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C27 spirostane-type steroidal saponin compound and pharmaceutical composition and application thereof

A technology of steroid saponins and spirostane, which is used in C27 spirostane type steroid saponins and their pharmaceutical compositions, applications in medicines, and application fields in the preparation of functional daily chemicals and health care products

Active Publication Date: 2017-07-21
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There is no C of formula (I) in the prior art 27 Spirosterane steroidal saponins and their pharmaceutical compositions, their use in the preparation of drugs for the treatment of bleeding disorders, including the use of drugs for the treatment of dysfunctional uterine bleeding, and reports on their use in the preparation of functional daily chemicals and health products

Method used

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  • C27 spirostane-type steroidal saponin compound and pharmaceutical composition and application thereof
  • C27 spirostane-type steroidal saponin compound and pharmaceutical composition and application thereof
  • C27 spirostane-type steroidal saponin compound and pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] The preparation of six compounds: saponin D, saponin M, saponin Tb, saponin Tc, saponin Tg and pachyflour saponin II:

[0047] 30kg of dried whole herb of Arthia japonica was crushed and extracted 3 times with 75% ethanol under reflux (2 hours each time), the extracts were combined, and the ethanol was recovered under reduced pressure to obtain an aqueous solution. Then the aqueous solution was passed through a macroporous resin (model: YWD-03F; dosage: 12L) column, and eluted with water, 30% EtOH, 70% EtOH, and 95% EtOH, respectively. The solvent of the 70% ethanol elution part was recovered and dried separately to obtain 1.5 kg of 70% EtOH eluate, mixed with 3 kg of silica gel (80-100 mesh), and subjected to 15 kg of silica gel (200-300 mesh) wet column chromatography, Gradient elution with chloroform-methanol-water (10:1:0→8:2:0.2→7:3:0.5), and finally washing the column with methanol, TLC detection and combined to obtain 5 components (Fr.1-Fr .5). Fr.3 (chloroform...

Embodiment 2

[0049] Preparation of saponin Tb, saponin Tc and saponin Tg three compounds:

[0050] Dried Jilin Trillium (Trilliumkamtschaticum) whole herb (10kg) was pulverized and then refluxed with 75% ethanol for 3 times for 2 hours each time. The extracts were combined and the ethanol was recovered under reduced pressure. The recovered solution was extracted three times with n-butanol, concentrated and recovered under reduced pressure to obtain 839.4 g of n-butanol extract. After the n-butanol extract was dissolved, it was eluted with water, 30% EtOH, 70% EtOH, and 95% EtOH respectively through a macroporous adsorption resin column. The solvent in the 70% EtOH eluted part was recovered to dryness respectively to obtain 170.2 g of 70% EtOH eluted product. After 70% ethanol elution was decolorized by MCI, 1700g of silica gel (300-400 mesh) was used for dry packing and loading, and gradient elution was carried out with chloroform-methanol-water (8:2:0.2,7:3:0.5) , combined to obtain 4 p...

Embodiment 3

[0052] Preparation of saponin Tb, saponin Tg, saponin II, 17-hydroxy diosgenin, Spiroconazole A and saponin H, six compounds:

[0053]5 kg of dried rhizomes of Paris polyphylla var. yunnanensis were crushed and extracted three times with 75% ethanol under reflux (2 hours each time). The extracts were combined, and the ethanol was recovered under reduced pressure to obtain an aqueous solution. Then the aqueous solution was passed through a macroporous resin (model: D-101) column, and eluted with water, 30% EtOH, 70% EtOH, and 95% EtOH, respectively. The solvent of the 70% elution part was recovered and dried separately to obtain 225g of 70% EtOH eluate, which was mixed with 450g silica gel (80-100 mesh) and subjected to 2200g silica gel (200-300 mesh) wet column chromatography. ‐methanol‐water (10:1:0→8:2:0.2→7:3:0.5) gradient elution, and finally wash the column with methanol, TLC detection combined to obtain 4 components (Fr.1‐Fr.5 ). Part of Fr.3 (chloroform-methanol-water...

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Abstract

The invention relates to C27 spirostane-type steroidal saponins isolated from Ypsilandra, Trillium and Paris and their preparation method, as well as their application in the preparation of drugs for treating hemorrhagic diseases, and application in the preparation of drugs for treating dysfunctional uterine bleeding, and the preparation of functional daily chemical products and health products. The materials used in a method of the invention are easy to obtain, the method is simple and easily operable, biological experiments of the compound produced show that the compound can induce platelet aggregation activity and hemostatic activity significantly.

Description

[0001] Technical field: [0002] The invention belongs to the field of medicines, in particular to C 27 Spirosterane-type steroidal saponins and pharmaceutical compositions thereof, their application in the preparation of medicines for treating bleeding disorders, including medicines for the treatment of dysfunctional uterine bleeding, and their use in the preparation of functional daily chemical products and health products application. [0003] Background technique: [0004] At present, there are many hemostatic drugs commonly used in clinical practice, and the hemostatic mechanism is also very complicated. The research on hemostatic drugs has always been a hot topic. There are many causes of bleeding, and the complications of certain diseases are often accompanied by bleeding. Therefore, symptomatic treatment is required at the same time as the application of hemostatic drugs. The corresponding hemostatic drugs should be selected according to different bleeding causes, blee...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/7048A61P15/08A61P7/04A23L33/11A23L33/125A61K8/63
CPCA23V2002/00A61K8/63C07J71/0005A23V2200/30A23V2250/2136
Inventor 刘海洋倪伟严欢秦徐杰陈昌祥
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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