Increased yield of biotransformation of exemestane with β-cyclodextrin complexation technique

Li, Guang; Li, Fu‐Shuang; Deng, Le; Fang, Xiaolan; Zou, Hui; Xu, Kangpin; Li, Tian; Tan, Gui‐Shan

doi:10.1016/j.steroids.2013.07.009

Cited by 9 publications

(3 citation statements)

References 10 publications

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“…[31]. In comparison with the earlier reports of bioconversion of 6-MeAD to exemestane by A. simplex in xylene-water two-phase system [32] and β-cyclodextrin complexation technique [33], higher bioconversion was achieved in the present work.…”

Section: Discussionsupporting

confidence: 69%

Substrate Carriers for C-1(2)-Dehydrogenation of 6-Methylene Androstenedione to Exemestane by Growing and Immobilized Arthrobacter Simplex Ncim 2449

Patil

Sharma

Banerjee

et al. 2017

Asian J Pharm Clin Res

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Objective: Permeability of hydrophobic steroid substrates across cell membrane is a critical factor during microbial bioconversion. To increase substrate intake, the feasibility of some organic solvents and emulsifiers as a substrate carrier on the bioconversion of 6-methylene androstenedione (6-MeAD) to exemestane was assessed.Methods: AD, a commonly available steroid precursor, was chemically converted 6-MeAD. The time course of exemestane accumulation was estimated after addition of 6-MeAD dissolved in some organic solvents or dispersed with emulsifiers by growing and immobilized cells of Arthrobacter simplex NCIM 2449 in shake flask cultures. Results Conclusion:The use of substrate carriers for addition of 6-MeAD increased the permeability of substrate and may be used to increase the yield of exemestane and reduce incubation time.

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Section: Discussionsupporting

confidence: 69%

Substrate Carriers for C-1(2)-Dehydrogenation of 6-Methylene Androstenedione to Exemestane by Growing and Immobilized Arthrobacter Simplex Ncim 2449

Patil

Sharma

Banerjee

et al. 2017

Asian J Pharm Clin Res

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“…A notable difference we distinguish on EXE chemical structure which is a steroidal neutral compound. There are published studies related to the complexation of EXE with β-CD derivatives in terms of increased aqueous solubility of drug, higher dissolution rate and intestinal permeation [27][28][29]. Thereby is very probable that EXE could form a complex more soluble with CM-β-CD from the BGE and that may explain the longest migration time.…”

Section: Resultsmentioning

confidence: 99%

Determination of letrozole, anastrozole and exemestane by capillary zone electrophoresis

Rusu¹,

Hancu²,

Berța³

et al. 2017

Studia UBB Chemia

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ABSTRACT.A new validated capillary zone electrophoresis method was developed for the quantification of three aromatase inhibitors -anastrozole, letrozole and exemestane. After preliminary analysis a sodium tetraborate background electrolyte containing carboxymethyl β-cyclodextrine was selected for the simultaneous determination of the three aromatase inhibitors. 100 mM sodium tetraborate containing 5 mM carboxymethyl β-cyclodextrine as buffer addtive, 25 kV applied voltage, 20 mbar/2 s injection pressure and 25°C temperature were selected as optimum parameters for the determination. Analysis was performed in approximately 10 minutes. Validation parameters, including linearity, precision, detection and quantification limits were determined. Our results prove the applicability of capillary zone electrophoresis for the simultaneous determination of the three aromatase inhibitors from pharmaceutical products. The applicability of the optimized method was also tested for biological samples, proving its reliability for the determination of letrozole without any special treatment of the analyzed spiked urine sample and presenting potential for other biological matrices.

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“…Therefore, to improve the transformation yield, increased substrate solubility is required to promote its contact with the cells. Guang et al used cyclodextrin technology to increase substrate solubility and greatly improved the conversion yield of exemestane [28,29], which is an antitumour drug. Moreover, the dissolved oxygen in the fermentation liquid is a direct factor that influences substrate conversion.…”

Section: Discussionmentioning

confidence: 99%

Biotransformation of cholesterol and 16,17‐alpha epoxypregnenolone by novel Cladosporium sp. strain IS547

Pang

Cao

Zhu

2016

J. Basic Microbiol.

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Nowadays, there are a few steroid drugs or intermediates that have been obtained via the transformation of microorganisms, and many strains of transformed steroids have not been found yet. Therefore, it is very significant to screen for the strains that have the abilities to transform steroids to produce valuable products. This study has focused on the screen and identification of strains, the structural identification of converted products, and the optimization of transformation conditions, as well as the establishment of transformation systems. A soil microbiota was screened for strain involved in the biotransformation of steroids. A new isolate IS547 is capable of converting a variety of steroids (such as cholesterol, ergosterol, hydrocortisone, progesterone, pregnenolone, and 16,17-alpha-epoxypregnenolone). Based on the 18S rDNA gene sequence comparison, the isolate IS547 has been demonstrated to be very closely related to Cladosporium sp. genus. Present paper is the first report regarding the microbial transformation by Cladosporium sp. to produce active intermediates, which include 7-hydroxy cholesterol, 20-droxyl-16α,17α-epoxypregna-4-dien-3-one, 7-ketocholesterol, and 7-droxyl-16α,17α-epoxypregna-4-dien-3,20-dione. Under the optimum conditions, the yields of product 3 and product 4 were 20.58 and 17.42%, respectively, higher than that prior to the optimization. The transformation rate increased significantly under the optimum fermentation conditions. This study describes an efficient, rapid, and inexpensive biotransformation system for the production of active pharmaceutical intermediates.

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Increased yield of biotransformation of exemestane with β-cyclodextrin complexation technique

Cited by 9 publications

References 10 publications

Substrate Carriers for C-1(2)-Dehydrogenation of 6-Methylene Androstenedione to Exemestane by Growing and Immobilized Arthrobacter Simplex Ncim 2449

Substrate Carriers for C-1(2)-Dehydrogenation of 6-Methylene Androstenedione to Exemestane by Growing and Immobilized Arthrobacter Simplex Ncim 2449

Determination of letrozole, anastrozole and exemestane by capillary zone electrophoresis

Biotransformation of cholesterol and 16,17‐alpha epoxypregnenolone by novel Cladosporium sp. strain IS547

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