Application of diosmetin(4-O-methyl) glucoside compound in preparation of lipid-lowering drugs

A technology of diosmin and glucoside, which is applied in the fields of drug combination, sugar derivatives, organic chemistry, etc., and can solve the problem of few reports on lipid-lowering activity

Active Publication Date: 2021-02-12
INST OF CROP SCI CHINESE ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is worth noting that due to a wide range of biological activities, diosmin derivatives are gradually being used in the fields of medicine and food, but their lipid-lowering activity is rarely reported

Method used

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  • Application of diosmetin(4-O-methyl) glucoside compound in preparation of lipid-lowering drugs
  • Application of diosmetin(4-O-methyl) glucoside compound in preparation of lipid-lowering drugs
  • Application of diosmetin(4-O-methyl) glucoside compound in preparation of lipid-lowering drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Methyl glycosylation modification of diosmin by Isaria fumosorosea ACCC 37814

[0016] 1.1 Instruments and materials

[0017] The strain used in the experiment: Isaria fumosorosea ACCC 37814 was obtained from the China Agricultural Microorganism Culture Collection Center (ACCC). Compounds: purchased from Shanghai Yuanye Biotechnology Co., Ltd. (Shanghai, China). The reagents used in the experiment were domestic analytically pure products. Culture medium: the fungal medium is potato dextrose agar (PDA, Difco, Sparks, MD, USA) medium and potato dextrose broth (PDB, Difco, Sparks, MD, USA) medium, if making solid medium, add 2 % agar powder.

[0018] High performance liquid chromatography (Agilent, Agilent 1260Infinity II HPLC and Agilent1290Infinity II HPLC), C 18 Chromatographic columns (Agilent, Poroshell 120SB-C18, 2.7 μm, 4.6 mm×150 mm and Zorbax SB-C18, 1.8 μm, 2.1×50 mm). Mass spectrometry (Agilent, Agilent QTOF 6530). Rotary evaporator (BUCHI compan...

Embodiment 2

[0027] Example 2 Extraction, separation and structural identification of compound 3a

[0028] 2.1 Instruments and materials

[0029] Chromatographic pure water, chromatographic acetonitrile, analytical pure ethyl acetate, chromatographic or ordinary pure methanol, dichloromethane, etc. used in the laboratory were purchased from Fisher (USA); column chromatography silica gel (100-200 mesh) was purchased from Qingdao Ocean Chemical Plant Company. BUCHIDL-400 rotary evaporator, produced by Swiss BUCHI company. The circulating cooler is produced by Zhengzhou Great Wall Science, Industry and Trade Co., Ltd. The semi-automatic preparative liquid chromatograph is Agilent 1260Infinity II, and the C18 chromatographic column is Eclipse XDB-C18, 5μm, 9.4×250mm. The Agilent 1260 Infinity II analytical HPLC instrument equipped with a Poroshell 120SB-C18 reverse-phase column (2.7 μm, 4.6 mm×150 mm) was used for sample purity testing. No impurity peaks were required, and pure samples were...

Embodiment 3

[0042] Example 3 Solubility test of diosmin and its glycosides

[0043] 3.1 Purpose of the experiment

[0044] Determination of the effect of sugar methylation on the solubility of naringenin in different solvents.

[0045] 3.2 Experimental method

[0046] Weigh 0.5mg of naringenin and compound 3 and 3a respectively, place in 500uL of different solvents at 25°C±2°C, shake vigorously for 30s every 5min; observe the dissolution within 30min, if no solute particles or liquid When dripping, it is considered to be completely dissolved. The selected solvents are distilled water, methanol, ethanol, etc.

[0047] 3.3 Experimental results and analysis

[0048] Table 2 shows the solubility of diosmin and its sugar methylated derivatives (compound 3a) in different solvents.

[0049] Table 2 Solubility of diosmin and compound 3a in different solvents

[0050]

[0051] Note: insoluble-; slightly soluble-+; partially soluble+; mostly soluble++; completely soluble+++

[0052] As sh...

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Abstract

The invention discloses an application of a diosmetin(4-O-methyl) glucoside compound as a lipid-lowering drug; in a biological activity test, the compound shows down-regulation or inhibition of mouse3T3-L1 precursor adipocyte proliferation and significant reduction of the number of lipid droplets generated in a cell differentiation process, and aglycones of the diosmetin(4-O-methyl) glucoside compound also have the functions, but the effect of the compound is more obvious; compared with the aglycones, the compound has the advantages that the water solubility of the compound is remarkably enhanced, the conversion rate of the compound is high, and the compound has wider application value.

Description

Technical field: [0001] The invention belongs to the field of lipid-lowering drugs, in particular to the use of diosmin (4-O-methyl) glucoside compounds in lipid-lowering drugs. Background technique: [0002] Diosmetin is a common natural flavonoid plant secondary metabolite, which is widely found in natural medicines such as chrysanthemum, spearmint, and spider incense, and in fruits such as lemons, citrus, and peanuts. Dioxynignin is considered to have a variety of biological and pharmacological activities on human health, such as antioxidant, antibacterial, antiviral, anti-inflammatory, antitumor, antithrombotic and hepatoprotective activities, so it has attracted widespread attention and can be used in Food, medicine and other fields can improve health and prevent diseases. However, diosmin is only slightly soluble in water, has a low extraction rate, has certain phytotoxicity, and has poor metabolic stability in mammals. And bioavailability decrease, which greatly hin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/07A61K31/7048A61P3/06
CPCC07H17/07A61K31/7048A61P3/06
Inventor 顿宝庆窦方敏王智幺杨李桂英
Owner INST OF CROP SCI CHINESE ACAD OF AGRI SCI
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