环肽研究新进展

本文对近年来环肽的合成方法及环肽的性质和应用的新进展进行了评述。     

环糊精醛及其衍生物的合成与性能研究进展

综述了环糊精醛及其衍生物的合成、分子识别作用和模拟酶催化方面的最新研究进展.     

甲烷单加氧酶化学模拟研究进展

本文综述了近年来对甲烷单加氧酶进行结构模拟和催化功能模拟研究工作的进展情况。就结构模拟而言，已合成和表征了很多模型化合物，并与天然酶进行了比较，获得了一些能较好地再现天然酶活性中心结构特征和诺学特征的模型化合物。在催化功能模拟方面，少数体系能将环己烷等经类转化为醇类或酮类。而真正能把甲烷转化成甲醇的体系仅有一例报道，这方面的工作比较薄弱，尚待加强。     

泽泻三萜类成分的提取工艺优化及活性评价

建立泽泻中三萜类成分的最佳提取工艺,并考察其对老年性耳聋小鼠血清生理学指标的影响.通过正交试验优化泽泻三萜类成分的提取工艺,并用紫外分光光度法(UV)测定含量.采用D-半乳糖建立小鼠老年性耳聋模型,灌胃给予泽泻三萜类成分提取物后,测定小鼠血清丙二醛(MDA)含量和超氧化物歧化酶(SOD)活力.结果表明:泽泻三萜类成分的...     

蛹虫草超氧化物歧化酶理化性质的研究

超氧化物歧化酶[Superoxide d ismutase,SOD,(EC.1.15.1.1)]是广泛存在于生物体内的超氧阴离子自由基(·O2-)的天然清除剂,在机体保护方面起重要作用。在对SOD进行的一系列研究中,发现SOD的存在与生物体抗衰老、抗肿瘤、营养状况、免疫性疾病、炎症及辐射防护[1]有关。许多动植     

仿硒酶研究进展

硒是人体中必需的微量元素,它与各种疾病和人类健康息息相关。硒在生物体内以硒代半胱氨酸形式表现其生理活性和功能。为了探索硒在硒蛋白中结构和功能关系并可能发展成硒相关的适用药物,人们付出许多努力来发展硒蛋白模拟化学。由于硒酶—谷胱甘肽过氧化物酶（GPX）重要的抗氧化作用以及潜在的药用价值,国际上广泛开展了对它的人工模拟研究。本文对近年来硒酶模拟化学和生物学相关研究进展进行了综述。     

A small-molecule catalyst of protein folding in vitro and in vivo

BACKGROUND: The formation of native disulfide bonds between cysteine residues often limits the rate and yield of protein folding. The enzyme protein disulfide isomerase (PDI) catalyzes the interchange of disulfide bonds in substrate proteins. The two -Cys-Gly-His-Cys- active sites of PDI provide a thiol that has a low pKa value and a disulfide bond of high reduction potential (Eo'). RESULTS: A synthetic small-molecule dithiol, (+/-)-trans-1,2-bis(2-mercaptoacetamido)cyclohexane (BMC), has a pKa value of 8.3 and an Eo' value of -0.24 V. These values are similar to those of the PDI active sites. BMC catalyzes the activation of scrambled ribonuclease A, an inactive enzyme with non-native disulfide bonds, and doubles the yield of active enzyme. A monothiol analog of BMC, N-methylmercaptoacetamide, is a less efficient catalyst than BMC. BMC in the growth medium of Saccharomyces cerevisiae cells increases by > threefold the heterologous secretion of Schizosaccharomyces pombe acid phosphatase, which has eight disulfide bonds. This effect is similar to that from the overproduction of PDI in the S. cerevisiae cells, indicating that BMC, like PDI, can catalyze protein folding in vivo. CONCLUSIONS: A small-molecule dithiol with a low thiol pKa value and high disulfide Eo' value can mimic PDI by catalyzing the formation of native disulfide bonds in proteins, both in vitro and in vivo.     

Photocytotoxic and anaerobic DNA cleavage activity of binuclear 3,3′-dithiodipropionic acid cobalt(II) complexes having phenanthroline bases

Dicobalt(II) complexes [{(B)Co^II}₂(μ-dtdp)₂] (1–3) of 3,3′-dithiodipropionic acid (dtdp) and phenanthroline bases (B), viz. 1,10-phenanthroline (phen in 1), dipyrido[3,2-d:2′,3′-f]quinoxaline (dpq in 2) and dipyrido[3,2-a:2′,3′-c]phenazine (dppz in 3), have been prepared, characterized and their photo-induced anaerobic DNA cleavage activity studied. The elemental analysis and mass spectral data suggest binuclear formulation of the complexes. The redox inactive complexes have magnetically non-interacting dicobalt(II) core showing magnetic moment of ∼3.9 μ_B per cobalt(II) center. The complexes show good binding propensity to calf thymus DNA giving K_b values within 4.3 × 10⁵–4.0 × 10⁶ M⁻¹. Thermal melting and viscosity data predict DNA groove binding and/or partial intercalative nature of the complexes. The complexes show significant anaerobic DNA cleavage activity in green light under argon atmosphere possibly involving radical species generated from the disulfide moiety in a type-I pathway. The DNA cleavage reaction under aerobic medium in green light is found to involve hydroxyl radical species. The dppz complex 3 exhibits significant photocytotoxicity in HeLa cervical cancer cells with an IC₅₀ value of 2.3 μM in UV-A light of 365 nm, while it is essentially non-toxic in dark giving an IC₅₀ value of >200 μM. A significant reduction of the dark toxicity of the organic dppz base (IC₅₀ = 8.3 μM in dark) is observed on binding to the cobalt(II) center while essentially retaining its photocytotoxicity in UV-A light (IC₅₀ = 0.4 μM).