2,6-epoxydiphenylheptane compounds and preparation method and application thereof, and pharmaceutical compositions and application thereof

A technology of epoxy diphenylheptane and compounds, which is applied in the field of drug preparation, and can solve problems such as treatment or improvement of diabetes with pyranol that has not been disclosed

Active Publication Date: 2020-03-24
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, the prior art has not disclosed tsaokopyranols (tsaokopyranols) compounds and their reports for treating or improving diabetes

Method used

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  • 2,6-epoxydiphenylheptane compounds and preparation method and application thereof, and pharmaceutical compositions and application thereof
  • 2,6-epoxydiphenylheptane compounds and preparation method and application thereof, and pharmaceutical compositions and application thereof
  • 2,6-epoxydiphenylheptane compounds and preparation method and application thereof, and pharmaceutical compositions and application thereof

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preparation example Construction

[0032] The present invention provides a preparation method for the 2,6-epoxydiphenylheptane compound described in the above technical scheme, comprising the following steps:

[0033] Carrying out reflux extraction of Tsao Kuo to obtain extract;

[0034] 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;

[0035] The subfraction 1 was subjected to the second silica gel column chromatography, the first Sephadex LH-20 column chromatography and thin layer chromatography to obtain the compound with the structure shown in formula 13;

[0036] The subfraction 2 is subjected to the third silica gel column chromatography and the second Sephadex LH-20 column chromatography column chromatography, and then the f...

Embodiment 1

[0058] Preparation of Compounds 1-13:

[0059] 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;

[0060] 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;

[0061] The seven fractions were tested by TLC respectively, and according to the test results, the fraction Fr.A-4 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 2,6-epoxydiphenylheptane compounds and a preparation method and application thereof, and pharmaceutical compositions and application thereof, belonging to the technical field ofdrug preparation. The 2,6-epoxydiphenylheptane compounds provided by the invention mainly include tsaokopyranol compounds with 13 structures, and the compounds have obvious inhibitory activity on alpha-glucosidase, can form pharmaceutical compositions with a medicinal carrier or an excipient, and can be used for preparing alpha-glucosidase inhibitor drugs, hypoglycemic drugs or health-care food.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to a 2,6-epoxydiphenylheptane compound, a preparation method and application thereof, a pharmaceutical composition and application thereof. Background technique [0002] Diabetes is one of the most serious chronic diseases in the world, caused by congenital or acquired defects in insulin secretion and decreased responsiveness of the body to insulin secretion. These deficiencies lead to elevated blood sugar and ultimately damage to the nervous and metabolic systems. An effective way to alleviate diabetes-related conditions is to control blood sugar levels by inhibiting α-glucosidase, a key enzyme in the gut that hydrolyzes carbohydrates into simple sugars. Clinically, acarbose and voglibose are used to inhibit the activity of α-glucosidase and treat type II diabetes. However, the use of these drugs can cause adverse gastrointestinal side effects and weight gain, so res...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D309/10C07D309/22A61P3/10A61K31/351
CPCA61P3/10C07D309/10C07D309/22
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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