Lewis‐X‐Containing Triterpenoid Saponins Inhibit DC‐SIGN‐ and L‐SIGN‐Mediated Transfer of HIV‐1 Infection
Bibliographic record
Abstract
Abstract Blocking dendritic cell‐specific intercellular adhesion molecule‐3‐grabbing nonintegrin (DC‐SIGN)‐ and liver/lymph node‐specific intercellular adhesion molecule‐3‐grabbing integrin (L‐SIGN)‐mediated human immunodeficiency virus 1 (HIV‐1) attachment to immune cells represents a promising strategy for developing antiretroviral agents effective during the early stages of sexual transmission. Although mannose‐ and fucose‐based ligands have received considerable attention, Lewis‐based inhibitors remain relatively underexplored. In this study, we report the first synthesis of Lewis‐X‐containing triterpenoid saponins featuring betulinic acid and echinocystic acid as aglycones. These saponins were stereoselectively and efficiently synthesized in six linear steps using a convergent approach that leveraged thioglycoside and trichloroacetimidate glycosylation chemistries. Notably, our findings demonstrate that these Lewis‐X‐containing triterpenoid saponins are among the most potent monovalent inhibitors reported to date of DC‐SIGN‐ and L‐SIGN‐mediated transfer of HIV‐1 infection to CD4‐positive cells, with IC50 values in the low micromolar range (21–50 µM). This work lays a valuable foundation for the development of saponin‐based antiviral agents targeting immune cells.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.001 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".