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25 Results Found

  • Article
  • Open Access
3 Citations
3,711 Views
17 Pages

Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone

  • Hyeongmin Kim,
  • Chung-Lyol Lee,
  • Seohyun Lee,
  • Tae Jin Lee,
  • Iqra Haleem,
  • Younghong Lee,
  • Na Jung Hwang,
  • Kyusun Shim,
  • Dohyun Kim and
  • Jaehwi Lee

In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the...

  • Article
  • Open Access
9 Citations
3,038 Views
16 Pages

Antibacterial and Antibiofilm Activities of β-Lapachone by Modulating the Catalase Enzyme

  • Mushtaq Ahmad Mir,
  • Somaya Ahmed Altuhami,
  • Sukanta Mondal,
  • Nasreena Bashir,
  • Ayed A. Dera and
  • Mohammad A. Alfhili

Background: Bacterial infections constantly have a large impact on public health, because of increased rates of resistance and reduced frequency of development of novel antibiotics. The utility of conventional antibiotics for treating bacterial infec...

  • Article
  • Open Access
3 Citations
2,893 Views
14 Pages

Single-Cell Kinetic Modeling of β-Lapachone Metabolism in Head and Neck Squamous Cell Carcinoma

  • Andrew D. Raddatz,
  • Cristina M. Furdui,
  • Erik A. Bey and
  • Melissa L. Kemp

Head and neck squamous cell carcinoma (HNSCC) cells are highly heterogeneous in their metabolism and typically experience elevated reactive oxygen species (ROS) levels such as superoxide and hydrogen peroxide (H2O2) in the tumor microenvironment. Tum...

  • Article
  • Open Access
5 Citations
2,593 Views
19 Pages

Artemisia annua L. Polyphenols Enhance the Anticancer Effect of β-Lapachone in Oxaliplatin-Resistant HCT116 Colorectal Cancer Cells

  • Eun Joo Jung,
  • Hye Jung Kim,
  • Sung Chul Shin,
  • Gon Sup Kim,
  • Jin-Myung Jung,
  • Soon Chan Hong,
  • Choong Won Kim and
  • Won Sup Lee

15 December 2023

Recent studies suggest that the anticancer activity of β-lapachone (β-Lap) could be improved by different types of bioactive phytochemicals. The aim of this study was to elucidate how the anticancer effect of β-Lap is regulated by poly...

  • Article
  • Open Access
24 Citations
5,139 Views
15 Pages

30 November 2018

Cancer stem cells (CSCs) exhibit self-renewal activity and give rise to other cell types in tumors. Due to the infinite proliferative potential of CSCs, drugs targeting these cells are necessary to completely inhibit cancer development. The β-la...

  • Article
  • Open Access
6 Citations
3,278 Views
18 Pages

β-lapachone (β-Lap), a topoisomerase inhibitor, is a naturally occurring ortho-naphthoquinone phytochemical and is involved in drug resistance mechanisms. Oxaliplatin (OxPt) is a commonly used chemotherapeutic drug for metastatic colorectal...

  • Review
  • Open Access
56 Citations
8,171 Views
22 Pages

Anticancer Potential of Resveratrol, β-Lapachone and Their Analogues

  • Danielly C. Ferraz da Costa,
  • Luciana Pereira Rangel,
  • Mafalda Maria Duarte da Cunha Martins-Dinis,
  • Giulia Diniz da Silva Ferretti,
  • Vitor F. Ferreira and
  • Jerson L. Silva

18 February 2020

This review aims to explore the potential of resveratrol, a polyphenol stilbene, and beta-lapachone, a naphthoquinone, as well as their derivatives, in the development of new drug candidates for cancer. A brief history of these compounds is reviewed...

  • Article
  • Open Access
6 Citations
2,947 Views
11 Pages

Anticancer Potential and Safety Profile of β-Lapachone In Vitro

  • Karina Motta Melo Lima,
  • Luana França Calandrini de Azevedo,
  • Jorge Dores Rissino,
  • Valdicley Vieira Vale,
  • Erica Vanessa Souza Costa,
  • Maria Fani Dolabela,
  • Cleusa Yoshiko Nagamachi and
  • Julio Cesar Pieczarka

21 March 2024

Ipê is a plant of the Bignoniaceae family. Among the compounds extracted from this tree, lapachol is notable because its structural modification allows the production of β-lapachone, which has anticancer properties. The objective of this w...

  • Article
  • Open Access
12 Citations
3,939 Views
20 Pages

Synergistic Effect of β-Lapachone and Aminooxyacetic Acid on Central Metabolism in Breast Cancer

  • Mario C. Chang,
  • Rohit Mahar,
  • Marc A. McLeod,
  • Anthony G. Giacalone,
  • Xiumei Huang,
  • David A. Boothman and
  • Matthew E. Merritt

22 July 2022

The compound β-lapachone, a naturally derived naphthoquinone, has been utilized as a potent medicinal nutrient to improve health. Over the last twelve years, numerous reports have demonstrated distinct associations of β-lapachone and NAD(P)...

  • Article
  • Open Access
11 Citations
4,785 Views
18 Pages

Measuring NQO1 Bioactivation Using [2H7]Glucose

  • Rohit Mahar,
  • Mario C. Chang and
  • Matthew E. Merritt

19 August 2021

Treatment of cancers with β-lapachone causes NAD(P)H: quinone oxidoreductase 1 (NQO1) to generate an unstable hydroquinone that regenerates itself in a futile cycle while producing reactive oxygen species (ROS) in the form of superoxide and subsequen...

  • Review
  • Open Access
208 Citations
18,897 Views
21 Pages

The Trypanocidal Activity of Naphthoquinones: A Review

  • Antônio Ventura Pinto and
  • Solange Lisboa de Castro

10 November 2009

Naphthoquinones are compounds present in several families of higher plants. Their molecular structures confer redox properties, and they are involved in multiple biological oxidative processes. In folk medicine, especially among Indian populations, p...

  • Article
  • Open Access
22 Citations
7,766 Views
12 Pages

Controlled Release of Nor-β-lapachone by PLGA Microparticles: A Strategy for Improving Cytotoxicity against Prostate Cancer Cells

  • Marcilia P. Costa,
  • Anderson C. S. Feitosa,
  • Fátima C. E. Oliveira,
  • Bruno C. Cavalcanti,
  • Eufrânio N. Da Silva,
  • Gleiston G. Dias,
  • Francisco A. M. Sales,
  • Bruno L. Sousa,
  • Ito L. Barroso-Neto and
  • Cláudia Pessoa
  • + 5 authors

Prostate cancer is one of the most common malignant tumors in males and it has become a major worldwide public health problem. This study characterizes the encapsulation of Nor-β-lapachone (NβL) in poly(d,l-lactide-co-glycolide) (PLGA) microcapsules...

  • Article
  • Open Access
1,521 Views
20 Pages

New Insights into the Anticancer Effects and Toxicogenomic Safety of Two β-Lapachone Derivatives

  • José Rivaldo De Lima,
  • Alexandre José Da Silva Góes,
  • Elizabeth Fernanda De Oliveira Borba,
  • Meykson Alexandre da Silva,
  • Rodrigo Ribeiro Alves Caiana,
  • Maria do Desterro Rodrigues,
  • Mariza Severina De Lima Silva,
  • Cristiano Aparecido Chagas,
  • Blandine Baratte and
  • Thomas Robert
  • + 4 authors

Background/Objectives: β-Lapachone (β-lap) is an o-naphthoquinone with potent antitumor activity. However, its clinical application is hindered by poor solubility and toxicity. Thiosemicarbazone derivatives of β-lap (BV3 and BV5) have...

  • Article
  • Open Access
7 Citations
2,715 Views
13 Pages

Naphth[1,2-d]imidazoles Bioactive from β-Lapachone: Fluorescent Probes and Cytotoxic Agents to Cancer Cells

  • Victória Laysna dos Anjos Santos,
  • Arlan de Assis Gonsalves,
  • Délis Galvão Guimarães,
  • Sidney Silva Simplicio,
  • Helinando Pequeno de Oliveira,
  • Lara Polyana Silva Ramos,
  • Marcília Pinheiro da Costa,
  • Fátima de Cássia Evangelista de Oliveira,
  • Claudia Pessoa and
  • Cleônia Roberta Melo Araújo

28 March 2023

Theranostics combines therapeutic and imaging diagnostic techniques that are extremely dependent on the action of imaging agent, transporter of therapeutic molecules, and specific target ligand, in which fluorescent probes can act as diagnostic agent...

  • Review
  • Open Access
15 Citations
5,346 Views
37 Pages

Human NQO1 as a Selective Target for Anticancer Therapeutics and Tumor Imaging

  • A. E. M. Adnan Khan,
  • Viswanath Arutla and
  • Kalkunte S. Srivenugopal

29 July 2024

Human NAD(P)H-quinone oxidoreductase1 (HNQO1) is a two-electron reductase antioxidant enzyme whose expression is driven by the NRF2 transcription factor highly active in the prooxidant milieu found in human malignancies. The resulting abundance of NQ...

  • Article
  • Open Access
23 Citations
5,425 Views
10 Pages

2 September 2019

Background: Cancer cell sensitivity to drugs may be associated with disturbed antioxidant enzymes expression. We investigated mechanisms of resistance by using oxidative stress-resistant MCF-7 breast cancer cells (Resox cells). Since nicotinamide ade...

  • Article
  • Open Access
4 Citations
2,372 Views
17 Pages

25 May 2023

In recent years, the coupling of structurally and functionally controllable polymers with biologically active peptide materials to obtain polymer-peptide hybrids with excellent properties and biocompatibility has led to important research progress in...

  • Review
  • Open Access
1,392 Views
27 Pages

In Vitro Antiproliferative Activity in Plants of the Genus Tabebuia: A Systematic Review

  • Laura Mosquera-Morales,
  • Lina Marcela Orozco,
  • Luz Angela Veloza and
  • Juan Carlos Sepúlveda-Arias

The use of plant extracts and the compounds isolated from them for the treatment of cancer is an area of active research, given their therapeutic potential. This work focused on evaluating the literature related to the antiproliferative activity of e...

  • Proceeding Paper
  • Open Access
1,571 Views
9 Pages

Smart Design Nano-Hybrid Formulations by Machine Learning

  • Raquel de Melo Barbosa,
  • Fabio Fonseca de Oliveira,
  • Gabriel Bezerra Motta Câmara,
  • Tulio Flavio Accioly de Lima e Moura,
  • Fernanda Nervo Raffin and
  • Marcelo Augusto Costa Fernandes

1 December 2020

Nano-hybrid formulations combine organic and inorganic materials in self-assembled platforms for drug delivery. Laponite is a synthetic clay, biocompatible, and a guest of compounds. Poloxamines are amphiphilic four-armed compounds and have pH-sensit...

  • Feature Paper
  • Article
  • Open Access
2 Citations
3,606 Views
16 Pages

New Machine Learning Approach for the Optimization of Nano-Hybrid Formulations

  • Raquel de M. Barbosa,
  • Cleanne C. Lima,
  • Fabio F. de Oliveira,
  • Gabriel B. M. Câmara,
  • César Viseras,
  • Tulio F. A. de Lima e Moura,
  • Eliana B. Souto,
  • Patricia Severino,
  • Fernanda N. Raffin and
  • Marcelo A. C. Fernandes

Nano-hybrid systems are products of interactions between organic and inorganic materials designed and planned to develop drug delivery platforms that can be self-assembled. Poloxamine, commercially available as Tetronic®, is formed by blocks of c...

  • Article
  • Open Access
1 Citations
2,410 Views
17 Pages

Augmented Concentration of Isopentyl-Deoxynyboquinone in Tumors Selectively Kills NAD(P)H Quinone Oxidoreductase 1-Positive Cancer Cells through Programmed Necrotic and Apoptotic Mechanisms

  • Jiangwei Wang,
  • Xiaolin Su,
  • Lingxiang Jiang,
  • Matthew W. Boudreau,
  • Lindsay E. Chatkewitz,
  • Jessica A. Kilgore,
  • Kashif Rafiq Zahid,
  • Noelle S. Williams,
  • Yaomin Chen and
  • Shaohui Liu
  • + 2 authors

14 December 2023

Lung and breast cancers rank as two of the most common and lethal tumors, accounting for a substantial number of cancer-related deaths worldwide. While the past two decades have witnessed promising progress in tumor therapy, developing targeted tumor...

  • Systematic Review
  • Open Access
2 Citations
2,087 Views
25 Pages

Esophageal cancer (EC) is a very common form of cancer in developing countries, and its exponential progression is a cause for concern. Available treatments face the phenomenon of multi-drug resistance, as well as multiple disabling side effects. The...

  • Review
  • Open Access
30 Citations
5,827 Views
42 Pages

3 August 2022

In recent decades, molecular hybridization has proven to be an efficient tool for obtaining new synthetic molecules to treat different diseases. Based on the core idea of covalently combining at least two pharmacophore fragments present in different...

  • Article
  • Open Access
7 Citations
3,681 Views
18 Pages

Controlled Drug Release and Cytotoxicity Studies of Beta-Lapachone and Doxorubicin Loaded into Cyclodextrins Attached to a Polyethyleneimine Matrix

  • Agata Kowalczyk,
  • Artur Kasprzak,
  • Magdalena Poplawska,
  • Monika Ruzycka,
  • Ireneusz P. Grudzinski and
  • Anna M. Nowicka

14 August 2020

This work presents a new look at the application of cyclodextrins (CD) as a drug nanocarrier. Two different cyclodextrins (αCD, βCD) were covalently conjugated to branched polyethylenimine (PEI), which was additionally functionalized with...

  • Feature Paper
  • Article
  • Open Access
1 Citations
1,875 Views
20 Pages

Characterization of the Interaction of a Novel Anticancer Molecule with PMMA, PCL, and PLGA Polymers via Computational Chemistry

  • Edwar D. Montenegro,
  • Jamylle M. Nunes,
  • Igor F. S. Ramos,
  • Renata G. Almeida,
  • Eufrânio N. da Silva Júnior,
  • Márcia S. Rizzo,
  • Edson C. da Silva-Filho,
  • Alessandra B. Ribeiro,
  • Heurison S. Silva and
  • Marcília P. Costa

6 January 2025

The development of anticancer drugs is costly and time intensive. Computational approaches optimize the process by studying molecules such as naphthoquinones. This research explores the quantitative structure–activity relationship (QSPR) and mo...