Anticancer, Apoptotic and Antibacterial, Effects of Thiosemicarbazid and bis-1,2,4-Triazole Derivatives

Abstract

In this study in vitro anticancer and apoptotic activities on the prostate cell line (PC-3) and antibacterial effects on some gram positive and gram negative bacteria of pyridine-2,5-dicarbohydrazine and synthesized thiosemicarbazide derivatives [2,2′ -(pyridine-2,5-diyldicarbonyl)-bis(N-ethylhydrazinecarbothioamide) (3B)and [2,2′-(pyridine-2,5-diyldicarbonyl)-bis[N-(p-methoxyphenyl)hydrazinecarbothioamide] (3C)] and bis-1,2,4- triazole-3-thiol derivatives [5,5′-pyridine-2,5-diylbis(4-ethyl-4H-1,2,4-triazole3-thiol) (4B) and 5,5′-pyridine-2,5- diylbis(4-(4-methoxy-phenyl)-4H1,2,4-triazole-3-thiol) (4C)] were determined. According to the results of cytotoxic studies cell numbers decreased by the concentration increase of all compounds. The maximum cytotoxic effects were found on 500 μM concentration. As a result of apoptotic activity it is found out that all of the compounds triggered the apoptosis and the lowest index was on 4B and the highest index was on 3C compounds. Antibacterial tests showed that all compounds used in this study were more effective on gram positive bacteria then gram negative bacteria. 

Keywords

• PC-3
• thiosemicarbazid
• triazole
• anticancer
• apoptotic effects
• antibacterial effects

Project Number

BAP-712-297-2015

Tiyosemikarbazit ve bis-1,2,4-triazol Türevlerinin Antikanser, Apoptotik ve Antibakteriyal Etkileri

Abstract

Bu çalışmada, çıkış maddesi [piridin-2,5-dikarbohidrazin (2)] ile tiyosemikarbazit türevleri [2,2’-(piridin-2,5-diildikarbonil-bis(N-etilhidrazinkarbotiyoamit) (3B) ve 2,2’-(piridin-2,5-diildikarbonil)-bis(N-(p-metoksifenil)hidrazinkarbotiyoamit (3C)] ve bu bileşiklerin halkalaşmasında oluşan bis-1,2,4-triazol türevlerinin [5,5-piridin-2,5-diilbis(4-etil-4H-1,2,4-triazol-3-tiyol) (4B) ve 5,5’-piridin-2,5diilbis[4-(4-metoksifenil)-4H-1,2,4-triazol-3-tiyol)] (4C)] in vitro ortamda prostat kanser hücre hattı (PC-3) üzerindeki antikanser ve apoptotik etkileri ile bazı gram pozitif ve gram negatif bakteriler üzerindeki antibakteriyel etkileri belirlenmiştir. Antikanser etki sonuçlarına göre tüm maddelerin artan konsantrasyonlara bağlı olarak canlı kanser hücre sayısında azalma tespit edilmiştir. Tüm uygulanan maddelerde en yüksek sitotoksik etkinin 500 μM konsantrasyonda olduğu belirlenmiştir. Tüm maddelerin apoptozu tetiklediği belirlenmiş olup apoptotik indeks oranlarına bakıldığında en düşük apoptotik indeks oranı 4B maddesi uygulandığında, en yüksek apoptotik indeks oranı ise 3C maddesi uygulandığında tespit edilmiştir. Antibakteriyel çalışmada tüm bileşiklerin gram pozitif bakteriler üzerinde gram negatiflere nazaran daha fazla etkili olduğu görülmüştür.

Keywords

• PC-3
• Tiyosemikarbazit
• Triazol
• Antikanser
• Apoptotik etki

Supporting Institution

Bingöl Üniversitesi BÜBAP

Project Number

BAP-712-297-2015

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