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1.
Org Biomol Chem ; 15(20): 4440-4448, 2017 May 23.
Article in English | MEDLINE | ID: mdl-28485453

ABSTRACT

Reduction of double bonds of α,ß-unsaturated carboxylic acids and esters by ene-reductases remains challenging and it typically requires activation by a second electron-withdrawing moiety, such as a halide or second carboxylate group. We showed that profen precursors, 2-arylpropenoic acids and their esters, were efficiently reduced by Old Yellow Enzymes (OYEs). The XenA and GYE enzymes showed activity towards acids, while a wider range of enzymes were active towards the equivalent methyl esters. Comparative co-crystal structural analysis of profen-bound OYEs highlighted key interactions important in determining substrate binding in a catalytically active conformation. The general utility of ene reductases for the synthesis of (R)-profens was established and this work will now drive future mutagenesis studies to screen for the production of pharmaceutically-active (S)-profens.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/metabolism , Oxidoreductases/metabolism , Propionates/chemistry , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Crystallography, X-Ray , Models, Molecular , Molecular Structure , Stereoisomerism , Nicotiana/enzymology
2.
Lett Appl Microbiol ; 61(6): 580-7, 2015 Dec.
Article in English | MEDLINE | ID: mdl-26394071

ABSTRACT

UNLABELLED: (+)-Terrein shows multiple bioactivities, however, its mass production is a big challenge. Aspergillus terreus strain PF26 derived from South China Sea sponge Phakellia fusca has been cultured to produce (+)-terrein successfully, but artificial sea water (ASW) of high salinity used in the fermentation medium may cause the corrosion risk of metal bioreactor, which limits the fermentation on a large scale. In this study, we modified the components of ASW by removing NaCl and CaCl2 from the original formula, which reduced about 80% salinity of ASW. As a result, 7·56 g l(-1) (+)-terrein production was achieved in shake flask, which was 78·72% higher than using the original ASW, and the cultivation time was decreased from 24 to 15 days. Then, the modified ASW was used for the fermentation of A. terreus strain PF26 in a 500 l stirred bioreactor, consequently 2·5 g l(-1) of (+)-terrein production was achieved. SIGNIFICANCE AND IMPACT OF THE STUDY: The fermentation of marine micro-organisms always needs to use sea water or artificial sea water (ASW), which limits the fermentation on a large scale, as the high-salinity medium may cause the corrosion risk of bioreactor. In this study, the ASW formula is simplified to reduce the sea water salinity and improve the yield of (+)-terrein, finally, the modified ASW was successfully used for the mass production of (+)-terrein by A. terreus strain PF26 in a 500 l bioreactor.


Subject(s)
Aspergillus/metabolism , Bioreactors/microbiology , Cyclopentanes/metabolism , Salinity , Seawater/chemistry , Animals , Aquatic Organisms/microbiology , Calcium Chloride/chemistry , China , Fermentation , Molecular Sequence Data , Porifera/microbiology , Sodium Chloride/chemistry
3.
Asian Pac J Trop Med ; 4(6): 486-91, 2011 Jun.
Article in English | MEDLINE | ID: mdl-21771705

ABSTRACT

OBJECTIVE: To isolate marine bacteria, statistically optimize them for maximum asparaginase production. METHODS: In the present study, statistically based experimental designs were applied to maximize the production of L-asparaginase from bacterial strain of Bacillus cereus (B. cereus) MAB5 (HQ675025) isolated and identified by 16S rDNA sequencing from mangroves rhizosphere sediment. RESULTS: Plackett-Barman design was used to identify the interactive effect of the eight variables viz. yeast extract, soyabean meal, glucose, magnesium sulphate, KH(2)PO(4), wood chips, aspargine and sodium chloride. All the variables are denoted as numerical factors and investigated at two widely spaced intervals designated as -1 (low level) and +1 (high level). The effect of individual parameters on L-asparaginase production was calculated. Soyabean meal, aspargine, wood chips and sodium chloride were found to be the significant among eight variables. The maximum amount of L-asparaginase produced (51.54 IU/mL) from the optimized medium containing soyabean meal (6.282 8 g/L), aspargine (5.5 g/L), wood chips (1.383 8 g/L) and NaCl (4.535 4 g/L). CONCLUSIONS: The study revealed that, it is useful to produce the maximum amount of L-asparaginase from B. cereus MAB5 for the treatment of various infections and diseases.


Subject(s)
Asparaginase/biosynthesis , Bacillus cereus/enzymology , Rhizophoraceae/microbiology , Fermentation
4.
Indian J Pathol Microbiol ; 45(3): 311-3, 2002 Jul.
Article in English | MEDLINE | ID: mdl-12785173

ABSTRACT

The leaf and seed extracts of the Plant Azardirachta indica were tested for antidermatophytic activity against dermatophytes such as Trichophyton ruberum, Trichophyton, Mentagrophytes, Trichophyton violaceum, Microsporum nanum and Epidermophyton floccosum by tube dilution technique. The minimum Inhibitory concentration (MIC) of neem seed extract was found to be lower tan that of neem leaf when tested against different species of Dermatophytes.


Subject(s)
Antifungal Agents , Antifungal Agents/pharmacology , Arthrodermataceae/drug effects , Azadirachta , Antifungal Agents/therapeutic use , Arthrodermataceae/growth & development , Azadirachta/chemistry , Dermatomycoses/drug therapy , In Vitro Techniques , Microbial Sensitivity Tests , Microsporum/classification , Microsporum/drug effects , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plants, Medicinal/chemistry , Trichophyton/drug effects
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