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Icariside I compound, derivative, pharmaceutical salt and application

A technology of icariin and compound, applied in the directions of sugar derivatives, organic chemistry, drug combination, etc., can solve the problems of aggravation of the patient's condition, the economic burden of the patient, and the large dose.

Inactive Publication Date: 2019-02-12
FOSHAN GOLDEN HEALTH TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there are many kinds of drugs used to treat liver cancer. Whether it is Chinese patent medicine or a combination of Chinese and Western medicine, they can only alleviate the patient's condition, and the large dose has caused serious psychological and physical damage to the patient. burden, and the antineoplastic drugs currently on the market have large toxic and side effects. Once the drug is stopped, the patient's condition will aggravate, causing a serious economic burden to the patient

Method used

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  • Icariside I compound, derivative, pharmaceutical salt and application
  • Icariside I compound, derivative, pharmaceutical salt and application
  • Icariside I compound, derivative, pharmaceutical salt and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: get 100mg icariside I, add 2mL of DMSO, 30mg iodomethane (CH 3 1), then add 10mg of silver oxide (Ag 2 O), stirred at 40 °C for 4 hours. The reaction solution was poured into distilled water, and then the precipitated yellow solid was suction-filtered, dried, and purified by column chromatography to obtain R 1 The group is the product of methoxy group.

Embodiment 2

[0034] Embodiment 2: get 100mg icariside I, add 2mL of DMSO, 100mg iodomethane (CH 3 1), then add 10mg of silver oxide (Ag 2O), stirred at 25 °C for 12 hours. The reaction solution was poured into distilled water, and then the precipitated yellow solid was suction-filtered, dried, and purified by column chromatography to obtain R 3 and R 1 The group is the product of methoxy group.

Embodiment 3

[0035] Example 3: Take 100 mg of icariside I, add 2 ml of DMSO, 50 mg of dimethyl sulfate, and stir at 80° C. for 2 hours. The reaction solution was poured into distilled water, and then the precipitated yellow solid was suction filtered, dried, and purified by column chromatography (silica gel column) to obtain R 3 The group is the product of methoxy group. Required R 3 Icaritin compounds with a methoxyl group.

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PUM

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Abstract

The invention provides an icariside I compound and a derivative and a pharmaceutical salt. A structure formula is shown as a formula I in the description. The compound, the derivative, the pharmaceutical salt or the composite is used for preparing medicine capable of being used for preventing, relieving or treating tumor diseases. The tumor includes liver cancer, lung cancer, colon cancer, ovariancancer, bile duct cancer, malignant lymphoma, liver cancer, bladder cancer and prostate cancer. The icariside I compound has obvious effects in aspects of improving the human immunity, improving thehuman IFN-gamma level, improving the apoptin NOXA expression and the like. Through in vivo experiments on mice and liver cancer cells (H22 cells and hepg2 cells) experiments, the results prove that the icariside I can obviously inhibit the tumor growth.

Description

technical field [0001] The present invention relates to an icariside I compound and its derivatives and pharmaceutically acceptable salts thereof, and the application of the compound in the prevention and treatment of tumors. Background technique [0002] Using a single compound as the main active ingredient of a natural product as a chemical drug itself or as a lead compound for drug development has been one of the important research methods used by drug researchers in the development of chemical drugs for many years, and the flavonoid glycoside compound icariin has also become a research hotspot. It shows that icariin has physiological activities such as anti-tumor effect, strengthening bone, regulating immune function, improving cardiovascular function, anti-aging and anti-oxidation function, enhancing anti-disease ability and enhancing sexual function. [0003] Epimedium is a traditional Chinese medicinal material blindly, and its use in the prior art is to use Epimedium...

Claims

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Application Information

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IPC IPC(8): C07H17/07A61P35/00A61K31/7048
CPCA61P35/00C07H17/07
Inventor 郭晓路周金林卢宇靖黄宝华林丽薇李慧灵
Owner FOSHAN GOLDEN HEALTH TECH CO LTD
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