New conjugate stilbene compound, and preparation method and medicinal use thereof

A compound and composition technology, applied in the field of conjugated stilbene compounds and their preparation, can solve the problems of remarkable anticancer activity and the like

Inactive Publication Date: 2016-05-11
吴金凤
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Zygonia is a traditional Chinese medicine in my country, rich in resources, in which the content of triterpenoid saponins is high, the structure is novel and complex, and the anticancer activity is remarkable

Method used

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  • New conjugate stilbene compound, and preparation method and medicinal use thereof
  • New conjugate stilbene compound, and preparation method and medicinal use thereof
  • New conjugate stilbene compound, and preparation method and medicinal use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0022] Sources of reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane were of analytical grade, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, of analytical grade, were purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0023] Preparation method: (a) Grind the dried whole grass (8kg) of Zygonia chinensis, extract with 85% ethanol under heat reflux (25L×3 times), combine the extracts, concentrate to no alcohol smell (3L), and successively add petroleum ether ( 3L×3 times), ethyl acetate (3L×3 times) and water-saturated n-butanol (3L×3 times) were extracted to obtain petroleum ether extract, ethyl acetate extract (347g) and n-butanol extract (b) In the step (a), the ethyl acetate extract is removed with AB-8 type macroporous resin, and first eluted with 15% ethanol for 8 column volumes, then with 75% ethanol for 12 column volumes, and c...

Embodiment 2

[0025] Embodiment 2: compound (I) pharmacological action test

[0026] 1. Materials and Instruments

[0027] Human gastric cancer cell line SGC-7901 was purchased from Purcell Reagent Company. Compound (I) is self-made, and the HPLC normalized purity is greater than 98%. PDTC, trypsin, MTT, dimethyl sulfoxide (DMSO), agarose, and glacial acetic acid were purchased from Sigma, USA. RPMI-1640 medium and PBS phosphate buffer solution were purchased from GIBCO, USA. Fetal bovine serum was purchased from Shandong Yinxiang Weiye Company. Trypan blue (Beijing Zhongshan Jinqiao Biotechnology Co., Ltd.), TUNEL kit (Kage Biotechnology Development Co., Ltd.), DAB chromogenic kit (Beijing Zhongshan Jinqiao Biology Co., Ltd.), formaldehyde (Fisher, USA), catalase (Tianjin Tianxin Fine Chemical Development Center).

[0028] WD-9403C UV Analyzer (Biometra, Germany), Gradient PCR (Biometra, Germany), Gel Imaging Analysis System (Shanghai Tianneng Company), Electrophoresis Instrument (Bei...

Embodiment 3

[0060] 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 to the excipient is 1:9, and the excipient is granulated and compressed into tablets.

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PUM

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Abstract

The invention discloses a new conjugate stilbene compound, and a preparation method and a medicinal use thereof. The compound is reported for the first time, is a conjugate stilbene compound with a novel structure, and can be obtained through extracting dry herb of Actinostemma tenerum Griff., separating and purifying. In vitro test proves that the compound can inhibit proliferation of gastric cancer cells and promote cell apoptosis, has an increasing trend in the gastric cancer cell growth inhibition with the increase of the concentration, and can be used to exploit gastric cancer treatment medicines.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a conjugated stilbene compound isolated from the dried whole herb of Zygmus chinensis and capable of treating gastric cancer and a preparation method thereof. Background technique [0002] Actinostemmalobatum Maxim. is a plant of the genus Boxgrass of Cucurbitaceae, also known as Celestial Grass and White Grass. Annual climbing herb. Leaves narrowly triangular or triangular heart-shaped, panicles axillary, flowers small, unisexual, monoecious. Corolla yellow-green, lobes triangular-lanceolate. Capsule ovoid, green, drooping, with spiny protrusions, upper part cracked when ripe. Seeds 2, gray. The flowering period is from July to August. The fruiting period is from September to October. The medicinal parts are the whole plant, seeds and leaves, which are distributed in the north and south of my country, and also in Korea, Japan, the Soviet Union, India, and the...

Claims

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Application Information

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IPC IPC(8): C07C43/23C07C41/34A61P35/00
CPCC07C43/23C07C41/34
Inventor 吴金凤
Owner 吴金凤
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