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Spirostanol saponins and application thereof

A compound and spirosteroid technology, which is applied to spirosteroids and their application fields, can solve the problem of insufficient research on chemical components of open arrows.

Active Publication Date: 2016-08-17
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing research on the chemical composition of open arrow is still not thorough enough, so the chemical composition of steroids in open arrow is worthy of further research and development

Method used

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  • Spirostanol saponins and application thereof
  • Spirostanol saponins and application thereof
  • Spirostanol saponins and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Extraction and identification of spiro steroids

[0028] 1. Extraction of spiro steroids

[0029] Take 17 kg of open arrow rhizomes, heat and reflux with 60% ethanol to extract 4 times, each time for 4 hours, combine the extracts to recover the solvent under reduced pressure, and obtain the total extract, suspend the total extract with water, and extract with equal volume of ethyl acetate for 4 Next, fat-soluble impurities were removed, and the aqueous layer was separated by D101 macroporous resin column chromatography, and eluted with water, 20% ethanol, 60% ethanol, 80% ethanol, and 95% ethanol respectively to obtain 5 fractions TA, TB, TC, TD, TE. Take fraction TC (60% ethanol eluted part) 200g, adopt silica gel column chromatography, ODS medium and low pressure column chromatography, reverse phase high performance liquid chromatography and other separation methods to separate and obtain compounds 1 and 2 of the present invention. Compound 3-9 of the pres...

Embodiment 2

[0086] Embodiment 2 Tumor inhibition test:

[0087] The compound of the present invention is to the in vitro antitumor activity experiment of 7 tumor strains of human body, these 7 tumor strains comprise FaDu (human pharyngeal squamous cell carcinoma cell), Detroit 562 (human pharyngeal carcinoma pleural effusion metastasis cell), CNE-1 (well-differentiated human Nasopharyngeal squamous cell carcinoma cells), CNE-2 (poorly differentiated human nasopharyngeal squamous cell carcinoma cells), HepG2 (human liver cancer cells), K562 (human chronic myelogenous leukemia cells), SPC-A-1 (human lung adenocarcinoma cells) Cytotoxic activity of seven human tumor cells and toxicity to normal cell L-929 (mouse fibroblasts). The anticancer drug cis-dichlorodiamineplatinum (II) (cisplatinum) was used as a positive control.

[0088] Inhibition of tumor cell proliferation (MTT method)

[0089] The tumor cells were inoculated in a 96-well plate, and after 24 hours of culture, the samples to b...

Embodiment 3

[0095] Embodiment 3 anti-inflammatory test:

[0096] For the anti-inflammatory activity test of the compound of the present invention in vitro, Raw 264.7 (mouse macrophage) cells induced by LPS (lipopolysaccharide) were used to establish an in vitro inflammation model. MTT and Griess experiments were used to investigate the effect of the compound of the present invention on the release of inflammatory mediator NO from Raw 264.7 cells induced by lipopolysaccharide. The anti-inflammatory drug Indomethacin (indomethacin) was used as a positive control.

[0097] 1) MTT experiment

[0098] Raw 264.7 cells were inoculated in a 96-well plate, and after 24 hours of culture, the product to be tested was added, and after another 24 hours of culture, the inhibition rate of the sample on tumor cell proliferation was measured by the MTT method. The cell proliferation inhibition rate was calculated according to the following formula, and the half inhibitory concentration (IC) of the teste...

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PUM

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Abstract

The invention discloses spirostanol saponins and application thereof. The spirostanol saponins is extracted and separated from tupistra chinensis rhizomes. The spirostanol saponins and the application have the advantages that as discovered in experimental research, excellent effects can be realized by nine types of spirostanol saponins in the aspects of cancer prevention and anti-inflammation actions, certain suppression effects can be realized by the spirostanol saponins for pharynx squamous cell carcinoma, pharynx cancer, nasopharyngeal squamous cell carcinoma, liver cancer, chronic myelocytic leukemia, lung adenocarcinoma and the like, and accordingly the spirostanol saponins is high in efficiency and low in toxicity and can be hopefully developed to obtain novel anticancer medicines and healthcare foods.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to spiro steroid compounds and applications thereof. Background technique [0002] Tumor is a new organism characterized by excessive cell proliferation produced by the cells of human organs and tissues under the long-term action of external and internal harmful factors. It can be divided into two categories: benign tumors and malignant tumors in medicine. Benign tumors have little impact on human health, while malignant tumors (also known as cancer) seriously threaten human health. According to the latest statistics from the World Health Organization and the American Cancer Society, cancer has become the leading cause of human death. In 2008, there were about 12.7 million newly diagnosed cancer cases and 7.6 million cancer deaths worldwide (accounting for about 13% of all deaths) , and approximately 70% of cancer deaths occur in low- and middle-income countries. It i...

Claims

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Application Information

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IPC IPC(8): C07J71/00A61K31/58A61K31/7048A61P35/00A61P29/00
CPCC07J71/0005
Inventor 何祥久向丽敏王宜海易晓敏
Owner GUANGDONG PHARMA UNIV
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