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Antitumor activity and interleukin-1 induction by tannins
K Miyamoto1, T Murayama, M Nomura
1Research Laboratory for Development of Medicine, Hokuriku University, School of Pharmacy, Kanazawa, Japan.
Abstract:
The relationships between structures, antitumor activities and interleukin-1 (IL-1) induction by fifteen tannins were studies. When tannins (10 mg/kg) were intraperitoneally injected into mice once, 4 days before intraperitoneal inoculation of S-180 cells, tellimagrandin II, rugosin A, hirtellin B, oenothein B and oenothein A, which have only tellimagrandins I or II units in their molecules, had significant antitumor activity. Although casuarictin and its related tannins were ineffective, agrimonin, which is a dimer, had a strong effect, as previously reported. On the other hand, monomeric ellagitannins such as tellimagrandins I and II, rugosin A and casuarictin also increased IL-1 beta production from human peripheral macrophages in vitro by 2-fold over the non-stimulated basal production and oligomeric ellagitannins with strong antitumor activity more potently stimulated the IL-1 beta induction. Other tannins having no antitumor activity induced less IL-beta. This study indicates that oligomeric ellagitannins, which consist of tellimagrandin I or II, casuarictin or their related structure units, have antitumor activity and induce IL-1 beta.
Insights
Oligomeric ellagitannins, particularly those with tellimagrandin I or II units, demonstrate significant antitumor activity and effectively induce interleukin-1 beta (IL-1 beta) production, suggesting a therapeutic potential.
Area of Science:
- Natural Products Chemistry
- Immunology
- Pharmacology
Background:
- Tannins are plant-derived polyphenols with diverse biological activities.
- Interleukin-1 (IL-1) plays a crucial role in immune responses and inflammation.
- Understanding the structure-activity relationship of tannins is key to developing new therapeutic agents.
Purpose of the Study:
- To investigate the relationship between the chemical structure of tannins, their antitumor activities, and their ability to induce IL-1.
- To identify specific tannin structures responsible for antitumor effects and IL-1 induction.
Main Methods:
- Fifteen different tannins were administered to mice intraperitoneally.
- Mice were subsequently inoculated with S-180 tumor cells.
- In vitro studies assessed IL-1 beta production by human peripheral macrophages stimulated with various tannins.
Main Results:
- Oligomeric ellagitannins containing tellimagrandin I or II units, such as tellimagrandin II, rugosin A, hirtellin B, oenothein B, and oenothein A, exhibited significant antitumor activity.
- Agrimonin, a dimer, also showed strong antitumor effects.
- Monomeric and oligomeric ellagitannins stimulated IL-1 beta production in macrophages, with more potent stimulation observed for those with strong antitumor activity.
Conclusions:
- Oligomeric ellagitannins, characterized by tellimagrandin I or II, casuarictin, or related structural units, possess antitumor properties.
- These active tannins effectively induce IL-1 beta, suggesting an immunomodulatory mechanism contributing to their antitumor effects.