Rifampisin Dirençli Mycobacterium tuberculosis Kompleks Suşları Üzerine Benzimidazolyum Tuzlarının Antimikobakteriyel Etkinliğinin Araştırılması

Yaren İnci; Suna Kızılyıldırım; Fatih Köksal; Muhammed Tılahun Muhammed; Senem Akkoç

doi:10.18016/ksutarimdoga.vi.1278595

EN TR

Investigation of the Antimicobacterial Activity of Benzimidazolium Salts on Rifampicin Resistant Mycobacterium tuberculosis Complex Strains

Abstract

In this study, it was aimed to determine the antimycobacterial activity of 3 different compounds ((S1): 1-(N-methylphthalimide)-3-benzylbenzimidazolium bromide, (S2): 1-(N-methylphthalimide)-3-(4-methylbenzyl) benzimidazolium bromide, (S3): 1-(N-methylphthalimide)-3-(naphthalen-1-ylmethyl) benzimidazolium bromide) containing benzimidazole nuclei on M. tuberculosis reference strain H37Rv and rifampicin resistant tuberculosis strains isolated from clinical samples sent to the Ministry of Health Adana Regional Tuberculosis Laboratory. Using the BACTEC MGIT 960 system, the antimycobacterial activity of benzimidazole derivative compounds were examined in vitro against M. tuberculosis H37Rv and 35 clinical strains of M. tuberculosis that were resistant to rifampicin. Furthermore, molecular docking was used to look into the possible interactions of the antimycobacterial compounds. According to the results of the study, compound S2 showed antimycobacterial activity against the M. tuberculosis H37Rv strain but it didn’t have any effect on rifampicin-resistant M. tuberculosis strains. Compounds S1 and S3 didn’t exhibit any antimycobacterial activity against both clinical and reference strains. The results of the molecular docking analysis revealed that S2 could bind to InhA and thus could exert its antimycobacterial activity by inhibiting it. As a result, the S2 compound can be suggested as a new agent for the treatment of tuberculosis, however, more comprehensive studies are needed.

Keywords

Rifampisin Dirençli Mycobacterium tuberculosis Kompleks Suşları Üzerine Benzimidazolyum Tuzlarının Antimikobakteriyel Etkinliğinin Araştırılması

Öz

Çalışmada, Sağlık Bakanlığı Adana Bölge Tüberküloz Laboratuvarı’na gönderilen klinik örneklerden izole edilen rifampisin dirençli tüberküloz suşları ile referans suş M. tuberculosis H37Rv üzerine benzimidazol çekirdeği içeren 3 farklı bileşiğin ((S1): 1-(N-metilftalimid)-3-benzilbenzimidazolyum bromür, (S2): 1-(N-metilftalimid)-3-(4-metilbenzil) benzimidazolyum bromür, (S3): 1-(N-metilftalimid)-3-(naftalen-1-ilmetil) benzimidazolyum bromür) antimikobakteriyel aktivitesinin tespiti amaçlandı. Benzimidazol türevi bileşiklerinin rifampisin dirençli 35 klinik M. tuberculosis ve H37Rv suşlarında antimikobakteriyel aktiviteleri in vitro şartlarda BACTEC MGIT 960 sistemi kullanılarak test edildi. Ayrıca, antimikobakteriyel etkili bileşiklerin olası etkileşimleri moleküler doking ile incelendi. Çalışma sonucunda sadece S2 bileşiğinin yalnız M. tuberculosis H37Rv suşuna karşı antimikobakteriyel aktivite gösterdiği, rifampisin dirençli M. tuberculosis suşlarına karşı aktivitesinin olmadığı belirlendi. S1 ve S3 bileşiklerinin ise hem klinik hem de referans suşa karşı antimikobakteriyel aktivitesi tespit edilemedi. Moleküler doking sonuçları S2’nin InhA ile bağlandığını ve onu inhibe ederek antimikobakteriyel etkisini gösterebileceği ortaya çıkardı. Sonuç olarak S2 bileşiğinin tüberküloz tedavisinde yeni ajan olarak sunulabilir ancak daha kapsamlı çalışmaların yapılmasına da ihtiyaç duyulmaktadır.

Anahtar Kelimeler

Supporting Institution

Çukurova Üniversitesi

Project Number

TYL-2021-14313

Thanks

Çukurova Üniversitesi’ne çalışmayı destekledikleri için teşekkür ederiz.

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Details

Primary Language

Turkish

Subjects

Structural Biology

Journal Section

Research Article

Authors

Yaren İnci
0000-0003-2159-9123
Türkiye

Suna Kızılyıldırım ^*
0000-0002-1039-8556
Türkiye

Fatih Köksal
0000-0003-0790-1525
Türkiye

Muhammed Tılahun Muhammed
0000-0003-0050-5271
Türkiye

Senem Akkoç
0000-0002-1260-9425
Türkiye

Early Pub Date

October 13, 2023

Publication Date

February 28, 2024

Submission Date

April 8, 2023

Acceptance Date

August 25, 2023

Published in Issue

Year 2024 Volume: 27 Number: 1

DOI

https://doi.org/10.18016/ksutarimdoga.vi.1278595

IZ

https://izlik.org/JA27BN85ZS

Cite

RIS / Bibtex

APA

İnci, Y., Kızılyıldırım, S., Köksal, F., Muhammed, M. T., & Akkoç, S. (2024). Rifampisin Dirençli Mycobacterium tuberculosis Kompleks Suşları Üzerine Benzimidazolyum Tuzlarının Antimikobakteriyel Etkinliğinin Araştırılması. Kahramanmaraş Sütçü İmam Üniversitesi Tarım Ve Doğa Dergisi, 27(1), 114-119. https://doi.org/10.18016/ksutarimdoga.vi.1278595

Cited By

Experimental and theoretical studies on antituberculosis activity of different benzimidazole derivatives

Heliyon

https://doi.org/10.1016/j.heliyon.2025.e42674