Antineoplastic medicine composition and application thereof

A technology for anti-tumor drugs and compositions, which can be used in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., and can solve problems such as no compounds

Inactive Publication Date: 2009-09-16
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] So far, compound 1 (5,17,20-triacetyl-ingen-3-angelate) and compound 2 (5,20-diacetyl-ingen-3- -Angelate) has anti-tumor efficacy reports

Method used

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  • Antineoplastic medicine composition and application thereof
  • Antineoplastic medicine composition and application thereof
  • Antineoplastic medicine composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1. Compound 1 (5,17,20-triacetyl-ingen-3-angelate) and compound 2 (5,20-diacetyl-ingen-3-angelate) preparation:

[0036] Take 10Kg (dry weight) of the above-ground part of Euphorbiaceae Euphorbia plant Bawangbian, crush it, extract it with 70% acetone water (20L×3), concentrate it under reduced pressure to a total volume of 2L, and extract it with ethyl acetate (2L×3) Finally, the ethyl acetate part was decolorized through an MCI column to obtain 120 g of medicinal extract. Eluted by silica gel column chromatography (petroleum ether-Me 2 CO=1:0~1:1) was divided into 5 parts A-E; part A was further separated by silica gel column chromatography (petroleumether-Me 2 CO=100:1) to obtain a total of 4 parts a-d; continue to use HPLC (Agilent1200HPLC system; Zorbax SB-C18, 250×9.4) to purify, part c was separated with 76% methanol and water to obtain 5,17,20-triacetyl - Ingen-3-angelate (3 mg).

[0037] Take 10Kg (dry weight) of the above-ground part of Euphorbiaceae Eupho...

Embodiment 2

[0045] Compound 1 (5,17,20-triacetyl-ingen-3-angelate) and compound 2 (5,20-diacetyl-ingen-3-angelate) on mice The impact of spontaneous metastasis of Lewis lung cancer:

[0046] Lewis lung cancer cell line was made into tumor cell suspension, and the trypan blue count was about 1×10 7 / mL tumor cells. Disinfect the right anterior armpit of the mouse, take 0.2mL (about 1×10 6 -2×10 6 Tumor cells) were inoculated subcutaneously. Passage 3 times. The subcutaneous tumor mass of Lewis lung cancer tumor-bearing mice was peeled off under sterile conditions, and the well-grown tumor tissue was selected, cut into pieces, weighed, made into a homogenate with a cell homogenizer, and added with normal saline at a volume ratio of 1:3 to make a tumor The cell suspension was inoculated subcutaneously in the armpit of the right forelimb of C57BL / 6J mice, each 0.2mL (about 1×10 6 ~2×10 6 tumor cells). The next day randomized grouping, compound 1 (5,17,20-triacetyl-ingen-3-angelate) an...

Embodiment 3

[0052] The effects of compound 1 (5,17,20-triacetyl-ingen-3-angelate) and compound 2 (5,20-diacetyl-ingen-3-angelate) on neovascularization generated inhibition

[0053] When the fertilized eggs of TG (VEGFR2:GFP) vascular fluorescence transgenic zebrafish were developed for 24 hours, normal zebrafish embryos were selected under a stereoscope and transferred to a 96-well culture plate, one embryo per well. Add a certain volume of medicine to the sample wells in advance, 32 wells per concentration, and then supplement the volume with nutrient water to 300 μl, and the control is embryo nutrient water. At 72 hours of fertilized egg development, the growth of zebrafish intersegmental blood vessels was observed with a fluorescence microscope, the inhibition rate was calculated, and the death of embryos or larvae was observed.

[0054] The vascular development process of zebrafish embryos is very similar to that of humans. The branches of the main blood vessels on the back of the z...

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Abstract

The invention provides a medicine composition with a compound 1 (5, 17, 20-trivinyl-ingenane-3-angelate) and a compound 2 (5, 20-diacetyl-ingenane-3-angelate) shown in formula (1) as active ingredients and an application thereof in preparing medicine for treating or preventing and controlling tumor diseases; when R is equal to OAc, the compound 1 is 5, 17, 20-trivinyl-ingenane-3-angelate; when R is equal to H, the compound 2 is 5, 20-diacetyl-ingenane-3-angelate.

Description

technical field [0001] The present invention relates to the field of pharmaceutical compounds and pharmacy, specifically, compound 1 (5,17,20-triacetyl-ingenine-3-angelate) and compound 2 (5,20-diacetyl- Ingenue-3-angelate) is a pharmaceutical composition as an active ingredient, and its application in the preparation of medicines for treating or preventing tumor diseases. Background technique [0002] Angiogenesis is considered an absolute requirement for the growth of tumors larger than 1–2 mm. In tumors smaller than this limit, oxygen and nutrients can be delivered to the cells by diffusion. However, when a certain size is reached, each tumor is dependent on angiogenesis in order to continue growing. Tumor-initiating cells in hypoxic areas respond by stimulating VEGF production, which causes activation of resting endothelial cells to stimulate new blood vessel formation. Furthermore, VEGF in tumor areas without any angiogenesis can proceed through the ras signaling pat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/22C07C69/533A61K36/47A61P35/00
Inventor 李晓莉杨永平李阳韩利文王思锋刘可春
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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