Composition for suppressing neuraminidase activity comprising geranylated flavonoid derived from paulownia tomentosa as active ingredient

A technology of neuraminidase and active ingredients, which is applied in the field of compositions that inhibit neuraminidase activity, and can solve problems such as side effects, low efficacy, and low bioavailability

Active Publication Date: 2016-06-15
IND ACADEMIC COOP FOUND GYEONGSANG NAT UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the case of zanamivir, although it has a high antiviral effect, it has the disadvantages of low bioavailability and rapid excretion from the kidneys (Ryan, D.M. et al. Antimicrob. Agents Chemother., 39, 2583, 1995), while Oseltamivir has been reported as a side effect causing severe vomiting
[0009] The antivirals developed so far have caused serious side effects, and their application requires more attention
In addition, there is a problem in the development of vaccines that if the circulating virus type is inconsistent with the virus of the vaccine, the effect will be low. Therefore, it is necessary to develop a new influenza virus agent with a significant infection inhibitory effect and good safety.

Method used

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  • Composition for suppressing neuraminidase activity comprising geranylated flavonoid derived from paulownia tomentosa as active ingredient
  • Composition for suppressing neuraminidase activity comprising geranylated flavonoid derived from paulownia tomentosa as active ingredient
  • Composition for suppressing neuraminidase activity comprising geranylated flavonoid derived from paulownia tomentosa as active ingredient

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0360] Preparation of Paulowniatomentosa Extract

[0361]To prepare Paulownia tomentosa extract, 1 kg of Paulownia tomentosa fruit (Jinju, Republic of Korea) dried in the shade was crushed and washed with methanol The extraction was repeated three times at room temperature. The Paulownia tomentosa methanol extract obtained by the above process was concentrated under reduced pressure to obtain 118 g of a dark brown crude extract (yield: 11.8%).

Embodiment 2

[0362] Preparation of Paulowniatomentosa Fraction

[0363] After dissolving 118g of the dark brown crude extract of Paulownia tomentosa in the in distilled water and ethyl acetate mixed solvent, the ethyl acetate was classified, passed through anhydrous Na 2 SO 4 The ethyl acetate fractionated above was dried to obtain 16 g of fractions.

Embodiment 3

[0364] Isolation and Purification of Novel Compounds from Paulowniatomentosa Extract

[0365] Isolation and purification of geranyl flavonoid (geranylatedflavonoid) compound

[0366] In order to separate and purify flavones from the ethyl acetate fraction obtained by the method of , silica gel column chromatography (200-400mesh) was carried out using a mixed solvent of hexane and ethyl acetate (50:11:1), Seven fractions (A-E) were obtained.

[0367] Fraction A (4.2 g) was subjected to silica gel column chromatography using a mixed solvent of hexane and acetone (100:11:1) to obtain nine fractions (A1-A9). Using Sephadex (LH-20, PharmaciaBiotech AB, Uppsla, Sweden) and by 80% methanol solvent, fractions A3 and A4 (460 mg) mixed with No. 5 and No. 9 compounds were experimented, and No. 5 compounds were isolated ( 25mg) and No. 9 compound (18mg). Fraction B (8.9 g) was subjected to silica gel column chromatography using a mixed solvent of chloroform and acetone (100:11:1) to o...

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PUM

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Abstract

The present invention relates to a composition for suppressing neuraminidase activity comprising a geranylated flavonoid derived from Paulownia tomentosa as an active ingredient. The Paulownia tomentosa extract and the geranylated flavonoid isolated therefrom exhibit an effect in significantly suppressing neuraminidase, which is an enzyme that plays an important role in the occurrence of pathogenic viral and bacterial infections and of the inflammation that accompanies such infection, and thus the Paulownia tomentosa extract or the geranylated flavonoid isolated therefrom can advantageously be used as an active ingredient in a composition for suppressing neuraminidase activity.

Description

technical field [0001] The present invention relates to a composition for inhibiting the activity of neuraminidase comprising geranylated flavonoids from Paulowniatomentosa. Background technique [0002] Paulowniatomentosa is a deciduous broad-leaved tree belonging to the genus Paulowniacese that is native to Ulleungdo and is widely grown nationwide. Its leaves are broadly oval and large, with acuminate tips and white cottony hairs. Its flowers are panicles with bell-shaped corollas and petals with purple stripes. The tree is geographically widely distributed in Korea, China, and Japan. In traditional Chinese medicine, it is believed that its bark is called paulownia, which is used for the treatment of gonorrhea, contusion, etc., and promotes hair moistening and regeneration, and is also used as a deodorant. [0003] Examples of components of Paulownia tomentosa known so far include catapol, syringin, aucubin, coniferin, acteoside, Paulownin (lignan), sesamin (+)-piperit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/80A61P31/16
CPCA61K31/353A61K36/185A61K36/80A61K45/06A61K2236/33A61P31/16
Inventor 朴基励严洙贤柳永培赵廷根
Owner IND ACADEMIC COOP FOUND GYEONGSANG NAT UNIV
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