Method for preparing cyclodextrin-loaded indolinopyrrole derivative and application of cyclodextrin-loaded indolinopyrrole derivative as anti-tumor drug

A technology of indole spiropyrrole and cyclodextrin, which is applied in the direction of antineoplastic drugs, drug combinations, and medical preparations of non-active ingredients, etc., can solve the problems of poor water solubility and high toxicity of solvent DMSO, and overcome poor solubility and solubility Good, obvious effect of inhibiting tumor cell proliferation

Inactive Publication Date: 2017-09-08
XUZHOU MEDICAL UNIV
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Problems solved by technology

However, due to the disadvantages of poor water solubility and high toxicity of the

Method used

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  • Method for preparing cyclodextrin-loaded indolinopyrrole derivative and application of cyclodextrin-loaded indolinopyrrole derivative as anti-tumor drug
  • Method for preparing cyclodextrin-loaded indolinopyrrole derivative and application of cyclodextrin-loaded indolinopyrrole derivative as anti-tumor drug
  • Method for preparing cyclodextrin-loaded indolinopyrrole derivative and application of cyclodextrin-loaded indolinopyrrole derivative as anti-tumor drug

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Embodiment 1

[0026] Weigh 600mg of 2-hydroxypropyl-β-cyclodextrin and dissolve it in 1ml of double-distilled water; then add concentrated hydrochloric acid drop by drop to adjust the pH to 2; solution, the concentration of which is 40% m / v) to adjust the pH value of the solution to 7.0 to obtain a clear and transparent 2-hydroxypropyl-β-cyclodextrin-loaded CPHSP medicinal solution.

[0027] The 2-hydroxypropyl-β-cyclodextrin prepared above was loaded with CPHSP for anti-cancer effect test:

[0028] A nude mouse liver cancer model in which HepG2 liver cancer cells were subcutaneously grafted was established, and when the tumor reached a diameter of 50-100 mm, they were randomly divided into a solvent control group and a treatment group. The treatment group was fed with 2-hydroxypropyl-β-cyclodextrin loaded with CPHSP, 50mg / kg, and the solvent control group was given 30g / kg 2-hydroxypropyl-β-cyclodextrin solution, once every two days, for 3 weeks . After two weeks of treatment, the tumor v...

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Abstract

The invention discloses a method for preparing a cyclodextrin-loaded indolinopyrrole derivative and application of the cyclodextrin-loaded indolinopyrrole derivative as anti-tumor drug. Through pH value adjustment and change, an indolinopyrrole derivative insoluble in water is loaded onto cyclodextrin, so that the problem of poor drug solubility is effectively solved; more importantly, on a mouse tumor model, the cyclodextrin-loaded indolinopyrrole derivative taking hexahydrospiro [indoline-3,3'-pyrroli zin]-2-one as nuclear parent a shows a definite anti-tumor effect and almost has no toxicity. Compared with the prior art, the cyclodextrin-loaded indolinopyrrole derivative has the advantages of good solubility, remarkable tumor cell proliferation inhibition effect, low toxic and side effect and the like, and can be used for treating the tumors including but not limited to liver cancer, renal cancer, skin cancer, nasopharynx cancer, gastrointestinal cancer and the like.

Description

technical field [0001] The invention belongs to the technical field of preparation of drugs for treating tumors. In particular, it relates to a class of indole spiropyrrole derivatives with hexahydrospiro[indoline-3,3'-pyrrolizine]-2-one as the core. After being loaded with cyclodextrin, in vitro and in vivo models Both can inhibit the proliferation of liver cancer cells and promote their apoptosis. Background technique [0002] With the development of medical technology, some tumors (Hodgkin's lymphoma, human choriocarcinoma, etc.) have been treated well, but the treatment of most malignant tumors is still a worldwide problem. Due to the continuous in-depth discussion and understanding of the mechanism of tumor occurrence and development, therapeutic drugs have gradually developed from low specificity and high toxicity to those with strong targeting and low side effects. upsurge. Molecular targeted drugs such as the multikinase inhibitor sorafenib are used in clinical pr...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/4439A61P35/00
CPCA61K31/4439
Inventor 姚宏朱松磊高晓鸽魏梦雪刘洪志
Owner XUZHOU MEDICAL UNIV
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