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Tripolybenzylisoquinoline alkaloid, and preparation method, pharmaceutical composition and application thereof

A composition and drug technology, applied in the field of medicine, can solve the problems of unprovided ingredients and activity data, tumor cell apoptosis, etc., and achieve the effect of strong effect and inhibition of NO production

Active Publication Date: 2021-08-06
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some studies suggest that kudzu alkaloids have an inhibitory effect on tumor cells and can induce tumor cell apoptosis; however, no clear composition and activity data have been given

Method used

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  • Tripolybenzylisoquinoline alkaloid, and preparation method, pharmaceutical composition and application thereof
  • Tripolybenzylisoquinoline alkaloid, and preparation method, pharmaceutical composition and application thereof
  • Tripolybenzylisoquinoline alkaloid, and preparation method, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The dried rhizomes (50kg) of Pueraria batica were pulverized, soaked overnight with 95% ethanol, and extracted three times under reflux, 120 L each time, 2 hours. The three extracts were combined and concentrated under reduced pressure to obtain 7kg of total extract. Dissolve 7kg extract in 70L aqueous solution, add hydrochloric acid to adjust pH = 2, filter to remove insoluble matter (4kg); after extraction with ethyl acetate, add ammonia water to the acidic aqueous solution to adjust pH = 10; dichloromethane (50L ) was extracted three times, the combined extracts were concentrated under reduced pressure to obtain 800 g of total alkaloids in the rhizome of Pueraria japonica.

[0055] 400 g of total alkaloids were taken for separation by basic silica gel (200-300 mesh) column chromatography. Use dichloromethane (100L), dichloromethane: methanol = 80: 1 (30L), dichloromethane: methanol = 40: 1 (15L), dichloromethane: methanol = 30: 1 (70L), dichloromethane Methane: Met...

Embodiment 2

[0062] The dried rhizomes (50kg) of Pueraria batica were pulverized, soaked overnight with 95% ethanol, and extracted three times under reflux, 120 L each time, 2 hours. The three extracts were combined and concentrated under reduced pressure to obtain 7kg of total extract. Dissolve 7kg extract in 70L aqueous solution, add hydrochloric acid to adjust pH = 2, filter to remove insoluble matter (4kg); after extraction with ethyl acetate, add ammonia water to the acidic aqueous solution to adjust pH = 10; dichloromethane (50L ) was extracted three times, the combined extracts were concentrated under reduced pressure to obtain 800 g of total alkaloids in the rhizome of Pueraria japonica.

[0063] 400 g of total alkaloids were taken for separation by basic silica gel (200-300 mesh) column chromatography. Use dichloromethane (100L), dichloromethane: methanol = 80: 1 (30L), dichloromethane: methanol = 40: 1 (15L), dichloromethane: methanol = 30: 1 (70L), dichloromethane Methane: Met...

Embodiment 3

[0071] The dried rhizomes (50kg) of Pueraria batica were pulverized, soaked overnight with 95% ethanol, and extracted three times under reflux, 120 L each time, 2 hours. The three extracts were combined and concentrated under reduced pressure to obtain 7kg of total extract. Dissolve 7kg extract in 70L aqueous solution, add hydrochloric acid to adjust pH = 2, filter to remove insoluble matter (4kg); after extraction with ethyl acetate, add ammonia water to the acidic aqueous solution to adjust pH = 10; dichloromethane (50L ) was extracted three times, the combined extracts were concentrated under reduced pressure to obtain 800 g of total alkaloids in the rhizome of Pueraria japonica.

[0072]400 g of total alkaloids were taken for separation by basic silica gel (200-300 mesh) column chromatography. Use dichloromethane (100L), dichloromethane: methanol = 80: 1 (30L), dichloromethane: methanol = 40: 1 (15L), dichloromethane: methanol = 30: 1 (70L), dichloromethane Methane: Meth...

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Abstract

The invention discloses a tripolybenzylisoquinoline alkaloid, and a preparation method, a pharmaceutical composition and application thereof, belongs to the field of medicines, and particularly relates to a group of tripolybenzylisoquinoline alkaloids from Menispermum dauricum DC., which are menidaurine E, menidaurine F, menidaurine G and menidaurine H. The compounds have remarkable anti-tumor and anti-inflammatory activity; and the compound shows a strong inhibition effect on a plurality of tumor cell strains. The invention also relates to the pharmaceutical composition containing an effective dose of the compound, a pharmaceutically acceptable carrier, and an application of the pharmaceutical composition in the field of tumor and immune disease treatment.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a group of trimeric benzylisoquinoline alkaloids with strong biological activity, its preparation method, pharmaceutical composition and application in the preparation of antitumor drugs or drugs for preventing or treating immune diseases. Background technique [0002] Malignant tumor is one of the important diseases that threaten human health. According to statistics, there were 4.292 million new cancer cases and 2.814 million cancer-related deaths in my country in 2015. Chemotherapy is one of the main means of treating cancer, including alkylating agents, antimetabolites, antibiotics, plant alkaloids, sterol hormones and other anticancer drugs. [0003] Searching for anti-cancer active ingredients from natural products and developing new drugs is an important way to create anti-tumor drugs with new structures. Among the discovered natural anti-tumor active ingredients, a considerable par...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D217/20A61P35/00A61P19/02A61P13/12A61P1/00A61P9/00A61P29/00A61P25/28A61P25/16A61P25/00A61K31/4725
CPCC07D217/20A61P35/00A61P19/02A61P13/12A61P1/00A61P9/00A61P29/00A61P25/28A61P25/16A61P25/00
Inventor 屈晶张丹季鸣金晶鲍秀琦臧彩霞陈龙代明珠
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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