Enzyme inhibitors · Konu · Munzur Üniversitesi

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MakaleAçık Erişim2025Scopus SJRQ3/r/munzur/2181
Establishing a link between the chemical composition and biological activities of Gladiolus italicus Mill. from the Turkish flora utilizing in vitro, in silico and network pharmacological methodologies
Zengin, Gokhan; Cetiz, Mehmet Veysi; Abul, Nurgul; Gulcin, Ilhami; Caprioli, Giovanni; Piatti, Diletta; Ricciutelli, Massimo; Koyuncu, Ismail; Yuksekdag, Ozgur; Bahşi, Muammer
Objectives: Five solvent extracts (n-hexane, ethyl acetate, ethanol, ethanol/water (70%), and water) of Gladiolus italicus Mill. from Turkey were evaluated for chemical and biological properties. Methods: Antioxidant activities, inhibitory properties against key enzymes involved in the etiology of chronic diseases were tested, as well as cytotoxic effects on different cell lines. Chemical characterization was also carried out to determine the most abundant compounds of each extract. Results: The highest total phenolic content (TPC) was observed in the water extract while highest TFC in ethanol/water extract. The most abundant compounds in the extracts were hyperoside (69041.06 mg kg−1), isoquercitrin (46239.49 mg kg−1), delphindin-3,5-diglucoside (42043.81 mg kg−1), myricetin (21486.61 mg kg−1), and kaempferol-3-glucoside (21199.76 mg kg−1). Molecular dynamic (MD) simulations confirmed the structural stability and dynamic conformational integrity of these complexes over a period of 100 ns. In network pharmacology, A total of 657 unique target genes were screened: 52 associated with programmed cell death-1 (PD-1), 85 with vascular endothelial growth factor receptor-2 (VEGFR2), and 130 with fibroblast growth factor receptor-2 (FGFR2), identifying crucial gene interactions for these proteins. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted, revealing significant interactions and pathways such as the advanced glycation end products (AGE) and their receptors (RAGE) signaling pathway in diabetic complications and T- helper 17 (Th17) cell differentiation, among others. This elucidation of complex networks involving key genes like AKT Serine/Threonine Kinase 1 (AKT1), MYC proto-oncogene (MYC), tumor protein 53 (TP53), Interleukin 6 (IL6), and tumor necrosis factor (TNF) provides a promising foundation for the development of targeted therapies in the treatment of non-communicable diseases. Conclusion: These results show that G. italicus could be a natural source of potent antioxidants and enzyme inhibitors which need to be further explored for the development of biopharmaceuticals.
AtıfScopus15OpenAlex13
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MakaleAçık Erişim2021Scopus SJRQ3/r/munzur/2962
Preliminary investigation on chemical composition and bioactivity of differently obtained extracts from Symphytum aintabicum Hub.- Mor. &Wickens
Zengin, Gokhan; Sinan, Kouadio Ibrahim; Ak, Gunes; Angeloni, Simone; Maggi, Filippo; Caprioli, Giovanni; Kaplan, Alevcan; Çakılcıoğlu, Uğur; Akan, Hasan; Jugreet, Sharmeen
Symphytum species, commonly known as comfrey, hold a long history of folk medicinal uses for healing wounds, bone fractures and other pain resulting from inflammation. However, many species belonging to this genus have not yet been scientifically investigated and hence investigation in this regard is warranted. In the present research, S. aintabicum extracts prepared by different extraction techniques (homogenizer assisted extraction, infusion and maceration) were assayed for their chemosystematic attributes (total phenolic, flavonoid) as well as bioactive compound contents, antioxidant and enzyme inhibition potentials. For instance, the extracts were found to possess phenolic and flavonoid levels ranging from 35.50 to 112.25 mg GAE/g and 2.54–25.12 mg RE/g, respectively. In general, the extracts displayed significant antioxidant activity. However, methanolic and infusion extracts were observed as the most potent radical scavengers and reducing agents, most likely related to their phenolic content. The extracts also showed metal chelating power and total antioxidant capacity in phosphomolybdenum assay. Moreover, while all extracts showed inhibition on amylase, only the methanolic extracts acted as inhibitors of cholinesterases and tyrosinase, most probably due to their relatively higher flavonoid content. The findings also indicated that the extraction method as well as the solvent type used to more or less affect the yield of the bioactive compounds and extracts’ bioactivity reported herein. Hence, as a first report highlighting the in vitro pharmacological properties of S. aintabicum, promising results were revealed from the quantitative chemosystematic analysis of bioactive components present and as sources of antioxidants and enzyme inhibitors against key human illnesses, thus providing scope for potential applications in phytomedicine development.
AtıfScopus15OpenAlex14
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MakaleYalnız künye2021Scopus SJRQ3/r/munzur/2898
Enzyme inhibition and antioxidant functionality of eleven Inula species based on chemical components and chemometric insights
Ceylan, Ramazan; Zengin, Gokhan; Mahomoodally, Mohamad Fawzi; Sinan, Kouadio Ibrahime; Ak, Gunes; Jugreet, Sharmeen; Cakır, Oguz; Ouelbani, Rayene; Paksoy, Mehmet Yavuz; Yılmaz, Mustafa Abdullah
The members of the genus Inula have been widely used in traditional medicinal. In the present study, 11 Inula species were investigated for their phytochemical composition, antioxidant and enzyme inhibitory effects. While quinic acid was the principal compound in I. anatolica, I. britannica, I. inuloides, I. oculus-christi, I. peacockiana, I. sechmenii, I. thapsoides and I. viscidula extracts (22.43–42.02 mg/g dry extract (DE)), I. aucheriana and I. discoidea extracts contained rutin as their most abundant compound (23.28 and 79.10 mg/g extract, respectively). Interestingly, all the Inula extracts were active inhibitors of the five key clinical enzymes (acetylcholinesterase (3.56–5.13 mg galantamine equivalent (GALAE)/g), butyrylcholinesterase (1.49–7.34 mg GALAE/g), tyrosinase (112.31–122.13 mg kojic acid equivalent (KAE)/g), α-glucosidase (0.77–2.08 mmol acarbose equivalent (ACAE)/g) and α-amylase (0.73–0.90 mmol ACAE/g)). Furthermore, the extracts were observed to exhibit substantial antioxidant capacity (1,1-diphenyl-2-picrylhydrazyl (DPPH): 58.99–188.22 mg trolox equivalent (TE)/g); 2,2-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) (ABTS): 90.51–220.97 mg TE/g; cupric reducing antioxidant capacity (CUPRAC): 169.88–460.53 mg TE/g; ferric reducing antioxidant power (FRAP): 81.57–237.99 mg TE/g; metal chelating activity: 8.31–25.39 mg ethylenediamine tetraacetate equivalent (EDTAE)/g; phosphomolybdenum: 1.55–2.49 mmol TE/g). In conclusion, the Inula species studied herein showed promising pharmacological potentials justified by the presence of a panoply of bioactive compounds.
AtıfScopus60OpenAlex60
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MakaleAçık Erişim2021Scopus SJRQ1/r/munzur/2535
Comprehensive biological and chemical evaluation of two seseli species (S. gummiferum and s. transcaucasicum)
Zengin, Gokhan; Stojković, Dejan; Mahomoodally, Mohamad Fawzi; Jugreet, Bibi Sharmeen; Paksoy, Mehmet Yavuz; Ivanov, Marija; Gašić, Uroš; Gallo, Monica; Montesano, Domenico
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.
AtıfScopus16OpenAlex15
İncele
MakaleAçık Erişim2019Scopus SJRQ1/r/munzur/3496
New 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.
AtıfScopus22OpenAlex23
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