Antitrypanosomal Properties of Panax ginseng C. A. Meyer: New Possibilities for a Remarkable Traditional Drug

Abstract

African trypanosomiasis is still a major health problem in many sub‐Saharan countries in Africa. We investigated the effects of three preparations of Panax ginseng, Panax notoginseng, isolated ginsenosides, and the polyacetylene panaxynol on Trypanosoma brucei brucei and the human cancer cell line HeLa. Hexane extracts and the pure panaxynol were toxic and at the same time highly selective against T. b. brucei, whereas methanol extracts and 12 isolated ginsenosides were significantly less toxic and showed only weak selectivity. Panaxynol was cytotoxic against T. b. brucei at the concentration of 0.01 µg/mL with a selectivity index of 858, superior even to established antitrypanosomal drugs. We suggest that the inhibition of trypanothione reductase, which is only found in trypanosomes, might explain the observed selectivity. The high selectivity together with a cytotoxic concentration in the range of the bioavailability makes panaxynol and other polyacetylenes in general very promising lead compounds for the treatment of African trypanosomiasis. Copyright © 2012 John Wiley & Sons, Ltd.

Comparative study on volatile oils of four Panax genus species in Southeast Asia by gas chromatography–mass spectrometry

“…Falcarinol is a natural pesticide and anti-cancer agent. Falcarinol also called panaxynol, was identified as an antitrypanosomal, anti-inflammatory, antiplatelet, potent alpha-glucosidase inhibitors and antitumor constituent from roots of P. ginseng and other Panax species (Chan et al, 2010;Herrmann et al, 2013;Mayer et al, 2003;Otsuka et al, 1981;Teng et al, 1989). Besides, there were many studies about the biological activities of falcarinol on other plants.…”

Medicinal Plants: A Source of Anti-Parasitic Secondary Metabolites

“…It is likely that secondary metabolites which can bind to the SH-group of trypanothione exhibit anti-trypanosomal activity. This has been shown for polyacetylenes which carry a reactive triple bond that can easily alkylate SH groups; e.g., the polyacetylene Carlina oxide from Carlina acaulis (Asteraceae) ( Figure 5 ) and polyacetylenes from ginseng ( Panax ginseng ) have significant cytotoxic activity against T. b. brucei but are hardly toxic to human cells [ 47 , 48 ].…”

Structural Elucidation and Cytotoxicity of a New 17-Membered Ring Lactone from Algerian Eryngium campestre

“…However, Falcarinol, also called panaxynol, was found to be strongly active and selective (IC 50 = 0.01 µg/mL, corresponding to 0.04 µM, and SI = 858) on Trypanosoma brucei brucei compared to HeLa cytotoxicity. The inhibition of the trypanothione reductase was proposed as one target of this very reactive alkylating agent [49]. Another two natural polyacetylenes, 8-hydroxyheptadeca-1-ene-4,6-diyn-3-yl ethanoate and 16-acetoxy-11-hydroxyoctadeca-17-ene-12,14-diynyl ethanoate, were highly active and selective on Trypanosoma brucei rhodesiense , T. cruzi , Plasmodium falciparum and Leishmania donovani axenic and the infected macrophages amastigotes compared on L6 rat skeletal myoblasts (IC 50 = 0.1–2.5 µM.…”