The fungitoxicity of substituted 2-phenylbenzofurans

Thirty-seven 2-phenylbenzofurans, variously substituted in the homocyclic rings, were synthesised and assessed for antifungal activity in laboratory tests. High activity was shown only by compounds containing a hydroxy group, though amino compounds were also fungitoxic but at a lower level. Possible mechanisms by which these substitutions impart fungitoxicity are discussed with particular reference to the partitioning properties of the molecule.     

Hydroxypyrimidine fungicides inhibit adenosine deaminase in barley powdery mildew

Adenine and adenosine are metabolized by the adenine salvage pathway during primary infection of barley powdery mildew, Erysiphe graminis f.sp. hordei. Operation of this pathway was affected by the hydroxypyrimidine fungicide, ethirimol. Adenosine deaminase, ADAase, which was detected in mildew conidia and infected plants, but not in healthy barley, was the only enzyme in this pathway inhibited by the fungicide in in vitro assays. This feature of the mildew enzyme was unusual, and correlates with the specificity of hydroxypyrimidines which act against powdery mildews only. Other properties of this enzyme were similar to ADAase from other sources. In structure/activity studies with dimethirimol analogs, poor fungicidal activity was often associated with failure to inhibit ADAase, especially when assayed during appressoria formation. Purine derivatives were much less specific, and their mode of action against powdery mildew is probably different. Ethirimol resistance was not related to changes in ADAase, nor was the fungicide altered to an inactive metabolite. It is concluded that ADAase is one site of hydroxypyrimidine action.     

Phloem transport of xenobiotics in Ricinus communis var. Gibsonii

Whole plants of Ricinus communis var. Gibsonii were used to study the mobility of some xenobiotics in the phloem. Solutions of ¹⁴C- or ³⁵S-labelled test compounds were introduced directly into the hollow petiole of a leaf that was exporting assimilates. Translocation was monitored by collecting phloem exudate from an incision in the stem bark beneath the treated leaf. Using [³H]sucrose as an internal standard, qualitative and quantitative results were obtained for a variety of model compounds, including herbicides, fungicides and a nematicide.     

Hydrogen isotopes in Eocene river gravels and paleoelevation of the Sierra Nevada

We determine paleoelevation of the Sierra Nevada, California, by tracking the effect of topography on precipitation, as recorded in hydrogen isotopes of kaolinite exposed in gold-bearing river deposits from the Eocene Yuba River. The data, compared with the modern isotopic composition of precipitation, show that about 40 to 50 million years ago the Sierra Nevada stood tall (>/=2200 meters), a result in conflict with proposed young surface uplift by tectonic and climatic forcing but consistent with the Sierra Nevada representing the edge of a pre-Eocene continental plateau.     

Insulin-like growth factor binding protein-3: its biological effect on bovine granulosa cells

This study was aimed at testing the hypothesis that insulin-like growth factor binding protein (IGFBP)-3 can modulate hormone-dependent differentiation of granulosa cells in vitro. Granulosa cells from small (1 to 5 mm) follicles were collected from cattle, cultured for 2 d in medium containing 10% fetal calf serum, washed, and then treated for an additional 2 d in serum-free medium with follicle-stimulating hormone (FSH) (50 ng/ml), recombinant human IGF-I (0, 1.3, 4.0, or 13.3 nM), or recombinant human IGFBP-3 (0 to 4.26 nM). In one series of experiments, IGFBP-3 (0.53 and 2.13 nM) inhibited (51% to 92% decreases; P < 0.05) progesterone and estradiol production induced by 1.3 nM of IGF-I, but did not influence (P > 0.10) granulosa cell numbers or steroidogenesis in the absence of IGF-I. Only 4.26 nM of IGFBP-3 inhibited (by 35%) the increase in granulosa cell numbers induced by 1.3 nM of IGF-I. In another series of experiments, 13.3 nM of IGF-I, but not 4.0 nM of IGF-I, was able to completely overcome the inhibitory effect of 4.26 nM of IGFBP-3 on estradiol production. The increase in cell numbers induced by 4.0 and 13.3 nM of IGF-I was attenuated (P < 0.001) by 4.26 nM of IGFBP-3. In a third series of experiments, IGFBP-3 inhibited 125I-IGF-I binding to granulosa cells. These results indicate that IGFBP-3 has a pronounced inhibitory effect on IGF-I action in cultured bovine granulosa cells, and that this inhibitory effect is likely attributable to IGFBP-3 binding/sequestering IGF-I. Thus, IGFBP-3 may play a significant role in regulating granulosa cell proliferation and steroidogenesis during follicular development in cattle.