Marsdenia tenacissima carbon-21 steroid saponin mixture with antineoplastic effect

A technology of steroid glycosides and hibiscus, applied in the field of medicine, can solve the problems that the active ingredients need to be confirmed, the extraction process needs to be improved, the anti-cancer active ingredients are not clear, etc., and the effect of obvious inhibitory effect can be achieved.

Inactive Publication Date: 2008-07-09
ZHEJIANG ACAD OF MEDICAL SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparations "Xiaoping Tablets" and "Xiaoaiping Injection" made from Aegypti aegypti are clinically used to treat esophageal cancer, gastric cancer, lung cancer, and liver cancer, and have achieved good curative effect, but there are the following problems: (1) The extraction process needs to be improved. "Xiaoaiping Tablets" is a tablet made after extraction of Wuguteng water. The daily dosage is 24-30 tablets.
(3) The active ingredients need to be confirmed
The phenolic acid components such as chlorogenic acid in Blackberry are only its anti-inflammatory active ingredients, but the anti-cancer active ingredients are not yet clear

Method used

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  • Marsdenia tenacissima carbon-21 steroid saponin mixture with antineoplastic effect
  • Marsdenia tenacissima carbon-21 steroid saponin mixture with antineoplastic effect
  • Marsdenia tenacissima carbon-21 steroid saponin mixture with antineoplastic effect

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Embodiment 1: the preparation of total glucosides H

[0107] After the cane stem is crushed, reflux 3 times with 70% ethanol for 1 hour each time, combine the extracts, and recover the solvent under reduced pressure to obtain an ethanol extract, which is subjected to silica gel column chromatography and gradient washing with chloroform-ethanol Detach, use thin-layer chromatography to detect chromatographic fractions, combine the fractions with the same single spot, concentrate, and obtain 1, 2, 3, 4, 5, 6, 7, 8, 9 fractions, of which 8 is the total glucosides H of Sage vine. Total glucosides H, yellow-brown powder, both Lieberman-Burchard and Keller-Killiani reactions were positive, showing that it is a steroid compound containing 2-deoxysugar.

Embodiment 2

[0108] Embodiment 2 prepares the clam vine glycoside A

[0109] After the cane stem is crushed, reflux 3 times with 70% ethanol for 1 hour each time, combine the extracts, and recover the solvent under reduced pressure to obtain an ethanol extract, which is subjected to silica gel column chromatography and gradient washing with chloroform-ethanol Detach, use thin-layer chromatography to detect chromatographic fractions, combine fractions with the same single spot, concentrate, and obtain 1, 2, 3, 4, 5, 6, 7, 8, and 9 fractions, divide fractions 8 was separated by low-pressure Rp-18 column (methanol: water) and purified by preparative HPLC (methanol: water) to obtain luciferin A.

[0110] Tongguang vineside A, white amorphous powder, mp142-144℃, [α] D 25 -16.1° (MeOH; c=0.5), molecular formula: C 48 h 74 o 19 . Spectral data analysis and physical and chemical properties determination and literature reports (Shuji Miyakawa, Kimiko Yamaura, Koji Hayashi et al.Five glycoside...

Embodiment 3

[0111] Embodiment 3 prepares the light rattan glycoside B

[0112] After the cane stem is crushed, reflux 3 times with 70% ethanol for 1 hour each time, combine the extracts, and recover the solvent under reduced pressure to obtain an ethanol extract, which is subjected to silica gel column chromatography and gradient washing with chloroform-ethanol Detach, use thin-layer chromatography to detect chromatographic fractions, combine fractions with the same single spot, concentrate, and obtain 1, 2, 3, 4, 5, 6, 7, 8, and 9 fractions, divide fractions 8 was separated by low-pressure Rp-18 column (methanol: water) and purified by preparative HPLC (methanol: water) to obtain luciferin B.

[0113] Tongguang vineside B, white amorphous powder, mp133-134℃, [α] D 25 +11.5°(MeOH; c=0.5), molecular formula: C 51 h 82 o 19 . Spectral data analysis and physical and chemical properties determination and literature reports (Shuji Miyakawa, Kimiko Yamaura, Koji Hayashi et al.Five glycosi...

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Abstract

The invention belongs to the medicine technology field, particularly relating to extract and separate carbon-21steroidal glycosides mixture from traditional medicine Marsdenia tenacissima. The compound mainly comprises five carbon-21 steroidal glycosides compounds which are respectively tenacissosides A, tenacissosides B, tenacissosides C, tenacissosides D and Marsdenoside K. The mixtures in which the content of the global weight of steroidal glycosides compound is larger or equal to 80% is named as Marsdenia tenacissima total glycoside H. The invention further relates to the preparation process of the compound, a medicine compound which uses the compound as active ingredient, and the application of the compound and the medicine compound of the invention in antitumor agent field.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a C-21 steroidal glycoside mixture with anti-tumor effect extracted and separated from the traditional Chinese medicine Marsdeniatenacissima (Marsdeniatenacissima) and total glucosides H of this type of compound as the active compound. Compositions of ingredients, and their application in antitumor. Background technique [0002] Cancer is one of the biggest intractable diseases in the world today. A large number of clinical and experimental studies have proved that Chinese medicine plays an important role in the prevention and rehabilitation of cancer. Finding anti-cancer active ingredients from Chinese herbal medicines not only has great potential for discovering new drugs, but also provides unique insights into the design of more ideal new drugs. chemical structure. [0003] Therefore, many countries and pharmaceutical companies have gradually shifted the focus of anticancer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/7048A61P35/00A61K36/185
Inventor 李晓誉叶益萍陈峰阳徐世芳
Owner ZHEJIANG ACAD OF MEDICAL SCI
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