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1.
BMC Infect Dis ; 24(1): 22, 2024 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-38166653

RESUMO

BACKGROUND: Dengue fever (DF) is a significant public health concern in Burkina Faso, particularly in the Central Region, previously endemic for malaria. However, limited research has focused on dengue prevalence and associated factors among adult febrile patients in this region. This study aimed to estimate the prevalence of symptomatic dengue fever among adults and identify the sociodemographic and clinical determinants of the disease. METHODS: A seroepidemiological cross-sectional study was conducted in the Central Region of Burkina Faso, through a three-stage sampling. Five health facilities, one from each of the region five districts, were purposively selected. Febrile patients aged 16 and older, suspected of having dengue, were included in the study, after consenting. Bivariate analyses and multivariate binary logistic regression were done at a 5% confidence level. RESULTS: A total of 637 patients between the ages of 16 and 90 years were included. Most of the participants were females (58.71%). Most dengue cases resided in Arrondissement 4 (59.62%), or were present in the Arrondissement 4 at daytime during the previous days (51.92%). 52.90% of the participants knew of dengue. Dengue prevalence was estimated at 8.16% (95% CI: 6.16%-10.57%). The most frequent markers for dengue were immunoglobulins M detected in 4.40% (2.94%-6.29%), followed by Antigen NS1 at 4.24% (95% CI: 2.81%-6.11%). The Antigen NS1 marker was associated with myalgia (p = 0.024), vomiting (p < 0.001), hemorrhagic manifestations (p = 0.001), and anorexia (p < 0.001). Staying at Arrondissement 4 (vs staying at Saaba) during daytime (aOR = 2.36 95% CI: 1.03-5.45; p = 0.044) significantly increased the odds of dengue. Dengue cases were about 3 times more likely to have vomited (aOR = 2.99 95% CI: 1.58-5.64; p = 0.001). Participants knowing of dengue (aOR = 0.53 95% CI: 0.29-0.98; p = 0.042) and those coinfected with malaria (aOR = 0.28 95% CI: 0.14-0.57; p < 0.001) instead had reduced odds of dengue. CONCLUSION: The study revealed a relatively high prevalence of symptomatic dengue fever among adults in the Central Region of Burkina Faso in 2022. These findings emphasize the need for continuous surveillance and targeted control measures. The low coinfection of dengue and malaria warrants further investigation.


Assuntos
Dengue , Malária , Adulto , Feminino , Humanos , Adolescente , Adulto Jovem , Pessoa de Meia-Idade , Idoso , Idoso de 80 Anos ou mais , Masculino , Dengue/epidemiologia , Estudos Transversais , Burkina Faso/epidemiologia , Prevalência , Malária/epidemiologia , Hospitais , Febre/epidemiologia
2.
Artigo em Inglês | MEDLINE | ID: mdl-38777924

RESUMO

BACKGROUND: Respiratory diseases have been associated with the exposure of populations to some environmental pollutants such as pesticides. To assess effects of pesticides on farmers' respiratory health, this study aimed to evaluate the pulmonary function of cotton farmers exposed to synthetic and natural pesticides in the Central-West region of Burkina Faso. METHODS: A cross-sectional study was conducted from June to July 2022 among 281 conventional and 189 organic cotton farmers. After collecting information on pesticide use conditions, pulmonary function tests (PFTs) were performed on each farmer according to the American Thoracic Society/European Respiratory Society guidelines, in order to assess chronic respiratory effects among cotton producers. Binary logistic regression was used to assess factors associated with the occurrence of ventilatory changes. RESULTS: Both conventional and organic cotton farmers reported similar chronic respiratory symptoms in different proportions. The main reported were rhinitis (54.45% conventional vs. 34.92% organic), chest pains (41.28% conventional vs. 23.81% organic), cough (33.45% conventional, 24.34% organic), breathlessness (31.67% conventional, 4.23% organic) (p<0.05). 16.18% and 27.50% of conventional male and female cotton farmers, respectively, had a restrictive defect. Among organic cotton farmers, 15.85% and 18.69%, respectively, of males and females had a restrictive defect. Furthermore, a significant increase in the predicted average percentage of FEV1/FVC ratio was observed among organic cotton farmers after salbutamol's use (p = 0.039). The type of cultivated cotton was not associated with ventilatory changes neither in the univariate analysis, nor in the multivariate analysis. Other factors such as farmers' age, BMI and insecticides use frequency per year were also important. Farmers who used insecticides more than 6 times per season had an increased risk of developing an obstructive defect (OR = 1.603; 95%CI: 0.484-5.309) compared to those who used them 6 times or less. CONCLUSION: Chronic respiratory signs and ventilatory impairments were found among conventional and, to our knowledge, for the first time among organic cotton producers. However, these health effects were more prevalent among conventional cotton farmers than organic ones.

3.
Infect Dis Poverty ; 13(1): 45, 2024 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-38867325

RESUMO

BACKGROUND: In 2023, Burkina Faso experienced the largest dengue epidemic ever in Africa. This study aimed to estimate the prevalence of symptomatic, subclinical, and asymptomatic dengue and determine the associated factors among adult contacts of dengue in the Central Region, Burkina Faso. METHODS: This cross-sectional study included contacts of dengue probable cases through cluster sampling in 2022-2023. These suspected cases that tested positive were identified from the five health facilities (Pissy CMA, Saaba CM, Kossodo CMA, Samandin CM, and Marcoussis CSPS) that reported the highest number of cases in 2021 per district. All participants underwent dengue and malaria rapid diagnostic tests (RDT). Samples positive for non-structural 1 protein antigen (AgNS1) and/or immunoglobulin M (IgM) were tested for serotype detection by reverse transcription polymerase chain reaction (RT-PCR). Binary logistic regression was done to identify the determinants of asymptomatic, subclinical, and symptomatic dengue among contacts of probable dengue cases. RESULTS: A total of 484 contacts were included, mostly in 2023 (75.2%). Most participants were females (58.6%), residing (24.3%) and passing their daytime (23.1%) in Saaba. The overall prevalence of dengue was estimated at 15.1% [95% confidence interval (CI): 12.0-18.6%], representing cases not seeking care in hospitals. Asymptomatic cases represented 2.9% (95% CI: 1.6-4.8%). Subclinical and symptomatic cases accounted for 6.0% (95% CI: 4.1-8.5%) and 6.2% (95% CI: 4.2-8.7%), respectively. Of the 58 samples tested by RT-PCR, 10 were confirmed for serotype 3 in 2023. Malaria cases were estimated at 5.6% (95% CI: 3.7-8.0%). After adjustment, participants claiming that a virus transmits dengue were likelier to have asymptomatic dengue [adjusted odds ratio (aOR) = 7.1, 95% CI: 2.4-21.0]. From the multivariable analysis, subclinical dengue was statistically associated with being included in the study in 2023 (aOR = 30.2, 95% CI: 2.0-455.5) and spending the daytime at Arrondissement 4 (aOR = 11.5, 95% CI: 1.0-131.0). After adjustment, symptomatic dengue was associated with living less than 50 m away from cultivated land (aOR = 2.8, 95% CI: 1.1-6.9) and living less than 50 m from a stretch of water (aOR = 0.1, 95% CI: 0.0-0.6). CONCLUSIONS: The overall burden of dengue among populations not seeking care in hospitals was quite high, with few asymptomatic cases. Efforts to manage dengue cases should also target non-hospital cases and raise population awareness. The 2023 epidemic could be due to dengue virus (DENV)-3.


Assuntos
Dengue , Humanos , Dengue/epidemiologia , Feminino , Masculino , Burkina Faso/epidemiologia , Adulto , Estudos Transversais , Adulto Jovem , Adolescente , Pessoa de Meia-Idade , Prevalência , Vírus da Dengue/isolamento & purificação , Vírus da Dengue/genética , Família , Análise por Conglomerados , Criança , Pré-Escolar
4.
Toxicol Rep ; 11: 273-282, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37771927

RESUMO

Pesticides are chemicals used to control pests with sometime harmful effects on human health. This paper presents results of self-reported health effects experienced by cotton farmers in the Central-West region of Burkina Faso. It was a cross-sectional survey conducted from October to December 2021 among 585 consenting conventional and organic cotton farmers. Data collected included pesticides used, they use conditions, farming practices, experienced health effects. Binary logistic regression was used to find relationships between self-reported health effects and the type of cotton produced. Results showed that all conventional cotton farmers (100%) reported using synthetic pesticides compared to organic ones who using only natural insecticides. Both conventional and organic farmers reported health effects that occurred at least once since they started using pesticides, involving skin effects (85.27% conventional, 65.52% organic), nervous (88.95% conventional, 48,71% organic), respiratory (88.10% conventional, 67.67% organic) systems. 99.72% of conventional farmers vs 46.98% of organic ones reported skin irritation following pesticide use. 69.97% of conventional vs 35.34% of organic cotton farmers reported acute signs such as severe headaches. In univariate and multivariate logistic regressions, severe headaches, dizziness, skin, and ocular effects were significantly associated with conventional farmers compared to organic ones (p < 0.05). There was a significant relationship between vomiting (p = 0.014), diarrhea (p = 0.003) and experience in synthetic pesticide use among conventional farmers. Among organic farmers, there was no significant relationship between health effects reported and experience in organic insecticides use. there was a significant relationship between severe headaches (p = 0.01), rhinitis (p = 0.006), cough (p = 0.0001), skin and ocular irritations (p = 0.007) and the frequency of synthetic insecticides use per year by conventional farmers. Study showed that conventional and organic cotton producers experience the same types of health effects. However, these health effects were significantly associated with conventional farmers compared to organic ones.

5.
Trop Med Infect Dis ; 7(9)2022 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-36136625

RESUMO

This study aims to evaluate the factors influencing the adherence to the 2nd and 3rd doses of Amodiaquine (AQ) during seasonal malaria chemoprevention (SMC) in Burkina Faso, Mali, and Niger. Overall, 3132 people were interviewed during surveys between 2019 and 2020 in 15 health districts. In Burkina Faso, Mali, and Niger, the proportions of non-adherence were 4.15%, 5.60%, and 13.30%, respectively, for the 2nd dose and 3.98%, 5.60% and 14.39% for the 3rd dose. The main cause of non-adherence to the 2nd and 3rd doses was other illnesses in 28.5% and 29.78%, respectively, in Burkina Faso, 5.35% and 5.35% in Mali and 1.6% and 0.75% in Niger. It was followed by vomiting in 12.24% and 10.63% for Burkina and 2.45% and 3.78% in Niger. The last cause was refusal in 6.12% and 4.25% in Burkina, 33.9% and 15.25% in Mali and 0.8% and 1.51% in Niger. Non-adherence of doses related to parents was primarily due to their absence in 28.5% and 27.65% in Burkina, 16.07% and 16.07% in Mali and 7.37% and 6.06% in Niger. Traveling was the second cause related to parents in 12.24% and 12.76% in Burkina, 19.64% and 19.64% in Mali and 0.81% and 0.75% in Niger. Non-adherence related to community distributors was mainly due to missing the doses in 4.08% and 4.25% in Burkina, 23.21% and 23.21% in Mali, 77.04% and 76.51% in Niger. Our study reported very small proportions of non-adherence to 2nd and 3rd doses of SMC and identified the main causes of non-adherence. These findings will provide helpful information for policymakers and public health authorities to improve adherence to SMC.

6.
J Exp Pharmacol ; 13: 739-754, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34393522

RESUMO

BACKGROUND: The present study investigates the effect of an aqueous extract of Anogeissus leiocarpa (AEAL) on normotensive Wistar rats and its chronic antihypertensive effects in L-NAME-induced hypertensive rats by using a non-invasive tail-cuff model. METHODS: The effects of AEAL (50mg/kg) and NaCl 0.9% on blood pressure were investigated by daily oral administration in normotensive Wistar rats over four weeks. L-NAME-induced hypertensive rats were produced by L-NAME (40mg/kg) daily oral administration for two weeks. For chronic antihypertensive effects, induced hypertensive rats have received L-NAME in combination with AEAL (10 or 50mg/kg/day) for two following weeks. RESULTS: In normotensive rats, daily administration of AEAL (50mg/kg) has no significant effect on their blood pressure, which was similar to that of the control group. L-NAME's daily oral administration induces a progressive increase in systolic blood pressure (SBP) from 115.8 ± 7.9mmHg to 153.5 ± 4.6mmHg after two weeks, which was maintained to the end of the treatment. In L-NAME-induced hypertensive rats, AEAL (50mg/kg/day) significantly decreases the SPB from 160.0 ± 5.8 mmHg to 108.8 ± 2.7mmHg after only four days of administration. However, the lower dose of AEAL (10mg/kg) also normalized the SBP of L-NAME-induced hypertensive rats but only evident after seven days of administration. Moreover, AEAL does not effect on the serum biochemical parameters (ALAT, ASAT, CREAT, etc.) and any macroscopic adverse effect was detected on the sensible organs involved during hypertension. In the aorta rings from treated rats, AEAL (50mg/kg/day) alone or in combination with L-NAME has enhanced the vasodilation effect of acetylcholine. However, the vasodilation effect of AEAL alone or in association with L-NAME has enhanced the sodium nitroprusside effect in treated rat aorta rings after autopsy. CONCLUSION: These findings suggest that AEAL affords significant antihypertensive effects against L-NAME-induced hypertensive rats without modification of serum parameters and deleterious effects.

7.
Artigo em Inglês | MEDLINE | ID: mdl-33995545

RESUMO

Waltheria indica L. (Malvaceae) is a plant used in Burkina Faso for the treatment of various ailments including asthma. The aim of the study was to evaluate the pharmacological relaxant effect of the leafy stem extracts of Waltheria indica and thereby verify claim of use in treating asthma. Aqueous decoction and hydroalcoholic extracts obtained from the powdered leafy stems were screened for the presence of some phytoconstituents. The in vitro relaxant effect of the two extracts was evaluated on acetylcholine- (ACh 10-5 M) and potassium chloride- (KCl 6 × 10-2 M) induced contractions on rat-isolated tracheal preparations. To examine whether the potassium (K+) channels are involved in the relaxant effect, glibenclamide, an ATP-sensitive potassium channel inhibitor, was used. Moreover, to assess the safety of the extracts, acute oral toxicity was carried out on mice. The phytochemical screening revealed the presence of alkaloids, flavonoids, saponins, steroids, triterpenoids, tannins, and coumarins in the hydroalcoholic extract. Tannins, steroids, triterpenoids, and coumarins were not detected in the aqueous decoction. With respective EC50 values of 1.517 ± 0.002 mg/mL and 1.433 ± 0.001 mg/mL on ACh-and KCl-provoked contractions, the hydroalcoholic extract was found more potent in relaxing the isolated rat tracheal preparations compared to the aqueous decoction. In the presence of glibenclamide, the relaxant effect of the hydroalcoholic extract (EC50 = 0.191 ± 0.002 mg/mL) increased and was higher than that of the aqueous decoction. At dose of 5000 mg/kg of body weight, the extracts did not produce deaths or any significant changes in the general behavior of mice. The results suggest that different mechanisms including modulation of calcium and potassium channels, particularly the ATP-sensitive K+ channels, could be involved in the relaxation effect. These findings could justify the traditional use of W. indica in the management of asthma.

8.
Oxid Med Cell Longev ; 2019: 9464608, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31183001

RESUMO

Traditional remedies prepared from Lannea microcarpa leaves, barks, roots, and fruits are used to treat many diseases including hypertension. This study investigated whether oral administration of the ethyl acetate fraction of Lannea microcarpa trunk barks (LMAE) corrects angiotensin (Ang) II-induced hypertension in mice. Its effects on vascular function were specifically investigated. Experiments explored hemodynamic and echocardiographic parameters in vivo and vascular reactivity to acetylcholine (ACh) and CaCl2 ex vivo on isolated aortas. Mice received LMAE for 3 weeks (50 mg/kg/day) by oral gavage. In the last two weeks of treatment, mice were implanted with osmotic minipumps delivering NaCl (0.9%) or Ang II (0.5 mg/kg/day). LMAE completely prevented the increase in systolic and diastolic blood pressure induced by Ang II. Echocardiographic and kidney parameters were not affected by the different conditions. LMAE abrogated Ang II-induced impairment of ACh-induced relaxation without affecting that of sodium nitroprusside. LMAE also completely prevented CaCl2-induced contraction in KCl-exposed aorta ex vivo. The extract alone did not modify superoxide (O2 -) and nitric oxide (NO·) production in femoral arteries from control mice but significantly limited Ang II-induced O2 - production. These effects were associated with reduced expression of inducible isoform of cyclooxygenase- (COX-) 2 and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase isoform NOX-2 in aortas. Finally, phytochemical analysis showed that LMAE contains sterols, triterpenes, coumarins, and anthraquinone. These results showed that LMAE prevents Ang II-induced hypertension and vascular dysfunction through a reduction of oxidative stress linked to COX-2 and NOX-2 pathway and inhibition of calcium entry. This study provides pharmacological basis of the empirical use of Lannea microcarpa trunk bark extract against hypertension.


Assuntos
Acetatos/química , Anacardiaceae/química , Angiotensina II/farmacologia , Hipertensão/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Animais , Pressão Sanguínea/efeitos dos fármacos , Hipertensão/induzido quimicamente , Camundongos , NADP/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Prostaglandina-Endoperóxido Sintases/metabolismo , Superóxidos/metabolismo
9.
J Basic Clin Physiol Pharmacol ; 29(6): 599-608, 2018 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-29723154

RESUMO

BACKGROUND: Anogeissus leiocarpus is a Sahel tree traditionally used by the residents of Burkina Faso for its antihypertensive properties. In this study, experiments were conducted to evaluate whether an aqueous extract of the Anogeissus leiocarpus (AEAL) trunk bark induces a vasorelaxant effect on porcine coronary artery rings and to investigate the underlying mechanism. METHODS: AEAL-induced relaxations were assessed using porcine coronary artery rings suspended in organ chambers. The phosphorylation levels of Src, Akt and endothelial nitric oxide synthase (eNOS) were assessed in a primary endothelial cell culture by Western blot. The reactive oxygen species (ROS) formation was assessed using dihydroethidine. RESULTS: In porcine coronary artery rings, AEAL at 0.1-300 µg/mL induced endothelium-dependent relaxations, which were inhibited in the presence of inhibitors of nitric oxide (NO) and the endothelium-derived hyperpolarization pathways. Moreover, the AEAL-induced NO-mediated relaxations were significantly reduced by the inhibitors of Src and PI3-kinase as well as by the membrane-permeant ROS scavengers. In cultured porcine coronary artery endothelial cells, treatment with AEAL is associated with an intracellular generation of ROS. Moreover, the AEAL induced the phosphorylations of Akt (Ser473), eNOS (Ser1177) and a transient phosphorylation of Src (Ser17) in a time-dependent manner. CONCLUSIONS: These findings indicate that AEAL is a potent inducer of endothelium-dependent NO-mediated relaxations in porcine coronary arteries through the redox-sensitive Src/PI3-kinase/Akt pathway-dependent activation of eNOS.


Assuntos
Combretaceae/química , Vasos Coronários/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Burkina Faso , Células Cultivadas , Vasos Coronários/metabolismo , Relação Dose-Resposta a Droga , Endotélio Vascular/metabolismo , Medicinas Tradicionais Africanas , Óxido Nítrico/metabolismo , Oxirredução , Fosfatidilinositol 3-Quinases/metabolismo , Fosforilação/efeitos dos fármacos , Casca de Planta , Extratos Vegetais/administração & dosagem , Proteínas Proto-Oncogênicas c-akt/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Suínos , Fatores de Tempo , Vasodilatação/efeitos dos fármacos , Quinases da Família src/metabolismo
10.
J Ethnopharmacol ; 93(2-3): 345-50, 2004 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-15234775

RESUMO

Aqueous extracts of Mitragyna inermis (AEMI) used traditionally as antihypertensive agents produced a concentration-dependent (0.1-3 mg/ml) ex vivo increase in cardiac contractile response and coronary flow but did not modify heart rate in the rat. Interestingly, AEMI produced relaxation in isolated porcine coronary artery at concentration up to 3 mg/ml that was exclusively dependent on the presence of endothelium. This relaxation involved partial depolarization (KCl 20, 40 mM) and NO synthase inhibitor-sensitive mechanisms but was not sensitive to the blockade of cyclo-oxygenase pathway. In contrast, the relaxant effect of AEMI was not dependent on the presence of endothelium in rat tail artery. Taken together, the present study demonstrates hypotensive, cardiotropic and vasodilatory properties of AEMI that contribute to better understanding of its beneficial effect against cardiovascular diseases.


Assuntos
Vasos Coronários/fisiologia , Mitragyna , Fitoterapia , Extratos Vegetais/farmacologia , Animais , Anti-Hipertensivos/administração & dosagem , Anti-Hipertensivos/farmacologia , Anti-Hipertensivos/uso terapêutico , Artérias/efeitos dos fármacos , Artérias/fisiologia , Cardiotônicos/administração & dosagem , Cardiotônicos/farmacologia , Cardiotônicos/uso terapêutico , Circulação Coronária , Vasos Coronários/efeitos dos fármacos , Relação Dose-Resposta a Droga , Masculino , Casca de Planta , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Suínos , Vasodilatação/efeitos dos fármacos , Vasodilatação/fisiologia , Vasodilatadores/administração & dosagem , Vasodilatadores/farmacologia , Vasodilatadores/uso terapêutico
11.
Pak J Biol Sci ; 17(6): 829-35, 2014 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-26035956

RESUMO

The leaves of Ficus sycomorus are used in Burkina Faso folk medicine for the treatment of sickle cell disease. The present comparative study of crude extracts of leaves (decoction, macerated extract and a 95% ethanol extract) was performed with the aim to assess the efficiency of this traditional use and to determine the most active of the three extracts. Antisickling activity was assessed by the Emmel's test. Vasorelaxant effect on rat aortic rings precontracted by phenylephrine with and without N-nitro-L-arginine methyl ester chloride (L-NAME) was also evaluated. The 95% ethanol extract (20 mg mL(-1)) showed the most antisickling activity on sickle erythrocytes, by inhibiting completely sickling of double heterozygote SC cells in 60 min and that of homozygote SS cells in 90 min. On the aorta this extract exhibited a significant (p<0.05) vasorelaxant activity, better than that of the other extracts, with an IC50 value of 6.86±0.13 mg mL(-1) against 18.78±0.38 and 28.56±1.27 mg mL(-1), respectively for the macerated extract and the decoction. When the aortic rings were pretreated with L-NAME, only the ethanolic extract conserved its vasorelaxant activity, up to 73% of relaxation. The acute toxicity of the decoction, assessed by intraperitoneal route and using the Litchfield and Wilcoxon method, led to an LD50 value of 1553.61 mg kg(-1) b.wt. This places the drug among those with low toxicity according to the WHO scale. These results confirm those previously obtained and provide a scientific basis supporting the use of this plant in folk medicine against sickle cell disease. They indicate the importance of Ficus sycomorus in the research of new antisickling molecules.


Assuntos
Anemia Falciforme/tratamento farmacológico , Moraceae/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Vasodilatação/efeitos dos fármacos , Adolescente , Animais , Criança , Pré-Escolar , Humanos , Concentração Inibidora 50 , Extratos Vegetais/uso terapêutico , Extratos Vegetais/toxicidade , Ratos , Ratos Wistar
12.
Artigo em Inglês | MEDLINE | ID: mdl-24146440

RESUMO

Many traditional medicinal herbs from Burkina Faso are used to treat arterial hypertension (HTA). Among them, Anogeissus leiocarpus (A. Leiocarpus) which is well known and widely used in Burkina traditional medicine. Herein we assess the effects of dichloromethane fraction from A. leiocarpus stem bark (ALF), selected as the most active on cyclic nucleotide phosphodiesterases (PDEs) and characterized its specificity towards purified vascular PDE1 to PDE5 isoenzymes and study its effects on a vascular model. ALF potently and preferentially inhibits (IC50=1.6 ± 0.6 µg/mL) the calmodulin-dependent phosphodiesterase PDE1, being mainly present in vascular smooth muscle and preferentially hydrolyses cGMP. In the same range (IC50 =2.8 ± 0.2 µg/ml) ALF inhibits PDE2, a cGMP-activated enzyme that is only present in endothelial cells and hydrolyses both cAMP and cGMP. PDE5, which specifically hydrolyses cGMP and which mainly contributes to cGMP hydrolysis is also potently inhibited by ALF (IC50=7.6 ± 3.5 µg/ml). The potencies of ALF on cAMP hydrolyzing isoenzymes was lesser, being more effective on PDE4 (IC50= 17.6 ± 3.5 µg/ml) than on PDE3 (60.9 ± 1.8 µg/ml). Since the major effect of ALF were against cGMP hydrolysis and since cGMP is implicated in endothelium-dependent relaxation, the endothelium-dependent vasorelaxation was studied on isolated porcine coronary arteries rings pre-contracted with U46619. The endothelium-dependent vasorelaxation is significantly inhibited by N(ω)-nitro-L-arginine (LNA 300 µmol/L, an inhibitor of endothelial NO synthase), but not affected by charybdotoxin (CTX, 100 nM) plus apamin (APA, 100 nM) (two inhibitors of EDHF-mediated responses). The combination of 4-aminopyridine (4-AP, 1 mmol/L, inhibitor of voltage-dependent potassium channels, Kv) plus baryum (Ba(2+), 30 µmol/L, inhibitor of the potassium channels with entering correction, Kir) plus ouabain (3 µmol/L, inhibitor of ATPase Na(+)/K(+) channels) partially inhibits endothelium-independent vasorelaxant effect. This endothelium-independent relaxant effect was also sensitive to combination of 1H-[1,2,4]-oxadiazole-[4,3-α]-quinoxalin1-one (ODQ, 10 µM, soluble guanylyl cyclase inhibitor) and N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinoline sulfonamide dihydrochloride (H89, 100 nM, Protein Kinase A inhibitor). Taken together, these results indicate that ALF is a powerful vasodilator modulated by the formation of NO from endothelium, but also act by directly relaxing the vascular smooth muscle cells, by inhibiting cGMP hydrolyzing PDEs (PDE1, PDE2 and PDE5) and to a lesser extend on cAMP degradation (PDE3 and PDE4), cAMP and cGMP being second messengers involved in vascular relaxation.


Assuntos
3',5'-AMP Cíclico Fosfodiesterases/antagonistas & inibidores , Combretaceae , Endotélio Vascular/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Extratos Vegetais/farmacologia , Vasodilatação/efeitos dos fármacos , Vasodilatadores/farmacologia , Animais , Bovinos , GMP Cíclico/metabolismo , Endotélio Vascular/metabolismo , Feminino , Humanos , Masculino , Músculo Liso Vascular/metabolismo , Inibidores de Fosfodiesterase/farmacologia , Suínos
13.
Artigo em Inglês | MEDLINE | ID: mdl-23983339

RESUMO

The spasmolytic properties of the aqueous extract of Aframomum melegueta (K Schum) and Citrus aurantifolia (Christm and Panzer) (AMCA) mixture were tested on isolated rat trachea. Inhibition of the contraction was observed the in presence of the AMCA (EC 50 = 1.80 ± 0.48 mg/mL) after a pre contraction of the trachea by acetylcholine (10⁻5 M). With propranolol (10⁻6 M), the spasmolytic activity of the mixture was inhibited and the concentration-response curve shifted to the right. The EC50 value was then 2.60 ± 0.41 mg/mL. AMCA also inhibited contraction induced by KCl (4.10⁻² M) with EC50 value = 1.86 ± 0.65 mg/mL. These results clearly show the relaxing effect of the aqueous extract on the isolated rat trachea. This effect involved some ß-adrenergic receptor inhibition.


Assuntos
Citrus , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Extratos Vegetais/farmacologia , Traqueia/efeitos dos fármacos , Zingiberaceae , Acetilcolina , Antagonistas Adrenérgicos beta/farmacologia , Animais , Masculino , Cloreto de Potássio , Propranolol , Ratos , Ratos Wistar
14.
Artigo em Inglês | MEDLINE | ID: mdl-23983344

RESUMO

The authors report here the results of study on Parkia biglobosa seeds used in Burkina Faso for arterial hypertension treatment. Investigations were done on acute toxicity and vascular properties of fermented and roasted seeds. Acute toxicity test using mice, revealed by the intraperitoneal route a lethal dose 50 (LD50) of 1800 mg/kg and 1600 mg/kg of body weight for aqueous extract from roasted and fermented seeds respectively. According to the scale of Hodge and Sterner and that of the World Health Organization, such drugs would be classified lightly toxic. Oral administration (up to 3000 mg/kg) did not induce any death of animal. For the vascular properties, the effects of these products were tested on the aorta isolated from rats. The cumulative administration of extract from roasted and fermented seeds (0.1-10 mg/mL) in an organ bath induced a concentration-dependent relaxation of the aorta pre contracted by phenylephrine, with or without functional endothelium. The extracts (10 mg/mL) inhibited for 100% the contraction induced by phenylephrine. The EC50 values in presence and absence of endothelium were respectively of 5.37 ± 0.12 and 4.19 ± 1.02 mg/mL for fermented seeds; for roasted seeds these values were respectively, 5.39 ± 1.12 and 5.93 ± 0.95 mg/mL. Nevertheless, low concentration of roasted seeds (1-4 mg/mL) induced endothelium-dependent relaxation and this effect was inhibited by indomethacin (10⁻5M), and not by L-NAME (310⁻4M). These experimental results revealed a vasorelaxant effect of P. biglobosa seeds. P. biglobosa seems to act directly on the smooth muscle and via endothelium involving the generation of vasodilatating prostaglandins. This vasodilator effect would be in favor of an anti hypertensive property of P. biglobosa seeds.


Assuntos
Anti-Hipertensivos/farmacologia , Aorta/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Fabaceae , Músculo Liso Vascular/efeitos dos fármacos , Preparações de Plantas/farmacologia , Vasoconstrição/efeitos dos fármacos , Vasodilatadores/farmacologia , Animais , Anti-Hipertensivos/uso terapêutico , Burkina Faso , Relação Dose-Resposta a Droga , Hipertensão/tratamento farmacológico , Indometacina/farmacologia , Dose Letal Mediana , NG-Nitroarginina Metil Éster/farmacologia , Fenilefrina , Fitoterapia , Preparações de Plantas/uso terapêutico , Prostaglandinas/metabolismo , Ratos , Ratos Wistar , Sementes , Vasodilatadores/uso terapêutico
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