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Anti-tumor compound extracted from house lizard as well as preparation method and application thereof

A compound and anti-tumor technology, applied in the field of anti-tumor compounds and their preparation, can solve the problems that the anti-tumor effect of active ingredients is not significant, and the anti-tumor effect of active ingredients is not obvious.

Inactive Publication Date: 2010-11-03
张仕状
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the relevant research on the traditional Chinese medicine gecko has failed to obtain monomer compounds with accurate chemical structures, and the anti-tumor effect of the obtained active ingredients is not obvious
[0005] Chinese patent number "ZL200310105343.6", patent name: "Preparation method of a new anti-cancer drug", in the method, anti-cancer ingredients are extracted from gecko raw materials, the anti-cancer active ingredients are 3.0 mg / mL, and the tumor inhibition rate is 65.9%, the anti-tumor effect of active ingredients is not significant enough

Method used

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  • Anti-tumor compound extracted from house lizard as well as preparation method and application thereof
  • Anti-tumor compound extracted from house lizard as well as preparation method and application thereof
  • Anti-tumor compound extracted from house lizard as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0114] Embodiment 1: A kind of preparation method of the antitumor compound extracted from gecko, the derivative of general formula (I) is the compound shown in general formula (II), comprising the following steps:

[0115] (1) Purification process: store the captured live geckos for 24-72 hours to digest and drain the existing food and waste in the body, wash with distilled water, and dry;

[0116] (2) Pulverization process: the gecko after the purification is transferred to the soaking tank, and the ethanol solution is added. The ethanol solution has a concentration of 95% by volume and is soaked. After soaking the gecko to death, the gecko and the soaking solution are transferred to In the high-speed crushing machine, the crushing liquid is obtained;

[0117]The volume percent concentration of the ethanol solution in the above steps is 95%. It has been proved by experiments that under the premise that other process conditions and steps remain unchanged, the volume percent c...

Embodiment 2

[0137] Embodiment 2, the compound shown in general formula (II), comprises the following initial purification and purification steps:

[0138] (6.1) Initial purification process of chromatographic samples:

[0139] Add purified water to the crude extract prepared in Example 1, fully dissolve it, let it stand for stratification, and obtain an aqueous solution with a concentration of 1.0 g / mL, take the supernatant, and carry out chromatographic separation. The sample is concentrated by vacuum distillation, the pressure is controlled below -0.096Mpa, the temperature is controlled at 40 ° C ~ 50 ° C, after concentration, it is freeze-dried, the pressure of freeze-drying is controlled at -0.099 ~ -0.100Mpa, and the temperature is controlled at -45 ° C ~-55°C, freeze-dried to obtain the primary purification chromatography sample;

[0140] (7) High performance liquid chromatography process:

[0141] a. Add pure water to the prepared primary purification chromatography sample, fully...

Embodiment 3

[0148] Embodiment 3. This embodiment provides another preparation method different from that of Embodiment 2. The compound represented by the general formula (II) includes the following initial purification and purification steps:

[0149] (6.2) High performance liquid chromatography initial purification process:

[0150] a. After fully dissolving the crude extract obtained in Example 1, let it stand for stratification to obtain an aqueous solution with a concentration of 1.0 g / mL, discard the insoluble solids, take the supernatant, and use a 0.45 μm microporous Injection after membrane filtration;

[0151] b. The filtrate was subjected to HPLC semi-preparative C18 column chromatography. The chromatographic conditions were: column temperature: 35°C, mobile phase: pure water and acetonitrile, C18 filler as the stationary phase, detection wavelength: 210nm, and ultraviolet spectrum wavelength range: 200~380nm, gradient elution: 0~5min, the ratio of acetonitrile is 0~0%, 5~10min...

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Abstract

The invention discloses an anti-tumor compound extracted from a house lizard, as well as a preparation method of the anti-tumor compound extracted from the house lizard and application of the compound as antitumor drugs. In clinical application, the anti-tumor compound extracted from the house lizard can be dissolved with normal saline and then used in an injection way or can be prepared into preparation for oral use directly; the anti-tumor compound extracted from the house lizard can be used for the chemotherapy of gastric cancer, lung cancer, liver cancer, colon cancer, breast cancer, leucocythemia, genital system tumors, and other common malignant tumors, plays remarkable anti-tumor effect without bone marrow suppression or damage to important organs under conventional dosage; and in addition, since the anti-tumor compound extracted from the house lizard can increase T cellular immunity, the anti-tumor compound has good Aids resistance.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and specifically relates to an antitumor compound extracted from geckos, a preparation method and application thereof. Background technique [0002] At present, under the premise that there is still no effective treatment for many cancer patients, it is of great theoretical significance and application value to find high-efficiency and low-toxicity drugs for the treatment of cancer. [0003] Gecko is a traditional Chinese medicinal material, which has a long history of using it to treat cancer. Gecko, also known as Shougong, Tianlong, Scorpion Tiger, etc., belongs to the genus Gecko of the family Lizardidae of the reptile phylum Lizard. Nature and flavor: Cheng, cold, slightly poisonous; Indications: expelling wind, calming convulsions, dispelling stagnation, detoxification. Treatment of paralysis due to apoplexy, chronic wind pain, wind-phlegm convulsions, scrofula, malignant sores, tetanus,...

Claims

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Application Information

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IPC IPC(8): C07D513/22A61K31/547A61P35/00A61P35/02A61P31/18
Inventor 张仕状李耀辉高志琴程鑫盛继文康建功
Owner 张仕状
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