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1.
Saudi Pharm J ; 32(4): 101998, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38414781

RESUMO

Boesenbergia rotunda (L.) comprises bioactive compounds with biological and pharmacological properties, especially flavonoid compounds with osteoblastogenesis-stimulating potential. However, the application of B. rotunda in the food and pharmaceutical industry is restricted by its low solubility and stability. Encapsulation becomes an alternative to overcome these restrictions. The purpose study was to encapsulate B. rotunda extract by freeze-drying and to investigate the effects of different wall materials (maltodextrin (MD), gum arabic (GA), and their combination (MDGA)) and extract contents on the physicochemical, bioactive properties and in vitro enhancement of osteogenesis of MC3T3-E1 cells of the obtained encapsulates. The results revealed that encapsulated B. rotunda can reduce cytotoxicity, enhance biological activity, and maintain the stability of bioactive compounds. The MD was a good wall material for yield percentage. However, the values of moisture content Aw, and solubility among all the encapsulated powders were no significant differences, with all encapsulated powders having similar structures based on scanning electron microscopy. Fourier transform infrared spectroscopy confirmed the extract was encapsulated by the selected wall materials. Combining the MD and GA encapsulation agents afforded the best protection of the bioactive compounds, increasing EE (MDGA-7 > MDGA-5), pinostrobin content, TPC, and antioxidant activities (MDGA-5 > MDGA-7). The MDGA-5 and MDGA-7 at 10-50 µg/mL were not toxic to cells and promoted MC3T3-E1 cell viability, while also enhancing the Alkaline phosphatase activity, and promoting matrix mineralization of pre-osteoblast MC3T3-E1 cells after 21 and 28 days. This result showed that MDGA was a suitable wall material for B. rotunda encapsulations and a potential source of bioactive ingredients that could applied in food or pharmaceutical products for osteoporosis prevention.

2.
Sci Rep ; 13(1): 21690, 2023 12 07.
Artigo em Inglês | MEDLINE | ID: mdl-38066118

RESUMO

Traditional remedies using natural ingredients have been handed down over generations, providing collective information for the development of modern therapeutics. These natural products have a long history of safe consumption with curative effects but lack of scientific-based evidence hinders the mass production of new remedies containing active ingredients with particular medicinal properties. This research investigated the phenolic profiles and biochemical properties of 29 herbal ingredients identified in two traditional Thai remedies, Prasachandaeng (PSCD) and Chantaharuethai (CHRT), and their effectiveness in combating chronic diseases. These two traditional remedies are used to reduce fever but some ingredients have been previously reported to possess other health-related properties. Statistical analysis by TOPSIS indicated that Biancaea sappan (L.) Tod. extract exhibited the highest overall closeness coefficient (C) score analyzed from all variables including total phenolic contents, antioxidant potentials, and enzyme inhibitions. Bouea macrophylla Griff. extract showed potential as an effective agent against diabetes through inhibition of two carbohydrate degrading enzymes, α-glucosidase and α-amylase, while Dischidia major (Vahl) Merr. showed strong properties as an anti-angiotensin-converting enzyme, leading to the control of hypertension. Dracaena cochinchinensis (Lour.) S.C. Chen effectively controlled the progression of Alzheimer's disease through the inhibition of cholinergic and ß-amyloid formation enzymes. These results can be used as preliminary data for the development of new remedies to prevent or treat particular chronic diseases.


Assuntos
Apocynaceae , Tailândia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , alfa-Amilases , Antioxidantes/farmacologia
3.
Plants (Basel) ; 12(7)2023 Mar 24.
Artigo em Inglês | MEDLINE | ID: mdl-37050065

RESUMO

Sacred lotus (Nelumbo nucifera) is a commercial product in Asian countries. Almost all parts of the lotus plant are consumed as food or used as traditional medicine due to their high contents of secondary metabolites such as phenolics and alkaloids. However, agricultural management of the sacred lotus occurs during the rainy season, and the plant enters a resting stage during the dry season. Thus, seasonal variation (beginning, middle and end of the rainy season) was investigated for total phenolic contents (TPCs), antioxidant capacities and inhibitions of the key enzymes relevant to chronic diseases including Alzheimer's disease (ß-secretase, acetylcholinesterase and butyrylcholinesterase), hypertension (angiotensin-converting enzyme), obesity (lipase) and diabetes (α-glucosidase) of different sacred lotus parts (seed embryo, petal, stamen, old leaf, leaf stalk and flower stalk). Results indicated that an aqueous extract of stamen in all harvesting seasons exhibited potentially high TPCs, which led to high antioxidant activities and most enzyme inhibitions (up to 53.7-fold higher) than the others collected in the same harvesting period. The phenolic content and biochemical activities in stamen harvested at the beginning of the rainy season were up to 4-fold higher than during other harvesting periods. This information benefits the agricultural management of sacred lotus and supports consumption of different sacred lotus parts for health promotion. Results can be used as an initial database for future product development from different sacred lotus parts.

4.
Pharmaceuticals (Basel) ; 15(5)2022 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-35631418

RESUMO

Alzheimer's disease (AD) is a progressive neurological illness with few effective treatments. Thus, ameliorating the effects of AD using natural products has attracted global attention with promising efficacy and safety. In this study, ten tropical fruits including Ananas comosus 'Phulae', Ananas comosus 'Pattavia', Carica papaya 'Khaekdum', Carica papaya 'Khaeknuan', Durio zibethinus 'Monthong', Durio zibethinus 'Chanee', Psidium guajava 'Kimju', Psidium guajava 'Keenok', Mangifera indica 'Kaew' and Mangifera indica 'Namdokmai' were screened for their inhibitory activities against the key enzymes, cholinesterases and ß-secretase (BACE-1), involved in AD pathogenesis. The top three fruit extracts with promising in vitro anti-AD activities were further investigated using rat pheochromocytoma PC-12 neuronal cell line and Drosophila AD model. Data showed that M. indica 'Kaew', M. indica 'Namdokmai' and P. guajava 'Kimju' reduced Aß1-42-mediated neurotoxicity by promoting glutathione-dependent enzymes, while M. indica 'Namdokmai' limited Aß1-42 peptide formation via BACE-1 inhibition and amended locomotory behavior of the Drosophila AD model. Results indicated the potential anti-AD properties of tropical fruits, particularly M. indica 'Namdokmai' in the prevention of Aß1-42-mediated neurotoxicity and as a BACE-1 blocker.

5.
Foods ; 10(11)2021 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-34828882

RESUMO

Thailand is located in the tropics and a wide variety of fruits are grown commercially. However, studies regarding the phytonutrients, anti-mutagenic and chemopreventive effects of these fruits are limited. Thus, phytochemical profiles and inhibition of key enzymes involved in obesity and diabetes, together with anti-mutagenic and chemopreventive properties of eight tropical fruit extracts cultivated in Thailand, including Psidium guajava 'Kimju', Psidium guajava 'Keenok', Ananas comosus 'Pattavia', Ananas comosus 'Phulae', Durio zibethinus 'Chanee', Durio zibethinus 'Monthong', Carica papaya 'Khaekdum' and Mangifera indica 'Namdokmai' were investigated. Different cultivars were also compared. Results showed that M. indica 'Namdokmai' was the most antioxidant-rich extract containing abundant 4-hydroxybenzoic acid and its derivative, gallic acid, as the main phenolics. M. indica 'Namdokmai' also exhibited high inhibitory capacities (>60% inhibition under studied conditions) against lipase, α-amylase and α-glucosidase, key enzymes as drug targets for controlling obesity and type 2 diabetes. Interestingly, all fruit extracts suppressed food mutagen-induced DNA mutations assayed by the Ames test, especially M. indica 'Namdokmai' and C. papaya 'Khaekdum' (>50% inhibition at 200 µg/plate). The M. indica 'Namdokmai' was also the most potent extract for suppression of cancer promotion (>90% inhibition at 200 µg/mL) followed by P. guajava 'Kimju', P. guajava 'Keenok' and C. papaya 'Khaekdum'. Results potentially indicated that fruit intake after overcooked meat consumption might supplement nutrients and fiber and also reduce DNA mutation sources.

6.
Molecules ; 25(16)2020 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-32824050

RESUMO

Sacred lotus (Nelumbo nucifera) has long been used as a food source and ingredient for traditional herbal remedies. Plant parts contain neuroprotective agents that interact with specific targets to inhibit Alzheimer's disease (AD). Organic solvents including methanol, ethyl acetate, hexane, and n-butanol, are widely employed for extraction of sacred lotus but impact food safety. Seed embryo, flower stalk, stamen, old leaf, petal, and leaf stalk of sacred lotus were extracted using hot water (aqueous extraction). The extractions were analyzed for their bioactive constituents, antioxidant and anti-AD properties as key enzyme inhibitory activities toward acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and ß-secretase 1 (BACE-1). Results showed that the sacred lotus stamen exhibited significant amounts of phenolics, including phenolic acids and flavonoids, that contributed to high antioxidant activity via both single electron transfer (SET) and hydrogen atom transfer (HAT) mechanisms, with anti-AChE, anti-BChE, and anti-BACE-1 activities. To enhance utilization of other sacred lotus parts, a combination of stamen, old leaf and petal as the three sacred lotus plant components with the highest phenolic contents, antioxidant activities, and enzyme inhibitory properties was analyzed. Antagonist interaction was observed, possibly from flavonoids-flavonoids interaction. Further in-depth elucidation of this issue is required. Findings demonstrated that an aqueous extract of the stamen has potential for application as a functional food to mitigate the onset of Alzheimer's disease.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Nelumbo/química , Fenóis/análise , Extratos Vegetais/farmacologia , Folhas de Planta/química , Acetilcolinesterase , Doença de Alzheimer/enzimologia , Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Butirilcolinesterase/química , Proteínas Ligadas por GPI/antagonistas & inibidores , Humanos
7.
Molecules ; 25(11)2020 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-32503261

RESUMO

Alzheimer's disease (AD) is a progressive neurodegenerative disorder. To fight the disease, natural products, including mulberry, with antioxidant activities and inhibitory activities against key enzymes (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1)) are of interest. However, even in the same cultivars, mulberry trees grown in different populated locations might possess disparate amounts of phytochemical profiles, leading to dissimilar health properties, which cause problems when comparing different cultivars of mulberry. Therefore, this study aimed to comparatively investigate the phytochemicals, antioxidant activities, and inhibitory activities against AChE, BChE, and BACE-1, of twenty-seven Morus spp. cultivated in the same planting area in Thailand. The results suggested that Morus fruit samples were rich in phenolics, especially cyanidin, kuromanin, and keracyanin. Besides, the aqueous Morus fruit extracts exhibited antioxidant activities, both in single electron transfer (SET) and hydrogen atom transfer (HAT) mechanisms, while strong inhibitory activities against AD key enzymes were observed. Interestingly, among the twenty-seven Morus spp., Morus sp. code SKSM 810191 with high phytochemicals, antioxidant activities and in vitro anti-AD properties is a promising cultivar for further developed as a potential mulberry resource with health benefits against AD.


Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Morus/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Acetilcolinesterase , Doença de Alzheimer/prevenção & controle , Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Butirilcolinesterase/química , Proteínas Ligadas por GPI/antagonistas & inibidores , Humanos
8.
Molecules ; 25(8)2020 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-32316271

RESUMO

Alzheimer's disease (AD) is the most common form of dementia, characterized by chronic neuron loss and cognitive problems. Aggregated amyloid beta (Aß) peptides, a product of cleaved amyloid precursor protein (APP) by beta-secretase 1 (BACE-1), have been indicated for the progressive pathogenesis of AD. Currently, screening for anti-AD compounds in foodstuffs is increasing, with promising results. Hence, the purpose of this study was to investigate the extraction conditions, phytochemical contents, and anti-AD properties, targeting Aß peptides of Morus cf. nigra 'Chiang Mai' (MNCM) both in vitro and in vivo. Data showed that the aqueous extract of MNCM contained high amounts of cyanidin, keracyanin, and kuromanin as anthocyanidin and anthocyanins. The extract also strongly inhibited cholinesterases and BACE-1 in vitro. Moreover, MNCM extract prevented Aß-induced neurotoxicity and promoted neurite outgrowth in neuronal cells. Interestingly, MNCM extract reduced Aß1-42 peptides and improved locomotory coordination of Drosophila co-expressing human APP and BACE-1, specifically in the brain. These findings suggest that MNCM may be useful as an AD preventive agent by targeting Aß formation.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Peptídeos beta-Amiloides/toxicidade , Antocianinas/administração & dosagem , Antioxidantes/administração & dosagem , Morus/química , Doença de Alzheimer/induzido quimicamente , Doença de Alzheimer/metabolismo , Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Secretases da Proteína Precursora do Amiloide/metabolismo , Animais , Antocianinas/isolamento & purificação , Antocianinas/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Colinesterases/metabolismo , Modelos Animais de Doenças , Drosophila , Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos , Humanos , Células PC12 , Compostos Fitoquímicos/química , Ratos
9.
Food Sci Biotechnol ; 28(2): 529-537, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30956865

RESUMO

This study aimed to investigate the effects of phospholipid composition on the properties and bioavailability of astaxanthin-loaded liposomes using cell culture. Two mixtures of phospholipids with different proportions of phosphatidylcholine (PC, 23% and 70%) were used at various concentrations (0.8, 1.6, and 2.0% w/v) to prepare astaxanthin-loaded liposomes, which were investigated for entrapment efficiency (EE), antioxidant activity, morphology and changes in astaxanthin properties during a storage period of 8 weeks at 4 °C. Furthermore, Caco-2 human colon adenocarcinoma cells were employed to examine the cellular uptake of astaxanthin-loaded liposomes. The highest EE was observed with astaxanthin-loaded liposomes containing 70% PC, and used at the concentration of 2.0% w/v. Liposomes maintained the antioxidant activity of astaxanthin. All liposomal preparations were non-toxic. Cellular uptake of astaxanthin-loaded liposomes containing 70% PC was significantly higher than that of 23% PC-containing liposomes (p < 0.05).

10.
Fitoterapia ; 82(7): 1093-101, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21787849

RESUMO

The present study investigated the cytotoxicity of enhydrin (1), uvedalin (2) and sonchifolin (3) in cervical cancer cells. We have found that SLs 1-3 in doses in range of 0.22-10 µM inhibited cell proliferation and induced apoptosis in both a dose- and time-dependent fashion. A significant cell death induction was supported by morphological studies. The apoptotic effect is associated with caspase-3/7 activation and NF-кB inhibition. Interestingly, enhydrin possessing two epoxide units was found to be the most cytotoxic compound. Therefore it can be assumed that number of epoxides and existence of α-methylene-γ-lactone moiety are essential for the acceleration of apoptosis.


Assuntos
Apoptose/efeitos dos fármacos , Asteraceae/química , Compostos de Epóxi/uso terapêutico , Lactonas/uso terapêutico , NF-kappa B/antagonistas & inibidores , Fitoterapia , Neoplasias do Colo do Útero/tratamento farmacológico , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/uso terapêutico , Caspase 3/metabolismo , Caspase 7/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Compostos de Epóxi/farmacologia , Feminino , Humanos , Lactonas/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Folhas de Planta , Sesquiterpenos/uso terapêutico , Neoplasias do Colo do Útero/metabolismo
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