Δ 9(15)-Africanene,a new sesquiterpene hydrocarbon from the soft coralSinularia erecta

Summary The isolation and structural elucidation of ⁹⁽¹⁵⁾-africanene from the soft coralSinularia erecta is presented.     

Wirkung von 6β-Methoxy-9β,10α-pregna-4,6-dien-3,20-dion

Summary 6-Methoxy-9,10 -pregna-4,6-diene-3,20-dione inhibites the ⁴-3-oxosteroid-5-reduction in microsomes and the ⁴-3-oxosteroid-5-reduction in the soluble fraction of male rat liver. The 3- and 3-hydroxysteroid dehydrogenase are not inhibited by this substance.

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Diese Arbeit wurde von der Firma Hoffmann-La Roche, Basel, unterstützt.     

A simple synthesis of (E)-3-formylbut-2-enenitrile,and its use as a precursor of isotope-labelled zeatin and (±) dihydrozeatin

Summary (E)-3-Formylbut-2-enenitrile (4) is synthesized in 2 steps by reacting pyruvaldehyde dimethylacetal and acetonitrile in the presence of sodium methoxide, followed by acid hydrolysis to give 58% overall yield on distillation. The aldehyde4 can be stepwise and selectively reduced to (E)-3-hydroxymethylbut-2-enylamine (7a) in 37% total yield or exhaustivelyb reduced in 1 step to (±)-4-hydroxy-3-methylbutylamine (6) in 46% total yield. Compound7a and6 can be condensed with 6-chloropurine to give zeatin and (±)dihydrozeatin respectively. This provides a readily accessible method for isotope-labelled zeatin and its derivatives at side chain.Contribution No. 1064, Alberta Research CouncilProcess for the Preparation oftrans-3-formylbut-2-enenitrile S. Chen and J. MacTaggart, patent applicatioin registered in Canada and the United States of America.Acknowledgment. The author thanks Mr J. M. MacTaggart and Mrs C. M. Goulet for valuable experimental assistance and Dr R. M. Elofson for helpful discussions.     

Totally synthetic (±)-13-Alkyl-3-hydroxy and methoxy-gona-1,3,5(10)-trien-17-ones and related compounds

Zusammenfassung Von mehreren (±) 3-Oxy- und (±) 3-Methoxy-13-alkylgona-1,3,5(10)trien-17-onen und verwandten Verbindungen, einschliesslich von Vertretern der (±) 13-Alkylgon-4-en-3-on-Reihe, werden Totalsynthese und biologische Wirksamkeit beschrieben.     

Identification of 3α, 17α, 21-trihydroxy-5α-pregnane (allotetrahydro-17α-hydroxy-cortexone) and 3α,21-dihydroxy-5α-pregnane (allo-tetrahydro-cortexone) in human urine

Résumé Le 3, 17, 21-trihydroxy 5-pregnane (allo-tétrahydro-17-hydroxy-cortexone) et le 3,21-dihydroxy 5-prégane (allo-tétrahydro-cortexone) ont été identifiés dans l'urine humaine. Ces composés avaient les mêmes migrations chromatographiques avant ou après acétylation ou oxydation que les respectifs stéroïdes de synthèse.     

Purification and characterization of aβ-glucosidase (linamarase) from the haemolymph ofZygaena trifolii Esper, 1783 (Insecta,Lepidoptera)

Summary A -glucosidase (linamarase) was purified 52-fold with a recovery of 27% from the haemolymph of the larvae ofZygaena trifolii, ESPER, 1783 (Lepidoptera, Zygaenidae). The final enzyme preparation was found to be nearly homogeneous on both disc polyacrylamide gel electrophoresis and SDS-polyacrylamide gel electrophoresis. The molecular weight of the enzyme was determined to be about 130 kDa; it consisted of two subunits of about 66 kDa. The enzyme showed an optimum between pH 4.5 and 5 with linamarin and a broad optimum between pH 3.5 and 6.5 for p-nitrophenyl--D-glucoside; the temperature optimum was 40°C. The -glucosidase showed a high specificity for its endogenous substrates linamarin and lotaustralin. Among the other natural and artificial substrates tested, only prunasin and p-nitrophenyl--D-glucoside were hydrolyzed by the enzyme, whereas linustatin, salicin, cellobiose and trehalose were not. The enzyme is strongly inhibited by -glucosylpiperidine.     

Über die Wirkung von Phenanthrenchinon (9, 10) und einer wasserlöslichen Transportform auf Glykolyse und Atmung des Ascites-Tumor

Summary Phenanthrenchinon (9, 10) and hydrochinon-bis-glycylester prepared as water-soluble transportform, are strong inhibitors of glycolysis. Glycolysing cells are depleted from ATP in a few minutes.     

9-α-hydroxyparthenolide,a novel antitumor sesquiterpene lactone fromAnvillea garcini (Burm.) DC1

Summary A novel sesquiterpene lactone, 9--hydroxyparthenolide (1) was isolated from a chloroform extract ofAnvillea garcini that was collected in Iran. The structure of1 was assigned on the basis of high field NMR decoupling experiments and other spectroscopic evidence. This -methylene lactone has shown significant activity in both the 9KB cell culture and P388 mouse leukemia test systems.The authors acknowledge the support of contract No. N01-CM-97296 from the National Cancer Institute and the use of the Purdue University Biochemical Magnetic Resonance Laboratory (NIH grant No. RR01077). This is paper 16 in the series Potential Antitumor Agents.     

1-(3′-methoxy-4′-hydroxy benzyl) 6–7 dimethoxy isoquinoline,a major metabolite of papaverine

Zusammenfassung An Glukorons?ure gebundenes 1-(3′-Methoxy-4′-hydroxy-phenyl)-6, 7-dimethoxy-chinolin ist als Metabolit des Papaverins beim Menschen und bei S?ugetieren erkannt und isoliert worden. Ein in den Lebermikrosomen enthaltenes Ferment, dassauerstoff-und TPNH-abh?ngig ist, bewirkt die Methoxylspaltung, und ein weiteres Ferment übertr?gt die Glukurons?ure aus ihrer Verbindung mit Uridinphosphat auf die entstandene phenolische Verbindung.      

12-Hydroxy-E-γ-bisabolene,a new sesquiterpene alcohol from a Caribbean sea whip of the genusPseudopterogorgia (Gorgonacea,Cnidaria)

Summary A new sesquiterpene alcohol, 12-hydroxy-E--bisabolene, is reported from an undescribed Caribbean sea whip of the genusPseudopterogorgia. The structure of this new alcohol was established based upon spectral analyses and through chemical interconversions.Acknowledgment. This research was supported by NOAA, Office of Sea Grant, Department of Commerce, under grant NA80AA-D-00120, and in part by the California State Resources Agency, project R/MP-22. The U.S. Government is authorized to reproduce and distribute reprints. We wish to acknowledge the mass spectral support provided by the Bioorganic Biomedical Mass Spectrometry Resource Center, University of California, San Francisco (A.L. Burlingame, Director) which is supported through NIH grant RR00719.     

热性惊厥儿童血液IL-6、IL-10和MMP-9表达的研究

目的 热性惊厥是儿童痫性发作最常见的形式.炎性细胞因子可能导致热性惊厥的发展.本研究探讨白介素-6(IL-6)、白介素-10(IL-100和金属蛋白酶-9(MMP-9)等炎性细胞因子在小儿热性惊厥中是否被激活以及其表达与原发性癫痫中的不同.方法 回顾性研究自2010年12月到2012年11月入院的相关病人资料.分热性惊厥组(N=43)、高热对照组(N=40)、原发性癫痫组(N=32)及正常儿童组(N=15).在惊厥发生的24h内收集病人血液.酶联免疫吸附试验(ELISA)进行IL-6、IL-10和MMP-9等细胞因子水平测定.结果 IL-6、IL-10和MMP-9在热性惊厥组的表达均高于原发性癫痫组(p＜0.05)和正常组(p＜0.05).IL-6与MMP-9在热性惊厥组的表达高于高热对照组,IL-10的表达在热性惊厥组与高热对照组之间无明显差异(P＞0.05).结论 IL-6、IL-10和MMP-9在热性惊厥儿童表达明显升高;炎性因子可能参与热性惊厥的病理过程,且其参与机制可能不同于其在原发性癫痫病理过程中的作用.     

Nα-quinaldyl-L-arginine·HCl,a new defensive alkaloid fromSubcoccinella-24-punctata (Coleoptera,Coccinellidae)

The isolation of N-quinaldyl-L-arginine·HCl (1) from the CoccinellidaeSubcoccinella-24-punctata is reported. The structure, first established on the basis of the analysis of the spectral properties of1, has been confirmed by synthesis. The alkaloid is of endogenous origin and markedly deterrent to ants.     

Hashish: Synthesis of Δ9-tetrahydrocannabinol (THC), a metabolite ofΔ 9-THC1

Summary The synthesis of (±)-211-dihydroxy- ⁹-THC, a difunctionalized metabolite of ⁹-THC, is presented.Acknowledgment. This work was carried out with the support of NIDA Grant No. DA 00574. We are grateful to Mr. J. Coe for assistance with some of the experiments.     

Cytogenetic effects of delta-9-tetrahydrocannabinol (Δ 9-THC) on hamster bone marrow

Summary Single s.c. injections of 10 or 1000 mg/kg of ⁹-THC did not induce discernable chromosomal damage but caused significant mitotic inhibition in the bone marrow of Syrian hamsters.Acknowledgments. The authors which to thank Mr R.H. Graham, Department of National Health and Welfare, Health Protection Branch, for the generous supply of ⁹-THC. This research was supported by a grant to Dr M.G. Joneja from the Department of National Health and Welfare.     

α-L-aspartyl-L-alanine (a neural dipeptide) enhances synaptic transmission

Summary -L-aspartyl-L-alanine, a dipeptide found in the brain, increases the amplitude of the miniature endplate potentials (MEPPs) in phrenic nerve-diaphragm preparations from rats. The peptide also stimulates the appearance of a population of giant MEPPs.This work was supported by NSF grant BNS 79-00352 and NIH grant CA-27031 to R. Lim.     

Aln (n = 3, 4, 6, 13, 19)团簇的结构稳定性与形态演化

采用第一原理赝势平面波方法, 计算了不同结构形态Al_n (n = 3, 4, 6, 13, 19)团簇的几何与电子结构, 通过结合能与HOMO-LUMO能隙表征和分析了其结构稳定性, 采用线性同步转变 (LST)方法考察了其不同结构形态间的演化与转 变. 结果表明: Al₃, Al₄, Al₆, Al₁₃和Al₁₉团簇的稳定结构形态分别为三角形、 菱形、八面体、二十面体、双二十面体. Al₃, Al₄与Al₁₃团簇不存在亚稳结构. Al6与Al19团簇存在亚稳结构, 其结构形态分别为平行四边形与八面体. Al₆团簇亚稳结构与稳定结构的能级差大、转变能垒低, 结构转变容易, 亚稳结构稳定性差. 而Al₁₉团簇亚稳结构与稳定结构的能级差小、转变能垒高, 结构演化不易, 因而实验和理论模拟中能观察到其亚稳结构形态——正八面体的存在.     

2,2′-dihydroxy-6,6′-dinaphthyl disulphide (DDD) diazo blue B reactive granules in the parathyroid gland of the rat and toad

Zusammenfassung Granula in Parenchymzellen von Ratten und Kröten-Epithelkörperchen treten durch 2,2-Dihydroxy-6,6-dinaphthyl-disulfid (DDD) Diazo-Blau-B-gefärbt, deutlich hervor. Ihre Menge, Färbbarkeit und Verteilung unter verschiedenen Bedingungen scheinen für die zelluläre Sekretionstätigkeit charakteristisch zu sein.     

10-Hydroxy-Δ2-decenoic acid in the honeybee(Apis mellifera)

Zusammenfassung Die Mandibulardrüsen der Honigbienen-Arbeiterinnen enthalten 10-Hydroxy-²-decensäure. Es wird angenommen, dass diese Drüsen die Quelle der im Weisel- und Arbeiterinnenlarvenfutter vorkommenden 10-Hydroxy-²-decensäure sind.     

模糊集生成的格的(λ,T)-模糊理想(滤子)

提出了由模糊子集生成的(λ,T)-模糊理想(滤子)的概念,并且用三角范数的性质及生成理想的概念刻画了(λ,T)-模糊理想(滤子)。研究了由模糊集生成的(λ,T)-模糊理想的逆像在同态映射下与模糊集的逆像生成的(λ,T)-模糊理想是相等的。     

Synthesis ofO 1.5-(β-D-galactopyranosyl) [DMet2, Hyp5] enkephalin amide,a new highly potent analgesic enkephalin-related glycosyl peptide

Summary A new series of O-glycosyl enkephalins has been prepared, following a convergent strategy, with high chemical yields. The galactosyl analogue,O ^1.5-(-D-galactopyranosyl) [DMet², Hyp⁵] enkephalin amide proved to be one of the most potent in vivo opioid agonists synthesized up to now.