- Spectroscopic evaluation of synthesized 5β-dihydrocortisol and 5β-dihydrocortisol acetate binding mechanism with human serum albumin and their role in anticancer activity
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Our study focus on the biological importance of synthesized 5β-dihydrocortisol (Dhc) and 5β-dihydrocortisol acetate (DhcA) molecules, the cytotoxic study was performed on breast cancer cell line (MCF-7) normal human embryonic kidney cell line (HEK293), th
- Kallubai, Monika,Reddy, Srinivasa P.,Dubey, Shreya,Ramachary, Dhevalapally B.,Subramanyam, Rajagopal
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- NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
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Described herein are neuroactive steroids of the Formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof; wherein R1a and R1b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
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Page/Page column 87
(2015/02/02)
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- Direct organocatalytic stereoselective transfer hydrogenation of conjugated olefins of steroids
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Kinetically controlled and organocatalytic syn-selective transfer hydrogenation has been successfully demonstrated for the reduction of the enone functional group of various steroids. Herein, diastereoselective synthesis of many 5β-steroids have been reported through organocatalysis, which have broad medicinal and pharmaceutical applications. The mechanistic studies and the selectivity of the products clearly indicated that the catalyst 1b·d-CSA is mild enough to activate the various chiral cyclic enones through iminium ion formation during the organocatalytic transfer hydrogenations with Hantzsch ester 2a as a hydrogen source. Further, clear evidence for the selective formation of intermediate iminium species [I]+ have been characterized through on-line monitoring of controlled experiments by NMR and ESI-HRMS analyses.
- Ramachary, Dhevalapally B.,Sakthidevi, Rajasekar,Reddy, P. Srinivasa
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p. 13497 - 13506
(2013/09/02)
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- METHODS FOR THE PURIFICATION OF DEOXYCHOLIC ACID
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Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12-α-hydroxy-steroids from Δ-9,11-ene, 11-keto or 11-hydroxy-β-steroids. This invention is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.
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Paragraph 0315; 0316
(2013/06/05)
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- METHODS FOR THE PURIFICATION OF DEOXYCHOLIC ACID
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Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12-α-hydroxysteroids from Δ-9,11-ene, 11-keto or 11-hydroxy-β-steroids. This invention is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.
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Page/Page column 67-68
(2011/07/07)
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- Molecular cloning and heterologous expression of progesterone 5β-reductase from Digitalis lanata Ehrh.
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A full-length cDNA clone that encodes progesterone 5β-reductase (5β-POR) was isolated from Digitalis lanata leaves. The reading frame of the 5β-POR gene is 1170 nucleotides corresponding to 389 amino acids. For expression, a Sph1/Sal1 5β-POR fragment was cloned into the pQE vector and was transformed into Escherichia coli strain M15[pREP4]. The recombinant gene was functionally expressed and the recombinant enzyme was characterized. The Km and vmax values for the putative natural substrate progesterone were calculated to be 0.120 mM and 45 nkat mg-1 protein, respectively. Only 5β-pregnane-3,20-dione but not its α-isomer was formed when progesterone was used as the substrate. Kinetic constants for cortisol, cortexone, 4-androstene-3,17-dione and NADPH were also determined. The molecular organization of the 5β-POR gene in D. lanata was determined by Southern blot analysis. The 5β-POR is highly conserved within the genus Digitalis and the respective genes and proteins share considerable homology to putative progesterone reductases from other plant species.
- Herl, Vanessa,Fischer, Gabriele,Müller-Uri, Frieder,Kreis, Wolfgang
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p. 225 - 231
(2008/02/09)
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