14例大疱性表皮坏死松解型药疹治疗体会

报告14例大疱性表皮坏死松解型药疹的治疗。以磺胺类药和解热镇痛药引起者居多,各4例。皮损面积按九分法计算,皮损面积80％以上者9例,80％以上者5例,治愈9例,死亡5例,我们认为早期使用足够剂量皮质激素类药物是有效措施。病程中注意防治感染,给予足够的液体以防止水电解质失平衡,局部治疗使用本院中药“五黄油”。     

Facile Synthesis and Preliminary Structure–Activity Analysis of New Sulfonamides Against Trypanosoma brucei

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Wavelength Dependence of the Transformation Mechanism of Sulfonamides Using Different LED Light Sources and TiO2 and ZnO Photocatalysts

The comparison of the efficiency of the commercially available photocatalysts, TiO₂ and ZnO, irradiated with 365 nm and 398 nm light, is presented for the removal of two antibiotics, sulfamethazine (SMT) and sulfamethoxypyridazine (SMP). The ^•OH formation rate was compared using coumarin, and higher efficiency was proved for TiO₂ than ZnO, while for 1,4-benzoquinone in O₂-free suspensions, the higher contribution of the photogenerated electrons to the conversion was observed for ZnO than TiO₂, especially at 398 nm irradiation. An extremely fast transformation and high quantum yield of SMP in the TiO₂/LED_398nm process were observed. The transformation was fast in both O₂ containing and O₂-free suspensions and takes place via desulfonation, while in other cases, mainly hydroxylated products form. The effect of reaction parameters (methanol, dissolved O₂ content, HCO₃⁻ and Cl⁻) confirmed that a quite rarely observed energy transfer between the excited state P25 and SMP might be responsible for this unique behavior. In our opinion, these results highlight that “non-conventional” mechanisms could occur even in the case of the well-known TiO₂ photocatalyst, and the effect of wavelength is also worth investigating.     

塞来昔布对实验性结肠癌原位移植瘤生长及血管形成的影响

目的:探讨塞来昔布对实验性结肠癌原位移植瘤生长及血管形成的影响。方法:使用对数生长期的人结肠癌细胞(HT-29)于裸鼠皮下接种成瘤后原位种植。术后随机分为对照组(C组)及塞来昔布高、中、低剂量组(H、M、L组)共四组进行研究。结果:24只裸鼠实验期间无1只死亡,成瘤率为100%,比较各组原位移植瘤体积和瘤质量差异有统计学意义,P值均<0·05。L、M和H组的抑瘤率分别为25·30%、38·80%和76·92%,与对照组比较差异有统计学意义,P=0·000,且存在明显的剂量依赖。干预组瘤组织中MVD、VEGFmRNA、MMP-2mRNA和匀浆上清中PGE2含量与对照组相比差异有统计学意义,P值分别为0·050、0·050、0·050和0·010,随着剂量增加,MVD、VEGFmRNA、MMP-2mRNA和匀浆上清中PGE2含量逐渐降低。瘤组织中PGE2含量与瘤质量,以及MVD与VEGFmRNA、MMP-2mRNA均存在显著的正相关性,r=0·8814,P=0·000;r=0·8573,P=0·000;r=0·6427,P=0·001。结论:塞来昔布通过抑制人结肠癌裸鼠原位移植瘤环氧化酶-2活性,抑制PGE2合成、VEGFmRNA和MMP-2mRNA表达,抑制肿瘤的血管形成,从而对结肠癌的生长有抑制作用。     

Drug-Induced Uveitis

Uveitis has been reported in association with a variety of topical, intraocular, periocular, and systemic medications. To establish causality of adverse events by drugs, in 1981, Naranjo and associates proposed seven criteria, which are related to the frequency and documentation of the event; circumstances of occurrence, recovery, and recurrence; and coexistence of other factors or medications. Rarely does a drug meet all seven criteria. The authors review reports of drug-associated uveitis, applying the seven criteria and examining possible mechanisms. Only systemically administered biphosphonates and, perhaps, topical metipranolol meet all seven criteria. Systemic sulfonamides, rifabutin, and topical glucocorticoids fulfill at least five criteria. (Surv Ophthalmol 42:557-570, 1998.     

An automated flow injection-serial dynamic dialysis technique for drug-protein binding studies

The interface of an automated flow injection analyzer with a dialysis unit to study drug-protein interactions using flow injection serial dynamic dialysis (FISDD) procedure is described. The method is based on the study of the kinetics of dialysis of the ligand in the absence and presence of protein. A study of the binding of sulfamethoxazole. sulfamethizole and sulfisoxazole to bovine serum albumin by means of such an automated system was undertaken to investigate the utility of FISDD technique for protein binding studies. The determination of dialysable sulfonamides was performed automatically by the FIA analyser. The influence of ionic strength and viscosity on the rate of dialysis was investigated. It was found that both variables did not affect the kinetic profile. Binding by the cellophane membrane was not encountered as a problem with the compounds studied. Binding parameters estimated for sulfamethoxazole were found to agree well with those reported in the literature. The Scatchard plots for the binding of sulfamethizole and sulfisoxazole with bovine serum albumin, revealed two classes of binding sites for each sulfonamide. The system was also used for the calculation of the dialytic rate constants. Experimental variables can be readily controlled to yield favoured conditions to study the protein binding phenomenon.