RESUMO
Borneol, camphor, and bornyl acetate are highly promising monoterpenoids widely used in medicine, flavor, food, and chemical applications. Bornyl diphosphate (BPP) serves as a common precursor for the biosynthesis of these monoterpenoids. Although bornyl diphosphate synthase (BPPS) that catalyzes the cyclization of geranyl diphosphate (GPP) to BPP has been identified in multiple plants, the enzyme responsible for the hydrolysis of BPP to produce borneol has not been reported. Here, we conducted in vitro and in vivo functional characterization to identify the Nudix hydrolase WvNUDX24 from W. villosa, which specifically catalyzes the hydrolysis of BPP to generate bornyl phosphate (BP), and then BP forms borneol under the action of phosphatase. Subcellular localization experiments indicated that the hydrolysis of BPP likely occurs in the cytoplasm. Furthermore, site-directed mutagenesis experiments revealed that four critical residues (R84, S96, P98, and G99) for the hydrolysis activity of WvNUDX24. Additionally, the functional identification of phosphatidic acid phosphatase (PAP) demonstrated that WvPAP5 and WvPAP10 were able to hydrolyze geranylgeranyl diphosphate (GGPP) and farnesyl diphosphate (FPP) to generate geranylgeranyl phosphate (GGP) and farnesyl phosphate (FP), respectively, but could not hydrolyze BPP, GPP, and neryl diphosphate (NPP) to produce corresponding monophosphate products. These findings highlight the essential role of WvNUDX24 in the first step of BPP hydrolysis to produce borneol and provide genetic elements for the production of BPP-related terpenoids through plant metabolic engineering and synthetic biology.
Assuntos
Canfanos , Nudix Hidrolases , Proteínas de Plantas , Pirofosfatases , Pirofosfatases/metabolismo , Pirofosfatases/genética , Proteínas de Plantas/metabolismo , Proteínas de Plantas/genética , Canfanos/metabolismo , Brassicaceae/genética , Brassicaceae/enzimologia , Brassicaceae/metabolismo , Fosfatos de Poli-Isoprenil/metabolismoRESUMO
BACKGROUND: Oleoylethanolamide (OEA), an endogenously generated cannabinoid-like compound, has been reported to be increased in patients with severe asthma and aspirin-exacerbated respiratory disease. Recruitment of activated eosinophils in the airways is a hallmark of bronchial asthma. OBJECTIVE: We explored the direct contribution of cannabinoid receptor 2 (CB2), a cognate receptor of OEA, which induces eosinophil activation in vitro and in vivo. METHODS: We investigated OEA signaling in the eosinophilic cell line dEol-1 in peripheral blood eosinophils from people with asthma. In order to confirm whether eosinophil activation by OEA is CB2 dependent or not, CB2 small interfering RNA and the CB2 antagonist SR144528 were used. The numbers of airway inflammatory cells and the levels of cytokines were measured in bronchoalveolar lavage fluid, and airway hyperresponsiveness was examined in the BALB/c mice. RESULTS: CB2 expression was increased after OEA treatment in both peripheral blood eosinophils and dEol-1 cells. It was also elevated after OEA-induced recruitment of eosinophils to the lungs in vivo. However, SR144528 treatment reduced the activation of peripheral blood eosinophils from asthmatic patients. Furthermore, CB2 knockdown decreased the activation of dEol-1 cells and the levels of inflammatory and type 2 cytokines. SR144528 treatment alleviated airway hyperresponsiveness and eosinophil recruitment to the lungs in vivo. CONCLUSION: CB2 may contribute to the pathogenesis of eosinophilic asthma. Our results provide new insight into the molecular mechanism of signal transduction by OEA in eosinophilic asthma.
Assuntos
Asma , Canfanos , Endocanabinoides , Ácidos Oleicos , Eosinofilia Pulmonar , Pirazóis , Receptor CB2 de Canabinoide , Animais , Humanos , Camundongos , Asma/metabolismo , Citocinas , Inflamação/patologia , Pulmão/patologia , Ácidos Oleicos/metabolismo , Eosinofilia Pulmonar/metabolismo , Receptores de Canabinoides , Receptor CB2 de Canabinoide/metabolismoRESUMO
2-methylisoborneol (2-MIB) is an odiferous metabolite mainly produced by cyanobacteria, contributing to taste and odor problems in drinking water. The mechanisms involved in 2-MIB biosynthesis in cyanobacteria are not yet completely understood. This study investigated the effect of light availability and wavelength on growth, 2-MIB synthesis, and related gene expression in Pseudanabaena foetida var. intermedia. A significantly lower 2-MIB production was observed in P. foetida var. intermedia during the dark period of a 12-h photoperiod. Exposure to green light resulted in a significant decrease in 2-MIB production compared to white light and red light. The relative expression levels of 2-MIB-related genes in P. foetida var. intermedia were significantly lower during the dark period of a 12-h photoperiod and when cultured under green light. The expression of 2-MIB-related genes in cyanobacteria appears to be light-dependent. This study suggests that the demand for photopigment synthesis under unfavorable light conditions affects the 2-MIB synthesis in cyanobacteria.
Assuntos
Canfanos , Cianobactérias , Luz , Cianobactérias/genética , Cianobactérias/metabolismo , Cianobactérias/efeitos da radiação , Cianobactérias/crescimento & desenvolvimento , Canfanos/metabolismo , Fotoperíodo , Regulação Bacteriana da Expressão Gênica , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismoRESUMO
Allergic contact dermatitis is reported among individuals using continuous glucose monitoring systems and insulin pumps. The aim of this study was to describe contact allergy patterns for allergens in the Swedish baseline series and medical device-related allergens among users. Contact allergy to baseline series allergens and isobornyl acrylate was compared between diabetes patients and dermatitis patients patch-tested at the Department of Occupational and Environmental Dermatology during 2017 to 2020. Fifty- four diabetes patients and 2,567 dermatitis patients were included. The prevalence of contact allergy to fragrance mix II and sesquiterpene lactone mix was significantly higher in diabetes patients compared with dermatitis patients. Of the diabetes patients 13.0% and of the dermatitis patients 0.5% tested positive to sesquiterpene lactone mix (p < 0.001). Of the diabetes patients 7.4% and of the dermatitis patients 2.3% tested positive to fragrance mix II (p = 0.041). Of the diabetes patients 70.4% tested positive to medical device-related allergens. Of the diabetes patients 63.0% and of the dermatitis patients 0.2% were allergic to isobornyl acrylate (p < 0.001). In conclusion, not only medical device-related contact allergies, but also contact allergy to baseline series allergens (fragrance mix II and sesquiterpene lactone mix), is overrepresented in diabetes patients who use medical devices.
Assuntos
Acrilatos , Canfanos , Dermatite Alérgica de Contato , Diabetes Mellitus , Sesquiterpenos , Humanos , Alérgenos/efeitos adversos , Estudos Retrospectivos , Suécia/epidemiologia , Automonitorização da Glicemia , Glicemia , Dermatite Alérgica de Contato/diagnóstico , Dermatite Alérgica de Contato/epidemiologia , Dermatite Alérgica de Contato/etiologia , Diabetes Mellitus/diagnóstico , Diabetes Mellitus/epidemiologia , Diabetes Mellitus/induzido quimicamente , Testes do Emplastro , LactonasRESUMO
BACKGROUND: In recent years, an increasing number of contact dermatitis cases triggered by acrylates contained in diabetes medical devices have been reported. Acrylates seem to play a major role in the development of irritant contact dermatitis and allergic contact dermatitis (ACD) in diabetic patients. OBJECTIVES: To study a group of patients with contact dermatitis caused by diabetes medical devices with a focus on acrylates as possible allergens responsible for contact dermatitis. PATIENTS AND METHODS: Fifteen patients with diabetes mellitus type 1 and contact dermatitis from diabetic devices were patch tested to 25 acrylate allergens. RESULTS: Three patients (20%) reacted to the following allergens: three patients reacted to isobornyl acrylate (IBOA) and one of them additionally to 2-hydroxyethyl acrylate (2-HEA); results were of clinical relevance. All three patients were using insulin pumps and glucose sensors (GS)-in one patient contact dermatitis was towards the insulin pump and the GS, in one patient only towards the insulin pump and in one patient only towards the GS. Twelve patients (80%) did not show any skin reaction towards the allergens tested. CONCLUSION: A majority of diabetic patients showed no reactions towards any acrylate allergen tested; yet, the presence of untested allergens must be kept in mind. IBOA proved to be a cause of ACD in diabetes patients. 2-HEA might be another culprit allergen, but its presence in the devices must first be confirmed.
Assuntos
Canfanos , Dermatite Alérgica de Contato , Dermatologia , Diabetes Mellitus Tipo 1 , Insulinas , Humanos , Dermatite Alérgica de Contato/etiologia , Polônia , Automonitorização da Glicemia , Acrilatos/efeitos adversos , Diabetes Mellitus Tipo 1/complicações , Alérgenos/efeitos adversos , Testes do Emplastro/efeitos adversosRESUMO
BACKGROUND: Allergic contact dermatitis (ACD) has been reported as an adverse effect from the use of several glucose sensors and insulin pumps from different manufacturers. Isobornyl acrylate (IBOA) has been identified as a major culprit sensitizer, but also other acrylates and (modified) colophonium have been reported as causes of ACD. OBJECTIVES: To report the two first cases diagnosed with ACD caused by the Dexcom G7 (DG7) glucose sensor. PATIENTS AND METHODS: Two children with suspected ACD from DG7 were patch tested with our medical device series with an addition of selected test preparations including two variants of modified colophonium - methyl hydrogenated rosinate (MHR) and glyceryl hydrogenated rosinate (GHR). Both patients were also tested with acetone extracts made from different parts of the DG7 sensor. The extracts were analysed by gas chromatography-mass spectrometry (GC-MS). RESULTS: Both patients tested positive to IBOA, hydroabietyl alcohol and GHR. In addition, patient 1 had a positive reaction to MHR and patient 2 had a positive reaction to colophonium. The GC-MS analyses showed the presence of IBOA and colophonium-related substances in the DG7 extracts. CONCLUSIONS: Both patients were diagnosed with contact allergy to well-known medical device-related sensitizers. The presence of IBOA and (modified) colophonium in a newly introduced (on the Swedish market in 2023) glucose sensor is remarkable and indicates an inadequate toxicological assessment of the materials used in the sensor.
Assuntos
Alérgenos , Canfanos , Dermatite Alérgica de Contato , Criança , Humanos , Alérgenos/efeitos adversos , Dermatite Alérgica de Contato/diagnóstico , Dermatite Alérgica de Contato/etiologia , Automonitorização da Glicemia/efeitos adversos , Adesivos/efeitos adversos , Acrilatos/efeitos adversos , Glucose , Testes do Emplastro/efeitos adversosRESUMO
The objective of the present study was to assess the difference in antimicrobial activity of Satureja kitaibelii Wierzb. ex Heuff. essential oil at three growth stages. In addition, using statistical and chemometric tools, we tried to explain why the essential oil from a certain vegetation stage shows the highest antimicrobial activity. S. kitaibelii essential oils demonstrated minimum inhibitory concentration values from 160 to 10000â µg mL-1 , and minimum microbicidal concentration values from 630 to 20000â µg mL-1 . Geraniol, borneol, limonene and p-cymene are the dominant compounds of S. kitaibelii essential oil. The most abundant compound, geraniol, possesses antimicrobial activity in a range of MIC values from 40 to 5000â µg mL-1 and MMC values from 80 to 10000â µg mL-1 . The highest activity of essential oil for all tested strains of microorganisms was recorded in November. Results of statistical analysis indicate that the percentage of dominant compounds of essential oils does not affect the antibacterial activity of essential oils. Chemometric analyses leads to the conclusion that borneol, spathulenol, caryophyllene oxide and limonene can be the main contributors to the antibacterial activity of essential oil from November and that their mutual ratio is important. These results may represent a new methodological approach for future research on essential oils.
Assuntos
Monoterpenos Acíclicos , Anti-Infecciosos , Canfanos , Óleos Voláteis , Satureja , Óleos Voláteis/farmacologia , Limoneno , Anti-Infecciosos/farmacologia , Antibacterianos/farmacologia , Testes de Sensibilidade MicrobianaRESUMO
OBJECTIVE: Glioma is the most common and deadly primary malignant tumor in adults. Treatment outcomes are ungratified due to the presence of blood-brain barrier (BBB), glioma stem cells (GSCs) and multidrug resistance (MDR). Docetaxel (DTX) is considered as a potential drug for the treatment of brain tumor, but its effectiveness is limited by its low bioavailability and drug resistance. Tetrandrine (TET) reverses the resistance of tumor cells to chemotherapy drugs. Borneol (BO) modified in micelles has been shown to promote DTX plus TET to cross the BBB, allowing the drug to better act on tumors. Therefore, we constructed BO-modified DTX plus TET micelles to inhibit chemotherapeutic drug resistance. SIGNIFICANCE: Provide a new treatment method for drug-resistant brain gliomas. METHODS: In this study, BO-modified DTX plus TET micelles were prepared by thin film dispersion method, their physicochemical properties were characterized. Its targeting ability was investigated. The therapeutic effect on GSCs was investigated by in vivo and in vitro experiments. RESULTS: The BO-modified DTX plus TET micelles were successfully constructed by thin film dispersion method, and the micelles showed good stability. The results showed that targeting micelles increased bEnd.3 uptake and helped drugs cross the BBB in vitro. And we also found that targeting micelles could inhibit cell proliferation, promote cell apoptosis and inhibit the expression of drug-resistant protein, thus provide a new treatment method for GSCs in vitro and in vivo. CONCLUSIONS: BO-modified DTX plus TET micelles may provide a new treatment method for drug-resistant brain gliomas.
Assuntos
Antineoplásicos , Benzilisoquinolinas , Canfanos , Glioma , Humanos , Docetaxel , Micelas , Glioma/tratamento farmacológico , Glioma/patologia , Encéfalo , Linhagem Celular TumoralRESUMO
The genus Cinnamomum encompasses diverse species with various applications, particularly in traditional medicine and spice production. This study focuses on Cinnamomum burmanni, specifically on a high-D-borneol-content chemotype, known as the Meipian Tree, in Guangdong Province, South China. This research explores essential oil diversity, chemotypes, and chloroplast genomic diversity among 28 C. burmanni samples collected from botanical gardens. Essential oils were analyzed, and chemotypes classified using GC-MS and statistical methods. Plastome assembly and phylogenetic analysis were conducted to reveal genetic relationships. Results showed distinct chemotypes, including eucalyptol and borneol types, with notable variations in essential oil composition. The chloroplast genome exhibited conserved features, with phylogenetic analysis revealing three major clades. Borneol-rich individuals in clade II suggested a potential maternal inheritance pattern. However, phylogenetic signals revealed that the composition of essential oils is weakly correlated with plastome phylogeny. The study underscores the importance of botanical gardens in preserving genetic and chemical diversity, offering insights for sustainable resource utilization and selective breeding of high-yield mother plants of C. burmanni.
Assuntos
Canfanos , Cinnamomum , Lauraceae , Óleos Voláteis , Humanos , Óleos Voláteis/química , Cinnamomum/genética , Filogenia , Herança MaternaRESUMO
Naturally occurring substances and their derivatives function as vital resources for pesticides that can be used in fields, such as insecticide production and fungicide development. As a botanical entity displaying multifaceted biological functions, wormwood has received thorough scrutiny across multiple sectors. The insect repellency potency combined with antibacterial and antifungal activities of wormwood position it as a potential candidate for prospective development into eco-friendly chemical pesticides. In this research, Wormwood essential oil was procured via ethanol water under ultrasonic scenarios and subsequently diluted with PEG 400 to formulate green chemical pesticides. The defensive efficacy of this green pesticide on plants was validated through 2 weeks of clustered plant growth experiments. Active constituents that exerted their effects were scrutinized by GC-MS. Furthermore, this green pesticide also displays efficacious effects on the prevention and management of aphids, exhibiting a dose-dependent relationship. 4-terpenol, eucalyptol, carvacrol, and L-borneol were identified by GC-MS as the predominant active constituents in this green chemical pesticide. Wormwood can be leveraged to develop green chemical pesticides, which can protect plants without contaminating the environment.
Assuntos
Inseticidas , Óleos Voláteis , Inseticidas/química , Inseticidas/farmacologia , Animais , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Cimenos/química , Cimenos/farmacologia , Química Verde/métodos , Afídeos/efeitos dos fármacos , Eucaliptol/química , Eucaliptol/farmacologia , CanfanosRESUMO
OBJECTIVE: To establishe an analysis and identification method for 2-methylisoborneol(2-MIB) and geosmin(GSM) in water using purge and trap-gas chromatography-mass spectrometry. METHODS: The samples were enriched and analyzed using a purge and trap system, followed by the separation on a DB-624(30 m×0.25 mm, 1.4 µm) chromatographic column. Quantification was performed using gas chromatography-mass spectrometry with the selected ion monitoring and internal standard calibration. RESULTS: The calibration curves for 2-MIB and GSM showed an excellent linearity in the range of 1 to 100 ng/L with R~2 values greater than 0.999. The detection limit and quantification limit for both 2-MIB and GSM were 0.33 ng/L and 1.0 ng/L, respectively. Spike recovery experiments were further carried on the source water and drinking water at three concentration levels. It showed that the average recoveries were from 82.0% to 111.0% for 2-MIB while 84.0% to 110% for GSM. Additionally, the test precision of 2-MIB and GSM ranged from 1.9% to 7.3% and 1.9% to 5.0%(n=6), respectively. The analysis of multiple samples including the local source water, treated water and distribution network water confirmed the existence of 2-MIB and GSM. CONCLUSION: Compared to the national standard(GB/T 5750.8-2023), the proposed method enables fully automated sample introduction and analysis without the extra pre-treatment. It provides the advantages of simplicity, good repeatability and high accuracy.
Assuntos
Água Potável , Naftóis , Poluentes Químicos da Água , Água/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Água Potável/análise , Canfanos/análise , Poluentes Químicos da Água/análise , Odorantes/análiseRESUMO
Cinnamomum camphora chvar. borneol, a rare camphor tree variant recently identified in China, is distinguished by its high concentration of D-borneol, also known as " plant gold" due to its significant value. The essential oil extracted from this variant,rich in monoterpenes and sesquiterpenes, demonstrates a broad spectrum of pharmacological activities, including analgesic, antiinflammatory, antioxidant, cognition-enhancing, anti-bacterial, and insecticidal effects. These properties, underscored by extensive research, highlight the oil's potential in the biomedical, chemical, and food sectors as a valuable commodity. Nonetheless, the safety profile of this valuable oil remains poorly characterized, with its chemical composition and therapeutic efficacy subject to variations in the factors like geographic origin, harvesting timing, part used for extraction, and processing techniques. Such variability poses challenges to its clinical application and hampers the efficient exploitation of this resource. This review synthesizes current studies on C. camphora chvar. borneol essential oil and provides a detailed examination of its chemical and pharmacological profiles. In this study, we discuss existing research gaps and propose strategies for advancing its clinical use and industrial application, aiming to provide a foundational reference for future investigations and the resolution of its commercial and therapeutic challenges.
Assuntos
Canfanos , Cinnamomum camphora , Óleos Voláteis , Cinnamomum camphora/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Humanos , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologiaRESUMO
2-Methylisoborneol is a widespread musty odourant that is produced by many bacteria including actinomycetes, cyanobacteria and myxobacteria. Two 2-methylisoborneol synthases (MIBS) that are phylogenetically distant to the known enzyme from Streptomyces coelicolor were found to be highly active for 2-methylisoborneol biosynthesis. Based on the enzyme structure and on an amino acid sequence alignment, the MIBS from S. coelicolor was extensively studied through site-directed mutagenesis.
Assuntos
Streptomyces coelicolor , Sequência de Aminoácidos , Streptomyces coelicolor/genética , Streptomyces coelicolor/metabolismo , Canfanos/química , Canfanos/metabolismo , Mutagênese Sítio-DirigidaRESUMO
Epilepsy is one common brain disorder, which is not well controlled by current pharmacotherapy. In this study we characterized the therapeutic potential of borneol, a plant-derived bicyclic monoterpene compound, in the treatment of epilepsy and elucidated the underlying mechanisms. The anti-seizure potency and properties of borneol were assessed in both acute and chronic mouse epilepsy models. Administration of (+)-borneol (10, 30, 100 mg/kg, i.p.) dose-dependently attenuated acute epileptic seizure in maximal-electroshock seizure (MES) and pentylenetetrazol (PTZ)-induced seizure models without obvious side-effect on motor function. Meanwhile, (+)-borneol administration retarded kindling-induced epileptogenesis and relieved fully kindled seizures. Importantly, (+)-borneol administration also showed therapeutic potential in kainic acid-induced chronic spontaneous seizure model, which was considered as a drug-resistant model. We compared the anti-seizure efficacy of 3 borneol enantiomers in the acute seizure models, and found (+)-borneol being the most satisfying one with long-term anti-seizure effect. In electrophysiological study conducted in mouse brain slices containing the subiculum region, we revealed that borneol enantiomers displayed different anti-seizure mechanisms, (+)-borneol (10 µM) markedly suppressed the high frequency burst firing of subicular neurons and decreased glutamatergic synaptic transmission. In vivo calcium fiber photometry analysis further verified that administration of (+)-borneol (100 mg/kg) inhibited the enhanced glutamatergic synaptic transmission in epilepsy mice. We conclude that (+)-borneol displays broad-spectrum anti-seizure potential in different experimental models via decreasing the glutamatergic synaptic transmission without obvious side-effect, suggesting (+)-borneol as a promising anti-seizure compound for pharmacotherapy in epilepsy.
Assuntos
Epilepsia , Excitação Neurológica , Camundongos , Animais , Anticonvulsivantes/farmacologia , Anticonvulsivantes/uso terapêutico , Epilepsia/induzido quimicamente , Epilepsia/tratamento farmacológico , Canfanos/uso terapêutico , Canfanos/farmacologia , Excitação Neurológica/fisiologia , Convulsões/induzido quimicamente , Convulsões/tratamento farmacológico , Modelos Animais de DoençasRESUMO
Borneol is an example of traditional Chinese medicine widely used in Asia. There are different isomers of chiral borneol in the market, but its toxicity and effects need further study. In this study, we used zebrafish embryos to examine the effects of exposure to three isomers of borneol [(-)-borneol, (+)-borneol, and isoborneol] on heart development and the association with Na+ /K+ -ATPase from 4 h post-fertilization (4 hpf). The results showed that the three isomers of borneol increased mortality and decreased hatching rate when the zebrafish embryo developed to 72 hpf. All three isomers of borneol (0.01-1.0 mM) significantly reduced heart rate from 48 to 120 hpf and reduced the expression of genes related to Ca2+ -ATPase (cacna1ab and cacna1da) and Na+ /K+ -ATPase (atp1b2b, atp1a3b, and atp1a2). At the same time, the three isomers of borneol significantly reduced the activities of Ca2+ -ATPase and Na+ /K+ -ATPase at 0.1 to 1.0 mM. (+)-Borneol caused the most significant reduction (p < 0.05), followed by isoborneol and (-)-borneol. Na+ /K+ -ATPase was mainly expressed in otic vesicles and protonephridium. All three isomers of borneol reduced Na+ /K+ -ATPase mRNA expression, but isoborneol was the most significant (p < 0.01). Our results indicated that (+)-borneol was the least toxic of the three isomers while the isoborneol showed the most substantial toxic effect, closely related to effects on Na+ /K+ -ATPase.
Assuntos
Cardiotoxicidade , Peixe-Zebra , Animais , Peixe-Zebra/metabolismo , Canfanos/toxicidade , ATPase Trocadora de Sódio-Potássio/genética , ATPase Trocadora de Sódio-Potássio/metabolismoRESUMO
Common valerian is a medicinal plant. The underground organs of this species are used as a mild sedative and sleeping aid. Poland is one of the largest producers of this raw material in Europe, with local cultivar 'Lubelski' as a primary cultivated form. Although valerian is the subject of more or less deliberate selection carried out by farmers, it is still genetically unstable. The aim of this study was to determine the diversity of the 'Lubelski' cultivar originating from four regions of Poland (forms: L1-L4) in relation to wild-growing populations of the species. The plants were assessed in terms of the mass of underground organs and the content of valerenic acids and essential oils (EOs). The content of valerenic acids was determined using HPLC, whereas the content of EOs was determined using hydrodistillation. The composition of EOs was assessed using GC-MS GC-FID. The ploidy level of the analyzed objects was determined as well. Wild-growing populations (diploids) were characterized by lower masses of underground organs and lower contents of valerenic acid than cultivated forms (tetraploids). However, they produced higher contents of EOs. All the cultivated forms were strongly diversified with respect to the analyzed traits, including the mass of the roots (CV 49-75%), the content of valerenic acids (CV 18-55%), and the content of EOs (CV 28-57%). A total of 44 compounds were identified in the EOs. The dominant compound of both wild-growing populations and the 'Lubelski' forms were: α-fenchene, bornyl acetate, and valerenal. Among 'Lubelski' forms, the most interesting seems to be the L2 form, which was characterized by a relatively high yield and high content of valerenic acids and EOs. Thus, it appears to be a promising source of objects for further valerian cultivar improvement.
Assuntos
Valeriana , Polônia , Valeriana/genética , Europa (Continente) , Canfanos , Cromatografia GasosaRESUMO
Fenchone (a bicyclic monoterpene) is present in the essential oils of plant species like Foeniculum vulgare and Peumus boldus and is used to treat GIT disorders. Research reports have indicated its strong anti-inflammatory, antioxidant, and anti-nociceptive properties. The present study was designed to investigate fenchone's anti-arthritic effects in a rat model of chronic joint inflammation (Complete Freud's Adjuvant-mediated inflammation [CFA]). Molecular docking analysis revealed a high binding interaction of fenchone with inducible nitric oxide synthase (iNOS), Interleukin-17, Prostaglandin E Receptor EP4, and Cycloxygenase-2 (COX-2), indicating its anti-inflammatory efficacy using computational tests. Fenchone treatment at 100 mg/kg, 200 mg/kg, and 400 mg/kg significantly enhanced the tail-flick latency when compared with the solvent-treated group. Correspondingly, the raised mRNA values of iNOS, IL-17, IL-1ß, IL-6, TNF-α, and COX-2 in solvent-treated group were significantly reduced following treatment with fenchone. Moreover, fenchone significantly lowered spleen and thymus indices, Nitric oxide (NO) and PGE2 values as compared to solvent-treated group. Hence, the results of the present study indicated that fenchone has a potent anti-inflammatory effect by inhibiting pro-inflammatory markers and thus may have therapeutic potential for chronic joint inflammation as well as chronic inflammatory disorders.
Assuntos
Artrite , Prostaglandinas , Animais , Ratos , Proteína C-Reativa , Óxido Nítrico , Ureia , Ciclo-Oxigenase 2 , Simulação de Acoplamento Molecular , Inflamação/tratamento farmacológico , Canfanos , Adjuvante de Freund , Monoterpenos/farmacologiaRESUMO
Hypertension is the main risk factor of cardiovascular and cerebrovascular diseases. In this paper, a novel compound known as 221s (2,9), which includes tanshinol, borneol and a mother nucleus of ACEI, was synthesized by condensation esterification, deprotection, amidation, deprotection, and amidation, with borneol as the initial raw material, using the strategy of combinatorial molecular chemistry. The structure of the compound was confirmed by 1H NMR, 13C NMR, and high-resolution mass spectrometry, with a purity of more than 99.5%. The compound 221s (2,9) can significantly reduce the systolic and diastolic blood pressure of SHR rats by about 50 mmHg and 35 mmHg after 4 weeks of administration. The antihypertensive effect of 221s (2,9) is equivalent to that of captopril. The use of 221s (2,9) can reduce the content of Ren, Ang II and ACE in the serum of SHR rats, inhibit the RAAS and enhance the vascular endothelial function by upregulating the level of NO. Pathological studies in this area have shown that high dosage of 221s (2,9) can notably protect myocardial fibrosis in rats and reduce the degeneration and necrosis of myocardial fibers, inflammatory cell infiltration, and proliferation of fibrous tissue in the heart of rat. Therefore, the existing work provided a foundation for preclinical research and follow-up clinical research of 221s (2,9) as a new drug.
Assuntos
Anti-Hipertensivos , Hipertensão , Ratos , Animais , Anti-Hipertensivos/uso terapêutico , Ratos Endogâmicos SHR , Canfanos/farmacologia , Pressão Sanguínea , Miócitos CardíacosRESUMO
Escherichia coli is considered the main cause of intestinal and extra-intestinal infections, they have virulence mechanisms in different pathotypes and the ability to receive or transmit antimicrobial resistance genes. The aim of this work was to investigate the antibacterial and antimicrobial modulating activity of α-pinene and borneol against E. coli and enteropathogenic (EPEC) and enterotoxigenic (ETEC) serotypes. The broth microdilution methodology with multidrug-resistant Escherichia coli, EPEC and ETEC was used to determine the Minimum Inhibitory Concentration (MIC) and evaluation of the modulating activity of antibiotics (ciprofloxacin, sulfamethoxazole-trimethoprim and metronidazole) of α-pinene and borneol. It was concluded that α-pinene and borneol showed a low antimicrobial action against multi-resistant E. coli, however, this action was not observed against the EPEC and ETEC serotypes. A synergistic action of borneol associated with ciprofloxacin against ETEC was noted.
Assuntos
Escherichia coli Enteropatogênica , Escherichia coli Enterotoxigênica , Infecções por Escherichia coli , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Monoterpenos Bicíclicos , Canfanos , Diarreia/tratamento farmacológico , Infecções por Escherichia coli/tratamento farmacológico , HumanosRESUMO
One of the characteristic aspects of odour sensing in humans is the activation of olfactory receptors in a slightly different manner in response to different enantiomers. Here, we focused on whether plants showed enantiomer-specific response similar to that in humans. We exposed Arabidopsis seedlings to methanol (control) and (+)- or (-)-borneol, and found that only (+)-borneol reduced the root length. Furthermore, the root-tip width was more increased upon (+)-borneol exposure than upon (-)-borneol exposure. In addition, root-hair formation was observed near the root tip in response to (+)-borneol. Auxin signalling was strongly reduced in the root tip following exposure to (+)-borneol, but was detected following exposure to (-)-borneol and methanol. Similarly, in the root tip, the activity of cyclin B1:1 was detected on exposure to (-)-borneol and methanol, but not on exposure to (+)-borneol, indicating that (+)-borneol inhibits the meristematic activity in the root. These results partially explain the (+)-borneol-specific reduction in the root length of Arabidopsis. Our results indicate the presence of a sensing system specific for (+)-borneol in Arabidopsis.