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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 poor water solubility and low antidepressant biological activity, and achieve the effects of good antidepression, recovery and good effect.

Active Publication Date: 2013-08-28
兰晟生物医药(苏州)有限公司
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  • Abstract
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  • Claims
  • Application Information

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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 relates to the technical field of medicine, in particular to a helexin amide derivative and its preparation method and application. Background technique [0002] Fuzhizi is the dry and nearly ripe fruit of Akebia, Akebia trifoliata or Akebia trifoliata. Traditional Chinese medicine believes that it is bitter in taste and flat in nature, and has the effects of soothing the liver and regulating qi, promoting blood circulation and relieving pain, softening and resolving hard masses. Hederagenin is the main product of the hydrolysis of triterpene saponins, the main component of the orchid seed. 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. [0003] The antidepressant mechanism and target of helexin are not yet clear. On the basis of summarizing previous experience in structural modification of helexin and its...

Claims

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Application Information

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Patent Type & Authority Applications(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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