Application of aphanalide I in preparation of neuroprotective medicines

A kind of technology of aphanalidei, 1.aphanalidei, be applied in the application field of Aphanalide I in the preparation of neuroprotective medicine, can solve the problems such as not having compound activity report yet

Inactive Publication Date: 2015-11-18
林天样
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] There is no report on the activity of this compound

Method used

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  • Application of aphanalide I in preparation of neuroprotective medicines
  • Application of aphanalide I in preparation of neuroprotective medicines
  • Application of aphanalide I in preparation of neuroprotective medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1: Isolation, preparation and structural confirmation of Aphanalide I

[0013] The preparation method of Aphanalide I is the same as that reported in the literature (BioactiveTerpenoids from the Fruits of Aphanamixis grandifolia, J.Nat.Prod., 2013, 76, 1191-1195).

[0014] Confirmation of structure: colorless crystal (methanol), melting point 273-274°C, molecular formula C 26 h 34 o 7 , with an unsaturation of 10. Infrared absorption is strong, indicating that it contains hydroxyl groups (3466cm -1 ), carbonyl (1729cm -1 ), and alkenes (1683cm -1 ) and other groups. It has ultraviolet absorption at 230nm, indicating that it contains α, β unsaturated ester carbonyl moiety. H NMR spectrum data δ H (ppm, DMSO-d 6 , 500MHz): H-1 (6.75, d, J=12.0), H-2 (5.79, d, J=12.0), H-5 (2.57, d, J=13.0), H-6 (1.45, dt , J=13.0, 3.5), H-6 (1.93, t, J=13.0), H-7 (3.50, s), H-9 (1.83, s), H-11 (4.22, s), H- 12 (3.56, t, J=4.5), H-14 (2.85, s), H-16 (2.56, dd, J=19.0, 11...

Embodiment 2

[0015] Embodiment 2: the pharmacological action test of Aphanalide I

[0016] 1. Materials and Instruments

[0017] Healthy female SD rats were provided by the Experimental Animal Center of Shanghai Second Military Medical University. AphanalideI is self-made, and the HPLC normalized purity is greater than 98%. Dimethyl sulfoxide, ginkgo extract (EGb761, positive drug), MTT, Aβ25-35, and L-polylysine were all purchased from SIGMA, USA. DMEM high-glucose medium, Neurobasal, and B27 were purchased from GIBCO, USA. NSE was purchased from ABCOM, UK. Tunel was purchased from Wuhan Boster Company. LDH kit was purchased from Nanjing Jiancheng Biochemical Reagent Company.

[0018] Electronic balance, Beijing Sartorius. 1815TCCO 2 Constant temperature incubator (Shel-Lab, USA), TH-2C constant temperature oscillator (Jiangsu Taicang Experimental Equipment Factory), dissecting microscope (OLYMPUS, Japan), desktop centrifuge (Heraeus, Germany), microplate reader (DynaTtech, Japan) ...

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Abstract

The invention discloses an application of aphanalide I in preparation of neuroprotective medicines, and belongs to the field of medicines. An in vitro test proves that the aphanalide I has a significant effect of resisting Abeta25-35-induced apoptosis on hippocampal neuron under the damage condition; the effect is similar to that of a positive medicine ginkgo leaf extract EGb761; and the aphanalide I can be further researched and developed to prepare the neuroprotective medicines.

Description

technical field [0001] The present invention relates to a new application of compound Aphanalide I, in particular to the application of Aphanalide I in the preparation of neuroprotective drugs. Background technique [0002] Yao Zhang et al. isolated and purified the compound Aphanalide I for the first time, and published the results in the famous Journal of Natural Products (Bioactive Terpenoids from the Fruits of Aphanamixis grandifolia, J. Nat. Prod., 2013, 76, 1191-1195). [0003] There is no activity report of this compound yet. Contents of the invention [0004] The purpose of the present invention is to provide a kind of medical use of AphanalideI. [0005] The above-mentioned purpose is achieved through the following technical solutions: [0006] The application of AphanalideI in the preparation of neuroprotective drugs, the chemical structural formula of AphanalideI is as follows, [0007] Description of drawings [0008] figure 1 : Effect of AphanalideI o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/34A61P25/00
Inventor 林天样
Owner 林天样
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