Title:Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review
Volume: 21
Issue: 12
Author(s): Justyna Żwawiak*, Anna Pawełczyk, Dorota Olender and Lucjusz Zaprutko
Affiliation:
- Department of Organic Chemistry, Pharmaceutical Faculty, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan,Poland
Keywords:
Triterpenes, oleanolic acid, betulinic acid, codrugs, conjugates, anticancer activity.
Abstract: Triterpenes are a wide and important group of compounds that have several promising
pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or
anticancer activities. Such potent substances can be successfully incorporated in more complex chemical
systems e.g. codrugs or pro-drugs that have a better pharmacological profile. The codrug is connected
with a drug formation pathway to chemically cohere at least two drug molecules to improve
positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to
generate effective compounds previously used as substrates. This article presents an overview of
codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to
their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid
codrugs are characterized by a wide range of biological activities. However, most of them have anticancer
potency.