Next Article in Journal
Melandrii Herba Extract Attenuates H2O2-Induced Neurotoxicity in Human Neuroblastoma SH-SY5Y Cells and Scopolamine-Induced Memory Impairment in Mice
Previous Article in Journal
Influence of Harvest Season and Cultivar on the Variation of Phenolic Compounds Composition and Antioxidant Properties in Vaccinium ashei Leaves
Article Menu
Issue 10 (October) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(10), 1631; doi:10.3390/molecules22101631

Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone

1
Pharmacy Department, Health Sciences Center, Universidade Federal do Rio Grande do Norte (UFRN), Natal RN 59012-570, Brazil
2
Crowfoot Group of X-ray Techniques, Universidade Estadual do Amazonas (UEA), Manaus AM 69065-020, Brazil
3
Biological Activities Laboratory, Universidade Federal do Amazonas (UFAM), Pharmaceutical Sciences, Manaus AM 69080-900, Brazil
4
Laboratory of Synthesis of Bioactive Molecules, Organic Chemistry Department, Universidade Federal Fluminense (UFF), Niterói RJ 24020-141, Brazil
5
Graduate Program in Biotechnology, Laureate International Universities—Universidade Potiguar (UnP), Natal RN 59056-000, Brazil
*
Author to whom correspondence should be addressed.
Received: 12 September 2017 / Revised: 25 September 2017 / Accepted: 28 September 2017 / Published: 30 September 2017
View Full-Text   |   Download PDF [1893 KB, uploaded 30 September 2017]   |  

Abstract

Chagas disease is an endemic parasitic infection that occurs in 21 Latin American countries. New therapies for this disease are urgently needed, as the only two drugs available (nifurtimox and benznidazol) have high toxicity and variable efficacy in the disease’s chronic phase. Recently, a new chemical entity (NCE) named Pyranaphthoquinone (IVS320) was synthesized from lawsone. We report herein, a detailed study of the physicochemical properties and in vitro trypanocidal activity of IVS320. A series of assays were performed for characterization, where thermal, diffractometric, and morphological analysis were performed. In addition, the solubility, permeability, and hygroscopicity of IVS320 were determined. The results show that its poor solubility and low permeability may be due to its high degree of crystallinity (99.19%), which might require the use of proper techniques to increase the IVS320’s aqueous solubility and permeability. The trypanocidal activity study demonstrated that IVS320 is more potent than the reference drug benznidazole, with IC50/24 h of 1.49 ± 0.1 μM, which indicates that IVS320 has potential as a new drug candidate for the treatment of Chagas disease. View Full-Text
Keywords: physicochemical characterization; IVS320; quinone; T. cruzi; Chagas disease; pyranaphthoquinone physicochemical characterization; IVS320; quinone; T. cruzi; Chagas disease; pyranaphthoquinone
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Dantas, E.D.; de Souza, F.J.J.; Nogueira, W.N.L.; Silva, C.C.; de Azevedo, P.H.A.; Soares Aragão, C.F.; Almeida, P.D.O.; Cardoso, M.F.C.; da Silva, F.C.; de Azevedo, E.P.; Guimarães Barbosa, E.; Lima, E.S.; Ferreira, V.F.; Lima, Á.A.N. Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone. Molecules 2017, 22, 1631.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top