Objective:To determine the anticancer potential of the methanolic extract from Ephedra alata against breast cancer both in vitro and in vivo.Methods:The effects of the methanolic extract of Ephedra alata on the viabil...Objective:To determine the anticancer potential of the methanolic extract from Ephedra alata against breast cancer both in vitro and in vivo.Methods:The effects of the methanolic extract of Ephedra alata on the viability,migration as well as apoptosis of breast cancer 4T1 cells were measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay,Transwell assay,and annexin V-FITC staining assay,respectively.Histological examination was also carried out.Moreover,a murine breast cancer model was established to evaluate the inhibitory effect of the extract.Biochemical parameters including hepatic and non-hepatic enzymes,malondialdehyde,and glutathione were investigated.Results:The methanolic extract of Ephedra alata showed a strong anti-proliferative and anti-migratory activity against 4T1 cells in a dose-dependent manner.It also induced apoptosis in 4T1 cells.In an in vivo mouse model,the extract markedly inhibited tumor growth,reduced malondialdehyde,and hepatic and non-hepatic enzymes as well as increased glutathione level.Conclusions:The methanolic extract of Ephedra alata inhibits breast cancer in vitro and in vivo,which may be a promising anticancer agent.展开更多
The heavy use of chemicals, pesticides, cosmetics and plastic packaging coincides with a resurgence of cardiovascular disease, in particular hypertension, which is affecting younger and younger populations. The aim of...The heavy use of chemicals, pesticides, cosmetics and plastic packaging coincides with a resurgence of cardiovascular disease, in particular hypertension, which is affecting younger and younger populations. The aim of this study was to analyze the cardiovascular risk factors in hypertensive farmers compared with hypertensive non farmers. This was a prospective case-control study that included 239 hypertensive farmers and non farmers aged 25 to 65 with blood pressure ≥ 140 mmHg and 90 mmHg. Hypertensive farmers (101) represented 42.25% of the population versus hypertensive non farmers (138) 57.74%. The median ages were 47 ± 11.3 years for farmers and 51.45 ± 9.77 years for non farmers. Biochemical analysisand screening for major cardiovascular disease risk factors such as metabolic syndrome were performed. Metabolic syndrome was defined according to the new definition of the International Diabetes Federation. Our results revealed higher blood glucose levels in farmers (47.77%) than in non farmers (27.20%) (p = 0.0132). Dyslipidemia was more frequent in non farmerswith high level of LDL cholesterol and total cholesterol. Farmers presented a high level of tryglycerides. The prevalence of obesity was higher in non farmers 51 (36.96%) than farmers 18 (17.82%). The prevalence of metabolic syndrome was 106 (44.35%) in our study population. There was not an important difference between farmers (39.60%) and non farmers (47.82%). However, the variation of metabolic syndrome according to age and sex showed a higher prevalence in young male farmers aged 25 to 45 whereas non farmers presented an increasing prevalence of metabolic syndrome according to age and the absence of metabolic syndrome between age 25 and 35. Our results showed that the cardiovascular risk appeared early in young farmers compared with non farmers suggesting a possible role of pesticides in the onset of this risk.展开更多
The apparent degradation rate constant of fluticasone propionate(FLT) in 0.1 M NaOH:methanol=1:1 at 37 °C was previously reported to be 0.169 ± 0.003 h^(-1), and four degradation products(products 1–4) were...The apparent degradation rate constant of fluticasone propionate(FLT) in 0.1 M NaOH:methanol=1:1 at 37 °C was previously reported to be 0.169 ± 0.003 h^(-1), and four degradation products(products 1–4) were observed in the solution. The aims of the present study were to assess the degradation rates of FLT in other alkaline solutions and clarify the chemical structures of the four degradation products in order to obtain basic data for designing an enema for inflammatory bowel disease. The apparent degradation rate constants in 0.05 M NaOH and 0.1 M NaOH:CH_3CN=1:1 were 0.472 ± 0.013 h^(-1) and 0.154 ± 0.000 h^(-1)(n=3), respectively. The chemical structures of products 1–4 in 0.1 M NaOH:methanol=1:1 were revealed by nuclear magnetic resonance(NMR)and mass spectrometry data. The chemical structure of products 2 was that the 17-position of the thioester moiety of FLT was substituted by a carboxylic acid. The degradation product in 0.1 M NaOH:CH_3CN=1:1 was found to be product 2 based on ~1H NMR data. The degradation product in 0.05 M NaOH was considered to be product 2 based on the retention time of HPLC. These results are useful for detecting the degradation products of FLT by enzymes of the intestinal bacterial flora in the large intestine after dosing FLT as an enema.展开更多
Objective:To improve the knowledge on the metabolite profile of five red grapes from D?o region(Portugal),concerning to the phenolic characteristics(coloured and non-coloured phenolics) and organic acid composition.Me...Objective:To improve the knowledge on the metabolite profile of five red grapes from D?o region(Portugal),concerning to the phenolic characteristics(coloured and non-coloured phenolics) and organic acid composition.Methods:Five red grapes collected from D?o region were studied.The profiles of phenolic compounds and organic acids were estimated by high-performance liquid chromatography with diode-array detection and high-performance liquid chromatography with UV detector,respectively.Results:Totally 24 phenolic compounds were identified,and distributed by several classes:8 anthocyanins,1 hydroxybenzoic acid,4 hydroxycinnamic acids,1 stilbene,4flavan-3-ols,6 flavonols.Additionally,10 organic acids were detected in all samples.Total contents of each phenolic class and organic acids amounts varied significantly among the different grape cultivars investigated.The principal components analysis differentiates the Touriga Nacional from the other varieties due to their high contents in anthocyanins,non-coloured phenolics and organic acids.Touriga Nacional is an important red grape cultivar,highly esteemed in D?o region for its ability to produce high quality wines.Conclusions:The results suggest that the red grapes from D?o region present a good composition in bioactive compounds,being important for the production of wines with superior quality.展开更多
Vegetables are very important sources of protein and minerals. Some of them even have medicinal properties recognized traditionally. Despite the large number of studies carried out on various vegetables and vegetable ...Vegetables are very important sources of protein and minerals. Some of them even have medicinal properties recognized traditionally. Despite the large number of studies carried out on various vegetables and vegetable crops, very few have scientifically explored the usefulness of S. macrocarpon. This study identified the main groups of chemicals and mineral elements to explain any medicinal or nutritional value. It has also identified some toxic elements contained in this vegetable. Phytochemical screening was carried out on the leaves and fruits of S. macrocarpon. Some mineral elements were determined by Atomic Absorption Spectrophotometry (sodium, potassium, calcium, magnesium) while protein, phosphorous, iron, copper, zinc and toxic metals (lead, cadmium) were determined by Molecular Absorption Spectrophotometry. Fat, ash, moisture and vitamins were sought. The study showed that the leaves of S. macrocarpon were more nutritious than fruits (P macrocarpon require that the consumption of vegetables should be as varied as possible and that the fruit may be consumed with caution. In addition, constraints about vegetable cultivation in Cotonou could lead to research findings that could help provide techniques for producing healthy vegetables.Vitamins A and K1 were found in both parts of this vegetable very rich in water while vitamin E has not been detected. S. macrocarpon also contains lipids at various levels.展开更多
In order to combat the counterfeiting of drugs, adapted HPLC analytical USP methods were applied to evaluate the quality of the amoxicillin (with or without potassium clavulanate) powder for suspension sold in some Co...In order to combat the counterfeiting of drugs, adapted HPLC analytical USP methods were applied to evaluate the quality of the amoxicillin (with or without potassium clavulanate) powder for suspension sold in some Congolese markets. The adaptation has been done by modifying the column dimensions and adjusting the flow rate. According to the intended deployment of these methods in Democratic Republic of Congo (DRC), 3 factors (analyst, day and equipment) were involved in the validation step while applying the classic total error measurement approach with an accuracy profile as decision tool. Since adequate results were obtained in terms of selectivity, precision, trueness and accuracy (tolerance limits of life expectancy: ?6.0% and 3.8%) for levels of interest concentration, the methods have been considered for routine use on several samples from different provenances and collected in 4 major DRC cities. Out of 278 samples collected, 200 were eligible for analysis from which 28% were found under standards with several figures: pH failure, out of specification for amoxicillin content, absence of potassium clavulanate, physical modifications of the powders. As evidenced by these findings, medicines of low-quality continue to be a major public health problem requiring appropriate action to effectively address this problem.展开更多
Pharmaceutical counterfeiting is a health scourge responsible for several cases of morbidity and mortality. Counterfeit medicines cause therapeutic failure, emergence of resistance in the treatment of infections. This...Pharmaceutical counterfeiting is a health scourge responsible for several cases of morbidity and mortality. Counterfeit medicines cause therapeutic failure, emergence of resistance in the treatment of infections. This study was conducted in order to identify counterfeit and authentic medicines in circulation in Lubumbashi. The study included artemether and artesunate for oral administration. A careful visual inspection of medicine, investigation of authenticity of pharmaceutical products from manufacturers and pharmaceutical regulatory authorities and determination of content were used as study parameters. 52 samples: 37 artemether and 15 of artésunate were collected. 7 samples (13%) have proven to be counterfeit. Artemether was the most counterfeit (71%) and 29% for artesunate. 6 (12%) samples were substandard according to the international pharmacopoeia in terms of content of active ingredient. Sixty-seven percent of non-compliance concerned counterfeit medicines. The proportion of non-compliance is highest among counterfeit medicines (71.43% vs 2.22%;p = 0.000004). It is obvious that strengthening the capacity of the drug regulatory authority of the DRC reduces the influx of counterfeit drug and substandard.展开更多
Algae(and their extracts)are increasingly important for pharmaceutical applications due to the diversity of useful compounds they contain.The genus Fucus contains one of the most studied species,Fucus vesiculosus.The ...Algae(and their extracts)are increasingly important for pharmaceutical applications due to the diversity of useful compounds they contain.The genus Fucus contains one of the most studied species,Fucus vesiculosus.The species F.ceranoides differs from the others of the genus by presenting longitudinal air-vesicles and a capacity to survive at low salinities.It is an alga that inhabits the Mondego River estuary(Portugal),at the southern limit of its distribution,and can serve as a role model to understand the effect of a salt gradient on the production of bioactive compounds.We assessed the phenolic content and antioxidant activity of different F.ceranoides extracts(e.g.methanolic,aqueous and polysaccharide)prepared from samples harvested from two different zones to evaluate if the adaptation of F.ceranoides to different salinity levels influenced its chemical composition.The antioxidant activity of the extracts was determined using 1,2-diphenyl-picrylhydrazyl(DPPH)and 2.2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS)radicals.These assays demonstrated that the methanolic extract of lyophilized F.ceranoides that grew at low salinities was the most bioactive,i.e.DPPH(IC 50=50.39μg/mL)and ABTS(TEAC=2.42).The total phenolic content(Folin-Ciocalteu method)and the methanolic extract of the lyophilized F.ceranoides collected from a low salinity habitat exhibited the highest phenolic content(PGE=49.48μg/mg of lyophilized extract)amongst those sampled.Thin layer chromatography(TLC)and Fourier transform infrared spectroscopy(FTIR)were used for the identification of compounds in the extracts.This characterization allowed confirmation that the various extracts contained almost the same compounds but with notable quantitative differences.Based on these results,we conclude that there were differences in the quantity of the compounds due to the effect of salinity.The drying methods used were also found to have influenced the quality of the extracted compounds.展开更多
Justicia secunda, Sorghum bicolor, Gossypiun barbadense and Hibiscus sabdariffa are dye plants traditionally used in Benin for the treatment of anemia. This work is part of the therapeutic valorization of dyes from th...Justicia secunda, Sorghum bicolor, Gossypiun barbadense and Hibiscus sabdariffa are dye plants traditionally used in Benin for the treatment of anemia. This work is part of the therapeutic valorization of dyes from these plants. Its objective is to characterize their composition in chemical groups and evaluate their harmlessness and their anti-anaemic property in laboratory rats. Anemia was induced in Wistar rats by phenylhydrazine hydrochloride followed by treatment by gavage with hydroethanolic extracts of the plants studied. Phytochemical screening of these extracts made it possible to characterize the major chemical groups, in particular alkaloids, polyphenols including tannins, flavonoids and leucoanthocyanins, as well as reducing compounds and saponosides in the plants studied. Cytotoxic analysis of these extracts on Artemia salina shrimp larvae revealed globally high LC<sub>50</sub> values of between 3.14 and 4.64 mg/mL, which testify a priori to the harmlessness of these extracts. The administration of the hydroethanolic extract of each plant to anaemic rats at doses of 2000 mg/kg/d promoted, after 15 days, an increase in hemoglobin levels, the number of red blood cells and hematocrit, going to more than 90% recovery of the hematological parameters involved. The highest rate, 99.06% being that of the species Justicia secunda followed closely by Sorghum bicolor (96.80%) compared to 93.93% obtained by treatment with the Ranferon-12 positive control used. Indeed, these results confirm the therapeutic indication of these plants in the resorption of anemia in traditional medicine.展开更多
Methanolic extracts from the leaves of <em>Manihot esculenta </em>(Two cultivars) and <em>Manihot glaziovii</em>, consumed as traditional vegetables in DR. Congo was chemically characterized by...Methanolic extracts from the leaves of <em>Manihot esculenta </em>(Two cultivars) and <em>Manihot glaziovii</em>, consumed as traditional vegetables in DR. Congo was chemically characterized by Thin layer Chromatography and High Performance Liquid Chromatography. <em>In vitro</em> biochemical activities of extracts against Radical Oxidative Species (ROS) production were assessed in cellular models, on enzymes, Myeloperoxidase (MPO) and Horseradish Peroxidase (HRP) involved in inflammation. The microscopic analysis of the powder of leaves showed that each species displays specific and discriminating botanical microscopic features. Varieties of<em> M. esculenta</em> had a chemical fingerprint different from <em>M. glaziovii</em>. The majority of compounds were polyphenols, represented mainly by rutin, kaempferol-3-O-rutinoside, amentoflavone, phenolic acids such as gallic acid. All extracts exhibited high cellular antioxidant activity in the range of 0.1 to 10 μg<span style="white-space:nowrap;">·</span>mL<sup>-1</sup> using lucigenin with neutrophils, but a moderate cellular antioxidant activity ranging between 10 and 100 μg<span style="white-space:nowrap;">·</span>mL<sup>-1</sup> with DCFDA on HL60 monocytes. Extracts from <em>Manihot</em> leaves showed a pronounced inhibitory effect on the production of extracellular ROS, on HRP and myeloperoxidase activity. Cellular antioxidant activities, the inhibitory effect on HRP of extracts from <em>M. glaziovii</em>, <em>M. esculenta</em> cultivar <em>Mwambu </em>were significantly higher, but their inhibitory effect on the activity of MPO was lower than those of <em>M. esculenta</em> cultivar TEM 419. The biological activities of <em>Manihot esculenta</em> and <em>Manihot glaziovii </em>were well correlated to their phytochemicals that could justify their traditional use as vegetables, potential functional foods or nutraceutical resources and medicines.展开更多
Panda oleosa Pierre (POP), a tropical plant tree, has been used in traditional medicine in Kisangani city and around to treat various diseases including diabetes and HIV/AIDs. This study aims to evaluate the chemical ...Panda oleosa Pierre (POP), a tropical plant tree, has been used in traditional medicine in Kisangani city and around to treat various diseases including diabetes and HIV/AIDs. This study aims to evaluate the chemical composition of POP extracts while setting up chromatographic fingerprints for their quality control, and the anti-hyperglycemic potential of trunk bark aqueous extracts of POP. Common chemical reactions were used for identification of main secondary metabolic groups. Thin layer chromatography was used to set up several chromatographic fingerprints of water and alcoholic extracts while evaluating chemical composition. Oral glucose tolerance test served to induce hyperglycemia in a rabbit model. The extracts were given as 25 mg/kg, 50 mg/kg, and 100 mg/kg body weight, 30 minutes before loading animals with glucose 4 g/kg. Blood samples were collected at various times: just before extracts (T-30), before (T0) and after glucose load (T30, T60, T120, and T180). Blood glucose levels were measured with One Touch Glucometer. The identification tests revealed the presence of saponins (3.58%), tannins (5%);alkaloids, quinones, flavonoids, and terpenes sterols could not be formerly detected by the reagents used. Interesting chromatographic spots were observed whose behaviors are of catechic tannin proanthocyanes. The extract significantly reduced glucose levels in dose dependent manner as compared to control and glibenclamide reference groups. The average of mean percentage of reduction in glucose level at T120 with the extract 100 mg/kg was close to that of glibenclamide 0.25 mg/kg (49% and 40.2%). These findings back the traditional use of the plant to treat diabetic patients and constitute a foundation for an extensive study to find a new antidiabetic phythomedicine.展开更多
The aim of this study was to characterize the polyphenolic composition by determination of chemical fingerprints of Methanolic extracts of Ocimum canum Sims, Ocimum basilicum L. and Ocimum gratissimum L. from Democrat...The aim of this study was to characterize the polyphenolic composition by determination of chemical fingerprints of Methanolic extracts of Ocimum canum Sims, Ocimum basilicum L. and Ocimum gratissimum L. from Democratic Republic of Congo and to compare their antisickling activity of that of rosmarinic acid, the major compound to those of methanolic extracts. Phytochemical analysis performed by TLC and HPLC analysis, showed that rosmarinic acid is the most abundant phenolic acid in these Ocimum species according to the following order O. basilicum L., O. gratissimum L. and O. canum Sims. Methanolic extracts of these three species and pure rosmarinic acid showed significant antisickling activities with minimal concentration of normalization values of 0.18 ± 0.03, 0.23 ± 0.04, 0.26 ± 0.04 and 0.31 ± 0.05 mg/mL for rosmarinic acid, O. basilicum L., O. gratissimum L. and O. canum Sims methanolic extracts respectively. The antisickling activity order is the same as that of the rosmarinic acid content, indicating that this polyphenolic acid would be among the main active molecules in these extracts.展开更多
Spilanthes oleracea Jacq.is an herbaceous plant whose scientific literature attributes among others,anti-malarial and anti-bilharzia properties.These virtues justify the placing on the market of drugs based on the pla...Spilanthes oleracea Jacq.is an herbaceous plant whose scientific literature attributes among others,anti-malarial and anti-bilharzia properties.These virtues justify the placing on the market of drugs based on the plant.Our study consisted on the one hand to evaluate the biomass of the plant on a soil of dune amended and on soil of unamended dune and to test its vegetative multiplication by transplanting,cuttings and layering.The results show that the growth of the species is greater on dune soil amended with an average biomass of 106.06 g compared to 71.06 g for un-amended soil plants.The transplanting of the plants and the layering were techniques that made it possible to multiply the plants.Spilanthes oleracea Jacq.can be produced using this agronomic data.展开更多
The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosom...The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).展开更多
The present study aim was to assess the preventive effects of Ananas comosus juice consumption on the risk factors of obesity in female Wistar rats. 108 rats were tested for 90 days. After randomization, they were sha...The present study aim was to assess the preventive effects of Ananas comosus juice consumption on the risk factors of obesity in female Wistar rats. 108 rats were tested for 90 days. After randomization, they were shared out into six groups including four experimental groups (GTc, GPlp, GEns and GBrS) and two control groups (<img src="Edit_22b6d494-c259-4132-9806-9c1843ee2402.png" width="15" height="3" align="right" alt="" /><img src="Edit_f761aee0-3be8-44aa-ba0a-865dcc4c7881.png" width="80" height="22" alt="" /><span style="font-family:Verdana;">). The control group consumed 1.20 ml of distilled water, the experimental rats received in oral, 1.20 ml of drinks made from the different parts of Ananas comosus fruit. The measurements of morphometric and biochemical parameters were carried out on Day 0 (D0), Day 30 (D30), Day 60 (D60) and Day 90 (D90). The analysis showed that compared to the positive control rats, the consumption of the various drinks slowed down significantly (P < 0.001);the evolution of the morphometric and biochemical parameters likely to induce obesity in experimental rats which have an increase in a protective factor (HDL;P < 0.001). These results indicate that consumption of different parts of Ananas comosus’s juices had preventive effects on risk factors related to obesity. Moreover, the fruit juice treatment has been found to be more effective.</span>展开更多
The Anonnaceae family has 2,500 species and 135 genera, which has about 14 representatives of species in Brazil,including Pseudoxandra cuspidata. The objective of this research was to study the aqueous-acid extract of...The Anonnaceae family has 2,500 species and 135 genera, which has about 14 representatives of species in Brazil,including Pseudoxandra cuspidata. The objective of this research was to study the aqueous-acid extract of P. cuspidata, evaluatingits antioxidant, larvicidal, antimicrobial and cytotoxic potential. In the preliminary phytochemical analysis, there were positivity toorganicacids and alkaloids. Inhibitory Activity of EAA was 65% against DPPH. The AAE presented to A. Salina nauplii at LC50%of 600.79 μg/mL for a periodof 24 hours. In relation to larvicidal activity to Aedes aegypti intermediates, AAE presented the LC50%in 24 Hours of 475.91 ppm and 290.73 ppm in 48 Hours. Regarding the antimicrobial action, the EAA presented 50 mg/mL MIC forP. Aeruginosa and MBC at 100 mg/mL, and for S. aureus it presented MIC of 50 mg/mL and did not present MBC. This researchcharacterized the presence of alkaloids and organicacids present in the aqueousacid extract of P. cuspidata. The extract presentedlowtoxicity in relation to the microcrustacean A. salina. It also had a relevant antioxidant potential (65% of Inhibition),larvicidalaction considered effective, antimicrobialaction for both P. Aeruginosa and S. Aureus even did not present bactericidalaction.展开更多
Sida pilosa Retz. (Malvaceae) is a medicinal plant used in Africa for the treatment of dysmenorrhea, lower abdominal pains and intestinal helminthiasis. S. pilosa aqueous extract and derived fractions were investigate...Sida pilosa Retz. (Malvaceae) is a medicinal plant used in Africa for the treatment of dysmenorrhea, lower abdominal pains and intestinal helminthiasis. S. pilosa aqueous extract and derived fractions were investigated for their bioactivity against Schistosoma mansoni. The aqueous extract from S. pilosa aerial parts (1.25 - 40 mg/mL) and derived fractions (n-hexane, DCM, EtOAc and n-BuOH: 0.25 - 8 mg/mL) were tested on adult S. mansoni maintained in a GMEN culture medium. Praziquantel was used as the reference drug. After 24 h of incubation, worms were monitored for their viability and egg output. The antioxidant activity of S. pilosa was evaluated by the ability to scavenge the 2,2-diphenyl-1-picrylhydrazyl free radicals. The chemical composition of the n-BuOH fraction was investigated by HPLC-MS analysis. S. pilosa aqueous extract and fractions significantly increased worm mortality in a concentration-dependent manner. The n-BuOH fraction was the most active with a LC50 of 1.25 mg/mL. Significant reduction of motor activity (25% to 100%) was recorded for surviving worms incubated in different concentrations of the extract and fractions. Incubation of S. mansoni in different concentrations of S. pilosa extract and fractions led to significant reduction of egg laying (52% to 100%). The aqueous extract and derived fractions exhibited antioxidant activity in a concentration-dependent manner. The highest antioxidant activity was found with the EtOAc fraction, followed by the DCM and n-BuOH fractions. HPLC-MS analysis of the n-butanol fraction revealed the presence of two indoloquinoline alkaloids. This study disclosed the schistosomicidal activity of the n-butanol fraction from S. pilosa aqueous extract. This activity is probably related to the indoloquinoline alkaloids identified in the fraction.展开更多
文摘Objective:To determine the anticancer potential of the methanolic extract from Ephedra alata against breast cancer both in vitro and in vivo.Methods:The effects of the methanolic extract of Ephedra alata on the viability,migration as well as apoptosis of breast cancer 4T1 cells were measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay,Transwell assay,and annexin V-FITC staining assay,respectively.Histological examination was also carried out.Moreover,a murine breast cancer model was established to evaluate the inhibitory effect of the extract.Biochemical parameters including hepatic and non-hepatic enzymes,malondialdehyde,and glutathione were investigated.Results:The methanolic extract of Ephedra alata showed a strong anti-proliferative and anti-migratory activity against 4T1 cells in a dose-dependent manner.It also induced apoptosis in 4T1 cells.In an in vivo mouse model,the extract markedly inhibited tumor growth,reduced malondialdehyde,and hepatic and non-hepatic enzymes as well as increased glutathione level.Conclusions:The methanolic extract of Ephedra alata inhibits breast cancer in vitro and in vivo,which may be a promising anticancer agent.
文摘The heavy use of chemicals, pesticides, cosmetics and plastic packaging coincides with a resurgence of cardiovascular disease, in particular hypertension, which is affecting younger and younger populations. The aim of this study was to analyze the cardiovascular risk factors in hypertensive farmers compared with hypertensive non farmers. This was a prospective case-control study that included 239 hypertensive farmers and non farmers aged 25 to 65 with blood pressure ≥ 140 mmHg and 90 mmHg. Hypertensive farmers (101) represented 42.25% of the population versus hypertensive non farmers (138) 57.74%. The median ages were 47 ± 11.3 years for farmers and 51.45 ± 9.77 years for non farmers. Biochemical analysisand screening for major cardiovascular disease risk factors such as metabolic syndrome were performed. Metabolic syndrome was defined according to the new definition of the International Diabetes Federation. Our results revealed higher blood glucose levels in farmers (47.77%) than in non farmers (27.20%) (p = 0.0132). Dyslipidemia was more frequent in non farmerswith high level of LDL cholesterol and total cholesterol. Farmers presented a high level of tryglycerides. The prevalence of obesity was higher in non farmers 51 (36.96%) than farmers 18 (17.82%). The prevalence of metabolic syndrome was 106 (44.35%) in our study population. There was not an important difference between farmers (39.60%) and non farmers (47.82%). However, the variation of metabolic syndrome according to age and sex showed a higher prevalence in young male farmers aged 25 to 45 whereas non farmers presented an increasing prevalence of metabolic syndrome according to age and the absence of metabolic syndrome between age 25 and 35. Our results showed that the cardiovascular risk appeared early in young farmers compared with non farmers suggesting a possible role of pesticides in the onset of this risk.
文摘The apparent degradation rate constant of fluticasone propionate(FLT) in 0.1 M NaOH:methanol=1:1 at 37 °C was previously reported to be 0.169 ± 0.003 h^(-1), and four degradation products(products 1–4) were observed in the solution. The aims of the present study were to assess the degradation rates of FLT in other alkaline solutions and clarify the chemical structures of the four degradation products in order to obtain basic data for designing an enema for inflammatory bowel disease. The apparent degradation rate constants in 0.05 M NaOH and 0.1 M NaOH:CH_3CN=1:1 were 0.472 ± 0.013 h^(-1) and 0.154 ± 0.000 h^(-1)(n=3), respectively. The chemical structures of products 1–4 in 0.1 M NaOH:methanol=1:1 were revealed by nuclear magnetic resonance(NMR)and mass spectrometry data. The chemical structure of products 2 was that the 17-position of the thioester moiety of FLT was substituted by a carboxylic acid. The degradation product in 0.1 M NaOH:CH_3CN=1:1 was found to be product 2 based on ~1H NMR data. The degradation product in 0.05 M NaOH was considered to be product 2 based on the retention time of HPLC. These results are useful for detecting the degradation products of FLT by enzymes of the intestinal bacterial flora in the large intestine after dosing FLT as an enema.
基金Supported by the European Union(FEDER funds through COMPETE)National Funds(FCT,Fundacao para a Cieencia e Tecnologia)through project Pest-C/EQB/LA0006/2013+1 种基金the European Union(FEDER funds)under the framework of QREN through Project NORTE-07-0124-FEDER-000069FCT the financial support for the Post-doc grant(SFRH/BPD/105263/2014)
文摘Objective:To improve the knowledge on the metabolite profile of five red grapes from D?o region(Portugal),concerning to the phenolic characteristics(coloured and non-coloured phenolics) and organic acid composition.Methods:Five red grapes collected from D?o region were studied.The profiles of phenolic compounds and organic acids were estimated by high-performance liquid chromatography with diode-array detection and high-performance liquid chromatography with UV detector,respectively.Results:Totally 24 phenolic compounds were identified,and distributed by several classes:8 anthocyanins,1 hydroxybenzoic acid,4 hydroxycinnamic acids,1 stilbene,4flavan-3-ols,6 flavonols.Additionally,10 organic acids were detected in all samples.Total contents of each phenolic class and organic acids amounts varied significantly among the different grape cultivars investigated.The principal components analysis differentiates the Touriga Nacional from the other varieties due to their high contents in anthocyanins,non-coloured phenolics and organic acids.Touriga Nacional is an important red grape cultivar,highly esteemed in D?o region for its ability to produce high quality wines.Conclusions:The results suggest that the red grapes from D?o region present a good composition in bioactive compounds,being important for the production of wines with superior quality.
文摘Vegetables are very important sources of protein and minerals. Some of them even have medicinal properties recognized traditionally. Despite the large number of studies carried out on various vegetables and vegetable crops, very few have scientifically explored the usefulness of S. macrocarpon. This study identified the main groups of chemicals and mineral elements to explain any medicinal or nutritional value. It has also identified some toxic elements contained in this vegetable. Phytochemical screening was carried out on the leaves and fruits of S. macrocarpon. Some mineral elements were determined by Atomic Absorption Spectrophotometry (sodium, potassium, calcium, magnesium) while protein, phosphorous, iron, copper, zinc and toxic metals (lead, cadmium) were determined by Molecular Absorption Spectrophotometry. Fat, ash, moisture and vitamins were sought. The study showed that the leaves of S. macrocarpon were more nutritious than fruits (P macrocarpon require that the consumption of vegetables should be as varied as possible and that the fruit may be consumed with caution. In addition, constraints about vegetable cultivation in Cotonou could lead to research findings that could help provide techniques for producing healthy vegetables.Vitamins A and K1 were found in both parts of this vegetable very rich in water while vitamin E has not been detected. S. macrocarpon also contains lipids at various levels.
文摘In order to combat the counterfeiting of drugs, adapted HPLC analytical USP methods were applied to evaluate the quality of the amoxicillin (with or without potassium clavulanate) powder for suspension sold in some Congolese markets. The adaptation has been done by modifying the column dimensions and adjusting the flow rate. According to the intended deployment of these methods in Democratic Republic of Congo (DRC), 3 factors (analyst, day and equipment) were involved in the validation step while applying the classic total error measurement approach with an accuracy profile as decision tool. Since adequate results were obtained in terms of selectivity, precision, trueness and accuracy (tolerance limits of life expectancy: ?6.0% and 3.8%) for levels of interest concentration, the methods have been considered for routine use on several samples from different provenances and collected in 4 major DRC cities. Out of 278 samples collected, 200 were eligible for analysis from which 28% were found under standards with several figures: pH failure, out of specification for amoxicillin content, absence of potassium clavulanate, physical modifications of the powders. As evidenced by these findings, medicines of low-quality continue to be a major public health problem requiring appropriate action to effectively address this problem.
文摘Pharmaceutical counterfeiting is a health scourge responsible for several cases of morbidity and mortality. Counterfeit medicines cause therapeutic failure, emergence of resistance in the treatment of infections. This study was conducted in order to identify counterfeit and authentic medicines in circulation in Lubumbashi. The study included artemether and artesunate for oral administration. A careful visual inspection of medicine, investigation of authenticity of pharmaceutical products from manufacturers and pharmaceutical regulatory authorities and determination of content were used as study parameters. 52 samples: 37 artemether and 15 of artésunate were collected. 7 samples (13%) have proven to be counterfeit. Artemether was the most counterfeit (71%) and 29% for artesunate. 6 (12%) samples were substandard according to the international pharmacopoeia in terms of content of active ingredient. Sixty-seven percent of non-compliance concerned counterfeit medicines. The proportion of non-compliance is highest among counterfeit medicines (71.43% vs 2.22%;p = 0.000004). It is obvious that strengthening the capacity of the drug regulatory authority of the DRC reduces the influx of counterfeit drug and substandard.
基金the support of Fundacao para a Ciência e Tecnologia(FCT),through the strategic project UID/MAR/04292/2013 granted to MAREfunding from European Structural&Investment Funds through the COMPETE ProgrammeNational Funds through FCT-Fundacao para a Ciência e a Tecnologia under the Programme(No.SAICTPAC/0019/2015)
文摘Algae(and their extracts)are increasingly important for pharmaceutical applications due to the diversity of useful compounds they contain.The genus Fucus contains one of the most studied species,Fucus vesiculosus.The species F.ceranoides differs from the others of the genus by presenting longitudinal air-vesicles and a capacity to survive at low salinities.It is an alga that inhabits the Mondego River estuary(Portugal),at the southern limit of its distribution,and can serve as a role model to understand the effect of a salt gradient on the production of bioactive compounds.We assessed the phenolic content and antioxidant activity of different F.ceranoides extracts(e.g.methanolic,aqueous and polysaccharide)prepared from samples harvested from two different zones to evaluate if the adaptation of F.ceranoides to different salinity levels influenced its chemical composition.The antioxidant activity of the extracts was determined using 1,2-diphenyl-picrylhydrazyl(DPPH)and 2.2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS)radicals.These assays demonstrated that the methanolic extract of lyophilized F.ceranoides that grew at low salinities was the most bioactive,i.e.DPPH(IC 50=50.39μg/mL)and ABTS(TEAC=2.42).The total phenolic content(Folin-Ciocalteu method)and the methanolic extract of the lyophilized F.ceranoides collected from a low salinity habitat exhibited the highest phenolic content(PGE=49.48μg/mg of lyophilized extract)amongst those sampled.Thin layer chromatography(TLC)and Fourier transform infrared spectroscopy(FTIR)were used for the identification of compounds in the extracts.This characterization allowed confirmation that the various extracts contained almost the same compounds but with notable quantitative differences.Based on these results,we conclude that there were differences in the quantity of the compounds due to the effect of salinity.The drying methods used were also found to have influenced the quality of the extracted compounds.
文摘Justicia secunda, Sorghum bicolor, Gossypiun barbadense and Hibiscus sabdariffa are dye plants traditionally used in Benin for the treatment of anemia. This work is part of the therapeutic valorization of dyes from these plants. Its objective is to characterize their composition in chemical groups and evaluate their harmlessness and their anti-anaemic property in laboratory rats. Anemia was induced in Wistar rats by phenylhydrazine hydrochloride followed by treatment by gavage with hydroethanolic extracts of the plants studied. Phytochemical screening of these extracts made it possible to characterize the major chemical groups, in particular alkaloids, polyphenols including tannins, flavonoids and leucoanthocyanins, as well as reducing compounds and saponosides in the plants studied. Cytotoxic analysis of these extracts on Artemia salina shrimp larvae revealed globally high LC<sub>50</sub> values of between 3.14 and 4.64 mg/mL, which testify a priori to the harmlessness of these extracts. The administration of the hydroethanolic extract of each plant to anaemic rats at doses of 2000 mg/kg/d promoted, after 15 days, an increase in hemoglobin levels, the number of red blood cells and hematocrit, going to more than 90% recovery of the hematological parameters involved. The highest rate, 99.06% being that of the species Justicia secunda followed closely by Sorghum bicolor (96.80%) compared to 93.93% obtained by treatment with the Ranferon-12 positive control used. Indeed, these results confirm the therapeutic indication of these plants in the resorption of anemia in traditional medicine.
文摘Methanolic extracts from the leaves of <em>Manihot esculenta </em>(Two cultivars) and <em>Manihot glaziovii</em>, consumed as traditional vegetables in DR. Congo was chemically characterized by Thin layer Chromatography and High Performance Liquid Chromatography. <em>In vitro</em> biochemical activities of extracts against Radical Oxidative Species (ROS) production were assessed in cellular models, on enzymes, Myeloperoxidase (MPO) and Horseradish Peroxidase (HRP) involved in inflammation. The microscopic analysis of the powder of leaves showed that each species displays specific and discriminating botanical microscopic features. Varieties of<em> M. esculenta</em> had a chemical fingerprint different from <em>M. glaziovii</em>. The majority of compounds were polyphenols, represented mainly by rutin, kaempferol-3-O-rutinoside, amentoflavone, phenolic acids such as gallic acid. All extracts exhibited high cellular antioxidant activity in the range of 0.1 to 10 μg<span style="white-space:nowrap;">·</span>mL<sup>-1</sup> using lucigenin with neutrophils, but a moderate cellular antioxidant activity ranging between 10 and 100 μg<span style="white-space:nowrap;">·</span>mL<sup>-1</sup> with DCFDA on HL60 monocytes. Extracts from <em>Manihot</em> leaves showed a pronounced inhibitory effect on the production of extracellular ROS, on HRP and myeloperoxidase activity. Cellular antioxidant activities, the inhibitory effect on HRP of extracts from <em>M. glaziovii</em>, <em>M. esculenta</em> cultivar <em>Mwambu </em>were significantly higher, but their inhibitory effect on the activity of MPO was lower than those of <em>M. esculenta</em> cultivar TEM 419. The biological activities of <em>Manihot esculenta</em> and <em>Manihot glaziovii </em>were well correlated to their phytochemicals that could justify their traditional use as vegetables, potential functional foods or nutraceutical resources and medicines.
文摘Panda oleosa Pierre (POP), a tropical plant tree, has been used in traditional medicine in Kisangani city and around to treat various diseases including diabetes and HIV/AIDs. This study aims to evaluate the chemical composition of POP extracts while setting up chromatographic fingerprints for their quality control, and the anti-hyperglycemic potential of trunk bark aqueous extracts of POP. Common chemical reactions were used for identification of main secondary metabolic groups. Thin layer chromatography was used to set up several chromatographic fingerprints of water and alcoholic extracts while evaluating chemical composition. Oral glucose tolerance test served to induce hyperglycemia in a rabbit model. The extracts were given as 25 mg/kg, 50 mg/kg, and 100 mg/kg body weight, 30 minutes before loading animals with glucose 4 g/kg. Blood samples were collected at various times: just before extracts (T-30), before (T0) and after glucose load (T30, T60, T120, and T180). Blood glucose levels were measured with One Touch Glucometer. The identification tests revealed the presence of saponins (3.58%), tannins (5%);alkaloids, quinones, flavonoids, and terpenes sterols could not be formerly detected by the reagents used. Interesting chromatographic spots were observed whose behaviors are of catechic tannin proanthocyanes. The extract significantly reduced glucose levels in dose dependent manner as compared to control and glibenclamide reference groups. The average of mean percentage of reduction in glucose level at T120 with the extract 100 mg/kg was close to that of glibenclamide 0.25 mg/kg (49% and 40.2%). These findings back the traditional use of the plant to treat diabetic patients and constitute a foundation for an extensive study to find a new antidiabetic phythomedicine.
文摘The aim of this study was to characterize the polyphenolic composition by determination of chemical fingerprints of Methanolic extracts of Ocimum canum Sims, Ocimum basilicum L. and Ocimum gratissimum L. from Democratic Republic of Congo and to compare their antisickling activity of that of rosmarinic acid, the major compound to those of methanolic extracts. Phytochemical analysis performed by TLC and HPLC analysis, showed that rosmarinic acid is the most abundant phenolic acid in these Ocimum species according to the following order O. basilicum L., O. gratissimum L. and O. canum Sims. Methanolic extracts of these three species and pure rosmarinic acid showed significant antisickling activities with minimal concentration of normalization values of 0.18 ± 0.03, 0.23 ± 0.04, 0.26 ± 0.04 and 0.31 ± 0.05 mg/mL for rosmarinic acid, O. basilicum L., O. gratissimum L. and O. canum Sims methanolic extracts respectively. The antisickling activity order is the same as that of the rosmarinic acid content, indicating that this polyphenolic acid would be among the main active molecules in these extracts.
文摘Spilanthes oleracea Jacq.is an herbaceous plant whose scientific literature attributes among others,anti-malarial and anti-bilharzia properties.These virtues justify the placing on the market of drugs based on the plant.Our study consisted on the one hand to evaluate the biomass of the plant on a soil of dune amended and on soil of unamended dune and to test its vegetative multiplication by transplanting,cuttings and layering.The results show that the growth of the species is greater on dune soil amended with an average biomass of 106.06 g compared to 71.06 g for un-amended soil plants.The transplanting of the plants and the layering were techniques that made it possible to multiply the plants.Spilanthes oleracea Jacq.can be produced using this agronomic data.
文摘The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).
文摘The present study aim was to assess the preventive effects of Ananas comosus juice consumption on the risk factors of obesity in female Wistar rats. 108 rats were tested for 90 days. After randomization, they were shared out into six groups including four experimental groups (GTc, GPlp, GEns and GBrS) and two control groups (<img src="Edit_22b6d494-c259-4132-9806-9c1843ee2402.png" width="15" height="3" align="right" alt="" /><img src="Edit_f761aee0-3be8-44aa-ba0a-865dcc4c7881.png" width="80" height="22" alt="" /><span style="font-family:Verdana;">). The control group consumed 1.20 ml of distilled water, the experimental rats received in oral, 1.20 ml of drinks made from the different parts of Ananas comosus fruit. The measurements of morphometric and biochemical parameters were carried out on Day 0 (D0), Day 30 (D30), Day 60 (D60) and Day 90 (D90). The analysis showed that compared to the positive control rats, the consumption of the various drinks slowed down significantly (P < 0.001);the evolution of the morphometric and biochemical parameters likely to induce obesity in experimental rats which have an increase in a protective factor (HDL;P < 0.001). These results indicate that consumption of different parts of Ananas comosus’s juices had preventive effects on risk factors related to obesity. Moreover, the fruit juice treatment has been found to be more effective.</span>
文摘The Anonnaceae family has 2,500 species and 135 genera, which has about 14 representatives of species in Brazil,including Pseudoxandra cuspidata. The objective of this research was to study the aqueous-acid extract of P. cuspidata, evaluatingits antioxidant, larvicidal, antimicrobial and cytotoxic potential. In the preliminary phytochemical analysis, there were positivity toorganicacids and alkaloids. Inhibitory Activity of EAA was 65% against DPPH. The AAE presented to A. Salina nauplii at LC50%of 600.79 μg/mL for a periodof 24 hours. In relation to larvicidal activity to Aedes aegypti intermediates, AAE presented the LC50%in 24 Hours of 475.91 ppm and 290.73 ppm in 48 Hours. Regarding the antimicrobial action, the EAA presented 50 mg/mL MIC forP. Aeruginosa and MBC at 100 mg/mL, and for S. aureus it presented MIC of 50 mg/mL and did not present MBC. This researchcharacterized the presence of alkaloids and organicacids present in the aqueousacid extract of P. cuspidata. The extract presentedlowtoxicity in relation to the microcrustacean A. salina. It also had a relevant antioxidant potential (65% of Inhibition),larvicidalaction considered effective, antimicrobialaction for both P. Aeruginosa and S. Aureus even did not present bactericidalaction.
文摘Sida pilosa Retz. (Malvaceae) is a medicinal plant used in Africa for the treatment of dysmenorrhea, lower abdominal pains and intestinal helminthiasis. S. pilosa aqueous extract and derived fractions were investigated for their bioactivity against Schistosoma mansoni. The aqueous extract from S. pilosa aerial parts (1.25 - 40 mg/mL) and derived fractions (n-hexane, DCM, EtOAc and n-BuOH: 0.25 - 8 mg/mL) were tested on adult S. mansoni maintained in a GMEN culture medium. Praziquantel was used as the reference drug. After 24 h of incubation, worms were monitored for their viability and egg output. The antioxidant activity of S. pilosa was evaluated by the ability to scavenge the 2,2-diphenyl-1-picrylhydrazyl free radicals. The chemical composition of the n-BuOH fraction was investigated by HPLC-MS analysis. S. pilosa aqueous extract and fractions significantly increased worm mortality in a concentration-dependent manner. The n-BuOH fraction was the most active with a LC50 of 1.25 mg/mL. Significant reduction of motor activity (25% to 100%) was recorded for surviving worms incubated in different concentrations of the extract and fractions. Incubation of S. mansoni in different concentrations of S. pilosa extract and fractions led to significant reduction of egg laying (52% to 100%). The aqueous extract and derived fractions exhibited antioxidant activity in a concentration-dependent manner. The highest antioxidant activity was found with the EtOAc fraction, followed by the DCM and n-BuOH fractions. HPLC-MS analysis of the n-butanol fraction revealed the presence of two indoloquinoline alkaloids. This study disclosed the schistosomicidal activity of the n-butanol fraction from S. pilosa aqueous extract. This activity is probably related to the indoloquinoline alkaloids identified in the fraction.