ABSTRACT
Ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS) was used to investigate the metabolites of maackiain in rats based on the prediction function of UNIFI data processing system and liver microsomal incubation in vitro. Ten metabolites of maackiain after oral absorption were reasonably deduced and characterized. It was found that the biotransformation of maackiain mainly included phase Ⅰ oxidation, dehydrogenation, phase Ⅱ sulfate conjugation, glucosylation conjugation, and glucuronic acid conjugation. Among them, the product of glucosylation conjugation, trifolirhizin, was identified by comparison with the reference for the first time. Liver microsomal incubation in vitro further confirmed the metabolites and metabolic pathways of maackiain in rats. The metabolites in the blood, urine, and feces complemented each other, which revealed the migration, metabolism, and excretion modes of maackiain in rats. This study lays a foundation for the further investigation of the metabolic mechanism of maackiain in vivo and the in-depth research on the mechanism of pharmacodynamics and toxicity.
Subject(s)
Animals , Rats , Chromatography, High Pressure Liquid , Chromatography, Liquid , Metabolic Networks and Pathways , Pterocarpans , Rats, Sprague-DawleyABSTRACT
Objective To explore an easily-controllable, environmentally-friendly method for synthesizing monastrol and its derivatives. Methods Monastrol and its derivatives were synthesized using (substituted) benzaldehyde, ethyl acetoacetate and thiourea (or urea) as the material through a Biginelli reaction catalyzed by green room temperature ionic liquid 1-butyl-3- methylimidazolium-L-camphorsulfonate under microwave irradiation without solvent. Results The green room temperature ionic liquid 1-butyl-3-methylimidazolium-L-camphorsulfonate catalyzed Biginelli reaction in obtaining the title compound under microwave irradiation without solvent. The process was easy to operate, time saving and environmentally-friendly. Conclusion Microwave-accelerated solvent-free Biginelli reaction using green room temperature ionic liquid 1-butyl-3-methylimidazolium-L- camphorsulfonate as catalyst is a convenient and environmentally-friendly method for synthesizing monastrol and its derivatives.
ABSTRACT
Objective To explore an easily-controllable, environmentally-friendly method for synthesizing monastrol and its derivatives. Methods Monastrol and its derivatives were synthesized using (substituted) benzaldehyde, ethyl acetoacetate and thiourea (or urea) as the material through a Biginelli reaction catalyzed by green room temperature ionic liquid 1-buty-3- methylimidazolium-L-camphorsulfonate under microwave irradiation without solvent. Results The green room temperature ionic liquid 1-buty-3-methylimidazolium-L-camphorsulfonate catalyzed Biginelli reaction in obtaining the title compound under microwave irradiation without solvent. The process was easy to operate, time saving and environmentally-friendly. Conclusion Microwave-accelerated solvent-free Biginelli reaction using green room temperature ionic liquid 1-buty-3-methylimidazolium-L- camphorsulfonate as catalyst is a convenient and environmentally-friendly method for synthesizing monastrol and its derivatives.
ABSTRACT
<p><b>OBJECTIVE</b>To identify the gene mutation for two Chinese families with autosomal dominant non-syndromic hearing impairment(NSHI).</p><p><b>METHODS</b>Two NSHI pedigrees with common ancestor were identified by clinical examination and family investigation. Linkage analysis was performed for all known NSHI loci, and all exons and exon-intron boundaries of the non-muscle myosin heavy chain 14 (MYH14) gene were amplified by PCR and sequenced.</p><p><b>RESULTS</b>The disease-causing gene of these 2 pedigrees was fine mapped to the DFNA4 locus on 19q13.33. A heterozygous transition of c. 359T>C (p.S120L) in MYH14 gene was identified. The mutation was detected in all patients but not in normal members in the two families.</p><p><b>CONCLUSION</b>It is the first report that mutation in MYH14 gene can cause dominant non-syndromic hearing impairment in Asian population, suggesting that MYH14 gene can be a disease-causing gene of Chinese patients with hearing impairment.</p>