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

A technology of hydroxycamptothecin and a processing method, applied in the directions of seed and rhizome treatment, organic chemistry, application, etc., can solve the problems of high cost, complicated process, low synthesis efficiency, etc., and achieves low comprehensive cost, high yield, natural active effect

Inactive Publication Date: 2004-08-18
NORTHEAST FORESTRY UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0009] Embodiment 1: get 50Kg dry camptothecin seeds, at first measure the dry weight content of its 10-hydroxycamptothecin and camptothecin, put it in temperature and be 25 ℃, be piled up under the condition of 100%~150% in humidity During the hydroponic germination, spray watering once every 10 to 12 hours, and stir once at the same time to ensure consistent humidity and sufficient oxygen in the camphor tree seed pile, change the conditions after 240 hours of germination, and change the conditions at a humidity of 70% to 80%, the temperature is 32 DEG C to 33 DEG C, after continuing to germinate for 72 hours, the seed buds producing 10-hydroxycamptothecin and camptothecin are obtained. The dry weight content of 10-hydroxycamptothecin and camptothecin in the camptothecin seeds before and after germination are shown in the following table respectively.

[0010] germination time

[0011] germination time

Embodiment 2

[0012] Embodiment 2: Get 50Kg dry camptothecin seeds, first measure the dry weight content of its 10-hydroxycamptothecin and camptothecin, and put it on April 10, 2001 and be 25 ℃ in temperature, humidity is 100%~150 Under the condition of %, it is piled up in the greenhouse for hydroponic germination. During this period, spray watering once every 10 to 12 hours, and stir once at the same time to ensure consistent humidity and sufficient oxygen in the philodendron seed pile, and germinate for 312 hours Finally, the seed buds producing 10-hydroxycamptothecin and camptothecin were obtained. The dry weight content of 10-hydroxycamptothecin and camptothecin in camptothecin seeds before and after germination are shown in the following table respectively.

[0013] germination time

[0014] germination time

[0015] Draw from above-mentioned two examples, the 10-hydroxycamptothecin dry weight content in the camptothecin bud body that finally obtains in embodiment ...

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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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01C1/00C07D491/22
Inventor 祖元刚唐中华付玉杰张宝友李庆勇赵春建史权
Owner NORTHEAST FORESTRY UNIVERSITY
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