Triterpenoid saponins from a cytotoxic root extract of Sideroxylon foetidissimum subsp. gaumeri

Evaluation of the cytotoxicity of an ethanolic root extract of Sideroxylonfoetidissimum subsp. gaumeri (Sapotaceae) revealed activity against the murine macrophage-like cell line RAW 264.7. Systematic bioassay-guided fractionation of this extract gave an active saponin-containing fraction from which four saponins were isolated. Use of 1D ((1)H, (13)C, DEPT135) and 2D (COSY, TOCSY, HSQC, and HMBC) NMR, mass spectrometry and sugar analysis gave their structures as 3-O-(beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl)-28-O-(alpha-L-rhamnopyranosyl-(1-->3)[beta-D-xylopyranosyl-(1-->4)]-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl)-16alpha-hydroxyprotobassic acid, 3-O-beta-D-glucopyranosyl-28-O-(alpha-L-rhamnopyranosyl-(1-->3)[beta-D-xylopyranosyl-(1-->4)]-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl)-16alpha-hydroxyprotobassic acid, 3-O-(beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl)-28-O-(alpha-L-rhamnopyranosyl-(1-->3)-beta-D-xylopyranosyl-(1-->4)[beta-D-apiofuranosyl-(1-->3)]-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl)-16alpha-hydroxyprotobassic acid, and the known compound, 3-O-beta-D-glucopyranosyl-28-O-(alpha-L-rhamnopyranosyl-(1-->3)[beta-D-xylopyranosyl-(1-->4)]-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl)-protobassic acid. Two further saponins were obtained from the same fraction, but as a 5:4 mixture comprising 3-O-(beta-D-glucopyranosyl)-28-O-(alpha-L-rhamnopyranosyl-(1-->3)-beta-D-xylopyranosyl-(1-->4)[beta-D-apiofuranosyl-(1-->3)]-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl)-16alpha-hydroxyprotobassic acid and 3-O-(beta-D-apiofuranosyl-(1-->3)-beta-D-glucopyranosyl)-28-O-(alpha-L-rhamnopyranosyl-(1-->3)[beta-D-xylopyranosyl-(1-->4)]-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl)-16alpha-hydroxyprotobassic acid, respectively. This showed greater cytotoxicity (IC(50)=11.9+/-1.5 microg/ml) towards RAW 264.7 cells than the original extract (IC(50)=39.5+/-4.1 microg/ml), and the saponin-containing fraction derived from it (IC(50)=33.7+/-6.2 microg/ml).

Observation of C60 film formation on a highly oriented pyrolitic graphite substrate via scanning tunnelling microscopy

We have investigated the early stages in the adsorption process of C60 molecules on a highly oriented pyrolitic graphite (HOPG) substrate. C60 powder was thermally evaporated in UHV of 10−8 Pa conditions onto a freshly cleaved HOPG surface. We did not observe individual fullerenes on the substrate for the case of short deposition times and low evaporation rates. However, small islands of C60 molecules with an fcc structure could be observed when the deposition rate was about 0.2 nm/min and the total thickness was above 1 nm. The islands did not grow in the vicinity of the HOPG steps. The typical lateral dimensions of these islands were of the order of a few hundred square nanometers, having thickness of up to five monolayers. We modified the shapes and positions of these islands by the STM tip, using a small (less than 1 V) bias voltage.

Simulation of transverse and longitudinal magnetic ripple structures induced by surface anisotropy

Micromagnetic ripple structures on the surfaces of thick specimens of ultra-soft magnetic material having strong surface anisotropy Ks favouring out-of-surface magnetization have been calculated. These ripples have wavelengths of the order of 0.1 μm and extend to a depth ∼ √A/Ms, where A is the exchange constant and Ms is the saturation magnetization. The wave-vectors of the ripple structures are either transverse or parallel to the bulk magnetization. Both structures have lower energy than the one-dimensional structure discussed by O'Handley and Woods, and they exhibit stronger normal magnetization. The transverse structure requires a surface anisotropy Ks ≥ 0.80K0, where is that required for the one-dimensional structure. The threshold for longitudinal ripples is 0.84K0. It is suggested that the transverse structure probably constitutes the ground state. The magnitudes of Ks and A should be obtainable from measurements of the ripple wavelength and amplitude, and Ms.

Estimating the flow rate capacity of an overturned rail carriage end exit in the presence of smoke

While incidents requiring the rapid egress of passengers from trains are infrequent, perhaps the most challenging scenario for passengers involves the evacuation from an overturned carriage subjected to fire. In this paper we attempt to estimate the flow rate capacity of an overturned rail carriage end exit. This was achieved through two full-scale evacuation experiments, in one of which the participants were subjected to non-toxic smoke. The experiments were conducted as part of a pilot study into evacuation from rail carriages. In reviewing the experimental results, it should be noted that only a single run of each trial was undertaken with a limited — though varied — population. As a result it is not possible to test the statistical significance of the evacuation times quoted and so the results should be treated as indicative rather than definitive. The carriage used in the experiments was a standard class Mark IID which, while an old carriage design, shares many features with those carriages commonly found on the British rail network. In the evacuation involving smoke, the carriage end exit was found to achieve an average flow rate capacity of approximately 5.0 persons/min. The average flow rate capacity of the exit without smoke was found to be approximately 9.2 persons/min. It was noted that the presence of smoke tended to reduce significantly the exit flow rate. Due to the nature of the experimental conditions, these flow rates are considered optimistic. Finally, the authors make several recommendations for improving survivability in rail accidents. Copyright © 2000 John Wiley & Sons, Ltd.

Predictions of segregation of granular material with the aid of PHYSICA, a 3-D unstructured finite-volume modelling framework

In this paper a continuum model for the prediction of segregation in granular material is presented. The numerical framework, a 3-D, unstructured grid, finite-volume code is described, and the micro-physical parametrizations, which are used to describe the processes and interactions at the microscopic level that lead to segregation, are analysed. Numerical simulations and comparisons with experimental data are then presented and conclusions are drawn on the capability of the model to accurately simulate the behaviour of granular matter during flow.

Across the bridge: CLEF 2001 - Non-English monolingual retrieval. The French task.

This paper presents work on document retrieval based on first time participation in the CLEF 2001 monolingual retrieval task using French. The experiment findings indicated that Okapi, the text retrieval system in use, can successfully be used for non-English text retrieval. A lot of internal pre-processing is required in the basic search system for conversion into Okapi access formats. Various shell scripts were written to achieve the conversion in a UNIX environment, failure of which would significantly have impeded the overall performance. Based on the experiment findings using Okapi - originally designed for English - it was clear that, although most European languages share conventional word boundaries and variant word morphemes formed by the additon of suffixes, there is significant difference between French and English retrieval depending on the adaptation of indexing and search strategies in use. No sophisticated method for higher recall and precision such as stemming techniques, phrase translation or de-compounding was employed for the experiment and our results were suggestively poor. Future participation would include more refined query translation tools.

Investigating the representation of merging behavior at the floor–stair interface in computer simulations of multi-floor building evacuations

In this article, the representation of the merging process at the floor— stair interface is examined within a comprehensive evacuation model and trends found in experimental data are compared with model predictions. The analysis suggests that the representation of floor—stair merging within the comprehensive model appears to be consistent with trends observed within several published experiments of the merging process. In particular: (a) The floor flow rate onto the stairs decreases as the stair population density increases. (b) For a given stair population density, the floor population's flow rate onto the stairs can be maximized by connecting the floor to the landing adjacent to the incoming stair. (c) In situations where the floor is connected adjacent to the incoming stair, the merging process appears to be biased in favor of the floor population. It is further conjectured that when the floor is connected opposite the incoming stair, the merging process between the stair and floor streams is almost in balance for high stair population densities, with a slight bias in favor of the floor stream at low population densities. A key practical finding of this analysis is that the speed at which a floor can be emptied onto a stair can be enhanced simply by connecting the floor to the landing at a location adjacent to the incoming stair rather than opposite the stair. Configuring the stair in this way, while reducing the floor emptying time, results in a corresponding decrease in the descent flow rate of those already on the stairs. While this is expected to have a negligible impact on the overall time to evacuate the building, the evacuation time for those higher up in the building is extended while those on the lower flows is reduced. It is thus suggested that in high-rise buildings, floors should be connected to the landing on the opposite side to the incoming stair. Information of this type will allow engineers to better design stair—floor interfaces to meet specific design objectives.

A sensitive bioassay for the mycotoxin aflatoxin B1, which also responds to the mycotoxins aflatoxin G1 and T-2 toxin, using engineered baker's yeast

A novel aflatoxin B(1) bioassay was created by introducing a Lipomyces kononenkoae alpha-amylase gene into a strain of S. cerevisiae capable of expressing the human cytochrome P450 3A4 (CYP3A4), and the cognate human CYP450 reductase. This strain and a dextranase-expressing strain were used in the development of a microtitre plate mycotoxin bioassay, which employed methanol as the solvent and polymyxin B nonapeptide as a permeation enhancer. Stable co-expression of the CYP3A4 gene system and of the dextranase and amylase genes in the two bioassay strains was demonstrated. The bioassay signalled toxicity as inhibition of secreted carbohydrase activity, using sensitive fluorimetric assays. The amylase-expressing strain could detect aflatoxin B(1) at 2 ng/ml, and was more sensitive than the dextranase-expressing strain. Aflatoxin G(1) could be detected at 2 microg/ml, and the trichothecene mycotoxin T-2 toxin was detectable at 100 ng/ml.

Triterpenoid saponins from the cytotoxic root extract of Sideroxylon foetidissimum, an endemic Yucatecan medicinal plant

The flora of the Yucatan peninsula (Mexico) includes approximately 3000 plant species. Sideroxylon foetidissimum Jacq. subsp. gaumeri (Sapotaceae) is an endemic plant to the Yucatan peninsula; its fruit is edible and local people use the plant for medicinal purposes, although no details on its preparation or application are available [1,2]. A preliminary cytotoxic evaluation of the ethanolic root extract of S. foetidissimum revealed a potent activity against murine macrophage like cell line RAW 264.7 (IC50=39.54±4.11µg/mL). The systematic bioassay-guided fractionation of the extract resulted in the identification of the active saponin-containing fraction (IC50=33.69±6.19µg/mL). Four new triterpenoid saponins and a 1:1 mixture of two saponins were isolated from the active saponin- containing fraction. The evaluation of their cytotoxic activity revealed no activity for the tested pure saponins; however, the 1:1 mixture of saponins showed a potent activity (IC50=11.91±1.49µg/mL). The isolation of the saponins was carried out using semi-preparative HPLC. The structural assignments of the pure saponins were based on 1D (1H and 13C and DEPT-135) and 2D (COSY, HMBC, HSQC and TOCSY) NMR and mass spectrometry analyses. In this presentation, the isolation, identification and cytotoxic activity of the isolated compounds is discussed in more detail.