RESUMO
Insomnia, a widespread public health issue, is associated with substantial distress and daytime functionality impairments and can predispose to depression and cardiovascular disease. Cognitive Behavioral Anti-insomnia therapies including benzodiazepines often face limitations due to patient adherence or potential adverse effects. This study focused on identifying novel bioactive compounds from medicinal plants, aiming to discover and develop new therapeutic agents with low risk-to-benefit ratios using computational drug discovery methods. Through a systematic framework involving compound library preparation, evaluation of drug-likeness and pharmacokinetics, toxicity prediction, molecular docking, and molecular dynamic simulations, two natural compounds such as 2-(4-hydroxy-3-methoxyphenyl)-8-methoxy-6-prop-2-enyl-3,4-dihydro-2H-chromen-3-ol from Ocimum tenuiflorum and 7-(2-hydroxypropan-2-yl)-1,4a-dimethyl-9-oxo-3,4,10,10a-tetrahydro-2H-phenanthrene-1-carboxylic acid from Poria cocos exhibited high binding affinity with orexin receptor type 1 (OX1R) and type 2 (OX2R), surpassing commercial drugs used in insomnia treatment. Additionally, they showed interactions with critical amino acid residues within the receptors that play crucial roles in competitive inhibitor activity, like commercial drugs such as Suvorexant, Lemborexant, and Daridorexant. Further, molecular dynamics simulations of the protein-ligand complexes under conditions that mimic the in vivo environment revealed both compounds' sustained and robust interactions with the OX1R and OX2R, reinforcing their potential as effective therapeutic candidates. Furthermore, upon evaluating both compounds' drug-likeness, pharmacokinetics, and toxicity profiles, it was discerned that they displayed considerable drug-like properties and favorable pharmacokinetics, along with diminished toxicity. The research provides a solid foundation for further exploring and validating these compounds as potential anti-insomnia therapeutics.
Assuntos
Simulação de Acoplamento Molecular , Ocimum , Distúrbios do Início e da Manutenção do Sono , Distúrbios do Início e da Manutenção do Sono/tratamento farmacológico , Humanos , Ocimum/química , Simulação de Dinâmica Molecular , Extratos Vegetais/química , Extratos Vegetais/uso terapêuticoRESUMO
Mosquitoes stand out as the most perilous and impactful vectors on a global scale, transmitting a multitude of infectious diseases to both humans and other animals. The primary objective of the current research was to assess the effectiveness of EOs from Ocimum tenuiflorum L. and Ocimum americanum L. in controlling Anopheles stephensi Liston. Culex quinquefasciatus Say and Aedes aegypti L. mosquitoes. The larvae, pupae and eggs of the mosquitoes were exposed to four different concentrations (6.25-50 ppm). The tested EOs resulted in >99-100 % mortality at 120 h for the eggs of all examined mosquito species. It also showed robust larvicidal and pupicidal activity with LC50 and LC90 values of 17-39, 23-60 ppm and 46-220, and 73-412 ppm against Aedes, Culex and Anopheles mosquito species, respectively, at 24 h of treatment. The Suitability Index or Predator Safety Factor demonstrated that the EOs extracted from O. tenuiflorum L. and O. americanum L. did not cause harm to P. reticulata, D. indicus (water bug), G. affinis and nymph (dragonfly). GC-MS analysis identified the major probable constituents of the oil, including Phenol, 2-Methoxy-4-(1-Propenyl)- (28.29 %); 1-Methyl-3-(1'-Methylcyclopropyl) Cyclopentene (46.46 %); (E,E,E)-3,7,11,15-Tetramethylhexadeca-1,3,6,10,14-Pentaene (18.91 %) and 1,3-Isobenzofurandione, 3a,4,7,7a-Tetrahydro-4,7-Dimethyl (33.02 %). These constituents may play a significant role in the mosquitocidal activity of the oil. The same results were identified in the formulation prepared from the EOs. This marks the first report confirming the successful utilization of EOs derived from O. tenuiflorum L. and O. americanum L. in mosquito population control initiatives.
Assuntos
Aedes , Anopheles , Culex , Inseticidas , Ocimum , Odonatos , Óleos Voláteis , Animais , Humanos , Óleos Voláteis/farmacologia , Óleos Voláteis/análise , Ocimum/química , Ocimum sanctum , Mosquitos Vetores , Inseticidas/análise , Larva , Extratos Vegetais/química , Folhas de Planta/químicaRESUMO
The composition of essential oils varies according to culture conditions and climate, which induces a need for simple and inexpensive characterization methods close to the place of extraction. This appears particularly important for developing countries. Herein, we develop an analytical strategy to determine the thymol content in Ocimum Gratissimum, a medicinal plant from Benin. The protocol is based on electrochemical techniques (cyclic and square wave voltammetry) implemented with a low cost potentiostat. Thymol is a phenol derivative and was directly oxidized at the electrode surface. We had to resort to submillimolar concentrations (25-300 µM) in order to minimize production of phenol oligomers that passivate the electrode. We worked first on two essential oils and realized that in one of them the thymol concentration was below our detection method. These results were confirmed by gas chromatography - mass spectrometry. Furthermore, we optimized the detection protocol to analyze an infusion made directly from the leaves of the plant. Finally, we studied whether the cost of the electrochemical cell may also be minimized by using pencil lead as working and counter electrodes.
Assuntos
Ocimum , Óleos Voláteis , Plantas Medicinais , Timol/análise , Ocimum/química , Óleos Voláteis/química , Folhas de Planta/química , Fenóis/análise , Óleos de Plantas/análiseRESUMO
BACKGROUND: Ocimum americanum L. (O. americanum) and Ocimum basilicum L. (O. basilicum) are highly valued aromatic medicinal plants. Their leaves are widely used as spices in traditional cuisine. Their essential oils (EOs) are extensively used in food, cosmetic, and pharmaceutical industries. This study aimed to investigate the main chemical profiles of O. americanum and O. basilicum leaf EOs and assess their effects on antibacterial, antioxidant, and larvicidal properties. METHODS: EOs were extracted from the leaves of O. basilicum and O. americanum using steam distillation in a Clevenger-type apparatus. The chemical constituents of the EOs were analyzed using gas chromatography-mass spectrometry. 2,2-Diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP), and metal-chelating techniques were used to assess the free-radical scavenging capability of the oils. The extracted oils were also tested for their antibacterial activities via a disk-diffusion test and the broth microdilution method. Furthermore, the mosquito larvicidal (Aedes aegypti) activity was tested using standard protocols. RESULTS: Camphor (33.869%), limonene (7.215%), longifolene (6.727%), caryophyllene (5.500%), and isoledene (5.472%) were the major compounds in O. americanum leaf EO. The EO yield was 0.4%, and citral (19.557%), estragole (18.582%) camphor (9.224%) and caryophyllene (3.009%) were the major compounds found among the 37 chemical constituents identified in O. basilicum oil. O. basilicum exhibited a more potent antioxidant activity in DPPH, FRAP, and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid tests than O. americanum. The zones of inhibition and minimum inhibitory concentration of the oils in the microdilution and disk diffusion methods were 8.00 ± 0.19 mm to 26.43 ± 2.19 mm and 3.12-100 µg/mL, respectively. At 400 ppm, O. basilicum and O. americanum EOs demonstrated larvicidal activity, with mortality ratios of 73.60% ± 0.89% and 78.00% ± 1.00%, respectively. Furthermore, after 30 min of exposure to O. americanum and O. basilicum EOs, the larval death rates were 73.60% ± 0.89% and 78.00% ± 1.00%, respectively. CONCLUSIONS: The findings revealed that the EOs extracted from the leaves of O. basilicum and O. americanum exhibited reasonable antioxidant, antibacterial, and mosquito larvicidal potentials, and can be used as alternative medicine for the treatment of human health and larvicidal mosquito control.
Assuntos
Anti-Infecciosos , Ocimum basilicum , Ocimum , Óleos Voláteis , Humanos , Antioxidantes/química , Ocimum basilicum/química , Cânfora/análise , Ocimum/química , Anti-Infecciosos/química , Óleos Voláteis/química , Antibacterianos/farmacologia , Antibacterianos/análise , Folhas de Planta/químicaRESUMO
INTRODUCTION: Selection of marker compounds for targeted chemical analysis is complicated when considering varying instrumentation and closely related plant species. High-resolution gas chromatography-mass spectrometry (GC-MS), via orbitrap detection, has yet to be evaluated for improved marker compound selection. OBJECTIVE: This study directly compares high- and low-resolution GC-MS for botanical maker compound selection using Ocimum tenuiflorum L. (OT) and Ocimum gratissimum L. (OG) for botanical ingredient authentication. METHODS: The essential oils of OT and OG were collected via hydrodistillation before untargeted chemical analysis with gas chromatography coupled to single-quadrupole (GC-SQ) and orbitrap (GC-Orbitrap) detectors. The Global Natural Products Social Molecular Networking (GNPS) software was used for compound annotation, and a manual search was used to find the 41 most common Ocimum essential oil metabolites. RESULTS: The GC-Orbitrap resulted in 1.7-fold more metabolite detection and increased dynamic range compared to the GC-SQ. Spectral matching and manual searching were improved with GC-Orbitrap data. Each instrument had differing known compound concentrations; however, there was an overlap of six compounds with higher abundance in OG than OT and three compounds with a higher abundance in OT than OG, suggesting consistent detection of the most variable compounds. An unsupervised principal component analysis (PCA) could not discern the two species with either dataset. CONCLUSION: GC-Orbitrap instrumentation improves compound detection, dynamic range, and feature annotation in essential oil analysis. However, considering both high- and low-resolution data may improve reliable marker compound selection, as GC-Orbitrap analysis alone did not improve unsupervised separation of two Ocimum species compared to GC-SQ data.
Assuntos
Ocimum , Óleos Voláteis , Óleos Voláteis/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Ocimum/químicaRESUMO
Faced with the serious consequences resulting from the abusive and repeated use of synthetic chemicals, today rethinking crop protection is more than necessary. It is in this context that the essential oils of the Lamiaceae Ocimum gratissimum and Ocimum canum, the Poaceae Cymbopogon citratus and nardus and a Rutaceae Citrus sp. of known chemical compositions were experimented. The evaluation of the larvicidal potential of the essential oils was done by the method of topical application of the test solutions, on the L1-L2 stage larvae from the first generation of S. frugiperda obtained after rearing in an air-conditioned room. Lethal concentrations (LC10 , LC50 and LC90 ) were determined after 48â h. After assessing the larvicidal potential of essential oils, molecular docking was carried out to study protein-ligand interactions and their propensity to bind to insect enzyme sites (AChE). The essential oil of O. gratissimum was the most effective with the lowest lethal concentrations (LC10 =0.91 %, LC50 =1.91 % and LC90 =3.92 %). The least toxic oil to larvae was Citrus sp. (LC10 =5.44 %, LC50 =20.50 % and LC90 =77.41 %). Molecular docking revealed that p-cymene and thymol from O. gratissimum essential oil are structurally similar and bind to the AChE active site via predominantly hydrophobic interactions and a H-bond with Tyr374 in the case of thymol. The essential oil of O. gratissimum constitutes a potential candidate for the development of biological insecticides for the fight against insect pests and for the protection of the environment.
Assuntos
Inseticidas , Ocimum , Óleos Voláteis , Animais , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Spodoptera , Óleos de Plantas/química , Simulação de Acoplamento Molecular , Timol/farmacologia , Côte d'Ivoire , Ocimum/química , Inseticidas/farmacologia , LarvaRESUMO
The chemical composition of the volatile fraction of Ocimum gratissimum concrete (romba) from Madagascar has been determined for the first time by GC/MS and GC-FID. A methyl cinnamate chemotype has been determined for this material, along with a set of compounds typical in essential oils and extracts from plants of the Ocimum genus. Variability was mostly observed on terpenes and terpenoids components. GC-O-MS was also used for a sensory evaluation of this material performed by a master perfumer. The chemical composition of this O. gratissimum extract was then compared with literature data to assess subtle differences between chemotypes of the same species and other species of the same genus within natural variability. A mapping illustrates the occurrence of the cinnamate chemotype in Eastern Africa, India and now Madagascar, while other origins generally present eugenol, thymol, camphor, or linalool chemotypes.
Assuntos
Ocimum , Óleos Voláteis , Ocimum/química , Madagáscar , Óleos Voláteis/química , Eugenol/análise , Timol/análise , Óleos de Plantas/químicaRESUMO
BACKGROUND: The aerial part of Ocimum lamiifolium is commonly used in Ethiopian traditional medicine. Although this plant is mostly used in traditional medicine, its safety profile has not been documented yet. The aim of this study was to assess the sub-chronic toxicity of O. lamiifolium aqueous extract in rats and to determine the toxicity profile of GC-MS identified bioactive compounds obtained from essential oil of O. lamiifolium using in silico toxicity methods. METHODS: Eighty rats (40 male and 40 female) were randomly assigned to four groups of ten rats per sex/group. For 90 days, Groups I-III received 200, 400, and 600 mg/kg bw of aqueous extract of O. lamiifolium, respectively. Distilled water was given to Group IV (control). Clinical observations, food intake, and rat weight were all recorded during the experiment. In addition, several biochemical parameters, organ weight, and histology of the liver and kidney were all evaluated. For the in-silico toxicity study, GC-MS identified bioactive compounds in O. lamiifolium essential oil were obtained from published articles. The compounds two-dimensional structures were constructed using Chemdraw. The two-dimensional structures were converted into a simplified molecular input line entry system (SMILES) using the Swiss ADMET web tool. Furthermore, the toxicity parameters were predicted using the ProTox II server. RESULTS: The administration of an aqueous extract of O. lamiifolium leaves significantly (p < 0.05) reduced the test animals' food intake and body weight gain. In the high dose (600 mg/kg bw) treated group, the serum alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase levels were significantly increased (p < 0.05). In female rats given 600 mg/kg bw of O. lamiifolium, the levels of serum urea were also increased. In addition, rats given 600 mg/kg bw had significantly lower blood glucose levels than the control group (p < 0.05). Doses up to 400 mg/kg bw didn't bring a significant change to the histology of the liver. However, in the high dose (600 mg/kg bw) treated group, some female rats' livers showed mild sinusoidal and central vein dilatation, as well as parenchymal necrosis. our findings showed that all compounds derived from the essential oil of O. lamiifolium showed no mutagenicity or cytotoxicity. However, 30% of the compounds tested were hepatotoxic, 20% carcinogenic, and 20% immunotoxin. CONCLUSION: Our findings showed that oral administration of O. lamiifoliums aqueous extract up to a dose of 400 mg/kg bw is not toxic. However, high-dose (600 mg/kg bw) significantly affected the food consumption and weight gain of the experimental rats and the serum concentration of some liver and kidney enzymes were also significantly increased. Additionally, a considerable proportion of the tested compounds were predicted to be hepatotoxic, carcinogenic and immunotoxin. Furthermore, before employing O. lamiifolium preparations as drugs, a chronic toxicity research on the essential oil as well as its components that exhibited toxicity in the in-silico toxicity study is needed. Finally, use high doses of O. lamiifolium leaves with caution.
Assuntos
Imunotoxinas , Ocimum , Animais , Ratos , Imunotoxinas/farmacologia , Rim , Fígado , Ocimum/química , Extratos Vegetais/farmacologiaRESUMO
Tropical vegetables remain one of the major sources of functional foods and nutraceuticals, while their constituent phytochemicals, especially alkaloids, have been reported to exhibit neuroprotective properties. Here, the protective effect of alkaloid extracts from Scent leaf (Ocimum gratissimum) and Water bitter leaf (Struchium sparganophora) on manganese (Mn)- induced toxicity in wild type fruit fly (Drosophila melanogaster) model was investigated. Flies were exposed to 30 mM of Mn, the alkaloid extracts (20 and 200 µg/g) and co-treatment of Mn plus extracts, respectively. The survival rate and locomotor performance of the flies were assessed 7 days post-treatment, after which the flies were homogenized and assayed for activities of acetylcholinesterase (AChE), monoamine oxidase (MAO), glutathione-S transferase (GST), catalase, superoxide dismutase SOD), as well as total thiol, reactive oxygen species (ROS) and neural L-DOPA levels. Results showed that the extract significantly reversed Mn-induced reduction in the survival rate and locomotor performance of the flies. Furthermore, both extracts counteracted the Mn-induced elevation in AChE and MAO activities, as well as reduced antioxidant enzyme activities, with a concomitant mitigation of Mn-induced elevated ROS and neural L-DOPA level. The HPLC characterization of the extracts revealed the presence of N-propylamine, Vernomine and Piperidine as predominant in Water bitter leaf extract, while 2, 6-dimethylpyrazine and sesbanimide were found in scent leaf extract. Therefore, the alkaloid extract of these leaves may thus be sources of useful nutraceuticals for the management of pathological conditions associated with manganese toxicity.
Assuntos
Alcaloides , Ocimum , Animais , Ocimum/química , Manganês/toxicidade , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Drosophila melanogaster , Espécies Reativas de Oxigênio , Água , Acetilcolinesterase , Levodopa/farmacologia , Odorantes , Antioxidantes/farmacologia , Alcaloides/farmacologia , Suplementos Nutricionais , Monoaminoxidase , Folhas de PlantaRESUMO
Background: This review is a great route for future researchers on the topic of alternative medicine. The review goes in depth with respect to Ocimum sanctum and its proposed mechanism of action for different types of cancers. Primary Study Objective: The primary objective of the study was to bring traditional therapy back, which can prove to be economically beneficial and may be helpful to many patients with cancer with few to no adverse events. Intervention: Ocimum sanctum (OS), commonly known as Holy Basil or tulsi, is a very important medicinal herb in parts of India and Southeast Asia. OS has been found to lower blood pressure and cholesterol, reduce the risk for heart attacks and may also be effective for treating depression and anxiety. It also protects the body from prolonged physical exertion, ischemia, exposure to cold and excessive noise, but its anti-tumorigenic effect remains largely unexplored. A few studies have observed that extracts of OS have inflammatory, analgesic, antipyretic, antidiabetic, hepatoprotective, hypolipidemic, anti-stress, and immunomodulatory activities. A few cell culture and animal studies have also shown that some of its phytochemicals like eugenol, rosmarinic acid, apigenin, myretenal, luteolin, ß-sitosterol and carnosic acid prevent chemical-induced skin, liver, oral and lung cancers and mediate these effects by increasing antioxidant activity, altering gene expression, inducing apoptosis and inhibiting angiogenesis and metastasis. They are also shown to prevent radiation-induced DNA damage. This review details the different chemoprotective and radioprotective properties of OS and also gives an idea for future research.
Assuntos
Neoplasias , Ocimum , Animais , Ocimum sanctum/química , Ocimum/química , Neoplasias/tratamento farmacológico , Extratos VegetaisRESUMO
The Nigerian Niger-Delta crude oil exploration often results in spills that affect indigenous medicinal plant biodiversity, likely changing the phytochemical profile of surviving species, their bioactivity or toxicity. In crude oil-rich Kokori and crude oil-free Abraka, classic examples of indigenous plants occupying the medicine-food interface include Vernonia amygdalina (VAL) and Ocimum gratissimum leaves (OGL). These plants are frequently utilised during pregnancy and in anaemia. To date, no scientific investigation has been reported on the potential changes to the phytochemical or bioactivity of the study plants. To discuss the similarities and dissimilarities in antisickling bioactivity and phytochemicals in VAL and OGL collected from Kokori (VAL-KK and OGL-KK) and Abraka (VAL-AB and OGL-AB), in silico, in vitro and comparative UPLC-QTOF-MS analysis was performed. Nine unique compounds were identified in OGL-KK, which have never been reported in the literature, while differences in antisickling potentials were observed in VAL-KK, OGL-KK and, VAL-AB, OGL-AB. Our findings show that VAL-AB and OGL-AB are richer and more diverse in phytochemicals and displayed a slightly higher antisickling activity than VAL-KK and OGL-KK. Ligand-based pharmacophore modelling was performed to understand the potential compounds better; this study may provide a basis for explaining the effect of crude oil spills on secondary metabolites and a reference for further research.
Assuntos
Ocimum , Petróleo , Plantas Medicinais , Vernonia , Ocimum/química , Vernonia/química , Folhas de Planta , Extratos Vegetais/farmacologiaRESUMO
The present study evaluated the acaricidal and anthelmintic action of Ocimum basilicum essential oil and its main components against ticks and helminth parasites as well as to relate these activities to acetylcholinesterase inhibition. The in vitro acaricidal activity against Hyalomma scupense was evaluated by Adult Immersion Test (AIT) and Larval Packet Test (LPT), while the in vivo nematocidal potential was assessed in laboratory mice infected with Heligmosomoides polygyrus using fecal egg count reduction (FECR) and total worm count reduction (TWCR). Chemical analyzes were performed by gas chromatography coupled to mass spectrometry (GC-MS). Estragole (80.87%) and linalool (16.12%) were the major compounds detected in O. basilicum essential oil. In the AIT assay for H. scupense tick, LC50 of estragole, O. basilicum oil and linalool were 0.73, 0.81 and 0.97 mg/mL, respectively. In LPT, estragole, linalool and essential oil showed LC50 of 0.22, 1.11 and 1.19 mg/mL, respectively. Against He. polygyrus, the highest activity was observed with estragole administered at 100 mg/kg body weight (bwt), which resulted in a FECR of 90.86% and a TWCR of 82.91%. The O. basilicum essential oil, estragole and linalool inhibited the enzyme acetylcholinesterase (AChE) extracted from both parasites species. Estragole was found the most active AChE inhibitor with IC50 of 0.176 mg/mL for H. scupense and IC50 of 0.138 mg/mL for He. polygyrus larvae. The results of the present study pointed out the importance of the traditional use of O. basilicum as an eco-friendly alternative against endo and ectoparasites. In vivo trials should also be conducted to confirm the above-mentioned activities and to assure the safe use of natural plants.
Assuntos
Acaricidas , Anti-Helmínticos , Ocimum basilicum , Ocimum , Óleos Voláteis , Acaricidas/farmacologia , Acetilcolinesterase , Monoterpenos Acíclicos , Derivados de Alilbenzenos , Animais , Anisóis , Camundongos , Ocimum/química , Ocimum basilicum/química , Óleos Voláteis/química , Óvulo , Óleos de Plantas/farmacologiaRESUMO
Ocimum sanctum is a sacred herb of India and is commonly known as 'Tulsi' or 'Holy Basil' in regional languages of the country. Various parts of O. sanctum are recognised to have remarkable therapeutic efficacy, and are therefore used in Indian traditional medicine system, Ayurveda. Scientific studies have shown that O. sanctum has a range of pharmacological activities. The presence of a substantial amount of polyphenols in O. sanctum could be the reason for its excellent bioactivity. Polyphenols are used to prevent or treat oncologic diseases due to their anti-cancer effects, which are related to activation of apoptotic signaling, cell cycle arrest, binding ability with membrane receptors, and potential effects on immunomodulation and epigenetic mechanisms. The poor bioavailability of polyphenols restricts their clinical use. The application of nanonization has been implemented to improve their bioavailability, penetrability, and prolong their anticancer action. The present review analyses the recent preclinical studies related to the chemo-preventive and therapeutic potential of polyphenols present in O. sanctum. Moreover, the current article also examines in-depth the biochemical and molecular mechanisms involved in the antineoplastic actions of the considered polyphenols.
Assuntos
Antineoplásicos , Ocimum , Óleos Voláteis , Humanos , Ocimum sanctum , Polifenóis/farmacologia , Ocimum/química , Extratos Vegetais/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêuticoRESUMO
Poly(lactic acid) (PLA) nanofibres containing different proportions of the essential oils from Ocimum basilicum L. and Ocimum gratissimum L. were prepared by solution blow spinning method. The essential oils were extracted by hydrodistillation and characterized by gas chromatography. MEV, contact angle, DSC and FTIR were used to characterize the nanofibres. The effect of bioative nanofibres on the growth of the fungus and on the production of ochratoxin A were evaluated using the fumigation test. Linalool, 1·8-cineole and camphor were the principal components of the essential oil from O. basilicum, and eugenol was the principal constituent in the oil from O. gratissimum. An increase in the average diameter of the nanofibres was observed with the addition of the essential oils. The essential oils acted as a plasticizer, resulting in a reduction in the crystallinity of the PLA. The encapsulation of essential oils in PLA nanofibres was verified by FTIR. An effective antifungal and antimicotoxygenic activity against Aspergillus ochraceus and Aspergillus westerdjikiae was observed for the bioative nanofibres. These results confirm the potential of PLA nanofibres containing the essential oils for the control of toxigenic fungi that cause the deterioration of food and are harmful to human health.
Assuntos
Nanofibras , Ocimum basilicum , Ocimum , Óleos Voláteis , Antifúngicos/farmacologia , Humanos , Ocimum/química , Ocimum basilicum/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Óleos de Plantas/química , Óleos de Plantas/farmacologia , PoliésteresRESUMO
This study aimed to revealed anti-inflammatory and antimicrobial activities of fermented Ocimum sanctum Linn. (FE). The fermentation process with Lactobacillus plantarum was compared with the solvent extraction methods. Antimicrobial activity against the growth of Staphylococcus aureus, Staphylococcus epidermidis, Propionibacterium acnes, Candida albicans, and Malassezia furfur was investigated via broth dilution method. High performance thin layer chromatography was used to determine eugenol content. The anti-inflammation was investigated by means of nuclear factor kappa B (NF-κB) expression inhibition by Western blot analysis. FE yielded the highest amount (11.93 % w/w), the highest eugenol content (39.3±12.6 % w/w), and the highest antimicrobial activities comparing to the extracts obtained from the solvent extractions. The fungal inhibition against M.â furfur 656 was equivalent to that of ketoconazole. Furthermore, the bacterial inhibition on S.â aureus and S.â epidermidis was compared to that of Penicillin G at minimum inhibitory concentration (MIC) of 0.125â mg/mL and 0.25â mg/mL, respectively. Interestingly, FE had lower MIC and minimum bactericidal concentration against P.â acnes than Penicillin G and also possessed comparable anti-inflammatory activity to indomethacin with the NF-κB suppression of 42.7±4.6 %. Therefore, FE are potentially natural anti-inflammation and antimicrobial agents for topical applications in the pharmaceutical and cosmetic industries.
Assuntos
Anti-Infecciosos , Ocimum , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Testes de Sensibilidade Microbiana , Ocimum/química , Ocimum sanctum , Extratos Vegetais/química , Couro Cabeludo , Staphylococcus aureusRESUMO
AIMS: To analyze the efficacy of eugenol on longevity by assessing its antioxidant effect using Caenorhabditis elegans as an animal model. BACKGROUND: Eugenol is a major polyphenolic component of Ocimum sanctum (Tulsi) which attributes wide pharmacological activities and can serve as a biomarker. However, the possible effect of eugenol on longevity in Caenorhabditis elegans has not been reported. OBJECTIVE: The objective of this investigation was to provide the first scientific based results about the effect of eugenol on longevity, slowing down of paralysis in Alzheimer's model and the mechanism behind it in Caenorhabditis elegans animal model system. METHODS: The phenolic components of methanolic extract of Ocimum sanctum were analyzed by RP-HPLC. Worms were exposed to different concentrations of extract and one of its components - eugenol. Lifespan, health span, survival in CL4176 Alzheimer's model and molecular mechanism were analyzed. RESULTS: Extract of Ocimum sanctum and eugenol increased lifespan and provided indemnity against pro-oxidants. It also significantly improved healthy ageing and slowed the progression of neurodegeneration in CL4176 Alzheimer's model of the worm by increasing survival against prooxidants and slowing down the paralysis. Longevity effect was independent of the DAF-16 as observed by using DAF-16::GFP and daf-16 null mutant strains. These results implicate eugenol as a potent therapeutic compound that may curtail ageing and age related disorders like- Alzheimer's disease. CONCLUSION: The present work demonstrated eugenol as a potential anti-ageing compound that may curtail ageing, improve heath span by enhancing resistance to oxidative stress and exerts its effect independent of DAF-16 pathway. So, it can be assumed that eugenol can be beneficial to humans as well, albeit further research is necessary before declaring it for human consumption.
Assuntos
Proteínas de Caenorhabditis elegans , Caenorhabditis elegans , Eugenol , Estresse Oxidativo , Doença de Alzheimer , Animais , Caenorhabditis elegans/efeitos dos fármacos , Caenorhabditis elegans/metabolismo , Proteínas de Caenorhabditis elegans/metabolismo , Proteínas de Caenorhabditis elegans/farmacologia , Modelos Animais de Doenças , Eugenol/farmacologia , Fatores de Transcrição Forkhead/metabolismo , Ocimum/química , Paralisia/tratamento farmacológico , Extratos Vegetais/farmacologiaRESUMO
Ocimum cufodontii ((Lanza) A.J.Paton) has been traditionally used in Ethiopia against bacteria. The extracts of the leaves and roots of O. cufodontii after silica gel column chromatography furnished compounds 1-5, compounds 3 and 4 are new natural products. The oil from the hydro-distillation of the leaves, after analyzed with GC-MS, has led to the identification of ß-caryophyllene as a principal component, suggesting the essential oil as medicine and spices to enhance the taste of food. The constituents of O. cufodontii were assessed for their antibacterial activity against E. coli, K. pneumonia, S. typhymurium and S. aureus. The best activity was displayed against S. aureus by the hexane extract of the roots, compound 4, and the essential oil with an inhibition zone of 17, 15, and 19 mm, respectively. Molecular docking analysis revealed that compound 1 has better docking efficiency and forms hydrophobic interactions with five amino acids (ARG192, PHE196, GLU185, GLU193, and LYS189). This suggests that the compounds may act as potential inhibitors of DNA gyrase. The constituents were also assessed for their antioxidant activities using DPPH, ferric thicyanate and ferric reducing power assay. The hexane extracts of the roots inhibited the DPPH radical and peroxide formation by 90.5 and 83%, respectively, suggesting the potential of the extract as an antioxidant. Furthermore, the hexane extract of the roots of O. cufodontii exhibited the maximum reducing power compared with the EtOAc and methanol extracts. Hence, the activity displayed herein indicated as the plant has great potential as a remedy for diseases caused by bacteria and radicals.
Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Ocimum/química , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Antibacterianos/química , Antioxidantes/química , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Cromatografia Gasosa-Espectrometria de Massas , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Óleos Voláteis/química , Extratos Vegetais/química , Folhas de Planta/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimentoRESUMO
Ultraviolet C (UVC) has been applied to treatment of infections in wounds for at least the last two decades, however, cells being treated can be damaged if exposure is prolonged, which calls for protective measures, such as drug or herbal pre-treatment, to minimize damage. Ocimum gratissimum contains plant polyphenols such as isoflavones and caffeic acid, which have antioxidant effects. We hypothesize that Ocimum gratissimum aqueous extracts (OGE) can inhibit UVC-induced oxidative damage on skin cells. In this study, HaCaT skin cells are used to test the protective effects of OGE on cell proliferation and migration after exposure to UVC radiation. Pretreatment with OGE (50~150µg/mL) before 40 J/m2 UVC exposure was able to restore survival from 32.25% to between 46.77% and 68.00%, and 80 J/m2 UVC exposure from 11.49% to between 19.07% and 43.04%. Morphological observation of primarily apoptotic cell death confirms the above findings. The flow cytometry analysis revealed that UVC increased the number of cells at the sub-G1 phase in a dose dependent manner, and when pre-treated with OGE the changes were partially reversed. Moreover, the wound healing test for observing migration showed that UVC 40-80 J/m2 decreased cell migration to 47-28% activity and 100 µg/mL OGE was able to restore cell activity to81-69% at day 3. Based on the above results, we suggest that OGE has a protective effect on UVC-induced inhibition of cell proliferation and migration of skin cells and thus has potential application in wound care.
Assuntos
Antioxidantes/farmacologia , Ocimum/química , Extratos Vegetais/farmacologia , Terapia Ultravioleta/efeitos adversos , Cicatrização/efeitos dos fármacos , Movimento Celular/efeitos dos fármacos , Movimento Celular/efeitos da radiação , Proliferação de Células/efeitos dos fármacos , Proliferação de Células/efeitos da radiação , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos da radiação , Células HaCaT , Humanos , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/efeitos da radiação , Raios Ultravioleta/efeitos adversos , Terapia Ultravioleta/métodos , Cicatrização/efeitos da radiaçãoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The population uses the aqueous extract as tea from leaves of Ocimum selloi Benth. (alfavaca) for pain and inflammation issues. This study is motivated by a lack of data about inflammation properties of O. selloi. AIM OF THE STUDY: This study investigated the chemical composition and anti-inflammatory activity, in mice models, of the aqueous extract (OSAE) and essential oil (OSEO) obtained from leaves of O. selloi. MATERIALS AND METHODS: The antioxidant activity and total phenolic content were evaluated for samples, although chemical composition was obtained by U-HPLC-DAD-ESI-MS for OSAE and GC-MS for OSEO. OSAE and OSEO were tested orally at doses of 30, 100 and 300 mg/kg at the carrageenan-induced pleurisy and paw edema, also mechanical hyperalgesia, in mice. RESULTS: Four glycosylated flavonoids and one organic acid were identified in OSAE, and nine substances in OSEO, the two majoritarian are E-anethole and methyl chavicol. Oral treatments with OSAE and OSEO significantly inhibited the carrageenan-induced pleurisy in female Swiss mice, besides OSAE and OSEO significantly prevented paw edema (after 1, 2, and 4 h), mechanical hyperalgesia (after 3 and 4 h), and cold hyperalgesia 3 h after carrageenan model in male Swiss mice. The dose of 300 mg/kg of OSEO reduced cold hyperalgesia 4 h after carrageenan. CONCLUSION: The results evidenced the anti-inflammatory, anti-edematogenic, anti-hyperalgesic, and anti-nociceptive potentials of both materials obtained from leaves of O. selloi, mainly OSAE, supporting the popular use of this species.
Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Ocimum/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/uso terapêutico , Antioxidantes/análise , Antioxidantes/farmacologia , Carragenina/toxicidade , Dexametasona/farmacologia , Dexametasona/uso terapêutico , Modelos Animais de Doenças , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Hiperalgesia/induzido quimicamente , Hiperalgesia/tratamento farmacológico , Leucócitos/efeitos dos fármacos , Masculino , Camundongos , Óleos Voláteis/uso terapêutico , Fenóis/análise , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Pleurisia/induzido quimicamente , Pleurisia/tratamento farmacológico , Soluções/químicaRESUMO
The present study aimed to detect the bioactive metabolites from Ocimum forskolei aerial parts which are responsible for the antiulcer activity of the total ethanol extract (TEE) as well as different fractions (petroleum ether, dichloromethane, ethyl acetate and aqueous). Six flavonoids were isolated from the dichloromethane fraction which was the most potent; with an ulcer index value of 2.67 ± 2.18*** and % inhibition of ulcer of 97.7%; following a bioassay-guided fractionation. The isolated flavonoids were subjected to molecular docking analysis in an attempt to explain their significant antiulcer potential, and the results revealed that salvitin followed by sideritiflavone were the main active ones acting against M3 and H-2 receptors, respectively. Moreover, a molecular dynamics simulation illustrated the formation of two persistent H-bonds between salvitin and the two amino acids of the active site (Asn507 and Asp147) formed in 42 and 65% of the frames, respectively.