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Macrocyclic polyphenol compound, and preparation and application thereof in pharmacy

A technology of polyphenolic compounds and compounds, applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., can solve the pharmacological reports of compounds that have not been seen in reducing blood sugar and anti-hepatic fibrosis, etc., to achieve inhibition of hepatic stellate Cell proliferation, rich sources of raw materials, and environmental protection

Active Publication Date: 2014-03-19
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Macrocyclic polyphenolic compounds have anti-hepatitis C pharmacological effects (Two antiviral compounds from the plant Stylogne cauliflora as inhibitors of HCV NS3protease, Bioorganic & Medicinal Chemistry Letters, 2003, 13(17): 2925-2928), but looking at the reports at home and abroad, There are no pharmacological reports on hypoglycemic and anti-hepatic fibrosis of these compounds

Method used

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  • Macrocyclic polyphenol compound, and preparation and application thereof in pharmacy
  • Macrocyclic polyphenol compound, and preparation and application thereof in pharmacy
  • Macrocyclic polyphenol compound, and preparation and application thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The preparation of embodiment 1 macrocyclic polyphenol compound

[0041] (1) Extraction and preliminary separation of herbal medicines

[0042] Grind 5kg of root vegetables, extract three times with 70% ethanol under hot reflux, each extraction time is 1 hour, add 15L of liquid each time, combine the extracts, concentrate under reduced pressure (55°C) until there is no alcohol smell to obtain the crude extract extract (relatively The density is 1.12~1.18), and its weight is 625g, and the yield is 12.5%. Then water (650ml) was suspended and passed through a macroporous resin column (D-101), followed by elution with water, 10% ethanol, 20% ethanol, 30% ethanol, 50% ethanol, 70% ethanol and 95% ethanol. The liquid is 10 to 12 times the volume of the column, and the eluents of water, 10% ethanol, 20% ethanol, 30% ethanol, 50% ethanol, 70% ethanol and 95% ethanol are respectively obtained, and concentrated under reduced pressure (55°C) to The extracts (relative density: 1....

Embodiment 2

[0049] Example 2 Determination of Macrocyclic Polyphenol Compounds 1-4 in Rhizoma Rhizoma Medicinal Materials

[0050] Its method and operation steps are as follows

[0051] (1) HPLC conditions

[0052] Chromatographic column: Diamonsil C18column (4.6mm×250mm, 5μm, Dikma);

[0053] Mobile phase: Gradient elution, A phase is acetonitrile, B phase is 0.2% formic acid aqueous solution;

[0054] Flow rate: 1.0ml / min, running time 70min, detection wavelength 280nm,

[0055] The column temperature is 25°C; the injection volume is 10 μl;

[0056] Table 1 Gradient elution program

[0057]

[0058]

[0059] (2) Content determination of compound 1-4

[0060] Take the compound 1-4 reference substance (prepared in Example 1), weigh it accurately, and prepare compound 1-4 solutions containing 350 μg, 100 μg, 200 μg, and 50 μg in each 2 mL with 60% methanol, respectively, as the reference solution.

[0061] Take an appropriate amount (equivalent to 10 g of the root vegetable) of...

Embodiment 3

[0062] Example 3 Compound 1-4 Hypoglycemic Activity Experiment in Vitro

[0063] 1 Materials and methods

[0064] 1.1 Test drugs

[0065] Embodiment 1 prepares gained monomer compound 1-4

[0066] Experimental Materials

[0067] Acarbose (Bayer, 50mg / tablet, commercially available), glucose detection kit (glucose oxidase-peroxidase method, Shanghai Rongsheng Biotechnology Co., Ltd.), α-amylase (Wako Pure Chemicals Ind., Osaka, Japan), microplate reader (EIx800, Biotek), 96-well cell culture plate (Corning / Costar)

[0068] 1.2 Experimental method

[0069] 1.3.1 Chromogenic reagent: Dissolve 10.8 grams of sodium benzoate and 5 grams of potassium iodide in 400ml of water, then dilute to 500ml.

[0070] 1.3.2 Make 1-4 into 10mg / ml solution with DMSO (dimethyl sulfoxide), and then dilute with water to 0.556mg / ml, 0.185mg / ml, 0.062mg / ml, 0.020mg / ml and 0.007mg / ml respectively There are 5 different concentrations of mg / ml; the starch is prepared into a starch solution with a co...

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Abstract

The invention provides a new use of a macrocyclic polyphenol compound separated from a penthorum chinense pursh extract in pharmacy. The macrocyclic polyphenol compound comprises a compound 1, a compound 2, a compound 3 and a compound 4, wherein the structural formulas of the compounds are as shown in the specification; the compounds have the following pharmacological activities that (1) the alpha-amylase activity is significantly inhibited, and the compounds have certain hypoglycemic effects, and (2) TGF (transforming growth factor)-beta1-induced hepatic stellate cell proliferation is significantly inhibited, and the compounds have anti-liver-fibrosis effects by pharmacology and efficacy experiments. The invention provides a novel medicament for preventing and treating diabetes mellitus, and an anti-liver fibrosis medicament. The medicament is abundant in raw material source, small in side effect, and beneficial to environmental protection, and has a relatively great clinical application value.

Description

technical field [0001] The present invention relates to traditional Chinese medicines, in particular to the use of traditional Chinese medicines, in particular to macrocyclic polyphenol compounds and their preparation and use in the preparation of medicines for preventing and treating diabetes and liver fibrosis. Background technique [0002] Diabetes mellitus is a metabolic disorder characterized by chronic hyperglycemia caused by various etiologies. With the change of human life style, the incidence of diabetes is gradually increasing, and it is expected to reach 300 million people by 2025, seriously endangering human health and social development. Abnormal glucose metabolism is the main pathological factor of diabetes, and the related enzymes involved in glucose metabolism have an important impact on glucose metabolism. Diabetes research progress, Chinese Journal of Traditional Chinese Medicine, 2012, 37(23): 3519-3525). Hypoglycemic drugs usually include traditional Ch...

Claims

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Application Information

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IPC IPC(8): C07H17/07C07H15/203C07H1/08A61K31/7048A61P3/10A61P1/16
Inventor 孙连娜黄豆豆李君丽韩军梁凤英陈万生
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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