Plumbagin and Its Role in Chronic Diseases

Panichayupakaranant, Pharkphoom; Ahmad, Iftekhar

doi:10.1007/978-3-319-41342-6_10

Cited by 41 publications

(29 citation statements)

References 66 publications

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“…Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone), a natural-derived naphthoquinone, isolated from the roots of Plumbaginaceae plants (Checker et al, 2018), has been reported to have anticancer effect in various types of cancer, including breast, lung, prostate, cervical, liver, colon, brain, and melanoma cancers (Panichayupakaranant & Ahmad, 2016;Rajalakshmi et al, 2018;Checker et al, 2018). These anticancer effects are mediated through the modulation of cellular redox balance and reduction of glutathione levels, as well as through the activation of apoptotic pathways in cancer cells (Checker et al, 2018).…”

Section: Introductionmentioning

confidence: 99%

Transferrin‐bearing liposomes entrapping plumbagin for targeted cancer therapy

Sakpakdeejaroen

Somani

Laskar

et al. 2019

J of Interdiscip Nanomed

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The therapeutic potential of plumbagin, a naphthoquinone extracted from the officinal leadwort with anticancer properties, is hampered by its failure to specifically reach tumours at a therapeutic concentration after intravenous administration, without secondary effects on normal tissues. Its use in clinic is further limited by its poor aqueous solubility, its spontaneous sublimation, and its rapid elimination in vivo . We hypothesize that the entrapment of plumbagin within liposomes grafted with transferrin, whose receptors are overexpressed on many cancer cells, could result in a selective delivery to tumours after intravenous administration. The objectives of this study were therefore to prepare and characterize transferrin‐targeted liposomes entrapping plumbagin and to evaluate their therapeutic efficacy in vitro and in vivo . The entrapment of plumbagin in transferrin‐bearing liposomes led to an increase in plumbagin uptake by cancer cells and improved antiproliferative efficacy and apoptosis activity in B16‐F10, A431, and T98G cell lines compared with that observed with the drug solution. In vivo, the intravenous injection of transferrin‐bearing liposomes entrapping plumbagin led to tumour suppression for 10% of B16‐F10 tumours and tumour regression for a further 10% of the tumours. By contrast, all the tumours treated with plumbagin solution or left untreated were progressive. The animals did not show any signs of toxicity. Transferrin‐bearing liposomes entrapping plumbagin are therefore highly promising therapeutic systems that should be further optimized as a therapeutic tool for cancer treatment.

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Section: Introductionmentioning

confidence: 99%

Transferrin‐bearing liposomes entrapping plumbagin for targeted cancer therapy

Sakpakdeejaroen

Somani

Laskar

et al. 2019

J of Interdiscip Nanomed

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“…Vancomycin-loaded PLGA core-shell nanoparticles have been found to reach complete release within 24 h 14 . For treating chronic diseases such as diabetes, long-term drug delivery, in the range from weeks to months or even longer, is important for patient compliance 1 , 15 , 16 . The relatively fast release rates of polymer nanoparticles are not suitable for long-term drug delivery applications.…”

Section: Introductionmentioning

confidence: 99%

Effects of Compositional Tailoring on Drug Delivery Behaviours of Silica Xerogel/Polymer Core-shell Composite Nanoparticles

Huang

Tsui

Tang

et al. 2018

Sci Rep

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Conventional core-shell polymer nanoparticles usually exhibit a rapid release rate with their release kinetics mainly adjusted through changing composition of the polymer shells, limiting their applications for prolonged drug delivery. As a solution to these problems, silica xerogel/polymer core-shell-structured composite nanoparticles have been proposed. Different with our previous work centring on studying process variables, we here focused on investigating the effects of key compositional variables on essential properties of the composite nanoparticles. The drug release profiles (in vitro) were well interpreted by the Baker and Lonsdale model on a predicted two-stage basis. The first stage (<1 day) was well controlled from 18.6% to 45.9%; the second stage (1–14 days) was tailored in a range from 28.7 to 58.2% by changing the composition of the silica xerogel cores and polymeric shells. A substantial achievement was reducing the release rate by more than 40 times compared with that of conventional polymer nanoparticles by virtue of the silica xerogel cores. A semi-empirical model was also established in the first attempt to describe the effects of polymer concentration and drug loading capacity on the size of the composite nanoparticles. All these results indicated that the composite nanoparticles are promising candidates for prolonged drug delivery applications.

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“…Plumbagin ( Figure 1A) is a naturally occurring 1,4-naphthoquinone and analogue of vitamin K3 isolated from plants of the Plumbaginaceae, Droseraceae, and Ebenaceae families. [1,2] Purified plumbagin inhibits the proliferation of various types of cancer cells, as reviewed extensively in, [3,4] therefore it is considered a valid oncology drug candidate. In vivo studies have shown that it reduces primary tumor burden across cancer types as measured by tumor growth rate as well as tumor weight and volume.…”

Section: Introductionmentioning

confidence: 99%

Plumbagin‐Serum Albumin Interaction: Spectral, Electrochemical, Structure‐Binding Analysis, Antiproliferative and Cell Signaling Aspects with Implications for Anticancer Therapy

et al. 2020

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Plumbagin (5‐hydroxy‐2‐methyl‐1,4‐naphthoquinone) is a small molecule with potent anticancer activity. Like other 1,4‐naphthoquinones, it exhibits electrophilic reactivity towards biological nucleophiles. We demonstrate that plumbagin and structurally related 1,4‐naphthoquinones with at least one unsubstituted quinoid carbon (C2 or C3) bind to albumin, an ubiquitously present nucleophile, with minimum recovery of free drug. Extraction recovery of plumbagin from albumin in solution showed one‐phase exponential decline with a half‐live of 9.3 min at 10 μmol/L. In the presence of albumin, plumbagin exhibited instant changes in UV/Vis absorption bands. Electrochemical analysis using cyclic voltammetry showed a decrease in redox peak currents over time until electro‐inactivity, thus suggesting the formation of a supramolecular adduct inaccessible for electron transfer. The adduct inhibited cell growth and caused cell‐cycle arrest of prostate cancer cells, in part by decreasing levels of the cell‐cycle regulator RBBP. The conjugate displayed similar cellular effects to those described for plumbagin, such as decreased levels of androgen receptor and protein kinase C epsilon. The effect of plumbagin‐albumin on cancer cells was species‐specific, suggesting a receptor‐mediated mechanism. Furthermore, it was blocked by cathepsin inhibitor pepstatin A, indicating that lysosomal degradation is involved in the processing of plumbagin‐albumin adduct. The spontaneously formed adduct of plumbagin with serum albumin is likely to mediate the biological activities of plumbagin in vivo and to fundamentally influence its pharmacodynamics.

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Plumbagin and Its Role in Chronic Diseases

Cited by 41 publications

References 66 publications

Transferrin‐bearing liposomes entrapping plumbagin for targeted cancer therapy

Transferrin‐bearing liposomes entrapping plumbagin for targeted cancer therapy

Effects of Compositional Tailoring on Drug Delivery Behaviours of Silica Xerogel/Polymer Core-shell Composite Nanoparticles

Plumbagin‐Serum Albumin Interaction: Spectral, Electrochemical, Structure‐Binding Analysis, Antiproliferative and Cell Signaling Aspects with Implications for Anticancer Therapy

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