Browsing by Author "Yerlikaya S."

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A multidirectional perspective for novel functional products: In vitro pharmacological activities and in silico studies on Ononis natrix subsp. hispanica
(2017-09-01) Yerlikaya S.; Zengin G.; Mollica A.; Baloglu M.C.; Altunoglu Y.C.; Aktumsek A.
The genus Ononis has important value as traditional drugs and foods. In the present work, we aimed to assess the chemical profiles and biological effects of Ononis natrix subsp. hispanica extracts (ethyl acetate, methanol, and water). For chemical profile, total and individual phenolic components were detected. For biological effects, antioxidant (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays), enzyme inhibitory (against cholinesterase, tyrosinase, α-amylase and α-glucosidase), antimicrobial, DNA protection and cytotoxic abilities were tested. The predominant phenolics were apigenin, luteolin, and quercetin in the tested extracts. Generally, the ethyl acetate and methanol extracts were noted as the most active in the antioxidant and enzyme inhibitory assays. Water extract with different concentrations indicated high level of DNA protection activity. Methanol and ethyl acetate extracts showed antibacterial effect against to Staphylococcus aureus and Staphylococcus epidermidis strains. The cytotoxic effects of O. natrix subsp. hispanica extracts on the survival of HeLa and PC3 cells were determined by MTT cell viability assay. Water and methanol extracts caused initiation of apoptosis for PC3 cell line. Furthermore, molecular docking was performed to better understand interactions between dominant phenolic compounds and selected enzymes. Our results clearly indicate that O. natrix subsp. hispanica could be considered a potential candidate for designing novel pharmaceuticals, cosmeceuticals and nutraceuticals.
Anticancer, antimicrobial, and DNA protection analysis of novel 2,4-dihydroxyquinoline dyes
(2018-10-01) Şener N.; Mohammed H.J.A.; Yerlikaya S.; Celik Altunoglu Y.; Gür M.; Baloglu M.C.; Şener İ.
A new series of 2,4-dihydroxyquinoline derived disazo dyes has been synthesized by the reaction of 5-amino-4-phenylazo-3-methyl-1H-pyrazole derivatives with 2,4-dihydroxyquinoline. The structures of the obtained dyes were identified by various spectrophotometric methods such as FT-IR, 1H-NMR, and elemental analysis. The synthesized compounds were also examined for different biological activities, including DNA protection, antimicrobial, and anticancer activities. Compound 3b was found most effective on Gram-positive bacteria. A DNA protection assay was applied to all compounds, and it was found that compounds 3h and 3j had a high capacity for binding to DNA. Besides, compounds 3h and 3j showed cytotoxicity against HeLa and PC3 cancer cell lines. These compounds could potentially be used as drugs or drug additives based on their effects on bacterial and cancer cell lines.
Antiproliferative properties and structural analysis of newly synthesized Schiff bases bearing pyrazole derivatives and molecular docking studies
(2021-10-05) Şener N.; Özkinali S.; Altunoglu Y.C.; Yerlikaya S.; Gökçe H.; Zurnaci M.; Gür M.; Baloglu M.C.; Şener İ.
New pyrazole Schiff bases containing azo groups were synthesized using the condensation reaction between p-nitrobenzaldehyde and (E)-4-(phenyl)-1-H-pyrazole-3,5-diamine in the molar ratio of 1:2. Characterization of the compounds was performed by spectroscopic techniques, including IR, UV-Vis, 1H-NMR and 13C-NMR. Biological activity of the compounds was evaluated by analyzing DNA protection, antimicrobial and anticancer properties. Compound 4 was effective for Salmonella typhimurium with the MIC concentration of 62.5 µg/mL. Moreover, this compound had the highest protection activity on DNA. Cytotoxic activity of compound 4 was determined on the HeLa cancer cell line with the IC50 concentration of 976.6 µM. The anti-cancer characteristic of compounds 4 and 5 for HeLa cancer was theoretically analyzed by molecular docking study as well. Among the tested compounds, compound 4 possessed significant results due to its in vitro cytotoxic properties. Therefore, it may be considered as a potential bioactive agent for cancer treatment studies. In addition, further in vivo analysis can be performed to indicate its anticancer property.
Antiproliferative-antimicrobial properties and structural analysis of newly synthesized Schiff bases derived from some 1,3,4-thiadiazole compounds
(2020-11-05) Gür M.; Yerlikaya S.; Şener N.; Özkınalı S.; Baloglu M.C.; Gökçe H.; Altunoglu Y.C.; Demir S.; Şener İ.
The 1,3,4-thiadiazole core has been mainly used as a pharmacological scaffold in medicinal chemistry. A series of Schiff bases derived from 5-substituted-1,3,4-thiadiazole-2-amine were designed and synthesized to investigate their biological activities. Structures of compounds were clarified with FTIR, 1H NMR and elemental analysis. Due to the importance of this core in pharmacology, all these newly synthesized compounds were tested for different biological properties at the same time. Compound 3A ((E)-N-(2,5-dimethoxybenzylidene)-5-(4-methoxyquinolin-2-yl)-1,3,4-thiadiazol-2-amine) and compound 4A ((E)-N-(2,5-dimethoxybenzylidene)-5-(3-methylbenzofuran-2-yl)-1,3,4-thiadiazol-2-amine) possessed high DNA protective ability against oxidative Fenton mixture. Compound 1A ((E)-N-(2,5-dimethoxybenzylidene)-5-(benzo[b]thiophen-2-yl)-1,3,4-thiadiazol-2-amine) and compound 2B ((E)-2-((5-(1H-indol-2-yl)-1,3,4-thiadiazol-2-ylimino)methyl)-6-methoxyphenol) showed strong antimicrobial activity against S. epidermidis. The most effective compound was detected as compound 3A which exhibited cytotoxicity on both PC-3 and MDA-MB-231 cancer cell lines. The IC50 of this compound was calculated as 370.7 μM and 505.1 μM for MDA-MB-231 and PC-3 cells, respectively. Molecular docking studies were also performed to examine the understanding of the mechanism behind the anti-cancer and anti-bacterial properties. For further study, compound 3A has the potential for utilization with chemotherapy drugs to establish a more efficient therapy strategy with minimum cytotoxicity against cancer cells.
Exploring of Coronilla varia L. extracts as a source of high-value natural agents: Chemical profiles and biological connections
(2021-12-01) Yerlikaya S.; Baloglu M.C.; Altunoglu Y.C.; Diuzheva A.; Jekő J.; Cziáky Z.; Zengin G.
Pharmacological studies have indicated that flavonoids are crucial compounds to eliminate drug resistance. In this report, the activity of ethyl acetate (EAE), methanol (ME) and water (WE) extracts of Coronilla varia L. on antioxidant and enzyme inhibitory activities, DNA protective effects, antiproliferative activities, apoptotic; autophagic and telomerase gene activity analysis in breast cancer cells and inhibitory effects on cell migration ability of malignant breast cancer cells were examined. In addition, HPLC-MS-MS was used for detection of chemical profiles of all extracts. Results showed that the highest concentration of the bioactive components was detected in EAE (50.86 mg GAE/g for phenolics and 25.66 mg RE/g for flavonoid). Also, EAE displayed significant antioxidant properties in radical scavenging and reducing power assays. Regarding enzyme inhibitory effects, EAE and ME were more active than WE. Some significant compounds such as, vitamin B5, riboflavin, citric acid, and isoflavonoid derivate – medicarpin, noscapine were detected only in WE. Apigenin was determined in all extracts. WE indicated the most shield effect on pDNA against oxidative damage. Half-maximal inhibitory concentrations of extracts on breast cancer cells were calculated with MTT cell viability test. Bax gene was up-regulated and anti-apoptotic gene known as Bcl-2 was down-regulated on MDA-MB-231 cells after treated with WE. TERT-1 gene was down-regulated after treated with EAE and ME for MDA-MB-231 and MCF-7 cells, respectively. Cell migration ability of both MDA-MB-231 and MCF-7 cells was prevented with EAE and ME. A more effective treatment strategy can be applied by combining these extracts with commercial chemotherapy drugs which cause apoptosis and cell migration inhibition in vitro.
Exploring the nutraceutical potential of dried pepper capsicum annuum L. on market from altino in abruzzo region
(2020-05-01) Valle A.D.; Dimmito M.P.; Zengin G.; Pieretti S.; Mollica A.; Locatelli M.; Cichelli A.; Novellino E.; Ak G.; Yerlikaya S.; Baloglu M.C.; Altunoglu Y.C.; Stefanucci A.
Sweet pepper is a typical type of Capsicum annuum from Abruzzo region, recognized as a traditional and local product, traditionally cultivated in the town of Altino (Abruzzo region, Italy). The aim of this study is to compare the sweet type of peppers from Altino with the hot pepper cultivated in the same area, in order to delineate their different phytochemical and biological profiles in vitro and in vivo. In this study, we elucidated their phytochemical composition, fatty acids composition and phenolic/flavonoid contents in extracts. Then antioxidant and enzyme inhibition assays were performed to evaluate their biological properties, together with in vitro cell assay and in vivo anti-inflammatory activity. Microwave (1000 mg/mL) extract of hot pepper showed the best inhibition value on in vitro cell growth assay; in fact, the number of survived cells was about 20% and 40% for microwave and Soxhlet extracts, respectively. In vivo anti-inflammatory assay revealed good activity for both species, which, when associated with in vitro cell inhibition results, could explain the protective effect on human prostatic hyperplasia.
Investigation of chemical profile, biological properties of Lotus corniculatus L. extracts and their apoptotic-autophagic effects on breast cancer cells
(2019-09-10) Yerlikaya S.; Baloglu M.; Diuzheva A.; Jekő J.; Cziáky Z.; Zengin G.
This study aimed to reveal chemical profiles and biological activities of ethyl acetate (EA), methanol (MeOH), and water extracts of Lotus corniculatus. Ethnobotanical reports have indicated the importance of phytochemical properties of the genus Lotus. In this study, the effects of medicinal plant extracts on antioxidant (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays), enzyme inhibitory (on cholinesterase, tyrosinase, a-amylase and a-glucosidase), DNA protection and anticancer properties (including anti-proliferative, cell death and telomerase activity marker gene analysis, apoptotic DNA fragmentation analysis, cell migration test) were evaluated. According to chemical analysis, quercetin derivatives geraldol, isorhamnetin and kaempferol-O-coumaroylhexoside-O-deoxyhexoside isomers were dominant in the extracts. MeOH extracts showed the highest total flavonoids capacity with 21.13 mg RE/g. EA extract showed the strongest anti-amylase activity among the tested extracts. Water extract had the most protective activity against plasmid DNA. To indicate cell survival, MTT test was performed against human MCF-7 and MDA-MB-231 breast cancer cells. Half-maximal inhibitory concentration for cells were calculated and used for detection of mechanisms behind the cancer cell death. EA extract showed up-regulation of Bax proapoptotic gene and apoptotic DNA fragmentation activity on highly invasive MDA-MB-231 cells. Beclin-1 and LC3-II autophagy genes were higly expressed after treatment of MCF-7 cells with EA extracts. EA and MeOH extracts inhibited cell migration ability of both cancer cells. Linoleamide, was dominant component in EA extract and caused apoptosis on MDA-MB-231 breast cancer cells via increasing intranuclear Ca²+. The detailed mechanism behind the anticancer properties should be further investigated.
Investigations into the therapeutic potential of Asphodeline liburnica roots: In vitro and in silico biochemical and toxicological perspectives
(2018-10-01) Locatelli M.; Yerlikaya S.; Baloglu M.; Zengin G.; Altunoglu Y.; Cacciagrano F.; Campestre C.; Mahomoodally M.; Mollica A.
This study aims to establish the biological and chemical profile of Asphodeline liburnica (Scop.) Rchb. root. The antioxidant, antimicrobial, enzyme inhibitory, DNA protection, apoptotic DNA ladder fragmentation analysis, and anti-proliferative of A. liburnica were established using standard assays. In silico study was also performed to understand interactions between quantified anthraquinones and key enzymes of clinical relevance. Total phenolic and flavonoid contents were found to be 9.67 mgGAE/g and 1.48 mgRE/g extract, respectively. Chrysophanol was detected as a major anthraquinone. The extract exhibited radical scavenging ability against DPPH and ABTS with values of 13.23 and 66.99 mgTE/g extract, respectively. Good inhibitory activity against tyrosinase was recorded. In silico experiments showed that the anthraquinones were able to establish coordinative bonds with the copper atoms present in the enzymatic cavity of tyrosinase. MTT cell viability test on MDA-MB-231 cells showed that at 0.1 and 1 μg of extracts induced anti-proliferative effect. Apoptotic DNA fragmentation analysis indicated nuclear condensation resulting in DNA fragmentation, which exhibited apoptotic cell death in the presence of A. liburnica. This study has provided insights on the potential usage of A. liburnica which could open new avenues for research and stimulate future interest for the development of safe novel biopharmaceuticals.
Pharmacological and polyphenolic profiles of Phyllanthus phillyreifolius var. commersonii Müll. Arg: An unexplored endemic species from Mauritius
(2019-01-01) Mahomoodally M.F.; Yerlikaya S.; Llorent-Martínez E.J.; Uğurlu A.; Baloglu M.C.; Altunoglu Y.C.; Mollica A.; Dardenne K.K.; Aumeeruddy M.Z.; Puchooa D.; Zengin G.
Phyllanthus phillyreifolius var. commersonii Müll. Arg is an endemic plant of Mauritius. To date, no study has been performed concerning its polyphenolic profile and pharmacological properties. In this study, a decoction (water), ethyl acetate and methanol extracts of the aerial parts of P. phillyreifolius, obtained from different extraction procedures (maceration and Soxhlet), were studied for antibacterial, antioxidant, anticancer, and enzyme inhibitory properties along with their polyphenolic profile. The ethyl acetate macerated extract showed high antibacterial activity against B. cereus (MIC = 0.293 mg/mL) and E. coli (MIC = 0.417 mg/mL) while S. epidermidis was most susceptible to the ethyl acetate-Soxhlet extract (MIC = 0.521 mg/mL). The methanol-Soxhlet extract displayed the most potent cupric and ferric reducing power, and metal chelating effect, while the macerated methanolic extract was the most effective DPPH and ABTS scavenger, and BChE inhibitor. Only the ethyl acetate-Soxhlet extract exhibited α-glucosidase inhibition. All extracts exhibited a strong anti-tyrosinase activity, which was further investigated by molecular docking and molecular dynamic. After 48 h exposure to the extracts for HeLa cell lines, the ethyl acetate-Soxhlet extract showed the highest inhibition (IC50 = 533.1 μg/mL) while the decoction extract was more cytotoxic to MDA-MB-231 cells (IC50 = 337.4 μg/mL). Treatment of cancer cell lines with all P. phillyreifolius extracts resulted in a time-dependent reduction of cell viability for HeLa and dose-and time-dependent reduction for MDA-MB-231. Gene expression ratio of Bcl-2 to Bax was higher for all Soxhlet-extracts. Total phenolics (TPC) and flavonoids (TFC) content were highest in the decoction and methanol-Soxhlet extract, respectively (122.43 mg GAE/g extract and 31.28 mg RE/g extract, respectively). The extracts were abundant in ellagitannins, although phenolic acids and flavonoids were also detected. Granatin B was detected for the first time in Phyllanthus species. Overall, the aerial parts of P. phillyreifolius exemplify a potent reservoir of bioactive phytochemicals for therapeutic applications.
Utilisation of Rhododendron luteum Sweet bioactive compounds as valuable source of enzymes inhibitors, antioxidant, and anticancer agents
(2020-01-01) Mahomoodally M.F.; Sieniawska E.; Sinan K.I.; Nancy Picot-Allain M.C.; Yerlikaya S.; Cengiz Baloglu M.; Altunoglu Y.C.; Senkardes I.; Rengasamy K.R.; Zengin G.
Ethnobotanical evidences report the use of Rhododendron luteum Sweet (Ericaceae) in traditional medicinal systems. However, R. luteum has been associated to the occurrence of ‘mad honey’ poisoning. In the present study, the ethyl acetate, methanol, and water extracts of R. luteum were investigated for their in vitro antioxidant, enzyme inhibition, and cytotoxic properties. The cytotoxicity of R. luteum extracts on A549 lung cancer cell line was evaluated using MTT cell viability assay. Besides, HPLC-ESI-MSn approach was employed to elucidate the secondary metabolite profiles of R. luteum in order to establish any structure-activity relationship. Methanol and water extracts of R. luteum possessed highest radical scavenging and reducing properties while the ethyl acetate extract showed highest metal chelating properties. In terms of enzyme inhibition, the methanol and ethyl acetate extracts of R. luteum, possessing epigallocatechin, were active inhibitors of cholinesterase enzymes, α-glucosidase, and tyrosinase. Water extract caused growth inhibition of A549 cells with 207.2 μg/ml IC50 value. Though R. luteum has received little scientific attention due to the occurrence of grayanotoxins in the plant, however, data presented in this work shows promising biological activity of R. luteum and highlighted its role as a potential source of antioxidant and key enzyme inhibitors.