The genus Rubus (Rosaceae) has great potential for and a history of use as natural agents in several traditional folk remedies. Based on this concept, this study focused on the antioxidant activities ...and enzyme inhibitory effects of extracts and fractions from Rubus caesius. Different chemical assays were performed to detect antioxidant capacity, namely, free radical scavenging (ABTS and DPPH assays), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating. Enzyme inhibitory effects were tested towards cholinesterases (AChE and BChE), tyrosinase, α-amylase and α-glucosidase. In addition, total amounts of phenolics and flavonoids were detected by colorimetric assays. Among the samples, the ethyl acetate fraction exhibited the strongest antioxidant potential with its higher concentration of total phenolics. The highest AChE and α-amylase inhibitory activities were observed in the diethyl ether fraction, while the n-butanol fraction had the strongest anti-tyrosinase inhibitor ability. The present study demonstrated that R. caesius may be considered a source of biologically active compounds to develop novel functional products or drugs in the pharmaceutical field.
•Chemical profiles and biological properties of three African plants were evaluated.•Stem bark extracts exhibited stronger antioxidant abilities than leaf extracts.•All extracts exhibited significant ...enzyme inhibitory activities.•Molecular docking against tyrosinase was in agreement with the in vitro results.•These plants are good sources of bioactive compounds for pharmaceutical area.
Africa is famous for its floral biodiversity, exploited by local people for therapeutic purposes. However, such plants need to be scrutinised scientifically for the presence of bioactive compounds and possible biological properties. This study attempts for the first time to highlight the pharmacological and phytochemical profile of extracts prepared from leaves and stem barks of three African plants (Macaranga hurifolia Beille, Sterculia tragacantha Lindl. and Zanthoxylum gilletii (De Wild.) P. G. Waterman. The extracts were tested for antioxidant and enzyme inhibitory effects. Free radical scavenging, metal chelator, reducing power and phosphomolybdenum assays were performed to evaluate antioxidant effects. To identify enzyme inhibitory effects, cholinesterases (acetylcholinesterase (AChE) and butrylcholinesterase (BChE)), tyrosinase, α-amylase and α-glucosidase were selected as target enzymes. High performance liquid chromatography-Electrospray tandem mass spectrometry (HPLC-ESI-MS) technique was also used for chemical profiling. ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) and DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging assays showed that the stem barks of all three African plants were better scavenger than leaf extracts. Sterculia tragacantha was found to be a better metal chelator (64.10 ± 4.66 mg EDTAE/g) among the studied plants. All extracts exhibited good clinical enzyme inhibitory activities. The stem bark of S. tragacantha exhibited the best acetylcholinesterase activity compared to the other plants. HPLC-ESI-MS characterization showed that the most abundant compounds in stem bark were flavonoids in M. hurifolia (4.2 ± 0.2 mg/g DE), proanthocyanidins in S. tragacantha (42 ± 1 mg/g DE) and similar concentrations of phenolic acids and flavonoids in Z. gilletii (2.8–3.1 mg/g DE). Based on the biological activity, the most abundant and relevant bioactive compounds in the extracts were studied using molecular modelling approach against tyrosinase. The studied African plants showed good antioxidant and enzymatic propensities and thus can be considered as potential bioresources for future development of nutraceuticals and/or for pharmaceutical applications.
•Biological and chemical fingerprints of three Salvia species were studied.•Antioxidant, enzyme inhibition and cytotoxic assays for biological fingerprint were carried out.•Chemical composition was ...examined by high-performance liquid chromatography with mass spectrometry detection.•Rosmarinic acid was the major component in the studied extracts.•These plants may be considered as potential sources of natural agents.
The genus Salvia has recently attracted great attention due to its notable biological activities. Within this context, in this study, the chemical characterization and biological effects of three extracts (dichloromethane (DCM), methanol (MeOH), and water) from three Salvia species (S. blepharochlaena (SB), S. euphratica var. leiocalycina (SE), and S. verticillata subsp. amasica (SV)) were assessed. For the chemical characterization, the qualitative and quantitative analysis of phenolic components in the methanol extracts was carried out by high-performance liquid chromatography with electrospray ionization mass spectrometry detection (HPLC-UV-ESI-MSn). Total phenolic, flavonoid and phenolic acid contents were also studied. Concerning the biological effects, antioxidant (DPPH and ABTS free radical scavenging; ferric (FRAP) and cupric (CUPRAC) reducing power; phosphomolybdenum, and metal chelating assays), enzyme inhibitory (cholinesterase, tyrosinase, amylase, glucosidase, lipase, and elastase) and cytotoxic effects (A-549 and MCF-7 cell lines) were evaluated. After the evaluation of the phytochemical profile by HPLC-UV-ESI-MSn, it was observed that the main compound in the analyzed extracts was rosmarinic acid, which was present at high concentrations, particularly in SV, which presented rosmarinic acid levels higher than the usual levels found in other Salvia species or related plants. Generally, the SV-water extract presented the strongest antioxidant abilities with higher levels of total bioactive compounds. However, the studied DCM extracts had higher enzyme inhibitory potentials compared with MeOH and water extracts. SE-DCM exerted the most potent cytotoxic effects, followed by SB-water and SB-MeOH extracts.
•Antioxidant and enzyme inhibitory properties of Tanacetum poteriifolium extracts.•Chemical profile was identified for the tested extracts.•Multicomponent analysis were done to provide a ...comprehensive classification.•The plant could be starting material for designing novel products.
The members of the genus Tanacetum have a long history in traditional medicine to manage several diseases. Thus, the present study attempts to determine the chemical composition and to probe into the biological activities of Tanacetum poteriifolium Grierson, a poorly studied medicinal plant. The enzyme inhibitory and antioxidant properties of the ethyl acetate, methanol, and water extracts were assessed using standard in vitro assays. Biological data were further investigated by multivariate analysis tools. The water extract showed the highest concentration of phenolics (83.38 mg gallic acid equivalent (GAE)/g extract), and was a potent radical scavenger (238.12 and 282.54 mg Trolox equivalent (TE)/g extract, towards 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), respectively) and had potent reducing power (555.03 and 285.79 mg TE/g extract, towards cupric reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP), respectively). The ethyl acetate extract (41.07 mg ethylenediaminetetraacetic acid equivalent (EDTAE)/g extract), rich in flavonoids (43.55 mg rutin equivalent (RE)/g extract), was a potent metal chelator. Besides, the ethyl acetate extract exhibited strong inhibitory action on cholinesterases (3.47 and 3.46 mg galantamine equivalent (GALAE)/g extract) and α-glucosidase (23.67 mmol acarbose equivalent (ACAE)/g extract). Tyrosinase was actively inhibited in the presence of the methanol extract of T. poteriifolium (128.54 mg kojic acid equivalent (KAE)/g extract). Liquid chromatography-electrospray ionisation quadrupole time-of-flight mass spectrometry analysis revealed the presence of quinic acid and methylquercetin derivatives in T. poteriifolium ethyl acetate extract. Two unknown compounds having m/z values 289.17, 267.23, 235.13, 211.14, 185.12, 121.06 and 275.21, 211.15, 171.11, 121.11 were identified from the T. poteriifolium methanol extract. Principal component analysis was performed to obtain an overview of the influence of solvents on T. poteriifolium biological activities which were satisfactorily discriminated. This study provides valuable baseline data on the biological activity of T. poteriifolium towards important enzymes targeted in the management of global health problems, such as Alzheimer’s disease, diabetes, and epidermal hyperpigmentation problems.
Rhoifolin (apigenin-7-O-β-neohesperidoside) belongs to the class of flavonoids and was reported to exhibit anti-inflammatory, cytotoxic, antidiabetic, hepatoprotective, and cardioprotective ...activities. The current study presents the in-vitro evaluation of the antioxidative effects of rhoifolin by many assays, namely DPPH, CUPRAC, ABTS, phosphomolybdenum, and FRAP. Enzyme inhibitory potential was also evaluated for acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, amylase, and glucosidase enzymes. While results revealed weak antioxidant activities for rhoifolin, the compound demonstrated some promising enzyme inhibitory effects against BChE (4.03 mg GALAE/g) and tyrosinase (7.44 mg KAE/g) but was not active on AChE. Regarding anti-diabetic enzymes, the compound was active on amylase but did not show any inhibition effect on glucosidase. In-silico molecular docking study was performed for rhoifolin on the active site of NADPH oxidase, BChE, and amylase enzymes to verify the observed enzyme inhibitory effect. Good binding affinities were observed for rhoifolin on all the docked enzymes, revealing numerous hydrogen bonds, carbon-hydrogen, van der Waals interactions. This is the first study to evaluate the enzyme inhibition potential of rhoifolin. We concluded that the increase in the degree of glycosylation might decrease the antioxidant abilities of flavonoids and that rhoifolin had moderate enzyme inhibition abilities to be investigated in future studies.
•Biological and chemical propensities of S. modesta and T. argaeus were investigated.•Several antioxidant assays were performed.•Inhibitory effects on key enzymes were tested.•Rosmarinic acid was ...found to be the main component in these extracts.•Both species are important natural agents for pharmaceutical and food industries.
The genus Salvia and Thymus have gained much popularity as an alternative therapy in Turkish folk medicine for abdominal pain, cold, nausea, among others. Nonetheless, some species are yet to be further explored for their bioactivities. We investigated the biological activities of 3 extracts (dichloromethane, methanol, and water (decoction)) of Salvia modesta Boiss. and Thymus argaeus (Fisch. & C.A.Mey.) Boiss. & Balansa. based on antioxidant and enzyme inhibition along with the determination of polyphenolic content. Antioxidant potential was assessed using six assays namely: 2,2-diphenyl-1-picrylhydrazyl, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid), cupric ion reducing antioxidant capacity, ferric reducing antioxidant power, phosphomolybdenum, and metal chelating. Moreover, enzyme inhibition activities of the extracts were studied against acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase, and α-glucosidase. Results revealed that the decoction of both plants was the strongest antioxidants. The methanol extracts displayed the highest tyrosinase inhibition while the dichloromethane extracts of both plants were the most effective butyrylcholinesterase and α-glucosidase inhibitors. In addition, the total phenolic and total flavonoid content was highest in the decoction and methanolic extract of Thymus argaeus, respectively. The most abundant phenolic compound was rosmarinic acid (6574 μg/g and 5390 μg/g in T. argaeus and S. modesta methanolic extracts, respectively). PASS prediction analysis revealed that chlorogenic acid showed the highest Pa value for antioxidant activity (0.809) including the mechanism of free radical scavenging (0.856), while rosmarinic acid showed the highest Pa value (0.798) for antidiabetic activity. To conclude, both Salvia modesta and Thymus argaeus can be regarded as new sources of antioxidants and enzyme inhibitors to manage oxidative stress and their complications.
Medicinal plants offer natural cures and inspire modern medicine's development. This study examined the antioxidant, enzyme-inhibitory, and antiproliferative activities of various extracts obtained ...from aerial and root fragments of Phlomoides molucelloides (Bunge) Salmaki. The extracts' overall phenolics, flavonoids, and compounds were defined using colorimetric and LC-MS/MS analyses. The highest total phenolic and flavonoid content was measured in the methanol and infusion extracts of the aerial fragments, with 102.21 mg RE/g and 51.33 mg GAE/g, respectively. Most compounds were defined as flavonoids, predominantly as apigenin and quercetin glycosides. Methanol, 70 % methanol, and infusion extracts from aerial parts had the highest antioxidant activity determined by DPPH, ABTS, CUPRAC, FRAP, metal chelation, and phosphomolybdenum analyses. Moreover, the methanol extract of the roots had the highest anti-acetylcholinesterase, anti-butyrylcholinesterase, and anti-glucosidase activities. The dichloromethane extracts of the roots displayed the highest anti-tyrosinase and anti-amylase activities. The antiproliferative activity of the extracts was investigated against MDA-MB-231, MCF-7, and HeLa cell lines. The lowest IC50 value (875.7 µg/mL) was computed for the methanol extract of the aerial part on the MCF-7 cell line at the 48th h. The findings showed that P. molucelloides extracts may offer a promising therapeutic approach due to their rich bioactive content.
Display omitted
•Antioxidant and enzyme-inhibitory properties of the extracts were carried out.•The extracts' phenolic and flavonoid content and compounds were defined.•The anticancer activity of the extracts was studied by MTT assay.•P. molucelloides extracts may offer a promising therapeutic approach.
The main goals of this research were the chemical and biological characterization of the bitter melon (Momordica charantia) isolate obtained by traditional (maceration) extraction, as well as ...optimization of this process using response surface methodology (RSM) and artificial neural networks (ANNs). Experiments were performed using Box-Behnken experimental design on three levels and three variables: extraction temperature (20 °C, 40 °C, and 60 °C), solvent concentration (30%, 50%, and 70%) and extraction time (30, 60, and 90 min). The measurements consisted of 15 randomized runs with 3 replicates in a central point. The antioxidant activity of obtained extracts was determined by the 1,1-diphenyl-2-picrylhydrazyl (DPPH), cupric ion reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP) assays while chemical characterization was done in terms of the total phenolic content (TPC). The methodology shows positive influence of solvent concentration on all four observed outputs, while temperature showed a negative impact. RSM showed that the optimal extraction conditions were 20 °C, 70% methanol, and an extraction time of 52.2 min. Under these conditions, the TPCs were 20.66 milligrams of gallic acid equivalents (mg GAE/g extract), DPPH 30.22 milligrams of trolox equivalents (mg TE/g extract), CUPRAC 67.78 milligrams of trolox equivalents (mg TE/g extract), and FRAP 45.48 milligrams of trolox equivalents (mg TE/g extract). The neural network coupled with genetic algorithms (ANN-GA) was also used to optimize the conditions for each of the outputs separately. It is anticipated that results reported herein will establish baseline data and also demonstrate that that the present model can be applied in the food and pharmaceutical industries.
•Usage of new eco-friendly technique for polyphenols extraction.•Extraction yield of polyphenols was influenced by pressure.•SWE provided high apigenin yield (61.5–1345 mg/kg).•Extracts obtained at ...30, 45 and 60 bar exhibited strong bioactivities.
The study was designed to determine the relationship between chemical structure, bioactivity and pressure during the subcritical water extraction (SCW) of chamomile. Extraction was carried out at isothermal conditions (100 °C) at five different pressures (10, 30, 45, 60 and 90 bar). Twenty three polyphenolic compounds were identified in the extracts, whereby apigenin was found to be the dominant compound (61.53–1344.99 mg/kg). Results suggest that the lowest applied pressure has negligible effect on phenolic recovery from chamomile, but also the use of pressures above than 45 bar was proven as needlessly. By using in vitro assays, influence of pressure on antioxidant, cytotoxic and enzyme-inhibitory activities of the extracts was evaluated. Extracts obtained at 30, 45 and 60 bar exhibited stronger bioactivities than at 10 and 90 bar. It was concluded that pressure exert a significant influence on chemical composition of extracts, and thus on biological activity of chamomile extracts.
•The extracts of Smyrnium olusatrum were investigated.•Antioxidant, enzyme inhibition and anticancer potentials were reported.•WNT1, APC, LEF1, and TCF7 genes were suppressed by ethanol and ...ethanol/water extracts.•All extracts exhibited downregulation action on NOTCH1, SHH, and SMO genes.•The plant can be considered as a potential candidate for designing functional preparations.
This research delves into the medicinal significance of Smyrnium olusatrum by investigating ethyl acetate, ethanol, ethanol/water, and infusion extracts. The chemical composition analysed through LC-MS-qTOF metabolomic analysis, determine total phenolic and flavonoid contents, evaluate antioxidant potential using six in vitro tests (DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum assay (PBD), and metal chelating assay (MCA)), assess enzyme inhibition activity against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase, and α-glucosidase, and explore their anticancer effects on HEp-2 cells. Additionally, qPCR analysis is conducted on HEp-2 larynx cancer cells to examine the impact of S. olusatrum on self-renewal and apoptosis pathways, along with the expression levels of key genes associated with these pathways. The findings indicated that the infusion extraction method demonstrated the highest levels, with a recorded TPC of 35.02 mg GAE/g and a TFC of 15.08 mg RE/g. All four extracts of S. olusatrum exhibited a total of 328 entities. The most significant metabolites, primarily comprising polyphenolics, flavonoids, non-structural carbohydrates, and amino acids in negative ionization mode, as well as sesquiterpene lactone and amino acids in positive ionization, were identified. Infusion exhibited the highest antioxidant effect among the extracts, with peak values ranged from 55.55 mg TE/g (DPPH) to 100.07 mg TE/g (ABTS). The extracts exhibited variable enzyme activities. Notably, ethyl acetate also demonstrated superior α-Amylase inhibition (0.69 mmol ACAE/g), while the ethanol extract exhibited higher α-Glucosidase inhibition (1.70 mmol ACAE/g). The HEp-2 cells demonstrated the quickest attainment of half maximal inhibitory concentration values with ethanol and ethanol/water extracts, yielding IC50 values of 250 µg/mL (24 h) and 125 µg/mL (24 h), respectively, among the applied extracts. The qPCR results revealed that S. olusatrum inhibited all self-renewal pathways and activated the apoptotic pathway. The ethanol and ethanol/water extracts of S. olusatrum significantly suppressed WNT1, APC, LEF1, and TCF7 genes. Furthermore, the downregulation of NOTCH1, SHH, and SMO gene expressions in all extracts suggests the activation of the Type 1 non-canonical hedgehog pathway in laryngeal cancer. The findings not only underscore the therapeutic potential of these extracts but also open the way for further exploration of their applications in combating oxidative stress, enzyme-related disorders, and potential anti-cancer effects through modulation of crucial cellular pathways.
