Synthesis, Cytotoxicity Evaluation, and Antifungal Activity of Novel Nitroglycerin Derivatives against Clinical Candida albi-cans Isolates

Background: Candida albicans remains the main cause of candidiasis in most clinical settings. Available drugs for candidiasis treatment have many side effects. In this work, novel nitroglycerin derivatives were synthesized and their cytotoxic and antifungal effects evaluated against fluconazole susceptible and resistant clinical C. albicans isolates. Methods: This experimental study was performed in Tehran University of Medical Sciences and Baqiatallah University of Medical Sciences, Tehran, Iran between Feb to Dec 2019. The in vitro activities of two novel nitroglycerin derivatives (1b and 2b) against 25 clinical fluconazole-susceptible and resistant C. albicans isolates and four standard C. albicans strains were determined according to CLSI reference M27-A3 documents. The cytotoxicity of chemical compounds was investigated near the SNL76/7 cells by colorimetric assay. Real-time PCRs were performed to evaluate the alterations in the regulation of ERG11 and CDR1 genes under nitroglycerin derivatives-treated and untreated conditions. Results: The derivatives 1b and 2b exhibited potent antifungal activity against C. albicans isolates; MICs and MFCs varied from 18 μg/ml to 72 μg/ml and 36 μg/ml to 144 μg/ml, respectively. The cell viability evaluation demonstrated that both chemical compounds are safe within 24h. The nitroglycerin derivatives were able to reduce the transcription level of CDR1 and ERG11 genes in all susceptible and resistant C. albicans isolates. Conclusion: Considering the potential and efficacy of these compounds against clinical C. albicans isolates, the complementary in vivo and clinical trials should be investigated.

Effects of Cinnamon (Cinnamomum spp.) in Dentistry: A Review

Dental medicine is one of the fields of medicine where the most common pathologies are of bacterial and fungal origins. This review is mainly focused on the antimicrobial effects of cinnamon essential oil (EO), cinnamon extracts, and pure compounds against different oral pathogens and the oral biofilm and the possible effects on soft mouth tissue. Basic information is provided about cinnamon, as is a review of its antimicrobial properties against the most common microorganisms causing dental caries, endodontic and periodontal lesions, and candidiasis. Cinnamon EO, cinnamon extracts, and pure compounds show significant antimicrobial activities against oral pathogens and could be beneficial in caries and periodontal disease prevention, endodontics, and candidiasis treatment.

Catechol-Bearing Hyaluronic Acid Coated Polyvinyl Pyrrolidone/Hydroxyl Propyl-β-Cyclodextrin/Clotrimazole Nanofibers for Oral Candidiasis Treatment

This research aimed to develop clotrimazole (CT)-loaded mucoadhesive nanofiber patches for oral candidiasis. The three-layered sandwich-like nanofiber patches were prepared by electrospinning technique. The spinning solution for the middle layer composed of 8 %wt polyvinylpyrrolidone (PVP), 90 mM hydroxy propyl-β-cyclodextrin (HPβCD) and 10 % (wt to polymer) of CT in a solvent mixture of ethanol:water:benzyl alcohol. The outer layers were fabricated from a mixture of 1 %wt hyaluronic acid (HA) or catechol bearing hyaluronic acid (HA-cat) and 10 %wt polyvinyl alcohol (PVA) at varied weight ratios. The thickness of the outer layers was varied by adjusting the volume of coating polymer solution ranging from 1 to 3 mL. Desirable smooth nanosized fibers were obtained from the electrospinning process. Increasing the thickness of the outer layer brought about a significant increase in the fiber strength and flexibility. The viscosity of HA-cat/mucin mixture showed good polymer-mucin interaction indicating higher mucoadhesive property of the nanofibers. The drug loading capacity (LC) displayed the potential of the nanofibers for drug encapsulation. The highest LC value of 123.80 ± 5.61 μg/mg was obtained from the nanofibers coated with 1 mL of the coating solution. CT was rapidly released from the nanofiber in the first hour followed by a steady release. The released amount reach above 80% in 2 h. The nanofibers provided superior antifungal activity against Candida albicans compared to CT powder. Moreover, they were found to be nontoxic to the human gingival fibroblast cells. Thus, the sandwich nanofibers may be further developed to be a potential candidate for oral candidiasis treatment in the near future.