Aminoadamantanes containing monoterpene-derived fragments as potent tyrosyl-DNA phosphodiesterase 1 inhibitors

The ability of a number of nitrogen-containing compounds that simultaneously carry the adamantane and monoterpene moieties to inhibit Tdp1, an important enzyme of the DNA repair system, is studied. Inhibition of this enzyme has the potential to overcome chemotherapeutic resistance of some tumor types. Compound (+)-3c synthesized from 1-aminoadamantane and (+)-myrtenal, and compound 4a produced from 2-aminoadamantane and citronellal were found to be most potent as they inhibited Tdp1 with IC₅₀ values of 6 and 3.5 µM, respectively. These compounds proved to have low cytotoxicity in colon HCT-116 and lung A-549 human tumor cell lines (CC₅₀ > 50 µM). It was demonstrated that compound 4a at 10 µM enhanced cytotoxicity of topotecan, a topoisomerase 1 poison in clinical use, against HCT-116 more than fivefold and to a lesser extent of 1.5 increase in potency for A-549.     

Planning connectivity at multiple scales for large mammals in a human-dominated biodiversity hotspot

Connectivity for large mammals across human-altered landscapes results from movement by individuals that can be described via nested spatial scales as linkages (or zones or areas) with compatible land use types, constrictions that repeatedly funnel movement (as corridors) or impede it (as barriers), and the specific paths (or routes) across completely anthropogenic features (such as highways). Mitigation to facilitate animal movement through such landscapes requires similar attention to spatial scale, particularly when they involve complex topography, diverse types of human land use, and transportation infrastructure. We modeled connectivity for Asian elephant (Elephas maximus) and gaur (Bos gaurus) in the Shencottah Gap, a multiple-use region separating two tiger reserves in the Western Ghats, India. Using 840 km of surveys for animal signs within a region of 621 km², we modeled landscape linkages via resource selection functions integrated across two spatial resolutions, and then potential dispersal corridors within these linkages using circuit theoretical models. Within these corridors, we further identified potential small-scale movement paths across a busy transportation route via least-cost paths and evaluated their viability. Both elephants and gaur avoided human-dominated habitat, resulting in broken connectivity across the Shencottah Gap. Predicted corridor locations were sensitive to analysis resolution, and corridors derived from scale-integrated habitat models correlated best with habitat quality. Less than 1% of elephant and gaur detections occurred in habitat that was poorer in quality than the lowest-quality component of the movement path across the transportation route, suggesting that connectivity will require habitat improvement. Only 28% of dispersal corridor area and 5% of movement path length overlapped with the upper 50% quantile of the landscape linkage; thus, jointly modeling these three components enabled a more nuanced evaluation of connectivity than any of them in isolation.     

Synthesis,antiproliferative and antibacterial activity of new amides of salinomycin

A series of 11 novel amides of salinomycin were synthesized for the first time. All the obtained compounds were found to show potent antiproliferative activity against human cancer cell lines including the drug-resistant cancer cells. Four new salinomycin derivatives revealed good antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus epidermidis (MRSE).     

多种天敌控制多种害虫的模糊数学模型

从生态经济学的原理出发，利用模糊集理论，探讨如何评价天敌控制多种害虫的为害作用，提出了多种天敌控制多种害虫的模糊数学模型。同时又得到了天敌对害虫的控制能力C，影响率G，影响强度H，及权数ω(x)的计算公式，以及在天敌作用下安全度的讨论与分析。     

A sex-specific test of selection in utero

We find support for the hypothesis that changes in the monthly odds of a twin among live-born males predict subsequent and opposite changes in the odds of a twin among live-born females. The hypothesis arises from the long standing argument that natural selection has conserved mechanisms by which pregnant women in stressed populations spontaneously abort fetuses least likely to yield grandchildren. Previous attempts to empirically test this argument focus almost entirely on males. We contribute to the literature by showing that, consistent with the logic of natural selection, maternal adaptations to environmental changes likely have effects on the survival of both male and female conceptuses and fetuses.     

Fire effects on ecosystem nitrogen cycling in a Californian bishop pine forest

Fire can cause severe nitrogen (N) losses from grassland, chaparral, and temperate and boreal forest ecosystems. Paradoxically, soil ammonium levels are markedly increased by fire, resulting in high rates of primary production in re-establishing plant communities. In a manipulative experiment, we examined the influence of wild-fire ash residues on soil, microbial and plant N pools in a recently burned Californian bishop pine (Pinus muricata D. Don) forest. Ash stimulated post-fire primary production and ecosystem N retention through direct N inputs from ash to soils, as well as indirect ash effects on soil N availability to plants. These results suggest that redistribution of surface ash after fire by wind or water may cause substantial heterogeneity in soil N availability to plants, and could be an important mechanism contributing to vegetation patchiness in fire-prone ecosystems. In addition, we investigated the impact of fire on ecosystem N cycling by comparing ¹⁵N natural abundance values from recently burned and nearby unburned P. muricata forest communities. At the burned site, ¹⁵N natural abundance in recolonising species was similar to that in bulk soil organic matter. By contrast, there was a marked ¹⁵N depletion in the same species relative to the total soil N pool at the unburned site. These results suggest that plant uptake of nitrate (which tends to be strongly depleted in ¹⁵N because of fractionation during nitrification) is low in recently burned forest communities but could be an important component of eco- system N cycling in mature conifer stands. Received: 29 June 1999 / Accepted: 24 October 1999     

Tree growth in the aftermath of A flood: A tree-ring based reconstruction of the impacts of the 1996-Biescas catastrophe

Catastrophic floods and large debris flows are natural hazards common in mountain areas. They cause injuries and impact the radial growth of trees growing in the affected basins. Reconstructing how these catastrophic events impact trees by using dendrochronology improves our understanding of natural hazards. The 1996-Biescas (Central Spanish Pyrenees) flood was a catastrophic event causing the loss of many lives in a campsite located on an active alluvial fan. We investigated using tree rings how this catastrophic flood impacted planted trees (poplars, cedars) located in the campsite. Conspicuous scars in the stem were more abundant in cedar trees (75 %) than in poplar (36 %) trees. Scarred cedar trees formed traumatic resin ducts after the flood. In cedar tree perimeter influenced the size of the wound formed after the flood, but this was not observed in poplar. On average, 63 % of trees showing scars formed them in the side of the stem (N-NW) where the impact of the flood was assumed to be strongest. We also detected sharp reductions of tree-ring width after the flood (–56 % and –16 % in poplar and cedar, respectively). However, this was not found when using basal area increment, which suggests there was an age effect on the post-flood growth changes. The two species mean chronologies were also more coupled after the flood in agreement with an increased responsiveness to climate, particularly a higher dependence of growth on June precipitation. To adequately reconstruct responses to flood and to assess the actual vulnerability of forests to debris flow impacts tree features such as species, age, growth rate and responsiveness to climate must be considered.     

Variation of chemical composition and antioxidant activity of essential oils of Mentha x rotundifolia (L.) Huds. (Lamiaceae) collected from different bioclimatic areas of Tunisia

The variation of the essential oils composition of 10 Tunisian Mentha x rotundifolia (L.) Huds. Populations and their antioxidant activity were assessed. Essential oils showed high percentages of oxygenated monoterpenes and sesquiterpene hydrocarbons. Rotundifolone, p-menthane-1,2,3-triol, β-caryophyllene and germacrene D were identified as main compounds at the species level. A variation in the essential oil composition was observed according to the populations and ecological factors. The populations 7, 8, 9 and 10 from the upper semi-arid bioclimatic zone and situated at high altitudes, exhibited the highest amount of rotundifolone. The populations 1, 2, 3, 4 and 5 from the lower humid showed a rotundifolone/β-caryophyllene/germacrene D chemotype. The population 6, situated at the lowest altitude, was characterized by the highest amount of p-menthane-1,2,3-triol. The level of antioxidant activity of the populations was linked to their chemical composition difference. The highest scavenging activity and the best ability to reduce ferric ions were recorded for the population 10. The most important capacity to inhibit β-carotene bleaching was revealed for the population 8. For all populations, the antioxidant activities were substantial but lower than antioxidant standards used (Trolox and BHT).The populations (7, 8, 9 and 10) from the upper semi-arid showed the best yields of essential oils and the highest contents of rotundifolone. Chemotypes within these populations could be selected for improvement programs.     

Structure–antimicrobial activity of some natural isocoumarins and their analogues

Three naturally occurring isocoumarins (paepalantine, paepalantine 9-O-beta-D-glucopyranoside and paepalantine 9-O-beta-D-allopyranosyl(1 --> 6) glucopyranoside) and two semi-synthetic analogues, 9,10-acylated compound and 9-OH-10-methylated compound, structurally similar to paepalantine, were evaluated for antimicrobial activity using a spectrophotometric microdilution technique. The paepalantine was active against S. aureus, S. epidermidis, and E. faecalis while the other four compounds proved ineffective against all microorganisms tested at concentrations of 500 microg/ml. Variations in phenolic substitution at OH-9 and/or OH-10 in the paepalantine molecule resulted in compounds without antimicrobial activity. A combination of structural features, two phenolic groups as cathecolic system, forms an oxygenated system arrangement that may reflect the potentially antimicrobial properties of paepalantine.