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Synthesis and biological evaluation of β-lapachone and nor-β-lapachone complexes with 2-hydroxypropyl-β-cyclodextrin as trypanocidal agents.

08:00 EDT 21st March 2020 | BioPortfolio

Summary of "Synthesis and biological evaluation of β-lapachone and nor-β-lapachone complexes with 2-hydroxypropyl-β-cyclodextrin as trypanocidal agents."

We study βLAP and its derivative nor-β-Lapachone (NβL) complexes with 2-hydroxypropyl-β-cyclodextrin to increase the solubility and bioavailability. The formation of true inclusion complexes between βLAP or NβL in 2-HP-β-CD in solid solution was characterization by FT-IR, DSC, powder X-ray was and was confirmed by one- and two-dimensional H NMR experiments. Additionally, the biological activities of βLAP, NβL, ICβLAP, and ICNβL were investigated through trypanocidal assays with T. cruzi and cytotoxicity studies with mouse peritoneal macrophages. Originally, we tested these complexes against T. cruzi viability and observed higher biological activities and lower cytotoxicity when compared to βLAP and NβL. Thus, the complexation of βLAP and NβL with 2-HP-β-CD increases the drug solubility, in addition vectorization was observed, increasing the biological activity against epimastigotes and trypomastigotes T. cruzi forms. Reduced the toxicity of the compounds against mammalian cells. In addition, the selectivity indices higher of the inclusion complexes comparing to substance free and those of benznidazole.

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Name: Journal of bioenergetics and biomembranes
ISSN: 1573-6881
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Medical and Biotech [MESH] Definitions

Polymeric compounds that contain repeating units of hydroxypropyl methylcellulose. The properties of hypromellose polymers can vary greatly and are defined by their molecular weight, the percentage of hydroxyl groups, the percentage of hydroxypropyl groups, and viscosity measurements. They are found a broad variety of commercial products such as FOOD ADDITIVES; EXCIPIENTS; and LUBRICANTS.

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