INVESTIGATION on THE ANTIPROLIFERATIVE ACTIVITY OF CHLORO[1-(2-METHYL-2-PROPENYL)-3-(2-CHLOROBENZYL) BENZIMIDAZOLE-2-YLIDENE Ag(I) COMPOUND on SH-SY5Y NEUROBLASTOMA CELLS

Abstract

In this study, it has been investigated the antiproliferative activities of benzimidazole-based NHC ligand (1) and its silver(I) complex (2) having chloride. Both ligand (1) and complex (2) have been tested for their antiproliferative activity on SH-SY5Y neuroblastoma cells and WI-38 human healthy fibroblast cells for 24 h, 48 h and 72 h using the (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. According to the experimental results, ligand (1) has not shown antiproliferative activity on WI-38 healthy cells in all-time points but has shown concentration- and time-dependent antiproliferative activity on SH-SY5Y neuroblastoma cells . Our results have shown that complex (2) has a dose and time-dependent antiproliferative activity against both SH-SY5Y neuroblastoma cells and WI-38 healthy cells. It has also been found that complex (2) has more antiproliferative activity than ligand (1) on SH-SY5Y neuroblastoma cells and WI-38 healthy cells. The IC50 value of the ligand (1) towards the SH-SY5Y neuroblastoma cell line was calculated > 20, 8.90, and 4.28 µM for 24 h, 48 h, and 72 h , respectively. IC50 values of ligand (1) against WI-38 normal lung fibroblast cell lines were calculated > 20 µM for 24, 48, and 72 hours. IC50 values of the complex (2) against SH-SY5Y neuroblastoma and WI-38 normal lung fibroblast cell lines were found to be 3.80, 3.15, and 2.21 µM; and 16.9, 14.6, and 8.34 µM for 24 h, 48 h and 72 h, respectively. The selectivity index (SI) was determined from the ratio of the IC50 value obtained from normal cells and IC50 value for cancer cells. Selectivity indexes of ligand (1) and complex (2) were calculated as >1, > 2.24, and >4.67; 4.44, 4.63 and 3.77 for 24 h, 48 and 72 h, respectively. These results indicated that complex (2) has shown good selectivity (more than 4-fold) between SH-SY5Y neuroblastoma cells and normal cells for 24 h and 48 h incubation time.

Keywords

• SH-SY5Y
• MTT
• Antiproliferative activity
• N-heterocyclic carben
• Silver

KLORO[1-(2-METİL-2-PROPENİL)-3-(2-KLOROBENZİL) BENZİMİDAZOL-2-İLİDEN] Ag(I) BİLEŞİĞİNİN SH-SY5Y NÖROBLASTOM HÜCRELERİNDEKİ ANTİPROLİFERATİF AKTİVİTESİNİN ARAŞTIRILMASI

Abstract

Bu çalışmada klor içeren benzimidazol-temelli N-heterosiklik karben (NHC) ligandı (1) ve ligandın gümüş-(I) kompleksinin (2) antiproliferatif aktiviteleri araştırılmıştır. Hem ligand (1) hem de kompleksin (2), SH-SY5Y nöroblastom hücrelerine ve WI-38 insan sağlıklı fibroblast hücrelerindeki antiproliferatif aktiviteleri 24 saat, 48 saat ve 72 saat boyunca (3-[4,5-Dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide; Thiazolyl blue (MTT) ölçümü kullanılarak test edilmiştir. Deney sonuçlarına göre ligand (1), tüm zaman noktalarında WI-38 sağlıklı hücrelerde antiproliferatif aktivite göstermemiş ancak SH-SY5Y nöroblastom hücrelerinde konsantrasyona ve zamana bağlı antiproliferatif aktivite göstermiştir. Sonuçlarımız, kompleksin (2), hem SH-SY5Y nöroblastom hücrelerine hem de WI-38 sağlıklı hücrelerine karşı doza ve zamana bağlı bir antiproliferatif aktiviteye sahip olduğunu göstermiştir. Ayrıca kompleksin (2), SH-SY5Y nöroblastom hücreleri ve WI-38 normal hücrelerinde liganda (1) göre daha yüksek antiproliferatif aktiviteye sahip olduğu bulunmuştur. Kompleks (2), SH-SY5Y nöroblastom hücreleri için 24 ve 48 saat zaman noktalarında 4 kattan fazla seçicilik göstermiştir.

Keywords

• SH-SY5Y
• MTT
• Antiproliferatif aktivite
• N-heterosiklik karben
• Gümüş

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