Production of a new terpenoid from biotransformation of (-)-isolongifolanol by Aspergillus niger and suppression of SOS-inducing activity

Abstract

The stereoselective oxidation of (—)-isolongifolanol (1) with a longifolene skeleton by Aspergillus niger (NBRC 4414) as a biocatalyst and suppressive effect on umuC gene expression by chemical mutagens furylfuramid and AFB1 of the SOS response in Salmonella typhimurium TA1535/pSK1002 were investigated. Compound 1 was converted to a new terpenoid, (-)-(2S,8R)-8,12-dihydroxy-isolongifolanol (2). Its structure was determined by NMR, IR, specific rotation and mass spectrometry. The metabolites suppressed the SOS-inducing activity of furylfuramid and AFB₁ in the umu test. Compound 1 suppressed 51% of the SOS-inducing activity against furylfuramid at < 1.0 mM. Compound 2 suppressed 15% and 24% of the SOS-inducing activity against furylfuramid and AFB1 at < 1.0 mM respectively.     

Abnormal ganglioside accumulation in cultured fibroblasts from patients with mucolipidosis IV.

Extracts of cultured skin fibroblasts derived from patients with mucolipidosis IV showed a marked increase and altered distribution of GM₃ and GD₃ gangliosides. GD₃ is elevated 1.5–2 times that of normal whereas GM₃ is elevated to a lesser extent. No abnormalities were found in the neutral glycolipids. These two gangliosides apparently comprise most of the accumulated lipid-like material observed on ultrastructural analysis in this disease.     

新型肝胆显影剂配体—Mebrofenin(莱溴氨乙酸)及其类似物的合成

通过溴化、成酐、氨解等反应,合成了新型肝胆显影剂配体(莱溴氨乙酸)及其四个未见报道的类似物。     

家蝇卵巢摄取卵黄蛋白的机理

在家蝇Musca domestica viaina 的卵黄发生过程中,卵母细胞摄取卵黄原蛋白与滤泡开放是相关的。观察不同发育时期的家蝇滤泡结果表明,在摄取活动最旺盛的时期也就是卵黄发生的顶盛时期,其滤泡开放程度最大,而在卵黄发生前期和后期基本上没有摄取活动,此时的滤泡上皮细胞间不开放。卵巢体外培养的激素处理表明,JH可以促进滤泡开放。家蝇卵巢微粒体制备物的Na⁺-K⁺ATP酶活力在卵巢发育过程中存在着动态变化。羽化后24小时时有一定的酶活性,随着卵黄发生的进行,酶活力逐渐增加,到羽化48小时时酶活力最高,然后又开始下降,到羽化72小时时已经很小。羽化32小时的家蝇点滴或注躬 JH之后,测得的卵巢微粒体制备物的Na⁺-K⁺ATP酶活力比正常羽化36小时的高,羽化44小时的家蝇点滴和注射JH之后,测得酶活力比正常羽化48小时的低。羽化36小时和48小时的家蝇卵巢微粒体制备物与JH共同作用后,其Na⁺-K⁺ATP酶的活力分别增加2.95倍和3.50倍,羽化48小时的家蝇卵巢在含有JH的培养液中培养启,其匀浆液的酶活性为对照组的1.26倍。 由此我们可以推测在家蝇的卵黄发生过程中,JH通过促进滤泡开放和增加卵巢微粒体制备物Na⁺-K⁺ATP酶的活力,从而调控卵母细胞对卵黄蛋白的摄取。     

Mutagenicity of BCNU and related chloroethylnitrosoureas in Drosophila.

BCNU and 10 related chloroethylnitrosoureas were tested for their ability to induce sex-linked recessive lethals in Drosophila spermatozoa. All chloroethylnitrosoureas tested were potent mutagens. Among the substances with one chloroethylnitrosourea group, chlorozotocin, BCNU and methanesulfonyloxyethyl chloroethylnitrosourea exhibited the strongest mutagenic effects. Two hydroxyalkyl chloroethylnitrosoureas behaved as potent mutagens too, although the mutation frequencies obtained were one order of magnitude lower relative to the other substances. Among the compounds with two chloroethylnitrosourea groups, bisCNU-ethane and bisCNU-diphenylmethane were most active. When the interconnecting polymethylene chain was elongated from 2 methylene groups (bisCNU-ethane) to 6 methylene groups (bisCNU-hexane), the mutagenic activity decreased by a factor of 2. The mutagenic activity of polymethylene bischloroethylnitrosoureas with connecting chains of intermediate length was not different from bisCNU-hexane. Differences in mutagenic activity were supposed to reflect different concentrations reaching the target cells, possibly in part as a result of differences in transportability of the substances.     

On the specificity of naloxone as an opiate antagonist.

Since the discovery of endogenous opioid peptides in brain (68,69,97,113, 128) and the pituitary gland (26,81,105,125) there has been considerable interest in their possible roles in a variety of physiological and pharmacological processes. Many studies have used antagonism by naloxone as a criterion for implicating endogenous opiates in a process, assuming that naloxene has no pharmacological actions other than those related to blockade of opiate receptors. The doses of naloxene used are often higher than those required to antagonize the analgesic and other effects of morphine. However, multiple forms of opiate receptors are present in nervous tissue and higher concentrations of naloxene are required to antagonize effects mediated by some of these receptors (83). Although the earlier literature supports the assumption that the effects of naloxene are due to the blockade of opiate receptors (87), there are an increasing number of reports which indicate that naloxene may have pharmacological actions unrelated to opiate receptor blockade. The subsequent review serves to emphasize that antagonism by naloxene is a necessary but not sufficient criterion for invoking the mediation of a response by an endogenous opiate (61). Additional lines of evidence which serve to strengthen the conclusion that endogenous opiates mediate a process will be considered.     

球形芽孢杆菌C3-41对致倦库蚊的毒效及在蚊体内的再循环

球形芽孢杆菌Csub3-41菌株(Bacillus sphaericus C3-41)对致倦库蚊(Culex puinquefa-seiatus)幼虫有很高毒效,对2龄和3-4龄幼虫的半致死剂量(LD₅₀)分别为63.1 和89.7芽孢/蚊幼虫。处理浓度越高,取食时间越长,蚊幼虫取食到的杀蚊活性物质量越多,死亡率越高。当蚊幼虫取食亚致死剂量杀蚊活性物质后,球形芽孢杆菌在感染的活幼虫体内不增殖;但当蚊幼虫取食致死剂量杀蚊活性物质后,蚊幼死亡,球形芽孢杆菌在死蚊幼虫体内增殖明显,6天内芽孢从感染初期的1.86X10²蚊幼虫增加到1.59X10⁶/蚊幼虫。芽孢在死蚊幼虫体内能正常萌发、生长、产孢和形成毒素。增殖的芽孢同样对致倦库蚊幼虫有较高毒力。     

猪毛蒿精油杀虫的有效成分

生物活性筛选试验表明,菊科植物猪毛蒿(Artemisia scoparia Waldst. Et Kitag)全草精油具杀虫活性。采用GC-MS方法分析了猪毛蒿精油的化学成分。共检出92个成分,鉴定了其中46个成分。通过柱层析分离出主成分,经各种波谱分析鉴定为1-苯基-2,4-己二炔。活性跟踪结果表明,l-苯基-2,4-己二炔为猪毛蒿精油中的主要杀虫成分。     

Synthesis and study of the labeling of pregnenolone and progesterone specifically tritiated at the 17 position

The action of tritiated acetic acid on 17-bromopreg-[3_H] nenolone acetate treated with zinc metal dust produces 17 pregnenolone acetate which is then hydrolyzed to form 17 [3_H] pregnenolone.The flavobacterium dehydrogenans transforms the 17-bromopregnenolone into 17-bromoprogesterone which can also be tritiated by tritiated acetic acid to obtain 17 [3_H] progesterone. The study of the label distribution by different analytic techniques (I.R., nuclear magnetic resonance, mass spectrometry) as well as the. chemical and selective biochemical reactions indicate a specific labeling higher than 85% on the 17 position.     

Lack of effect of excitatory amino acids on endogenous cyclic AMP levels in rat cerebrocortical tissue in vitro.

The spin-traps, 5,5′-Dimethyl-1-pyrroline-1-oxide and phenyltertiary-butylnitrone have been used to investigate the primary free radical involved in lipid peroxidation. In this report, we wish to present evidence that a NADPH-dependent hydroxyl radical (OH·), which may be the primary free radical that initiates lipid peroxidation, is generated in liver microsomes. A mechanism for the generation of the hydroxyl radical in liver microsomes is also postulated.     

Unique presence of 2-methylthio-ribosylzeatin in the transfer ribonucleic acid of the bacterium Pseudomonas aeruginosa

Analysis of ³⁵S labled nucleosides prepared from tRNA of Pseudomonas aeruginosa by phosphocellulose column chromatography, thin layer chromatography and Sephadex LH-20 column chromatography revealed the presence of 2-methylthioribosylzeatin in it.     

Membrane reconstitution in chl-r mutants of Escherichia coli K 12 VI. Morphological study of membrane assembly during complementation between extracts of chl-r mutants

The particles formed during the complementation between supernatant extracts of mutants chl A⁻ and chl B⁻ of Escherichia coli K 12 have been examined under the electron microscope. These particles look like membranous formations with a vesicular structure limited by a triple-layered membrane. The observations made on these particles at various incubation times during complementation show that the aggregation progresses through several stages of organization. When the phenomenon becomes steady, the population of reaggregated particles shows a large structural heterogeneity: it consists of small aggregates, filaments and particulary well-organized closed vesicles. As we had previously shown for the reconstitution of nitrate reductase, the rate of formation and the structure of newly formed aggregates depend on various parameters (temperature, dialysis).     

Mutagenesis in cultured human diploid cells. III. Induction of 8-azaguanine-resistant mutations by furylfuramide.

Trans-2-(2-furyl)-3-(5-nitro-2-furyl) acrylamide (furylfuramide: FF or AF2) was tested for ability to induce 8-azaguanine (8AG) resistant mutations in cultured human diploid cells. FF had a relatively severe cytotoxic effect on the cells. From the concentration-survival curve, the D0 value for 2-h treatment with FF was estimated to be 11 mug/ml. When cells were treated with FF at various concentrations for 2 h, cultured in normal medium for 48 h, and then selected in medium containing 8AG at 30 mug/ml, the induced mutation frequency increased gradually with increase in concentration of FF. When cells were treated with FF at 10 mug/ml for 2 h, cultured in normal medium for various periods of mutation expression time, and selected with 8AG at 30 mug/ml, the highest induced mutation frequency was obtained with 48 h of mutation expression time. Microscopic examination of the numbers of cells in colonies indicated that the total number of cells increased by half during this mutation expression time of 48 h.     

Purification and succinylation of cyclic GMP from large volume samples and radioimmunoassay of succinyl cyclic GMP.

Improved procedures for isolation of cyclic GMP and cyclic AMP and radioimmunoassay of cyclic GMP with succinylation are described. Procedures involved include modified chromatography on alumina and succinylation of cyclic GMP followed by purification of succinyl cyclic GMP on a Dowex AG 1×8 column. These procedures are convenient and applicable to any volume up to 50 ml of tissue extracts and especially for isotonic incubation mixtures. This assay system is sensitive to 6 femtomoles of cyclic GMP/tube. On radioimmunoassay, free and antibody bound [¹²⁵I]-labeled cyclic GMP are separated by Millipore filtration. Cyclic GMP levels in several tissue samples were determined in order to show the applicability of the procedures.     

三棱的化学成分研究

目的：研究三棱Sparganium stoloniferum Buch．-Ham．的化学成分。方法：采用硅胶柱层析,Sephadex LH-20,ODSC-18,重结晶等方法,根据理化性质和光谱鉴定化合物的结构。结果：从三棱中得到8个化合物,分别为棕榈酸（1）,5-羟甲基糠醛（2）,6,7,10-三羟基-8-十八烯酸（3）,棕榈酸单甘油酯（4）,5-Hydroxy-2-（hydroxymethyl）pyridine（5）,β-谷甾醇（β-sitosterot）（6）,β-胡萝卜苷（daucosterol）（7）,Betulinic acid（8）。结论：化合物5,8为首次从该植物中分离得到。