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Cucurbitacins, cell adhesion inhibitors from Conobea scoparioides
L L Musza1, P Speight, S McElhiney
1Sterling Winthrop Pharmaceuticals Research Division, Malvern, Pennsylvania 19355.
Journal of Natural Products
|November 1, 1994
Summary
Researchers discovered cucurbitacin E from Conobea scoparioides inhibits CD18-mediated cell adhesion. This natural product shows potential for therapeutic development by targeting cell adhesion mechanisms.
Area of Science:
- Natural Product Chemistry
- Immunology
- Pharmacology
Background:
- CD18-mediated cell adhesion plays a crucial role in inflammatory processes.
- Natural products are a rich source of potential therapeutic agents.
- Previous studies have identified various biological activities for cucurbitacins.
Purpose of the Study:
- To screen natural products for antagonists of CD18-mediated cell adhesion.
- To isolate and identify the active compound from Conobea scoparioides.
- To investigate the potential of cucurbitacin E in inhibiting cell adhesion.
Main Methods:
- Screening of natural product extracts for bioactivity.
- Bioassay-guided fractionation to isolate the active compound.
- Spectroscopic methods for compound identification (e.g., NMR, Mass Spectrometry).
- Assays to measure CD18-mediated cell adhesion inhibition.
Main Results:
- An extract from Conobea scoparioides stems and leaves exhibited inhibitory activity against CD18-mediated cell adhesion.
- Cucurbitacin E was isolated and identified as the active compound.
- This is the first report of cucurbitacin E inhibiting cell adhesion.
- Related cucurbitacin analogues showed varying potencies, highlighting key structural features for activity.
Conclusions:
- Cucurbitacin E is a novel inhibitor of CD18-mediated cell adhesion.
- The study identifies a new biological activity for cucurbitacins.
- Structural analysis suggests specific features of cucurbitacin E are critical for its cell adhesion inhibitory effects.
- Conobea scoparioides is a potential source for developing new anti-adhesion therapies.
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