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Callicarpa nudiflora extract, diterpene compound and application of pharmaceutical composition to preparation of medicines for treating gliomas

A technology of glioma, naked flower purple pearl, applied in the field of medicine

Inactive Publication Date: 2016-06-08
WENZHOU TONGYI BIOMEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In recent years, there have been few domestic and foreign research reports on the chemical constituents of Auranthus nudica, and the main constituents isolated from it are flavonoids, terpenes, volatile oils and phenols, etc.

Method used

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  • Callicarpa nudiflora extract, diterpene compound and application of pharmaceutical composition to preparation of medicines for treating gliomas
  • Callicarpa nudiflora extract, diterpene compound and application of pharmaceutical composition to preparation of medicines for treating gliomas
  • Callicarpa nudiflora extract, diterpene compound and application of pharmaceutical composition to preparation of medicines for treating gliomas

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the application of a kind of Nadiflora purple pearl extract in the preparation of the medicine for the treatment of glioma,

[0032] Nude flower purple pearl extract is obtained by separating and extracting the aerial parts of nude flower purple pearl. The extraction steps include:

[0033] (a) Dry and pulverize the aerial part of Auranthus nudica, extract with ethanol under hot reflux, combine the extracts, concentrate until there is no alcohol smell, extract with petroleum ether, ethyl acetate and water-saturated n-butanol in sequence, respectively to obtain Petroleum ether extract, ethyl acetate extract and n-butanol extract;

[0034] (b) Take the n-butanol extract to remove impurities, first elute with 10% ethanol for 6 column volumes, then use 70% ethanol for 8 column volumes, collect the 70% ethanol eluate, and concentrate under reduced pressure to obtain 70% ethanol elution concentrate;

[0035] (c) The concentrate eluted with 70% ethanol in step ...

Embodiment 2

[0037] Example 2: The application of diterpene compound (I) in the preparation of drugs for the treatment of glioma, the separation, preparation and structural confirmation of diterpene compound (I) are as follows:

[0038] (a) The dry aerial part (10kg) of Auranthus nudiflora is pulverized, extracted with 75% ethanol under heat reflux (25L×3 times), the extracts are combined, concentrated to no alcohol smell (6L), and then washed with petroleum ether (6L×3 times) 3 times), ethyl acetate (6L × 3 times) and water-saturated n-butanol (6L × 3 times) were extracted to obtain petroleum ether extract, ethyl acetate extract (377g) and n-butanol extract respectively; ( b) The ethyl acetate extract in step (a) is removed with AB-8 macroporous resin, first eluted with 10% ethanol for 6 column volumes, then with 70% ethanol for 8 column volumes, and collected 70% ethanol Dehydration, concentrated under reduced pressure to obtain 70% ethanol elution concentrate (129g); (c) 70% ethanol elu...

Embodiment 3

[0040] Embodiment 3: compound (I) pharmacological action test

[0041] 1. Materials and Instruments

[0042] In this experiment, the human brain malignant glioblastoma U251 cell line was purchased from the American Type Culture Collection. DMEM high-glucose medium was purchased from Hyclone Company of the United States; sodium chloride, sodium hydroxide, potassium chloride, oxygen chloride, sodium hydroxide, disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, and methanol were purchased from Nanjing chemical plant. Compound (I) is self-made, and the HPLC normalized purity is greater than 98%. Glycine, Tris, Tween20, and dimethyl sulfoxide (DMEM) were purchased from Sigma, USA; Aimexin-V / PI cell death kit was purchased from Invitrogen, USA; cell lysate, 0.25% trypsin, CellCountingKit-8 kit , penicillin, streptomycin, Hoechst33258, nuclear dye DAPI, PMSF, Westernblot gel preparation kit, nuclear protein extraction kit, Coomassie brilliant...

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a callicarpa nudiflora extract or a diterpene compound separated from an overground part of callicarpa nudiflora and medical application of pharmaceutical composition prepared from the callicarpa nudiflora extract and the diterpene compound to preparation of medicines for treating gliomas. According to in-vitro tests, the callicarpa nudiflora extract and the diterpene compound can play a role in inhibition of human brain malignant spongioblastoma U251 cells by inhibition of cell proliferation and induction of cell apoptosis and can be used for development of the medicines for treating the gliomas.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to extracts or diterpenoids isolated from the aerial parts of Auranthus nudica, and pharmaceutical compositions prepared from them in the preparation of drugs for treating glioma. medicinal use in. Background technique [0002] Callicarpanudiflora Hook.etArn. is a plant of the genus Verbenaceae. It grows in hillsides, roadsides, valleys, streams or shrubs from plains to 1200m above sea level. The annual average temperature is 15-25°C and the humidity is high. It grows well in the environment. It is mainly distributed in Guangdong, Guangxi, Hainan and other places in China. It is produced in Ding'an, Danzhou, Chengmai, Baisha, Changjiang, Dongfang, Sanya, Lingshui, Baoting, Qiongzhong and other places in Hainan, among which Hainan Wuzhishan is the top grade; foreign countries are mainly distributed in India, Indochina Peninsula, Malay Peninsula and Singapore. [0003]...

Claims

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Application Information

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IPC IPC(8): C07D493/08A61K31/343A61K36/85A61P35/00
CPCC07D493/08A61K36/85A61K2236/333A61K2236/35A61K2236/51
Inventor 王赛波
Owner WENZHOU TONGYI BIOMEDICAL TECH CO LTD
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