4.7 Article

Ultrasound-assisted biosynthesis of novel methotrexate-conjugates

Journal

ULTRASONICS SONOCHEMISTRY
Volume 48, Issue -, Pages 51-56

Publisher

ELSEVIER
DOI: 10.1016/j.ultsonch.2018.05.017

Keywords

Biosynthesis; Lipases; Ultrasound; Methotrexate; Triacylglycerols; Cyclodextrins

Funding

  1. Portuguese Foundation for Science and Technology (FCT) [UID/BIO/04469/2013]
  2. COMPETE 2020 [POCI-01-0145-FEDER-006684]
  3. BioTecNorte operation - European Regional Development Fund [NORTE-01-0145-FEDER-000004]
  4. FCT - Fundacao para a Ciencia e a Tecnologia [SFRH/BD/121673/2016]
  5. European Union Horizon 2020 research and innovation programme [NMP-06-2015-683356 FOLSMART]
  6. Fundação para a Ciência e a Tecnologia [SFRH/BD/121673/2016] Funding Source: FCT

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New methotrexate-acylglycerols and methotrexate-cyclodextrins (alpha, beta and gamma-CD) conjugates were obtained via esterification or transesterification reactions. All reactions were catalysed by esterases namely immobilized Lipase from Candida antarctica B and Lipase from Thermomyces lanuginosus. The use of ultrasound to assist the reactions revealed to be a key factor to obtain high conversion yields on both MTX conjugates. Transesterification reactions including long chain triacylglycerols were only successful when ultrasound was applied. In cyclodextrins esterification a higher number of MTX molecules was also linked to cyclodextrins when ultrasound was used. All the conjugates were characterized by MALDI-TOF and NMR spectroscopy.

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