New imidazoquinoxaline derivatives: Synthesis,biological evaluation on melanoma,effect on tubulin polymerization and structure–activity relationships

Microtubules are considered as important targets of anticancer therapy. EAPB0503 and its structural imidazo[1,2-a]quinoxaline derivatives are major microtubule-interfering agents with potent anticancer activity. In this study, the synthesis of several new derivatives of EAPB0503 is described, and the anticancer efficacy of 13 novel derivatives on A375 human melanoma cell line is reported. All new compounds show significant antiproliferative activity with IC₅₀ in the range of 0.077–122 μM against human melanoma cell line (A375). Direct inhibition of tubulin polymerization assay in vitro is also assessed. Results show that compounds 6b, 6e, 6g, and EAPB0503 highly inhibit tubulin polymerization with percentages of inhibition of 99%, 98%, 90%, and 84% respectively. Structure–activity relationship studies within the series are also discussed in line with molecular docking studies into the colchicine-binding site of tubulin.     

Differential influence of Pomphorhynchus laevis (Acanthocephala) on the behaviour of native and invader gammarid species.

Although various species of acanthocephalan parasites can increase the vulnerability of their amphipod intermediate hosts to predation, particularly by altering their photophobic behaviour, their influence on the structure of amphipod communities and the success of invader species has so far received little attention. We compared the prevalence and behavioural influence of a fish acanthocephalan parasite, Pomphorhynchus laevis, in two species of amphipods, Gammarus pulex and Gammarus roeseli in sympatry in the river Ouche (Burgundy, eastern France). There, G. pulex is a resident species, whereas G. roeseli is a recent coloniser. Both uninfected G. pulex and G. roeseli were strongly photophobic, although less so in the invading species. However, there was no significant difference in reaction to light between infected and uninfected G. roeseli, whereas infected G. pulex were strongly photophilic. We discuss our results in relation to the parasite's ability to manipulate invading host species, the possibility that resistant individuals have been selected during the invasion process, and the role that acanthocephalan parasites can play in shaping the structure of amphipod communities.     

Reduced aboveground tree growth associated with higher arbuscular mycorrhizal fungal diversity in tropical forest restoration

Establishing diverse mycorrhizal fungal communities is considered important for forest recovery, yet mycorrhizae may have complex effects on tree growth depending on the composition of fungal species present. In an effort to understand the role of mycorrhizal fungi community in forest restoration in southern Costa Rica, we sampled the arbuscular mycorrhizal fungal (AMF) community across eight sites that were planted with the same species (Inga edulis, Erythrina poeppigiana, Terminalia amazonia, and Vochysia guatemalensis) but varied twofold to fourfold in overall tree growth rates. The AMF community was measured in multiple ways: as percent colonization of host tree roots, by DNA isolation of the fungal species associated with the roots, and through spore density, volume, and identity in both the wet and dry seasons. Consistent with prior tropical restoration research, the majority of fungal species belonged to the genus Glomus and genus Acaulospora, accounting for more than half of the species and relative abundance found on trees roots and over 95% of spore density across all sites. Greater AMF diversity correlated with lower soil organic matter, carbon, and nitrogen concentrations and longer durations of prior pasture use across sites. Contrary to previous literature findings, AMF species diversity and spore densities were inversely related to tree growth, which may have arisen from trees facultatively increasing their associations with AMF in lower soil fertility sites. Changes to AMF community composition also may have led to variation in disturbance susceptibility, host tree nutrient acquisition, and tree growth. These results highlight the potential importance of fungal–tree–soil interactions in forest recovery and suggest that fungal community dynamics could have important implications for tree growth in disturbed soils.     

基于核基因RAG1部分序列探讨菊头蝠科和蹄蝠科的系统发育关系

应用核基因重组激活基因1(Recombination activating gene,RAG1)部分序列对贵州9种菊头蝠和5种蹄蝠的系统发育关系进行了研究,运用贝叶斯法(Bayesian inference,BI)、最大似然法(Maximum likelihood,ML)和邻接法(Neighbor-joining,NJ)构建了系统进化树。研究结果表明:1.菊头蝠科和蹄蝠科形成两个平行的分支,支持它们是两个平行科的结论。2.马铁菊头蝠是菊头蝠科中第一个独立出来的亚分支,与其余8种菊头蝠的亲缘关系最远;Rhinolophus sp.与大菊头蝠聚合为一支,推测Rhinolophus sp.可能是大菊头蝠,或者是大菊头蝠的近缘种,它们是继马铁菊头蝠之后分离出来的第二亚分支;中华菊头蝠、栗黄菊头蝠、中菊头蝠聚合为第三亚分支,贵州菊头蝠、大耳菊头蝠、菲菊头蝠聚合为第四亚分支,此两分支形成姊妹群。3.在蹄蝠科的亚分支中,三叶蹄蝠、小蹄蝠、普氏蹄蝠依次分离出来,最后分出的是大蹄蝠和中蹄蝠。     

Triterpenes from the fungus Poria cocos and their inhibitory activity on nitric oxide production in mouse macrophages via blockade of activating protein-1 pathway

Two new triterpenes, 29-hydroxydehydrotumulosic acid (1) and 29-hydroxydehydropachymic acid (2), together with six known compounds, dehydropachymic acid (3), dehydrotumulosic acid (4), 29-hydroxypolyporenic acid C (5), polyporenic acid C (6), tumulosic acid (7), and pachymic acid (8), were isolated from the dried sclerotia of Poria cocos. In the in vitro bioassays, these isolated compounds reduced, in a dose-dependent manner, nitric oxide (NO) production from lipopolysaccharide (LPS)-induced RAW 264.7 cells, with compounds 5 and 6, the IC(50) values of which were 16.8±2.7 and 18.2±3.3 μM, respectively, exhibiting the greatest inhibition activity. Further Western blot analysis conducted on cells pre-treated with compounds 5 and 6, and luciferase assays on activator protein 1-dependent gene expression revealed that the inhibited NO release was attributed to the reduced expression of iNOs (=inducible NO synthase) enzymes, which might be regulated via the blockade of activator protein-1 signaling pathway.     

法国蜜环菌Armillaria gallica菌株遗传多样性的ISSR分析

在中国东北地区共采集到53个法国蜜环菌Armillaria gallica菌株,用ISSR（Inter-Simple Sequence Repeat）标记技术对这些菌株进行遗传多样性分析。用6个ISSR引物扩增所得条带表明,ISSR标记在蜜环菌中存在较高的多态性;亲缘关系树状图表明,有3个菌株遗传分化明显;其余50个分别来自3个不同地理居群的菌株聚成一类,亲缘关系较近,没有表现出地理隔离。     

岷江上游不同树种林地客土混合对土壤生物化学性质和枯落叶分解的影响

人工纯林的长期经营会引发连栽障碍,影响森林的可持续发展,解决途径是引进更新树种形成混交林。为了指导四川岷江上游人工纯林更新树种和混交比例的选择,尝试通过针阔叶树种林地腐殖质土壤及其枯落物的客置和混合原位培养试验,探讨不同树种种间关系的协调性。结果表明:(1)连香树、云南松和云杉林地经过各种客土混合后酶活性普遍都有所提高,而在糙皮桦林地,经云南松土壤客土混合后酶活性普遍有所下降,经云杉土壤客土混合后脲酶和过氧化氢酶活性有不同程度的提高,蔗糖酶活性却有所下降;(2)连香树和云南松林地经过各种客土混合后,加速了C和N由枯落物进入土壤,而在糙皮桦和云杉林地经过各种客土混合后,促进了N从枯落物和有机质矿化分解进入土壤的过程,但却会对有机C进入土壤产生抑制作用;(3)所有不同针阔叶树种林地经土壤客土混合后,对原有土壤的酸碱性起到中和的作用,即原来的阔叶林地土壤向偏酸性方向发展,而原来的针叶林地土壤向偏碱性方向发展;(4)所有不同树种林地的客土混合对枯落叶分解均具有明显的促进作用;(5)连香树林地的LM0.15~0.50和LY0.15~0.35、糙皮桦林地的HM0.15和HY0.15~0.50、云南松林地的ML0.15~0.50和MH0.35~0.50、云杉林地的YL0.35~0.50和YH0.35类型是相对较好的选择,可作为确定更新树种和混交比例的参考。     

Does the niche breadth or trade‐off hypothesis explain the abundance–occupancy relationship in avian Haemosporidia?

Two hypotheses have been proposed to explain the abundance–occupancy relationship (AOR) in parasites. The niche breadth hypothesis suggests that host generalists are more abundant and efficient at colonizing different host communities than specialists. The trade‐off hypothesis argues that host specialists achieve high density across their hosts' ranges, whereas generalists incur the high cost of adaptation to diverse immuno‐defence systems. We tested these hypotheses using 386 haemosporidian cytochrome‐b lineages (1894 sequences) recovered from 2318 birds of 103 species sampled in NW Africa, NW Iberia, W Greater Caucasus and Transcaucasia. The number of regions occupied by lineages was associated with their frequency suggesting the presence of AOR in avian Haemosporidia. However, neither hypothesis provided a better explanation for the AOR. Although the host generalist Plasmodium SGS1 was over three times more abundant than other widespread lineages, both host specialists and generalists were successful in colonizing all study regions and achieved high overall prevalence.     

Spectroscopic characterization of mononuclear, binuclear, and insoluble polynuclear oxovanadium(IV)-Schiff base complexes and their oxidation catalysis

The objective was to prepare mononuclear, binuclear, and insoluble polynuclear oxovanadium(IV)-Schiff base complexes and to use them for sulfoxidation and epoxidation of organic substrates. [VO(salen)] (complex 1) with tetradentate salen(salicylideneethylenediamine) being coordinated in the equatorial plane of oxovanadium(IV), [VO(salap)] (complex 2), and [(VO)₂(sal₂-dhdabp)] (complex 3) with tridentate salap(salicylideneorthoaminophenol) and sal₂-dhdabp(salicylidene-3,3^′-dihydroxy-4,4^′-diaminobiphenyl) being bound, respectively, in the equatorial plane, of which polynuclear complexes were constituted as monomer units, were prepared and spectroscopically characterized. A sulfide and olefins were oxidized by use of complexes 1 and 2 (mononuclear), complex 3 (binuclear), and the polynuclear complexes (poly-1 and poly-3) synthesized with 1 and 3, respectively. The reaction rates for poly-1 and -3 were a little lower than those of the corresponding 1 and 3. On oxidation of sulfides, poly-3 exhibited lowering of activity by about 15% in three cycles, while poly-1 showed significant lose of activity with each use. Poly-3 was efficient for the oxidation of the olefins only in the first cycle. It was suggested that the loss of activity depends not only on the coordination geometry of the oxovanadium complex, but also on the kind of the substrate.