A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials

beta-Lapachone (beta-lap, 1), an ortho-naphthoquinone natural product isolated from the lapacho tree (Tabebuia avellanedae) in many regions of South America, has received extensive attention due to various pharmacological activities, such as antitumor, anti-Trypanosoma cruzi, anti-Mycobacterium tuberculosis, antibacterial, and antimalarial activities. Related mechanisms of beta-lap have been widely investigated for a full understanding of its therapeutic potentials. Numerous derivatives of beta-lap have been reported with aims to generate new chemical entities, improve the corresponding biological potency, and overcome disadvantages of its physical and chemical properties and safety profiles. This review will give insight into the pharmacological mechanisms of beta-lap and provide a comprehensive understanding of its structural modifications with regard to different therapeutic potentials. The available clinical trials related to beta-lap and its derivatives are also summarized. (C) 2020 Elsevier Masson SAS. All rights reserved.

Automated summary

Beta-Lapachone, a natural product from South America, has diverse pharmacological activities and its derivatives are studied for enhanced potency and overcoming limitations.Clinical trials related to beta-lap and its derivatives are summarized.