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Use of flavonoids from marine fungi

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

Active Publication Date: 2020-10-02
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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  • Use of flavonoids from marine fungi
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  • Use of flavonoids from marine fungi

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0056] The specific operations are as follows:

[0057] (1) Inoculate the metabolites of the marine fungus ArthriniμM sp.UJNMF0008 on the plate, put the inoculated bacteria on the culture medium, in a shaker at 28°C, 160r, shake for 3 days to obtain the seed solution of UJNMF008, and add UJNMF0008 The seed liquid was transferred to a 1L Erlenmeyer flask with solid rice culture medium. Statically cultured 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, and then extracted with ethyl acetate three times...

Embodiment 2

[0060] Example 2: Benzo-γ-pyrone and 2,3,4,6,8-pentahydroxy-1-methylflavonoids 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 PLA 456 Hospital, taken out for cryopreservation, and extracted within 2 hours) in a 2 ml petri dish. After the cell area reaches 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 at concentrations of 1μM, 5μM and 50μM under serum-free conditions 2, 3, 4, 6, 8-pentahydroxy-1-methylflavonoids of 1μM, 5μM and 50μM were cultured for 24h and then treated with medicine. 37°C, CO 2 After 6 hours of incubation in the incubator, discard the old culture medium and gently wash the cells twice with 0.1M PBS; discard 0.1M PBS and fix the cells with 4% paraformaldehyde for 15 mi...

Embodiment 3

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

[0063] Experimental method: inoculate endothelial cells in a petri 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; experimental group: culture after serum removal Under the conditions, 2, 3, 4, 6, 8-pentahydroxy-1-methylflavonoids of 1μM, 5μM and 50μM were added, and benzo-γ-pyrone of 1μM, 5μM and 50μM were cultured. 37°C, CO 2 After culturing in an incubator for 6 hours, the cells were lysed, the cell lysate was collected, centrifuged at 12000g at 4°C for 15 minutes, 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 control ox-LDL group, the addition of compounds 2, 3, 4, 6, 8-pentahydroxy-1-methyl...

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Abstract

The invention discloses use of flavonoids from marine fungi, specifically use of two flavonoids extracted from marine microorganisms, 2, 3, 4, 6, 8-pentahydroxy-1-methylxanthon and chromone arthone, as activators of Nrf2 in the treatment of cardiovascular and cerebrovascular diseases. The flavonoids are extracted from metabolites of deep-sea fungi. Through research of the invention, it is found that 2, 3, 4, 6, 8-pentahydroxy-1-methylxanthon and chromone arthone can reduce the expression of reactive oxygen species (ROS) in cells by activating Nrf2, protect endothelial cells from oxidative stress and damage, and play a role in antioxidant protection of endothelial cells. The invention provides support for researching 2, 3, 4, 6, 8-pentahydroxy-1-methylxanthon and chromone arthone as activators of Nrf2 to treat cardiovascular and cerebrovascular diseases.

Description

Technical field [0001] The invention relates to the technical field of medical applications, and relates to the use of flavonoids derived from marine fungi, in particular to the use of 2, 3, 4, 6, 8-pentahydroxy-1-methylflavonoids and benzo-γ-pyrone . Background technique [0002] The transcription factor Nrf2 belongs to CNC-Bzip (capncollar subfamily of basic leucine-zipper), which is a family of CNC leucine zipper transcription activators. It is an important transcription factor that regulates cellular oxidative stress response and also maintains intracellular redox homeostasis. Central regulator. By inducing and regulating the constitutive and inducible expression of a series of antioxidant proteins, Nrf2 can reduce cell damage caused by reactive oxygen species and electrophiles, keep cells in a stable state, and maintain the body's redox homeostasis, thus becoming a cell anti-oxidant stress Important pathway. A large number of studies have shown that Nrf2 is related to the...

Claims

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Application Information

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Patent Type & Authority Applications(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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