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.     

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.     

Assessing water scarcity by simultaneously considering environmental flow requirements,water quantity,and water quality

Water scarcity is a widespread problem in many parts of the world. Most previous methods of water scarcity assessment only considered water quantity, and ignored water quality. In addition, the environmental flow requirement (EFR) was commonly not explicitly considered in the assessment. In this study, we developed an approach to assess water scarcity by considering both water quantity and quality, while at the same time explicitly considering EFR. We applied this quantity–quality-EFR (QQE) approach for the Huangqihai River Basin in Inner Mongolia, China. We found that to keep the river ecosystem health at a “good” level (i.e., suitable for swimming, fishing, and aquaculture), 26% of the total blue water resources should be allocated to meet the EFR. When such a “good” level is maintained, the quantity- and quality-based water scarcity indicators were 1.3 and 14.2, respectively; both were above the threshold of 1.0. The QQE water scarcity indicator thus can be expressed as 1.3(26%)|14.2, indicating that the basin was suffering from scarcity problems related to both water quantity and water quality for a given rate of EFR. The current water consumption has resulted in degradation of the basin's river ecosystems, and the EFR cannot be met in 3 months of a year. To reverse this situation, future policies should aim to reduce water use and pollution discharge, meet the EFR for maintaining healthy river ecosystems, and substantially improve pollution treatment.     

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。     

Gender identification of shovelnose sturgeon using ultrasonic and endoscopic imagery and the application of the method to the pallid sturgeon

Monthly sampling of shovelnose sturgeon Scaphirhynchus platorynchus , a biological surrogate for the endangered pallid sturgeon Scaphirhynchus albus , was conducted to develop a multi‐seasonal profile of reproductive stages. Data collected included histological characteristics of gonads from wild caught fish and laboratory and field ultrasonic and endoscopic images. These data were used to compare effectiveness of ultrasonic and endoscopic techniques at identifying gender of adult shovelnose sturgeon at different reproductive stages. The least invasive method ( i.e . ultrasound) was least effective while the most invasive ( i.e . endoscope through an abdominal incision) was the most effective at identifying shovelnose sturgeon gender. In most cases, success rate for identifying males was greater than females, with success at identifying both genders greater in more advanced reproductive stages. Concomitantly, for most months average reproductive stage was more advanced for males than females. April and May were the months with the most advanced reproductive stage, and were the months when ultrasound was most effective. Methods were also applied in the Upper Missouri River to validate their use on pallid sturgeon Scaphirhynchus albus . Ultrasound was successful at identifying pallid sturgeon gender, however, endoscopic examination through the urogenital duct was only successful at identifying pallid sturgeon gender when the urogenital duct was not opaque.     

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.     

Path analysis of natural selection on plant chemistry: the xylem resin of ponderosa pine

We analyzed the pattern of correlations among fitness components, herbivory, and resin characteristics in a natural all-aged stand of ponderosa pine, to infer the strength and mechanism of natural selection on plant chemistry. Male and female cone production were monitored yearly for 15 years, and levels of herbivory for 9 years in 165 trees. Resin flow rate and monoterpene composition were determined for these same trees. Multiple regression of fitness components on resin characteristics showed significant associations consistent with directional selection for increased resin flow rates and increased proportions of α- and β-pinene, myrcene and terpinolene. However, negative correlations among monoterpene fractions of the resin constrained the overall selection. Selective herbivory by aphids approached statistical significance and monoterpenes showed some (non-significant) effect as deterrents against deer browse. Resin characteristics were not correlated with attack by cone insects or porcupines. However, the association between resin characteristics and fitness is significantly different from that predicted by the path coefficients involving herbivores. Therefore the hypothesis that these herbivores mediate selection on the resin is not supported by the observed pattern of correlations among resin characteristics, herbivory, growth and fecundity. In this population, most of the association between resin characteristics and fitness appears to be mediated by some other factor independent of attack by herbivore species present. Received: 18 March 1996/Accepted: 18 July 1996     

Pyridine alkaloids with activity in the central nervous system

This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate.     

Differential human impact and vegetation history in two adjacent Pyrenean valleys in the Ariège basin,southern France,from 3000 B.P. to the present

Detailed palynological studies in two adjoining French Pyrenean valleys, complemented by the study of archives, demonstrate that under similar climatic conditions, the forest history of each valley from the Bronze Age to present time was essentially determined by socio-economical constraints, possibly modified by natural characteristics such as topography. The studies show why the expansion of Fagus (beech) at c. 4000 B.P. was asynchronous on the northern slope of the Pyrenees and emphasize the effects of the human impact on the recent lowering of the tree-line.A contribution to the 8th IPC, Aix-en-Provence, 1992