Microbial biotransformation of beclomethasone dipropionate by Aspergillus niger

Na pesquisa presente o fármaco esteróide antiasmático dipropionato de beclometasona foi submetido à biotransformação microbiana pelo Aspergillus niger. O dipropionato de beclometasona foi transformado, pela primeira vez, em metabólitos variados por biotransformação microbiana. Novos metabólitos do fármaco produzidos podem agir como novas moléculas potenciais e podem substituir os fármacos antigos em questão de segurança, eficácia e mínima resistência. Eles foram purificados por cromatografia em camada delgada preparativa e as suas estruturas foram elucidadas usando técnicas espectroscópicas modernas, como 13C NMR, 1H NMR; HMQC; HMQC; COSY, NOESY e espectrometria de massas, por exemplo, EI-MS. Purificaram-se quatro metabólitos, denominados (i) 17-monopropionato de beclometasona; (ii) 21-monopropionato de beclometasona: (iii) beclometasona e (iv) 21-propionato de 9beta,11beta-epoxi-17,21-diidroxi-16beta-metilpregna-1,4-dieno-3,20-diona.In the present research, the steroidal anti-asthmatic drug beclomethasone dipropionate was subjected to microbial biotransformation by Aspergillus niger. Beclomethasone dipropionate was transformed into various metabolites first time from microbial transformation. New drug metabolites produced can act as new potential drug molecules and can replace the old drugs in terms of safety, efficacy, and least resistance. They were purified by preparative thin layer chromatography technique, and their structures were elucidated using modern spectroscopic techniques, such as 13C NMR, 1H NMR, HMQC, HMQC, COSY, and NOESY, and mass spectrometry, such as EI-MS. Four metabolites were purified: (i) beclomethasone 17-monopropionate, (ii) beclomethasone 21-monopropionate, (iii) beclomethasone, and (iv) 9beta,11beta-epoxy-17,21-dihydroxy-16beta-methylpregna-1,4-diene-3,20-dione 21-propionate

Use of Dark Chocolate for Diabetic Patients: A Review of the Literature and Current Evidence

Dietary changes are a major lifestyle factor that can influence the progression of chronic diseases such as diabetes. Recently, flavanols, a subgroup of plant-derived phytochemicals called flavonoids, have gained increasing attention, due to studies showing an inverse correlation between dietary intake of flavanols and incidence of diabetes. Flavanoids in the cocoa plant may ameliorate insulin resistance by improving endothelial function, altering glucose metabolism, and reducing oxidative stress. Oxidative stress has been proposed as the main culprit for insulin resistance. The well-established effects of cocoa on endothelial function also points to a possible effect on insulin sensitivity. The relationship between insulin resistance and endothelial function is a reciprocal one. Overall, the evidence from these studies suggests that cocoa may be useful in slowing the progression to type 2 diabetes and ameliorating insulin resistance in metabolic syndrome. Additionally, results from several small studies indicate that cocoa may also have therapeutic potential in preventing cardiovascular complications in diabetic patients. Studies highlighting the potential of cocoa-containing diets, in large-randomized controlled trials should be performed which might give us a better opportunity to analyze the potential health-care benefit for reducing the risk of complications in diabetic patients at molecular level

In vitro Studies on Anti-diabetic and Anti-ulcer Potentials of Jatropha gossypifolia (Euphorbiaceae)

Purpose: To evaluate α-glucosidase and α-chymotrypsin enzyme inhibitory activity of Jatropha gossypifolia as a probable remedy for the management of diabetes and ulcer.Methods: Different extracts and fractions of the root, leaf and stem bark of the plant were screened for their α-glucosidase and α-chymotrypsin inhibitory activity using standard in vitro inhibition assays. Acarbose and chymostatin were used as positive control, respectively.Results: n-Butanol and ethyl acetate fraction showed maximum enzyme inhibition for α-glucosidase with 67.93 ± 0.66 and 67.67 ± 0.71 % and half maximal concentration (IC50) of 218.47 ± 0.23 and 213.45 ± 0.12 μg/ml, respectively. Dichloromethane and ethyl acetate leaf fractions exhibited maximum α-chymotrypsin inhibition activity of 85.08 ± 0.38 and 83.87 ± 0.70 %, and IC50 of 133.1 ± 0.68 and 134.5 ± 0.12 μg/ml, respectively, Acarbose exhibited enzyme inhibition activity of 92.14 ± 0.38 % with IC50 of 38.24 ± 0.1 μg/ml, while chymostatin exhibited 93.67 ± 0.38 % enzyme inhibition and IC50 of 8.24 ± 0.11 μg/ml.Conclusion: The presence of bioactive secondary metabolities with enzyme-inhibiting activity lends some support for the traditional use of this plant in the management of diabetes and ulcer. However, further investigation of the plant including identification of its active components is required.Keywords: α-Chymotrypsin, α-Glucosidase, Inhibition, Jatropha gossypifolia, Anti-diabetic, Anti-ulce

Arsenic speciation and biotransformation pathways in the aquatic ecosystem: The significance of algae

© 2020 Elsevier B.V. The contamination of aquatic systems with arsenic (As) is considered to be an internationally-important health and environmental issue, affecting over 115 countries globally. Arsenic contamination of aquatic ecosystems is a global threat as it can enter the food chain from As-rich water and cause harmful impacts on the humans and other living organisms. Although different factors (e.g., pH, redox potential, iron/manganese oxides, and microbes) control As biogeochemical cycling and speciation in water systems, the significance of algal species in biotransformation of As is poorly understood. The overarching attribute of this review is to briefly elaborate various As sources and its distribution in water bodies and factors affecting As biogeochemical behavior in aqueous ecosystems. This review elucidates the intriguing role of algae in biotransformation/volatilization of As in water bodies under environmentally-relevant conditions. Also, we critically delineate As sorption, uptake, oxidation and reduction pathways of As by algae and their possible role in bioremediation of As-contaminated water (e.g., drinking water, wastewater). The current review provides the updated and useful framework for government and water treatment agencies to implement algae in As remediation programs globally

Efficacy and Safety of Whey Protein Supplements on Vital Sign and Physical Performance Among Athletes: A Network Meta-Analysis

Introduction: Athletes train physically to reach beyond their potential maximum aerobic threshold. Whey protein supplements (WPS) are often used in conjunction with physiotherapy and psychotherapy to regain better vital sign and physical performances. This review aimed to explore the clinical evidence on the efficacy and safety of WPS in sports performance and recovery among athletes.Methodology: A comprehensive literature search was performed to identify relevant randomized control trials (RCTs) that investigated the efficacy and safety of WPS on the vital sign and physical performance among athletes. The Cochrane Risk of Bias (ROB) Assessment tools were used to assess the quality of the studies. Meta-analysis was conducted using the frequentist model with STATA version 14.2®.Results: A total of 333,257 research articles were identified out of which 20 RCTs were included for qualitative synthesis and network meta-analysis with 351 participants. Among the studies, 7 had low ROB and 3 RCTs had high ROB. Of these 20 trials, 16 trials were randomized clinical trials which compared whey protein supplements (WPS) with various comparators i.e., L-alanine, bovine colostrum, carbohydrate, casein, leucine, maltodextrin, rice, protein + caffeine were compared with placebo. Analysis from the pairwise meta-analysis revealed that for respiratory exchange ratio (RER) WPS was found to be significantly improving compared to maltodextrin (WMD = 0.012; 95%CI = 0.001, 0.023). Similarity to RPE (Rate Perceived Exertion), slight difference between WPS and the comparators, however, when the estimation was favorable to the comparators, there was moderate-high heterogeneity. For VO2max, high heterogeneity appeared when WPS compared to maltodextrin with the I2 = 97.8% (WMD = 4.064; 95% CI = −4.230, 12.359), meanwhile bovine colostrum (WMD = −2.658; 95%CI = −6.180, 0.865) only comparator that was better than WPS. According to the estimated effect of the supplements on physical performance outcome results, maximum power (8 studies, 185 athletes), highest ranked was bovine colostrum (SUCRA = 70.7%) and the lowest ranked was placebo (SUCRA = 17.9%), yet all insignificant. Then again, on average power (nine studies, 187 athletes), WPS was the highest ranked (SUCRA = 75.4 %) about −112.00 watt (−187.91, −36.08) and most of the estimations were significant. Body mass was reported in 10 studies (171 athletes), carbohydrate may be at the highest ranked (SUCRA = 66.9%) but it is insignificant. Thought the second highest ranked was WPS (SUCRA = 64.7%) and it is significant (WMD = −6.89 kg; CI = −8.24, −5.54).Conclusion: The findings of this review support the efficacy and safety of WPS as an ergogenic aid on athletes' sports performance and recovery. The overall quality of clinical evidence was found to be valid and reliable from the comprehensive search strategy and ROB assessment

AN ESTIMATION OF TECHNICAL EFFICIENCY OF GARLIC PRODUCTION IN KHYBER PAKHTUNKHWA PAKISTAN

This study was conducted to estimate the technical efficiency of farmers in garlic production in Khyber Pakhtunkhwa province, Pakistan. Data was randomly collected from 110 farmers using multistage sampling technique. Maximum likelihood estimation technique was used to estimate Cob-Douglas frontier production function. The analysis revealed that the estimated mean technical efficiency was 77 percent indicating that total output can be further increased with efficient use of resources and technology. The estimated gamma value was found to be 0.93 which shows 93% variation in garlic output due to inefficiency factors. The analysis further revealed that seed rate, tractor hours, fertilizer, FYM and weedicides were positive and statistically significant production factors. The results also show that age and education were statistically significant inefficiency factors, age having positive and education having negative relationship with the output of garlic. This study suggests that in order to increase the production of garlic by taking advantage of their high efficiency level, the government should invest in the research and development aspects for introducing good quality seeds to increase garlic productivity and should organize training programs to educate farmers about garlic production

AN ESTIMATION OF TECHNICAL EFFICIENCY OF GARLIC PRODUCTION IN KHYBER PAKHTUNKHWA PAKISTAN

This study was conducted to estimate the technical efficiency of farmers in garlic production in Khyber Pakhtunkhwa province, Pakistan. Data was randomly collected from 110 farmers using multistage sampling technique. Maximum likelihood estimation technique was used to estimate Cob-Douglas frontier production function. The analysis revealed that the estimated mean technical efficiency was 77 percent indicating that total output can be further increased with efficient use of resources and technology. The estimated gamma value was found to be 0.93 which shows 93% variation in garlic output due to inefficiency factors. The analysis further revealed that seed rate, tractor hours, fertilizer, FYM and weedicides were positive and statistically significant production factors. The results also show that age and education were statistically significant inefficiency factors, age having positive and education having negative relationship with the output of garlic. This study suggests that in order to increase the production of garlic by taking advantage of their high efficiency level, the government should invest in the research and development aspects for introducing good quality seeds to increase garlic productivity and should organize training programs to educate farmers about garlic production

Global scale arsenic pollution : increase the scientific knowledge to reduce human exposure

La contamination de l'eau par l'arsenic constitue un défi sanitaire et scientifique crucial à l’échelle globale. Des concentrations en arsenic supérieures à la limite recommandée par l'organisation mondiale de la santé (10 μg / L) ont été fréquemment trouvées dans les eaux souterraines de plusieurs pays du monde et des millions de personnes ont ainsi été exposées à l’arsenic. Dans ce contexte, l’objectif de cette communication est de fournir une synthèse de connaissances interdisciplinaires récentes sur l'arsenic, en particulier pour les jardiniers et agriculteurs urbains qui peuvent être confrontés à la pollution des eaux des puits ou des légumes produits. Les origines, les formes chimiques, les voies de transfert de l'arsenic et son impact sur la santé humaine sont discutés. L’arsenic d’origine géogénique représente une menace sanitaire majeure pour la santé dans de nombreux pays, notamment en Asie. Des conseils sont donc finalement proposés pour éviter et réduire l'exposition humaine à l'arsenic dans le contexte des agricultures urbaines.Arsenic contamination in water is a crucial human health and scientific challenge worldwide. Actually, high As levels above the recommended limit set by world health organization (10 µg/L) have been found in ground water of several countries around the world and millions of people have been exposed to As contaminated drinking water. The aim of the present paper is therefore to provide a synthesis of recent interdisciplinary knowledge on arsenic, in particular for urban gardeners and farmers who may be confronted with well water pollution or contamination of produced vegetables. The origins, chemical forms, routes of arsenic transfer and its impact on human health are discussed. Geogenic As contamination represents a major health threat in many countries, especially Asia. Advices are therefore finally proposed to avoid and reduce human exposure to arsenic in the context of urban agricultures