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Application of maca imidazole alkaloid in preparation of cardiovascular drugs

A technology of macamidazole and alkaloid, applied in the field of natural medicinal chemistry, can solve the problems of restricting the research and development of macamidazole alkaloid, large losses, many steps and the like

Inactive Publication Date: 2010-06-30
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The method has many steps, and the loss in the extraction process of maca imidazole alkaloids is relatively large. 10 kilograms of maca dry powder is finally purified to 22 mg of Lepidiline A and less Lepidiline B. This defect restricts maca to a certain extent. The research and development of imidazole alkaloids, especially their application in activity screening and pharmacology, has resulted in the current application of maca imidazole alkaloids being limited to the treatment of proliferative diseases such as tumors

Method used

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  • Application of maca imidazole alkaloid in preparation of cardiovascular drugs
  • Application of maca imidazole alkaloid in preparation of cardiovascular drugs
  • Application of maca imidazole alkaloid in preparation of cardiovascular drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Weigh 1 kg of 40-mesh dry maca root powder and place it in the stainless steel extraction container of a Chinese herbal medicine flash extractor, add 15 kg of ethanol with a mass percentage concentration of 100%, extract for 5 minutes at 8000 rpm, and filter through a 400-mesh filter After the cloth is suction filtered, the filter residue is extracted once again, the filtrate is combined and the extract is recovered, the obtained extract is added to methanol with an equal volume mass percentage concentration of 20% to fully dissolve, and added to a HP20 macroporous adsorption resin column (70×5.5cm i.d.) , using 10 times column volume of water, 5 times column volume mass percent concentration of 10% methanol, 10 times column volume mass percent concentration of 40% methanol solution for elution (containing 0.8% volume fraction of glacial acetic acid), collecting the first The three eluted fractions were evaporated under reduced pressure at 60°C to recover the solvent, th...

Embodiment 2

[0037] Accurately weigh 0.2 g of the macamiazole alkaloid composition (Lepidilines) in Example 1 and dissolve it with methanol, and further purify the macamiazole alkaloid composition through a C18 solid-phase extraction column (the extraction column is 10g / 60ml, and the filler is ODS -A amorphous silicone, Aperture, particle diameter 40-60 μ m), elution adopts methanol: tetrahydrofuran: ammonium acetate solution (19: 1: 80v / v) of 20 mmol / liter, adopts high-performance liquid chromatography technology to monitor four kinds of macamidazole alkaloids Collected, after the solvent is recovered by rotary evaporation under reduced pressure at 50°C, four kinds of macamidazole alkaloid monomers can be obtained by crystallization, and accurately weighed after drying, Lepidiline A is 0.0863 grams (purity 98.5%), and Lepidiline B is 0.0402 grams (purity 98.2%), 0.0192 g (purity 96.8%), 0.0117 g (purity 95.6%). Carry out microscopic observation to these four kinds of monomers and adopt ...

Embodiment 3

[0043] Antitumor effects of macamidazole alkaloid composition and its four monomers:

[0044] Take the maca imidazole alkaloid composition and various imidazole alkaloid monomers in Example 1 and Example 2 to prepare 1 microgram / ml, 10 microgram / ml, 20 microgram / ml, 40 microgram / ml, 80 microgram / ml A total of 5 concentration gradients per milliliter of the test solution were used to study the effects of these substances on human lung cancer cells NCI-H460, human liver cancer cells HepG-2, human bladder cancer cells UMUC3, human pancreatic cancer cells PACA2, human thymoma cancer cells MDA231 and In vitro cytotoxicity of human ovarian cancer cell FDIGROV. Take logarithmic phase tumor cells to make cell suspension (20000 cells / ml), inoculate in the culture plate, 200 microliters per well, pour out the culture medium after culturing for 48 hours, add 20 microliters of various test solutions (set Blank control), after culturing for 24 hours, add 20 microliters of MTT solution, co...

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Abstract

The invention discloses an application of maca imidazole alkaloid, in particular to an application to the preparation of cardiovascular drugs. All or part of the components are prepared from one or mixture of compounds having the following chemical structural formula as shown in formula (I), wherein R1 can be H or CH3, and R2 is H or OCH3. The invention first discovers the remarkable pharmaceutical activity of the compounds on blood pressure drop and arrhythmia resistance. Therefore, the maca imidazole alkaloid prepared by the new process can be used for developing antineoplastic drugs and can be expected to act as drugs for treating corresponding cardiovascular diseases. Formula (I).

Description

technical field [0001] The present invention relates to the field of natural medicine chemistry, in particular, the present invention relates to a kind of imidazole alkaloid directly separated from the natural plant maca (Lepidium meyenii Walper, also commonly known as Lepidium peruvianum Chacon sp.) Applications in cardiovascular medicine. Background technique [0002] Cardiovascular disease is the number one killer of human health, including hypertension, arrhythmia, hyperlipidemia, coronary heart disease and other forms of disease. According to the prediction of the World Health Organization, by 2020, non-communicable diseases will account for the cause of death in my country 79%, of which cardiovascular disease will take the first place. Hypertension is the most common cardiovascular disease, and its prevalence rate is the highest in all countries in the world, and the population of the disease tends to be younger. The population of hypertensive population in my country ...

Claims

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Application Information

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IPC IPC(8): A61K31/4174A61P9/12A61P9/06A61P9/00
Inventor 金文闻余龙江敖明章
Owner HUAZHONG UNIV OF SCI & TECH
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