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1.
Br J Pharmacol ; 2024 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-38644540

RESUMEN

BACKGROUND AND PURPOSE: White adipose tissue (WAT) is involved in rheumatoid arthritis (RA). This study explored its potential as an antirheumatic target. EXPERIMENTAL APPROACH: WAT status of healthy and adjuvant-induced arthritis (AIA) rats were compared. The contribution of WAT to RA pathology was evaluated by pre-adipocyte transplant experiments and by dissecting perirenal fat pads of AIA rats. The impact of RA on WAT was investigated by culturing pre-adipocytes. Proteins differentially expressed in WAT of healthy and AIA rats were identified by the UPLC/MS2 method. These together with PPARγ siRNA and agonist were used to treat pre-adipocytes in vitro. The medium was used for THP-1 monocyte culture. KEY RESULTS: Compared with healthy controls, AIA WAT was smaller but secreted more leptin, eNAMPT, MCP-1, TNF-α, and IL-6. AIA rat pre-adipocytes increased the levels of these adipokines in healthy recipients. RA patients' serum induced a similar secretion change and impaired differentiation of pre-adipocytes. Adipectomy eased AIA-related immune abnormalities and arthritic manifestations. Hepatokines PON1, IGFBP4, and GPIHBP1 were among the differential proteins in high levels in RA blood, and induced inflammatory secretions by pre-adipocytes. GPIHBP1 inhibited PPARγ expression and caused differentiation impairment and inflammatory secretion by pre-adipocytes, a similar outcome to PPARγ-silencing. This endowed the cells with an ability to activate monocytes, which can be abrogated by rosiglitazone. CONCLUSION AND IMPLICATIONS: Certain hepatokines potentiate inflammatory secretions by pre-adipocytes and expedite RA progression by inhibiting PPARγ. Targeting this signalling or abnormal WAT secretion by various approaches may reduce RA severity.

2.
J Pharm Pharmacol ; 2024 Feb 29.
Artículo en Inglés | MEDLINE | ID: mdl-38422325

RESUMEN

OBJECTIVES: Schisandrin B (Sch B) has been shown to possess anti-inflammatory and antioxidant properties, however, its antirheumatoid arthritis properties and potential mechanism remain unexplored. This study evaluated the potential of Sch B in adjuvant-induced arthritic (AIA) rats. METHODS: AIA was induced by injecting 0.1 ml of CFA into the paw of rats and the animals were administered with Sch B (50 mg/kg) for 28 days. The effects of Sch B were evaluated using arthritis severity, serum levels of oxido-inflammatory, and metabolic index parameters. KEY FINDINGS: Sch B eased arthritic symptoms by significantly reducing paw swelling and arthritic score and increased body weight gain. Moreover, Sch B alleviated the levels of oxido-inflammatory markers including interleukin-1 beta, interleukin-6, tumor necrosis factor alpha, nuclear factor kappa B, transforming growth factor ß1, inducible nitric oxide synthase and malonaldehyde, as well as increased the levels of superoxide dismutase, glutathione, and Nrf2. Sch B also remarkably restored the altered levels of triglyceride, aspartate aminotransferase, lactic acid, pyruvate, phosphoenolpyruvate carboxylase, glucose, hypoxia inducible factor-1 alpha, and vascular endothelial growth factor. In addition, Sch B markedly alleviated p65 expression in the treated AIA rats. CONCLUSION: This study suggests that Sch B alleviated AIA by reducing oxidative stress, inflammation, and angiogenesis.

4.
J Inflamm Res ; 16: 4271-4285, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37791116

RESUMEN

Background: Rheumatoid arthritis (RA) patients are prone to developing different metabolic complications. Traditional Chinese Medicine attributes this uncertainty to varied syndrome types. Methods and Results: We retrospectively analyzed some serological indicators of active RA patients and healthy individuals. Randomly selected RA patients were divided into three groups according to NAMPT and SIRT1 expression levels in white blood cells (WBCs). Their disease severity and metabolic status were compared. Representative blood samples were subjected to a UPLC-MS/MS-based metabolomics analysis. Different human WBCs were treated with oleic acid and palmitic acid in vitro. The results indicated that blood glucose and lipid levels were decreased in RA patients, but their decrease was not in accordance with disease severity. Nutrients in the patients highly expressing SIRT1 were well preserved, with the lowest levels of RF and ß-CTX and the highest levels of adiponectin and resistin. Most of them exhibited cold symptoms. When SIRT1 deficiency was obvious, lipid depletion became evident, irrespective of expression levels of NAMPT. Simultaneous high-expression of SIRT1 and NAMPT coincided with the increase in production of lactic acid and the prevalence of hot symptoms. Despite the low levels of IL-6, joint injuries were severe. The corresponding WBCs were especially sensitive to fatty acids anti-inflammatory treatments. The levels of CCL27, CCL11, CCL5, AKP, CRP and ESR were similar among all the groups. Conclusion: NAMPT overexpression is a risk factor for joint injuries and nutrient depletion in RA. Supplementation with lipids would exert beneficial effects on these RA patients. Its aftermath would cause even severe inflammation. Contrarily, SIRT1 up-regulation restrains inflammation and lipid depletion.

5.
Tissue Cell ; 85: 102254, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37866152

RESUMEN

This study investigated the protective activities of pinostrobin (PIN) against methotrexate (MTX)-induced ovarian toxicity. Female rats were administered with PIN (50 mg/kg) for 4 weeks, while MTX was administered from weeks 2-4 of PIN treatment. Serum hormonal profiles, ovarian oxidative stress, inflammatory and apoptotic biomarkers as well as ovarian histomorphometry were evaluated. MTX administration elicited profound deficit in serum progesterone and estrogen (E2) levels, while luteinizing hormone (LH) and follicle stimulating hormone (FSH) were significantly increased. Additionally, MTX administration was associated with significant increases in ovarian malondialdehyde, nitric oxide, NF-кB, TNF-α, IL-6, IL-1ß, iNOS and caspase-3 activity, as well as notable reduction in the activities of glutathione peroxidase, catalase and superoxide dismutase as well as the level of glutathione. Whereas, treatment with PIN significantly decreased serum levels of FSH and LH, as well as ovarian levels of NO, MDA, caspase 3, NF-κB, IL-1ß, IL-6, TNF-α and iNOS. PIN also significantly upregulated GSH, GPx, CAT and SOD in the ovarian tissues as well as increased serum E2 and progesterone levels compared to the MTX group. Furthermore, PIN significantly restored altered ovarian histoarchitecture in the treated group. These findings suggests that PIN exerts protective effects against MTX-triggered ovarian damages.


Asunto(s)
Antioxidantes , Metotrexato , Ratas , Femenino , Animales , Antioxidantes/farmacología , Metotrexato/toxicidad , Flavonoides/farmacología , Factor de Necrosis Tumoral alfa/metabolismo , Interleucina-6/farmacología , Progesterona/farmacología , Estrés Oxidativo , Glutatión/metabolismo , Antiinflamatorios/farmacología , FN-kappa B/metabolismo , Hormona Folículo Estimulante/farmacología
6.
Molecules ; 28(19)2023 Sep 29.
Artículo en Inglés | MEDLINE | ID: mdl-37836717

RESUMEN

Ethnomedicinal plants are important sources of drug candidates, and many of these plants, especially in the Western Ghats, are underexplored. Humboldtia, a genus within the Fabaceae family, thrives in the biodiversity of the Western Ghats, Kerala, India, and holds significant ethnobotanical importance. However, many Humboldtia species remain understudied in terms of their biological efficacy, while some lack scientific validation for their traditional uses. However, Humboldtia sanjappae, an underexplored plant, was investigated for the phytochemical composition of the plant, and its antioxidant, enzyme-inhibitory, anti-inflammatory, and antibacterial activities were assessed. The LC-MS analysis indicated the presence of several bioactive substances, such as Naringenin, Luteolin, and Pomiferin. The results revealed that the ethanol extract of H. sanjappae exhibited significant in vitro DPPH scavenging activity (6.53 ± 1.49 µg/mL). Additionally, it demonstrated noteworthy FRAP (Ferric Reducing Antioxidant Power) activity (8.46 ± 1.38 µg/mL). Moreover, the ethanol extract of H. sanjappae exhibited notable efficacy in inhibiting the activities of α-amylase (47.60 ± 0.19µg/mL) and ß-glucosidase (32.09 ± 0.54 µg/mL). The pre-treatment with the extract decreased the LPS-stimulated release of cytokines in the Raw 264.7 macrophages, demonstrating the anti-inflammatory potential. Further, the antibacterial properties were also evident in both Gram-positive and Gram-negative bacteria. The observed high zone of inhibition in the disc diffusion assay and MIC values were also promising. H. sanjappae displays significant anti-inflammatory, antioxidant, antidiabetic, and antibacterial properties, likely attributable to its rich composition of various biological compounds such as Naringenin, Luteolin, Epicatechin, Maritemin, and Pomiferin. Serving as a promising reservoir of these beneficial molecules, the potential of H. sanjappae as a valuable source for bioactive ingredients within the realms of nutraceutical and pharmaceutical industries is underscored, showcasing its potential for diverse applications.


Asunto(s)
Fabaceae , Plantas Medicinales , Plantas Medicinales/química , Antioxidantes/farmacología , Antioxidantes/química , Extractos Vegetales/química , Antibacterianos/farmacología , Antibacterianos/química , Luteolina , Bacterias Grampositivas , Bacterias Gramnegativas , Fitoquímicos/farmacología , Fitoquímicos/química , Etanol/química , Antiinflamatorios/farmacología , Antiinflamatorios/química
7.
Sci Rep ; 13(1): 11398, 2023 07 14.
Artículo en Inglés | MEDLINE | ID: mdl-37452121

RESUMEN

This study evaluated the cardioprotective properties of Boesenbergia rotunda extract (BrE) against doxorubicin (DOX) induced cardiotoxicity. Rats received oral gavage of BrE for 28 days and DOX (5 mg/kg/week for 3 weeks). Thereafter the animals were sacrificed, blood and cardiac samples were collected for biochemical, histological and immunohistochemical analyses. The results indicated that BrE attenuated DOX triggered body and cardiac weight loss and prevented against cardiac injury by mitigating histopathological alterations in cardiac tissues as well as serum cardiac function enzymes. BrE significantly reduced serum levels of aspartate transaminase (AST), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), troponin T (TnT) and creatine kinase-MB (CK-MB) in DOX-treated rats. Furthermore, BrE alleviated cardiotoxicity by reducing DOX instigated oxidative stress and potentiating the level of glutathione, as well as the activities superoxide dismutase and catalase in cardiac tissues. In addition, BrE significantly decreased the characteristic indices of DOX-induced cardiac inflammation and apoptosis. Immuno-histochemical analysis revealed that BrE decreased the stain intensity of p53 and myeloperoxidase (MPO) proteins compared to the DXB alone group. In conclusion, our results indicated that BrE modulated oxidative stress, inflammation and apoptosis to attenuate DOX-induced cardiac damage.


Asunto(s)
Antioxidantes , Zingiberaceae , Ratas , Animales , Antioxidantes/metabolismo , Cardiotoxicidad/metabolismo , Miocardio/metabolismo , Doxorrubicina/farmacología , Estrés Oxidativo , Antiinflamatorios/uso terapéutico , Inflamación/metabolismo , Zingiberaceae/metabolismo , Apoptosis
8.
Antibiotics (Basel) ; 12(5)2023 May 22.
Artículo en Inglés | MEDLINE | ID: mdl-37237843

RESUMEN

Cinnamomum species are a group of plants belonging to the Lauraceae family. These plants are predominantly used as spices in various food preparations and other culinary purposes. Furthermore, these plants are attributed to having cosmetic and pharmacological potential. Cinnamomum malabatrum (Burm. f.) J. Presl is an underexplored plant in the Cinnamomum genus. The present study evaluated the chemical composition by a GC-MS analysis and antioxidant properties of the essential oil from C. malabatrum (CMEO). Further, the pharmacological effects were determined as radical quenching, enzyme inhibition and antibacterial activity. The results of the GC-MS analysis indicated the presence of 38.26 % of linalool and 12.43% of caryophyllene in the essential oil. Furthermore, the benzyl benzoate (9.60%), eugenol (8.75%), cinnamaldehyde (7.01%) and humulene (5.32%) were also present in the essential oil. The antioxidant activity was indicated by radical quenching properties, ferric-reducing potential and lipid peroxidation inhibition ex vivo. Further, the enzyme-inhibitory potential was confirmed against the enzymes involved in diabetes and diabetic complications. The results also indicated the antibacterial activity of these essential oils against different Gram-positive and Gram-negative bacteria. The disc diffusion method and minimum inhibitory concentration analysis revealed a higher antibacterial potential for C. malabatrum essential oil. Overall, the results identified the predominant chemical compounds of C. malabatrum essential oil and its biological and pharmacological effects.

10.
Sci Rep ; 13(1): 5698, 2023 04 07.
Artículo en Inglés | MEDLINE | ID: mdl-37029128

RESUMEN

This present study investigated the protective effects of asperuloside (ASP) against cadmium-induced nephrocardiac toxicity. Rats were treated with 50 mg/kg of ASP for five weeks and CdCl2 (5 mg/kg, p.o., once daily) during the last 4 weeks of ASP treatment. The serum levels of blood urea nitrogen (BUN), creatinine (Scr), aspartate transaminase (AST), creatine kinase-MB (CK-MB), troponin T (TnT) and lactate dehydrogenase (LDH) were evealuted. Oxido-inflammatory parameters were detected via malondialdehyde (MDA), reduced glutathione (GSH), catalase (CAT), superoxide dismutase (SOD), tumor necrosis factor alpha (TNF-α), interleukin-6 (IL-6), interleukin-1beta (IL-1ß) and nuclear factor kappa B (NF-κB). Additionally, the cardiorenal levels of caspase 3, transforming growth factor-ß (TGF-ß), α-smooth muscle actin (α-SMA), collagen IV and Bcl2 were measured by ELISA or immunohistochemical assays. The results indicated that ASP significantly decreased Cd-instigated oxidative stress, serum BUN, Scr, AST, CK-MB, TnT and LDH as well as histopathological alterations. Furthermore, ASP notably attenuated Cd-induced cardiorenal and apoptosis and fibrosis by reducing caspase 3 and TGF-ß levels, as well as reducing the stain intensity of a-SMA and collagen IV, while increasing Bcl2 intensity. These results revealed that ASP attenuated Cd induced cardiac and renal toxicity which may be attributed to reducing oxidative stress, inflammation, fibrosis and apoptosis.


Asunto(s)
Intoxicación por Cadmio , Cadmio , Ratas , Animales , Cadmio/toxicidad , Caspasa 3/metabolismo , Estrés Oxidativo , Inflamación , Fibrosis , Forma MB de la Creatina-Quinasa , Apoptosis , Factor de Crecimiento Transformador beta/farmacología , Colágeno/farmacología , Antioxidantes/farmacología
11.
Biomed Pharmacother ; 162: 114689, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-37058820

RESUMEN

Mitragyna speciosa is a medicinal plant with a reputation for treating pains, diabetes as well as increasing energy and sexual desires. However, there is no scientific evidence to validate the antidiabetic effect of M. speciosa. This study investigated the antidiabetic effects of M. speciosa (Krat) ethanolic extract on fructose and streptozocin (STZ)-induced type 2 diabetic rats. In vitro antioxidant and antidiabetic effects were evaluated using DPPH, ABST, FRAP and α-glucosidase inhibitory assays. Rats with fructose/STZ induced T2D were treated with Krat (100 and 400 mg/kg) or metformin (200 mg/kg) for 5 weeks via oral gavage. Krat showed good antioxidant activity and also displayed potent α-glucosidase inhibitory activity. Administration of Krat to the diabetic rats significantly improved body weight gain, restored alterations in blood glucose level, glucose tolerance, dyslipidemia (increased cholesterol, triglycerides, low-density lipoprotein-cholesterol and reduced high-density lipoprotein), hepatorenal biomarkers alterations (alanine transaminase, aspartate transaminase, alanine phosphatase, creatinine and blood urea nitrogen) and oxidative stress indices (superoxide dismutase, glutathione and malondialdehyde)in the treated diabetic rats. Furthermore, Krat also restored pancreatic histological and increased immunohistochemical aberrations in the diabetic rats. These results for the first time demonstrated the antidiabetic and antihyperlipidemic potentials of M. speciosa, thus providing scientific reinforcement for the traditional use of the plant in the treatment of diabetes.


Asunto(s)
Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Mitragyna , Ratas , Animales , Hipoglucemiantes/farmacología , Antioxidantes/farmacología , alfa-Glucosidasas , Glucemia , Extractos Vegetales/farmacología , Colesterol , Estreptozocina
12.
Inflamm Res ; 72(5): 1021-1035, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-37016140

RESUMEN

OBJECTIVE: This study investigated the impacts of SIRT1 activation on rheumatoid arthritis (RA)-related angiogenesis. METHODS: HUVECs were cultured by different human serum. Intracellular metabolites were quantified by UPLC-MS. Next, HUVECs and rat vascular epithelial cells under different inflammatory conditions were treated by a SIRT1 agonist resveratrol (RSV). Cytokines and biochemical indicators were detected by corresponding kits. Protein and mRNA expression levels were assessed by immunoblotting and PCR methods, respectively. Angiogenesis capabilities were evaluated by migration, wound-healing and tube-formation experiments. To down-regulate certain signals, gene-specific siRNA were applied. RESULTS: Metabolomics study revealed the accelerated glycolysis in RA serum-treated HUVECs. It led to ATP accumulation, but did not affect GTP levels. RSV inhibited pro-angiogenesis cytokines production and glycolysis in both the cells, and impaired the angiogenesis potentials. These effects were mimicked by an energy metabolism interrupter bikini in lipopolysaccharide (LPS)-primed HUVECs, largely independent of HIF-1α. Both RSV and bikinin can inhibit the activation of the GTP-dependent pathway Rho/ROCK and reduce VEGF production. Abrogation of RhoA signaling reinforced HIF-1α silencing-brought changes in LPS-stimulated HUVECs, and overshadowed the anti-angiogenesis potentials of RSV. CONCLUSION: Glycolysis provides additional energy to sustain Rho/ROCK activation in RA subjects, which promotes VEGF-driven angiogenesis and can be inhibited by SIRT1 activation.


Asunto(s)
Artritis Reumatoide , Neovascularización Patológica , Humanos , Ratas , Animales , Resveratrol/farmacología , Neovascularización Patológica/tratamiento farmacológico , Factor A de Crecimiento Endotelial Vascular/genética , Sirtuina 1/genética , Sirtuina 1/metabolismo , Lipopolisacáridos/metabolismo , Cromatografía Liquida , Espectrometría de Masas en Tándem , Artritis Reumatoide/tratamiento farmacológico , Artritis Reumatoide/metabolismo , Citocinas/metabolismo , Glucólisis , Guanosina Trifosfato/metabolismo , Subunidad alfa del Factor 1 Inducible por Hipoxia/metabolismo
13.
Tissue Cell ; 81: 102035, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36753813

RESUMEN

5-fluorouracil (5-FU) is an efficacious fluoropyrimidine antimetabolite anticancer drug, however, its clinical utility is constrained due to side effect toxicity on delicate organs, including the heart. This study thus aimed at exploring the cardioprotective potentials of naringin (NRG) against 5-FU-induced cardiotoxicity in rats. We divided Wistar rats into four experimental groups (n = 6) for the administration of NRG (100 mg/kg bw, orally) and/or 5-FU (150 mg/kg bw, intraperitoneal). NRG was administered for 10 days, while 5-FU was injected on the 8th day only. Serum troponin-I (cTn-I) and creatine kinase (CK) were estimated. Cardiac activities/level of catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPx), reduced glutathione (GSH), malondialdehyde (MDA), interleukin-1ß (IL-1ß), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), inducible nitric oxide synthase (iNOS) and nuclear factor-ĸB (NF-κB) and caspase-3 were determined. 5-FU markedly increased cTn-I, CK, cardiac inflammatory mediators and caspase-3 expressions, whereas antioxidant mediators decreased appreciably when compared to the control groups. Interestingly, the prophylactic administration of NRG prominently inhibited the 5-FU-provoked oxidative stress, pro-inflammation and apoptosis in the heart of rats. Histopathology confirmed the biochemical results of the heart. Therefore, NRG is a potential natural flavonoid for mitigation of 5-FU cardiotoxicity in rats.


Asunto(s)
Cardiotoxicidad , Fluorouracilo , Ratas , Animales , Cardiotoxicidad/metabolismo , Caspasa 3/metabolismo , Ratas Wistar , Fluorouracilo/toxicidad , Doxorrubicina/farmacología , Estrés Oxidativo , Antioxidantes/farmacología , Antioxidantes/metabolismo , FN-kappa B/metabolismo
14.
Food Chem ; 414: 135691, 2023 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-36808030

RESUMEN

The dietary protein requirement for the world population that just clocked 8 billion should ideally come from the environmentally sustainable lithosphere and should be a plant-based and cost-affordable resource. Hemp proteins and peptides come to mind based upon increasing interest by consumers worldwide. We herein describe the composition and nutrition of hemp protein, including the enzymatic production of hemp peptides (HPs), which reportedly have hypoglycemic, hypocholesterolemic, antioxidative, antihypertensive, and immunomodulatory effects. The action mechanisms involved in each of the reported bioactivities are presented, while not undermining the applications or opportunities associated with HPs. The study's major goal is to compile the status of the art of the various therapeutic HPs and their prospect as drugs for multiple diseases while highlighting needed future developments. We present first the composition, nutrition, and functionality of hemp proteins, prior to reports on their hydrolysis for the production of HPs. It is concluded that HPs present excellent functional ingredients as nutraceuticals targeting hypertension and other degenerative diseases, which have yet to be capitalized upon for commercial uses.


Asunto(s)
Cannabis , Cannabis/química , Suplementos Dietéticos , Péptidos/química , Dieta , Antihipertensivos
15.
Mol Nutr Food Res ; 67(2): e2200429, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-36433679

RESUMEN

SCOPE: This study investigates the impacts of lard and related fatty acids intake on rheumatoid arthritis (RA) animal models. METHOD AND RESULTS: Collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) are induced in SD rats and C57 BL/6 mice respectively, which are fed by lard-rich diet (LRD) for 42 days with intake restriction or not. AIA SD rats are treated by representative fatty acids for 30 days. Body weight, arthritis score, and metabolic profile are periodically recorded. Monocyte distribution, cytokine/metabolites levels, gene expression, and tissue damages are investigated by flow cytometry, ELISA, colorimetry, PCR, and histological methods. After being treated by fatty acids in vitro, THP-1 monocytes and the corresponding medium are collected for ELISA, PCR, immunoblotting, and reporter gene assays. Irrespective of intake amounts, LRD decreases inflammatory cytokines and inhibits glycolysis in all rheumatic rodents. Furthermore, it alters monocyte distribution and promotes PPAR-γ expression in AIA mice. Overall evidences show that both saturated (SF) and unsaturated fatty acids (USF) from lard can attenuate inflammation by activating PPAR-γ. Silencing PPAR-γ abrogates their anti-inflammatory effects in vitro. Besides, SF can stimulate TLR4/NF-κB pathway. CONCLUSION: Lard consumption is beneficial for active inflammatory arthritis recovery. Even SF can activate PPAR-γ and consequently attenuate inflammation.


Asunto(s)
Artritis Experimental , PPAR gamma , Ratas , Ratones , Animales , PPAR gamma/genética , PPAR gamma/metabolismo , Ácidos Grasos , Artritis Experimental/tratamiento farmacológico , Artritis Experimental/patología , Ratas Sprague-Dawley , Citocinas/metabolismo , FN-kappa B/metabolismo , Inflamación
16.
Phytochemistry ; 206: 113504, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-36403669

RESUMEN

Phytochemical investigation of the underground parts of Arundina graminifolia D.Don Hochr was conducted leading to the isolation of nine new glucosyloxybenzyl 2R-benzylmalate and two new glucosyloxybenzyl 2R-isobutylmalate derivatives. The compounds were purified using chromatographic techniques and their structures were deduced based on spectroscopic techniques including nuclear magnetic resonance and high-resolution mass spectrometry as well as comparing with previous literature. The antioxidant activities of the isolated compounds were also evaluated. The compounds showed potent antioxidant activities in the ABTS radical scavenging, DPPH radical scavenging and FRAP activities. Furthermore, the isolated compounds were observed to exert minimal cytotoxic effects against RAW 264.7 cell, suggesting biocompatibility as well as cytoprotective effects against hydrogen peroxide induced cell toxicity.


Asunto(s)
Antineoplásicos , Orchidaceae , Antioxidantes/farmacología , Estructura Molecular , Espectroscopía de Resonancia Magnética , Orchidaceae/química
17.
Arch Physiol Biochem ; 129(6): 1187-1199, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33983859

RESUMEN

Diabetes mellitus is the most deadly and most prevalent metabolic disease of contemporary times. This study evaluated the antidiabetic, antioxidant, and pancreato-protective effects of Securidaca inappendiculata extract (SIE) in high-fructose/streptozotocin-induced type 2 diabetes. SIE (50, 100, and 200 mg/kg) was administered to diabetic rats for 8 weeks, thereafter glycaemic parameters, pancreatic ß cell function, lipid profile, hepatorenal function, and antioxidant parameters were evaluated in diabetic rats treated SIE. The results indicated that treatment with SIE markedly lowered blood glucose, lipid parameters, hepatorenal function parameters, and lipid peroxidation at the end of the intervention. Additionally, serum insulin levels were significantly increased as supported by restoration of pancreatic ß-cell cells in the H&E staining. Moreover, SIE also upregulated serum antioxidant enzyme activities in the treated diabetic rats. The results revealed that SIE possesses potent antihyperglycemic and antihyperlipidemic and antioxidant effects with the considerable restoration of pancreatic ß-cells function.


Asunto(s)
Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Securidaca , Ratas , Animales , Hipoglucemiantes/efectos adversos , Antioxidantes/efectos adversos , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Estreptozocina , Diabetes Mellitus Experimental/inducido químicamente , Cromatografía Líquida de Alta Presión , Ratas Wistar , Extractos Vegetales/efectos adversos , Lípidos
18.
Arch Physiol Biochem ; 129(1): 261-267, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33522287

RESUMEN

The present study investigated the effect of polyphenol-rich extract of Parkia speciosa (PPS) against pancreatic and hepatorenal dysfunction in high-fat diet (HFD)/streptozotocin (STZ)-induced diabetes. Diabetic rats were treated with PPS (100 and 400 mg/kg) and glibenclamide. The results revealed that diabetic rats displayed marked hyperglycaemia, hyperlipidaemia, hypoinsulinemia as well as alterations in serum renal and kidney function markers. Furthermore, diabetic rats showed significant increase in hepatorenal level of malonaldehyde as well as suppression of antioxidant enzyme activities. Whereas, diabetic rats that received PPS displayed marked attenuation in most of the aforementioned parameters compared to the untreated diabetic rats. Additionally, histological examination revealed restoration of histopathological alterations of the pancreas, liver, and kidney of PPS treated diabetic rats. In conclusion, the results demonstrated that PPS could decrease serum lipids and blood glucose level, enhance insulin level and hepatorenal antioxidant capacity, as well as ameliorate hepatorenal dysfunction in rats.


Asunto(s)
Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Fabaceae , Animales , Ratas , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Glucemia , Diabetes Mellitus Experimental/patología , Diabetes Mellitus Tipo 2/complicaciones , Diabetes Mellitus Tipo 2/patología , Dieta Alta en Grasa/efectos adversos , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Hígado , Páncreas/patología , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Estreptozocina/toxicidad , Gliburida/farmacología , Gliburida/uso terapéutico
19.
Molecules ; 27(23)2022 Nov 25.
Artículo en Inglés | MEDLINE | ID: mdl-36500302

RESUMEN

Plants are known to have numerous phytochemicals and other secondary metabolites with numerous pharmacological and biological properties. Among the various compounds, polyphenols, flavonoids, anthocyanins, alkaloids, and terpenoids are the predominant ones that have been explored for their biological potential. Among these, chalcones and bis-chalcones are less explored for their biological potential under in vitro experiments, cell culture models, and animal studies. In the present study, we evaluated six synthetic bis-chalcones that were different in terms of their aromatic cores, functional group substitution, and position of substitutions. The results indicated a strong antioxidant property in terms of DPPH and ABTS radical-scavenging potentials and ferric-reducing properties. In addition, compounds 1, 2, and 4 exhibited strong antibacterial activities against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Salmonella enteritidis. The disc diffusion assay values were indicative of the antibacterial properties of these compounds. Overall, the study indicated the antioxidant and antimicrobial properties of the compounds. Our preliminary studies point to the potential of this class of compounds for further in vivo investigation.


Asunto(s)
Antiinfecciosos , Chalconas , Animales , Antioxidantes/farmacología , Antioxidantes/química , Pruebas de Sensibilidad Microbiana , Chalconas/farmacología , Antocianinas , Extractos Vegetales/química , Antiinfecciosos/farmacología , Antibacterianos/farmacología , Antibacterianos/química , Escherichia coli
20.
Molecules ; 27(23)2022 Nov 29.
Artículo en Inglés | MEDLINE | ID: mdl-36500421

RESUMEN

Citrus plants are widely utilized for edible purposes and medicinal utility throughout the world. However, because of the higher abundance of the antimicrobial compound D-Limonene, the peel waste cannot be disposed of by biogas production. Therefore, after the extraction of D-Limonene from the peel wastes, it can be easily disposed of. The D-Limonene rich essential oil from the Citrus limetta risso (CLEO) was extracted and evaluated its radical quenching, bactericidal, and cytotoxic properties. The radical quenching properties were DPPH radical scavenging (11.35 ± 0.51 µg/mL) and ABTS scavenging (10.36 ± 0.55 µg/mL). There, we observed a dose-dependent antibacterial potential for the essential oil against pathogenic bacteria. Apart from that, the essential oil also inhibited the biofilm-forming properties of E. coli, P. aeruginosa, S. enterica, and S. aureus. Further, cytotoxicity was also exhibited against estrogen receptor-positive (MCF7) cells (IC50: 47.31 ± 3.11 µg/mL) and a triple-negative (MDA-MB-237) cell (IC50: 55.11 ± 4.62 µg/mL). Upon evaluation of the mechanism of action, the toxicity was mediated through an increased level of reactive radicals of oxygen and the subsequent release of cytochrome C, indicative of mitotoxicity. Hence, the D-Limonene rich essential oil of C. limetta is useful as a strong antibacterial and cytotoxic agent; the antioxidant properties exhibited also increase its utility value.


Asunto(s)
Citrus , Aceites Volátiles , Aceites Volátiles/farmacología , Aceites Volátiles/química , Citrus/química , Antioxidantes/farmacología , Antioxidantes/química , Staphylococcus aureus , Escherichia coli , Limoneno , Bacterias , Antibacterianos/farmacología , Pseudomonas aeruginosa
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