A novel tetraphenylethylene (TPE) functionalized aminoglycoside antibiotic kanamycin (TPE-kana 1) has been successfully synthesized and characterized by means of modern analytical and spectroscopic techniques. The probe TPE-kana 1 showed strong affinity towards bovine serum albumin (BSA) compared to its other biological competitors. The recognition of BSA have been investigated employing UV-Vis absorption and fluorescence emission spectroscopy. The significant color change of TPE-kana 1 with BSA can be observed by necked eye, where the role of AIE-active TPE molecule is handle in both optical and colorimetric changes. The quenching of fluorescence of TPE-kana 1 with BSA was characterized by fluorescence spectroscopy, with 71.16% of quenching efficiency. Moreover, the Stern-Volmer quenching constant was calculated and found to be 2.46 × 10 M. Probe TPE-kana 1 showed detection limit of 2.87 nM (nM) towards BSA with binding constant 7.56 × 10 M. A molecular docking study is also performed to investigate the detail interactions between TPE-kana 1 with the sites of BSA via non-covalent i.e., H-bonding, π-cation interactions, π-donor hydrogen bonds and π-π interactions. The lowest binding energy conformation was found at - 10.42 kcal/mol.
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http://dx.doi.org/10.1038/s41598-022-15890-4 | DOI Listing |
Eur J Trauma Emerg Surg
January 2025
Dr C Lal Hospital, Ambala Cantt, Haryana, 133001, India.
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View Article and Find Full Text PDFBrucellosis, caused by a facultative intracellular gram-negative coccobacillus, is one of the most common zoonotic infections worldwide. Very rarely, brucellosis can cause periprosthetic joint infections (PJI). In this case-based literature review, we summarize the current medical literature regarding Brucella PJI, with the aim to raise awareness among clinicians, particularly in non-endemic areas.
View Article and Find Full Text PDFTechnol Cancer Res Treat
January 2025
Cell Therapy Center, The University of Jordan, Amman, Jordan.
Background: Doxorubicin (DOX) is a potent chemotherapeutic agent for breast cancer, but its effectiveness is often diminished by resistance mechanisms, particularly through p-glycoprotein (P-gp) mediated drug efflux. Clarithromycin (CAM), a macrolide antibiotic, inhibits multiple metabolic pathways including CYP3A and P-gp, potentially countering DOX resistance.
Objective: This study aimed to evaluate the potentiation of DOX and its effectiveness against the MCF-7 breast cancer cell line by encapsulating both DOX and CAM in PEGylated liposomes.
J Comput Chem
January 2025
Regional Center of Advanced Technologies and Materials, Czech Advanced Technology and Research Institute (CATRIN), Palacký University Olomouc, Olomouc, Czech Republic.
Doxorubicin (DOX) is a widely used chemotherapeutic agent known for intercalating into DNA. However, the exact modes of DOX interactions with various DNA structures remain unclear. Using molecular dynamics (MD) simulations, we explored DOX interactions with DNA duplexes (dsDNA), G-quadruplex, and nucleosome.
View Article and Find Full Text PDFPharmacol Res Perspect
February 2025
Department of Pharmaceutical Health Care and Sciences, Tokyo University of Pharmacy and Life Sciences, Tokyo, Japan.
Doxorubicin (DOXO) has long been used clinically and remains a key drug in cancer therapy. DOXO-induced cardiomyopathy (DICM) is a chronic and fatal complication that severely limits the use of DOXO. However, there are very few therapeutic agents for DICM, and there is an urgent need to identify those that can be used for a larger number of patients.
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