Investigation of the cytotoxic and antimicrobial properties of new quinoline peptide conjugates

Öz

Background: Cancer is one of the most important health problems causing deaths in Turkey and the world. Nowadays, many treatment methods such as radiotherapy and chemotherapy are applied in cancer patients. Quinoline and its derivatives, which belong to heterocyclic compounds, have many biological activities for drug development. Quinoline compounds play a crucial role in the development of antitumor drugs due to their anticancer activity. Materials and Methods: In this study, the cytotoxic effects of synthesized seven different quinoline derivatives on lung cancer (A549) and healthy lung epithelial cell (BEAS2B), liver cancer (Hep 3B), and endothelial cell (HUVEC) were determined. Different concentrations were applied and IC50 values were calculated at different time courses. The antimicrobial activites of the compounds were also determined. Results: The IC50 values of compound 2 on the A549 cell line were determined to be 10.48 μg/mL, 9.738 μg/mL, and 10.14 μg/mL. IC50 values of compound 6 on the same cell line were determined to be 7.307 µg/mL, 9.888 µg/mL, 10.63 µg/mL. Conclusions: Compounds 2 and 6 had a cytotoxic effect on the BEAS2B cell line. The antimicrobial activity of the compounds was determined by the minimum inhibition concentration method on different strains of bacteria and yeast. The compounds showed no antimicrobial activity on bacteria and yeast.

Anahtar Kelimeler

• Antimicrobial
• Quinoline-peptide conjugates
• Cytotoxic

Proje Numarası

2623

Teşekkür

We would like to thank Inonu University Scientific Research Projects Unit for supporting this study as project number 2021/2623.

Yeni kinolin peptit konjugatlarının sitotoksik ve antimikrobiyal özelliklerinin araştırılması

Öz

Amaç: Kanser, Türkiye’de ve dünyada ölüme neden olan önemli sağlık sorunlarından biridir. Günümüzde radyoterapi ve kemoterapi gibi birçok tedavi yöntemi kanser hastalarında uygulanmaktadır. Heterosiklik bileşikler arasında olan kinolin ve türevleri ilaçların geliştirilmesi açısından birçok biyolojik aktivite bulundurmaktadır. Kinolin bileşikleri, antikanser aktivite gösterdikleri için antikanser ilaç gelişiminde önemli bir rolü vardır. Materyal ve Metot: Bu çalışmada, sentezlenmiş yedi farklı kinolin türevinin akciğer kanseri (A549) ve sağlıklı akciğer epitel (BEAS2B), karaciğer kanseri (Hep 3B) ve endotelial hücreler (HUVEC) üzerine sitotoksik etkileri belirlenmiştir. Farklı konsantrasyonlar uygulanmış ve farklı zaman aralıklarında IC50 değerleri hesaplanmıştır. Aynı zamanda bileşiklerin antimikrobiyal aktiviteleri de belirlenmiştir. Bulgular: A549 hücre hattı üzerine bileşik 2’nin IC50 değerleri 10.48 μg/mL, 9.738 μg/mL, 10.14 μg/mL olarak tespit edilmiştir. Bileşik 6’nın aynı hücre hattı üzerine IC50 değerleri 7.307 μg/mL, 9.888 μg/mL, 10.63 μg/mL olarak belirlenmiştir. Sonuç: Bileşik 2 ve 6’nın BEAS2B hücre hattı üzerine sitotoksik etkisi görülmüştür. Bileşiklerin antimikrobiyal etkileri çeşitli bakteri ve maya suşları üzerine minimum inhibisyon konsantrasyonu yöntemi ile belirlenmiştir. Bileşikler bakteriler ve maya üzerine antimikrobiyal etki göstermemiştir.

Anahtar Kelimeler

• Antimikrobiyal
• Kinolin- Peptidkonjugatı
• Sitotoksisite.

Destekleyen Kurum

İnönü Üniversitesi

Proje Numarası

2623

Teşekkür

Bu çalışmayı 2021/2623 proje numarasıyla destekleyen İnönü Üniversitesi Bilimsel Araştırma Projeleri Birimine teşekkür ederiz.

Kaynakça

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