Antineoplastic pentacyclic triterpenoid and extraction method thereof

A technology for pentacyclic triterpenes and an extraction method, which is applied in the field of anti-tumor pentacyclic triterpenoids, can solve the problems of inability to prevent ovarian cancer metastasis, large side effects of chemotherapy drugs, adverse reactions, etc. Simple method and good antitumor activity

Inactive Publication Date: 2013-07-03
WENZHOU MEDICAL UNIV
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Problems solved by technology

The clinical treatment of ovarian cancer is mainly to use surgical resection combined with chemotherapy, but surgical resection cannot prevent further metastasis of ovarian cancer; at the same time, the side effects of chemotherapy drugs are also relatively large, often causing gastrointestinal reactions, stomatitis, bone marrow suppression, Adverse reactions such as hair loss, nervous system adverse reactions, and renal toxicity have caused great pain to patients

Method used

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  • Antineoplastic pentacyclic triterpenoid and extraction method thereof
  • Antineoplastic pentacyclic triterpenoid and extraction method thereof
  • Antineoplastic pentacyclic triterpenoid and extraction method thereof

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Embodiment 1

[0028] ① Soak 10 kg of dry leaves of the succulent tree with 20 L of 95% ethanol at room temperature for 3 h, then perform ultrasonic extraction, and the extract is concentrated in a vacuum to obtain a crude extract of about 150 g;

[0029] ② Add the crude extract in ① to distilled water to suspend it in water, and extract with petroleum ether and ethyl acetate to obtain the corresponding extract;

[0030] ③ The 20 g extract obtained in ② was divided into 20 parts through silica gel column chromatography;

[0031] ④ Separate about 4.0 g of the sixth part in ③ using n-hexane-ethyl acetate-ethanol-water by high-speed countercurrent chromatography, and finally obtain about 460 mg of dry powder.

[0032] High-speed countercurrent chromatography is a commonly used technique known to those skilled in the art, and there are existing textbook guidance, such as "High-speed countercurrent chromatography" (author: Zhang Tianyou Wang Xiao , Chemical Industry Press), in addition, the...

experiment example 1

[0035] 1. Experimental method

[0036] (1) MTT assay to detect the effect of THA on cell proliferation

[0037] Succinate dehydrogenase in the mitochondria of living cells can reduce exogenous MTT to water-insoluble blue-purple crystal formazan, which is then deposited in the cell, but dead cells have no such function. DMSO can dissolve formazan, and measure its absorbance within a certain range of cell mass. The larger the absorbance value, the stronger the cell activity. In this study, this method was used to detect the effect of THA on cell proliferation. The specific operation is as follows:

[0038] ① Collect logarithmic phase cells and adjust the concentration to 2~5×10 4 cells / 100 μl;

[0039] ② Add 100 μl / well to a 96-well plate, and fill the edge wells with sterile PBS;

[0040] ③a After 24 hours of cell growth, add 2.5, 5, 10, 20, 40 and 80 μg / ml THA to treat the cells, DMSO as a control, and set 3 replicate wells;

[0041] ③b After the cells grew for 24 hours...

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Abstract

The invention discloses an antineoplastic pentacyclic triterpenoid and an extraction method of the antineoplastic pentacyclic triterpenoid. The antineoplastic pentacyclic triterpenoid is extracted and separated from Sinojackia sarcocarpa L.Q.Luo, the chemical name is 2a, 3a, 19 beta, 23 beta-tetrahydroxyurs-12-en-28-oicacid, and pharmaceutical analysis finds that the compound has better antineoplastic activity and smaller toxicity towards normal cells. In addition, the invention further relates to the extraction method of the antineoplastic pentacyclic triterpenoid, and the method has the advantages of simplicity and rapidness.

Description

technical field [0001] The invention relates to an anti-tumor pentacyclic triterpenoid compound extracted from the succulent tree, and provides an extraction method. Background technique [0002] Ovarian cancer is one of the common malignant tumors in gynecology, its incidence rate ranks third among gynecological malignancies, and its mortality rate ranks first. Thousands of people die from ovarian cancer every year, and the death toll is still rising, which seriously threatens the life and health of women. The clinical treatment of ovarian cancer is mainly to use surgical resection combined with chemotherapy, but surgical resection cannot prevent further metastasis of ovarian cancer; at the same time, the side effects of chemotherapy drugs are also relatively large, often causing gastrointestinal reactions, stomatitis, bone marrow suppression, Adverse reactions such as hair loss, nervous system adverse reactions, and renal toxicity have caused great pain to patients. Ther...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61P35/00A61P15/00
Inventor 鲁新成廖婉琴刘素君王瓯晨邹家尉
Owner WENZHOU MEDICAL UNIV
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