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- MakaleAçık Erişim2026Scopus SJRQ1Ajuga vestita Boiss: a “natural gold mine” for the design of novel nutraceuticals and phytopharmaceuticals
Cetiz, Mehmet Veysi; Zengin, Gokhan; Leyva-Jiménez, Francisco Javier; Fernández-Ochoa, Álvaro; de la Luz Cádiz-Gurrea, Maria; Custódio, Luísa; Rodrigues, Maria João; Pereira, Catarina G.; Lazarova, Irina; Balos, Mehmet Maruf
Members of the Ajuga genus are of significant interest due to their traditional applications in various countries, and have therefore been the subject of phytochemical research investigating their natural bioactive compounds. The aim of this study was to determine the chemical composition and biological activities of various Ajuga vestita extracts (ethyl acetate, ethanol, ethanol/water and water). The biological effects assessed included antioxidant, enzyme inhibition and cytotoxic activities. The extracts were chemically profiled using ultra-high-performance liquid chromatography – electrospray ionization – quadrupole time-of-flight mass spectrometry (UHPLC-ESI-QTOF-MS), which identified 121 compounds, including iridoids, flavonoids, and phenolic acids. The ethanol/water extract exhibited superior radical scavenging activity (2,2-Diphenyl-1-picrylhydrazyl (DPPH): 43.13 mg Trolox equivalent (TE)/g; 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS): 45.37 mg TE/g) and reducing power (cupric reducing antioxidant capacity (CUPRAC): 103.43 mg TE/g; ferric reducing antioxidant power (FRAP): 45.29 mg TE/g). Regarding enzyme inhibition, the ethanol extract exhibited the greatest inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), glucosidase, and tyrosinase, whereas the ethyl acetate extract was most effective against amylase. Regarding cytotoxicity, the ethyl acetate extract exhibited the strongest effect, significantly reducing cell viability in all cell lines and having a particularly strong impact on murine bone marrow stromal (S17) cells, with viability at 30.8 ± 2.7% at a concentration of 100 µg/mL. By contrast, the aqueous extract exhibited low cytotoxicity, maintaining high cell viability (over 94% at 50 µg/mL and over 74% at 100 µg/mL). Additionally, network pharmacology, molecular docking and molecular dynamics simulations were employed to investigate the multi-target mechanisms and binding stability of A. vestita phytochemicals. These findings provide new, detailed insights into A. vestita and suggest its potential as a raw material for developing health-promoting nutraceutical and pharmaceutical products.
- MakaleAçık Erişim2024Scopus SJRQ2Cytotoxic, antioxidant, and enzyme inhibitory activities of Centaurea stapfiana extracts and their HPLC-ESI-QTOF-MS profiles: Insights into an unexplored Centaurea species
Zengin, Gokhan; Fernández-Ochoa, Álvaro; de la Luz Cádiz-Gurrea, María; Jiménez, Francisco-Javier Leyva; Uba, Abdullahi Ibrahim; Ak, Gunes; Soomro, Sanam Iram; Balos, Maruf; Cakilcioglu, Ugur; Rodrigues, Maria João
The members of the genus Centaurea have a great interest in pharmaceutical and nutraceutical fields due to their biological potential. Based on this information, we aimed to evaluate the biological properties (antioxidant, enzyme inhibition and cytotoxicity) and chemical profile of the extract of Centaurea stapfiana, an unstudied species. The highest total phenolic content was found in the ethanol/water extract with 32.17 mg GAE/g. A total of 102 of them were identified by HPLC-ESI-QTOF-MS analysis. These compounds were mainly hydroxybenzoic acid and hydroxycinnamic acid as well as flavonoids. In the antioxidant tests, the ethanol/water extract had the best free radical scavenging and reducing ability. However, in the enzyme inhibition test, the ethanol extract was the most active. The extracts were also tested on two tumour cell lines (RAW 264.7 and HepG2) and one non-tumour cell line (S17). The ethanol extract showed the promising effect on HepG2 (cell viability: 28.6 % at 50 g/ml). Furthermore, we examined the interactions between the compounds and enzymatic and cellular targets. A good interaction was found between quercetin-3-xylosyl-(1- > 6)-glucoside and iNOS. In summary, our results suggest that C. stapfiana can be considered as a versatile raw material for the development of health-promoting applications in the pharmaceutical and cosmeceutical fields.
AtıfScopus13OpenAlex14
İncele - MakaleAçık Erişim2021Scopus SJRQ1Chemical profiling and biological evaluation of nepeta baytopii extracts and essential oil: An endemic plant from turkey
Zengin, Gokhan; Mahomoodally, Mohamad Fawzi; Aktumsek, Abdurrahman; Jekő, József; Cziáky, Zoltán; Rodrigues, Maria João; Custodio, Luisa; Polat, Rıdvan; Cakilcioglu, Ugur; Ayna, Adnan
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.
AtıfScopus32OpenAlex32İncele - MakaleYalnız künye2020Scopus SJRQ1Chemical profile, antioxidant, antimicrobial, enzyme inhibitory, and cytotoxicity of seven Apiaceae species from Turkey: A comparative study
Zengin, Gokhan; Sinan, Kouadio Ibrahime; Ak, Gunes; Mahomoodally, Mohamad Fawzi; Paksoy, Mehmet Yavuz; Picot-Allain, Carene; Glamocilja, Jasmina; Sokovic, Marina; Jekő, József; Cziáky, Zoltán
Several Apiaceae species, used as both food and in complementary and alternative medicine, represents a rich source of potential valuable phytopharmaceuticals which necessitates scientific contemplation. In the present study, the antioxidant, enzyme inhibitory, antimicrobial, and cytotoxic properties of methanol extracts of seven Apiaceae species, (Chaerophyllum macrospermum (Willd. ex Spreng.) Fisch. & C.A.Mey. ex Hohen, Ferula rigidula Fisch. ex DC., Ferula orientalis L., Prangos ferulacea Lindl., Prangos peucedanifolia Fenzl., Ferulago setifolia K. Koch, and Pimpinella anthriscoides Boiss.) were evaluated. Species belonging to the Prangos genus exhibited the highest total phenolic content, namely P. peucedanifolia and P. ferulacea, with values of 47.90 and 44.44 mg gallic acid equivalent/g extract, respectively. P. peucedanifolia also displayed the highest radical scavenging capacity (81.53 and 102.70 mg Trolox equivalent [TE]/g extract for 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), respectively) and reducing power (165.87 and 100.09 mg TE/g extract for cupric reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP), respectively). C. macrospermum showed the most potent inhibition against Alzheimer's disease related enzymes, namely acetylcholinesterase (4.53 mg galantamine equivalent [GALAE]/g extract) and butyrylcholinesterase (3.22 mg GALAE/g extract). P. ferulacea (131.94 mg kojic acid (KAE) equivalent/g extract) and P. peucedanifolia (4.97 mmol acarbose equivalent (ACAE)/g extract) were potent inhibitors of tyrosinase and α-glucosidase, respectively. In general, studied species were able to reduce cellular viabilities. P. peucedanifolia possessed promising antibacterial potential against Bacillus cereus (Minimum inhibition concentration (MIC): 0.37 mg/mL), L. monocytogenes (MIC: 0.56 mg/mL), P. aeruginosa and Escherichia coli (MIC: 0.27 mg/mL), Salmonella typhimurium and Enterobacter cloacae (MIC: 0.75 mg/mL). F. rigidula showed the highest antifungal effect against Aspergillus ochraceus and Trichoderma viride (MIC: 0.10 mg/mL). The present findings could be the scientific starting point towards the pharmaceutical and/or commercial utilization of these Apiaceae species.
AtıfScopus65OpenAlex64İncele - MakaleAçık Erişim2019Scopus SJRQ1New insights into the chemical profiling, cytotoxicity and bioactivity of four Bunium species
Zengin, Gokhan; Paksoy, Mehmet Yavuz; Aumeeruddy, Muhammad Zakariyyah; Glamocilja, Jasmina; Sokovic, Marina; Diuzheva, Alina; Jekő, József; Cziáky, Zoltán; Rodrigues, Maria João; Custodio, Luisa
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.
AtıfScopus22OpenAlex23İncele - MakaleAçık Erişim2019Scopus SJRQ1Phytochemical characterization and bioactivities of five Apiaceae species: Natural sources for novel ingredients
Zengin, Gokhan; Mahomoodally, Mohamad Fawzi; Paksoy, Mehmet Yavuz; Picot-Allain, Carene; Glamocilja, Jasmina; Sokovic, Marina; Diuzheva, Alina; Jekő, József; Cziáky, Zoltán; Rodrigues, Maria João
Several species of the Apiaceae family have been employed in traditional cultures for their curative virtues. The present study focused on five Apiaceae species, (Falcaria vulgaris (FV), Smyrniopsis aucheri (SA), Smyrniopsis munzurdagensis (SM), Smyrnium cordifolium (SC), and Actinolema macrolema (AM)). The antioxidant, enzyme inhibitory (α-amylase, α-glucosidase, acetyl- and butyrylcholinesterase, lipase, and tyrosinase), antimicrobial, phytochemical, and cytotoxicity profiles of the methanol extracts of the selected Apiaceae species were determined. SC extract (35.68 mg gallic acid equivalent/g extract) possessed the highest phenolic content while the AM extract (56.79 mg rutin equivalent/g extract) had the highest flavonoid content. HPLC-ESI-MS (High performance liquid chromatography-electrospray tandem mass spectrometry) analyses showed presence of ferulic acid in all the five species. SC extract exhibited high radical scavenging (59.28 and 94.31 mg Trolox equivalent [TE]/g extract, DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS (2,2′-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid), respectively) and reducing activity (161.44 and 113.62 mg TE/g extract, for CUPRAC (cupric reducing antioxidant capacity) and FRAP (ferric reducing antioxidant power), respectively). SM extract exhibited the highest cholinesterase's inhibitory action (3.82 and 4.76 mg galantamine equivalent/g extract, for acetyl- and butyrylcholinesterase, respectively). The extracts showed higher inhibition against α-glucosidase (7.32-11.99 mmol acarbose equivalent [ACAE]/g extract) compared to α-amylase (0.51-0.55 mmol ACAE/g extract). SC extract was the most active (137.54 mg kojic acid equivalent/g extract) tyrosinase inhibitor and FV extract (113.75 mg Orlistat equivalent/g) the best lipase inhibitor. SM extract showed potent antibacterial effect against B. cereus (MIC (minimum inhibitory concentration) 0.180 mg/mL), P. mirabilis (MIC 0.180 mg/mL), M. flavus (MIC 0.560 mg/mL), P. aeruginosa (MIC 0.275 mg/mL), and S. typhimurium (MIC 1.500 mg/mL). FV extract (MIC 0.140 mg/mL) suppressed A. fumigatus growth. Cytotoxicity was assessed on murine macrophage (RAW 264.7), human embryonic kidney (HEK 293), and human hepatocellular carcinoma (HepG2) cell lines. FV (60.3%) and SM (57.4%) showed the highest reduction on RAW 264.7 cellular viability, whereas SM (74.1%) showed toxicity against HepG2. This study supports that the Apiaceae species could be considered as promising candidates for the development of novel pharmacophores for the management of several human ailments.
AtıfScopus51OpenAlex47İncele