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1.
AMB Express ; 6(1): 60, 2016 Dec.
Article in English | MEDLINE | ID: mdl-27568226

ABSTRACT

A novel lignocellulose material, holocellulose from rice straw via the pretreatment of SO3 micro-thermal explosion, was developed to produce sophorolipids (SLs) with Wickerhamiella domercqiae var. sophorolipid CGMCC 1576. The influence factors of inoculum dose, yeast extract concentration and pH regulators (chemical regents used for adjusting/influencing pH) was investigated and discussed. Results showed that W. domercqiae can grow in the rice straw holocellulose hydrolysate, and acquire relative high SL yield of 53.70 ± 2.61 g/L in shake flask culture. Inoculum dose, yeast extract concentration and pH regulator made obvious influence on fermentation parameters, especially on final broth pH and SLs production. Furthermore, there is a strong negative linear correlation existing between final broth pH and lactonic SL or ratio of lac SL/tot SL. Additionally, comparison between SL production and non-glucose carbon sources, culture methods, microbes in previous reports was carried out. These results will be benefit for acquiring SL mixture with suitable lac SL/tot SL ratio for specific purpose and scope economically.

2.
Bioorg Med Chem Lett ; 23(19): 5361-6, 2013 Oct 01.
Article in English | MEDLINE | ID: mdl-23972441

ABSTRACT

A series of novel tri-2,3,5-substituted tetrahydropyran analogs were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the series provided inhibitors with good DPP-4 potency and selectivity over other peptidases (QPP, DPP8, and FAP). Compound 23, which is very potent, selective, efficacious in the diabetes PD model, and has an excellent pharmacokinetic profile, is selected as a clinical candidate.


Subject(s)
Dipeptidyl-Peptidase IV Inhibitors/chemical synthesis , Heterocyclic Compounds, 2-Ring/chemical synthesis , Pyrans/chemical synthesis , Animals , Diabetes Mellitus, Type 2/drug therapy , Dipeptidyl-Peptidase IV Inhibitors/chemistry , Dipeptidyl-Peptidase IV Inhibitors/pharmacology , Dogs , Enzyme Activation/drug effects , Glucose Tolerance Test , Haplorhini , Humans , Inhibitory Concentration 50 , Pyrans/chemistry , Pyrans/pharmacology , Rats , Stereoisomerism
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