Sürdürülebilir Kalkınma Amaçları
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- MakaleAçık Erişim2026Evaluation of antioxidant and antiproliferative activities of shogaol and its modulatory effects on key metabolic enzymes
Yapıcı, İsmail; Gülçin, İlhami
Phenolic compounds are versatile bioactive molecules, particularly in food applications. In this study, the antioxidant capacity of Shogaol, a member of the phenolic class, was evaluated using several methods. Additionally, its inhibitory effects on human carbonic anhydrase I and II (hCA I and II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glycosidase, and α-amylase enzymes, as well as its antiproliferative effects on A-549 lung cancer, HT-29 colon cancer, MCF-7 and MDA-MB-453 breast cancer cell lines, and the 3T3-L1 mouse fibroblast normal cell line, were investigated. To determine the antioxidant capacity of Shogaol, DPPH and ABTS radical scavenging assays, as well as Cu²⁺, Fe³⁺, and FRAP reduction methods, were employed. Its inhibitory effects on hCA I and II, AChE, BChE, α-glycosidase, and α-amylase enzymes were examined. Furthermore, cell counting was performed using the TBE method, and cell viability was measured with the XTT assay to assess the antiproliferative effects of Shogaol on A-549, HT-29, MCF-7, MDA-MB-453, and 3T3-L1 cell lines. Shogaol demonstrated higher antioxidant capacity than BHA, BHT, and Trolox in the FRAP assay (60 µg/mL), higher than BHT in the DPPH scavenging assay, and higher than Trolox in the ABTS, Cu²⁺, and Fe³⁺ reduction assays. Shogaol also exhibited significant inhibitory effects against hCA I, hCA II, AChE, BChE, and α-glycosidase, with IC₅₀ values of 75.91, 47.04, 37.44, 24.11, and 35.72 nM, respectively. Moreover, Shogaol showed a more potent antiproliferative effect than the standard chemotherapeutic drug Carboplatin in A-549 lung cancer and HT-29 colon cancer cell lines, and greater efficacy than Docetaxel in the MCF-7 breast cancer cell line.
- MakaleYalnız künye2024Assessment of Anticholinergic and Antidiabetic Properties of Some Natural and Synthetic Molecules: An In Vitro and In Silico Approach
Çomaklı, Veysel; Aygül, İmdat; Sağlamtaş, Rüya; Kuzu, Müslüm; Demirdağ, Ramazan; Akincioğlu, Hülya; Adem, Şevki; Gülçin, İlhami
Introduction: This study aimed to determine the in vitro and in silico effects of some natural and synthetic molecules on acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α-glucosidase enzymes. Background: Alzheimer's disease (AD) and Type II diabetes mellitus (T2DM) are considered the most important diseases of today’s world. However, the side effects of therapeutic agents used in both diseases limit their use. Therefore, developing drugs with high therapeutic efficacy and better pharmacological profile is important. Objectives: This study sets out to determine the related enzyme inhibitors used in treating AD and T2DM, considered amongst the most important diseases of today’s world. Methods: In the current study, the in vitro and in silico effects of dienestrol, hesperetin, L-thyroxine, 3,3',5-Triiodo-L-thyronine (T3) and dobutamine molecules on AChE, BChE and α-glycosidase enzyme activities were investigated. Results: All the molecules showed an inhibitory effect on the enzymes. The IC50 and Ki values of the L-Thyroxine molecule, which showed the strongest inhibition effect for the AChE enzyme, were determined as 1.71 µM and 0.83 ± 0.195 µM, respectively. In addition, dienestrol, T3, and dobutamine molecules showed a more substantial inhibition effect than tacrine. The dobutamine molecule showed the most substantial inhibition effect for the BChE enzyme, and IC50 and Ki values were determined as 1.83 µM and 0.845 ± 0.143 µM, respectively. The IC50 and Ki values for the hesperetin molecule, which showed the strongest inhibition for the α-glycosidase enzyme, were determined as 13.57 µM and 12.33 ± 2.57 µM, respectively. Conclusion: According to the results obtained, the molecules used in the study may be considered potential inhibitor candidates for AChE, BChE and α-glycosidase.
- MakaleAçık Erişim2024Exploring the Impacts of Angelica purpurascens Extracts on Anticholinergic, Antidiabetic, Antibacterial Potential, and Antioxidant Capacity
Topal, Meryem; Topal, Fevzi; Yilmaz, Fırat
In Kars-Sarıkamış-Soğanlı, Angelica purpurascens (A. purpurascens) emerges as a promising natural antioxidant source. Extracts from its leaves, branches, and flowers underwent thorough bioanalytical assessments. The leaf extract exhibited the highest concentrations of herbal flavonoids (45.22 µg QE/mg extract) and total phenolics (28.96 µg GAE/mg extract). Branch extracts demonstrated significant enzymatic activity against AChE and BChE with IC50 values of 37.26 mg/mL and 9.08 mg/mL respectively. The flower extract displayed notable antibacterial properties. This study sheds light on the therapeutic potential of A. purpurascens ethanol extracts, suggesting benefits for Alzheimer’s, cell damage-induced diseases, and diabetes mellitus. It pioneers new enzymatic and antioxidant insights and contributes to understanding this abundant Türkiye species. A. purpurascens holds promise for pharmaceutical exploration, offering potential solutions for challenging health conditions.
- MakaleAçık Erişim2022Evaluation of the in vitro antioxidant, antidiabetic and anticholinergic properties of rosmarinic acid from rosemary (Rosmarinus officinalis L.)
Topal, Meryem; Gulcin, İlhami
In this study, antidiabetic, anticholinergic, and antioxidant abilities of rosmarinic acid were evaluated and compared to standards. To determine its antioxidant activity different in vitro bioanalytical methods, including total antioxidant activity (TAA), ABTS•+ scavenging activity, O2•- scavenging activity, DPPH· scavenging activity, DMPD•+ scavenging activity, potassium ferric cyanide reduction ability, cupric ion (Cu2+) reduction capacity, H2O2 scavenging activity, and ferrous ions (Fe2+) binding activities were separately performed. Also, butylated hydroxyanisole (BHA), Trolox, α-tocopherol, and butylated hydroxytoluene (BHT) were used as the reference antioxidants. Rosmarinic acid inhibited the linoleic acid emulsion peroxidation by 89.2% while BHA, BHT, Trolox and α-tocopherol inhibited as 87.3, 97.6, 90.3 and 75.3%, respectively, at the same concentration (30 μg/mL). When these results are evaluated, rosmarinic acid had effective TAA than BHA and α-tocopherol and close to BHT and Trolox. In addition, rosmarinic acid exhibited Kİ values of 9.67 ± 0.81 nM towards acetylcholinesterase (AChE) and 33.56 ± 2.96 nM against α-glycosidase enzymes.
- MakaleAçık Erişim2019Anticholinergic and antidiabetic effects of isoeugenol from clove (Eugenia caryophylata) oil
Topal, Fevzi
Isoeugenol (2-methoxy-4-(prop-1-en-1-yl)phenol), a component of from clove (Eugenia caryophylata) oil, is a starting material for both the biotechnological and synthetic production of vanillin and vanillic acid. In this article, the isoeugenol showed excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes, α-glycosidase, and α-amylase. Isoeugenol has the IC50 values of 411.5 for α-amylase, 19.25 nM for α-glycosidase and 77.00 nM for AChE. Ki values of isoeugenol were found as 21 ± 9 nM and 16 ± 3 nM against α-glycosidase and AChE, respectively. On the other hand, tacrine as standard AChE inhibitor exhibited IC50 value of 20.38 nM. α-Glycosidase inhibitors, commonly referred to as starch blockers, are anti-diabetic drugs that help reduce edible blood glucose levels. AChE inhibitors are used for the treatment of some neurologic degenerational diseases, which involve Alzheimer’s disease. Also, there is a growing interest and the need to search for newer effective and safe AChE, α-amylase, and α-glycosidase inhibitors for the treatment of some metabolic disorder.
- MakaleAçık Erişim2019The inhibition profile of sesamol against α-glycosidase and acetylcholinesterase enzymes
Topal, Meryem
Sesamol (1,3-benzodioxol-5-ol) is found in the oilseed product, sesame. In our study, the inhibitory effects of sesamol compound on acetylcholinesterase and α-glycosidase enzymes were evaluated. Another aim of this study was to compare the inhibitory effects of sesamol to acarbose for α-glycosidase enzyme and tacrine for acetylcholinesterase (AChE). Sesamol exhibited non-competitive inhibition for both metabolic enzymes. IC50 values for AChE and α-glycosidase enzymes were calculated as 86.63 nM and 99.00 nM, respectively. On the other hand, Ki values were calculated as 46.68 nM and 75.33 nM for AChE and α-glycosidase enzymes, respectively. According to the obtained results showed effective inhibition at low concentrations.
- MakaleYalnız künye2019Inhibition profiles of Voriconazole against acetylcholinesterase, α-glycosidase, and human carbonic anhydrase I and II isoenzymes
Topal, Fevzi
In this work, the inhibitory activity of Voriconazole was measured against some metabolic enzymes, including human carbonic anhydrase (hCA) I and II isoenzymes, acetylcholinesterase (AChE), and α-glycosidase; the results were compared with standard compounds including acetazolamide, tacrine, and acarbose. Half maximal inhibition concentration (IC50) values were obtained from the enzyme activity (%)-[Voriconazole] graphs, whereas Ki values were calculated from the Lineweaver-Burk graphs. According to the results, the IC50 value of Voriconazole was 40.77 nM for α-glycosidase, while the mean inhibition constant (Ki) value was 17.47 ± 1.51 nM for α-glycosidase. The results make an important contribution to drug design and have pharmacological applications. In addition, the Voriconazole compound demonstrated excellent inhibitory effects against AChE and hCA isoforms I and II. Voriconazole had Ki values of 29.13 ± 3.57 nM against hCA I, 15.92 ± 1.90 nM against hCA II, and 10.50 ± 2.46 nM against AChE.