10-hydroxy camptothecine, and method for processing raw material of camptothecine

Abstract

A process for preparing the raw material used to prepare 10-hydroxy camptothecine and camptothecine includes such steps as stacking dendrophilous seeds, and germinating at 15-30 deg.C and 100-150 % of humidity for 240-264 hr and then at 32-33 deg.C and 70-80% of humidity for 36-72 hr. The content of 10-hydroxy camptothecine in the raw material can be increased by 15-16 times. Its advantages are low cost, high output rate and good natural activity.

Description

technical field [0001] The invention relates to a processing method for producing 10-hydroxycamptothecin and camptothecin raw materials by using a biotransformation method. Background technique [0002] 10-Hydroxycamptothecin (10-Hydroxycamptothecin, HCPT) and camptothecin (camptothecin, CPT) are the secondary metabolites in the endemic tree species of my country—Camptotheca acuminata Decne. Significant inhibitory effect (see: American scholar Wall et al. in 1966 in the "American Chemical Bulletin" article "Plant Anti-tumor Reagent I: Isolation and Structure of Camptothecin, a Tumor Inhibitor from Camptothecin"; American Scholars Yaw-Huei et al published an article in "Journal of Chemical Biology" in 1985 "Camptothecin can induce the fragmentation of protein-DNA complexes through the expression of DNA topoisomerase I") (see references 1, 2 for details ). As an important anticancer drug, 10-hydroxycamptothecin has the characteristics of high efficiency, low toxicity and good s...

AI Technical Summary

Problems solved by technology

As an important anticancer drug, 10-hydroxycamptothecin has the characteristics of high efficiency, low toxicity and good solubility, and it is the camptothecin anticancer drug approved by the U.S. Food and Drug Administration (FDA). Litecan (Irinotecan, CPT-11) and Topotecan (Topotecan, TPT) are important precursors for artificial synthesis. However, because the natural content of 10-hydroxycamptothecin in camptothecin is very small, it is currently impossible to obtain it from camptothecin. The natural 10-hydroxycamptothecin is directly extracted from the environment, and a large amount of urgently needed 10-hydroxycamptothecin is generally obtained by artificial semi-synthesis with camptothecin as the parent compound

However, the above-mentioned method is costly, complex process, low synthesis efficiency, and poor natural activity. Therefore, it is very important to find low-cost raw materials for simultaneously producing natural 10-hydroxycamptothecin and camptothecin