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Norsquaraine endowed with anticancer and antibacterial activities
Institution:1. Department of Biotechnology and Molecular Biology & ASUBTAM M. Bilmez BioNanoTech Lab., Aksaray University, TR-68100, Aksaray, Turkey;2. Department of Chemistry & ASUBTAM M. Bilmez BioNanoTech Lab., Aksaray University, TR-68100, Aksaray, Turkey;3. Health Vocational School & ASUBTAM M. Bilmez BioNanoTech Lab., Aksaray University, TR-68100 Aksaray, Turkey;1. Department of Chemistry, KG Reddy College of Engineering and Technology, Moinabad, Hyderabad, Telangana 500075, India;2. School of Mechanical Engineering, Beijing Institute of Technology, Beijing 100081, China;3. Department of Chemistry, College of Engineering Guindy, Anna University, Chennai, Tamil Nadu 600 0025, India;4. Department of Physics, St. Joseph''s College of Engineering, Chennai, Tamil Nadu, India;5. Department of Chemistry, C. Kandaswami Naidu College for Women, Cuddalore, Tamilnadu, India;6. Department of Biotechnology, Saveetha School of Engineering, SIMATS, Thandalam, Chennai, Tamilnadu 602105, India;1. São Paulo State University (Unesp), School of Pharmaceutical Sciences, 14800-903, Araraquara, SP, Brazil;2. Federal University of São Carlos, Department of Chemistry, 13565-905, São Carlos, SP, Brazil;3. São Paulo State University (Unesp), Institute of Chemistry, 14800-060, Araraquara, SP, Brazil;4. São Paulo State University (Unesp), School of Dentistry, 14801-903, Araraquara, SP, Brazil;1. Graduate School of Engineering, Osaka University, 2-1, Yamadaoka, Suita, Osaka, 565-0871, Japan;2. Graduate School of Medicine, Osaka Metropolitan University, 1-4-3, Asahimachi, Abeno-ku, Osaka, 545-8585, Japan;3. Global Center for Medical Engineering and Informatics, Osaka University, 2-2, Yamadaoka, Suita, Osaka, 565-0871, Japan;1. Faculty of Health Sciences, Izmir Katip Çelebi University, Izmir Kâtip Çelebi Üniversitesi Balatçık Kampüsü, Çiğli, İzmir 35620, Turkey;2. Faculty of Pharmacy, Department of Pharmaceutical Microbiology, Ege University, Turkey;3. Faculty of Engineering, Department of Biomedical Engineering, İzmir Katip Çelebi University, Turkey;4. Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ege University, Turkey;6. Faculty of Medicine, Department of Microbiology, İzmir Katip Çelebi University, Turkey;1. Department of Endodontics, Faculty of Dentistry, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran;2. Iranian Center for Endodontic Research, Research Institute of Dental Sciences, Dental School, Shahid Beheshti University of Medical Sciences, Tehran, Iran;3. Dental Research Center, Dentistry Research Institute, Tehran University of Medical Sciences, Tehran, Iran
Abstract:BackgroundPhotodynamic therapy (PDT) is a method for the treatment of cancer. Furthermore, PDT can also be used for the eradication of bacteria. The photo-sensitizing drug, a.k.a photosensitizer, is critical for the success of PDT. Although norsquaraines are analogs of squaraine dyes, they are overlooked as photosensitizers.MethodsIn this work, synthesis, characterization, bioimaging and in vitro PDT applications of a new norsquaraine dye 1 were described. We also prepared nanoparticles from norsquaraine 1 and Pluronic F127 to obtain 1@F127.ResultsNorsquaraine 1 boosted the generation of reactive oxygen species over a wide range of pH (pH 8.0, 7.0, 6.0, and 2.2.). Furthermore, 1 was internalized by epidermoid laryngeal carcinoma Hep-2 (Hep-2) cells and used for fluorescence imaging. Remarkably, norsquaraine 1 destroyed most of the cancer cells (ca. 77% to 89%) after illumination with red light. Most strikingly, 1 successfully inhibited the growth of Methicillin-resistant Staphylococcus aureus (MRSA) upon illumination. Last but not least, photodynamic sterilization of tomato juice, an acidic beverage, was feasible using 1 as a photo sterilizer. Nano formulation of 1 with Pluronic F127 provided 1@F127 nanoparticles. It is lucid that 1@F127 nanoparticles permeate into Hep-2 cells and boost the generation of ROS upon illumination.ConclusionNorsquaraine 1 shows superior features as a photosensitizer pertinent to PDT in a wide range of pH. This norsquaraine is endowed with anticancer and antibacterial activities. Which should be further evaluated.
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