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1.
An Acad Bras Cienc ; 96(3): e20230604, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39016352

RESUMO

This study aims to evaluate the phytochemical properties of Bauhinia holophylla (Bong.) Steud leaf extract, and their impact on maternal reproductive and fetal development in diabetic rats. For this, adult female Wistar rats (100 days of life) received streptozotocin (40 mg/Kg, intraperitoneal) for induction of diabetes, were mated and distributed into four groups: Nondiabetic; Nondiabetic given B. holophylla; Diabetic; and Diabetic given B. holophylla. The plant extract was given by gavage at increasing doses: 200, 400, and 800 mg/Kg. At day 21 of pregnancy, liver and blood samples were obtained for oxidative parameters and biochemical analysis, respectively. The uterus was removed for maternal-fetal outcomes. Phytochemical analysis showed a high content of phenolic components and biogenic amines. B. holophylla extract did not alter the glycemic levels but improved the lipid profile in diabetic animals. Besides that, the number of live fetuses and maternal weight gain were decreased in Diabetic group, and were not observed in animals treated. The group Diabetic treated presented a higher percentage of fetuses classified as adequate for gestational age compared to the Diabetic group. However, the treatment with plant extract caused embryo losses, fetal growth restriction, and teratogenicity in nondiabetic rats. Thus, the indiscriminate consumption requires carefulness.


Assuntos
Bauhinia , Diabetes Mellitus Experimental , Hipoglicemiantes , Extratos Vegetais , Ratos Wistar , Animais , Feminino , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Bauhinia/química , Gravidez , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Ratos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Desenvolvimento Fetal/efeitos dos fármacos , Estreptozocina , Glicemia/efeitos dos fármacos , Glicemia/análise , Folhas de Planta/química
2.
Phytother Res ; 38(6): 2656-2668, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38487990

RESUMO

Tubular ferroptosis significantly contributes to renal inflammation and fibrosis, critical factors in chronic kidney disease (CKD). This study aims to investigate Kaempferitrin, a potent flavonoid glycoside from Bauhinia forficata leaves, renowned for its anti-inflammatory and antitumor effects, and to elucidate its potential mechanisms in mitigating inflammation and fibrosis induced by tubular ferroptosis. The study investigated Kaempferitrin's impact on tubular ferroptosis using a unilateral ureteral obstruction (UUO) model-induced renal inflammation and fibrosis. In vitro, erastin-induced ferroptosis in primary tubular epithelial cells (TECs) was utilized to further explore Kaempferitrin's effects. Additionally, NADPH oxidase 4 (NOX4) transfection in TECs and cellular thermal shift assay (CETSA) were conducted to identify Kaempferitrin's target protein. Kaempferitrin effectively improved renal function, indicated by reduced serum creatinine and blood urea nitrogen levels. In the UUO model, it significantly reduced tubular necrosis, inflammation, and fibrosis. Its renoprotective effects were linked to ferroptosis inhibition, evidenced by decreased iron, 4-hydroxynonenal (4-HNE), and malondialdehyde (MDA) levels, and increased glutathione (GSH). Kaempferitrin also normalized glutathione peroxidase 4 (GPX4) and Solute Carrier Family 7 Member 11(SLC7A11) expression, critical ferroptosis mediators. In vitro, it protected TECs from ferroptosis and consistently suppressed NOX4 expression. NOX4 transfection negated Kaempferitrin's antiferroptosis effects, while CETSA confirmed Kaempferitrin-NOX4 interaction. Kaempferitrin shows promise as a nephroprotective agent by inhibiting NOX4-mediated ferroptosis in tubular cells, offering potential therapeutic value for CKD.


Assuntos
Ferroptose , Fibrose , NADPH Oxidase 4 , Obstrução Ureteral , Animais , Ferroptose/efeitos dos fármacos , NADPH Oxidase 4/metabolismo , Camundongos , Fibrose/tratamento farmacológico , Obstrução Ureteral/tratamento farmacológico , Masculino , Quempferóis/farmacologia , Camundongos Endogâmicos C57BL , Inflamação/tratamento farmacológico , Modelos Animais de Doenças , Bauhinia/química , Túbulos Renais/patologia , Túbulos Renais/efeitos dos fármacos , Rim/efeitos dos fármacos , Rim/patologia , Células Epiteliais/efeitos dos fármacos
3.
Pharm Biol ; 62(1): 577-591, 2024 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-39016037

RESUMO

CONTEXT: The botanical species Bauhinia guianensis Aublet (Leguminosae-Cercidoideae) is traditionally used in the Amazon for medicinal purposes. OBJECTIVE: The acute toxicity of the hydroethanolic extracts from B. guianensis leaves and stems (HELBg and HESBg) was evaluated in zebrafish (Danio rerio), with emphasis on the embryonic developmental stage and adult alterations. MATERIALS AND METHODS: Extracts were analyzed on LC-DAD-MS/MS. Zebrafish eggs were inoculated individually with concentrations of HELBg and HESBg (0.25, 0.5, 0.75, 1.0, and 1.5 µg/mL), observed for 96 h. Adult zebrafish were treated with a single oral dose (100, 200, 500, 1000, and 2000 mg/kg) of HELBg and HESBg, observed for 48 h. RESULTS: HELBg and HESBg analysis detected 55 compounds. Both extracts exhibited toxicity, including embryo coagulation at higher doses of HELBg and absence of heartbeats in embryos at all doses of HESBg. Behavioral variations were observed; tissue alterations in adult zebrafish were found at the highest doses, primarily in the liver, intestine, and kidneys because of HELBg and HESBg effects. The LD50 of HESBg was 1717 mg/kg, while HELBg exceeded the limit dose of 2000 mg/kg. CONCLUSIONS: The study on acute toxicity of B. guianensis extracts exhibits significant toxic potential, emphasizing effects on embryonic and adult zebrafish. The results suggest relative safety of the species preparations, encouraging further clinical trials on potential biological activities.


Assuntos
Bauhinia , Embrião não Mamífero , Extratos Vegetais , Folhas de Planta , Testes de Toxicidade Aguda , Peixe-Zebra , Animais , Extratos Vegetais/toxicidade , Extratos Vegetais/isolamento & purificação , Bauhinia/química , Embrião não Mamífero/efeitos dos fármacos , Dose Letal Mediana , Relação Dose-Resposta a Droga , Caules de Planta , Etanol/toxicidade , Espectrometria de Massas em Tandem , Masculino , Solventes/química , Feminino
4.
Pharm Biol ; 61(1): 938-948, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37345554

RESUMO

CONTEXT: The antidiabetic effects of flavonoids have been reported, but it is still unclear whether 5,7,3',4',5'-pentamethoxyflavone, isolated from Bauhinia championii Benth. (Fabaceae), also exhibits such properties. OBJECTIVE: To isolate 5,7,3',4',5'-pentamethoxyflavone from B. championii using high-speed countercurrent chromatography and examine its potential in treating diabetic nephropathy. MATERIALS AND METHODS: The phytochemical constituents from the stems of B. championii were separated and purified with high-speed countercurrent chromatography; 5,7,3',4',5'-pentamethoxyflavone (PMF) was identified by mass spectrum, 1H-NMR, and 13C-NMR. After exposing mesangial cells to 30 mM glucose and either 5 µM or 10 µM PMF for 6 h, the levels of fibronectin (FN) and p-Smad2/3 were analyzed using Western blotting. Male Sprague-Dawley rats were injected intraperitoneally with 55 mg/kg streptozotocin to induce diabetes and then were randomized into three groups (n = 10): vehicle administration, low-dose (5 mg/kg) PMF, and high-dose (25 mg/kg) PMF by intragastric gavage for 3 months. A healthy group was included as the control. RESULTS: Compared to the diabetic group, low-dose and high-dose PMF treatment decreased the phosphorylation of Smad2/3 by 0.54- and 0.52-fold, and the accumulation of FN decreased by 0.82- and 0.77-fold in vitro; the phosphorylation of Smad2/3 was decreased by 0.39- and 0.37-fold, and the accumulation of FN decreased by 0.47- and 0.40-fold in vivo, respectively. Furthermore, PMF alleviated the glomerular basement membrane thickness and foot process fusion. CONCLUSION: The findings suggest for the first time that PMF may be a promising treatment option for diabetic kidney fibrosis, which warrants additional clinical investigation.


Assuntos
Bauhinia , Diabetes Mellitus Experimental , Nefropatias Diabéticas , Ratos , Masculino , Animais , Bauhinia/química , Estreptozocina , Ratos Sprague-Dawley , Diabetes Mellitus Experimental/tratamento farmacológico , Rim , Nefropatias Diabéticas/tratamento farmacológico
5.
Molecules ; 27(17)2022 Aug 24.
Artigo em Inglês | MEDLINE | ID: mdl-36080183

RESUMO

This study aimed to evaluate Bauhinia forficata infusions prepared using samples available in Rio de Janeiro, Brazil. As such, infusions at 5% (w/v) of different brands and batches commercialized in the city (CS1, CS2, CS3, and CS4) and samples of plant material botanically identified (BS) were evaluated to determine their total phenolic and flavonoid contents (TPC and TFC), antioxidant capacity (ABTS•+, DPPH•, and FRAP assays), phytochemical profile, volatile compounds, and inhibitory effects against the α-amylase enzyme. The results showed that infusions prepared using BS samples had lower TPC, TFC and antioxidant potential than the commercial samples (p < 0.05). The batch averages presented high standard deviations mainly for the commercial samples, corroborating sample heterogeneity. Sample volatile fractions were mainly composed of terpenes (40 compounds identified). In the non-volatile fraction, 20 compounds were identified, with emphasis on the CS3 sample, which comprised most of the compounds, mainly flavonoid derivatives. PCA analysis demonstrated more chemical diversity in non-volatile than volatile compounds. The samples also inhibited the α-amylase enzyme (IC50 value: 0.235−0.801 mg RE/mL). Despite the differences observed in this work, B. forficata is recognized as a source of bioactive compounds that can increase the intake of antioxidant compounds by the population.


Assuntos
Bauhinia , Antioxidantes/química , Bauhinia/química , Brasil , Flavonoides/farmacologia , Extratos Vegetais/química , alfa-Amilases
6.
J Recept Signal Transduct Res ; 41(2): 159-169, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32718219

RESUMO

INTRODUCTION: Natural products play a pivotal role in innovative drug discovery by providing structural leads for the development of new therapeutic agents against various diseases.The present study aims to focus on the in silico assessment of the therapeutic potential of antidiabetic phytoconstituents which were identified and isolated from the extracts of Bauhinia rufescens Lam, a medicinal plant traditionally used for various pharmacotherapeutic purposes. METHOD: The physicochemical and pharmacokinetic parameters of the previously isolated thirty eight compounds were predicted using SwissADME web tool whereas OSIRIS Property Explorer was used for toxicity risk assessment and drug- likeliness. Twelve compounds were selected for docking on human α-glucosidase and α-amylaseenzymes using Autodock 4.0 software. Furthermore, the active extract was in vivo tested for the antidiabetic activity and then identified usingTLC bioautographic method. RESULTS AND DISCUSSION: Eriodictyol was found to have the highest potential as an inhibitor against α-amylase with binding energy of -9.92 kcal/mol. Rutin was the most potent against α-glucosidase with binding energy of-9.15 kcal/mol. A considerable number of hydrogen bonds and hydrophobic interactions were computed between the compounds and the enzymes thereby making them energetically favorable and suggesting inhibition of these two enzymes as a plausible molecular mechanism for their antidiabetic effect. CONCLUSION: These two flavonoids could therefore be used as potential leads for structure- based design of new effective hypoglycemic agents.


Assuntos
Bauhinia/química , Inibidores de Glicosídeo Hidrolases/química , Hipoglicemiantes/química , alfa-Amilases/química , alfa-Glucosidases/química , Produtos Biológicos/química , Produtos Biológicos/uso terapêutico , Simulação por Computador , Diabetes Mellitus/tratamento farmacológico , Descoberta de Drogas , Flavonoides/química , Flavonoides/uso terapêutico , Inibidores de Glicosídeo Hidrolases/uso terapêutico , Humanos , Hipoglicemiantes/uso terapêutico , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Plantas Medicinais/química , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/efeitos dos fármacos
7.
Molecules ; 26(19)2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-34641514

RESUMO

The aim of this research was to establish the constituents of Bauhinia pulla as anti-diabetic agents. A phytochemistry analysis was conducted by chromatographic and spectroscopic techniques. The alpha-glucosidase inhibitory assay screening resulted in the isolation of eight known compounds of quercetin, quercitrin, luteolin, 5-deoxyluteolin, 4-methyl ether isoliquiritigenin, 3,2',4'-trihydroxy-4-methoxychalcone, stigmasterol and ß-sitosterol. Ethanol leaf extracts showed potential effects, which led to a strong inhibitory activity of isolated quercetin at 138.95 µg/mL and 5.41 µg/mL of IC50, respectively. The docking confirmed that flavonoids and chalcones had the same potential binding sites and responsibilities for their activity. This study was the first report of Bauhinia pulla chemical constituents and its alpha-glucosidase inhibition.


Assuntos
Bauhinia/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Flavonoides/química , Flavonoides/metabolismo , Simulação de Acoplamento Molecular , Estrutura Molecular , Extratos Vegetais/química , Folhas de Planta/química , Plantas Medicinais/química
8.
Molecules ; 26(23)2021 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-34885819

RESUMO

The present study reports a cost-effective, environmentally friendly method to increase the bioavailability and bio-efficacy of B. rufescens stem bark extract in the biological system via functional modification as B. rufescens stem bark nanoparticles (BR-TO2-NPs). The biosynthesis of BR- -NPs was confirmed by UV-visible (UV-vis) and Fourier-transform infrared (FT-IR) spectroscopy, transmission electron microscopy (TEM), and X-ray diffraction analyses. The shifts in FT-IR stretching vibrations of carboxylic and nitro groups (1615 cm-1), the O-H of phenolics or carboxylic acids (3405 cm-1), alkanes, and alkyne groups (2925 and 2224 cm-1) of the plant extract and lattice (455) indicated successful biosynthesis of BR- -NPs. Compared with the stem bark extract, 40 ng/dL dose of BR- -NPs led to a reduction in adipogenesis and an increase in mitochondrial biogenesis-related gene expressions, adiponectin-R1, PPARγC1α, UCP-1, and PRDM16, in maturing-adipocytes. This confirmed the intracellular uptake, bioavailability, and bio-efficiency of BR-TiO2-NPs. The lipid-lowering capacity of BR-TiO2-NPs effectively inhibited the metabolic inflammation-related gene markers, IL-6, TNF-α, LTB4-R, and Nf-κb. Further, BR-TiO2-NPs stimulating mitochondrial thermogenesis capacity was proven by the significantly enhanced CREB-1 and AMPK protein levels in adipocytes. In conclusion, BR-TiO2-NPs effectively inhibited lipid accumulation and proinflammatory adipokine levels in maturing adipocytes; it may help to overcome obesity-associated comorbidities.


Assuntos
Adipócitos/citologia , Adipócitos/metabolismo , Adipocinas/metabolismo , Bauhinia/química , Metabolismo dos Lipídeos , Nanopartículas Metálicas/química , Casca de Planta/química , Titânio/farmacologia , Adipogenia/efeitos dos fármacos , Adipogenia/genética , Morte Celular/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Diferenciação Celular/genética , Forma Celular/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Metabolismo dos Lipídeos/genética , Lipólise/efeitos dos fármacos , Lipólise/genética , Células-Tronco Mesenquimais/efeitos dos fármacos , Células-Tronco Mesenquimais/metabolismo , Nanopartículas Metálicas/ultraestrutura , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Caules de Planta/química , Termogênese/efeitos dos fármacos , Termogênese/genética
9.
J Nat Prod ; 83(6): 1980-1989, 2020 06 26.
Artigo em Inglês | MEDLINE | ID: mdl-32453565

RESUMO

Our previous study showed that kaempferitrin, the main flavonoid from Bauhinia forficata Link leaves, induces diuresis and saluresis when orally given to rats. Since afzelin (AFZ) and kaempferol (KFL) are active compounds from the biometabolism of kaempferitrin, the diuretic and renal protective properties of these two compounds were evaluated. While the acute treatment with AFZ evoked a diuretic action associated with an increase in Cl- excretion and a Ca2+-sparing effect, KFL did not present any activity. The pretreatment with a muscarinic receptor blocker or with an inhibitor of the cyclooxygenase fully avoided AFZ-induced diuresis. AFZ also induced a prolonged (7-day treatment) diuretic effect in normotensive (NTR) and hypertensive rats (SHR), with an increase of urinary Na+ and Cl- excretion, while it decreased the elimination of Ca2+. AFZ was able to decrease ROS and nitrite generation on kidney homogenates in comparison with the SHR group treated with the vehicle, as well as mitigated the changes in the renal corpuscle region (glomerulus and Bowman's capsule). Moreover, AFZ significantly reduced calcium oxalate crystal formation in urine, with inhibition rates of 41% for the NTR and 92% for the SHR group. Taken together, this study shows that AFZ exerts acute and prolonged diuretic effects plus protective renal properties.


Assuntos
Diuréticos/farmacologia , Hipertensão/tratamento farmacológico , Quempferóis/farmacologia , Nefropatias/prevenção & controle , Manosídeos/farmacologia , Proantocianidinas/farmacologia , Substâncias Protetoras/farmacologia , Animais , Antioxidantes/farmacologia , Bauhinia/química , Cálcio/metabolismo , Cloretos/metabolismo , Inibidores de Ciclo-Oxigenase/farmacologia , Nefropatias/patologia , Estrutura Molecular , Antagonistas Muscarínicos/farmacologia , Folhas de Planta/química , Ratos , Ratos Endogâmicos SHR , Ratos Wistar , Espécies Reativas de Oxigênio/metabolismo
10.
Environ Toxicol ; 35(7): 774-782, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32061153

RESUMO

This study aims to investigate the protective effects of the Bauhinia championii (BC) against ischemia/reperfusion (I/R)-induced injury in an isolated heart model. Langendorff-perfused C57BL/6JNarl mice hearts were performed with 30 minutes ischemia and 60 minutes reperfusion by left anterior descending artery ligation. Before reperfusion, boiling water extracts of BC (10 mg/L) was pretreated for 15 minutes. During reperfusion, BC significantly decreased the occurrence of ventricular arrhythmias by lead II electrocardiogram (ECG). Electrophysiological effect of BC was further determined in isolated ventricular myocytes by whole-cell patch clamp technique. The underlying mechanism may result from its Na+ channel blocking activity characterized with reduced rise slope of action potential and Na+ current density. Moreover, BC dramatically reduced I/R-caused infarct size, which was accessed by 2,3,5-triphenyltetrazolium chloride (TTC) assay. Since BC decreased I/R-induced myoglobin release and oxidation of Ca2+ -calmodulin-dependent protein kinase, inhibition of myocardial necroptosis may account for the protective effects of BC on myocytes lose. This study indicated that BC may prevent I/R induced ventricular arrhythmias and myocyte death by blocking Na+ channels and decreasing necroptosis, respectively. Since most of the available antiarrhythmic remedies have unwanted adverse actions, BC could be a novel candidate for the treatment of myocardial infarction and ventricular arrhythmia.


Assuntos
Bauhinia/química , Coração/efeitos dos fármacos , Traumatismo por Reperfusão Miocárdica/prevenção & controle , Extratos Vegetais/farmacologia , Bloqueadores dos Canais de Sódio/farmacologia , Animais , Eletrocardiografia , Técnicas In Vitro , Masculino , Potenciais da Membrana/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos C57BL , Infarto do Miocárdio/metabolismo , Infarto do Miocárdio/patologia , Infarto do Miocárdio/prevenção & controle , Traumatismo por Reperfusão Miocárdica/metabolismo , Traumatismo por Reperfusão Miocárdica/patologia , Miocárdio/metabolismo , Miocárdio/patologia , Miócitos Cardíacos/metabolismo , Miócitos Cardíacos/patologia , Necroptose/efeitos dos fármacos , Técnicas de Patch-Clamp , Componentes Aéreos da Planta/química , Extratos Vegetais/isolamento & purificação , Bloqueadores dos Canais de Sódio/isolamento & purificação , Canais de Sódio/metabolismo
11.
Trop Anim Health Prod ; 52(6): 3045-3059, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32592112

RESUMO

Within the evaluation of the quality of forage resources, the main parameter that defines it is the digestibility of dry matter, which together with the amount of neutral and acidic detergent fibers and crude protein constitutes the basic information to assess forages which are supplied in the diet of the cattle. This research was carried out at the University of Los Llanos (Villavicencio, Colombia), and its objective was to determine the digestibility of three forages in cattle through three different in vitro techniques: inoculation with ruminal fluid and with feces and enzymatic digestibility technique, making the comparison with the in situ technique in order to validate the techniques and equipment that are being used for these procedures. The following species were evaluated: Pennisetum purpureum (PP), Tithonia diversifolia (TD), and Bauhinia variegata (BV), assessing the curve and rate of degradation of dry matter (DM), neutral detergent fiber (NDF), and total protein (TP) (0 to 72 h). A design of repeated measures was used, under which the analysis of variance was carried out to determine the ranges of deviation between the techniques and thus establish the trend of the data; the variables evaluated were the DM, NDF, and TP digestibilities of the three forages using the four techniques (three in vitro and one in situ). After verifying the differences between the variances of the digestibilities and checking the sphericity assumption with the Mauchly test, multiple comparisons were made with the Bonferroni test with a significance of 5%. The digestibility of DM, NDF, and TP varied between 38.62 and 44.22, 54.18 and 66.97, and 47.54 and 57.05%; 49.07 and 70.70, 72.52 and 75.44, and 62.61 and 74.02%; 29.93 and 34.84, 26.21 and 70.88, and 25.67 and 50.60% respectively in forages PP, TD, and BV, depending on the technique used for their estimation. Despite finding statistically significant differences between several of the comparisons made in the digestibility techniques, a high coefficient of determination and a high correlation between the in vitro estimations with respect to the in situ estimation were found; therefore, it is possible to use these techniques routinely thus avoiding the need to have cattle with fistulae to perform digestibility tests, with enzymatic digestibility technique being the most practical one.


Assuntos
Bauhinia/química , Digestão , Pennisetum/química , Tithonia/química , Fenômenos Fisiológicos da Nutrição Animal , Animais , Bovinos/fisiologia , Colômbia
12.
Phytother Res ; 33(1): 90-106, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30281176

RESUMO

This study evaluated the effects of flavonoid-rich fraction from Bauhinia forficata leaves (FRF-BF), against intestinal toxicity induced by irinotecan. The leaves of this plant are used like tea in Brazilian folk medicine, and it is rich in flavonoids, mainly kaempferitrin. First, the chemopreventive effects of FRF-BF and kaempferitrin were evaluated in intestinal cells (IEC-6 cells) exposed to irinotecan. Next, the effects were evaluated against irinotecan-induced mucositis in mice. Lastly, melanoma was induced in C57BL/6 mice to evaluate FRF-BF interference on irinotecan antitumor activity. The results showed that FRF-BF and kaempferitrin exert no cytotoxic effects in IEC-6 cells and confirmed that pretreatment with FRF-BF and kaempferitrin displays chemoprotective effects against cytotoxicity induced by irinotecan. Interestingly, the FRF-BF (100 mg/kg, p.o) reduced the intestinal motility in mice and attenuated parameters linked to irinotecan-induced intestinal mucositis, including diarrhea, histological damage, depletion of duodenal GSH, amount of TNF-α, and MPO activity in the small intestine. Also, FRF-BF does not interfere in the antitumor activity of irinotecan and exerted antitumoral activity in murine melanoma. In conclusion, FRF-BF (100 mg/kg, p.o) presents promising pharmacological potential to prevent and attenuate the severity of intestinal mucositis during chemotherapy treatment, related to the presence of kaempferitrin.


Assuntos
Bauhinia/química , Flavonoides/química , Irinotecano/efeitos adversos , Extratos Vegetais/química , Folhas de Planta/química , Animais , Irinotecano/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL
13.
Bioprocess Biosyst Eng ; 42(2): 305-319, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30421171

RESUMO

The synthesis of metal nanoparticles by green methods attained enormous attention in recent years due to its easiness, non-toxicity, and eco-friendly nature. In the present study, noble metal nanoparticles such as silver and gold were prepared using an aqueous leaf extract of a medicinal plant, Bauhinia purpurea. The leaf extract performed as both reducing and stabilizing agents for the development of nanoparticles. The formations of silver and gold nanoparticles were confirmed by observing the surface plasmon resonance peaks at 430 nm and 560 nm, respectively, in UV-Vis absorption spectrum. Various properties of nanoparticles were demonstrated using the characterization techniques such as FTIR, XRD, TEM, and EDX. The synthesized silver and gold nanoparticles had a momentous anticancer effect against lung carcinoma cell line A549 in a dose-dependent manner with IC50 values of 27.97 µg/mL and 36.39 µg/mL, respectively. The antimicrobial studies of synthesized nanoparticles were carried out by agar well diffusion method against six microbial strains. Silver and gold nanoparticles were also showed high antioxidant potentials with IC50 values of 42.37 µg/mL and 27.21 µg/mL, respectively; it was measured using DPPH assay. Additionally, the nanoparticles were observed to be good catalysts for the reduction of organic dyes.


Assuntos
Anti-Infecciosos/química , Antineoplásicos/química , Antioxidantes/química , Bauhinia/química , Nanopartículas Metálicas/química , Folhas de Planta/química , Células A549 , Catálise , Ouro/química , Química Verde , Humanos , Concentração Inibidora 50 , Tamanho da Partícula , Extratos Vegetais/química , Plantas Medicinais/química , Prata/química , Espectroscopia de Infravermelho com Transformada de Fourier , Ressonância de Plasmônio de Superfície , Difração de Raios X
14.
Pharm Biol ; 57(1): 269-279, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31007116

RESUMO

CONTEXT: Bauhinia L. species, including Bauhinia holophylla (Bong.) Steud. (Fabaceae), have traditionally been used to treat diabetes. Bauhinia is a complex botanical genus, and the indiscriminate use of the diverse Bauhinia species is reflected in the experimental divergence of their medicinal potential. OBJECTIVE: The hypoglycaemic and hypolipidaemic effects, molecular mechanism of action and phytochemical properties of an authentic extract of B. holophylla leaves were evaluated. MATERIALS AND METHODS: A phytochemical study of a 70% EtOH extract was performed using FIA-ESI-IT-MS/MSn and HPLC-PAD-ESI-IT-MS. The extract (200 or 400 mg/kg b.w.) was administered for 14 days to streptozotocin-induced diabetic Swiss mice. Glucose tolerance and insulin sensitivity, blood parameters, gene and protein expression, and the in vivo and in vitro inhibition of intestinal glucosidases were assessed. RESULTS: HPLC-PAD-ESI-IT-MS analysis identified flavonoid derivatives of quercetin, myricetin, luteolin and kaempferol. Treatment with 400 mg/kg of the extract reduced blood glucose (269.0 ± 32.4 mg/dL vs. 468.0 ± 32.2 mg/dL for diabetic animals), improved glucose tolerance, decreased cholesterol and triglyceride levels, and increased the mRNA expression of proteins involved in glucogenesis in the liver and muscle, such as PI3-K/Akt, GS, GSK3-ß (ser-9), AMPK and Glut4. The activity of intestinal maltase was inhibited in vitro (IC50: 43.0 µg/mL for the extract compared to 516.4 µg/mL for acarbose) and in vivo. DISCUSSION AND CONCLUSIONS: Treatment with B. holophylla was associated with a marked hypoglycaemic effect through the stimulation of glycogenesis and inhibition of gluconeogenesis and intestinal glucose absorption, without increasing basal insulinaemia.


Assuntos
Bauhinia/química , Glicemia/biossíntese , Diabetes Mellitus Experimental/tratamento farmacológico , Glicogênio Sintase Quinase 3 beta/antagonistas & inibidores , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Diabetes Mellitus Experimental/sangue , Relação Dose-Resposta a Droga , Hipoglicemiantes/isolamento & purificação , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Estreptozocina
15.
BMC Complement Altern Med ; 18(1): 70, 2018 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-29463252

RESUMO

BACKGROUND: Bauhinia kockiana originates from Peninsular Malaysia and it is grown as a garden ornamental plant. Our previous study reported that this plant exhibited fairly strong antioxidant and antimicrobial activities. This paper focused on the assessment of the antibacterial activity of B. kockiana towards methicillin-resistance Staphylococcus aureus (MRSA), to purify and to identify the antibacterial compounds, and to determine the mechanism of antibacterial activity. METHODS: Antibacterial activity of B. kockiana flower was evaluated qualitatively and quantitatively using disc diffusion assay and microbroth dilution method. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of extracts were examined. Phytochemical analysis was performed to determine the classes of phytochemicals in the extracts. Bioactivity guided isolation was employed to purify the antibacterial agents and identified via various spectroscopy methods. Scanning electron microscopy (SEM) technique was used to evaluate the antibacterial mechanism of extract and compounds isolated. RESULTS: B. kockiana flower was found to exhibit fairly strong antibacterial activity towards both strains of MRSA bacteria used, MIC varies from 62.5-250 µg/mL. Tannins and flavonoids have been detected in the phytochemical analysis. Gallic acid and its ester derivatives purified from ethyl acetate extract could inhibit MRSA at 250-500 µg/mL. SEM revealed that the cells have undergone plasmolysis upon treatment with the extract and compounds. CONCLUSION: Tannins and polyphenols are the antibacterial components towards MRSA in B. kockiana. Massive leakage of the cell content observed in treated cells showed that the phytochemicals have changed the properties of the cell membranes. Amphiphilic nature of the compounds exhibited the antibacterial activity towards MRSA via three stages: (1) cell membrane attachment; (2) cell membrane fluidity modification; and (3) cell membrane structure disruption.


Assuntos
Antibacterianos/farmacologia , Bauhinia/química , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Extratos Vegetais/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Humanos , Staphylococcus aureus Resistente à Meticilina/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Infecções Estafilocócicas/microbiologia
16.
Drug Dev Res ; 79(4): 157-164, 2018 06.
Artigo em Inglês | MEDLINE | ID: mdl-29732583

RESUMO

Hit, Lead & Candidate Discovery The acetic acid-induced writhing and hot plate models in mice were utilized to determine the analgesic effect of epicatechin gallate (ECG) isolated from Bauhinia hookeri. The anti-inflammatory activity of ECG was determined using carrageenan-induced paw edema model. The pro-inflammatory mediators (PGE2 , TNF-α, IL-1ß, and IL-6) were estimated in the plasma of different treatment groups. ECG was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard drug (100 mg/kg) in all experiments. ECG significantly (p < .001) suppressed the writhing response in mice. The inhibition percentages were 32, 52, and 62%, at the tested doses of ECG, respectively as compared to the positive control group receiving acetic acid only. Furthermore, ECG significantly (p < .001) increased the reaction time in hot plate model. The maximum analgesic effect was evident after 120 min. ECG demonstrated a significant anti-inflammatory activity as evidenced by the inhibition of carrageenan-induced paw edema (46, 50, and 58%, at the tested doses, respectively). This effect was persistent all over the experimental period. ECG produced a significant (p < .001) reduction in plasma PGE2 (by 27, 38, and 50%), TNF-α (15, 33, and 41%), IL-1ß (17, 25, and 33%), and IL-6 (22, 32, and 43%), at the tested doses, respectively. This study supports the use of ECG as both analgesic and anti-inflammatory agent.


Assuntos
Anti-Inflamatórios/farmacologia , Bauhinia/química , Catequina/análogos & derivados , Medição da Dor/efeitos dos fármacos , Analgésicos/farmacologia , Animais , Catequina/isolamento & purificação , Catequina/farmacologia , Catequina/toxicidade , Diclofenaco/farmacologia , Dinoprostona/sangue , Relação Dose-Resposta a Droga , Interleucina-1beta/sangue , Interleucina-6/sangue , Masculino , Camundongos , Fator de Necrose Tumoral alfa/sangue
17.
Inflammopharmacology ; 26(2): 539-550, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28176198

RESUMO

The Bauhinia genus is known as "Pata-de-Vaca" and a wide variety of these species are used in Brazilian folk medicine due to their gastroprotective properties. This study aimed to investigate the antiulcer efficacy of the hydroalcoholic extract from B. curvula (HEBC) leaves, as well as its semi-purified fraction (SPFr) and the contribution of their phytochemicals constituents for this effect. For that, ethanol 60%/HCl 0.3 M- and indomethacin-induced gastric ulcer were performed in rodents. Gastric ulcerated tissues were processed for histological, histochemical and biochemical analysis. The oral treatment with HEBC and SPFr decreased the gastric ulcer induced by ethanol/HCl in mice and by indomethacin (only HEBC) in rats. The gastroprotective effect of HEBC was abolished in mice pretreated with Nω-Nitro-L-arginine methyl ester, N-Ethylmaleimide, glibenclamide or indomethacin. Both HEBC and SPFr reduced myeloperoxidase activity in parallel with a decrease of lipoperoxides content at the site of the lesion. On the other hand, HEBC did not alter volume, pH, total acidity or pepsin activity of acid gastric secretion in rats, and neither inhibited the in vitro H(+),K(+)-ATPase activity. Additionally, the compounds identified and isolated from the SPFr, the flavonoids quercitrin (65%) and kaempferol (35%), were able to diminish the extent of ulcerated area induced by both ethanol/HCl and indomethacin. Taking together, these findings show that B. curvula extracts present gastroprotective effect, mainly explained by the presence of flavonoids quercitrin and kaempferol, which may possibly improve the defensive factors of gastric mucosa.


Assuntos
Bauhinia/química , Mucosa Gástrica/efeitos dos fármacos , Quempferóis/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Substâncias Protetoras/farmacologia , Quercetina/análogos & derivados , Animais , Antiulcerosos/farmacologia , Flavonoides/farmacologia , Indometacina/farmacologia , Masculino , Camundongos , Fitoterapia/métodos , Quercetina/farmacologia , Ratos , Ratos Wistar , Roedores , Úlcera Gástrica/tratamento farmacológico
18.
An Acad Bras Cienc ; 89(1): 65-71, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28423074

RESUMO

A new lactone, 7-epi-griffonilide (1), and six known compounds, 2, 3a - 3c, 4a and 4b, were isolated from the leaves of Bauhinia pentandra (Fabaceae). The structures elucidation of 1 and 2 were based on detailed 2D NMR techniques and spectral comparison with related compounds, leading to complete assignment of the 1H and 13C NMR spectra.


Assuntos
Bauhinia/química , Lactonas/química , Lactonas/isolamento & purificação , Folhas de Planta/química , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13/métodos , Estrutura Molecular , Espectroscopia de Prótons por Ressonância Magnética/métodos , Valores de Referência , Estereoisomerismo
19.
An Acad Bras Cienc ; 89(1): 263-272, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28225851

RESUMO

Bauhinia holophylla, commonly known as "cow's hoof", is widely used in Brazilian folk medicine for the diabetes treatment. Therefore, the aim of this study was at evaluating the aqueous extract effect of Bauhinia holophylla leaves treatment on the streptozotocin-induced diabetic rats. Diabetes was induced by Streptozotocin (40 mg/Kg) in female Wistar rats. Oral administration of aqueous extract of Bauhinia holophylla leaves was given to non-diabetic and diabetic rats at a dose of 400 mg/kg during 21 days. On day 17 of treatment, the Oral Glucose Tolerance Test was performed to determine the area under the curve. At the end of the treatment, the animals were anesthetized and blood was collected for serum biochemical parameters analysis. After treatment with Bauhinia holophylla extract, non-diabetic and diabetic rats presented no glycemic changes. On the other hand, the plant treatment decreased body weight and increased ALT and AST activities. In conclusion, the treatment with aqueous extract of B. holophylla leaves given to diabetic rats presented no hypoglycemic effect in nondiabetic animals and no antidiabetic effect in diabetic animals with the doses studied. In addition, the diabetic animals treated with the B. holophylla extract showed inconvenient effects and its indiscriminate consumption requires particular carefulness.


Assuntos
Bauhinia/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Glicemia/análise , Glicemia/efeitos dos fármacos , Peso Corporal , Ingestão de Líquidos , Ingestão de Alimentos , Feminino , Teste de Tolerância a Glucose , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Ratos Wistar , Reprodutibilidade dos Testes , Estreptozocina , Fatores de Tempo , Resultado do Tratamento
20.
Phytother Res ; 31(10): 1521-1528, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28752576

RESUMO

Although Bauhinia forficata Link is popularly used in Brazil to induce diuresis, no scientific investigation has focused on demonstrating its efficacy in preclinical trials. For that, normotensive male Wistar and spontaneously hypertensive rats were used to test the effect of extracts and kaempferitrin obtained from Bauhinia forficata leaves in the experimental model of diuresis. Cumulative urine volume, Na+ and K+ excretion, calcium, creatinine, prostaglandin E2 , pH, density, and conductivity were measured at the end of the experiment (after 8 or 24 h). The treatment with aqueous infusion, methanolic extract, trichloromethane, or ethyl acetate-butanolic fractions significantly increase urinary volume and electrolytes levels when orally given to rats, without altering the pH or density parameters. Kaempferitrin induced diuretic, natriuretic, but not kaliuretic effects in both normotensive and hypertensive rats. In addition, kaempferitrin enhanced urinary creatinine and prostaglandin E2 excretion, without modifying calcium levels. Kaempferitrin-induced diuresis was unaffected by previous treatment with a nonselective inhibitor of nitric oxide synthase and neither with a nonselective muscarinic receptor antagonist. On the other hand, a cyclooxygenase inhibitor was able to decrease its effect when compared with vehicle-treated rats, suggesting that the diuretic and natriuretic properties from kaempferitrin are associated with endogenous prostanoids generation. Copyright © 2017 John Wiley & Sons, Ltd.


Assuntos
Bauhinia/química , Diuréticos/farmacologia , Quempferóis/farmacologia , Natriuréticos/farmacologia , Extratos Vegetais/farmacologia , Prostaglandinas/farmacologia , Animais , Pressão Sanguínea/efeitos dos fármacos , Inibidores de Ciclo-Oxigenase/farmacologia , Hipertensão/tratamento farmacológico , Masculino , Folhas de Planta/química , Ratos , Ratos Endogâmicos SHR , Ratos Wistar
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