Prednisone and prednisolone are steroids widely used as anti-inflammatory drugs. Development of the pharmaceutical industry is currently aimed at introducing biotechnological processes and replacing ...multiple-stage chemical syntheses. In this work we evaluated the ability of bacteria belonging to the
genus to biotransform substrates, such as cortisone and hydrocortisone, to obtain prednisone and prednisolone, respectively. These products are of great interest from a pharmaceutical point of view as they have higher anti-inflammatory activity than the starting substrates. After an initial lab-scale screening of 13
strains, to select the highest producers of prednisone and prednisolone, we reported the 200 ml-batch scale-up to test the process efficiency and productivity of the most promising
strains.
,
and
gave the Δ1-dehydrogenation products of cortisone and hydrocortisone (prednisone and prednisolone) in variable amounts. In these biotransformations, the formation of products with the reduced carbonyl group in position C
of the lateral chain of the steroid nucleus was also observed (i.e., 20β-hydroxy-prednisone and 20β-hydroxy-prednisolone). The yields, the absence of collateral products, and in some cases the absence of starting products allow us to say that cortisone and hydrocortisone are partly degraded.
A Berlino nel 1815 l’epigrafia greca entra ufficialmente a far parte delle scienze dell’antichità con l’inaugurazione di un Thesaurus di tutte le iscrizioni greche allora note sotto la direzione del ...filologo August Boeckh. Nel Corpus Inscriptionum Graecarum (CIG), dal 1902 denominato Inscriptiones Graecae (IG), si realizza la visione leibniziana di imprese scientifiche che all‘interno di Accademie coniughino «theoria cum praxi ». Dopo aver attraversato due secoli di alterne vicende connesse con le dinamiche storico-politiche della Germania, l’impresa IG possiede oggi l’archivio epigrafico più ricco del mondo e prosegue il suo lavoro con numerosi progetti in corso, di cui è tracciato un sintetico report.
Phytopathogenic fungi are among the main causes of productivity losses in agriculture. To date, synthetic chemical pesticides, such as hydroxyanilides, anilinopyrimidines and azole derivatives, ...represent the main treatment tools for crop plant defence. However, the large and uncontrolled use of these substances has evidenced several side effects, namely the resistance to treatments, environmental damage and human health risks. The general trend is to replace chemicals with natural molecules in order to reduce these side effects. Moreover, the valorisation of agri-food industry by-products through biotransformation processes represents a sustainable alternative to chemical synthesis in several sectors. This research is aimed at comparing the anti-phytopathogenic activity of waste bovine and porcine bile with secosteroids obtained by biotransformation of bile acids with
strains. The ultimate goal is to apply these natural products on food crops affected by phytopathogenic fungi.
Bile acids (BAs) are a family of steroids synthesized from cholesterol in the liver. Among bile acids, ursodeoxycholic acid (UDCA) is the drug of choice for treating primary biliary cirrhosis and ...dissolving cholesterol gallstones. The clinical effectiveness of UDCA includes its choleretic activity, the capability to inhibit hydrophobic bile acid absorption by the intestine under cholestatic conditions, reducing cholangiocyte injury, stimulation of impaired biliary output, and inhibition of hepatocyte apoptosis. Despite its clinical effectiveness, UDCA is poorly soluble in the gastro-duodeno-jejunal contents, and pharmacological doses of UDCA are not readily soluble in the stomach and intestine, resulting in incomplete absorption. Indeed, the solubility of 20 mg/L greatly limits the bioavailability of UDCA. Since the bioavailability of drug products plays a critical role in the design of oral administration dosages, we investigated the enzymatic esterification of UDCA as a strategy of hydrophilization. Therefore, we decided to enzymatically synthesize a glyceric ester of UDCA bile acid to produce a more water-soluble molecule. The esterification reactions between UDCA and glycerol were performed with an immobilized lipase B from Candida antarctica (Novozym 435) in solvent-free and solvent-assisted systems. The characterization of the UDCA-monoglyceride, enzymatically synthesized, has been performed by 1H-NMR, 13C-NMR, COSY, HSQC, HMBC, IR, and MS spectroscopy.
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) introduced in the 1960s and widely used as an analgesic, anti-inflammatory, and antipyretic. In its acid form, the solubility of 21 mg/L ...greatly limits its bioavailability. Since the bioavailability of a drug product plays a critical role in the design of oral administration dosage, this study investigated the enzymatic esterification of ibuprofen as a strategy for hydrophilization. This work proposes an enzymatic strategy for the covalent attack of highly hydrophilic molecules using acidic functions of commercially available bioactive compounds. The poorly water-soluble drug ibuprofen was esterified in a hexane/water biphasic system by direct esterification with sorbitol using the cheap biocatalyst porcine pancreas lipase (PPL), which demonstrated itself to be a suitable enzyme for the effective production of the IBU-sorbitol ester. This work reports the optimization of the esterification reaction.
Bivalves aquaculture is already considered a very sustainable for of food production and might become an essential pillar on which to develop future global food security. However, with the increase ...in production, a correspondingly great amount of waste will be produced all around the earth, principally in the form of shells, which can represent up to 90% of the fresh mollusk weight. Nowadays, shell waste has no notable use and is commonly regarded as waste, often dumped in landfill, or thrown back into the sea, causing a significant level of environmental concern, and resulting in a loss of natural and valuable resources. Bivalve shells are mainly formed by CaCO3, giving them the potential to become a promising secondary raw material for several applications, from a circular economy perspective. This paper aims to review the scientific literature of the last twenty years and the principal recent trends in shell waste reuse, describing applications that are already in place on a large scale in agriculture and livestock, soils, water and wastewater remediation, biodiesel production and biofilters, as well as niche applications that now simply have the potential to be scaled up.
Biocatalyzed synthesis can be exploited to produce high-value products, such as prodrugs. The replacement of chemical approaches with biocatalytic processes is advantageous in terms of environmental ...prevention, embracing the principles of green chemistry. In this work, we propose the covalent attachment of xylitol to ibuprofen to produce an IBU-xylitol ester prodrug. Xylitol was chosen as a hydrophilizer for the final prodrug, enhancing the water solubility of ibuprofen. Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) extensively used as an analgesic, anti-inflammatory, and antipyretic. Despite being the third-most-prescribed medicine in the world, the aqueous solubility of ibuprofen is just 21 mg/L. This poor water solubility greatly limits the bioavailability of ibuprofen. We aimed to functionalize ibuprofen with xylitol using the reusable immobilized N435 biocatalyst. Instead of a biphasic media, we proposed a monophasic reaction environment. The characterization of the IBU-xylitol ester was performed by
H,
C-NMR, DEPT, COSY, HMQC, HMBC, FTIR, and MS spectroscopy. Preliminary in vitro tests showed that this enzymatically synthesized prodrug of ibuprofen reduced the expression of the interleukin 8 genes in human bronchial epithelial cells (IB3-1) from cystic fibrosis (CF) patients.
Cortisone is a steroid widely used as an anti-inflammatory drug able to suppress the immune system, thus reducing inflammation and attendant pain and swelling at the site of an injury. Due to its ...numerous side effects, especially in prolonged and high-dose therapies, the development of the pharmaceutical industry is currently aimed at finding new compounds with similar activities but with minor or no side effects. Biotransformations are an important methodology towards more sustainable industrial processes, according to the principles of "green chemistry". In this work, the biotransformation of cortisone with
DSM 43960 to give two new steroids, i.e., 1,9β,17,21-tetrahydoxy-4-methyl-19-nor-9β-pregna-1,3,5(10)-trien-11,20-dione and 1,9β,17,20β,21-pentahydoxy-4-methyl-19-nor-9β-pregna-1,3,5(10)-trien-11-one, is reported. These new steroids have been fully characterized.
Introduction: Lactic acid (LA) production from fossil resources is unsustainable owing to their depletion and environmental concerns. Thus, this study aimed to optimize the production of LA by ...Lactobacillus casei in a cultured medium containing fruit wastes (FWs) from agro-industries and second cheese whey (SCW) from dairy production, supplemented with maize steep liquor (MSL, 10% v/v) as the nitrogen source. Methods: The FWs were selected based on seasonal availability early summer (early ripening peach), full summer (melon), late summer (pear), and early autumn (apple) and SCW as annual waste. Small-scale preliminary tests as well as controlled fermenter experiments were performed to demonstrate the potential of using various food wastes as substrates for LA fermentation, except for apple pomace. Results and discussion: A 5-cycle repeated batch fermentation was conducted to optimize waste utilization and production, resulting in a total of 180.56 g/L of LA with a volumetric productivity of 0.88 g/L∙h. Subsequently, mechanical filtration and enzymatic hydrolysis were attempted. The total amount of LA produced in the 5-cycle repeated batch process was 397.1 g/L over 288 h, achieving a volumetric productivity of 1.32 g/L∙h. These findings suggest a promising biorefinery process for low-cost LA production from agri-food wastes.
The organic fraction of municipal solid waste (OFMSW) is recognized as a suitable substrate for the anaerobic digestion (AD) process and is currently considered a mature technology. A promising ...strategy to enhance biogas yield and productivity is the co-digestion of OFMSW with other organic biomass, such as green waste (GW), a mixture of leaves, grass, and woody materials originated from private yards and public greenspace management. The main limitation to the use of GW for biogas production is the high percentage of the lignocellulosic fraction, which makes necessary a pretreatment of delignification to dissolve the recalcitrant structure. In this study, a new strategy of sustainable bio-delignification using the white-rot fungi Bjerkandera adusta (BA) in comparison with other chemical pretreatments were investigated. Untreated and treated GW were, respectively, submitted to anaerobic co-digestion with OFMSW. AD processes were carried out in a lab-scale plant for 30 days in thermophilic conditions (55 °C). Biogas cumulative production was increased by about 100% in the case of treated GW compared with that of just OFMSW, from 145 to 289 Nm3 CH4/ton SV, and productivity almost doubled from 145 to 283 Nm3/ton FM * day. The measured average methane content values in the cumulative biogas were 55% from OFMSW and 54% from GW. Moreover, over 95% of the biogas was produced in 20 days, showing the potential opportunity to reduce the AD time.
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