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1.
Biomed Chromatogr ; 38(9): e5936, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38956791

RESUMO

Mangifera indica peels are a rich source of diverse flavonoids and xanthonoids; however, generally these are discarded. Computational studies revealed that mangiferin significantly interacts with amino acid residues of transcriptional regulators 1IK3, 3TOP, and 4f5S. The methanolic extract of Langra variety of mangoes contained the least phenol concentrations (22.6 ± 0.32 mg/gGAE [gallic acid equivalent]) compared to the chloroform (214.8 ± 0.12 mg/gGAE) and ethyl acetate fractions (195.6 ± 0.14 mg/gGAE). Similarly, the methanolic extract of Sindhri variety contained lower phenol concentrations (42.3 ± 0.13 mg/gRUE [relative utilization efficiency]) compared with the chloroform (85.6 ± 0.15 mg/gGAE) and ethyl acetate (76.1 ± 0.32 mg/gGAE) fractions. Langra extract exhibited significant α-glucosidase inhibition (IC50 0.06 mg/mL), whereas the ethyl acetate fraction was highly active (IC50 0.12 mg/mL) in Sindhri variety. Mangiferin exhibited significant inhibition (IC50 0.026 mg/mL). A moderate inhibition of 15-LOX was observed in all samples, whereas mangiferin was least active. In advanced glycation end product inhibition assay, the chloroform fraction of Langra variety exhibited significant inhibition in nonoxidative (IC50 64.4 µg/mL) and oxidative modes (IC50 54.7 µg/mL). It was concluded that both Langra and Sindhri peel extracts and fractions possess significant antidiabetic activities. The results suggest the potential use of peel waste in the management and complications of diabetes.


Assuntos
Antioxidantes , Produtos Finais de Glicação Avançada , Hipoglicemiantes , Mangifera , Extratos Vegetais , Xantonas , Xantonas/química , Xantonas/farmacologia , Xantonas/análise , Mangifera/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/análise , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Produtos Finais de Glicação Avançada/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Simulação de Acoplamento Molecular , Frutas/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/análise , Simulação por Computador
2.
Biomed Chromatogr ; 38(9): e5950, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38973522

RESUMO

Litchi chinensis Sonn (Litchi) has been listed in the Chinese Pharmacopeia, and is an economically and medicinally valuable species within the family Sapindaceae. However, the material basis of its pharmacological action and the pharmacodynamic substances associated with its hypoglycemic effect are still unclear. The predominant objective of this study was to establish the fingerprint profile of litchi leaves and to evaluate the relationship between the components of the high-performance liquid chromatography (HPLC) fingerprint of litchi leaves, assess its hypoglycemic effect by measuring α-glucosidase and α-amylase inhibition, and find the spectrum-effect relationship of litchi leaves by bivariate correlation analysis, Grey relational analysis and partial least squares regression analysis. In this study, the fingerprint of litchi leaves was established by HPLC, and a total of 15 common peaks were identified that clearly calibrated eight components, with P1 being gallic acid, P2 being protocatechuic acid, P3 being catechin, P6 being epicatechin, P12 being rutin, P13 being astragalin, P14 being quercetin and P15 being kaempferol. The similarities between the fingerprints of 11 batches of litchi leaves were 0.766-0.979. Simultaneously, the results of the spectrum-effect relationship showed that the chemical constituents represented by peaks P8, P3, P12, P14, P2, P13, and P11 were relevant to the hypoglycemic effect.


Assuntos
Hipoglicemiantes , Litchi , Extratos Vegetais , Folhas de Planta , Litchi/química , Folhas de Planta/química , Cromatografia Líquida de Alta Pressão/métodos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/análise
3.
J Food Sci ; 89(6): 3430-3444, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38638068

RESUMO

The utilization of coffee leaves in kombucha production has intrigued researchers; however, the lack of understanding regarding the characteristics of coffee leaf kombucha (CK) and its differentiation from black tea kombucha (BK) has impeded its application in the beverage industry. Therefore, this study aimed to characterize and compare the physiochemical properties, phytochemical compositions, antioxidant activity, and α-glucosidase inhibitory ability of kombucha prepared from the leaves of Coffea arabica (CK) and black tea (Camellia sinensis, BK) and their extracts (CT and BT). After fermentation, pH and the contents of total sugars, reducing sugars, and free amino acids of BK and CK were decreased, whereas the levels of total acids and organic acids, such as gluconic, lactic, and acetic acid were increased. Notably, the concentration of vitamin C in CK was 48.9% higher than that in BK. HPLC analysis exhibited that 5-caffeoylquinic acid in CT was significantly decreased by 48.0% in CK, whereas the levels of 3-caffeoylquinic acid and 4-caffeoylquinic acid were significantly increased after fermentation. The content of caffeine was significantly (p < 0.05) reduced by 9.5% and 22.0% in BK and CK, respectively, whereas the theobromine level was significantly increased in CK. Notably, CK has superior total phenolic and flavonoid contents and antioxidant activity than BK, whereas BK possesses higher α-glucosidase inhibitory capacity. Electronic nose analysis demonstrated that sulfur-containing organics were the main volatiles in both kombuchas, and fermentation significantly increased their levels. Our study indicates that coffee leaves are a promising resource for preparing kombucha. PRACTICAL APPLICATION: This article investigates the differences in physicochemical properties, bioactive constituents, antioxidant activity, and α-glucosidase inhibitory activity of kombucha preparation from black tea and coffee leaves. We have found that after fermentation BK had brighter soup color and higher α-glucosidase inhibitory capacity, whereas CK had higher levels of total phenols, flavonoids, vitamin C, and antioxidants and lower contents of sugars. This study provides valuable information for the preparation of CK with high-quality attributes and antioxidant activity.


Assuntos
Antioxidantes , Camellia sinensis , Coffea , Extratos Vegetais , Folhas de Planta , Folhas de Planta/química , Antioxidantes/análise , Coffea/química , Camellia sinensis/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Fermentação , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/análise , Chá de Kombucha/análise , Café/química , Compostos Fitoquímicos/análise , Chá/química , Ácido Ascórbico/análise , Fenóis/análise , Cafeína/análise , Ácido Quínico/análogos & derivados , Ácido Quínico/análise , Flavonoides/análise
4.
Plant Foods Hum Nutr ; 79(2): 381-386, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38436827

RESUMO

Edgeworthia gardneri (Wall.) Meisn., a member of the genus Edgeworthia in the family Thymelaeaceae, has long been applied as an edible and medicinal plant in China. E. gardneria has a hypoglycemic effect and is used to prepare daily drinks for the prevention and treatment of diabetes. However, the hypoglycemic substances involved remain unknown. The present study aimed to screen the α-glucosidase-inhibitors of E. gardneri and analyze its chemical profile using a ultraperformance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS/MS) method. As a result, the ethyl acetate fraction (EAF) had significant α-glucosidase-inhibitory and antioxidant activities but did not show an α-amylase-inhibitory activity. A total of 67 compounds were identified in the EAF by UPLC-Q-TOF-MS/MS analysis; among them, 48 compounds were first discovered in the genus Edgeworthia. Additionally, five flavonoids, namely, isoorintin, secoisolaricirinol, tiliroside, chrysin, and kaempferol, had α-glucosidase-inhibitory activities. Rutin had a α-amylase-inhibitory activity. Daphnoretin, a kind of coumarin, has α-glucosidase and α-amylase-inhibitory activities. These findings enrich the chemical library of E. gardneria. EAF has a selective α-glucosidase-inhibitory activity, and flavonoids and coumarins may be the active components of EAF. E. gardneria has important value for developing multiple-target hypoglycemic drugs.


Assuntos
Antioxidantes , Flavonoides , Inibidores de Glicosídeo Hidrolases , Hipoglicemiantes , Espectrometria de Massas em Tandem , Thymelaeaceae , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/farmacologia , Espectrometria de Massas em Tandem/métodos , Thymelaeaceae/química , Hipoglicemiantes/análise , Hipoglicemiantes/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/análise , Antioxidantes/análise , Antioxidantes/farmacologia , alfa-Glucosidases , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/análise , alfa-Amilases/antagonistas & inibidores , China
5.
Molecules ; 28(10)2023 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-37241909

RESUMO

Polygoni Cuspidati Rhizoma et Radix (PCR), the rhizome and root of Polygonum cuspidatum Sieb. et Zucc., has been used as an herbal medicine for a long time. In this study, the ultrafiltration combined with high performance liquid chromatography (UF-HPLC) method was developed to screen tyrosinase (TYR), α-glucosidase (α-GLU), and xanthine oxidase (XOD) inhibitors from PCR. Firstly, the inhibitory activity of 50% methanol PCR extract on TYR, α-GLU, XOD, and acetylcholinesterase (ACHE) was tested. The extract showed a good inhibition on the enzymes, except for ACHE. Therefore, UF-HPLC experiments were carried out to screen TYR, α-GLU, and XOD inhibitors from PCR extract. Seven potential bioactive components were discovered, including methylgallate (1), 1,6-di-O-galloyl-D-glucose (2), polydatin-4'-O-D-glucoside (3), resveratrol-4'-O-D-glucoside (4), polydatin (5), malonyl glucoside resveratrol (6), and resveratrol-5-O-D-glucoside (7). Most of them were found as enzyme inhibitors from PCR for the first time, except polydatin (5), which had been reported as an α-GLUI in PCR in the literature. Finally, molecular docking analysis was applied to validate the interactions of these seven potential active components with the enzymes. Compounds 1-7 were proven as TYR inhibitors, compounds 2, 4-7 were identified as XOD inhibitors, and compounds 4-6 were confirmed as α-GLU inhibitors. In short, the current study provides a good reference for the screening of enzyme inhibitors through UF-HPLC, and provides scientific data for future studies of PCR.


Assuntos
Medicamentos de Ervas Chinesas , Rizoma , Rizoma/química , Monofenol Mono-Oxigenase , Medicamentos de Ervas Chinesas/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/análise , Cromatografia Líquida de Alta Pressão/métodos , Xantina Oxidase , Resveratrol/análise , Acetilcolinesterase , Simulação de Acoplamento Molecular , Ultrafiltração , Glucosídeos/análise
6.
Biomed Chromatogr ; 37(3): e5571, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36520456

RESUMO

Morus alba leaves are a natural product with great antidiabetic potential. However, the therapeutic efficacy of natural products is usually achieved through the interaction of active compounds with specific targets. Among them, active compounds with multi-target therapeutic functions are more effective than single-target enzymes. In this study, a bienzyme system was constructed by co-immobilizing α-amylase and α-glucosidase onto Fe3 O4 for affinity screening of dual-target active components in the complex extract from M. alba leaves. As a result, a potential active compound was selectively screened by ligand fishing, separated by high-speed countercurrent chromatography using a solvent system of ethyl acetate-n-butanol-water (3:2:5, v/v), and identified as rutin. In addition, the result of molecular docking showed that rutin could interact with the active center of α-amylase and α-glucosidase through multiple hydrogen bonds, van der Waals forces, etc. to play an inhibitory role. These results demonstrate the effectiveness of the polydopamine magnetically immobilized bienzyme system for dual-target affinity screening of active substances. This study not only reveals the chemical basis of the antidiabetic activity of M. alba leaves from a dual-target perspective, but also promotes the progress of multitarget affinity screening.


Assuntos
Inibidores de Glicosídeo Hidrolases , Morus , Inibidores de Glicosídeo Hidrolases/análise , Extratos Vegetais/química , Enzimas Imobilizadas/análise , alfa-Glucosidases , alfa-Amilases/análise , Simulação de Acoplamento Molecular , Hipoglicemiantes/análise , Rutina/análise , Fenômenos Magnéticos , Morus/química , Folhas de Planta/química
7.
Braz. j. biol ; 83: 1-9, 2023. graf, tab
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1468957

RESUMO

Allium cepa L. is a commonly consumed vegetable that belongs to the Amaryllidaceae family and contains nutrients and antioxidants in ample amounts. In spite of the valuable food applications of onion bulb, its peel and outer fleshy layers are generally regarded as waste and exploration of their nutritional and therapeutic potential is still in progress with a very slow progression rate. The present study was designed with the purpose of doing a comparative analysis of the antioxidant potential of two parts of Allium cepa, i.g., bulb (edible part) and outer fleshy layers and dry peels (inedible part). Moreover, the inhibitory effect of the onion bulb and peel extracts on rat intestinal α-glucosidase and pancreatic α-amylase of porcine was also evaluated. The antioxidant potential of onion peel and bulb extracts were evaluated using 2,2-diphenyl- 1-picryl hydrazyl (DPPH), ferric-reducing antioxidant power assay (FRAP), 2,2’-azino-bis- 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging assay, H2O2 radical scavenging activity and Fe2+ chelating activity. Total flavonoids and phenolic content of ethanolic extract of onion peel were significantly greater as compared to that of onion bulb. Ethanolic extract of onion peel also presented better antioxidant and free-radical scavenging activity as compared to the ethanolic extract of bulb, while the aqueous extract of bulb presented weakest antioxidative potential. Onion peel extract's α-glucosidase inhibition potential was also correlated with their phenolic and flavonoid contents. The current findings presented onion peel as a possible source of antioxidative agents and phenolic compounds that might be beneficial against development of various common chronic diseases that might have an association with oxidative stress. Besides, outer dry layers and fleshy peels of onion exhibited higher phenolic content and antioxidant activities, compared [...].


Allium cepa pertence à família Liliaceae e é rica em nutrientes e antioxidantes. Apesar das expressivas aplicações alimentares do bulbo da cebola, sua casca e outras camadas externas são geralmente consideradas resíduos, e seu potencial nutricional e terapêutico ainda é pouco explorado. O presente estudo foi delineado com o objetivo de investigar comparativamente o potencial antioxidante de duas partes de Allium cepa, por exemplo o bulbo (parte comestível) e camadas externas e cascas secas (parte não comestível). Além disso, o efeito inibitório dos extratos do bulbo de cebola e casca sobre a α-glucosidase intestinal de ratos e α-amilase pancreática suína também foi avaliado. O potencial antioxidante dos extratos da casca de cebola e bulbo foi avaliado utilizando-se 2,2-difenil-1-picrilhidrazil (DPPH), método de poder antioxidante de redução do ferro (FRAP), método 2,2’-azino-bis-3-etilbenzotiazolina-6-ácido sulfônico (ABTS) de eliminação de radicais, atividade de eliminação de radicais H2O2 e atividade quelante do Fe2+. Os flavonoides totais e os teores fenólicos do extrato de etanol da casca de cebola foram significativamente maiores quando comparados ao do bulbo. O extrato de etanol da casca de cebola também apresentou melhor atividade antioxidante e eliminação de radicais livres quando comparado ao extrato de etanol do bulbo, enquanto o extrato aquoso de bulbo apresentou menor potencial antioxidante. O potencial de inibição da α-glicosidase dos extratos de casca de cebola correlacionou-se com seus teores fenólicos e de flavonoides. Os resultados encontrados identificaram que a casca de cebola é uma possível fonte de agentes antioxidantes e compostos fenólicos que podem ser benéficos contra o desenvolvimento de várias doenças crônicas que estão associadas ao estresse oxidativo. Além disso, as camadas externas secas e as cascas da cebola exibiram maior conteúdo fenólico e atividades [...].


Assuntos
Antioxidantes/análise , Cebolas , Estresse Oxidativo/efeitos dos fármacos , Inibidores de Glicosídeo Hidrolases/análise
8.
Molecules ; 27(1)2022 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-35011541

RESUMO

This study investigated the effect of co-ingesting Natal plums (Carissa macrocarpa) and Marula nuts (Sclerocarya birrea) on the bioaccessibility and uptake of anthocyanins, antioxidant capacity, and the ability to inhibit α-glucosidase. A Natal plum-Marula nut bar was made by mixing the raw nuts and the fruit pulp in a ratio 1:1 (v/v). The cyanidin-3-O-sambubioside (Cy-3-Sa) and cyanidin-3-O-glucoside content (Cy-3-G) were quantified using the ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC/Q-TOF-MS). Inclusion of Natal plum in the Marula nut bar increased the Cy-3-Sa, Cy-3-G content, antioxidants capacity and α-glucosidase inhibition compared to ingesting Marula nut separately at the internal phase. Adding Natal plum to the Marula nut bar increased bioaccessibility of Cy-3-Sa, Cy-3-G, quercetin, coumaric acid, syringic acid and ferulic acid to 80.2% and 71.9%, 98.7%, 95.2%, 51.9% and 89.3%, respectively, compared to ingesting the Natal plum fruit or nut separately.


Assuntos
Anacardiaceae/química , Nozes/química , Fenóis/análise , Prunus domestica/química , Lanches , Antocianinas/análise , Antocianinas/química , Antioxidantes/química , Digestão , Ingestão de Alimentos , Análise de Alimentos , Suco Gástrico/metabolismo , Inibidores de Glicosídeo Hidrolases/análise , Polifenóis , Saliva/metabolismo
9.
Biomed Chromatogr ; 36(4): e5313, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34981537

RESUMO

Cyclocarya paliurus is an edible and medicinal plant exhibiting significant hypoglycemic effect. However, its active components are still unclear and need further elucidation. In this research, the active components of the leaves of C. paliurus responsible for the α-glucosidase inhibitory activity were screened and identified based on a spectrum-effect relationship study in combination with ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) analysis. The 70% ethanol eluate fraction of the leaves of C. paliurus with the strongest α-glucosidase inhibitory activity was obtained after extraction and purification with macroporous resin. Their chromatographic fingerprints (15 batches) were established by UPLC analysis and 32 common peaks were specified by similarity analysis. Their IC50 values for α-glucosidase inhibition were measured by an enzymatic reaction. Several multivariate statistical analysis methods including hierarchical cluster analysis, principal component analysis, partial least square analysis and gray relational analysis were applied to explore the spectrum-effect relationship between common peaks and IC50 values, and the chromatographic peaks making a large contribution to efficacy were screened out. To further elucidate the active components of leaves of C. paliurus, the 70% ethanol eluate fraction was characterized by UPLC-MS/MS analysis, and 10 compounds were identified. This study provides a valuable reference for further research and development of hypoglycemic active components of C. paliurus.


Assuntos
Inibidores de Glicosídeo Hidrolases , Espectrometria de Massas em Tandem , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Inibidores de Glicosídeo Hidrolases/análise , Extratos Vegetais/química , Folhas de Planta/química , Pesquisa
10.
BMC Complement Med Ther ; 22(1): 26, 2022 Jan 27.
Artigo em Inglês | MEDLINE | ID: mdl-35086537

RESUMO

BACKGROUND: Natural phenolic compounds and Phenolics-rich medicinal plants are also of great interest in the management of diabetes. The current study was aimed to analyze phenolics in P. hydropiepr L extracts via HPLC-DAD analysis and assess their anti-diabetic potentials using in-vitro and in-silico approaches. METHODS: Plant crude methanolic extract (Ph.Cme) was evaluated for the presence of phenolic compounds using HPLC-DAD analysis. Subsequently, samples including crude (Ph.Cr), hexane (Ph.Hex), chloroform (Ph.Chf), ethyl acetate (Ph.EtAc), butanol (Ph.Bt), aqueous (Ph.Aq) and saponins (Ph.Sp) were tested for α-glucsidase and α-amylase inhibitory potentials and identified compounds were docked against these target enzymes using Molecular Operating Environment (MOE) software. Fractions were also analyzed for the nutritional contents and acute toxicity was performed in animals. RESULTS: In HPLC-DAD analysis of Ph.Cme, 24 compounds were indentfied and quantified. Among these, Kaemferol-3-(p-coumaroyl-diglucoside)-7-glucoside (275.4 mg g- 1), p-Coumaroylhexose-4-hexoside (96.5 mg g- 1), Quercetin-3-glucoronide (76.0 mg g- 1), 4-Caffeoylquinic acid (58.1 mg g- 1), Quercetin (57.9 mg g- 1), 5,7,3'-Trihydroxy-3,6,4',5'-tetramethoxyflavone (55.5 mg g- 1), 5-Feruloylquinic acid (45.8 mg g- 1), Cyanidin-3-glucoside (26.8 mg g- 1), Delphinidin-3-glucoside (24 mg g- 1), Quercetin-3-hexoside (20.7 mg g- 1) were highly abundant compounds. In α-glucosidase inhibition assay, Ph.Sp were most effective with IC50 value of 100 µg mL-1. Likewise in α-amylase inhibition assay, Ph.Chf, Ph.Sp and Ph.Cme were most potent fractions displayed IC50 values of 90, 100 and 200 µg mL-1 respectively. Docking with the α-glucosidase enzyme revealed top ranked conformations for majority of the compounds with Kaemferol-3-(p-coumaroyl-diglucoside)-7-glucoside as the most active compound with docking score of - 19.80899, forming 14 hydrogen bonds, two pi-H and two pi-pi linkages with the Tyr 71, Phe 158, Phe 177, Gln 181, Arg 212, Asp 214, Glu 276, Phe 300, Val 303, Tyr 344, Asp 349, Gln 350, Arg 439, and Asp 408 residues of the enzyme. Likewise, docking with α-amylase revealed that most of the compounds are well accommodated in the active site residues (Trp 59, Tyr 62, Thr 163, Leu 165, Arg 195, Asp 197, Glu 240, Asp 300, His 305, Asp 356) of the enzyme and Cyanidin-3-rutinoside displayed most active compound with docking score of - 15.03757. CONCLUSIONS: Phytochemical studies revealed the presence of highly valuable phenolic compounds, which might be responsible for the anti-diabetic potentials of the plant samples.


Assuntos
Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Polygonaceae/química , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo , Animais , Cromatografia Líquida de Alta Pressão , Diabetes Mellitus/tratamento farmacológico , Diabetes Mellitus/enzimologia , Inibidores de Glicosídeo Hidrolases/análise , Humanos , Hipoglicemiantes/análise , Simulação de Acoplamento Molecular , Fenóis/análise , Fenóis/farmacologia , Compostos Fitoquímicos/análise , Extratos Vegetais/química , Saponinas/análise , Saponinas/farmacologia , alfa-Amilases/antagonistas & inibidores
11.
Molecules ; 26(24)2021 Dec 18.
Artigo em Inglês | MEDLINE | ID: mdl-34946757

RESUMO

The current study aimed to explore the crude oils obtained from the n-hexane fraction of Scutellaria edelbergii and further analyzed, for the first time, for their chemical composition, in vitro antibacterial, antifungal, antioxidant, antidiabetic, and in vivo anti-inflammatory, and analgesic activities. For the phytochemical composition, the oils proceeded to gas chromatography-mass spectrometry (GC-MS) analysis and from the resultant chromatogram, 42 bioactive constituents were identified. Among them, the major components were linoleic acid ethyl ester (19.67%) followed by ethyl oleate (18.45%), linolenic acid methyl ester (11.67%), and palmitic acid ethyl ester (11.01%). Tetrazolium 96-well plate MTT assay and agar-well diffusion methods were used to evaluate the isolated oil for its minimum inhibitory concentrations (MIC), minimum bactericidal concentration (MBC), half-maximal inhibitory concentrations (IC50), and zone of inhibitions that could determine the potential antimicrobial efficacy's. Substantial antibacterial activities were observed against the clinical isolates comprising of three Gram-negative bacteria, viz., Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and one Gram-positive bacterial strain, Enterococcus faecalis. The oils were also effective against Candida albicans and Fusarium oxysporum when evaluated for their antifungal potential. Moreover, significant antioxidant potential with IC50 values of 136.4 and 161.5 µg/mL for extracted oil was evaluated through DPPH (1,1-Diphenyl-2-picryl-hydrazyl) and ABTS assays compared with standard ascorbic acid where the IC50 values were 44.49 and 67.78 µg/mL, respectively, against the tested free radicals. The oils was also potent, inhibiting the α-glucosidase (IC50 5.45 ± 0.42 µg/mL) enzyme compared to the standard. Anti-glucosidase potential was visualized through molecular docking simulations where ten compounds of the oil were found to be the leading inhibitors of the selected enzyme based on interactions, binding energy, and binding affinity. The oil was found to be an effective anti-inflammatory (61%) agent compared with diclofenac sodium (70.92%) via the carrageenan-induced assay. An appreciable (48.28%) analgesic activity in correlation with the standard aspirin was observed through the acetic acid-induced writhing bioassay. The oil from the n-hexane fraction of S. edelbergii contained valuable bioactive constituents that can act as in vitro biological and in vivo pharmacological agents. However, further studies are needed to uncover individual responsible compounds of the observed biological potentials which would be helpful in devising novel drugs.


Assuntos
Antibacterianos/análise , Antifúngicos/análise , Antioxidantes/análise , Inibidores de Glicosídeo Hidrolases/análise , Óleos de Plantas/análise , Scutellaria/química , Animais , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Carragenina , Edema/induzido quimicamente , Edema/tratamento farmacológico , Fungos/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Inibidores de Glicosídeo Hidrolases/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hexanos/química , Humanos , Camundongos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Picratos/antagonistas & inibidores , Óleos de Plantas/farmacologia , Plantas Medicinais , Ácidos Sulfônicos/antagonistas & inibidores , alfa-Glucosidases/metabolismo
12.
Molecules ; 26(22)2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34833966

RESUMO

Most of the health benefits derived from cereals are attributed to their bioactive compounds. This study evaluated the levels of the bioactive compounds, and the antioxidant and starch-hydrolyzing enzymes inhibitory properties of six pipeline Striga-resistant yellow-orange maize hybrids (coded AS1828-1, 4, 6, 8, 9, 11) in vitro. The maize hybrids were grown at the International Institute of Tropical Agriculture (IITA), Nigeria. The bioactive compounds (total phenolics, tannins, flavonoids, and phytate) levels, antioxidant (DPPH• and ABTS•+ scavenging capacity and reducing power) and starch-hydrolyzing enzymes (α-amylase and α-glucosidase) inhibitory activities of the maize hybrids were determined by spectrophotometry. At the same time, carotenoids were quantified using a reverse-phase HPLC system. The ranges of the bioactive compounds were: 11.25-14.14 mg GAE/g (total phenolics), 3.62-4.67 mg QE/g (total flavonoids), 3.63-6.29 mg/g (tannins), 3.66-4.31% (phytate), 8.92-12.11 µg/g (total xanthophylls), 2.42-2.89 µg/g (total ß-carotene), and 3.17-3.77 µg/g (total provitamin A carotenoids). Extracts of the maize hybrids scavenged DPPH• (SC50: 9.07-26.35 mg/mL) and ABTS•+ (2.65-7.68 TEAC mmol/g), reduced Fe3+ to Fe2+ (0.25 ± 0.64-0.43 ± 0.01 mg GAE/g), and inhibited α-amylase and α-glucosidase, with IC50 ranges of 26.28-52.55 mg/mL and 47.72-63.98 mg/mL, respectively. Among the six clones of the maize hybrids, AS1828-9 had the highest (p < 0.05) levels of tannins and phytate and the strongest antioxidant and starch-hydrolyzing enzymes inhibitory activities. Significant correlations were observed between total phenolics and the following: ABTS•+ (p < 0.01, r = 0.757), DPPH• SC50 (p < 0.01, r = -0.867), reducing power (p < 0.05, r = 0.633), α-amylase IC50 (p < 0.01, r = -0.836) and α-glucosidase IC50 (p < 0.05, r = -0.582). Hence, the Striga-resistant yellow-orange maize hybrids (especially AS1828-9) may be beneficial for alleviating oxidative stress and postprandial hyperglycemia.


Assuntos
Antioxidantes/análise , Inibidores de Glicosídeo Hidrolases/análise , Compostos Fitoquímicos/análise , Zea mays/química , alfa-Amilases/antagonistas & inibidores , Antioxidantes/farmacologia , Resistência à Doença , Flavonoides/análise , Flavonoides/farmacologia , Geobacillus stearothermophilus/enzimologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Estresse Oxidativo , Fenóis/análise , Fenóis/farmacologia , Compostos Fitoquímicos/farmacologia , Doenças das Plantas/parasitologia , Proteínas de Plantas/análise , Striga/fisiologia , Taninos/análise , Taninos/farmacologia , Zea mays/parasitologia
13.
Artigo em Inglês | MEDLINE | ID: mdl-34500401

RESUMO

Extracts from the bran of Chenopodium quinoa Willd. (QBE) were reported to be active in inhibiting α-glycosidase, a promising target for treatment of diabetes mellitus. However, the constituents responsible for the α-glucosidase-inhibiting activity of QBE have not been fully characterized. The present study aimed to set up a method for rapid identification of glycosidase inhibiting compounds from the quinoa bran. With surface plasmon resonance (SPR) coupled with liquid chromatography-mass spectrometry (LC-MS), we identified eight flavonoids and ten triterpenoid saponins that may bind to the α-glycosidase. Analysis of the interaction kinetics by molecular docking supported their α-glucosidase-inhibiting activity and revealed the potential mechanisms for the inhibitory effects. In summary, this study established a SPR and LC-MS-based method for rapid in vitro screening of α-glucosidase inhibitors and suggested the quinoa bran a potential natural source of α-glucosidase inhibitors.


Assuntos
Chenopodium quinoa/química , Cromatografia Líquida de Alta Pressão/métodos , Fibras na Dieta/análise , Inibidores de Glicosídeo Hidrolases , Ressonância de Plasmônio de Superfície/métodos , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/química , Espectrometria de Massas , Simulação de Acoplamento Molecular
14.
Mar Drugs ; 19(6)2021 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-34199233

RESUMO

Fish discards and by-products can be transformed into high value-added products such as fish protein hydrolysates (FPH) containing bioactive peptides. Protein hydrolysates were prepared from different parts (whole fish, skin and head) of several discarded species of the North-West Spain fishing fleet using Alcalase. All hydrolysates had moisture and ash contents lower than 10% and 15%, respectively. The fat content of FPH varied between 1.5% and 9.4% and had high protein content (69.8-76.6%). The amino acids profiles of FPH are quite similar and the most abundant amino acids were glutamic and aspartic acids. All FPH exhibited antioxidant activity and those obtained from Atlantic horse mackerel heads presented the highest 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, reducing power and Cu2+ chelating activity. On the other hand, hydrolysates from gurnard heads showed the highest ABTS radical scavenging activity and Fe2+ chelating activity. In what concerns the α-amylase inhibitory activity, the IC50 values recorded for FPH ranged between 5.70 and 84.37 mg/mL for blue whiting heads and whole Atlantic horse mackerel, respectively. α-Glucosidase inhibitory activity of FPH was relatively low but all FPH had high Angiotensin Converting Enzyme (ACE) inhibitory activity. Considering the biological activities, these FPH are potential natural additives for functional foods or nutraceuticals.


Assuntos
Inibidores da Enzima Conversora de Angiotensina , Anti-Hipertensivos , Antioxidantes , Proteínas de Peixes , Inibidores de Glicosídeo Hidrolases , Quelantes de Ferro , Hidrolisados de Proteína , Inibidores da Enzima Conversora de Angiotensina/análise , Inibidores da Enzima Conversora de Angiotensina/química , Inibidores da Enzima Conversora de Angiotensina/isolamento & purificação , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Animais , Anti-Hipertensivos/análise , Anti-Hipertensivos/química , Anti-Hipertensivos/isolamento & purificação , Anti-Hipertensivos/farmacologia , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Produtos Biológicos/análise , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/farmacologia , Proteínas de Peixes/análise , Proteínas de Peixes/química , Proteínas de Peixes/isolamento & purificação , Proteínas de Peixes/farmacologia , Pesqueiros , Peixes , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/farmacologia , Quelantes de Ferro/análise , Quelantes de Ferro/química , Quelantes de Ferro/isolamento & purificação , Quelantes de Ferro/farmacologia , Peso Molecular , Hidrolisados de Proteína/análise , Hidrolisados de Proteína/química , Hidrolisados de Proteína/isolamento & purificação , Hidrolisados de Proteína/farmacologia , Espanha
15.
Biomed Chromatogr ; 35(12): e5215, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34269469

RESUMO

Contents of total flavonoids (TFc), total phenolics (TPc), and total crude polysaccharide (TCPc) in licorice from different origins were determined by optimized colorimetric methods, whereas five monomer ingredients (liquiritin [LQ], isoliquiritin [ILQ], liquiritigenin [LQG], isoliquiritigenin [ILQG], and glycyrrhizic acid [GA]) were simultaneously identified and quantified by HPLC-MS and HPLC. The results indicated that the contents of chemical compounds in licorice showed significant difference in different origins. Hierarchical cluster analysis and principal component analysis further proved that producing area indeed affected the quality including compounds and pharmacological activity in licorice. Licorice from Inner Mongolia exhibited the excellent DPPH assay, whereas samples from Gansu and Xinjiang showed high scavenging capacity to OH and ABTS free radicals. Meanwhile, α-Glu inhibitory activity of licorice samples was four times higher than the antioxidant activity. Correlation analysis made clear that TFc and TCPc both strongly contribute to DPPH scavenge capacity at P < 0.01 level, whereas TCPc contributed to α-Glu inhibitory activity at P < 0.05 level. This study would contribute to the comprehensive quality evaluation based on the compounds and pharmacological activity of licorice, and provide a reference for the choice of producing area to ensure the quality of licorice as a medicine.


Assuntos
Antioxidantes , Inibidores de Glicosídeo Hidrolases , Glycyrrhiza/química , Extratos Vegetais , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/farmacologia , Quimiometria , Cromatografia Líquida de Alta Pressão , Flavonoides , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Espectrometria de Massas , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Reprodutibilidade dos Testes
16.
Food Chem ; 361: 130144, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34082387

RESUMO

Effect of high-intensity ultrasound (HIU) compared with thermal treatments on baobab fruit pulp (BFP) quality and bioactive properties were investigated. HIU treatments, particularly at intensities of 687.5 W/cm2 for 5 min, and 344 W/cm2 for 15 min significantly (p < 0.05) increased the cloudiness index, ascorbic acid (AA) retention, total phenolic and flavonoid contents, and antioxidant capacity besides a more potent α-amylase and α-glucosidase inhibition relative to thermally treated samples. Moreover, the physicochemical parameters, colour index, and browning index were maintained with HIU besides lower 5-hydroxymethylfurfural values than thermal processing. HPLC analysis revealed that the content of most phenolic compounds was the highest in HIU treatments besides a 235-256% increase in procyanidin C1 compared with control samples. The AA retention following HIU treatments was 87.62-102.86% compared to 30.47-61.90% in thermally treated samples. Our analyses portrayed ultrasound as a feasible alternative to conventional thermal processing of BFP.


Assuntos
Adansonia/química , Inibidores Enzimáticos/farmacologia , Frutas/química , Ultrassom/métodos , alfa-Amilases/antagonistas & inibidores , Antioxidantes/análise , Antioxidantes/química , Ácido Ascórbico/análise , Biflavonoides/análise , Catequina/análise , Inibidores Enzimáticos/análise , Inibidores Enzimáticos/química , Flavonoides/análise , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Fenóis/análise , Proantocianidinas/análise , alfa-Glucosidases/metabolismo
17.
Food Funct ; 12(9): 3939-3953, 2021 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-33977959

RESUMO

Nowadays, it is very important to identify the traditional uses of different plants and to create the context in which new cultural or economic value is given to local resources. In this study, two wild fruits traditionally harvested in autumn in Romania were selected to investigate the effects of drying conditions on the chemical compositions and bioactivities exerted by the extracts and to select the best conditions in terms of air temperature and time of drying. The extracts obtained were assessed in terms of antioxidant capacity and enzyme inhibitory activity, and their main bioactive compounds were identified and quantified. The data presented in this article represent a step forward in applying this process on an industrial-scale.


Assuntos
Dessecação , Flavonoides/análise , Conservação de Alimentos , Hippophae/química , Extratos Vegetais , Rosa/química , Animais , Anti-Inflamatórios não Esteroides/análise , Anti-Inflamatórios não Esteroides/farmacologia , Antioxidantes/análise , Antioxidantes/farmacologia , Linhagem Celular , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Flavonoides/farmacologia , Frutas/química , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos
18.
Food Chem ; 359: 129889, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-33934030

RESUMO

The objective was to analyze the phenolic composition, antioxidant capacity, and physical characteristics of 10 blackcurrant cultivars, their juices, and the enzymatic inhibition of dipeptidyl peptidase-IV, α-amylase, α-glucosidase, nitric oxide synthase, and cyclooxygenase-2. Fruit masses ranged from 0.47 to 1.22 g and diameters from 7.42 to 14.42 mm. For the juices, pH ranged from 2.80 to 2.96, soluble solids from 11.33% to 17.5%, total acidity from 3.17 to 4.26 g/100 mL, and viscosity from 1.28 to 273.83 mPa·s. Total anthocyanins (TA) ranged from 1.81 to 5.48 mg eq cyanidin 3-O-glucoside/100 g, total polyphenols (TP) from 7.67 to 39.70 mg eq gallic acid/100 g, total condensed tannins from 3.24 to 7.76 g eq catechin/100 g, and antioxidant capacity from 219.24 to 499.26 µmol eq Trolox/100 g. Juices of the cultivars Coronet and Consort contained the highest levels of TA, TP, and antioxidants. Whistler cultivar contained high concentrations of major anthocyanins. Juices from all cultivars favorably inhibited the activities of enzymes used as surrogate biochemical markers for T2 diabetes and inflammation.


Assuntos
Antocianinas/análise , Antioxidantes/análise , Extratos Vegetais/farmacologia , Polifenóis/análise , Proantocianidinas/análise , Ribes/química , Antocianinas/farmacologia , Inibidores de Ciclo-Oxigenase 2/análise , Inibidores da Dipeptidil Peptidase IV/análise , Frutas/química , Sucos de Frutas e Vegetais/análise , Inibidores de Glicosídeo Hidrolases/análise , Óxido Nítrico Sintase/antagonistas & inibidores , Fenóis/análise , Extratos Vegetais/química , Polifenóis/farmacologia , Proantocianidinas/farmacologia , alfa-Amilases/antagonistas & inibidores
19.
Int J Food Microbiol ; 348: 109204, 2021 Jun 16.
Artigo em Inglês | MEDLINE | ID: mdl-33930838

RESUMO

The survival kinetics of Listeria monocytogenes (9 log CFU/mL) as a post-fermentation contaminant in probiotic fermented milk (Lactobacillus acidophilus La-5, 8-9 log CFU/mL) processed with milk subjected to ohmic heating (0, 4, 6, and 8 V/cm; CONV, OH4, OH6, OH8, 90-95 °C/5 min) was investigated using Weibull predictive model. Additionally, the presence of bioactive compounds (antioxidant activity, inhibition of the enzymes α-glucosidase, α-amylase, and angiotensin-converting) and sensory analysis (consumer test) of probiotic fermented milks were evaluated. Overall, OH provided a decrease in the viability of Listeria monocytogenes, suitable Lactobacillus acidophilus counts, and satisfactory results in the gastrointestinal tract survival. The Weibull model presented an excellent fit to the data of all conditions. Furthermore, lower δ values (217-298 against 665 h, CONV), and increased R2 values (0.99 against 0.98, CONV) were obtained for the OH-treated samples, emphasizing the best performance of OH data. In addition, OH improved the generation of bioactive compounds as well as the sensory acceptance. Indeed, considering functional and safety purposes, OH presented as an interesting technology to be used in milk for manufacturing probiotic fermented milk.


Assuntos
Produtos Fermentados do Leite/microbiologia , Lactobacillus acidophilus/metabolismo , Listeria monocytogenes/isolamento & purificação , Leite/microbiologia , Probióticos/metabolismo , Inibidores da Enzima Conversora de Angiotensina/análise , Animais , Antioxidantes/análise , Reatores Biológicos/microbiologia , Produtos Fermentados do Leite/análise , Fermentação , Inibidores de Glicosídeo Hidrolases/análise , Calefação , Cinética , Percepção Gustatória , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/química
20.
J Chromatogr A ; 1642: 462041, 2021 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-33721816

RESUMO

Cortex Lycii, as a kind of traditional Chinese medicines, have shown prospects in the prevention of diabetes and its complications. However, there is comparatively little information regarding the characterization of potentially hypoglycemic compounds derived from Cortex Lycii. In this study, we performed a global non-selective investigation of α-glucosidase inhibitors in Cortex Lycii based on a bioactivity-labeling high-resolution mass spectrometry-metabolomics method. Samples of Cortex Lycii were collected from different Chinese provinces and their ethyl acetate extracts were analyzed using an in vitro α-glucosidase inhibition assay for bioactivity-labeling. The ethyl acetate extracts were also subjected to liquid chromatography-mass spectrometry analysis and multivariate data analysis was subsequently conducted to identify correlations between the bioactivity measured from the enzyme-involved test and the profiles obtained based on high-resolution mass spectrometry. The variables contributing significantly to the separation of the more-active from the less-active samples were considered to indicate the potential target ions of active compounds. MS/MS fragment patterns and nuclear magnetic resonance analyses were used to identify the potential target ions. The developed platform mentioned above facilitated rapid identification of four α-glucosidase inhibitors, namely, N-p-trans-coumaroyltyramine (1), N-trans-caffeoyl-tyramine (2), (9R,10E,12Z)-9-hydroxy-10,12-octadecadienoic acid (3a), and (9S,10E,12Z)-9-hydroxy-10,12-octadecadienoic acid (3b) from Cortex Lycii. The α-glucosidase inhibitory activities of compounds 3a and 3b with IC50 values of 1.0413±0.0551 and 1.0423±0.0049 mM, respectively, are reported here for the first time. Enzyme kinetics revealed that both 3a and 3b were non-competitive inhibitors of α-glucosidase, with Ki values of 2.20 and 2.24 mM, respectively. In short, the presented work identified compounds 3a and 3b as potential α-glucosidase inhibitors with higher inhibitory activity and a different mode of inhibition compared to the standard α-glucosidase inhibitor, acarbose. The integrated approach adopted in this study can be extended as a normalized procedure to rapidly identify active compounds, even from complex extracts, and can readily be adapted for the study of other natural products.


Assuntos
Medicamentos de Ervas Chinesas/química , Inibidores de Glicosídeo Hidrolases/análise , Espectrometria de Massas , Metabolômica , Cromatografia Líquida de Alta Pressão , Inibidores de Glicosídeo Hidrolases/química , Concentração Inibidora 50 , Íons , Cinética , Espectroscopia de Ressonância Magnética , Análise Multivariada , Extratos Vegetais/química , Análise de Componente Principal , Reprodutibilidade dos Testes , alfa-Glucosidases/metabolismo
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