The modification of the esterification structure of JZ-001 was carried out by “Jiuzhang Biotech”, and 12 kinds of analogues were synthesized by chemical and structural modification of the ester moiety. A comparative study of the relationship between structure and inhibition of enzyme activity showed that the activity of the modified derivative was much stronger than that of its own.
Further studies have confirmed that the derivative of plant active factor JZ-001 after the modification of esterification structure has more stable chemical properties, thus making it more conducive to the preparation and preservation of pharmaceutical active ingredients, and is beneficial to the stability of the preparation process and storage. Help to ensure the content and efficiency of efficacious active ingredients came into the body.
In addition, the properties of the derivatives after esterification have been increased, which is beneficial to the effective time in vivo as a pharmaceutically active ingredient and improved the long-term efficacy and bioavailability of the drug. The properties is beneficial to moving to patient's tissue and improving its targeting in the tissues and organs.
The pharmacodynamics studies further showed that: class 1 anti-cancer drug ester derivatives have a stronger effect of liver protection and immune regulation, and have a good therapeutic effect on leukemia in animal pre-test.
Liver protection study:
The company commissioned the Sichuan Institute of Antibiotics conducted the study of "the treatment and protection effect of liver injury which is induced by carbon tetrachloride ", the results showed that the monoesters and polyesters derivatives of class 1 anti-cancer drug have a more therapeutic effect and liver function in liver injury.
The company commissioned the Sichuan Institute of Antibiotics carried out the test of mouse carbon clearance. The results showed that the monoesters and polyesters could significantly increase the phagocytic index K and the corrected phagocytic index of macrophages. It can be seen that monoesters and polyesters can increase phagocytosis of macrophages and enhance the nonspecific immune function in mice.