10696, 2020 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-32924469

RESUMO

Saffron (Crocus sativus L.) byproducts are considered as a cheap source of bioactive polyphenolics endowed with potential antioxidant effects. The saffron biowaste is utilized for extraction of flavonoid glycosides and their potential biological properties. The total amount of polyphenolics and polysaccharides was found to be higher in the tepal than in the stamen. The bioactive compounds quercetin-3-O-sophoroside (Q-3-sop) and kaempferol-3-O-sophoroside (K-3-sop) were analyzed using high-performance liquid chromatography equipped with a photodiode array detector (HPLC-PDA) and identified by high-resolution mass spectrometry (HRMS) and nuclear magnetic resonance (NMR). The antioxidant effects were studied using 2,2 diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), ferric ion reducing antioxidant power (FRAP), and oxygen radical absorbance capacity (ORAC); Q-3-sop showed stronger antioxidant effects compared to K-3-sop, crocin-I, and crocin-II. Furthermore, Q-3-sop also inhibited cell apoptosis caused by H2O2 by reducing the levels of cellular reactive oxygen species (ROS). In terms of cytogenetic effects, Q-3-sop revealed no cytogenic effects on onion root meristem cells but chromosomal aberration was observed at the highest dose (200 ppm). Thus, saffron byproducts and its flavonoids could be utilized as natural antioxidant agents with no cytogenetic effects.


Assuntos
Crocus/química , Flavonoides/química , Glicosídeos/química , Extratos Vegetais/química , Antioxidantes/química , Antioxidantes/farmacologia , Apoptose/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Flavonoides/farmacologia , Flores/química , Glicosídeos/farmacologia , Humanos , Espectroscopia de Ressonância Magnética , Cebolas/efeitos dos fármacos , Cebolas/crescimento & desenvolvimento , Extratos Vegetais/farmacologia , Raízes de Plantas/crescimento & desenvolvimento , Resíduos/análise
13.
Artigo em Inglês | MEDLINE | ID: mdl-32612988

RESUMO

The present study explores the influence of mycophenolic acid (MPA) in combination therapy with quercetin (QC) (impeding MPA metabolic rate) delivered using the liposomal nanoparticles (LNPs). Mycophenolic acid liposome nanoparticles (MPA-LNPs) and quercetin liposome nanoparticles (QC-LNPs) were individually prepared and comprehensively characterized. The size of prepared MPA-LNPs and QC-LNPs were found to be 183 ± 13 and 157 ± 09.8, respectively. The in vitro studies revealed the higher cellular uptake and cytotoxicity of combined therapy (MPA-LNPs + QC-LNPs) compared to individual ones. Moreover pharmacokinetics studies in female SD-rat shown higher T 1 / 2 value (1.94 fold) of combined therapy compared to MPA. Furthermore, in vivo anticancer activity in combination of MPA-LNPs and QC-LNPs was also significantly higher related to other treatments groups. The combination therapy of liposomes revealed the new therapeutic approach for the treatment of breast cancer.

14.
Cytokine Growth Factor Rev ; 53: 66-70, 2020 06.
Artigo em Inglês | MEDLINE | ID: mdl-32418715

RESUMO

The outbreak of the novel SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2) responsible for coronavirus disease 2019 (COVID-19) has developed into an unprecedented global pandemic. Clinical investigations in patients with COVID-19 has shown a strong upregulation of cytokine and interferon production in SARS-CoV2- induced pneumonia, with an associated cytokine storm syndrome. Thus, the identification of existing approved therapies with proven safety profiles to treat hyperinflammation is a critical unmet need in order to reduce COVI-19 associated mortality. To date, no specific therapeutic drugs or vaccines are available to treat COVID-19 patients. This review evaluates several options that have been proposed to control SARS-CoV2 hyperinflammation and cytokine storm, eincluding antiviral drugs, vaccines, small-molecules, monoclonal antibodies, oligonucleotides, peptides, and interferons (IFNs).


Assuntos
Monofosfato de Adenosina/análogos & derivados , Alanina/análogos & derivados , Antivirais/uso terapêutico , Betacoronavirus/efeitos dos fármacos , Infecções por Coronavirus/tratamento farmacológico , Infecções por Coronavirus/patologia , Interferons/uso terapêutico , Pneumonia Viral/tratamento farmacológico , Pneumonia Viral/patologia , Monofosfato de Adenosina/uso terapêutico , Alanina/uso terapêutico , Anticorpos Monoclonais/uso terapêutico , COVID-19 , Síndrome da Liberação de Citocina/tratamento farmacológico , Síndrome da Liberação de Citocina/patologia , Citocinas/sangue , Quimioterapia Combinada , Humanos , Inflamação/tratamento farmacológico , Inflamação/patologia , Oligonucleotídeos/uso terapêutico , Pandemias , SARS-CoV-2 , Vacinas Virais/uso terapêutico
15.
Nanomedicine ; 24: 102147, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-31884040

RESUMO

Mycophenolic acid (MPA) has promising anticancer properties; however, it has limited clinical applications in vivo due to hydrophobic nature, high first-pass metabolism, lack of targeting, etc. These associated problems could be addressed by developing a suitable delivery vehicle, inhibiting the first-pass metabolism and additive/synergistic pharmacodynamic effect. Thus, MPA loaded highly stable lipid polymer hybrid nanoparticles (LPNs) were developed and investigated with the combination of quercetin (QC), a CYP 450 inhibitor cum anticancer. LPNs of MPA and QC (size; 136 ±â€¯12 and 176 ±â€¯35 nm, respectively) demonstrated higher cellular uptake and cytotoxicity of combination therapy (MPA-LPN + QC-LPN) compared to individual congeners in MCF-7 cells. In vivo pharmacokinetics demonstrated 2.17 fold higher T1/2 value and significantly higher pharmacodynamic activity in case of combination therapy compared to free MPA. In nutshell, the combinatory therapeutic regimen of MPA and QC could be a promising approach in improved breast cancer management.


Assuntos
Lipídeos/química , Ácido Micofenólico/química , Nanopartículas/química , Polímeros/química , Quercetina/química , Animais , Antioxidantes/química , Apoptose/efeitos dos fármacos , Neoplasias da Mama/tratamento farmacológico , Sobrevivência Celular/efeitos dos fármacos , Sistemas de Liberação de Medicamentos/métodos , Feminino , Humanos , Células MCF-7 , Ácido Micofenólico/uso terapêutico , Quercetina/uso terapêutico , Espectroscopia de Infravermelho com Transformada de Fourier
16.
Food Chem Toxicol ; 132: 110659, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31276745

RESUMO

Subcritical water extraction (SWE) applied to analyses the bioactives from ashwagandha (W. somnifera) at varying temperature (100-200 °C) and extraction time (10-30 min). The effect of temperature and time has been investigated in terms of extraction yield (EY), total phenolic content (TPC), cytotoxicity, antioxidant, and enzyme inhibitory activities. The withanosides and withanolides responsible for various biological effects were quantified using high performance liquid chromatography (HPLC). The HPLC analysis revealed Withanoside V, Withanoside IV, 12-Deoxywithastramonolide, Withanolide A, and Withaferin A as a principle bioactive compounds in SWE, with high in concentration compared to microwave-assisted extraction (MAE), Soxhlet extraction (SE) and maceration (MC). For SWE the highest EY (65.6%; 200 °C for 30 min), TPC (82.5 mg GAE/g DE), antioxidant activity (DPPH: 80.3%, FRAP: 60.5% and ABTS: 78.9), and potent enzyme inhibitory effects were observed. The SWE and Withaferin A showed significant reduction in cell viability of cervical cancer (HeLa) cells, with IC50 values 10 mg/ml and 8.5 µM/ml, respectively but no cytotoxic effect for normal cells (MDCK). Thus, SWE can provide effective extraction for ashwagandha withanosides and withanolides compared MAE, SE and MC to conventional methods, which could be used for extraction of pharmacologically active fractions with therapeutic applications.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Vitanolídeos/farmacologia , Animais , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Cães , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Células HeLa , Humanos , Células Madin Darby de Rim Canino , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Raízes de Plantas/química , Saponinas/química , Saponinas/isolamento & purificação , Extração em Fase Sólida/métodos , Água/química , Withania/química , Vitanolídeos/química , Vitanolídeos/isolamento & purificação
17.
Food Chem Toxicol ; 131: 110563, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31199992

RESUMO

Apple pomace (AP) utilised for analysis of triterpenic acids (TTAs) using HPLC-MS/MS. The methanol, ethanol and ethyl acetate extracts showed high phenolic content with significant antioxidant activity compared to chloroform and n-hexane. AP TTAs; ursolic acid, betulinic acid and maslinic acid showed potent antioxidant and enzyme inhibitory effects. The IC50 values were 13.2-30.8 µg/mL (tyrosinase), 19.6-42.5 µg/mL (xanthine oxidase) and 16.6-38.6 µg/mL (urease) for AP extracts and 8.4-25.8 µg/mL (tyrosinase), 12.6-30.2 µg/mL (xanthine oxidase) and 10.1-28.6 µg/mL (urease) for TTAs, compared to the positive controls; kojic acid (10.4 ±â€¯0.06 µg/mL), allopurinol (9.6 ±â€¯0.04 µg/mL) and thiourea (8.9 ±â€¯0.02 µg/mL) towards respective enzymes. UA showed a competitive type of inhibition for tyrosinase, while BA showed a noncompetitive type of inhibition towards xanthine oxidase. In addition, the AP extracts and TTAs exerted significant cytotoxic effects towards the proliferation of cancer cell lines. AP methanol extract (IC50 of 38.5 ±â€¯4.1, 47.1 ±â€¯3.5, 70.6 ±â€¯2.3, and 50.5 ±â€¯3.9 µg/mL) and ursolic acid (IC50 of 6.5 ±â€¯0.7, 15.5 ±â€¯1.4, 20.8 ±â€¯1.3, and 5.6 ±â€¯0.8 µg/mL) showed prominent anticancer activity on Hela, Skov-3, Caski, and NCL cancer cell lines, respectively. Thus, this study shows that the AP & TTAs could be utilized for functional food development and as a potent antioxidant, anticancer, skin whitening, and anti-urolithic agents.


Assuntos
Antineoplásicos/farmacologia , Inibidores Enzimáticos/farmacologia , Sequestradores de Radicais Livres/farmacologia , Frutas/química , Malus/química , Triterpenos/farmacologia , Animais , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Cães , Ensaios Enzimáticos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/isolamento & purificação , Humanos , Células Madin Darby de Rim Canino , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/análise , Extratos Vegetais/química , Extração em Fase Sólida , Triterpenos/química , Triterpenos/isolamento & purificação , Urease/antagonistas & inibidores , Xantina Oxidase/antagonistas & inibidores
18.
Environ Sci Pollut Res Int ; 26(21): 21127-21139, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31144182

RESUMO

The farmers and agrochemical industries lack science-based knowledge about sustainable utilization of pesticides and insecticides. The investigation on rising use of chemical pesticides and insecticides has remarkable issue related to environment pollution, soil fertility, and human health; as such, nowadays, many people prefer natural alternatives over synthetic chemicals. Natural products, like horticultural oils, play a significant role for sustainable and safe integrated pest management, providing natural alternatives to chemical pesticides and insecticides. For several decades, both plant- and petroleum-based spray oils have been always used to control various pests, mites, and insects. Currently, these horticultural oils are used as a part of the integrated pest management, which utilizes secure and non-chemical pesticides rather than conventional pesticides. Horticultural oil refers to a complex mixture of hydro-carbons with traces of sulfur- and nitrogen-based compounds, extracted from plants. The key components of horticultural oils include paraffin and olefin. The horticultural oils are considered suitable since they are non-toxic to both plants and animals, are applied easily, have low risk properties, cost-effective, and play significant role in pest control, but show little effects on the beneficial insects. As a result, these attributes make horticultural oils to be considered as secure and effective alternative for chemical insecticides and pesticides for both commercial and domestic agriculture.


Assuntos
Controle de Pragas/métodos , Óleos de Plantas , Agricultura , Animais , Fazendeiros , Alimentos , Humanos , Insetos , Inseticidas/análise , Praguicidas , Plantas , Solo
19.
Food Chem Toxicol ; 125: 313-321, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30654095

RESUMO

Dianthus superbus (DS) is a traditional medicinal herb well known for its medicinal and therapeutic potential and widely distributed in various Asian countries. The ethyl acetate (EA), butanol (Bu) and distilled water (DW) extracts of DS assessed for extraction of bioactive compounds and their biological activities. The chemical analysis was done using LC-MS/MS and antioxidant, anticancer and antiviral activities were determined. EA extracts showed strong anticancer activity with IC50 of 9.5, 13.8 and 69.9 µg/mL on SKOV, NCL-H1299 and Caski cancer cell lines, respectively. The Bu extracts exhibited strongest antiviral activity with respect to both influenza A and B viruses with IC50 values of 4.97 and 3.9 µg/mL, respectively. Also the metabolic profile for EA, Bu and DW extracts shows high variations and influence precisely the antioxidant, anticancer and antiviral properties. The quercetin 3- rutinoside and isorhamnetin 3- glucoside showed higher neuraminidase inhibition activity in dose dependent manner. Molecular docking study revealed that flavonol glycosides have higher binding activities towards influenza polymerase membrane glycoprotein. Correlation study showed that flavonol glycosides were linked to anti-influenza activity and cyclic peptides with anticancer activities. This study provides vital information for effective utilization of DS for medicinal, food and therapeutic purposes.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Antivirais/farmacologia , Dianthus/química , Flavonóis/farmacologia , Glicosídeos/farmacologia , Animais , Antineoplásicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Antivirais/isolamento & purificação , Linhagem Celular Tumoral , Cães , Flavonóis/isolamento & purificação , Glicosídeos/isolamento & purificação , Humanos , Vírus da Influenza A/efeitos dos fármacos , Vírus da Influenza B/efeitos dos fármacos , Células Madin Darby de Rim Canino , Simulação de Acoplamento Molecular , Neuraminidase/antagonistas & inibidores , Proteínas Virais/antagonistas & inibidores
20.
Food Chem ; 271: 239-247, 2019 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-30236673

RESUMO

A biflavonoid, amentoflavone isolated from Nandina domestica and characterized by NMR spectral-data analyses was assessed for its antioxidant, and antibacterial potential in vitro and in food-model systems. Amentoflavone exhibited potent antioxidant ability (19.21-75.52%) on scavenging DPPH, ABTS, superoxide, and hydroxyl radicals. Fluorescent images confirmed bacterial membrane depolarization of both the tested pathogens Staphylococcus aureus and Escherichia coli, with a significant reduction in cell viabilities at their respective MIC of 62.5 and 125 µg/mL. Increasing rates of membrane permeability observed in 260 nm-absorbing material, potassium ion, extracellular ATP, and relative electrical conductivity assays confirmed antibacterial mechanistic role of amentoflavone as also evidenced by microscopic studies of SEM and TEM. There was a marked inhibitory effect of amentoflavone with a significant reduction in cell counts of S. aureus and E. coli in minced chicken and apple juice at 4 °C, thus suggesting its nutritional enhancing efficacy as a natural antioxidant and antimicrobial agent.


Assuntos
Antibacterianos/farmacologia , Berberidaceae/química , Biflavonoides/farmacologia , Malus/microbiologia , Produtos Avícolas/microbiologia , Animais , Galinhas , Escherichia coli/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos
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