2. Academic Validation
  3. Structure-Activity Relationship Study of Momordica Saponin II Derivatives as Vaccine Adjuvants

Structure-Activity Relationship Study of Momordica Saponin II Derivatives as Vaccine Adjuvants

  • J Med Chem. 2022 Nov 10;65(21):14589-14598. doi: 10.1021/acs.jmedchem.2c01087.
Hyunjung Kim 1,  Di Bai 1,  Sadashib Ghosh 2,  Michael L Franks 2,  Xifeng Wang 3,  Cheng Yan 3,  Zheng Liu 3,  Ping Zhang 4,  Suzanne M Michalek 5,  Jianmei W Leavenworth 2 5 6,  Pengfei Wang 1 6
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Alabama at Birmingham, 901 14th Street South, Birmingham, Alabama 35294, United States.
  • 2 Department of Neurosurgery, University of Alabama at Birmingham, 901 14th Street South, Birmingham, Alabama 35294, United States.
  • 3 Department of Chemistry, Central China Normal University, 152 Luoyu Road, Wuhan, Hubei 430079, P. R. China.
  • 4 Department of Pediatric Dentistry, University of Alabama at Birmingham, 901 14th Street South, Birmingham, Alabama 35294, United States.
  • 5 Department of Microbiology, University of Alabama at Birmingham, 901 14th Street South, Birmingham, Alabama 35294, United States.
  • 6 The O'Neal Comprehensive Cancer Center, University of Alabama at Birmingham, 901 14th Street South, Birmingham, Alabama 35294, United States.
PMID: 36318612 DOI: 10.1021/acs.jmedchem.2c01087
Abstract

VSA-2 is a recently developed semisynthetic saponin immunostimulant. It is prepared by incorporating a terminal-functionalized side chain to the branched trisaccharide domain at the C3 position of Momordica saponin II (MS II) isolated from the seeds of perennial Momordica cochinchinensis Spreng. Direct comparison of VSA-2 and the clinically proven saponin Adjuvant QS-21 shows that VSA-2 is comparable to QS-21 in enhancing humoral and cellular immune responses. Structure-activity relationship studies show that structural changes in the side chain have a significant impact on saponins' Adjuvant activity. However, with the VSA-2 molecular framework intact, the new VSA-2 analogues with various substitution(s) at the terminal benzyl group of the side chain retain the ability of potentiating antigen-specific humoral and cellular responses.

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