دورية أكاديمية
Bioactivity Studies of β-Lactam Derived Polycyclic Fused Pyrroli-Dine/Pyrrolizidine Derivatives in Dentistry: In Vitro, In Vivo and In Silico Studies.
| العنوان: | Bioactivity Studies of β-Lactam Derived Polycyclic Fused Pyrroli-Dine/Pyrrolizidine Derivatives in Dentistry: In Vitro, In Vivo and In Silico Studies. |
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| المؤلفون: | Gowri Meiyazhagan, Rajesh Raju, Sofi Beaula Winfred, Bhavani Mannivanan, Hemadev Bhoopalan, Venkatesh Shankar, Sathiya Sekar, Deepa Parvathi Venkatachalam, Ravishankar Pitani, Venkateshbabu Nagendrababu, Malini Thaiman, Kandaswamy Devivanayagam, Jeyakanthan Jayaraman, Raghunathan Ragavachary, Ganesh Venkatraman |
| المصدر: | PLoS ONE, Vol 10, Iss 7, p e0131433 (2015) |
| بيانات النشر: | Public Library of Science (PLoS), 2015. |
| سنة النشر: | 2015 |
| المجموعة: | LCC:Medicine LCC:Science |
| مصطلحات موضوعية: | Medicine, Science |
| الوصف: | The antibacterial activity of β-lactam derived polycyclic fused pyrrolidine/pyrrolizidine derivatives synthesized by 1, 3-dipolar cycloaddition reaction was evaluated against microbes involved in dental infection. Fifteen compounds were screened; among them compound 3 showed efficient antibacterial activity in an ex vivo dentinal tubule model and in vivo mice infectious model. In silico docking studies showed greater affinity to penicillin binding protein. Cell damage was observed under Scanning Electron Microscopy (SEM) which was further proved by Confocal Laser Scanning Microscope (CLSM) and quantified using Flow Cytometry by PI up-take. Compound 3 treated E. faecalis showed ROS generation and loss of membrane integrity was quantified by flow cytometry. Compound 3 was also found to be active against resistant E. faecalis strains isolated from failed root canal treatment cases. Further, compound 3 was found to be hemocompatible, not cytotoxic to normal mammalian NIH 3T3 cells and non mutagenic. It was concluded that β-lactam compound 3 exhibited promising antibacterial activity against E. faecalis involved in root canal infections and the mechanism of action was deciphered. The results of this research can be further implicated in the development of potent antibacterial medicaments with applications in dentistry. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1932-6203 |
| العلاقة: | https://doaj.org/toc/1932-6203Test |
| DOI: | 10.1371/journal.pone.0131433 |
| الوصول الحر: | https://doaj.org/article/255c4a7d665d4571a544843372958a88Test |
| رقم الانضمام: | edsdoj.255c4a7d665d4571a544843372958a88 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 19326203 |
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| DOI: | 10.1371/journal.pone.0131433 |