Nootkatone (NTK) is a sesquiterpenoid found in essential oils of many species of
(Rutaceae). Considering previous reports demonstrating that NTK inhibited inflammatory signaling pathways, this study ...aimed to investigate the effects of this compound in mice models of acute and chronic inflammation. Murine models of paw edema induced by carrageenan, dextran, histamine, and arachidonic acid, as well as carrageenan-induced peritonitis and pleurisy, were used to evaluate the effects of NTK on acute inflammation. A murine model of granuloma induced by cotton pellets was used to access the impact of NTK treatment on chronic inflammation. In the acute inflammation models, NTK demonstrated antiedematogenic effects and inhibited leukocyte recruitment, which was associated with decreased vascular permeability, inhibition of myeloperoxidase (MPO), interleukin (IL)1-β, and tumor necrosis factor (TNF)-α production. In silico analysis suggest that NTZ anti-inflammatory effects may also occur due to inhibition of cyclooxygenase (COX)-2 activity and antagonism of the histamine receptor type 1 (H
). These mechanisms might have contributed to the reduction of granuloma weight and protein concentration in the homogenates, observed in the chronic inflammation model. In conclusion, NTK exerted anti-inflammatory effects that are associated with inhibition of IL1-β and TNF-α production, possibly due to inhibition of COX-2 activity and antagonism of the H1 receptor. However, further studies are required to characterize the effects of this compound on chronic inflammation.
The genus Ocimum are used in cooking, however, their essential oils are utilized in traditional medicine as aromatherapy. The present study was carried out to investigate the chemical composition and ...systemic anti-inflammatory activity of the Ocimum basilicum essential oil (EOOB) and its major component estragole, as well as its possible mechanisms of action. The Ocimum basilicum essential oil was obtained by hydrodistillation and analyzed by GC-MS. The anti-inflammatory action was verified using acute and chronic in vivo tests as paw edema, peritonitis, and vascular permeability and granulomatous inflammation model. The anti-inflammatory mechanism of action was analyzed by the participation of histamine and arachidonic acid pathways. The chemical profile analysis identified fourteen components present in the essential oil, within them: estragole (60.96%). The in vivo test results show that treatment with EOOB (100 and 50 mg/kg) and estragole (60 and 30 mg/kg) significantly reduced paw edema induced by carrageenan and dextran. The smallest doses of EOOB (50 mg/kg) and estragole (30 mg/kg) showed efficacy in the reduction of paw edema induced by histamine and arachidonic acid, vascular permeability inhibition and leukocyte emigration in the peritoneal fluid. Theses doses were capable of reducing the chronic inflammatory process. The results observed between the EOOB and estragole demonstrate efficacy in anti-inflammatory activity, however, the essential oil is more efficacious in the acute and chronic anti-inflammatory action. This study confirms the therapeutic potential of this plant and reinforces the validity of its use in popular medicine.
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•Determination of chemical finger print of EOOB by GC-MS.•Screening of activity show anti-inflammatory action of essential oil and Estragole majority compound of EOOB.•Screening of activity show anti-edematogenic action of essential oil and Estragole majority compound of EOOB.•Elucidations of mechanism of actions by histamine and arachidonic assay.
Terpinolene, a monoterpene that is naturally found in a variety of herbs, is widely used as a flavoring agent in the industry. Although it's well established in the literature that terpinolene is an ...important component of plant extracts, the biological properties and the potential therapeutic use of this compound remain poorly explored.
This work aimed to answer the following guiding question: "What are the biological activities of terpinolene demonstrated through in silico, in vitro, and in vivo assays?".
A systematic review was carried out in four electronic databases (Embase, Web of Science, Scopus, and PubMed) according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines, using the following search terms: terpinolene “AND” activity “OR” properties “OR” therapeutic “OR” treatment. This search included manuscripts published between 1960 and June 2020. Study selection was conducted by two independent reviewers according to predefined criteria.
The initial search found a total of 2449 articles. However, only 57 of them were selected as they met the inclusion criteria and answered the guiding question. The analysis of these studies indicated that terpinolene presents a series of biological effects, from which the antioxidant, larvicide, and insecticide activities stand out. Despite the evidence demonstrating that terpinolene has the potential to be used in a broad pharmacological context, the mechanisms underlying its cellular and molecular effects remain to be better elucidated. In addition, the in vivo efficacy and safety of the administration of this compound have been poorly evaluated through either preclinical and clinical trials. Therefore, this study highlights the importance of characterizing the biological aspects and mechanisms of action of this natural compound.
The data summarized in the present systematic review demonstrates the pharmacological potential of terpinolene. Nevertheless, most studies included in this review provide a superficial characterization of terpinolene biological effects and therefore, further research elucidating its mechanism of action and potential therapeutic benefits through preclinical and clinical trials are required. Nevertheless, due to its wide range of different biological activities, terpinolene will certainly attract the interest of scientific research, which could significantly contribute to the development of new products with both therapeutic and environmental applications.
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Due to the increase in fungal resistance to existing drugs, a need exists to search for new antifungals. This study aimed to evaluate the antifungal activity of α, β, and δ-damascone and inclusion ...complexes with β-cyclodextrin against different Candida spp. The inclusion complex of β-damascone was prepared by the co-evaporation method using three molar proportions (1:1; 2:1; 3:1 (βDA-βCD)) and analyzed using Fourier transform infrared spectroscopy (FTIR). Standard
Candida albicans
(CA INCQS 40,006),
Candida krusei
(CK INCQS 40,095), and
Candida tropicalis
(CT INCQS 40,042) strains were used to evaluate antifungal activity. The substances were tested individually or in association with fluconazole (FCZ). The IC
50
and cell viability curve constructions were performed using the microdilution method. The minimum fungicidal concentration (MFC) was determined by the subculture method in a solid medium. The α, β, and δ-DA isolated or in combination with fluconazole (FCZ) showed significant antifungal activity. β-damascone showed effective complexation in the three molar proportions assayed; however, none of the inclusion complexes was demonstrated clinically significant effects against the fungal tested. Then, all compounds have shown promising antifungal activities; however, in vivo assays are necessary to have therapeutical application in the future.
Cyclodextrins (CDs) are cyclic oligosaccharides can enhance the bioavailability of drugs. Ocimum basilicum is an aromatic plant found in Brazil used in culinary. The essential oil of this plant ...presents anti-edematogenic and anti-inflammatory activities in acute and chronic inflammation. The aim of this study was to investigate the anti-inflammatory effects of the essential oil obtained from O. basilicum complexed with β – cyclodextrin (OBEO/β-CD) in mice. The complexation with β-cyclodextrin (β-CD) was performed by different methods and analyzed by differential scanning calorimetry (DSC), thermogravimetry (TG) and scanning electron microscopy (SEM). The anti-inflammatory activity was evaluated using mice models of paw edema induced by carrageenan, dextran, histamine and arachidonic acid (AA); vascular permeability and peritonitis induced by carrageenan and granuloma induced by cotton block introduction. The DSC, TG and SEM analysis indicated that the OBEO was successfully complexed with β-CD. The oral administration of OEOB/β-CD prevented paw edema formation by decreasing vascular permeability in vivo, inhibited leukocyte recruitment to the peritoneal cavity, and inhibited granuloma formation in mice. Our results indicate that conjugation with β-CD improves the anti-inflammatory effects of OBEO in mice models of acute and chronic inflammation, indicating that this complex can be used in anti-inflammatory drug development.
Antiedematogenic and Analgesic Activities of Abietic Acid in Mice Lima Silva, Maria Gabriely; Santos da Silva, Lucas Yure; Torres Pessoa, Renata ...
Chemistry & biodiversity,
December 2023, 2023-Dec, 2023-12-00, 20231201, Letnik:
20, Številka:
12
Journal Article
Recenzirano
Odprti dostop
Exacerbated inflammatory responses to harmful stimuli can lead to significant pain, edema, and other complications that require pharmacological intervention. Abietic acid (AA) is a diterpene found as ...a significant constituent in pine species, and evidence has identified its biological potential. The present study aimed to evaluate abietic acid‘s antiedematogenic and anti‐inflammatory activity in mice. Swiss mice (Mus musculus) weighing 20–30 g were treated with AA at 50, 100, and 200 mg/kg. The central nervous system (CNS) effects were evaluated using open‐field and rotarod assays. The antinociceptive and anti‐inflammatory screening was assessed by the acetic acid and formalin tests. The antiedematogenic activity was investigated by measuring paw edema induced by carrageenan, dextran, histamine, arachidonic acid, and prostaglandin, in addition to using a granuloma model. The oral administration of abietic acid (200 mg/Kg) showed no evidence of CNS effects. The compound also exhibited significant antiedematogenic and anti‐inflammatory activities in the carrageenan and dextran models, mostly related to the inhibition of myeloperoxidase (MOP) activity and histamine action and, to a lesser extent, the inhibition of eicosanoid‐dependent pathways. In the granuloma model, abietic acid‘s effect was less expressive than in the acute models investigated in this study. In conclusion, abietic acid has analgesic and antiedematogenic activities related to anti‐inflammatory mechanisms.
Abietic acid is a diterpene found in resins mainly from diverse species of genus Pinus. The present study evaluated the antibacterial and inhibitory effect against the NorA and MepA efflux pump of ...Staphylococcus aureus by abietic acid using in vitro and in silico assays. The microdilution bacterial assay was used to evaluate antibacterial activity in standard bacteria (SA 25923 and EC 25922) and clinical isolates bacteria multiresistant (SA-10 and EC-06). Their association with antibiotics ampicillin, gentamicin, and ciprofloxacin was also estimated. Staphylococcus aureus (SA-1199B and SA-K2068) was used with a NorA and MepA pump machine, respectively, to verify the inhibitory effect using MIC methodology proposed by CLSI and Ethidium Bromide, an indicator of an efflux pump. Molecular dynamics and molecular docking calculations were used to evaluate and validate the interaction of abietic acid with NorA and MepA efflux pumps. The results demonstrated a significate reduction of MIC values to EC 25922 and SA 10 and showed a synergistic effect when combined with increased gentamicin susceptibility against multiresistant strains. The abietic acid showed direct activity against Staphylococcus aureus overexpressing gene of efflux pump, demonstrating the possibility of interference in the efflux pump NorA (SA 1199B) and MepA (SA K2068) mediated by hydrogen bonds and hydrophobic interactions. Together, these findings are promisors validating the potential antimicrobial activity and the possibility of using abietic acid as antibiotic adjuvant resistance breakers (ARBs) to treat infections caused by multiresistant bacteria. However, other studies are necessary to confirm this potential using the in vivo model.
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•The abietic acid demonstrated inhibitory effect against EP by in silico assays.•The abietic acid had synergic effects with different antibiotics.•The abietic acid is a potential break antibiotic resistance (BRA) compound class.
The increasing antifungal resistance rates against conventional drugs reveal the urgent need to search for new therapeutic alternatives. In this context, natural bioactive compounds have a critical ...role in antifungal drug development. Since evidence demonstrates that abietic acid, a diterpene found in Pinus species, has significant antimicrobial properties, this study aimed to evaluate the antifungal activity of abietic acid against Candida spp and its ability to potentiate the activity of fluconazole. Abietic acid was tested both individually and in combination with fluconazole against Candida albicans (CA INCQS 40006), Candida krusei (CK INCQS 40095), and Candida tropicalis (CT INCQS 40042). The microdilution method was used to determine the IC50 and the cell viability curve. Minimum Fungicidal Concentration (MFC) was determined by subculture in a solid medium. The plasma membrane permeability was measured using a fluorescent SYTOX Green probe. While the IC50 of the drugs alone ranged between 1065 and 3255 μg/mL, the IC50 resulting from the combination of abietic acid and fluconazole ranged between 7563 and 160.1 μg/mL. Whether used in combination with fluconazole or isolated, abietic acid exhibited Minimum Fungicidal Concentration (MFC) values exceeding 1024 μg/mL against Candida albicans, Candida krusei and Candida tropicalis. However, it was observed that the antifungal effect of fluconazole was enhanced when used in combination with abietic acid against Candida albicans and Candida tropicalis. These findings suggest that while abietic acid alone has limited inherent antifungal activity, it can enhance the effectiveness of fluconazole, thereby reducing antifungal resistance.
The species Croton rhamnifolioides, belonging to the Croton genus, is known in ethnomedicine as “quebra faca” and is used in the treatment of stomach pain, vomiting and fever. This study aims to ...evaluate the anti-edematogenic and anti-inflammatory effect of Croton rhamnifolioides leaf essential oil (OEFC) and its major constituent: 1,8-cineole (eucalyptol). The essential oil was extracted from fresh leaves through a hydrodistillation system. The chemical analysis was determined by gas chromatography-mass spectrometry (GC–MS). The acute anti-inflammatory activity was determined from the models of: ear edema by the single application of croton oil, paw edema induced by: carrageenan, dextran, histamine and arachidonic acid, while vascular permeability was determined by Evans blue extravasation and chronic anti-inflammatory activity by granuloma induction using the implantation of cotton pellets. The GC–MS results identified and quantified 11 constituents, with the major component being 1,8-cineole (41.33%). The OEFC (20mg/mL) and 1,8-cineole (8.26mg/mL) significantly reduced the edema induced by croton oil by 42.1 and 34.9%, respectively. The OEFC (25, 50, 100 and 200mg/kg) and 1,8-cineole (10.33, 20.66, 41.33 and 82.66mg/kg) statistically reduced paw edema induced by carrageenan, dextran as well as vascular permeability (protein extravasation). The OEFC (25mg/kg) and 1,8-cineole (10.33mg/kg) demonstrated efficacy in reducing edema induced by histamine and arachidonic acid and granuloma. In conclusion, the OEFC and 1,8-cineole have anti-inflammatory activity in the acute and chronic phase, suggesting therapeutic potential as a source for the development of new anti-inflammatory agents.
This work aimed to analyze the chemical composition and evaluate the anti-inflammatory and antinociceptive properties of the essential oil obtained from the leaves of
Lantana montevidensis
(OEFLM) in ...mice. The chemical composition of the OEFLM was analyzed by GC–MS, and its effects on the central nervous system were determined by the open field and rotarod tests. The antinociceptive and anti-inflammatory screenings were conducted using the formalin test, as well as the acetic acid-induced abdominal contortion assay. The antinociceptive activity was assessed by the tail-flick and hot plate tests. The systemic anti-inflammatory activity was determined using models of paw edema induced by carrageenan, dextran, histamine, or arachidonic acid. The effects of the essential oil on vascular permeability and granuloma formation were also investigated. The chemical composition of the OEFLM revealed the presence of valencene (17.93%), bicyclogermacrene (16.35%), trans-caryophyllene (12.84%) and germacrene D (12.18%). The administration of OEFLM at the dose of 2000 mg/Kg caused no evident toxicity. While OEFLM (25, 50, 100, and 200 mg/kg) did not present significant anxiolytic-loke or sedative effects, it showed promising antinociceptive and anti-inflammatory activities. The results of this study indicate that the OEFLM has analgesic and anti-inflammatory activities in animal models by inhibiting acute and chronic inflammation.
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