RESUMO
This study reports the isolation of four new ß-carboline alkaloids (1-4) and six previously identified alkaloids (5-10) from the roots of Peganum harmala L. Among these compounds, 1 and 2 were characterized as rare ß-carboline-quinazoline dimers exhibiting axial chirality. Compound 3 possessed a unique 6/5/6/7 tetracyclic ring system with an azepine ring, and compound 4 was a novel annomontine ß-carboline. The structures of these compounds were elucidated by spectroscopic data and quantum mechanical calculations. The biosynthetic pathways of 1-3 were proposed. Additionally, the cytotoxicity of some isolates against four cancer cell lines (HL-60, A549, MDA-MB-231, and DU145) was evaluated. Notably, compound 4 exhibited significant cytotoxicity against HL-60, A549, and DU145 cells with IC50 values of 12.39, 12.80, and 30.65 µmol·L-1, respectively. Furthermore, compound 2 demonstrated selective cytotoxicity against HL-60 cells with an IC50 value of 17.32 µmol·L-1.
Assuntos
Alcaloides , Peganum , Humanos , Peganum/química , Peganum/metabolismo , Alcaloides/química , Carbolinas/química , Células HL-60RESUMO
This work gives a comprehensive chromatographic assessment of biodiesel generation from plant seed oil using ecologically friendly nano-catalysts. Researchers all over the world are actively looking for new ways to satisfy the urgent need for clean and renewable energy sources. The resultant biodiesel was fully characterized utilizing modern techniques like scanning electron microscopy, energy diffraction X-ray and X-ray diffraction. The biodiesel gas chromatography/mass spectrometry analysis revealed four significant peaks of fatty acid methyl esters, indicating high-quality biodiesel production. Furthermore, the biodiesel fuel qualities were discovered to be comparable with international standards such as ASTM D-6571 and EN-14214. This indicates that the iron-modified clay nano-catalyst can be used as a catalyst for large-scale biodiesel production. This work is important because it could lead to the large-scale production of a novel, non-food feedstock. We may lessen our reliance on fossil fuels and contribute to a more sustainable and ecologically friendly energy future by leveraging the usage of biodiesel produced in this way. The chromatographic assessment of biodiesel production from non-edible seed oil using environmentally benign nano-catalysts holds significant promise in advancing sustainable and eco-friendly biodiesel production methods, contributing to a cleaner and more environmentally responsible energy sector.
Assuntos
Biocombustíveis , Peganum , Sementes , Ácidos Graxos , Cromatografia Gasosa-Espectrometria de Massas , Óleos de PlantasRESUMO
Peganum harmala L. and Lavandula angustifolia are two traditional herbs with probable antiseizure effects. This study evaluated the effects of these two herbal extracts on pentylenetetrazol- (PTZ-) induced seizures in mice. We prepared hydroalcoholic extracts using P. harmala seeds and the aerial parts of L. angustifolia and then randomly divided 190 mice into 19 groups. Normal saline (10 mg/kg), diazepam (2 mg/kg), P. harmala (2.5, 5, 10, 15, 30, 45, and 60 mg/kg), and L. angustifolia (200, 400, 600, and 800 mg/kg) were intraperitoneally (IP) administrated 30 min before an IP administration of PTZ (90 mg/kg). Animals were observed for behavioral changes for one hour. In addition, the effects of flumazenil and naloxone on the antiseizure activity of P. harmala and L. angustifolia were assessed. P. harmala showed antiseizure activity at the dose of 10 mg/kg; it prolonged the seizure latency and decreased the seizure duration. The mortality protection rate was 90% for this herbal extract. L. angustifolia (600 mg/kg) prolonged the seizure latency and decreased both seizure duration and mortality. Neither flumazenil nor naloxone significantly reversed the antiseizure activities of P. harmala and L. angustifolia. In mice, the hydroalcoholic extracts of P. harmala and L. angustifolia showed antiseizure activity against PTZ-induced seizures. We could not delineate the exact antiseizure mechanisms of these extracts in the current study.
Assuntos
Lavandula , Peganum , Camundongos , Animais , Extratos Vegetais/farmacologia , Flumazenil/farmacologia , Convulsões/induzido quimicamente , Convulsões/tratamento farmacológico , Naloxona/farmacologiaRESUMO
Harmaline and harmine are naturally occurring closely related ß-carboline alkaloids found in Peganum and Banisteriopsis plants. They have historical significance in traditional practices due to their potential psychoactive and therapeutic properties. Herein, a highly sensitive spectrofluorometric method was developed for the quantifying of harmaline and harmine in diverse matrices, including pure forms, seed samples, and spiked plasma. The procedures lie in addressing the challenge of overlapping fluorescence spectra exhibited by harmaline and harmine through the incorporation of hydroxypropyl-ß-cyclodextrin, altering their chemical properties and fluorescence characteristics. Synchronous fluorescence measurements coupled with first derivative mathematical technique make it possible to distinguish between the harmaline and harmine at 419 and 456 nm, respectively. The method effectiveness is demonstrated through spectral analysis, optimization of the measurement conditions, adopting validation parameters and application to the pure form, seed samples and spiked human plasma. This methodology facilitates accurate determination of these alkaloids over the concentration range of 10â200 ng/mL. Thus, the developed approach provides a robust mean for the precise determination of harmaline and harmine, contributing to analytical chemistry's ongoing efforts to address complex challenges in quantification across diverse matrices.
Assuntos
Alcaloides , Peganum , Humanos , Harmina , Harmalina , Alcaloides/análise , Extratos Vegetais/química , Peganum/químicaRESUMO
The complex heterogenic environment of tumour mass often leads to drug resistance and facilitate chemo insensitivity triggering more malignant phenotypes among cancer patients. Major DNA-damaging cancer drugs have been consistently proven unsuccessful in terms of elevating chemo-resistance. (±)-peharmaline A, a hybrid natural product isolated from seeds of Peganum harmala L. possesses significant cytotoxic activities. Herein, we have described the design, and synthesis of a novel library of close and simplified analogues around the anticancer natural product (±)-peharmaline A and investigated their cytotoxic activities, which led to the identification of three structurally simplified lead compounds exhibiting better potency than parent natural product. Among them, demethoxy analogue of peharmaline A was further investigated for its anticancer potential eliciting demethoxy analogue as potent DNA-damage inducing agent attenuating the expression of the proteins responsible for the DNA damage repair. Therefore, this demethoxy analogue warrants detailed investigations for the confirmations of the molecular mechanism-based studies responsible for its anticancer activity. ______________________________________________________________________________.
Assuntos
Antineoplásicos , Produtos Biológicos , Neoplasias , Peganum , Produtos Biológicos/farmacologia , Antineoplásicos/farmacologia , Extratos Vegetais/farmacologia , DNARESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Peganum harmala L. is a traditional medicinal plant used for centuries in folk medicine. It has a wide array of therapeutic attributes, which include hypoglycemic, sedative, anti-inflammatory, and antioxidant properties. The fruit decoction of this plant was claimed by Avicenna as traditional therapy for urolithiasis. Also, P. harmala seed showed a clinical reduction in kidney stone number and size in patients with urolithiasis. AIM OF THE STUDY: In light of the above-mentioned data, the anti-urolithiatic activities of the seed extracts and the major ß-carboline alkaloids of P. harmala were investigated. MATERIALS AND METHODS: Extraction, isolation, and characterization of the major alkaloids were performed using different chromatographic and spectral techniques. The in vivo anti-urolithiatic action was evaluated using ethylene glycol (EG)-induced urolithiasis in rats by studying their mitigating effects on the antioxidant machinery, serum toxicity markers (i.e. nitrogenous waste, such as blood urea nitrogen, uric acid, urea, and creatinine), minerals (such as Ca, Mg, P, and oxalate), kidney injury marker 1 (KIM-1), and urinary markers (i.e. urine pH and urine output). RESULTS: Two major alkaloids, harmine (P1) and harmalacidine HCl (P2), were isolated and in vivo evaluated alongside the different extracts. The results showed that P. harmala and its constituents/fractions significantly reduced oxidative stress at 50 mg/kg body weight, p.o., as demonstrated by increased levels of glutathione (GSH), glutathione reductase (GR), glutathione peroxidase (GPx), and catalase (CAT) in kidney homogenate as compared to the EG-treated group. Likewise, the total extract, pet. ether fraction, n-butanol fraction, and P1, P2 alleviated malondialdehyde (MDA) as compared to the EG-treated group. Serum toxicity markers like blood urea nitrogen (BUN), creatinine, uric acid, urea, kidney injury molecule-1 (Kim-1), calcium, magnesium, phosphate, and oxalate levels were decreased by total extract, pet. ether fraction, n-butanol fraction, P1, and P2 as compared to the EG-treated group. Inflammatory markers like NFκ-B and TNF-α were also downregulated in the kidney homogenate of treatment groups as compared to the EG-treated group. Moreover, urine output and urine pH were significantly increased in treatment groups as compared to the EG-treated group deciphering anti-urolithiatic property of P. harmala. Histopathological assessment by different staining patterns also supported the previous findings and indicated that treatment with P. harmala caused a gradual recovery in damaged glomeruli, medulla, interstitial spaces and tubules, and brown calculi materials as compared to the EG-treated group. CONCLUSION: The current research represents scientific evidence on the use of P. harmala and its major alkaloids as an effective therapy in the prevention and management of urolithiasis.
Assuntos
Alcaloides , Cálculos Renais , Peganum , Urolitíase , 1-Butanol , Alcaloides/farmacologia , Animais , Antioxidantes , Cálcio , Oxalato de Cálcio/urina , Catalase , Creatinina , Éteres , Etilenoglicol/uso terapêutico , Etilenoglicol/toxicidade , Glutationa , Glutationa Peroxidase , Glutationa Redutase , Harmina , Hipnóticos e Sedativos/uso terapêutico , Hipoglicemiantes/uso terapêutico , Cálculos Renais/tratamento farmacológico , Magnésio , Malondialdeído , Peganum/química , Fosfatos , Extratos Vegetais , Ratos , Fator de Necrose Tumoral alfa , Ureia , Ácido Úrico , Urolitíase/induzido quimicamente , Urolitíase/tratamento farmacológico , Urolitíase/patologiaRESUMO
The high nutritional value of egg makes it vital to the human diet. Salmonella enteritidis is one of the major global causes of foodborne enteritis in humans. The chicken intestine is the main source of S. enteritidis. Therefore, eggs play an important role in the transmission of salmonellosis. In this study, we evaluated the effectiveness of coatings made of zein either alone or in combination of hydro-alcoholic extract of Peganum harmala on the quality of eggs and control of S. enteritidis at 7°C during a period of 28 days. Results demonstrated that both types of the coating significantly improved the physicochemical properties of eggs including weight loss, Haugh unit, and yolk index compared to controls during storage. However, neither of coatings resulted in significant changes in yolk color and pH (p < 0.05). Both types of coating caused two log CFU/ml reductions in S. enteritidis population from the first day and eliminated the contamination at the end of the experiment (for 28 days). Salmonella elimination occurred at day 21 for zein-plant extract coating. Our findings demonstrate zein coating can be an appropriate approach for maintaining the quality of eggs during shelf life and an effective and economic strategy for control of S. enteritidis in eggs. PRACTICAL APPLICATION: This study shows that the application of zein coating can preserve the internal quality and freshness of eggs during storage. Moreover, zein coating is a highly effective strategy in the control of Salmonella. This method can be used on a commercial scale for enhancing the safety and quality of eggs.
Assuntos
Peganum , Zeína , Animais , Humanos , Salmonella enteritidis , Casca de Ovo , Zeína/farmacologia , Ovos , Galinhas , Extratos Vegetais/farmacologiaRESUMO
Infectious diseases have always been the number one enemy threatening health and well-being. With increasing numbers of infectious diseases, growing resistance of pathogens, and declining roles of antibiotics in the treatment of infectious diseases, it is becoming increasingly difficult to treat new infectious diseases, and there is an urgent need to develop new antibiotics to change the situation. Natural products tend to exhibit many special biological properties. The genus Peganum (Zygophyllaceae) has been used, for a long time, to treat cough, asthma, lumbago, hypertension, diabetes, and Alzheimer's disease. Over the past two decades, a growing number of studies have shown that components from Peganum harmala Linn and its derivatives can inhibit a variety of microorganisms by inducing the accumulation of ROS in microorganisms, damaging cell membranes, thickening cell walls, disturbing cytoplasm, and interfering with DNA synthesis. In this paper, we provide a review on the antibacterial, antifungal, antiviral, and antiparasitic activities of P. harmala, with a view to contribute to research on utilizing P. harmala for medicinal applicaitons and to provide a reference in the field of antimicrobial and a basis for the development of natural antimicrobial agents for the treatment of infectious diseases.
Assuntos
Peganum , Antibacterianos/farmacologia , Antifúngicos , Antiparasitários/farmacologia , Antivirais/farmacologia , Extratos Vegetais/farmacologia , SementesRESUMO
The COVID-19 pandemic has provided an opportunity for repurposing of drugs, including complex, natural drugs, to meet the global need for safe and effective antiviral medicines which do not promote multidrug resistance nor inflate medical costs. The author herein describes his own repurposing of herbal tinctures, previously prepared for oncology, into a possibly synergistic, anti-COVID 41 "herb" formula of extracts derived from 36 different plants and medicinal mushrooms. A method of multi-sample in vitro testing in green monkey kidney vero cells is proposed for testing the Hypothesis that even in such a large combination, antiviral potency may be preserved, along with therapeutic synergy, smoothness, and complexity. The possibility that the formula's potency may improve with age is considered, along with a suitable method for testing it. Collaborative research inquiries are welcome.
Assuntos
Tratamento Farmacológico da COVID-19 , Peganum , Animais , Antivirais/farmacologia , Antivirais/uso terapêutico , Chlorocebus aethiops , Humanos , Pandemias , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Sementes , Células VeroRESUMO
Wild medicinal herbs have been used as folk and traditional medicines all across the world since well before recorded history. This present study was designed to test the antimicrobial activities of five different solvent extracted samples (n-hexane, n-butanol, ethyl acetate, methanol, and water) of Peganum harmala using stems and seeds. Two different strains of Gram-negative bacteria (Escherichia coli and Klebsiella pneumonia), two Gram-positive bacteria (Bacillus subtilus and Staphylococcus aureus), and one fungal strain (Candida albicans) were used. The antimicrobial activities were measured using a disc diffusion assay. Two concentrations of the extracts (1 and 2mgDisc-1) were used. Ethyl acetate fraction was found more affective among the tested solvents and showed maximum activity (zone of inhibition) against S. aureus (65.53 and 81.10%), E. coli (46.22 and 61.29%) while n-butanol and water fractions gave maximum activity against S. aureus (78.86 and 70.00%) and K. pneumonia (57.00 and 61.39%) respectively. Water fraction showed maximum activity against C. albicans (60.00 and 81.88%). In the case of the stem, Ethyl acetate again showed more activity against B. subtilus (38.57 and 42.10%) and S. aureus (36.66 and 46.66%) while n-butanol showed maximum activity against K. pneumonia (24.55 and 32.44%) and E. coli (27.93 and 37.61%). Methanol was found more effective against C. albicans (25.71 and 43.80%). Seed extracted samples were found more effective compared to the stem. Ethyl acetate, butanol, and aqueous extracted samples showed good activity against the tested microbes, so these fractions are recommended for study their mechanism of actions and isolation of bioactive metabolites responsible for antimicrobial activities. The P. harmala should be evaluated for their bioactive compounds to be used in future studies. Our objective is to provide the framework for future study on the roles of P. harmala as traditional medicines.
Assuntos
Peganum , 1-Butanol/farmacologia , Antibacterianos/farmacologia , Candida albicans , Escherichia coli , Metanol/farmacologia , Testes de Sensibilidade Microbiana , Extratos Vegetais/farmacologia , Sementes , Solventes/farmacologia , Staphylococcus aureus , Água/farmacologiaRESUMO
Echinococcosis is a common and endemic disease that affects both humans and animals. In this study, the in vitro activities of methanolic extracts of Ruta graveolens, Peganum harmala aerial parts, and Citrullus colocynthis seeds against protoscolosis and isolated bacterial strains from hydatid cysts were assessed using disc diffusion methods and Minimum Inhibitory Concentration (MIC). The chemical composition of three methanolic extracts was studied using LC-MS. After 3 h of exposure to 40 mg/mL R. graveolens extract, a tenfold protoscolocidal effect was seen when compared to the convintional medication (ABZ) for the same duration (P < 0.05). The bacteria listed below were isolated from hydatid cyst fluid collected from a variety of sick locations, including the lung and liver. Micrococcus spp., E. coli, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter amnigenus, Pseudomonas aeruginosa, Staphylococcus xylosus, and Achromobacter xylosoxidans are among the bacteria that have been identified. The most effective extract was R. graveolens, followed by P. harmala and C. colocynthis, according to the results of antibacterial activity using the disc diffusion method. R. graveolens extract had the lowest MIC values (less than 2 mg/mL) against all microorganisms tested. This shows that the R. graveolens extract has additional properties, such as the ability to be both scolocidal and bactericidal. Because these bacteria are among the most prevalent pathogenic bacteria that increase the risk of secondary infection during hydatid cysts, the results of inhibitory zones and MICs of the R. graveolens methanol extract are considered highly promising.
Assuntos
Citrullus colocynthis , Equinococose , Echinococcus , Peganum , Ruta , Animais , Bactérias , Escherichia coli , Metanol , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ruta/químicaRESUMO
BACKGROUND: Because of increasing antibiotic failure and recurrence of infections in patients with P. aeruginosa, the present study was designed to determine the antibiotic resistance status, presence of persister cells and investigate the antipersister effect of Peganum harmala in P. aeruginosa clinical isolates in vitro in Ilam, Iran. METHODS: Thirty P. aeruginosa urinary clinical isolates were collected from hospitals in Ilam, Iran and identified by common microbiological and biochemical tests. Afterward, antibiotic susceptibility assay, persister cell assay, P. harmala extraction, cell culture, and cell viability assays were performed. RESULTS: A high rate of antibiotic resistance was observed. All isolates were resistant to co-amoxiclav. Also, 83.3% (n = 25), 90% (n = 27), and 36.6% (n = 11) of isolates showed resistance to ceftazidime, kanamycin, and tobramycin, respectively. The MIC and MBC values for imipenem were ≤ 2 and 2 µg/mL for susceptible isolates, respectively. In addition, 6.66% (n = 2) of isolates were persister cells and were also sensitive to imipenem by MIC but did not show any MBC. IC50 for P. harmala was 35 µg/mL. Eventually, MIC value of P. harmala against two P. aeruginosa persister cell producer isolates was 3 µg/mL and 1 µg/mL, and the value of MBC was 10 µg/mL and 30 µl/mL. CONCLUSIONS: Our findings demonstrated that P. harmala may be a suitable antipersister herbal medicine against P. aeruginosa clinical isolates. In this regard, comprehensive research is needed in the future to gain more information in this area.
Assuntos
Peganum , Infecções por Pseudomonas , Ceftazidima , Humanos , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosaRESUMO
Six alkaloids peharmalines F-K, along with 14 known ones, were isolated from the aerial part of Peganum harmala L.. The structures of the isolated compounds were determined based on their HR-ESI-MS data, extensive NMR spectroscopic analyses, and ECD calculations. 3-(4-Hydroxyphenyl)quinoline exhibited potent antiproliferative activity against the HepG-2 cell lines with an IC50 value of 3.05 µM. Norharmane displayed a moderate inhibition against A549 and HepG-2 cells with IC50 values of 16.45 µM and 17.27 µM, respectively.
Assuntos
Alcaloides , Antineoplásicos Fitogênicos , Peganum , Células A549 , Alcaloides/química , Antineoplásicos Fitogênicos/química , Células Hep G2 , Humanos , Peganum/química , Extratos Vegetais/químicaRESUMO
Biofilm formation of the opportunistic pathogen Pseudomonas (P). aeruginosa is one of the major global challenges to control nosocomial infections due to their high resistance to antimicrobials and host defense mechanisms. The present study aimed to assess the antibacterial and the antibiofilm activities of Peganum (P). harmala seed extract against multidrug-resistant P. aeruginosa isolates. Chemical identification of the active compound and determination of its molecular mechanism of action were also investigated. Results showed that P. harmala n-butanol "n-BuOH" extract exhibited antibacterial activity against multidrug-resistant P. aeruginosa isolates. This extract was even more active than conventional antibiotics cefazolin and vaamox when tested against three P. aeruginosa multidrug-resistant isolates. In addition, P. harmala n-BuOH extract exhibited potent bactericidal activity against PAO1 strain at MIC value corresponding to 500 µg/mL and attained 100% killing effect at 24 h of incubation. Furthermore, P. harmala n-BuOH extract showed an antibiofilm activity against P. aeruginosa PAO1 and exhibited 80.43% inhibition at sub-inhibitory concentration. The extract also eradicated 83.99% of the biofilm-forming bacteria. The active compound was identified by gas chromatography-mass spectrometry as an indole alkaloid harmaline. Transcriptomic analysis showed complete inhibition of the biofilm-related gene pilA when PAO1 cells were treated with harmaline. Our results revealed that P. harmala seed extract and its active compound harmaline could be considered as a candidate for a new treatment of multidrug-resistant P. aeruginosa pathogens-associated biofilm infections.
Assuntos
Antibacterianos , Biofilmes/efeitos dos fármacos , Peganum , Extratos Vegetais , Pseudomonas aeruginosa/efeitos dos fármacos , Antibacterianos/farmacologia , Farmacorresistência Bacteriana Múltipla , Peganum/química , Extratos Vegetais/farmacologiaRESUMO
Peganum genus is rich with its high phytochemical and botanical variability. Peganum species have been used as a sedative, antitumor, analgesic and antidepressant. This paper aims to study the molecular diversity of Peganum genus and to shed more light on the structure-activity relationship of the alkaloids isolated from Peganum genus. All Peganum alkaloids were grouped according to their structural properties. A chemoinformatic approach (SwissTargetPrediction) was used to determine the molecular targets of these alkaloids. To analyze and visualize the results, R software was used to generate hierarchical clustering heatmaps. The results of this study can help researchers to better understand the structure-activity relationship of Peganum alkaloids and how substitution can affect the biological activity of those alkaloids.
Assuntos
Alcaloides , Peganum , Alcaloides/química , Alcaloides/farmacologia , Quimioinformática , Peganum/química , Extratos Vegetais/química , Relação Estrutura-AtividadeRESUMO
BACKGROUND & OBJECTIVE: Peganum harmala has been traditionally used to manage rheumatoid arthritis (RA) and other inflammatory conditions. However, its use against RA has not been scientifically evaluated. The current study was designed to assess the anti-arthritic and anti-inflammatory activities of the methanolic extract of P. harmala leaves by in vitro and in vivo methods. METHODS: The in vitro assays were carried out to determine the effect of plant extract on inhibition of egg albumin denaturation and human red blood cell membrane (HRBC) stabilization. Moreover, 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity was performed to determine the antioxidant potential. In vivo anti-arthritic activity was performed by determining the curative effect against Complete Freund's adjuvant (0.1 ml). The plant extract was administered to rats orally at 200, 400 and 600 mg/kg/day for 21 days. RESULTS: The values of IC50 of plant extract in protein denaturation, stabilization of HRBC and DPPH assays were 77.54 mg/ml, 23.90 mg/ml and 58.09 µg/ml, respectively. Moreover, the plant extract significantly attenuated the poly-arthritis and weight loss, anemia and paw edema. The plant extract restored the level of C-reactive protein, rheumatoid factor, alanine transaminase, aspartate transaminase and alkaline phosphatase in poly-arthritic rats. Moreover, the plant extract restored the immune organs' weight in treated rats. Treatment with P. harmala also significantly subdued the oxidative stress by reinstating superoxide dismutase, reduced glutathione, catalase and malondialdehyde in poly-arthritic rats. The plant extract notably restored the prostaglandin-E2 and tumor necrosis factor (TNF)-α in the serum of poly-arthritic rats. CONCLUSION: It was concluded that P. harmala extract had potential antioxidant, anti-inflammatory and antiarthritic activities, which primarily might be attributed to alkaloids, flavonoids and phenols.
Assuntos
Artrite Experimental/tratamento farmacológico , Peganum/química , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/uso terapêutico , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Artrite Experimental/patologia , Células Cultivadas , Membrana Eritrocítica/efeitos dos fármacos , Membrana Eritrocítica/metabolismo , Adjuvante de Freund/farmacologia , Adjuvante de Freund/uso terapêutico , Humanos , Medicina Tradicional , Fitoterapia , Plantas Medicinais/química , RatosRESUMO
Mosquito-borne diseases result in the loss of life and economy, primarily in subtropical and tropical countries, and the emerging resistance to insecticides is increasing this threat. Botanical insecticides are promising substitutes for synthetic insecticides. This study evaluated the larvicidal and growth index of Culex pipiens of four solvent extracts of Terminalia chebula, Aloe perryi, and Peganum harmala against Cx. pipiens. None of the 12 extracts exhibited larvicidal potential against third instars except the ethyl acetate extract of P. harmala. After 24 h of exposure, the LC50 value was 314.88 ppm, and the LC90 value was 464.19 ppm. At 320 ppm, the hatchability was 25.83%, and it resulted in 100% mortality. In addition, the eggs treated with the EtOAc extract of P. Harmala exhibited a long larval period compared with the control. The larval period continued for 12 days, and the pupal period took three days in the treatment groups. The growth index data also exhibited a decrease (0.007.53) in the treated groups compare with 8.5 in the control. The transformation of eggs into adults decreased with increasing concentrations. This paper is the first report on the development and growth index of Cx. pipiens potential using P. harmala seeds.
As doenças transmitidas por mosquitos resultam na perda de vidas e economia, principalmente em países subtropicais e tropicais, e a resistência emergente aos inseticidas está aumentando essa ameaça. Os inseticidas botânicos são substitutos promissores dos inseticidas sintéticos. Este estudo avaliou o índice larvicida e de crescimento de Culex pipiens de quatro extratos solventes de Terminalia chebula, Aloe perryi e Peganum harmala contra Cx. pipiens. Nenhum dos 12 extratos exibiu potencial larvicida contra o terceiro ínstar, exceto o extrato de acetato de etila de P. harmala. Após 24 horas de exposição, o valor LC50 era 314,88 ppm e o valor LC90 era 464,19 ppm. A 320 ppm, a eclodibilidade foi de 25,83% e resultou em 100% de mortalidade. Além disso, os ovos tratados com o extrato de EtOAc de P. harmala exibiram um longo período larval em comparação com o controle. O período larval continuou por 12 dias, e o período pupal durou três dias nos grupos de tratamento. Os dados do índice de crescimento também exibiram uma diminuição (0,00-7,53) nos grupos tratados em comparação com 8,5 no controle. A transformação de ovos em adultos diminuiu com o aumento das concentrações. Este artigo é o primeiro relatório sobre o índice de desenvolvimento e crescimento de Cx. potencial de pipiens usando sementes de P. harmala.
Assuntos
Animais , Aedes , Culex , Peganum , Inseticidas , Anopheles , Sementes , Extratos Vegetais/farmacologia , LarvaRESUMO
Extract of natural plants is one of the most important metallic corrosion inhibitors. They are readily available, nontoxic, environmentally friendly, biodegradable, highly efficient, and renewable. The present project focuses on the corrosion inhibition effects of Peganum Harmala leaf extract. The equivalent circuit with two time constants with film and charge transfer components gave the best fitting of impedance data. Extraction of active species by sonication proved to be an effective new method to extract the inhibitors. High percent inhibition efficacy IE% of 98% for 283.4 ppm solutions was attained using impedance spectroscopy EIS measurements. The values of charge transfer Rct increases while the double layer capacitance Cdl values decrease with increasing Harmal extract concentration. This indicates the formation of protective film. The polarization curves show that the Harmal extract acts as a cathodic-type inhibitor. It is found that the adsorption of Harmal molecules onto the steel surface followed Langmuir isotherm. Fourier-transform infrared spectroscopy FTIR was used to determine the electron-rich functional groups in Harmal extract, which contribute to corrosion inhibition effect. Scanning electron microscopy SEM measurement of a steel surface clearly proves the anticorrosion effect of Harmal leaves.
Assuntos
Peganum/química , Extratos Vegetais/química , Aço/química , Corrosão , Espectroscopia Dielétrica , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Peganum harmala (P. harmala) belongs to the family Zygophyllaceae, and is utilized in the traditional medicinal systems of Pakistan, China, Morocco, Algeria, and Spain to treat several chronic health disorders. The aim of the present study was to identify the chemical constituents and to evaluate the antioxidant, anti-inflammatory, and toxicity effects of P. harmala extracts both in vitro and in vivo. Sequential crude extracts including 100% dichloromethane, 100% methanol, and 70% aqueous methanol were obtained and their antioxidant and anti-inflammatory effects evaluated both in vitro and in vivo. The anti-inflammatory effect of the extract was investigated using the carrageenan-induced paw edema method in mice, whereas the toxicity of the most active extract was evaluated using an acute and subacute toxicity rat model. In addition, we have used the bioassay-guided approach to obtain potent fractions, using solvent-solvent partitioning and reversed phase high performance liquid chromatography from active crude extracts; identification and quantification of compounds from the active fractions was achieved using electrospray ionization mass spectrometry and high performance liquid chromatography techniques. Results revealed that the 100% methanol extract of P. harmala exhibits significant in vitro antioxidant activity in DPPH assay with an IC50 of 49 µg/mL as compared to the standard quercetin with an IC50 of 25.4 µg/mL. The same extract exhibited 63.0% inhibition against serum albumin denaturation as compared to 97% inhibition by the standard diclofenac sodium in an in vitro anti-inflammatory assay, and in vivo anti-inflammatory against carrageenan-induced paw edema (75.14% inhibition) as compared to 86.1% inhibition caused by the standard indomethacin. Furthermore, this extract was not toxic during a 14 day trial of acute toxicity when given at a dose of 3 g/kg, indicating that the lethal dose (LD50) of P. harmala methanol extract was greater than 3 g/kg. P. harmala methanolic fraction 2 obtained using bioassay-guided fractionation showed the presence of quinic acid, peganine, harmol, harmaline, and harmine, confirmed by electrospray ionization mass spectrometry and quantified using external standards on high performance liquid chromatography. Taken all together, the current investigation further confirms the antioxidant, anti-inflammatory, and safety aspects of P. harmala, which justifies its use in folk medicine.
Assuntos
Anti-Inflamatórios/administração & dosagem , Antioxidantes/administração & dosagem , Carragenina/efeitos adversos , Edema/tratamento farmacológico , Peganum/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Modelos Animais de Doenças , Edema/induzido quimicamente , Indometacina/farmacologia , Dose Letal Mediana , Camundongos , Extratos Vegetais/química , Quercetina/farmacologia , Ratos , Testes de Toxicidade Aguda , Testes de Toxicidade SubagudaRESUMO
Harmaline is a naturally occurring ß-carboline alkaloid that is isolated from Peganum harmala. It has shown efficacy in treating Parkinson's disease and has been reported to exhibit antimicrobial and anticancer properties. However, the molecular mechanism of harmaline in the context of esophageal squamous cell carcinoma (ESCC) has not been characterized. Here, we report that harmaline attenuates ESCC growth by directly targeting the mammalian target of rapamycin (mTOR). Harmaline strongly reduced cell proliferation and anchorage-independent cell growth. Additionally, harmaline treatment induced G2/M phase cell-cycle arrest through upregulation of p27. The results of in vitro and cell-based assays showed that harmaline directly inhibited the activity of mTOR kinase and the phosphorylation of its downstream pathway components. Depletion of mTOR using an shRNA-mediated strategy in ESCC cell lines indicated that reduced mTOR protein expression levels are correlated with decreased cell proliferation. Additionally, we observed that the inhibitory effect of harmaline was dependent upon mTOR expression. Notably, oral administration of harmaline suppressed ESCC patient-derived tumor growth in vivo. Taken together, harmaline is a potential mTOR inhibitor that might be used for therapeutically treating ESCC.