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1.
Cent Nerv Syst Agents Med Chem ; 23(2): 126-136, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37608652

RESUMO

BACKGROUND: The primary phytoconstituents reported to have neuroprotective effects are flavonoids and phenolic compounds. Aerva persica roots are reported to be rich in flavonoids and phenolic compounds. Therefore, this study aimed to explore the nootropic potential of Aerva persica roots. OBJECTIVE: The objective of this study was to evaluate the nootropic potential of Aerva persica roots against D-galactose-induced memory impairment. METHODS: In this study, the roots of Aerva persica were extracted with 70% ethanol. The obtained extract was evaluated for total phenolic content using the Folin-Ciocalteu method and total flavonoid content using the aluminium chloride colorimetric assay. Afterward, the acute oral toxicity of the extract was determined following the Organisation for Economic Co-operation and Development (OECD) guideline 423. Additionally, two doses of Aerva persica (100 and 200 mg/kg body weight (BW)) were evaluated for their nootropic potential against D-galactose-induced memory impairment. The nootropic potential of the crude extract was assessed through a behavioural study and brain neurochemical analysis. Behavioural studies involved the evaluation of spatial reference- working memory using the radial arm maze test and the Y-maze test. Neurochemical analysis was performed to determine the brain's acetylcholine, acetylcholinesterase, glutathione (GSH), and malondialdehyde (MDA) levels. RESULTS: The total phenolic content and total flavonoid content were found to be 179.14 ± 2.08 µg GAE/mg and 273.72 ± 3.94 µg QE/mg, respectively. The Aerva persica extract was found to be safe up to 2000 mg/kg BW. Following the safety assessment, the experimental mice received various treatments for 14 days. The behavioural analysis using the radial maze test showed that the extract at both doses significantly improved spatial reference-working memory and reduced the number of total errors compared to disease control groups. Similarly, in the Y-maze test, both doses significantly increased the alteration percentage and the percentage of novel arm entry (both indicative of intact spatial memory) compared to disease control. In neurochemical analysis, Aerva persica at 200 mg/kg significantly normalised the acetylcholine level (p<0.0001) and GSH level (p<0.01) compared to disease control. However, the same effect was not observed with Aerva persica at 100 mg/kg. Additionally, Aerva persica at 200mg/kg BW significantly decreased the acetylcholinesterase level (p<0.0001) and decreased the brain's MDA level (p<0.01) compared to the disease control, whereas the effect of Aerva persica at 100 mg/kg BW in reducing acetylcholinesterase was non-significant. CONCLUSION: Based on the results, it can be concluded that the nootropic potential of Aerva persica was comparable to that of the standard drug, Donepezil, and the effect might be attributed to the higher content of flavonoids and phenolic compounds.


Assuntos
Amaranthaceae , Nootrópicos , Camundongos , Animais , Nootrópicos/farmacologia , Galactose/toxicidade , Acetilcolinesterase , Acetilcolina/efeitos adversos , Transtornos da Memória/induzido quimicamente , Transtornos da Memória/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Glutationa/efeitos adversos , Etanol , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Aprendizagem em Labirinto
2.
Gels ; 8(10)2022 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-36286177

RESUMO

Hydrogels can provide instant relief to pain and facilitate the fast recovery of wounds. Currently, the incorporation of medicinal herbs/plants in polymer matrix is being investigated due to their anti-bacterial and wound healing properties. Herein, we investigated the novel combination of chitosan (CS) and chondroitin sulfate (CHI) to synthesize hydrogels through freeze gelation process and enriched it with garlic (Gar) by soaking the hydrogels in garlic juice for faster wound healing and resistance to microbial growth at the wound surface. The synthesized hydrogels were characterized via Fourier-transform infrared spectroscopy (FTIR), which confirmed the presence of relevant functional groups. The scanning electron microscopy (SEM) images exhibited the porous structure of the hydrogels, which is useful for the sustained release of Gar from the hydrogels. The synthesized hydrogels showed significant inhibition zones against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). Furthermore, cell culture studies confirmed the cyto-compatibility of the synthesized hydrogels. Thus, the novel hydrogels presented in this study can offer an antibacterial effect during wound healing and promote tissue regeneration.

3.
Curr Drug Metab ; 23(6): 447-459, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35676849

RESUMO

At present, people and patients worldwide are relying on the medicinal plant as a therapeutic agent over pharmaceuticals because the medicinal plant is considered safer, especially for chronic disorders. Several medicinal plants and their components are being researched and explored for their possible therapeutic contribution to CNS disorders. Thymoquinone (TQ) is one such molecule. Thymoquinone, one of the constituents of Plant Nigella Sativa, is effective against several neurodegenerative diseases like, Alzheimer's, Depression, Encephalomyelitis, Epilepsy, Ischemia, Parkinson's, and Traumatic. This review article presents the neuropharmacological potential of TQ's, their challenges, and delivery prospects, explicitly focusing on neurological disorders along with their chemistry, pharmacokinetics, and toxicity. Since TQ has some pharmacokinetic challenges, scientists have focused on novel formulations and delivery systems to enhance bioavailability and ultimately increase its therapeutic value. In the present work, the role of nanotechnology in neurodegenerative disease and how it improves the bioavailability and delivery of a drug to the site of action has been discussed. There are a few limitations to developing novel drug formulations, including solubility, pH, and compatibility of nanomaterials. Since here we are targeting CNS disorders, the bloodbrain barrier (BBB) becomes an additional challenge. Hence, the review summarized the novel aspects of delivery and biocompatible nanoparticles-based approaches for targeted drug delivery into CNS, enhancing TQ bioavailability and its neurotherapeutic effects.


Assuntos
Doenças do Sistema Nervoso Central , Doenças Neurodegenerativas , Nigella sativa , Plantas Medicinais , Benzoquinonas/farmacologia , Benzoquinonas/uso terapêutico , Doenças do Sistema Nervoso Central/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Humanos , Doenças Neurodegenerativas/tratamento farmacológico , Nigella sativa/química
4.
Molecules ; 27(4)2022 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-35209242

RESUMO

The objective of the current research is to develop ZnO-Manjistha extract (ZnO-MJE) nanoparticles (NPs) and to investigate their transdermal delivery as well as antimicrobial and antioxidant activity. The optimized formulation was further evaluated based on different parameters. The ZnO-MJE-NPs were prepared by mixing 10 mM ZnSO4·7H2O and 0.8% w/v NaOH in distilled water. To the above, a solution of 10 mL MJE (10 mg) in 50 mL of zinc sulfate was added. Box-Behnken design (Design-Expert software 12.0.1.0) was used for the optimization of ZnO-MJE-NP formulations. The ZnO-MJE-NPs were evaluated for their physicochemical characterization, in vitro release activity, ex vivo permeation across rat skin, antimicrobial activity using sterilized agar media, and antioxidant activity by the DPPH free radical method. The optimized ZnO-MJE-NP formulation (F13) showed a particle size of 257.1 ± 0.76 nm, PDI value of 0.289 ± 0.003, and entrapment efficiency of 79 ± 0.33%. Drug release kinetic models showed that the formulation followed the Korsmeyer-Peppas model with a drug release of 34.50 ± 2.56 at pH 7.4 in 24 h. In ex vivo studies ZnO-MJE-NPs-opt permeation was 63.26%. The antibacterial activity was found to be enhanced in ZnO-MJE-NPs-opt and antioxidant activity was found to be highest (93.14 ± 4.05%) at 100 µg/mL concentrations. The ZnO-MJE-NPs-opt formulation showed prolonged release of the MJE and intensified permeation. Moreover, the formulation was found to show significantly (p < 0.05) better antimicrobial and antioxidant activity as compared to conventional suspension formulations.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Nanopartículas Metálicas/química , Extratos Vegetais/química , Rubia/química , Pele/efeitos dos fármacos , Óxido de Zinco/química , Animais , Anti-Infecciosos/química , Antioxidantes/química , Fenômenos Químicos , Química Farmacêutica , Composição de Medicamentos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Testes de Sensibilidade Microbiana , Modelos Químicos , Ratos , Pele/metabolismo , Análise Espectral
5.
Nutrients ; 13(10)2021 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-34684454

RESUMO

The microecological environment of the gastrointestinal tract is altered if there is an imbalance between the gut microbiota phylases, resulting in a variety of diseases. Moreover, progressive age not only slows down physical activity but also reduces the fat metabolism pathway, which may lead to a reduction in the variety of bacterial strains and bacteroidetes' abundance, promoting firmicutes and proteobacteria growth. As a result, dysbiosis reduces physiological adaptability, boosts inflammatory markers, generates ROS, and induces the destruction of free radical macromolecules, leading to sarcopenia in older patients. Research conducted at various levels indicates that the microbiota of the gut is involved in pathogenesis and can be considered as the causative agent of several cardiovascular diseases. Local and systematic inflammatory reactions are caused in patients with heart failure, as ischemia and edema are caused by splanchnic hypoperfusion and enable both bacterial metabolites and bacteria translocation to enter from an intestinal barrier, which is already weakened, to the blood circulation. Multiple diseases, such as HF, include healthy microbe-derived metabolites. These key findings demonstrate that the gut microbiota modulates the host's metabolism, either specifically or indirectly, by generating multiple metabolites. Currently, the real procedures that are an analogy to the symptoms in cardiac pathologies, such as cardiac mass dysfunctions and modifications, are investigated at a minimum level in older patients. Thus, the purpose of this review is to summarize the existing knowledge about a particular diet, including trimethylamine, which usually seems to be effective for the improvement of cardiac and skeletal muscle, such as choline and L-carnitine, which may aggravate the HF process in sarcopenic patients.


Assuntos
Carnitina/efeitos adversos , Colina/efeitos adversos , Suplementos Nutricionais , Insuficiência Cardíaca/epidemiologia , Insuficiência Cardíaca/etiologia , Sarcopenia/complicações , Sarcopenia/epidemiologia , Biodiversidade , Biomarcadores , Carnitina/administração & dosagem , Colina/administração & dosagem , Suplementos Nutricionais/efeitos adversos , Suscetibilidade a Doenças , Disbiose , Microbioma Gastrointestinal , Insuficiência Cardíaca/metabolismo , Humanos , Metilaminas/administração & dosagem , Metilaminas/efeitos adversos , Sarcopenia/diagnóstico , Sarcopenia/etiologia
6.
Curr Drug Metab ; 21(9): 661-673, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32445453

RESUMO

Herbal medicines are being used since ancient times and are an important part of the alternative and traditional medicinal system. In recent decades, scientists are embracing herbal medicines based on the fact that a number of drugs that are currently in use are derived directly or indirectly from plant sources. Moreover, herbal drugs have lesser side effects, albeit are potentially strong therapeutic agents. The herbal medicine market is estimated to be around US $62 billion globally. Herbal medicine has gained widespread acceptance due to its low toxicity, low cost, ease of accessibility and efficacy in treating difficult diseases. Safety and efficacy are another important factors in the commercialization process of herbal medicines. Nanotechnology has been shown to be potentially effective in improving the bioactivity and bioavailability of herbal medicines. Development of nano-phytomedicines (or by reducing the size of phytomedicine), attaching polymers with phytomedicines and modifying the surface properties of herbal drugs, have increased the solubility, permeability and eventually the bioavailability of herbal formulations. Novel formulations such as niosomes, liposomes, nanospheres, phytosomes etc., can be exploited in this area. This article reviews herbal medicines, which have prominent activity in the Central Nervous System (CNS) disorders and reported nano-phytomedicines based delivery systems.


Assuntos
Doenças do Sistema Nervoso Central/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Fitoterapia , Animais , Humanos , Nanomedicina
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