Crystal form of diterpenoid compound

A compound and crystal form technology, applied in the field of new crystal forms of diterpenoids, can solve the problems of lack of research on anticoagulant components

Active Publication Date: 2014-10-08
CHENGDU FIRST PHARMACEDTICAL CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The anti-platelet aggregation effect is related to the traditional effect of motherwort "blood circulation", but the research on anti-coagulant components is very lacking

Method used

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  • Crystal form of diterpenoid compound
  • Crystal form of diterpenoid compound
  • Crystal form of diterpenoid compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 (-)-(3R,5S,7R,8R,9R,10S,13R,15R)-3-acetoxy-7-hydroxyl-15-ethoxy-9,13; 15,16-bis Extraction, Purification and Structure Identification of Epoxyhalan-6-one (Crystal Form of Compound II)

[0027] (1) Experimental materials:

[0028] ① Medicinal materials

[0029] Motherwort is collected from Wenjiang District, Chengdu, Sichuan, and identified as the whole herb of Lamiaceae Leonurus japonicus Houtt.

[0030] ②Reagents and fillers

[0031] Column chromatography silica gel, 200-300 mesh (reagent grade), purchased from Qingdao Haiyang Silica Gel Desiccant Factory;

[0032] TLC silica gel G, GF 254 and H (chemically pure), purchased from Qingdao Haiyang Silica Gel Desiccant Factory;

[0033] MCI gel CHP 20P, 75-150 μm, is a reversed-phase polystyrene resin, purchased from Mitsubishi Chemical Corporation, Japan;

[0034] Sephadex LH-20 glucan gel, purchased from Sweden Amersham company;

[0035] GF 254 Silica gel preparation thin layer, purchased from Yantai Ji...

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Abstract

The invention provides a crystal form of a compound as shown in the formula II. The crystal form belongs to an orthorhombic crystal system; the space group is P212121; the crystal cell parameters are as shown in the specification, wherein alpha is equal to 90.00 DEG, beta is equal to 99.00 DEG, and gamma is equal to 90.00 DEG; Z is equal to 4; the crystal cell volume is as shown in the specification. The invention also provides a preparation method and application of the crystal form. The compound with the crystal form in the formula II, which is separated from leonurus japonicus, has a certain inhibiting effect on platelet aggregation and has a better effect than clopidogrel bisulfate as an anti-platelet aggregation drug under the same concentration (0.1mM), so that a new choice is provided for developing a novel natural anti-platelet aggregation drug.

Description

technical field [0001] The present invention relates to a new crystal form of diterpenoids. Background technique [0002] Motherwort was first recorded in "Shen Nong's Materia Medica", formerly known as Chiwei, and was listed as top grade. In "Compendium of Materia Medica", it is called "the holy medicine of the blood family". [0003] Motherwort mainly contains alkaloids, diterpenes, flavonoids, iridoid glycosides, phenylethanol glycosides, volatile oils, peptides and fatty acids, etc. Currently, the active researches are mainly alkaloids and diterpenes: [0004] (1) Alkaloids: mainly include stachydrine, leonurine, leonurin, and leonurin. Modern studies have shown that the total alkaloids of Motherwort have a therapeutic effect on cerebral ischemia-reperfusion injury, among which Leonurine can not only protect myocardial cells from ischemic injury through anti-oxidation, but also has neuroprotective activity. [0005] (2) Diterpene: In recent years, the research on its ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/10A61K31/34A61P7/02
CPCC07D493/10
Inventor 彭成熊亮谢晓芳周勤梅郭力刘昭华
Owner CHENGDU FIRST PHARMACEDTICAL CO LTD
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