How is camptothecin produced?
It is commercially produced from plants, mainly Camptotheca acuminata and Nothapodytes nimmoniana2. Camptothecin is the third most in-demand alkaloid after taxol and vinca-alkaloids for anti-cancer applications, and inhibits DNA topoisomerase I in cancer cells leading to cell death3.Jan 14, 2021
Where is camptothecin from?
Abstract. 20-(S)-Camptothecin (CPT) is a natural alkaloid extracted from the bark of Camptotheca acuminata (Chinese happy tree).Feb 15, 2017
Is camptothecin a natural product?
Irinotecan and topotecan are structurally related semisynthetic derivatives of the natural product camptothecin, an alkaloid derived from extracts of the tree Camptotheca acuminata.
How does camptothecin work?
Camptothecin binds to the topoisomerase I and DNA complex resulting in a ternary complex, stabilizing it and preventing DNA re-ligation and therefore causes DNA damage which results in apoptosis.Sep 11, 2007
What does camptothecin do to cancer cells?
Cyclosert-Camptothecin
CPT, an alkaloid extract, displays anticancer activity as an inhibitor of DNA topoisomerase I. This action prevents resealing of DNA following DNA synthesis, halting nucleic acid synthesis and cell death.
How does camptothecin block the activity of topoisomerase?
Camptothecin-derived TopI inhibitors function by forming a ternary complex with TopI-DNA and are able to stack between the base pairs that flank the cleavage site due to their planar structure. Normal cells have multiple DNA checkpoints that can initiate the removal of these stabilized complexes, preventing cell death.
What does camptothecin block?
Since camptothecin is known to be a specific inhibitor of type I DNA topoisomerase, we suggest that this enzyme is acting very near the replication forks.
How is topoisomerase inhibited?
Topoisomerase inhibitors block the ligation step of the cell cycle, which generates DNA single- and double-strand breaks, leading to apoptotic cell death. Topoisomerase I inhibitors include irinotecan, topotecan, and camptothecin, and topoisomerase II inhibitors include etoposide, doxorubicin, and epirubicin.
What prevents topoisomerase?
Topoisomerases are enzymes that are abundantly present in our cells and can temporarily cut and rejoin our DNA to remove knots and tangles that form during important biological processes.Mar 19, 2020
Is camptothecin an alkaloid?
Camptothecin (CPT), a natural alkaloid isolated from Camptotheca acuminata Decne, is found to show potential insecticidal activities with unique action mechanisms by targeting at DNA-topoisomease I (Top1) complex and inducing cell apoptosis.Dec 2, 2019