Total Synthesis and in Vivo Evaluation of 8-Deoxypumiliotoxin 193H

Natural Product Research 2021
L. Zvejniece, Maija Dambrova, Gints Šmits

The total synthesis of both the double bond isomers of indolizine alkaloid 8-deoxypumiliotoxin 193H has been accomplished. Both the double bond isomers Z-4 and E-4 induced convulsions and inhibited neuro-muscular activity at a dose of 25 mg/kg after intraperitoneal injection in mice. The lethal dose of Z-4 and E-4 was 100 mg/kg, indicating that 8-deoxypumiliotoxin 193H is 10-times less toxic than the known pumiliotoxin (+)-251 D.

Keywords
deoxypumiliotoxin 193H, in vivo studies, stereoselectivity, Total synthesis
DOI
10.1080/14786419.2019.1636244
Hyperlink
https://www.tandfonline.com/doi/abs/10.1080/14786419.2019.1636244

Zvejniece, L., Dambrova, M., Šmits, G. Total Synthesis and in Vivo Evaluation of 8-Deoxypumiliotoxin 193H. Natural Product Research, 2021, Vol. 35, No. 3, pp.440-446. ISSN 1478-6419. Available from: doi:10.1080/14786419.2019.1636244

Publication language
English (en)