Temel Eczacılık Bilimleri Bölümü Koleksiyonu

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https://hdl.handle.net/20.500.12418/440

Listeleniyor 1 - 20 / 95

Use of newly synthetized magnetic Fe3O4 nanoparticles modified with hexadecyl trimethyl ammonium bromide for the sensitive analysis of antidepressant drugs, duloxetine and vilazodone in wastewater and urine samples
(2023) Ulusoy,Halil İbrahim; Polat,Ümmügülsüm; Ulusoy,Songül
A new enrichment and determination method involving HPLC-DAD analysis following magnetic solidphase extraction (MSPE) was developed to detect trace amounts of two antidepressant drugs, namely, duloxetine (DUL) and vilazodone (VIL). In this study, a solid-phase sorbent was newly synthesized for use in the MSPE and its characterization was carried out by scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, Raman spectroscopy and X-ray diffraction (XRD) techniques. In this proposed method, DUL and VIL molecules were enriched using newly synthesized magnetic-based nanoparticles in the presence of pH 10.0 buffer and desorbed with acetonitrile to a smaller volume prior to chromatographic determinations. After experimental variables were optimized, the VIL and DUL molecules were analyzed at wavelengths of 228 nm for DUL and 238 nm for VIL with isocratic elution of methanol, trifluoroacetic acid (TFA) (0.1%), and acetonitrile (10 : 60 : 30). The detection limits obtained under optimized conditions were 1.48 ng mL−1 and 1.43 ng mL−1, respectively. The %RSD values were found to be lower than 3.50% with model solutions containing 100 ng mL−1 (N:5). Finally, the developed method was successfully applied to wastewater samples and simulated urine samples, and quantitative results were obtained in the recovery experiments.
Application of magnetic solid?phase extraction for sensitive determination of anticancer drugs in urine by means of diamino benzidine tetrachlorohydrate modified magnetic nanoparticles
(Şubat, 2023) Akyol,Emin; Ulusoy,Halil İbrahim; Yilmaz,Erkan; Polat,Ümmügülsüm; Soylak,Mustafa
Background The analysis of drug active molecules and residues in the treatment of cancer is important for the sustainability of human life and therapeutic effects. For this purpose, a new magnetic sorbent was developed to use in solid phase extraction prior to conventional high-performance liquid chromatography (HPLC) analysis of Paclitaxel (PAC) and Gemcitabine (GEM) molecules. Methods In this study, a separation and pre-concentration approach based on magnetic solid phase extraction (MSPE) was proposed for PAC and GEM by means of using a newly synthesized magnetic sorbent. After the MSPE procedure, an HPLC system with a diode array detector (DAD) was used to analyze trace amounts of PAC and GEM anticarcinogenic drugs in urine samples. Surface modification of magnetic Fe3O4 nanoparticles was carried out by diaminobenzidinetetrachloro hydrate (DABTC) for the first time and a useful sorbent was obtained for MSPE experiments. Results In the proposed method, PAC and GEM molecules were retained on the c in the presence of a pH 5.0 medium and desorbed to 300 μL of acetonitrile: methyl alcohol (1:1) eluent phase before HPLC–DAD analysis. Under the optimized conditions, the limit of detection (LOD) values for PAC and GEM were 1.38 and 1.44 ng mL− 1 while the enhancement factor for PAC and GEM were 139.5 and 145.3, respectively. The relative standard deviations (RSD %) for PAC and GEM were below 3.50% in inter-day repeated experiments by means of model solutions containing 100 ng mL− 1 drug active ingredients. Conclusions Synthesis and characterization of DABTC-Fe3O4 nanoparticles were performed using suitable methodologies. Optimization of MSPE was done step by step. And finally, the developed method was successfully applied to urine samples with quantitative recoveries in the range of 99.0% and 105.0%.
Use of Fe3O4@ MPTMS-Dithizone Magnetic Nanoparticles as Solid Phase Sorbent for Sensitive Analysis of Sibutramine Molecules in Herbal Slimming Products.
(2023) Demir,Özge; Ulusoy,Halil İbrahim; Polat,Ümmügülsüm; Ulusoy,Songül
Background: A new enrichment and sensitive determination method, which includes HPLCDAD analysis after Magnetic Solid Phase Extraction (MSPE), has been developed for trace analysis of Sibutramine molecules in herbal slimming products. Sibutramine is one of the most adulterated drug molecules in herbal products. Method: In the proposed method, Sibutramine molecules were pre-concentrated by using Fe3O4@MPTMS-Dithizone magnetic sorbent synthesized in our laboratory. Desorption of Sibutramine molecules from the sorbent phase was carried out by using acetonitrile: methanol (1:1) solvent in the presence of pH 8.0 buffer before chromatographic determinations. Results: Analytical parameters of the method, such as linear range, enrichment factor, and determination limit, were determined after optimizing experimental variables such as interaction time, desorption solvent, pH, etc. The sibutramine molecule was analyzed by isocratic elution of acetonitrile and KH2PO4 (pH 3.0, 0.05 M) (40:60) with a DAD detector at 223 nm wavelength. Limit of detection (LOD) value was calculated as 1.43 ng mL-1. Conclusion: Relative standard deviations (RSD) were below 3.20% for determinations of model solutions, including 100 ng mL-1 of Sibutramine. Finally, the developed method has been applied to herbal slimming tea samples with quantitative recovery experiments.
Vitamin D increases the efcacy of cisplatin on bladder cancer cell lines
(2023) Özgen,Özge; Eroğlu,Güneş Özen; Küçükhüseyin,Özlem; Akdeniz,Nilgün; Hepokur,Ceylan; Kuruca,Serap; Yaylım,İlhan
Background 1,25(OH)2D3(Calcitriol), which is a broad regulatory molecule, plays a role in changing the efcacy of chemo therapeutic drugs. Cisplatin is one of a current standard chemotherapy regimen for bladder cancer. Increasing the efectiveness of the treatment and reducing the side efects to chemotherapeutics are of great importance in bladder cancer. We aimed to investigate the efect of the combination of cisplatin and calcitriol in order to create a possible advantage in treatment of bladder cancer. Methods T24, ECV-304 and HUVEC cell lines were treated with calcitriol and cisplatin individually and in combination. Dose determination and combination treatments of calcitriol and cisplatin were evaluated using the MTT assay for cytotox icity analysis on the cells. Annexin V-PI staining method was used for apoptosis determination by fow cytometry. Also the P-gp expression levels were determined by fow cytometry. Results The combination treatment increased the anti-proliferative efcacy compared to the efcacy in cisplatin alone in T24 cells and reduced the cytotoxicity in the HUVEC healthy cells compared to cisplatin alone. Combination treatment achieved signifcantly higher apoptosis rate in T24 cells compared with the rates in treatment of cisplatin alone. However apoptosis decreased in HUVEC cell line. P-gp ratios were increased in HUVEC and decreased in T24 cells with combina tion treatment compared to the numbers in the control cells. The rate of apoptosis and P-gp levels showed no signifcant change in ECV-304 cells. Conclusion Our study revealed that the combination of calcitriol and cisplatin allows the use of cisplatin at lower doses in T24 bladder cancer cell line
Anti-adhesive effect of naturally obtained dicalcium phosphate dihydrate nanoparticles in the rat uterine wound model
(2023) Kurt,Begum; Oksuz,Kerim E.; Sahin-Inan,Zeynep D.; Hepokur,Ceylan
Objective: In this study, we aimed to compare the anti-adhesive effects of contractubex and dicalcium phosphate dihydrate (DCPD) particles in rats treated with the uterine horn adhesion model. Materials and methods: Newly adult, 60 Wistar albino rats were used as experimental animals. The modified rat uterine horn adhesion model was used to induce intra-abdominal adhesion. Tumor necrosis factor (TNF)-α, interleukin (IL)-1, vascular endothelial growth factor (VEGF) and transforming growth factor (TGF)-β1 were studied for biochemical and immunohistochemical examination. Results: TNF-α decreased in each group, while it decreased more in G2 and G3 than in G1. IL-1β decreased in each group, while it decreased the most in G3. TGF-β1 and VEGF localization was less in the G2 compared to G1, the least TGF-β1 and VEGF immunolocalization was detected in the G3 and G4. For both antibodies, the least localization among all groups belonged to G3. From day 7 to day 21, the high est TGF-β1 immunolocalization was observed in G1, lesser localization in G2 and lowest in G3. Conclusion: DCPD nanopar ticles show promise as a clinical antiadhesive agent and should be further evaluated in experimental animal models and human trials
Propolis nanoparticles synthesis and characterization with cytotoxic and apoptotic effects on breast cancer cells
(2023) Ay,Ebru Nur; Caner,Armağan; Hepokur,Ceylan; Danişman Kalindemirtaş,Ferdane; Eroğlu, Güneş Özen; Kariper,Afşin
The aim of this work was to investigate the antiproliferative and pro-apoptotic effects of propolis on human breast cancer cells using a simple and inexpensive nanoformulation. Various meth ods were used to characterize the surface and morphology of propolis nanoparticles (NP-Pro), including UV-VIS, FTIR, DLS, and EDX-SEM. The cytotoxic activity of MCF-7, MDA-MB-231 breast cancer cells was measured by XTT technique and compared with healthy cells (MCF-10A). The apoptotic effect of NP-Pro was assessed by flow cytometry using Annexin/PI. The IC50 values of NP-Pro on MCF-7, MDA-MB-231 and MCF-10A cells were 13.67 ± 0.89, 17.89 ± 0.6, 29.9 ± 0.56 μg, respectively. According to these findings, the NP-Pro form we prepared was more cytotoxic on cancer cells than propolis. Cancer cells had much stronger apoptotic activity than healthy cells (p < 0.0001). In this work, NP-Pro was produced through a distinct, straightforward, and low-cost method. In summary, the NP-Pro we synthesized may be a promising potential agent for breast cancer treatment due to its specific cytotoxicity via apoptosis.
Plant?inspired adhesive and injectable natural hydrogels: in vitro and in vivo studies
(2023) Bohórquez‑Moreno,Cristian Daniel; Öksüz, Kerim Emre; Dinçer, Emine; Hepokur, Ceylan; Şen, İlker
The development of alternative thera peutic treatments based on the use of medicinal and aromatic plants, such as Juniper communis L., has aroused interest in the medical feld to fnd new alter natives to conventional therapeutic treatments, which have shown problems related to bacterial resistance, high costs, or sustainability in their production. The present work describes the use of hydrogels based on sodium alginate and carboxymethyl cellulose, with combinations of juniperus leaves and berry extracts, in order to characterize their chemical characteris tics, antibacterial activity, tissue adhesion test, cyto toxicity in the L929 cell line, and their efects on an in vivo model in mice to maximize the use of these materials in the healthcare feld. Overall, an adequate antibacterial potential against S. aureus, E. coli and P. vulgaris was obtained with doses above 100 mg.mL−1 of hydrogels. Likewise, low cytotoxicity in hydrogels combined with extracts has been identifed accord ing to the IC50 value at 17.32 µg.mL−1, compared to the higher cytotoxic activity expressed by the use of control hydrogels with a value at 11.05 µg.mL−1. Moreover, in general, the observed adhesion was high to diferent tissues, showing its adequate capacity to be used in diferent tissue typologies. Furthermore, the invivo results have not shown erythema, edema, or other complications related to the use of the pro posed hydrogels. These results suggest the feasibility of using these hydrogels in biomedical applications given the observed safety
New Fluoro- and Trifluoromethyl-Substituted Trimethoxychalcones as Anticancer Agents: Synthesis, Bioevaluation, and Computational Studies
(2023) Polat,M. Fatih; Aktas Anil, Derya; Ozkemahli,Gizem; Turkmenoglu, Burcin; Hepokur,Ceylan; Burmaoglu,Serdar; Algul,Oztekin
We designed and synthesized a novel series of trimethoxy chalcones with CF3 or F substituents at various positions of ring B, characterized using IR, NMR spectral data, and elemental analyses, based on the fact that methoxy and fluoro-substituted chalcones are included in the literature as a pharmacophore due to their anticancer activities. All compounds (12-21) were tested for cytotoxicity against A549, HEPG2, MCF7, and normal mouse fibroblasts (L929) using the XTT assay. The most active compound, 13, was also shown to induce MCF7 cell cycle arrest at the G0/G1 phase, indicating that they exert their antitumor potency via MCF7 cell apoptosis. The mechanisms involved in apoptotic cell death induced by compound 13 were also investigated to see if apoptotic proteins such as Bax, Bcl-2, and p53 were involved. In addition, the compounds with the strongest apoptotic effects against human EGFR and VEGFR-2 receptors were studied in silico. Finally, methoxy and fluoro substituted chalcones derivatives have been shown to have potent anticancer properties.
Assessing the Antiangiogenic Effects of Chalcones and Their Derivatives
(19 Jan 2023) Hepokur ,Ceylan; Serdar, Burmaoglu; Arzu,Gobek; Derya,Aktas Anil; Mehmet ,Abdullah Alagoz; Adem,Guner; Cem, Guler; N. Ulku,Karabay Yavasoglu; Oztekin,Algul
Pathological angiogenesis plays a critical role in tumorigenesis and tumor pro gression, and anti-angiogenesis therapies have evinced promising antitumor effects in solid tumors. Chalcone skeleton has been regarded as a potential antitumor agent that also targets angiogenesis. In this study, we designed twenty-one non-fluoro-substituted chalcones (13–18, 24–27) and saturated chalcone derivatives (19–23, 28–33) as anti-angiogenic compounds. During the initial stage, these compounds were assessed for their anti-cancer activities against MCF-7 cancer cell lines according to the MTT assay. The compounds revealed satisfactory anti-proliferative capability. An ex vivo fertilized hens’ egg-chorioallantoic membrane (HET-CAM) angiogenic study was conducted for the compounds to gauge their mortality and toxicity, which, in turn, revealed a potent anti-angiogenic effect. Eight compounds (16, 17, 21, 24, 26, 27, 29, and 31) significantly reduced densities of capillaries on CAM, whereas compounds 27 and 29 were the most effective anti-angiogenic agents, when compared with Suramin. Moreover, RT-qPCR analysis demonstrated that the anti-angiogenic activity was associated with the fold changes of VEGFR2. Molecular docking studies were conducted for compounds to investigate their mode of interaction within the binding site of VEGFR-2 kinases. This work pro vided a basis for further design, structural modification, and development of chalcone derivatives as new anti-angiogenic agents.
Synthesis and Molecular Docking of New N-Acyl Hydrazones- Benzimidazole as hCA I and II Inhibitors
(20.01.2023)
Background: The carbonic anhydrases (CAs) which are found in most living organisms is a member of the zinc-containing metalloenzyme family. The abnormal levels and activities are frequently associated with various diseases therefore CAs have become an attractive target for the design of inhibitors or activators that can be used in the treatment of those diseases. Methods: Herein, we have designed and synthesized new benzimidazole-hydrazone derivatives to investigate the effects of these synthesized compounds on CA isoenzymes. Chemical structures of synthesized compounds were confirmed by 1H NMR, 13C NMR, and HRMS. The synthetic derivatives were screened for their inhibitory potential against carbonic anhydrase I and II by in vitro assay. Results: These compounds have IC50 values of 5.156-1.684 μM (hCA I) and 4.334-2.188 μM (hCA II). Inhibition types and Ki values of the compounds were determined. The Ki values of the compounds were 5.44 ± 0.14 μM-0.299 ± 0.01 μM (hCA I) and 3.699 ± 0.041 μM-1.507 ± 0.01 μM (hCA II). The synthetic compounds displayed inhibitory action comparable to that of the clinically utilized reference substance, acetazolamide. According to this, compound 3p was the most effective molecule with an IC50 value of 1.684 μM. Accordingly, the type of inhibition was noncompetitive and the Ki value was 0.299 ± 0.01 μM. Conclusion: According to the in vitro test results, detailed protein-ligand interactions of the compound 3p, which is more active against hCA I than standard azithromycin (AZM), were analyzed. In addition, the cytotoxic effects of the compounds on the L929 healthy cell line were evaluated.
IMMUNOTHERAPY IN CANCER TREATMENT
(31.06.2023)
Cancer, which causes the death of approximately 10 million people every year, is a type of disease that begins to spread to other parts of the body by uncontrolled proliferation of cells in the tissues and organs of our body. There are more than 100 types of cancer diagnosed. Cancer types are named according to the tissue or organ in which they occur. The most known and generally preferred cancer treatment methods are surgery, radiotherapy and chemotherapy. However, when the studies conducted in recent years are examined, it is seen that immunotherapeutic treatment methods also show promise (Hamilton, 2010). In this section, many topics such as the emergence of immunotherapy, different application methods, advantages, disadvantages and the future of immunotherapy are mentioned.
Nekroz
(31.12.2023)
Nekroz, hücrenin ani bir şok (radyasyon, ısı, kimyasallar, hipoksi, iskemi vb.), mekanik stres gibi şiddetli çevresel bozulmalar ve donma-çözülme sonrası gibi ciddi şekilde hasar gördüğü, enerjiden bağımsız bir hücre ölümü şeklidir. Bu gibi durumlarda herhangi bir özel sinyal yolunun aktivasyonu gerekmeden hücrede nekroz görülür. En yaygın nedeni olarak hipoksi bilinmektedir (Vermeulen ve ark, 2005). Hücre, çevresi ile homeostazı sürdüremediği için genellikle şişerek yanıt verir (Green ve ark, 2015). Hücre içeriğinin çevre dokulara dökülmesi ile inflamasyon gözlenir. İnflamatuar hücrelerin toplanması ile kemotatik sinyaller gönderilir (D’arcy, 2019). Sinyalleşme veya hasara bağlı lezyonlardan sonra nekroz, mitokondriyal işlev bozukluğunu ve bunların belirtilerini içerir. Sitoplazmik boşlukların oluşumu, yoğunlaşmış, şişmiş veya parçalanmış mitokondri, artan reaktif oksijen türleri (ROS) oluşumu, ATP tükenmesi, Ca 2+ kanallarının açılması ve homeostazının gerçekleştirilememesi, organellerin perinükleer kümelenmesi, kalpainler ve katepsinler tarafından proteoliz, şişmiş lizozomlar, lizozomal yırtılma ve erken plazma zarı rüptürü gibi belirtileri içerir. Ayrıca bu nekrotik aracılar genellikle ölmekte olan hücrede aynı anda indüklenir ve hücrenin ölümünü başlatmak için birbirlerinin yeteneklerini güçlendirir. Ek olarak, apoptoz veya otofajinin düzenlenmesinde yer alan spesifik proteinlerin inhibisyonu, hücre ölümü tipini nekroza değiştirebilir (Golstein ve ark, 2007).
Synthesis, biological evaluation and in silico studies of novel thiadiazole-hydrazone derivatives for carbonic anhydrase inhibitory and anticancer activities
(04.08.2023)
ABSTRACT Thiadiazole and hydrazone derivatives (5a–5i) were synthesized and their chemical structures were verified and described by 1 H NMR, 13 C NMR, and HRMS spectra. Three cancer cell lines (MCF-7, MDA, and HT-29) and one healthy cell line (L929) were used to test the cytotoxicity activity of synthesized compounds as well as their inhibitory activity against carbonic anhydrase I, II and IX isoenzymes. Compound 5d (29.74 µM) had a high inhibitory effect on hCA I and compound 5b (23.18 µM) had a high inhibitory effect on hCA II. Furthermore, compound 5i was found to be the most potent against CA IX. Compounds 5a- 5i, 5b and 5i showed the highest anticancer effect against MCF- 7 cell line with an IC value of 9.19 and 23.50 µM, and compound 5d showed the highest anticancer effect against MDA cell line with an IC 50 50 value of 10.43 µM. The presence of fluoro substituent in the o-position of the phenyl ring increases the effect on hCA II, while the methoxy group in the o-position of the phenyl ring increases the activity on hCA I as well as increase the anticancer activity. Cell death induction was eval- uated by Annexin V assay and it was determined that these compounds cause cell death by apoptosis. Molecular docking was performed for compounds 5b and 5d to understand their biological interactions. The physical and ADME properties of compounds 5b and 5d were evaluated using SwissADME.
Antioksidan Miktarını Total Olarak Tayin Etme Yöntemleri
(31.12.2023)
Zararlı serbest radikallere karşı savaşan ve hücreleri koruyan moleküller olan antioksidanlar tüm canlıların hayatta kalması için hayati önem taşır. Bu da bilim insanlarını, gıdaların antioksidan özelliklerini ölçme amacıyla basit ama etkili testler geliştirmeye yönlendirmiştir. Bu testler, antioksidanların kapasite tahlillerini ölçmek için dünya çapında kabul görmüş ve geliştirilerek kullanılan önemli analitik araçlardır. Çalışma prensibi olarak, tahliller, antioksidanlara izin veren bir kimyasal reaksiyon içerir ve ayarlanmış bir konsantrasyonla reaksiyona girmek için numunede mevcut tahlil reaktifi bulundurulur. Böylelikle hangi konsantrasyonda bu reaksiyonu vereceği ve bunun zamana bağlı eğrisi göz önünde bulundurularak yorum yapılabilir (1). Antioksidan kapasiteyi ölçme amacıyla yapılan çalışmalar sonunda birçok yöntem geliştirilmiş olup bunları temelde ikiye ayırmak mümkündür: Elektron transferine dayanan (ET) yöntemler, hidrojen atomunun transferine bağlı yöntemler (HAT). Hidrojen atom transferine bağlı yöntemlerin büyük kısmında en basit şekilde moleküler yapısında (-N=N-) barındıran ve azo- bileşiği olarak da adlandırılan yapıların peroksil radikallerini bozunmaya uğrayarak oluşturması sonucunda antioksidan-substrat yarışına dayalı yarışmalı kinetik reaksiyonları kullanılır. Diğer bir deyişle oksijen ve azot temelli bileşiklerin reaksiyonu sonucu floresan maddenin sürüme uğratılması ve antioksidan maddenin bu sürümü engellemesine dayalıdır. ET temelli yöntemlerse renk değişimine dayalı yöntemleri temsil eder. Bu reaksiyonlarda antioksidan madde, oksidanı indirgeyerek bir renk değişimine sebep olur (2). Renk değişiminin skalası da örnek maddelerin antioksidan içerikleri hakkında bilgi sahibi olmamızı sağlar.
The Effect of Vitamins on Oxidation in Experimentally Diabetes Conditioned Rats
(27.07.2023)
Diabetes Mellitus (DM) is a metabolic disorder that is very common in our society, is caused by a combination of hereditary and environmental factors, and results in an increase in blood glucose levels. Diabetes mellitus develops as a result of increased blood glucose level and impaired insulin secretion. Antioxidant enzymes cannot be synthesized enough in patients with diabetes mellitus and free radicals damage tissues. In this study, the effects of vitamin C and vitamin E on lipid peroxidation and antioxidant enzyme activities in kidney tissue of streptozotocin-induced diabetic rats were investigated. Male wistar rats, were grouped into five each consisting 8 rats as (nondiabetic control (K), diabetic (D), diabetic Vitamin E (E), diabetic Vitamin C (C), and diabetic Vitamin E and C (EC). Diabetes mellitus was induced in rats by intraperitoneal injection of 55mg/ kg STZ. After the injection, i.p. 268mg/kg. vitamin E, 250 mg/ kg vitamin C by gavage were administrated for four weeks. As an indicator of lipid peroxidation malondialdehyde (MDA) levels, antioxidant enzymes as superoxide dismutase (SOD), catalase (CAT) and and glutothione peroxides (GSH-PX) activities were measured in kidney tissue homogenates. In the study, MDA level of group D was significantly higher than groups K, E, C and EC. Statistically significant difference was not observed in CAT levels among the groups. SOD enzyme levels in group D was higher compared to group K, and lower in group EC compared to groups C, and D. GSH-Px enzyme levels in group D and group C were significantly higher compared to group K. Group D GSH-Px levels were significantly lower whwn compared to group E, C and EC, GSH-Px levels of EC group was lower compared to group C. As a result, in this study it was demonstrated that vitamin C and vitamin E have positive effect on lipid peoxidation and as a result decreased the high levels of MDA, SOD, GSH-Px levels of diabetic rat kidney tissues.
Investigation of the Relationship between the Chemical Structures and the Cytotoxicity of Some Maleic Anhydride-Containing Copolymers as Polymeric Drug Carriers
(23.11.2023)
Polymer-based substances have been an important biomaterial in the advancement of drug delivery systems as they enabled the controlled release of therapeutic agents in fixed doses with high bioavailability, lower toxicity, and higher pharmaceutical efficacy. This study aimed to find out whether there is a relationship between cytotoxicity and the chemical structure of the copolymers that act as carriers in many copolymer-drug conjugates by carrying out their characterization using spectroscopy and morphology-elucidated techniques described in our previous studies. Selected maleic anhydride, including polymeric carriers such as poly(maleic anhydride-co-methyl methacrylate) (MAMMA), poly(maleic anhydride-alt-vinyl acetate) (MAVA), and poly(maleic anhydride-alt-allylphenyl ether (MAAPE) were synthesized via a charge transfer complex (CTC) produced by a radical chain copolymerization reaction. 1,2,3 In addition, the commercial form of poly(4-styrenesulfonic acid-comaleic acid) (PSSMA) was purchased. The cytotoxic effects of all samples were examined using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) analysis for L929 (fibroblast cell), MDA (breast cancer), MCF7 (breast cancer), and C6 cell lines (glial tumor) were examined in vitro by comparison with cisplatin (reference compound). The Annexin V binding assay was also studied for all copolymers. When compared with cisplatin, which is actively used in the clinic for cancer therapy, PSSMA was found to have a cytotoxic effect on C6 cells, although not as strong as cisplatin, but the most effective copolymer was MAMMA due to its low IC50 value. In summary, the pharmaceutical agents delivered with these carriers could represent a promising and effective therapeutic modality for glioblastoma.
INVESTIGATION OF SALVIA CADMICA’S ANTIOXIDANT PROPERTIES AND CYTOTOXIC PROPERTIES IN BREAST CANCER CELL LINE AND ITS APOPTOTIC INDUCTION
(30.05.2023)
Salvia cadmica is an endemic species known to have antioxidant, antimicrobial and aromatic properties and the existence of Salvia species is known to date back to 753 BC. This species, whose medicinal properties were first discovered by the Romans at this time, is used in a wide variety of fields. Salvia species, which have a content especially rich in essential oils, are often used in cosmetic, medical, and industrial fields. In addition, it has been shown by past studies that the root parts of salvia species contain terpenoids, polyphenols and essential fatty acids. Numerous cancer studies have been conducted with salvia species, and it seems that not enough research has been done for salvia cadmica. In this study, IC50 values for Total Antioxidant Status (TAS) were determined by ethanol extract taken from the above-ground parts of Salvia cadmica. Then, the cytotoxicity in the breast cancer cell line (MCF-7) and healthy fibroblast cell line was determined by using the MTT method. Accordingly, the IC50 dose of Salvia Cadmica was higher than 78.13 ± 4.82 μg/mL for the MCF-7 cell line.
New imidazole derivatives as aromatase inhibitor: Design, synthesis, biological activity, molecular docking, and computational ADME-Tox studies
(06.01.2023)
In this study, a series of imidazole derivatives was designed, synthesized, and evaluated for in vitro bi- ological activity on the human breast cancer cell line MCF7 by MTT assay. To determine the selectivity of the compounds, their cytotoxic effects on the L929 (healthy mouse ﬁbroblast) cell line were also in- vestigated. Compounds 1a, 1b , and 1d were found to be more effective than the reference drug cisplatin against the MCF7 cell line. It is seen that the cytotoxic effects of the compounds on the L929 cell line are quite low, and the compounds are found to be highly selective. The inhibition potentials of the com- pounds 1a, 1b, 1d , and 1k which were effective on the MCF7 cell line, and on the aromatase enzyme were evaluated and it was found that the compounds had similar effects to the reference drug letro- zole. Further, the interactions between the best active compounds and the human aromatase cytochrome P450 (CYP) enzyme were analyzed through a molecular docking study. The ﬁndings suggest that these compounds could be a promising candidate for the creation of a new family of non-steroidal aromatase inhibitors. Finally, computational ADME-Tox studies of compounds 1a, 1b, 1d , and 1k were performed and found to have the appropriate proﬁle.
INVESTIGATION OF THE ANTIPROLIFERATIVE EFFECT OF SALVIA CADMICA ON COLON CANCER
(07.05.2023)
Salvia cadmica is an endemic species known to have antioxidant, antimicrobial and aromatic properties and the existence of Salvia species is known to date back to 753 BC. This species, whose medicinal properties were first discovered by the Romans at this time, is used in a wide variety of fields. Salvia species, which have a content especially rich in essential oils, are often used in cosmetic, medical, and industrial fields. In addition, it has been shown by past studies that the root parts of salvia species contain terpenoids, polyphenols and essential fatty acids. Numerous cancer studies have been conducted with salvia species, and it seems that not enough research has been done for salvia cadmica. In this study, IC50 values for Total Antioxidant Status (TAS) were determined by ethanol extract taken from the above-ground parts of Salvia cadmica. Then, using the MTT method, their cytotoxicity in the human colorectal adenocarcinoma cancer cell line (HT-29) and healthy fibroblast cell line (L929) was determined. Accordingly, Salvia Cadmica's IC50 dose was 64.22 ± 6.31 for the HT-29 cell line. For healthy fibroblast cell lines, this ratio was higher than 400 μg/mL.
New benzimidazole?oxadiazole derivatives: Synthesis, ??glucosidase, ??amylase activity, and molecular modeling studies as potential antidiabetic agents
(23.01.2023)
Benzimidazole‐1,3,4‐oxadiazole derivatives (5a–z) were synthesized and characterized with different spectroscopic techniques such as 1 HNMR, 13 CNMR,andHRMS.The synthesized analogs were examined against α‐glucosidase and α‐amylase enzymes to determine their antidiabetic potential. Compounds 5g and 5q showed the most activity with 35.04 ± 1.28 and 47.60 ± 2.16 µg/mL when compared with the reference drug acarbose (IC = 54.63 ± 1.95 µg/mL). Compounds 5g, 5o, 5s,and5x were screened against the α‐amylase enzyme and were found to show excellent potential, with IC 50 values ranging from 22.39 ± 1.40 to 32.07 ± 1.55 µg/mL, when compared with the standard acarbose (IC = 46.21 ± 1.49 µg/mL). The antioxidant activities of the effective compounds (5o, 5g, 5s, 5x,and5q) were evaluated by TAS methods. A molecular docking research study was conducted to identify the active site and explain the functions of the active chemicals. To investigate the most likely binding mode of the substances 5g, 5o, 5q, 5s,and5x, a molecular dynamics simulation was also carried out. 50 50

Güncel Gönderiler