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Anti-tumor medicine

An anti-tumor drug and anti-tumor technology, applied in the field of anti-tumor drugs, can solve the problems of poor prognosis of cancer patients

Inactive Publication Date: 2008-01-16
殷正丰 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The expression of FAS starts to be up-regulated in the early stage of tumorigenesis, and further increases with the development of tumors, and the prognosis of tumor patients with high FAS expression is poor

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Preparation of noricariin (see Ye Haiyong et al., Journal of Zhejiang University (Medical Edition), 2005, 34(2): 131-136).

[0058] Take 2 kg of Epimedium arrowleaf collected in the mountainous area of ​​southern China, grind it into powder, and then extract it with 95% ethanol (10 L). 250 g of concentrated starting material were obtained, which were then further extracted with 2.5 L of chloroform, ethyl acetate and n-butanol. 8 g of ethyl acetate extract and 10 g of n-butanol extract were loaded onto a silica gel column with CHCl 3 -MeOH-HCOOH (150:1:0.5) and CHCl 3 -MeOH (8:2) eluted separately. Through this process, 300 mg of icariin and icariin, the precursor of noricariin, can be prepared. The precursor is then hydrolyzed as briefly described below to first produce icariin. Solution A: 80 mg of the precursor was dissolved in 18 ml of methanol solution by ultrasonic; Solution B: 500 U (0.433 g) of cellulase was dissolved in 180 ml (0.1 mol / L) of acetic acid buff...

Embodiment 2

[0060] with (2- 14 C) Determination of the inhibitory activity of noricariin on cellular lipid production by acetate incorporation assay

[0061] After treatment of LnCAP cells with different concentrations of noricariin for 5 h or 24 h, 2- 14 C-labeled acetate (57 mCi / mmol; 2 μCi / dish; Amersham Biosciences) was added to LnCAP cell culture medium. After 4 hours of incubation, cells and medium were collected, and the cells collected by centrifugation were resuspended in 0.8 ml of PBS. Lipids were extracted using the Bligh Dyer method (Swinnen J.V. et al., Endocrinology, 1996; 137: 4468-4474), and scintillation counting was used to quantify (2- 14 C) Acetate incorporation. The results obtained were normalized to the sample protein content. Figure 1 shows the lipid production-noricariin concentration curve of LnCAP cells treated with noricariin.

Embodiment 3

[0063] Experiment on the inhibition of fatty acid synthase activity of LnCAP cell extract by noricaridin

[0064] FAS enzymatic activity was determined using LnCAP cellular protein extracts (Brusselmans K. et al., JBiol Chem, 2005 Feb 18;280(7):5636-5645). LnCAP cells were harvested by centrifugation, resuspended in hypotonic buffer (1 mM EDTA, 20 mM Tris-HCl, pH 7.5), and then the protein content of the samples was determined using the BCA method (Pierce). Equal amounts of protein (50 μg) and different concentrations of noricaridin (0.03-30 μM) were placed in 2.5 ml of phosphate buffer (100 mM, pH 7.0) and pre-incubated at 37° C. for 30 minutes. Then 20 μl of reaction solution [2.5 mM NADPH, 1.25 mM acetyl-CoA, 1.25 mM malonyl-CoA, 0.02 mM [2- 14 C]malonyl-CoA (60mCi / mmol; PerkinElmer Life Sciences)], incubate at 37°C for another 15 minutes, add 3ml of ice-cold 1M hydrochloric acid / methanol mixture (6:4, v / v) to stop the reaction, and use petroleum Ether-extracted fatty aci...

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Abstract

Disclosed is an anti-tumor drug with nor-icariin as the effective ingredient. Pharmacological test effect proves that the nor-icariin has the activity to inhibit the production of cellular lipid, can reduce the production of cellular fatty acid by inhibiting the activity of FAS, has a function of inhibiting the production and causing withering of microvascular endothelial cells, shows a broad-spectrum anti-tumor function in a cytotoxicity test of thirty-three tumor cell strains of a human body, and shows a function in strongly inhibiting the production of tumor, such as prostate cancer cells LnCAP, lung cancer cells NCI-H23 and colon cancer cells HCT-116 of a human body in a tumor transplantation nude mice model test. A pharmacokinetics test of the nor-icariin in the body of a little mouse proves that the nor-icariin can be kept with a certain concentration, good for better anti-humor effect. The acute toxicity test of the nor-icariin in the body of the mouse shows nontoxicity; therefore the nor-icariin is proved to be a newly-developed broad spectrum anti-humor drug with broad development prospect.

Description

technical field [0001] The present invention relates to an antitumor drug, in particular to an antitumor drug with noricariin as an active ingredient. Background technique [0002] Commonly found in Asia and the Mediterranean region, Epimedium is a spicy ornamental herb. Epimedium is called epimedium in English because of its resemblance to a plant in the ancient Asian kingdom of Media (now part of Iran). Epimedium is a genus that includes a variety of related plants, some of which have been used medicinally, including Epimedium sagittae, Epimedium berberi, Epimedium grandiflorum, and Epimedium korea. Epimedium is an important traditional Chinese herbal medicine widely used in China, Japan and Korea as a tonic and anti-rheumatic medicine, and has been shown to be effective in the treatment of osteoporosis, cardiovascular disease and tumors. [0003] Icariin (ICA) (molecular weight 676), a flavonol glycoside, is the main component of Epimedium serrata. Icariin is a novel b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 张南殷正丰
Owner 殷正丰
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