Abstract:
:We have derivatized Momordica saponins (MS) I and II through their coupling at C3 glucuronic acid site with dodecylamine. The derivatives show significantly different immunostimulant activity profiles from their respective natural parent saponins. In particular, adjuvant VSA-1 (5), the derivative of MS I, potentiates a significantly higher IgG2a responose than the corresponding natural product. Its IgG1 and IgG2a production is similar to that of GPI-0100, indicating a potential mixed and antigen-specific Th1/Th2 immune response, which is different from the Th2 immunity induced by the natural saponin MS I. In addition, toxicity evaluations show that adjuvant VSA-1 (5) is much less toxic than the widely used natural saponin mixture Quil A. These results prove that derivatizing Momordica saponins can be a viable way for easy access to structurally defined saponin immunostimulants with favorable adjvuant activity and low toxicity.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Wang P,Ding X,Kim H,Škalamera Đ,Michalek SM,Zhang Pdoi
10.1021/acs.jmedchem.9b01511subject
Has Abstractpub_date
2019-11-14 00:00:00pages
9976-9982issue
21eissn
0022-2623issn
1520-4804journal_volume
62pub_type
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