Based on the heterocyclic core of bendamustine, four series (4a-g, 5a-f, 8a-b and 9a-b) of benzimidazole derivatives were designed and synthesized starting from 4-(1H-benzo[d]imidazol-2-yl)-4-oxobutanehydrazide. In the rational design of target molecules, the benzimidazole ring of bendamustine was retained and the bis-(chloroethyl) amine group (mechlorethamine) was substituted with several biologically active scaffolds such as oxadiazole, thiadiazole, and triazolothiadiazines, in the hope of obtaining novel cytotoxic agents with improved efficacy and safety. Cytotoxic activities of the designed analogues were carried out at the National Cancer Institute (NCI), USA, against full NCI 60 human cell lines. Among all the tested compounds, 4f
This paper describes the in situ bioconversion of glycyrrhizin of Glycyrrhiza glabra root to 18-β glycyrrhetinic acid by solid state fermentation. Fermentation was carried out with two different fungal strains, Penicillium chrysogenum and Rhizopus oryzae. The solid state fermentation was carried out under stationary state and under rotating state. Penicillium chrysogenum is a better producer of 18-β glycyrrhetinic acid than Rhizopus oryzae . The induced P. chrysogenum seed culture produces higher 18-β glycyrrhetinic acid with 2.955 mg g −1 and maximum β-glucuronidase activity of 3,583.8 U ml −1 under stationary solid state fermentation. The mycelium growth and bioconversion rate is highest at pH of 5.5 and 4.5, respectively. G. glabra root supplemented with a solution of dextrose 9 g l −1 , MnSO 4 •H 2 O 3 g l −1 and (NH 4 ) 2 SO 4 0.540 g l −1 produces 48.580 mg of 18-β glycyrrhetinic acid per gram of G. glabra root, i.e. 86.74 % bioconversion by P. chrysogenum in 96 h under stationary state solid state fermentation.
Microbial biotransformation of Glycyrrhizinic acid (GL) into 18-beta Glycyrrhetinic Acid (GA) was achieved using Escherichia coli MTCC 1652 whole cell. The E. coli whole cell was immobilized by entrapment method within calcium alginate beads using cell suspension of equal volume with sodium alginate 8%. The pH of solution, reaction volume and % of GL were optimized during the immobilization procedure and optimum pH 6.5, reaction volume of 4 mL and at 3% GL concentration for 12 h of incubation time showed highest concentration of GA (72.649 microg mL(-1)) with 76% bioconversion of GL to GA. Under optimized condition the immobilized cell produces 58.663 microg per mL of GA in licorice root extract containing 95.118 microg of GL per mL of the extract with 61% conversion at 12 h.
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