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Medicinal application of 15-benzyl subunit-1 4-deoxy-11,12-dehydrogenation andrographolide derivative

A technology of andrographolide and derivatives is applied in the field of medicine to achieve the effect of expanding the range of options and clarifying the anti-tumor activity

Active Publication Date: 2012-06-06
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the structural modification of the above research work is mainly at C-3, C-14 and C-19 hydroxyl, D 8 、D 12 isotopic double bond

Method used

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  • Medicinal application of 15-benzyl subunit-1 4-deoxy-11,12-dehydrogenation andrographolide derivative
  • Medicinal application of 15-benzyl subunit-1 4-deoxy-11,12-dehydrogenation andrographolide derivative
  • Medicinal application of 15-benzyl subunit-1 4-deoxy-11,12-dehydrogenation andrographolide derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Inhibition of tumor cell clone formation

[0019] 1.1 Materials and methods

[0020] 1) Cell lines: gastric cancer cell line SGC7901, lung cancer cell line A549 and cervical cancer cell line Hela were purchased from Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences.

[0021] 2) Reagents and equipment: RPMI1640 medium, DMEM high glucose medium and trypsin are all GIBICO products. Standard fetal bovine serum (FBS) was purchased from Tianjin Haoyang Biological Products Technology Co., Ltd.; mycoplasma-free fetal bovine serum (FCS) was purchased from Hangzhou Sijiqing Bioengineering Materials Co., Ltd. Andrographolide (1) and andrographolide derivatives (2, 4, 5, 6, 7) synthesized by the present invention were provided by the New Drug Research and Development Center of Zhengzhou University. CO 2 Incubator (German Binder company CB150 type); inverted microscope (Japanese Nikon company TS100-F-PH type). 6-well plates were purchased from Co...

Embodiment 2

[0028] Example 2 Inhibition of Tumor Cell Migration

[0029] 2.1 Materials and methods

[0030] 1) Cell lines: human bladder cancer 5637, human esophageal cancer Ec109, and human colon cancer HT-29 were purchased from Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences

[0031] 2) Reagents and equipment: same as Example 1.

[0032] 3) Test method: Digest conventionally cultured cells with trypsin, spread in a 96-well plate after suspension and dilution, 200 cells per well . After culturing to a confluent monolayer state, replace it with a medium containing 1% serum, and then streak it after 12 hours of synchronous culture, wash it twice with PBS, take pictures under a microscope immediately after adding the drug, and measure the scratch distance. Drug concentrations were 2.50, 5.00, 10.00 , four wells were repeated and a vehicle control was set. After culturing for 24 hours, they were photographed and measured under a microscope, and the migration i...

Embodiment 3

[0035] Example 3 Anti-angiogenic effect

[0036] 3.1 Materials and methods

[0037] 1) Two-dimensional migration of anti-ECV304 (same as Example 2)

[0038] 2) Three-dimensional migration of anti-ECV304

[0039] Serum-free medium was first added to the upper and lower chambers of the Transwell chamber, and placed in a 37°C incubator for 1 hour; human vascular endothelial cells ECV304 (purchased from the Type Culture Collection Center of the Chinese Academy of Sciences) cultured to 80-90% were digested, Resuspend in medium containing 10% fetal bovine serum, adjust cell concentration to 1x10 6 / mL; Take out the medium in the upper and lower chambers of the Transwell chamber, add the above cell solution to the upper chamber, 100 / hole; add 600 to the lower chamber Medium containing 10% serum at 37°C, 5% CO 2 After culturing in the incubator for 2 hours, replace the medium in the upper chamber with serum-free or drug-containing serum-free medium, set 3 replicate wells in ea...

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Abstract

The invention belongs to the technical field of medicine, discloses the application of andrographolide derivative in preparation antineoplastic agents, and relates to 15-benzyl subunit -14-deoxy-11,12-dehydrogenation andrographolide derivative and 3,19 esters thereof. The experience shows that the chemical compounds have the remarkable effects of restraining cancer cell cloning and forming and resisting migration of cancer cell and human vascular endothelial; and the chemical compounds show stronger effects of restraining tumor growth, antimetastasis and antiangiogenic in a mice transplantingtumour animal model. The chemical compounds are used as activity components for preparing antineoplastic agents, have the advantages of high efficient and low toxicity. the invention provides a new drug way for curing and preventing transfer of the tumour, expands selection range of clinical pharmacy, and is significant to taking full advantage of plant resources of the common andrographis herb.

Description

technical field [0001] The invention relates to the medicinal use of andrographolide derivatives, in particular to 15-benzylidene-14-deoxy-11,12-dehydroandrographolide derivatives and their 3,19 esters, belonging to the technical field of medicine. Background technique [0002] In recent years, due to intensified competition in modern society, increased living pressure, serious environmental pollution and other factors, the incidence and mortality of malignant tumors have remained high, and it has become the second "killer disease" that seriously threatens human health. The development of anti-tumor drugs will benefit mankind and is of great significance. [0003] Andrographolide is a diterpene lactone compound extracted from Andrographis paniculata (Burm. f.) Nees, a plant of the Acanthaceae family. It is one of the main active ingredients of the traditional Chinese medicine Andrographis paniculata. It has antipyretic, anti-inflammatory, Antibacterial, antiviral and other ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61K31/443A61P35/00
CPCC07D307/33A61K31/341A61K31/365A61K45/06A61P1/00A61P1/16A61P11/00A61P13/08A61P13/10A61P15/00A61P17/00A61P35/00A61P35/04
Inventor 戴桂馥徐海伟刘宏民董瑞静闫丽君朱丽平李伟义蒋志雯王亚楠巫凤娟
Owner ZHENGZHOU UNIV
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