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Meroganocochlearin, pharmaceutical composition thereof and application of pharmaceutical composition

A mixed-source terpene dimer and compound technology, applied in the field of pharmacy, can solve the problems of unreported pharmacological effects

Active Publication Date: 2018-11-27
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

However, there is no report on the pharmacological effects of mixed-source terpene dimer compounds derived from G. cochlear in the treatment of diabetes and obesity

Method used

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  • Meroganocochlearin, pharmaceutical composition thereof and application of pharmaceutical composition
  • Meroganocochlearin, pharmaceutical composition thereof and application of pharmaceutical composition
  • Meroganocochlearin, pharmaceutical composition thereof and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] G. cochlear fruiting bodies (20kg) were crushed and extracted four times with 150L of 95% ethanol, once every 3 days, the extract was concentrated to 4L by vacuum distillation, and then extracted four times with ethyl acetate. The ester layer was concentrated under reduced pressure to obtain 850 g of extract. The extract was eluted with a silica gel column (chloroform: methanol, V / V, 100:0 to 0:100) to obtain 11 fragments I-XI. The VII was eluted by medium pressure column chromatography (MeOH:H 2 O, V / V, 20:80, 40:60, 60:40, 80:20, 100:0) to obtain fragments A-E. Put fragment D by LH-20 (methanol), LH-20 (acetone), normal phase silica gel column chromatography to obtain the crude meroganocochlearin, and then pre-HPLC (MeOH-H 2 O, MeCN-H 2 O) The 98% pure compound meroganocochlearin is obtained. The identification of the compound structure is determined by the comparison and analysis of spectral data. See Table 1 for specific nuclear magnetic data

[0026] Table 1. NMR...

Embodiment 2

[0029] Inhibition experiment of compound meroganocochlearin on α-glucosidase activity:

[0030] Experimental reagents: α-glucosidase, 4-Nitrophenylα-D-glucopyranoside, and positive control Quercetin were purchased from Sigma.

[0031] Experimental method: add different concentrations of the test compound and α-glucosidase solution (final concentration 0.025U / ml), buffer, and substrate (final concentration 1mM) into 96-well microtiter plate in sequence, and mix well. The concentration is set to 3 repeat wells. At the same time, a blank control without drugs and a quercetin positive control were set. Incubate at 37°C for 50 minutes, measure the OD value at 405 nm with a microplate reader, and calculate the inhibition rate of α-glucosidase activity.

[0032] α-Glucosidase inhibition rate (%) = (1-test hole OD 405nm / Control well OD 405nm )×100%

[0033] Experimental results: The compound meroganocochlearin has a strong inhibitory effect on α-glucosidase, and it is concentration-depen...

Embodiment 3

[0036] Inhibition experiment of compound meroganocochlearin on pancreatic lipase activity:

[0037] Experimental reagents: Pancreatic lipase (PPL), p-nitrophenyl butyrate (p-NPB), Tris, positive control Orlistat were purchased from Sigma; D-PBS was purchased from Hyclone; Anhydrous calcium chloride was a chemical reagent from Chengdu Kelon Factory products.

[0038] Experimental method: On a 96-well microtiter plate, mix the test compounds of different concentrations with the PPL solution (final concentration 1.25U / mL) thoroughly, set 3 replicate wells for each concentration, 37℃, 15min; add p -NPB (final concentration 0.5mM), mix well, 37℃, 15min; BioTek PowerWave XS microplate reader measures OD400nm / 630nm value, the detection wavelength is 400nm, and the reference wavelength is 630nm. The experiment set up blank control wells and Orlistat positive control wells at the same time.

[0039] Inhibition rate of PPL activity (%) = (1-experimental well OD 400nm / 630nm / Control well OD...

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Abstract

The invention provides meroganocochlearin which is separated from an ethyl acetate layer of Ganoderma cochlear and is novel in structure, a pharmaceutical composition which takes the meroganocochlearin as an active ingredient, a preparation method of the pharmaceutical composition and application thereof in pharmacy. Through in vitro experiment research, the meroganocochlearin can effectively inhibit activity of alpha-glucosidase and pancrelipase, and therefore can be used for treating diabetes and obesity and used as health-care functional food.

Description

Technical field [0001] The present invention belongs to the field of pharmacology, and specifically relates to meroganocochlearin, a mixed-source terpene dimer compound with a novel structure obtained from the ethyl acetate layer of G. cochlear, and its pharmaceutical composition, as well as its preparation method and application Use in preparing medicines for diabetes or obesity. technical background: [0002] With the continuous improvement of living standards and the increasingly diversified dietary structure, diabetes has become the third most serious disease threatening human health after tumors and cardiovascular diseases. According to statistics from the International Diabetes Federation, approximately 425 million adults worldwide suffered from diabetes in 2017, and it is estimated that by 2045, the number of diabetic patients may reach 629 million. Therefore, it is particularly important to explore effective drugs to prevent and treat diabetes. Alpha-glucosidase belongs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/60A61K31/365A61P3/04A61P3/10
CPCA61P3/04A61P3/10C07D307/60
Inventor 白雪刘吉开姚建能孔清华
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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