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    Anti-Cancer and Antimicrobial Properties of St. John's Wort (Hypericum perforatum)
    (Inonu University, 2025) Karci, Hüseyin
    St. John's Wort (Hypericum perforatum) is a medicinal plant widely used in traditional medicine, known for its significant pharmacological properties, including antimicrobial and antitumor activities. In this study, extracts of Hypericum perforatum were prepared using the maceration method from plants collected at the foothills of Kubbe Mountain, located in the Pütürge district of Malatya province. These extracts were evaluated for their antimicrobial and anticancer activities. Antimicrobial activity was investigated against microorganisms, including Escherichia coli (ATCC 25922), Staphylococcus aureus (ATCC 29213), Pseudomonas aeruginosa (ATCC 27853), Candida albicans (SC5314/ATCC MYA-2876), and Candida glabrata (ATCC 2001), using the Disk Diffusion Test. Anticancer activity was assessed in HCT116 (human colon cancer), SH-SY5Y (human brain cancer), and BEAS-2B (human healthy lung cell) lines using the MTT assay, with IC50 values compared to those of the standard anticancer drug, Cisplatin. Regarding antimicrobial activity, the inhibition zones were measured as 9.33±0.78 mm for E. coli, 12.17±0.53 mm for P. aeruginosa, and 11.73±0.41 mm for S. aureus. No inhibition was observed for the yeasts C. albicans and C. glabrata. Low cytotoxicity was observed in the healthy cell line BEAS-2B, with an IC50 value of 48.87 ± 7.03 μg/mL, whereas high cytotoxicity was detected in cancer cell lines, with IC50 values of 23.27±3.35 μg/mL for SH-SY5Y and 10.67±3.05 μg/mL for HCT116. These findings indicate that Hypericum perforatum extract can effectively target cancer cells while sparing healthy cells, suggesting its potential for selective toxicity. In conclusion, Hypericum perforatum extract demonstrated significant antimicrobial activity against P. aeruginosa and S. aureus, as well as strong cytotoxicity in cancer cell lines, highlighting its potential as a natural therapeutic agent. © 2025, Inonu University. All rights reserved.
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    Gümüş-benzimidazol-2-iliden kompleksleri ve biyolojik özellikleri
    (İnönü Üniversitesi, 2022) Karci, Hüseyin
    Bu çalışmada azota bağlı farklı hacimli ve fonksiyonel grup içeren alkil grupları 5,6-dimetilbenzimidazole bağlanarak yeni karben öncülleri 2a-j sentezlendi. Bu bileşikler Ag2O ile etkileştirilerek Ag-NHC kompleksleri 3a-i sentezlendi. Bileşiklerin yapıları 1H NMR, 13C NMR ve mikroanaliz teknikler ile aydınlatıldı. Sentezlenen bileşiklerin antimikrobiyal aktiviteleri Mantar alt grubu olan mayalardan C. albicans (SC5314/ ATCC MYA-2876) ve C. glabrata (ATCC 2001), Bakterilerden E. coli (ATCC 25922), S. aureus (ATCC 29213) ve P. aeruginosa (ATCC 27853) karşı incelendi ve MIC (μg/ml) değerleri hesaplandı. Benzimidazolyum tuzlarının (2a-j) antimikrobiyal aktivite sonuçlarını değerlendirdiğimizde; 2d ve 2e bileşiklerinin S. aureus bakterisine karşı en etkili bileşikler olduğu ve göstermiş oldukları antibakteriyel aktiviteler ile 12,5 µg/mL MIC değerlerine ulaştıklarını belirledik. 2a, 2c, 2f, 2g bileşiklerinde de antimikrobiyal aktiviteler gözlendi ve MIC değerleri hesaplandı. Yeni Ag-NHC komplekslerinin (3a-i) antimikrobiyal aktivite sonuçlarını değerlendirdiğimizde; 3b bileşiğinin tüm bakteri ve maya türlerine karşı en etkili bileşik olduğunu saptadık. 3b bileşiğinin özellikle C. glabrata mayasına karşı gösterdiği antifungal aktivite ile 6,25 µg/mL MIC değerine ulaştığını belirledik. 3c, 3d, 3f ve 3g bileşiklerinde de antimikrobiyal aktiviteler gözlendi ve MIC değerleri hesaplandı. Anahtar Kelimeler: N-Heterosiklik Karben, Bezimidazolyum Tuzları, Gümüş-benzimidazol-2-iliden kompleksleri, Antimikrobiyal aktivite.
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    Synthesis, characterization, and anticancer evaluation of N-Heterocyclic entities: ADME profiling and In Silico predictions
    (Elsevier Inc., 2026) Abbaoui, Zakariae; Khibech, Oussama; Karci, Hüseyin; Dündar, Muhammed; Özdemir, İlknur; Gürbüz, Nevin; Koç, Ahmet
    This study aimed to synthesize a novel series of N-heterocyclic compounds and evaluate their integrated pharmacological potential by coupling in vitro selective cytotoxicity on tumor and normal cell lines with predictive in silico ADME-Tox profiling. This research highlights the anti-cancer potential of twelve synthesized compounds, five of which are new chemical entities never before described in the literature. Their detailed structural characterization (NMR 1H, 13C, IR), combined with in silico predictions (ADME-Tox), confirmed their ability to cross essential biological barriers, in particular the intestinal membrane and, for certain derivatives, the BBB. Biological evaluations conducted on SH-SY5Y (neuroblastoma) and HCT116 (colorectal carcinoma) cell lines revealed several compounds with IC50 values lower than those of cisplatin while exhibiting reduced cytotoxicity towards the normal human epithelial BEAS-2B cell line. In particular, the compound (1H-imidazol-1-yl)methanol (designated as Compound 6) stands out with IC50 values of 6.97 ± 0.06 µM on SH-SY5Y and 10.70 ± 0.33 µM on HCT116, significantly lower than those of cisplatin under the same experimental conditions. This profile, combined with virtually no toxicity on normal BEAS-2B cells (IC50 > 800 µM), highlights its remarkable selectivity. These results highlight optimized pharmacological properties and suggest the potential for developing selective therapeutic agents against different types of cancer, particularly neuronal and colorectal tumors. Future research will focus on in-depth mechanistic studies and in vivo validation to optimize the efficacy, pharmacokinetics, and safety of these promising molecules. © 2025