RESUMO
BACKGROUND: Ocimum tenuiflorum L. is a highly traded medicinal with several therapeutic values. Green Tulsi and purple Tulsi are two subtypes in O. tenuiflorum and both have the same medicinal properties. Recent reports have revealed that purple Tulsi contains higher quantities of methyl eugenol (ME), which is moderately toxic and potentially carcinogenic. Therefore, we developed an allele-specific PCR (AS-PCR) method to distinguish the green and purple Tulsi. METHODS AND RESULT: Using the green Tulsi as a reference, 12 single nucleotide polymorphisms (SNPs) and 10 insertions/deletions (InDels) were identified in the chloroplast genome of the purple Tulsi. The C > T SNP at the 1,26,029 position in the ycf1 gene was selected for the development of the AS-PCR method. The primers were designed to amplify 521 bp and 291 bp fragments specific to green and purple Tulsi, respectively. This AS-PCR method was validated in 10 accessions from each subtype and subsequently verified using Sanger sequencing. Subsequently, 30 Tulsi powder samples collected from the market were subjected to molecular identification by AS-PCR. The results showed that 80% of the samples were purple Tulsi, and only 3.5% were green Tulsi. About 10% of the samples were a mixture of both green and purple Tulsi. Two samples (6.5%) did not contain O. tenuiflorum and were identified as O. gratissimum. CONCLUSION: The market samples of Tulsi were predominantly derived from purple Tulsi. The AS-PCR method will be helpful for quality control and market surveillance of Tulsi herbal powders.
Assuntos
Eugenol/análogos & derivados , Ocimum sanctum , Ocimum , Extratos Vegetais , Ocimum sanctum/genética , Ocimum/genética , Alelos , Reação em Cadeia da PolimeraseRESUMO
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
Background and Objectives: To investigate the antiplaque properties of two plant-based mouthwashes, Morinda citrifolia (MC) and Ocimum sanctum (OS), and their effect on TNF-α, IL-α, IL-ß, IL-2, and IL-6 in gingival crevicular fluid (GCF) of patients undergoing fixed orthodontic treatment. Materials and Methods: Seventy-five individuals were recruited according to defined inclusion and exclusion criteria. This study was structured into two distinct phases. Phase I was a combination of toothbrushing using toothpaste containing fluoride (Protocol A), while Phase II toothbrushing included fluoride toothpaste and use of a mouthwash (Protocol B). For Phase II, individuals participating in this study were allocated into different groups through a randomization process: Group 1-0.12% CHX, Group 2-5% MC, and Group 3-4% OS. Each individual's Phase I and Phase II scores were assessed. GCF was measured in three phases to determine the level of inflammatory biomarkers. The paired t-test evaluated the disparities between the pre- and post-plaque index. Categorical data were subjected to crosstab analysis to assess qualitative variables. The mean values of cytokine levels were presented. An unpaired t-test was employed to assess the levels of cytokines between individuals in Phase I and Phase II. Results: Toothbrushing, fluoride toothpaste, and the supplementary use of mouthwash (Phase II) resulted in mean plaque scores significantly lower than group A (p < 0.001). Cytokines TNF-α, IL-α, and IL-ß demonstrated a significant downward trend in herbal mouthwash users. Conclusions: In conjunction with fluoridated toothpaste and brushing, OS and MC can serve as a viable alternative to conventional synthetic mouthwash CHX. This combination demonstrates reducing mean plaque scores and diminishing the levels of cytokines TNF-α, IL-α, and IL-ß.
Assuntos
Morinda , Antissépticos Bucais , Humanos , Antissépticos Bucais/uso terapêutico , Fator de Necrose Tumoral alfa , Interleucina-2 , Interleucina-6 , Cremes Dentais , Líquido do Sulco Gengival , Fluoretos/uso terapêutico , Ocimum sanctum , CitocinasRESUMO
Smoking has been associated with an increased risk of asthma, lung cancer, cardiovascular diseases, chronic bronchitis, and a massive amount of oxidative stress. The present study was undertaken to determine the modulatory effects of Holi Basil/Tulsi, (Ocimum sanctum) leaf extract on cigarette smoke-induced pulmonary damage in mice. Cigarette smoke (CS) inhalation increased the levels of pulmonary lipid peroxidation, and reactive oxygen species and decreased the levels of glutathione. Histoarchitectural alterations and enhanced tissue lactate dehydrogenase (LDH) activity in pulmonary tissue was distinctly indicative of damage. Enhanced mucin production was also observed through mucicarmine and Alcian Blue-Periodic Acid Schiff (PAS) staining. Increased expression of MUC5AC was also observed. Alterations in the lung were also evident through FTIR studies. Administration of Ocimum sanctum leaf extract (80 mg/kg b.w) to CS exposed mice ameliorated these alterations to a greater extent. These findings are suggestive of the fact that Ocimum sanctum leaf extract effectively modulated CS-induced deleterious effects on pulmonary tissue.
Assuntos
Fumar Cigarros , Lesão por Inalação de Fumaça , Animais , Camundongos , Roedores , Ocimum sanctum , PulmãoRESUMO
BACKGROUND AND OBJECTIVE: Rheumatoid arthritis is a chronic progressive autoimmune disorder, characterised by destruction of cartilage and under line bones. Though exact etiology of rheumatoid arthritis (RA) remains unknown. It is believed that alteration in control of cellular or molecular responses is involved in the chronic inflammation. Earlier in RA patients it was observed the circulating RA specific biomarkers and immunoglobulin deposits in the synovial joints. Zinc Oxide Nanoparticles (ZnO NPs) is used as an anti-inflammatory and anticancer agent, however there is nil/very less scientific data shows the anti-arthritic activity of green synthesis ZnO nanoparticles (Ocimum sanctum water extract in-situ synthesis of ZnO NPs having active compound Caffeic acid and Rosmerinic acid). Hence, the present activity was planned to assess the anti-arthritic activity of ZnO NPs in CIA rats. METHODS: Arthritis in rats were induced by subcutaneous injection of collagen type II (CII) (200 µl) at the base of tail on day 0 followed by booster dose on day 14. ZnO NPs were given (2 mg/kg b.wt./day) orally for 20 days. At the end of the study serum, joint homogenate was used to assess the level of biomarkers (RF, a-CCP, a-CII and CRP) and inflammatory mediators. In addition, m-RNA expression of various genes such as Nuclear factor-kB (NF-kB), inflammatory mediators like tumour necrosis factor-α (TNF-α), cyclooxygenase-2 (COX-2) etc. were assayed in joint tissue. Finally all these biochemical and molecular results were confirmed by microscopic study of joint tissue. RESULTS: ZnO NPs, treated rats showed decrease in inflammation and clinical severity. This was related with decrease in the level of biomarkers (like RF, a-CCP and CRP), inflammatory mediators (TNF-α, COX-2) and activity of transcription factor NF-kB. All these findings were positively correlated with microscopic analysis of joint tissue that showed reduced inflammation and bone erosion in treated group. CONCLUSION: This study validates the anti-arthritic activity of ZnO NPs as it mitigates the arthritis related symptoms in CIA rats.
Assuntos
Artrite Experimental , Artrite Reumatoide , Nanopartículas , Óxido de Zinco , Ratos , Animais , Óxido de Zinco/farmacologia , Óxido de Zinco/uso terapêutico , Fator de Necrose Tumoral alfa , Ciclo-Oxigenase 2/metabolismo , Ocimum sanctum/metabolismo , Citocinas/metabolismo , Artrite Experimental/tratamento farmacológico , Artrite Experimental/patologia , Artrite Reumatoide/tratamento farmacológico , Inflamação/tratamento farmacológico , Colágeno Tipo II/efeitos adversos , Mediadores da Inflamação/metabolismo , Mediadores da Inflamação/uso terapêutico , BiomarcadoresRESUMO
Ocimum tenuiflorum L. is found throughout semitropical and tropical parts of Southeast Asia. In Nepal, O. tenuiflorum L. is popular with two variants: Krishna Tulsi consisting of purple-colored leaves and Sri Tulsi consisting of green-colored leaves. O. tenuiflorum L. is considered the queen of herbs and is a traditionally and clinically proven medicinal herb for its application and efficacy. However, no commercial pharmaceutical preparations of O. tenuiflorum L. are available using effervescent vehicles. Therefore, the present study aimed to compare the antioxidant activity of leaves from the two varieties of O. tenuiflorum L. and formulate and evaluate the quality parameters of effervescent granules of the potent extract. The antioxidant activity of O. tenuiflorum L. ethanolic extracts was evaluated by DPPH radical scavenging assay at 1, 10, and 100 µg/mL concentrations, where ascorbic acid was used as the positive control. The antioxidant activity of purple-leafed O. tenuiflorum L. was found to be higher than that of green-leafed O. tenuiflorum L. Therefore, effervescent granules of the ethanolic extract of purple-leafed O. tenuiflorum L. were formulated using the pharmaceutical excipients tartaric acid, citric acid, and sodium bicarbonate and the quality parameters of the granules were evaluated. The formulated granules met the quality parameters assessed from the angle of repose, bulk density, tapped density, Carr's Index, Hausner's ratio, effervescent cessation time, and stability studies. Thus, the formulated effervescent granules of O. tenuiflorum L. can be used for therapeutic purposes or as a functional food.
Assuntos
Ocimum , Plantas Medicinais , Ocimum sanctum , Antioxidantes , Extratos VegetaisRESUMO
Chronic lymphocytic leukemia (CLL) is an incurable neoplasm of B-lymphocytes, which accounts for about one-third of all leukemias. Ocimum sanctum, an herbaceous perennial, is considered as one of the important sources of drugs for the treatment of various diseases, including cancers and autoimmune diseases. The present study was designed to screen various phytochemicals of O. sanctum for discovering their potential to inhibit Bruton's tyrosine kinase (BTK), a well-known drug target of CLL. Various phytochemicals of O. sanctum were screened for their potential to inhibit BTK using several in silico protocols. First, the molecular docking approach was used to calculate the docking scores of the selected phytochemicals. Then, the selected top-ranked phytochemicals were screened for their physicochemical characteristics using ADME analysis. Finally, the stability of the selected compounds in their corresponding docking complexes with BTK was analysed using molecular dynamics simulations. Primarily, our observations revealed that, out of the 46 phytochemicals of O. sanctum, six compounds possessed significantly better docking scores (ranging from -9.2 kcal/mol to -10 kcal/mol). Their docking scores were comparable to those of the control inhibitors, acalabrutinib (-10.3 kcal/mol), and ibrutinib (-11.3 kcal/mol). However, after ADME analysis of these top-ranked six compounds, only three compounds (Molludistin, Rosmarinic acid, and Vitexin) possessed drug likeliness characteristics. During the MD analysis, the three compounds Molludistin, Rosmarinic acid, and Vitexin were found to remain stable in the binding pocket in their corresponding docking complexes with BTK. Therefore, among the 46 phytochemicals of O. sanctum tested in this study, the three compounds, Molludistin, Rosmarinic acid, and Vitexin are the best inhibitors of BTK. However, these findings need to be confirmed by biological experiments in the laboratory.
Assuntos
Leucemia Linfocítica Crônica de Células B , Humanos , Leucemia Linfocítica Crônica de Células B/tratamento farmacológico , Leucemia Linfocítica Crônica de Células B/metabolismo , Tirosina Quinase da Agamaglobulinemia/metabolismo , Simulação de Acoplamento Molecular , Ocimum sanctum/metabolismo , Inibidores de Proteínas Quinases/química , Ácido RosmarínicoRESUMO
BACKGROUND & OBJECTIVES: The main aim of this research is to provide literature on the Ocimum plant, and to know the significance of the Ocimum species carried out by pharmacognostic study and experimental design for GC-MS. Ocimum genus are very important for their therapeutic potential among the most important aromatic herbs. METHODS: Extreme attention has been put on literature reports in which the utilization of tulsi and their pharmacognostic study has been done by performing morphological and microscopic leaf experimental design and by using essential oil through the GC-MS instrumentation method. RESULTS: The utilization of these characteristics would be important for the drug discovery scientist to develop a specific formulation of the crude drug, which will be a magical therapeutic agent in the future, with many advantages. GC-MS chromatogram of Ocimum sanctum, Ocimum canum, and Ocimum gratissimum oil showed major peaks and has been identified after comparison of the mass spectra with the NIST library, indicating the presence of three phytocomponents. From the results, the GC-MS study suggested that anethole which is well reported antimicrobial compound is more in O. canum (2.66%) in comparison to O. sanctum (1,28%) but absent in O. gratissimum. The results indicated that the antimicrobial activity is more in O. canum due to the presence ofa high amount of anethole in comparison to O. gratissimum and O. sanctum. INTERPRETATION & CONCLUSION: The result revealed that O. canum has a microscopic character that can be identified by the characteristic GC MS analysis of extracts to distinguish between different species of the ocimum plant.
Assuntos
Ocimum , Óleos Voláteis , Óleos Voláteis/análise , Ocimum sanctum , Cromatografia Gasosa-Espectrometria de MassasRESUMO
In most cases, cancer develops due to abnormal cell growth and subsequent tumour formation. Due to significant constraints with current treatments, natural compounds are being explored as potential alternatives. There are now around 30 natural compounds under clinical trials for the treatment of cancer. Tulsi, or Holy Basil, of the genus Ocimum, is one of the most widely available and cost-effective medicinal plants. In India, the tulsi plant has deep religious and medicinal significance. Tulsi essential oil contains a valuable source of bioactive compounds, such as camphor, eucalyptol, eugenol, alpha-bisabolene, beta-bisabolene, and beta-caryophyllene. These compounds are proposed to be responsible for the antimicrobial properties of the leaf extracts. The anticancer effects of tulsi (Ocimum sanctum L.) have earned it the title of "queen of herbs" and "Elixir of Life" in Ayurvedic treatment. Tulsi leaves, which have high concentrations of eugenol, have been shown to have anticancer properties. In a various cancers, eugenol exerts its antitumour effects through a number of different mechanisms. In light of this, the current review focuses on the anticancer benefits of tulsi and its primary phytoconstituent, eugenol, as apotential therapeutic agent against a wide range of cancer types. In recent years, tulsi has gained popularity due to its anticancer properties. In ongoing clinical trials, a number of tulsi plant compounds are being evaluated for their potential anticancer effects. This article discusses anticancer, chemopreventive, and antioxidant effects of tulsi.
Assuntos
Ocimum sanctum , Plantas Medicinais , Eugenol/farmacologia , Eugenol/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêuticoRESUMO
Oxidative stress and inflammation are hypothesised as the main contributor for Chronic Obstructive Pulmonary Disease (COPD). Cigarette smoke (CS), a major cause of COPD leads to inflammation resulting in recruitment of neutrophils and macrophages which are rich sources of oxidants. Activation of these cells produces excess oxidants and depletes antioxidants resulting in stress. Presently, effective drug for COPD is limited; therefore, novel compounds from natural sources, including plants are under exploration. The present study aims to investigate the protective effect of Ocimum sanctum leaf extract (OLE) in CS - induced model of COPD. Exposure to CS was performed thrice a week for 8 weeks and OLE (200 mg/kg and 400 mg/kg) was administered an hour before CS exposure. Control group (negative control) were exposed to ambient air while COPD group was exposed to CS (positive control). Administration of OLE doses reduced inflammation, decreased oxidant concentration and increased antioxidant concentration (p < 0.01). Molecular docking studies between the major phytocompounds of OLE (Eugenol, Cyclohexane and Caryophyllene) and antioxidant enzymes Superoxide dismutase (SOD), Catalase, Glutathione peroxidase (GPx), Glutathione reductase (GR) and Glutathione S Transferase (GST) showed strong binding interaction in terms of binding energy. In vivo and in silico findings for the first time indicates that OLE extract significantly alleviates oxidative stress by its potent free radical scavenging property and strong interaction with antioxidant enzymes. OLE extract may prove to be a therapeutic option for COPD prevention and treatment.
Assuntos
Lesão Pulmonar , Doença Pulmonar Obstrutiva Crônica , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Ocimum sanctum , Lesão Pulmonar/metabolismo , Simulação de Acoplamento Molecular , Extratos Vegetais/uso terapêutico , Oxirredução , Estresse Oxidativo , Oxidantes/metabolismo , Inflamação/metabolismo , Pulmão/metabolismoRESUMO
This study was designed to evaluate the oxidative damage, genotoxicity, and DNA damage in the liver of rats treated with titanium nanoparticles (TiO2-NPs) with an average size of 28.0 nm and ξ-potential of - 33.97 mV, and to estimate the protective role of holy basil essential oil nanoemulsion (HBEON). Six groups of Male Sprague-Dawley rats were treated orally for 3 weeks as follows: the control group, HBEO or HBEON-treated groups (5 mg/kg b.w), TiO2-NPs-treated group (50 mg/kg b.w), and the groups treated with TiO2-NPs plus HBEO or HBEON. Samples of blood and tissues were collected for different analyses. The results revealed that 55 compounds were identified in HBEO, and linalool and methyl chavicol were the major compounds (53.9%, 12.63%, respectively). HBEON were semi-round with the average size and ζ-potential of 120 ± 4.5 nm and - 28 ± 1.3 mV, respectively. TiO2-NP administration increased the serum biochemical indices, oxidative stress markers, serum cytokines, DNA fragmentation, and DNA breakages; decreased the antioxidant enzymes; and induced histological alterations in the liver. Co-administration of TiO2-NPs plus HBEO or HBEON improved all the tested parameters and the liver histology, and HBEON was more effective than HBEO. Therefore, HEBON is a promising candidate able to protect against oxidative damage, disturbances in biochemical markers, gene expression, DNA damage, and histological changes resulting from exposure to TiO2-NPs and may be applicable in the food and pharmaceutical sectors.
Assuntos
Nanopartículas Metálicas , Nanopartículas , Ratos , Masculino , Animais , Titânio/toxicidade , Ratos Sprague-Dawley , Ocimum sanctum , Estresse Oxidativo , Nanopartículas/toxicidade , Dano ao DNA , Nanopartículas Metálicas/toxicidadeRESUMO
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
Coronavirus disease (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has compelled the scientific community to search for an effective drug that can cure or a vaccine that can prevent the disease. Alternatively, symptomatic treatment and traditional immunity boosters are prescribed. Holy Tulsi (Ocimum sanctum) has been known as an ancient remedy for cure of common cold and respiratory ailment. Several reports have come on virtual screening of phytochemicals including those of Tulsi against various enzymes of the virus. We undertook in silico analysis of the ethanol extracted phytochemicals of Tulsi as inhibitors of SARS-CoV-2 (2019-nCoV) main protease with an approach to look into the possibility of covalent ligand binding with the catalytic residue Cys145, which makes the report unique. The results suggest that the flavonoids and polyphenolic compounds of Tulsi, have potential to covalently bind to the catalytic residue Cys145 of main protease and irreversibly inhibit the viral enzyme. Luteolin-7-O-glucuronide is specially considered for its optimum properties, namely, low toxicity (LD50 5000 mg/kg body weight), high drug-likeness score (0.71), the active site binding free energy (ΔGbind) -19.19 kcal/mol by GBSA method and covalent binding energy -24.23 kcal/mol. Further experimental validations are required to establish the theoretical findings.Communicated by Ramaswamy H. Sarma.
Assuntos
COVID-19 , SARS-CoV-2 , Ocimum sanctum , Compostos Fitoquímicos/farmacologia , Peptídeo Hidrolases , Simulação de Acoplamento Molecular , Inibidores de Proteases/farmacologia , Simulação de Dinâmica MolecularRESUMO
Context: Oral submucous fibrosis (OSMF) is a chronic insidious oral potentially malignant disorder characterized by increased collagen deposition and reduced collagen degradation causing burning sensation and difficulty in mouth opening. Aim: To assess the efficacy of topical Tulsi (Ocimum sanctum) paste for the management of OSMF. Settings and Design: Institution-based clinical trial. Materials and Methods: The study included a total of 60 OSMF patients categorized into three Groups A, B and C (20 in each) depending on the severity according to Lai DR et al. classification. The patients were advised for topical Tulsi paste application and were evaluated for the reduction in the burning sensation and improvement in mouth opening every month for 3 subsequent months using the numeric pain rating scale (NRS) and a Vernier calliper, respectively. Statistical Analysis: The baseline and 3-month recordings were subjected to inter- and intra-group statistical analysis using Kruskal-Wallis analysis of variance (ANOVA), Mann-Whitney U, one-way ANOVA, Tukey's multiple post-hoc and Wilcoxon matched-pairs tests. Results: There was a reduction in the burning sensation and improvement in the mouth opening in all three groups. The reduction in the burning sensation was statistically significant among all the groups (P < 0.05) and the NRS scores after 3 months among the three groups were not statistically significant (P > 0.05). There was a statistically significant difference (P < 0.05) in the improvement of mouth opening between Group A and B; A and C; but not between B and C. Conclusion: Tulsi paste showed a significant reduction in the burning sensation and improvement of the mouth opening thereby proving to be a safe and promising medicament for OSMF.
Assuntos
Óleos Voláteis , Fibrose Oral Submucosa , Antioxidantes , Humanos , Ocimum sanctum , Fibrose Oral Submucosa/tratamento farmacológicoRESUMO
Diabetes mellitus is a major global health concern in the current scenario which is chiefly characterized by the rise in blood sugar levels or hyperglycemia. In the context, DPP4 enzyme plays a critical role in glucose homeostasis. DPP4 targets and inactivates incretin hormones such as glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) as physiological substrates, which are essential to regulate the amount of insulin that is secreted after eating. Since the inactivation of incretins occurs, the hyperglycemic conditions continue to rise, and result in adverse physiological conditions linked with diabetes mellitus. Hence, inhibition of DPP4 has been the center of focus in the present antidiabetic studies. Although few DPP4 inhibitor drugs, such as alogliptin, saxagliptin, linagliptin, and sitagliptin, are available, their adverse effects on human metabolism are undeniable. Therefore, it becomes essential for the phytochemical intervention of the disease using computational methods prior to performing in vitro and in vivo studies. In this regard, we used an in-silico approach involving molecular docking, molecular dynamics simulations, and binding free energy calculations to investigate the inhibitory potential of Ocimum tenuiflorum phytocompounds against DPP4. In this regard, three phytocompounds (1S-α-pinene, ß-pinene, and dehydro-p-cymene) from O. tenuiflorum have been discovered as the potential inhibitors of the DPP4 protein. To summarize, from our in-silico experiment outcomes, we propose dehydro-p-cymene as the potential lead inhibitor of DPP4 protein, thereby discovering new a phytocompound for the effective management of hyperglycemia and diabetes mellitus. The reported compound can be taken for in vitro and in vivo analyses in near future.
Assuntos
Diabetes Mellitus Tipo 2 , Diabetes Mellitus , Inibidores da Dipeptidil Peptidase IV , Hiperglicemia , Computadores , Diabetes Mellitus Tipo 2/tratamento farmacológico , Dipeptidil Peptidase 4/metabolismo , Inibidores da Dipeptidil Peptidase IV/farmacologia , Polipeptídeo Inibidor Gástrico/metabolismo , Humanos , Hipoglicemiantes/farmacologia , Incretinas , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Ocimum sanctum/metabolismoRESUMO
DPP-4 inhibitors have been shown to reverse amyloid deposition in Alzheimer's disease (AD) patients with cognitive impairment. Ocimum sanctum L. leaves reported the presence of important phytoconstituents which are reported to have DPP-4 inhibitory activity. To investigate the effects of petroleum ether extract of Ocimum sanctum L. (PEOS) in Intracerebroventricular streptozotocin (ICV-STZ) induced AD rats. ICV-STZ (3 mg/kg) was injected bilaterally into male Wistar rats, while sham animals received the artificial CSF. The ICV-STZ-induced rats were administered with three doses of PEOS (100, 200, and 400 mg/kg, p.o.) for thirty days. All experimental rats were subjected to behaviour parameters (radial arm maze task and novel object recognition test), neurochemical parameters such as GLP-1, Aß42, and TNF-α levels, and histopathological examination (Congo red staining) of the left brain hemisphere. PEOS significantly reversed the spatial learning and memory deficit exhibited by ICV-STZ-induced rats. Furthermore, PEOS also shows promising results in retreating Aß deposition, TNF α, and increasing GLP-1 levels. The histopathological study also showed a significant dose-dependent reduction in amyloid plaque formation and dense granule in PEOS -treated rats as compared to the ICV-STZ induced rats (Negative control). The results show that extract of Ocimum sanctum L. attenuated ICV-STZ-induced learning and memory deficits in rats and has the potential to be employed in the therapy of AD.
Assuntos
Doença de Alzheimer , Disfunção Cognitiva , Inibidores da Dipeptidil Peptidase IV , Peptídeo 1 Semelhante ao Glucagon , Extratos Vegetais , Animais , Masculino , Ratos , Doença de Alzheimer/tratamento farmacológico , Disfunção Cognitiva/induzido quimicamente , Disfunção Cognitiva/tratamento farmacológico , Vermelho Congo , Inibidores da Dipeptidil Peptidase IV/farmacologia , Modelos Animais de Doenças , Peptídeo 1 Semelhante ao Glucagon/análise , Inflamação/induzido quimicamente , Aprendizagem em Labirinto , Transtornos da Memória/induzido quimicamente , Transtornos da Memória/tratamento farmacológico , Ocimum sanctum/química , Ratos Wistar , Estreptozocina/toxicidade , Fator de Necrose Tumoral alfa , Extratos Vegetais/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
This study aims to clarify the bioactive constituents responsible for the anti-dementia effects of Ocimum sanctum Linn. ethanolic extract (OS) using olfactory bulbectomized (OBX) mice, an animal model of dementia. The effects of OS or its extract further fractionated with n-hexane (OS-H), ethyl acetate (OS-E), and n-butanol (OS-B) on the spatial cognitive deficits of OBX mice were elucidated by the modified Y-maze tests. The effects of the major constituents of the most active OS fraction were also elucidated using the reference drug donepezil. The administration of OS and OS-E ameliorated the spatial cognitive deficits caused by OBX, whereas OS-H or OS-B had no effect. Two major constituents, ursolic acid (URO) and oleanolic acid (OLE), and three minor constituents were isolated from OS-E. URO (6 and 12 mg/kg) and OLE (24 mg/kg) attenuated the OBX-induced cognitive deficits. URO (6 mg/kg) and donepezil reversed the OBX-induced down-regulation of vascular endothelial growth factor (VEGF) and choline acetyltransferase expression levels in the hippocampus. URO inhibited the ex vivo activity of acetylcholinesterase with similar efficacy to donepezil. URO inhibited the in vitro activity of acetylcholinesterase (IC50 = 106.5 µM), while the effects of OS, OS-E, and other isolated compounds were negligible. These findings suggest that URO and OLE are responsible for the anti-dementia action of OS extract, whereas URO possesses a more potent anti-dementia effect than its isomer OLE. The effects of URO are, at least in part, mediated by normalizing the function of central cholinergic systems and VEGF protein expression.
Assuntos
Ocimum sanctum , Ácido Oleanólico , Acetilcolinesterase , Animais , Donepezila , Camundongos , Ácido Oleanólico/farmacologia , Ácido Oleanólico/uso terapêutico , Bulbo Olfatório/cirurgia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Triterpenos , Fator A de Crescimento do Endotélio Vascular , Ácido UrsólicoRESUMO
Lifestyle complications are major health concerns around the globe and are recognized as a major factor for the development of various chronic diseases such as obesity, diabetes, inflammatory bowel diseases, cancer, and cardiac diseases. An unhealthy diet and poor lifestyle impose a serious threat to human health. Numerous studies have suggested the role of human microbiota in human health and diseases. Microbiota resides in the human body symbiotically and the composition of microorganisms is crucial for maintaining the healthy state of an individual. A dysbiotic gut microbiome is responsible for the release of toxic metabolites such as trimethylamine, lipopolysaccharides, bile acids, and uremic toxins and is associated with impaired organ functions. Dietary and herbal intervention of dysbiosis proposes a promising strategy to counteract gut alterations and repairing of the microbial ecosystem and health. The objective of the present comparative study was to observe the effect of therapeutic herbs in gut dysbiosis. In silico studies were performed to identify human microbiota associated with various diseases, ADME, and toxicity properties of phytoconstituents of "Tinospora cordifolia" and "Ocimum sanctum." Furthermore, co-interaction studies were performed to observe the affinity of selected phytochemicals against choline trimethylamine lyase, a critical enzyme involved in dysbiosis-induced human diseases. The antimicrobial potential of phytocompounds was done by the disc diffusion method. In conclusion, our work discusses the herbal intervention of gut dysbiosis and proposes a natural, safe, and effective herbal formulation to correct microbial dysbiosis and associated diseases.
Assuntos
Disbiose , Inibidores Enzimáticos , Proteínas de Escherichia coli/antagonistas & inibidores , Escherichia coli/enzimologia , Ocimum sanctum/química , Compostos Fitoquímicos , Tinospora/química , Animais , Disbiose/tratamento farmacológico , Disbiose/microbiologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Microbioma Gastrointestinal/efeitos dos fármacos , Humanos , Liases/antagonistas & inibidores , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologiaRESUMO
Background: To overcome some of the disadvantages of the current primary root canal obturating materials, there is a continued interest in search for chemical compounds with broader and more effective antibacterial action and less cytotoxicity. Aim: This study aimed to evaluate and compare in vivo the clinical and radiographic success of mixtures of zinc oxide-Ocimum sanctum extract, zinc oxide-ozonated oil, and zinc oxide-eugenol (ZOE) as obturating materials in pulpectomy of primary molars. Settings and Design: This was an in vivo randomized controlled clinical trial. Materials and Methods: Ninety primary molars selected were randomly divided into three groups. Group A was obturated with zinc oxide-O. sanctum extract, Group B with zinc oxide-ozonated oil, and Group C with ZOE. All the groups were evaluated for success or failure based on clinical and radiographic criteria at the end of 1, 6, and 12 months. Statistical Analysis Used: The intra- and inter-examiner reliability of the first and the second co-investigators was calculated by Cohen's kappa statistic. The data were analyzed using Chi-square test, P ≤ 0.05 (indicates statistical significance). Results: By the end of 12 months, the overall clinical success rate was 88%, 95.7%, and 90.9% in Groups A, B, and C, respectively; whereas the radiographic success rate was found to be 80%, 91.3%, and 86.4% in Groups A, B, and C, respectively. Conclusion: On the basis of the overall success rates of all the three obturating materials, the following order of performance can be concluded: zinc oxide-ozonated oil > ZOE > zinc oxide-O. sanctum extract.