国产檀香中α-反式香柠烯醇化学结构研究

从国产檀香木Santalum ablum L.分得一个新倍半萜醇,根据光谱(IR,MS,¹H-¹H COSY,¹³C-¹H COSY和¹H-¹H NOESY)解析,确定了它的化学结构和相对立体化学为9(10)-顺,α-反式香柠烯醇[9(10)Z,α-trans-bergamotenol](Ia)。     

Adult asthma review in general practice: nurses' perception of their role

BACKGROUND: Asthma clinics have become widespread in general practice with nurses now playing an important role in asthma review. However, little is known about training of nurses carrying out reviews and how this affects the nurse role in patient management. OBJECTIVES: We aimed to discover the level of asthma training of practice nurses carrying out review of adult asthma patients in one Health Authority and to see if this has any effect on their perception of their role. METHOD: All 187 practice nurses in Grampian were sent a postal questionnaire investigating how asthma review is organized in general practice, their role in review and the asthma training they had received. Personal interviews were carried out with 17 nurses, exploring in more depth the topics covered in the questionnaire. RESULTS: A total of 167 nurses from 92% of the practices in Grampian responded, of whom 61% carried out asthma reviews. Among nurses carrying out reviews 71% did so on their own. 49% of nurses had or were training for advanced asthma qualification. Nurses without an asthma qualification were significantly more likely to feel that their training was not sufficient for their asthma related tasks (54% versus 11%, P = 0.0002). Nurses without advanced asthma qualifications were less likely to provide or review a self-management plan (29% versus 49%, P = 0.01), to review patient PEF recording (38% versus 65%, P < 0.01), to discuss patient worries (75% versus 94%, P < 0.05) or to make the initial diagnosis of asthma (24% versus 76%, P < 0.005). Nurses were unlikely to view their role as fully responsible unless they had an asthma qualification (13% versus 49%, P < 0.001). CONCLUSION: Nurses without advanced asthma qualifications do not feel fully confident in responsibility for patient management. Nurses without training are more likely to only carry out routine monitoring at reviews while nurses with asthma training are more likely to actively develop patient self- management skills. This suggests that nurses should be supported to obtain asthma qualifications if they are to give the best possible care to asthma patients.      

中药材X-射线衍射图谱研究

为探讨中药材道地性的客观规律,以期建立相应的评估指标系统,本文选择常用中药材茜草类、贝母类、山药类三组样品,应用X-射线粉末衍射法进行图谱分析,获得了可用于标识中药材的衍射图形几何拓扑规律与图谱特征标记峰,由此观察到:不同产地茜草样品的相似性及其与欧茜草的差别;同属不同种贝母样品的相似性与差异;不同产地山药样品的相似性及与伪品的区别。本文结果预示着这一方法在揭示中药材道地性客观规律方面的广阔应用前景。     

TMB-8对去甲肾上腺素和BHQ引起新生大鼠单个脑细胞内游离钙增高的影响

应用AR-CM-MIC阳离子测定系统,研究TMB-8对体外新生SD大鼠单个脑细胞内游离钙的抑制作用及其机制。结果表明,在无细胞外钙情况下,静息[Ca²⁺]i为79±13nmol·L^-1。TMB-810,30μmol·L^-1能明显降低静息[Ca²⁺]i。TMB-8100μmol·L^-1对高钾去极化引起的[Ca²⁺]i显著增高无明显影响。在细胞外钙为1.3mmol·L^-1时,去甲肾上腺素诱导的细胞内[Ca²⁺]i升高可部分被TMB-8抑制;TMB-8(30μmol·L^-1)对BHQ引起的[Ca²⁺]i的升高无明显抑制作用。而当细胞外液[Ca²⁺]i为0时,TMB-8几乎完全抑制了去甲肾上腺素和BHQ的作用。提示TMB-8降低脑细胞内游离钙的作用机制是通过促使细胞内钙进入肌浆网以抑制内钙的释放,并通过饱和肌浆网内Ca²⁺间接地阻滞细胞膜钙通道。     

1-[2-(取代苯基甲硫基)-2-(2,4-二氟苯基)乙基]-1H-1,2,4-三唑类化合物的合成及抗真菌活性

设计合成了21个1-[2-(取代苯基甲硫基)-2-(2,4-二氟苯基)乙基]-1H-1,2,4-三唑类化合物,其中19个为首次报道。体外抑菌试验表明:所有目标化合物对8种试验真菌均有不同程度的抗菌活性,其中化合物1,2,5对絮状表皮癣菌的活性为硫康唑的512倍以上;化合物5对白色念株菌的活性为硫康唑的32倍;化合物2对申克孢子丝菌的活性为硫康唑的32倍;化合物2,14对新型隐球菌的活性分别为硫康唑的64倍,32倍;化合物1,5对熏烟色曲菌的活性分别为硫康唑的16倍以上。     

Cytochrome P450 mediated bioactivation of methyleugenol to 1'- hydroxymethyleugenol in Fischer 344 rat and human liver microsomes

Cytochrome P450 mediated metabolism of methyleugenol to the proximate carcinogen 1'-hydroxymethyleugenol has been investigated in vitro. Kinetic studies undertaken in liver microsomes from control male Fischer 344 rats revealed that this reaction is catalyzed by high affinity (Km of 74.9 +/- 9.0 microM, Vmax of 1.42 +/- 0.17 nmol/min/nmol P450) and low affinity (apparent Km several mM) enzymic components. Studies undertaken at low substrate concentration (20 microM) with microsomes from livers of rats treated with the enzyme inducers phenobarbital, dexamethasone, isosafrole and isoniazid indicated that a number of cytochrome P450 isozymes can catalyze the high affinity component. In control rat liver microsomes, 1'- hydroxylation of methyleugenol (assayed at 20 microM substrate) was inhibited significantly (P < 0.05) by diallylsulfide (40%), p- nitrophenol (55%), tolbutamide (30%) and alpha-naphthoflavone (25%) but not by troleandomycin, furafylline, quinine or cimetidine. These results suggested that the reaction is catalyzed by CYP 2E1 and by another as yet unidentified isozyme(s) (most probably CYP 2C6), but not by CYP 3A, CYP 1A2, CYP 2D1 or CYP 2C11. Administration of methyleugenol (0-300 mg/kg/day for 5 days) to rats in vivo caused dose- dependent auto-induction of 1'-hydroxylation of methyleugenol in vitro which could be attributed to induction of various cytochrome P450 isozymes, including CYP 2B and CYP 1A2. Consequently, high dose rodent carcinogenicity studies are likely to over-estimate the risk to human health posed by methyleugenol. The rate of 1'-hydroxylation of methyleugenol in vitro in 13 human liver samples varied markedly (by 37- fold), with the highest activities being similar to the activity evident in control rat liver microsomes. This suggests that the risk posed by dietary ingestion of methyleugenol could vary markedly in the human population.      

K-Ⅱ和U-50488H对κ阿片受体亲和力的比较

3,4-二氯-N-甲基-N-[反式-2-(1-△³-吡咯啉基)环己基]苯乙酰胺(K-Ⅱ)是新合成的U-50488H类似物,其对小鼠的镇痛效应和对离体兔输精管的抑制作用均比U-50488H强。本文用放射受体结合试验方法对这两种化合物在富含x阿片受体的豚鼠小脑和大脑皮层前叶上的亲和力进行了比较,并求出这两种化合物的Ki值.结果表明K-Ⅱ对k阿片受体的亲和力比U-50488H强6～42倍。K-Ⅱ对阿片受体亚型选择性比较研究正在进行中。     

溶剂系统对18-甲基炔诺酮渗透皮肤的影响

本文对乙醇、水、油酸等溶剂系统对左旋18-甲基炔诺酮(简称LNG)及消旋18-甲基炔酮(简称NG)渗透皮肤的影响进行了研究。实验采用Vaila-Chien双室扩散池及成人离体皮肤。结果表明,在80%乙醇水溶液中,LNG与NG的皮肤渗透速率比用生理盐水提高5～6倍,其中NG的皮肤渗透速率比LNG高1～2倍.含水乙醇与油酸复合使用时,对LNG通透皮肤具有明显的协同促进作用。当油酸—80%乙醇(0.75:9.25v/v)作为复合溶剂时。所获得的LNG皮肤渗透速率为0.53μg/cm²·h,分别比油酸或80%乙醇单独使用时提高29倍和3倍。提示正确地采用复合溶剂系统,能有效地提高LNG或NG透皮速率。