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Tetraterpene compound and derivatives thereof for treating cancer, inflammation and central nervous system diseases

A kind of technology of compounds and derivatives, applied in the field of pentacyclic triterpenoids and derivatives thereof

Inactive Publication Date: 2010-08-11
朱永亮
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no research on the anticancer components of this genus of plants

Method used

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  • Tetraterpene compound and derivatives thereof for treating cancer, inflammation and central nervous system diseases
  • Tetraterpene compound and derivatives thereof for treating cancer, inflammation and central nervous system diseases
  • Tetraterpene compound and derivatives thereof for treating cancer, inflammation and central nervous system diseases

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Dry coarse powder of Salacia hainanensis root, reflux extraction with 80% methanol each twice, recover solvent respectively, and obtain ethanol extraction extract. Extract with ethyl acetate, concentrate, go through silica gel column chromatography, and elute with ethyl acetate respectively. After recovering the solvent, it is detected by TLC and HPLC. The purity is above 90%. It is further identified and confirmed by UV, H-NMR and MS. Is the above-mentioned compound of formula II.

Embodiment 2

[0030] Human liver cancer cell line Huh-7 and breast cancer cell line T47D were tested for their inhibitory effect on tumor cell growth by MTT method; they were treated with different doses of the compound of formula II, compared with the control, the compound of formula II significantly inhibited Cell growth of the human liver cancer cell line Huh-7 and the breast cancer cell line T47D, the half-inhibitory concentrations were 3.0 and 11.0 micromolar, respectively.

Embodiment 3

[0032] The compound of formula II was used in experiments on mice. Model mouse L1210 was obtained from implanted leukemia cells. It is an important model animal for testing whether compounds have anticancer activity. Screening based on the model mouse L1210 provided a variety of small molecule compounds approved by the FDA for the treatment of leukemia or lymphoma. CDF1 mice grew tumors very quickly after being implanted with leukemia cells L1210. In this experiment, the compound of formula II was dissolved in alcohol and saline solution, and intravenously injected into mice at 0.5 mg / kg animal. Compared with the control group, the survival rate of the treatment group was significantly improved.

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PUM

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Abstract

The invention discloses a pentacyclic triterpene compound and derivatives thereof. The pentacyclic triterpene compound and the derivatives thereof can inhibit the growth of tumour cells and can be used to treat cancer, inflammation and central nervous system diseases. The invention also discloses a method for extracting and chemically synthesizing the pentacyclic triterpene compound and the derivatives thereof.

Description

technical field [0001] The present invention relates to a pentacyclic triterpene compound and its derivatives. This triterpene compound and its derivatives can be used in the treatment of cancer, inflammation and central nervous system diseases. Background technique [0002] The genus Salacia belongs to the Pterodactylaceae, about 168 species, distributed in the tropical regions of the world. There are many foreign research reports. Since the 1960s, the studied plants include S.prinoides, S.fruticosa, S.beddomei, S.macrosperrna, S.kraussii, S.chinensis, s.oblonga, S.madagascar iensis, S.reticulata, s.cordata, S.1ehmbachii, etc., the research parts of plants are mainly roots and stems, and a total of more than 60 components have been isolated from this genus, mainly triterpenoids and polyphenols; pharmacological studies have shown : Most of the water-soluble parts of the plant roots or stems of this genus have anti-oxidation, liver protection, fat-lowering, weight-loss, and...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/573A61K36/77A61P35/00A61P35/02A61P29/00A61P19/02A61P25/28A61P25/14A61P25/16
Inventor 朱永亮
Owner 朱永亮
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