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Novel limonin compound as well as preparation method and medical application thereof

A compound and drug technology, applied in the field of limonoid compounds and their preparation, can solve problems such as photosensitivity, skin adverse reactions, and phototoxicity

Inactive Publication Date: 2015-12-30
ZIBO KUAKE MEDICINE TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furanocoumarins also have photosensitizing, phototoxic and mutagenic effects, which can cause skin adverse reactions

Method used

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  • Novel limonin compound as well as preparation method and medical application thereof
  • Novel limonin compound as well as preparation method and medical application thereof
  • Novel limonin compound as well as preparation method and medical application 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 herb of rue (10kg), extract with 80% ethanol under heat reflux (25L×3 times), combine the extracts, concentrate until 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 (431g) and n-butanol extract respectively; (b) In the step (a), the ethyl acetate extract is removed with AB-8 type macroporous resin, first eluted with 10% ethanol for 8 column volumes, then with 75% ethanol for 10 column volumes, and co...

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 novel limonin compound as well as a preparation method and medical application thereof. The compound is reported for the first time, is a limonin compound with a novel structure, and can be extracted, separated and purified from the dried whole herb of Grace. In vitro tests prove that the compound can inhibit the proliferation of gastric carcinoma cells, and promote the apoptosis of the cells, and the growth inhibiting effect on the gastric carcinoma cells is strengthened gradually along with the increase of concentration, these findings provide a basis for a clinical research of drug of the compound (I) for curing gastric carcinoma, and the compound can be developed into a drug for curing the gastric carcinoma.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a limonoid compound with the effect of treating gastric cancer isolated from dried rue herb and a preparation method thereof. Background technique [0002] Rutagarveolens L., also known as seven lixiang, vanilla, rue grass, small lemon grass, wild rue herb, lime grass, stinky grass, is a perennial herb of Rutaceae. The whole plant is used for medicinal purposes. It is widely cultivated for medicinal purposes in many parts of the world. It can be harvested throughout the year, washed and dried in the shade or used fresh. Pungent, slightly bitter, cool. Heat-clearing and toxic substances removing, blood stasis dispelling and pain relieving. Used for cold and fever, toothache, irregular menstruation, and eczema in children; externally used to treat sores, furuncles, swollen toxins, and traumatic injuries. [0003] Modern research shows that the plant contains compou...

Claims

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Application Information

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IPC IPC(8): C07D307/54A61K31/341A61P35/00A61P1/00
CPCC07D307/54
Inventor 高忠青
Owner ZIBO KUAKE MEDICINE TECH
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