title: Saponins can perturb biologic membranes and reduce the surface tension of aqueous solutions: a correlation?
abstract: Saponins are secondary plant compounds. They have a triterpenoid or steroidal backbone. Sugars are attached to one or more points of this structure, forming chains that can be branched. This appearance leads to amphiphilic properties giving saponins the ability to interact with both lipophilic and hydrophilic structures. The surfactant behavior lets them lower the surface tension in aqueous solutions and form micelles when reaching the critical micelle concentration (cmc). It also lets them interact with biologic membrane layers that usually consist of phospholipids and cholesterol. This action may perturb the membrane and its function leading to membrane perforation or complete lysis. Thus saponins are also known for their cytotoxicity and membranolytic, respectively hemolytic features. In our studies we wanted to answer the question if there is a correlation between the unspecific detergent behavior when lowering the surface tension and the ability to perforate cell membranes and to act cytotoxic. Do saponins showing a considerable reduction in the surface tension also reveal an evident cytotoxicity or/and a marked cell membrane perforation? We tested a variety of saponins with distinct structures. The reduction in the surface tension and the cmc were analyzed on a tensiometer using the Wilhelmy plate method. The general cytotoxicity was determined in a cell model by DNA quantification. The cell membrane toxicity or membrane perforation was explored in a cell model by quantification of the leakage of the intracellular enzyme lactate dehydrogenase (LDH). The experiments revealed a correlation between the membrane toxicity and the reduction in surface tension.
authors.affiliation: Institut für Pharmazie, Pharmazeutische Biologie, Freie Universität Berlin, Königin-Luise-Str. 2+4, 14195 Berlin, Germany.
authors.forename: Stefan
authors.initials: S
authors.lastname: Böttger
authors.forename: Katja
authors.initials: K
authors.lastname: Hofmann
authors.forename: Matthias F
authors.initials: MF
authors.lastname: Melzig
mesh_terms: D045744:Cell Line, Tumor; D002462:Cell Membrane / Q000187:drug effects*; D006801:Humans; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008823:Micelles; D012503:Saponins / Q000737:chemistry / Q000302:isolation & purification / Q000633:toxicity*; D013500:Surface Tension / Q000187:drug effects*; D014867:Water / Q000737:chemistry
chemical_list: D008823:Micelles; D012503:Saponins; D014867:Water; D007770:L-Lactate Dehydrogenase