Quantitative ion determination in eccrine sweat gland cells correlates to sweat reduction of antiperspirant actives.

OBJECTIVE: Axillary wetness represents an unwanted effect of the physiologically vital sweating mechanism, especially when it becomes excessive. Cosmetic products reducing sweat secretion rely on aluminium salts as the active ingredient acting by physically blocking the sweat gland. Driven by the interest to better understand the sweat mechanism and to develop alternative technologies against excessive sweating a search for an effective testing approach started as up to now, cost- and time-consuming in vivo studies represent the standard procedure for testing and identifying these alternatives. MATERIAL AND METHODS: The herein described in vitro test system is based on the measurement of intracellular changes of the ion equilibrium in cultured eccrine sweat gland cells. Subsequently, in vivo studies on the back of volunteers were conducted to verify the sweat-reducing effect of in vitro newly discovered substance. RESULTS: In this study, we describe an effective cell-based in vitro method as a potent tool for a more targeted screening of alternatives to aluminium salts. Testing the commonly used aluminium chlorohydrate as one example of an aluminium-based active in this screening procedure, we discovered a distinct influence on the ion equilibrium: Intracellular levels of sodium ions were decreased while those of chloride increased. Screening of various substances revealed a polyethyleneimine, adjusted to pH 3.5 with hydrochloric acid, to evoke the same alterations in the ion equilibrium as aluminium chlorohydrate. Subsequent in vivo studies showed its substantial antiperspirant action and confirmed the high efficiency of the polyethyleneimine solution in vivo. Further, specific investigations connecting the chloride content of the tested substances with the resulting sweat reduction pointed towards a substantial impact of the chloride ions on sweating. CONCLUSION: The newly described in vitro cell-based screening method represents an effective means for identifying new antiperspirant actives and suggests an additional biological mechanism of action of sweat-reducing ingredients which is directed towards unbalancing of the ion equilibrium inside eccrine sweat gland cells.

OBJECTIF: l'humidité axillaire représente un effet indésirable du mécanisme physiologiquement vital de la sudation, en particulier lorsqu'elle devient excessive. Les produits cosmétiques réduisant la sécrétion de sueur reposent sur les sels d'aluminium comme principe actif agissant en bloquant physiquement la glande sudoripare. Motivée par l'intérêt de mieux comprendre le mécanisme de la sudation et de développer des technologies alternatives contre l'hypersudation, une recherche pour une approche de test efficace a commencé car, jusqu'à présent, les études in vivo coûteuses et chronophages représentent la procédure standard pour tester et identifier ces alternatives. MATÉRIELS ET MÉTHODES: le système de test in vitro décrit ici est basé sur la mesure des changements intracellulaires de l'équilibre ionique dans les cellules des glandes sudoripares exocrines cultivées. Par la suite, des études in vivo sur le dos de volontaires ont été menées pour vérifier l'effet réducteur de la sudation d'une substance nouvellement découverte in vitro. RÉSULTATS: dans cette étude, nous décrivons une méthode cellulaire efficace in vitro en tant qu'outil puissant pour un dépistage plus ciblé des alternatives aux sels d'aluminium. En testant le chlorohydrate d'aluminium couramment utilisé comme exemple d'un principe actif à base d'aluminium dans cette procédure de dépistage, nous avons découvert une influence distincte sur l'équilibre ionique : les taux intracellulaires d'ions sodium ont diminué tandis que ceux du chlorure ont augmenté. La recherche de diverses substances a révélé une polyéthylèneimine, ajustée au pH 3,5 avec de l'acide chlorhydrique, pour évoquer les mêmes altérations de l'équilibre ionique que le chlorohydrate d'aluminium. Des études in vivo ultérieures ont montré son action anti-transpirante substantielle et ont confirmé la haute efficacité de la solution de polyéthylèneimine in vivo. De plus, des études spécifiques établissant un lien entre la teneur en chlorure des substances testées et la réduction de la sudation qui en résulte ont indiqué que les ions chlorure ont un impact substantiel sur l'hypersudation. CONCLUSION: la nouvelle méthode de dépistage cellulaire in vitro décrite représente un moyen efficace d'identifier de nouveaux agents anti-transpirants actifs et suggère un mécanisme d'action biologique supplémentaire des ingrédients réducteurs de la sudation, dirigé vers le déséquilibre de l'équilibre ionique à l'intérieur des cellules des glandes sudoripares exocrines.

Identification of compounds inhibiting the C-S lyase activity of a cell extract from a Staphylococcus sp. isolated from human skin.

UNLABELLED: The C-S lyase activity of bacteria in the human armpit releases highly malodorous, volatile sulfur compounds from nonvolatile precursor molecules. Such compounds significantly contribute to human body odour. Hence, C-S lyase represents an attractive target for anti-body-odour cosmetic products. Here, aiming at a final use in an ethanol-based deodorant formulation, 267 compounds and compound mixtures were screened for their ability to inhibit the C-S lyase activity of a Stapyhlococcus sp. crude extract. Staphylococcus sp. Isolate 128, closely related to Staphylococcus hominis, was chosen as the test bacterium, as it showed a reproducibly high specific C-S lyase activity on three different culturing media. Using a photometric assay and benzylcysteine as substrate, six rather complex, plant-derived compound mixtures and five well defined chemical compounds or compound mixtures were identified as inhibitors, leading to an inhibition of ≥70% at concentrations of ≤0·5% in the assay. The inhibition data have demonstrated that compounds with two vicinal hydroxyl groups or one hydroxyl and one keto group bound to an aryl residue are characteristic for the inhibition. The substances identified as C-S lyase inhibitors have the potential to improve the performance of anti-body-odour cosmetic products, for example, ethanol-based deodorants. SIGNIFICANCE AND IMPACT OF THE STUDY: Bacterial C-S lyase represents one of the key enzymes involved in human body odour formation. The aim of this study was to identify compounds inhibiting the C-S lyase activity of a Staphylococcus sp. isolate from the human skin. The compounds identified as the best inhibitors are characterized by the following features: two vicinal hydroxyl groups or one hydroxyl and one keto group bound to an aryl residue. They might be used to improve the performance of cosmetic products aiming to prevent the formation of microbially caused human body odour, for example, ethanol-based deodorants.