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1.
Food Chem ; 368: 130782, 2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-34392121

RESUMO

In this study, the aerial parts and bulbs of nine Allium species were investigated for their functional phytochemical profile, in vitro antioxidant activities, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, α-glucosidase, and tyrosinase inhibitory properties. Phenolics, alkaloids, glucosinolates and other sulfur-containing compounds were distinctively profiled in the different species. Maceration in methanol allowed recovering the highest cumulative phenolic content in A. scabrifolium (42.31 mg/g), followed by A. goekyigiti (33.15 mg/g) and A. atroviolaceum (28.35 mg/g). The aerial parts of all Allium species showed high in vitro antioxidant activity whereas methanolic extract of A. cappadocicum bulb showed the highest inhibition against AChE (2.44 mg galantamine equivalent/g) and the water extracts of A. isauricum aerial part were the best BChE inhibitors (4.31 mg galantamine equivalent/g). Bulbs were the richer source of oligosaccharides, and in vitro digestion determined an increase of oligosaccharides bioaccessibility. A promising nutraceutical potential could be highlighted in our understudied Allium species.


Assuntos
Allium , Antioxidantes , Acetilcolinesterase , Antioxidantes/farmacologia , Butirilcolinesterase , Inibidores Enzimáticos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia
2.
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.

3.
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.

4.
Antioxidants (Basel) ; 10(10)2021 Sep 24.
Artigo em Inglês | MEDLINE | ID: mdl-34679647

RESUMO

Seseli L. is one of the largest genera of the Apiaceae family widely known for their traditional uses as herbal remedies. In the present study, the methanolic and water extracts of two Seseli species, S. gummiferum and S. transcaucasicum were evaluated for their bioactive contents and biological activities. The total phenolic and flavonoid contents in the extracts ranged from 19.09 to 24.33 mg GAE/g and from 0.45 to10.09 mg RE/g, respectively. Moreover, while narcissin was detected as the most abundant component in the methanolic extract of S. transcaucasicum (261.40 µg/g), chlorogenic acid was identified as the major component in all the other extracts, although a high amount was also present in the methanolic S. transcaucasicum extract (107.48-243.12 µg/g). The total antioxidant capacity was also determined by the phosphomolybdenum assay (0.66-1.18 mM TE/g). Other antioxidant assays such as the radical scavenging assays (DPPH: 5.51-11.45 mg TE/g; ABTS: 43.46-51.91 mg TE/g), reducing assays (CUPRAC: 41.67-53.20 mg TE/g; FRAP: 31.26-34.14 mg TE/g), as well as the metal chelating activity assay (14.38-38.57 mg EDTAE/g) were conducted. All the extracts showed inhibitory potential against the enzyme's amylase (0.12-0.78 mM ACAE/g), acetyl- and butyryl-cholinesterase (0.15-9.71 mg GALAE/g), while only the methanolic extracts acted as inhibitors of tyrosinase (107.15 and 109.37 mg KAE/g) and only the water extract of S. gummiferum displayed anti-glucosidase activity (0.13 mM ACAE/g). Interestingly, the methanolic extracts of both Seseli species showed lower cytotoxicity towards HaCaT cells (IC50: >500 µg/mL), compared to the water extracts (IC50: 267.8 and 321.41 µg/mL). Besides, only the methanolic extracts showed a slight wound healing effect (28.21 and 31.23%). All extracts showed antibacterial action against Staphylococcus lugdunensis (minimum inhibitory and bactericidal concentrations: 0.025-2 mg/mL). S. gummiferum methanolic extract, which exhibited the highest antibacterial potency was found to inhibit adhesion and invasion of S. lugdunensis to HaCaT cells as well. Taken together, this study demonstrated the two Seseli species to harbour interesting bioactive components, in particular polyphenolics and to exhibit several biological properties that could be further investigated for their potential exploitation as healing agents as supported by various traditional medicinal uses.

5.
Molecules ; 26(19)2021 Sep 23.
Artigo em Inglês | MEDLINE | ID: mdl-34641314

RESUMO

The recent emergence of Zika virus (ZIKV) in Brazil and the increasing resistance developed by pathogenic bacteria to nearly all existing antibiotics should be taken as a wakeup call for the international authority as this represents a risk for global public health. The lack of antiviral drugs and effective antibiotics on the market triggers the need to search for safe therapeutics from medicinal plants to fight viral and microbial infections. In the present study, we investigated whether a mangrove plant, Bruguiera gymnorhiza (L.) Lam. (B. gymnorhiza) collected in Mauritius, possesses antimicrobial and antibiotic potentiating abilities and exerts anti-ZIKV activity at non-cytotoxic doses. Microorganisms Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Klebsiella pneumoniae ATCC 70603, methicillin-resistant Staphylococcus aureus ATCC 43300 (MRSA), Salmonella enteritidis ATCC 13076, Sarcina lutea ATCC 9341, Proteus mirabilis ATCC 25933, Bacillus cereus ATCC 11778 and Candida albicans ATCC 26555 were used to evaluate the antimicrobial properties. Ciprofloxacin, chloramphenicol and streptomycin antibiotics were used for assessing antibiotic potentiating activity. ZIKVMC-MR766NIID (ZIKVGFP) was used for assessing anti-ZIKV activity. In silico docking (Autodock 4) and ADME (SwissADME) analyses were performed on collected data. Antimicrobial results revealed that Bruguiera twig ethyl acetate (BTE) was the most potent extract inhibiting the growth of all nine microbes tested, with minimum inhibitory concentrations ranging from 0.19-0.39 mg/mL. BTE showed partial synergy effects against MRSA and Pseudomonas aeruginosa when applied in combination with streptomycin and ciprofloxacin, respectively. By using a recombinant ZIKV-expressing reporter GFP protein, we identified both Bruguiera root aqueous and Bruguiera fruit aqueous extracts as potent inhibitors of ZIKV infection in human epithelial A549 cells. The mechanisms by which such extracts prevented ZIKV infection are linked to the inability of the virus to bind to the host cell surface. In silico docking showed that ZIKV E protein, which is involved in cell receptor binding, could be a target for cryptochlorogenic acid, a chemical compound identified in B. gymnorhiza. From ADME results, cryptochlorogenic acid is predicted to be not orally bioavailable because it is too polar. Scientific data collected in this present work can open a new avenue for the development of potential inhibitors from B. gymnorhiza to fight ZIKV and microbial infections in the future.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antivirais/farmacologia , Extratos Vegetais/farmacologia , Rhizophoraceae/química , Zika virus/crescimento & desenvolvimento , Antibacterianos/química , Antifúngicos/química , Antivirais/química , Brasil , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Simulação por Computador , Sinergismo Farmacológico , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Klebsiella pneumoniae/efeitos dos fármacos , Klebsiella pneumoniae/crescimento & desenvolvimento , Maurício , Testes de Sensibilidade Microbiana , Viabilidade Microbiana/efeitos dos fármacos , Extratos Vegetais/química , Proteus mirabilis/efeitos dos fármacos , Proteus mirabilis/crescimento & desenvolvimento , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/crescimento & desenvolvimento , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento , Zika virus/efeitos dos fármacos
6.
Crit Rev Food Sci Nutr ; : 1-16, 2021 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-34672234

RESUMO

Phytochemicals are important bioactive components present in natural products. Although the health benefits of many food products are well-known and accepted as a common knowledge, the identity of the main bioactive molecules and the mechanism by which they interact in the body of human are often unknown. It was only in the last 30 years when the field of metabolomics had matured that the identification of such molecules with bioactivity has been made possible through the development of instruments to separate and computational techniques to characterize complex samples. This in turn has enabled in vitro studies to quantify the biological activity of the respective phytochemical either in mice models or in humans. In this review, the importance of key dietary phytochemicals such as phenolic acids, flavonoids, carotenoids, resveratrol, curcumin, and capsaicinoids are discussed together with their potential functions for human health. Untargeted metabolomics, in particular, liquid chromatography mass spectrometry, is the most used method to isolate, identify and profile bioactive compounds in the study of phytochemicals in foods. The application of metabolomics in drug discovery is a common practice nowadays and has boosted the drug and/or supplement manufacturing sector.HighlightsPhytochemicals are beneficial compounds for human healthPhytochemicals are plant-based bioactive and obtainable from natural productsUntargeted metabolomics has boosted the discovery of phytochemicals from foodTargeted metabolomics is key in the authentication and screening of phytochemicalsMetabolomics of phytochemicals is reshaping the road to drug and supplement manufacture.

7.
Front Mol Biosci ; 8: 649395, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34540888

RESUMO

Resveratrol is a polyphenolic stilbene derivative widely present in grapes and red wine. Broadly known for its antioxidant effects, numerous studies have also indicated that it exerts anti-inflammatory and antiaging abilities and a great potential in cancer therapy. Regrettably, the oral administration of resveratrol has pharmacokinetic and physicochemical limitations such as hampering its effects so that effective administration methods are demanding to ensure its efficiency. Thus, the present review explores the published data on the application of resveratrol nanoformulations in cancer therapy, with the use of different types of nanodelivery systems. Mechanisms of action with a potential use in cancer therapy, negative effects, and the influence of resveratrol nanoformulations in different types of cancer are also highlighted. Finally, the toxicological features of nanoresveratrol are also discussed.

8.
Antioxidants (Basel) ; 10(9)2021 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-34573021

RESUMO

Epilobium hirsutum is extensively used as a traditional remedy in folk medicine, especially against prostate inflammation. Therefore, we evaluated the chemical profiles and biopharmaceutical potentials of different extracts of E. hirsutum aerial parts and roots. Metabolomic, antioxidant, and enzyme inhibitory profiles were investigated. Human prostate cancer PC3 cells were exposed to the extracts to evaluate antiproliferative effects. Gene expression and bioinformatics analyses were performed to investigate anti-inflammatory mechanisms. Oenothein B and myricetin were prominent compounds in the extracts. In scavenging/reducing assays, the methanol, infusion, and methanol/water extracts exhibited similar activities. We also observed the reduction of PC3 viability occurring following exposure to methanol and methanol/water extracts. According to bioinformatics analysis, myricetin was predicted to interact with COX-2 and TNFα. The interaction between TNFα and oxo-dihydroxy-octadecenoic acid was predicted as well. Intriguingly, the gene expression of COX-2 and TNFα was reduced in PC3 cells after exposure to methanol and methanol/water extracts. These effects were paralleled by the decreased gene expression of IL-8 and NFkB and the inhibition of PGE2 release. Therefore, the present findings suggest the potential use of E. hirsutum for the management of the burden of inflammation and oxidative stress occurring in lower urinary tract diseases, including prostatitis.

9.
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.

10.
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.

11.
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.

12.
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.

13.
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
14.
Food Chem Toxicol ; 155: 112404, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34246708

RESUMO

Capparis spinose L. also known as Caper is of great significance as a traditional medicinal food plant. The present work was targeted on the determination of chemical composition, pharmacological properties, and in-vitro toxicity of methanol and dichloromethane (DCM) extracts of different parts of C. spinosa. Chemical composition was established by determining total bioactive contents and via UHPLC-MS secondary metabolites profiling. For determination of biological activities, antioxidant capacity was determined through DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays while enzyme inhibition against cholinesterase, tyrosinase, α-amylase and α-glucosidase were also tested. All the extracts were also tested for toxicity against two breast cell lines. The methanolic extracts were found to contain highest total phenolic and flavonoids which is correlated with their significant radical scavenging, cholinesterase, tyrosinase and glucosidase inhibition potential. Whereas DCM extracts showed significant activity for reducing power, phosphomolybdenum, metal chelation, tyrosinase, and α-amylase inhibition activities. The secondary metabolites profiling of both methanolic extracts exposed the presence of 21 different secondary metabolites belonging to glucosinolate, alkaloid, flavonoid, phenol, triterpene, and alkaloid derivatives. The present results tend to validate folklore uses of C. spinose and indicate this plant to be used as a potent source of designing novel bioactive compounds.

15.
Plants (Basel) ; 10(6)2021 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-34207852

RESUMO

Nepeta baytopii is a poorly studied, endemic Nepeta species (Lamiaceae) of Turkey. For the first time, the biological activities (antioxidant, enzyme inhibition, and cytotoxicity properties) of the hexane, ethyl acetate, methanol, water/methanol, and water extracts and essential oil prepared from N. baytopii aerial parts were assessed. Hydro-methanol (41.25 mg gallic acid equivalent (GAE)/g) and water extracts (50.30 mg GAE/g), respectively showed the highest radical scavenging (94.40 and 129.22 mg Trolox equivalent (TE)/g, for 2,2-diphenyl-1-picrylhydrazyl radical and 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid radical scavenging assays) and reducing (229.37 and 129.55 mg TE/g, for ferric-reducing antioxidant power and cupric-reducing antioxidant capacity assays) capacities in vitro. An interestingly high inhibition was observed for ethyl acetate extract against butyrylcholinesterase (10.85 mg galantamine equivalent/g). The methanol extract showed high cytotoxicity (31.7%) against HepG2 cells. Caryophyllene oxide was identified in high concentrations in the essential oil (39.3%). Luteolin and apigenin and their derivatives were identified from the methanol and water extracts. The results obtained from this study highlighted that the abundance of highly bioactive compounds from Nepeta baytopii ensures the multiple biological activities of the tested extracts, and this suggests a potential use in the pharmaceutical and nutraceutical fields, and therefore should be investigated further.

16.
Molecules ; 26(11)2021 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-34200152

RESUMO

Lupin seeds can represent a valuable source of phenolics and other antioxidant compounds. In this work, a comprehensive analysis of the phytochemical profile was performed on seeds from three Lupinus species, including one cultivar (Lupinus albus) and two wild accessions (Lupinus cossentinii and Lupinus luteus), collected from the northern region of Tunisia. Untargeted metabolomic profiling allowed to identify 249 compounds, with a great abundance of phenolics and alkaloids. In this regard, the species L. cossentinii showed the highest phenolic content, being 6.54 mg/g DW, followed by L. luteus (1.60 mg/g DW) and L. albus (1.14 mg/g DW). The in vitro antioxidant capacity measured by the ABTS assay on seed extracts ranged from 4.67 to 17.58 mg trolox equivalents (TE)/g, recording the highest values for L. albus and the lowest for L. luteus. The DPPH radical scavenging activity ranged from 0.39 to 3.50 mg TE/g. FRAP values varied between 4.11 and 5.75 mg TE/g. CUPRAC values for lupin seeds ranged from 7.20 to 8.95 mg TE/g, recording the highest for L. cossentinii. The results of phosphomolybdenum assay and metal chelation showed similarity between the three species of Lupinus. The acetylcholinesterase (AChE) inhibition activity was detected in each methanolic extract analyzed with similar results. Regarding the butyrylcholinesterase (BChE) enzyme, it was weakly inhibited by the Lupinus extracts; in particular, the highest activity values were recorded for L. albus (1.74 mg GALAE/g). Overall, our results showed that L. cossentinii was the most abundant source of polyphenols, consisting mainly in tyrosol equivalents (5.82 mg/g DW). Finally, significant correlations were outlined between the phenolic compounds and the in vitro biological activity measured, particularly when considering flavones, phenolic acids and lower-molecular-weight phenolics.


Assuntos
Antioxidantes/química , Lupinus/química , Compostos Fitoquímicos/química , Sementes/química , Alcaloides/química , Alcaloides/metabolismo , Antioxidantes/metabolismo , Lupinus/metabolismo , Metabolômica/métodos , Fenóis/química , Fenóis/metabolismo , Compostos Fitoquímicos/metabolismo , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Sementes/metabolismo , Tunísia
17.
Food Chem Toxicol ; 156: 112432, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34293424

RESUMO

Herbals in the form of medicine are employed extensively around the world. Herbal and conventional medicine combination is a potentially dangerous practice mainly in comorbid, hepato insufficient and frail patients leading to perilous herb-drug interactions (HDI) and toxicity. This study features potential HDI of 15 globally famous plant species through data mining and computational methods. Several plant species were found to mimic warfarin. Phytochemicals from M. charantia induced hypoglycemica. M. chamomila and G. biloba possessed anticoagulant activities. S. hispanica reduces postprandial glycemia. R. officinalis has been reported to inhibit the efflux of anticancer substrates while A. sativum can boost the clearance of anticancer agents. P. ginseng can alter blood coagulation. A cross link of the biological and in silico data revealed that a plethora of herbal metabolites such as ursolic and rosmarinic acid among others are possible/probable inhibitors of specific CYP450 enzymes. Consequently, plant species/metabolites with a given pharmacological property/metabolizing enzyme should not be mixed with drugs having the same pharmacological property/metabolizing enzyme. Even if combined with drugs, herbal medicines must be used at low doses for a short period of time and under the supervision of a healthcare professional to avoid potential adverse and toxic effects.

18.
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.

19.
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
20.
Neurochem Res ; 46(9): 2205-2225, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34120291

RESUMO

Epilepsy is a related chronic neurological condition of a predisposition for recurrent epileptic seizures, with various manifestations and causes. Although there are antiepileptic drugs, complementary natural therapies are widely used. The purpose of this systematic review was to analyze the antiepileptic/anticonvulsant pharmacological properties of plant-food derived bioactive molecules. In this regard, a systematic review of the PubMed database was made based on the inclusion criteria. Natural compounds/herbs with scientifically proven antiepileptic properties were selected. Experimental pharmacological studies in vitro and in vivo have shown that flavonoids, alkaloids and terpenoids may have anticonvulsant mechanisms similar to the new generation antiepileptic drugs. The relationships of structure-anticonvulsant effect, pharmacological models, seizure-inducing factors and response, effective dose were also analyzed and discussed. The results of in vitro and in vivo pharmacological studies analyzed in this systematic review support the clinical importance of plant-food-derived bioactive molecules for the complementary treatment of epilepsy. Thus, are opened new perspectives to develop new natural anticonvulsant drugs.


Assuntos
Anticonvulsivantes/uso terapêutico , Epilepsia/tratamento farmacológico , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/uso terapêutico , Plantas Medicinais/química , Convulsões/tratamento farmacológico , Alcaloides/farmacologia , Alcaloides/uso terapêutico , Animais , Anticonvulsivantes/farmacologia , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Humanos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Terpenos/farmacologia , Terpenos/uso terapêutico
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