PubMed İndeksli Yayınlar Koleksiyonu
https://hdl.handle.net/11421/23089
PubMed Indexed Publications Collection2024-03-28T11:04:32ZSynthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones
https://hdl.handle.net/11421/24192
Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones
Bilginer, Sinan; Gul, Halise Inci; Erdal, Feyza Sena; Sakagami, Hiroshi; Levent, Serkan; Gulcin, Ilhami; Supuran, Claudiu T.
In this study, new chalcone compounds having the chemical structure of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones (1?8) were synthesised and were characterised by H-1-NMR, C-13?-NMR, and HRMS spectra. Cytotoxic and carbonic anhydrase (CA) inhibitory effects of the compounds were investigated. Cytotoxicity results pointed out that compound 4, 6-[3-(4-trifluoromethylphenyl)-2-propenoyl]-3H-benzoxazol-2-one, showed the highest cytotoxicity (CC50) and potency-selectivity expression (PSE) value, and thus can be considered as a lead compound of this study. According to the CA inhibitory results, IC50 values of the compounds 1?8 towards hCA I were in the range of 29.74?69.57??M, while they were in the range of 18.14 ? 48.46??M towards hCA II isoenzyme. K-i values of the compounds 1?8 towards hCA I were in the range of 28.37???6.63?70.58???6.67??M towards hCA I isoenzyme and they were in the range of 10.85???2.14 ? 37.96???2.36??M towards hCA II isoenzyme.
GULCIN, Ilhami/0000-0001-5993-1668; Sakagami, Hiroshi/0000-0001-8001-2121; Bilginer, Sinan/0000-0001-5676-2045; Supuran, Claudiu/0000-0003-4262-0323; WOS: 000488460400001; PubMed: 31576761
2019-01-01T00:00:00ZPlant- and Nutraceutical-based Approach for the Management of Diabetes and its Neurological Complications: A Narrative Review
https://hdl.handle.net/11421/24182
Plant- and Nutraceutical-based Approach for the Management of Diabetes and its Neurological Complications: A Narrative Review
Ozturk, Yusuf; Ozturk, Nilgun
Diabetes is an important metabolic disease affecting many organs and systems in the body. the nervous system is one of the body systems affected by diabetes and neuropathic complications are troublesome in diabetic patients with many consequences. As diabetes has deleterious influences almost on bodily systems, an integrative approach seems to be necessary accepting the body as a whole and integrating body systems with lifestyle and living environment. Like some traditional health systems such as Ayurveda, integrative approach includes additional modalities to overcome both diabetes and diabetic complications. in general, these modalities consist of nutraceuticals and plant products. Prebiotics and probiotics are two types of nutraceuticals having active ingredients, such as antioxidants, nutrient factors, microorganisms, etc. Many plants are indicated for the cure of diabetes. All of these may be employed in the prevention and in the non-pharmacological management of mildto-moderate diabetes. Severe diabetes should require appropriate drug selection. Being complementary, prebiotics, probiotics, plants and exercise may be additive for the drug therapy of diabetes. Similarly, there are complementary approaches to prevent and cure neurological and/or behavioral manifestations of diabetes, which may be included in therapy and prevention plans. A scheme is given for the prevention and therapy of comorbid depression, which is one of the most common behavioral complications of diabetes. Within this scheme, the main criterion for the selection of modalities is the severity of diseases, so that personalized management may be developed for diabetic patients using prebiotics and probiotics in their diets, plants and drugs avoiding possible interactions.
WOS: 000497948900004; PubMed: 31612820
2019-01-01T00:00:00ZCytotoxicity of naturally occurring phenolics and terpenoids from Kenyan flora towards human carcinoma cells
https://hdl.handle.net/11421/24137
Cytotoxicity of naturally occurring phenolics and terpenoids from Kenyan flora towards human carcinoma cells
Kuete, Victor; Omosa, Leonidah K.; Midiwo, Jacob O.; Karaosmanoglu, Oguzhan; Sivas, Hulya
Background: Cancer constitutes a major hurdle worldwide and its treatment mainly relies on chemotherapy. Objectives: the present study was designed to evaluate the cytotoxicity of eleven naturally occurring compounds including six phenolics amongst them were 4 chalcones and 2 flavanones as well as 5 terpenoids (3 clerodane and 2 trachylobane diterpenoids) against 6 human carcinoma cell lines and normal CRL2120 fibroblasts. Materials and methods: the neutral red uptake (NR) assay was used to evaluate the cytotoxicity of the compounds, whilst caspase-Glo assay was used to detect caspase activation. Cell cycle and mitochondrial membrane potential (MMP) were all analyzed via flow cytometry meanwhile levels of reactive oxygen species (ROS) was measured by spectrophotometry. Results: Chalcones: 2',4'-dihydroxy-6'-methoxychalcone (1); 4',6'-dihydroxy-2',5'-dimethoxychalcone (2); 2',4',6'-trihydroxy-5'-methoxychalcone (3); 2',6'-diacetate-4'-methoxychalcone (4), trachylobane diterpenoids: 2,6,19-trachylobanetriol; (ent-2 alpha,6 alpha)-form (10) and 2,18,19-trachylobanetriol; (ent-2 alpha)-form (11) as well as doxorubicin displayed IC50 values below 110 mu M in the six tested cancer cell lines. the IC50 values of the most active compounds were between 6.30 mu M and 46.23 mu M for compound 1 respectively towards breast adenocarcinoma MCF-7 cells and small lung cancer A549 cells and between 0.07 mu M and 1.01 mu M for doxorubicin respectively against SPC212 cells and A549 cells. Compounds 1 induced apoptosis in MCF-7 cells mediated by increasing ROS production and MMP loss. Conclusion: Chalcones 1-3 are potential cytotoxic phytochemicals that deserve more investigations to develop novel anticancer drugs against human carcinoma. (C) 2018 Transdisciplinary University, Bangalore and World Ayurveda Foundation. Publishing Services by Elsevier B.V.
WOS: 000489004200005; PubMed: 30389223
2019-01-01T00:00:00ZChemical composition and antioxidant, cytotoxic, and insecticidal potential of Valeriana alliariifolia in Turkey
https://hdl.handle.net/11421/24128
Chemical composition and antioxidant, cytotoxic, and insecticidal potential of Valeriana alliariifolia in Turkey
Sen-Utsukarci, Burcu; Taskin, Turgut; Goger, Fatih; Tabanca, Nurhayat; Estep, Alden S.; Kessler, Sonja M.; Mat, Afife
Valeriana is a common plant species used for various healing purposes in folk medicine since antiquity. This study investigates the phytochemical profile, antioxidant, cytotoxic, and insecticidal activity of Valeriana alliariifolia Adams, a species that has traditionally been used in Turkey. For the analyses we prepared four root extracts of V. alliariifolia Adams using hexane (HM1), chloroform (CM1), ethanol (EM1), and water (WM1) for maceration. Additionally, two extracts were also prepared from its roots by maceration separately with ethanol (EM2) and water (WM2). One sample was prepared as a water infusion (WI), according to the procedure used in Turkish traditional medicine. the 2,2-Diphenyl1-picrylhydrazyl (DPPH) scavenging and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) radical cation scavenging activity tests showed that ethanol extracts had the strongest antioxidant activity: EM1 (IC50 - DPPH: 17.694 mu g/mL; ABTS: 23.8 mu g/mL) and EM2 (IC50 - DPPH: 20 mu g/mL; ABTS: 21.5 mu g/mL). the hexane extract, HM1, was the most cytotoxic (IC50<10 mu g/mL against HepG2 and HUVEC) and EM2 strongly cytotoxic (IC50<10 mu g/mL against HepG2 and IC50: 11.96 mu g/mL against HUVEC). the extracts with demonstrated cytotoxic activities were further examined to check their insecticidal activity against adult female mosquito Aedes aegypti and first instar Ae. aegypti larvae. HM1 was the most effective (90 +/- 10 %), which was consistent with its cytotoxic activity. Because of the high antioxidant, cytotoxic, and insecticidal activities, we ran phytochemical analyses of the HM1, EM1, and EM2 extracts with GC-MS (for HM1) and LC-MS/MS (for EM1 and EM2). We also analysed the composition of the essential oil obtained from V. alliariifolia roots by micro-distillation in order to compare its content with HM1, which contains volatile compounds. Phytochemical analyses revealed that the major compound in HM1 was isovaleric acid (16 %) and in the essential oil 1,8-cineole (2.9 %). EM1 and EM2 contained 5-O-caffeoylquinic acid (chlorogenic acid), verbascoside (acteoside), and 3,5-dicaffeoylquinic acid as major components. in the light of our findings and available literature, we can conclude that V. alliariifolia has a good bioactive potential that could be used for different purposes, including the development of new agents for the treatment of various diseases. the difference in the content between the essential oil and HM1 was remarkable. It suggests that the variability observed in the activity of the samples was a result of composition and that, therefore, the aim of treatment should dictate which type of preparation is to be selected. An added value of our study is that it determined verbascoside and methylquercetin rutinoside for the first time in the Valeriana extracts.
Kiemer, Alexandra K./0000-0002-7224-9900; DAGISTAN, OZLEM AKBAL/0000-0002-6524-3535; WOS: 000489295500007; PubMed: 32597129
2019-01-01T00:00:00Z