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1.
Molecules ; 28(13)2023 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-37446770

RESUMO

In this study, we examined the sub-acute toxicity of quercetin and ferulic acid and evaluated their effects on protein, cholesterol, and estrogen levels in vivo. Six groups of female Wistar rats were fed by gavage. The first and second groups represent the positive (Clomiphene citrate 10 mg/kg) and negative (NaCl 0.9%) control groups, while the other groups received quercetin and ferulic acid at doses of 5 and 10 mg/kg/day for 28 days. The sub-acute toxicity was monitored by examining the weights, biochemical parameters (AST, ALT, ALP, urea, and CREA), and histological changes in the kidneys and liver of the treated animals. Furthermore, the in vivo estrogenic effects were studied in terms of the serum and ovarian cholesterol levels, serum estradiol, and uterine proteins. Finally, Docking studies were conducted to evaluate the binding affinity of quercetin and ferulic acid for alpha and beta estrogen receptors. Results showed that both compounds were devoid of any signs of nephrotoxicity or hepatotoxicity. Additionally, quercetin and ferulic acid caused significant estrogenic effects evidenced by an increase of 8.7 to 22.48% in serum estradiol, though to a lesser amount than in the reference drug-treated group (64.21%). Moreover, the two compounds decreased the serum cholesterol levels (12.26-32.75%) as well as the ovarian cholesterol level (11.9% to 41.50%) compared to the negative control. The molecular docking in estrogen alpha and estrogen beta active sites showed high affinity of quercetin (-10.444 kcal/mol for estrogen alpha and -10.662 kcal/mol for estrogen beta) and ferulic acid (-6.377 kcal/mol for estrogen alpha and -6.3 kcal/mol for estrogen beta) to these receptors. This study provides promising insights into the potential use of quercetin as a therapeutic agent for the management of female fertility issues.


Assuntos
Estrogênios , Quercetina , Ratos , Animais , Feminino , Quercetina/farmacologia , Ratos Wistar , Simulação de Acoplamento Molecular , Estrona , Estradiol , Colesterol
2.
Molecules ; 28(4)2023 Feb 13.
Artigo em Inglês | MEDLINE | ID: mdl-36838767

RESUMO

Caralluma europaea (Guss.) is an important medicinal plant widely used in Morocco for various traditional purposes. Our work aimed to evaluate the phenolic composition, wound healing, antinociceptive, and anticancer activities of C. europaea extracts. Moreover, this study assessed the beneficial effect of C. europaea phytocompounds on the TRADD, cyclooxegenase-2, Wnt/ß-catenin, and tyrosine kinase signaling pathways. The wound healing effect of C. europaea formulations against skin burn was evaluated for 21 days. The cytotoxic effect of the C. europaea extracts was evaluated against human leukemic (K562 and HL60) and liver cancer cell lines (Huh-7) using the MTT test. All the phytoconstituents identified by UHPLC in the polyphenols were docked for their inhibitory power on protein casein kinase-1, glycogen synthase kinase-3-ß, cyclooxegenase-2, tyrosine kinase, and TRADD. Luteolin and kaempferol are the main compounds identified in C. europaea polyphenols. The group treated with polyphenols showed the greatest wound contractions and all tested extracts presented a significant antinociceptive effect. Polyphenols showed a remarkable antitumoral activity against the K562, HL60 and Huh-7 cell lines. Saponins exerted an important cytotoxic effect against the Huh-7 cell line, whereas no cytotoxicity was observed for the hydroethanolic and flavonoids extracts. Hesperetin and trimethoxyflavone presented the highest docking G-score on tyrosine kinase and cyclooxygenase, respectively.


Assuntos
Analgésicos , Antineoplásicos Fitogênicos , Extratos Vegetais , Polifenóis , Cicatrização , Humanos , Analgésicos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Apocynaceae/química
3.
Molecules ; 28(14)2023 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-37513251

RESUMO

The present study is based on a multidisciplinary approach carried out for the first time on Anacyclus pyrethrum var. pyrethrum and Anacyclus pyrethrum var. depressus, two varieties from the endemic and endangered medicinal species listed in the IUCN red list, Anacyclus pyrethrum (L.) Link. Therefore, morphological, phytochemical, and genetic characterisations were carried out in the present work. Morphological characterisation was established based on 23 qualitative and quantitative characters describing the vegetative and floral parts. The phytochemical compounds were determined by UHPLC. Genetic characterisation of extracted DNA was subjected to PCR using two sets of universal primers, rbcL a-f/rbcL a-R and rpocL1-2/rpocL1-4, followed by sequencing analysis using the Sanger method. The results revealed a significant difference between the two varieties studied. Furthermore, phytochemical analysis of the studied extracts revealed a quantitative and qualitative variation in the chemical profile, as well as the presence of interesting compounds, including new compounds that have never been reported in A. pyrethrum. The phylogenetic analysis of the DNA sequences indicated a similarity percentage of 91%. Based on the morphological characterisation and congruence with the phytochemical characterisation and molecular data, we can confirm that A. pyrethrum var. pyrethrum and A. pyrethrum var. depressus represent two different taxa.


Assuntos
Asteraceae , Chrysanthemum cinerariifolium , Chrysanthemum cinerariifolium/genética , Filogenia , Extratos Vegetais/química , Asteraceae/química , Compostos Fitoquímicos
4.
Molecules ; 27(13)2022 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-35807240

RESUMO

Ethnobotanical studies have reported the traditional medicinal uses of Acacia senegal (L.) Willd. and Argania spinosa (L.) Skeels against kidney stone formation and other chronic kidney diseases. The present work is undertaken to study the litholytic activity and the inhibiting activity of calcium oxalate crystallization by bioactive compounds identified in Argania spinosa (L.) Skeels press-cake (residue of Argan oil) and in Acacia senegal (L.) Willd. The litholytic activity was studied in vitro on cystine and uric acid stones using a porous bag and an Erlenmeyer glass. The study of the inhibiting activity of calcium oxalate crystallization, was based on temporal measurements of the optical density, registered at a 620 nm wavelength for 30 min using an ultraviolet−visible spectrophotometer. The silylation method was performed to identify phytochemicals, followed by gas chromatography coupled with mass spectrophotometry (GC/MS) analysis. The results show significant litholytic activity of Argania Spinosa press-cake hydro-ethanolic extract on uric acid and cystine stones, respectively, with dissolution rates (DR) of 86.38% and 60.42% versus 3.23% and 9.48% for the hydro-ethanolic extract of Acacia senegal exudate. Furthermore, the percentages of nucleation inhibition are 83.78% and 43.77% (p ˂ 0.05) for Argania spinosa and Acacia senegal, respectively. The results point to the detection of 17 phytochemicals in Argania spinosa press-cake extract, the majority of which are phenolic acids and have potent anti-urolithiatic action.


Assuntos
Acacia , Sapotaceae , Oxalato de Cálcio , Cistina , Frutas/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Sapotaceae/química , Senegal , Ácido Úrico/análise
5.
Saudi Pharm J ; 30(8): 1200-1214, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-36164579

RESUMO

Thymus vulgaris, Thymus satureioides, and Thymus zygis are endemic Moroccan species that are intensively used due to their extensive medications and culinary properties. To enhance and preserve these overexploited species, the effect of provenance on the chemical composition of essential oils and antimicrobial activity against human pathogens were studied. Essential oils (EO) obtained by hydrodistillation from the flowering tops of thyme species were analyzed by GC-SM. The determination of minimum inhibitory (MIC), bactericidal (MBC), and fungicide (MFC) concentrations of EO were studied by microplate microdilution. The correlation between the chemical composition of EO and antimicrobial properties were evaluated using R software. The samples studied gave variable yields, ranging from 0.70 ± 0.03% to 4.12 ± 0.21%. The main constituents of Thymus vulgaris harvested from the municipality of El Hammam are carvacrol (68.8%), γ-terpinene (11.5%), and p-cymene (3.9%), while borneol (41.3% and 31.7%) and carvacrol (14.6% and 9.8%) are the most abundant in Thymus satureioides of the communes of Tata and Tigrigra respectively. For Thymus zygis, the results revealed the dominance of carvacrol (51.7% and 57.5%) for the municipalities of Tigrigra and Ain Aghbal, thymol (47.1% and 42.1%) for the municipalities of Bensmim and Timahdite respectively. These chemical profiles have similarities, but also reveal differences from the results given in the literature. In addition, the essential oils most active towards the microorganisms evaluated were those of Thymus vulgaris, followed by Thymus zygis and Thymus satureioides. These EO have very powerful MIC (MIC â©½ 300 µg/ml) against Gram-negative bacteria, and in particular, concerning Enterobacters cloacae, Citrobacter koseri, and Acinetobacter baumannii. Thymus zygis EO is the most active on candidates compared to Thymus vulgaris and Thymus satureioides EO, except Candida dubliniensis which was inhibited by Thymus satureioides EO from the commune of Azrou with a MIC = 18.75 µg/ml. The correlation determined between the major components and MIC showed that phenols have the strongest positive effects on antimicrobial properties, followed by terpenes and non-aromatic alcohols. In addition, different sensitivities of pathogens to chemical families have been observed against Enterobacter cloacae, Citrobacter koseri, Candida parapsilosis, Staphylococcus aureus multiresistant, Pseudomonas aeruginosa, Acinetobacter baumannii, and Aspergillus niger. Our results support the idea that these oils could be very useful in flavoring, food preservation, as well as a source of antimicrobial agents of great power against multidrug-resistant strains.

6.
Molecules ; 26(7)2021 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-33808152

RESUMO

Numerous scientific studies have confirmed the beneficial therapeutic effects of phenolic acids. Among them gentisic acid (GA), a phenolic acid extensively found in many fruit and vegetables has been associated with an enormous confirmed health benefit. The present study aims to evaluate the antidiabetic potential of gentisic acid and highlight its mechanisms of action following in silico and in vitro approaches. The in silico study was intended to predict the interaction of GA with eight different receptors highly involved in the management and complications of diabetes (dipeptidyl-peptidase 4 (DPP4), protein tyrosine phosphatase 1B (PTP1B), free fatty acid receptor 1 (FFAR1), aldose reductase (AldR), glycogen phosphorylase (GP), α-amylase, peroxisome proliferator-activated receptor gamma (PPAR-γ) and α-glucosidase), while the in vitro study studied the potential inhibitory effect of GA against α-amylase and α-glucosidase. The results indicate that GA interacted moderately with most of the receptors and had a moderate inhibitory activity during the in vitro tests. The study therefore encourages further in vivo studies to confirm the given results.


Assuntos
Frutas/química , Gentisatos/metabolismo , Inibidores de Glicosídeo Hidrolases/metabolismo , Hipoglicemiantes/metabolismo , alfa-Amilases , alfa-Glucosidases/metabolismo , Humanos , Simulação de Acoplamento Molecular , Ligação Proteica , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo
7.
Molecules ; 26(22)2021 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-34833872

RESUMO

The study of bioactive molecules of natural origin is a focus of current research. Thymus algeriensis and Artemisia herba-alba are two medicinal plants widely used by the Moroccan population in the traditional treatment of several pathologies linked to inflammation. This study aimed to evaluate the single and combined antioxidant, anti-inflammatory and analgesic effects of the essential oils extracted from these two medicinal plants, and also their potential toxicity. Essential oils were extracted using hydro-distillation in a Clevenger-type apparatus. The antioxidant activity was evaluated by two methods: the scavenging of the free radical DPPH, and the reduction in iron. Anti-inflammatory activity was evaluated by evaluating the edema development induced by carrageenan injecting, while the analgesic power was evaluated according to the number of abdominal contortions induced by the intraperitoneal injection of acetic acid (0.7%). The acute oral toxicity was performed to assess the potential toxicity of the studied EOs, followed by an analysis of the blood biochemical parameters. The results of the two antioxidant tests indicated that our extract mixture exhibits good iron reduction capacity and very interesting DPPH free radical scavenging power, with an IC50 of around 4.38 ± 0.98 µg/mL higher than that of the benchmark antioxidant, BHT. The anti-inflammatory test demonstrated that the mixture administered orally at a dose of 150 mg/kg has a better activity, exceeding that of 1% Diclofenac, with a percentage of maximum inhibition of the edema of 89.99 ± 4.08. The number of cramps in the mice treated with the mixture at a dose of 150 mg/kg is significantly lower (29.80 ± 1.92) than those of the group treated with Tramadol (42.00 ± 2.70), respectively. The toxicity results show no signs of toxicity with an LD50 greater than 150 mg/Kg. These interesting results show that the two plants' EOs had an important anti-inflammatory, analgesic, and antioxidant activity, and also a powerful synergistic effect, which encourages further in-depth investigations on their pharmacological proprieties.


Assuntos
Artemisia/metabolismo , Óleos Voláteis/química , Thymus (Planta)/metabolismo , Analgésicos/química , Animais , Anti-Inflamatórios/química , Antioxidantes/química , Artemisia/química , Carragenina/uso terapêutico , Edema/tratamento farmacológico , Óleos Voláteis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/efeitos dos fármacos , Ratos , Thymus (Planta)/química
8.
Molecules ; 26(7)2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33916097

RESUMO

Depression and anxiety are major mental health problems in all parts of the world. These illnesses are associated with a number of risk factors, including oxidative stress. Psychotropic drugs of a chemical nature have demonstrated several side effects that elevated the impact of those illnesses. Faced with this situation, natural products appear to be a promising alternative. The aim of this study was to evaluate the anxiolytic and antidepressant effects of the Petroselinum sativum polyphenols in vivo, as well as its correlated antioxidant properties in vitro. Anxiolytic activity of the extract (50 and 100 mg/kg) was evaluated using the open field and the light-dark chamber tests, while the antidepressant activity was evaluated using the forced swimming test. The antioxidant activity of the extract was evaluated by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical test and the FRAP (iron-reducing capacity) test. The phenolic extract showed very powerful anxiolytic and antidepressant-like effects, especially at a dose of 100 mg/kg, decreasing the depressive behavior in mice (decreased immobility time) and also the anxiolytic behavior (tendency for discovery in the center and illuminated areas) better even than those of paroxetine and bromazepam (classic drugs) concomitant with those results the extract also showed an important antioxidant capacity. These preliminary results suggest that Petroselinum sativum exhibits anxiolytic and antidepressant potential for use as a complement or independent phytomedicine to treat depression and anxiety.


Assuntos
Ansiolíticos/farmacologia , Antidepressivos/farmacologia , Antioxidantes/farmacologia , Petroselinum/química , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Animais , Ansiolíticos/química , Antidepressivos/química , Antioxidantes/química , Ansiedade/tratamento farmacológico , Comportamento Animal/efeitos dos fármacos , Compostos de Bifenilo/antagonistas & inibidores , Depressão/tratamento farmacológico , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Aprendizagem em Labirinto/efeitos dos fármacos , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Polifenóis/química , Ratos , Ratos Wistar
9.
Molecules ; 26(2)2021 Jan 18.
Artigo em Inglês | MEDLINE | ID: mdl-33477662

RESUMO

Coriandrum sativum L. seeds are traditionally used to treat diabetes and its complications (inflammation and formation of reactive oxygen species) around the world. The present study investigates the antidiabetic, anti-inflammatory, and antioxidant effects of the polyphenol fraction of Coriandrum sativum seeds (PCS). Diabetic mice were orally administered with PCS (25 and 50 mg/kg b.w.) for 28 days. Oral glucose tolerance (OGTT) was also evaluated along with the anti-inflammatory effect, assessed by measuring paw edema development induced with carrageenan in Wistar rat and the antioxidant activity assessed using two tests (ß-carotene discoloration and DPPH). Treatment of diabetic mice with PCS for four weeks managed their high fasting blood glucose levels, improved their overall health, also revealed an excellent antihyperlipidemic activity. The OGTT result showed a potent antihyperglycemic activity, and following the anti-inflammatory and antioxidant effects, the PCS exhibited a perfect activity. LC-MS/MS result revealed the presence of 9 polyphenols. This modest work indicates that the PCS have an important antidiabetic, antihyperglycemic, antihyperlipidemic, anti-inflammatory, and antioxidant effect that can be well established treatment of diabetes and its complications.


Assuntos
Antioxidantes/farmacologia , Coriandrum/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Animais , Cromatografia Líquida , Diabetes Mellitus Experimental/patologia , Hiperglicemia/prevenção & controle , Camundongos , Ratos , Ratos Wistar , Sementes/química , Espectrometria de Massas em Tandem
10.
Molecules ; 26(3)2021 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-33530597

RESUMO

Caralluma europaea (Guss.) N.E.Br.: (C. europaea) is a wild medicinal plant belonging to the family Apocynaceae. It is commonly used in traditional medicines for treating several diseases. The present work aims to evaluate the anti-inflammatory, antibacterial, and antifungal potentials of C. europaea fractions including hydro ethanol (ET CE), n-butanol (But CE), and polyphenol (Poly CE). The chemical composition of hydroethanol, n-butanol, and polyphenol-rich fractions from C. europaea were determined using GC-MS after silylation. The anti-inflammatory effect of hydroethanol, n-butanol, and polyphenol-rich fractions was studied by carrageenan-induced paw edema. Antibacterial and antifungal activities of hydroethanol, n-butanol, and polyphenol-rich fractions against Gram-positive bacteria, Gram-negative bacteria, and yeasts were assessed using the disc diffusion and micro-dilution assays. The findings of the chemical characterization affirmed the presence of interesting bioactive compounds in C. europaea fractions. The polyphenol-rich fraction was the best inhibitor of edema by75.68% after 6 h of treatment. The hydroethanol fraction was the most active against both bacteria and yeasts. This study contributes to society as it provides potential bioactive compounds in C. europaea extract, which may help in fighting nosocomial antibiotic-resistant microbes.


Assuntos
Anti-Infecciosos/administração & dosagem , Anti-Inflamatórios/administração & dosagem , Apocynaceae/química , Infecção Hospitalar/microbiologia , Inflamação/tratamento farmacológico , Compostos Fitoquímicos/administração & dosagem , 1-Butanol/administração & dosagem , 1-Butanol/isolamento & purificação , 1-Butanol/farmacologia , Animais , Antibacterianos/administração & dosagem , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antifúngicos/administração & dosagem , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Carragenina/efeitos adversos , Infecção Hospitalar/tratamento farmacológico , Farmacorresistência Bacteriana/efeitos dos fármacos , Farmacorresistência Fúngica/efeitos dos fármacos , Feminino , Cromatografia Gasosa-Espectrometria de Massas , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Inflamação/induzido quimicamente , Masculino , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Polifenóis/administração & dosagem , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Ratos , Saccharomyces cerevisiae/efeitos dos fármacos
11.
Molecules ; 26(2)2021 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-33430115

RESUMO

Withania frutescens L. is a wild perennial woody plant used by the local population for diverse therapeutic purposes. This work aims to study for the first time the potential inhibitory effect of this plant hydroethanolic extract on α-amylase and α-glucosidase activities using in vitro methods and its antidiabetic and antihyperglycemic activities using alloxan-induced diabetic mice as a model for experimental diabetes. Two doses were selected for the in vivo study (200 and 400 mg/kg) and glibenclamide, a well-known antidiabetic drug (positive control) in a subacute study (28 days) where the antihyperglycemic activity was also assessed over a period of 12 h on diabetic mice. The continuous treatment of diabetic mice with the extract of Withania frutescens for 4 weeks succeeded to slowly manage their high fasting blood glucose levels (after two weeks), while the antihyperglycemic test result revealed that the extract of this plant did not control hyperglycemia in the short term. No toxicity signs or death were noted for the groups treated with the plant extract, and it shows a protective effect on the liver and kidney. The in vitro assays demonstrated that the inhibition of alpha-amylase and alpha-glucosidase might be one of the mechanisms of action exhibited by the extract of this plant to control and prevent postprandial hyperglycemia. This work indicates that W. frutescens have an important long term antidiabetic effect that can be well established to treat diabetes.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Inibidores de Glicosídeo Hidrolases , Hipoglicemiantes , Extratos Vegetais , Folhas de Planta/química , Withania/química , alfa-Amilases/antagonistas & inibidores , Animais , Diabetes Mellitus Experimental/enzimologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Camundongos , Extratos Vegetais/química , Extratos Vegetais/farmacologia
12.
Saudi Pharm J ; 29(10): 1185-1204, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34703372

RESUMO

Since their existence on earth, humans have used herbal medicine to meet their requirements for medication. The aim of the study: This work refers to a study conducted to carry out an ethnopharmacological survey of medicinal plants used for the treatment of cancer in Fez-Meknes region of Morocco. Material and Methods: To achieve this goal, 300 informants including 237 local people and 63 herbalists. They were requested to fill a survey related questionnaire aiming at the collection of data about the addressed objective. Informants were asked about the vernacular names, parts of medicinal plants used, mode of preparation, route of administration, reference area as well as the ecological distribution. The Relative Frequency of Citation (RFC) and Fidelity Level (FL) were calculated to identify the most effective plants recommended by informants for disease treatment. Results: The findings obtained in the present survey revealed that 94 species belonging to 47 families have been used for cancer treatment in the region of Fez-Meknes. Fruits, leaves, and seeds are the most commonly used plant parts, by the time powder and infusion arethe most common methods used fordrug preparations. Conclusion: This work may contribute towards the society as it provides interesting data on traditional medicinal knowledge of medicinal plantsused to fight cancer.

13.
Molecules ; 25(19)2020 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-33023252

RESUMO

Withania frutescens (W. frutescens) is a medicinal plant widely used to treat several diseases. This work aims to study phytochemical composition as well as acute and subacute toxicity of W. frutescens hydroethanolic extract in mice. The phytochemical composition of W. frutescens extract was performed using gas chromatographic analysis. Acute toxicity was studied in vivo with oral administration of single doses 400 mg/kg, 1000 mg/kg, and 2000 mg/kg for 14 days. Subacute toxicity was studied with the administration of repeated doses of 400 mg/kg/day and 2000 mg/kg/day for 28 days. Phytochemical analysis of W. frutescens hydro-ethanolic extract confirmed the presence of interesting chemical compounds. Acute toxicity results showed no toxic symptoms in mice treated with an increasing dose up to a maximum of 2000 mg/kg. Alongside acute toxicity, subacute data showed no clinical symptoms nor biochemical or histological alteration in mice treated with an increasing dose up to a maximum of 2000 mg/kg compared to the control group (p < 0.05). This study shows no toxic effects in animals treated with W. frutescens extract, and, therefore, this plant can be considered safe in animals up to 2000 mg/kg under both acute and subacute toxicity conditions.


Assuntos
Compostos Fitoquímicos/análise , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Folhas de Planta/química , Testes de Toxicidade Aguda , Withania/química , Animais , Peso Corporal/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Camundongos , Tamanho do Órgão/efeitos dos fármacos
14.
Molecules ; 25(21)2020 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-33139638

RESUMO

BACKGROUND: Olea europea L. subsp. europaea var. sylvestris (Mill) Lehr (Oleaster) is a wild endemic olive tree indigenous to the Mediterranean region. Olea europea leaves represent a natural reservoir of bioactive molecules that can be used for therapeutic purposes. AIM OF THE STUDY: This work was conducted to study antidiabetic and antihyperglycemic activities of flavonoids from oleaster leaves using alloxan-induced diabetic mice. The mode of action of flavonoids against eight receptors that have a high impact on diabetes management and complication was also investigated using molecular docking. RESULTS: During 28 days of mice treatment with doses 25 and 50 mg/kg b.w, the studied flavonoids managed a severe diabetic state (<450 mg/dL), exhibiting a spectacular antidiabetic and antihyperglycemic activity, and improved mice health status compared to diabetic control. The in-silico mode of action of oleaster flavonoids revealed the inhibition of protein tyrosine phosphatase 1B (PTP1B), Dipeptidyl-peptidase 4 (DPP4), α-Amylase (AAM), α-Glucosidase inhibition, Aldose reductase (AldR), Glycogen phosphorylase (GP), and the activation of free fatty acid receptor 1 (FFAR1). CONCLUSION: The findings obtained in the present work indicate that the flavonoids from the oleaster may constitute a safe multi-target remedy to treat diabetes.


Assuntos
Diabetes Mellitus Experimental , Flavonoides , Hipoglicemiantes , Modelos Biológicos , Olea/química , Folhas de Planta/química , Animais , Simulação por Computador , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patologia , Flavonoides/química , Flavonoides/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Camundongos
15.
Molecules ; 25(22)2020 Nov 23.
Artigo em Inglês | MEDLINE | ID: mdl-33238392

RESUMO

BACKGROUND: Anacyclus pyrethrum (A. pyrethrum) is a wild species belonging to the family Asteraceae, which is used in traditional medicines. AIM OF THE STUDY: This work was undertaken to study the chemical composition, analgesic, anti-inflammatory, and wound healing properties of hydroalcoholic extracts of different parts (roots, seeds, leaves, and capitula) of A. pyrethrum. Material and Methods: The phytochemical analysis of the studied extracts was conducted by GC-MS. The analgesic activity was evaluated in mice using acetic acid and formaldehyde methods. The anti-inflammatory activity was tested using the inhibitory method of edema induced in rats. The healing activity of the hydroethanolic extracts was explored by excision and incision wound healing models in rats. RESULTS: The phytochemical analysis of the studied plant extracts affirmed the presence of interesting compounds, including some newly detected elements, such as sarcosine, N-(trifluoroacetyl)-butyl ester, levulinic acid, malonic acid, palmitic acid, morphinan-6-One, 4,5.alpha.-epoxy-3-hydroxy-17-methyl, 2,4-undecadiene-8,10-diyne-N-tyramide, and isovaleric acid. The extracts of different parts (roots, seeds, leaves, and capitula) exhibited promising anti-inflammatory, analgesic, and wound healing effects, with percentages of inhibition up to 98%, 94%, and 100%, respectively. CONCLUSION: This study might contribute towards the well-being of society as it provides evidence on the potential analgesic, anti-inflammatory, and wound healing properties of A. pyrethrum.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Asteraceae/química , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Ácido Acético/análise , Analgésicos/administração & dosagem , Analgésicos/química , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Edema/tratamento farmacológico , Cromatografia Gasosa-Espectrometria de Massas , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Folhas de Planta/química , Raízes de Plantas/química , Ratos
16.
Molecules ; 25(23)2020 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-33266220

RESUMO

Origanum majorana L. is a plant commonly used in folk medicine to treat depression and several neurological disorders. This study aims to evaluate the antidepressant-like effect of the Origanum majorana L. polyphenols (OMP) obtained from the aerial parts using two different depression model tests: The forced swimming test (FST) and the tail suspension test (TST) in Swiss albino mice. The experiments were performed on days 1, 7, 14, and 21 with daily administration of different treatments. Two different doses were chosen for this study (50 and 100 mg/kg), and paroxetine was used as a positive control. Immobility as a consequence of the depression state was significantly reduced following the treatment with OMP, indicating an antidepressant effect. A subacute toxicity study was also performed following the Organization for Economic Co-operation and Development (OECD) Guidelines (407), showing no sign of toxicity for the studied doses. The phytochemical screening revealed the presence of 12 components, all belonging to polyphenols: Arbutin, rosmarinic acid, ursolic acid, quercetin-3-O-glucoside, quercetin-7-O-glucuronic acid, luteolin-7-O-glucoside, kaempferol-3-0-glucuronic acid, Kaempferol-3-0-pentose, caffeic acid, catechin, quercetin, and rutin. These findings suggest that O. majorana has interesting antidepressant-like properties, which deserve further investigation.


Assuntos
Antidepressivos/farmacologia , Depressão/tratamento farmacológico , Atividade Motora/efeitos dos fármacos , Origanum/química , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Animais , Antidepressivos/toxicidade , Depressão/patologia , Elevação dos Membros Posteriores , Masculino , Camundongos , Extratos Vegetais/toxicidade , Polifenóis/toxicidade , Natação , Testes de Toxicidade
17.
Bioorg Chem ; 93: 103337, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31627061

RESUMO

Our objective in this work is evaluated the antibacterial, antifungal and antioxidant activity of the phytochymic compounds of the roots and leaves of a species Withania frutescens. In the first part, the phenolic compound is determinate by the Folin-Ciocalteau reaction, the richness of the roots in polyphenols (53.33 ±â€¯1.20 mg EGA/g Extract) is six times higher than that of the leaves. The antioxidant test is evaluated by four methods: DPPH test, reducing power test (FRAP), total antioxidant capacity (CAT) and the ß-carotene discoloration test. The IC-50 values of the DPPH test of the studied parts are of the order of 0.36 µg/ml and 6.63 µg/ml, which showed a lower anti-free radical activity than that of BHT (0.12 µg/ml). The results obtained by the FRAP method revealed a low reducing power of iron for two extracts (EC-50 of 0.45%) compared to Quercetine (EC-50 of 0.03%). The compounds of root and leaf extracts have a significant total antioxidant capacity, respectively 477.65 ±â€¯37.60 and 317.03 ±â€¯46.64 mg EAA/g Extract. In the ß-carotene discoloration test, extracts from the aerial and underground parts showed antioxidant activity of 57% followed by (36%), respectively. The evaluation of the antibacterial activity of in vitro extracts against microorganisms is carried out by two methods: disc diffusion and microdilution. The results show that the extracts exert an intermediate inhibitory effect (inhibition diameter between 8 and 15 mm, the smallest MIC obtained is 2.80 mg/ml) on all strains tested. The antifungal activity was estimated by determining the growth inhibition rate of the fungus tested. Indeed, the compounds studied exhibit a good antifungal effect since the minimum inhibitory concentration (MIC) of 4.5 mg/ml for root extract and 9 mg/ml for leaf extract.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Polifenóis/farmacologia , Withania/química , Etanol/química , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/isolamento & purificação
18.
ScientificWorldJournal ; 2018: 7470384, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30510491

RESUMO

The aim of this study is to investigate in vitro antioxidant and antibacterial activities of the aqueous and hydroethanolic extracts for aerial parts of Herniaria hirsuta. Extracts were screened for their possible antioxidant activities by three tests: DPPH free radical-scavenging, reducing power, and molybdenum systems. The screening of antibacterial activity of extracts was individually evaluated against sixteen bacteria species using a disc diffusion method. Flavonoids, total phenols, and tannins content were performed for both extracts. It shows higher content in the hydroethanolic extract. The hydroethanolic extract showed a significant antioxidant activity for the three methods studies to the aqueous extract, but nonsignificant results compared to the reference (BHT). However, both extracts have negative effect on the strains studies for the antibacterial activity.


Assuntos
Antibacterianos/análise , Antioxidantes/análise , Caryophyllaceae , Compostos Fitoquímicos/análise , Extratos Vegetais/análise , Polifenóis/análise , Avaliação Pré-Clínica de Medicamentos , Marrocos , Componentes Aéreos da Planta
19.
Am J Ther ; 24(6): e706-e712, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-27058575

RESUMO

In this work, we characterized by high-performance liquid chromatography, the γ-tocopherol (573.66 µg/g), and by gas chromatography-mass spectrometry, the linoleic acid (62.05%) as major components from Peganum harmala L. seeds oil and evaluated their potential in vivo acute antiinflammatory, analgesic activities, and in vitro antioxidative capacity. The 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay showed an important antioxidant activity (62.50% with an IC50 of 4.8 mg/mL). In addition, the antiinflammatory effect of the formulation cream at 20% caused a reduction in inflammation at 5 hours after carrageenan application compared with diclofenac at 1% (60.4%; 45.65%; respectively). A slight potential peripheral analgesia was noted in plantar test in treated rats with cream (20 s). Therefore, our findings demonstrate that formulation cream of P. harmala seeds oil has an interesting antiinflammatory activity with a slight peripheral analgesic effect due mainly to its richness on linoleic acid, γ-tocopherol, and polyphenols and to its important antioxidant capacity.


Assuntos
Dermatite Atópica/tratamento farmacológico , Peganum/química , Extratos Vegetais/farmacologia , Óleos de Plantas/química , Sementes/química , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Carragenina/toxicidade , Cromatografia Líquida de Alta Pressão/métodos , Dermatite Atópica/induzido quimicamente , Modelos Animais de Doenças , Cromatografia Gasosa-Espectrometria de Massas/métodos , Humanos , Ácido Linoleico/farmacologia , Masculino , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Creme para a Pele/farmacologia , gama-Tocoferol/farmacologia
20.
Am J Ther ; 23(6): e1554-e1559, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26934730

RESUMO

This study is designed to evaluate the analgesic and anti-inflammatory activities of aqueous extract (AE) of Cistus ladanifer L. leaves in experimental animal models. The central analgesic activity of C. ladanifer AE is studied using hot plate method in rats, and the acute anti-Inflammatory activity of C. ladanifer is investigated by rats paw edema induced by subplantar injection of 0.5% carrageenan into the right hind paw. Rats are pretreated with AE of C. ladanifer at different doses (150, 175, and 200 mg/kg, i.p.). The tramadol and indomethacin are used as reference drugs for analgesic and anti-inflammatory studies, respectively. Our results show that the AE of C. ladanifer exhibited anti-inflammatory and analgesic effects dose dependent. In anti-inflammatory activity, the AE of C. ladanifer at all doses reduced significantly the edema paw inflammation after carrageenan injection. Furthermore at 200 mg/kg, the effect of AE is highly important than that of other doses. In addition, the same AE demonstrates significant analgesic effect in thermal-induced pain model. So, this activity is proved by significant reduction of pain score after administration of AE at all doses. The nociception protection effects in this case are, respectively, 70.3%, 74.55%, and 93.33% after administration of AE of C. ladanifer at doses 150, 175, and 200 mg/kg b.w. The results of our findings suggest that AE of C. ladanifer has potential analgesic and anti-inflammatory activities with evidence of possible involvement of peripheral and central effects in its actions.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Cistus/química , Extratos Vegetais/farmacologia , Analgésicos/administração & dosagem , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Carragenina , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Edema/tratamento farmacológico , Indometacina/farmacologia , Inflamação/tratamento farmacológico , Inflamação/patologia , Masculino , Marrocos , Dor/tratamento farmacológico , Dor/patologia , Extratos Vegetais/administração & dosagem , Ratos , Ratos Wistar , Tramadol/farmacologia
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