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Acylphloroglucinol derivative as well as pharmaceutical composition and application thereof

A technology for acyl phloroglucinol and derivatives, which is applied in the field of medicine, can solve the problems such as no dearylation prenyl phloroglucinol derivative compound activity, etc., and achieves the effect of convenient operation

Active Publication Date: 2020-05-19
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the dearomatization isopentenylphloroglucinol derivative compound hypatone A and its activity in the existing technology so far.

Method used

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  • Acylphloroglucinol derivative as well as pharmaceutical composition and application thereof
  • Acylphloroglucinol derivative as well as pharmaceutical composition and application thereof
  • Acylphloroglucinol derivative as well as pharmaceutical composition and application thereof

Examples

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preparation example Construction

[0027] The present invention provides a preparation method of the compound hypatone A described in the above technical scheme, comprising the following steps: extracting the dried Rhizoma chinensis (12kg) with methanol for 3 times, each time for 2 days, and obtaining the obtained extract by distillation under reduced pressure Extraction, mix the extract with 100-200 mesh silica gel, carry out silica gel column chromatography, the eluent used is chloroform, obtain chloroform section, then mix the obtained chloroform section with polyamide, and use 70%- 100% methanol-water was used as the mobile phase to pass through the MCI column, and five components A to E were collected sequentially. The A (16.4g) component was subjected to silica gel column chromatography under gradient elution conditions, using petroleum ether / acetone as the The eluent was collected in sequence to obtain 5 fractions, which were denoted as fractions A1-A5; fraction A2 was separated and purified by HPLC to ob...

Embodiment 1

[0037] The preparation method of compound hypotone A, comprises the following steps:

[0038] The present invention provides a preparation method of the compound hypatone A described in the above technical scheme, comprising the following steps: extracting the dried Rhizoma chinensis (12kg) with methanol for 3 times, each time for 2 days, and obtaining the obtained extract by distillation under reduced pressure Extraction, mix the extract with 100-200 mesh silica gel, carry out silica gel column chromatography, the eluent used is chloroform, obtain chloroform section, then mix the obtained chloroform section with polyamide, and use 70%- 100% methanol-water was used as the mobile phase to pass through the MCI column, and five components A to E were collected sequentially. The A (16.4g) component was subjected to silica gel column chromatography under gradient elution conditions, using petroleum ether / acetone as the The eluent was collected in sequence to obtain 5 fractions, whi...

Embodiment 2

[0047] The present invention dearomatizes isopentenylphloroglucinol derivatives hypatone A to Ca v 3.1 and mutant Ca v 3.1 (Arg1723His) Activation Activity Experimental methods and results are as follows:

[0048] 1. Cell preparation and expression

[0049] Human embryonic kidney (HEK) 293 cells were cultured in DMEM (HyClone) medium supplemented with 10% calf serum (Gibco) and double antibodies of penicillin (100 units / ml) and streptomycin (0.1 mg / ml) (Biological Industries) . 293 cells in the logarithmic growth phase were treated with LipoD293 TM (SignaGen Laboratories) transfection reagent mouse pCDNA3.1-Ca v 3.1, pCDNA3.1-Ca v 3.1 (Arg1723His) and pCDNA3.1-EGFP plasmids were transfected into cells. Transfected human embryonic kidney (HEK) 293 cells should be used within 48 hours.

[0050] 2. Electrophysiology experiment

[0051] All experiments were performed at room temperature (22-25°C). Using a microelectrode puller (P-1000, Sutter Instrument) and heating polis...

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Abstract

The invention provides a dearylated isopentenyl acylphloroglucinol derivative, a preparation method thereof, a pharmaceutical composition for neurodegenerative diseases and an application of the pharmaceutical composition, and belongs to the technical field of medicines. The compound Hypatone A provided by the invention has a new rare cage structure, is the strongest Cav3.1 low-voltage gated calcium ion channel activator at present, and has potential medicinal value in Alzheimer's disease and spinal cerebellar ataxia 42.

Description

technical field [0001] The present invention relates to the field of pharmaceutical technology, in particular to v 3.1 Hypatone A, a new compound with low-voltage-gated calcium channel activation, its preparation method, and its application in drugs for the treatment of neurodegenerative diseases Alzheimer's disease and spinocerebellar ataxia type 42. Background technique [0002] Hypericum (Hypericum) is a large genus in the family Guttiferae, with about 400 species worldwide. There are about 55 species and 8 subspecies in my country, which are distributed all over the country, and are mainly produced in the southwest region. The plants of this genus are widely used as medicinal plants at home and abroad, and have a long history. For example, there are 25 species of Hypericum plants in my country that are used as medicines among the people, and have various pharmacological activities such as antidepressant, antitumor, antiviral and antibacterial. So far, various types of...

Claims

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Application Information

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IPC IPC(8): C07D307/00A61K31/343A61P25/28
CPCC07D307/00A61P25/28C07B2200/07
Inventor 许刚年寅叶岩松杜叔宗杨建阎慧
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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