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Anti‐Elastase and Anti‐Hyaluronidase Activities of Saponins and Sapogenins from Hedera helix, Aesculus hippocastanum , and Ruscus aculeatus : Factors Contributing to their Efficacy in the Treatment of Venous Insufficiency
Author(s) -
Facino Roberto Maffei,
Carini Marina,
Stefani Rita,
Aldini Giancarlo,
Saibene Luisella
Publication year - 1995
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19953281006
Subject(s) - sapogenin , aesculus hippocastanum , hedera helix , saponin , traditional medicine , hyaluronidase , chemistry , achene , araliaceae , elastase , botany , pharmacognosy , biology , medicine , biological activity , biochemistry , enzyme , alternative medicine , pathology , in vitro , ginseng
Triterpene and steroid saponins and sapogenins of medicinal plants ( Aesculus hippocastanum L., Hedera helix L., Ruscus aculeatus L.) are claimed to be effective for the treatment/prevention of venous insufficiency. In this work we evaluated the inhibitory effects of these plant constituents on the activity of elastase and hyaluronidase, the enzyme systems involved in the turnover of the main components of the perivascular amorphous substance. The results evidence that for Hedera helix L., the sapogenins only non‐competitively inhibit hyaluronidase activity in a dose‐dependent fashion, showing comparable IC 50 values (hederagenin IC 50 = 280.4 μM; oleanolic acid IC 50 = 300.2 μM); both the saponins hederacoside C and α‐hederin are very weak inhibitors. The same behaviour is observed for serine protease porcine pancreatic elastase: the glycosides are devoid of inhibitory action, while genins are potent competitive inhibitors (oleanolic acid IC 50 = 5.1 μM; hederagenin IC 50 = 40.6 μM). Constituents from Aesculus hippocastanum L. show inhibitory effects only on hyaluronidase, and this activity is mainly linked to the saponin escin (IC 50 = 149.9 μM), less to its genin escinol (IC 50 = 1.65 μM). By contrast, ruscogenins from Ruscus aculeatus L., ineffective on hyaluronidase activity, exhibit remarkable anti‐elastase activity (IC 50 = 119.9 μM; competitive inhibition). The mechanism of elastase inhibition by triterpene and steroid aglycones, with a nitroanilide derivative as substrate, is discussed.