Preparation method and application of cinchonain Ib

A technology containing cinerene and plants, applied in the direction of effective components of heterocyclic compounds, metabolic diseases, cardiovascular system diseases, etc., can solve the problem of high-efficiency extraction of Ib without cinerene, achieve high safety, lower blood lipids, good synergistic effect

Active Publication Date: 2016-10-26
天津市尖峰天然产物研究开发有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no record about how cinchonaine Ib is efficiently extracted in plants, nor is there any report on its application in medicine

Method used

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  • Preparation method and application of cinchonain Ib
  • Preparation method and application of cinchonain Ib
  • Preparation method and application of cinchonain Ib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 The liquid phase detection method of cinchonine Ib

[0027] Chromatographic column: C-18 250×4.6mm

[0028] Detection wavelength: 280nm

[0029] Flow rate: 1.0ml / min

[0030] Mobile phase: A: 1% phosphoric acid

[0031] B: acetonitrile: water = 40:60

[0032] Detecting the liquid chromatographic peaks of cinchonaine Ib such as figure 1 shown.

Embodiment 2

[0033] Example 2 Extraction of cinchonaine Ib from apple polyphenols

[0034] 1) Add 2000 mL of water to 200 g of apple polyphenols (provided by Tianjin Jianfeng Natural Products Research and Development Co., Ltd., with a polyphenol content of 80%) and stir to dissolve at room temperature, and set aside;

[0035] 2) Macroporous resin adsorption separation: the apple polyphenol solution in 1) is adsorbed by HP20 type macroporous resin, and water, volume percentage concentration is 10%, 30%, 50%, 70%, 95% ethanol aqueous solution gradient elution , each half of the column bed volume is used as a receiving volume, and the fractions rich in cinchonaine Ib are collected by thin-layer chromatography combined with analytical HPLC detection, and combined, at a temperature ≤ 60 ° C, a vacuum of Concentrated under reduced pressure at 0.06-0.08 MPa, with a sugar content of 40, to obtain the primary enrichment of Xinconine Ib;

[0036] 3) Silica gel column separation: the primary enric...

Embodiment 3

[0042] Example 3 Extraction of cinchonaine Ib from grape vines

[0043] 1) 20 kg of grape vines were continuously extracted twice with 8-fold and 6-fold amounts of 60% ethanol, combined the extracts, concentrated under reduced pressure to a sugar content of 40, added 2 times the amount of water to disperse, and set aside.

[0044] 2) Macroporous resin adsorption separation: the grapevine extract solution obtained in 1) is adsorbed by HP20 type macroporous resin, water, volume percentage concentration is 10%, 30%, 50%, 70%, 95% ethanol aqueous solution gradient For elution, each half of the column bed volume is used as a receiving volume, and the components rich in cinchonaine Ib are collected by thin-layer chromatography combined with analytical HPLC detection, combined, at a temperature ≤ 60 ° C, vacuum Concentrated under reduced pressure with a concentration of 0.06-0.08MPa, a sugar content of 40, and a primary enrichment of Xinconine Ib with a content of 8.2%;

[0045] 3...

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Abstract

The invention provides a preparation method of cinchonain Ib. In the method, alcohol extracts of roots, fruits, stems and / or leaves of rosaceous plants, vitaceous vitis plants and smilacaceous plants are used as raw materials, and the raw materials are subjected to multiple liquid chromatographic enrichment and refining to obtain high-purity cinchonain Ib. The invention also provides application of cinchonain Ib in the preparation of drugs for preventing and treating diabetics or diabetic vascular complications, and a pharmaceutical composition comprising cinchonain Ib. The cinchonain Ib has the effect of lowering blood lipid in diabetic rats, has good synergy in controlling the progress of diabetic vascular complications, helps prevent and control metabolic syndromes so that the cinchonain Ib is more significantly advantageous in preventing and treating diabetic vascular complications, is efficient and nontoxic and high in safety and accordingly has a promising application prospect in the clinical prevention and treatment of diabetic vascular complications.

Description

technical field [0001] The invention relates to a preparation method of cinchonine Ib and the application of cinchonine Ib in the preparation of medicines for preventing and treating diabetes and its vascular complications. Background technique [0002] Diabetes mellitus is a metabolic disease characterized by hyperglycemia due to defects in insulin secretion or insulin action. Recent epidemiological surveys have confirmed that the prevalence of diabetes in my country is as high as 11.6%, which has become the highest in the world in terms of the absolute number of diabetic population. In addition, according to the statistics of the World Health Organization, there are more than 100 complications of diabetes, which is currently the disease with the most known complications. The harm of diabetes mainly comes from diabetic vascular complications. Long-term high blood sugar will induce damage to large blood vessels and microvessels and endanger the heart, brain, kidney, periphe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04A61K31/37A61P3/10A61P9/00
CPCC07D493/04
Inventor 刘岱琳宋光明赵艳敏郭敏娜
Owner 天津市尖峰天然产物研究开发有限公司
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