Miyamoto K, Murayama T, Nomura M, Hatano T, Yoshida T, Furukawa T, Koshiura R, Okuda T
Research Laboratory for Development of Medicine, Hokuriku University, School of Pharmacy, Kanazawa, Japan.
Anticancer Res. 1993 Jan-Feb;13(1):37-42.
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.
研究了15种单宁的结构、抗肿瘤活性与白细胞介素-1（IL-1）诱导之间的关系。在腹腔接种S-180细胞前4天，将单宁（10mg/kg）腹腔注射到小鼠体内一次，分子中仅含有tellimagrandins I或II单元的tellimagrandin II、rugosin A、hirtellin B、oenothein B和oenothein A具有显著的抗肿瘤活性。尽管casuarictin及其相关单宁无效，但如先前报道的，作为二聚体的仙鹤草素具有很强的作用。另一方面，单体鞣花单宁如tellimagrandins I和II、rugosin A和casuarictin在体外也能使人类外周巨噬细胞的IL-1β产生量比未刺激的基础产量增加2倍，具有强抗肿瘤活性的低聚鞣花单宁更有效地刺激IL-1β的诱导。其他无抗肿瘤活性的单宁诱导的IL-β较少。本研究表明，由tellimagrandin I或II、casuarictin或其相关结构单元组成的低聚鞣花单宁可具有抗肿瘤活性并诱导IL-1β。
