10-Hydroxycamptothecin Water-Soluble Macromolecular Conjugates for pH Sensitive Release, Preparation Method and Application

A technology of water-soluble macromolecules and hydroxycamptothecin, which is applied in the direction of organic active ingredients, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as drug resistance and achieve drug loading High, no drug leakage, improved pharmacokinetic properties

Active Publication Date: 2019-05-24
ZHENGZHOU UNIV
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  • Abstract
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Problems solved by technology

The reason is that some tumor cells overexpressing P-gp are not resistant to CPT drugs, such as human leukemia K562ADM cells overexpressing P-gp and unmutated K562 cells are almost as sensitive to CPT in vivo; and Carolyn However, studies by et al. have confirmed that: P-gp plays an ATP-dependent drug efflux role in some tumor cells, which leads to the generation of drug resistance.

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  • 10-Hydroxycamptothecin Water-Soluble Macromolecular Conjugates for pH Sensitive Release, Preparation Method and Application
  • 10-Hydroxycamptothecin Water-Soluble Macromolecular Conjugates for pH Sensitive Release, Preparation Method and Application
  • 10-Hydroxycamptothecin Water-Soluble Macromolecular Conjugates for pH Sensitive Release, Preparation Method and Application

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[0046] The technical solutions of the present invention will be clearly and completely described below in conjunction with the accompanying drawings. Apparently, the described embodiments are some of the embodiments of the present invention, but not all of them. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0047] For the molecular structure of 10-hydroxycamptothecin (10-HCPT), see figure 1 , is composed of a pyrroloquinoline ring, a conjugated pyridine ring and a six-membered α-hydroxy lactone ring (ring E), molecular formula C 20 h 16 N 2 o 5 , molar mass 364.357, yellow prismatic monohydrate crystal, melting point 268-270°C, slightly soluble in a few organic solvents, insoluble in water, dissolved in the form of ring-opening carboxylate in dilute alkali solution, the solution has a blue color fluorescence....

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Abstract

The invention discloses a pH sensitive-released 10-hydroxycamptothecine water soluble macromolecular conjugate as well as a preparation method and application thereof. The conjugate is capable of greatly improving the water solubility of 10-HCPT through structural transformation; the pharmacokinetic property of 10-HCPT is improved; by means of the characteristic of a tumor microenvironment, a medicament is released in a pH responsive manner, so that the conjugate has a controlled-release effect; chemical bonds carry the drug with a high drug loading capacity and no drug leakage; a chemotherapeutic can be targeted to tumors and is left for a relatively long time, and the conjugate has a good targeting property.

Description

technical field [0001] The invention relates to the technical field of chemical pharmacy, in particular to a pH-sensitive released 10-hydroxycamptothecin water-soluble macromolecular conjugate, a preparation method and an application. Background technique [0002] 10-Hydroxycamptothecine (10-HCPT) is a camptothecin alkaloid with significant anti-cancer activity extracted from the fruit and leaves of the deciduous plant Camptothecin genus Eclipta genus in the Davidiaceae family. Synthetic resin obtained. Its anticancer effect is equivalent to 30 times that of camptothecin. 10-HCPT has obvious curative effect on pancreatic cancer, prostate cancer, bladder cancer, oral squamous cell carcinoma, colorectal cancer, gastric cancer, liver cancer, non-small cell lung cancer, etc. It also has a good curative effect on oral cavity, neck and face cancer, head and neck cancer, cylindrical adenocarcinoma of the head and neck and skin cancer; it also has good curative effect on malignant...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/334A61K47/60A61K31/4745A61P35/00
CPCA61K31/4745C08G65/3348
Inventor 刘洋
Owner ZHENGZHOU UNIV
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