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Combretastatins: An Overview of Structure, Probable Mechanisms of Action and Potential Applications.


ABSTRACT: Combretastatins are a class of closely related stilbenes (combretastatins A), dihydrostilbenes (combretastatins B), phenanthrenes (combretastatins C) and macrocyclic lactones (combretastatins D) found in the bark of Combretum caffrum (Eckl. & Zeyh.) Kuntze, commonly known as the South African bush willow. Some of the compounds in this series have been shown to be among the most potent antitubulin agents known. Due to their structural simplicity many analogs have also been synthesized. Combretastatin A4 phosphate is the most frequently tested compounds in preclinical and clinical trials. It is a water-soluble prodrug that the body can rapidly metabolize to combretastatin A4, which exhibits anti-tumor properties. In addition, in vitro and in vivo studies on combretastatins have determined that these compounds also have antioxidant, anti-inflammatory and antimicrobial effects. Nano-based formulations of natural or synthetic active agents such as combretastatin A4 phosphate exhibit several clear advantages, including improved low water solubility, prolonged circulation, drug targeting properties, enhanced efficiency, as well as fewer side effects. In this review, a synopsis of the recent literature exploring the combretastatins, their potential effects and nanoformulations as lead compounds in clinical applications is provided.

SUBMITTER: Karatoprak GS 

PROVIDER: S-EPMC7321081 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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Combretastatins: An Overview of Structure, Probable Mechanisms of Action and Potential Applications.

Karatoprak Gökçe Şeker GŞ   Küpeli Akkol Esra E   Genç Yasin Y   Bardakci Hilal H   Yücel Çiğdem Ç   Sobarzo-Sánchez Eduardo E  

Molecules (Basel, Switzerland) 20200531 11


Combretastatins are a class of closely related stilbenes (combretastatins A), dihydrostilbenes (combretastatins B), phenanthrenes (combretastatins C) and macrocyclic lactones (combretastatins D) found in the bark of <i>Combretum caffrum</i> (Eckl. & Zeyh.) Kuntze, commonly known as the South African bush willow. Some of the compounds in this series have been shown to be among the most potent antitubulin agents known. Due to their structural simplicity many analogs have also been synthesized. Com  ...[more]

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