10-Hydroxycamptothecin

Описание

10-Hydroxycamptothecin: An Inhibitor of Topoisomerase I with Antitumor Activity
10-hydroxycamptothecin (10-HCPT) is an inhibitor of topoisomerase I originally isolated from the Chinese tree C. acuminata. 10-HCPT, a member of the camptothecin family, interferes with DNA synthesis by inhibiting the enzyme topoisomerase-I and has a broad spectrum of antitumor activity and less toxicity as camptothecins. However, 10-HCPT is insoluble in both water and physiological acceptable organic solvents and tends to change into its carboxylate form, which shows minimal antitumor activity and several unpredictable side effects. Therefore, appropriate drug delivery systems (DDS) for 10-HPCT have been developed to improve the stability of its lactone form. 10-HCPT is also an important precursor for the synthesis of clinically useful anticancer agents, such as irinotecan[1].

Химические свойства

mp 268-270°C loss on drying <1%

Использование

Topoisomerase inhibitor

использованная литература

[1] Chunjian Zhao. “Determination of Camptothecin and 10-Hydroxycamptothecin in Camptotheca acuminata by LC-ESI-MS/MS.” Analytical Letters 6 1 (2010): 2681–2693.
[2] Ruonan Shuang. “Pharmacokinetics of 10-hydroxycamptothecin–tetrandrine liposome complexes in rat by a simple and sensitive ultra-high performance liquid chromatography with tandem mass spectrometry.” Journal of separation science 43 3 (2019): 569–576.