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Terpenoid and preparation method and application thereof

A technology for terpenoids and hydrates, which is applied in the field of terpenoids and their preparation, can solve the problems such as failure to elucidate the effective material basis of Motherwort herbal medicine, lack of research, influence on development and application, and the like, so as to shorten the time of thrombin Original time, the effect of enhancing blood coagulation function

Active Publication Date: 2014-02-05
CHENGDU FIRST PHARMACEDTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because motherwort not only has the effect of "activating blood" but also has the effect of "hemostatic", its traditional efficacy is closely related to the regulation of blood coagulation, but there are not many studies on this kind of ingredients, and the material basis of the medicinal effect of motherwort has not been well elucidated , which seriously affects the further development and application of

Method used

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  • Terpenoid and preparation method and application thereof
  • Terpenoid and preparation method and application thereof
  • Terpenoid and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1 (-)-(3α, 6β)-3-acetyl-6-hydroxyl-15,16-nor-docahelane-8(9)-en-13-yn-7-ketone (formula III compound) extraction, separation and preparation

[0039] (1) Experimental materials:

[0040] ① Medicinal materials

[0041] Motherwort is collected from Wenjiang District, Chengdu, Sichuan, and identified as the whole herb of Lamiaceae Leonurus japonicus Houtt.

[0042] ②Reagents and fillers

[0043] Column chromatography silica gel, 200-300 mesh (reagent grade), purchased from Qingdao Haiyang Silica Gel Desiccant Factory;

[0044] TLC silica gel G, GF 254 and H (chemically pure), purchased from Qingdao Haiyang Silica Gel Desiccant Factory;

[0045] MCI gel CHP20P, 75-150 μm, is a reversed-phase polystyrene resin, purchased from Mitsubishi Chemical Corporation of Japan;

[0046] Sephadex LH-20 glucan gel, purchased from Sweden Amersham company;

[0047] GF 254 Silica gel preparation thin layer, purchased from Yantai Jiangyou Silica Gel Development Co., Ltd.; ...

Embodiment 2

[0066] Example 2 (-)-(3α, 6β)-3-acetyl-6-hydroxyl-15,16-nordicarbahane-8(9)-en-13-yne-7-ketone (formula III compound) extraction, separation and preparation

[0067] (1) Experimental materials are the same as in Example 1;

[0068] (2) The extraction of medicinal materials is the same as in Example 1;

[0069] (3) Separation and purification of components:

[0070] ① Disperse 1.2Kg of ethanol extract with water (10L), extract with ethyl acetate (3×10L) and n-butanol (3×10L) successively, combine the ethyl acetate part, recover the solvent under reduced pressure, and obtain ethyl acetate extract Cream 400g;

[0071] ②Use silica gel column chromatography to separate the ethyl acetate extract. The type and amount of silica gel are 200-300 mesh and 4Kg respectively, and the petroleum ether-acetone=(100:1)-(0:1) gradient elution is used to collect Petroleum ether-acetone (8:1) elution fraction, denoted as F 6 ;

[0072] ③Further use MCI resin column (reversed-phase polystyren...

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Abstract

The invention provides a terpenoid shown by the formula I or pharmaceutically acceptable salt, ester or hydrate thereof. The invention also provides a preparation and application of the terpenoid. In the invention, a carbon-drop diterpene new compound separated from leonurus is carbon-drop labdane diterpene obtained from the nature for the first time. The compound can obviously shorten the PT (prothrombin time), APTT (activated partial thromboplastin time) and TT (thrombin time) in vitro and obviously increase the amount of FIB (fibrinogen) in blood, and realizes a certain effect on enhancing the coagulation function, thereby providing a new option for developing a novel natural coagulation drug.

Description

technical field [0001] The present invention relates to a terpenoid compound and its preparation method and application. Background technique [0002] Motherwort is listed as the top grade in "Shen Nong's Materia Medica", and its original name is Wei Wei. In "Compendium of Materia Medica", it is called "the holy medicine of the blood family", and it is mainly used to treat "fetal leakage and dystocia, retained placenta, blood dizziness, blood wind, blood pain, metrorrhagia, hematuria" and other diseases. According to modern research, motherwort mainly contains alkaloids, diterpenoids, flavonoids, iridoid glycosides, phenylpropanol glycosides, volatile oils, peptides and fatty acids, etc., and the active researches are mainly alkaloids and diterpenoids. kind: [0003] (1) Alkaloids: Mainly include stachydrine, leonurine, leonurin and leonurin, etc. Modern studies have shown that the total alkaloids of Motherwort have a therapeutic effect on cerebral ischemia-reperfusion in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/16C07C67/48A61K31/22A61P7/04
CPCC07C49/743C07C67/48C07C69/16C07C2602/28
Inventor 彭成熊亮彭芙赵晓梅
Owner CHENGDU FIRST PHARMACEDTICAL CO LTD
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