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Hederagenin amide derivative and preparation method and application thereof

A technology of helexin and aglycone amide, applied in the field of medicine, can solve the problems of low antidepressant biological activity, poor water solubility and the like, and achieve the effects of being beneficial to recovery, good antidepressant and good effect

Active Publication Date: 2015-04-01
兰晟生物医药(苏州)有限公司
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AI Technical Summary

Problems solved by technology

Both Fructus Akebiae extracts (FAE) and helexin have certain antidepressant activity, but their water solubility is poor, and their antidepressant biological activity is not high

Method used

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  • Hederagenin amide derivative and preparation method and application thereof
  • Hederagenin amide derivative and preparation method and application thereof
  • Hederagenin amide derivative and preparation method and application thereof

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Embodiment Construction

[0035] The present invention will be further described in detail below in conjunction with the accompanying drawings and embodiments.

[0036] A helexin amide derivative, wherein: the hedera amide derivative is N-(3-dimethylaminopropyl)-helexin-17-carboxamide, abbreviated as HGA, and the general formula is .

[0037] The 3-dimethylaminopropyl group in N-(3-dimethylaminopropyl)-helexin-17-carboxamide is formed by introducing 3-dimethylaminopropylamine at the 28-position of helexin.

[0038] When preparing N-(3-dimethylaminopropyl)-helexin-17-carboxamide of the present invention, the experimental instruments and reagents that need to be used are:

[0039] Determination by nuclear magnetic resonance (TMS is internal standard, CD 3 OD is the solvent); rotary evaporator, electronic balance, circulating water vacuum pump, liquid chromatograph, quaternary low-pressure gradient pump, automatic sampler, diode array detector, chromatographic workstation, 4.6mm×250mm Agela 18 C chrom...

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Abstract

The invention discloses a hederagenin amide derivative which is N-(3-dimethylaminopropyl)-hederagenin-17-formamide (HGA). According to the hederagenin amide derivative, 3-dimethylamino propylamine is introduced at the 28th position of the hederagenin, the hederagenin and a drone form a hydrogen bond due to the existence of amino, so that the biological activity of the hederagenin is improved, and an anti-depression effect of the hederagenin is better, and furthermore, a lot of experiments prove that the N-(3-dimethylaminopropyl)-hederagenin-17-formamide also has a good effect in neuroprotection and anti-tumor. The hederagenin amide derivative shows that neuroplasticity and depression are closely related, and a BDNF (brain derived neurotrophic factor) has a certain relationship with depression and is beneficial for the nerve plasticity to recover. The invention also discloses a mechanism studying an HGA neuroprotective effect from the point of view of BDNF and neuroplasticity.

Description

Technical field [0001] The invention involves the technical field of medicine, and it specially involves a kind of ivyamide amamide derivatives and their preparation methods and applications. Background technique [0002] The predictor is the dry and near -mature fruits of Muzong plant Muyun, Sanye Muyun or Baimu Tong.Traditional Chinese medicine believes that it has a bitter taste, flat nature, has the effects of relieving liver and qi, promoting blood circulation and relieving pain, and softening.Hedragenin is the main product of hydrolysis of the main ingredients of Sanxia Saucer.FRUCTUS AKEBIAE EXTRACTS (FAE) and Ivyevo Sauvis have certain antidepressants. [0003] The antidepressant mechanism and target of Ivimotoside Elastin are not yet clear. Based on the experience of the reconstruction of Ivy Sauhinhide and its analog structure before summing up, we hope that through the existence of amino groups to form hydrogen bonds with targets to improve it to improve itBiological a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61P25/24A61P35/00A61P25/00
Inventor 徐江平王国华
Owner 兰晟生物医药(苏州)有限公司
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