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Preparation method of Ovatodiolide and application of Ovatodiolide in anti-tumor drugs

A technology of dilactone and parsnip dilactone, which is applied in the field of preparation of parsnip dilactone, can solve the problems such as the anti-tumor application patent report of the preparation method of high-content parsnip dilactone, etc.

Inactive Publication Date: 2014-10-01
NANJING ZELANG MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] At present, there are no relevant patent reports on the preparation method of high-content parsnip dilactone and its anti-tumor application

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Preparation of parsnip dilactone

[0025] Take 1 kg of parsnip leaves, crush them into coarse powder, feed from the feed inlet of the head of the continuous countercurrent ultrasonic extraction equipment, add 10 times 90%% ethanol solution from the solvent inlet at the tail of the continuous countercurrent ultrasonic extraction equipment, and carry out continuous countercurrent at 65 °C Ultrasonic extraction for 60 minutes, the ultrasonic frequency is 80KHz, to obtain the extract, the extract is decompressed and the reagent is recovered to obtain the extract, add aluminum oxide (120 mesh) to the extract, mix well, dry and pack the column, and use 6 times the column volume of chloroform- Methanol (2:1) mixed solution was used for elution, TLC detection, and the dilactone fraction of parsnip was collected, concentrated and dried to obtain the crude product of parsnip dilactone. With acetonitrile-0.2% ethylenediamine aqueous solution as the mobile phase, the volume ratio i...

Embodiment 2

[0027] Antitumor Application of Parsnip Dilactone

[0028] 1. Materials

[0029] Animals: Kunming mice, male and female, weighing 20±2g, provided by Nanjing University of Traditional Chinese Medicine.

[0030] Cell line: KB oral epidermoid carcinoma cell line (KB), provided by Shanghai Institute of Materia Medica, Chinese Academy of Sciences.

[0031] 2. Method

[0032] Take 50 mice, each mouse was inoculated with KB tumor fluid, and the next day, they were randomly divided into 5 groups, 10 mice in each group, which were normal saline control group (NS group), positive control group, and low-dose parsnip dilactone group (1mg / kg), middle dose group (2mg / kg), high dose group (4mg / kg). 24 hours after inoculation, the parsnip dilactone administration group was intragastrically administered for 7 consecutive days, and the positive control group was intraperitoneally injected twice during the test, and administered every other day. During this period, the general activities, fu...

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Abstract

The invention discloses a preparation method of Ovatodiolide and an application of Ovatodiolide in anti-tumor drugs. The preparation method comprises the following steps: (1) taking Indian epimeredi herb leaf coarse powder, and performing continuous counter-current ultrasonic extraction by using a 90% ethanol solution to obtain an extracting solution; (2) concentrating the extracting solution, and then performing aluminum oxide column chromatography; (3) performing preparative liquid chromatography separation; (4) performing acetone recrystallization to obtain a high-purity Ovatodiolide crystallization product. The preparation method disclosed by the invention is simple and convenient in process operation, high in yield and small in pollution, and is suitable for producing high-purity Indian epimeredi herb dilactone. Indian epimeredi herb dilactone has an anti-tumor effect, and an intestinal absorption promoter is added into an oral formula of Indian epimeredi herb dilactone so as to facilitate the improvement of bioavailability.

Description

technical field [0001] The invention discloses a preparation method and application of a plant extract, in particular to a preparation method and antitumor application of parsnip dilactone. Background technique [0002] Ovatodiolide, the molecular formula is C20H24O4, the molecular weight is 328.41, and the structural formula is [0003] [0004] Parsnip dilactone is derived from the leaves of the Lamiaceae (Labiatae) parsnip Anisomeles indica (L.) O.Ktze. Parsnip dilactone has cytotoxic activity, and its IC50 on KB cells is 0.6 μg / mL; it has antihypertensive effect, and inhibits the contraction and Ca 2+ flow, causing a transient hypotensive effect in dogs, but not inhibiting angiotensin-converting enzyme (ACE). Inhibition of myocardial contraction, orange anti-calcium ion flow. [0005] At present, there are no relevant patent reports on the preparation method of high-content parsnip dilactone and its anti-tumor application. Contents of the invention [0006] In o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/08A61K31/365A61P35/00
CPCC07D493/08
Inventor 刘东锋杨成东
Owner NANJING ZELANG MEDICAL TECH
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