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A kind of aaptamine alkaloid compound extracted from the sponge and its application in the preparation of antitumor drugs

A technology of alkaloids and compounds, applied in antitumor drugs, drug combinations, organic chemistry, etc., to achieve significant antitumor activity and simple preparation methods

Inactive Publication Date: 2016-08-24
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, no aaptamine alkaloid C with antitumor activity has been isolated from this genus of sponges so far. 16 h 17 N 3 o 2 report

Method used

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  • A kind of aaptamine alkaloid compound extracted from the sponge and its application in the preparation of antitumor drugs
  • A kind of aaptamine alkaloid compound extracted from the sponge and its application in the preparation of antitumor drugs
  • A kind of aaptamine alkaloid compound extracted from the sponge and its application in the preparation of antitumor drugs

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Embodiment 1

[0027] Embodiment 1. Preparation of compounds of the present invention

[0028] 1. Prepare dichloromethane crude extract

[0029] Take 2.3 kg of dry and pulverized sponge sponge, use 15 L of 95% ethanol to percolate and extract 4 times, each time for 3 days, combine the extracts, concentrate the extracts under reduced pressure to obtain extracts, and extract with dichloromethane solution to obtain dichloromethane For the total extract of dichloromethane, suspend the total extract of dichloromethane with 90% methanol, degrease with n-hexane, add water to adjust the methanol concentration of the suspension to 60%, extract 3 times with dichloromethane, and concentrate the extract Obtain 84.4g of dichloromethane crude extract;

[0030] 2. Separation and purification

[0031] 1) Separation and purification: the crude dichloromethane extract was subjected to VLC decompression column chromatography, and methanol:dichloromethane=100:1, 80:1, 60:1, 50:1, 30:1, 20:1, 10:1, 8:1, 5:1, ...

Embodiment 2

[0040] Embodiment 2 The in vitro antitumor activity experiment of the compound of the present invention:

[0041] For compound C of the present invention 14 h 13 N 3 o 3 In vitro anti-tumor experiments were carried out, and the tumor cell lines used were as follows:

[0042] Human acute leukemia cell HL60 (HL60), purchased from ATCC, ATCC number is CCL-240;

[0043] Human chronic leukemia cell K562 (K562), purchased from ATCC, ATCC number is CCL-243;

[0044] Human breast cancer cell MCF-7 (MCF-7), purchased from ATCC, ATCC number is HTB-22;

[0045] Human nasopharyngeal carcinoma cell line KB (KB), purchased from ATCC, ATCC number is CCL-17;

[0046] Human liver cancer Hep G2 (Hep G2), purchased from ATCC, ATCC number is HB-8065;

[0047] Human colon cancer cell line HT-29 (HT-29), purchased from ATCC, ATCC number is HTB-38.

[0048] Human acute leukemia cells HL60 and human chronic leukemia cells K562, both cell lines were grown in suspension in RPMI-1640 medium with...

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Abstract

The invention relates to the technical field of marine organisms and medicines and provides an aaptamine alkaloid compound extracted, separated and purified from a marine animal aaptos originating from surrounding waters of the Xisha Islands. The chemical structure of the aaptamine alkaloid compound is shown in a formula (I) as shown in the specification. In-vitro activity tests prove that the compound has obvious inhibitory activity on various tumor cells such as human acute leukemic cells HL60, human chronic leukemic cells K562, human breast cancer cells MCF-7, human nasopharyngeal cancer cells KB, human liver cancers Hep G2, human colon cancer cells HT-29 and the like and can be used for preparing antitumor medicines.

Description

technical field [0001] The present invention relates to the technical field of marine biology and medicine, in particular to a novel alkaloid compound obtained through extraction, separation and purification from Aaptos aaptos, a marine animal sponge produced in the waters near the Xisha Islands, and its use in the preparation of antitumor drugs. in the application. Background technique [0002] The sponge is a low-level multicellular animal, which is widely distributed and often contains many secondary metabolites with rare structures and anti-tumor activities. Therefore, it has always been the first choice for marine natural product chemists to study marine organisms. [0003] The medicinal source material Aaptos aaptos of the present invention belongs to the class Demospongiae, order Hardromerida, and the family Suberitidae, and is produced in the sea near the Paracel Islands. Some alkaloid compounds have been isolated from sponges of this genus, and these alkaloid compo...

Claims

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Application Information

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IPC IPC(8): C07D471/06A61P35/00A61P35/02
CPCC07D471/06
Inventor 林厚文于豪冰杨帆焦伟华
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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