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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 the problems of few literature reports on pharmacological activity research and the like

Inactive Publication Date: 2015-12-02
HANGZHOU QICHENG TECH CO LTD
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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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  • 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

[0022] Example 1: Compound (I) isolation preparation and structure confirmation

[0023] Reagent sources: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane are of analytical grade, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd., methanol, of analytical grade, purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0024] Preparation method: (a) Crush the dried roots (10kg) of Dongfeng orange, extract with 75% ethanol under reflux (25L×3 times), combine the extracts, concentrate to no alcohol (3L), and use petroleum ether (3L) in turn ×3 times), ethyl acetate (3L×3 times) and water-saturated n-butanol (3L×3 times) to obtain petroleum ether extract, ethyl acetate extract (378g) and n-butanol extract respectively; (B) In step (a), the ethyl acetate extract is removed with AB-8 macroporous resin, first eluted with 10% ethanol for 8 column volumes, and then eluted with 75% ethanol for 8 column volumes, and collected 75 % Ethanol eluate, concentrat...

Embodiment 2

[0026] Example 2: Compound (I) Pharmacological Action Test

[0027] 1. Materials and Instruments

[0028] The HL7702 liver cell line was provided by the Shanghai Institute of Biological Sciences, Chinese Academy of Sciences. Compound (I) is self-made, the method is shown in Example 1, and the HPLC normalized purity is greater than 98%. High glucose DMEM medium, high glucose DMEM / F12=1:1 medium, and fetal bovine serum were all purchased from HycLone. EDTA was purchased from Shanghai No. 1 Reagent Factory. Trypan Blue was purchased from Beijing Chemical Plant. Sugar-free DMEM medium was purchased from Gibco. Pancreatin, MTT and DMSO were all purchased from Amresco. The LDH release method detection kit was purchased from GENMDE. The ALT biochemical test kit, AST biochemical test kit, and LDH biochemical test kit were all purchased from Beckman Reagent Co., Ltd. of the United States. Western and IP cell lysate, PMSF, BCA protein concentration determination kit, MDA detection kit...

Embodiment 3

[0085] Preparation of tablets: According to the method in Example 1, compound (I) is first prepared, and the salt is made with organic acid such as tartaric acid, or citric acid, formic acid, or oxalic acid, and inorganic acid such as hydrochloric acid or sulfuric acid or phosphoric acid. The weight ratio of the excipient to the excipient is 1:9, and the excipient is added for granulation and tableting.

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Abstract

The invention discloses a novel limonin compound as well as a preparation method and a medical application thereof. The compound which is reported for the first time is a limonin compound having a novel structure and can be obtained by extracting, separating and purifying from dried roots of attalanteae buxifoliae. In-vitro experiments prove that the compound has the capabilities of reducing ischemia reperfusion injury of human hepatocytes and playing a role of hepatic cell protection and can be used for being developed into medicaments for protecting the liver.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a limonoid compound with a liver-protecting effect isolated from the dried root of Dongfeng orange and a preparation method thereof. Background technique [0002] Dongfeng Orange Atalantia buxifolia (Poir).Oliv. is a plant of the Rutaceae wine cake genus. It was first recorded in "Lingnan Herb Collection", and is currently included in the "National Chinese Herbal Medicine Compilation" and "Ministry of Health Drug Standards". 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 reducing phlegm, relieving cough, and relieving asthma. As a kind of folk med...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00A61K31/58A61P1/16
Inventor 叶澄
Owner HANGZHOU QICHENG TECH CO LTD
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