Abstract
Oridonin (ORI), an ent-kaurene tetracyclic diterpenoid compound, is isolated from Chinese herb Rabdosia rubescens with various biological and pharmacological activities including anti-tumor, anti-microbial and anti-inflammatory effects. However, the clinical application of ORI is limited due to its low solubility and poor bioavailability. In order to overcome these shortcomings, many strategies have been explored such as structural modification, new dosage form, etc. This review provides a detailed discussion on the research progress to increase the solubility and bioavailability of ORI.
Highlights
Oridonin (ORI), an ent-kaurene tetracyclic diterpenoid compound, is isolated from Chinese herb Rabdosia rubescens with various biological and pharmacological activities including anti-tumor, anti-microbial and anti-inflammatory effects
On the D-ring is the essential structure of the anti-cancer activity, which can be impaired by ring splitting or methylene saturation [20]
The anti-cancer activity can be enhanced by the esterification of 14-hydroxyl group whose nucleophilic property is amplified by the parallel 7-hydroxyl group; the antitumor activity decreases without the 7-hydroxyl group [21]
Summary
Oridonin (ORI), an ent-kaurene tetracyclic diterpenoid compound, is isolated from Chinese herb Rabdosia rubescens with various biological and pharmacological activities including anti-tumor, anti-microbial and anti-inflammatory effects. The clinical application of ORI is limited due to its low solubility and poor bioavailability. The 2015 edition of the Chinese Pharmacopoeia records its efficacy of clearing away heat and detoxifying, promoting blood circulation and relieving pain. It is commonly used in the treatment of acute and chronic pharyngitis, bronchitis, tonsillitis and insect bites [1,2]. Despite the wide spectra of pharmacological activities, the application of ORI is limited due to Reducing colonic EC cell hyperplasia and 5-HT. The rapid plasma clearance of ORI, the first-pass effect after oral administration, and the lack of proper dosage forms for intravenous injection hinder
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