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New limonin compound, preparation method and medical uses thereof

A compound and drug technology, applied in the field of limonin compound and its preparation, can solve the problem of few literature reports on pharmacological activity research

Inactive Publication Date: 2016-01-13
徐建立
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Hainan, Guangxi, Guangdong, Fujian and other places have always used Dongfengju to treat acute and chronic bronchitis, and achieved good clinical results, but there are relatively few literature reports on the pharmacological activity of this product

Method used

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  • New limonin compound, preparation method and medical uses thereof
  • New limonin compound, preparation method and medical uses thereof
  • New limonin compound, preparation method and medical uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0025] 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.

[0026] Preparation method: (a) The dried root (8kg) of Dongfeng orange is pulverized, extracted with 85% ethanol under heat reflux (25L×3 times), the extracts are combined, concentrated to no alcohol smell (6L), and successively washed with petroleum ether (6L× 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 (355g) and n-butanol extract respectively; ( b) In the step (a), the ethyl acetate extract is removed with AB-8 type macroporous resin, eluted with 15% ethanol (8L) and 75% (12L) ethanol successively, collect...

Embodiment 2

[0028] Embodiment 2: compound (I) pharmacological action test

[0029] 1. Materials and Instruments

[0030] Vascular endothelial cells (ECV-304) were donated by the Department of Immunology, School of Medicine, Shandong University. Compound (I) is self-made, the preparation method is shown in Example 1, and the HPLC normalized purity is greater than 98%. RPMI-1640 dry powder medium and trypsin were purchased from Gibeo, USA. Fetal bovine serum was purchased from Tianjin TBD Company. MTT, agarose, and AnnexinV-FITC were purchased from Sigma, USA. LDH, MDA, SOD, GSH-Px assay kits were purchased from Nanjing Jiancheng Bioengineering Institute. DMSO was purchased from China Pharmaceutical (Group) Shanghai Chemical Reagent Co., Ltd. Hematoxylin was purchased from Fuzhou Maixin Biotechnology Co., Ltd. Rhodamine123 was purchased from Solarbic Corporation of the United States. The positive drug ligustrazine was purchased from Shanghai Yuanye Biotechnology Co., Ltd.

[0031] I...

Embodiment 3

[0067] 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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Abstract

The present invention discloses a new limonin compound, a preparation method and medical uses thereof. According to the present invention, the compound is firstly reported, is the limonin compound having a novel structure, and can be obtained by extracting the dried root of Atalantia buxifolia(Poir.)Oliv and carrying out separation purification; the in vitro test results prove that the compound provides protection effects for H2O2 oxidative injury ECV-304 cells; and the determination results of the MDA content, the SOD activity and the GSH-Px activity of the cell supernatant prove that the compound (I) has free radical and reactive oxygen scavenging anti-oxidation property, and can be used for developing blood vessel protection drugs.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a limonoid compound with blood vessel protection effect isolated from the dry root of Dongfeng orange and a preparation method thereof. Background technique [0002] Dongfengju Atalantiabuxifolia (Poir).Oliv. is a plant of the Rutaceae wine cake genus, which was first recorded in "Lingnan Herb Collection", and is currently an appendix to the third volume of traditional Chinese medicine preparations in "National Compilation of Chinese Herbal Medicine" and "Drug Standards of the Ministry of Health" load. The medicinal roots and rhizomes of Dongfeng orange are pungent, bitter, and slightly warm in nature, and return to the lung, stomach, and spleen meridian. Hainan, Guangxi, Guangdong, Fujian and other places have always used this product to treat acute and chronic bronchitis, and the clinical effect is good. In addition, studies have shown that it has good effects on...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00A61K31/58A61P9/14
Inventor 徐建立
Owner 徐建立
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