Synthesis and Biological Evaluation of Novel Cinnamic Acid-Based Antimicrobials

Mingoia, Marina; Conte, Carmela; Rienzo, Annalisa Di; Dimmito, Marilisa Pia; Marinucci, Lorella; Türkez, Hasan; Cufaro, Maria Concetta; Boccio, Piero Del; Stefano, Antonio Di; Cacciatore, Ivana

doi:10.3390/ph15020228

Cited by 22 publications

(17 citation statements)

References 41 publications

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“…The most isolated organisms in surgical site infections are S. aureus, coagulase-negative staphylococci, Enterococcus spp., and Escherichia coli. An increasing number of SSIs are attributable to antibiotic-resistant pathogens, such as methicillin-resistant S. aureus (MRSA) or Candida albicans [ 67 , 68 , 69 ]. To address these challenges, extensive antibacterial and in vivo studies are required to understand the impact of antibiotic-drug–NP-coated sutures during the treatment of SSIs, which are currently ongoing in our laboratories.…”

Section: Discussionmentioning

confidence: 99%

Development of Biocompatible Ciprofloxacin–Gold Nanoparticle Coated Sutures for Surgical Site Infections

et al. 2022

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Surgical site infections (SSIs) are mainly observed after surgeries that use biomaterials. The aim of this present work was to develop ciprofloxacin hydrochloride (CPH)-loaded gold nanoparticles. These ciprofloxacin–gold nanoparticles were coated onto a sterile surgical suture using an adsorption technique, followed by rigidization via ionotropic crosslinking using sodium alginate. Furthermore, UV-visible spectroscopy, infrared spectroscopy, and scanning electron microscopy were used to characterize the samples. The particle size of the nanoparticles was 126.2 ± 13.35 nm with a polydispersity index of 0.134 ± 0.03, indicating nanosize formation with a monodispersed system. As per the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) guidelines, stability studies were performed for 30 days under the following conditions: 2–8 °C, 25 ± 2 °C/60 ± 5% RH, and 40 ± 2 °C/75 ± 5% RH. For both Gram-negative and Gram-positive bacteria, the drug-coupled nanoparticle-laden sutures showed a twofold higher zone of inhibition compared with plain drug-coated sutures. In vitro drug release studies showed a prolonged release of up to 180 h. Hemolysis and histopathology studies displayed these sutures’ acceptable biocompatibility with the healing of tissue in Albino Swiss mice. The results depict that the use of antibiotic-coated sutures for preventing surgical site infection for a long duration could be a viable clinical option.

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Section: Discussionmentioning

confidence: 99%

Development of Biocompatible Ciprofloxacin–Gold Nanoparticle Coated Sutures for Surgical Site Infections

et al. 2022

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“…This effect of Madhugrit might be due to the presence of a plethora of phytochemicals namely ellagic acid, coumarin, cinnamic acid, and palmatine which are known to enhance wound healing (69)(70)(71)(72). Also, it has been reported that cinnamic acid-based formulations in addition to wound healing, have antimicrobial properties as well (73). This further augments the therapeutic potential of Madhugrit.…”

Section: Discussionmentioning

confidence: 99%

Anti-hyperglycemic contours of Madhugrit are robustly translated in the Caenorhabditis elegans model of lipid accumulation by regulating oxidative stress and inflammatory response

et al. 2022

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BackgroundThe prevalence of diabetes has considerably increased in recent years. In the long run, use of dual therapy of anti-diabetic agents becomes mandatory to attain euglycemia. Also, the incidences of diabetes-related co-morbidities have warranted the search for new therapeutic approaches for the management of the disease. Traditional herbo-mineral, anti-diabetic agents like Madhugrit are often prescribed to mitigate diabetes and related complications. The present study aimed to thoroughly characterize the pharmacological applications of Madhugrit.MethodsPhytometabolite characterization of Madhugrit was performed by ultra-high performance liquid chromatography. Evaluation of cell viability, α-amylase inhibition, glucose uptake, inflammation, and wound healing was performed by in vitro model systems using AR42J, L6, THP1, HaCaT cells, and reporter cell lines namely NF-κB, TNF-α, and IL-1β. The formation of advanced glycation end products was determined by cell-free assay. In addition, the therapeutic potential of Madhugrit was also analyzed in the in vivo Caenorhabditis elegans model system. Parameters like brood size, % curling, glucose and triglyceride accumulation, lipid deposition, ROS generation, and lipid peroxidation were determined under hyperglycemic conditions induced by the addition of supraphysiological glucose levels.ResultsMadhugrit treatment significantly reduced the α-amylase release, enhanced glucose uptake, decreased AGEs formation, reduced differentiation of monocyte to macrophage, lowered the pro-inflammatory cytokine release, and enhanced wound healing in the in vitro hyperglycemic (glucose; 25 mM) conditions. In C. elegans stimulated with 100 mM glucose, Madhugrit (30 µg/ml) treatment normalized brood size, reduced curling behavior, decreased accumulation of glucose, triglycerides, and lowered oxidative stress.ConclusionsMadhugrit showed multimodal approaches in combating hyperglycemia and related complications due to the presence of anti-diabetic, anti-inflammatory, anti-oxidant, wound healing, and lipid-lowering phytoconstituents in its arsenal. The study warrants the translational use of Madhugrit as an effective medicine for diabetes and associated co-morbidities.

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“…It has also been demonstrated that Car possesses a wide range of properties, including antimicrobial and anti-inflammatory activity [ 30 ]. In the last decade, medicinal chemistry-based approaches (prodrugs, codrugs, derivatives, and/or hybrids) were also used by us to improve the efficacy and pharmacokinetic properties of Car [ 31 , 32 , 33 , 34 , 35 ]. Using these strategies, Car was linked to amino acids (to improve water solubility) [ 31 ], cinnamic acid derivatives (to obtain topic drugs for the treatment of skin infections) [ 32 ], antioxidants (to enhance its potency as an antimicrobial and antifungal drug) [ 33 ], and benzyl moiety, especially meta- or para-substituted (to obtain dual inhibitors of H. pylori strains and AGS cell proliferation) [ 34 ].…”

Section: Introductionmentioning

confidence: 99%

“…In the last decade, medicinal chemistry-based approaches (prodrugs, codrugs, derivatives, and/or hybrids) were also used by us to improve the efficacy and pharmacokinetic properties of Car [ 31 , 32 , 33 , 34 , 35 ]. Using these strategies, Car was linked to amino acids (to improve water solubility) [ 31 ], cinnamic acid derivatives (to obtain topic drugs for the treatment of skin infections) [ 32 ], antioxidants (to enhance its potency as an antimicrobial and antifungal drug) [ 33 ], and benzyl moiety, especially meta- or para-substituted (to obtain dual inhibitors of H. pylori strains and AGS cell proliferation) [ 34 ]. In this context, considering the wide potential of this terpenoid as a pharmaceutical compound, the aim of this work was to develop a small series of Car derivatives ( CD1-3 ) with anti-adipogenic and anti-inflammatory properties endowed with reduced side effects typical of NSAIDs.…”

Section: Introductionmentioning

confidence: 99%

Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells

et al. 2023

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(1) Background: Obesity, a complex metabolic disease resulting from an imbalance between food consumption and energy expenditure, leads to an increase in adipocytes and chronic inflammatory conditions. The aim of this paper was to synthesize a small series of carvacrol derivatives (CD1-3) that are able to reduce both adipogenesis and the inflammatory status often associated with the progression of the obesity disease. (2) Methods: The synthesis of CD1-3 was performed using classical procedures in a solution phase. Biological studies were performed on three cell lines: 3T3-L1, WJ-MSCs, and THP-1. The anti-adipogenic properties of CD1-3 were evaluated using western blotting and densitometric analysis by assessing the expression of obesity-related proteins, such as ChREBP. The anti-inflammatory effect was estimated by measuring the reduction in TNF-α expression in CD1-3-treated THP-1 cells. (3) Results: CD1-3—obtained through a direct linkage between the carboxylic moiety of anti-inflammatory drugs (Ibuprofen, Flurbiprofen, and Naproxen) and the hydroxyl group of carvacrol—have an inhibitory effect on the accumulation of lipids in both 3T3-L1 and WJ-MSCs cell cultures and an anti-inflammatory effect by reducing TNF- α levels in THP-1 cells. (4) Conclusions: Considering the physicochemical properties, stability, and biological data, the CD3 derivative—obtained by a direct linkage between carvacrol and naproxen—resulted in the best candidate, displaying anti-obesity and anti-inflammatory effects in vitro.

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Synthesis and Biological Evaluation of Novel Cinnamic Acid-Based Antimicrobials

Cited by 22 publications

References 41 publications

Development of Biocompatible Ciprofloxacin–Gold Nanoparticle Coated Sutures for Surgical Site Infections

Development of Biocompatible Ciprofloxacin–Gold Nanoparticle Coated Sutures for Surgical Site Infections

Anti-hyperglycemic contours of Madhugrit are robustly translated in the Caenorhabditis elegans model of lipid accumulation by regulating oxidative stress and inflammatory response

Anti-Obesity and Anti-Inflammatory Effects of Novel Carvacrol Derivatives on 3T3-L1 and WJ-MSCs Cells

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