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Gliptins vs. Milk-derived Dipeptidyl-Peptidase IV Inhibiting Biopeptides: Physicochemical Characterization and Pharmacokinetic Profiling 格立汀与牛奶衍生二肽基肽酶IV抑制生物肽:物理化学表征和药代动力学分析
Vitae Pub Date : 2021-10-04 DOI: 10.17533/udea.vitae.v28n3a346531
Jorge A. Barrero, F. Cabrera, C. M. Cruz
{"title":"Gliptins vs. Milk-derived Dipeptidyl-Peptidase IV Inhibiting Biopeptides: Physicochemical Characterization and Pharmacokinetic Profiling","authors":"Jorge A. Barrero, F. Cabrera, C. M. Cruz","doi":"10.17533/udea.vitae.v28n3a346531","DOIUrl":"https://doi.org/10.17533/udea.vitae.v28n3a346531","url":null,"abstract":"Background: Milk-derived biopeptides have reported in vitro dipeptidyl-peptidase IV (DPP-IV) inhibition, suggesting a glycemic-regulatory effect in Type 2 Diabetes Mellitus (T2DM). Nonetheless, the therapeutic application of these nutraceuticals is limited by the scarcity of knowledge regarding their pharmacokinetic profile. Objective: This study aimed to characterize and assess the pharmacokinetics of milk-derived biopeptides. Through an in silico comparative analysis with gliptins, we expected to identify enhanced properties in food-hydrolysates and suitable DPP-IV inhibiting peptides as candidates for T2DM therapy. Methods: A comparison between gliptins and biopeptides was conducted based on in silico evaluation of drug-likeness, physicochemical properties, pharmacokinetics, and synthetic accessibility. Suitable target proteins for gastrointestinal-absorbable biopeptides were determined as well. Data collection was performed on SwissADME, ADMETlab, DrugBank, SwissTargetPrediction, ChemDes, and BIOPEP-UWM platforms. Statistical analysis was carried out using a one-way ANOVA test. Results: Drug-likeness compliance showed no significant difference between gliptins and biopeptides (p>0.05) in three out of nine assessed rules, though gastrointestinal-absorbable biopeptides exhibited no significant difference with gliptins in five drug-likeness guidelines. The physicochemical evaluation revealed a significant difference (p<0.05) between both groups, with peptides exhibiting enhanced solubility, flexibility, and polarity. Nine out of thirty-six assessed biopeptides reported being likely gastrointestinal-absorbable molecules, from which six displayed ≥30% predicted bioavailability, two reported CYP450 interactions, and all were determined to be blood confined. Biopeptides showed a slightly lower clearance than gliptins yet counteracted by a significantly lower half-life. Moreover, synthetic accessibility scores indicated higher synthetic ease for biopeptides. In addition, absorbable bioactive peptides reported a considerable binding affinity to DPP-IV and Calpain-I. Conclusions: Compared to gliptins, gastrointestinal-absorbable biopeptides exhibit superior physicochemical properties (higher solubility, flexibility, and polarity), lesser CYP450 interactions, higher synthetic ease, and some reported an important affinity for DPP-IV and Calpain-I. Only a small fraction of milk-derived biopeptides are suitable drug-like compounds and feasible candidates for T2DM therapy; yet, testing their therapeutic potency remains subject to further studies.","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"52 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74758736","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
Comparison of the Effectiveness of Leaf Extracts of Anredera cordifolia, Psidium guajava and Pogostemon cablin on Inhibitory Power Over Escherichia coli Bacteria 菖蒲叶提取物、番石榴叶提取物和广藿香叶提取物对大肠杆菌抑制作用的比较
Vitae Pub Date : 2021-10-04 DOI: 10.17533/udea.vitae.v28n3a345386
Budianto Budianto, Alif Gita Arum sari, N. Inayah, F. Fatmaningrum, A. Suparmi
{"title":"Comparison of the Effectiveness of Leaf Extracts of Anredera cordifolia, Psidium guajava and Pogostemon cablin on Inhibitory Power Over Escherichia coli Bacteria","authors":"Budianto Budianto, Alif Gita Arum sari, N. Inayah, F. Fatmaningrum, A. Suparmi","doi":"10.17533/udea.vitae.v28n3a345386","DOIUrl":"https://doi.org/10.17533/udea.vitae.v28n3a345386","url":null,"abstract":"Background: the current research studies why it is effective using Anredera cordifolia, Psidium guajava, and Pogostemon cablin by the local community as a traditional medicine for diarrhea treatment caused by Escherichia colibacteria. Objectives: We compared the inhibitor effectiveness of three leaf extracts against Escherichia coli; we also identified the anti-bacterial substances contained in leaf extracts. Methods: We determined the bacterial test activity using the \"agar diffusion\" method and the thin layer chromatography (TLC) as qualitative analysis for determining the anti-bacterial substances contained in the extract. Results: The Pogostemon cablin leaf extract contained terpenoids, phenolic, and flavonoids compound as bacterial inhibitors, and the comparison showed that Pogostemon cablin leaf extract had the greatest bacterial inhibition power. Conclusion: The antibiotic substances found in the leaf extracts of Anredera cordifolia, Psidium guajava, and Pogostemon cablin can be used as traditional medicine. The breakthrough was evidenced by the ability to inhibit Escherichia coli bacteria. This research shows that traditional medicine has ancient knowledge used by this paper","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"78 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86720305","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Wound healing activity of Allium cepa L. bulbs in a second-degree burn wound model in Holtzman rats 大蒜球茎在Holtzman大鼠二度烧伤模型中的创面愈合活性
Vitae Pub Date : 2021-08-18 DOI: 10.17533/udea.vitae.v28n3a345737
A. Guevara-Vásquez, C. Marín-Tello
{"title":"Wound healing activity of Allium cepa L. bulbs in a second-degree burn wound model in Holtzman rats","authors":"A. Guevara-Vásquez, C. Marín-Tello","doi":"10.17533/udea.vitae.v28n3a345737","DOIUrl":"https://doi.org/10.17533/udea.vitae.v28n3a345737","url":null,"abstract":"Background: The bulb of Allium cepa Linnaeus (onion) is used in traditional medicine as an antidiabetic, antioxidant, antihypertensive, anti-inflammatory, and antihyperlipidemic, among others. The lack of information or little knowledge about the effects of Allium cepa L. on skin lesions, specifically burn wounds, arouses interest in studying its effects on these skin disorders. Objective: This study assessed the wound healing activity of Allium cepa L. on second-degree burns induced in Holtzman rats. Method: Thirty-two albino rats were randomly distributed into four groups of 8 rats each, including the Healthy group, the Control group, the Experimental group (Allium cepa L.), and the Standard group (1% silver sulfadiazine). Burn wounds were induced, and topical treatments were performed daily for 21 days. The reduction of the burned body area (mm2) was determined during the experimental time. Albino rats were sacrificed with an excess of surgical anesthesia to obtain tissue samples for histopathological analysis. Results: Standard and experimental groups significantly reduced burned body area (p<0.01) compared to the control group. Histopathological studies showed hyperemic chorion in the Control group, fibroblasts, and collagen in the Standard group, and dermis composed of a reticular stratum of fibroblasts, collagen, and few blood vessels in the Experimental group. Conclusion: Allium cepa L. revealed wound-healing activity on burns induced in Holtzman rats and reduced the damage produced by burns.","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"231 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73832857","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
Validation of a method employing liquid chromatography to identify and quantify glycomacropeptide of casein in raw milk 用液相色谱法鉴定和定量原料奶中酪蛋白糖宏肽的方法的验证
Vitae Pub Date : 2021-08-11 DOI: 10.17533/udea.vitae.v28n3a345256
Orlando Bernal Chia, Fernando Murcia Rubiano, Olga Lucía Ávila Guzmán, Jenifer Yaneth Guzman Gualteros, Willinton Arturo Arias Casallas, Maria Victoria Morales
{"title":"Validation of a method employing liquid chromatography to identify and quantify glycomacropeptide of casein in raw milk","authors":"Orlando Bernal Chia, Fernando Murcia Rubiano, Olga Lucía Ávila Guzmán, Jenifer Yaneth Guzman Gualteros, Willinton Arturo Arias Casallas, Maria Victoria Morales","doi":"10.17533/udea.vitae.v28n3a345256","DOIUrl":"https://doi.org/10.17533/udea.vitae.v28n3a345256","url":null,"abstract":"BACKGROUND: The information on official testing methods, or regulatory methods in Colombia to test whey in milk is limited; this restriction of information goes against the possibility of mitigating the risk of food fraud. OBJECTIVES: The validation of an HPLC method to determine casein glycomacropeptide (c-GMP), a protein that countries such as Brazil, Spain, and Ecuador have used as an indicator of raw milk adulteration with whey, was carried out. METHODS: A 10mL sample of raw milk is precipitated with 24% TCA using ultrasound, a process followed by filtration. The collected fraction ensured the separation of c-GMP and then injected into the liquid chromatography. RESULTS: A 30 minutes analysis allowed the determination of c-GMP with a retention time of 12.9 ± 0.5 minutes. The performance characteristics method in the validation exercise were: recovery percentage 99.97%, linearity R2> 0.95; % RSD accuracy <5.3%. CONCLUSION, the method exhibits desirable attributes for the intended purpose.","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"29 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83652393","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Iodine deficiency in women of childbearing age in Brazil: systematic review and meta-analysis 巴西育龄妇女碘缺乏:系统回顾和荟萃分析
Vitae Pub Date : 2021-07-07 DOI: 10.17533/UDEA.VITAE.V28N2A345572
R. Lucchetta, A. Gini, Sophia de Andrade Cavicchioli, Marcela Forgerini, F. Varallo, M. N. de Nadai, F. Fernandez‐Llimos, P. Mastroianni
{"title":"Iodine deficiency in women of childbearing age in Brazil: systematic review and meta-analysis","authors":"R. Lucchetta, A. Gini, Sophia de Andrade Cavicchioli, Marcela Forgerini, F. Varallo, M. N. de Nadai, F. Fernandez‐Llimos, P. Mastroianni","doi":"10.17533/UDEA.VITAE.V28N2A345572","DOIUrl":"https://doi.org/10.17533/UDEA.VITAE.V28N2A345572","url":null,"abstract":"Background: Despite current policies of salt iodination, iodine deficiency is still a global public health problem, especially in women. So far, conflicting evidence has been suggested for the prevalence of iodine deficiency in Brazil. Objective: To estimate the prevalence of iodine deficiency and associated factors in women of childbearing age in Brazil. Methods: A systematic review was conducted using databases (PubMed, LILACS, WHO, Scopus, and Capes’ dissertation and thesis), from inception to May 2020. Meta-analyses of proportions were performed using the variance inverse for the fixed model. Reporting and methodological quality were assessed using the Joanna Briggs Institute tool to prevalence studies. Results: Our review identified seven studies published between 2002 e 2017, including 1354 participants, especially pregnant women. All studies presented at least one quality limitation, mainly regarding the sampling method (i.e., convenience) and small sample size. The prevalence of iodine deficiency ranged among studies from 16% to 62%. In contrast, the meta-analysis identified a mean prevalence of 40% (95% confidence interval, CI 37%-43%) for pregnant women and 13% (95% CI 4%-24%) for non-pregnant women. Cumulative meta-analysis suggests a tendency of higher iodine deficiency prevalence from 2018 in pregnant women. Conclusions: Although this systematic review identified studies with poor methodological and reporting quality, a high prevalence of iodine deficiency was identified in pregnant women, reinforcing the importance of national nutritional policies for monitoring iodine status in this population. Future studies should consider random probabilistic sampling, appropriate sample size, and pre-defined subgroup analysis to adequately inform the prevalence of iodine deficiency and associated factors in women of childbearing age and support health policies.","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"50 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83602302","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Voltammetric Determination of Ascorbic Acid in Pharmaceutical Formulations Using Modified Iodine-Coated Platinum Electrode 用修饰碘包覆铂电极伏安法测定药物制剂中的抗坏血酸
Vitae Pub Date : 2021-06-29 DOI: 10.17533/udea.vitae.v28n2a346228
Mohammad Amayreh, W. Hourani, M. Hourani
{"title":"Voltammetric Determination of Ascorbic Acid in Pharmaceutical Formulations Using Modified Iodine-Coated Platinum Electrode","authors":"Mohammad Amayreh, W. Hourani, M. Hourani","doi":"10.17533/udea.vitae.v28n2a346228","DOIUrl":"https://doi.org/10.17533/udea.vitae.v28n2a346228","url":null,"abstract":"Background: Despite the high reactivity of the platinum electrode, the iodine-coated platinum electrode shows obvious inertness toward adsorption and surface processes. For that, iodine-coated platinum electrodes accommodate themselves to interesting voltammetric applications. Objectives: This study reports using the modified iodine-coated polycrystalline platinum electrode as a voltammetric sensor for ascorbic acid determination in pharmaceutical formulations. Methods: The developed voltammetric method based on recording cyclic voltammograms of ascorbic acid at iodine-coated electrode The optimized experimental parameters for the determination of ascorbic acid were using 0.1 M KCl as a supporting electrolyte with a scan rate of 50mV/s. Results: The anodic peak related to ascorbic acid oxidation was centered at nearly 0.28V. An excellent and extended linear dependence of the oxidative peak current on the concentration of ascorbic acid was observed in the range 2.84x10-3 - 5.68 mM. The limit of detection (LOD) and limit of quantitation (LOQ) were 1.0 µM and 3.01 µM, respectively, attesting to the method’s sensitivity. The investigation for the effect of potential interference from multivitamin tablet ingredients (vitamins B1, B6, B12, folic acid, citric acid, sucrose, glucose, and zinc) indicated specific selectivity toward ascorbic acid and the absence of any electrochemical response toward these components. Recovery results in the range 98.93±2.78 - 99.98±5.20 for spiked standard ascorbic acid in pharmaceutical formulations further confirmed the potential applicability of the developed method for the determination of ascorbic acid in real samples. Conclusions: The developed method was successfully applied to the analysis of ascorbic acid (vitamin C), and the obtained results were in good agreement with the labeled values; besides, the statistical tests indicated no significant difference at p=0.05 with a 95% confidence level.","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"8 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88181743","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
Consumption of osmo-dehydrated Andean Berry (Vaccinium meridionale Swartz) decreases levels of pro-inflammatory biomarkers of overweight and obese adults 食用渗透脱水的安第斯浆果(Vaccinium meridionale Swartz)可降低超重和肥胖成年人的促炎生物标志物水平
Vitae Pub Date : 2021-06-17 DOI: 10.17533/udea.vitae.v28n2a343810
Emerson Gallego Peláez, Maria Elena Maldonado Celis, Luz Gladys Posada Jhonson, A. Gómez García, David Torres Camargo
{"title":"Consumption of osmo-dehydrated Andean Berry (Vaccinium meridionale Swartz) decreases levels of pro-inflammatory biomarkers of overweight and obese adults","authors":"Emerson Gallego Peláez, Maria Elena Maldonado Celis, Luz Gladys Posada Jhonson, A. Gómez García, David Torres Camargo","doi":"10.17533/udea.vitae.v28n2a343810","DOIUrl":"https://doi.org/10.17533/udea.vitae.v28n2a343810","url":null,"abstract":"Background: A Body Mass Index (BMI) greater than 24.9 Kg/m2 promotes chronic inflammation due to increased secretion of pro-inflammatory adipokines. Consuming fruits rich in bioactive compounds such as berries is a promising strategy to counteract this effect. Objectives: Determine the effect of osmo-dehydrated Andean Berry consumption on inflammatory biomarkers (TNF-α, IL-6, IL-1β, and adiponectin) and plasma antioxidant capacity in overweight and obese adults after 21 days. Methods: Andean Berry was osmo-dehydrated in 70% sucrose syrup. Antioxidant activity, proximal composition, phenolic content, microbiological analysis, and sensory analysis of the product were determined. Twenty-five obese and overweight subjects consumed 35g of osmo-dehydrated berry for 21 days. Inflammatory biomarkers and antioxidant capacity in plasma were evaluated at the beginning and end of the study. Results: Osmo-dehydrated Andean Berry presented a total phenolic content of 692.7 ± 47.4 mg Gallic Acid Equivalents/100 g. All biomarkers evaluated in the subjects showed statistically significant differences (p> 0.05), except for CRP, before and after the study. IL-6 presented the more significant reduction among all pro-inflammatory adipokines with an effect size of 18.4 Conclusions: Regular consumption of osmo-dehydrated Andean Berry contributes to decreasing pro-inflammatory biomarkers and improves the plasma antioxidant capacity of overweight and obese adults.","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87383449","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Determination of ochratoxin a in coffee by ELISA method and its relationship with the physical, physicochemical and microbiological properties ELISA法测定咖啡中赭曲霉毒素a及其与理化、微生物特性的关系
Vitae Pub Date : 2021-05-22 DOI: 10.17533/UDEA.VITAE.V28N2A343838
Robinson Monsalve-Atencio, Karolay Sanchez, Jairo Camaño, Seneida Lopera-Cardona, B. Ortiz-Reyes
{"title":"Determination of ochratoxin a in coffee by ELISA method and its relationship with the physical, physicochemical and microbiological properties","authors":"Robinson Monsalve-Atencio, Karolay Sanchez, Jairo Camaño, Seneida Lopera-Cardona, B. Ortiz-Reyes","doi":"10.17533/UDEA.VITAE.V28N2A343838","DOIUrl":"https://doi.org/10.17533/UDEA.VITAE.V28N2A343838","url":null,"abstract":"BACKGROUND: Coffee is one of the most consumed beverages in the world; however, it may contain toxic compounds such as ochratoxin A (OTA). OBJECTIVES: Determine the OTA’s presence in different types of coffee, intended for beverage preparation and marketed in Colombia through the application of the enzyme-linked immunosorbent assay (ELISA) and analyze its relationship with the physical, physicochemical and microbiological properties. METHODS: 8 samples of coffee commercialized in the Colombian market were selected, in which the OTA content was determined by applying the ELISA method. Likewise, a microbiological analysis was performed, and physicochemical properties were determined, such as moisture content, aw, percentage total dissolved solids (%TDS), and extraction yield (%EY). Physical properties such as free-flow densities, compacted bulk densities (CBD), porosity, average particle size (ASP), and color. The data were treated with multivariate analysis using Principal Component Analysis (PCA) and Cluster Analysis (CA) to quantitatively investigate the relationships between the coffee samples concerning their physical, physicochemical properties, and OTA content. LSD test was applied with a significance level of 95 % and Pearson correlation test. RESULTS: All the samples had OTA content, but only 2 exceeded the limits allowed by the regulations, with a maximum value of 15.449 µg/Kg, which represents 31.449 % of the tolerable daily intake according to the parameters defined by Joint FAO/WHO Expert Committee on Food Additives (JECFA). According to the PCA and CA, the samples were grouped harmonically according to the type of coffee associated with its commercial presentation and industrial process, OTA content, and ASP. OTA content was significantly and positively correlated (p < 0.05) with %EY, %TDS, ASP, porosity, CBD, and moisture. CONCLUSIONS: The coffees marketed in Colombia showed a variable range of OTA, where soluble coffees had higher OTA contents than roasted coffees, and 25 % of the coffees analyzed do not meet the levels defined by Colombian regulations. The OTA content in coffee is related to properties that define the ability to extract solutes from coffee.","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"23 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84891248","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats 巴豆主要黄酮在Wistar大鼠离体主动脉环中的血管相互作用
Vitae Pub Date : 2021-05-18 DOI: 10.17533/UDEA.VITAE.V28N2A343923
Mario Francisco Guerrero Pabón, S. Ortiz, Dra. Pilar Puebla Ibáñez
{"title":"Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats","authors":"Mario Francisco Guerrero Pabón, S. Ortiz, Dra. Pilar Puebla Ibáñez","doi":"10.17533/UDEA.VITAE.V28N2A343923","DOIUrl":"https://doi.org/10.17533/UDEA.VITAE.V28N2A343923","url":null,"abstract":"Background: Ayanin (3,7,4’-Tri-O-methylquercetin) and 3,7-Di-O-methylquercetin (DMQ) are the main active metabolites isolated by bioguided fractionation from Croton schiedeanus, species known popularly in Colombia as “almizclillo”, which has been studied in experimental models in rats, exerting vasodilator and antihypertensive effects. Also, when the effect of these flavonoids was studied separately, important vasodilation was observed. Objective: To evaluate whether flavonoids from Croton schiedeanus have synergistic vasodilator properties when different combinations are used in isolated aorta rings. Methods: Cumulative concentrations of ayanin (10-8 M - 6x10-5 M or 0.01 μM - 60 μM) were assayed in the absence and presence of an increasing concentration of 3,7-Di-O-methylquercetin (DMQ) (10-8 – 3x10-5 M or 0.01–30 μM) in isolated rings from Wistar rats, pre-contracted with phenylephrine. The concentration-response curve with the maximal effect was compared with that obtained by Croton schiedeanus whole ethanolic extract (10-6 – 3x10-4 g/mL). Also, this combination was assayed in the presence of the nitric oxide synthetase inhibitor L-NAME (10-4 M) and the guanylate cyclase inhibitor methylene blue (10-4 M) to assess the role of the NO/cGMP pathway in this interaction. Results: Ayanin and DMQ display a dual interaction in vascular relaxant response: agonism at higher concentration ranges (10-6 – 3x10-5 M or 1–30 μM) and antagonism at lower concentration ranges (10-8 – 3x10-7 M or 0.01–0.3 μM). The efficacy at the highest concentration was greater than that obtained by the whole extract (Emax: 98.4% vs. 33.9%). This response was decreased but not reverted in the presence of L-NAME and methylene blue. Thus, the vasodilator effect of this combination does not depend entirely on the NO/cGMP cyclic pathway. Conclusion: The combined use of appropriate concentrations of these flavonoids could represent an advantage over Croton schiedeanus whole extract for vasodilator purposes.","PeriodicalId":51213,"journal":{"name":"Vitae","volume":"44 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73842872","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
In-vitro effect of the methanolic extract of Momordica charantia on hatching of eggs of Haemonchus sp. 苦瓜甲醇提取物对血螨卵体外孵化的影响。
Vitae Pub Date : 2021-04-08 DOI: 10.17533/udea.vitae.v28n1a345215
Dumar Alexander Jaramillo Hernández, Adolfo VÁSQUEZ TRUJILLO, Lida Carolina LESMES RODRÍGUEZ
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引用次数: 1
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