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Marsdenia tenacissima carbon-21 steroid saponin mixture with antineoplastic effect

A technology of steroidal glycosides and black bone vine, which is applied in the field of medicine, can solve problems such as active ingredients to be confirmed, anti-cancer active ingredients not clear, and extraction process to be improved, and achieve obvious inhibitory effect

Inactive Publication Date: 2010-06-09
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • 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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Example 1: Preparation of total glucoside H

[0107] After being crushed, the cane was refluxed with 70% ethanol for 3 times for 1 hour each time, the extracts were combined, and the solvent was recovered under reduced pressure to obtain an ethanol extract, which was subjected to silica gel column chromatography and washed with a gradient of chloroform-ethanol. Detach, use thin layer chromatography to detect chromatographic fractions, combine fractions with the same single spot, concentrate, and get 1, 2, 3, 4, 5, 6, 7, 8, and 9 fractions, among which fractions 8 is the total glycosides H of hibiscus.

[0108] Total syringosides H, yellow-brown powder, positive for Lieberman-Buchard and Keller-Killiani reactions, showed steroids containing 2-deoxysugar.

Embodiment 2

[0109] Example 2 Preparation of fenugreek A

[0110] After being crushed, the cane was refluxed with 70% ethanol for 3 times for 1 hour each time, the extracts were combined, and the solvent was recovered under reduced pressure to obtain an ethanol extract, which was subjected to silica gel column chromatography and washed with a gradient of chloroform-ethanol. The chromatographic fractions were detected by thin-layer chromatography, the fractions with the same single spot were combined, concentrated, and fractions 1, 2, 3, 4, 5, 6, 7, 8, and 9 were obtained. 8 After separation by a low pressure Rp-18 column (methanol: water) and purification by preparative HPLC (methanol: water), luciferin A was obtained.

[0111] Tengguanoside 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 physicochemical properties determination and literature reports (Shuji Miyakawa, Kimiko Yamaura, Koji Hayashi et ...

Embodiment 3

[0112] Example 3 Preparation of luciferin B

[0113] After being crushed, the cane was refluxed with 70% ethanol for 3 times for 1 hour each time, the extracts were combined, and the solvent was recovered under reduced pressure to obtain an ethanol extract, which was subjected to silica gel column chromatography and washed with a gradient of chloroform-ethanol. The chromatographic fractions were detected by thin-layer chromatography, the fractions with the same single spot were combined, concentrated, and fractions 1, 2, 3, 4, 5, 6, 7, 8, and 9 were obtained. 8 After separation by a low pressure Rp-18 column (methanol: water) and purification by preparative HPLC (methanol: water), sulmoside B was obtained.

[0114] Tengguanoside B, white amorphous powder, mp133-134℃, [α] D 25 +11.5° (MeOH; c=0.5), formula: C 51 H 82 O 19 . Spectral data analysis and physicochemical properties determination and literature reports (Shuji Miyakawa, Kimiko Yamaura, Koji Hayashi et al.Five gl...

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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 whichthe 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, and in particular relates to a mixture of carbon-21 steroid glycosides with anti-tumor effect-total glycosides H extracted from the traditional Chinese medicine Radix Radix (Marsdeniatenacissima) and using the compound as active Pharmaceutical compositions of ingredients, and their use in antitumor. Background technique [0002] Cancer is one of the most difficult diseases in the world today. A large number of clinical and experimental studies have proved that traditional Chinese medicine plays an important role in the prevention and treatment of cancer and rehabilitation. The search for anti-cancer active ingredients from Chinese herbal medicine not only has great potential for the discovery of new drugs, but also provides a unique and unique design for the design of more ideal new drugs. chemical structure. Therefore, many countries and pharmaceutical companies have gradually shifted the foc...

Claims

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Application Information

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