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    Comparative Studies on Phenolic Composition, Antioxidant, Wound Healing and Cytotoxic Activities of Selected Achillea L. Species Growing in Turkey
    (Mdpi, 2015) Agar, Osman Tuncay; Dikmen, Miris; Ozturk, Nilgun; Yilmaz, Mustafa Abdullah; Temel, Hamdi; Turkmenoglu, Fatma Pinar
    Turkey is one of the most important centers of diversity for the genus Achillea L. in the world. Keeping in mind the immense medicinal importance of phenols, in this study, three species growing in Turkey, A. coarctata Poir. (AC), A. kotschyi Boiss. subsp. kotschyi (AK) and A. lycaonica Boiss. & Heldr. (AL) were evaluated for their phenolic compositions, total phenolic contents (TPC), antioxidant properties, wound healing potencies on NIH-3T3 fibroblasts and cytotoxic effects on MCF-7 human breast cancer cells. Comprehensive LC-MS/MS analysis revealed that AK was distinctively rich in chlorogenic acid, hyperoside, apigenin, hesperidin, rutin, kaempferol and luteolin (2890.6, 987.3, 797.0, 422.5, 188.1, 159.4 and 121.2 mu g analyte/g extract, respectively). The findings exhibited a strong correlation between TPC and both free radical scavenging activity and total antioxidant capacity (TAC). Among studied species, the highest TPC (148.00 mg GAE/g extract) and TAC (2.080 UAE), the strongest radical scavenging (EC50 = 32.63 g/mL), the most prominent wound healing and most abundant cytotoxic activities were observed with AK. The results suggested that AK is a valuable source of flavonoids and chlorogenic acid with important antioxidant, wound healing and cytotoxic activities. These findings warrant further studies to assess the potential of AK as a bioactive source that could be exploited in pharmaceutical, cosmetics and food industries.
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    Öğe
    Essential oil content, in-vitro and in-silico activities of Hypericum triquetrifolium Turra, H. empetrifolium subsp. empetrifolium Willd., and H. pruinatum Boiss. & Balansa species
    (Istanbul Univ, Fac Pharmacy, 2023) Akdeniz, Mehmet; Yener, Ismail; Kocakaya, Safak Ozhan; Yolcu, Murat; Yigitkan, Serkan; Aydin, Firat; Turkmenoglu, Fatma Pinar
    Background and Aims: The importance of Hypericum species that are used traditionally against many diseases is increasing day by day.Methods: In this study, the essential oil contents of Hypericum triquetrifolium, H. empetrifolium subsp. empetrifolium, and H. pruinatum species were determined with GC-MS/ FID. This is the first study on the antioxidant, anticholinesterase, anti-urease, antityrosinase, antielastase, and anticollagenase activities of these species. Also, in silico and in vitro enzyme in-hibitory activities of the major compounds in the essential oil samples of the species have been evaluated. In addition, the cytotoxic effects of the essential oils were determined by the MTT method.Results: According to GC-MS/ FID results, the major compounds were determined as caryophyllene oxide (16.76%) for H. triquetrifolium, alpha-pinene (21.67%) for H. empetrifolium subsp. empetrifolium, and germacrene D (22.47%) for H. pruinatum. Especially, H. pruinatum sample showed a high cytotoxic effect (IC50: 34.78 +/- 0.22 and 29.06 +/- 0.40 mu g/mL, respectively) on HT -29 and MCF-7 cell lines. It was determined that the same sample showed a promising inhibitory activity on acetyl (18.33 +/- 2.79, 36.48 +/- 2.40, and 56.97 +/- 0.94, respectively) and butyryl (71.63 +/- 2.78, 73.88 +/- 1.16, and 56.97 +/- 0.97, respectively) cholinesterase enzymes.Conclusion: Results of the in-vitro activity studies indicated that H. pruinatum essential oil could be used in the pharmaceuti-cal industry.
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    Öğe
    Flavonoids from Sideritis Species: Human Monoamine Oxidase (hMAO) Inhibitory Activities, Molecular Docking Studies and Crystal Structure of Xanthomicrol
    (Mdpi, 2015) Turkmenoglu, Fatma Pinar; Baysal, Ipek; Ciftci-Yabanoglu, Samiye; Yelekci, Kemal; Temel, Hamdi; Pasa, Salih; Ezer, Nurten
    The inhibitory effects of flavonoids on monoamine oxidases (MAOs) have attracted great interest since alterations in monoaminergic transmission are reported to be related to neurodegenerative diseases such as Parkinson's and Alzheimer's diseases and psychiatric disorders such as depression and anxiety, thus MAOs may be considered as targets for the treatment of these multi-factorial diseases. In the present study, four Sideritis flavonoids, xanthomicrol (1), isoscutellarein 7-O-[6'''-O-acetyl--d-allopyranosyl-(12)]--d-glucopyranoside (2), isoscutellarein 7-O-[6'''-O-acetyl--d-allopyranosyl-(12)]-6''-O-acetyl--d-glucopyranoside (3) and salvigenin (4) were docked computationally into the active site of the human monoamine oxidase isoforms (hMAO-A and hMAO-B) and were also investigated for their hMAO inhibitory potencies using recombinant hMAO isoenzymes. The flavonoids inhibited hMAO-A selectively and reversibly in a competitive mode. Salvigenin (4) was found to be the most potent hMAO-A inhibitor, while xanthomicrol (1) appeared as the most selective hMAO-A inhibitor. The computationally obtained results were in good agreement with the corresponding experimental values. In addition, the x-ray structure of xanthomicrol (1) has been shown. The current work warrants further preclinical studies to assess the potential of xanthomicrol (1) and salvigenin (4) as new selective and reversible hMAO-A inhibitors for the treatment of depression and anxiety.