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Medicinal diterpenoid compound and preparation method thereof

A kind of compound, technology of diterpenes, applied in the field of diterpenoids and preparation thereof

Inactive Publication Date: 2016-06-22
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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  • Medicinal diterpenoid compound and preparation method thereof
  • Medicinal diterpenoid compound and preparation method thereof
  • Medicinal diterpenoid compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0021] (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 Deliquidation, concentrated under reduced pressure to obtain 70% ethanol elution concentrate (129g); (c) 70% ethanol elution concentrate in step (b) was separated with normal phase silica gel, and the volume ratio was 40:1 (8 column volume), 20:1 (8 c...

Embodiment 2

[0023] Embodiment 2: compound (I) pharmacological action test

[0024] 1. Materials and Instruments

[0025] 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...

Embodiment 3

[0049] Preparation of tablets: firstly prepare compound (I) according to the method of Example 1, and utilize organic acids such as tartaric acid, or citric acid, formic acid or oxalic acid, etc., inorganic acids such as hydrochloric acid or sulfuric acid or phosphoric acid to make salts, according to its The weight ratio of the excipient is 1:7, and the excipient is granulated and compressed into tablets.

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PUM

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Abstract

The invention relates to a medicinal diterpenoid compound separated from dried aerial parts of Callicarpa nudiflora and a preparation method of the compound. The diterpenoid compound is reported for the first time, adopts a novel structure, and can be obtained through extraction from the dried aerial parts of the Callicarpa nudiflora, separation and purification. In-vitro tests prove that the compound plays a role in inhibiting human brain glioblastoma U251 cells by inhibiting cell proliferation and inducing cell apoptosis and can be developed into drugs for treating neuroglioma.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a diterpene compound isolated from the dry aerial parts of Auranthus nudica and a preparation method thereof. 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] The medicinal part of naked flower purple pearl is the dry part above the ground. It ...

Claims

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Application Information

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IPC IPC(8): C07D493/08A61K31/343A61P35/00
CPCC07D493/08
Inventor 王赛波
Owner WENZHOU TONGYI BIOMEDICAL TECH CO LTD
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