Abstract

Plumbagin (PLB), a natural naphthoquinone constituent isolated from the roots of the medicinal plant Plumbago zeylanica L., exhibited anticancer activity against a variety of cancer cell lines including breast cancer, hepatoma, leukemia, melanoma, prostate cancer, brain tumor, tongue squamous cell carcinoma, esophageal cancer, oral squamous cell carcinoma, lung cancer, kidney adenocarcinoma, cholangiocarcinoma, gastric cancer, lymphocyte carcinoma, osteosarcoma, and canine cancer. PLB played anticancer activity via many molecular mechanisms, such as targeting apoptosis, autophagy pathway, cell cycle arrest, antiangiogenesis pathway, anti-invasion, and antimetastasis pathway. Among these signaling pathways, the key regulatory genes regulated by PLB were NF-kβ, STAT3, and AKT. PLB also acted as a potent inducer of reactive oxygen species (ROS), suppressor of cellular glutathione, and novel proteasome inhibitor, causing DNA double-strand break by oxidative DNA base damage. This review comprehensively summarizes the anticancer activity and mechanism of PLB.

Highlights

  • Plumbagin (5-hydroxy-2-methyl-1,4-napthoquinone, PLB, Figure 1) is a naturally occurring naphthoquinone isolated from the roots of the medicinal plant Plumbago zeylanica L

  • We mainly report the recent advances in research on the anticancer activity of PLB and summarized the possible mechanism of PLB, which will provide theoretical references for its clinical application

  • Due to the side effects of cancer treatment and drug resistance, cancer treatment is in urgent need of a multitarget treatment

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Summary

Introduction

Plumbagin (5-hydroxy-2-methyl-1,4-napthoquinone, PLB, Figure 1) is a naturally occurring naphthoquinone isolated from the roots of the medicinal plant Plumbago zeylanica L. As a vitamin K3 analog and a prooxidant, PLB has been reported to possess diverse biological activities, such as anti-inflammatory, anticancer, antidiabetic, antioxidant, antibacterial, antifungal, anti-atherosclerosis, and analgesic activities [1,2,3,4,5,6]. The anticancer activity and mechanism of PLB have become a research hotspot and increasing attention has been paid by scholars. Some scholars had reviewed the advances in tumor suppression and mechanism by PLB in year 2014 [7] and the cytotoxic potential and pharmaceutical relevance towards cancer therapy [8]. We mainly report the recent advances in research on the anticancer activity of PLB and summarized the possible mechanism of PLB, which will provide theoretical references for its clinical application

Antitumor Activity
Conclusions and Future Perspective
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