scholarly journals Engineering the Steroid Hydroxylating System from Cochliobolus lunatus in Mycolicibacterium smegmatis

2021 ◽  
Vol 9 (7) ◽  
pp. 1499
Author(s):  
Carmen Felpeto-Santero ◽  
Beatriz Galán ◽  
José Luis García
Keyword(s):  
Cytochrome P450 ◽  
Commercial Production ◽  
Industrial Scale ◽  
Shuttle Plasmid ◽  
Cochliobolus Lunatus ◽  
Anti Inflammatory ◽  
High Yields ◽  
Synthetic Operon

14α-hydroxylated steroids are starting materials for the synthesis of contraceptive and anti-inflammatory compounds in the steroid industry. A synthetic bacterial operon containing the cytochrome P450 CYP103168 and the reductase CPR64795 of the fungus Cochlioboluslunatus able to hydroxylate steroids has been engineered into a shuttle plasmid named pMVFAN. This plasmid was used to transform two mutants of Mycolicibacterium smegmatis named MS6039-5941 and MS6039 that accumulate 4-androstene-3,17-dione (AD), and 1,4-androstadiene-3,17-dione (ADD), respectively. The recombinant mutants MS6039-5941 (pMVFAN) and MS6039 (pMVFAN) were able to efficiently express the hydroxylating CYP system of C.lunatus and produced in high yields 14αOH-AD and 14αOH-ADD, respectively, directly from cholesterol and phytosterols in a single fermentation step. These results open a new avenue for producing at industrial scale these and other hydroxylated steroidal synthons by transforming with this synthetic operon other Mycolicibacterium strains currently used for the commercial production of steroidal synthons from phytosterols as feedstock.

The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
Author(s):  
Ghodsi M. Ziarani ◽  
Fatemeh Mohajer ◽  
Razieh Moradi ◽  
Parisa Mofatehnia
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Microtubule Assembly ◽  
Heterocyclic Molecules ◽  
Biological Perspective ◽  
Highly Active ◽  
Anti Inflammatory ◽  
High Yields ◽  
Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

Novel Metabolic Bioactivation Mechanism for a Series of Anti-Inflammatory Agents (2,5-Diaminothiophene Derivatives) Mediated by Cytochrome P450 Enzymes

2010 ◽  
Vol 38 (9) ◽  
pp. 1522-1531 ◽  
Author(s):  
Yiding Hu ◽  
Shengtian Yang ◽  
F. Barclay Shilliday ◽  
Bruce R. Heyde ◽  
Kathy M. Mandrell ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 Enzymes ◽  
Anti Inflammatory

scholarly journals Complete Genome Sequence of an Efficient Vitamin D3-Hydroxylating Bacterium, Pseudonocardia autotrophica NBRC 12743

2018 ◽  
Vol 7 (12) ◽  
Author(s):  
Keitaro Yoshida ◽  
Yoshiaki Yasutake ◽  
Tomohiro Tamura
Keyword(s):  
Vitamin D ◽  
Cytochrome P450 ◽  
Genome Sequence ◽  
Vitamin D3 ◽  
Complete Genome Sequence ◽  
Complete Genome ◽  
Commercial Production ◽  
Content Type ◽  
Hydroxyvitamin D

Pseudonocardia autotrophica NBRC 12743 contains a cytochrome P450 vitamin D3 hydroxylase, and it is used as a biocatalyst for the commercial production of hydroxyvitamin D3, a valuable compound for medication. Here, we report the complete genome sequence of P. autotrophica NBRC 12743, which could be useful for improving the productivity of hydroxyvitamin D3.

scholarly journals Acute and Chronic Toxicity, Cytochrome P450 Enzyme Inhibition, and hERG Channel Blockade Studies with a Polyherbal, Ayurvedic Formulation for Inflammation

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Debendranath Dey ◽  
Sunetra Chaskar ◽  
Nitin Athavale ◽  
Deepa Chitre
Keyword(s):  
Cytochrome P450 ◽  
Radioligand Binding ◽  
Curcuma Longa ◽  
Raw 264.7 Cells ◽  
Cytochrome P450 Enzyme ◽  
Sprague Dawley ◽  
Cytochrome P450 Enzymes ◽  
Boswellia Serrata ◽  
Cell Counts ◽  
Anti Inflammatory

Ayurvedic plants are known for thousands of years to have anti-inflammatory and antiarthritic effect. We have recently shown that BV-9238, a proprietary formulation ofWithania somnifera, Boswellia serrata, Zingiber officinale,andCurcuma longa,inhibits LPS-induced TNF-alpha and nitric oxide production from mouse macrophage and reduces inflammation in different animal models. To evaluate the safety parameters of BV-9238, we conducted a cytotoxicity study in RAW 264.7 cells (0.005–1 mg/mL) by MTT/formazan method, an acute single dose (2–10 g/kg bodyweight) toxicity study and a 180-day chronic study with 1 g and 2 g/kg bodyweight in Sprague Dawley rats. Some sedation, ptosis, and ataxia were observed for first 15–20 min in very high acute doses and hence not used for further chronic studies. At the end of 180 days, gross and histopathology, blood cell counts, liver and renal functions were all at normal levels. Further, a modest attempt was made to assess the effects of BV-9238 (0.5 µg/mL) on six major human cytochrome P450 enzymes and3H radioligand binding assay with human hERG receptors. BV-9238 did not show any significant inhibition of these enzymes at the tested dose. All these suggest that BV-9238 has potential as a safe and well tolerated anti-inflammatory formulation for future use.

scholarly journals Active Anti-Inflammatory and Hypolipidemic Derivatives of Lorazepam

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3277
Author(s):  
Panagiotis Theodosis-Nobelos ◽  
Georgios Papagiouvannis ◽  
Panos N. Kourounakis ◽  
Eleni A. Rekka
Keyword(s):  
Acute Inflammation ◽  
Current Knowledge ◽  
Rat Plasma ◽  
Straightforward Method ◽  
Inflammatory Drugs ◽  
Multifunctional Agents ◽  
Anti Inflammatory ◽  
High Yields ◽  
Derivatives Of ◽  
And Oxidative Stress

Novel derivatives of some non steroidal anti-inflammatory drugs, as well as of the antioxidants α-lipoic acid, trolox and (E)-3-(3,5-di-tert-butyl-4-hydroxyphenyl)acrylic acid with lorazepam were synthesised by a straightforward method at satisfactory to high yields (40%–93%). All the tested derivatives strongly decreased lipidemic indices in rat plasma after Triton induced hyperlipidaemia. They also reduced acute inflammation and a number of them demonstrated lipoxygenase inhibitory activity. Those compounds acquiring antioxidant moiety were inhibitors of lipid peroxidation and radical scavengers. Therefore, the synthesised compounds may add to the current knowledge about multifunctional agents acting against various disorders implicating inflammation, dyslipidaemia and oxidative stress.

scholarly journals Convenient Synthesis and Biological Activity of 4-minomethylene 1-phenylpyrazolidine-3,5-diones

2017 ◽  
Vol 59 (3) ◽  
Author(s):  
Eman A. Ahmed
Keyword(s):  
Biological Activity ◽  
Nucleophilic Substitution ◽  
Hydrazine Hydrate ◽  
New Products ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Dimethylamino Group ◽  
Convenient Synthesis ◽  
Anti Inflammatory ◽  
High Yields

Reaction of (<em>Z</em>)-4-((dimethylamino)methylene)-1-phenylpyrazolidine-3,5-dione (<strong>1</strong>) with different nucleophiles is described. Treatment of enaminone <strong>1 </strong>with phenylhydrazine led to 3-oxo-<em>N’</em>,2-diphenyl-2,3-dihydro-1<em>H</em>-pyrazole-4-carbohydrazide <strong>7</strong>. New enaminone derivatives <strong>2–6 </strong>and <strong>12–14 </strong>were conveniently obtained in high yields via nucleophilic substitution of the dimethylamino group in enaminone <strong>1 </strong>when reacted with <em>o</em>-aminophenol, <em>o</em>-aminothiophenol, ethanolamine, cysteamine hydrochloride, piperidine, morpholine, 2-aminopyridine and glycine. Reaction of enaminone <strong>1 </strong>with diaza-nucleophiles, such as hydrazine hydrate, ethylenediamine and <em>o</em>-phenylenediamine, afforded the corresponding <em>bis</em>-enaminones <strong>9–11</strong>. Anti-inflammatory and antimicrobial activities of some new products were evaluated. Compounds <strong>1, 2, 4, 7, 12a</strong>, and <strong>12b </strong>showed high anti- inflammatory activity compared with indomethacin as the reference, while the highest antimicrobial effect was observed in the case of compound <strong>3</strong>.

Nutrition and Fertilization Practices for Southern Highbush Blueberry in Florida

EDIS ◽  
2020 ◽  
Vol 2020 (1) ◽  
Author(s):  
Doug Phillips ◽  
Jeffrey G. Williamson
Keyword(s):  
Plant Nutrition ◽  
Field Experience ◽  
Commercial Production ◽  
Highbush Blueberry ◽  
Southern Highbush ◽  
High Yields

Research and field experience have demonstrated that fertilization is necessary to achieve proper growth and high yields in cultivated production of blueberries. This new 7-page publication of the UF/IFAS Horticultural Sciences Department provides guidance and management suggestions to Florida growers of southern highbush blueberry (SHB) for monitoring, supplying, and maintaining proper plant nutrition in commercial production operations. Written by Doug Phillips and Jeffrey G. Williamson. https://edis.ifas.ufl.edu/hs1356

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