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Diphenyl heptane compound and preparation method and application thereof, and pharmaceutical composition and application thereof

A technology for diphenylheptane and compound, which is applied in the field of diphenylheptane compound and its preparation, can solve the problems of treating or improving diabetes without an alpha-glucosidase inhibitor of oxalol

Active Publication Date: 2020-04-07
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there is no report of herbitol in the prior art, and there is no report of herbitol as an α-glucosidase inhibitor and for the treatment or improvement of diabetes

Method used

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  • Diphenyl heptane compound and preparation method and application thereof, and pharmaceutical composition and application thereof
  • Diphenyl heptane compound and preparation method and application thereof, and pharmaceutical composition and application thereof
  • Diphenyl heptane compound and preparation method and application thereof, and pharmaceutical composition and application thereof

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preparation example Construction

[0033] The present invention provides the preparation method of diphenylheptane compound described in above-mentioned technical scheme, comprises the following steps:

[0034] Carrying out reflux extraction of Tsao Kuo to obtain extract;

[0035] The extract is mixed with an extraction solvent for extraction, the obtained extract is subjected to the first silica gel column chromatography separation, the obtained fraction is subjected to TLC detection, and then the fraction containing the target compound is subjected to MCI column chromatography to obtain sub Fraction 1~5;

[0036] The sub-fraction 1 was sequentially subjected to the second silica gel column chromatography and the first Sephadex LH-20 column chromatography to obtain compounds with structures shown in formula 10 and formula 11;

[0037] The sub-fraction 2 is subjected to the third silica gel column chromatography to obtain sub-fractions 1-5;

[0038] The sub-fraction 2 is sequentially subjected to the fourth s...

Embodiment 1

[0062] Preparation of Compounds 1-11:

[0063] Take the dried fruit of Cao Guo, crush it, and reflux extract it with 50% ethanol for three times, each time for 2 hours, combine the ethanol extract, recover the ethanol under reduced pressure, and obtain the extract;

[0064] The extract was dispersed in water and extracted with ethyl acetate, and the ethyl acetate extraction part (fraction) was concentrated; the fraction (Fr.A) was subjected to silica gel column chromatography, and methanol-chloroform (0:100 , 5:95, 10:90, 20:80 and 40:60, v / v) were obtained by gradient elution of the eluent to obtain seven fractions, which were respectively denoted as Fr.A-1~Fr.A-7;

[0065] The seven fractions were tested by TLC respectively, and according to the test results, the fraction Fr.A-5 was subjected to MCI column chromatography (the eluent was methanol-water, and the volume ratios of methanol and water were 40:60, 60:40, respectively). , 80:20, 90:10, 100:0) were eluted to obtain ...

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Abstract

The invention provides a diphenyl heptane compound and a preparation method and application thereof, and a pharmaceutical composition and an application thereof, and relates to the technical field ofmedicine preparation. The diphenyl heptane compound provided by the invention mainly comprises amomum tsao-ko alcohol compounds with 11 structures, and the compounds have obvious inhibitory activity on alpha-glucosidase, can form a pharmaceutical composition with a medicinal carrier or excipient, and can be used for preparing alpha-glucosidase inhibitor drugs, hypoglycemic drugs or health-care foods.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to a diphenylheptane compound, a preparation method and application thereof, a pharmaceutical composition and application thereof. Background technique [0002] Diphenylheptane is a kind of natural product characterized by 1,7-diphenylheptane, which is mainly distributed in Zingiberaceae, Betaceae, Myricaceae, Aceraceae, Olive and Juglandaceae and other plants. Diphenylheptanes have various structures, they can be intramolecularly cyclized and polymerized, and can also be combined with other types of compounds. These compounds have various biological activities such as anti-inflammatory, anti-oxidant, anti-tumor, anti-obesity, estrogenic, leishmaniacidal, melanogenic, hepatoprotective and neuroprotective. Therefore, diphenylheptane is increasingly considered as a potential therapeutic drug. [0003] Amomum tsao-ko Crevost et Lemaire is a perennial herb belonging to th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04C07D319/06C07D307/32C07D309/30C07D305/08C07C49/255C07C45/78A61K31/365A61K31/357A61K31/341A61K31/351A61K31/337A61K31/12A61P3/10A23L33/10
CPCA23V2002/00A23L33/10A61P3/10C07C49/255C07D305/08C07D307/32C07D309/30C07D319/06C07D493/04A23V2200/328
Inventor 耿长安何小凤陈纪军张雪梅黄晓燕马云保李天泽胡敬
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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