RESUMO
The prevalence of reproductive dysfunction in males has risen in the last few years, and alternative therapies are gradually gaining in popularity. Our in vitro study aimed to evaluate the potential impact of Lepidium sativum L. on mice TM3 Leydig cells, concerning basal parameters such as cell viability, cell membrane integrity, and lysosomal activity, after 24 h and 48 h exposure. Moreover, reactive oxygens species generation, sex-steroid hormone secretion, and intercellular communication were quantified. In the present study, the microgreen extract from Lepidium was rich in ferulic acid, 4-OH benzoic acid, and resveratrol, with a significant antioxidant activity. The results showed that lower experimental doses (62.5-250 µg/mL) could positively affect the observed parameters, with significant differences at 250 µg/mL after 24 h and 48 h, respectively. Potential risks could be associated with higher concentrations, starting at 500 µg/mL, 1000 µg/mL, and 2000 µg/mL of Lepidium. Nevertheless, biochemical quantification indicated a significant antioxidant potential and a rich content of biologically active molecules at the applied doses, and time determined the intracellular response of the cultured model.
Assuntos
Lepidium sativum , Lepidium , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Comunicação Celular , Sobrevivência Celular , Lepidium/metabolismo , Lepidium sativum/química , Células Intersticiais do Testículo/metabolismo , Masculino , Camundongos , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia , Testosterona/metabolismoRESUMO
Background: Lepidium sativum (garden cress) is a member of the Brassicaceae family that has been utilized for medicinal and culinary purposes in centuries. Anti-inflammatory, antioxidant, immunomodulatory, hepatoprotective, antihypertensive, antiasthmatic, and hypoglycemic properties are found in various portions of the plant. The anti-inflammatory, antioxidant, and immunomodulatory effects of L. sativum were the subject of this review. Methods: The required information was gathered by searching the Web of Science, PubMed, and Scopus databases for the terms anti-inflammatory, antioxidant, immunomodulatory, immune system, and Lepidium sativum. Up until February 2022, the search was conducted. Results: TNF-, IL-6, IL-1, NO, iNOS, and HO-1 levels were reduced, indicating that L. sativum has anti-inflammatory and immunomodulatory properties. Flavonoids, alkaloids, cyanogenic glycosides, tannins, glucosinolates, sterols, and triterpenes are the key chemical components that contribute to the anti-inflammatory effects. In peritoneal neutrophils, L. sativum reduced oxidative stress by scavenging free radicals, as evidenced by a drop in superoxide anion and an increase in glutathione. Conclusion: The anti-inflammatory, antioxidant, and immunomodulatory activities of L. sativum could be explored in clinical trials to treat inflammatory and immune system illnesses.
Assuntos
Anti-Inflamatórios , Antioxidantes , Agentes de Imunomodulação , Lepidium sativum , Extratos Vegetais , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Agentes de Imunomodulação/farmacologia , Lepidium sativum/química , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologiaRESUMO
Physiochemical properties, lipid breakdown, ß-carotenoids, tocopherols, and vitamins as well as amino and fatty acid profiles of Soxhlet-extracted oil from five different garden cress (Lepidium sativum L.) seed genotypes (namely: CG8, CG7, CG17, CG4, and 207910) across Ethiopia regions were investigated. Results showed that despite the seeds' proximate peak and least values, the extraction yield, viscosity, specific gravity, refractive index, lipid breakdown, and boiling point of garden cress seed oil across the genotypes noticeably varied with promising amino and fatty acid profiles. Further, the genotype CG17 obtained greater quantities of ß-carotenoids, tocopherols and vitamin values compared to the other genotypes.
Assuntos
Lepidium sativum , Tocoferóis , Carotenoides/análise , Etiópia , Ácidos Graxos/análise , Genótipo , Lepidium sativum/química , Lepidium sativum/metabolismo , Óleos de Plantas/química , Sementes/química , Sementes/genética , Tocoferóis/análise , Vitamina A/análise , Vitaminas/análiseRESUMO
The current study focused on important bioactive compounds in plants that make them pharmacologically valuable. Therefore, this study was aimed to develop Lepidium sativum (L. sativum) seed extract loaded solid lipid nanoparticles and explore its cytotoxic effect on human liver cancer cells (HepG2 cells). The ethanolic extract of L. sativam used to develop L. sativum seed extract loaded solid lipid nanoparticles (SLNs) was analyzed by gas chromatography-mass spectrometry, thin-layer chromatography (TLC) and high-performance thin-layer chromatography (HPTLC) for phytochemical profiling. The L. sativum seed extract loaded SLNs were efficaciously prepared by the nanoprecipitation method and screened on the basis of physicochemical properties. The L. sativum seed extract loaded SLN-2 was characterized using various parameters like particle size (237.1±0.104), % entrapment efficiency (80±1.15), zeta potential (42.1±0.102) and % drug release (45% at the end 8 hours and release the entire amount in 12 h). The SLN-2 formulation was optimized based on the recipient factor, and SLN-2 was used to further evaluate the in vitro cytotoxicity of HepG2 cells in a dose-dependent manner by 3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide (MTT) assay. The IC50 value of SLN2 was 52.37 ug/ml and sub IC50 26.1 ug/ml at 24 h and 48 h, respectively. Thus, we concluded that L. sativum extract loaded SLN-2 could act as an alternative therapy, possibly controlling therapeutic action by making a substantial reduction in side effects.
Assuntos
Lepidium sativum , Nanopartículas , Portadores de Fármacos/química , Humanos , Lepidium sativum/química , Lipossomos , Nanopartículas/química , Tamanho da Partícula , Extratos Vegetais/farmacologiaRESUMO
The roots, leaves, and seeds of Lepidium sativum L., popularly known as Garden cress in different regions, have high economic importance; although, the crop is particularly cultivated for the seeds. In traditional medicine, this plant has been reported to possess various biological activities. This review is aimed at providing updated and critical scientific information about the traditional, nutritional, phytochemical, and biological activities of L. sativum. In addition, the geographic distribution is also reviewed. The comprehensive literature search was carried out with the help of different search engines PubMed, Web of Science, and Science Direct. This review highlighted the importance of L. sativum as an edible herb that possesses a wide range of therapeutic properties along with high nutritional values. Preclinical studies (in vitro and in vivo) displayed anticancer, hepatoprotective, antidiabetic, hypoglycemic, antioxidant, antimicrobial, gastrointestinal, and fracture/bone healing activities of L. sativum and support the clinical importance of plant-derived bioactive compounds for the treatment of different diseases. Screening of literature revealed that L. sativum species and their bioactive compounds may be a significant source for new drug compounds and also could be used against malnutrition. Further clinical trials are needed to effectively assess the actual potential of the species and its bioactive compounds.
Assuntos
Suplementos Nutricionais/análise , Lepidium sativum/química , Compostos Fitoquímicos/química , Extratos Vegetais/químicaRESUMO
Plants, as with humans, require photoprotection against the potentially damaging effects of overexposure to ultraviolet (UV) radiation. Previously, sinapoyl malate (SM) was identified as the photoprotective agent in thale cress. Here, we seek to identify the photoprotective agent in a similar plant, garden cress, which is currently used in the skincare product Detoxophane nc. To achieve this, we explore the photodynamics of both the garden cress sprout extract and Detoxophane nc with femtosecond transient electronic absorption spectroscopy. With the assistance of liquid chromatography-mass spectrometry, we determine that the main UV-absorbing compound in garden cress sprout extract is SM. Importantly, our studies reveal that the photoprotection properties of the SM in the garden cress sprout extract present in Detoxophane nc are not compromised by the formulation environment. The result suggests that Detoxophane nc containing the garden cress sprout extract may offer additional photoprotection to the end user in the form of a UV filter booster.
Assuntos
Lepidium sativum/química , Extratos Vegetais/química , Plântula/química , Protetores Solares/químicaRESUMO
BACKGROUND: Diabetes mellitus (DM) is a metabolic disorder characterized by high blood glucose levels that occurs either due to insufficient insulin production or mounting resistance to its action. The purpose of this study was to investigate if methanolic extracts of Lepidium sativum seeds, Ficus carica, and Punica granatum leaves had any effect on blood sugar levels in normal and streptozotocin (STZ) diabetic rats, as well as to explore the most effective extract. METHOD: Healthy male albino rats weighing 185-266 g were divided into nine groups of eight rats each: normal control, diabetic control, diabetic rats with dietary supplements of L. sativum, F. carica, and P. granatum methanolic extracts, and diabetics treated with insulin. All of the rats were fed on ordinary diet with nutritional pellets and were given water ad libitum. To induce diabetes, all animals were administered with STZ intraperitoneal injection at a dose of 60 mg/kg body weight. For five weeks, the crude plant extracts were given orally to various groups of rats at doses of one hundred and two hundred mg/kg body weight. After that, animal groups were sacrificed and blood samples were taken. RESULTS: Phytochemical analysis revealed that the highest amounts of polyphenolic compounds were present in L. sativum seeds and P. granatum leaves, while leaves of F. carica showed the highest amounts of alkaloid and flavonoid content compared to other extracts. Oral administration of F. carica and L. sativum extracts at the dosage of 100 and 200 mg/kg significantly reduced glucose, lipid profile, kidney, and liver enzyme levels. A significant increase in HbAlc levels was also observed with L. sativum extract at a dose of 200 mg/kg compared to diabetic controls. Mellitus rats supplemented with 100 and 200 mg/kg methanolic extracts of P. granatum had higher serum triglycerides and lower serum low-density lipoprotein cholesterol (LDL-C) than normal control rats. F. carica extract is more effective than L. sativum and P. granatum extracts in the prevention and control of type 2 diabetes mellitus (T2DM) and its consequences.
Assuntos
Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/tratamento farmacológico , Ficus , Hiperlipidemias/tratamento farmacológico , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Lepidium sativum , Lipídeos/sangue , Extratos Vegetais/farmacologia , Punica granatum , Animais , Biomarcadores/sangue , Glicemia/metabolismo , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Ficus/química , Hemoglobinas Glicadas/metabolismo , Hiperlipidemias/sangue , Hiperlipidemias/induzido quimicamente , Hipoglicemiantes/isolamento & purificação , Hipolipemiantes/isolamento & purificação , Lepidium sativum/química , Masculino , Extratos Vegetais/isolamento & purificação , Punica granatum/química , Ratos , EstreptozocinaRESUMO
CONTEXT: Garden cress (GC), fenugreek (FG), and black seed (BS) are traditional herbal medicine for managing hypertension. OBJECTIVE: The effects of the three herbs on the pharmacodynamics of metoprolol tartrate (MT) in hypertensive rats were investigated. MATERIALS AND METHODS: Wistar rats were divided in five groups (n = 6). Group I served as normal control group and Group II (hypertensive control group) had rats treated orally with N-nitro L-arginine methyl ester (L-NAME, 40 mg/kg/day) only. Groups III, IV, and V rats were orally treated with L-NAME (40 mg/kg/day) + GC (300 mg/kg, once daily), L-NAME (40 mg/kg/day) + FG (300 mg/kg, once daily) and L-NAME (40 mg/kg/day) + BS (300 mg/kg, once daily), respectively, for 2 weeks, and on the 14th day, blood pressure and heart rate were recorded using a tail-cuff blood pressure-measuring system. On the 16th day, a single dose of MT (10 mg/kg) was orally administered, and the rats' blood pressure and heart rate were recorded. RESULTS: GC, FG, and BS decreased systolic blood pressure (SBP) by 8.7%, 8.5%, and 8.7%, respectively, in hypertensive rats. A greater decrease in SBP by 14.5%, 14.8%, and 16.1% was observed when hypertensive rats were treated with L-NAME + GC + MT, L-NAME + FG + MT, and L-NAME + BS + MT, respectively. Similarly, hypertensive rats treated with the combination of herbs and MT had significantly lower diastolic blood pressure (DBP) than those treated with herbs alone and those treated with L-NAME alone. CONCLUSIONS: The combination of investigated herbs and MT had a beneficial effect on hypertension. However, the concurrent administration of drugs, particularly those predominantly cleared through CYP450 2D6-catalyzed metabolism, with the three investigated herbs should be considered with caution.
Assuntos
Anti-Hipertensivos/farmacologia , Interações Ervas-Drogas , Hipertensão/tratamento farmacológico , Metoprolol/farmacologia , Animais , Pressão Sanguínea/efeitos dos fármacos , Citocromo P-450 CYP2D6/metabolismo , Modelos Animais de Doenças , Frequência Cardíaca/efeitos dos fármacos , Lepidium sativum/química , NG-Nitroarginina Metil Éster , Nigella sativa/química , Ratos , Ratos Wistar , Trigonella/químicaRESUMO
The nutritional and health-promoting properties of plants are largely determined by their tissue chemistry. Tuning growth conditions could affect the accumulation of phytochemicals and, therefore, enhance the biological activities. Herein, the impact of elevated CO2 (eCO2; 620 µmol CO2 mol-1 air) on growth and chemical composition of sprouts of three Lepidium sativum cultivars (Haraz, Khider and Rajab) was investigated. Changes in the sprout actions against some human chronic diseases were evaluated. eCO2 induced biomass accumulation (1.46-, 1.47- and 2-fold in Haraz, Khider and Rajab, respectively) and pigment accumulation and reduced the level of antinutrients in L. sativum cultivars. Compared to the control, eCO2 induced total glucosinolate accumulation (0.40-, 0.90- and 1.29-fold in Khider, Haraz and Rajab, respectively), possibly through increased amino acid production, and their hydrolysis by myrosinase. In line with increased polyphenol production, improved phenylalanine ammonia lyase activity was observed. The antioxidant, anti-inflammatory, hypocholesterolemic, antibacterial and anticancer activities of the produced sprouts were significantly improved by sprouting and eCO2 exposure. PCA indicated that the cultivars showed interspecific responses. Thus, the present study confirms the synergistic effect of sprouting with eCO2 exposure as a promising approach to produce more bioactive L. sativum sprouts.
Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Dióxido de Carbono/metabolismo , Glucosinolatos/farmacologia , Lepidium sativum , Linhagem Celular Tumoral , Glucosinolatos/isolamento & purificação , Humanos , Lepidium sativum/química , Lepidium sativum/metabolismo , Extratos Vegetais/farmacologiaRESUMO
OBJECTIVE: The present study is carried out to screen the anticholinesterase effect of the total alkaloids of L. sativum seeds and other plants, and studied the ability of Lepidine B & E to inhibit AChE, BuChE, BACE, and MAGL. Hence, determining the main interactions in the inhibitorenzyme complex. METHODS: Inhibitory effect of Lepidium sativum, Juniperus phoenicea and Juniperus oxycedrus extracts on acetylcholinesterase using the Ellman method was investigated with Donepezil as the positive control. A molecular docking study is achieved using Autodock Vina. The structures of target molecules Lepidine B & E and the four enzymes were obtained from the PubChem database and Protein databank. RESULTS: Alkaloidal extract of Lepidium sativum and ethyl acetate extracts of Juniperus phoenicea and Juniperus oxycedrus exhibit a strong acetylcholinesterase inhibitory activity with IC50 values of 0.59 ± 0.04, 0.57 ± 0.00 and 0.49 ± 0.00 mg/mL, respectively using Donepezil <0.25 mg/mL as a positive control. The major components of alkaloids of L. sativum, Lepidine B & E bind tightly to AChE and BuChE as much as galantamine and donepezil. We suggest that Lepidine B is a noncompetitive inhibitory by interacting with PAS of AChE and BuChE, therefore it is capable to prevent the HuAChE-induced Aß aggregation. All the complexes of Lepidine B &E with the four enzymes show significant, several and different interactions. CONCLUSION: Our current study indicates that Lepidine B & E are promising anti-AD drugs and might become drug candidates to prevent Alzheimer's disease due to their multiple roles as potent inhibitors for AChE, BuChE, BACE, and MAGL. Indeed, they could inhibit Aß fibrillogenesis. No previous results about the inhibitory effect of Lepidine B & E on the AChE, BuChE, ß secretase, and monoacylglycerol lipase were reported.
Assuntos
Alcaloides/farmacologia , Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/farmacologia , Imidazóis/uso terapêutico , Extratos Vegetais/farmacologia , Acetilcolinesterase/efeitos dos fármacos , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/uso terapêutico , Doença de Alzheimer/enzimologia , Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Butirilcolinesterase/efeitos dos fármacos , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Donepezila/farmacologia , Humanos , Imidazóis/química , Imidazóis/isolamento & purificação , Concentração Inibidora 50 , Juniperus/química , Lepidium sativum/química , Simulação de Acoplamento Molecular , Monoacilglicerol Lipases/antagonistas & inibidores , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , SementesRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Obesity-induced insulin resistance and chronic inflammation appears to be the most frequent cause of diabetes and its related metabolic complications; in this way a new therapeutic approaches are needed to prevent the chronic obesity and insulin resistance. Lepidium sativum has been extensively used in traditional alternative medicine for cough, skin disease, liver disorder, diuretic, gastrointestinal problems, hair loss treatment, milk secretion during lactation as well as antioxidant, antihypertensive, anti-inflammatory, and antidiabetic activities. The hypoglycemic and hypolipidemic effect of Lepidium sativum have been observed by previous studies, but the underlying molecular mechanisms are unclear. AIM OF THE STUDY: In this study, we investigated the beneficial effect of Lepidium sativum ethanol and aqueous seed extracts on obesity, oxidative, inflammatory, and insulin sensitivity changes in the liver tissue of high fat diet (HFD)-fed rats. The bioactive constituents responsible for these activities have been identified for both extracts using HPLC and GC-MS. MATERIALS AND METHODS: Rats were fed HFD for 10 weeks. The obese rats were treated orally with the Lepidium sativum ethanol extracts (LSEE) at dose 200 and 400 mg/kg body weight (BW) and Lepidium sativum aqueous extracts (LSAE) at dose 200 mg/kg BW daily for 8 weeks. RESULTS: The findings of the present study pointed out a significant increase in the hepatic transaminases, lipid profile, leptin, and hepatic oxidative stress with decreased antioxidant capacity of HFD-fed rats. Consistent with this depiction; we determined the up-regulation of liver inflammatory markers with a significant down-regulation of insulin signaling components phospho-insulin receptor (p-IR), p-AKT, p-mammalian target of rapamycin (p-mTOR), and p-p70S6K after consumption of HFD for 10 weeks that indicates a deterioration of insulin sensitivity. Interestingly, the phytochemical screening of LSEE and LSAE exhibited positive results for phenolic, flavonoid, lipid, and some bioactive components as well as the in vitro antioxidant activity of both extracts clearly demonstrated their high antioxidant activities. Notably, LSEE and LSAE displayed a wide range of biological features including anti-obesity, anti-inflammatory, and antioxidant properties. Both extracts significantly decreased high glucose, leptin, lipid profile, liver enzymes levels, and body weight. We also found that LSEE and LSAE significantly alleviated lipid peroxidation and restored the antioxidant enzymes to normal levels. In parallel, the intracellular phosphorylation of classical markers of insulin signaling cascade p-IR/p-AKT/p-mTOR/p-p70S6K was up-regulated in the hepatic tissues of LSEE and LSAE-treated groups. CONCLUSION: This study provides evidence that LSEE and LSAE might be one promising dietary supplementation that could safely and effectively prevent the early metabolic alterations and weight gain caused by HFD further regulate the activation of insulin signaling pathway beside their powerful antioxidant and low-toxicity properties.
Assuntos
Inflamação/tratamento farmacológico , Lepidium sativum/química , Hepatopatias/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Dieta Hiperlipídica/efeitos adversos , Relação Dose-Resposta a Droga , Inflamação/patologia , Insulina/metabolismo , Resistência à Insulina , Hepatopatias/patologia , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ratos , Ratos Sprague-Dawley , Sementes , Serina-Treonina Quinases TOR/metabolismo , Aumento de Peso/efeitos dos fármacosRESUMO
BACKGROUND: Lepidium sativum (L. sativum), an annual herb belonging to family Brassicaceae is commonly known as Garden cress of Egyptian origin but now a day's cultivated worldwide. The plant material and its constituents are used in various traditional and folk medicines for the treatment of various liver diseases and other ailments. OBJECTIVE: This review aims to gather comprehensive information on L. sativum's bioactive constituents, and it's antioxidant, hepato-protective and anticancer activity. METHOD: Systematic exploration for research evidences were carried out using well-structured and focused review question and presented data in the tabular form for readers' convenience. RESULTS: The comprehensive literature survey was conducted, and we found that specific studies on L. Sativum and its bioactive compounds had been carried out to date. We explored the unique and selective effect of L. Sativum and its bioactive constituents to combat oxidative stress and hepatic carcinoma. CONCLUSION: The present article appraised that L. sativum extract has a potential therapeutic effect against liver toxicity and hepato-carcinoma. Graphical Abstract.
Assuntos
Lepidium sativum/química , Extratos Vegetais/farmacologia , Animais , Antioxidantes/farmacologia , Humanos , Fígado/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Estudos ProspectivosRESUMO
Lepidium sativum seeds are used traditionally to accelerate healing of bone fracture in addition to its culinary uses. This study aimed to characterize the osteoprotective effect of L. sativum in an ovariectomized rat model at two dose levels (50 and 100 mg/kg) using 17ß-estradiol as a positive reference standard. Moreover, a complete metabolite profile of L. sativum via UHPLC/PDA/ESI-MS, as well as headspace solid-phase microextraction (SPME)-GC/MS is presented. Results revealed that L. sativum extract exhibited significant anti-osteoporotic actions as evidenced by mitigating the decrease in relative bone weight concurrent with improved longitudinal and perpendicular femur compression strength. Further, the extract enhanced the serum bone formation biomarkers lactate dehydrogenase (LDH) activity and osteocalcin levels. The extract also inhibited exhaustion of superoxide dismutase (SOD) as well as glutathione peroxidase (GPx) activities and accumulation of lipid peroxides in bone tissues. This is in addition to ameliorating the rise in the markers of bone resorption carboxyterminal telopeptide, type I (CTXI) and tartrate-resistant acid phosphatase (TRAP) and modulating receptor activator of nuclear factor kappa-Β ligand (RANKL)/ osteoprotegerin (OPG) expression. Metabolite characterization suggests that glucosinolates, lignans, coumarins, phenolic acids, and alkaloids mediate these anti-osteoporotic effects in a synergistic manner.
Assuntos
Conservadores da Densidade Óssea , Osso e Ossos/metabolismo , Lepidium sativum/química , Osteoporose/metabolismo , Osteoporose/prevenção & controle , Ovariectomia/efeitos adversos , Fitoterapia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Sementes/química , Animais , Antioxidantes , Modelos Animais de Doenças , Feminino , Cromatografia Gasosa-Espectrometria de Massas , L-Lactato Desidrogenase/metabolismo , Osteocalcina/metabolismo , Osteogênese/efeitos dos fármacos , Osteogênese/genética , Osteoporose/etiologia , Extratos Vegetais/isolamento & purificação , Ratos , Ratos Wistar , Superóxido Dismutase/metabolismoRESUMO
Relatively few studies have been focused so far on magnesium-isotope fractionation during plant growth, element uptake from soil, root-to-leaves transport and during chlorophylls biosynthesis. In this work, maize and garden cress were hydroponically grown in identical conditions in order to examine if the carbon fixation pathway (C4, C3, respectively) might have impact on Mg-isotope fractionation in chlorophyll-a. The pigment was purified from plants extracts by preparative reversed phase chromatography, and its identity was confirmed by high-resolution mass spectrometry. The green parts of plants and chlorophyll-a fractions were acid-digested and submitted to ion chromatography coupled through desolvation system to multiple collector inductively coupled plasma-mass spectrometry. Clear preference for heavy Mg-isotopes was found in maize green parts (∆26Mgplant-nutrient 0.65, 0.74 for two biological replicates, respectively) and in chlorophyll-a (∆26Mgchlorophyll-plant 1.51, 2.19). In garden cress, heavy isotopes were depleted in green parts (∆26Mgplant-nutrient (-0.87)-(-0.92)) and the preference for heavy isotopes in chlorophyll-a was less marked relative to maize (∆26Mgchlorophyll-plant 0.55-0.52). The observed effect might be ascribed to overall higher production of energy in form of adenosine triphosphate (ATP), required for carbon fixation in C4 compared to C3, which could reduce kinetic barrier and make equilibrium fractionation prevailing during magnesium incorporation to protoporphyrin ring.
Assuntos
Clorofila A/análise , Lepidium sativum/crescimento & desenvolvimento , Magnésio/química , Zea mays/crescimento & desenvolvimento , Ciclo do Carbono , Fracionamento Químico , Clorofila A/química , Cromatografia de Fase Reversa , Hidroponia , Isótopos/química , Lepidium sativum/química , Extratos Vegetais/análise , Extratos Vegetais/química , Zea mays/químicaRESUMO
BACKGROUND: A mouse model in which diabetes mellitus was induced by low-dose streptozotocin (STZ) injection combined with a high-fat diet was used to study the effect of two water cress (Lepidium savitum) preparations. Diabetic mice were treated with dried cress powder or with water-soluble extracts (tested at two doses), together with proper control groups. The mice were evaluated after 4 weeks of continuous intervention for type 2 diabetic and associated markers. We determined blood glucose, body weight, total cholesterol (TC), triglyceride (TG), low-density lipoprotein (LDL), high-density lipoprotein (HDL), serum insulin levels, and DNA integrity of hepatic cells. The concentrations of malondialdehyde (MDA) and lipid peroxide (LPO) and the activities of four enzymes that are part of the antioxidant defense system were determined in liver samples, as well as gene expression (by semi-quantitative reverse transcription polymerase chain reaction) and enzyme activity of IRS-1, IRS-2, PI3K, AKT-2, and GLUT4. RESULTS: After 4 weeks of intervention, the levels of TC, TG, and LDL cholesterol were significantly (P < 0.5) decreased and HDL cholesterol was significantly increased. Enzyme activities of liver superoxide dismutase, glutathione, glutathione peroxidase, and catalase were significantly increased, whereas MDA and LPO concentrations were significantly reduced. The transcription level of the five genes assessed was increased, with corresponding increases in protein expression. CONCLUSION: Oral uptake of garden cress can significantly reduce the blood glucose and improve the blood lipid metabolism of diabetic mice. Considerable improvements in the activity of antioxidant defense enzymes were observed in type 2 diabetic mice that improved the body's antioxidant emergency response. © 2019 Society of Chemical Industry.
Assuntos
Glicemia/metabolismo , Dieta Hiperlipídica , Lepidium sativum/química , Lipídeos/sangue , Animais , Antioxidantes/metabolismo , Catalase/metabolismo , HDL-Colesterol/sangue , LDL-Colesterol/sangue , Fragmentação do DNA , Diabetes Mellitus Experimental/prevenção & controle , Regulação da Expressão Gênica , Transportador de Glucose Tipo 4/genética , Transportador de Glucose Tipo 4/metabolismo , Glutationa/metabolismo , Glutationa Peroxidase/metabolismo , Hemoglobinas Glicadas/metabolismo , Hipoglicemiantes/farmacologia , Insulina/sangue , Proteínas Substratos do Receptor de Insulina/genética , Proteínas Substratos do Receptor de Insulina/metabolismo , Peróxidos Lipídicos/metabolismo , Masculino , Malondialdeído/metabolismo , Camundongos , Camundongos Endogâmicos ICR , Estresse Oxidativo/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/genética , Fosfatidilinositol 3-Quinases/metabolismo , Extratos Vegetais/farmacologia , Superóxido Dismutase/metabolismo , Triglicerídeos/sangueRESUMO
BACKGROUND AND OBJECTIVE: The present paper aims to study the inhibition of Candida albicans growth as candidiasis treatment, using seeds of Lepidium sativum as source. METHODS: In vitro assays were carried out on the antifungal activity of three kinds of extracts from L. sativum seeds against four strains of C. albicans, then testing the same phytochemicals on the inhibition of Lipase (LCR). A new in silico study was achieved using molecular docking, with Autodock vina program, to find binding affinity of two important and major lepidine alkaloids (lepidine E and B) towards the four enzymes secreted by C. albicans as target drugs, responsible of vitality and virulence of this yeast cells: Lipase, Serine/threonine phosphatase, Phosphomannose isomerase and Sterol 14-alpha demethylase (CYP51). RESULTS: The results of the microdillution assay show that the hexanic and alkaloidal extracts have an antifungal activity with MICs: 2.25 mg/ml and 4.5mg/ml, respectively. However, Candida rugosa lipase assay gives a remarkable IC50 values for the hexanic extract (1.42± 0.04 mg/ml) followed by 1.7± 0.1 and 2.29 ± 0.09 mg/ml of ethyl acetate and alkaloidal extracts respectively. The molecular docking confirms a significant correlation between C. albicans growth and inhibition of crucial enzymes involved in the invasion mechanism and cellular metabolisms, for the first time there were an interesting and new positive results on binding modes of lepidine E and B on the four studied enzymes. CONCLUSION: Through this work, we propose Lepidine B & E as potent antifungal drugs.
Assuntos
Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Inibidores Enzimáticos/farmacologia , Proteínas Fúngicas/antagonistas & inibidores , Lepidium sativum , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Sementes , Antifúngicos/química , Antifúngicos/isolamento & purificação , Candida albicans/enzimologia , Candida albicans/crescimento & desenvolvimento , Sistema Enzimático do Citocromo P-450/metabolismo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Proteínas Fúngicas/química , Proteínas Fúngicas/metabolismo , Lepidium sativum/química , Lipase/antagonistas & inibidores , Lipase/metabolismo , Manose-6-Fosfato Isomerase/antagonistas & inibidores , Manose-6-Fosfato Isomerase/metabolismo , Terapia de Alvo Molecular , Fosfoproteínas Fosfatases/antagonistas & inibidores , Fosfoproteínas Fosfatases/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Conformação Proteica , Sementes/química , Relação Estrutura-Atividade , VirulênciaRESUMO
BACKGROUND AND OBJECTIVES: Environmental pollution with the different Aluminum (Al) containing compounds has been increased. Liver and kidney are two vital organs targeted by Al accumulation. The aim of this study was to assess the possible protective and curative effects of Lepidium sativum Linn (LS) against Al-induced impairment of liver and kidney in albino rat and to explore the mechanism behind this effect. MATERIALS AND METHODS: This experimental animal-based study included fifty albino rats divided into five groups, the control, LS-treated (20 mg/kg), AlCl3-treated (10 mg/kg), AlCl3 then LS, and AlCl3 plus LS-treated, simultaneously for 8 weeks. At the end of the experiment, hepatic and renal functions as well as the biomarkers of antioxidants activities were assessed in the serum. Both liver and kidney were dissected out and histopathologically examined. RESULTS: This study showed that administration of AlCl3 caused a significant (p<0.05) reduction in rats body weight. It significantly increased serum AST, ALT, ALP, bilirubin, urea, and creatinine levels and decreased total protein and albumin. AlCl3 significantly reduced enzymatic (catalase), nonenzymatic (reduced glutathione), and ferric reducing antioxidant power (FRAP) in the serum. Histopathologically, it induced necrosis and degeneration of hepatocytes, glomeruli, and renal tubules. Administration of LS after or along with AlCl3 significantly restored the serum biomarkers of liver and kidney functions to their near-normal levels and had the ability to overcome Al-induced oxidative stress and preserved, to some extent, the normal hepatic and renal structure. The coadministration of LS had a superior effect in alleviating Al-induced changes. CONCLUSION: Exposure to AlCl3 induced a set of functional and structural changes in the liver and kidney of rats evident through both biochemical and histopathological assessment. The antioxidant activity of LS seeds mediated a protective and curative effect of LS against such changes. Further study through a rigorous clinical trial to prove LS activity on human is recommended.
Assuntos
Cloreto de Alumínio/toxicidade , Doença Hepática Induzida por Substâncias e Drogas , Nefropatias , Lepidium sativum/química , Extratos Vegetais/farmacologia , Alumínio/toxicidade , Animais , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Nefropatias/induzido quimicamente , Nefropatias/metabolismo , Nefropatias/patologia , Nefropatias/prevenção & controle , Extratos Vegetais/química , RatosRESUMO
AIMS: This study aims to evaluate the impact of solid-state fermentation (SSF) by Trichoderma reesei on the phenolic content, antioxidant and antimicrobial activities of garden cress seeds (GCS). METHODS AND RESULTS: The factorial statistical design was employed to optimize the SSF conditions, incubation time, pH, temperature and moisture, for maximum production of the phenolic content and microbial carbohydrate-cleaving enzymes from GCS. The total phenolic content significantly increased from unfermented GCS (401 mg gallic acid equivalent (GAE) 100 g-1 ) to fermented GCS (3600 mg GAE 100 g-1 ) by ninefold. The total antioxidant activity significantly increased in fermented GCS. Fifteen phenolic compounds were detected in fermented GCS with high concentrations compared to 14 in unfermented GCS using high-performance liquid chromatography. A strong correlation between the production of the carbohydrate-cleaving enzymes and the phenolic content of fermented GCS was observed. The phenolic compounds of fermented GCS showed higher antimicrobial activity. CONCLUSIONS: The fermented GCS is a powerful source of phenolic compounds with high antioxidant potentials, which can be used as dietary supplement and antimicrobial agent. SIGNIFICANCE AND IMPACT OF THE STUDY: Solid-state fermentation is a promising technique used for production of added-value bioactive compounds. SSF increased the total phenolic content and antioxidant activity of GCS several folds compared to germination process, which recently studied.
Assuntos
Antioxidantes/farmacologia , Lepidium sativum/química , Lepidium sativum/microbiologia , Fenóis/química , Extratos Vegetais/farmacologia , Trichoderma/metabolismo , Antioxidantes/química , Antioxidantes/metabolismo , Cromatografia Líquida de Alta Pressão , Fermentação , Lepidium sativum/metabolismo , Fenóis/metabolismo , Fenóis/farmacologia , Extratos Vegetais/química , Sementes/química , Sementes/metabolismo , Sementes/microbiologiaRESUMO
The present study aimed to investigate the phytochemical and pharmacological identities of a Lepidium sativum L. (LS) flavonoid-rich extract and its beneficial effects on metabolic, hormonal, and histological status. Chemical screening, as well as high-performance liquid chromatography with diode-array detection (HPLC-DAD) identified high concentrations of the main flavonoid compounds in LS crude extract such as flavonols (quercetin, kaempferol), flavones (luteolin, apigenin), and especially flavanones (naringin, naringenin). Examinations of the biochemical and histopathological aspects showed the curative effects carried by LS flavonoid-rich extracts on high-fat diet-fed Wistar rats. In this study, we propose that these molecules probably exerted the bioactivity observed in the treated group through improving insulin sensitivity, dyslipidemia, inflammation, and pancreas ß cell integrity. PRACTICAL APPLICATIONS: The LS seed is widely used in traditional medicine to treat hyperglycemia and inflammation. During the traditional mixture preparation, the thermal procedures could impair the bioactions of the most interesting group of LS phytoconstituants, flavonoids. In the present study, we propose an appropriate procedure to preserve those phytochemicals and suggest them as a substitute for the management of metabolic diseases. The dried LS extract showed an incredible set of effective flavonoids, which revealed hypoglycemic, hypolipidemic, anti-inflammatory, cytoprotective, and antidiabetic activities. Thus, LS flavonoids constitute a remarkable product to consider in pharmaceutical industry targeting diabetes and heart diseases. Due to their enormous antioxidant potential, the LS flavonoids could be also used in food engineering and cosmetic preparations. Their practical applications is however often limited by low solubility and stability in lipophilic media. Therefore, a modification of the flavonoid structure is possibly required.
Assuntos
Suplementos Nutricionais/análise , Flavonoides/administração & dosagem , Lepidium sativum/química , Síndrome Metabólica/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/análise , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Humanos , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/análise , Hipolipemiantes/administração & dosagem , Hipolipemiantes/análise , Resistência à Insulina , Masculino , Síndrome Metabólica/metabolismo , Extratos Vegetais/análise , Ratos , Ratos Wistar , Sementes/químicaRESUMO
The aim of this study was to evaluate chemical and biological potential of garden cress (Lepidium sativum L.) to receive valuable plant extracts with potential application in pharmacy or food industry. Four techniques of extraction and three environmentally friendly solvents such as water, supercritical CO2 and ethanol have been tested. Biological activity and chemical profile were evaluated in obtained extracts. GC/MS analysis showed that SFE extract from dried sprouts of L. sativum was especially rich in such glucosinolate derivatives as benzyl cyanide and benzyl thiocyanate. However, the extract obtained from freeze-dried sprouts by SFE with addition of 96% ethanol as co-solvent was especially rich in flavonoids and simultaneously exhibited the best antimicrobial activity. Comparison of MALDI-TOF-MS spectra of all obtained extracts clearly indicates that both SFE and maceration with water are the most selective techniques of extraction due to the lowest level of interfering substances with high molecular masses.