New type natural active compound for anti tumor, preparation method, and application

A technology of anti-tumor activity and compounds, applied in the field of medicine, can solve the problems that tumors have not been further studied and the active ingredients are not clear, and achieve good anti-multidrug resistance, simple, safe and easy preparation methods, and high selectivity Effect

Inactive Publication Date: 2007-10-10
深圳市国盛源药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Myrica rubra mainly contains natural compounds such as metacyclic diarylheptane, flavonoids and triterpenes, but its active ingredients are not clear, and whether it has the effect of inhibiting tumors has not been further studied

Method used

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  • New type natural active compound for anti tumor, preparation method, and application
  • New type natural active compound for anti tumor, preparation method, and application
  • New type natural active compound for anti tumor, preparation method, and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 30Kg (dry weight) of the whole plant of Myrica rubra is crushed and extracted with 95% ethanol (50L × 3 times), concentrated under reduced pressure to obtain 1680g of total extract. The total extract was dissolved in 3.0L of warm water at about 40-60°C, cooled, extracted with chloroform (1.0L x 10 times), concentrated under reduced pressure to obtain 250g of chloroform partial extract. Part of the chloroform extract was subjected to silica gel column chromatography, petroleum ether (60-90°C)-acetone (petroleum ether, 50:1, 20:1, 10:1, 5:1, 2:1, acetone) gradient elution, Divided into 9 parts (TLC for detection, the same parts were combined together); Fr.4 was prepared through silica gel thin layer, the developing solvent was petroleum ether: ethyl acetate (4:1, V / V), separated and purified to obtain 250 mg of compound 1 .

[0022] Compound 1 is an orange-red oil, which reacts with 10% ethanol sulfate on a TLC silica gel thin-layer plate to appear light blue. The HRMS o...

Embodiment 2

[0034] Embodiment 2: anti-inflammatory effect of the present invention

[0035] According to the pharmacy method, the extract of the present invention can be used for preparation as medicine for enhancing body immunity or anti-inflammation.

[0036] The following pharmacological experiments show that the extract of the present invention has pharmacological activities such as enhancing immunity and anti-inflammation: 40 mice, half male and half female, with a body weight of 80-150 g, were subcutaneously injected with 0.5% 2,4-ONFB ethanol solution 100 pl via the back As an antigen to sensitize it, the sensitization was established 4 days after the injection of 2,4-DNFB, and on the 6th day, 1% 2,4-DNFB-olive oil solution was applied to the right ear of the mouse as an antigen challenge, so that the mouse developed ear fringe Contact dermatitis. They were randomly divided into 4 groups, and the bayberry extract was orally administered for 7 consecutive days from the day before t...

Embodiment 3

[0037] Embodiment 3: antitumor effect of the present invention

[0038] The survival rate of cells was detected by SRB method, and the apoptosis of cells was detected by Hoechst33258 nuclear staining method, agarose gel electrophoresis method and flow cytometry to evaluate the anti-tumor activity of compound 1.

[0039] 1. Reagent DMEM and calf serum were purchased from GIBCO BRL Company, ethidium bromide (EB) was purchased from Shanghai Sangon Company, Hoechst33258 was purchased from Sigma Company, Proteinase K (Proteinase K), 100bp DNA ladder was purchased from NEB Company, RNA Enzyme A (RNaseA) was purchased from PROMEGA Company, pyridinium iodide (PI) was purchased from Merck Company, agarose (Argarose) was purchased from BioWest Company in Spain, and other reagents were of domestic analytical grade.

[0040] 2. Instrument CO 2 Incubator, inverted microscope, fluorescence microscope, high-speed refrigerated centrifuge, horizontal electrophoresis device, gel scanning analy...

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Abstract

This invention discloses a novel natural anti-tumor compound with novel molecular frame and high anti-tumor activity. The novel natural anti-tumor compound is derived from waxmyrtle. This invention also discloses its preparation method. The method comprises: lixiviating waxmyrtle coarse powder, vacuum-concentrating, dispersing in water, extracting with an appropriate organic solvent, separating, and purifying to obtain the compound. The compound has wide applications in anti-tumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a novel natural antitumor active compound and its preparation method and application. Background technique [0002] Myrica ruba Lour (Sieb. Et Zucc.) is a plant of Myrica family Myricae. The fruit, bark, root or kernel of bayberry are all available for medicine. Its fruit is sweet and sour, warm, has the effect of promoting body fluid to quench thirst, harmonizing stomach and eliminating food, and can cure polydipsia, vomiting and diarrhea, dysentery, abdominal pain; its bark is warm in nature, bitter and astringent, can cure dysentery, bruises, toothache, soup burns Its roots are pungent and warm, have the effects of regulating qi, stopping bleeding, and removing blood stasis, and can cure stomachache, diaphragmatic food, vomiting, and hematemesis embolism; its seeds can cure beriberi. Myrica rubra mainly contains natural compounds such as metacyclic diarylheptane...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C50/34C07C46/10A61K31/122A61K36/185A61P35/00A61P29/00
Inventor 王定勇臧林泉谢启宇刘恩桂潘雪刁陈健
Owner 深圳市国盛源药业有限公司
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