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Vibsanin B, preparation method and uses thereof

A technology of viburnin and acetone is applied in the field of its preparation and viburnin, which can solve the problems that there is no anti-inflammatory activity or antitumor activity of viburnin and its mechanism of action.

Inactive Publication Date: 2016-03-02
RUIJIN HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the anti-inflammatory activity or anti-tumor activity of viburnum and its mechanism of action.

Method used

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  • Vibsanin B, preparation method and uses thereof
  • Vibsanin B, preparation method and uses thereof
  • Vibsanin B, preparation method and uses thereof

Examples

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preparation Embodiment 1

[0030] The preparation of viburnum B: after 22 kg of dry grass branches and leaves are pulverized, extract 3 times (2 days / time) with 80% acetone at room temperature, combine the extracts, concentrate under reduced pressure, add water to disperse, extract with ethyl acetate, water The volume ratio to ethyl acetate was 1:1.2, and the combined organic phase was concentrated to obtain 700 g of the crude extract. After the crude extract was dissolved, the sample was mixed with 100-200 mesh silica gel (the mass ratio of crude extract to silica gel was 1:1), Put on a 100-200 mesh silica gel column, and use petroleum ether / acetone system (volume ratio v / v is 9:1, 8:2, 7:3, 6:4, 0:1 in sequence) for gradient elution. Then the 7:3 and 6:4 section concentrates are mixed with polyamide respectively (the mass ratio of concentrate to polyamide is 1:1), and put on the RP-18 medium pressure chromatographic column (MPLC,), and the mass fraction is 75 %, 80%, 85% methanol aqueous solution elut...

preparation Embodiment 1

[0043] According to the method of Preparation Example 1, vibinin and salts made from organic acids (tartaric acid, citric acid, formic acid, oxalic acid, etc.) or inorganic acids (hydrochloric acid, sulfuric acid, phosphoric acid, etc.) were prepared, and conventionally added Water for injection, finely filtered, potted and sterilized to make injection solution.

preparation Embodiment 2

[0045] According to the method of Preparation Example 1, vibinin and salts made from organic acids (tartaric acid, citric acid, formic acid, oxalic acid, etc.) or inorganic acids (hydrochloric acid, sulfuric acid, phosphoric acid, etc.) were prepared, and dissolved In sterile water for injection, stir to dissolve, filter with a sterile suction filter funnel, and then aseptic fine filter, then pack in 2 ampoules, lyophilize at low temperature and seal aseptically to obtain a powder injection.

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Abstract

The present invention relates to vibsanin B, a preparation method and uses thereof. The vibsanin B preparation method comprises: (1) crushing dried viburnum awabuki branches and leaves, extracting with acetone, concentrating, adding water, dispersing, extracting with ethyl acetate, combining the organic phase, and concentrating to obtain a crude extract; (2) loading the crude extract onto a silica gel column chromatography segment; (3) decolorizing and removing large polar components through polyamide medium pressure column chromatography; and (4) purifying through normal phase column chromatography to obtain the vibsanin B. The present invention further provides the uses of the vibsanin B in preparation of anti-inflammatory drugs and anti-leukemia drugs. According to the present invention, the vibsanin B provides significant anti-inflammatory activity in the transgenic zebrafish inflammation model, and provides significant inhibition effects on leukemia cell line Kasumi-1 cell proliferation.

Description

technical field [0001] The invention relates to the field of pharmaceutical compounds and pharmaceutical technology. Specifically, the present invention relates to vibinin, its preparation method and use. Background technique [0002] Vibsane-type diterpenes are a very rare class of natural products. So far, only four species of Viburnum and one lichen have been isolated, and they are mainly divided into three types of skeletons: eleven-membered rings, seven-membered rings, and rearranged skeletons, and these compounds have a wide range of biological activities, such as neurogrowth-stimulating activity, fish-killing activity, anti-tumor activity, etc. (see Heterocycles, 2010, 81, 1571). For example, neovibsanin, neovibsanin A, and neovibsanin B can significantly promote the growth of nerve cells at a concentration of 40 μM (see J.Neurochem.1995, 64, 1954; Science, 2002, 296, 1648). Viburnum C (VibsaninC), 5-epi-VibsaninC (5-epi-VibsaninC), 5-epi-VibsaninC (5-epi-Vibsanin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C67/48C07C69/533A61K31/22A61P29/00A61P35/02
Inventor 陈竺陈赛娟赵勤实邓旭叶柏新何隽罗柳飞
Owner RUIJIN HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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