Potent immunosuppressive principles, dimeric sesquiterpene thioalkaloids, isolated from nupharis rhizoma, the rhizoma of Nuphar pumilum (nymphaeaceae): structure-requirement of nuphar-alkaloid for immunosuppressive activity

Biol Pharm Bull. 1996 Sep;19(9):1241-3. doi: 10.1248/bpb.19.1241.

Abstract

Potent immunosuppressants, the dimeric sesquiterpene thioalkaloids, 6-hydroxythiobinupharidine (2), 6,6'-dihydroxythiobinupharidine (3), 6-hydroxythionuphlutine B (5) and 6'-hydroxythionuphlutine B (6), were isolated from a natural medicine, Nupharis Rhizoma, the rhizoma of Nuphar pumilum (TIMM.) DC., through bioassay-guided separation together with five quinolizidine alkaloids (8, 9, 10, 11, 12). Dimeric sesquiterpene thioalkaloids (2, 3, 5, 6) were found to significantly inhibit anti-sheep erythrocyte plaque forming cell formation in mice spleen cells at 10(-6) M concentration. At this concentration, 2, 5 and 6 were found to exhibit no cytotoxicity to mice spleen cells, and 3 also showed only a little cytotoxicity. In addition, the inhibitory activity of several Nuphar alkaloids, dimeric sesquiterpene thioalkaloids (1, 4, 7, 8), and monomeric sesquiterpene alkaloids (9, 10, 11, 12) on anti-sheep erythrocyte plaque forming cell formation was examined and some structural requirement of Nuphar alkaloid for immunosuppressive activity was determined.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Cyclosporine / pharmacology
  • Erythrocytes / immunology
  • Female
  • Hydrocortisone / pharmacology
  • Immunosuppressive Agents / isolation & purification*
  • Immunosuppressive Agents / pharmacology
  • Mice
  • Mice, Inbred C57BL
  • Plant Roots / chemistry
  • Plants, Medicinal / chemistry*
  • Quinolizines / isolation & purification*
  • Quinolizines / pharmacology
  • Sheep / immunology
  • Spiro Compounds / isolation & purification*
  • Spiro Compounds / pharmacology
  • Spleen / cytology
  • Spleen / immunology
  • Structure-Activity Relationship
  • Thiophenes / isolation & purification*
  • Thiophenes / pharmacology

Substances

  • Anti-Inflammatory Agents
  • Immunosuppressive Agents
  • Quinolizines
  • Spiro Compounds
  • Thiophenes
  • Cyclosporine
  • Hydrocortisone