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

Identification of Antimotilins, Novel Inhibitors of Helicobacter pylori Flagellar Motility That Inhibit Stomach Colonization in a Mouse Model

“…For further studies, we selected one small molecule, named Active1 (β-lapachone, a 2,4-naphthoquinone) long-known to have antibacterial effects on a variety of species ( 44 , 46 ), but not yet characterized to be active against H. pylori . β-lapachone derivatives, due to their cell-killing activity, are currently being further developed as anticancer agents ( 45 , 47 , 72 ) and were also strongly active against H. pylori in our hands. Furthermore, we selected the phenyl-pyrazolone small compound Active2, which represents a novel class of anti-virulence, anti-motility compounds with a yet unknown target, for further studies of its activities against H. pylori .…”

Beta-Lapachone Attenuates BMSC-Mediated Neuroblastoma Malignant Transformation by Inhibiting Gal-3/Gal-3BP/IL6 Axis

“…LPC is a pleiotropic natural product, which has attracted much attention because of its strong antitumor activity in a variety of tumors ( Gomes et al, 2021 ; Gong et al, 2021 ). LPC has limited therapeutic use because of its narrow treatment window, poor water solubility and high toxicity ( Gomes et al, 2021 ).…”

“…Natural products extracted from plants, animals or microorganisms have played an important role in the struggle against diseases for centuries ( Wang et al, 2020 ). Beta-Lapachone (ARQ-501, LPC), an ortho -naphthoquinone natural product isolated from the lapacho tree ( Tabebuia avellanedae ), has attracted extensive attention due to its multiple pharmacological activities of anti-tumor, anti-bacterial, anti-malarial, ant-viral and anti-inflammatory activities ( Guiraud et al, 1994 ; Gupta et al, 2002 ; Mokarizadeh et al, 2020 ; Gong et al, 2021 ). As the activatable substrate of NQO1, LPC can produce a large amount of reactive oxygen species after being reduced, which exert powerful anti-tumor activity in many cancers, such as lung cancer, colon cancer and pancreatic cancer ( Kim et al, 2005 ; Bey et al, 2007 ; Gong et al, 2021 ).…”

“…Beta-Lapachone (ARQ-501, LPC), an ortho -naphthoquinone natural product isolated from the lapacho tree ( Tabebuia avellanedae ), has attracted extensive attention due to its multiple pharmacological activities of anti-tumor, anti-bacterial, anti-malarial, ant-viral and anti-inflammatory activities ( Guiraud et al, 1994 ; Gupta et al, 2002 ; Mokarizadeh et al, 2020 ; Gong et al, 2021 ). As the activatable substrate of NQO1, LPC can produce a large amount of reactive oxygen species after being reduced, which exert powerful anti-tumor activity in many cancers, such as lung cancer, colon cancer and pancreatic cancer ( Kim et al, 2005 ; Bey et al, 2007 ; Gong et al, 2021 ). In addition, LPC also exhibits anti-inflammatory effects in many inflammatory diseases such as acute pancreatitis, Alzheimer’s disease, multiple sclerosis, arthritis ( Shen et al, 2017 ; Mokarizadeh et al, 2020 ).…”

High‐Contrast Fluorescence Diagnosis of Cancer Cells/Tissues Based on β‐Lapachone‐Triggered ROS Amplification Specific in Cancer Cells

“…Our design strategy originated from the understanding of the action mechanism of b-Lap,anovel anticancer therapeutic agent (in clinical form, ARQ761), which induces extensive oxidative DNAl esions and tumor-selective cell death by rapidly generating al arge amount of intracellular ROSv ia af utile redox cycling between it and its hydroquinone form under the catalysis of NAD(P)H:quinone oxidoreductase-1( NQO1, ac ytosolic two-electron oxidoreductase) (Scheme 1A). [49][50][51][52] Since NQO1 is overexpressed in aw ide spectrum of human tumors,i ncluding pancreas,c olon, breast, lung,l iver, stomach, kidney,h ead/neck, and ovaries cancers, at levels 5-200 fold greater than in normal tissues, [53] b-Lap may be regarded to be ag eneric ROSa mplifier for cancer cells/tissues over normal ones.W ee nvisioned that using b-Lap to selectively amplify ROSl evel in cancer cells over normal cells would greatly improve the efficacyoffluorescent ROSprobes in distinguishing between cancer cells/tissues and normal ones (Scheme 1B).…”