期刊
BIOMOLECULES
卷 10, 期 12, 页码 -出版社
MDPI
DOI: 10.3390/biom10121640
关键词
chemical synthesis; extraction; mipsagargin; trilobolide isolation from fruits; optimization and scale-up; Laser trilobum cultivation; sarco /endoplasmic reticulum calcium ATPase (SERCA); sesquiterpene lactones; thapsigargin; trilobolide; 8-O-(12-aminododecanoyl)-8-O-debutanoylthapsigargin
资金
- UCT Prague
- [A1_FPBT_2020_004]
In spite of the impressing cytotoxicity of thapsigargin (Tg), this compound cannot be used as a chemotherapeutic drug because of general toxicity, causing unacceptable side effects. Instead, a prodrug targeted towards tumors, mipsagargin, was brought into clinical trials. What substantially reduces the clinical potential is the limited access to Tg and its derivatives and cost-inefficient syntheses with unacceptably low yields. Laser trilobum, which contains a structurally related sesquiterpene lactone, trilobolide (Tb), is successfully cultivated. Here, we report scalable isolation of Tb from L. trilobum and a transformation of Tb to 8-O-(12-aminododecanoyl)-8-O-debutanoylthapsigargin in seven steps. The use of cultivated L. trilobum offers an unlimited source of the active principle in mipsagargin.
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