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1.
Biomed Pharmacother ; 170: 116080, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38147737

RESUMO

The current study aimed to explore the possible prophylactic and therapeutic effect of Nigella sativa L. oil (NSO) against disruption of endocrine signals and injuries in the thyroid gland, ovary, and uterine tissues induced by sodium fluoride (NaF). Twenty-eight mature female Wistar rats were randomly allocated into four experimental groups (n = 7/group) as follows: control group; NaF group, orally received NaF (20 mg/kg b.wt.) daily; NSO/NaF, orally received NSO (300 mg/kg b.wt.) two weeks before being given NaF and continued throughout the experiment; and NSO+NaF group orally received NSO concurrently with NaF. Our results indicated that NSO restored hormonal balance and suppressed oxidative damage and inflammation. Moreover, the levels of triiodothyronine, thyroxine, thyroid peroxidase, estrogen (E2), progesterone, follicle-stimulating hormone, and luteinizing hormone were elevated, while prostaglandins F2-α and cortisol levels were decreased in NSO treated groups compared to NaF-intoxicated rats. As well, NSO significantly boosted levels of antioxidant molecules, and lowered lipid peroxidation of examined tissues, unlike NaF-treated group. NSO also up-regulated antioxidant enzymes, anti-apoptotic protein, zona pellucida sperm-binding protein, bone morphogenetic protein, and thyroid stimulating hormone, conversely down-regulated inflammatory cytokines, apoptotic proteins, estrogen receptor-α, estrogen receptor-ß, and thyroid stimulating hormone receptors compared to NaF-intoxicated group. Additionally, NSO ameliorated tissue damage of the thyroid gland, ovary, and uterus induced by NaF. -Overall, the prophylactic group (NSO/NaF) performed better antioxidant and anti-inflammatory activities than the treated group almost in all examined tissues, which is reflected by the improvement in the structure of the thyroid, ovarian, and uterine tissues.


Assuntos
Nigella sativa , Glândula Tireoide , Ratos , Feminino , Masculino , Animais , Ratos Wistar , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Ovário , Fluoreto de Sódio/toxicidade , Fluoreto de Sódio/metabolismo , Óleos de Plantas/farmacologia , Estresse Oxidativo , Útero/metabolismo , Receptores de Estrogênio/metabolismo , Sementes
2.
BMC Complement Med Ther ; 23(1): 370, 2023 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-37864233

RESUMO

BACKGROUND: Obesity is a global health issue arising from the unhealthy accumulation of fat. Medicinal plants such as Alstonia boonei stem bark has been reported to possess body weight reducing effect in obese rats. Thus, this study sought to investigate the in vitro and in silico effects of fractions from Alstonia boonei stem bark on selected obesity-related digestive enzymes and adipogenesis in 3T3-L1 preadipocytes. METHOD: Two fractions were prepared from A. boonei: crude alkaloid fraction (CAF) and crude saponin fraction (CSF), and their phytochemical compounds were profiled using Liquid chromatography with tandem mass spectrometry (LCMS/MS). The fractions were assayed for inhibitory activity against lipase, α-amylase and α-glucosidase, likewise their antiadipogenic effect in 3T3-L1 adipocytes. The binding properties with the 3 enzymes were also assessed using in silico tools. RESULTS: Eleven alkaloids and six saponin phytochemical compounds were identified in the CAF and CSF using LCMS/MS. The CAF and CSF revealed good inhibitory activity against pancreatic lipase enzyme, but weak and good activity against amylase respectively while only CSF had inhibitory activity against α-glucosidase. Both fractions showed antiadipogenic effect in the clearance of adipocytes and reduction of lipid content in 3T3-L1 adipocytes. The LCMS/MS identified compounds (41) from both fractions demonstrated good binding properties with the 3 enzymes, with at least the top ten compounds having higher binding energies than the reference inhibitors (acarbose and orlistat). The best two docked compounds to the three enzymes were firmly anchored in the substrate binding pockets of the enzymes. In a similar binding pattern as the reference acarbose, Estradiol-17-phenylpropionate (-11.0 kcal/mol) and 3α-O-trans-Feruloyl-2 α -hydroxy-12-ursen-28-oic acid (-10.0 kcal/mol) interacted with Asp197 a catalytic nucleophile of pancreatic amylase. Estradiol-17-phenylpropionate (-10.8 kcal/mol) and 10-Hydroxyyohimbine (-10.4 kcal/mol) interacted with the catalytic triad (Ser152-Asp176-His263) of pancreatic lipase while Estradiol-17-phenylpropionate (-10.1 kcal/mol) and 10-Hydroxyyohimbine (-9.9 kcal/mol) interacted with Asp616 and Asp518 the acid/base and nucleophilic residues of modelled α-glucosidase. CONCLUSION: The antiobesity effect of A. boonei was displayed by both the alkaloid and saponin fractions of the plant via inhibition of pancreatic lipase and adipogenesis.


Assuntos
Alcaloides , Alstonia , Saponinas , Camundongos , Ratos , Animais , Adipogenia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Alstonia/metabolismo , Células 3T3-L1 , Acarbose/farmacologia , alfa-Glucosidases , Casca de Planta , Obesidade/metabolismo , Lipase/metabolismo , Alcaloides/farmacologia , Amilases/farmacologia , Saponinas/farmacologia
3.
Biomed Pharmacother ; 165: 115126, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37494787

RESUMO

Several medicinal plants have drawn the attention of researchers by its phytochemical composition regarding their potential for treating chronic complications of diabetes mellitus. In this context, plants of the Myrtaceae family popularly used in Brazil for the treatment of diabetes mellitus, including Eugenia sonderiana, have shown beneficial effects due to the presence of phenolic compounds and saponins in their chemical constitution. Thus, the present work aimed to perform the phytochemical characterization of the hydroethanolic extract of E. sonderiana leaves using high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS), along with in vitro and in vivo studies of antidiabetic activity. The chemical characterization revealed the presence of phenolic compounds, flavonoids, neolignans, tannins, and saponins. In addition, the extract exhibited minimum inhibitory concentrations of alpha-amylase and alpha-glycosidase higher than the acarbose in the in vitro tests. Also, the in vivo tests revealed a slight increase in body mass in diabetic rats, as well as a significant decrease in water and feed consumption provided by the extract. Regarding serum biochemical parameters, the extract showed significant activity in decreasing the levels of glucose, hepatic enzymes, and triglycerides, in addition to maintaining HDL cholesterol levels within normal ranges, protecting the cell membranes against oxidative damage. Thus, the extract of E. sonderiana leaves was considered promising pharmaceutical ingredient in the production of a phytotherapy medication.


Assuntos
Diabetes Mellitus Experimental , Eugenia , Saponinas , Ratos , Animais , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Compostos Fitoquímicos/uso terapêutico , Fenóis/farmacologia , Folhas de Planta/química , Saponinas/uso terapêutico
4.
Toxics ; 11(6)2023 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-37368609

RESUMO

Jambolan fruit extract and choline were investigated for Aluminum tri chloride (AlCl3)-induced Alzheimer's disease in rats. Thirty-six male "Sprague Dawley" rats weighing (150 ± 10 g) were allocated into six groups; the first group was fed a baseline diet and served as a negative control. Alzheimer's disease (AD) was induced in Group 2 rats by oral administration of AlCl3 (17 mg/kg body weight) dissolved in distilled water (served as a positive control). Rats in Group 3 were orally supplemented concomitantly with both 500 mg/kg BW of an ethanolic extract of jambolan fruit once daily for 28 days and AlCl3 (17 mg/kg body weight). Group 4: Rivastigmine (RIVA) aqueous infusion (0.3 mg/kg BW/day) was given orally to rats as a reference drug concomitantly with oral supplementation of AlCl3 (17 mg/kg body weight) for 28 days. Group 5 rats were orally treated with choline (1.1 g/kg) concomitantly with oral supplementation of AlCl3 (17 mg/kg body weight). Group 6 was given 500 mg/kg of jambolan fruit ethanolic extract and 1.1 g/kg of choline orally to test for additive effects concurrently with oral supplementation of AlCl3 (17 mg/kg bw) for 28 days. Body weight gain, feed intake, feed efficiency ratio, and relative brain, liver, kidney, and spleen weight were calculated after the trial. Brain tissue assessment was analyzed for antioxidant/oxidant markers, biochemical analysis in blood serum, a phenolic compound in Jambolan fruits extracted by high-performance liquid chromatography (HPLC), and histopathology of the brain. The results showed that Jambolan fruit extract and choline chloride improved brain functions, histopathology, and antioxidant enzyme activity compared with the positive group. In conclusion, administering jambolan fruit extract and choline can lower the toxic impacts of aluminum chloride on the brain.

5.
Molecules ; 27(13)2022 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-35807566

RESUMO

Solanum elaeagnifolium is among the invasive plants of Morocco; studies on its chemical composition and biological activities are few in number in Morocco. S. elaeagnifolium has shown molluscicidal and nematicidal and cancer-inhibitory effects, anti-inflammatory, analgesic activity, and antibacterial activity. The objective of this research is to improve this plant and assess its antibacterial and antioxidant properties as well as its total polyphenolic content (TPC) and total flavonoid content (TFC). The Folin-Ciocalteu method and the aluminium-trichloride method were used to determine TPC and TFC in hydro-ethanolic (HEE) and hydro-acetonic (HAE) leaf extract. Three assays were performed to determine the antioxidant activity: the DPPH test (radical 2,2'-diphenyl-1-picrylhydrazyl), the FRAP test (Ferric Reducing Antioxidant Power), and the TAC test. Disk diffusion and microdilution were used to test antibacterial activity against four pathogenic bacteria and Candida albicans. The hydro-ethanolic extract 2.54 ± 0.4 mg EAG/g has a greater polyphenol concentration than the hydro-acetonic extract 1.58 ± 0.03 mg EAG/g. Although the flavonoid content of the hydro-acetonic extract (0.067 ± 0.001 mg EQ/g) is larger than that of the hydro-ethanolic extract (0.012 ± 0.001 mg EQ/g), the flavonoid content of the hydro-ethanolic extract (0.012 ± 0.001 mg EQ/g). The DPPH values were IC-50 = 0.081 ± 0.004 mg/mL for hydro-ethanoic extract and 0.198 ± 0.019 mg/mL for hydro-acetonic extract, both extracts superior to BHT (0.122 ± 0.021 g/mL). While the FRAP assay showed a low iron-reducing power values for both extracts compared to BHT), the overall antioxidant activity of the two extracts was found to be considerable. The overall antioxidant activity of the hydro-ethanolic extract was 8.95 ± 0.42 mg EAA/g, whereas the total antioxidant activity of the hydro-acetonic extract was 6.44 ± 0.61 mg EAA/g. In comparison with the antibiotic Erythromycin, HAE and HEE from S. elaeagnifolium leaves demonstrated significant antibacterial action. HAE had the best inhibitory efficacy against Bacillus subtilis DSM 6333, with an inhibition diameter of 10.5 ± 0.50 mm and a MIC of 7.5 ± 0.00 mg/mL, as well as against Proteus mirabilis ATCC 29906, with an inhibitory diameter of 8.25 ± 0.75 mm and a MIC of 15 ± 0.00 mg/mL.


Assuntos
Polifenóis , Solanum , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Hidroxitolueno Butilado , Flavonoides/farmacologia , Marrocos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Polifenóis/análise , Polifenóis/farmacologia
6.
Life (Basel) ; 12(5)2022 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-35629362

RESUMO

Obesity is a serious public health issue worldwide. Finding safe and efficacious products to reverse obesity has proven to be a difficult challenge. This study showed the effects of Coffea arabica or green coffee bean extract (GCBE) on obesity disorders and the improvement of obesity-induced insulin resistance, dyslipidemia, and inflammation. The active constituents of GCBE were identified via high-performance liquid chromatography. Twenty-four male albino Wistar rats were divided into two groups. The first group (Group I) was fed a control diet, whereas the second group was fed a high-fat diet (HFD) for eight weeks till obesity induction. The second group was equally subdivided into Group II, which received HFD, and Group III, which received HFD + GCBE for another eight weeks. The body and organ weights of the animals were measured, and blood and adipose tissue samples were collected for analysis. The results indicated that the administration of GCBE significantly decreased the body and organ weights. Furthermore, it had an ameliorative effect on serum biochemical parameters. It dramatically reduced total cholesterol, triacylglycerol, low-density lipoprotein cholesterol, very low-density lipoprotein cholesterol, glucose, and insulin levels. In addition, an improvement in homeostasis model assessment-insulin resistance and an enhancement of high-density lipoprotein cholesterol levels were observed compared with the HFD group. In addition, the group treated with GCBE exhibited a marked increase in serum levels of adiponectin (an anti-inflammatory adipokine). In addition, a considerable reduction in adipocyte hypertrophy was found following GCBE treatment. Remarkably, the administration of GCBE resulted in a remarkable decrease in the expression of RBP4 (a pro-inflammatory cytokine), whereas an increase in GLLUT4 expression was observed in the adipose tissue. This improved insulin resistance in GCBE-administered HFD rats compared with other HFD rats. Our study showed that GCBE exhibits anti-obesity activity and may be used as a natural supplement to prevent and treat obesity and its associated disorders.

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