Dear Colleagues,

For thousands of years, plants have provided therapeutic solutions for numerous pathologies initially in the form of raw extracts and then as source of active compounds which served as a starting point for the synthesis of new drugs. A significant share of existing small-molecule drugs, including certain anticancer medications, are directly derived or inspired by phytochemicals. Natural compounds may offer advantages over synthetic ones in terms of fewer and less severe side effects as well as reduced drug resistance. However, despite global efforts, the in vitro studies conducted on several phytocompounds have often resulted in unreliable information which could not support their clinical use under the current medical regulations. Therefore, rigorous scientific research must continue in order to assess the efficacy and safety of natural compounds as pharmacologically active agents.

This Special Issue is dedicated to the investigation of molecular mechanisms involved in the anticancer activity of pentacyclic triterpenes and their semisynthetic derivatives based on in vitro and in vivo studies. Pentacyclic triterpenes are secondary plant metabolites found in a wide variety of species with documented anti-inflammatory, anticancer, analgesic, and immunomodulatory effects. The chemical scaffold of pentacyclic triterpenes provides a promising platform for the synthesis of semisynthetic derivatives with improved pharmacokinetics and bioavailability.

Pentacyclic triterpenoids are able to act on multiple molecular targets and to regulate several cell proliferation pathways involved in the process of uncontrolled cell proliferation. In vitro and in vivo studies have shown that triterpenoids inhibit DNA polymerase, interfere with angiogenesis and cell differentiation, induce cell death through apoptosis, inhibit nuclear factor-κB (NF-κB) activation and signal transduction, and induce mitochondrial dysfunction, resulting in overall inhibition of proliferation and metastasis. Trit­erpenoid acids, monoalcohols, and diols exert antioxidant effects by reducing the production of free reactive oxidative species (ROS). Despite the identification of numerous molecular targets, detailed investigations are still needed in order to clarify the anticancer potential of this class of phytocompounds. In addition, given the sometimes contradictory results between in vitro and in vivo studies, more in vivo assessments are required to support in vitro findings. Systematic toxicological studies that are scientifically designed according to international guidelines are needed to accelerate the pharmaceutical development of triterpenoid compounds.

This Special Issue will collect a selection of recent research topics and current review articles related to the molecular mechanisms involved in the anticancer effects of pentacyclic triterpenoids in order to update the current knowledge in this field. Original papers, up-to-date review articles, short communications, and commentaries are all welcome.

Prof. Dr. Codruta Soica
Guest Editor

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• pentacyclic triterpenes
• in vitro studies
• in vivo studies
• molecular mechanisms
• semisynthetic derivatives
• molecular targets
• proliferation and metastasis inhibition