Goniothalamicin and annonacin: Bioactive acetogenins fromGoniothalamus giganteus (Annonaceae)

Summary Using brine shrimp lethality for activity-directed fractionation, goniothalamicin (I), a new tetrahydroxy-mono-tetrahydrofuran fatty acid -lactone (acetogenin), has been isolated from ethanolic extracts of the stem bark ofGoniothalamus giganteus Hook. f., Thomas (Annonaceae). This novel compound was found to be cytotoxic and insecticidal and inhibited the formation of crown gall tumors on potato discs. Annonacin (II), the only other reported mono-tetrahydrofuran acetogenin, was also isolated; the previously reported 9ASK (astrocytoma reversal) activity ofII was confirmed, andII is now also found to be weakly active against 3PS murine leukemia.     

Pharmacodynamic profile of CQP 201-403, a novel 8α-amino-ergoline

Summary The profile of action in animals of CQP 201-403, a novel 8-amino-ergoline, is in most aspects that of a very potent dopaminomimetic, both as a prolactin secretion inhibitor, and at the levels of the CNS and the cardiovascular system. Qualitatively CQP 201-403 differs slightly from bromocriptine and apomorphine in its effects on the CNS (no influence on serotonin metabolism in the rat cortex; induction of masculine mounting behavior in rats) and the cardiovascular system of the dog (reflex tachycardia in response to a blood-pressure fall). In man the new compound proved to be highly active in lowering prolactin serum levels and to be more potent than bromocriptine (Parlodel^®).In memory of Dr Annemarie Closse, who died 14 June 1987.     

In vitro protein synthesis and α amylase activity in F cells from hepatopancreas ofPalaemon serratus (Crustacea; Decapoda)

In crustaceans, all the steps in the assimilation of food take place in the hepatopancreas. To facilitate the study of this organ, a method for the dissociation of cell types was developed. The hepatopancreas of the prawnPalaemon serratus was mechanically dissociated and the cells separated by Percoll density-gradient centrifugation. The E and R cells had similar densities of around 1.05 g/ml. The F cells were separated into two distinct fractions with densities of 1.075 and 1.082 g/ml. The B cells sedimented at a density of 1.12 g/ml. The ratio between the two populations of F cells was found to vary during the intermolt cycle while B cells disappeared after the molt. When the density gradient fractions were incubated with³H-leucine, incorporation was highest in the F cell fractions. Measurements of -amylase activity, indicated that the two populations of F cells may be derived from the same cell type.     

Antidiuretic effects of oxytocin in the Brattleboro rat

Summary The antidiuretic activity of oxytocin (OT) was measured in Brattleboro rats with congenital diabetes insipidus. A dose dependent antidiuretic response was found in animals receiving chronic infusions of 0.1 g/h, 1.0 g/h, and 5 g/h of OT. OT infused at the rate of 5 g/h over a 7-day period completely reversed the symptoms of diabetes insipidus. The results support the concept that OT serves as a weak agonist of vasopressin at the level of the kidney and at pharmacological levels exhibits antidiuretic activity.     

微生物共培养产生新颖活性次生代谢产物的研究进展

微生物源天然产物是药物先导化合物的重要资源之一.近年来,利用微生物共培养产生各类天然产物的研究发展迅速.微生物共培养是一种通过模拟（微生物）栖息地/栖息环境以激活可能的沉默生物合成基因簇并进而诱导微生物产生新次生代谢物的有效方法.与菌株纯培养相比,共培养不仅增加了次级代谢产物的种类多样性,而且其生物活性及产量也得到了提高.文章就近5年来真菌与真菌、真菌与细菌、细菌与细菌等3种类型的微生物共培养研究成果进行了综述,同时简要介绍了用于分析共培养作用机制的多组学技术,并在此基础上探讨了微生物共培养相互作用机制研究的进展及挑战.综述旨在为微生物共培养的深入研究提供借鉴,并为微生物药物的开发提供新思路.     

胍基化壳聚糖季铵盐的制备及其抗菌性能

以三聚氯氰(TCT)为中间桥梁,将聚六亚甲基双胍(PHMB)接枝到N-(2-羟丙基-3-甲基氯化铵)壳聚糖(HTCC)上,制备胍基壳聚糖季铵盐(HCP).研究制备HCP的最佳反应条件,采用元素分析、傅里叶变换红外光谱(FTIR)和核磁共振氢谱(¹H NMR)对产物的结构进行表征,并测试其抗菌性能.得到HCP的最佳反应条件为HTCC和TCT的摩尔比1.0∶2.5,HTCC和PHMB的质量比1.0∶1.2,缚酸剂为三乙胺,TCT一取代的反应时间8 h,二取代的反应时间14 h,反应温度40℃.结果表明：制得的HCP对大肠杆菌(E.coli)和金黄色葡萄球菌(S.aureus)的最低抑菌质量浓度分别为0.020,0.005 mg·mL^-1;质量浓度为1.0 mg·mL^-1的HCP对E.coli和S.aureus的抑菌率分别为89.8%和100.0%,高于相同质量浓度下HTCC对E.coli和S.aureus的抑菌率18.2%和18.7%.     

鄂尔多斯盆地长7储层致密油水平井CO2补充能量与吞吐参数优化

长7储层是鄂尔多斯盆地主要的致密区块,近一半的致密油分布其中。针对长7储层开采渗透率低、开采难度大、依靠弹性开采产能较低、能量衰竭较快等问题,通过数值模拟的方法,构建水平井分段压裂数值模拟模型,首先对比不同吞吐方式对油田产能的影响,优选出CO₂吞吐为首选的补充能量方式。其次对井网形式、井网参数及吞吐参数进行优化研究。最终优选出合适的吞吐方案,达到提高生产效率的目的。结果表明,该储层的最优注采吞吐参数为：周期注入量为2 673 t、注入压力为21 MPa、注入速度为90 t/d、焖井时间为10 d。研究对鄂尔多斯盆地长7储层提高采收率具有一定的参考意义。     

高岭土负载绿色合成纳米铁的制备及其对孔雀石绿和铅离子的去除性能研究

红背桂树叶提取物绿色合成铁纳米颗粒（Fe NPs）在水环境修复领域具有很高的应用潜力。但由于Fe NPs存在团聚、易氧化等不稳定因素,在去除污染物时抑制了反应活性。为了解决这一问题,使用一步法制备了高岭土负载Fe NPs （K-Fe NPs）,并系统地检测了其对孔雀石绿和Pb²⁺混合污染物的去除反应活性。采用X射线衍射（XRD）和傅里叶红外光谱（FTIR）对Fe NPs、高岭土和K-Fe NPs进行表征和分析。3种材料对比实验结果表明,K-Fe NPs对单独的孔雀石绿和Pb²⁺的去除效率（99.10%和93.41%）优于Fe NPs（93.67%和85.33%）和高岭土（32.54%和12.50%）。此外,K-Fe NPs经过4次重复循环对孔雀石绿和Pb²⁺的去除率仍分别为74.02%和55.48%。结果表明,K-Fe NPs在染料和重金属离子复合污染修复领域具有一定应用前景。