Rationale for the synthesis and preliminary biological evaluation of highly active new antitumor nitrosoureido sugars.

Various new nitrosoureido derivatives of di- or trideoxy sugars were synthesized. The influence of the hydroxyl substitution pattern, the configuration at the anomeric center, and the absolute configuration of the sugar moiety on the antitumor activity of a series of nitrosoureido derivatives of di- and trideoxy sugars was studied. All compounds showed a very significant activity in vivo against L1210 leukemia, B16 melanocarcinoma, and Lewis lung carcinoma. Methyl 3-[3-(2-chloroethyl)-3-nitrosoureido]-2,3-dideoxy-alpha-D-arabino- hexopyranoside, 24 (NSC 609224), was found to be the most active compound. When treated with 24 (NSC 609224) at 20 mg/kg on day 1, at least 90% of the L1210 leukemia and B16 melanocarcinoma bearing mice showed a survival of over 60 days for a LD50 value for this compound of 42 mg/kg.

Electrophysiological and inotropic effects of natural amino-deoxyglyco-cardenolides.

The electrophysiological, inotropic and chronotropic effects of the two first natural amino-dexoyglyco-cardenolides, mitiphylline and holarosine B, were studied. Mitiphylline has qualitatively the same properties as those of common cardiac glycosides but is more potent; holarosine B has a similar action on cardiac electrophysiological parameters of the guinea pig heart but is less potent. The difference in activity between these two compounds could be attributed to the configuration in 5-and 17-positions of the genins. Holarisone B has the particularity of increasing the action potential plateau amplitude and its duration in rat heart; this could be part of the role of the aminosugar moiety.

[Micronutritional requirements during women's life]. / Besoins micronutritionnels au cours de la vie d'une femme.

The recommended nutrition requirements differ according to the age and sex as well as to physiological events and life habits of women. Whereas the role of antioxidants in the slowing of metabolic aging or reduction of the consequences of the stress is widely stated in the media, scientifically established benefits are less well known, such as the role played by the antioxidants on the phaners and the tegumental resistance to ultraviolet aggressions or the major role played by the antioxidants in the fight against opacity of lens and macular degeneration. Folates have a well-known preventive action on the prevention of abnormal closing of the neural tube, on the reduction of the risks of hypotrophy and prematurity during pregnancy. The reduction of hyperhomocysteinemia by vitamin B9 participates actively in the reduction of the cardiovascular risk. As the benefits expected are documented and needed daily doses higher than those brought by a balanced diet, or too often assumed as such, mineral-vitamin supplementation of women living in developed countries appears to warranted.

[Taurine: a particular aminoacid with multiple functions]. / La taurine: un aminoacide particulier aux fonctions multiples.

Taurine has multiple biological and metabolic functions: this particular B-amino acid is an antioxidant, it conjugates biliary acids, detoxifies some xenobiotics and modulates intracellular calcium levels. Moreover, taurine plays an important part in osmoregulation, neuromodulation and stabilization of the membranes. Taurine is looked upon as an "essential amino acid" in some particular situations associating inadequate intake or synthesis and major loss of biliary salts. Clinically, taurine has been used with varying degrees of success in the treatment of several pathologies (cardiovascular diseases, cystic fibrosis, alcoholism, retinal degeneration, hepatic disorders). Being found in the secretions of the mammalian reproductive tract, it preserves the motility of the spermatozoa, supports their capacitation, improves the chances of success of fertilization and the early embryonic development. This is why it can be found in some culture media for in vitro fertilization.

[Value of micronutrient supplements in the prevention or correction of disorders accompanying menopause]. / Intérêt d'une supplémentation en micronutriments pour la prévention ou la correction des troubles accompagnant la ménopause.

The risk of nutritional disturbances, in particular vitamin and trace element deficiencies, is high during the menopause. Such deficiency, revealed by nutritional surveys, results for life style as well as the natural events of ageing, together with hormonal disturbances. The consequences of these deficiencies concern sensitivity to estrogens, structure of the skin and its accessory structures, bone metabolism, immune function and increased risk of degenerative pathology, in particular cardiovascular. Balanced and appropriate, multivitamin and mineral supplements i.e. containing all vitamin (A, B2, B5, B6, B9, E) and minerals (Cr, Cu, Mg, Se, Si, Zn), thus appear to be justified.