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Limonin compound as well as preparation method and neuroprotective effect thereof

A neuroprotective, compound technology, applied in the direction of steroids, nervous system diseases, drug delivery, etc., can solve problems such as skin adverse reactions, phototoxicity, photosensitivity, etc.

Inactive Publication Date: 2016-04-20
吴金凤
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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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  • Limonin compound as well as preparation method and neuroprotective effect thereof
  • Limonin compound as well as preparation method and neuroprotective effect thereof
  • Limonin compound as well as preparation method and neuroprotective effect thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0024] Sources of medicinal materials and reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane are analytically pure, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, analytically pure, are purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0025] Preparation method: (a) Grind the dried whole herb of Rutacea (8kg), extract with 75% ethanol under heat reflux (25L×3 times), combine the extracts, concentrate until there is no alcohol smell (6L), and successively add petroleum ether (6L ×3 times), ethyl acetate (6L×3 times) and water-saturated n-butanol (6L×3 times) were extracted, concentrated to obtain petroleum ether extract, ethyl acetate extract (315g) and n-butanol extract (b) ethyl acetate extract in step (a) is dissolved to 2L with pure water, and medical absorbent cotton is filtered, and the filtrate is separated with AB-8 type macr...

Embodiment 2

[0027] Embodiment 2: compound (I) pharmacological action test

[0028] 1. Materials and Instruments

[0029] The PC12 cell line was donated by the Experimental Center of Anhui University of Traditional Chinese Medicine. Aβ 1-40 Protein was purchased from Sigma Company. Compound (I) is self-made, and the HPLC normalized purity is greater than 98%. DMEM / F12 medium (imported packaging was purchased from Beijing Thermo Fisher Biochemical Products Co., Ltd. NewbomCalfSerum was purchased from Beijing SolarbioScience&Technology Co., Ltd. MTT was purchased from Amresco, USA. KGI AnnexinV-FITC Cell Apoptosis Detection Kit was purchased from From Nanjing KGI Biotechnology Co., Ltd. Paraformaldehyde was purchased from China Pharmaceutical Group Chemical Reagent Co., Ltd. Bcl-2 polyclonal antibody was purchased from Wuhan Boster Biotechnology Co., Ltd. Bax polyclonal antibody was purchased from Beijing Boaosen Biotechnology Co., Ltd. Cyt-c polyclonal antibody was purchased from Wuhan ...

Embodiment 3

[0048] 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 Add the excipient at a weight ratio of 1:9, granulate and compress into tablets.

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Abstract

The invention discloses a limonin compound as well as a preparation method and a neuroprotective effect thereof, belongs to the field of drugs and in particular relates to a new limonin compound separated from dried whole herb of ruta graveolens as well as a preparation method and a medical application thereof. The compound is reported for the first time, can be obtained by extracting from the dried whole herb of ruta graveolens, separating and purifying and is high in purity. In vitro tests prove that Abeta1-40 toxicity can damage nerve cells and cause large-scale PC12 apoptosis, cell viability is reduced, and apoptosis situation is alleviated after intervention of a compound (I), so that the limonin compound can be further researched and developed into a neuroprotective drug.

Description

technical field [0001] The invention belongs to the field of medicaments, and in particular relates to a new limonoid compound isolated from dried rue herb, a preparation method and a medical application 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 compounds such as acridone alk...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J73/00A61K31/585A61P25/00
CPCC07J73/003A61K9/0019A61K9/0053A61K9/08A61K9/19
Inventor 吴金凤
Owner 吴金凤
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