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1.
Antioxidants (Basel) ; 10(11)2021 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-34829642

RESUMO

Spondias species have been used in traditional medicine for different human ailments. In this study, the effect of different solvents (ethyl acetate, methanol, and water) and extraction methods (infusion, maceration, and Soxhlet extraction) on the enzyme inhibitory activity against acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase, α-glucosidase, and antioxidant properties of S. mombin and S. dulcis leaves and stem bark were evaluated. Ultra-high-performance liquid chromatography-high resolution mass spectrometry (UHPLC-HRMS) yield in the identification and/or annotation of 98 compounds showing that the main secondary metabolites of the plant are gallic and ellagic acids and their derivatives, ellagitannins, hydroxybenzoic, hydroxycinnamic, acylquinic acids and flavonols, flavanones, and flavanonols. The leaves infusion of both Spondias species showed highest inhibition against acetylcholinesterase (AChE) (10.10 and 10.45 mg galantamine equivalent (GALAE)/g, for S. dulcis and S. mombin, respectively). The ethyl acetate extracts of the stem bark of S. mombin and S. dulcis actively inhibited α-glucosidase. Methanolic extracts of the leaves and stem bark exhibited highest tyrosinase inhibitory action. Antioxidant activity and higher levels of phenolics were observed for the methanolic extracts of Spondias. The results suggested that the Spondias species could be considered as natural phyto-therapeutic agents in medicinal and cosmeceutical applications.

2.
Plants (Basel) ; 10(10)2021 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-34685855

RESUMO

The widespread genus Cirsium Mill. (Asteraceae) is renowned in traditional medicine. In the present study, an innovative biochemometric-assisted metabolite profiling of the flower heads, aerial parts and roots of Cirsium appendiculatum Griseb. (Balkan thistle) in relation to their antioxidant and enzyme inhibitory potential was developed. The workflow combines ultra-high-performance liquid chromatography-high-resolution mass spectrometry (UHPLC-HRMS) with partial least-square analysis to discriminate the herbal extracts and identify the most prominent biological activities. The annotation and dereplication of 61 secondary metabolites were evidenced, including 15 carboxylic (including hydroxybenzoic and hydroxycinnamic) acids and their glycosides, 11 acylquinic acids, 26 flavonoids and 9 fatty acids. All compounds were reported for the first time in the studied species. The root extract revealed the highest cupric and ferric reducing power (618.36 ± 5.17 mg TE/g and 269.89 ± 8.50 mg TE/g, respectively) and antioxidant potential in phosphomolybdenum (3.36 ± 0.15 mmol TE/g) as well as the most prominent enzyme inhibitory potential on α-glucosidase (0.72 ± 0.07 mmol ACAE/g), acetylcholinesterase (4.93 ± 0.25 mg GALAE/g) and butyrylcholinesterase (3.80 ± 0.26 mg GALAE/g). Nevertheless, the flower heads were differentiated by their higher metal chelating activity (32.53 ± 3.51 mg EDTAE/g) and total flavonoid content (46.59 ± 0.89 mgRE/g). The partial least-square discriminant and heat-map analysis highlighted the root extract as the most active and a promising source of bioactive compounds for the therapeutic industry.

3.
Antioxidants (Basel) ; 10(10)2021 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-34679706

RESUMO

The impact of two extraction solvents on the phenolic composition, antioxidant, and enzymes inhibitory and antimicrobial activities of two parts (leaves and stem bark) of P. kotschyi was studied. Two different LC-DAD-MSn approaches were used to identify and quantify the bioactive compounds in the different extracts. A total of thirty-two compounds were quantified, being the procyanidin the most abundant in stem bark while catechin and flavonoids are most abundant in leaves. Overall, the stem bark extraction using methanol showed higher amounts of total phenolic (131.83 ± 1.81 mg GAE/g) and flavanol (14.14 ± 0.11 mg CE/g) while the leaves extraction using water exhibited stronger levels of total flavonoid (44.95 ± 0.38 mg RE/g) and phenolic acid (63.58 ± 2.00 mg CAE/g). As regards the antioxidant assays, methanol stem bark extracts were characterized by the highest antioxidant activities (DPPH: 1.94 ± 0.01 mmol TE/g, ABTS: 3.31 ± 0.01 mmol TE/g, FRAP: 2.86 ± 0.02 mmol TE/g, CUPRAC: 5.09 ± 0.08 mmol TE/g, phosphomolybdenum: 5.16 ± 0.23 mmol TE/g and metal chelating: 17.12 ± 0.46 mg EDTAE/g). In addition, the methanolic extracts of stem bark had highest impact on acetylcholinesterase (2.54 mg GALAE/g), butyrylcholinesterase (5.48 mg GALAE/g). In contrast, the methanolic extracts of leaves was potent against tyrosinase (77.39 ± 0.21 mg KAE/g) and α-glucosidase (0.97 ± 0.01 mmol ACAE/g), while a higher anti-α-amylase (0.97 ± 0.01 mmol ACAE/g) was observed for water extracts of the same part. All of the tested extracts showed inhibitory effects on elastase, except methanolic leaves extracts. Additionally, the extracts exhibited appreciable antifungal toward A. ochraceus, A. fumigatus, P. ochrochloron, T. viride, and P. funiculosum and promising antibacterial activity against M. flavus, S. aureus, L. monocytogenes, E. coli, P. aeruginosa, E. cloacae, and S. typhimurium. Taken together, the outcomes demonstrated P. kotschyi as a novel source of bioactive molecules of interest with an evident therapeutic value.

4.
Plants (Basel) ; 10(9)2021 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-34579358

RESUMO

Comfrey (Symphytum officinale L.) roots are well-known bioactive ingredients included in various cosmeceutical and pharmaceutical preparations. In this study, the influence of the post-harvest storage on the chemico-biological potential of roots collected from different European regions and stored for up to six months was investigated. Total phenolic content (TPC) and total phenolic acid content (TPAC) were spectrophotometrically estimated, whereas the levels of individual phenolic and pyrrolizidine alkaloidal markers were determined by HPLC-DAD and HPLC-MS/MS, respectively. The changes in the biological potential was tracked via antioxidant (DPPH, ABTS, CUPRAC, and FRAP) and anti-enzymatic (cholinesterase, tyrosinase, glucosidase, and amylase) assays. TPC and TPAC varied from 6.48-16.57 mg GAE/g d.w. root and from 2.67-9.03 mg CAE/g, respectively. The concentration of the four phenolics (rosmarinic acid, globoidnan A, globoidnan B, rabdosiin) and six pyrrolizidine alkaloids generally showed maximum values at 1-3 months, after which their levels significantly decreased. With respect to the bioassays, the samples showed a wide range of antioxidant and anti-enzymatic effects; however, a direct storage time-bioactivity relationship was not observed. Similar conclusions were also revealed by the multivariate and correlation analyses. Our study could improve the current knowledge of the shelf-life properties of comfrey-based products and enhance their industrial exploitation.

5.
Antioxidants (Basel) ; 10(8)2021 Jul 24.
Artigo em Inglês | MEDLINE | ID: mdl-34439428

RESUMO

In the current study, Achillea santolinoides and Achillea aleppica aeral parts and root were extracted with ethyl acetate, methanol, and water. Detailed phytochemical profiles were obtained using UHPLC-MS, yielding the identification of hydroxybenzoic and hydroxycinnamic acids, phenolic acid glycosides and sugar esters, acylquinic acids, O-glycosyl flavones and flavonols, and flavonoid aglycons, among others. The antioxidant properties and enzyme inhibitory activities of the extracts were assayed with in vitro tests. The phenolic content of the water extracts was significantly higher as compared to the ethyl acetate and methanol ones. A. aleppica aerial parts methanol extract possessed highest flavonoid content (49.18 mg rutin equivalent/g). Antioxidant properties assessment revealed that the methanol extract of A. santolinoides roots actively scavenged DPPH (54.11 mg TE/g) and ABTS radicals (112.53 mg TE/g) and possessed highest reducing potential (183.55 and 129.92 mg TE/g, for CUPRAC and FRAP, respectively). The ethyl acetate extracts of aerial parts and roots of both species showed highest inhibition against BuCHE (6.07-6.76 mg GALAE/g). The ethyl acetate extract of A.santolinoides aerial part showed highest inhibition against tyrosinase (73.00 mg KAE/g). These results showed that the tested Achillea species might represent novel phytotherapeutic avenues for the management of Alzheimer's disease and epidermal hyperpigmentation conditions, which are both associated with oxidative stress. This paper could shed light into future potential industrial applications using the tested Achillea species.

6.
Chem Biodivers ; 18(10): e2100356, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34398524

RESUMO

The aim of the present study was to quantify selected phenolic compounds, determine antioxidant activity and enzyme inhibitory effects of the aerial parts of Alkanna trichophylla Hub.-Mor. (A. trichophylla) and Convolvulus galaticus Rost.ex Choisy (C. galaticus) extracts prepared by homogenizer-assisted extraction (HAE), maceration (MAC) and infusion techniques. This is the first time such study has been designed to validate the phytochemical composition and bioactivity of these plants. Multivariate analysis was conducted on collected data. Rutin and caffeoylquinic acid derivatives were the most significant compounds in A. trichophylla and C. galaticus, respectively. The highest antioxidant activity of A. trichophylla was mostly exhibited by HAE/methanolic extracts as determined by DPPH, ABTS, FRAP (51.39, 112.70 and 145.73 mg TE/g, respectively) and phosphomolybdenum (2.05 mmol TE/g) assays. However, significant antioxidant activities varied within the extracts of C. galaticus. HAE/methanolic extract of A. trichophylla significantly depressed AChE (2.70 mg GALAE/g), BChE (5.53 mg GALAE/g) and tyrosinase (26.34 mg KAE/g) activities and that of C. galaticus inhibited AChE (2.04 mg GALAE/g), tyrosinase (31.25 mg KAE/g) and α-amylase (0.53 mmol ACAE/g) activities significantly. We concluded that HAE was the most efficient extraction technique as high yield of compounds and promising bioactivities were recorded from extracts prepared. Multivariate analysis showed that types of solvents influenced recovery of compounds and biological activities. This research study can be used as one methodological starting point for further investigation on these plants as all results are clearly promising and open the door to further research challenges such as cytotoxicity evaluation, molecular docking analysis, and more screening of pharmacological actions.

7.
Food Chem Toxicol ; 156: 112446, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34339749

RESUMO

The genus Acacia (Family Leguminosae) is composed of several medicinal plants used for treating miscellaneous diseases. Amid the important members of this genus, A. nilotica and A. ataxacantha are widely employed for their tremendous healing properties. Hence, this present work aimed to determine the total phenolic and flavonoid contents and investigate the antioxidant, antiproliferative, anti-enzyme and antimicrobial potentials of methanolic and water extracts of leaves and stem bark of A. nilotica and A. ataxacantha obtained by maceration and ultrasonication. The total phenolic and flavonoid contents were obtained in the range of 33.35-116.60 mg GAE/g and 0.26-49.90 mg RE/g, respectively, with the methanolic leaf extracts of both species showing the highest contents. Moreover, the methanolic extracts were observed to display higher antioxidant potentials in almost all antioxidant assays performed compared to the water extracts (ABTS: 52.66-943.81 mg TE/g, DPPH: 8.51-493.90 mg TE/g, CUPRAC: 106.39-1193.75 mg TE/g; FRAP: 31.38-416.21 mg TE/g, and phosphomolybdenum: 0.90-4.17 mM TE/g). However, the water extracts were seen to be better metal chelators than the methanolic extracts (8.47-36.85 mg EDTAE/g). Additionally, all extracts were found to exhibit anti-tyrosinase (30.79-74.80 mg KAE/g) and anti-amylase (0.10-1.10 mM ACAE/g) properties. With the exception of a few extracts, glucosidase and acetylcholinesterase inhibitions (1.69-2.12 mg ACAE/g and 0.42-2.61 mg GALAE/g, respectively) were also demonstrated. While the methanolic extracts of both species showed antimicrobial potency against all the 18 tested microorganisms (gram positive, gram negative, and fungi), the water extracts were effective only against the gram positive bacteria. The extracts were also found to exhibit antiproliferative effects on SH-SY5Y human neuroblastoma cells, with the methanolic extracts showing higher cytotoxic potential than the water extracts. Therefore, this study showed these species to be good sources of antioxidants, enzyme inhibitors, antimicrobials and antiproliferative agents, which could be of great interest for their applications as natural bioactive ingredients in the development of pharmaceuticals and nutraceuticals.

8.
Chem Biodivers ; 18(10): e2100371, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34390173

RESUMO

Spermacoce verticillata (L.) G. Mey. is commonly used in the folk medicine by various cultures to manage common diseases. Herein, the chemical and biological profiles of S. verticillata were studied in order to provide a comprehensive characterization of bioactive compounds and also to highlight the therapeutic properties. The in vitro antioxidant activity using free-radical scavenging, phosphomolybdenum, ferrous-ion chelating and reducing power assays, and the inhibitory activity against key enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase of S. verticillata extracts (dichloromethane, ethyl acetate, methanol and water) were investigated. The highest total phenolic and flavonoid content were observed in the methanolic and aqueous extracts. Exhaustive 2DNMR investigation has revealed the presence of rutin, ursolic and oleanoic acids. The methanolic extract, followed by aqueous extract have showed remarkable free radical quenching and reducing ability, while the dichloromethane extract was the best source of metal chelators. The tested extracts showed notable inhibitory activity against cholinesterases (AChE: 1.63-4.99 mg GALAE/g extract and BChE: 12.40-15.48 mg GALAE/g extract) and tyrosinase (60.85-159.64 mg KAE/g extract). No inhibitory activity was displayed by ethyl acetate and aqueous extracts against BChE and tyrosinase, respectively. All the tested extracts showed modest α-amylase inhibitory activity, while only the ethyl acetate and aqueous extracts were potent against α-glycosidase. This study further validates the use of S. verticillata in the traditional medicine, while advocating for further investigation for phytomedicine development.

9.
J Pharm Biomed Anal ; 204: 114283, 2021 Sep 10.
Artigo em Inglês | MEDLINE | ID: mdl-34329923

RESUMO

This study was aimed at providing a comprehensive phytochemical characterization and multi-biological assessment of Symphytum officinale L., a medicinal plant with a noteworthy traditional use, and Anchusa ochroleuca M. Bieb., a Boraginaceae species from the Romanian flora. The dichloromethane, methanol and 65 % ethanol extracts obtained from the roots and aerial parts of both plants revealed the presence of numerous phenolic acids, oxygenated fatty acids, pyrrolizidine alkaloids (PAs) and flavonoids, as assessed by LC-HRMS/MS analysis. Consistent with their higher total phenolic content, the polar aerial part extracts of S. officinale and root extracts of A. ochroleuca showed the most significant antioxidant activities, as evaluated by DPPH (173.22-216.98 mg TE/g) and ABTS (219.41-311.97 mg TE/g) radical scavenging, CUPRAC (387.18-626.40 mg TE/g), FRAP (199.36-299.86 mg TE/g) and total antioxidant capacity (2.28-2.68 mmol TE/g). Furthermore, both plants exhibited good tyrosinase (19.11-43.89 mg KAE/g) and α-glucosidase (2.45-12.54 mmol ACAE/g) inhibitory effects. The orthogonal projections to latent structures discriminant analysis (OPLS-DA) allowed the objective differentiation between the roots and aerial parts of the two investigated species based on their phytochemical and biological profiles. The partial least square (PLS) analysis showed that several individual phenolic acids, such as danshensu, rabdosiin and rosmarinic acid, significantly contributed to the antioxidant potential of both Boraginaceae species, whilst the relative levels of sucrose were positively correlated with the anti-enzymatic properties. Overall, S. officinale and A. ochroleuca could be regarded as rich sources of bioactive phytochemicals that could further lead to developing novel phyto-pharmaceutical commodities.


Assuntos
Boraginaceae , Confrei , Antioxidantes/farmacologia , Cromatografia Líquida , Compostos Fitoquímicos , Extratos Vegetais/farmacologia
10.
Int J Mol Sci ; 22(14)2021 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-34299238

RESUMO

This study focused on the biological evaluation and chemical characterization of Geranium pyrenaicum Burm. f. Different solvent extracts (hexane, ethyl acetate, methanol, and water extracts) were prepared. The phytochemical profile, antioxidant, and enzyme inhibitory activity were investigated. Cytotoxicity was assessed using VERO, FaDu, HeLa and RKO cells. The antiviral activity was carried out against HSV-1 (Herpes simplex virus 1) propagated in VERO cell line. The aqueous extract, possessing high phenolic content (170.50 mg gallic acid equivalent/g extract), showed the highest reducing capacity (613.27 and 364.10 mg Trolox equivalent/g extract, for cupric reducing antioxidant capacity and ferric reducing antioxidant power, respectively), radical scavenging potential (469.82 mg Trolox equivalent/g extract, against 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)), metal chelating ability (52.39 mg ethylenediaminetetraacetic acid equivalent/g extract) and total antioxidant capacity (3.15 mmol Trolox equivalent/g extract). Liquid chromatography-electrospray ionization-quadrupole time-of-flight-mass spectrometry (LC-ESI-QTOF-MS/MS) alloved to tentatively identify a total of 56 compounds in the extracts, including ellagitannins, gallic acid and galloyl derivatives amongst others. The ethyl acetate extracts substantially depressed cholinesterase enzymes (4.49 and 12.26 mg galantamine equivalent/g extract against AChE and BChE, respectively) and α-amylase enzyme (1.04 mmol acarbose equivalent/g extract). On the other hand, the methanolic extract inhibited tyrosinase (121.42 mg kojic acid equivalent/g extract) and α-glucosidase (2.39 mmol acarbose equivalent/g extract) activities. The highest selectivity towards all cancer cell lines (SI 4.5-10.8) was observed with aqueous extract with the FaDu cells being the most sensitive (CC50 40.22 µg/mL). It can be concluded that the presence of certain bioactive antiviral molecules may be related to the high anti HSV-1 activity of the methanolic extract. This work has generated vital scientific data on this medicinal plant, which is a prospective candidate for the creation of innovative phyto-pharmaceuticals.


Assuntos
Geranium/metabolismo , Extratos Vegetais/química , Animais , Antioxidantes , Antivirais , Linhagem Celular , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/análise , Humanos , Fenóis/análise , Compostos Fitoquímicos/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Estudos Prospectivos , Espectrometria de Massas por Ionização por Electrospray/métodos , Espectrometria de Massas em Tandem/métodos
11.
J Pharm Biomed Anal ; 203: 114184, 2021 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-34107441

RESUMO

The methanolic and water extracts of Carapa procera leaves and stem barks were screened for their phytochemical content using a multi-technique approach. The extracts were also assessed for their in vitro antioxidant capacity along with their anti-diabetic (α-amylase, α-glucosidase), anti-tyrosinase, anti-elastase and anti-cholinesterase (AChE, BChE) activities. Furthermore, antibacterial and antifungal effects were determined against several bacterial and fungal strains. Data Integration Analysis for Biomarker discovery using Latent components (DIABLO) integrative analysis was conducted on collected data to determine the influence of extraction solvents and plant parts on phytochemical content, antioxidant properties and enzyme inhibitory properties of C. procera samples. Additionally, the major identified compounds were screened as modulators of multiple pathways involved in human diseases via Gene Ontology (GO) enrichment analysis. Results showed that methanolic stem bark extract exhibited the most potent ABTS scavenging, Cu2+ and Fe3+ reducing power, total antioxidant capacity and Fe2+ chelating power and displayed the highest total flavanol content. Methanolic extracts of leaves and stem barks were abounded with phenolics and had the greatest anti-AChE, anti-BChE, anti-tyrosinase and anti-elastase activities. A significant antifungal activity was observed, with the lowest minimum inhibitory concentration and minimum fungicidal values of 0.07 and 0.15 mg/mL, respectively. DIABLO integrative analysis suggested that the phytochemical content and biological activities varied significantly within the plant parts and were influenced by types of solvent used. GO enrichment analysis on the main bioactive compounds showed modulation of multiple pathways associated with cancer. Obtained results demonstrated that stem bark and leaves of C. procera can be considered as promising sources of bioactive molecules with high pharmacological values.


Assuntos
Meliaceae , Extratos Vegetais , Antioxidantes/farmacologia , Cromatografia Líquida , Porcelana Dentária , Humanos , Ligas Metalo-Cerâmicas , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Espectrometria de Massas em Tandem , Titânio
12.
Antioxidants (Basel) ; 10(5)2021 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-34067702

RESUMO

Jatropha L. species, in particular, J. curcas and J. gossypiifolia, are well known medicinal plants used for treating various diseases. In the present study, leaf and stem bark extracts of J. curcas and J. gossypiifolia obtained by maceration or homogenizer assisted extraction, were investigated for their phytochemical contents and biological potential as antioxidants, enzyme inhibitors and neuromodulators. In this regard, the gene expression of tumor necrosis factor α (TNFα) and brain-derived neurotrophic factor (BDNF) was investigated in hypothalamic HypoE22 cells. Finally, a bioinformatics analysis was carried out with the aim to unravel the putative mechanisms consistent with both metabolomic fingerprints and pharmacological effects. The leaf extracts of J. curcas showed higher total phenolic content (TPC) and total flavonoid content (TFC) than the stem bark extracts (range: 5.79-48.95 mg GAE/g and 1.64-13.99 mg RE/g, respectively), while J. gossypiifolia possessed TPC and TFC in the range of 42.62-62.83 mg GAE/g and 6.97-17.63 mg RE/g, respectively. HPLC-MS/MS analysis revealed that the leaf extracts of both species obtained by homogenizer assisted extraction are richer in phytochemical compounds compared to the stem bark extracts obtained by the same extraction method. In vitro antioxidant potentials were also demonstrated in different assays (DPPH: 6.89-193.93 mg TE/g, ABTS: 20.20-255.39 mg TE/g, CUPRAC: 21.07-333.30 mg TE/g, FRAP: 14.02-168.93 mg TE/g, metal chelating activity: 3.21-17.51 mg EDTAE/g and phosphomolybdenum assay: 1.76-3.55 mmol TE/g). In particular, the leaf extract of J. curcas and the stem bark extract of J. gossypiifolia, both obtained by homogenizer assisted extraction, showed the most potent antioxidant capacity in terms of free radical scavenging and reducing activity, which could be related to their higher TPC and TFC. Furthermore, anti-neurodegenerative (acetylcholinesterase inhibition: 1.12-2.36 mg GALAE/g; butyrylcholinetserase inhibition: 0.50-3.68 mg GALAE/g), anti-hyperpigmentation (tyrosinase inhibition: 38.14-57.59 mg KAE/g) and antidiabetic (amylase inhibition: 0.28-0.62 mmol ACAE/g; glucosidase inhibition: 0.65-0.81 mmol ACAE/g) properties were displayed differentially by the different extracts. Additionally, the extracts were effective in reducing the gene expression of both TNFα and BDNF, which could be partially mediated by phenolic compounds such as naringenin, apigenin and quercetin. Indeed, the scientific data obtained from the present study complement the several other reports highlighting the pharmacological potentials of these two species, thus supporting their uses as therapeutically active plants.

13.
Food Chem Toxicol ; 154: 112330, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34116105

RESUMO

Astragalus L. (Fabaceae) is an important genus with numerous species having various traditional medicinal uses making them of interest for scientific investigations to ascertain their therapeutic benefits. In the present study, the quantitative polyphenolic profiles of methanolic extracts from different parts (leaves, flowers, and roots) of two endemic Astragalus species growing in Turkey, i.e. A. campylosema Boiss. and A. hirsutus Vahl were determined, along with their antioxidant and enzyme inhibitory properties. A. campylosema and A. hirsutus extracts showed varying total phenolic (25.80-40.60 and18.59-29.46 mg GAE/g, respectively) and total flavonoid (11.21-105.91 and 16.06-131.91 mg RE/g, respectively) contents. HPLC-MS/MS revealed rutin to be the predominant phenolic compound in all the extracts of A. campylosema and leaf extract of A. hirsutus (133.53-752.42 µg g-1), while hyperoside was the major one in the flower and root extracts of A. hirsutus (2014.07 and 123.13 µg g-1, respectively). In DPPH and ABTS assays, radical scavenging capacity was demonstrated by all extracts of A. campylosema (47.13-48.10 and 87.03-115.36 mg TE/g, respectively) and A. hirsutus (17.82-38.67 and 47.84-57.29 mg TE/g, respectively). Reducing activity was also displayed by the extracts in CUPRAC and FRAP assays (A. campylosema: 83.06-135.20 and 59.15-90.19 mg TE/g, respectively; A. hirsutus: 53.02-83.42 and 31.25-43.25 mg TE/g, respectively). All extracts were also found to act as metal chelators (12.32-21.45 mg EDTAE/g) and exhibited total antioxidant capacity ranging from 1.16 to 1.60 mmol TE/g, in phosphomolybdenum assay. Acetyl- and butyryl-cholinesterase inhibitory effects were observed by all the extracts of the two species (1.56-4.99 mg GALAE/g). Anti-hyperpigmentation potential by inhibiting tyrosinase (54.55-67.35 mg KAE/g) was reported as well. Carbohydrate hydrolyzing enzymes, amylase and glucosidase were also inhibited (0.22-1.03 mmol ACAE/g). Overall, A. campylosema extracts showed relatively better antioxidant and enzyme inhibitory potentials compared to A. hirsutus extracts. Strikingly, A. hirsutus extracts was found to have higher AGE inhibition activity than A. campylosema. Although the cytotoxic effect of three different organs obtained from A. campylosema and A. hirsutus increased depending on the dose (from 10 to 200 µg/mL), it was found that both plant extracts did not show a genotoxic effect at the highest concentration of 200 µg/mL. Indeed, data amassed from this current scientific work showed the two selected Astragalus species to be rich in bioactive polyphenols that could be responsible for the various pharmacological activities and hence demands to be further explored for their possible applications as natural health promoting agents.


Assuntos
Astrágalo (Planta)/química , Flavonoides/análise , Extratos Vegetais/análise , Polifenóis/análise , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/toxicidade , Astrágalo (Planta)/classificação , Inibidores Enzimáticos/análise , Inibidores Enzimáticos/química , Inibidores Enzimáticos/toxicidade , Flavonoides/química , Flavonoides/toxicidade , Flores/química , Produtos Finais de Glicação Avançada/efeitos dos fármacos , Células HeLa , Humanos , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Folhas de Planta/química , Raízes de Plantas/química , Polifenóis/química , Polifenóis/toxicidade , Turquia
14.
Food Chem Toxicol ; 153: 112268, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34015423

RESUMO

The Tanacetum genus is a big treasure with the presence of biologically-active compounds and members of this genus are widely used for the treatment of several diseases in traditional medicine system. Considering this fact, we aimed to analyze the extracts from Tanacetum vulgare L. in case of chemical profiles and biological effects. Chemical characterization was performed by using UHPLC-HRMS technique and showed the presence of several phytochemical groups (107 compounds were identified, including phenolic acids, flavonoids, terpenoids and fatty acids. Biological abilities were examined by using antioxidant (DPPH, ABTS, FRAP, CUPRAC, metal chelating and phosphomolybdenum assays) and enzyme inhibition (tyrosinase, amylase, glucosidase and cholinesterase) properties. Pharmaco-toxicological investigations were also performed with the aim to identify limits of biocompatibility, anti-oxidant and neuromodulatory effects, in hypothalamic HypoE22 cells. A bioinformatic analysis was also carried to unravel the putative protein-targets for the observed biological effects. Generally, the tested hexane and hydroalcoholic extracts displayed stronger activities in antioxidant and enzyme inhibitory assays, when compared with water. In addition, multivariate analysis was performed to understand the differences in both solvents and plant parts and we clearly observed the separation of these parameters. The extracts (10 µg/mL) also stimulated DAT and inhibited TNFα and BDNF gene expression, in HypoE22 cells. In parallel, the extracts were also able to stimulate norepinephrine release from this cell line. By contrast, in the concentration range 50-100 µg/mL, the extracts reduced the HypoE22 viability, thus demonstrating cytotoxicity at concentrations 5-10 fold higher compared to those effective as neuromodulatory. Our observations manifested that T. vulgare has several beneficial effects and it can be used as a potential natural raw material for designing further health-promoting applications in nutraceutical, cosmeceutical, and pharmaceutical areas.


Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Tanacetum/química , Animais , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/toxicidade , Artemia/efeitos dos fármacos , Linhagem Celular , Inibidores Enzimáticos/análise , Inibidores Enzimáticos/química , Inibidores Enzimáticos/toxicidade , Etanol/química , Flores/química , Hexanos/química , Análise Multivariada , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/química , Compostos Fitoquímicos/toxicidade , Componentes Aéreos da Planta/química , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Caules de Planta/química , Mapas de Interação de Proteínas , Ratos , Solventes/química , Água/química
15.
Front Pharmacol ; 12: 660735, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33841167

RESUMO

Hypericum triquetrifolium and H. neurocalycinum were evaluated for their phytochemical content and in vitro bioactivity. NMR analyses were performed on the methanol extract of the aerial parts of H. triquetrifolium to establish the main classes of phytoconstituents. Then, LC-DAD-MSn analyses were performed in order to compare the composition of aerial parts and roots extracts of both Hypericum species, obtained using either methanol or water as solvents. Results, processed using multivariate data analysis, showed a significantly higher phenolic content of methanol extracts compared to water extracts, while minor qualitative differences were observed between the two. Distinctive flavonoid and PAC patterns were observed for H. triquetrifolium and H. neurocalycinum, and specific compounds were exclusively detected in one or the other species. Specifically, the phloroglucinols 7-epiclusianone, hyperfirin and hyperforin were present only in H. neurocalycinum, while hyperforin was detected only in H. triquetrifolium. Extracts were assayed using different in vitro tests to evaluate their antioxidant properties and their inhibitory activity against several enzymes, showing significant antioxidant and metal chelating activities. Furthermore, inhibitory properties against acetylcholinesterase, butyrylcholinesterase and tyrosinase were observed. Multivariate approaches were used to correlate biological data with the phytochemical composition of the different extracts. The results, showing positive correlations between specific chemical constituents and the measured bioactivities, represent preliminary data that could guide future studies aimed at isolating bioactive constituents from H. neurocalycinum and H. triquetrifolium for further pharmacological evaluations.

16.
Pharmaceuticals (Basel) ; 14(4)2021 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-33921724

RESUMO

To date, the leading causes of mortality and morbidity worldwide include viral infections, such as Ebola, influenza virus, acquired immunodeficiency syndrome (AIDS), severe acute respiratory syndrome (SARS) and recently COVID-19 disease, caused by the SARS-CoV-2 virus. Currently, we can count on a narrow range of antiviral drugs, especially older generation ones like ribavirin and interferon which are effective against viruses in vitro but can often be ineffective in patients. In addition to these, we have antiviral agents for the treatment of herpes virus, influenza virus, HIV and hepatitis virus. Recently, drugs used in the past especially against ebolavirus, such as remdesivir and favipiravir, have been considered for the treatment of COVID-19 disease. However, even if these drugs represent important tools against viral diseases, they are certainly not sufficient to defend us from the multitude of viruses present in the environment. This represents a huge problem, especially considering the unprecedented global threat due to the advancement of COVID-19, which represents a potential risk to the health and life of millions of people. The demand, therefore, for new and effective antiviral drugs is very high. This review focuses on three fundamental points: (1) presents the main threats to human health, reviewing the most widespread viral diseases in the world, thus describing the scenario caused by the disease in question each time and evaluating the specific therapeutic remedies currently available. (2) It comprehensively describes main phytochemical classes, in particular from plant foods, with proven antiviral activities, the viruses potentially treated with the described phytochemicals. (3) Consideration of the various applications of drug delivery systems in order to improve the bioavailability of these compounds or extracts. A PRISMA flow diagram was used for the inclusion of the works. Taking into consideration the recent dramatic events caused by COVID-19 pandemic, the cry of alarm that denounces critical need for new antiviral drugs is extremely strong. For these reasons, a continuous systematic exploration of plant foods and their phytochemicals is necessary for the development of new antiviral agents capable of saving lives and improving their well-being.

17.
Molecules ; 26(7)2021 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-33800622

RESUMO

Croton hirtus L'Hér methanol extract was studied by NMR and two different LC-DAD-MSn using electrospray (ESI) and atmospheric pressure chemical ionization (APCI) sources to obtain a quali-quantitative fingerprint. Forty different phytochemicals were identified, and twenty of them were quantified, whereas the main constituents were dihydro α ionol-O-[arabinosil(1-6) glucoside] (133 mg/g), dihydro ß ionol-O-[arabinosil(1-6) glucoside] (80 mg/g), ß-sitosterol (49 mg/g), and isorhamnetin-3-O-rutinoside (26 mg/g). C. hirtus was extracted with different solvents-namely, water, methanol, dichloromethane, and ethyl acetate-and the extracts were assayed using different in vitro tests. The methanolic extracts presented the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), and ferric reducing antioxidant power (FRAP) values. All the tested extracts exhibited inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with a higher activity observed for dichloromethane (AChE: 5.03 and BChE: 16.41 mgGALAE/g), while the methanolic extract showed highest impact against tyrosinase (49.83 mgKAE/g). Taken together, these findings suggest C. hirtus as a novel source of bioactive phytochemicals with potential for commercial development.


Assuntos
Antioxidantes/química , Inibidores da Colinesterase/química , Croton/química , Glucosídeos/química , Compostos Fitoquímicos/química , Fitosteróis/química , Terpenos/química , Acetatos/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Antioxidantes/classificação , Antioxidantes/isolamento & purificação , Benzotiazóis/antagonistas & inibidores , Benzotiazóis/química , Compostos de Bifenilo/antagonistas & inibidores , Compostos de Bifenilo/química , Butirilcolinesterase/química , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/isolamento & purificação , Croton/metabolismo , Glucosídeos/classificação , Glucosídeos/isolamento & purificação , Humanos , Metanol/química , Cloreto de Metileno/química , Compostos Fitoquímicos/classificação , Compostos Fitoquímicos/isolamento & purificação , Fitosteróis/classificação , Fitosteróis/isolamento & purificação , Picratos/antagonistas & inibidores , Picratos/química , Extratos Vegetais/química , Solventes/química , Relação Estrutura-Atividade , Ácidos Sulfônicos/antagonistas & inibidores , Ácidos Sulfônicos/química , Terpenos/classificação , Terpenos/isolamento & purificação , Água/química
18.
J Pharm Biomed Anal ; 198: 114018, 2021 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-33730614

RESUMO

Caesalpinia bonduc and C. decapeleta var. japonica have great importance in traditional medicine systems but scientific information's are still lacking for their potentials. To explore their bioactivity, we assessed the antioxidant, enzyme inhibitory abilities of the dichloromethane (DCM), ethyl acetate, methanol, and water extracts prepared from the leaves and bark. The cytotoxicity and anticancer properties of the extracts were also assessed in vitro. The water extract of C. decapeleta leaves possessed highest phenolic content (108.16 mg gallic acid equivalent (GAE)/g extract), while the highest flavonoid content was recorded for the C. bonduc leaf methanolic extract (27.89 mg rutin equivalent (RE)/g extract). In general, C. decapeleta extracts possessed higher radical scavenging potential compared to C. bonduc extracts. C. decapeleta DCM leaves extract (10.20 mg galantamine equivalent (GALAE)/g extract) showed highest inhibition against butyrylcholinesterase. The cytotoxicity of the most potent methanolic and aqueous extracts were assessed against four cell lines. The chemical profiles of both species appeared to be different. C. bonduc was abundant in organic and phenolic acids as well as their esters. Flavonoid glycosides, bonducellin and its derivatives and caesalminaxins were identified. Whereas, C. decalpetala possessed many galloylated compounds. The cytotoxicity of C. bonduc and C. decapetala extracts was tested using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) based assay on VERO (kidney of an adult African Green monkey cells), HeLa (human cervical adenocarcinoma cells), RKO (human colon carcinoma cells), FaDu (human hypopharyngeal squamous carcinoma cells) cell lines. C. bonduc bark water extract exhibited the highest cytotoxicity towards HeLa (50 % cytotoxic concentration (CC50): 28.5 µg/mL) cancer cell line, as compared to normal VERO cells (CC50:35.87 µg/mL). For C. decapetala, the highest cytotoxicity was found for bark methanol extract on the HeLa cells with CC50 of 46.08 µg/mL and selectivity index of 3.33. In the gene ontology analysis, prostate cancer, nuclear factor kappa B (NF-kappa B) signaling, proteoglycans in cancer pathways might support the results of the cytotoxic assays. These results showed that the tested Caesalpinia species, showing potent inhibitory action against butyrylcholinesterase, might represent novel phytotherapeutic avenues for the management of Alzheimer's disease.


Assuntos
Farmácia , Extratos Vegetais , Animais , Antioxidantes/farmacologia , Chlorocebus aethiops , Biologia Computacional , Células HeLa , Humanos , Extratos Vegetais/farmacologia , Células Vero
19.
Antibiotics (Basel) ; 10(2)2021 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-33672329

RESUMO

To avail the possible pharmacological actions of Brideliaferruginea Benth., the present investigation was designed to quantitatively analyze the total flavonoid and phenolic contents and assess the various antioxidant and enzyme inhibition properties of leaf and stem bark extracts (ethyl acetate, water and methanolic) of B. ferruginea. Anti-proliferative effect was also investigated against human colon cancer cells (HCT116) as well as the antimicrobial potential against multiple bacterial and fungal (yeasts and dermatophytes) strains. The methanolic and water extracts of the stem bark demonstrated the highest phenolic content (193.58 ± 0.98 and 187.84 ± 1.88 mg/g, respectively), while the leaf extracts showed comparatively higher flavonoid contents (24.37-42.31 mg/g). Overall, the methanolic extracts were found to possess the most significant antioxidant potency. Compared to the other extracts, methanolic extracts of the B. ferruginea were revealed to be most potent inhibitors of acetyl- and butyryl-cholinesterases, tyrosinase α-amylase, except α-glucosidase. Only the ethyl acetate extracts were found to inhibit glucosidase. Additionally, the stem bark methanolic extract also showed potent inhibitory activity against E. coli and gram-positive bacteria (MIC (minimum inhibitory concentration): 2.48-62.99 µg/mL), as well as all the tested fungi (MIC: 4.96-62.99 µg/mL). In conclusion, B. ferruginea can be regarded as a promising source of bioactive compounds displaying multifunctional pharmacological activities and thus is a potential candidate for further investigations in the endeavor to develop botanical formulations for pharmaceutical and cosmeceutical industries.

20.
Biomolecules ; 11(2)2021 02 04.
Artigo em Inglês | MEDLINE | ID: mdl-33557215

RESUMO

Alchornea cordifolia (Schumach. & Thonn.) Müll. Arg. is a well-known African medicinal plant traditionally used for various healing purposes. In the present study, methanolic, ethyl acetate and infusion extracts of A. cordifolia leaves were studied for their total phenolic and flavonoid contents and screened for their chemical composition. Moreover, the enzyme (acetyl- and butyryl-cholinesterases, α-amylase, α-glucosidase, and tyrosinase) inhibitory and cytotoxicity activities on HepG2: human hepatocellular carcinoma cells, B16 4A5: murine melanoma cells, and S17: murine bone marrow (normal) cells of extracts were evaluated. Finally, components-targets and docking analyzes were conducted with the aim to unravel the putative mechanisms underlying the observed bio-pharmacological effects. Interestingly, the infusion and methanolic extracts showed significantly higher total phenolic and flavonoid contents compared with the ethyl acetate extract (TPC: 120.38-213.12 mg GAE/g and TFC: 9.66-57.18 mg RE/g). Besides, the methanolic extracts followed by the infusion extracts were revealed to contain a higher number of compounds (84 and 74 compounds, respectively), while only 64 compounds were observed for the ethyl acetate extract. Gallic acid, ellagic acid, shikimic acid, rutin, quercetin, myricetin, vitexin, quercitrin, kaempferol, and naringenin were among the compounds that were commonly identified in all the studied extracts. Additionally, the methanolic and infusion extracts displayed higher antioxidant capacity than ethyl acetate extract in all assays performed. In ABTS and DPPH radical scavenging assays, the methanol extract (500.38 mg TE/g for DPPH and 900.64 mg TE/g for ABTS) exhibited the best ability, followed by the water and ethyl acetate extracts. Furthermore, the extracts exhibited differential enzyme inhibitory profiles. In particular, the methanolic and infusion extracts showed better cytotoxic selectivity activity against human hepatocellular carcinoma cells. Overall, this study demonstrated A cordifolia to be a species worthy of further investigations, given its richness in bioactive phytochemicals and wide potentialities for antioxidants and pharmacological agents.


Assuntos
Antioxidantes/química , Euphorbiaceae/química , Euphorbiaceae/metabolismo , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Animais , Antioxidantes/farmacologia , Benzotiazóis/química , Compostos de Bifenilo/química , Carcinoma Hepatocelular/tratamento farmacológico , Biologia Computacional , Avaliação Pré-Clínica de Medicamentos , Flavonoides/farmacologia , Sequestradores de Radicais Livres , Células Hep G2 , Humanos , Quempferóis , Neoplasias Hepáticas/tratamento farmacológico , Melanoma Experimental , Metanol/química , Camundongos , Monofenol Mono-Oxigenase , Fenóis/química , Picratos/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plantas Medicinais , Ácidos Sulfônicos/química
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