Oligonucleotide-displaced organic monolayer-protected silver nanoparticles and enhanced luminescence of their salted aggregates

N-(2-mercaptopropionyl)glycine (tiopronin) monolayer-protected silver particles were partially displaced by single-stranded oligonucleotides through ligand exchanges. The oligonucleotide-displaced particles could be hybridized with complementary fluorophore-labeled oligonucleotides. Both the oligonucleotide-displaced and hybridized particles could be aggregated by electrostatic interactions with salt in buffer solution, and the aggregates displayed enhanced luminescence from fluorophores. This result suggests the possible application of surface-enhanced fluorescence from metallic nanoparticle aggregation for DNA detection.     

硫普罗宁治疗慢性乙型肝炎的临床疗效对照研究

目的：评价硫普罗宁治疗慢性乙型肝炎的效果及安全性。方法：慢性乙型肝炎80例,随机分为两组。治疗组40例,以硫普罗宁0.2g加入5%葡萄糖溶液250ml中静滴,1次/日,连续治疗4周,对照组40例,以甘草酸二铵150mg加入5%葡萄糖溶液250ml中静滴,1次/日,连续治疗4周;同时分别监测肝功能指标：丙氨酸氨基转移酶（ALT）,天冬氨酸转移酶（AST）、总蛋白（TP）、总胆红素（TBi）、肝纤维化指标（HA、PCⅢ）及凝血酶原活动度（PTA）等,并进行比较分析。结果：硫普罗宁治疗组较对照组在肝功能复常方面显示良好的治疗效应,可使转氨酶及HA明显下降,两组显效率分别为50%（20/40）和25%（10/40）,总有效率为85%（34/40）和47.5%（19/40）,两组比较差异有显著性（p〈0.01）。结论：短期临床研究提示硫普罗宁治疗慢性乙型肝炎,可明显改善肝脏功能,有抗纤维化作用,且副作用少,疗效显著。     

Thiorphan, tiopronin, and related analogs as substrates and inhibitors of peptidylglycine alpha-amidating monooxygenase (PAM)

Peptidyglycine alpha-amidating monooxygenase is a copper- and zinc-dependent, bifunctional enzyme that catalyzes the cleavage of glycine-extended peptides or N-acylglycines to the corresponding amides and glyoxylate. This reaction is a key step in the biosynthesis of bioactive alpha-amidated peptides and, perhaps, the primary fatty acids amides also. Two clinically useful N-acylglycines are thiorphan and tiopronin, each with a thiol moiety attached to the acyl group. We report here that thiorphan and tiopronin are substrates for PAM, exhibiting relatively low K(M,app) and V(MAX,app) values. The low V(MAX,app) values result, most likely, from a decrease in active PAM.2Cu(II) as the enzyme competes ineffectively with thiorphan and tiopronin for free copper.