Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 1, Pages 51-55Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.11.016
Keywords
Ginsenoside Compound K; Asthma; Glycosylation; Saponin; IgE
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Funding
- National Major Scientific and Technological Special Project of China [2018ZX09711002-006-008]
- National Natural Science Foundation of China [81773576]
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Ginsenoside Compound K (CK) showed potent activity against IgE for the treatment of asthma. A series of CK analogues were then synthesized by straightforward procedures. The in vivo anti-IgE activity evaluations using the OVA-induced asthmatic mouse model revealed preliminary SARs of the CK analogues, which showed that the sugar type, modifications on A-ring and the C20 side chain of CK all affected much on the activities. Primary SARs optimization led to the discovery of compounds T1, T2, T3, T8 and T12, which displayed superior or comparable anti-asthmatic effects (IgE value = 1237.11 +/- 106.28, 975.82 +/- 160.32, 1136.96 +/- 121.85, 1191.08 +/- 107.59 and 1258.27 +/- 148.70 ng/mL, respectively) in comparison with CK (1501.85 +/- 184.66 ng/mL). These potent compounds could serve as leads for further development.
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