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1.
Plants (Basel) ; 12(19)2023 Sep 26.
Artículo en Inglés | MEDLINE | ID: mdl-37836131

RESUMEN

This study assessed the halophyte species Limonium spathulatum (Desf.) as a possible source of natural ingredients with the capacity to inhibit enzymes related to relevant human health disorders and food browning. Extracts using food-grade solvents such as water and ethanol were prepared by maceration from dried L. spathulatum leaves. They were evaluated for in vitro inhibition activity of enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), α-glucosidase, tyrosinase and lipase, related to Alzheimer's disease, type-2-diabetes mellitus, skin hyperpigmentation, and obesity, respectively. These extracts were also appraised for in vitro acute toxicity on tumoral and non-tumoral cell lines and their chemical composition by high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS/MS). The extracts were more effective towards BChE than AChE. The best results were obtained with the hydroethanolic and water extracts, with IC50 values of 0.03 mg/mL and 0.06 mg/mL, respectively. The hydroethanolic extract had the highest capacity to inhibit α-glucosidase (IC50: 0.04 mg/mL), higher than the positive control used (acarbose, IC50 = 3.14 mg/mL). The ethanol extract displayed the best inhibitory activity against tyrosinase (IC50 = 0.34 mg/mL). The tested samples did not inhibit lipase and exhibited low to moderate cytotoxic activity against the tested cell lines. The hydroethanolic extract had a higher diversity of compounds, followed by the ethanol and water samples. Similar molecules were identified in all the extracts and were mainly hydroxybenzoic acids, hydroxycinnamic acids, and flavonoids. Taken together, these results suggest that L. spathulatum should be further explored as a source of bioactive ingredients for the food, cosmetic, and pharmaceutical industries.

2.
Front Plant Sci ; 13: 979343, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36466224

RESUMEN

This work explored the nutritional and antioxidant properties of the leaves of the halophytic species Limonium spathulatum (Desf.) Kuntze from Tunisian sea cliffs. Furthermore, the analysis of the total phenolics and flavonoids contents and their individual compounds using high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS/MS) were also studied. L. spathulatum leaves had high levels of moisture, ash, neutral detergent fiber, and acid detergent fiber, but low concentrations of crude protein, crude fat and acid detergent lignin. It contained low carbohydrates levels, and low energetic values. The most abundant macroelements were Cl, Na and Ca while the microelements detected in the highest levels were Fe and Zn. No relevant α-amylase inhibition was observed, and no toxic metals (Pb and Cd) and phytic acid were detected. The ethanol and the hydroethanolic extracts had the highest capacity to scavenge free radicals, to chelate iron and copper and to inhibit lipid peroxidation. The same samples were also the most active towards oxidative haemolysis. These extracts contained high total phenolic and flavonoid contents. HPLC analysis, performed on ethanolic extracts identified 58 individual compounds known for their high antioxidant actvitiy including hydroxybenzoic acids (gallic, syringic acids), hydroxycinnamic acids (caffeic, coumaric, ferulic acids) and flavonoids (catechin, epigallocatechin gallate and naringin).In conclusion, the leaves of Tunisian accession of L. spathulatum were good source of minerals and fibers useful in the human diet for attaining nutritional sufficiency. The high in vitro and ex vitro antioxidant activities associated with high favonoids contents and compounds suggest the possibility to use the extracts of L. spathulatum in herbal products with the aim of improving general health and well-being, and/or as food additives for preventing lipid oxidation of lipid-rich foods.

3.
Plants (Basel) ; 11(10)2022 May 19.
Artículo en Inglés | MEDLINE | ID: mdl-35631777

RESUMEN

This work explored the medicinal halophyte Frankenia laevis L. (sea heath) as a potential source of bioactive natural products. In this sense, methanol and dichloromethane extracts were prepared from aerial organs containing flowers, leaves and stems, and were profiled for their chemical composition using high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS/MS). The extracts were evaluated for their in vitro antioxidant capacity using five complementary methods: enzyme inhibitory effects on enzymes related with neurodegeneration (acetyl (AChE) and butyrylcholinesterase (BuChE)), Type 2 diabetes (α-glucosidase and α-amylase), hyperpigmentation/food oxidation (tyrosinase), and cytotoxicity towards human hepatocarcinoma (HepG2) cells. Fifty-one molecules were identified in the extracts, including several derivatives of phenolic acids, lignans and flavonoids, monoterpenes, and hydroxylated derivatives of linoleic acid. The methanol extract was effective in DPPH and ABTS radical scavenging (EC50 = 0.25 and 0.65 mg/mL, respectively), copper chelation (EC50 = 0.78 mg/mL), and iron reduction (EC50 = 0.51 mg/mL) activities, whereas the dichloromethane extract had high iron chelating ability (EC50 = 0.76 mg/mL). Both extracts showed the capacity to inhibit α-glucosidase, especially the dichloromethane (EC50 = 0.52 mg/mL). This extract also exerted a significant selective cytotoxicity towards HepG2 cells (EC50 = 52.1 µg/mL, SI > 1.9). In conclusion, extracts from the aerial parts of sea heath were shown to be a promising source of natural products for pharmaceutical and/or food additive applications due to their high antioxidant, anti-diabetic, and cytotoxic properties.

4.
Anal Methods ; 13(34): 3779-3784, 2021 09 02.
Artículo en Inglés | MEDLINE | ID: mdl-34350441

RESUMEN

This research paper presents simple and quick eco-friendly spot test and spectrophotometric methods for the determination of L-glutathione. The spot test assay is based on the formation of a color complex with phenazine methosulphate and L-glutathione on a thin-layer chromatography plate followed by image analysis using a scanner as a detector. For analysis, the image was converted into red, green, and blue (RGB) histograms. A series of parameters that influenced the color formation were investigated, and under the optimal conditions, a good linearity was observed in the range of 200-1000 µg mL-1 and 249-1000 µg mL-1 of L-glutathione with correlation coefficients of 0.9907 for B and 0.9903 for G channels. For the spectrophotometric method, a good linearity was obtained in the range of 2.1-60 µg mL-1 of L-glutathione concentration with a correlation coefficient of 0.9961. A mechanism of the reaction of L-glutathione with phenazine was proposed and confirmed by Fourier transform infrared and mass spectroscopy.


Asunto(s)
Glutatión , Fenazinas , Cromatografía en Capa Delgada , Metosulfato de Metilfenazonio , Espectrofotometría
5.
Molecules ; 26(14)2021 Jul 19.
Artículo en Inglés | MEDLINE | ID: mdl-34299641

RESUMEN

The reaction of a diene nitroxide precursor with dichlorophenylphosphine in a McCormac procedure afforded 1,1,3,3-tetramethyl-5-phenyl-1,2,3,4,5,6-hexahydrophospholo[3,4-c]pyrrole-5-oxide-2-oxyl. Lithiation of the protected 3-iodo-pyrroline nitroxide followed by treatment with chlorodiphenylphosphine after deprotection afforded (1-oxyl-2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrol-3-yl)diphenylphosphine oxide, and after reduction, (1-oxyl-2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrol-3-yl)diphenylphosphine was realized, which was also supported by X-ray single crystal diffraction measurements. This pyrroline diphenylphosphine derivative was converted to hexadecylphosphonium salt, which is an analogue of antineoplastic agent, MITO-CP.

6.
Plants (Basel) ; 10(6)2021 Jun 09.
Artículo en Inglés | MEDLINE | ID: mdl-34207852

RESUMEN

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.

7.
Antioxidants (Basel) ; 10(5)2021 May 17.
Artículo en Inglés | MEDLINE | ID: mdl-34067702

RESUMEN

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.

8.
Antibiotics (Basel) ; 10(2)2021 Feb 23.
Artículo en Inglés | MEDLINE | ID: mdl-33672329

RESUMEN

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.

9.
Biomolecules ; 11(2)2021 02 04.
Artículo en Inglés | MEDLINE | ID: mdl-33557215

RESUMEN

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.


Asunto(s)
Antioxidantes/química , Euphorbiaceae/química , Euphorbiaceae/metabolismo , Simulación del Acoplamiento Molecular , Fitoquímicos/farmacología , Extractos Vegetales/química , Animales , Antioxidantes/farmacología , Benzotiazoles/química , Compuestos de Bifenilo/química , Carcinoma Hepatocelular/tratamiento farmacológico , Biología Computacional , Evaluación Preclínica de Medicamentos , Flavonoides/farmacología , Depuradores de Radicales Libres , Células Hep G2 , Humanos , Quempferoles , Neoplasias Hepáticas/tratamiento farmacológico , Melanoma Experimental , Metanol/química , Ratones , Monofenol Monooxigenasa , Fenoles/química , Picratos/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Plantas Medicinales , Ácidos Sulfónicos/química
10.
RSC Adv ; 11(10): 5295-5310, 2021 Jan 28.
Artículo en Inglés | MEDLINE | ID: mdl-35423082

RESUMEN

In the present study, the methanolic, hydro-methanolic, dichloromethane, hexane and aqueous extracts of Salvia ceratophylla L. (Family: Lamiaceae), a lemon-scented herb, were tested for total phenolic (TPC) and flavonoid content (TFC) and antioxidant activities were evaluated using a battery of assays (2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity, total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating). Enzyme inhibitory effects were investigated using acetyl- (AChE), butyryl-cholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase as target enzymes. Regarding the cytotoxic abilities, HepG2, B164A5 and S17 cell lines were used. The phytochemical profile was conducted using liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS). Our data showed that the methanolic aerial extracts possessed the highest phenolic (72.50 ± 0.63 mg gallic acid equivalent per g) and flavonoid (43.77 ± 1.09 mg rutin equivalent per g) contents. The hydro-methanolic aerial extract showed significant DPPH radical scavenging activity (193.40 ± 0.27 mg TE per g) and the highest reducing potential against CUPRAC (377.93 ± 2.38 mg TE per g). The best tyrosinase activity was observed with dichloromethane root extract (125.45 ± 1.41 mg kojic acid equivalent per g). Among the tested extracts, hexane root extract exerted the highest antimicrobial potential with a minimum inhibitory concentration value of 0.048 mg mL-1. Methanolic root extract showed the lowest cytotoxicity (28%) against HepG2 cells. Phytochemical analysis revealed the presence of important polyphenolic compounds including luteolin, gallic acid, rosmarinic acid, to name a few. This research can be used as one methodological starting point for further investigations on this lemon-scented herb.

11.
Food Res Int ; 133: 109129, 2020 07.
Artículo en Inglés | MEDLINE | ID: mdl-32466933

RESUMEN

The Crocus and Cyclamen genus have been reported to possess diverse biological properties. In the present investigation, two geophytes from these genus, namely Crocus pallasi and Cyclamen cilicium have been studied. The in vitro antioxidant, enzyme inhibitory, and cytotoxic effects of the methanol extracts of Crocus pallasii and Cyclamen cilicium aerial and underground parts were investigated. Antioxidant abilities of the extracts were investigated via different antioxidant assays (metal chelating, radical quenching (ABTS and DPPH), reducing power (CUPRAC and FRAP) and phosphomolybdenum). Cholinesterases, amylase, tyrosinase, and glucosidase were used as target enzymes for detecting enzyme inhibitory abilities of the samples. Regarding the cytotoxic abilities, breast cancer cell lines (MDA-MB 231 and MCF-7) and prostate cancer cell lines (DU-145) were used. The flowers extracts of Crocus pallasii and C. cilicium possessed the highest flavonoid content. The highest phenolic content was recorded from C. cilicium root extract (47.62 mg gallic acid equivalent/g extract). Cyclamen cilicium root extract showed significantly (p < 0.05) high radical scavenging (94.28 and 139.60 mg trolox equivalent [TE]/g extract, against DPPH and ABTS radicals, respectively) and reducing potential (173.30 and 109.53 mg TE/g extract, against CUPRAC and FRAP, respectively). The best acetylcholinesterase, glucosidase and tyrosinase inhibition was observed in C. cilicium root (4.46 mg GALAE/g; 15.75 mmol ACAE/g; 136.99 mg KAE/g, respectively). Methanolic extracts of C. pallasii and C. cilicium showed toxicity against breast cancer cell lines. In light of the above findings, C. cilicium might be considered as an interesting candidate in the development of anti-cancer agent coupled with antioxidant properties.


Asunto(s)
Antioxidantes/análisis , Crocus/química , Cyclamen/química , Inhibidores Enzimáticos/análisis , Extractos Vegetales/análisis , Flavonoides/análisis , Flores/química , Metanol/análisis , Fenoles/análisis
12.
Antioxidants (Basel) ; 9(2)2020 Feb 17.
Artículo en Inglés | MEDLINE | ID: mdl-32079363

RESUMEN

In this study, ethyl acetate, methanol, and water extracts of Bersama abyssinica (Melianthaceae) stem bark were screened for enzyme inhibitory and antioxidant properties. The water extract possessed the highest concentration of phenols (230.83 mg gallic acid equivalent/g extract), while the methanol extract was rich in flavonoids (75.82 mg rutin equivalent/g extract), and the ethyl acetate extract possessed the highest amount of saponins (97.37 mg quillaja equivalent/g). The aim of this study was to investigate the antiproliferative effects against the human colon cancer HCT116 cell line challenged with serotonin (5-HT) as a stimulating-proliferation factor. The level of HCT116 cell-deriving pool of kynurenic acid (KA) was also assessed. The UHPLC results confirmed the presence of 58, 68, and 63 compounds in the ethyl acetate, methanol, and water extracts, respectively. Mangiferin, vitexin and its isomer isovitexin were tentatively identified in all extracts and KA (m/z 190.05042 [M-H]+) was also tentatively identified in the methanol and water extracts. The methanol extract (1464.08 mg Trolox equivalent [TE]/g extract) showed the highest activity in the CUPRAC assay, whereas the water extract (1063.70 mg TE/g extract) showed the highest activity with the FRAP technique. The ethyl acetate extract was the most active acetylcholinesterase (4.43 mg galantamine equivalent/g extract) and α-glucosidase (mmol acarbose equivalent /g extract) inhibitor. The water extract was able to inhibit 5-HT-stimulated viability of HCT116 cells, and blunt 5-HT-induced reduction of cell-deriving KA. The scientific data generated in this study provide baseline data regarding the biological properties of B. abyssinica stem bark, highlighting its potential use for the development of new pharmaceutic and cosmetic agents.

13.
Antioxidants (Basel) ; 9(2)2020 Feb 02.
Artículo en Inglés | MEDLINE | ID: mdl-32024319

RESUMEN

Bridelia species have been used in traditional African medicine for the management of diverse human ailments. In the current work, the detailed phytochemical profiles of the extracts of the stem bark of B. speciosa were evaluated and the antioxidant and enzyme inhibitory properties of the extracts were assessed. The anti-bacterial and anti-mycotic effects of the extracts were evaluated against selected pathogen strains. Additionally, the anti-proliferative effects were studied on the liver cancer HepG2 cell line. Finally, the putative protective effects were assessed on isolated rat liver that was challenged with lipopolysaccharide (LPS). The results revealed the presence of 36 compounds in the ethyl acetate extract, 44 in the methanol extract, and 38 in the water extract. Overall, the methanol extract showed the highest antioxidant activity, particularly in LPS-stimulated rat liver. Additionally, this extract exerted the highest antimycotic effect on C. albicans, whereas the water extract showed a promising anti-proliferative effect on liver cancer HepG2 cells. The methanol extract was also the most active as enzyme inhibitor, against acetylcholinesterase and butyrylcholinesterase. The current study appraises the antioxidant and enzyme inhibition properties of B. speciosa methanol extract and showed that this specie could be a promising source of biologically active phytochemicals, with potential health uses.

14.
Antioxidants (Basel) ; 8(9)2019 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-31480498

RESUMEN

Anogeissus leiocarpus (DC.) Guill. & Perr. (Combretaceae) has a long history of use by folk populations for the management of multiple human ailments. Based on the published literature, there has been no attempt to conduct a comparative assessment of the biological activity and the phytochemical profiles of the leaves and stem bark of A. leiocarpus extracted using methanol, ethyl acetate, and water. By high-performance liquid chromatography with electrospray ionization mass spectrometric detection (HPLC-ESI-MSn) analysis, quinic, shikimic, gallic, and protocatechuic acids were tentatively identified from all the extracts, while chlorogenic, caffeic, ferulic, and dodecanedioic acids were only characterised from the leaves extracts. Additionally, a pharmacological study was carried out to evaluate potential protective effects that are induced by the extracts in rat colon and colon cancer HCT116 cell line. In general, the methanol and water extracts of A. leiocarpus leaves and stem bark showed potent radical scavenging and reducing properties. It was noted that the stem bark extracts were more potent antioxidants as compared to the leaves extracts. The methanol extract of A. leiocarpus leaves showed the highest acetyl (4.68 mg galantamine equivalent/g) and butyryl (4.0 mg galantamine equivalent/g) cholinesterase inhibition. Among ethyl acetate extracts, the pharmacological investigation suggested stem bark ethyl acetate extracts to be the most promising. This extract revealed ability to protect rat colon from lipopolysaccharide-induced oxidative stress, without exerting promoting effects on HCT116 cell line viability and migration. As a conclusion, A. leiocarpus represents a potential source of bioactive compounds in the development of novel therapeutic agents.

15.
Food Res Int ; 123: 414-424, 2019 09.
Artículo en Inglés | MEDLINE | ID: mdl-31284993

RESUMEN

Bunium species have been reported to be used both as food and in traditional medicines. The scientific community has attempted to probe into the pharmacological and chemical profiles of this genus. Nonetheless, many species have not been investigated fully to date. In this study, we determined the phenolic components, antimicrobial, antioxidant, and enzyme inhibitory activities of aerial parts of four Bunium species (B. sayai, B. pinnatifolium, B. brachyactis and B. macrocarpum). Results showed that B. microcarpum and B. pinnatifolium were strong antioxidants as evidenced in the DPPH, ABTS, CUPRAC, and FRAP assays. B. brachyactis was the most effective metal chelator, and displayed high enzyme inhibition against cholinesterase, tyrosinase, amylase, glucosidase, and lipase. The four species showed varied antimicrobial activity against each microorganism. Overall, they showed high activity against P. mirabilis and E. coli (MIC and MBC <1 mg mL-1). B. brachyactis was more effective against Aspergillus versicolor compared to the standard drug ketoconazole. B. brachyactis was also more effective than both ketoconazole and bifonazole against Trichoderma viride. B. sayai was more effective than ketoconazole in inhibiting A. fumigatus. B. sayai was most non-toxic to HEK 293 (cellular viability = 117%) and HepG2 (cellular viability = 104%). The highest level of TPC was observed in B. pinnatifolium (35.94 mg GAE g-1) while B. microcarpum possessed the highest TFC (39.21 mg RE g-1). Seventy four compounds were detected in B. microcarpum, 70 in B. brachyactis, 66 in B. sayai, and 51 in B. pinnatifolium. Quinic acid, chlorogenic acid, pantothenic acid, esculin, isoquercitrin, rutin, apigenin, and scopoletin were present in all the four species. This study showed that the four Bunium species are good sources of biologically active compounds with pharmaceutical and nutraceutical potential.


Asunto(s)
Apiaceae/química , Apiaceae/clasificación , Amilasas/antagonistas & inhibidores , Amilasas/metabolismo , Animales , Antiinfecciosos/análisis , Antiinfecciosos/farmacología , Antioxidantes/análisis , Antioxidantes/farmacología , Apigenina/análisis , Apigenina/metabolismo , Ácido Clorogénico/análisis , Ácido Clorogénico/farmacología , Inhibidores de la Colinesterasa/análisis , Inhibidores de la Colinesterasa/farmacología , Enterobacter cloacae/efectos de los fármacos , Enterobacter cloacae/metabolismo , Inhibidores Enzimáticos/análisis , Inhibidores Enzimáticos/farmacología , Escherichia coli/efectos de los fármacos , Escherichia coli/metabolismo , Esculina/análisis , Esculina/farmacología , Glucosidasas/antagonistas & inhibidores , Glucosidasas/metabolismo , Células HEK293 , Células Hep G2 , Humanos , Lipasa/antagonistas & inhibidores , Lipasa/metabolismo , Ratones , Pruebas de Sensibilidad Microbiana , Monofenol Monooxigenasa/antagonistas & inhibidores , Monofenol Monooxigenasa/metabolismo , Ácido Pantoténico/análisis , Ácido Pantoténico/farmacología , Fenoles/análisis , Fenoles/farmacología , Extractos Vegetales/análisis , Extractos Vegetales/farmacología , Proteus mirabilis/efectos de los fármacos , Proteus mirabilis/metabolismo , Pseudomonas aeruginosa/efectos de los fármacos , Pseudomonas aeruginosa/metabolismo , Quercetina/análogos & derivados , Quercetina/análisis , Quercetina/farmacología , Ácido Quínico/análisis , Ácido Quínico/farmacología , Células RAW 264.7 , Rutina/análisis , Rutina/farmacología
16.
J Pharm Biomed Anal ; 174: 286-299, 2019 Sep 10.
Artículo en Inglés | MEDLINE | ID: mdl-31185340

RESUMEN

This study aimed to reveal chemical profiles and biological activities of ethyl acetate (EA), methanol (MeOH), and water extracts of Lotus corniculatus. Ethnobotanical reports have indicated the importance of phytochemical properties of the genus Lotus. In this study, the effects of medicinal plant extracts on antioxidant (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays), enzyme inhibitory (on cholinesterase, tyrosinase, a-amylase and a-glucosidase), DNA protection and anticancer properties (including anti-proliferative, cell death and telomerase activity marker gene analysis, apoptotic DNA fragmentation analysis, cell migration test) were evaluated. According to chemical analysis, quercetin derivatives geraldol, isorhamnetin and kaempferol-O-coumaroylhexoside-O-deoxyhexoside isomers were dominant in the extracts. MeOH extracts showed the highest total flavonoids capacity with 21.13 mg RE/g. EA extract showed the strongest anti-amylase activity among the tested extracts. Water extract had the most protective activity against plasmid DNA. To indicate cell survival, MTT test was performed against human MCF-7 and MDA-MB-231 breast cancer cells. Half-maximal inhibitory concentration for cells were calculated and used for detection of mechanisms behind the cancer cell death. EA extract showed up-regulation of Bax proapoptotic gene and apoptotic DNA fragmentation activity on highly invasive MDA-MB-231 cells. Beclin-1 and LC3-II autophagy genes were higly expressed after treatment of MCF-7 cells with EA extracts. EA and MeOH extracts inhibited cell migration ability of both cancer cells. Linoleamide, was dominant component in EA extract and caused apoptosis on MDA-MB-231 breast cancer cells via increasing intranuclear Ca²+. The detailed mechanism behind the anticancer properties should be further investigated.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Apoptosis , Autofagia , Neoplasias de la Mama/tratamiento farmacológico , Lotus/química , Extractos Vegetales/farmacología , Acetatos/química , Amilasas/antagonistas & inhibidores , Animales , Antioxidantes/farmacología , Línea Celular Tumoral , Fragmentación del ADN , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Flavonoides/análisis , Flavonoides/farmacología , Humanos , Células MCF-7 , Melanoma Experimental , Metanol/química , Ratones , Estrés Oxidativo , Agua/química
17.
J Pharm Biomed Anal ; 171: 118-125, 2019 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-30986761

RESUMEN

This study was geared towards assessing the possible antioxidant, enzyme inhibitory, and cytotoxic activities of ethyl acetate, methanol, and water extracts of Sideritis ozturkii Aytaç & Aksoy. The phytochemical profiles of the studied extracts were characterised by HPLC-MS/MS. The methanol extract, rich in phenolics (78.04 mg gallic acid equivalent/g), exhibited the strongest antioxidant activities. However, the ethyl acetate extract was the most active extract in the enzyme inhibitory assays. The water extract of S. ozturkii (1 mg/ml, 48 h incubation) slightly inhibited (22%) growth of human breast cancer cell line (MDA-MB-231 cells). On the other hand, the ethyl acetate and methanol extracts showed strong inhibition (98% and 97%, respectively) of MDA-MB-231 cells and caused apoptotic cell death. Scientific data generated from this study further appraises the multiple biological activities of plants belonging to the Sideritis genus. In addition, preliminary evidence gathered from the current investigation advocates for further studies geared towards the preparation of therapeutic formulations from S. ozturkii.


Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Inhibidores Enzimáticos/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación , Sideritis/química , Acetatos/química , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Inhibidores Enzimáticos/farmacología , Humanos , Metanol/química , Extractos Vegetales/farmacología , Sideritis/crecimiento & desarrollo , Solventes/química , Turquía , Agua/química
18.
Talanta ; 194: 446-451, 2019 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-30609556

RESUMEN

A new analytical method for sensitive determination of cysteine based on its interaction with phenazine methosulfate was developed using salting-out liquid-liquid microextraction followed by spectrophotometric detection. The mechanism of the reaction was studied and confirmed by Fourier transform infrared and mass spectroscopy. Experimental parameters affecting the extraction efficiency were investigated and under the optimal conditions, good linearity was observed in the range 0.2 - 6.0 µg mL-1 with a correlation coefficient of 0.9972. The limit of detection and limit of quantification were found to be 0.07 and 0.21 µg mL -1, respectively. The enrichment factor was 25. The developed methodology was applied for analysis of cysteine in food supplements. The obtained data were in good agreement with LC-MS/MS analysis.


Asunto(s)
Cisteína/análisis , Cisteína/aislamiento & purificación , Microextracción en Fase Líquida/métodos , Sales (Química)/química , Espectrofotometría , Cisteína/química , Análisis de los Alimentos , Metosulfato de Metilfenazonio/química
19.
J Pharm Biomed Anal ; 164: 581-589, 2019 Feb 05.
Artículo en Inglés | MEDLINE | ID: mdl-30466026

RESUMEN

In the quest for new drugs of herbal origin, the ethyl acetate (EAE), methanol (ME), and water (WE) extracts of Crocus chrysanthus (Herb.) Herb. flowers were analyzed for their polyphenolic composition, antioxidant, and enzyme inhibitory potential. WE showed the highest antioxidant activities in all assays including metal chelating, phosphomolybdenum, FRAP, CUPRAC, ABTS and DPPH. EAE was the most effective enzyme inhibitor, exhibiting the highest inhibition against some enzymes linked to Alzheimer's disease (cholinesterases), diabetes mellitus (α-glucosidase and α-amylase) and hyperpigmentation problems (tyrosinase). The highest total phenolics (34.99 mg GAE/g) and flavonoids content (77.58 mg RE/g) were observed in WE and ME, respectively. Eight compounds were identified in EAE, 24 in ME, and 15 in WE. Kaempferol 3-O glucoside was found in all extracts. In conclusion, C. chrysanthus flowers can be suggested as a source of bioactive components with potential use against chronic disorders caused by oxidative stress. Future in-depth studies are recommended to determine the biological effects of isolated compounds from C. chrysanthus to identify the main compounds modulating the observed activities.


Asunto(s)
Antioxidantes/farmacología , Crocus/química , Inhibidores Enzimáticos/farmacología , Extractos Vegetales/farmacología , Polifenoles/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Cromatografía Líquida de Alta Presión/métodos , Pruebas de Enzimas/métodos , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Flores/química , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/química , Polifenoles/química , Polifenoles/aislamiento & purificación , Solventes/química , Espectrometría de Masas en Tándem/métodos
20.
Int J Environ Health Res ; 29(6): 607-621, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30569760

RESUMEN

This study investigated into the phytochemical profile and biological properties of extracts (methanol and aqueous) of Origanum onites based on the antioxidant, enzyme inhibitory, and antibacterial activities. The aqueous extract exhibited higher antioxidant activities in the 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), ferric reducing antioxidant power, cupric reducing antioxidant capacity, phosphomolybdenum, and metal chelating assays, compared to the methanol extract. In contrast, the methanol extract was the most effective inhibitor of acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase, and α-glucosidase. The methanol extract also showed higher antibacterial activity with highest inhibition against Escherichia coli (MIC = 6.25 mg/mL). The total phenolic content was higher in the aqueous extract while the methanol extract possessed higher total flavonoid content. A total of 28 and 18 compounds (belonging to polyphenols, flavonoids, terpenoids, and ester classes) were identified from the methanol and water extracts, respectively. These findings suggest that O. onites could be helpful in the management of oxidative stress-associated diseases including diabetes and neurodegenerative complications. Abbreviations: ABTS: 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid; ACAE: acarbose equivalent; AChE: acetylcholinesterase; AD: Alzheimer's disease; BChE: butyrylcholinesterase; CUPRAC: cupric reducing antioxidant capacity; DPPH: 1,1-diphenyl-2-picrylhydrazyl; EDTAE: EDTA equivalent; FRAP: ferric reducing antioxidant power; GAE: gallic acid equivalent; GALAE: galatamine equivalent; HPLC: high performance liquid chromatography; KAE: kojic acid equivalent; RE: rutin equivalents; TE: trolox equivalent; TPC: total phenolic content; TFC: total flavonoid content.


Asunto(s)
Origanum/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Plantas Medicinales/química , Antibacterianos/análisis , Antibacterianos/farmacología , Antioxidantes/análisis , Antioxidantes/farmacología , Cromatografía Líquida de Alta Presión , Inhibidores Enzimáticos/análisis , Inhibidores Enzimáticos/farmacología , Flavonoides/análisis , Fenoles/análisis , Espectrometría de Masas en Tándem
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