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

β-Lapachone (β-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 tuberculos...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2021-01, Vol.210, p.112962-112962, Article 112962
Main Authors: Gong, Qijie, Hu, Jiabao, Wang, Pengfei, Li, Xiang, Zhang, Xiaojin
Format: Article
Language:English
Subjects:
Animals
Anti-Infective Agents - chemistry
Anti-Infective Agents - pharmacology
Anti-Infective Agents - therapeutic use
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
Drug Discovery
Humans
Naphthoquinones - chemistry
Naphthoquinones - pharmacology
Naphthoquinones - therapeutic use
Natural product
Neoplasms - drug therapy
Quinone derivatives
Structural modification
Tabebuia - chemistry
β-Lapachone
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Summary:β-Lapachone (β-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 β-lap have been widely investigated for a full understanding of its therapeutic potentials. Numerous derivatives of β-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 β-lap and provide a comprehensive understanding of its structural modifications with regard to different therapeutic potentials. The available clinical trials related to β-lap and its derivatives are also summarized. [Display omitted] •Pharmacological mechanisms of β-lapachone are included.•Various modification strategies toward β-lapachone are provided.•Numerous derivatives of β-lapachone are reviewed and classified.•Derivatives undergoing clinical evaluation are summarized.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2020.112962