Quillaja saponaria extract is rich in aldehyde-containing triterpene saponins and have shown to possess immune stimulating activities. One of the most active saponin QS-21 is being used as adjuvant in several vaccine preparations for clinical trial and shown to be highly potent. However their commercial use has been limited, due to low stability in solution and high toxicity. Several synthetic analogs have been developed such as GPI-0100 and semisynthetic QS21 analogs. GPI-0100 is prepared by replacing hydrolytically unstable ester side chain with lipophilic dodecylamide linked by hydrolytically stable amide bonds on the glucuronic acid residue. Herein, the progress on semi-synthetic saponin analogs, their design, synthesis, purification, characterization, and structure/activity relationships will be discussed. These saponin analogs have less toxicity, greater stability, and excellent immune stimulating activity. Immunological results showed these adjuvants generate a Th1-type (or mixed Th1/Th2-type) immune response and cell-mediated immunity (CMI), including antigen-specific T cell proliferation and generation of cytotoxic T lymphocytes (CTLs).This presentation is dedicated to late Prof. David Gin

Triterpene saponins and its synthetic analogs as vaccine adjuvants for humoral and cellular immune activities

243rd National Meeting (2012)

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