Determining antifungal, anti-biofilm and anticancer activities of “1,3-di(thiophen-2-yl) prop-2- en-1-one” chalcone derivative

Uğur Tutar; Cem Çelik; Hayreddin Gezegen; Ceylan Hepokur

doi:10.7197/223.v39i29491.316366

TR EN

“1,3-di(thiophen-2-yl) prop-2-en-1-one” kalkon türevinin antifungal, anti-biyofilm ve anti-kanser aktivitelerinin belirlenmesi

Öz

Amaç: Çalışmamızın amacı, literatürde rapor edilen beş kalkon bileşiğinin Candida albicans ve Candida tropicalis’e karşı potansiyel antifungal ve antibiyofilm aktivitelerinin belirlenmesidir. Ayrıca antimikrobiyal aktivitesi belirlenen “1,3-di(thiophen-2-yl)prop-2-en-1-one” kalkon bileşiğinin antioksidan ve insan meme kanseri (MCF-7) ve kemik kanseri (MG63) hücre hatları üzerindeki etkilerinin belirlenmesi amaçlanmıştır.

Yöntem: Çalışmada kullanılan kalkonlar dimeti sülfoksit (DMSO) içinde iki kat seyreltilmiş ve 1000-15 μg/mL konsantrasyonda hazırlanmıştır. Kalkonların antifungal ve anti-biyofilm aktiviteleri mikrodilüsyon yöntemi kullanılarak belirlenmiştir. Radikal süpürücü etkisi 2, 2-diphenyl-1-picrylhydrazyl (DPPH) ile test edilmiştir. Hücre canlılığı , kültür ortamına ilave edilen tetrazolium tuzları ile değerlendirilmiştir.

Bulgular: Çalışmamızda antimikrobiyal aktivite gösteren “1,3-di (tiyofen-2-il) prop-2-en-1-on” C. albicans ve C. tropicalis üzerinde MIC değerleri 0.06 mg/mL bulunmuştur. MBC değerleri ise sırasıyla 0.12 mg/mL ve 0.5 mg/mL olarak saptanmıştır. MBIC aktiviteleri ise sırasıyla 0.06 ve 0.25 mg/mL olarak bulunmuştur. MBEC değerleri her iki mikroorganizma için 1 mg/mL bulunmuştur. C. albicans ve C. tropicalis’ in 48 saatlik biyofilm yapılarına MIC değeri uygulandığında yapının sırasıyla 83% ve 81% oranında azaldığı saptanmıştır. “1,3-di(thiophen-2-yl) prop-2-en-1-one” IC50 değeri 13,52 µg/L olarak bulundu. MCF-7 ve MG63 hücre hatlarında 5 µg/mL konsantrasyonda 24 saat inkübasyon sonrasında sırasıyla hücrelerin % 30’u ve % 65’ i canlı kalmıştır.

Sonuç: Elde edilen sonuçlara göre tiyofen halkası içeren kalkon bileşiği C. albicans ve C. tropicalis suşları üzerinde hem üremelerini inhibe edici etki göstermiş hem de gerek biyofilm oluşumunda gerekse oluşan biofilm üzerinde etkili olduğu görülmüştür. Çalışmanın sonuçları tiyofen halkası içeren kalkon bileşiğinin potansiyel antimikrobiyal, antibiyofilm ve antikanser ajan olarak değerli olabileceğini ortaya koymuştur.

Anahtar Kelimeler

Determining antifungal, anti-biofilm and anticancer activities of “1,3-di(thiophen-2-yl) prop-2- en-1-one” chalcone derivative

Abstract

Objective: Our study aims to determine antifungal and anti-biofilm activity potential of five chalcone derivatives, which have been already reported in the literature, against Candida albicans and Candida tropicalis. In addition, it aimed to determine antioxidant property and anti-cancer activity of 1,3-di(thiophen-2-yl)prop-2-en-1-one chalcone derivative, whose antimicrobial activity was revealed within the study, in human breast cancer cell line (MCF-7) and human bone cancer cell line (MG63).

Method: Chalcones used in the study were diluted two times in dimethyl sulfoxide (DMSO) and prepared at concentration between 1000-15 µg/mL. Antifungal and anti-biofilm activity of chalcones determined by using microdilution method. Radical scavenging activity was tested by employing 2, 2-diphenyl-1-picrylhydrazyl (DPPH). The cell viability was assessed using the cleavage of tetrazolium salts added to the culture medium.

Results: In our study, MIC values of “1,3-di(thiophen-2-yl) prop-2-en-1-one”, which showed its antimicrobial activity on C. albicans and C. tropicalis, were found to be 0.06 mg/mL for both organisms, whereas its MBC values were found to be 0.12 mg/mL and 0.50 mg/mL respectively. MBIC activities were found to be 0.06 and 0.25 mg/mL respectively, whereas MBEC values were found to be 1 mg/mL. When MIC was applied to 48-hours biofilm formation, it was observed that the formation has decreased by 83% and 81%. IC50 value of “1,3-di(thiophen-2-yl) prop-2-en-1-one” was found to be 13,52 µg / mL. Regarding MCF-7 and MG63 cell line at 5 µg / mL concentration, 30% and 65% preserve its viability after 24 hours of incubation respectively.

Conclusions: According to these results, it can be said that chalcone compound that include thiophen ring has shown an inhibiting effect on the multiplication and both on the formation of the biofilm of C. albicans and C. tropicalis strains. The results of the study revealed that chalcone compound may be valuable as an antifungal, anti-biofilm and anti-cancer agent.

Keywords

Kaynakça

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Ayrıntılar

Birincil Dil

İngilizce

Konular

Sağlık Kurumları Yönetimi

Bölüm

Araştırma Makalesi

Yazarlar

Yayımlanma Tarihi

17 Mayıs 2017

Gönderilme Tarihi

6 Aralık 2016

Kabul Tarihi

21 Mart 2017

Yayımlandığı Sayı

Yıl 2017 Cilt: 39 Sayı: 2

DOI

https://doi.org/10.7197/223.v39i29491.316366

IZ

https://izlik.org/JA68KW85AY

Kaynak Göster

RIS / Bibtex

AMA

1.Tutar U, Çelik C, Gezegen H, Hepokur C. Determining antifungal, anti-biofilm and anticancer activities of “1,3-di(thiophen-2-yl) prop-2- en-1-one” chalcone derivative. CMJ. 2017;39(2):466-472. doi:10.7197/223.v39i29491.316366