对－苯二甲酸衍生物的合成及其诱导分化HL－60细胞的活性

作者合成了１３个对－苯二甲酸衍生物，其中有９个化合物尚未见文献报道。通过对ＨＬ－６０细胞诱导分化活性试验，发现有两个化合物在浓度为５×１０￣（－６）ｍｏｌ／Ｌ时，可使细胞分化率达５５％，低于维Ａ酸的分化率（７９％，１０￣（－７）ｍｏｌ／Ｌ）。     

Ionone derivatives from Alternanthera sessilis

The chloroform extract of the air-dried leaves of Alternanthera sessilis afforded a mixture of diastereomers of a new ionone derivative 1 whose structures were elucidated by extensive 1D and 2D NMR spectroscopy and mass spectrometry. Oxidative cleavage of 1 to aldehyde 3 with manganese dioxide confirmed diastereoisomerism arose from a racemic side chain chiral centre. Antimicrobial tests on the mixture of diastereomers and the derivative indicated that they have low activities against Pseudomonas aeruginosa and Trichophyton mentagrophytes.     

卡莫司他衍生物的合成

目的 合成一种具有游离伯胺的卡莫司他衍生物.方法 以对羟基苯乙酸为原料,经4步反应得到目标化合物.结果与结论 成功制备了目标产物,所得产物的化学结构经1HNMR、MS确认.     

医学英语派生词的特点及教学方法探讨

从词源学、构词方法、同义词等几个方面讨论了医学英语派生词的特点，并以此为基础探讨了医学英语派生词的教学方法。     

Investigating the potential of erythromycin and derivatives as chiral selector in capillary electrophoresis

Macrocyclic antibiotics are present in an increasing number of chiral separation applications. In this study, erythromycin and some derivatives, belonging to the group of macrolide antibiotics, were investigated for their potential as chiral selector. Erythromycin A itself and five related substances namely erythromycin A N-oxide, anhydroerythromycin A, anhydroerythromycin A N-oxide, erythralosamine and erythralosamine N-oxide were included. Twenty-one chiral compounds with a wide difference in physico-chemical properties were used to test the chiral activity of the erythromycins. The chiral compounds were analysed using capillary zone electrophoresis with the erythromycins dissolved in the running buffer at different concentrations ranging from 0.1 to 10 mM, with three different BGEs: sodium phosphate pHs 3.0 and 7.0 and sodium borate pH 9.2. The erythromycins showed more interactions with the acidic compounds (as observed with leucovorin, dopa, carbidopa, ketoprofen, indoprofen and warfarin) than with the neutral or weakly basic ones, especially in acidic medium. Unfortunately, no chiral separations were obtained for any of the 21 racemic mixtures. The complexation constants were calculated for the compounds showing interaction, based on the variation of electrophoretic mobility of the compounds in the presence of different concentrations of erythromycins. Finally, the size of erythromycin A was calculated using computational modelling. It was shown that the aglycone ring is only half as big as the β-cyclodextrin cavity, giving a possible explanation for the negative response of erythromycin in this study.     

鬼臼毒素及其衍生物的波谱特征及药理活性

本文对鬼臼毒素及其衍生物的波谱特征和药理活性进行了系统的综述,为今后的深入研究提供信息和借鉴.     

丹皮酚衍生物的研究进展

丹皮酚从中药牡丹、芍药的干燥根皮和徐长卿的根或全草中分离,具有广泛的药理活性,且结构简单。近年来,对丹皮酚衍生物的研究也有诸多报道,在解热镇痛、抗过敏与抗炎、抗氧化等呈现出良好的药理活性。对丹皮酚衍生物以及其药理活性作系统性回顾。     

阿魏酸和咖啡酸衍生物的抗氧化能力研究

采用人血浆低密度脂蛋白（ＬＤＬ）氧化反应体外实验体系，研究了合成的阿魏酸（Ｆｅｒｕｌｉｃａｃｉｄ）和咖啡酸（Ｃａｆｆｅｉｃａｃｉｄ）衍生物的抗氧化性能，并与已知的抗氧化剂ＶｉｔＥ等作了对比。结果显示其中阿魏酸、香草醛肟，及二乙酰基咖啡酸抗氧化能力较强，超过了ＶｉｔＥ，另外五个衍生物抗氧化能力不及ＶｉｔＥ，但均在其功能基因被保护的状态下。本文对抗氧剂的构效关系作了探讨。     

The development of virus-free labile blood derivatives — A review

Human blood plasma derived coagulation factor concentrates carry a substantial risk of virus transmission as traditionally prepared. Intensive investigations during the past 5 years have led to the development of several virus sterilization procedures which can be applied to these concentrates as well as to other labile protein derivatives. This review summarizes detailed information which is now available establishing the virucidal potency of these procedures, particularly with regard to the contaminating viruses of most concern: hepatitis B, non-A, non-B hepatitis and the AIDS virus.Currently utilized virus sterilization procedures have greatly reduced or eliminated the transmission of AIDS virus, HIV. The transmission of non-A, non~B hepatitis virus (NANBHV) has also been greatly reduced by some but not all of these procedures. Additional virus safety data in man will be required to establish whether any of the procedures gives products which arc totally safe from NANBHV transmission and to assess their impact on other blood-borne-viruses.Corresponding author.     

HIV-1 gp41 heptad repeat 2 (HR2) possesses an amino acid domain that resembles the allergen domain in <Emphasis Type="Italic">Aspergillus fumigatus Asp f1</Emphasis> protein: review,hypothesis and implications

Enfuvirtide (ENF, T-20, Fuzeon) is the first synthetic peptide to be modeled according to the amino acid sequence of HIV-1 heptad repeat 2, which was used to treat cohorts of HIV-1-infected individuals who had failed to respond to treatment with the anti-HIV-1 cocktail HAART. It was reported that when injected subcutaneously, Enfuvirtide reduced viral RNA in patients’ blood by 1.96 log₁₀, leading to a subsequent increase in the number of CD4⁺ T cells in the blood. The drug treatment caused adverse effects at the injection site in a small number of treated individuals, and a gradual increase in IgE in the blood during prolonged treatment. Enfuvirtide was approved for treatment of HIV-1 patients who developed resistance to HAART. The present review attempts to explain the adverse effects of Enfuvirtide at the skin site of injection, and the gradual increase in IgE in patients’ blood during treatment. These phenomena were reported to resemble the effect of allergens that cause asthma in humans. It is hypothesized that since the amino acid domain of the Asp f1 allergen from Aspergillus fumigatus was identified in the N-terminus of an 18 kDa protein, it may be useful to compare Asp f1 peptide aa 7–22 from the β-hairpin sequence to the β-hairpin sequence of the heptad repeat 2 of HIV-1 gp41. The comparison revealed that the amino acid sequence resembles part of the Asp f1 aa 7–22 allergenic domain. The heptad repeat 1 of gp41 also resembles the fungal allergen. It is suggested that the Enfuvirtide peptide be tested experimentally to determine if ENF peptide is capable of binding to IgE antibodies from Enfuvirtide-treated, HIV-1-infected patients, and whether the HR2-derived peptide is capable of inducing basophils that were isolated from healthy individuals and from ENF-treated and untreated HIV-1 patients to release histamine and IL-4.