Total alkaloid extract of willow-leaved wintersweet and its preparation method and application

An alkaloid and willow leaf technology, which is applied in the fields of food science, drug combination, pharmaceutical formulation, etc., can solve problems such as the research on alkaloid monomer compounds that have not been seen, achieve simple and easy extraction and preparation processes, simplify treatment plans, reduce effect of treatment cost

Active Publication Date: 2018-07-24
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, there has been no application of willow-leaved wintersweet extract for gastric cancer and colon cancer drugs, and there has been no report on the relevant research on the willow-leaved wintersweet total alkaloid extract and its alkaloid monomer compounds

Method used

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  • Total alkaloid extract of willow-leaved wintersweet and its preparation method and application
  • Total alkaloid extract of willow-leaved wintersweet and its preparation method and application
  • Total alkaloid extract of willow-leaved wintersweet and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Embodiment 1: Preparation of the total alkaloid extract of Wintersweet willow

[0024] Take a dry weight of 2.0 kg of wax plum branches and leaves, crush them, and cold-soak them with 3 times the amount of 90% methanol at room temperature for 24 hours, a total of 3 times. Combine 3 extracts, concentrate under reduced pressure to obtain 300 g extract, suspend with 2 times the amount of 3% tartaric acid aqueous solution, extract three times with ethyl acetate equal to the volume of the suspension, and then use Na 2 CO 3 The tartaric acid aqueous solution was adjusted to pH = 10, and then extracted three times with chloroform, and the chloroform extracted part was concentrated under reduced pressure to obtain 2.3 g of extract, which was the total alkaloid extract of Waxwort.

Embodiment 2

[0025] Embodiment 2: Preparation of the total alkaloid extract of Chimerus osmanthus

[0026] Take 2.0 kg dry wintersweet branches and leaves, crush them, reflux with 80% ethanol at room temperature for 3 hours, repeat 3 times, combine the extracts, concentrate under reduced pressure to obtain 330 g of extract, use 2 times the amount of 3% tartaric acid for the extract Suspended in aqueous solution, extracted three times with ethyl acetate equal to the volume of the suspension, and then washed with Na 2 CO 3 The tartaric acid aqueous solution was adjusted to pH = 10, extracted three times with an equal volume of chloroform, and the chloroform extracted part was concentrated under reduced pressure to obtain 2.6 g of the total alkaloid extract of Wintersweet.

Embodiment 3

[0027] Embodiment 3: Preparation of alkaloid monomer compound (1−4)

[0028] Mix 2.0 g of the prepared total alkaloid extract with equal-fold silica gel (100-200 mesh), and perform column chromatography with 50 times the amount of silica gel (200-300 mesh), using dichloromethane: methanol as the mobile phase Gradient elution (volume ratio 1:0-0:1). Collect dichloromethane:methanol (15:1, volume ratio) elution fraction, this fraction continues through silica gel column, adopts dichloromethane:methanol 50:1, 30:1, 10:1 elution, for 30: 1. The eluted fraction was purified by preparative HPLC, eluted isocratically with methanol:water:diethylamine (68:32:0.05%), and the fraction was collected for 17.2 minutes to obtain 12.2 mg of white amorphous powder (−) -chimonanthine (3), the fraction was collected for 13.0 min, and 8.1 mg of white amorphous powder salicifoxazine B (2) was obtained; it was eluted isocratically with methanol: water: diethylamine (75:25:0.05%), and the fraction ...

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Abstract

The invention belongs to the field of medicines and health products, and concretely relates to an application of Chimonanthus salicifolius total alkaloid extract and monomer compounds thereof in the preparation of medicines or health products for treating gastrointestinal tumor diseases. The Chimonanthus salicifolius total alkaloid extract and chimonanthine monomer compounds (1-4) are extracted and prepared from a Calycanthaceae Chimonanthus plant Chimonanthus salicifolius, and experiments prove that the Chimonanthus salicifolius total alkaloid extract can substantially inhibit proliferation of stomach cancer SGC-7901, colorectal carcinoma SW1116 and colorectal carcinoma HCT116 cells and induce cancer cell apoptosis, and the alkaloid monomer compounds have different inhibition effects on the stomach cancer SGC-7901, colorectal carcinoma SW1116 and colorectal carcinoma HCT116 cells. The Chimonanthus salicifolius extract and the monomer compounds thereof can be applied individually or together or be combined with a suitable excipient, can be processed through a routine method to prepare an oral or non-oral dosage form used for treatment or assisted treatment of gastrointestinal tumor diseases, and is especially suitable for being used to prepare medicines or health products for treating stomach cancer and colorectal carcinoma.

Description

technical field [0001] The invention belongs to the field of medicine and health care products, and in particular relates to a total alkaloid extract of Chimerus osmanthus and its preparation method and application, in particular to the use of the total alkaloid extract of Chimera osmanthus and its monomer compounds in the preparation and treatment of digestive tract tumor diseases Applications in medicine or health care products. technical background [0002] The prior art discloses that gastric cancer and colon cancer are common digestive system tumors in my country. In terms of morbidity and mortality, gastric cancer ranks first in various malignant tumors in my country, and colon cancer is also on the rise year by year in my country. Developed countries should be listed in the top three. For the two common tumors of the digestive system, modern medicine usually uses surgical treatment as the main treatment, supplemented by chemotherapy. Medical practice shows that the ab...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D519/00A61K36/185A61K31/5365A61K31/407A61P1/00A61P35/00A23L33/10
Inventor 胡金锋麻光磊杨国勋熊娟
Owner FUDAN UNIV
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