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Aspidospermine dipolymer and its drug composition, preparation method thereof and application

A compound and pharmaceutical technology, applied in the direction of drug combination, pharmaceutical formula, antineoplastic drugs, etc., can solve the problems of patients with severe toxicity

Inactive Publication Date: 2017-08-04
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the chemotherapy drugs currently used clinically have certain curative effects, they bring huge physical pain and mental stress to the patients due to their high toxicity and drug resistance. It is one of the frontier topics of current medicinal chemistry research

Method used

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  • Aspidospermine dipolymer and its drug composition, preparation method thereof and application
  • Aspidospermine dipolymer and its drug composition, preparation method thereof and application
  • Aspidospermine dipolymer and its drug composition, preparation method thereof and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Extraction separation and preparation:

[0049] Dried stems and leaves (15kg) of Tabernaemontana corymbosa Roxburgh ex Wallich (or E.yunnanensis Tsiang; E.yunnanensis var.heterosepala Tsiang) were crushed and leached three times with methanol at room temperature (3×25L). At intervals of 2 days, the extract was recovered under reduced pressure to obtain the total extract. Dissolve the total extract with 0.5% HCl solution completely, adjust the pH to 2-3, and extract 3 times with an equal volume of ethyl acetate; Extracted 3 times, the ethyl acetate layers were combined and concentrated to obtain the total alkaloids (61.5 g). Use 70g (200-300 mesh) silica gel plate sample, 650g (200-300 mesh) silica gel packing column for silica gel column chromatography, chloroform-acetone gradient elution (from 1:0 to 2:1), and detect with TLC. Eight segments (Fr.I‐VIII) were obtained after combining the same fractions. Fr.VIII (20.3g) was divided into two components, VIII-I and VIII...

Embodiment 2

[0071] Tests have proved that the general formula (I) bisindole compound of the present invention is effective on human breast cancer cell line (SK-BR-3), human liver cancer cell line (SMMC7721), human leukemia cell line (HL-60), human pancreatic cancer The half inhibitory concentration (IC50) of cell line (PANC‐1) and the growth of human lung cancer cell line (A549) is between 0.1‐1000 μM, which has the effect of preventing or treating proliferative diseases such as cancer. The experimental methods and results are as follows:

[0072] 1.1 Materials and methods:

[0073] 1.1.1. Sample and preparation:

[0074] The sample was colorless, and was dissolved in dimethyl sulfoxide (DMSO) to prepare a stock solution with a concentration of 10 mg / ml and stored in the dark for future use.

[0075] 1.1.2. Cell lines:

[0076] HL‐60, a human leukemia cell line

[0077] A‐549, a human lung cancer cell line

[0078] SMMC‐7721, a human hepatoma cell line

[0079] MCF‐7, a human breast...

Embodiment 3

[0095]According to the method of Example 1, 3α-acetonyl-conophyllidine and 3α-acetonyl-melodinine K were first prepared, 4% sulfuric acid ethanol solution was added, pH=4, filtered, and dried to make sulfuric acid 3α-acetonyl-conophyllidine and 3α-acetonyl- melodinine K.

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PUM

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Abstract

The invention provides an aspidospermine dipolymer with anti-cancer activity, a preparation method thereof and a drug composition containing them. The invention further provides an extractive of ervatamia heyneana or melodinus suaveolens, and a drug composition taking them as active components, and application of aspidospermine dipolymer ot its plant extractive in preparing drugs for treating or preventing leukemia, cancer of the liver, cancer of the liver, breast cancer, pancreatic cancer, and other cancer diseases.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular, it relates to furan-linked quinaryl dimers, organic and inorganic acid salts with antitumor activity, pharmaceutical compositions containing them and extracts of Bermudagrass or Bergamot japonica, and Their use in the preparation of medicines for treating or preventing cancer. Background technique [0002] Tumor is a worldwide problem. Millions of tumor patients die every year in China. Although the chemotherapy drugs currently used clinically have certain curative effects, they bring huge physical pain and mental stress to the patients due to their high toxicity and drug resistance. It is one of the frontier topics of current medicinal chemistry research. Contents of the invention [0003] The object of the present invention is to: provide the compound of formula (I), and utilize organic acid (for example tartaric acid, citric acid, formic acid, acetic acid, oxalic acid etc...

Claims

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Application Information

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IPC IPC(8): C07D491/22A61K31/438A61P35/00A61P35/02A61K36/185A61K36/24
CPCA61K36/185A61K36/24C07D491/22
Inventor 蔡祥海张冰洁保梅芬
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI