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Oleanane derivatives for pharmaceutical use: a patent review (2000-2016).
Milena Masullo1, Cosimo Pizza1, Sonia Piacente1
1a Dipartimento di Farmacia , Università degli Studi di Salerno , Fisciano , Italy.
Oleanane triterpenoids show promise in treating inflammation and cancer, but clinical trials revealed safety concerns. Oleanane saponins may be valuable as vaccine adjuvants.
Area of Science:
- Natural Product Chemistry
- Medicinal Chemistry
- Pharmacology
Background:
- Oleanolic acid serves as a versatile starting material for synthesizing numerous oleanane triterpenoids.
- Patents highlight the biological activities and pharmaceutical potential of synthesized oleanane derivatives and oleanane-type saponins.
Purpose of the Study:
- To review patents on the biological activities of oleanane derivatives and saponins.
- To assess the therapeutic potential and challenges of these compounds in drug development.
Main Methods:
- Examination of patent literature concerning oleanane derivatives and saponins.
- Analysis of reported biological activities, including anti-inflammatory, anti-proliferative, and adjuvant properties.
Main Results:
- 2-cyano-3,12-dioxoolean-1,9(11)-dien-28-oic acid derivatives show potential in modulating inflammation, oxidative stress, and cell proliferation.
- Oleanane-type saponins are patented for antiproliferative effects and as vaccine adjuvants.
- CDDO-Me, an oleanane derivative, faced clinical trial termination due to adverse effects, though further trials are ongoing.
Conclusions:
- Further research is needed to develop oleanane derivatives with improved activity and safety profiles for therapeutic use.
- Oleanane-type saponins hold significant promise as adjuvants in vaccine formulations.
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