Sulfogriseofulvin Derivatives. Synthesis by [4+2]Cycloaddition,Structure, Properties,Crystal Structure Analysis,and Antifungal Activity of Spiro[1,3-benzoxathiole-2,1′-cyclohex-2′-en]-4′-one 3,3-Dioxides

Syntheses of substituted, especially of fluoro substituted benzoxathiole 1,1-dioxides, are described. These derivatives were transformed via the Peterson olefination into substituted 2-alkylidene derivatives 27. Diels-Alder reactions of 27 with 1,1-dimethoxy- and 1-methoxy-3-trimethylsiloxy-1,3-butadiene ( 30, 32 ) gave sulfone analogues 31 of griseofulvin (named sulfogriseofulvins). From Z- 27 , a number of cis-isomers with the relative stereochemistry of griseofulvin (cis- 31 ) was prepared, and from E-isomers of 27 , compounds (trans- 31 ) with relative stereochemistry of epigriseofulvin were obtained. Some related compounds ( 33, 38 ) are synthesized by slight modifications. The stereochemistry is established by spectroscopic methods and crystal structure analyses. The compounds 31 were tested against three species of dermatophytes. The biological activities were all significantly lower than that of griseofulvin.     

Transcutaneous bilirubinometry in Chinese, Malay and Indian infants

The objective of this study was to investigate the correlation of transcutaneous bilirubinometry (TcB) and plasma bilirubin concentrations in full-term Chinese, Malay and Indian infants. TcB was performed with the Minolta Airshields bilirubinometer on Chinese, Malay and Indian full-term infants. The readings were taken on the chest (sternum) and forehead (glabella) when capillary blood was sampled for bilirubin determination. Five hundred and forty TcB indices in 253 Chinese infants, 282 in 169 Malay infants, and 182 in 120 Indian infants were obtained over the sternum and forehead. A good correlation between the TcB indices and the bilirubin concentrations was observed in Chinese, Malay and Indian infants: r = 0.78 (chest), r = 0.73 (forehead); r = 0.86 (chest), r = 0.84 (forehead); and r = 0.84 (chest), r = 0.82 (forehead). The correlation was just as good when the combined values were evaluated together: r = 0.80 (chest) r = 0.75 (forehead). In Chinese infants, correlation at values below 250 μmol ⁻¹ was significantly better than that at values over 250μmoll⁻¹ r = 0.80 versus r =−0.20, < 0.00001 (chest), and r = 0.74 versus r = 0.07, < 0.00001 (forehead). However, a safer cut-off point clinically would be 200 μmoll⁻¹, since only relatively few higher bilirubin values were encountered when TcB indices were below 200 μmoll⁻¹ The same pattern was noticed with the other two groups, and the combined group. Thus, TcB provides a non-invasive, cost-effective screening method for significant neonatal jaundice, sparing infants and parents physical and emotional stress, and medical and nursing personnel extra work and inconvenience.     

Human myelogenous leukemia: enhanced clonal proliferation in the presence of phorbol diesters

Phorbol diesters, including 12-0-tetradecanoyl-phorbol-13-acetate (TPA) at low concentrations, enhanced the clonal proliferation of a human myelogenous leukemia cell line (KG-1). TPA (1.0 X 10(-9) -5.0 X 10(-11) M) increased KG-1 clonal growth by four to tenfold in the presence of suboptimal concentrations of colony stimulating factor (CSF) and by two to fourfold in the presence of maximally stimulating concentrations of CSF. The ability of TPA analogs to enhance KG-1 clonal growth paralleled their reported ability to promote tumors in mice. Only slight CSF activity was detected in the conditioned medium from KG-1 cells cultured in liquid medium with TPA. TPA was unable to increase myeloid clonal growth of CSF-stimulated normal human model to study TPA enhancement of CSF-stimulated growth.     

Association with prior fluoroquinolone therapy of widespread ciprofloxacin resistance among gram-negative isolates in a Veterans Affairs medical center.

We performed a case-control study of risk factors for the acquisition of ciprofloxacin-resistant gram-negative isolates in a Veterans Affairs medical center. Sixty-five patients with resistant isolates and 50 control patients were identified. Prior fluoroquinolone use was significantly more frequent among patients with resistant isolates than it was among controls (58 versus 20%; P = 0.0001). The association with prior quinolone use was stronger in the long-term-care division (81 versus 32%; P = 0.0005) than it was in the acute-care division (29 versus 0%; P = 0.015). On multivariate analysis, prior receipt of a fluoroquinolone was the single most significant risk factor for isolation of a ciprofloxacin-resistant gram-negative organism (P = 0.0001).     

Hevea latex-associated allergies: piecing together the puzzle of the latex IgE reactivity profile

ABSTRACT

Introduction: IgE-mediated Hevea latex allergy and associated food-allergies constitute a significant health issue with serious consequences of diagnostic error. Hence, there is a need for more reliable confirmatory diagnostics.

Areas covered: Here, we summarize the major limitations of conventional tests using native extracts and describe how piecing together the IgE reactivity profile can benefit correct diagnosis in difficult cases in whom conventional tests yield equivocal or negative results. A diagnostic algorithm integrating traditional sIgE and component-resolved diagnosis (CRD) is presented.

Expert opinion: Moreover, it is clear that the discoveries in the field of the Hevea latex proteome will contribute to our understandings and accurate approach of sometimes complex cross-reactivity phenomena that extend beyond the ‘latex-fruit syndrome.’     

纵跳和闭目单足站立对跟骨骨密度的影响

目的:为有效预防和控制骨质疏松,实验测定苏州市成年人跟骨骨密度,探讨其与纵跳高度、闭目单足站立时间的相关性。方法:实验于2004-10/2005-04在苏州市体育科学研究所完成。①实验对象:随机选取苏州市158名普通成年人进行测试,对本实验均知情同意。②实验方法:受试者踏上纵跳计踏板,当测试计的显示屏显示"00"时,受试者尽最大力量向上跳起,落地后测试计自动显示纵跳高度值。受试者闭目,用习惯脚单脚穿鞋站立在平地上,另一腿屈膝使脚离开地面,姿势不限,从提起脚离开地面开始计时,至离地脚落地停表,计算闭目单足站立的时间。采用sonost-2000超声骨密度仪测量实验对象的跟骨超声波传导速度和超声波衰减系数,仪器与电脑相连,自动算出跟骨骨质量指数。结果:①闭目单足站立时间和纵跳高度对跟骨超声参数的影响:闭目单足站立时间和纵跳高度均与跟骨骨质量指数、超声波衰减系数呈线性关系。②闭目单足站立时间和纵跳高度与跟骨超声参数的相关性:与闭目单足站立时间与跟骨超声参数的相关性比较,纵跳高度与跟骨超声参数的相关性明显升高(P<0.01)。结论:①闭目单足站立时间和纵跳高度均与跟骨的骨密度、骨强度存在线性关系,但纵跳高度呈中度相关,闭目单足站立时间相关性较低。②纵跳高度越高,反映下肢肌肉力量越大,骨密度和骨强度较大;闭目单足站立时间长,反映身体的平衡能力强。     

In vitro activities of newer quinolones against bacteroides group organisms

The activities of BMS-284576, clinafloxacin, moxifloxacin, sitafloxacin, trovafloxacin, imipenem, cefoxitin, and clindamycin against 589 Bacteroides fragilis group isolates were determined. The activity of BMS-284576 was comparable to that of trovafloxacin. Sitafloxacin and clinafloxacin were the most active quinolones, and moxifloxacin was the least active. B. fragilis was the most susceptible of the species, and Bacteroides vulgatus was the most resistant. Association of specific antibiotic resistance with Bacteroides species was noted for all quinolones.     

Effect of the F508del genotype on outcomes of endoscopic sinus surgery in children with cystic fibrosis

Objective

Numerous authors have sought to describe genotype–phenotype correlations in cystic fibrosis (CF), notably to pancreatic insufficiency and lung disease. However, few studies have focused on the association between the F508del genotype and response to sinus surgery. The objective of this study is to assess the effect of the F508del genotype on sinonasal disease severity and outcomes following functional endoscopic sinus surgery (FESS) in a pediatric population.

Methods

A retrospective chart review of 153 children with CF seen at a tertiary care pediatric hospital from 1995 to 2008 was performed. Patients were classified into one of three groups according to F508del genotype, either as homozygous, heterozygous or not carrying a F508del mutation. The sinonasal disease phenotype of the three groups was compared based on clinical and radiological findings, extent of endoscopic sinus surgery and rate of revision surgery.

Results

The relationship between the F508del genotype and pancreatic insufficiency was confirmed (p < 0.05). There was no association between the F508del genotype and increased need for FESS (p = 0.75). Moreover, no association was established between F508del homozygosity and presence of nasal polyps, Lund–Mackay score, extent of surgery or length of postoperative hospitalization. The rates of revision surgery did not differ significantly among the three genotypes analyzed (p = 0.59).

Conclusion

There is no clear association between the F508del genotype and an increased need for FESS, extent of surgery, or revision surgery. Given the phenotypic variability of sinonasal disease in patients with CF, a prospective study is needed to better understand outcomes following FESS and the contribution of gene modifiers to this effect.