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Uses of flavonoids of marine fungal origin

A technology of flavonoids and marine fungi, applied in the field of medical applications, to achieve the effects of protecting oxidative stress, reducing the expression of ROS, and protecting against

Active Publication Date: 2022-02-25
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There are structural differences between flavonoids and 2-phenylchromone, and the role of these compounds as Nrf2 activators has not been reported at home and abroad.

Method used

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  • Uses of flavonoids of marine fungal origin
  • Uses of flavonoids of marine fungal origin
  • Uses of flavonoids of marine fungal origin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1: Preparation of benzo-γ-pyrone and 2,3,4,6,8-pentahydroxyl-1-methylflavone (preparation method quoted from "New Chromones from a Marine-Derived Fungus, Arthrinium sp ., and Their Biological Activity", Jie Bao et al., Molecules 2018,23,1982. 2,3,4,6,8-pentahydroxy-1-methylflavone is numbered 73, and benzo-γ-pyrone is numbered for 75)

[0056] The specific operation is as follows:

[0057] (1) Inoculate the metabolites of the marine fungus ArthriniμM sp.UJNMF0008 on the plate, put the inoculated bacteria in the culture medium, shake the bacteria in a shaker at 28°C and 160r for 3 days to obtain the seed liquid of UJNMF008, and inoculate UJNMF0008 The seed liquid was transferred to a 1 L Erlenmeyer flask with solid rice medium. Cultured statically at 28°C for 30 days. After fermentation, it was extracted three times with 95% ethanol. The EtOH extract was evaporated under reduced pressure to obtain an aqueous solution, then extracted three times with ethyl ace...

Embodiment 2

[0060] Example 2: Benzo-γ-pyrone and 2,3,4,6,8-pentahydroxy-1-methylflavone can promote Nrf2 into the nucleus

[0061]Experimental method: inoculate endothelial cells (the endothelial cells used in the present invention are obtained from the umbilical cord of the puerpera from the 456 Hospital of the People's Liberation Army, take out and store in low temperature, and extract within 2 hours) in a 2ml culture dish. After the cells are spread to 80%, the normal group: Add LDL culture under normal conditions without serum, set up control group: culture under normal conditions without serum; experimental group: add benzo-γ-pyrone and concentrations of 1 μM, 5 μM and 50 μM under serum-free conditions, respectively 1μM, 5μM and 50μM 2,3,4,6,8-pentahydroxy-1-methylflavone were incubated for 24 hours and then treated with drugs. 37°C, CO 2 After culturing in the incubator for 6 hours, discard the old culture medium, gently wash the cells twice with 0.1M PBS; discard the 0.1M PBS, fix...

Embodiment 3

[0062] Example 3: Benzo-γ-pyrone and 2,3,4,6,8-pentahydroxy-1-methylflavone can activate nrf2 downstream antioxidant protein HO-1

[0063] Experimental method: Inoculate endothelial cells in a culture dish with a diameter of 6 cm. Normal group: add LDL culture under normal conditions without serum, set up control group: add ox-LDL culture under normal conditions without serum; Add 2,3,4,6,8-pentahydroxy-1-methylflavone at concentrations of 1 μM, 5 μM and 50 μM, and 1 μM, 5 μM and 50 μM benzo-γ-pyrone under the conditions for incubation. 37°C, CO 2 After culturing in the incubator for 6 hours, the cells were lysed, the cell lysate was collected, centrifuged at 12000 g at 4 °C for 15 min, the supernatant was taken, and the expression level of HO-1 in endothelial cells was detected by western blot.

[0064] The results showed that: compared with the ox-LDL group in the control group, the addition of compound 2,3,4,6,8-pentahydroxy-1-methylflavone (1 μM, 5 μM, 50 μM) while adding...

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Abstract

The invention discloses the use of flavonoids derived from marine fungi. The general formula of the flavonoids is specifically 2, 3, 4, 6, 8-pentahydroxy-1-methylflavone and benzo-γ-pyrone The use of flavonoids extracted from two marine microorganisms as Nrf2 activators in the treatment of cardiovascular and cerebrovascular diseases. The flavonoids in the present invention are extracted from the metabolites of deep-sea fungi. Through the research of the present invention, it is found that 2, 3, 4, 6, 8-pentahydroxy-1-methyl flavone and benzo-γ-pyran By activating Nrf2, ketones can reduce the expression of intracellular reactive oxygen species ROS, protect endothelial cells from oxidative stress and damage, and play a role in antioxidant protection of endothelial cells. The invention provides support for studying 2, 3, 4, 6, 8-pentahydroxy-1-methylflavone and benzo-γ-pyrone as Nrf2 activators for treating cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The present invention relates to the technical field of medical application, relates to the use of flavonoids derived from marine fungi, and in particular to the use of 2,3,4,6,8-pentahydroxy-1-methylflavone and benzo-γ-pyrone . Background technique [0002] The transcription factor Nrf2 belongs to CNC-Bzip (capncollar subfamily of basic leucine-zipper), which is the family of CNC leucine zipper transcription activators. central regulator. By inducing and regulating the constitutive and inducible expression of a series of antioxidant proteins, Nrf2 can reduce the cell damage caused by reactive oxygen species and electrophiles, keep the cells in a stable state, and maintain the body's redox dynamic balance. important access. A large number of studies have shown that Nrf2 is related to the occurrence of various diseases. [0003] Flavonoids (flavonoids) are a class of compounds that exist in nature and have a 2-phenylchromone (flavone) structure. Th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P39/06A61P9/00A61P9/10A61P7/02
CPCA61K31/352A61P39/06A61P9/00A61P9/10A61P7/02
Inventor 孟宁王艳红鲍洁牟鑫
Owner UNIV OF JINAN
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