Eugenol-Loaded Transethosomal Gel for Improved Skin Delivery and Treatment of Atopic Dermatitis.

Atopic dermatitis is a skin condition characterized by lichenification (thickening and increased skin marking), eczematous lesions, dry skin, itching, and pruritus. Eugenol is an aromatic polyphenolic compound that has attracted the attention of researchers due to its anti-inflammatory, anti-oxidant, and anti-cancer properties. The primary goal of the present study was to develop and evaluate eugenol-loaded transethosomes for the treatment of AD. Eugenol-loaded transethosomes were formulated using the ethanol injection method and subsequently subjected to particle size analysis, zeta potential, entrapment efficiency, deformability index, and HRTEM analysis. Transethosomal gel was prepared by direct-dispersion method by using Carbopol 940®. Results showed transethosomes to be lipid bilayer structures with acceptable size, and high entrapment efficiency. Transethosomal formulation showed shear-thinning behavior. Eugenol-loaded transethosomal gel was significantly able to enhance the retention of the drug in the skin. Transethosomal gel was significantly able to reduce Ear thickness, DLC, TLC, and IL-6 levels in mice model of AD. These results indicate that the eugenol-loaded transethosomal gel could be a promising carrier for the topical administration of eugenol for the treatment of AD.

Eugenol Possesses Colitis Protective Effects: Impacts on the TLR4/MyD88/NF-[Formula: see text]B Pathway, Intestinal Epithelial Barrier, and Macrophage Polarization.

Eugenol (EU) has been shown to ameliorate experimental colitis due to its anti-oxidant and anti-inflammatory bioactivities. In this study, DSS-induced acute colitis was established and applied to clarify the regulation efficacy of EU on intestinal barrier impairment and macrophage polarization imbalance along with the inflammatory response. Besides, the adjusting effect of EU on macrophages was further investigated in vitro. The results confirmed that EU intervention alleviated DSS-induced colitis through methods such as restraining weight loss and colonic shortening and decreasing DAI scores. Microscopic observation manifested that EU maintained the intestinal barrier integrity in line with the mucus barrier and tight junction protection. Furthermore, EU intervention significantly suppressed the activation of TLR4/MyD88/NF-[Formula: see text]B signaling pathways and pro-inflammatory cytokines gene expressions, while enhancing the expressions of anti-inflammatory cytokines. Simultaneously, WB and FCM analyses of the CD86 and CD206 showed that EU could regulate the DSS-induced macrophage polarization imbalance. Overall, our data further elucidated the mechanism of EU's defensive effect on experimental colitis, which is relevant to the protective efficacy of intestinal barriers, inhibition of oxidative stress and excessive inflammatory response, and reprogramming of macrophage polarization. Hence, this study may facilitate a better understanding of the protective action of the EU against UC.

Eugenol Suppresses Platelet Activation and Mitigates Pulmonary Thromboembolism in Humans and Murine Models.

Platelets assume a pivotal role in the pathogenesis of cardiovascular diseases (CVDs), emphasizing their significance in disease progression. Consequently, addressing CVDs necessitates a targeted approach focused on mitigating platelet activation. Eugenol, predominantly derived from clove oil, is recognized for its antibacterial, anticancer, and anti-inflammatory properties, rendering it a valuable medicinal agent. This investigation delves into the intricate mechanisms through which eugenol influences human platelets. At a low concentration of 2 µM, eugenol demonstrates inhibition of collagen and arachidonic acid (AA)-induced platelet aggregation. Notably, thrombin and U46619 remain unaffected by eugenol. Its modulatory effects extend to ATP release, P-selectin expression, and intracellular calcium levels ([Ca2+]i). Eugenol significantly inhibits various signaling cascades, including phospholipase Cγ2 (PLCγ2)/protein kinase C (PKC), phosphoinositide 3-kinase/Akt/glycogen synthase kinase-3ß, mitogen-activated protein kinases, and cytosolic phospholipase A2 (cPLA2)/thromboxane A2 (TxA2) formation induced by collagen. Eugenol selectively inhibited cPLA2/TxA2 phosphorylation induced by AA, not affecting p38 MAPK. In ADP-treated mice, eugenol reduced occluded lung vessels by platelet thrombi without extending bleeding time. In conclusion, eugenol exerts a potent inhibitory effect on platelet activation, achieved through the inhibition of the PLCγ2-PKC and cPLA2-TxA2 cascade, consequently suppressing platelet aggregation. These findings underscore the potential therapeutic applications of eugenol in CVDs.

Multi-Omics Approaches for Liver Reveal the Thromboprophylaxis Mechanism of Aspirin Eugenol Ester in Rat Thrombosis Model.

Aspirin eugenol ester (AEE) is a novel medicinal compound synthesized by esterifying aspirin with eugenol using the pro-drug principle. Pharmacological and pharmacodynamic experiments showed that AEE had excellent thromboprophylaxis and inhibition of platelet aggregation. This study aimed to investigate the effect of AEE on the liver of thrombosed rats to reveal its mechanism of thromboprophylaxis. Therefore, a multi-omics approach was used to analyze the liver. Transcriptome results showed 132 differentially expressed genes (DEGs) in the AEE group compared to the model group. Proteome results showed that 159 differentially expressed proteins (DEPs) were identified in the AEE group compared to the model group. Six proteins including fibrinogen alpha chain (Fga), fibrinogen gamma chain (Fgg), fibrinogen beta chain (Fgb), orosomucoid 1 (Orm1), hemopexin (Hpx), and kininogen-2 (Kng2) were selected for parallel reaction monitoring (PRM) analysis. The results showed that the expression of all six proteins was upregulated in the model group compared with the control group. In turn, AEE reversed the upregulation trend of these proteins to some degree. Metabolome results showed that 17 metabolites were upregulated and 38 were downregulated in the model group compared to the control group. AEE could reverse the expression of these metabolites to some degree and make them back to normal levels. The metabolites were mainly involved in metabolic pathways, including linoleic acid metabolism, arachidonic acid metabolism, and the tricarboxylic acid (TCA) cycle. Comprehensive analyses showed that AEE could prevent thrombosis by inhibiting platelet activation, decreasing inflammation, and regulating amino acid and energy metabolism. In conclusion, AEE can have a positive effect on thrombosis-related diseases.

Antimicrobial activity of eugenol and carvacrol against Salmonella enterica and E. coli O157:H7 in falafel paste at different storage temperatures.

The objectives of the current study were: i) to investigate the antimicrobial activity of 0.125, 0.250 and 0.50 % (7.54, 15.08 and 30.17 mmol/Kg of eugenol) and (8.15, 16.31, and 33.61 mmol/Kg of carvacrol) against S. enterica and E. coli O157:H7 in falafel paste (FP) stored at 4, 10 or 25 °C for 10 d; and ii) to study the sensory properties of fried falafel treated with eugenol and carvacrol. S. enterica grew well in untreated falafel (control) samples at 10 and 25 °C, while E. coli O157:H7 grew only at 25 °C. However, numbers of S. enterica and E. coli O157:H7 in FP stored at 4 °C were reduced by 1.4-1.6 log CFU/g after 10 d. The antimicrobial agents were more effective at 25 °C against S. enterica, but were better at 4 and 10 °C against E. coli O157:H7. Addition of 0.125-0.5 % eugenol or carvacrol reduced the S. enterica numbers to undetectable level by direct plating (2 log CFU/g) by 2-10 d at 25 °C. FP samples treated with 0.5 % eugenol or 0.25-0.5 % carvacrol were negative for S. enterica cells by enrichment (1 CFU/5 g) by 10 d at 25 °C. In contrast, viable E. coli O157:H7 were not detected by direct plating when FP was treated with 0.25-0.5 % carvacrol or 0.5 % eugenol and stored at 4 °C by 2 d. Addition of eugenol or carvacrol did not affect the color, texture, and appearance of fried falafel but decreased the flavor and overall acceptability scores compared to untreated falafel. Using eugenol and carvacrol as natural antimicrobials have the potential to enhance the safety of FP by reducing the threat from foodborne pathogens.

A novel perspective on eugenol as a natural anti-quorum sensing molecule against Serratia sp.

Serratia marcescens is commonly noted to be an opportunistic pathogen and is often associated with nosocomial infections. In addition to its high antibiotic resistance, it exhibits a wide range of virulence factors that confer pathogenicity. Targeting quorum sensing (QS) presents a potential therapeutic strategy for treating bacterial infections caused by S. marcescens, as it regulates the expression of various virulence factors. Inhibiting QS can effectively neutralize S. marcescens' bacterial virulence without exerting stress on bacterial growth, facilitating bacterial eradication by the immune system. In this study, the antibacterial and anti-virulence properties of eugenol against Serratia sp. were investigated. Eugenol exhibited inhibitory effects on the growth of Serratia, with a minimal inhibitory concentration (MIC) value of 16.15 mM. At sub-inhibitory concentrations, eugenol also demonstrated antiadhesive and eradication activities by inhibiting biofilm formation. Furthermore, it reduced prodigiosin production and completely inhibited protease production. Additionally, eugenol effectively decreased swimming and swarming motilities in Serratia sp. This study demonstrated through molecular modeling, docking and molecular dynamic that eugenol inhibited biofilm formation and virulence factor production in Serratia by binding to the SmaR receptor and blocking the formation of the HSL-SmaR complex. The binding of eugenol to SmaR modulates biofilm formation and virulence factor production by Serratia sp. These findings highlight the potential of eugenol as a promising agent to combat S. marcescens infections by targeting its virulence factors through quorum sensing inhibition.

A Promising Plant-Based Eugenol-Loaded Nano Delivery System (EUG@CMC-PGMA-CS) for Enhanced Antibacterial and Insect Repellent Behavior.

Pathogens and pests pose significant threats to global crop productivity and plant immunity, necessitating urgent measures from researchers to prevent pathogen contamination and pest damage to crops. A natural plant-based antibacterial agent, eugenol (EUG), has demonstrated excellent antimicrobial and insect repellent capabilities, but the characteristics of volatilization and poor dissolution limit the practical application. The nanoization of pesticide formulations holds promise in the development of highly effective pesticides for antibacterial and insecticidal purposes. Herein, a eugenol-loaded nano delivery system (EUG@CMC-PGMA-CS) was synthesized using glycidyl methacrylate (GMA) as a functional monomer to connect carrier core structure carboxymethyl cellulose (CMC) with shell structure chitosan (CS), and EUG was encapsulated within the carrier. EUG@CMC-PGMA-CS demonstrated excellent leaf affinity, with minimum contact angles (CAs) of 37.83 and 70.52° on hydrophilic and hydrophobic vegetable leaf surfaces, respectively. Moreover, the maximum liquid holding capacity (LHC) of EUG@CMC-PGMA-CS on both hydrophilic and hydrophobic vegetable leaf surfaces demonstrates a noteworthy 55.24% enhancement compared to the LHC of pure EUG. The in vitro release curve of EUG@CMC-PGMA-CS exhibited an initial burst followed by stable sustained release. It is with satisfaction that the nano delivery system demonstrated exceptional antibacterial properties against S. aureus and satisfactory insecticidal efficacy against Spodoptera litura. The development of this eugenol-loaded nano delivery system holds significant potential for enhanced antibacterial and insect repellents in agriculture, paving the way for the application of volatile bioactive substances.

Phosphoproteomics analysis reveals the anti-bacterial and anti-virulence mechanism of eugenol against Staphylococcus aureus and its application in meat products.

The increasing risk of food poisoning caused by Staphylococcus aureus (S. aureus) contamination has aroused great concern about food safety. Eugenol is highly favored due to its broad-spectrum antibacterial activity and non-drug resistance property. The study aimed to reveal the anti-bacterial and anti-virulence mechanisms of eugenol against S. aureus using phosphoproteomics. The results indicated that eugenol could inhibit the phosphorylation levels of enzyme I in the bacterial phosphotransferase system (PTS). Meanwhile, it could also inhibit the phosphorylation levels of key enzymes in bacterial carbon metabolism (such as glucose-6-phosphate isomerase of glycolysis and succinyl-CoA synthetase of tricarboxylic acid cycle), thereby decreasing the content of ATP and accelerating bacterial death. In addition, eugenol could inhibit the phosphorylation of AgrA in the quorum sensing system, thereby inhibiting the expression of agr operons (agrA and agrC) and downstream virulence genes (RNAIII, hla and seb). Finally, the application on beef indicated that eugenol could effectively decrease the content of enterotoxins and improve its storage quality. These findings provide a new way for eugenol to prevent S. aureus contamination and food poisoning in meat products.

Cornstarch aerogels with thymol, citronellol, carvacrol, and eugenol prepared by supercritical CO2- assisted techniques for potential biomedical applications.

This study focuses on the development of bioactive materials using environmentally friendly techniques, renewable, biocompatible, and biodegradable polysaccharide, as well as natural bioactive compounds (NBCs) found in plant extracts. First, cornstarch aerogels with a porosity of 86 % and a specific surface area of 225 m2/g were produced via supercritical CO2- assisted drying. Further, thymol, citronellol, carvacrol, and eugenol were incorporated into the aerogels by supercritical CO2- assisted impregnation, which allowed variation in loadings of NBCs (12.8-17.6 %). Interaction between cornstarch aerogels and NBCs determined impregnation rate, pore wall thickness (in the range 18-95 nm), liquid absorption capacity (from 265 to 569 %), dehydration mass loss, and release in phosphate-buffered saline. Controlled release of NBCs was maintained over a 3-day period. Moreover, impregnated aerogels showed a significant antioxidant effect with the highest value for DPPH radical inhibition of 25.5 % determined for the aerogels impregnated with eugenol. Notable antimicrobial activity against tested Gram-negative bacteria, Gram-positive bacteria, and fungi was also observed, being the highest for thymol-loaded aerogel with the diameter of the inhibition zones of up to 37.5 mm. This work shows a promising green approach for the production of bioactive two-component starch-based materials for potential applications in skin infection treatment.

Biofilm formation of C. albicans on occlusal device materials and antibiofilm effects of chitosan and eugenol.

STATEMENT OF PROBLEM: Microbial adhesion on occlusal devices may lead to oral diseases such as candidiasis. Whether chitosan and eugenol provide antibiofilm effects is unclear. PURPOSE: The purpose of this in vitro study was to evaluate the biofilm formation of C. albicans strains on occlusal device materials and the antibiofilm effects of chitosan and eugenol against C. albicans on these surfaces. MATERIAL AND METHODS: A total of 88 specimens (5×10×2 mm) were produced from occlusal device materials with 4 production techniques: vacuum-formed thermoplastic (Group V), head-press (Group H), computer-aided design and computer-aided manufacture (CAD-CAM) (Group C), and 3-dimensionally (3D) printed (Group D) (n=22). After various finishing procedures, the surface properties of the specimens were evaluated by using surface free energy (SFE), surface roughness (SR) measurements, and elemental and topographic analysis. Biofilm formation of C. albicans strain and the antibiofilm effects of chitosan and eugenol against biofilm formation on these surfaces were also examined with a crystal violet assay. The distribution's normality was statistically analyzed with the Kolmogorov-Smirnov test. One-way and two-way analysis of variance with post hoc Tukey tests were used for statistical evaluations (α=.05). RESULTS: Surface roughness values in Groups D and H were significantly higher than in other groups (P<.05). While the highest surface free energy values (except γp) were in Group V, Group C had the highest γp. The lowest biofilm value appeared in Group H. Chitosan exhibited an antibiofilm effect in all groups except Group H, while eugenol was effective in all groups. CONCLUSIONS: The production method affected the susceptibility of occlusal device materials to the adhesion of C. albicans. Eugenol was an effective antibiofilm agent for device materials.

Pharmacodynamic, pharmacokinetic, toxicity, and recent advances in Eugenol's potential benefits against natural and chemical noxious agents: A mechanistic review.

The active biological phytochemicals, crucial compounds employed in creating hundreds of medications, are derived from valuable and medicinally significant plants. These phytochemicals offer excellent protection from various illnesses, including inflammatory disorders and chronic conditions caused by oxidative stress. A phenolic monoterpenoid known as eugenol (EUG), it is typically found in the essential oils of many plant species from the Myristicaceae, Myrtaceae, Lamiaceae, and Lauraceae families. One of the main ingredients of clove oil (Syzygium aromaticum (L.), Myrtaceae), it has several applications in industry, including flavoring food, pharmaceutics, dentistry, agriculture, and cosmeceuticals. Due to its excellent potential for avoiding many chronic illnesses, it has lately attracted attention. EUG has been classified as a nonmutant, generally acknowledged as a safe (GRAS) chemical by the World Health Organization (WHO). According to the existing research, EUG possesses notable anti-inflammatory, antioxidant, analgesic, antibacterial, antispasmodic, and apoptosis-promoting properties, which have lately gained attention for its ability to control chronic inflammation, oxidative stress, and mitochondrial malfunction and dramatically impact human wellness. The purpose of this review is to evaluate the scientific evidence from the most significant research studies that have been published regarding the protective role and detoxifying effects of EUG against a wide range of toxins, including biological and chemical toxins, as well as different drugs and pesticides that produce a variety of toxicities, throughout view of the possible advantages of EUG.

Succinylated starch emulsified Eugenol and Carvacrol nanoemulsions improved digestive stability, bio-accessibility and Salmonella typhimurium inhibition.

The ultrasonically processed Eugenol (EU) and Carvacrol (CAR) nanoemulsions (NE) were successfully optimized via response surface methodology (RSM) to achieve broad spectrum antimicrobial efficacy. These NE were prepared using 2 % (w/w) purity gum ultra (i.e., succinylated starch), 10 % (v/v) oil phase, 80 % (800 W) sonication power, and 10 min of processing time as determined via RSM. The second order Polynomial method was suitable to RSM with a co-efficient of determination >0.90 and a narrow polydispersity index (PDI) ranging 0.12-0.19. NE had small droplet sizes (135.5-160 nm) and low volatility at high temperatures. The EU & CAR entrapment and heat stability (300 °C) confirmed by Fourier transform infrared spectroscopy (FTIR) and thermogravimetric analysis (TGA). Further, the volatility of EU & CAR NE was 18.18 ± 0.13 % and 12.29 ± 0.11 % respectively, being lower than that of bulk/unencapsulated EU & CAR (i.e., 23.48 ± 0.38 % and 19.11 ± 0.08 %) after 2 h at 90 °C. Interestingly, both EU & CAR NE showed sustained release behaviour till 48 h. Their digest could inhibit Salmonella typhimurium (S. typhimurium) via membrane disruption and access to cellular machinery as evident from SEM images. Furthermore, in-vivo bio-accessibility of EU & CAR in mice serum was up to 80 %. These cost-effective and short-processed EU/CAR NE have the potential as green preservatives for food industry.

Eugenol alleviates acrylamide-induced rat testicular toxicity by modulating AMPK/p-AKT/mTOR signaling pathway and blood-testis barrier remodeling.

This study aimed to investigate the effects of eugenol treatment on reproductive parameters in acrylamide (ACR)-intoxicated rats. The study evaluated alterations in relative testes and epididymides weights, sperm quality, serum hormonal status, seminal plasma amino acids, testicular cell energy and phospholipids content, oxidative and nitrosative stress parameters, adenosine monophosphate-activated protein kinase/ phosphoinositide 3-kinase/phosphor-protein kinase B/mammalian target of rapamycin (AMPK/PI3K/p-AKT/mTOR) signaling pathway, blood-testis barrier (BTB) remodeling markers, testicular autophagy and apoptotic markers, as well as histopathological alterations in testicular tissues. The results revealed that eugenol treatment demonstrated a significant improvement in sperm quality parameters, with increased sperm cell concentration, progressive motility live sperm, and a reduction in abnormal sperm, compared to the ACR-intoxicated group. Furthermore, eugenol administration increased the levels of seminal plasma amino acids in a dose-dependent manner. In addition, eugenol treatment dose-dependently improved testicular oxidative/nitrosative stress biomarkers by increasing oxidized and reduced glutathione levels and reducing malondialdehyde and nitric oxide contents as compared to ACRgroup. However, eugenol treatment at a high dose restored the expression of AMPK, PI3K, and mTOR genes, to levels comparable to the control group, while significantly increasing p-AKT content compared to the ACRgroup. In conclusion, the obtained findings suggest the potential of eugenol as a therapeutic agent in mitigating ACR-induced detrimental effects on the male reproductive system via amelioration of ROS-mediated autophagy, apoptosis, AMPK/p-AKT/mTOR signaling pathways and BTB remodeling.

pH-responsive on-demand release of eugenol from metal-organic frameworks for synergistic bacterial killing.

Bacterial infections are a big challenge in clinical treatment, making it urgent to develop innovative antibacterial systems and therapies to combat bacterial infections. In this study, we developed a novel MOF-based synergistic antibacterial system (Eu@B-UiO-66/Zn) by loading a natural antibacterial substance (eugenol) with hierarchically porous MOF B-UiO-66 as a carrier and further complexing it with divalent zinc ions. Results indicate that the system achieved a controlled release of eugenol under pH responsive stimulation, with the complexation ability of eugenol and Zn2+ ions as a switch. Due to the destruction of a coordination bond between eugenol and Zn2+ ions by an acidic medium, the release of eugenol loaded in Eu@B-UiO-66/Zn reached 80% at pH 5.8, which was significantly higher than that under pH 8.0 (51%). Moreover, the inhibitory effect of Eu@B-UiO-66/Zn against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) after 24 h was 96.4% and 99.7%, respectively, owing to the synergistic antibacterial effect of eugenol and Zn2+ ions, which was significantly stronger than free eugenol and Eu@B-UiO-66. We hope that this strategy for constructing responsive MOF-based antibacterial carriers could have potential possibilities for the application of MOF materials in antibacterial fields.

Self-assembly of sophorolipid and eugenol into stable nanoemulsions for synergetic antibacterial properties through alerting membrane integrity.

Exploring the natural, safe, and effective antimicrobial is one of the preferable ways to control foodborne bacteria. In this work, novel oil-in-water nanoemulsions were formulated with sophorolipids and eugenol without any co-surfactant using a self-assembling strategy. These nanoemulsions showed high stability with sizes less than 200 nm when exposure to low concentrations of salt ions, various pH values (5.0, 7.0, 10.0), storage temperature and time. The synergistic antibacterial effects against both Gram-negative Escherichia coli and Gram-positive Bacillus cereus were determined with a minimum inhibitory concentration (MIC) value of 0.5 mg/mL and 0.125 mg/mL, respectively. Further microscopy (SEM, TEM, LCSM) examination and ATP/Na+-K+-ATPase assay results showed that the morphological changes, intensive cell membrane permeability, leakage of ATP, and decreased Na+-K+-ATPase contributed to the antibacterial effects. Moreover, the bonding mechanism between nanoemulsions and cell membranes were further evaluated by FTIR and ITC using a DPPC vesicle model, which demonstrated that the nanoemulsions adsorbed on the surface of bilayer, interacted with the hydrophobic chains of DPPC membrane mainly through the hydrophobic interaction, and altered the structural integrity of the lipid bilayer. These results not only provide a facile green strategy for fabricating stable nanoemulsions, but also highlight a new perspective for stabilizing essential oils for their widely application in food industry.

Antibiofilm Activity of Eugenol-Loaded Chitosan Coatings against Common Medical-Device-Contaminating Bacteria.

The formation of pathogenic biofilms on medical devices is a major public health concern accounting for over 65% of healthcare-associated infections and causing high infection morbidity, mortality, and a great burden to patients and the healthcare system due to its resistance to treatment. In this study, we developed a chitosan-based antimicrobial coating with embedded mesoporous silica nanoparticles (MSNs) to load and deliver eugenol, an essential oil component, to inhibit the biofilm formation of common bacteria in medical-device-related infections. The eugenol-loaded MSNs were dispersed in a chitosan solution, which was then cross-linked with glutaraldehyde and drop-casted to obtain coatings. The MSNs and coatings were characterized by dynamic light scattering, Brunauer-Emmett-Teller analysis, attenuated-total-reflectance Fourier transform infrared spectroscopy, X-ray photoelectron spectroscopy, 3D optical profilometry, and scanning electron microscopy. The release behavior of eugenol-loaded MSNs and coatings and the antibiofilm and antimicrobial activity of the coatings against adherent Staphylococcus aureus, methicillin-resistant S. aureus, and Pseudomonas aeruginosa were investigated. Eugenol was released from the MSNs and coatings in aqueous conditions in a controlled manner with an initial low release, followed by a peak release, a decrease, and a plateau. While the chitosan coatings alone or with unloaded MSNs demonstrated limited antimicrobial effects and still supported biofilm formation after 24 h, the coating containing eugenol not only reduced biofilm formation but also killed the majority of the attached bacteria. It also showed biocompatibility in indirect contact with NIH/3T3 fibroblasts and a high percentage of live cells in direct contact. However, further investigations into cell proliferation in direct contact are recommended. The findings indicated that the chitosan-based coating with eugenol-loaded MSNs could be developed into an effective strategy to inhibit biofilm formation on medical devices.

Development and In-Vitro Evaluation of Eugenol-Based Nanostructured Lipid Carriers for Effectual Topical Treatment Against C. albicans.

The main objective of the experiment is to develop and evaluate hydrogel-bearing nanostructured lipid carriers (NLCs) loaded with ketoconazole (KTZ) for the effective treatment of candidiasis. The eugenol was used as a liquid lipid (excipient) for the development of KTZ-loaded NLCs and was explored for anti-fungal effect. The production of NLCs involves high energy processes to generate spherical, uniform particles, having a higher percentage of entrapment efficiency (%EE) for KTZ with 89.83 ± 2.31 %. The data from differential scanning calorimeter (DSC), powder x-ray diffraction (PXRD), and attenuated total reflectance (ATR) demonstrated the KTZ dispersion in NLCs. The NLCs loaded hydrogel possessed optimum spreadability and exhibited shear thinning behavior, indicating the ease of application of the final formulation. The 6.41-fold higher transdermal flux (Jss) was governed for KTZ from KTZ-NLC than coarse-KTZ, which explains the usefulness of NLCs. The KTZ-NLCs exhibited significant 2.58 and 6.35-fold higher retention in the stratum corneum and viable epidermis of the skin. The cell cytotoxicity studies using human dermal fibroblast cell (HDFS) lines depicted the usefulness of NLCs in reducing cell toxicities for KTZ. The KTZ-NLCs were found to inhibit planktonic growth and hyphal transition and showed a larger zone of inhibition against C. albicans strains with a MIC-50 value of 0.39 µg/mL. The antibiofilm activity of KTZ-NLCs at lower concentrations, in contrast to plain KTZ, explained the interaction of developed NLCs with fungal membranes. The overall results depicted the effectiveness of the loading KTZ in the lipid matrix to achieve antifungal activity against C. albicans.

Protective role of eugenol against diabetes-induced oxidative stress, DNA damage, and apoptosis in rat testes.

Diabetes mellitus, a metabolic disorder alters gonadal development and spermatogenesis, reactive oxygen species production, DNA damage, and apoptosis, which subsequently lead to male subfertility. Eugenol is an antioxidant, traditionally used as medication for digestive disorders and antioxidant therapy, decrease transport of glucose from GIT to systemic circulation. This experiment was aimed to decipher cellular and molecular insights of eugenol in protecting diabetic germ cells in rats. Rats were assigned randomly into five groups: control, eugenol control (Eugenol 400; EUG), diabetic (DIA), diabetic + eugenol 100 (DIA + EUG 100), and diabetic + eugenol 400 (DIA + EUG 400). EUG 400 and DIA + EUG 400 groups received 400 mg/kg eugenol orally. DIA + EUG 100 group received 100 mg/kg eugenol. Treatment was conducted for 4 weeks. Type 1 diabetes was induced by injecting a single i.p. dose of streptozotocin (55 mg/kg). Morphometric, biochemical, sperm parameters, oxidative stress, hormonal levels, histopathology, and fibrosis in the testis and epididymis, were evaluated. DNA damage was evaluated using halo and comet assays; DNA fragmentation and apoptosis using TUNEL assay. Eugenol treatment significantly normalized biochemical parameters, reduced MDA while increased albumin and GSH levels in diabetes. Eugenol significantly increased sperm numbers, motility and attenuated abnormal sperm head morphology in diabetes. Moreover, eugenol significantly reversed diabetes-induced cellular damages, altered spermatogenesis, and collagen deposition in testis and epididymis. It also significantly attenuated diabetes-associated DNA breaks and apoptosis. These findings suggest that 4 weeks treatment with 400 mg/kg of eugenol could be beneficial for diabetic patients to prevent subfertility.

Nanocomposites of iron oxide, sodium alginate, and eugenol induce apoptosis via PI3K/Akt/mTOR signaling in Hep3 cells and in vivo hepatotoxicity in the zebrafish model.

Hepatic cancer is among the most recurrently detected malignancies worldwide and one of the main contributors to cancer-associated mortality. With few available therapeutic choices, there is an instant necessity to explore suitable options. In this aspect, Nanotechnology has been employed to explore prospective chemotherapeutic approaches, especially for cancer treatment. Nanotechnology is concerned with the biological and physical properties of nanoparticles in the therapeutic use of drugs. In the current work, formulation, and characterization of α-Fe2O3-Sodium Alginate-Eugenol nanocomposites (FSE NCs) using several approaches like SEM and TEM, UV-visible, FTIR, and PL spectroscopy, XRD, EDAX, and DLS studies have been performed. With an average size of 50 nm, the rhombohedral structure of NCs was identified. Further, their anticancer activity against Hep3B liver cancer cell lines has been performed by cell viability, dual staining, DCFH-DA, Annexin-V/-FITC/PI, cell cycle analysis methods, and PI3K/Akt/mTOR signaling proteins were studied to assess the anticancer effects of the NCs in Hep3B cells. Also, anti-cancer activity on animal modeling in-vivo using zebra fishes to hematological parameters, liver enzymes, and histopathology study effectiveness was noticed. Moreover, the NCs reduced the viability, elevated the ROS accumulation, diminished the membrane integrity, reduced the antioxidants, blocked the cell cycle, and triggered the PI3K/Akt/mTOR signaling axis that eventually resulted in cell death. As a result, FSE NCs possess huge potential for use as a possible anticancer candidate.

Effect of a blend of cinnamaldehyde, eugenol, and Capsicum oleoresin on methane emission and lactation performance of Holstein-Friesian dairy cows.

This study aimed to investigate the effect of administering a standardized blend of cinnamaldehyde, eugenol, and Capsicum oleoresin (CEC) to lactating dairy cattle for 84 d (i.e., 12 wk) on enteric CH4 emission, feed intake, milk yield and composition, and body weight. The experiment involved 56 Holstein-Friesian dairy cows (145 ± 31.1 d in milk at the start of the trial; mean ± standard deviation) in a randomized complete block design. Cows were blocked in pairs according to parity, lactation stage, and current milk yield, and randomly allocated to 1 of the 2 dietary treatments: a diet including 54.5 mg of CEC/kg of DM or a control diet without CEC. Diets were provided as partial mixed rations in feed bins, which automatically recorded individual feed intake. Additional concentrate was fed in the GreenFeed system that was used to measure emissions of CO2, CH4, and H2. Feeding CEC decreased CH4 yield (g/kg DMI) by on average 3.4% over the complete 12-wk period and by on average 3.9% from 6 wk after the start of supplementation onward. Feeding CEC simultaneously increased feed intake and body weight, and tended to increase milk protein content, whereas no negative responses were observed. These results must be further investigated and confirmed in longer-term in vivo experiments.