1,721,295 research outputs found
Oleanane derivatives for pharmaceutical use: a patent review (2000-2016)
No full textIntroduction: Oleanolic acid has been considered a good start molecule for synthetic exploitation. Thus hundreds of oleanane triterpenoids have been synthesized and patented. Also many oleanane saponins have been patented for their biological activities and possible pharmaceutical use. Areas covered: Patents reporting the biological activities of oleanane derivatives and saponins with oleanane-type aglycones were examined. Among the synthesized oleanane derivatives, the most promising seem to be 2-cyano-3,12-dioxoolean-1,9(11)-dien-28-oic acid derivatives which interfere with many pathways involved in inflammation, oxidative stress and cell proliferation. Regarding oleanane-type saponins, several patents claiming their antiproliferative activity or their possible use as adjuvants in vaccines, were reported. Expert opinion: Despite the great number of synthesized oleanane triterpenoids, only CDDO-Me entered clinical development as a possible drug for the treatment of chronic kidney disease (CKD) but a phase 3 clinical trial was terminated due to heart-related adverse effects. Further phase 2 clinical trials of CDDO-Me are in progress for the treatment of CKD and PAH (pulmonary arterial hypertension) patients without heart-related risk factors. Additional investigations leading to compounds with an improved activity/toxicity profile along with well-designed preclinical and clinical trials are needed. Regarding oleanane-type saponins, the real perspective seems to be as adjuvants in vaccines
Ruscus Genus: A Rich Source of Bioactive Steroidal Saponins
No full textThe genus Ruscus (Asparagaceae family) is native to the Mediterranean, Southern and Western Europe and is represented by perennial, rhizomatous, and evergreen shrubs. Among the approximately seven species spread throughout Europe up to Iran, Ruscus aculeatus L. (butcherʼs broom) is the most widely distributed and appreciated. This review provides an overview of the traditional use of Ruscus spp., the current knowledge of the chemistry of this genus, and the pharmacological studies carried out on Ruscus spp. extracts. The underground parts of Ruscus plants are a source of steroidal saponins that can be classified into two structural classes: the hexacyclic spirostanol saponins and the pentacyclic furostanol saponins. The main aglycones are ruscogenin and neoruscogenin. From the pharmacological point of view, the most studied Ruscus species is undoubtedly R. aculeatus, a very ancient phlebotherapeutic agent. Pharmacological investigations since the discovery of the vasoconstrictive and venotonic properties of ruscogenin and neoruscogenin in the underground parts of R. aculeatus are discussed. Preparations based on Ruscus species are currently used for the treatment of chronic venous insufficiency, varicose veins, haemorrhoids, and orthostatic hypotension. Finally, analytical techniques for the quality control of R. aculeatus extracts are reported
- …
