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    Biopotential of Bersama abyssinica fresen stem bark extracts: UHPLC profiles, antioxidant, enzyme inhibitory, and antiproliferative propensities
    (MDPI AG, 2020) Sinan, K. I.; Chiavaroli, A.; Orlando, G.; Bene, K.; Zengin, Gökhan; Cziáky, Z.; Jek?, J.
    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 ?-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. © 2020 by the authors. Licensee MDPI, Basel, Switzerland.
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    Bridelia speciosa müll.Arg. stem bark extracts as a potential biomedicine: From tropical western africa to the pharmacy shelf
    (MDPI AG, 2020) Mahomoodally, Mohamad Fawzi; Sinan, K. I.; Bene, K.; Zengin, Gökhan; Orlando, G.; Menghini, L.; Veschi, S.
    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. © 2020 by the authors. Licensee MDPI, Basel, Switzerland.
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    Chemical characterization, antioxidant, enzyme inhibitory and cytotoxic properties of two geophytes: Crocus pallasii and Cyclamen cilicium
    (Elsevier Ltd, 2020) Zengin, Gökhan; Mahomoodally, Mohamad Fawzi; Sinan, K. I.; Picot-Allain, M. C. N.; Yıldıztugay, Evren; Cziáky, Z.; Jek?, J.
    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. © 2020 Elsevier Ltd
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    A comparative exploration of the phytochemical profiles and bio-pharmaceutical potential of Helichrysum stoechas subsp. barrelieri extracts obtained via five extraction techniques
    (Elsevier Ltd, 2020) Zengin, Gökhan; Cvetanovi?, A.; Gaši?, U.; Teši?; Stupar, A.; Bulut, G.; Sinan, K. I.
    We endeavoured to probe into and compare the possible effect(s) of different extraction techniques (accelerated solvent extraction (ASE), microwave-assisted extraction (MAE), ultrasonication-assisted extraction (UAE), maceration, and Soxhlet extraction (SE)) on the bioactivity (antioxidant and enzyme inhibitory activities) of the aerial parts of Helichrysum stoechas subsp. barrelieri (Ten.) Nyman. Total phenolic and flavonoid contents of the extracts obtained by different extraction methods followed the order of ASE > MAE > UAE > maceration > SE. Extract obtained by ASE was the most potent radical scavenger (219.92 and 313.12 mg Trolox equivalent [TE]/g, against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2?-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), respectively) and reducing agent (927.39 and 662.87 mg TE/g, for cupric reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP), respectively). Helichrysum stoechas extract obtained by UAE (18.67 mg ethylenediaminetetraacetic equivalent [EDTAE]/g) was the most active metal chelator and inhibitor of acetylcholinesterase (4.23 mg galantamine equivalent [GALAE]/g) and butyrylcholinesterase (6.05 mg GALAE/g) cholinesterase. Extract from maceration (183.32 mg kojic acid equivalent [KAE]/g) was most active against tyrosinase while ASE extract (1.66 mmol acarbose equivalent [ACAE]/g) effectively inhibited ?-glucosidase. In conclusion, data amassed herein tend to advocate for the use of non-conventional extraction techniques, namely ASE and UAE, for the extraction of bioactive secondary metabolites from H. stoechas aerial parts. © 2019 Elsevier Ltd