Anticancer Effects and Mechanisms of Action of Plumbagin: Review of Research Advances

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.

Plumbagin, a Biomolecule with (Anti)Osteoclastic Properties

“…The plant-derived naphthoquinone plumbagin is a bioactive compound that was originally isolated from the roots of the Plumbago genus [ 24 ]. Because plumbagin is an effective mediator of ROS production in a variety of different cells, the focus of research has been on its anti-cancer properties [ 10 ]. The first report that addressed the modulatory abilities of plumbagin on macrophages was published in 1995 and suggested a potentiation of bactericidal activity [ 25 ].…”

“…Like other naphthoquinones, plumbagin activates cellular signalling through redox reactions, the inhibition of cellular phosphatases and through direct protein alkylation [ 8 ]. In cancer cells, plumbagin mainly acts through the induction of apoptosis via the upregulation of ROS [ 9 , 10 ] and cell cycle arrest through the induction of DNA strand breaks [ 7 , 11 ]. This apoptotic function is supported by other molecular mechanisms that ultimately inhibit tumour growth and metastasis.…”

Plumbagin Elicits Cell-Specific Cytotoxic Effects and Metabolic Responses in Melanoma Cells

“…Several natural phytochemical compounds with high anticancer potential are promising drugs in cancer therapy, including the treatment of melanoma [ 5 , 6 , 7 ]. Plumbagin (PLB), a naphthoquinone derivative mainly extracted from the plant, exhibits anticancer potential in different cancers, including inhibition of invasion and metastasis, induction of autophagy and apoptosis, and alteration of the cell cycle [ 8 , 9 , 10 , 11 ]. PLB is also considered a potent suppressor of cellular glutathione and an inducer of ROS [ 9 , 12 ].…”

“…Plumbagin (PLB), a naphthoquinone derivative mainly extracted from the plant, exhibits anticancer potential in different cancers, including inhibition of invasion and metastasis, induction of autophagy and apoptosis, and alteration of the cell cycle [ 8 , 9 , 10 , 11 ]. PLB is also considered a potent suppressor of cellular glutathione and an inducer of ROS [ 9 , 12 ]. Furthermore, PLB shows an anticancer effect on breast cancer depending on NQ01 activity [ 13 ], an inhibiting effect on mitochondrial electron transport, and an Nrf-2-mediated antioxidative response in several cancer cell lines [ 14 ].…”

Plumbagin, a Potent Naphthoquinone from Nepenthes Plants with Growth Inhibiting and Larvicidal Activities

“…NQ derivatives are also described for tissues of various Nepenthes species including the pitchers [ 12 , 15 , 16 , 17 ]. In particular, plumbagin is of broad pharmaceutical interest because it is a candidate that may be used in therapies against various cancers or chronic diseases [ 18 , 19 , 20 , 21 ]. In addition to NQ, carotenoids, flavonoids, sterols, and triterpenes are described for Nepenthes leaves [ 1 , 22 , 23 ].…”