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1.
J Ethnopharmacol ; 318(Pt B): 116960, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37517570

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Metabolic diseases are the major causes of macrovascular and microvascular complications which lead to morbidity and mortality. Traditionally, garlic has been used as food and medicine for more than 5000 years. However, efficacy studies have shown conflicting results regarding the garlic effect. AIM OF THE STUDY: This study aims to evaluate the efficacy of garlic on the components of metabolic syndrome (MetS) in metabolic disease patients. MATERIALS AND METHODS: This study was a systematic review and meta-analysis of randomized controlled trials (RCTs). Pubmed, Cochrane Central Register of Controlled Trials (CENTRAL), and Google scholar were searched till December 25, 2021 for identifying the relevant studies that have shown the effects of garlic on components of metabolic syndrome in metabolic disease patients. The mean difference with 95% CI was calculated using fixed-effect or random-effect models. RESULTS: The effect of garlic has shown significant changes on waist circumference (p-value= <0.0001), total cholesterol (p < 0.0001), low density lipoprotein (p = 0.01), high density lipoprotein (p < 0.00001), triglycerides (p < 0.00001), systolic blood pressure (p < 0.00001), diastolic blood pressure (p < 0.00001), glucose (p < 0.00001), Homeostatic Model Assessment for Insulin Resistance (HOMA-IR) (p = 0.04), C-reactive protein (p < 0.00001), tumor necrosis factor (TNF)-α (p = 0.002), interleukin (IL)-6 (p = 0.0001). Subgroup analysis has shown the favorable effects of garlic in metabolic disease patients. CONCLUSION: Our meta-analysis results confirm the findings that garlic could be useful as an anti-hyperlipidemic, anti-hyperglycemic, anti-hypertensive and anti-inflammatory drug.


Assuntos
Produtos Biológicos , Alho , Síndrome Metabólica , Humanos , Síndrome Metabólica/tratamento farmacológico , Ensaios Clínicos Controlados Aleatórios como Assunto , Pressão Sanguínea , Anti-Hipertensivos/farmacologia , Antioxidantes/farmacologia , Produtos Biológicos/farmacologia
2.
J Ethnopharmacol ; 318(Pt B): 116974, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37517571

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Dendrobium officinale Kimura & Migo is traditionally used to treat skin diseases, gastrointestinal diseases, and other diseases. Dendrobium officinale polysaccharides (DOP) are the main component of Dendrobium officinale that accounts for its bioactivity, which shows a variety of effects such as moisturizing, antioxidant and anti-fatigue. However, there is no comprehensive study on the effect of DOP on skin photoaging combined with in vitro and in vivo models, and its specific mechanism is still unclear. AIM OF THE STUDY: Our study aimed to explore the effect and underlying mechanism of DOP on skin photoaging, as well as to improve the stability and transdermal absorption of DOP. MATERIALS AND METHODS: DOP was extracted, purified and structurally characterized. In vitro HaCaT cell photoaging model was used to examine the photoprotection effect of DOP. Cell viability was detected by CCK-8; Intracellular reactive oxygen species were determined by DCFH-DA; DNA damage, cell apoptosis and cell cycle arrest were examined by flow cytocytometry. For autophagy flux detection, the adenovirus loaded with mRFP-GFP-LC3 was introduced into cells. Further, to enhance the stability and absorption of DOP, we designed and prepared the W/O/W type DOP multilayer emulsions (ME) by a two-step emulsification method. The emulsion stability, drug loading and encapsulation rate, DOP stability and DOP transdermal rate were detected. In vivo photoaging animal model was applied to compare the difference of photoaging protection effect between DOP solution and DOP ME. Specifically, skin appearance, histological change, antioxidant system, proinflammatory indicators, matrix metalloproteinases and autophagy level of skin tissues were examined and compared. RESULTS: The results showed that DOP achieve photoaging protection by inhibiting oxidative stress, alleviating cell cycle arrest and apoptosis, and enhancing autophagy flux in photoaged HaCaT cells. The W/O/W type DOP multilayer emulsion (ME) with high encapsulation rate and strong stability was found to significantly improve the stability and transdermal absorption of DOP. In addition, our results showed that DOP (ME) remarkably improved skin condition of photoaged mice. Specifically, DOP (ME) enhanced the expression of antioxidant enzymes and autophagy and decreased the levels of pro-inflammatory factors and matrix metalloproteinases in the skin of photoaged mice as compared with DOP solution. CONCLUSIONS: In conclusion, DOP was effective in improving skin photoaging, and the DOP multilayer emulsion we designed enhanced the stability and skin absorption of DOP, boosting DOP's protective effect against photoaging.


Assuntos
Dendrobium , Envelhecimento da Pele , Camundongos , Animais , Antioxidantes/farmacologia , Emulsões , Polissacarídeos/farmacologia , Metaloproteinases da Matriz
3.
J Ethnopharmacol ; 318(Pt B): 117009, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37557936

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Corydalis hendersonii Hemsl. (CH), is a traditional Tibetan medicine used in highland areas for the treatment of alpine polycythemia, ulcers and various inflammatory diseases. Its antioxidant and anti-inflammatory effects have been demonstrated in experimental mice. Loss of dopaminergic neurons due to oxidative damage is thought to be an important factor in the development of PD, the potential antioxidant, anti-inflammatory effects of CH could potentially be used for PD treatment. AIM OF THE STUDY: To identify potential targets of CH using network pharmacology and to investigate the neuroprotective effects in cultured cell models and in MPTP-intoxicated mice. MATERIALS AND METHODS: The main chemical components of CH were analyzed by UPLC-MS/MS and their potential targets of action or signaling pathways were analyzed using network pharmacology. MPP + or LPS was added to SH-SY5Y or BV2 cells, respectively, to establish cellular models. MPTP was administered to C57BL/6J mice to induce inflammation and dopaminergic neuron loss as well as dyskinesia, followed by behavioral analysis to determine the role of CH in eliminating inflammation, avoiding neuron loss, and improving dyskinesia. RESULTS: CH contains 241 alkaloids, 213 flavonoids, 177 terpenoids and 114 phenolic compounds. The targets crossover between CH and PD yielded 210 potential therapeutic targets, especially growth factors and inflammatory pathway-related genes, such as BDNF, NF-κB, as potential key targets. In cultured cells, CHE eliminated MPP + -induced impairment of cell viability as well as LPS-induced inflammation, respectively. In mice, CHE ameliorated MPTP-induced dyskinesia and rescued the loss of dopaminergic neurons in the substantia nigra and striatum. Mechanistically, CHE effectively maintained the activity of the BDNF-TrkB/Akt signaling pathway, accordingly, inhibited inflammatory signaling pathways such as HIF-1α/PKM2 and Notch/NF-kB. CONCLUSIONS: CH performed well in eliminating inflammation and improving locomotor deficits in mice, and its potent active ingredients are worthy of subsequent research and development.


Assuntos
Corydalis , Neuroblastoma , Fármacos Neuroprotetores , Humanos , Animais , Camundongos , Doenças Neuroinflamatórias , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Antioxidantes/farmacologia , Cromatografia Líquida , Lipopolissacarídeos/farmacologia , Farmacologia em Rede , Camundongos Endogâmicos C57BL , Neuroblastoma/tratamento farmacológico , Espectrometria de Massas em Tandem , Inflamação/tratamento farmacológico , Inflamação/metabolismo , NF-kappa B/metabolismo , Neurônios Dopaminérgicos , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios/metabolismo , Modelos Animais de Doenças
4.
Food Chem ; 432: 137175, 2024 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-37633143

RESUMO

Brazilian propolis from Apis mellifera is widely studied worldwide due to its unique chemical composition and biological properties, such as antioxidant, antimicrobial, and anti-inflammatory. However, although many countries produce honey, another bee product, the consumption of propolis as a functional ingredient is linked to hydroethanolic extract. Hence, other food uses of propolis still have to be incorporated into food systems. Assuming that propolis is a rich source of flavonoids and is regarded as a food-grade ingredient for food and pharmaceutical applications, this review provides a theoretical and practical basis for optimising the bioactive properties of Brazilian propolis, encompassing the extraction processes and incorporating its bioactive compounds in the delivery systems for food applications. Overall, pharmacotechnical resources can optimise the extraction and enhance the chemical stability of phenolic compounds to ensure the bioactivity of food formulations.


Assuntos
Ascomicetos , Ingredientes de Alimentos , Mel , Própole , Abelhas , Animais , Brasil , Antioxidantes/farmacologia
5.
Food Chem ; 432: 137202, 2024 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-37634342

RESUMO

The pequi (Caryocar brasiliense) external mesocarp is rich in phenolic compounds and pectin and demonstrates the potential to produce active and biodegradable films. Thus, the present study aimed to produce films with pequi mesocarp as a polymer matrix and evaluate the influence of crosslinking agents (calcium chloride and citric acid) on the film's properties. The films obtained from pequi mesocarp (MF), showed in general, complete biodegradation in 33 days, good antioxidant capacity, and inhibition against S. aureus (24.7 mm) and E. coli (23.0 mm). The crosslinking agents reduced solubility by up to 35% and increased the elongation of the films by up to 3.5-fold. Calcium chloride promoted a higher reduction in solubility, and both agents increase the antioxidant and antimicrobial activities, compared to MF. Citric acid proved to be the best agent to modify the properties of pequi mesocarp films. In addition to the crosslinking action, it presented plasticizing effect.


Assuntos
Antioxidantes , Malpighiales , Antioxidantes/farmacologia , Cloreto de Cálcio , Escherichia coli , Staphylococcus aureus , Ácido Cítrico
6.
J Ethnopharmacol ; 318(Pt A): 116792, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37356745

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Fufangmuniziqi formula (FFMN), a traditional Uyghur medicine used in China, is derived from an ancient Uyghur medical book and consists of 13 herbs. The herbs of FFMN, such as Peganum harmala L., Glycyrrhiza uralensis Fisch., and Nigella glandulifera, have been demonstrated to have acetylcholinesterase (AChE) inhibitory, anti-neuroinflammatory, or antioxidant effects. Therefore, FFMN may have a good anti-Alzheimer's disease (AD) effect, but its specific action and mechanism need to be further proven. AIM OF THE STUDY: This study aims to investigate the anti-AD effects of FFMN and the role played by alkaloids, flavonoids, and saponins in anti-AD. MATERIALS AND METHODS: The alkaloids, flavonoids, and saponins fractions of FFMN were prepared by macroporous resin chromatography. The absorbed ingredients in the drug-containing serum were identified by UPLC⁃Q⁃TOF⁃MS. An AD mouse model was established by intraperitoneal injection of scopolamine (SCO). The role of different fractions of FFMN in the anti-AD process was examined by Morris water maze (MWM), in-vitro cell, and AChE inhibition assay. RESULTS: A total of 20 ingredients were identified in the serum samples collected after oral administration of FFMN, and seven compounds were selected as candidate active compounds. MWM experiments showed that different fractions of FFMN could significantly improve SCO-induced learning memory impairment in mice. The alkaloids fraction (ALK) regulated cholinergic function by inhibiting AChE activity, activating choline acetyltransferase activity, and protein expression. Flavonoids and saponins were more potent than the ALK in downregulating pro-inflammatory factors or inflammatory mediators, such as TNF-α, MPO, and nitric oxide. Western blot results further confirmed that flavonoids and saponins attenuated neuroinflammation by inhibiting the phosphorylation of IκB and NF-κB p65. This result was also verified by in-vitro cellular assays. FFMN enhanced antioxidant defense by increasing the activity of superoxide dismutase and reducing the production of MDA. Combined with cellular experiments, flavonoids and saponins were proven more protective against oxidative damage. CONCLUSION: FFMN improved cognitive and memory impairment in the SCO-induced AD mouse model. ALK mainly enhanced the function of the cholinergic system. Flavonoid and saponin fractions mainly attenuated neuroinflammation and oxidative stress by modulating the NF-κB pathway. All these findings strongly suggested that the combination of alkaloid, flavonoid, and saponin fractions derived from FFMN is a promising anti-AD agent that deserves further development.


Assuntos
Alcaloides , Disfunção Cognitiva , Saponinas , Camundongos , Animais , Escopolamina/farmacologia , Acetilcolinesterase/metabolismo , Saponinas/farmacologia , Saponinas/uso terapêutico , Flavonoides/farmacologia , Flavonoides/uso terapêutico , NF-kappa B/metabolismo , Doenças Neuroinflamatórias , Alcaloides/efeitos adversos , Disfunção Cognitiva/induzido quimicamente , Disfunção Cognitiva/tratamento farmacológico , Antioxidantes/farmacologia , Transtornos da Memória/induzido quimicamente , Transtornos da Memória/tratamento farmacológico , Transtornos da Memória/metabolismo , Estresse Oxidativo , Colinérgicos/farmacologia , Receptores Proteína Tirosina Quinases/efeitos adversos , Receptores Proteína Tirosina Quinases/metabolismo , Aprendizagem em Labirinto
7.
J Ethnopharmacol ; 318(Pt A): 116890, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37423514

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Marveled at the discovery of artemisinin, the world's expectations for traditional Chinese medicine are rising. He's Yangchao formula (HSYC) is a traditional Chinese herbal formula with the effects of tonifying kidney and essence, and reconciling yin and yang. It has been clinically proven to have anti-ovarian aging effects. Age is the primary cause of diminished ovarian reserve and assisted reproductive failure in women, whether HSYC has the potential to improve in vitro maturation of oocytes from advanced maternal age (AMA) mice has yet to be determined. AIM OF THE STUDY: This study aims to evaluate the efficacy and possible mechanism of HSYC in promoting in vitro maturation of oocytes from AMA mice. MATERIALS AND METHODS: The GV oocytes were obtained from young and aged mice. The GV oocytes from young mice were cultured in drops of M16 medium, and the GV oocytes from AMA mice were randomly divided four groups: Vehicle group (cultured in 90% M16 medium +10% blank serum), Low HSYC group (cultured in 90% M16 medium + 10% Low HSYC-medicated serum), High-HSYC group (cultured in 90% M16 medium +10% High HSYC-medicated serum), and Quercetin group (cultured in M16 medium supplemented with 10 µM quercetin). The rates of first polar body extrusion, reactive oxygen species (ROS), intracellular calcium, and mitochondrial membrane potential levels in each groups were observed. In addition, expression levels of mitochondrial function, autophagy, DNA damage, and antioxidant-related proteins were assessed. RESULTS: Supplementation of HSYC in vitro alleviated age-associated meiotic progression defects in maternally aged oocytes. Importantly, HSYC supplementation eliminated the age-related ROS accumulation to suppress DNA damage and autophagy during the in vitro maturation of maternally aged oocytes. Meanwhile, the mitochondrial function was improved after HSYC treatment, as manifested by higher mitochondrial membrane potential and lower Ca2+ levels. Furthermore, we found that HSYC supplementation during in vitro maturation of maternally aged oocytes upregulated the expression level of SIRT3, a crucial protein in regulating mitochondrial function. Consistently, the expression levels of the SOD2, PCG1α, and TFAM were increased, while the SOD2 acetylation level was decreased, which further proved its antioxidant function. CONCLUSIONS: HSYC supplementation promotes in vitro maturation of oocytes from AMA mice mainly via improving mitochondrial function and alleviating oxidative stress. The mechanism may be related to the regulation of SIRT3-dependent deacetylation of the SOD2 pathway.


Assuntos
Técnicas de Maturação in Vitro de Oócitos , Sirtuína 3 , Masculino , Feminino , Animais , Camundongos , Idade Materna , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Quercetina/farmacologia , Oócitos
8.
J Ethnopharmacol ; 318(Pt A): 116870, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37423517

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Danggui Shaoyao San (DSS) has effective in treating hepatic ascites and liver disease. AIM OF THE STUDY: To explore the chemical characterization of DSS and protective effect on CCl4-induced hepatic fibrosis and its mechanism, especially its anti-oxidative stress and anti-inflammation. MATERIALS AND METHODS: The chemical characterization of DSS was determined by HPLC-Q-Exactive Orbitrap MS. And the antioxidant activity of DSS in vitro was determined. The hepatic fibrosis model was established using intragastric administration of 40% CCl4/soybean oil (v/v) twice weekly for 13 weeks. From 6th week, the DSS group and the positive control group were given DSS (2, 4, 8 g/kg/d) and silymarin (50 mg/kg/d), respectively. The livers of rats were examined histologically by H&E. The ALT, AST, ALB and TBIL were determined, and hepatic fibrosis markers (HA, LN, CIV, PIIINP), oxidative stress (SOD, MDA, GST, GSH) and inflammatory factor (IL-6, TNF-α) were tested using ELISA kits. In addition, the levels of TAC, TOS, LOOH and AOPP in the liver were also determined. RESULTS: The chemical characterization of DSS was determined by HPLC-Q-Exactive Orbitrap MS. The results show that DSS mainly includes triterpenoids, monoterpenes, phenols, sesquiterpenes, butyl phthalide, etc., and DSS has good antioxidant activity in vitro. In addition, the ALT, AST and TBIL of rats were remarkably reduced after treatment with DSS at three doses. Liver histopathological analysis showed that DSS alleviated the inflammatory infiltration, hepatocyte swelling, necrosis and hepatic fibrosis induced by CCl4. DSS significantly decreased HA, IV-C, PIIINP and LN. Further determination showed that DSS significantly increased TAC, OSI and decreased TOC, LOOH and MDA, indicating that DSS could regulate redox balance and reduce lipid peroxidation in vivo. DSS also increased the activity of GST, SOD and GSH concentration. In addition, DSS also reduced IL-6 and TNF-α. CONCLUSIONS: In this study, we described the chemical characterization of DSS and found that it has good antioxidant activity. We proved that DSS has the functions of reducing oxidative stress, anti-inflammatory, protecting liver cells and reducing hepatic fibrosis.


Assuntos
Antioxidantes , Fator de Necrose Tumoral alfa , Ratos , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Interleucina-6/metabolismo , Cirrose Hepática/induzido quimicamente , Cirrose Hepática/tratamento farmacológico , Cirrose Hepática/patologia , Estresse Oxidativo , Fígado , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Anti-Inflamatórios/efeitos adversos , Superóxido Dismutase/metabolismo , Tetracloreto de Carbono/farmacologia
9.
J Ethnopharmacol ; 318(Pt A): 116862, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37437789

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Asthma is a common chronic disease characterized by inflammation of the airways. One of the most devastating consequences of this inflammatory process is the production of reactive oxygen species responsible for oxidative stress. Nasturtium officinale commonly known as watercress has traditionally been applied in Iranian folk medicine to treat respiratory disorders and diseases mainly bronchitis and asthma. In accordance with these ethnopharmacological reports, through our previous in vivo experiment, we have confirmed significant effect of its hydroalcoholic extract in reducing lung inflammation and oxidative stress in an ovalbumin-induced asthmatic rat model. AIM OF THE STUDY: The aim of the present study was to investigate the anti-inflammatory and antioxidant effects of N. officinale hydroalcoholic extract (NOE) in patients with asthma, in order to confirm our findings of the previous performed in vivo study. MATERIAL AND METHODS: The NOE capsules (500 mg) were treated twice daily for 4 weeks as a supplementary treatment in a randomized, double-blind, and placebo-controlled trial in asthmatics. The primary outcome was Asthma Control Test score. The blood samples were taken at the beginning and end of the study. Then, the level of inflammatory markers, oxidative stress markers and antioxidant enzyme activity were measured. RESULTS: Treatment with NOE for one month caused a reduction in the levels of MDA, PCO and NO metabolite markers compared to the placebo group. In addition, FRAP levels as an indicator of total antioxidant capacity in the intervention group was significantly increased at the end of the treatment period compared to pre-treatment values. CONCLUSION: Findings demonstrated that NOE may have a therapeutic effect on asthma by improving oxidative stress. However, more studies are required to support these results. Moreover, bio-assay guided fractionation and isolation approach can be conducted to identify major bioactive compound/s.


Assuntos
Asma , Nasturtium , Ratos , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/metabolismo , Nasturtium/metabolismo , Irã (Geográfico) , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Estresse Oxidativo , Asma/tratamento farmacológico
10.
J Ethnopharmacol ; 318(Pt A): 116911, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37451488

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: In traditional system of medicine, Piper species, or its components are widely used to treat many diseases including memory improvement. One of the wild species Piper trioicum Roxb. (Piperaceae) is found in South Asian countries. The whole plant is used as folk medicine to improve memory. AIM OF THE STUDY: To our knowledge, no previous research has investigated the neuroprotective activities of P. trioicum. So, we studied the ameliorative effect of P. trioicum in attenuating cognitive deficit in scopolamine induced neurotoxicity in experimental rats. MATERIALS AND METHODS: Wistar rats were exposed to scopolamine (3 mg/kg, i. p.) for 14 consecutive days, and the effect of P. trioicum (HAPT; oral, 300, 400 mg/kg) on scopolamine-invoked neurotoxicity in brain were studied. During the experimental period, behaviour analyses of rats were observed 30 min post-drug administration. The role of antioxidants of HAPT in scavenging cellular oxygen/peroxyl radicals were studied. Acetylcholinesterase and butyrylcholinesterase inhibitions, and mode of inhibition kinetics of HAPT were studied. Pathogenic cellular oxidative (MDA, GSH, SOD, and CAT), DNA damage (8-oxodG), neurochemical (acetyl- and, butyryl-cholinesterase), ß-secretase (BACE-1 and 2), MAPτ, and neuroinflammation (IL-6, TNF-α) biomarkers in extension to the histopathological observation of brain cortex were studied. GC-MS/MS analysis was carried out to investigate the presence of bioactive constituents in HAPT. RESULTS: HAPT, a rich source of phenol and flavonoid type antioxidants were responsible in quenching oxygen/peroxyl radicals and protected the cellular membrane, and lipoproteins against ROS in DPPH, ORAC, and CAPe tests. HAPT inhibited acetylcholinesterase and butyrylcholinesterase activities, and showed competitive-inhibition (reversible) towards cholinesterase activities. HAPT-400 significantly improved the learning and memory-impairment by restoring oxidative MDA, GSH, SOD, CAT, and DNA damage (8-oxodG) markers of serum, and cortex. It also improved acetyl- and, butyryl-cholinesterase, ß-secretase, and MAPτ level in brain by restoring proinflammatory cytokines IL-6, and TNF-α indicators in neurotoxic rats. GC-MS/MS reported therapeutic significance active compounds were molecular-docked towards target proteins, found that proscillaridin showed the highest affinity towards AChE, BuChE, BACE1, and BACE2 with binding energy of ΔGb -9.1, ΔGb -10.2, ΔGb -11.4 and ΔGb -11.5 Kcal/mol, respectively. Cymarin and morphine-3-glucuronide showed the second highest binding affinity towards AChE (ΔGb -8.8) and BuChE (ΔGb -10.0), respectively. In BACE-1, betulin showed the second highest binding affinity ΔGb -10.7 Kcal/mol and in BACE-2, morphine-3-glucuronide showed the second highest binding affinity ΔGb -9.8 Kcal/mol. CONCLUSIONS: Synergistic impact of proscillaridin, Cymarin, morphine-3-glucuronide, betulin like compounds in HAPT improved memory impairment, healing of tissue architecture of cortex with the restoration of neurochemical, neuroinflammation, and oxidative indicators in neurotoxic rats.


Assuntos
Piper , Proscilaridina , Ratos , Animais , Escopolamina/farmacologia , Secretases da Proteína Precursora do Amiloide , Butirilcolinesterase/metabolismo , Acetilcolinesterase/metabolismo , Antioxidantes/farmacologia , Ratos Wistar , Piper/metabolismo , 8-Hidroxi-2'-Desoxiguanosina , Cimarina , Interleucina-6 , Doenças Neuroinflamatórias , Espectrometria de Massas em Tandem , Fator de Necrose Tumoral alfa , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ácido Aspártico Endopeptidases/metabolismo , Superóxido Dismutase , Cognição , Oxigênio , Inibidores da Colinesterase/farmacologia
11.
J Ethnopharmacol ; 318(Pt A): 116918, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37453619

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: As the second-largest traditional medical system in China, Tibetan medicine has a long history and abundant resources. To promote the development of the Tibetan medicine industry, it is essential to study the pharmacological activities of Tibetan medicine based on its traditional usage methods. AIM OF THE STUDY: Pneumonia has been a worldwide health problem with high morbidity and mortality rates, especially in the context of the COVID-19 epidemic. Given the unique advantages of traditional Tibetan medicine in treating pulmonary diseases, further research is warranted to develop potential anti-pneumonia drugs. MATERIALS AND METHODS: In our study, the potential combined decoction from traditional Tibetan medicine was determined by the data mining method. The antioxidant activity in vitro, anti-inflammatory effects on the macrophage cell model, as well as the anti-pulmonary inflammation effects on the LPS-induced mice model, have been explored to investigate the potential anti-pneumonia role of the decoction. Additionally, we conducted network pharmacology analysis to identify the potential targets against pneumonia, which were further confirmed by western blot assays. RESULTS: Following the combination therapy of Pterocephalodes hookeri (C.B.Clarke) V.Mayer & Ehrend. and Onosma hookeri var. longiflora (Duthie) A.V.Duthie ex Stapf ('P-O'), the clearance of DPPH radical and the total reducing power were all improved, as well as alleviated the toxicity. On the in vitro level, 'P-O' pre-treatment reduced the secretion of NO, TNF-α, IL-6, and IL-1ß in LPS-stimulated RAW264.7 cells, while promoting the concentration of IL-10. Meanwhile, on the in vivo level, the 'P-O' pre-treating also could alleviate LPS-induced pulmonary inflammation by reducing the pulmonary edema and leakage of the lung microvascular, improving the pathological change of lung tissue and regulating the cytokines content in bronchoalveolar lavage fluid (BALF). Furthermore, network pharmacology analysis revealed that the mechanism of 'P-O' in treating pneumonia in a multi-component, multi-target, and multi-pathway network, with the TLR4/NF-κB signaling pathway playing a crucial role, as demonstrated by the western blot assay results. CONCLUSION: In summary, the combination therapy of 'P-O' exhibited good antioxidant activity and anti-inflammatory activity in vitro, as well as a therapeutic effect against pulmonary inflammation in vivo. These findings provide evidence for the clinical application of 'P-O' and offer new approaches for treating pneumonia.


Assuntos
COVID-19 , Pneumonia , Camundongos , Animais , NF-kappa B/metabolismo , Receptor 4 Toll-Like/metabolismo , Lipopolissacarídeos/toxicidade , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Transdução de Sinais , Pneumonia/induzido quimicamente , Pneumonia/tratamento farmacológico , Pneumonia/prevenção & controle , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico
12.
J Ethnopharmacol ; 318(Pt A): 116881, 2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-37460029

RESUMO

ETHNOPHARMACOLOGY RELEVANCE: Petiveria alliacea L., commonly known as macura and gully root, is an important medicinal plant used in the Caribbean and Central America to treat ailments associated to the central nervous system, including poor memory. AIM OF THE STUDY: To assess the effects of the P. alliacea leaves methanol fraction (PMF) on a scopolamine-induced learning and memory impairment mouse model related to acetylcholinesterase activity and oxidative stress. MATERIAL AND METHODS: After PMF administration at doses of 500 or 900 mg/kg, cognitive ability was evaluated using the Morris water maze (MWM), Y-maze (YM) and novel object recognition (NOR) tests. The mouse brain tissue was further assessed for acetylcholinesterase activity and antioxidant activity. Levels of oxidative stress were also evaluated by measuring malondialdehyde (MDA) and glutathione activity. Acute toxicity was also evaluated. RESULTS: PMF led to memory improvement in the behavioral tests in mice with scopolamine-induced cognitive impairment. Moreover, PMF inhibited acetylcholinesterase activity and showed antioxidant potential that in turn attenuated cholinergic degradation. Additionally, PMF increased glutathione levels and glutathione reductase activity and reduced MDA levels in the brain. Moreover, no acute toxicity was detected with the use of PMF. CONCLUSION: In a mouse model of scopolamine-induced cognitive deficit, PMF exhibited protective effects, decreasing oxidative damage and regulating cholinergic function in the brain bearing significant memory enhancing potency. These data suggest that PMF is a promising candidate for developing therapies for neurodegenerative disorders.


Assuntos
Fármacos Neuroprotetores , Phytolaccaceae , Camundongos , Animais , Escopolamina/toxicidade , Acetilcolinesterase/metabolismo , Fármacos Neuroprotetores/efeitos adversos , Aprendizagem em Labirinto , Transtornos da Memória/induzido quimicamente , Transtornos da Memória/tratamento farmacológico , Transtornos da Memória/metabolismo , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/metabolismo , Estresse Oxidativo , Glutationa/metabolismo , Colinérgicos/farmacologia , Extratos Vegetais/efeitos adversos
13.
Braz. j. biol ; 84: e253696, 2024. graf
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1355862

RESUMO

Abstract Transplanting time and genotype contribute to improving crop yield and quality of eggplant (Solanum melongena L.). A field experiment was conducted to investigate the impact of foliar applied of triacontanol (TRIA) and eggplant genotypes 25919, Nirala, 28389 and Pak-10927,transplanted on 1 March,15 March, and 1 April on exposure to high air temperature conditions. The experiment was performed according to Randomized Complete Block Design and the data was analyzed by using Tuckey,s test . The TRIA was applied at 10µM at flowering stage; distilled water was used as the control. Rate of photosynthesis and transpiration, stomatal conductance, water use efficiency, and effects on antioxidative enzymes (superoxide dismutase, catalase and peroxidase) were evaluated. The 10µM TRIA increased photosynthesis rate and water use efficiency and yield was improved in all genotypes transplanted at the different dates. Foliar application of 10µM TRIA increased antioxidative enzyme activities (SOD, POD & CAT) and improved physiological as well as biochemical attributes of eggplant genotypes exposed to high heat conditions. Highest activity of dismutase enzyme 5.41mg/1g FW was recorded in Nirala genotype in second transplantation. Whereas, lowest was noted in PAK-10927 (2.30mg/g FW). Maximum fruit yield was found in accession 25919 (1.725kg per plant) at 1st transplantation with Triacontanol, whereas accession PAK-10927 gave the lowest yield (0.285 kg per plant) at control treatment on 3rd transplantation. Genotype, transplanting date and application of TRIA improved growth, yield and quality attributes under of heat stress in eggplant.


Resumo O tempo de transplante e o genótipo contribuem para melhorar a produtividade e a qualidade da cultura da berinjela (Solanum melongena L.). Um experimento de campo foi conduzido para investigar o impacto da aplicação foliar de triacontanol (TRIA) e genótipos de berinjela 25919, Nirala, 28389 e Pak-10927, transplantados em 1 de março, 15 de março e 1 de abril de exposição a condições de alta temperatura do ar. O experimento foi realizado de acordo com o Randomized Complete Block Design e os dados foram analisados pelo teste de Tuckey. O TRIA foi aplicado a 10 µM na fase de floração; água destilada foi utilizada como controle. Taxa de fotossíntese e transpiração, condutância estomática, eficiência do uso da água e efeitos sobre as enzimas antioxidantes (superóxido dismutase, catalase e peroxidase) foram avaliados. O TRIA 10 µM aumentou a taxa de fotossíntese e a eficiência do uso da água e o rendimento foi melhorado em todos os genótipos transplantados nas diferentes datas. A aplicação foliar de TRIA 10µM aumentou as atividades das enzimas antioxidantes (SOD, POD e CAT) e melhorou os atributos fisiológicos e bioquímicos de genótipos de berinjela expostos a condições de alto calor. A atividade mais elevada da enzima dismutase 5,41mg / 1g FW foi registrada no genótipo Nirala no segundo transplante. Considerando que o mais baixo foi observado em PAK-10927 (2,30 mg / g FW). A produtividade máxima de frutos foi encontrada no acesso 25919 (1,725 ​​kg por planta) no 1º transplante com Triacontanol, enquanto o acesso PAK-10927 deu a menor produção (0,285 kg por planta) no tratamento de controle no 3º transplante. Genótipo, data de transplante e aplicação de TRIA, melhoramento do crescimento, rendimento e atributos de qualidade sob estresse térmico em berinjela.


Assuntos
Solanum melongena/genética , Solanum melongena/metabolismo , Fotossíntese , Resposta ao Choque Térmico , Álcoois Graxos , Antioxidantes/metabolismo , Antioxidantes/farmacologia
14.
Sci Rep ; 13(1): 14716, 2023 09 07.
Artigo em Inglês | MEDLINE | ID: mdl-37679486

RESUMO

Since the dawn of civilization, people have turned to plants as a safe and efficient form of treatment for a variety of diseases. It has long been known that Calotropis procera has the potential to treat a number of diseases. In this study, the C. procera leaf aqueous extract was obtained using the maceration method, and p-coumaric was found to be the main compound. The extract was rich in phenols (174.82 mg gallic acid equivalent/g) and flavonoids (1781.7 µg quercetin equivalent/g). The extract had high antioxidant properties, as indicated by the IC50 values obtained for 2,2-diphenyl-1-picrylhydrazyl (DPPH) (366.33 µg/mL) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) (169.04 µg/mL), as well as the ferric ions reducing antioxidant power (FRAP) (1.67 µg ascorbic acid equivalent/g of the extract). The cytotoxicity of the extract was evaluated against the survival of HT 29 cells, and the IC50 was found to be 236.87 µg/mL. The most resistant and sensitive strains to the extract were Escherichia coli and Staphylococcus aureus, respectively. The morphological changes of these strains were demonstrated through scanning electron microscopy and confocal laser scanning microscopy. The C. procera extract could be therefore used as an antioxidant, antimicrobial, and anticancer agent.


Assuntos
Anti-Infecciosos , Calotropis , Humanos , Antioxidantes/farmacologia , Ácido Ascórbico , Anti-Infecciosos/farmacologia , Escherichia coli
15.
Front Cell Infect Microbiol ; 13: 1181516, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37680749

RESUMO

Introduction: One of the promising leads for the rapid discovery of alternative antimicrobial agents is to repurpose other drugs, such as nonsteroidal anti-inflammatory agents (NSAIDs) for fighting bacterial infections and antimicrobial resistance. Methods: A series of new carbazole derivatives based on the readily available anti-inflammatory drug carprofen has been obtained by nitration, halogenation and N-alkylation of carprofen and its esters. The structures of these carbazole compounds were assigned by NMR and IR spectroscopy. Regioselective electrophilic substitution by nitration and halogenation at the carbazole ring was assigned from H NMR spectra. The single crystal X-ray structures of two representative derivatives obtained by dibromination of carprofen, were also determined. The total antioxidant capacity (TAC) was measured using the DPPH method. The antimicrobial activity assay was performed using quantitative methods, allowing establishment of the minimal inhibitory/bactericidal/biofilm eradication concentrations (MIC/MBC/MBEC) on Gram-positive (Staphylococcus aureus, Enterococcus faecalis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) strains. Computational assays have been performed to assess the drug- and lead-likeness, pharmacokinetics (ADME-Tox) and pharmacogenomics profiles. Results and discussion: The crystal X-ray structures of 3,8-dibromocarprofen and its methyl ester have revealed significant differences in their supramolecular assemblies. The most active antioxidant compound was 1i, bearing one chlorine and two bromine atoms, as well as the CO2Me group. Among the tested derivatives, 1h bearing one chlorine and two bromine atoms has exhibited the widest antibacterial spectrum and the most intensive inhibitory activity, especially against the Gram-positive strains, in planktonic and biofilm growth state. The compounds 1a (bearing one chlorine, one NO2 and one CO2Me group) and 1i (bearing one chlorine, two bromine atoms and a CO2Me group) exhibited the best antibiofilm activity in the case of the P. aeruginosa strain. Moreover, these compounds comply with the drug-likeness rules, have good oral bioavailability and are not carcinogenic or mutagenic. The results demonstrate that these new carbazole derivatives have a molecular profile which deserves to be explored further for the development of novel antibacterial and antibiofilm agents.


Assuntos
Anti-Inflamatórios não Esteroides , Cloro , Bromo , Antioxidantes/farmacologia , Reposicionamento de Medicamentos , Anti-Inflamatórios , Carbazóis/farmacologia , Antibacterianos/farmacologia , Biofilmes
16.
Nutrients ; 15(17)2023 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-37686853

RESUMO

Lycopene is a compound of colored origin that shows strong antioxidant activity. The positive effect of lycopene is the result of its pleiotropic effect. The ability to neutralize free radicals via lycopene is one of the foundations of its pro-health effect, including the ability to inhibit the development of many civilization diseases. Therefore, this study focuses on the importance of the antioxidant effect of lycopene in inhibiting the development of diseases such as cardiovascular diseases, diseases within the nervous system, diabetes, liver diseases, and ulcerative colitis. According to the research mentioned, lycopene supplementation has significant promise for the treatment of illnesses marked by chronic inflammation and oxidative stress. However, the majority of the supporting data for lycopene's health benefits comes from experimental research, whereas the evidence from clinical studies is both scarcer and less certain of any health benefits. Research on humans is still required to establish its effectiveness.


Assuntos
Doenças Cardiovasculares , Colite Ulcerativa , Humanos , Antioxidantes/farmacologia , Licopeno/farmacologia , Estresse Oxidativo , Doenças Cardiovasculares/prevenção & controle
17.
Nutrients ; 15(17)2023 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-37686887

RESUMO

Medicinal plants, such as Talisia esculenta, are rich in antioxidant biomolecules, which are used in the treatment and prevention of many diseases. The antioxidant potential of T. esculenta extracts obtained from leaves and fruit peels was investigated using biochemical and 3T3 cell line assays as well as in vivo assays using an organism model Tenebrio molitor. Four extracts were tested: hydroethanolic extracts from leaves (HF) and from fruit peels (HC), and infusion extracts from leaves (IF) and from fruit peels (IC). The biochemical assays demonstrated an antioxidant capacity verified by TAC, reducing power, DPPH, and copper chelating assays. None of the extracts exhibited cytotoxicity against 3T3 cells, instead offering a protection against CuSO4-induced oxidative stress. The antioxidant activity observed in the extracts, including their role as free radical scavengers, copper chelators, and stress protectors, was further confirmed by T. molitor assays. The CLAE-DAD analysis detected phenolic compounds, including gallic acid, rutin, and quercitrin, as the main constituents of the samples. This study highlights that leaf and fruit peels extracts of T. esculenta could be effective protectors against ROS and copper-induced stress in cellular and invertebrate models, and they should be considered as coadjutants in the treatment and prevention of diseases related to oxidative stress and for the development of natural nutraceutical products.


Assuntos
Produtos Biológicos , Sapindaceae , Animais , Camundongos , Antioxidantes/farmacologia , Cobre , Extratos Vegetais/farmacologia
18.
Molecules ; 28(17)2023 Sep 03.
Artigo em Inglês | MEDLINE | ID: mdl-37687245

RESUMO

Lavender is a valued plant due to its cosmetic, perfumery, culinary, and health benefits. A wide range of applications is related to the composition of bioactive compounds, the quantity and quality of which is determined by various internal and external factors, i.e., variety, morphological part of the plant, and climatic and soil conditions during vegetation. In the presented work, the characterization of antimicrobial properties as well as the qualitative and quantitative assessment of bioactive compounds in the form of polyphenols in ethanol extracts from leaves and flowers of Lavandula angustifolia Mill. intended for border hedges, cultivated in the region of southern Poland, were determined. The composition of the fraction of volatile substances and antioxidant properties were also assessed. The conducted research shows that extracts from leaves and flowers significantly affected the viability of bacterial cells and the development of mold fungi. A clear decrease in the viability of bacteria and C. albicans cells was shown in the concentration of 0.32% of extracts. Leaf extracts were characterized by a much higher content of polyphenols and antioxidant properties than flower extracts. The composition of volatiles measured by GC-MS was significantly different between the extracts. Linalyl acetate and ocimene isomers mix dominated in flower extracts, whereas coumarin, γ-cadinene, and 7-methoxycoumarin were identified as dominant in leaf extracts.


Assuntos
Anti-Infecciosos , Lavandula , Antioxidantes/farmacologia , Polônia , Anti-Infecciosos/farmacologia , Candida albicans , Extratos Vegetais/farmacologia
19.
Molecules ; 28(17)2023 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-37687260

RESUMO

The present study reports the biomimetic synthesis of silver nanoparticles (AgNPs) using a simple, cost effective and eco-friendly method. In this method, the flavonoid extract of Perilla frutescens (PFFE) was used as a bioreduction agent for the reduction of metallic silver into nanosilver, called P. frutescens flavonoid extract silver nanoparticles (PFFE-AgNPs). The Ultraviolet-Visible (UV-Vis) spectrum showed a characteristic absorption peak at 440 nm that confirmed the synthesis of PFFE-AgNPs. A Fourier transform infrared spectroscopic (FTIR) analysis of the PFFE-AgNPs revealed that flavonoids are involved in the bioreduction and capping processes. X-ray diffraction (XRD) and selected area electron diffraction (SAED) patterns confirmed the face-centered cubic (FCC) crystal structure of PFFE-AgNPs. A transmission electron microscopic (TEM) analysis indicated that the synthesized PFFE-AgNPs are 20 to 70 nm in size with spherical morphology and without any aggregation. Dynamic light scattering (DLS) studies showed that the average hydrodynamic size was 44 nm. A polydispersity index (PDI) of 0.321 denotes the monodispersed nature of PFFE-AgNPs. Further, a highly negative surface charge or zeta potential value (-30 mV) indicates the repulsion, non-aggregation, and stability of PFFE-AgNPs. PFFE-AgNPs showed cytotoxic effects against cancer cell lines, including human colon carcinoma (COLO205) and mouse melanoma (B16F10), with IC50 concentrations of 59.57 and 69.33 µg/mL, respectively. PFFE-AgNPs showed a significant inhibition of both Gram-positive (Listeria monocytogens and Enterococcus faecalis) and Gram-negative (Salmonella typhi and Acinetobacter baumannii) bacteria pathogens. PFFE-AgNPs exhibited in vitro antioxidant activity by quenching 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydrogen peroxide (H2O2) free radicals with IC50 values of 72.81 and 92.48 µg/mL, respectively. In this study, we also explained the plausible mechanisms of the biosynthesis, anticancer, and antibacterial effects of PFFE-AgNPs. Overall, these findings suggest that PFFE-AgNPs have potential as a multi-functional nanomaterial for biomedical applications, particularly in cancer therapy and infection control. However, it is important to note that further research is needed to determine the safety and efficacy of these nanoparticles in vivo, as well as to explore their potential in other areas of medicine.


Assuntos
Besouros , Neoplasias do Colo , Nanopartículas Metálicas , Perilla frutescens , Humanos , Animais , Camundongos , Antioxidantes/farmacologia , Prata/farmacologia , Peróxido de Hidrogênio , Antibacterianos/farmacologia
20.
BMC Complement Med Ther ; 23(1): 311, 2023 Sep 08.
Artigo em Inglês | MEDLINE | ID: mdl-37684643

RESUMO

BACKGROUND: Pomegranate is known for its beneficial properties due to its high content in antioxidants and might constitute a natural option for preventing and treatment of different pathologies including cancer. Since mitochondria are involved in tumorigenesis through ROS production and modulation of oxidative metabolism, we investigated the biological effects of pomegranate on cellular redox state, proliferation and metabolism in the breast cancer cell line MDA-MB-231 (MDA). METHODS: MDA were treated for 24 h with graded concentration of filtered Pomegranate juice (PJ) and tested for metabolic Flux Analysis with XFe96 Extracellular Flux Analyzer, for proliferation using the xCELLigence System Real-Time Cell Analyzer and for intracellular ROS content by Confocal Microscopy Imaging. RESULTS: Cells-treatment with freshly prepared pomegranate juice (PJ) resulted in a significant reduction of the intracellular ROS content already at the lower concentration of PJ tested. Additionally, it enhanced mitochondria respiration, and decreased glycolysis at high concentrations, inhibiting at the same time cell proliferation. As pomegranate is a seasonal fruit, assessment of optimum storage conditions preserving its bio-active properties was investigated. Our results indicated that storage conditions under controlled atmosphere for 30 days was able to enhance mitochondrial respiration at the same extent than freshly extracted PJ. Conversely, freezing procedure, though retaining the antioxidant and cell-growth inhibitory property, elicited an opposite effect on the metabolic profile as compared with fresh extract. CONCLUSION: Overall, the results of our study, on the one hand, confirms the preventive/therapeutic potential of PJ, as well as of its post-harvested processing, for cancer management. On the other hand, it highlights the intrinsic difficulties in attaining mechanistic insights when a multiplicity of effects is elicited by a crude mixture of bio-active compounds.


Assuntos
Punica granatum , Células MDA-MB-231 , Espécies Reativas de Oxigênio , Oxirredução , Proliferação de Células , Antioxidantes/farmacologia , Cafeína , Metaboloma , Misturas Complexas
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