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
- PMID: 8554461
- DOI: 10.1002/ardp.19953281006
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
Abstract
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 IC50 values (hederagenin IC50 = 280.4 microM; oleanolic acid IC50 = 300.2 microM); both the saponins hederacoside C and alpha-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 IC50 = 5.1 microM; hederagenin IC50 = 40.6 microM). Constituents from Aesculus hippocastanum L. show inhibitory effects only on hyaluronidase, and this activity is mainly linked to the saponin escin (IC50 = 149.9 microM), less to its genin escinol (IC50 = 1.65 mM). By contrast, ruscogenins from Ruscus aculeatus L., ineffective on hyaluronidase activity, exhibit remarkable anti-elastase activity (IC50 = 119.9 microM; competitive inhibition). The mechanism of elastase inhibition by triterpene and steroid aglycones, with a nitroanilide derivative as substrate, is discussed.
Similar articles
-
The structure-hemolysis relationship of oleanolic acid derivatives and inhibition of the saponin-induced hemolysis with sapogenins.J Pharmacobiodyn. 1981 Nov;4(11):833-7. doi: 10.1248/bpb1978.4.833. J Pharmacobiodyn. 1981. PMID: 7328484
-
Free radicals scavenging action and anti-enzyme activities of procyanidines from Vitis vinifera. A mechanism for their capillary protective action.Arzneimittelforschung. 1994 May;44(5):592-601. Arzneimittelforschung. 1994. PMID: 8024628
-
Ruscus Genus: A Rich Source of Bioactive Steroidal Saponins.Planta Med. 2016 Dec;82(18):1513-1524. doi: 10.1055/s-0042-119728. Epub 2016 Nov 8. Planta Med. 2016. PMID: 27825178 Review.
-
Hyaluronidase inhibitory saponins and a trypanocidal isoflavonoid from the aerial parts of Oxytropis lanata.Fitoterapia. 2020 Sep;145:104608. doi: 10.1016/j.fitote.2020.104608. Epub 2020 May 6. Fitoterapia. 2020. PMID: 32387375
-
Phytochemical, ethanomedicinal and pharmacological applications of escin from Aesculus hippocastanum L. towards future medicine.J Basic Clin Physiol Pharmacol. 2020 Jul 10;31(5):/j/jbcpp.2020.31.issue-5/jbcpp-2019-0115/jbcpp-2019-0115.xml. doi: 10.1515/jbcpp-2019-0115. J Basic Clin Physiol Pharmacol. 2020. PMID: 32649293 Review.
Cited by
-
Remnants from the Past: From an 18th Century Manuscript to 21st Century Ethnobotany in Valle Imagna (Bergamo, Italy).Plants (Basel). 2023 Jul 24;12(14):2748. doi: 10.3390/plants12142748. Plants (Basel). 2023. PMID: 37514363 Free PMC article.
-
Inhibitory effect of β-escin on Zika virus infection through the interruption of viral binding, replication, and stability.Sci Rep. 2023 Jun 20;13(1):10014. doi: 10.1038/s41598-023-36871-1. Sci Rep. 2023. PMID: 37340032 Free PMC article.
-
Can Extracts from the Leaves and Fruits of the Cotoneaster Species Be Considered Promising Anti-Acne Agents?Molecules. 2022 May 2;27(9):2907. doi: 10.3390/molecules27092907. Molecules. 2022. PMID: 35566257 Free PMC article.
-
16-Tigloyl linked barrigenol-like triterpenoid from Semen Aesculi and its anti-tumor activity in vivo and in vitro.RSC Adv. 2019 Oct 7;9(54):31758-31772. doi: 10.1039/c9ra06015d. eCollection 2019 Oct 1. RSC Adv. 2019. PMID: 35527978 Free PMC article.
-
Paving the way towards effective plant-based inhibitors of hyaluronidase and tyrosinase: a critical review on a structure-activity relationship.J Enzyme Inhib Med Chem. 2022 Dec;37(1):1120-1195. doi: 10.1080/14756366.2022.2061966. J Enzyme Inhib Med Chem. 2022. PMID: 35470749 Free PMC article. Review.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources