千层塔中三萜成分的研究

前曾报道自千层塔[Huperzia serrata Thunb.(Trev)=Lycopodium serratum Thunb(Trev.)]中分得具有胆碱酯酶抑制活性的新生物碱——石杉碱甲、石杉碱乙、甲基石杉碱乙及已知生物碱8-deoxyserratinine,serratinine,lycodoline及lycoclavine。为进一步阐明该植物的化学成分,我们对其三萜成分进行了研究。从浙江安吉产的千层塔植物中分到六个石松三萜,其中一个为新化合物,经下述方法推定为serratenediol-21-acetate(Ⅰ)。另五     

国产麻黄的形态组织学研究——Ⅱ.西南主产种及其它种

本文报道我国西南产麻黄——丽江麻黄Ephedra likiangensis Florin、匍枝丽江麻黄E.likiangensis f.mairei(Florin)C.Y.Cheng、藏麻黄E.saxatilis Royle ex Florin、山岭麻黄E.gerardiana Wall、垫状山岭麻黄E.gerardiana Var.congesta C.Y.Cheng、矮麻黄E.minuta Florin和异株矮麻黄E.minuta var.dioeca C.Y.Cheng,以及形态组织特征较特殊的宁夏产斑子麻黄E.lepidosperma C.Y.Cheng、新疆产窄膜麻黄E.lomatolepis Schrenk,西藏产西藏中麻黄E.intermedia var.tibetica Stapf的生药形态组织学研究结果。并根据对国产麻黄的生药形态组织学的系统研究结果,分别编写了各种国产麻黄(包括13种3变种1变型)的生药性状和生药显微特征检索表。     

蜜环菌菌丝体化学成分的研究——Ⅴ.蜜环菌辛素和蜜环菌壬素的分离与鉴定

从人工液体发酵培养的蜜环菌[Armillaria mellea(Vahl.ex Fr.)Quel.]菌丝体的石油醚提取物中,经硅胶柱层析,低压柱层析和制备性薄层层析分离得到两个新的原伊鲁烷型倍半萜芳香酸酯类化合物。命名为蜜环菌辛素(armillarilin)和蜜环菌壬素(armillarinia),根据光谱(UV,IR,~1HNMR,~(13)CNMR和MS)分析,推定它们的化学结构分别为Ⅰ和Ⅱ。     

固相法合成心肌兴奋肽及其类似物

用Boc-和Tos-基团分别保护氨基和侧链胍基,以1%交联度聚苯乙烯二苯甲氨基树脂为载体,用DCC固相法合成肽,HF断裂肽树脂键和去除侧链保护基团,粗产物经高效液相层析纯化,合成了心肌兴奋肽Phe-Met-Arg-Phe-NH_2及其类似物Phe-Pro-Arg-Phe-NH_2,并观察了此二种肽对大鼠血压和心率的影响。     

Hearing-related,health-related quality of life in patients who have undergone otosclerosis surgery: A long-term follow-up study

Objectives: The aims of the study were to assess health-related quality of life and hearing-related disability in subjects with otosclerosis 30 years after surgery. Design: An observational study was performed. Medical records were reviewed, a clinical examination as well as audiometric assessments were performed. Generic health-related quality of life was assessed by the SF-36v2 and hearing disability by a shortened version of SSQ (speech spatial and qualities of hearing scale). Study sample: Sixty-five individuals, who had undergone stapedectomy in 1977-79 at a tertiary referral center. Results: Generic health-related quality of life according to SF-36 subscale scores was comparable to that of an age- and sex-matched reference population. The SF-36 mental component summary score (MCS) was, however, significantly better than that of the reference population. The mental and physical summary component scores correlated significantly to hearing disability measured by the SSQ but not to hearing impairment. Hearing disability was displayed in all SSQ sub-scores, especially in more complex listening situations and in the localization of sounds. Conclusions: This study shows that individuals with otosclerosis, 30 years after surgery, have a good generic health-related quality of life, despite moderate to severe hearing loss and significant hearing disabilities.     

Intrauterine fetal death associated with Rothia dentocariosa: a case report

We report a case of intrauterine fetal death at term with a possible association to an oral bacterium, Rothia dentocariosa. A healthy primiparous woman was admitted at term with an intrauterine fetal death after an uncomplicated pregnancy. R. dentocariosa was found in the fetal blood culture.     

Model-Based Estimates of the Effects of Efavirenz on Bedaquiline Pharmacokinetics and Suggested Dose Adjustments for Patients Coinfected with HIV and Tuberculosis

Safe, effective concomitant treatment regimens for tuberculosis (TB) and HIV infection are urgently needed. Bedaquiline (BDQ) is a promising new anti-TB drug, and efavirenz (EFV) is a commonly used antiretroviral. Due to EFV''s induction of cytochrome P450 3A4, the metabolic enzyme responsible for BDQ biotransformation, the drugs are expected to interact. Based on data from a phase I, single-dose pharmacokinetic study, a nonlinear mixed-effects model characterizing BDQ pharmacokinetics and interaction with multiple-dose EFV was developed. BDQ pharmacokinetics were best described by a 3-compartment disposition model with absorption through a dynamic transit compartment model. Metabolites M2 and M3 were described by 2-compartment models with clearance of BDQ and M2, respectively, as input. Impact of induction was described as an instantaneous change in clearance 1 week after initialization of EFV treatment and estimated for all compounds. The model predicts average steady-state concentrations of BDQ and M2 to be reduced by 52% (relative standard error [RSE], 3.7%) with chronic coadministration. A range of models with alternative structural assumptions regarding onset of induction effect and fraction metabolized resulted in similar estimates of the typical reduction and did not offer a markedly better fit to data. Simulations to investigate alternative regimens mitigating the estimated interaction effect were performed. The results suggest that simple adjustments of the standard regimen during EFV coadministration can prevent reduced exposure to BDQ without increasing exposures to M2. However, exposure to M3 would increase. Evaluation in clinical trials of adjusted regimens is necessary to ensure appropriate dosing for HIV-infected TB patients on an EFV-based regimen.