In silico target fishing for rationalized ligand discovery exemplified on constituents of Ruta graveolens

The identification of targets whose interaction is likely to result in the successful treatment of a disease is of growing interest for natural product scientists. In the current study we performed an exemplary application of a virtual parallel screening approach to identify potential targets for 16 secondary metabolites isolated and identified from the aerial parts of the medicinal plant RUTA GRAVEOLENS L. Low energy conformers of the isolated constituents were simultaneously screened against a set of 2208 pharmacophore models generated in-house for the IN SILICO prediction of putative biological targets, i. e., target fishing. Based on the predicted ligand-target interactions, we focused on three biological targets, namely acetylcholinesterase (AChE), the human rhinovirus (HRV) coat protein and the cannabinoid receptor type-2 (CB (2)). For a critical evaluation of the applied parallel screening approach, virtual hits and non-hits were assayed on the respective targets. For AChE the highest scoring virtual hit, arborinine, showed the best inhibitory IN VITRO activity on AChE (IC (50) 34.7 muM). Determination of the anti-HRV-2 effect revealed 6,7,8-trimethoxycoumarin and arborinine to be the most active antiviral constituents with IC (50) values of 11.98 muM and 3.19 muM, respectively. Of these, arborinine was predicted virtually. Of all the molecules subjected to parallel screening, one virtual CB (2) ligand was obtained, i. e., rutamarin. Interestingly, in experimental studies only this compound showed a selective activity to the CB (2) receptor ( Ki of 7.4 muM) by using a radioligand displacement assay. The applied parallel screening paradigm with constituents of R. GRAVEOLENS on three different proteins has shown promise as an IN SILICO tool for rational target fishing and pharmacological profiling of extracts and single chemical entities in natural product research.

Cryptic invertebrates on subtidal rocky reefs vary with microhabitat structure and protection from fishing

The deployment of flat concrete blocks on subtidal rocky reefs can replicate natural reef microhabitats and provides a means for standardized sampling of cryptic invertebrates. The shape of the cavity beneath the block is related to reef topography and may influence the invertebrate community by affecting the amount of space for cryptic fauna to colonise and influencing the effectiveness of their predator-defence mechanisms. To determine the effect of sub-block reef structure and different levels of external predators on cryptic molluscs and echinoderms, I deployed concrete blocks at locations inside and outside the Maria Island marine reserve in eastern Tasmania, Australia. Relationships between sub-block reef structure and the cryptic invertebrate assemblage were evident between locations, whereas only a small but significant proportion of variation of assemblages between blocks within location was explained by reef surface area. No clear association with external predation pressure was evident in multivariate analyses of variation in assemblage structure. Juvenile abalone Haliotis rubra were not influenced by micro-habitat structure but were significantly less abundant at protected locations, the only species to exhibit such a response. This result follows a decline of emergent adult abalone in the marine reserve and raises the possibility of recruitment failure of abalone at some fully protected locations in the longer term.

Les villages préhistoriques des bords des lacs circum-alpins entre le Ve et IVe millénaire av. J.-C.

Connus sous le nom populaire de palafittes, les habitats préhistoriques construits sur les rives des lacs subalpins du Néolithique à l’aube de l’âge du Fer (entre 5300 et 700 av. J.-C.) offrent des informations exceptionnelles sur l’évolution culturelle d’une importante région européenne, grâce à la préservation remarquable des matériaux organiques, en particulier du bois. À partir de la deuxième moitié du XXe siècle, le perfectionnement des techniques de fouille subaquatiques et de la dendrochronologie permettront la construction d’un schéma chronologique précis pour l’Europe nord-alpine. Les recherches contribueront à des observations d’ordre écologique à l’échelle locale et régionale et à l’identification des rythmes de développement des villages. Sous l’égide de l'UNESCO, les années 2010 verront la constitution d’un inventaire vaste et uniforme des sites préhistoriques des lacs circumalpins, classés Patrimoine culturel mondial en juin 2011.

Adaptation to Changes in the Coffee Value Chain and the Price of Coiffee among Coffee Producers in Two Villages in Kilimanjaro, Tanzania

Market liberalization in Tanzania has eroded the monopoly of the cooperative unions by allowing private coffee buyers (PCBs) to compete with them on equal footing. Similarly, farmers groups and primary societies are now allowed to sell coffee at auction. Thus, farmers have various options for selling their coffee. Similarly, the coffee industry has experienced large fluctuations in prices and stagnation in production. How do farmers react to these changes? Can and do farmers profit from different market conditions and sell to different traders at the lower end of the value chain, or do they remain with cooperatives or farmers groups? This study was conducted in Mruwia and Mshiri villages in Moshi Rural district. Whereas Mshiri village remains attached to the Kilimanjaro Native Cooperative Union (KNCU), Mruwia has detached from this organization and sells coffee independently. The sample (103) was randomly selected from the coffee farmers in the two villages. Data were collected through surveys, focus group discussions (FGDs), and socio-anthropological methods (participant-observation, biographies, and thematic interviews). Results indicate that the selection of whom to sell coffee depends largely on farmers’ dependence on coffee and prices, other benefits accrued, and whether the initial costs are covered by buyers. Additionally, most respondents did not sell coffee to PCBs. Thus, prices, the institutional infrastructure, and the structure of local communities were important when making decisions about how and with whom to trade.

Do relocated villages experience more forest cover change? Resettlements, shifting cultivation and forests in the Lao PDR

This study explores the relationships between forest cover change and the village resettlement and land planning policies implemented in Laos, which have led to the relocation of remote and dispersed populations into clustered villages with easier access to state services and market facilities. We used the Global Forest Cover Change (2000–2012) and the most recent Lao Agricultural Census (2011) datasets to assess forest cover change in resettled and non-resettled villages throughout the country. We also reviewed a set of six case studies and performed an original case study in two villages of Luang Prabang province with 55 households, inquiring about relocation, land losses and intensification options. Our results show that resettled villages have greater baseline forest cover and total forest loss than most villages in Laos but not significant forest loss relative to that baseline. Resettled villages are consistently associated with forested areas, minority groups, and intermediate accessibility. The case studies highlight that resettlement coupled with land use planning does not necessarily lead to the abandonment of shifting cultivation or affect forest loss but lead to a re-spatialization of land use. This includes clustering of forest clearings, which might lead to fallow shortening and land degradation while limited intensification options exist in the resettled villages. This study provides a contribution to studying relationships between migration, forest cover change, livelihood strategies, land governance and agricultural practices in tropical forest environments.

Baseline Survey Report: Case study of Uluguru and Usambara mountains (Bigwa, Tangeni, Peko Misegese, Mashewa and Misalai villages)

Agriculture is the back borne of the economy of Tanzania and its main objective is to ensure food security and eradication of rural poverty through the promotion of production systems, technologies and practices that are environmental sound (Tanzania National Environmental Policy, 1999). However, this has not been achieved due to rapid land degradation, which has consequently lead to massive soil loss, decline in crop yields, disruption of water resources and the destruction of the natural resources in general. This report highlights the extent to which agricultural related activities like agronomic and cultural practices such as use of fire for preparation of farms and cutting of trees to meet villagers’ needs have devastating effect on the quality of the environment. Besides these observed difficulties this paper argued that as the survival, well being and future of the Uluguru and Usambara people it is essential to provide continuous training to farmers, so that they know how best to continue farming and harvesting forest products on a sustainable basis without causing much harm to the environment. Most of all this paper recommends the introduction of Ngolo cultivation technology on steep slopes of Usambara and Uluguru mountains in order to enhance the conservation of the environment.