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1.
J Insect Sci ; 24(3)2024 May 01.
Article in English | MEDLINE | ID: mdl-38805647

ABSTRACT

The parasitic mite Varroa destructor (Anderson and Trueman) is one of the greatest stressors of Apis mellifera (L.) honey bee colonies. When Varroa infestations reach damaging levels during fall, rapid control is necessary to minimize damage to colonies. We performed a field trial in the US Southeast to determine if a combination of registered treatments (Apivar, amitraz-based; and Apiguard, thymol-based) could provide rapid and effective control of Varroa. We compared colonies that received this combination treatment against colonies that received amitraz-based positive control treatments: (i) Apivar alone; or (ii) amitraz emulsifiable concentrate ("amitraz EC"). While not registered, amitraz EC is used by beekeepers in the United States in part because it is thought to control Varroa more rapidly and effectively than registered products. Based on measurements of Varroa infestation rates of colonies after 21 days of treatment, we found that the combination treatment controlled Varroa nearly as rapidly as the amitraz EC treatment: this or other combinations could be useful for Varroa management. At the end of the 42-day trial, colonies in the amitraz EC group had higher bee populations than those in the Apivar group, which suggests that rapid control helps reduce Varroa damage. Colonies in the combination group had lower bee populations than those in the amitraz EC group, which indicates that the combination treatment needs to be optimized to avoid damage to colonies.


Subject(s)
Acaricides , Thymol , Toluidines , Varroidae , Animals , Toluidines/pharmacology , Bees/parasitology , Varroidae/drug effects , Varroidae/physiology , Thymol/pharmacology , Beekeeping/methods
2.
Neoplasma ; 71(2): 193-200, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38766852

ABSTRACT

Colorectal cancer (CRC) is one of the most commonly diagnosed malignancies with a high mortality rate. In the last few years, attention has been focused on substances of natural origin with anticancer activity. One such substance is thymol and its derivatives, which have been shown to have an antitumor effect also against CRC cells. In our study, we focused on determining the biological and antibacterial effects of thymol and thymol derivatives. Analyses were performed on a 3D model of human colon carcinoma cell lines (HCT-116 and HT-29) - spheroids. The cytotoxic (MTT assay) and genotoxic effect (comet assay) of thymol and derivatives: acetic acid thymol ester and thymol ß-D-glucoside were determined. ROS levels (ROS-Glo™ H2O2 Assay) and total antioxidant status (Randox TAS Assay) were also monitored. Last but not least, we also detected the effect of the derivatives using a disk diffusion assay and determined the number of colonies on the plates on selected bacteria such as Lacticaseibacillus rhamnosus, Lactiplantibacillus plantarum, Lacticaseibacillus paracasei, Lactobacillus brevis, Lactobacillus pentosus and Weizmannia coagulans. The derivatives did not show a significant inhibitory effect on the growth of LAB bacteria (lactic acid bacteria) in contrast to thymol. Overall, thymol derivatives are cytotoxic, genotoxic and increase ROS levels. Among the derivatives tested, acetic acid thymol ester (IC50 ~ 0.2 µg/ml) was more effective. The second derivative tested (thymol ß-D-glucoside) was effective at higher concentrations than thymol. Our research confirmed that thymol derivatives have a toxic effect on the 3D model of intestinal tumor cells, while they do not have a toxic effect on selected intestinal bacteria. Thus, they could bring new significance to the prevention or treatment of CRC.


Subject(s)
Colorectal Neoplasms , Spheroids, Cellular , Thymol , Humans , Thymol/pharmacology , Colorectal Neoplasms/drug therapy , Colorectal Neoplasms/pathology , Spheroids, Cellular/drug effects , HCT116 Cells , HT29 Cells , Reactive Oxygen Species/metabolism , Antioxidants/pharmacology , Antineoplastic Agents/pharmacology
3.
Int J Mol Sci ; 25(9)2024 May 01.
Article in English | MEDLINE | ID: mdl-38732168

ABSTRACT

Antimicrobial resistance (AMR) poses an emanating threat to humanity's future. The effectiveness of commonly used antibiotics against microbial infections is declining at an alarming rate. As a result, morbidity and mortality rates are soaring, particularly among immunocompromised populations. Exploring alternative solutions, such as medicinal plants and iodine, shows promise in combating resistant pathogens. Such antimicrobials could effectively inhibit microbial proliferation through synergistic combinations. In our study, we prepared a formulation consisting of Aloe barbadensis Miller (AV), Thymol, iodine (I2), and polyvinylpyrrolidone (PVP). Various analytical methods including SEM/EDS, UV-vis, Raman, FTIR, and XRD were carried out to verify the purity, composition, and morphology of AV-PVP-Thymol-I2. We evaluated the inhibitory effects of this formulation against 10 selected reference strains using impregnated sterile discs, surgical sutures, gauze bandages, surgical face masks, and KN95 masks. The antimicrobial properties of AV-PVP-Thymol-I2 were assessed through disc diffusion methods against 10 reference strains in comparison with two common antibiotics. The 25-month-old formulation exhibited slightly lower inhibitory zones, indicating changes in the sustained-iodine-release reservoir. Our findings confirm AV-PVP-Thymol-I2 as a potent antifungal and antibacterial agent against the reference strains, demonstrating particularly strong inhibitory action on surgical sutures, cotton bandages, and face masks. These results enable the potential use of the formulation AV-PVP-Thymol-I2 as a promising antimicrobial agent against wound infections and as a spray-on contact-killing agent.


Subject(s)
Microbial Sensitivity Tests , Thymol , Thymol/pharmacology , Thymol/chemistry , Iodine/chemistry , Iodine/pharmacology , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Aloe/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Humans , Drug Compounding/methods
4.
Molecules ; 29(10)2024 May 12.
Article in English | MEDLINE | ID: mdl-38792138

ABSTRACT

Cancer is ranked among lethal diseases globally, and the increasing number of cancer cases and deaths results from limited access to effective therapeutics. The use of plant-based medicine has been gaining interest from several researchers. Carvacrol and its isomeric compound, thymol, are plant-based extracts that possess several biological activities, such as antimalarial, anticancer, antifungal, and antibacterial. However, their efficacy is compromised by their poor bioavailability. Thus, medicinal scientists have explored the synthesis of hybrid compounds containing their pharmacophores to enhance their therapeutic efficacy and improve their bioavailability. Hence, this review is a comprehensive report on hybrid compounds containing carvacrol and its isomer, thymol, with potent anticancer and antibacterial agents reported between 2020 and 2024. Furthermore, their structural activity relationship (SAR) and recommended future strategies to further enhance their therapeutic effects will be discussed.


Subject(s)
Anti-Bacterial Agents , Antineoplastic Agents , Cymenes , Thymol , Thymol/chemistry , Thymol/pharmacology , Cymenes/chemistry , Cymenes/pharmacology , Cymenes/therapeutic use , Humans , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Structure-Activity Relationship , Neoplasms/drug therapy , Animals
5.
Pestic Biochem Physiol ; 201: 105886, 2024 May.
Article in English | MEDLINE | ID: mdl-38685252

ABSTRACT

This study evaluates the pediculicidal activity of nanoformulations containing different binary essential oil component mixtures (eugenol:linalool, 1,8 -cineole:linalool, and eugenol:thymol) using immersion bioassays. These have allowed us to evaluate the knockdown time affecting 50% of the individuals (KT50). In addition, the type of interaction between the components in each mixture was established in terms of the combination index (IC). The KT50 values were 6.07; 8.83; 7.17 and 27.23 h for linalool, 1,8 -cineole, eugenol, and thymol, respectively. For the eugenol:linalool mixtures, the efficacy was lower or equal to that obtained for the nanoformulations of the pure compounds, with values of KT50 about 13.33, 8.16 and 6.71 h for mixtures with ratios 3:1, 1:1 and 1:3, respectively. These mixtures present IC > 1, evidencing antagonistic interaction, which is enhanced with eugenol content. In the case of the binary mixtures of 1,8 -cineole: linalool, KT50 values were similar to those obtained for eugenol:linalool mixtures with similar ratios. In this case, IC assumes values close to unity, suggesting additive interactions independently of the mixture composition. On the other side, mixtures of eugenol:thymol with 1:1 and 1:3 ratios showed values of 9.40 and 32.93 h, while the mixture with a 3:1 ratio showed the greatest effectiveness (KT50 of 4.42 h). Eugenol:thymol mixtures show synergistic interaction (IC < 1) for combinations 3:1 and 1:1, while no interaction was observed for 1:3 combination. This indicates that eugenol enhances thymol activity. These results must be considered an important step forward to the development of effective pediculicidal nanoformulations based on botanical compounds.


Subject(s)
Acyclic Monoterpenes , Eucalyptol , Eugenol , Monoterpenes , Monoterpenes/pharmacology , Monoterpenes/chemistry , Animals , Eugenol/pharmacology , Eugenol/chemistry , Eucalyptol/pharmacology , Acyclic Monoterpenes/pharmacology , Acyclic Monoterpenes/chemistry , Pediculus/drug effects , Insecticides/pharmacology , Insecticides/chemistry , Thymol/pharmacology , Thymol/chemistry , Micelles , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Nanoparticles/chemistry , Lice Infestations/drug therapy
6.
J Appl Microbiol ; 135(4)2024 Apr 01.
Article in English | MEDLINE | ID: mdl-38587823

ABSTRACT

AIM: In this study, it was aimed to examine the antibacterial activity of the essential oil components (EOCs), carvacrol (CAR), cinnamaldehyde (CIN), thymol (TH), alpha pinene (α-PN), eucalyptol (EU), limonene (LIM), and the antibiotics, linezolid (LZD), vancomycin (VAN), gentamicin (GEN), ciprofloxacin (CIP), clindamycin (CLN), and penicillin (PEN) against 50 multidrug resistant Corynebacterium striatum strains, and the synergistic interactions of CAR and CIN with the antibiotics against 10 randomly selected Coryne. striatum strains to explore synergistic interactions to determine if their combined use could enhance antibiotic activity and potentially reduce resistance. METHODS AND RESULTS: The activity of the EOCs and the antibiotics against Coryne. striatum strains isolated from clinical specimens, was examined by broth microdilution method. The synergistic interactions of the EOCs with the antibiotics against 10 randomly selected Coryne. striatum strains were determined by checkerboard method. EOCs, CIN, and CAR and antibiotics, LZD, VAN, GEN, CIP, and CLN were detected to have antibacterial activity against Coryne. striatum strains alone and either synergistic interactions were observed in combinations of the antibiotics with EOCs. CONCLUSIONS: All Coryne. striatum strains were determined to be susceptible to VAN and LZD and resistant to GEN, PEN, CIP, and CLN. Synergistic interactions were observed in all combinations of antibiotics tested with CAR and CIN.


Subject(s)
Acrolein , Acrolein/analogs & derivatives , Anti-Bacterial Agents , Corynebacterium , Drug Resistance, Multiple, Bacterial , Drug Synergism , Microbial Sensitivity Tests , Monoterpenes , Oils, Volatile , Anti-Bacterial Agents/pharmacology , Corynebacterium/drug effects , Oils, Volatile/pharmacology , Drug Resistance, Multiple, Bacterial/drug effects , Acrolein/pharmacology , Monoterpenes/pharmacology , Cymenes/pharmacology , Ciprofloxacin/pharmacology , Gentamicins/pharmacology , Vancomycin/pharmacology , Linezolid/pharmacology , Limonene/pharmacology , Eucalyptol/pharmacology , Thymol/pharmacology , Clindamycin/pharmacology , Humans , Penicillins/pharmacology , Terpenes/pharmacology , Cyclohexenes/pharmacology , Corynebacterium Infections/microbiology
7.
Int J Biol Macromol ; 268(Pt 2): 131669, 2024 May.
Article in English | MEDLINE | ID: mdl-38642683

ABSTRACT

Reducing contamination from percolate is critical to the preservation of foods with high water content, such as pork. This study aims to develop a novel active packaging material for meat preservation by precisely controlled dual-channel one-step electrospinning. Compared to traditional strategies of preparing Janus films, this method allows for greater flexibility and efficiency. The structure and properties of the Janus film are characterized by scanning electron microscopy (SEM), water contact angle (WCA), directional liquid transport investigation, Thymol release and permeation features, and biocompatibility evaluation. Moreover, the Janus film is applied to the packaging of pork with modified atmosphere packaging to demonstrate its practical application prospects in the food active packaging field. The results revealed that the two sides of the film showed completely different wettability, and the change rate of WCA increased with the increase of the scale of hydrophilic fibers. The permeation features of thymol loaded in the film was consistent with the results of antibacterial properties and biocompatibility assessment. Moreover, the Janus film can effectively prolong the shelf life, improve the quality and safety of the pork.


Subject(s)
Anti-Bacterial Agents , Chitosan , Food Packaging , Polyesters , Thymol , Thymol/chemistry , Thymol/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Chitosan/chemistry , Chitosan/pharmacology , Polyesters/chemistry , Food Packaging/methods , Animals , Food Preservation/methods , Swine , Meat
8.
Eur J Med Chem ; 270: 116381, 2024 Apr 15.
Article in English | MEDLINE | ID: mdl-38604097

ABSTRACT

The high prevalence of methicillin-resistant Staphylococcus aureus (MRSA) strains and the formation of non-growing, dormant "persisters" subsets help bacteria evade antibiotic treatment and enhance bacterial resistance, which poses a serious threat to human life and health. It is urgent to discover novel antibacterial therapies effective against MRSA persisters. Thymol is a common nutraceutical with weak antibacterial and antitumor activities. A series of Thymol triphenylphosphine (TPP) conjugates (TPP-Thy3) was designed and synthesized. These compounds showed significantly improved inhibitory activity against Gram-positive bacteria compared with Thymol. Among them, Thy3d displayed a low probability of resistance selection and showed excellent biocompatibility. Interestingly, Thy3d elicited a rapid killing effect of MRSA persisters (99.999%) at high concentration. Fluorescence experiments, electron microscopy, molecular dynamics simulation and bilayer experiment confirmed that Thy3d conjugates exerted potent antimicrobial activity by disrupting the integrity of the membrane of bacterial even the persister. Furthermore, Thy3d exhibited considerable efficacy in a mouse model of subcutaneous murine MRSA infection. In summary, TPP-Thy3 conjugates are a series of novel antibacterial agents and could serve as a new therapeutic strategy for combating antibiotic resistance.


Subject(s)
Anti-Bacterial Agents , Methicillin-Resistant Staphylococcus aureus , Organophosphorus Compounds , Humans , Animals , Mice , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/therapeutic use , Thymol/pharmacology , Microbial Sensitivity Tests , Bacteria
9.
BMC Complement Med Ther ; 24(1): 138, 2024 Apr 02.
Article in English | MEDLINE | ID: mdl-38566054

ABSTRACT

Herbal components are highly useful assets for the advancement of novel antibacterial drugs. Nanotechnology holds great promise as an approach to enhance the effectiveness and develop the composition of these substances. The study developed nanogels incorporating camphor, thymol, and a combination derived from the initial nanoemulsions with particle sizes of 103, 85, and 135 nm, respectively. The viscosity of nanogels and the successful loading of compounds in them were examined by viscometery and ATR-FTIR studies. The bactericidal properties of the nanogels were examined against four bacterial strains. The nanogel containing camphor and thymol at 1250 µg/mL concentration exhibited complete growth suppression against Pseudomonas aeruginosa and Staphylococcus aureus. The thymol nanogel at 1250 µg/mL and the camphor nanogel at 2500 µg/mL exhibited complete inhibition of growth on Listeria monocytogenes and Escherichia coli, respectively. Both nanogels showed favorable effectiveness as antibacterial agents and could potentially examine a wide range of pathogens and in vivo studies.


Subject(s)
Camphor , Polyethylene Glycols , Polyethyleneimine , Thymol , Thymol/pharmacology , Nanogels , Camphor/pharmacology , Anti-Bacterial Agents/pharmacology , Escherichia coli
10.
Sci Rep ; 14(1): 5608, 2024 03 07.
Article in English | MEDLINE | ID: mdl-38454146

ABSTRACT

Essential oil from Thymus vulgaris L. has valuable therapeutic potential that is highly desired in pharmaceutical, food, and cosmetic industries. Considering these advantages and the rising market demand, induced polyploids were obtained using oryzalin to enhance essential oil yield. However, their therapeutic values were unexplored. So, this study aims to assess the phytochemical content, and antimicrobial, antioxidant, and anti-inflammatory activities of tetraploid and diploid thyme essential oils. Induced tetraploids had 41.11% higher essential oil yield with enhanced thymol and γ-terpinene content than diploid. Tetraploids exhibited higher antibacterial activity against all tested microorganisms. Similarly, in DPPH radical scavenging assay tetraploid essential oil was more potent with half-maximal inhibitory doses (IC50) of 180.03 µg/mL (40.05 µg TE/mg) than diploid with IC50 > 512 µg/mL (12.68 µg TE/mg). Tetraploids exhibited more effective inhibition of in vitro catalytic activity of pro-inflammatory enzyme cyclooxygenase-2 (COX-2) than diploids at 50 µg/mL concentration. Furthermore, molecular docking revealed higher binding affinity of thymol and γ-terpinene towards tested protein receptors, which explained enhanced bioactivity of tetraploid essential oil. In conclusion, these results suggest that synthetic polyploidization using oryzalin could effectively enhance the quality and quantity of secondary metabolites and can develop more efficient essential oil-based commercial products using this induced genotype.


Subject(s)
Cyclohexane Monoterpenes , Dinitrobenzenes , Oils, Volatile , Plant Oils , Sulfanilamides , Thymus Plant , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Thymol/pharmacology , Thymus Plant/chemistry , Tetraploidy , Molecular Docking Simulation , Phytochemicals/pharmacology
11.
Exp Appl Acarol ; 92(3): 555-565, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38468022

ABSTRACT

The main way to avoid contact with ticks and consequently tick-borne disease is the use of synthetic repellents. The search of new repellent compounds to increase the possibilities of use in strategies controls are necessary. The present study evaluated the repellent activity of two natural terpenes carvacrol and thymol in each one two different formulation (encapsulated and nonencapsulated with yeast cell wall) against the ticks Amblyomma sculptum and Rhipicephalus sanguineus sensu lato nymphs. Nymphs of A. sculptum and R. sanguineus s.l. of a single generation were used. The vertical filter paper repellency assay were performed with different concentration of both terpenes encapsulated and nonencapsulated in yeast cell wall. The repellent concentration 50% (RC50) were calculated to each compound formulation. Both carvacrol and thymol (encapsulated and nonencapsulated), had a repellent activity against A. sculptum and R. sanguineus s.l nymphs. Amblyomma sculptum was more sensitive to nonencapsulated carvacrol (RC50 values: 0.0032 to 0.0082 mg/cm2 after 1 and 15 min) (P < 0.05), while R. sanguineus s.l. was more sensitive to encapsulated carvacrol (RC50 values: 0.00008 to 0.0035 mg/cm2 after 1 and 15 min) (P < 0.05). Among tick species, R. sanguineus s.l. was more sensitive for most compounds than A. sculptum (P < 0.05). Although with distinct repellent activities, carvacrol and thymol encapsulated can be a promising alternative to synthetic repellents against A. sculptum and R. sanguineus s.l.


Subject(s)
Amblyomma , Cymenes , Nymph , Rhipicephalus sanguineus , Thymol , Cymenes/pharmacology , Animals , Thymol/pharmacology , Nymph/drug effects , Nymph/growth & development , Rhipicephalus sanguineus/drug effects , Cell Wall/drug effects , Acaricides/pharmacology , Monoterpenes/pharmacology , Insect Repellents/pharmacology , Saccharomyces cerevisiae/drug effects
12.
J Agric Food Chem ; 72(13): 6803-6814, 2024 Apr 03.
Article in English | MEDLINE | ID: mdl-38507708

ABSTRACT

Neurodegenerative diseases pose a growing global health challenge, with limited effective therapeutic options. Mitochondrial dysfunction, oxidative stress, neuroinflammation, apoptosis, and autophagy are common underlying mechanisms in these diseases. Thymol is a phenolic monoterpene compound that has gained attention for its diverse biological properties, including antioxidant, anti-inflammatory, and immunomodulatory activities. Thymol supplementation could provide potential neuroprotection and improve cognitive deficits, depressant-like effects, learning, and memory impairments in rodents. Mechanistic investigations reveal that the neuroprotective effects of thymol involve the improvement of oxidative stress, mitochondrial dysfunction, and inflammatory response. Several signaling pathways, including mitochondrial apoptotic, NF-κB, AKT, Nrf2, and CREB/BDNF pathways are also involved. In this review, the neuroprotective effects of thymol, the potential molecular mechanisms, safety, applications, and current challenges toward development as a neuroprotective agent were summarized and discussed. We hope that this review provides valuable insights for the further development of this promising natural product as a promising neuroprotective agent.


Subject(s)
Mitochondrial Diseases , Neuroprotective Agents , Humans , Neuroprotective Agents/pharmacology , Neuroprotective Agents/therapeutic use , Thymol/pharmacology , Signal Transduction , Antioxidants/pharmacology , Antioxidants/metabolism , Oxidative Stress , Mitochondrial Diseases/drug therapy
13.
Carbohydr Polym ; 331: 121874, 2024 May 01.
Article in English | MEDLINE | ID: mdl-38388060

ABSTRACT

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.


Subject(s)
Acyclic Monoterpenes , Cymenes , Starch , Thymol , Starch/chemistry , Thymol/pharmacology , Eugenol/pharmacology , Carbon Dioxide/chemistry , Gels/chemistry
14.
Vet Parasitol ; 327: 110149, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38412588

ABSTRACT

The tick Rhipicephalus microplus is a parasite of great importance in cattle breeding. It is responsible for huge economic losses. The application of synthetic acaricides is used as a form of control. However, resistant strains have been selected over the years, making it necessary to search for new alternative formulations. The present study aimed to formulate biodegradable films impregnated with the terpenes carvacrol and thymol and evaluate their efficacy on larvae and adults of R. microplus through in vitro tests. The following formulations were prepared: Film 1 (starch based); Film 2 (based on starch and glycerol); Film 1 + Carvarcol or Thymol; Film 2 + Carvarcol or Thymol. Terpenes had a final concentration of 5.0 mg/mL. To evaluate the formulations on larvae, the immersion test was performed by dividing into six groups according to the concentration of terpenes: 5.0, 2.5, 1.25, 0.625, 0.313, 0.156 mg/mL and the control groups: 1% ethanol solution; 10% ethanol solution; Film 1; and Film 2. For the evaluations on adult ticks, ten experimental groups (n = 10) were used: 1) Carvacrol; 2) Film 1 + Carvacrol; 3) Film 2 + Carvacrol; 4) Thymol; 5) Film 1 + Thymol; 6) Film 2 + Thymol; 7) Distilled water; 8) 10% ethanol solution; 9) Film 1; and 10) Film 2. In experimental groups 1-6, carvacrol and thymol (free or incorporated in two different biodegradable film formulations) were evaluated at the same concentration (5.0 mg/mL). Each group of ticks was immersed in their respective solutions for five minutes. The results of the tests on larvae showed that the Film 1 + thymol and Film 2 + carvacrol formulations had the lowest lethal concentrations (0.076 and 0.255 mg/mL, respectively), values up to 9.0-fold lower than the monoterpenes tested outside the formulation. Carvacrol and thymol at the concentrations tested were effective in controlling engorged females with a percentage of 32.2% and 63.8%, respectively. When incorporated into biodegradable film formulations, these monoterpenes showed much greater efficacy. Film 1 + carvacrol and Film 2 + carvacrol with control percentages of 71.6% and 97.2%, respectively, while the formulations Film 1 + thymol and Film 2 + thymol showed values of 96.9% and 100.0%. The tick control activity of the biopolymer formulations with thymol and carvacrol was demonstrated through the high mortality rates of larvae and engorged females of the tick R. microplus. Therefore, the results obtained indicate that these formulations have great potential for tick control mainly because of the percentage of control up to 100% in engorged females in in vitro tests.


Subject(s)
Acaricides , Cymenes , Rhipicephalus , Female , Animals , Cattle , Thymol/pharmacology , Terpenes/pharmacology , Zea mays , Starch/pharmacology , Plant Breeding , Monoterpenes/pharmacology , Acaricides/pharmacology , Ethanol/pharmacology , Larva
15.
Chem Biodivers ; 21(5): e202302115, 2024 May.
Article in English | MEDLINE | ID: mdl-38415904

ABSTRACT

There is a burgeoning focus on utilizing the antifungal and antioxidant properties of essential oils derived from various plants as a modern and natural approach to combat the growth of fungi that contaminate food. In this study, we used essential oils extracted from Thymus daenensis Celak. subsp. daenensis to address three mycotoxin-producing species of Aspergillus, specifically A. flavus, A. parasiticus, and A. niger, all of which are recognized contaminants of food and agricultural products. Concurrently, the antioxidant properties of the essential oils were evaluated, revealing their noteworthy role in the antifungal activity. Essential oils were derived from T. daenensis subsp. daenensis was observed to have a significant inhibitory effect on all three species of Aspergillus, as evidenced by the minimum inhibitory concentration (MIC) ranging from 575 to 707 ppm and the half-maximal inhibitory concentration (IC50) ranging from 237 to 280 ppm. These results confirm the strong antifungal activity of the essential oils. Furthermore, the essential oil exhibited free radical scavenging activity, resulting in an EC50 value of 37.1 µg/ml. In summary, T. daenensis subsp. daenensis essential oil demonstrated a competitive advantage over other similar plants and synthetic antibiotics. This indicates the promising potential of this essential oil as a natural antifungal agent to control Aspergillus growth and mycotoxin contamination. It offers an alternative or complementary approach to conventional antifungal agents and could be a valuable addition to the arsenal of natural remedies to address fungal contamination in food and agricultural products.


Subject(s)
Antifungal Agents , Aspergillus , Free Radical Scavengers , Microbial Sensitivity Tests , Oils, Volatile , Thymol , Thymus Plant , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Aspergillus/drug effects , Aspergillus/chemistry , Thymus Plant/chemistry , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Antifungal Agents/isolation & purification , Free Radical Scavengers/pharmacology , Free Radical Scavengers/chemistry , Thymol/pharmacology , Thymol/chemistry , Monoterpenes/pharmacology , Monoterpenes/chemistry , Monoterpenes/isolation & purification
16.
Int J Nanomedicine ; 19: 1225-1248, 2024.
Article in English | MEDLINE | ID: mdl-38348173

ABSTRACT

Purpose: Acne vulgaris is one of the most prevalent dermal disorders affecting skin health and appearance. To date, there is no effective cure for this pathology, and the majority of marketed formulations eliminate both healthy and pathological microbiota. Therefore, hereby we propose the encapsulation of an antimicrobial natural compound (thymol) loaded into lipid nanostructured systems to be topically used against acne. Methods: To address this issue, nanostructured lipid carriers (NLC) capable of encapsulating thymol, a natural compound used for the treatment of acne vulgaris, were developed either using ultrasonication probe or high-pressure homogenization and optimized using 22-star factorial design by analyzing the effect of NLC composition on their physicochemical parameters. These NLC were optimized using a design of experiments approach and were characterized using different physicochemical techniques. Moreover, short-term stability and cell viability using HaCat cells were assessed. Antimicrobial efficacy of the developed NLC was assessed in vitro and ex vivo. Results: NLC encapsulating thymol were developed and optimized and demonstrated a prolonged thymol release. The formulation was dispersed in gels and a screening of several gels was carried out by studying their rheological properties and their skin retention abilities. From them, carbomer demonstrated the capacity to be highly retained in skin tissues, specifically in the epidermis and dermis layers. Moreover, antimicrobial assays against healthy and pathological skin pathogens demonstrated the therapeutic efficacy of thymol-loaded NLC gelling systems since NLC are more efficient in slowly reducing C. acnes viability, but they possess lower antimicrobial activity against S. epidermidis, compared to free thymol. Conclusion: Thymol was successfully loaded into NLC and dispersed in gelling systems, demonstrating that it is a suitable candidate for topical administration against acne vulgaris by eradicating pathogenic bacteria while preserving the healthy skin microbiome.


Subject(s)
Acne Vulgaris , Anti-Infective Agents , Nanostructures , Humans , Thymol/pharmacology , Drug Carriers/chemistry , Lipids/chemistry , Nanostructures/chemistry , Anti-Infective Agents/pharmacology , Gels/chemistry , Particle Size
17.
Int J Biol Macromol ; 263(Pt 2): 130338, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38387626

ABSTRACT

Thymol (Th) and d-limonene (L) exhibit low stability and are prone to oxidation when exposed to air, light, humidity, and high temperatures. This study examined the coencapsulation of Th and L into Ferula assafoetida gum (AFG) microparticles. Scanning electron microscope (SEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and thermogravimetric analyzer (TGA) were done to characterize the obtained complexes. Furthermore, the encapsulation efficiency, antibacterial properties, cytotoxicity, and anticancer properties of both the free and encapsulated forms of L and Th were measured. For all samples, by increasing the percentage of bioactive compound (L, Th, and L-Th) from 2.5 to 5 % w/w, the EE was increased. FTIR and XRD analysis results demonstrated that Th and L were successfully incorporated into the AFG. Additionally, thermogravimetric analysis showed that in the thermal graphs of all samples, the first weight loss occurred between 30 °C and 160 °C, which was due to the evaporation of water. In the free L and Th graph, a sharp reduction peak was observed in which 80 % of compounds were lost. These reduction peaks disappeared in the thermal graphs of L: AFG and Th: AFG revealing that the thermal stability of Th and L was significantly increased upon their incorporation into the AFG. The inclusion of Th into the AFG also led to an increase in its antibacterial activity, while L exhibited acceptable antibacterial activity, albeit not as high as Th. Additionally, according to the MIC results, Th: AFG had the best antibacterial activity among all compounds, especially on gram-positive bacteria. According to the result of the MTT assay, there was a significant difference between the IC50 of free Th (123.4 µg/ml) and Th: AFG (2312 µg/ml), and free L (1762 µg/ml) and L: AFG (2480 µg/ml) showing that encapsulated Th and L into the AFG has decreased the cytotoxicity of free compounds against L929 cell line. Also, Th: AFG had the best anticancer activity against Hella and CT26 cell lines among all compounds. Finally, the flow cytometry analysis demonstrated that the encapsulated particles effectively eliminated cancer cells. The outcomes imply that AFG can be employed as a suitable delivery system to enhance the use of Th and L into the food and pharmaceutical industries.


Subject(s)
Anti-Infective Agents , Ferula , Thymol/pharmacology , Limonene , Ferula/chemistry , Anti-Infective Agents/pharmacology , Anti-Bacterial Agents/pharmacology
18.
Braz J Microbiol ; 55(1): 689-698, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38227116

ABSTRACT

The use of fungicides in the postharvest treatment of mangoes has been widespread due to the incidence of pathogens, but awareness of the health risks arising from their use has increased, driving the search for more sustainable treatments. This study aimed to evaluate the activity of antifungal treatment of seven essential oils (EO) against four fungi that cause postharvest diseases in mangoes and define the minimum inhibitory concentration (MIC) and chemical composition, analyzed by gas chromatography (GC-MS). The results showed that the EOs of oregano, rosemary pepper, cinnamon bark, and clove inhibited 100% of the mycelial growth of the studied pathogens, with MIC ranging from 250 to 2000 µL.L-1. The main compound found in oregano was carvacrol (69.1%); in rosemary and pepper oil, it was thymol (77.2%); cinnamaldehyde (85.1%) was the main constituent of cinnamon bark, and the eugenol (84.84%) in cloves. When evaluating the antifungal activity of these compounds, thymol and carvacrol showed greater inhibitory activity against fungi. Therefore, this study showed the great potential of oregano, clove, rosemary pepper, and cinnamon bark essential oil as alternative treatments to synthetic fungicides in controlling postharvest diseases in mangoes.


Subject(s)
Cymenes , Fungicides, Industrial , Mangifera , Oils, Volatile , Thymol/pharmacology , Antifungal Agents/pharmacology , Fungicides, Industrial/pharmacology , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Fungi , Microbial Sensitivity Tests
19.
Mol Biol Rep ; 51(1): 61, 2024 Jan 03.
Article in English | MEDLINE | ID: mdl-38170326

ABSTRACT

BACKGROUND: Breast adenocarcinoma cells (MCF-7) are characterized by the overexpression of apoptotic marker genes and proliferative cell nuclear antigen (PCNA), which promote cancer cell proliferation. Thymol, derived from Nigella sativa (NS), has been investigated for its potential anti-proliferative and anticancer properties, especially its ability to suppress Cyclin D1 and PCNA expression, which are crucial in the proliferation of cancer cells. METHODS: The cytotoxicity of thymol on MCF-7 cells was assessed using 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) and lactate dehydrogenase (LDH) release methods. Thymol was tested at increasing concentrations (0-1000 µM) to evaluate its impact on MCF-7 cell growth. Additionally, Cyclin D1 and PCNA gene expression in thymol-treated and vehicle control groups of MCF-7 were quantified using real-time Polymerase Chain Reaction (RT-qPCR). Protein-ligand interactions were also investigated using the CB-Dock2 server. RESULTS: Thymol significantly inhibited MCF-7 cell growth, with a 50% inhibition observed at 200 µM. The gene expression of Cyclin D1 and PCNA was down-regulated in the thymol-treated group relative to the vehicle control. The experimental results were verified through protein-ligand interaction investigations. CONCLUSIONS: Thymol, extracted from NS, demonstrated specific cytotoxic effects on MCF-7 cells by suppressing the expression of Cyclin D1 and PCNA, suggesting its potential as an effective drug for MCF-7. However, additional in vivo research is required to ascertain its efficacy and safety in medical applications.


Subject(s)
Breast Neoplasms , Nigella sativa , Humans , Female , Proliferating Cell Nuclear Antigen/genetics , Proliferating Cell Nuclear Antigen/metabolism , MCF-7 Cells , Breast Neoplasms/genetics , Thymol/pharmacology , Thymol/therapeutic use , Nigella sativa/metabolism , Antigens, Nuclear/genetics , Antigens, Nuclear/metabolism , Antigens, Nuclear/therapeutic use , Cyclin D1/genetics , Cyclin D1/metabolism , Down-Regulation , Ligands , Cell Proliferation
20.
Int J Mol Sci ; 25(2)2024 Jan 11.
Article in English | MEDLINE | ID: mdl-38256015

ABSTRACT

This study aimed to evaluate the protective action of oregano (Origanum vulgare) essential oil and its monoterpene constituents (thymol and carvacrol) in L-arginine-induced kidney damage by studying inflammatory and tissue damage parameters. The determination of biochemical markers that reflect kidney function, i.e., serum levels of urea and creatinine, tissue levels of neutrophil-gelatinase-associated lipocalin (NGAL), and kidney injury molecule-1 (KIM-1), as well as a panel of oxidative-stress-related and inflammatory biomarkers, was performed. Furthermore, histopathological and immunohistochemical analyses of kidneys obtained from different experimental groups were conducted. Pre-treatment with the investigated compounds prevented an L-arginine-induced increase in serum and tissue kidney damage markers and, additionally, decreased the levels of inflammation-related parameters (TNF-α and nitric oxide concentrations and myeloperoxidase activity). Micromorphological kidney tissue changes correlate with the alterations observed in the biochemical parameters, as well as the expression of CD95 in tubule cells and CD68 in inflammatory infiltrate cells. The present results revealed that oregano essential oil, thymol, and carvacrol exert nephroprotective activity, which could be, to a great extent, associated with their anti-inflammatory, antiradical scavenging, and antiapoptotic action and, above all, due to their ability to lessen the disturbances arising from acute pancreatic damage. Further in-depth studies are needed in order to provide more detailed explanations of the observed activities.


Subject(s)
Cymenes , Oils, Volatile , Origanum , Animals , Rats , Oils, Volatile/pharmacology , Thymol/pharmacology , Kidney , Inflammation/drug therapy , Arginine/pharmacology
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