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Abietane type diterpene enantiomer compounds, and preparation method and application thereof

A compound, rosinane technology, applied in the field of medicine, can solve the problems of chemical composition and biological activity without any reports, etc.

Active Publication Date: 2016-07-27
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Folks use the root as medicine, which has the functions of expelling wind and cold, relaxing tendons and strengthening bones, promoting blood circulation and dissipating blood stasis, reducing swelling and relieving pain, but its chemical composition and biological activity have not been reported yet.

Method used

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  • Abietane type diterpene enantiomer compounds, and preparation method and application thereof
  • Abietane type diterpene enantiomer compounds, and preparation method and application thereof
  • Abietane type diterpene enantiomer compounds, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] 6.8 kg of the whole plant of Sichuan Chrysanthemum orchids was soaked in 20L of pure methanol at room temperature for 24 hours, a total of 3 times. Combine 3 extracts afterwards, concentrate under reduced pressure, obtain 463 grams total extract. The obtained extract was dispersed with 2L of water, and then extracted with petroleum ether, ethyl acetate and n-butanol in sequence. 248 grams of all ethyl acetate fractions were preliminarily segmented with a large silica gel column (10×80cm; 100-200mesh), and the eluent was petroleum ether and acetone (from 9:1 to 0:1, v / v ), to obtain 6 components Fr.A-Fr.F. After Fr.A was separated by silica gel column for many times, it was finally purified by semi-preparative HPLC to obtain sessilifolF (1.8mg, t R =19.1min) and sessilifolI (1.7mg, t R = 22.8 min). Fr.D was further fractionated using MCI column (6.0×30cm), and the eluents were methanol and water (from 50% to 100%, v / v). The 70-80% methanol part was gradient eluted w...

Embodiment 2

[0022] Example 2: Anti-neuroinflammatory activity test

[0023] Mouse microglial BV-2 cells were purchased from the American Type Culture Collection (Manassas, VA, USA) and cultured in DMEM (Dulbecco'smodified Eagle's medium) medium (including 1800 mg / L NaHCO 3 , 10% (v / v) heat-inactivated fetal bovine serum (FBS), 100unit / mL penicillin G sodium salt and 100μg / mL streptomycin), 37°C, 5% CO 2 environment, in the incubator. The amount of NO produced was determined by Griess kit (Beyotime Biotechnology, China), that is, BV-2 cells were pretreated with different concentrations of test compounds for 4 h, and then added lipopolysaccharide (LPS, 1 μg / ml, Sigma-Aldrich) and incubated for 24 h (blank group without LPS). Aspirate the culture supernatant, mix it with an equal amount of Griess reagent, let it stand at room temperature in the dark for 10 minutes, measure the OD value of each group at a wavelength of 540nm with a microplate reader (M200, TECAN, AustriaGmbH, Austria), and ...

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Abstract

The invention relates to the technical field of medicines, and to abietane type diterpene enantiomer compounds, and a preparation method and application thereof. Specifically, the invention relates to diterpene compounds, i.e., sessilifols F, I and P, and the preparation method and application thereof in preparation of drugs used for treatment of neurodegenerative diseases. According to the invention, Chloranthus sessilifolius is extracted and separated to prepare the novel abietane type diterpene enantiomer compounds, i.e., sessilifols F, I and P, with a structural formula as shown in the specification; and pharmacological experiments show that the diterpene compounds have significant inhibitory activity of nerve inflammation (IC50 is smaller than 10 [mu]M), is free of toxic effect on cell survival, and can be applied in preparation of the drugs used for prevention and / or treatment of the neurodegenerative diseases which comprise, but not limited to, Alzheimer's disease (AD) and Parkinson's disease (PD).

Description

technical field [0001] The present invention relates to the field of medical technology, and relates to a new abietane-type diterpene enantiomer compound and its preparation method and application, in particular to the diterpene compound sessilifolsF, I and P, its preparation method and its use in the preparation of medicines for treating neurodegenerative diseases The purposes in the above mentioned include neurodegenerative diseases Alzheimer's disease, Parkinson's disease, stroke and so on. Background technique [0002] At present, the pathological mechanism of neurodegenerative disorder (neurodegenerative disorder, ND) is still not very clear, however, it is characterized by the degeneration and loss of neurons in the brain, which is beyond doubt. Neuroinflammation is complex in the pathological process of neurological disorders (ND), such as familial neuroautonomia (dysautonomia), Alzheimer's disease (AD), Parkinson's disease (PD) and stroke (stroke). Studies have foun...

Claims

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Application Information

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IPC IPC(8): C07C49/753C07C49/737C07C45/78C07C39/23C07C37/70A61P25/28A61P25/16A61P9/00
Inventor 胡金锋王立军潘礼龙熊娟杨国勋
Owner FUDAN UNIV
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