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New medicinal application of morin hydrate

A technology of morin and drugs, which can be applied in the direction of drug combinations, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve problems such as the difficulty in the development of LXRs agonists and the lack of research on LXRs antagonists

Inactive Publication Date: 2016-02-10
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because the activation of LXRs and their signaling pathways has shown a significant cholesterol-lowering effect, and previous studies have also shown that the synthetic LXRs agonist GW3965 can slow down the apoE - / - and LDLR - / - The development of arteriosclerosis in mice, however, while agonists activate LXRs and lower cholesterol, they can also increase triglyceride synthesis by increasing the expression of its downstream lipogenic genes, leading to severe fatty liver and hypertriglyceridemia , and even adverse reactions such as obesity, which makes the research and development of LXRs agonists encounter great difficulties
[0005] Compared with LXRs agonists, LXRs antagonists are rarely studied

Method used

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  • New medicinal application of morin hydrate
  • New medicinal application of morin hydrate
  • New medicinal application of morin hydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] Example 1: Effect of Morin on Nuclear Receptor LXRα, β Transcriptional Activity

[0100] The GAL4-DBD-LBD expression plasmids of LXRα and β nuclear receptors and the GAL4-responsive luciferase reporter gene system were used to analyze the effect of morin on the transcriptional activity of the two nuclear receptors.

[0101] After co-transfection of GAL4-DBD-LBD expression plasmid and GAL4-luciferase reporter gene plasmid into 293T cells, they were treated with LXR agonist GW3965 (10 μM) and morin (5, 10, 20 μg / mL) for 24 hours, and their Firefly luciferase activity. Renilla activity was used as an internal reference to determine reporter gene activity. Data are the results of three experiments, expressed as means±SE, *P<0.05.

[0102] The results showed that in the presence of the LXRs agonist GW3965, morin competitively inhibited the activity of LXRβ in a concentration-dependent manner, and the drug showed a significant effect at three different concentrations of 12....

Embodiment 2

[0103] Example 2: Verification of the weight loss effect of morin

[0104] Since the transcriptional activity of LXRβ is closely related to fatty acid synthesis and triglyceride metabolism, inhibiting the transcriptional activity of LXRβ can inhibit triglyceride synthesis and reduce weight. Therefore, the inventors of this patent used the 3T3L1 adipocyte model to verify whether morin has an in vitro effect of inhibiting adipocyte differentiation.

[0105] The results show that: morin has the effect of inhibiting the differentiation of 3T3L1 adipocytes (see figure 2 as shown, figure 2 Middle: Photo A is the 3T3-L1 cells grown in culture medium, which is a negative control; Photo B is the adipocytes induced by insulin and dexamethasone; photo C is the 3T3-L1 adipocytes treated with morin ). In further in vivo experiments (the mice were fed with normal diet, high-fat diet and high-fat diet mixed with 0.01% morin for 8 weeks, and the body weight of the mice was measured every...

Embodiment 3

[0106] Example 3: Verification of the preventive and therapeutic effects of morin on hyperlipidemia induced by high-fat meal in C57BL / 6 mice

[0107] The mice fed with normal feed, high-fat feed, and high-fat feed mixed with 0.01% morin for 8 weeks were fasted for 12 hours, and then the blood samples of mice after fasting were collected by heart blood collection, and the small blood of each group was determined. Total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL-c), low-density lipoprotein cholesterol (LDL-c) levels in mouse serum. Data are mean±SE, n=7 for each group.

[0108] The result shows: morin can significantly reduce the levels of TC, TG and LDL-c in mouse serum (see Figure 5 shown), indicating that morin has a preventive effect on hyperlipidemia induced by high-fat diet in C57BL / 6 mice.

[0109] Obese mice fed with high-fat diet for three months were fed with high-fat diet mixed with 0.01% morin for 4 weeks, and then the mice were...

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Abstract

The invention discloses a new medicinal application of morin hydrate, wherein the new medicinal application refers that the morin hydrate is used as an active component for preparing a liver X receiver-[beta] antagonist and as an active component for preparing a medicine for preventing, alleviating and / or treating metabolic diseases induced by the liver X receiver-[beta]. A test result proves that the morin hydrate can selectively inhibit transcriptional activity of the LXR-[beta] and has a significant in-vitro effect of inhibiting differentiation of fat cells, and also has the in-vivo effects of blocking C57BL / 6 mouse weight gain induced by high-fat diet, inhibiting volume gain of body fat cells, improving fasting blood-glucose, insulin resistance and dyslipidemia of mice. The morin hydrate is hopeful to be developed into a low-toxic and high-effective LXR[beta] receiver antagonist and the medicine for preventing, alleviating and / or treating the metabolic diseases induced by the liver X receiver-[beta].

Description

technical field [0001] The invention relates to a new medicinal application of morin, which belongs to the technical field of traditional Chinese medicines. Background technique [0002] Liver X receptor (liverXreceptors, LXR) is a member of the nuclear receptor transcription factor family, which is divided into two homologous subtypes, LXRα (NR1H3) and LXRβ (NR1H2). LXRα is only highly expressed in limited tissues such as liver, small intestine, spleen, kidney, and fat, while LXRβ is widely distributed in various tissues of the human body. In the past two decades, many physiological functions of LXRs have been discovered, which can regulate lipid metabolism, glucose metabolism and immune function regulation by regulating the expression of a series of downstream target genes. Abnormalities in these physiological functions are directly related to the development of diseases such as arteriosclerosis, fatty liver, obesity, diabetes and tumors. [0003] Currently known target ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P5/50A61P3/06A61P3/04A61P9/10A61P1/16
Inventor 黄诚顾明张玉
Owner SHANGHAI UNIV OF T C M
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