Enantiospecific total synthesis of aciphyllene

Enantiospecific total synthesis of the sesquiterpene aciphyllene and its three epimers have been described starting from the readily available monoterpene (R)-limonene employing an intramolecular type II carbonyl ene reaction as the key step. (C) 2010 Elsevier Ltd. All rights reserved.

Enantiospecific first total synthesis and confirmation of the relative and absolute stereostructure of isocalamusenone

The enantiospecific total synthesis of two epimers of the sesquiterpene isocalamusenone has been accomplished starting from the readily available monoterpene (R)-limonene which of the natural product established the stereostructure and the absolute configuration (C) 2010 Elsevier Ltd All rights reserved

Enantiospecific approach to AB-ring system of the diterpenes fusicoccanes

Enantiospecific synthesis of the AB ring system of 5-8-5 tricyclic diterpenes fusicoccanes has been accomplished, starting from the readily available monoterpene (R)-limonene employing an reaction as the key step.

Enantiospecific synthesis and confirmation of the relative and absolute stereostructure of 11-hydroxyguaiadienes

Enantiospecific total synthesis of two epimeric sesquiterpenes 11-hydroxyguaiadienes has been accomplished starting from the readily available monoterpene (R)-limonene, which confirmed the structure and absolute configuration of the natural products. (C) 2010 Elsevier Ltd. All rights reserved.

Model studies directed towards the synthesis of functionalised chiral A-ring derivatives of taxanes

Model studies, starting from the monoterpene R-carvone, directed towards the synthesis of chiral A-ring derivatives of taxanes with oxygen functionalities at C-2, 9 and 13 carbon atoms as in taxol is described.

An enantiospecific approach to 8,9-seco-C-aromatic taxanes

An enantiospecific approach to functionalised C-aromatic-8,9-seco-taxanes starting from the readily available monoterpene (R)-carvone is described.

A convenient enantiospecific methodology for (-)-(1R,5S)-1,5-dimethylbicyclo[3.3.0]octa-2,7-dione: A formal total synthesis of (-)-ceratopicanol

An enantiospecific formal total synthesis of (-)-ceratopicanol starting from the readily and abundantly available monoterpene (R)-limonene is described. A combination of Claisen rearrangement-intramolecular diazo-ketone cyclopropanation-regiospecific reductive cyclopropane cleavage reactions are employed for the stereo- and regiospecific generation of the two vicinal ring junction quaternary carbon atoms.

An Enantiospecific Approach to Irregular Ligusticum grayi Sesquiterpenes: Synthesis of cis-Preisothapsa-2,8(12)-diene

Enantiospecific syntheses of 1-epi- (or cis-)-preisothapsa-2,8(12)-diene and 1-epi- and 1,8-diepipreisothapsa-2-en-12-ols, starting from the readily available monoterpene (R)-carvone, have been accomplished.

Enantiospecific First Total Synthesis of ent-Allothapsenol

The enantiospecific first total synthesis of the enantiomer of the irregular sesquiterpene from Ligusticumgrayi allothapsenol, starting from the readily available monoterpene (R)-carvone, is described, which confirmed the assumed absolute configuration of the natural product.

The substrate dependent competitive formation of cyclobutanones and cyclopentanones in an intramolecular rhodium carbenoid CH insertion reaction: enantiospecific total synthesis of silphiperfol-6-ene

The enantiospecific total synthesis of silphiperfol-6-ene has been accomplished starting from the readily available monoterpene (R)-limonene, employing a rhodium carbenoid insertion into the CH bond of a tertiary methyl group. A substrate dependent competitive insertion of the rhodium carbenoid in the gamma- and beta-CH bonds to form cyclopentanone and cyclobutanones, respectively, has been described. (C) 2012 Elsevier Ltd. All rights reserved.

Functional characterization, homology modeling and docking studies of beta-glucosidase responsible for bioactivation of cyanogenic hydroxynitrile glucosides from Leucaena leucocephala (subabul)

Glycosyl hydrolase family 1 beta-glucosidases are important enzymes that serve many diverse functions in plants including defense, whereby hydrolyzing the defensive compounds such as hydroxynitrile glucosides. A hydroxynitrile glucoside cleaving beta-glucosidase gene (Llbglu1) was isolated from Leucaena leucocephala, cloned into pET-28a (+) and expressed in E. coli BL21 (DE3) cells. The recombinant enzyme was purified by Ni-NTA affinity chromatography. The optimal temperature and pH for this beta-glucosidase were found to be 45 A degrees C and 4.8, respectively. The purified Llbglu1 enzyme hydrolyzed the synthetic glycosides, pNPGlucoside (pNPGlc) and pNPGalactoside (pNPGal). Also, the enzyme hydrolyzed amygdalin, a hydroxynitrile glycoside and a few of the tested flavonoid and isoflavonoid glucosides. The kinetic parameters K (m) and V (max) were found to be 38.59 mu M and 0.8237 mu M/mg/min for pNPGlc, whereas for pNPGal the values were observed as 1845 mu M and 0.1037 mu M/mg/min. In the present study, a three dimensional (3D) model of the Llbglu1 was built by MODELLER software to find out the substrate binding sites and the quality of the model was examined using the program PROCHEK. Docking studies indicated that conserved active site residues are Glu 199, Glu 413, His 153, Asn 198, Val 270, Asn 340, and Trp 462. Docking of rhodiocyanoside A with the modeled Llbglu1 resulted in a binding with free energy change (Delta G) of -5.52 kcal/mol on which basis rhodiocyanoside A could be considered as a potential substrate.

Efetividade da cirurgia bariátrica, com ênfase na técnica sleeve gástrico, para o controle ou reversão do diabetes mellitus tipo 2: revisão sistemática

A obesidade e o Diabetes mellitus tipo 2 se tornaram importantes problemas de saúde pública nos últimos anos. O aumento da prevalência do diabetes está intimamente relacionado ao aumento da prevalência da obesidade. As cirurgias bariátricas surgiram nos últimos cinqüenta anos e vêm se popularizando como uma opção terapêutica efetiva para a redução do peso e controle ou reversão do diabetes no paciente obeso. Dentre as técnicas cirúrgicas disponíveis, o Sleeve gástrico, que era utilizado como parte integrante da técnica de derivação bílio-pancreática ou como primeiro estágio, em pacientes de alto risco, a fim de prepará-los para a cirurgia definitiva, tem sido adotado, por alguns grupos de cirurgiões, como técnica definitiva. Como é recente sua utilização como procedimento bariátrico definitivo, faltam estudos que avaliem sua efetividade. O presente estudo teve por objetivo avaliar o Sleeve gástrico, para o controle ou reversão do Diabetes mellitus tipo 2, no paciente obeso. Para tanto, foi realizada uma revisão sistemática. A busca na literatura resultou em 698 títulos e resumos. Após aplicação dos critérios de inclusão foram recuperados 96 textos completos e incluídos, na revisão sistemática, sete artigos com ensaios clínicos controlados. Foi possível realizar metanálise entre estudos comparando o Sleeve gástrico à derivação gástrica com Y de Roux e com a bandagem gástrica. Foram avaliados os desfechos glicemia de jejum e hemoglobina glicosilada. O resultado da metanálise foi favorável ao Sleeve gástrico, em comparação ao Y de Roux, para o desfecho redução pós-operatória da hemoglobina glicosilada. O Sleeve gástrico se apresenta como mais uma opção terapêutica para a obesidade e correção das co-morbidades associadas. Porém, os resultados são bastante preliminares, e ensaios clínicos controlados, de boa qualidade metodológica, são necessários para melhor avaliação.

锡林河流域温带草地植物VOC释放及其对草地生态系统碳循环的贡献

植物源挥发性有机碳化合物（Volitale organic compounds, VOC）是大气VOC的主要来源，与对流层大气质量、大气化学密切相关。鉴于温带草地的分布范围很广，草地植物VOC释放潜力某种程度上影响植物源VOC的总释放量。另外，植物源VOC也是光合作用固定碳素的损失方式之一，可能在特定区域或生态系统中具有重要意义。基于上述想法，本文设计了四个方面的实验作为研究内容：1） 温带草地物种水平VOC释放潜力、及其与植物功能群的关系？2) 沙地植物物种水平VOC释放潜力、及其与植物功能群的关系？3) 沙地植物-草地植物VOC释放潜力存在显著性差异吗？4) 温带典型草地和退化草地的VOC释放速率如何？在生态系统水平，植物源VOC对温带草地碳循环的贡献多大？ 在所测定的175种温带草地植物中，不同植物间异戊二烯和单萜释放潜力差异很大;除少数物种外，大多数植物的异戊二烯和单萜释放潜力都较低，尤其是典型草地的优势物种。在此基础上，作者探讨了分类学赋值方法对温带草地植被的可行性，并初步建立了锡林河流域温带草地植物的VOC释放目录（共277种植物）。另外，温带草地植物的异戊二烯和单萜释放潜力与植物功能群（植物生活型和水分功能群）具有一定的联系，尤其是植物生活型。总的来说，温带草原的优势生活型（物种），即多年生根茎禾草（或多年生丛生禾草），具有较低的异戊二烯和单萜释放潜力。各水分功能群间差异不显著，但中旱生植物、旱中生植物 (温带草原的优势功能群)，具有较低的异戊二烯、单萜释放潜力。因此，温带草原退化过程中，那些具有较高VOC释放潜力的植物，重要性将会增加。 沙地植物种类组成非常丰富，不同物种间的异戊二烯和单萜释放潜力变异也很大。另外，沙地植物的异戊二烯和单萜释放潜力与其功能群间关系较密切，不同植物生活型间差异显著;其中也以多年生根茎禾草、多年生从生禾草的释放潜力最低，而乔木的释放潜力相对最高;该结论基本与草地的研究结论一致。然而，沙地植物的异戊二烯和单萜释放潜力与其水分功能群的关系比较模糊，中生植物具有更高的释放潜力，湿生植物的释放潜力较小。 通过对比沙地植物和草地植物的释放潜力，发现沙地植物的异戊二烯和单萜释放潜力比草地植物高，且这种差异整体上显著。另外，这种显著性差异，在不同植物生活型、水分功能群间也同样存在。沙地植物比对应的草地植物具有更高的异戊二烯和单萜释放潜力，最可能的原因：沙地正午的温度明显比草地温度高，前者实测温度可超过 45 ℃,这种经常性、周期性高温，促使沙地植物采用与草地植物不同的适应策略，即沙地植物通过释放更多的异戊二烯或单萜来减少其可能遭的热胁迫或热伤害，这种长期适应策略，使沙地植物具有更高的萜类化合物释放潜力。 本文还调查了温带典型草地生态系统和退化草地生态系统的异戊二烯和单萜释放速率，结果表明典型草地的标准异戊二烯和单萜释放速率分别为0.50 μgC g-1 h-1和0.69 μgC g-1 h-1;退化草地的标准异戊二烯和单萜释放潜力分别为0.32 μgC g-1 h-1和1.59 μgC g-1 h-1。总的来说，温带草地的异戊二烯和单萜释放速率都比较低，尤其是典型草地。整个生长季，典型草地释放的异戊二烯和单萜分别为31.6 mgC•m-2　和 70.4 mgC•m-2;退化草地的异戊二烯和单萜释放量分别为20.8 mgC•m-2 和 168.8 mgC•m-2。退化草地萜类化合物总释放速率远高于典型草地，尤其是单萜释放能力。过度放牧引起的草地退化，通过改变植被种类组成，对温带草地的异戊二烯和单萜释放速率产生显著影响;总体而言，温带草地退化将会使草地释放更多萜类化合物。 在温带草地生态系统中，Clost as VOC相对其NPP而言很小，在环境PAR和温度高时,它的贡献率相对较大;Clost as VOC约占典型草地生态系统NEP的5.32 %，退化草地生态系统NEP的0.23 %。植物源VOC释放所损失的碳素相对草地生态系统NPP而言几乎可以忽略不计;但是，相对其NEP，Clost as VOC还是具有一定的相关性。虽然，草地生态系统Clost as VOC对NPP或NEP的贡献率较小，但考虑到全球尺度植物源VOC的巨大释放速率，它在碳循环中的贡献率仍然不容忽视;在某些特殊的生态系统中，仍可能扮演重要角色。

Chemical Constituents from the Leaves and Stems of Schisandra lancifolia

A new nortriterpenoid, 20-hydroxymicrandilactone D (1) and a novel lignan glycoside, lancilignanside A (2) were isolated from leaves and stems of Schisandra lancifolia, together with three known nortriterpenoids (3-5) and nine known phenolics (6-14). The structures of new compounds 1 and 2 were determined by detailed analysis of their 1D and 2D NMR spectra, and chemical evidences. In addition, compounds 1-2, 6-7, and 9-11 showed anti-human immunodeficiency virus (HIV)-1 activities with 50% effective concentration (EC50) in the range of 3.0-99.0 mu g/ml. Compound 12 was not bioactive in this assay with EC50 more than 200 mu g/ml.

In vitro anti-HIV and -HSV activity and safety of sodium rutin sulfate as a microbicide candidate

Sodium rutin sulfate (SRS) is a sulfated rutin modified from the natural flavonol glycoside rutin. Here, we investigated its in vitro anti-HIV and -HSV activities and its cytotoxic profile. Fifty percent inhibitory concentration (IC50) values of SRS against HIV-1 X4 virus IIIB, HIV-1 R5 isolates Ada-M and Ba-L were 2.3 +/- 0.2, 4.5 +/- 2.0 and 8.5 +/- 3.8 mu M with a selectivity index (SI) of 563, 575 and 329, respectively. Its IC50 against primary R5 HIV-1 isolate from Yunnan province in China was 13.1 +/- 5.5 mu M, with a Sl of 197. In contrast, unsulfated rutin had no activity against any of the HIV-1 isolates tested. Further study indicated that SRS blocked viral entry and virus-cell fusion likely through interacting with the HIV- I envelope glycoprotein. SRS also demonstrated some activity against human herpes simplex virus (HSV) with an IC50 of 88.3 +/- 0.1 mu M and a Sl of 30. The 50% cytotoxicity concentration (CC50) of SRS was >3.0 mM, as determined in human genital ME 180, HeLa and primary human foreskin fibroblast cells. Minimum inhibitory concentration of SRS for vaginal lactobacilli was >3.0 mM. These results collectively indicate that SRS represents a novel candidate for anti-HIV-1/HSV microbicide development. (C) 2007 Elsevier B.V. All rights reserved.