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Compound, extraction method thereof, application thereof to preparation of antitumor drugs, and antitumor drugs prepared by using compound

A technology of anti-tumor drugs and extraction methods, applied in the field of medicinal chemistry, can solve the problems that there may be undiscovered in camellia oleifera roots

Inactive Publication Date: 2014-04-23
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Camellia oleifera saponins are mainly extracted from camellia oleifera, but previous studies on camellia oleifera focused on tea seed heart, tea seed cake, camellia oleifera, and camellia oil, and less research was done on camellia oleifera root. There may be undiscovered biologically active substances in camellia oleifera root. Camellia oleifera saponins, therefore, the study of saponins in Camellia oleifera root has important significance

Method used

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  • Compound, extraction method thereof, application thereof to preparation of antitumor drugs, and antitumor drugs prepared by using compound
  • Compound, extraction method thereof, application thereof to preparation of antitumor drugs, and antitumor drugs prepared by using compound
  • Compound, extraction method thereof, application thereof to preparation of antitumor drugs, and antitumor drugs prepared by using compound

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Experimental program
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Effect test

Embodiment 1

[0092] The extraction of embodiment 1 compound

[0093] Take 2kg of dry Camellia oleifera root, grind it into 10-40 mesh wood chips with a grinder, soak in 6L water at 40°C for 8h, heat and reflux at 100°C for 0.5h, filter, add 3L water to the filter residue, and heat to reflux at 100°C 3.0h, filter, the filter residue was mixed with 3L of water, heated to reflux at 100°C for 2h, filtered, combined the filtrate obtained from three times of filtration, and concentrated under reduced pressure at 80°C for 6h to obtain 2000mL of liquid extract.

[0094] Take the prepared liquid extract and mix it with 20000mL water, filter it with a 100-mesh filter cloth, centrifuge the filtrate, take the supernatant and separate it through a D101 macroporous resin column, and then use water, 30% ethanol, 50% ethanol, 60% ethanol, 70 % ethanol, 80% ethanol, and 95% ethanol were eluted, and the components eluted with 70% ethanol to 95% ethanol were collected and concentrated under reduced pressure ...

Embodiment 2

[0107] The extraction of embodiment 2 compound

[0108] Take 2kg of dried Camellia oleifera root, crush it into 10-mesh sawdust with a pulverizer, soak it in 40L of 95% ethanol at 40°C for 24h, heat and reflux at 80°C for 0.5h, filter, add 2L of 95% ethanol to the filter residue, and heat it at 80°C Heat to reflux for 3.0 h, filter, combine the filtrates obtained from two filtrations, and concentrate under reduced pressure at 90° C. for 2 h to obtain 4,200 mL of liquid extract.

[0109] Take the obtained liquid extract and mix it with 4200mL water, filter it with a 200-mesh filter cloth, centrifuge the filtrate, take the supernatant and separate it through a D101 macroporous resin column, and then use water, 30% ethanol, 50% ethanol, 60% ethanol, and 70% ethanol in sequence. % ethanol, 80% ethanol, and 95% ethanol were eluted, and the components eluted with 70% ethanol to 95% ethanol were collected and concentrated under reduced pressure to obtain total saponins of camellia ol...

Embodiment 3

[0111] The extraction of embodiment 3 compound

[0112] Take 2kg of dried camellia oleifera root, grind it into 10-60 mesh sawdust with a grinder, soak it in 20L of 70% ethanol at 80°C for 8h, heat and reflux at 85°C for 3h, filter, collect the filtrate, and concentrate under reduced pressure at 70°C After 6 hours, 2000 mL of liquid extract was obtained.

[0113] Take the prepared liquid extract and mix it with 6000mL water, filter it with a 300-mesh filter cloth, centrifuge the filtrate, take the supernatant and separate it through a D101 macroporous resin column, and then use water, 30% ethanol, 50% ethanol, 60% ethanol, and 70% ethanol in sequence. % ethanol, 80% ethanol, and 95% ethanol were eluted, and the components eluted with 70% ethanol to 95% ethanol were collected and concentrated under reduced pressure to obtain total saponins of camellia oleifera.

[0114] The obtained total saponins of camellia oleifera were first separated by a decompression silica gel column o...

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Abstract

The invention relates to the technical field of medicinal chemistry, in particular to a compound, an extraction method of the compound, application of the compound to the preparation of antitumor drugs, and the antitumor drugs prepared by using the compound. The compound is extracted from a camellia oleifera abel root; structure identification results show that the compound is a novel compound, and the structural formula is shown in the formula I; an in vitro cell test shows that after the compound shown in the formula I acts for 24 h, the compound has a remarkable inhibiting effect (P is less than 0.05) on the growth of human lung cancer A549 cells, B16 murine melanoma cells, human liver cancer BEL-7402 cells and human breast cancer MCF-7 cells; a murine transplantation tumor model test shows that the compound has a remarkable inhibiting effect (P is less than 0.05) on the growth of murine liver cancer H22 transplantation tumors and murine S180 sarcomas, and the dose-effect relationship is remarkable.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a compound, its extraction method, its application in the preparation of anti-tumor drugs and the prepared anti-tumor drugs. Background technique [0002] Camellia oleifera (CameLLia oLeifera AbeL) belongs to the family Theaceae (Theaceae) Camellia genus (CameLLia Linn), is a small evergreen tree. It is named Camellia oleifera because its seeds can be squeezed for oil (tea oil) for consumption. Camellia oleifera is mainly distributed in tropical and subtropical regions, and is produced in the southwest and southeast of my country, covering 17 provinces. The unsaturated fatty acid content of camellia oil is as high as 90%, which is much higher than that of vegetable oil, peanut oil and soybean oil, and the content of vitamin E is twice as high as that of olive oil. It has extremely high nutritional value, so camellia oil has attracted much attention. [0003] In addi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00C07H15/256C07H1/08A61K31/704A61P35/00
Inventor 许琼明杨世林李夏刘艳丽李笑然陈重
Owner SUZHOU UNIV
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