Abstract

In this study, three of the saponins present in leaves of Hedera helix L., α-hederin, hederagenin, and hederacoside C were studied for their antiproliferative activity. The three saponins were analyzed in different concentrations by in vitro tests on normal fibroblasts cells and cervix ephitelial tumor cells. Determination of cytotoxicity and antitumor effects was performed using the MTT method. From the tested saponins, α-hederin was biocompatible in normal fibroblasts cells at concentrations between 2–10 μg/mL. Its antiproliferative activity was exerted in the concentration range of 10–400 μg/mL in cervix ephitelial tumor cells. Similarly, hederagenin presented antiproliferative activity at concentrations between 25–400 μg/mL. In turn, hederacoside C was shown to be noncytotoxic in normal fibroblasts and cervix ephitelial tumor cell culture at all the tested concentrations. The obtained experimental results were analyzed by “Mixture design”, a specialized form of the response surface method (RSM) provided by the Design Expert 11 software, and the optimal composition of obtained saponins mixture was selected and verified in vitro for antiproliferative activity. The results showed that an optimal saponins mixture has the potential to be used in pharmacological applications.

Highlights

  • Saponins are found in a variety of higher plants, and display a wide range of pharmacological activities, including expectorant, anti-inflammatory, vasoprotective, gastroprotective, antihelmintic, antileishmanial, antifungal, and antimicrobial properties [1,2,3,4]

  • The aim of this study was to evaluate the in vitro cytotoxic and antiproliferative activity induced by the three triterpenic saponins, i.e., α-hederin, hederagenin, and hederacoside C, and to optimize a mixture of the three standard saponins for a maximal antiproliferative effect

  • Fibroblasts were seeded at a density of 4 × 104 cells/mL for NCTC culture and 4 × 104 cells/ mL, while Hep-2 cells were seeded at a density of 6 × 104 cells/ mL in 96-well culture plates and incubated at 37◦ C in a humid atmosphere with 5% CO2 for 24 h using a Bioquell biology security cabinet

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Summary

Introduction

Saponins are found in a variety of higher plants, and display a wide range of pharmacological activities, including expectorant, anti-inflammatory, vasoprotective, gastroprotective, antihelmintic, antileishmanial, antifungal, and antimicrobial properties [1,2,3,4]. Saponins are amphiphilic compounds composed of one or more hydrophilic sugar parts and a lipophilic steroidal or triterpenic part (sapogenin). Saponins can be classified into monodesmosidic, bidesmosidic, or polydesmosidic saponins, having one, two, or more sugar chains. A large structural variety can be found in nature, due to the presence of different sugars, sugar branchings, and sapogenins [9,10,11]. The interesting properties of saponins have led us to investigate the monodesmosidic saponin α-hederin, which has shown activities towards cancer cells [12].

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