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.     

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.     

Differential response of nematode colonist communities to the intertidal placement of dredged material

The use of fine-grained maintenance dredged material for habitat enhancement has increased in recent years, particularly recharge schemes which provide a means of combating the erosion of intertidal flats and saltmarsh. This article investigates the development of meiofaunal nematode communities following a natural experiment in 2003, when fine-grained dredged material was deposited concurrently at four adjacent intertidal recharge sites on the southeast coast of the United Kingdom. A 12-month survey of nematode assemblages was carried out to compare univariate, multivariate, allometric and functional attributes of colonist communities in relation to the different environmental conditions prevailing at the four sites. Developing assemblages were increasingly affected by the spatial differences in the elevation, consolidation and exposure of bed material. The results indicated that the colonisation sequence was the result of random settling of suspended nematodes, sequential reproduction and differential survival and reproductive success of colonising species. For the first time, this experiment provided insights into the development of adaptive and functional types of meiofaunal nematodes following the intertidal deposition of uncontaminated fine-grained dredged material. This, in turn, will contribute considerably to the development of ecological models of the evolution of the large-scale placement of muddy dredged material in the intertidal environment.     

Awareness of a conservation unit: a Brazilian case study

The range of uses of a conservation area by a nearby population was quantified by questionnaires applied to residents of Santa Helena county, Brazil. Of the 312 responses compiled, 71.2% of the residents acknowledged the presence of a conservation unit within the county limits while only 59.3% of the respondents had participated in some recreational or leisure outdoor activity within the unit. Activities cited by respondents included games (11.7%), beach visits (11.4%), cross-country walks (9.4%), and fishing (8.3%). A possible visitor fee to improve infrastructure within the area was approved by 64.9% of the interviewees. Suggested visitor fee varied from 50 cents to two dollars.