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Different terpenoid intermolecular adducts in Pseudotsuga forrestii Craib and preparation method and pharmaceutical application thereof

An intermolecular and adduct technology, applied in the separation/purification of carboxylic acid compounds, medical preparations containing active ingredients, drug combinations, etc., to achieve significant ACL inhibitory activity

Active Publication Date: 2021-09-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on its chemical composition. If we can collect a few samples of Douglas lancang for protection and conduct systematic chemical composition research, it will actively promote scientific understanding, actively protect and utilize this rare plant resource to serve mankind.

Method used

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  • Different terpenoid intermolecular adducts in Pseudotsuga forrestii Craib and preparation method and pharmaceutical application thereof
  • Different terpenoid intermolecular adducts in Pseudotsuga forrestii Craib and preparation method and pharmaceutical application thereof
  • Different terpenoid intermolecular adducts in Pseudotsuga forrestii Craib and preparation method and pharmaceutical application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: prepare compound described in the present invention

[0025] (1) After drying and pulverizing the branches and leaves of Douglas chinensis collected from Dali, Yunnan (first batch: collected in October 2017, dry weight 13kg), they were extracted 7 times with 90% methanol (6L) solution at room temperature, each time 24 hours;

[0026] (2) Combine the extracts obtained in step (1), concentrate under reduced pressure to remove methanol to obtain 2.46kg (semi-dry) extract, disperse the extract with 2L of water, and use equal volumes of petroleum ether, ethyl acetate and n-butyl Alcohol was extracted three times respectively, and each extract was concentrated under reduced pressure to obtain petroleum ether part, ethyl acetate part, n-butanol part and water 4 components respectively, wherein, ethyl acetate part crude extract (409g) was passed through silica gel column Chromatography (washing with petroleum ether-ethyl acetate gradient, 30:1→0:1, v / v) separated...

example 2

[0042] Example 2: ACL inhibitory activity test of the compound prepared by the present invention

[0043] Experimental method: In this experiment, ACL can catalyze the conversion of citric acid into acetyl-CoA, and then produce the precursor molecule of fatty acid synthesis - malonyl-CoA. This reaction is accompanied by the consumption of ATP, so ADP-Glo ​​and kinase can be used The detection kit detects the change of ATP, and the inhibitory effect of the indirect reaction compound on the ACL enzyme activity; in this embodiment, the percentage inhibition rate of the ACL enzyme activity was investigated when the concentration of the compound selected for the primary screening was 20 μg / ml, and the test results It shows that the above compounds all have enzyme activity inhibitory effect;

[0044] Further determination of IC 50 Value: the sample is dissolved in DMSO to make a suitable concentration before use, 3-fold dilution, 7 dilutions, triplicate wells, take 2μL sample solut...

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Abstract

The invention relates to the field of medicines, in particular to a Diels-Alder type adduct between different terpenoid molecules, which is separated from branches and leaves of a Pseudotsuga plant (Pseudotsuga forrestii Craib) of Pinaceae plants, as well as a preparation method and application of the Diels-Alder type adduct. The Diels-Alder type adduct is shown in the specification. According to the present invention, the in vitro activity test results show that the compound has significant ATP-citrate lyase (ACL) inhibition activity; the compound can be used for preparing drugs for preventing, delaying or treating ACL-mediated glycolipid metabolism disorder and other related diseases, and provides a lead compound for research and development of novel drugs for diseases related to the glycolipid metabolism disorder.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to different terpene intermolecular adducts in Pseudotsuga forrestii Craib and its preparation method and pharmaceutical application, in particular to the adduct prepared from the branches and leaves of Pseudotsuga forrestii Craib of Pinaceae plant Diels-Alder type adducts between different terpenoid molecules, and the preparation method of such compounds, and the use of such compounds in the preparation of ATP-citrate lyase inhibitors, the ATP-citrate lyase inhibitors are used It is used to prevent and treat diseases related to glucose and lipid metabolism disorders mediated by ATP-citrate lyase (ATP-citrate lyase, ACL), such as hyperlipidemia, non-alcoholic fatty liver, type II diabetes, etc. Background technique [0002] The prior art discloses that endogenous cholesterol synthesis is the key source of plasma cholesterol in systemic circulation, and acetyl-CoA produced by mitochon...

Claims

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Application Information

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IPC IPC(8): C07C62/38C07C51/42C07C51/47C07C51/48A61P3/06A61P1/16A61P3/10A61P3/04A61K31/194A61K31/19
CPCC07C62/38A61P3/06A61P1/16A61P3/10A61P3/04C07C2601/16C07C2603/94C07C2603/95
Inventor 熊娟胡金锋周鹏军黄婷何宇航
Owner FUDAN UNIV