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

Financial Development, Institutional Quality, and Environmental Degradation Nexus: New Evidence from Asymmetric ARDL Co-Integration Approach

The aim of this study is threefold; first, the study investigates the symmetric impact of trade openness, financial development, and institutional quality on environmental degradation and environmental sustainability. Second, the study examines the asymmetric relationship between financial development, institutional quality, and environmental degradation. Third, the study examines the asymmetric relationship between financial development, institutional quality, and environmental sustainability. For this purpose, the study utilized the data of Pakistan from 1996 to 2018. The study applied Augmented Dickey–Fuller (ADF), Phillips Parron (PP) and Zivote, and Andrews unit root test to check the properties of stationarity of the data. This study applied the Auto Regressive Distributive Lags (ARDL) model to investigate symmetric relationships while the Non-Linear Auto Regressive Distributive Lag Model (NARDL) approach is utilized to investigate the asymmetric relationship among variables. ARDL bounds testing approach utilized to investigate long-run co-integration while short-run dynamics have been investigated by applying the error correction method (ECM). This study found the significant long-run symmetric and asymmetric association of institutional quality (IQ) and financial development (FD) with environmental degradation (ED) and environmental sustainability. However, IQ- has an insignificant association with environmental sustainability. Moreover, dynamic multiplier analysis indicates that positive shock to FD and IQ has a stronger impact on environmental degradation while a positive or negative shock to FD; both have a stronger impact on environmental sustainability. However, a positive or negative shock to IQ has a smaller impact on environmental sustainability. Moreover, the study also found a significant long-run symmetric association of trade openness with environmental degradation and environmental sustainability. This study suggests that the quality of institutions, financial development, and trade openness is necessary to enhance the quality of the environment

Pneumococcal Conjugate Vaccine impact assessment in Bangladesh [version 1; referees: 1 approved, 2 approved with reservations]

The study examines the impact of the introduction of 10-valent Pneumococcal Conjugate Vaccine (PCV10) into Bangladesh’s national vaccine program. PCV10 is administered to children under 1 year-old; the scheduled ages of administration are at 6, 10, and 18 weeks. The study is conducted in ~770,000 population containing ~90,000 <5 children in Sylhet, Bangladesh and has five objectives: 1) To collect data on community-based pre-PCV incidence rates of invasive pneumococcal diseases (IPD) in 0-59 month-old children in Sylhet, Bangladesh; 2) To evaluate the effectiveness of PCV10 introduction on Vaccine Type (VT) IPD in 3-59 month-old children using an incident case-control study design. Secondary aims include measuring the effects of PCV10 introduction on all IPD in 3-59 month-old children using case-control study design, and quantifying the emergence of Non Vaccine Type IPD; 3) To evaluate the effectiveness of PCV10 introduction on chest radiograph-confirmed pneumonia in children 3-35 months old using incident case-control study design. We will estimate the incidence trend of clinical and radiologically-confirmed pneumonia in 3-35 month-old children in the study area before and after introduction of PCV10; 4) To determine the feasibility and utility of lung ultrasound for the diagnosis of pediatric pneumonia in a large sample of children in a resource-limited setting. We will also evaluate the effectiveness of PCV10 introduction on ultrasound-confirmed pneumonia in 3-35 month-old children using an incident case-control design and to examine the incidence trend of ultrasound-confirmed pneumonia in 3-35 month-old children in the study area before and after PCV10 introduction; and 5) To determine the direct and indirect effects of vaccination status on nasopharyngeal colonization on VT pneumococci among children with pneumonia.  This paper presents the methodology. The study will allow us to conduct a comprehensive and robust assessment of the impact of national introduction of PCV10 on pneumococcal disease in Bangladesh

Food Insecurity, Population Growth, Urbanization and Water Availability: The Role of Government Stability

To examine the impact of population growth, urbanization and water availability on food insecurity, this study utilized time series data for the period of 1990–2019, from World Development Indicators (WDI), Food and Agriculture Organization (FAO), and World Bank. The study applied an Auto-regressive distributive lag (ARDL) co-integration approach to test the hypothesized relationships among modeled variables. The study found a negative and significant association of water resources and agriculture research with food insecurity while urbanization and population growth has a significant and positive impact on food insecurity in the short-run as well as in the long-run period. Moreover, the study found that political stability has a negative and significant association with food insecurity in the short-run and long-run periods. Results also indicated that political stability significantly strengthens the relationship of water resources, and agriculture research with food insecurity while political stability weakens the relationship of urbanization and food insecurity significantly

A comprehensive phytochemical, biological, and toxicological studies of roots and aerial parts of <i>Crotalaria burhia</i> Buch.-Ham:An important medicinal plant

This study was designed to seek the phytochemical analysis, antioxidant, enzyme inhibition, and toxicity potentials of methanol and dichloromethane (DCM) extracts of aerial and root parts of Crotalaria burhia. Total bioactive content, high-performance liquid chromatography-photodiode array detector (HPLC-PDA) polyphenolic quantification, and ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS) analysis were utilized to evaluate the phytochemical composition. Antioxidant [including 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH)], 2,2′-azino-bis[3-ethylbenzothiazoline-6-sulfonic acid (ABTS), ferric reducing antioxidant power assay (FRAP), cupric reducing antioxidant capacity CUPRAC, phosphomolybdenum, and metal chelation assays] and enzyme inhibition [against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glucosidase, α-amylase, and tyrosinase] assays were carried out for biological evaluation. The cytotoxicity was tested against MCF-7 and MDA-MB-231 breast cell lines. The root-methanol extract contained the highest levels of phenolics (37.69 mg gallic acid equivalent/g extract) and flavonoids (83.0 mg quercetin equivalent/g extract) contents, and was also the most active for DPPH (50.04 mg Trolox equivalent/g extract) and CUPRAC (139.96 mg Trolox equivalent /g extract) antioxidant assays. Likewise, the aerial-methanol extract exhibited maximum activity for ABTS (94.05 mg Trolox equivalent/g extract) and FRAP (64.23 mg Trolox equivalent/g extract) assays. The aerial-DCM extract was noted to be a convincing cholinesterase (AChE; 4.01 and BChE; 4.28 mg galantamine equivalent/g extract), and α-glucosidase inhibitor (1.92 mmol acarbose equivalent/g extract). All of the extracts exhibited weak to modest toxicity against the tested cell lines. A considerable quantities of gallic acid, catechin, 4-OH benzoic acid, syringic acid, vanillic acid, 3-OH-4-MeO benzaldehyde, epicatechin, p-coumaric acid, rutin, naringenin, and carvacrol were quantified via HPLC-PDA analysis. UHPLC-MS analysis of methanolic extracts from roots and aerial parts revealed the tentative identification of important phytoconstituents such as polyphenols, saponins, flavonoids, and glycoside derivatives. To conclude, this plant could be considered a promising source of origin for bioactive compounds with several therapeutic uses

pH-sensitive docetaxel-loaded chitosan/thiolated hyaluronic acid polymeric nanoparticles for colorectal cancer - supplementary material

Supplementary figure 1Supplementary Table S1. Thiol group quantification assaySupplementary Table S2. Kinetic characteristics of DTX release from formulations of CS/SH-HA nanoparticlesSupplementary Table S3. An acute oral toxicity investigation for SH-HA nanoparticles with clinical outcomesSupplementary Table S4. Stability study of the thiolated NP formulation at different storage conditions for three months</p