10-hydroxy camptothecin arginine salt, and its preparing method and use

Abstract

This invention relates to 10-hydroxycamptothecin arginine salt like the structure of formula (I). The preparation of this compound is in anhydrous solvent. 10-hydroxycamptothecin arginine reacts with arginine, obtaining related arginine salt and its compound. The quantity of adding arginine can be from 1 to 10 times of molar ratio. The water solubility of 10-hydroxycamptothecin arginine salt and its association object is obviously better than 10-hydroxycamptothecin, and possessing conspicuous liver target. It overcomes flaws such as noxious property of camptothecin sodium is high, stability is bad. It provides a medicine of which curative effect is reliable, medication is safe and cost is low for tumor patient.

Description

technical field The invention relates to a 10-hydroxycamptothecin arginine salt, a preparation method and application thereof, and belongs to the field of medicine and chemical industry. Background technique In 1966, American scholar Wall et al. extracted camptothecin from the unique tree species Campptotheca acuminata in my country, and found that it has a unique anticancer effect, but the side effects are large, which limits the clinical application of camptothecin. Therefore, camptothecin derivatives that not only maintain the anticancer activity of camptothecin but also have lower toxicity have always been the focus of attention. Subsequently, 10-hydroxycamptothecin (HCPT) was isolated from camptothecin, and clinical trials showed that it has a wide anti-cancer spectrum, significant curative effect, and less toxic and side effects, especially for primary liver cancer, Gastrointestinal cancer bladder cancer, head and neck skin cancer, leukemia, cervical cancer and other ...

AI Technical Summary

Problems solved by technology

However, due to its preparation itself, its physical and chemical properties are unstable, easy to oxidize, the toxicity increases after oxidation, and the solution changes color, which affects the curative effect.

And the solubility of 10-hydroxycamptothecin in commonly used solvents such as chloroform, ethanol, methanol, water is all bad, limits its use

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