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Antiinflammatory and antinociceptive effects of 1,8-cineole a terpenoid oxide present in many plant essential oils

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Abstract

1,8-Cineole (cineole), a terpenoid oxide present in many plant essential oils displays an inhibitory effect on some types of experimental inflammation in rats, i.e. paw oedema induced by carrageenan and cotton pellet-induced granuloma. Cineole also inhibits in mice, the acetic acid-induced increase in peritoneal capillary permeability and the chemical nociception induced by intraplantar formalin and intraperitoneal acetic acid. Activity was present in these tests, at an oral dose range of 100-400 mg/kg. In the formalin test, the antinociceptive effect of cineole was not reversed by pretreatment of mice with naloxone (1 mg/kg, s.c.), a mu-opioid receptor antagonist, suggesting the involvement of a non-opioid mechanism. Cineole demonstrated a significant inhibitory effect on locomotion and also potentiated the pentobarbital sleeping time in mice, indicating a plausible depressant effect on the central nervous system. The present results, when taken together with the recent reports that describe the inhibitory effects of cineole on the formation of prostaglandins and cytokines by stimulated monocytes in vitro, may provide additional evidence for its potential beneficial use in therapy as an antiinflammatory and analgesic agent.

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... Similar results were observed in a study using the essential oil from the leaves of P. brownianum at a concentration of 200 mg/kg, which was effective in reducing contortions by 41.79% (Souza et al. 2019). In a study by Santos and Rao (2000) using 1,8-cineole, a major compound in PgEO, the compound at a concentration of 200 mg/kg could reduce abdominal contortions by 53% compared with the control group. ...
... have been proven to be efficient in inhibiting carrageenan-induced paw edema; for example, the essential oil obtained from P. guineense leaves when tested at concentrations of 30, 100, and 300 mg/kg showed a reduction of 48.48, 51.03, and 59.46%, respectively (Nascimento et al. 2018). Furthermore, 1,8-Cineole showed an anti-edematogenic effect, and at a dose of 400 mg/kg, it reduced edema by 46% (Santos and Rao 2000). Thus, it is suggested suggest that the anti-edematogenic activity of PgEO can be Fig. 3 Antinociceptive effect of P. glaziovianum essential oil (PgEO) in the tail-immersion assay. ...
... Nal, Naloxone (2 mg/kg); Glib, Glibenclamide (5 mg/kg); Atro, Atropine (1 mg/ kg); Yoh, Yohimbine (1 mg/kg); Praz: Prazosin (1 mg/kg). Values represent the mean ± SEM. *p < 0.001 compared with control, oneway analysis of variance (ANOVA) followed by Dunnett's test Santos and Rao (2000) reported that 1,8-cineol at a dose of 400 mg/kg reduced up to 37% of the granuloma formation induced by cotton pellets after 7 days of treatment. They also reported that both the wet weight and dry weight of the granulation tissue around the pellets were significantly lower in the group treated with 1,8-cineol than in the group treated with indomethacin. ...
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Plants of the genus Psidium have been employed in “in natura” consumption and agroindustry, and owing to the diversity of phytochemicals, the development of new pharmaceutical forms has received remarkable research interest. In this study, the essential oil obtained from Psidium glaziovianum (PgEO) leaves were evaluated antinociceptive and anti-inflammatory activities were evaluated in mouse models. Initially, PgEO was characterized by gas chromatography–mass spectrometry and gas chromatography with flame ionization detection, and the profile was dominated by sesquiterpene compounds. In the evaluation of acute antinociceptive activity (abdominal contortions induced by acetic acid, formalin, tail immersion, and hot plate tests), PgEO promoted a reduction in nociception in the chemical and thermal models. Additionally, the potential underlying mechanism was investigated using pain pathway blockers, and the results revealed a combined action of opioidergic and muscarinic pathways. The anti-inflammatory potential was confirmed by anti-edematogenic action, reduced cell migration, pro-inflammatory cytokine production, and granuloma formation in chronic processes. This study provides evidence that PgEO can be effective for the treatment of pain and acute and chronic inflammation.
... Eucalyptol (1, 8-cineol) is present in Cannabis, although its levels vary depending on the growth conditions (Brenneisen, 2007;Naz et al., 2017). When administered either orally or intraperitoneally, eucalyptol produced antinociception on the hot plate and tail-flick tests (Liapi et al., 2007), alleviated acute and chronic inflammatory pain (Santos and Rao, 2000;Caceres et al., 2017;Yin et al., 2020) and alleviated visceral pain induced by acetic acid (Santos and Rao, 2000;Liu et al., 2013). Eucalyptol-induced antinociception was not reversed by naloxone (Santos and Rao, 2000) and was not present in TRPM8 knockout mice (Caceres et al., 2017), suggesting a nonopioid mechanism of action. ...
... Eucalyptol (1, 8-cineol) is present in Cannabis, although its levels vary depending on the growth conditions (Brenneisen, 2007;Naz et al., 2017). When administered either orally or intraperitoneally, eucalyptol produced antinociception on the hot plate and tail-flick tests (Liapi et al., 2007), alleviated acute and chronic inflammatory pain (Santos and Rao, 2000;Caceres et al., 2017;Yin et al., 2020) and alleviated visceral pain induced by acetic acid (Santos and Rao, 2000;Liu et al., 2013). Eucalyptol-induced antinociception was not reversed by naloxone (Santos and Rao, 2000) and was not present in TRPM8 knockout mice (Caceres et al., 2017), suggesting a nonopioid mechanism of action. ...
... When administered either orally or intraperitoneally, eucalyptol produced antinociception on the hot plate and tail-flick tests (Liapi et al., 2007), alleviated acute and chronic inflammatory pain (Santos and Rao, 2000;Caceres et al., 2017;Yin et al., 2020) and alleviated visceral pain induced by acetic acid (Santos and Rao, 2000;Liu et al., 2013). Eucalyptol-induced antinociception was not reversed by naloxone (Santos and Rao, 2000) and was not present in TRPM8 knockout mice (Caceres et al., 2017), suggesting a nonopioid mechanism of action. Eucalyptol decreased TRPV1 expression and expression of various inflammatory cytokines in animals with inflammation (Caceres et al., 2017;Yin et al., 2020). ...
Article
Cannabis has been used for centuries for its medicinal properties. Given the dangerous and unpleasant side effects of existing analgesics, the chemical constituents of Cannabis have garnered significant interest for their antinociceptive, anti-inflammatory and neuroprotective effects. To date, Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD) remain the two most widely studied constituents of Cannabis in animals. These studies have led to formulations of THC and CBD for human use; however, chronic pain patients also use different strains of Cannabis (sativa, indica and ruderalis) to alleviate their pain. These strains contain major cannabinoids, such as THC and CBD, but they also contain a wide variety of cannabinoid and noncannabinoid constituents. Although the analgesic effects of Cannabis are attributed to major cannabinoids, evidence indicates other constituents such as minor cannabinoids, terpenes and flavonoids also produce antinociception against animal models of acute, inflammatory, neuropathic, muscle and orofacial pain. In some cases, these constituents produce antinociception that is equivalent or greater compared to that produced by traditional analgesics. Thus, a better understanding of the extent to which these constituents produce antinociception alone in animals is necessary. The purposes of this review are to (1) introduce the different minor cannabinoids, terpenes, and flavonoids found in Cannabis and (2) discuss evidence of their antinociceptive properties in animals.
... The anti-inflammatory activity of EOs can be attributed not only to their antioxidant properties but also to interactions with signaling cascades involving cytokines and transcriptional regulatory factors and in the expression of pro-inflammatory genes [126,142]. Some studies carried out in animal models with terpenes present in EOs, such as linalool, limonene, myrcene, 1,8-cineole, demonstrated that these compounds showed analgesic activity [143][144][145][146][147][148][149][150][151][152]. The analgesic and anti-inflammatory potential of OEs are preferentially attributed to the high content of terpene compounds [143,145,146,[153][154][155][156] as well as to the synergetic effect of minor components that can influence the pharmacokinetics and bioavailability of compounds with pharmacological action [157]. ...
... Regarding the species of the genus Thymus, the most studied species is T. vulgaris, being widely recognized for the potential of its EOs and their major components as anti-inflammatory agents [159][160][161]. On the other hand, the literature reports that the monoterpenes 1,8-cineole, anethole and fenchone, major components present in the EOs of C. nepeta and T. mastichina may be also responsible for the anti-inflammatory effect [77,143,144,[147][148][149][150][151][152]162]. ...
Book
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Over the years, natural products such as essential oils have been gaining more and more prominence due to their perceived health benefits. Plants rich in essential oils represent a viable source of biomolecules for use in the most varied human activities, such as agricultural, cosmetic, and pharmaceutical applications. Essential oils are natural volatile fractions extracted from aromatic plants that are formed by classes of substances such as fatty acid esters, mono and sesquiterpenes, phenylpropanoids, and aldehyde alcohols, and in some cases, aliphatic hydrocarbons, among others. In this context, this book includes twelve chapters that present new information on the extraction and application of essential oils in various industrial segments. It is divided into three sections that discuss the general concepts of essential oils and techniques for their extraction, topics in food science and technology, and essential oils and their pharmacological properties in various activities and applications.
... albumin-induced paw edema, xylene-induced ear edema, and formalin-induced arthritic inflammation in rats (Rao and Raju, 2009;Arora and Arora, 2016). The essential oils obtained from the bark, leaf, and seed of G. pentaphylla are enriched with numerous bioactive constituents (Ahmed et al., 2000), and some of them have well-documented anti-inflammatory activity such as borneol (12) (Zou et al., 2017), 1, 8-cineole (13) (Santos and Rao, 2000), α-pinene (14) (Kim DS. et al., 2015;Özbek and Yılmaz, 2017), caryophyllene (15), caryophyllene oxide (Tung et al., 2008), and spathulenol (16) ( Figure 6) (do Nascimento et al., 2018). In studies in China, a number of prenylated sulfur-containing amides and a phenolic glycoside (tachioside) (17) (Figure 6) isolated from this plant also exhibited anti-inflammatory activity via downregulation of nitric oxide (NO) production in LPSstimulated RAW 264.7 macrophages (Tian et al., 2014;Nian et al., 2020). ...
... Santos and Rao (2000);Souza et al. (2003); Tung et al. (2008); Miguel (2010); de Cássia da Silveira et al. (2014); Kim et al. (2015b); Özbek and Yılmaz ...
Article
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Inflammatory diseases are considered major threats to human health worldwide. In Bangladesh, a number of medicinal plants have been used in traditional medicine from time immemorial in the treatment of diverse diseases, including inflammatory disorders. This assignment aims at providing the status of the medicinal plants of Bangladesh which are traditionally used in the management of inflammatory disorders and are investigated for their anti-inflammatory prospects using different preclinical studies and future research directions. The information of medicinal plants assembled in this review was obtained from a literature search of electronic databases such as Google Scholar, PubMed, Scopus, Web of Science and ScienceDirect up to December, 2020 from publications on plants investigated for their anti-inflammatory activities, in which the place of plant sample collection was identified as Bangladesh. Keywords for primary searches were “anti-inflammatory,” “Bangladeshi,” and “medicinal plants.” Criteria followed to include plant species were plants that showed significant anti-inflammatory activities in 1) two or more sets of experiments in a single report, 2) same or different sets of experiments in two or more reports, and, 3) plants which are traditionally used in the treatment of inflammation and inflammatory disorders. In this study, 48 species of medicinal plants have been reviewed which have been used in traditional healing practices to manage inflammatory disorders in Bangladesh. The mechanistic pathways of the in vivo and in vitro study models used for the evaluation of anti-inflammatory properties of plant samples have been discussed. Selected plants were described in further detail for their habitat, anti-inflammatory studies conducted in countries other than Bangladesh, and anti-inflammatory active constituents isolated from these plants if any. Medicinal plants of Bangladesh have immense significance for anti-inflammatory activity and have potential to contribute toward the discovery and development of novel therapeutic approaches to combat diseases associated with inflammation. However, the plants reviewed in this article had chiefly undergone preliminary screening and require substantial investigations including identification of active molecules, understanding the mechanism of action, and evaluation for safety and efficacy to be followed by the formulation of safe and effective drug products.
... As already mentioned, PL extract GC-MS data demonstrated a predominance of terpenes (monoterpenes and sesquiterpenes). In this regard, previous studies showed that sesquiterpenes owned anti-inflammatory properties [78,79], and the contained-monoterpene in plant-derived EO effectively inhibited carrageenan-induced edema and neutrophil migration [78]. Cell migration is a highly integrated, multi-step process that plays an important role in the progression of various diseases, including cancer, atherosclerosis, and arthritis. ...
... As already mentioned, PL extract GC-MS data demonstrated a predominance of terpenes (monoterpenes and sesquiterpenes). In this regard, previous studies showed that sesquiterpenes owned anti-inflammatory properties [78,79], and the contained-monoterpene in plant-derived EO effectively inhibited carrageenan-induced edema and neutrophil migration [78]. Cell migration is a highly integrated, multi-step process that plays an important role in the progression of various diseases, including cancer, atherosclerosis, and arthritis. ...
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Green chemistry is emerging as a useful tool for producing valuable chemicals from biomass. However, extracted compounds need to be tested for safety, quality, and efficacy before their use in humans. Here we investigate the chemical composition and biological effects of leaves Pistacia lentiscus L . essential oil (EO) extract obtained with supercritical carbon dioxide (SCCO 2 ). Extract's phytoconstituents profiling was performed by GC-MS/MS, while antioxidant activity was evaluated on human primary endothelial cells (ECs) using the reactive oxygen species (ROS) probe H 2 DCFDA. Potentil extract toxicity and protective effect against H 2 O 2 -induced oxidative stress were investigated using LDH-leakage and BrdU-proliferation tests. Extract’s effect on ECs migration was determined by trans-well assay. Terpenes represented the main extraction process fraction yielding 0.14% of EO. Germacrene D (11.18%), delta-cadinene (10.54%), and alpha-pinene (8.7%) were the most abundant OE molecules. Challenged with ECs, increasing extract concentrations failed to affect cell proliferation or promote cell death. ROS assessment in unstressed and H 2 O 2 -treated ECs demonstrated an extract dose-dependent antioxidant activity. The exposure of H 2 O 2 -treated ECs to increasing extract concentrations dose-dependently rescued cells from the H 2 O 2 -induced impairments of cell proliferation and death. Extract was able to significantly counteract fetal calf serum-induced ECs migration. For the first time, we report that a SCCO 2 extract obtained from PL leaves is safe on ECs and may be a useful source of valuable compounds with vasculoprotective properties.
... In mice, eucalyptol demonstrated a synergic action with oseltamivir for the treatment of influenza A , and provided crossprotection against the influenza virus if co-administered with the vaccination . Finally, eucalyptol has a Transient Receptor Potential (TRP)-mediated activity, exerting an antinociceptive effect with inhibition of pain perception, as summarized in Table 2 (Bautista et al., 2007;Haeseler et al., 2002;Liedtke and Heller, 2007;Millqvist et al., 2013;Santos and Rao, 2000;Sherkheli et al., 2009;Takaishi et al., 2012). ...
... Moreover, menthol was found to increase the ciliary beat frequency of human nasal epithelial cells, which can contribute to mechanical defenses against microorganisms (Neher et al., 2008). The TRP-mediated activity of menthol is summarized in Table 2 (Bautista et al., 2007;Haeseler et al., 2002;Liedtke and Heller, 2007;Millqvist et al., 2013;Santos and Rao, 2000;Sherkheli et al., 2009;Takaishi et al., 2012). ...
Article
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Introduction The involvement of the upper respiratory tract is common in COVID-19, and the majority of patients are treated at home with a mild-to-moderate form of the disease. Many approaches based on essential oils have been proposed for the symptomatic treatment of COVID-19. This work aims to outline the potential and safe evidence-based uses of essential oils and their major components for the clinical management of mild respiratory symptoms caused by uncomplicated coronavirus infections, including SARS-CoV-2. Due to their wide use, a focus on the constituents eucalyptol and menthol has been provided. Methods An overview of the scientific literature with a critical discussion of retrieved evidence and clinical recommendations. Results In general, eucalyptol and essential oils or blends whose content is rich in it, may be used as an integrative remedy for the symptomatic improvement of patients with mild and uncomplicated infections caused by coronaviruses. Menthol is not recommended in patients with COVID-19, due to a potential reduction of the self-perception of dyspnea, which can lead infected patients to underestimate the actual disease severity and to delay medical attention. Discussion Based on available evidence, symptomatic remedies for COVID-19, such as essential oils and their isolated compounds, can be useful, but are not an alternative to standard medical therapy and do not exempt patients from following precautionary measures issued by health authorities. Clinical recommendations on the appropriate use of essential oils for the management of upper airway symptoms of COVID-19 are provided. Further studies on the topic are advised.
... The antinociceptive effect of Euca has been previously reported in a pain model (Santos, Rao, 2000). In a model of gouty arthritis, analgesic activity has been associated with the downregulation of cell migration in joint tissues (Yin et al., 2020). ...
... Importantly, besides their antioxidant activity, these molecules are implicated in the regulation of GIT [39]. Indeed, anti-inflammatory activity of cineole through the inhibition of inflammatory mediators releasing was previously demonstrated [40,41]. In fact, this terpens blockade prostaglandin and other inflammatory mediator's formation in diarrhea which may in part explain its antisecretory effect. ...
... In this study, the concentrations of IL-2 were upregulated in the serum and small intestine and the gene expression of IL-2 was also signi cantly increased in the ileum of weaned piglets, indicating a weaker intestinal barrier function in weaning piglets. In addition, both the antiin ammatory and pro-in ammatory cytokines are secreted by Th1 cells and Th2 cells [50]. In the immune response system, the Th1/Th2 dynamic balance is an important factor in maintaining immune stability [51]. ...
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A total of 40 piglets with similar body weights were selected in pairs at 21 days old and divided into the suckling group (SG: breastfed by their mothers) and weaning group (WG: weaned at 21 days old). Eight piglets from each group were randomly selected and sacrificed at 24 days (SG3 and WG3) and 28 days of age (SG7 and WG7). The growth performance, T lymphocyte subpopulations, the concentration of cytokines and immunoglobulins, and the expression of Notch2 signaling proteins were determined. The weaning caused a decrease in body weight ( P < 0.01) and the ratio of CD3 ⁺ CD4 ⁺ /CD3 ⁺ CD8 ⁺ T cells in thymus ( P < 0.05). Compared to SG3, the concentration of secretory immunoglobulin A (sIgA) in jejunum was decreased, and that of interleukin 2 (IL-2) in serum and ileum, IL-1β and IL-2 in jejunum were upregulated ( P < 0.01), while IL-10 in the small intestine was downregulated ( P < 0.05) in WG3. Weaning downregulated gene expression of IL-4 and upregulated gene expression of IL-1β, IL-12, and interferon γ (IFN-γ) in small intestine ( P < 0.05). Further, weaning downregulated protein expression of Notch2 and Hes1 but upregulated Jagged1 expression in small intestine of piglets ( P < 0.05). In summary, weaning caused an imbalance in T lymphocytes distribution, thus impairing the intestinal immune function of piglets, which might be associated with the Notch2 signaling. Furthermore, the impairment of intestinal immune barrier function was more severe at 3 days post-weaning than that at the 7 days post-weaning in piglets.
... Geraniol is repellent (Brito et al. 2015) and antitumoral (Carnesecchi et al. 2001). 1,8-cineole is decongestant and antitussive (Santos and Rao 2000). Terpineol exhibits antimicrobial effects on periodontopathic and cariogenic bacteria (Park et al 2012). ...
Article
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The use of teas made by medicinal plants is a consolidated practice in Brazil. The chemical profile of teas can be affected by the storage and handling conditions of the plant material. These conditions can cause volatilization, enzymatic degradation, hydrolysis and oxidation of the secondary metabolites, which can affect the biological properties of the teas. This paper describes how the chemical profile of basil extracts, prepared by aqueous infusion, is affected by variations on the contact time between plant material and boiling water (5, 10 20 and 30 minutes), and the use of whole and fragmented fresh leaves, that were stored according to the methods commonly used by the population: cooling and freezing (7 days). The chemical profile of the extracts was evaluated by GC-MS. The tea in which the highest number of metabolites was extracted, 15 in total. was obtained using fresh fragmented leaves with 20 minutes of infusion. In the teas prepared by using whole fresh leaves (infusion by 5 to 30 minutes) and frozen leaves (infusion by 30 minutes), 11 metabolites were observed. The teas prepared by using cooled leaves (infusion by 5 to 30 min) and dried leaves (infusion by 30 min) presented 5 metabolites each. In the tea prepared by using dried leaves, with infusion time of 5 minutes, only 2 metabolites were observed. The results indicate that the presence of pharmacological bioactive metabolites in homemade basil’s tea may vary according to the form of storage of the leaves and preparation methods of the tea.
... Sesquiterpene lactones are found in roots and leaves, and two different chemical types have been identified, with laurenobiolide and costunolide as significant components, respectively (15). The pharmacological characteristics of sesquiterpene lactones discovered in Bay leaf include the inhibition of nitric oxide generation (anti-inflammatory) (16) and an increase in the glutathione S-transferase activity in the liver (17). ...
Article
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This study aimed to evaluate the effects of Laurus Nobilis (Bay leaves) alcoholic extract on glucose, hemoglobin A1c (HbA1c), alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatinine, and urea levels; moreover, it was attempted to examine the histological changes induced in the liver and kidney among female albino rats treated with Depakene (Sodium Valproate). The L. nobilis leaves were dried in the shade, and they were then ground in mechanical processing. The resulting substance (250 gm) was processed in 70% ethanol for 24 h using a Soxhlet extractor at 45°C. Before being measured, the extract was concentrated in vacuo and stored in a vacuum desiccator until the elimination of all the solvents. In total, 20 female adult Wistar rats (230-250 g) were bred in the Animal House Lab at the University of Kufa, Faculty of Education for Girls, Kufa, Iraq. These animals were randomly divided into four groups (n=5), housed in a typical laboratory setting, and given a standard diet and water. Each animal received the treatments intraperitoneally for 30 days. The experimental groups were designed as follows: group 1 (the control) was given only physiological saline solution; group 2 received alcoholic extract of L. nobilis leaves at a dose of 150 mg/kg BW; group 3 received Depakene (Sodium Valproate) at a dose of 500 mg/kg BW; and group 4 received alcoholic extract+Depakene at a dose of 150 mg/kg BW and 500 mg/kg BW. The animals were euthanized following anaesthesia 24 h after the last day of the experiment. Heart blood samples were gathered in gel tubes, the serum was then centrifuged for 15 min at 3000 rpm to measure the biochemical parameter levels, which included glucose, HbA1C, ALT, AST, creatinine, and urea. The liver and kidney organs were removed and placed in a 10% formaldehyde solution instantly. Following fixation, they were processed as usual before being embedded in paraffin for histological analysis. Morphological changes were assessed using hematoxylin and eosin staining techniques. The recorded data showed a major drop (P<0.05) in blood glucose and HbA1c levels in group 2 which was given ethanol extract, compared to the other groups. Interestingly, the level of blood glucose and HbA1c levels reduced significantly in group 4, which was given L. nobilis+Depakene, compared to the control and the animals treated with only Depakene. Moreover, the results showed a major rise (P<0.05) in the liver enzyme among the animals treated with Depakene, compared to other groups. On the other hand, the recorded data showed a substantial drop (P<0.05) in creatinine levels in the animals treated with L. nobilis leaves extract (group 2) and group 4, compared to group 3 and the control group, respectively. However, no changes were recorded in the case of urea levels among the groups. Finally, the findings of this study showed that the ethanol extract of L. nobilis leaves was effectively reduced the adverse effects of Depakene. On the other hand, it had a significant effect on the reduction of blood glucose.
... ## indicates a statistically significant difference (P < 0.01) with the Control group free radicals in laboratory animals (El-Hadary 2015). Cineol affects inflammatory reactions by reducing the production of inflammatory agents such as IL-1β and IL-6 (Jiang et al. 2019;Kutlu et al. 2021;Santos 2000) and also increases antioxidant enzymes such as SOD (Porres-Martinez et al. 2016). In agreement with our results, Hsu et al. (2021) showed that HA leads to microglia activation, brain inflammation and IL-1β up-regulation, which are involved in the development of brain dysfunction (Hsu et al. 2021). ...
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In hepatic encephalopathy, hyperammonemia (HA) causes cognitive impairment and anxiety by causing neuroinflammation. Ibuprofen and 1,8- cineol have anti-inflammatory and antioxidant properties, respectively. The aim of this study was to evaluate the effects of ibuprofen alone and in combination with 1,8- cineol on anxiety and oxidative stress in a HA rat animal model. For this purpose, 36 rats were divided into six groups (n = 6) including the HA (received intraperitoneally (IP) ammonium acetate 2.5 mg/kg for four week), ibuprofen (induced HA rats that received 15 mg/kg, IP), cineol (induced HA rats that received 5 and 10 mg/kg, IP), Ib + cineol (induced HA rats that received 15 and 10 mg/kg, respectively, IP), and the control groups (received normal saline, IP). Except the HA group, all other groups received the aforementioned treatment for two weeks.. The Morris water maze and elevated plus maze were used to assess cognitive function and anxiety in the animals, respectively. Superoxide dismutase (SOD) activity was measured to evaluate oxidative stress. The mRNA expression levels of interleukin (IL)-6 and IL-1β was assessed by real-time PCR in the animal’s brain. The results showed a significant improvement in spatial memory and anxiety of the Ib group compared to the HA group (P < 0.01), but no significant change was observed in SOD activity (P > 0.05). There was a significant improvement in spatial memory and anxiety as well as a significant increase in SOD activity in the Ib + cineol group (P < 0.01) compared to the HA group. These results indicate that the Ib + cineol, not only improve cognitive function and reduce anxiety, also reduce oxidative stress, therefore, the simultaneous use of these two compounds may be useful in improving HA-induced cognitive disorders and anxiety.
... Eucalyptol is the main component of Artemisia argyi [11,12]. Eucalyptol has been reported to inhibit the proliferation of many cancer cells [22,23,[31][32][33]. In this study, we revealed the anti-tumor effect and mechanism of eucalyptol against human neuroblastoma SH-SY5Y cells by transcriptome sequencing. ...
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Eucalyptol (1.8-cineole), an active component in traditional Chinese medicine Artemisia argyi for moxibustion. Previous studies have shown that eucalyptol has anti-tumor effects on leukemia and colon cancer. Nonetheless, the effect and mechanism of eucalyptol on neuroblastoma remains unclear. In the present study, we intended to reveal the effect and mechanism of eucalyptol treatment on the neuroblastoma cell line SH-SY5Y through transcriptome analysis. In the group treated with eucalyptol, 566 brain genes were up-regulated, while 757 genes were down-regulated. GO function analysis showed that positive regulation of cell cycle was down-regulated in biological processes. Meanwhile, cancer-related pathways were identified in KEGG (Kyoto Encyclopedia of Genes and Genomes) enrichment analysis, including pathways in cancer, PI3K-Akt signaling pathway, cAMP signaling pathway, TGF-beta signaling pathway, Hippo signaling pathway, p53 signaling pathway, and additional pathways. Furthermore, we found a key gene, such as MYC, by constructing a network of cancer related pathways with differentially expressed genes and transcription factor analysis. In conclusion, our research indicates that MYC might play a central role in the anit-tumor mechanisms of eucalyptol.
... The search for new drugs including herbal products with a broad range of pharmacological activities and economic affordability has increased in recent years (Singh et al., 2013).Various researchers have positively evaluated and explored a broad range of pharmacological activities among them Laurus nobilis ethanolic extract has antioxidant and wound healing effect . In the treatment of gastrointestines, rheumatism, migraines, and diuretic, antimicroscopic, improving appetite and digestion are also used (Santos & Rao, 2000). The volatile laurel oils suppress tuberculosis development and stimulate immunity. ...
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The potential protective effect of alcoholic extracts of some herbs on hepatotoxicity induced by paracetamol in experimental rats. Abstract There are many plants which are used as herbs by many people such as Laurus nobilis and Elettaria cardamomum. The purpose of this study was to find out protective alcoholic Extract's effect of Laurus nobilis and Elettaria cardamomum on hepatotoxicity induced by paracetamol in experimental rats. 30 healthy adult rats of male albino weighing (150±10 g) were used and divided into 6 equal groups, one of them was kept as a negative control, Group (2): was fed on basal diet as a positive control group, All groups were fed on basal diet + orally doses of herbs as the following: (3 and 4) treated with Laurus nobilis extract 100and 200 mg/ Kg b.w. respectively ; (5 and 6) treated with Elettaria cardamomum extract 100 and 200 mg/ Kg b.w. respectively Once a day for twenty- eight days on twenty -one day, during the administration of the respective treatments, all animals of groups 2, 3, 4, 5 and 6were administered with paracetamol 400 mg/kg orally for one week. At the end of experiment, biological evaluation was calculated. Liver enzymes, bilirubin, proteins and lipid profile were determined in serum. In liver tissue (GPX, SOD, CAT, MDA and α –TNF) were determined. Livers of rats were histopathologically examined. The results showed that alcoholic extract of Laurus nobilis and cardamomum improved biological evaluation, liver functions, and antioxidant enzymes compared with positive control groups. It could be concluded that take Laurus nobilis and cardamomum have markedly protected against the harmful effects of paracetamol on liver.
... It has been shown to reduce mucus production, block inflammation through inhibiting cytokines tumor necrosis factor (TNF)-a and interleukin (IL)-1b, and produce antinociceptive effects. [40][41][42] A prospective DBRCT comparing cineole (200 mg three times per day) with placebo in 152 patients with acute nonpurulent RS, showed a statistically significant difference in symptoms-sum-scores in the cineole group, in addition to a reduction in secondary symptoms, such as headache on bending, frontal headache, nasal obstruction, and nasal secretion. 43 Mild side effects included heartburn and exanthem. ...
Article
Rhinosinusitis is characterized by inflammation of the mucosa involving the paranasal sinuses and the nasal cavity and is one of the most common and significant health care problems, with significant impairment of quality of life. Current standard conventional management of rhinosinusitis commonly uses multiple therapeutic modalities to break the cycle of chronic disease. However, to date, there is no consensus as to the optimal treatment algorithm for patients with chronic rhinosinusitis. There is a growing interest in the use of complementary and integrative medicine for the treatment of rhinosinusitis. This article update focuses on an integrative approach to rhinosinusitis.
... In this context, in the Lamiaceae family, there are a plethora of species with rich content in essential oils, which are used in popular medicine as an alternative treatment for diseases [2]. For example, the genus Hyptis is considered of great economic importance since it is composed of triterpenes [3], diterpenes [4] and sesquiterpenes [5], that are responsible for interesting antimicrobial [6,7], insecticide [8], analgesic [9][10][11], and hypnotic-sedative and antipsychotic-like activity [12]. ...
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Hyptis martiusii Benth. also known as "cidreira brava", has some activities verified in the literature, such as antiulcerogenic, antimicrobial and antiedematogenic. This study aimed to verify the anti-inflammatory and antinociceptive effect of the leaves essential oil. For the evaluation of the anti-inflammatory activity of OEHM (100 mg/kg/p.o.), models paw edema induced by dextran and histamine, peritonitis and vascular permeability were used. Regarding the anti-nociceptive activity of the OEHM, abdominal contortion tests by acetic acid, formalin, hot plate (50.75 and 100 mg/kg/p.o.), open field and mechanical plantar hyper-nociception (100 mg/ kg/p.o.) were carried out. OEHM (100 mg/kg) showed anti-inflammatory activity, being able to remarkably deducing the paw edema induced by dextran and histamine, the total number of cell leukocytes/neutrophils in peritonitis, and exudate in vascular permeability. In antinociceptive activity, the OEHM did not promote significant effect in central nervous system in the open field assay, remarkably reduced abdominal contortions (50, 75 and 100 mg/kg), the time in the formalin assay and the mechanical hyper-nociception (100 mg/kg); however, only doses between 75 and 100 mg/kg were capable of ameliorating the reponse latency time. Regarding the probable mechanism of action, the antinociceptive activity includes the participation in the activation of opioid, TRPV1, and α2-noradrenergic systems. In short, data obtained here reveal that OEHM has anti-inflammatory and antinociceptive activity, implying that its action may be involved in the mechanism of inhibition or liberation of pro-inflammatory mediators involved in pain and inflammation.
... A recent study revealed that CIN showed interesting selective inhibitory activity against acetylcholinesterase [18]. CIN is widely used in the pharmaceutical industry [24] and is also used as a condiment in food and cosmetics [25]. The oral administration of CIN (550 mg/kg bodyweight) in Wistar albino rats could restore their normal fasting blood glucose and blood lipid levels [26]. ...
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Advanced glycation end products (AGEs) are stable products produced by the reaction of macromolecules such as proteins, lipids or nucleic acids with glucose or other reducing monosaccharides, which can be identified by immunohistochemistry in the senile plaques and neurofibrillary tangles of Alzheimer’s disease (AD) patients. Growing evidence suggests that AGEs are important risk factors for the development and progression of AD. 1,8-cineole (CIN) is a monoterpenoid compound which exists in many plant essential oils and has been proven to have neuroprotective activity, but its specific effect and molecular mechanisms are not clear. In this study, AGEs-induced neuronal injury and intracerebroventricular-AGE animals as the possible models for AD were employed to investigate the effects of CIN on AD pathology as well as the molecular mechanisms involved both in vivo and in vitro. Our study demonstrated that CIN could ameliorate tau phosphorylation by down-regulating the activity of GSK-3β and reducing Aβ production by inhibiting the activity of BACE-1 both in vivo and in vitro. It is suggested that CIN has certain therapeutic value in the treatment of AD.
... Essential oils extracted from herbs, plants, and flowers are often used to manage pain, ease psychological distress, induce relaxation, and enhance well-being [1,2]. Lavender (Lavandula angustifolia) oil (LO) is an antispasmodic, anticonvulsant, antidepressant, painkilling, and carminative substance used to treat various conditions [3,4]. ...
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(1) Background: Essential oils have long been used as therapeutic agents. Lavender (Lavandula angustifolia) oil (LO) is an antispasmodic, anticonvulsant, relaxant, painkilling, and antimicrobial essential oil investigated as a natural substance for biomedical therapies. Nanoparticles have shown significant promise in improving drug delivery and efficacy. Considering these benefits, the aim of this study was to evaluate the toxicity of LO and lavender oil niosomes (LONs) in stem cells and myofibroblast models cultured in vitro. (2) Methods: Adipose tissue-derived stem cells and myometrial cells were cultured with LO or LONs at different concentrations (0, 0.016%, 0.031%, and 0.063%) and toxicity was evaluated with PrestoBlue™ and live/dead assay using calcein and ethidium homodimer. (3) Results: Cell viability was similar to controls in all groups, except in 0.063% LO for myometrial cells, which showed lower viability than the control medium. (4) Conclusion: These results suggest that both LO and LONs are safe for cell culture and may be used for pharmaceutical and biomedical therapies in future applications in regenerative medicine. View Full-Text
... Sesquiterpene lactones are found in roots and leaves, and two different chemical types have been identified, with laurenobiolide and costunolide as significant components, respectively (15). The pharmacological characteristics of sesquiterpene lactones discovered in Bay leaf include the inhibition of nitric oxide generation (anti-inflammatory) (16) and an increase in the glutathione S-transferase activity in the liver (17). ...
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This study aimed to evaluate the effects of Laurus Nobilis (Bay leaves) alcoholic extract on glucose, hemoglobin A1c (HbA1c), alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatinine, and urea levels; moreover, it was attempted to examine the histological changes induced in the liver and kidney among female albino rats treated with Depakene (Sodium Valproate). The L. nobilis leaves were dried in the shade, and they were then ground in mechanical processing. The resulting substance (250 gm) was processed in 70% ethanol for 24 h using a Soxhlet extractor at 45°C. Before being measured, the extract was concentrated in vacuo and stored in a vacuum desiccator until the elimination of all the solvents. In total, 20 female adult Wistar rats (230-250 g) were bred in the Animal House Lab at the University of Kufa, Faculty of Education for Girls, Kufa, Iraq. These animals were randomly divided into four groups (n=5), housed in a typical laboratory setting, and given a standard diet and water. Each animal received the treatments intraperitoneally for 30 days. The experimental groups were designed as follows: group 1 (the control) was given only physiological saline solution; group 2 received alcoholic extract of L. nobilis leaves at a dose of 150 mg/kg BW; group 3 received Depakene (Sodium Valproate) at a dose of 500 mg/kg BW; and group 4 received alcoholic extract+Depakene at a dose of 150 mg/kg BW and 500 mg/kg BW. The animals were euthanized following anaesthesia 24 h after the last day of the experiment. Heart blood samples were gathered in gel tubes, the serum was then centrifuged for 15 min at 3000 rpm to measure the biochemical parameter levels, which included glucose, HbA1C, ALT, AST, creatinine, and urea. The liver and kidney organs were removed and placed in a 10% formaldehyde solution instantly. Following fixation, they were processed as usual before being embedded in paraffin for histological analysis. Morphological changes were assessed using hematoxylin and eosin staining techniques. The recorded data showed a major drop (P<0.05) in blood glucose and HbA1c levels in group 2 which was given ethanol extract, compared to the other groups. Interestingly, the level of blood glucose and HbA1c levels reduced significantly in group 4, which was given L. nobilis+Depakene, compared to the control and the animals treated with only Depakene. Moreover, the results showed a major rise (P<0.05) in the liver enzyme among the animals treated with Depakene, compared to other groups. On the other hand, the recorded data showed a substantial drop (P<0.05) in creatinine levels in the animals treated with L. nobilis leaves extract (group 2) and group 4, compared to group 3 and the control group, respectively. However, no changes were recorded in the case of urea levels among the groups. Finally, the findings of this study showed that the ethanol extract of L. nobilis leaves was effectively reduced the adverse effects of Depakene. On the other hand, it had a significant effect on the reduction of blood glucose.
... Also, essential oils can be used as an antiviral drug alone or in synergy with synthetic antiviral agents (Bary and El Amraoui, 2020). In addition, they are used as dietary supplements to relieve symptoms or strengthen the immune system of affected patients; in fact, linalool, β-caryophyllene and 1,8-cineole have anti-inflammatory and anti-nociceptive activity (Klauke et al., 2014;Li et al., 2016;Peana et al., 2003;Santos and Rao, 2000). Thymol and camphor have antitussive activity (Gavliakova et al., 2013a;2013b). ...
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Context: The contagious global pandemic of coronavirus 2019 (COVID-19) has prompted many Moroccans to turn to traditional phytoremedies. Aims: To highlight the ethnopharmacological information and the risks of intoxication related to the use of herbal medicine to combat COVID-19. Methods: Through a semi-structured questionnaire and using the "Free listing" technique, an ethnobotanical survey was conducted among 36 herbalists of the Meknes prefecture to collect ethnopharmacological data on species used in the fight against COVID-19. Then, many databases were used to document their pharmacological and toxicological activities. Results: A total of 36 species in 22 families were reported to be used to prepare traditional recipes against COVID-19. According to the relative frequency index of citation, the species Artemisia herba-alba Asso, Eucalyptus globulus Labill, Syzygium aromaticum (L.) Merr. & L.M. Perry, Citrus limon (L.) Osbeck, and Zingiber officinale Roscoe. were recommended by all respondents and recorded the highest usage values. Based on the value of the plant parts index, leaves were the most used part (PPV = 0.37). Most of the remedies were prepared as infusions and administered orally. The bibliographic research revealed that the plants used have several biological activities and are frequently used to treat respiratory diseases. However, some of them have been reported to be toxic. Conclusions: Recommended species are endowed with innumerable biological activities. They can be a promising alternative to combat COVID-19. However, their toxic effects require pharmacotoxicological studies to ensure the safety and efficacy of these natural remedies. Keywords: COVID-19; ethnobotany; herbalism; Morocco; Meknes; phytotherapy; toxicity.
... Percentage inhibition of the different concentrations of REO and diclofenac, after the 6 hours of experimentation were quite similar (P < 0.05). Bozin et al., (2007) realised that Rosmarinus officinalis has anti-oxidative effects as well as anti-inflammatory, this essential oil contains a rich mixture of terpenes; the most represented compound was 1.8-cineole, which is known to have anti-inflammatory effects (Santos and Rao 2000;Juergens et al., 2003), in particular, the highest concentration of REO (containing eucalyptol, α-pinene and borneol) inhibited the acetylcholinesterase (Savelev et al., 2003). Table 5. ...
... [20,50] Moreover, 1,8-cineole (eucalyptol), a terpenoid oxide present in many plant essential oils such as S. officinalis EO, displayed an inhibitory effect on some types of experimental inflammation in rats, i.e. paw oedema induced by carrageenan and cotton pellet-induced granuloma. [52] Finally, β-pinene, present at 1.18% in our oil, has also been shown to exhibit anti-inflammatory effects. [53] In comparison to our results obtained from the EO of S. officinalis, S. libanotica had shown, at the lowest concentration of EO used (1%), a lower antiinflammatory effect (23.89%) than S. officinalis (29.57%). ...
... Karadag et al. evaluated the in-vitro antibacterial, antioxidant and anti-inflammatory and analgesic effects of flower extracts of rosemary and the results obtained supported the traditional use of herb as an anti-inflammatory agent (Karadag et al., 2019). Essential oil extracted from Rosemary flowers consisted of terpenes particularly 1,8-cineole a very potent anti-inflammatory component reported by Santos and Rao (Santos and Rao, 2000). Rosemary extract was also found to be quite effective against Staphylococcus aureus that tend to worsen inflammation in patients suffering from eczema thereby lowering the rate of the condition from becoming worst. ...
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Background: Atopic eczema a chronic inflammatory skin disorder affecting 2-3% of world's population worldwide and is characterised by the appearance of rashes, itchiness and excessive dryness on the skin. The manifestation is triggered by the genetic and environmental factors hampering with the integrity of skin barrier and increasing its susceptibility to enhanced penetration by various allergens/pathogens worsening the condition further and could result in lethal hypersensitivity reactions too therefore listing as one of the most serious ailments globally. Methods: Application of synthetic drugs suffers from the worst kind of side effects and long-term adverse reactions affecting the quality of life adversely. As per the literature available, medicinal plants possess compounds with varying chemical configuration including free fatty acids, phenolic compounds, sterols, terpenoids, alkaloids destined to modulate pathological conditions hence used. The article reviews many such structures and their related chemistry along with the recent advances in knowing their mechanism of action and pharmacological function executed by them owing to the presence of stereo-specific and regio-selective chemical structures present in them. Discussion and Conclusions: Nimbidin, nimbolide, morgolon, tocopherols, unsaturated fatty acids, oleic acid, linoleic acid, rosmarinic acid, gamma linoleic acid are some of the prominent ones used to manage the skin infections, possessing the excellent ability to heal the eczematous skin and the lesions associated with atopic eczemaby maintaining the integrity of skin, retaining its hydration capacity and normal tone, balancing skin pH and supporting its microbial flora. They have been found to protect the outer layers of epidermis from pathogenic bacteria, fungi, virus and many more invaders as they do possess the effective penetration tendency and able to seep into the depth of stratum thus providing complete relief in comparatively short duration with almost minimal side effects.
... These components are common herbal essential oils similar to eucalyptus and fennel oil. 1,8cineole has anti-inflammatory properties (16,18), and is able to penetrate human skin (19). Terpinen-4-ol has the same properties of 1,8-cineol as an anti-bacterial and antiinflammatory (14,(20)(21)(22)(23)(24). ...
... The anti-inflammatory capacity of the crude oils from S. edelbergii is listed in Table 5. Doses at a concentration of 5, 10, and 15 mg/kg were used which produced an appreciable inhibition from low to high dose 48.22, 58.15, and 61% inhibition, respectively, in comparison to the standard diclofenac sodium which possessed (70.92%) inhibition against the decrease in the paw diameter in the tested experimental animals caused by carrageenan, whereas the control normal saline did not affect paw edema. Santos et al. [57] also described that the oils are accountable to inhibit paw edema. The constituent required to cope with the inflammation is thymol, which is present in the understudied plant and was reported previously by Escobar et al. for its pharmacological effect [40]. ...
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The current study aimed to explore the crude oils obtained from the n-hexane fraction of Scutellaria edelbergii and further analyzed, for the first time, for their chemical composition, in vitro antibacterial, antifungal, antioxidant, antidiabetic, and in vivo anti-inflammatory, and analgesic activities. For the phytochemical composition, the oils proceeded to gas chromatography-mass spec-trometry (GC-MS) analysis and from the resultant chromatogram, 42 bioactive constituents were identified. Among them, the major components were linoleic acid ethyl ester (19.67%) followed by ethyl oleate (18.45%), linolenic acid methyl ester (11.67%), and palmitic acid ethyl ester (11.01%). Tetrazolium 96-well plate MTT assay and agar-well diffusion methods were used to evaluate the isolated oil for its minimum inhibitory concentrations (MIC), minimum bactericidal concentration (MBC), half-maximal inhibitory concentrations (IC50), and zone of inhibitions that could determine the potential antimicrobial efficacy's. Substantial antibacterial activities were observed against the clinical isolates comprising of three Gram-negative bacteria, viz., Escherichia coli, Klebsiella pneu-moniae, and Pseudomonas aeruginosa, and one Gram-positive bacterial strain, Enterococcus faecalis. The oils were also effective against Candida albicans and Fusarium oxysporum when evaluated for their antifungal potential. Moreover, significant antioxidant potential with IC50 values of 136.4 and 161.5 µg/mL for extracted oil was evaluated through DPPH (1,1-Diphenyl-2-picryl-hydrazyl) and ABTS assays compared with standard ascorbic acid where the IC50 values were 44.49 and 67.78 µg/mL, respectively, against the tested free radicals. The oils was also potent, inhibiting the α-glucosidase (IC50 5.45 ± 0.42 µg/mL) enzyme compared to the standard. Anti-glucosidase potential was visualized through molecular docking simulations where ten compounds of the oil were found to be the Citation: Shah, M.; Murad, W.; Rehman, N.U.; Mubin, S.; Alsabahi, J.N.; Ahmad, M.; Zahoor, M.; Ullah, O.; Waqas, M.; Ullah, S.; et al. GC-MS Analysis and Biomedical
... The search for new drugs including herbal products with a broad range of pharmacological activities and economic affordability has increased in recent years (Singh et al., 2013).Various researchers have positively evaluated and explored a broad range of pharmacological activities among them Laurus nobilis ethanolic extract has antioxidant and wound healing effect . In the treatment of gastrointestines, rheumatism, migraines, and diuretic, antimicroscopic, improving appetite and digestion are also used (Santos & Rao, 2000). The volatile laurel oils suppress tuberculosis development and stimulate immunity. ...
... In the case of carrageenan paw edema in rats, 1,8-cineole at doses of 100, 200, and 400 mg/kg caused a significant reduction in paw swelling by 26%, 26%, and 46%, respectively. In the case of the granuloma induced by cotton granules, after 7 days in the group that was administered eucalyptol at a dose of 400 mg/kg, the inhibition of the wet and dry mass of the granuloma was 37 and 40%, respectively [65]. ...
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One of the primary reasons for the search for new antimicrobial agents is the increasing and spreading resistance of microorganisms to previously used drugs. This is particularly important in the case of rapidly progressing infections that require the rapid administration of an appropriately selected antibiotic. However, along with the administration of antibiotics, complications in the disease-weakened body may arise in the form of systemic mycoses, viral infections, and protozoan infections. Therefore, there is an increasing interest among researchers focusing on the use of naturally occurring terpenic compounds in stand-alone or combined therapies with antibiotics. In this publication, the aim of our work is to present the results of a literature review on the antimicrobial activity of eucalyptol.
... The second major terpene is cineole present in the essential oil of Ocimum basilicum. It has been reported that 1,8-cineole exerts anticonvulsant activity, potentiates pentobarbitone sleeping time, and has an inhibitory effect on locomotor activity (Santos and Rao, 2000). ...
... For what concerns the biological activity of the three major common compounds across all the analyzed plant parts, 1,8-cineole, which accumulated in particular in the leaves after drying, plays a major role in the treatment of upper and lower airway diseases due to its anti-inflammatory properties, and appears to be active against antibiotic-susceptible and antibiotic-resistant pathogens [32][33][34]. In vitro experiments suggest anti-nociceptive properties [35] and a protective effect against ethanol-induced gastric mucosal damage and liver failure [36]. α-Terpineol, which prevailed in the fruits, shows antihypertensive and antiproliferative effect on human erythroleukemic cells [37,38], as well as antioxidant, anticancer, anticonvulsant, antiulcer, anti-nociceptive, and anti-inflammatory actions [39][40][41][42][43]. Finally, sabinene, principally abundant in the leaves, is known to exhibit anti-inflammatory properties [44]. ...
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In the present paper, we focused our attention on Cinnamomum camphora (L.) J. Presl. (Lauraceae), studied at three levels: (i) micromorphological, with the analysis of the secretory structures and a novel in-depth histochemical characterization of the secreted compounds; (ii) phytochemical, with the characterization of the essential oils from young stems, fruits, and leaves, subjected to different conservation procedures (fresh, dried, stored at −20 °C, stored at −80 °C) and collected in two different years; (iii) bioactive, consisting of a study of the potential antibacterial activity of the essential oils. The micromorphological investigation proved the presence of secretory cells characterized by a multi-layered wall in the young stems and leaves. They resulted in two different types: mucilage cells producing muco-polysaccharides and oil cells with an exclusive terpene production. The phytochemical investigations showed a predominance of monoterpenes over sesquiterpene derivatives; among them, the main components retrieved in all samples were 1,8-cineole followed by α-terpineol and sabinene. Conservation procedures seem to only influence the amounts of specific components, i.e., 1,8-cineole and α-terpineol, while analyses on each plant part revealed the presence of some peculiar secondary constituents for each of them. Finally, the evaluation of the antibacterial activity of the essential oil showed a promising activity against various microorganisms, as Listeria monocytogenes, Staphylococcus aureus, Enterococcus faecalis and Pseudomonas aeruginosa. In conclusion, we combined a micromorphological and phytochemical approach of the study on different plant parts of C. camphora, linking the occurrence of secretory cells to the production of essential oils. We compared, for the first time, the composition of essential oils derived from different plant matrices conserved with different procedures, allowing us to highlight a relation between the conservation technique and the main components of the profiles. Moreover, the preliminary antibacterial studies evidenced the potential activity of the essential oils against various microorganisms potentially dangerous for plants and humans.
... 1,8-Cineole and Terpinen-4-ol are the main active components of TTO and it was reported that 1,8-Cineole has anti-inflammatory properties [29,30], and can penetrate human skin [31]. Other studies revealed that Terpinen-4-ol doesn't have the same properties of 1,8-cineol as anti-inflammatory component [26,32] only, but also has an anti-bacterial activity. ...
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Background The gold standard in treatment of periodontitis is mechanical removing of dental biofilm but using local delivery drugs as adjunctive to SRP is widely used to modulate inflammatory host and eradicate microbes. Tea tree oil (TTO) has a broad-spectrum antimicrobial, anti-inflammatory, antifungal, antiviral, antioxidant effect. This study aimed to assess clinically and biochemically the effect of intrapocket application of TTO (Melaleuca alternifolia) gel adjunctive to scaling and root planing (SRP) in the treatment of stage 2 (moderate) periodontitis and to correlate the biochemical levels with clinical response. Methods A randomized, controlled clinical trial was conducted on thirty patients with stage 2 periodontitis. Patients were equally divided into two groups: Control Group treated with (SRP) alone and Test Group treated with SRP and locally delivered 5% TTO gel. Clinical assessment included pocket probing depth (PPD), clinical attachment loss (CAL), gingival index (GI) and bleeding on probing (BOP) measured at baseline and after 3 and 6 months. The level of matrix metalloproteinase-8 (MMP-8), in the gingival crevicular fluid (GCF) was also assessed at baseline and after1, 3 and 6 months by Enzyme-linked immunosorbent assay (ELISA) kit. Chi-square, Student t- tests, Mann–Whitney U test and Spearman correlation were the statistical tests used in the study. Results An improvement of all clinical and biochemical parameters was observed (at p < 0.001) in both groups. A significant difference between the two groups was found in both clinical and biochemical parameters. Conclusion The local delivery of TTO gel adjunctive to SRP proved to be effective in the treatment of stage II periodontitis. Trial registration The study was retrospectively registered at clinicaltrials.gov NCT04769271, on 24/2/2021.
... They inhibit cyclooxygenase (COX) enzyme and pro-inflammatory cytokines, for example tumor necrosis factor-α (TNFα), interleukins (IL-1β, IL-6) and nuclear factor kappa-lightchain-enhancer of activated B cells (NF-κB). [12][13][14] To clarify analgesic and anti-inflammatory activity we aimed to evaluate in vivo activity and in silico molecular docking analysis that give potent candidature. ...
Article
The objective of our present study is to scrutinize the analgesic and anti-inflammatory potentials of essential oil of Eucalyptus camaldulensis leaf using different in vivo assay models at doses of 100, 200, and 400 mg/kg body weight. Twenty chemical compounds, which were isolated from the leaves essential oil of E. camaldulensis, were docked using AutodockVina against cyclooxygenase 2, tumor necrosis factor-α, and interleukin-1β convertase to elucidate the analgesic and anti-inflammatory activity. The essential oil of E. camaldulensis exhibited noteworthy analgesic activities in the writhing test. In the tail immersion and hot-plate test, the essential oil significantly extended the latency period. The number of licks in the formalin-induced paw licking test was markedly reduced following essential oil administration. In addition, E. camaldulensis essential oil revealed notable anti-inflammatory responses in carrageenan-induced paw edema, xylene induced ear edema and cotton pellet induced granuloma methods. Among 20 compounds, 5 ( cis-sabinol, globulol, α-eudesmol, β-eudesmol, and γ-eudesmol) showed better binding for cyclooxygenase-2 while β-eudesmol exhibited higher affinity for TNFα than that of TNF-alpha-IN-1 and standard drug. In the case of interleukin 1β convertase, maximum affinity was shown by α-eudesmol than the synthetic drug belnacasan. Chemical components of the essential oil interacted with diverse amino acid residues which were similar to the natural substrate and standard drugs. In conclusion, E. camaldulensis essential oil can be an effective source of analgesic and anti-inflammatory treatment and additional modification and docking studies will be required to justify the efficiency of globulol, α-eudesmol, β-eudesmol, and γ-eudesmol.
... Previous studies have shown that 1,8-cineole decreases proinflammatory cytokines such as TNF-α and IL-1β, and arachidonic acid metabolism, besides reducing NF-κβ and toll-like receptor 4 expression, and MPO activity (Juergens et al., 1998;Santos & Rao, 2000;Zhao et al., 2014). Other studies have confirmed its antioxidant activity, demonstrating that 1,8-cineole can restore the function and integrity of liver cells, thus decreasing the leakage of serum aminotransferases into the blood, in addition to increasing the amount of antioxidant enzymes such as CAT (Abdallah et al., 2019;Ciftci et al., 2011;Santos, 2004;Santos et al., 2001). ...
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Acetaminophen (N-acetyl-p-aminophenol, APAP) is the most popular drug recommended and consumed for relieving mild and moderate pain and fever. Although effective in therapeutic doses, APAP overdose induces hepatotoxicity, causing acute liver failure. In this study, the hepatoprotective effects and the underlying mechanisms of Lavandula officinalis essential oil (LEO) were investigated in APAP-induced hepatotoxicity. To evaluate the hepatoprotective effect, Balb /c mice were pretreated with LEO at doses of 200 and 400 mg/kg, once daily for seven days. On the seventh day, mice were treated with APAP (250 mg/kg) to induce hepatotoxicity. LEO significantly decreased serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (γ-GT) compared to the APAP group. Besides, a decrease in myeloperoxidase (MPO) activity, nitric oxide (NO), and pro-inflammatory cytokines levels were observed in liver samples of the LEO treated mice. Moreover, pretreatment with LEO showed significant antioxidant activity by decreasing the levels of malondialdehyde (MDA), carbonylated proteins, reactive oxygen species (ROS), and glutathione (GSH), in addition to increasing levels of the hepatic superoxide dismutase (SOD), catalase (CAT), and oxidized glutathione (GSSG). Our results showed that LEO improved liver functions altered by APAP by inhibiting oxidative stress and inflammatory induced by APAP and other oxidative stress-mediated toxicities.
... 1,8-cineole (eucalyptol) is an oily monoterpene present in essential oils of plants and herbs including tea, rosemary, bay, and the main component of eucalyptus essential oil. Several biological and pharmacological properties such as penetration enhancer, expectorant, antibacterial, antifungal, anti-inflammatory activities were reported for 1, 8-cineole [27,28]. Moreover, 1,8-cineole showed anticancer properties in a wide variety of cancer cells [29][30][31], including hepatocellular carcinoma (HepG2) and lung adenocarcinoma (A549) cells, previously reported by our group [32,33]. ...
Article
The development of versatile carriers to deliver chemotherapeutic agents to specific targets with establishing drug release kinetics and minimum undesirable side effects is becoming a promising relevant tool in the medical field. Magnetic hybrid nanostructured lipid carriers (NLC) were prepared by incorporation of 1,8-cineole (CN, a monoterpene with antiproliferative properties) and maghemite nanoparticles (MNPs) into a hybrid matrix composed of myristyl myristate coated with chitosan. Hybrid NLC characterized by DLS and TEM confirmed the presence of positively charged spherical nanoparticles of around 250 nm diameter and +10.2 mV of Z-potential. CN encapsulation into the lipid core was greater than 75% and effectively released in 24 h. Modification of the crystalline structure of nanoparticles after incorporation of CN and MNPs was observed by XRD, DSC, and TGA analyses. Superparamagnetic NLC behavior was verified by recording the magnetization using a vibrating scanning magnetometer. NLC resulted in more cytotoxic than free CN in HepG2 and A549 cell lines. Particularly, viability inhibition of HepG2 and A549 cells was increased from 35% to 55% and from 38% to 61%, respectively, when 8 mM CN was incorporated into the lipid NPs at 24 h. Green fluorescent-labeled NLC with DIOC18 showed an enhanced cellular uptake with chitosan-coated NLC. Besides, no cytotoxicity of the formulations in normal WI-38 cells was observed, suggesting that the developed hybrid NLC system is a safe and good potential candidate for the selective delivery and potentiation of anticancer drugs.
... Based on this, it can be thought that the antimicrobial effect of N. pisidica essential oils is caused by camphor and 1,8-cineole. Furthermore, the antinociceptive and antiinflammatory activities of 1,8-cineole, camphor and essential oils that contain large proportional amounts of 1,8-cineole and camphor were proven (Lenardão et al., 2016;Chandrakanthan et al., 2020;Santos et al., 2000;Barkin, 2013). Thus, antinociceptive and antiinflammatory activities may explain the folkloric usage of N. piscidica for toothache. ...
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The fruits, aerial parts and roots of Neomuretia pisidica (Kit Tan) Kljuykov, Degtjareva & Zakharova were extracted with n-hexane. Total of 18 compounds were characterised by GC analyses of the n-hexane extracts. Main volatile components of the n-hexane extract of aerial parts were characterized as 1,8-cineole (23.4%), camphor (21.4%), 2-ethyl hexanol (14.6%), α-pinene (7.2%), and verbenone (6.4%). Methyl linoleate (19.3%), 1,8-cineole (16.5%), camphor (13.2 %), α-pinene (6.1 %) and 2-ethyl hexanol (4.9%) were found in the n-hexane extract of roots. Whereas, 1,8-cineole (23.3 %), camphor (20.3%), 2-ethyl hexanol (14.2 %), α-pinene (9.9%), and limonene (4.1%) were the major components of the n-hexane extract of fruits. Antimicrobial activity were identified using a microdilution assay against selected human pathogenic strains. The most potent inhibitor activities with 156 µg/mL concentrations were detected against S. aureus and E. faecalis.
... Monoterpenoids often show several biological activities, having potential applications in different fields. Cineole has been previously examined for its biological and pharmacological activities, including anti-inflammatory and analgesic effects [3]. Recently, it has been shown that 1,8-cineole significantly stimulates the transactivation of liver X receptor modulator LXR-a and LXR-b. ...
Article
The compound 1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-9-ol (9-hydroxyeucaliptol) has been prepared and characterized by single-crystal X-ray diffraction analysis, infrared, Raman, and UV-visible spectroscopies. The molecular geometry of the title compound was also investigated theoretically by density functional theory (DFT) calculations to compare with the experimental data. The substance crystallizes in the trigonal crystal system, space group P32 with Z = 9 molecules per unit cell. There are three independent molecules in the crystal asymmetric unit having the same chirality and showing some differences in the orientation of the H-atom of the hydroxyl group. The crystal structure of 9-hydroxyeucaliptol shows that the hydroxyl group presents an anti-conformation with respect to the O-atom of the ether group. The crystal packing of 9-hydroxyeucaliptol is stabilized by intermolecular O-H···O hydrogen bonds involving the hydroxyl groups of different molecules, which play a decisive role in the preferred conformation adopted in solid state. The intermolecular interactions observed in solid state were also studied through the Hirshfeld surface analysis and quantum theory of atoms in molecules (QTAIM) approaches. Energy framework calculations have also been carried out to analyze and visualize the topology of the supramolecular assembly, and the results indicate a significant contribution from electrostatic energy over the dispersion.Graphical abstract
... Furthermore, the antioxidant activity may be altered by synergistic and antagonistic effects between some components of the essential oil [72]. e synergistic activity of 1.8cineole and α-caryophyllene has been documented [73]. Our ...
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Cineole (eucalyptol) is the isolated active agent of eucalyptus oil. Traditionally, it is recommended for treating the symptoms of airway diseases exacerbated by infection. We have examined the inhibitory effect of 1.8-cineole on LPS-and IL1beta-stimulated mediator production by human monocytes in vitro. For the first time, we report on a dose-dependent and highly significant inhibition of production of tumor necrosis factor-alpha, interleukin-1beta, leukotriene B4 and thromboxane B2 by 1.8-cineole. In summary, this is the first report on a new mechanism of action of monoterpenes suggesting 1.8-cineole as a strong inhibitor of cytokines that might be suitable for longterm treatment of airway inflammation in bronchial asthma and other steroid-sensitive disorders.
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The importance of absorption of drugs and poisons through the skin and mucous membranes needs no emphasis. This subject is of vital interest not only to medical men but to all biologists concerned with that borderline science known as pharmacology, which has to do with the relationship of the physicochemical sciences, on the one hand, and the biologic, on the other. It is also of great practical significance, particularly to dermatologists and other medical specialists who prescribe drugs and chemicals for application to skin or mucous membranes.I have taken a lively interest in experimental investigations on absorption of drugs and poisons for more than twenty years. Indeed, in 1910 I recorded a research on lavage in the treatment of acute phenol poisoning in which the absorption of phenol through both the skin and the mucosa of the stomach and the intestines was experimentally studied. This research led to some
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The rationale for using essential oils to alleviate headache is based on several assumptions. Especially for peppermint oil certain analgesic mechanisms were recently described. Local application of peppermint oil generates a long-lasting cooling effect on the skin, caused by a steric alteration of the calcium channels of the cold-receptors. Further it was shown that peppermint oil inhibits non-competively 5-hydroxytryptamin (Serotonine) and substance P induced smooth muscle contraction in animal-models. It is also known that peppermint oil induces a significant increase of the skin blood flow of the forehead after local application, measured by laser doppler. Assuming that a clinical relevant analgesic action exists, this ought to be observable in experimental algesimetric human tests. Therefore the effects of peppermint oil and eucalyptus oil preparations on neurophysiological, psychological and experimental algesimetric parameters were investigated in 32 healthy subjects in a double-blind, placebo-controlled, randomized cross-over design. Four different test preparations were used: preparation 1 (LI1701) consisted of 10 g peppermint oil and 5 g eucalyptus oil plus ethanol 90% to 100 g; preparation 2 (LI1702) of 10 g peppermint oil and traces of eucalyptus oil plus ethanol 90% to 100g; preparation 3 (LI1703) of traces of peppermint oil and 5 g eucalyptus oil plus ethanol 90% to 100 g; and preparation 4 (placebo) of traces of peppermint oil and traces of eucalyptus oil plus ethanol 90% to 100 g. The test preparations were applied to large areas of the forehead and temples using a small sponge. The treatment effect of the preparations was evaluated by comparing baseline and treatment measurements. The combination of peppermint oil, eucalyptus oil and ethanol can increase cognitive performance while having a muscle-relaxing and mentally relaxing effect, but has little influence on pain sensitivity. A significant analgesic effect with a reduction in sensitivity to headache is however produced by the combination of peppermint oil and ethanol. The essential plant oil preparations can thus be shown by laboratory tests to exert significant effects on mechanisms associated with the pathophysiology of clinical headache syndromes. Further, to investigate the efficacy of essential oil preparations compared to usual analgesics (paracetamol or acetylsalicylicacid) a double blind, placebo controlled, randomized study should be performed.
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Volatile oils are frequently employed in the local treatment of pain. 1,8-Cineole, the principal component of eucalyptus oil, was used as a model substance to determine whether this active component can be detected in effective amounts at the target area in the skeletal muscles after at the target area in the skeletal muscles after dermal application. The investigation showed surprisingly large differences depending on the manner of application. The relative bioavailability of the model substance 1,8-cineole obtained by using an applicator was 320% as compared with that obtained by using an occlusive dressing. This has practical effects on the dosage and on the frequency of application.
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A computer optimization technique based on response surface methodology was applied for the optimization of a hydrogel formulation containing indomethacin as a model drug. As the penetration enhancer, a combination of three cyclic monoterpenes, limonene, menthol, and cineole, was employed. Pharmacokinetic parameters, from an in vivo percutaneous absorption study on rats of model formulations prepared according to the composite experimental design for five factors, were determined as prime response variables. The skin damage evoked by each formulation was microscopically judged and graded as the response variable concerning skin safety. The response variables were predicted by multiple regression equations comprising combinations of the five formulation factors. The regression equations for the response variables assembled as a simultaneous optimization problem based on the generalized distance function. The simultaneous optimum was predicted as a function of individual optima within a 95% confidence region. The predicted response values for the optimum formulation have been successfully validated in a repeated in vivo percutaneous absorption study.
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A series of terpenes has been assessed as skin penetration enhancers towards the model polar penetrant 5-fluorouracil (5-FU). Cyclic terpenes were selected from the chemical classes of hydrocarbons (e.g., alpha-pinene), alcohols (e.g., alpha-terpineol), ketones (e.g., carvone), and oxides (e.g., 1.8-cineole, ascaridole). Permeation experiments were performed on excised human epidermal membranes and the terpenes varied in their activities; alpha-pinene only doubled the permeability coefficient of aqueous 5-FU, whereas 1.8-cineole caused a near 95-fold increase. Essential oils, e.g., chenopodium (70% ascaridole), were less effective than the corresponding isolated terpenes, 5-FU is less soluble in the terpenes than in water, and the terpenes did not exert their action by increasing partitioning of the drug into the membranes as illustrated by stratum corneum:water partitioning studies. The penetration enhancers increased drug diffusivity through the membranes, an effect which correlated empirically with the enhancer activities. The principal mode of action of these accelerants may be described by the lipid-protein-partitioning theory: the terpenes interacted with intercellular stratum corneum lipids to increase diffusivity, and the accelerant effects were not due to partitioning phenomena. Keratin interaction was assumed negligible.
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Volatile oils are frequently employed in the local treatment of pain. 1,8-Cineole, the principal component of eucalyptus oil, was used as a model substance to determine whether this active component can be detected in effective amounts at the target area in the skeletal muscles after dermal application. The investigation showed surprisingly large differences depending on the manner of application. The relative bioavailability of the model substance 1,8-cineole obtained by using an applicator was 320% as compared with that obtained by using an occlusive dressing. This has practical effects on the dosage and on the frequency of application.
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The antinociceptive properties of diazepam were evaluated in mice, using four different pain tests and different doses of the drug (0.2, 0.5, 1.0 and 2.0 mg/kg). In the tail flick test and the increasing temperature hot plate test there were no effects. In the formalin test reduced licking was observed for the highest dose of diazepam. However, this dose also induced clear sedation possibly causing the reduced licking response. In the constant temperature hot plate test a hyperalgesia was found for all doses tested. This hyperalgesia was not observed in animals adapted to the test apparatus, suggesting that the "hyperalgesic" effect of diazepam may be due to reduced stress analgesia. The serum concentrations of the drug were comparable to therapeutic levels in humans. It was concluded that the sedative and anxiolytic effects of diazepam may influence the results of nociceptive tests, but the drug has probably no effect on nociception in itself.
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The formalin test in mice is a valid and reliable model of nociception and is sensitive for various classes of analgesic drugs. The noxious stimulus is an injection of dilute formalin (1% in saline) under the skin of the dorsal surface of the right hindpaw. The response is the amount of time the animals spend licking the injected paw. Two distinct periods of high licking activity can be identified, an early phase lasting the first 5 min and a late phase lasting from 20 to 30 min after the injection of formalin. In order to elucidate the involvement of inflammatory processes in the two phases, we tested different classes of drugs in the two phases independently. Morphine, codeine, nefopam, and orphenadrine, as examples of centrally acting analgesics, were antinociceptive in both phases. In contrast, the non-steroid anti-inflammatory drugs indomethacin and naproxen and the steroids dexamethasone and hydrocortisone inhibited only the late phase, while acetylsalicylic acid (ASA) and paracetamol were antinociceptive in both phases. The results demonstrate that the two phases in the formalin test may have different nociceptive mechanisms. It is suggested that the early phase is due to a direct effect on nociceptors and that prostaglandins do not play an important role during this phase. The late phase seems to be an inflammatory response with inflammatory pain that can be inhibited by anti-inflammatory drugs. ASA and paracetamol seem to have actions independent of their inhibition of prostaglandin synthesis and they also have effects on non-inflammatory pain.
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One hour after the addition of 0.5 ml rosemary oil per cage for evaporation (141 of volume) the concentration of 1,8-cineole in the blood, 11.15 nl/g, approached that in the breathing air, 13.65 nl/ml. Inhalation and oral administration of various doses of rosemary oil produced dose-related increases in blood levels of 1,8-cineole. An increase in locomotor activity was observed in both cases. The disappearance of 1,8-cineole from the blood immediately after the termination of a 60-min inhalation period was biphasic: a rapid phase of elimination of about 10 min with a short blood half life (t/2 = 6 min) was followed by a slower rate of elimination (t/2 = 45 min). Since the blood levels of 1,8-cineole (if taken as an indicator for the blood levels of rosemary oil) associated with the stimulation of locomotor activity were similar regardless of whether the oil was administered by inhalation or orally, it is suggested that the stimulation of locomotor activity by rosemary oil is due at least in part to the direct pharmacological action of one or more of its constituents.
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1. Using the rat paw oedema assay procedure a comparison was made between the anti-inflammatory and irritant properties of the inflammatory exudate obtained from polyester sponges implanted subcutaneously in adrenalectomized rats. Where necessary, comparison was also made with a known counter-irritant, carrageenin.2. A significant correlation between the anti-inflammatory and irritant properties of sponge exudate was observed when each parameter was determined in relation to dose. A similar result was obtained with carrageenin.3. A comparison of the two activities of sponge exudate samples harvested at various times following sponge implantation did not give a significant correlation although in each case significant anti-inflammatory activity was accompanied by marked irritation.4. Time-effect curves of the two activities of sponge exudate showed a significant correlation over the time period examined. However, no such correlation was obtained using carrageenin.5. Both activities of sponge exudate were retained following dialysis.6. These findings are discussed in relation to a counter-irritant mode of action for sponge exudate.
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1 Dexamethasone and hydrocortisone induced the release of anti-phospholipase proteins into the peritoneal cavities of rats. 2 Adrenocorticotrophic hormone (ACTH) also releases these proteins in normal but not in adrenalectomized rats. 3 Peritoneal lavage proteins were separated by ion-exchange and size exclusion chromatography. The anti-phospholipase activity occurred in four separate fractions with the major component having an apparent mol. wt. of 40 k. 4 Column fractions containing these anti-phospholipase proteins had anti-inflammatory effects in the rat carrageenin pleurisy model whereas other fractions were inactive. 5 The proteins appear to be identical to macrocortin and lipomodulin, the 'second messengers' of glucocorticoid hormone action on the arachidonate system.
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The effects of withdrawal from chronic ethanol administration on locomotion and rearing frequencies of rats and mice were studied. Ethanol withdrawal induced a significant increase in animal's activity. In mice a positive correlation was found between locomotion plus rearing frequencies and audiogenic-induced seizures susceptibility 25 hr after ethanol removal. Results show that general activity evaluated through the open-field method might be used as a simple, non-drastic and reliable procedure to detect ethanol withdrawal symptoms in laboratory animals.
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As part of a series of short-term studies on peppermint oil constituents for their possible induction of the encephalopathy found with peppermint oil, 1,8-cineole and l-limonene were studied. Groups of 10 male Wistar rats were given 0, 500, or 1000 mg 1,8-cineole/kg body wt./day or 0, 800, or 1600 mg l-limonene/kg body wt./day for 28 days. 1,8-Cineole and l-limonene both induced accumulation of protein droplets containing alpha 2 mu-globulin in proximal tubular epithelial cells in male rats. These results suggest that both 1,8-cineole and l-limonene possibly belong to the group of chemicals characterized by their induction of excessive alpha 2 mu-globulin accumulation. Neither of the 2 substances induced encephalopathy.
Article
Menthol and other aromatic vapours have been widely used in the symptomatic treatment of upper respiratory tract infections, although there is little objective evidence as to their benefit. We have investigated the action of aromatic vapours on the cough reflex in conscious guinea-pigs. Animals (n = 13) were pretreated with air or test vapours for 5 min at a rate of 1 l/min. One minute later the animal was challenged with aerosolized citric acid for 2 min. Control responses to air pretreatment were not significantly different throughout the procedures. Three concentrations of each aromatic vapour were used (3, 10 and 30 micrograms/l menthol, 50, 133 and 500 micrograms/l camphor and 0.8, 2.7 and 8 mg/l cineole). Menthol proved the most effective antitussive--10 and 30 micrograms/l produced a significant 28 and 56% reduction in cough frequency--500 micrograms/l camphor gave a significant 33% reduction, while cineole, at the concentrations used, had no significant effect. An increase in cough latency coincided with a reduction in cough frequency. These results demonstrate the efficacy of aromatic vapours as antitussives in chemically induced cough.
Article
A computer optimization technique based on response surface methodology was applied for the optimization of a hydrogel formulation containing indomethacin as a model drug. As the penetration enhancer, a combination of three cyclic monoterpenes, limonene, menthol, and cineole, was employed. Pharmacokinetic parameters, from an in vivo percutaneous absorption study on rats of model formulations prepared according to the composite experimental design for five factors, were determined as prime response variables. The skin damage evoked by each formulation was microscopically judged and graded as the response variable concerning skin safety. The response variables were predicted by multiple regression equations comprising combinations of the five formulation factors. The regression equations for the response variables assembled as a simultaneous optimization problem based on the generalized distance function. The simultaneous optimum was predicted as a function of individual optima within a 95% confidence region. The predicted response values for the optimum formulation have been successfully validated in a repeated in vivo percutaneous absorption study.
Article
The present studies tested the ability of 1,8-cineole to produce inflammatory oedema in the hind paw of the rat and verified the possible involvement of mast cells in the response. Subplantar injection of 1,8-cineole (10, 15 and 20 microl/paw) induced a dose-dependent paw oedema which was apparent within 30 min. At higher doses the oedema effect was persistent, peaked at 2 h, and then decreased gradually but was still pronounced at 24 h post injection. In contrast, the oedema produced by mast cell degranulator compound 48/80 (10 microg/paw) had a rapid onset with a peak effect at the first hour, followed by a gradual decrease thereafter and at 24 h post injection it was almost absent. The oedema response to 20 microl 1,8-cineole was significantly inhibited throughout its time-course in rats pretreated with antihistaminic and antiserotonergic drugs such as diphenhydramine, methysergide and cyproheptadine or with ketotifen, a mast cell stabilizer. A more effective blockade of the oedema response was, however, observed in rats depleted of mast cell granules by systemic treatment with compound 48/80. Furthermore, 1,8-cineole was able to cause rat peritoneal mast cell degranulation (94%) in vitro, in a concentration as low as 0.3 microl/ml, which was almost comparable to that produced by 0.1 microg/ml of compound 48/80. The data provide evidence of a key role for the mast cell in 1,8-cineole-induced hind paw oedema in the rat.
Article
A method is presented for measuring the edema induced by injection of 0.05 ml of 1% solution of carrageenin, an extract of Chondrus, into the plantar tissues of the hind paw of the rat. Peak edema develops within the first 3 to 4 hours, and is inhibited by pretreatment of the animals by single oral doses of antiinflammatory agents, steroid or non-steroid. Log dose responses to drugs are linear and parallel, and yield potency ratios with relatively narrow confidence limits. The potency ratios obtained for aspirin, phenylbutazone and hydrocortisone are fairly close to the ratios of their respective daily doses in the treatment of rheumatic disease. A potent antihistaminic-antiserotonin compound, cyproheptadine, is without effect on carrageenin-induced edema.
An extension of the "squirming test" is described which makes the method specific for nonnarcotic analgesics. The intraperitoneal injection of acetic acid causes squirming and an increase in capillary permeability that is measured by direct estimation of plasma-bound dye (Pontamine Sky Blue) which has leaked into the peritoneal cavity. Nonnarcotic analgesics inhibit squirming and leakage of dye. Values for the oral ED50s for both effects are given for a number of typical compounds. Narcotic analgesics, in doses that produce analgesia, inhibit squirming but do not significantly affect leakage of dye. Drugs that stimulate the central nervous system and also inhibit squirming have no significant effect on leakage of dye over the range of doses which inhibit squirming. Corticosteroids do not significantly inhibit either squirming or leakage of dye.
The mast cell degranulating peptide from the bee venom
  • B E C Banks
  • C L Dempsey
  • C A Vernon
Banks, B. E. C., Dempsey, C. L., Vernon, C. A., and Yanney, J. (1980). The mast cell degranulating peptide from the bee venom. J. Physiol. London 308, 95±96.
Inhibition of carrageenan-induced in¯ammation by urethane anaesthesia in adrenalectomized and sham operated rats
  • D E Griswold
  • S Alessi
  • E F Webb
  • D T Waltz
Griswold, D. E., Alessi, S., Webb, E. F., and Waltz, D. T. (1982). Inhibition of carrageenan-induced in¯ammation by urethane anaesthesia in adrenalectomized and sham operated rats. J. Pharmacol. Methods 8, 161±164.
Aroma Therapy. Ultimate Editions
  • C Mcgilevery
  • J Reed
McGilevery, C., and Reed, J. (1993). Aroma Therapy. Ultimate Editions, London.
Essential Oil Safety: A Guide for Health Care Professionals
  • R Tisserand
  • T Balacs
Tisserand, R., and Balacs, T. (1995). Essential Oil Safety: A Guide for Health Care Professionals. pp. 2±216. Churchill Livingstone, New York.