Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0149514 (bronchitis)
 6,902 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Seventy-four pulmonologists and one allergist were recruited to assess the efficacy and safety of iodinated glycerol (Organidin), 60 mg qid, vs placebo in patients with stable chronic obstructive bronchitis in a randomized, double-blind, placebo-controlled, parallel design. A total of 361 patients (180 to iodinated glycerol and 181 to placebo) who complained of cough and difficulty bringing up sputum entered the eight-week study. Evaluations were based upon eight primary symptom efficacy parameters (cough frequency, cough severity, chest discomfort, dyspnea, ease in bringing up sputum, patient and physician global assessments, and a derived patients' global assessment), and six secondary parameters (frequency of aerosol bronchodilator use, incidence and duration of acute exacerbations, frequency of concomitant medication use, incidences of adverse experiences and dropouts). Cough frequency, cough severity, chest discomfort, patients' ease in bringing up sputum, patients' overall condition, and a derived subject global assessment were significantly (p less than 0.05) improved by iodinated glycerol as compared with placebo within eight weeks of treatment. Dyspnea showed a trend toward improvement and the physicians' global evaluation showed no significant difference between groups. Similar findings were noted in a subgroup analysis of moderately-to-severely affected patients. The mean duration (days) of acute exacerbations and number of dropouts attributable to adverse experiences were significantly less (p less than 0.05) in the iodinated glycerol group.(ABSTRACT TRUNCATED AT 250 WORDS)
 ...
PMID:The National Mucolytic Study. Results of a randomized, double-blind, placebo-controlled study of iodinated glycerol in chronic obstructive bronchitis. 222 98

(R)-chlorprenaline, a selective activator of beta2 receptor and an effective drug for bronchitis and asthma, is industrially prepared from (R)-2'-chloro-1-phenyl-ethanol. In this communication, we describe (1) the identification of Saccharomyces cerevisiae B5 as an effective host for stereoselective reduction of 2'-chloroacetophenone to (R)-2'-chloro-1-phenyl-ethanol; (2) the presence of ethanol enhances the conversion; and (3) the biochemical factors that effect the yield of the product. Among the four yeast strains capable of reduction 2'-chloroacetophenone to (R)-2'-chloro-1-phenyl-ethanol we screened, Saccharomyces cerevisiae B5 showed the highest activity and stereoselectivity, and was used for the subsequent study. The effect of the presence of methanol, ethanol, 2-propanol, 1-butanol, glucose, glycerol and lactic acid was first investigated, as it was previously reported that they increased the yield and stereoselectivity of the reaction. The addition of the co-substrate methanol, ethanol, 2-propanol, 1-butanol, glucose and glycerol favored the formation of the 2'-chloroacetophenone to (R)-2'-chloro-1-phenyl-ethanol. Lactic acid inhibited the enzyme activity. Ethanol is the best co-substrate among the seven co-substrates and under the optimum concentration of 5% , the yield of (R)-2'-chloro-1-phenyl-ethanol was increased from 17% to 74%. The oxidation of ethanol regenerates NADH required for the reduction. The effects of the reaction time, pH, cell concentration, substrate concentration and temperature on the reduction were investigated next. The enantiometric excess of (R)-2'-chloro-1-phenyl-ethanol reached 100% under the optimal condition: pH8.0, 25 degrees C and 5% ethanol. The product yield went up with the increasing Saccharomyces cerevisiae B5 concentration and reached 100% when the cell dry weight was 10.75 mg/mL and 2'-chloroacetophenone was 6.47 mmol/L. The yield of (R)-2'-chloro-1-phenyl-ethanol decreased sharply with the increase of substrate concentration, as the high concentration of substrates is toxic to the cell and inhibits the activity of reductases. The aerobic cultivation of the yeast and shaking during the reaction increased the yield of (R)-2'-chloro-1-phenyl-ethanol. The yeast can be reused up to 15 times. This research paves the way for economical preparation of chiral 2'-chloroacetophenone to R-2'-chloro-1-phenylethanol.
 ...
PMID:[Saccharomyces cerevisiae B5 efficiently and stereoselectively reduces 2'-chloroacetophenone to R-2'-chloro-1-phenylethanol in the presence of 5% ethanol]. 1596 23