CN110269855A - Flavonoid micromolecule compound inhibits the application in pancreatic lipase activity drug in preparation - Google Patents

Flavonoid micromolecule compound inhibits the application in pancreatic lipase activity drug in preparation Download PDF

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Publication number
CN110269855A
CN110269855A CN201910654444.XA CN201910654444A CN110269855A CN 110269855 A CN110269855 A CN 110269855A CN 201910654444 A CN201910654444 A CN 201910654444A CN 110269855 A CN110269855 A CN 110269855A
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China
Prior art keywords
pancreatic lipase
eriodictyol
application
lipase activity
drug
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CN201910654444.XA
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Chinese (zh)
Inventor
刘剑利
缪静宜
孔宇驰
刘悦
曹怡阳
张毓旸
陈俊良
仇萱
纪月
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Liaoning University
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Liaoning University
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Botany (AREA)
  • Hematology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Medical Informatics (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Biotechnology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)

Abstract

The invention belongs to drug or field of health care products, specifically provides a kind of flavonoid micromolecule compound and be applied alone or be used in conjunction with other drugs and inhibit the application in pancreatic lipase activity drug in preparation.The flavonoid micromolecule compound is eriodictyol.Eriodictyol, to inhibit the absorption to triglycerides in diet, has better effects to preventing/treating obesity by inhibiting pancreatic lipase activity.Eriodictyol disclosed by the invention derives from peanut shell, can preferably inhibit pancreatic lipase activity, provides foundation and reference for the drug of pre- preventing obesity, health care product exploitation.Therefore, natural materials eriodictyol disclosed by the invention has bright prospects as the exploitation of fat reducing health product.

Description

Flavonoid micromolecule compound inhibits the application in pancreatic lipase activity drug in preparation
Technical field
The present invention relates to eriodictyols to inhibit the application in pancreatic lipase activity drug, especially pre- preventing obesity in preparation Application in terms of disease belongs to drug or health food research and development technology field.
Background technique
Just announce that obesity is the primary health problem in the whole world early in the World Health Organization in 1997.Obesity can not only cause The cardiovascular diseases such as diabetes, hypertension, dyslipidemia and coronary heart disease will also result in some chronic diseases even mental disease, Reduce quality of life.Heredity, disease, surplus energy will lead to fat generation, the intake of especially food fat is easier to Increase and fat risk occurs.Therefore, the intake or absorption for controlling food fat, can efficiently control obesity.Food fat needs It can be just absorbed after lipase hydrolysis, main reason is that the triglycerides in diet is mostly only by rouge in esophagus Fat enzyme effect is just absorbed by the body after being degraded to diglyceride, monoglyceride, glycerol and fatty acid.In these lipase, pancreas rouge Fat enzyme is the important enzyme of hydrolyzed fat, therefore, can control fertilizer caused by high fat diet by inhibiting the activity of pancreatic lipase It is fat.
It is present on the market there are many slimming drugs at present, such as orlistat, Dihydroberine, panclicin. They all reach weight-reducing purpose by inhibiting lipase active, but are all synthesis class drugs, there is different degrees of side effect, Such as: rebound, anorexia, insomnia, palpitaition.Such case further to seek from natural plants that safe and efficient, side effect is low Pancreatic lipase inhibitor have become a hot topic of research problem.
In recent years, health-care effect and medical value of the functions such as the anti-oxidant, anti-inflammatory of flavone compound, anticancer to the mankind More and more concerns are attracted.Eriodictyol is the flavanone kind composition being widely distributed in plant, is primarily present in flower In raw and peanut shell, there are a variety of pharmacological activity, such as anti-oxidant, anti-inflammatory, analgesia, improves diabetes and glycosuria complication at diuresis Deng, and be applied in the food such as beverage, food and drinks frequently as antioxidant.The present invention is that flavone compound eriodictyol exists Inhibit to provide experimental basis in the application of pancreatic lipase activity.
Currently, eriodictyol inhibits the application in pancreatic lipase activity drug to have not been reported in preparation.
Summary of the invention
It is an object of the present invention to provide a kind of flavonoid micromolecules to inhibit the application in pancreatic lipase activity drug in preparation.This Invention to eriodictyol inhibit pancreatic lipase activity mechanism illustrate, for exploitation prevention obesity health care product provide experiment according to According to.
The technical solution adopted by the present invention are as follows: flavonoid micromolecule compound is applied alone or is preparing with other drugs combination Inhibit the application in pancreatic lipase activity drug.
Above-mentioned application, flavonoid micromolecule compound are preparing the application in preventing/treating antiobesity agents.
Above-mentioned application, the flavonoid micromolecule compound is eriodictyol.
Above-mentioned application, the eriodictyol derive from peanut shell.
Above-mentioned application, the dosage of eriodictyol are 0.5 × 10-5-1.5×10-5mol·L-1。
The invention has the following advantages:
Flavonoid micromolecule eriodictyol of the present invention plays inhibiting effect to pancreatic lipase activity, and pancreatic lipase activity is suppressed The digestion and absorption that food fat can be slowed down afterwards has better effects to preventing/treating obesity.It is small that the present invention provides a kind of flavonoids Whole new set of applications of the molecule eriodictyol in the drug that preparation inhibits pancreatic lipase activity and its related disease.Eriodictyol as the result is shown It is able to suppress pancreatic lipase activity.
Detailed description of the invention
Fig. 1 be mountain balsam phenol solution and pancreatic lipase solution concentration multiple than be respectively 0.5,1,1.5 fluorescence spectrum.
Fig. 2 be mountain balsam phenol solution and pancreatic lipase solution concentration multiple than be respectively 0.5,1,1.5 synchronous fluorescent spectrum Δ λ=15nm.
Fig. 3 be mountain balsam phenol solution and pancreatic lipase solution concentration multiple than be respectively 0.5,1,1.5 synchronous fluorescent spectrum Δ λ=60nm.
In Fig. 1-Fig. 3, curve 1~4 represents eriodictyol concentration successively as 0,0.5 × 10-5、1×10-5、1.5×10- 5mol·L-1。
Specific embodiment
Embodiment 1
Fluorescent spectrometry detects eriodictyol to the inhibiting effect of pancreatic lipase
Take the 1 × 10 of 30 μ L-3mol·L-1The PBS phosphate buffer of pancreatic lipase mother liquor and 2970 μ L mix, then distinguish It is added 3 × 10-3mol·L-15 μ L, 10 μ L, 15 μ L eriodictyol mother liquor mix, make the dense of mountain balsam phenol solution in mixed solution Degree is respectively 0.5 × 10-5、1×10-5、1.5×10-5mol·L-1, 3min is reacted under the conditions of 25 DEG C.
The measurement of fluorescence spectrum: the mountain balsam phenol solution of pancreatic lipase solution and various concentration is mixed in the cuvette of 1cm It is even, it is put into sepectrophotofluorometer, and it is 280nm that excitation wavelength, which is arranged, excitation and transmitted bandwidth are 5nm, launch wavelength model It encloses for 200-500nm.
The measurement of synchronous fluorescent spectrum: by the mountain balsam phenol solution of pancreatic lipase solution and various concentration 1cm cuvette Middle mixing, is put into sepectrophotofluorometer, and scan pattern is arranged to synchronous fluorescence mode Δ λ=15 or 60nm, transmitting Wave-length coverage is set in 200-500nm, and excitation and transmitted bandwidth are 5nm.
Fluorescence results: Fig. 1 is the fluorescence intensity change of pancreatic lipase after various concentration eriodictyol is added under the conditions of 25 DEG C Situation, with being continuously increased for eriodictyol concentration, the fluorescence intensity of pancreatic lipase is gradually decreased, and illustrates to exist therebetween mutual Effect.
Synchronous fluorescent spectrum can measure the variation of fluorescent emission group tyrosine, trp residue surrounding microenvironment, as Δ λ When=15nm, it is able to reflect tyrosine residue surrounding microenvironment situation of change；When Δ λ=60nm, it is able to reflect trp residue Surrounding microenvironment situation of change.As Δ λ=15nm, with the increase of eriodictyol concentration, the emission maximum wave of tyrosine residue It is long to show slight blue shift, as shown in Fig. 2, illustrating that hydrophobicity enhances around tyrosine residue；As Δ λ=60nm, with sage There is apparent red shift in the maximum emission wavelength of the increase of careless phenol concentration, trp residue, as shown in figure 3, illustrating that tryptophan is residual Primitive period encloses increased hydrophilicity, polarity enhancing.The result shows that the addition of eriodictyol changes protein structure, this structure change It may inhibit the activity of pancreatic lipase.

Claims (5)

1. flavonoid micromolecule compound is applied alone or inhibits in pancreatic lipase activity drug with other drugs combination in preparation Using.
2. application as described in claim 1, which is characterized in that flavonoid micromolecule compound is preparing preventing/treating obesity Application in drug.
3. application as claimed in claim 1 or 2, which is characterized in that the flavonoid micromolecule compound is eriodictyol.
4. application as claimed in claim 3, which is characterized in that the eriodictyol derives from peanut shell.
5. application as claimed in claim 3, which is characterized in that the dosage of eriodictyol is 0.5 × 10-5、1×10-5、1.5×10-5mol·L-1。
CN201910654444.XA 2019-07-19 2019-07-19 Flavonoid micromolecule compound inhibits the application in pancreatic lipase activity drug in preparation Pending CN110269855A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111620917A (en) * 2020-05-08 2020-09-04 广西壮族自治区中国科学院广西植物研究所 Isovitexin-2' -O-beta-D-glucopyranoside, and preparation method and application thereof
WO2022207950A1 (en) * 2021-03-29 2022-10-06 Fundacion Universitaria San Antonio (Ucam) Treatment for obesity

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Publication number Priority date Publication date Assignee Title
US20050271755A1 (en) * 2004-05-12 2005-12-08 Ilya Raskin Phytomedicinal compositions for the control of lipid accumulation and metabolism in mammals
JP2009057319A (en) * 2007-08-31 2009-03-19 Hiroshima Pref Gov alpha-GLUCOSIDASE INHIBITOR, METHOD FOR PRODUCING MATERIAL CONTAINING ERIODICTYOL-7-O-GLUCOSIDE, AND FOOD AND DRINK CONTAINING THE SAME
CN103005442A (en) * 2012-12-26 2013-04-03 青岛文创科技有限公司 Chinese herbal medicinal prescription with weight reducing effect
CN107614475A (en) * 2015-09-24 2018-01-19 欣耀生医股份有限公司 Effective in treatment hepatotoxicity wind agitation and the compound of Fatty Liver Disease and application thereof
CN109715170A (en) * 2015-11-19 2019-05-03 财团法人国际教育基金会 The composition and method for preventing or treating fatty pancreas, improve pancreopathy change caused by fatty pancreas, diabetes or other associated diseases
CN109890376A (en) * 2016-10-27 2019-06-14 三得利控股株式会社 Composition is used in PGC-1 α activation

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050271755A1 (en) * 2004-05-12 2005-12-08 Ilya Raskin Phytomedicinal compositions for the control of lipid accumulation and metabolism in mammals
JP2009057319A (en) * 2007-08-31 2009-03-19 Hiroshima Pref Gov alpha-GLUCOSIDASE INHIBITOR, METHOD FOR PRODUCING MATERIAL CONTAINING ERIODICTYOL-7-O-GLUCOSIDE, AND FOOD AND DRINK CONTAINING THE SAME
CN103005442A (en) * 2012-12-26 2013-04-03 青岛文创科技有限公司 Chinese herbal medicinal prescription with weight reducing effect
CN107614475A (en) * 2015-09-24 2018-01-19 欣耀生医股份有限公司 Effective in treatment hepatotoxicity wind agitation and the compound of Fatty Liver Disease and application thereof
CN109715170A (en) * 2015-11-19 2019-05-03 财团法人国际教育基金会 The composition and method for preventing or treating fatty pancreas, improve pancreopathy change caused by fatty pancreas, diabetes or other associated diseases
CN109890376A (en) * 2016-10-27 2019-06-14 三得利控股株式会社 Composition is used in PGC-1 α activation

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111620917A (en) * 2020-05-08 2020-09-04 广西壮族自治区中国科学院广西植物研究所 Isovitexin-2' -O-beta-D-glucopyranoside, and preparation method and application thereof
WO2022207950A1 (en) * 2021-03-29 2022-10-06 Fundacion Universitaria San Antonio (Ucam) Treatment for obesity
ES2925124A1 (en) * 2021-03-29 2022-10-13 Fundacion Univ San Antonio OBESITY TREATMENT (Machine-translation by Google Translate, not legally binding)

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