Increase in the survival time of mice exposed to ionizing radiation by a new class of free radical scavengers

Summary N-acyl dehydroalanines react with and scavenge mainly superoxide radical and hydroxyl radical (HO^.). The ortho-methoxyphenylacetyl dehydroalanine derivative, indexed as AD-20, protects mice against damage resulting from total body X-irradiation, as measured by the increase in their survival time. AD-20 increases the LD₅₀ at 30 days from 6.1 to 7.3 Gy in animals exposed to a wide range of X-rays (6 to 10 Gy). The dose reduction factor (D R F) of AD-20 is 1.20. We postulate that such radioprotective effect may result from its free radical scavenging activity.     

Effects of a new cholecystokinin antagonist (GE 410) on the smooth muscle of the guinea pig ileum

Summary Suc-Tyr-(SE)-Met-Gly-Trp-Met-Asp--phenethylamide (GE 410) competitively antagonized the contractions of smooth muscle strips from guinea pig ileum (pA₂=7.6, n=0.95) induced by cholecystokinin-octapeptide (CCK8). GE 410 inhibited the electrically-induced cholinergically mediated contractile responses and the [³H]ACh release in the ileum, as well as the CCK-stimulated electrical contractile responses and the [³H]ACh release in the cholinergic nerve terminals. The results suggest the existence of CCK-receptors not only in the smooth muscles but also on the neurons.     

Gigantecin: A novel antimitotic and cytotoxic acetogenin,with nonadjacent tetrahydrofuran rings,fromGoniothalamus giganteus (Annonaceae)

Summary Gigantecin (I), a novel tetrahydroxy-di-tetrahydrofuran fatty acid -lactone (acetogenin), was isolated from an ethanolic extract of the stem bark ofGoniothalamus giganteus Hook. f., Thomas (Annonaceae), by means of activity-directed fractionation (brine shrimp lethality test). This new compound is extremely cytotoxic to human tumor cells, inhibits crown gall tumors on potato discs, and is active in an assay designed to detect antimitotic agents (9 ASK).     

Proton-induced dismutation of superoxide in aprotic media by bile pigments

Summary Cyclic voltammetry of molecular oxygen in aprotic media (dimethylformamide) and in the presence of bilirubin and other bile pigments shows that superoxide anion ( ) undergoes proton-induced dismutation. Lactam hydrogens of bile pigments are sufficiently acid to induce disproportionation to O₂ and H₂O₂. Because of its characteristic lipophilic behavior, a biological role for natural bilirubin similar to that of other non-enzymatic lipophilic scavengers of is suggested.     

Inhibition of the growth of cariogenic bacteria in vitro by plant falvanones

Phytoalexins, defensive compounds produced by plants against microbial infections, were purified fromSophora exigua (Leguminosae) and their growth inhibitory effects on oral cariogenic bacteria were determined in vitro. Among three isolated compounds, 5,7,2,4-tetrahydroxy-8-lavandulylflavanone completely inhibited the growth of oral bacteria including primary cariogenic mutans streptococci, other oral streptococci, actinomycetes, and lactobacilli, at concentrations of 1.56 to 6.25 g/ml.     

Variability of sterol utilization in stored-products insects

A comparison of sterol utilization by 3 stored-products insects revealed very different capabilities. The fluor beetle,Tribolium castaneum dealkylates and converts dietary sitosterol to about equal amounts of cholesterol (43.7%) and 7-dehydrocholeterol (39.8%), whereas another flour beetle,Tenebrio molitor, produces considerably less 7-dehydrocholesterol (16.8%) and relatively more cholesterol (66.7%) from sitosterol. The lepidopteran,Plodia interpunctella, utilized dietary sterol very similar to plant-feeding lepidoptera, producing primarily cholesterol (86.5%) from sitosterol.     

A novel mechanism for jumping in the indian ant<Emphasis Type="Italic">Harpegnathos saltator</Emphasis> (Jerdon) (Formicidae,Ponerinae)

The Indian antHarpegnathos saltator may be unique among insects in using its jumping capacity not only as an escape mechanism but also as a normal means of locomotion, and for catching its prey in flight. High-speed cinematography used to analyse the various phases of the jump suggests thatHarpegnathos employs a novel jumping mechanism to mediate these behaviours: namely the synchronous activation of its middle and hindlegs. Electrophysiological recordings from muscles or nerves in pairs of middle and hindlegs show remarkably synchronous activity during fictive jumping, supporting the synchronous activation hypothesis.Harpegnathos is not the only ant to jump, and a cladistic analysis suggests that jumping behaviour evolved independently three times during ant evolutionary history.     

Influence of bistramide A on the twitch tension in rat atrial heart muscle

Bistramide A, a new toxin isolated from the UrochordateLissoclinum bistratum Sluiter, was applied to rat auricular heart muscle bundles. At a stimulation frequency of 0.2 Hz, the toxin induces a dose-dependent reduction of the stimulated twitch tension force; it decreases and shortens the duration of the plateau and the slow repolarizing phase of the action potential. In the control solution, switching from a stimulation frequency of 0.2 Hz to 1 Hz decreases the force with which a positive potentiation develops either at a maintained high frequency or after switching from 1 Hz to 0.2 Hz. Bistramide A reduces both the force evoked at 1 Hz and the potentiation. The data suggest that Bistramide A blocks Na⁺ conductance; inhibits Ca⁺⁺ channels in a time-and frequency-dependent manner; reduces Na⁺–Ca⁺⁺ exchange activity; but does not modify the ability of the sarcoplasmic reticulum to be refilled although the rate of Ca⁺⁺ accumulation is decreased.     

The in vivo expression of the globin genes of theβ cistron in γ-,δ-, andδβ-thalassemia heterozygotes

There is considerable evidence suggesting that the switch from to and chain production after birth is due, in part, to silencing of the genes by stage-specific factors which bind to their promoters and to the competition from the adult ( and ) genes for a common enhancer element located in the locus control region. As a consequence one can expect that the increased Hb F production in adults with hereditary persistence of fetal hemoglobin or -thalassemia is directed mainly by -globin genes in cis to the deletion(s) responsible for these conditions. Here we review data on heterozygotes with -, -, or -thalassemia, who also had an^AT mutation, in cis or in trans, which was used as a marker of gene expression. The results show that a deletion affecting adult genes favors the expression of genes in cis, while the deletion of a single gene does not affect the expression of the gene in cis but leads to a faster switch postnatally.