CN108524678A - A kind of tea seed cake is used as inhibitor for squalene synthetic enzyme and the purposes for lipid-loweringing - Google Patents

A kind of tea seed cake is used as inhibitor for squalene synthetic enzyme and the purposes for lipid-loweringing Download PDF

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Publication number
CN108524678A
CN108524678A CN201810769428.0A CN201810769428A CN108524678A CN 108524678 A CN108524678 A CN 108524678A CN 201810769428 A CN201810769428 A CN 201810769428A CN 108524678 A CN108524678 A CN 108524678A
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China
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tea seed
seed cake
squalene
inhibitor
lipid
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张振强
谢治深
王辉
刘佩
徐江雁
赵振彪
宋军营
闫敏
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Henan University of Traditional Chinese Medicine HUTCM
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Henan University of Traditional Chinese Medicine HUTCM
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/82Theaceae (Tea family), e.g. camellia
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105Plant extracts, their artificial duplicates or their derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23VINDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00Food compositions, function of food ingredients or processes for food or foodstuffs

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  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • General Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Mycology (AREA)
  • Botany (AREA)
  • Nutrition Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Food Science & Technology (AREA)
  • Cardiology (AREA)
  • Polymers & Plastics (AREA)
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  • Gastroenterology & Hepatology (AREA)
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Abstract

It is used as inhibitor for squalene synthetic enzyme the invention discloses a kind of tea seed cake and for the purposes of lipid-loweringing.It is a discovery of the invention that the tea seed cake of camellia meiocarpa is effective inhibitor of squalene synthetase.Squalene synthetase be cholesterol biosynthesis, metabolism a kind of important enzyme, it can be catalyzed two molecule farnesyl diphosphates through reproducibility dimerization, intermediate presqualene diphosphonic acid be generated, under NADPH reductions, presqualene diphosphonic acid generates squalene, the latter's further synthetic cholesterol.Inhibit squalene synthetase activity that can reduce cholesterol levels.Moreover, it has been also reported that, inhibitor for squalene synthetic enzyme can not only reduce cholesterol levels, also reduce triglyceride levels, and then reach lipid-lowering effect.Therefore, the tea seed cake of camellia meiocarpa can be prepared into the food, drug or health products of lipid-loweringing by inhibiting squalene synthetase to play effect for reducing fat.

Description

A kind of tea seed cake is used as inhibitor for squalene synthetic enzyme and the purposes for lipid-loweringing
Technical field
It is used as inhibitor for squalene synthetic enzyme the present invention relates to the tea seed cake of camellia meiocarpa and for the purposes of lipid-loweringing.
Background technology
Camellia meiocarpa (Camellia meiocarpa Hu.) also known as Jiangxi, small tea, heart, Camellia yuansienensis, sheep dung Son etc..Fruit is small, leaf is small, bud is small, and it is its notable feature that bud, bract, which do not have hair,.Camellia meiocarpa it is resistance to it is shady, fruit is small, thin skin, yield are high, Its cultivated area and annual output are only second to C. olelfera, are distributed in the provinces such as Fujian, Jiangxi, Guangxi, Hunan, Guizhou, Jiangsu and Zhejiang Provinces.
Chemical composition contained by camellia meiocarpa mainly has saponin(e, flavones, polyphenol, polysaccharide and protein compound etc..Pharmacology is ground Study carefully and show that oil tea plant not only has antibacterial, anti-inflammatory, clearing heat and detoxicating and other effects, but also is also shown anti-oxidant, antitumor etc. Preferable bioactivity is shown, wherein Sasanguasaponin is notable to the pharmacological activity of cardiovascular and cerebrovascular, however camellia meiocarpa and Related Drug It is seldom to manage active reporter.
Invention content
It is used as inhibitor for squalene synthetic enzyme the purpose of the present invention is to provide the tea seed cake of camellia meiocarpa and for lipid-loweringing Purposes.
The above-mentioned purpose of the present invention is achieved by following technical solution:
The tea seed cake of camellia meiocarpa is used as the purposes of inhibitor for squalene synthetic enzyme.
The tea seed cake of camellia meiocarpa is used to prepare the purposes of the food, drug or health products that reduce cholesterol levels.
The tea seed cake of camellia meiocarpa is used to prepare the purposes of the food, drug or health products that reduce triglyceride levels.
The tea seed cake of camellia meiocarpa is used to prepare the purposes of the food of lipid-loweringing, drug or health products.
The tea seed cake of camellia meiocarpa is used to prepare the use of the food of prevention hyperlipidemia and its caused disease, drug or health products On the way.
Further, disease caused by hyperlipidemia includes hyperlipidemia, atherosclerosis, nonalcoholic fatty liver.
A kind of inhibitor for squalene synthetic enzyme, the tea seed cake containing camellia meiocarpa, also containing can in food, drug or health products With the carrier or excipient of receiving, acceptable dosage form in food, drug or health products is made.
It is a discovery of the invention that the tea seed cake of camellia meiocarpa is effective inhibitor of squalene synthetase.Squalene synthetase is body A kind of important enzyme in inner cholesterol synthesis, metabolic pathway, it can be catalyzed two molecule farnesyl diphosphates through reproducibility dimerization With, intermediate presqualene diphosphonic acid is generated, under the reduction of NADPH, presqualene diphosphonic acid generation squalene, the latter Again through being further synthetically generated cholesterol.Inhibit squalene synthetase activity that can reduce cholesterol levels.It is reported moreover, also having Road points out that inhibitor for squalene synthetic enzyme can not only reduce cholesterol levels, also reduces triglyceride levels (bibliography: Synthesis and biological evaluation of quinuclidine derivatives incorporating phenothiazine moieties as squalene synthase inhibitors.Chem Pharm Bull,2004, 52:1204-1209), and then reach lipid-lowering effect.Therefore, the tea seed cake of camellia meiocarpa can be by inhibiting squalene synthetase hair Wave effect for reducing fat.
Specific implementation mode
Essentiality content of the present invention is specifically introduced with reference to embodiment.
One, experiment material
Take the tea fruit of camellia meiocarpa to clean, air-dry after squeezing deoil after the tea seed cake of camellia meiocarpa is prepared.
C57BL/6J male mices, 18~22g of weight are purchased from Beijing Vital River Experimental Animals Technology Co., Ltd.. Illumination 12h, dark 12h place mouse 5 per cage.Chow diet, high lipid food (D12492,60kcal%) are purchased from Jiangsu Province Cooperate with medical bioengineering Co., Ltd.
Two, experimental method
1, modeling, grouping and administration
After C57BL/6J male mices adaptable fed 1 week, mouse is numbered by weight, using random table by mouse It is divided into blank control group and modeling group, gives corresponding experiment feed diet.Model control group and tea seed cake is low, high dose group is (small Fruit Extracted From Oil-tea-cake 50,100mg/kg), every group 10, sub-cage rearing gives high lipid food nursing in addition to blank group.It weighs within every 7 days One time weight adjusts dosage, and blank control group and model control group give isometric solvent, and the daily gavage of each group mouse is given Relative medicine 1 time, successive administration 10w.
2, lipid determination
It cuts tail and takes total cholesterol, triglycerides, high-density lipoprotein cholesterol and low-density lipoprotein in hematometry blood plasma White cholesterol.Plasma triglyceride, total cholesterol assay kit are purchased from Shanghai Kehua Bio-engineering Co., Ltd, blood plasma Low density lipoprotein cholesterol, high-density lipoprotein cholesterol, glutamic-pyruvic transaminase, glutamic-oxalacetic transaminease assay kit are purchased from Nanjing Bioengineering Research Institute is built up, determination step is carried out by corresponding instructions.
3, squalene expression measures
Last time administration cuts tail and blood is taken to take liver, -80 DEG C of refrigerators to freeze spare for after surveying blood fat, putting to death mouse.
The total serum IgE in liver is extracted by Trizol one-step method, onedrop surveys its purity and concentration, wherein OD260/OD280 It is preferable that its purity is represented 1.8~2.0.After extracting total serum IgE, promise only praises reverse transcription reagent box and carries out reverse transcription acquisition cDNA, instead It is expanded according to RT-PCR reaction systems after transcription, using GAPDH as internal reference, carries out the quantitative analysis of PCR product. Primer sequence is:
Squalene sense primer:5'-AGAGTGGCGGTTCACTGAGA-3';
Squalene downstream primer:5'-GAGAAAGGCCAATTCCCACCA-3';
GAPDH sense primers:5'-TGTGTCCGTCGTGGATCTGA-3';
GAPDH downstream primers:5'-CCTGCTTCACCACCTTCTTGAT-3'.
PCR reaction conditions:95 DEG C of pre-degeneration 10min, 95 DEG C of denaturation 15s, 60 DEG C of annealing 30s, 75 DEG C of extension 30s, 75 DEG C Ultimate extension 1min, totally 45 recycle.Using 2-ΔΔCtMethod calculates the relative expression levels of squalene mRNA.
4, data processing and inversion
Using SPSS19.0 softwares, more comparison among groups are examined using one-way analysis of variance, are compared two-by-two between group and are examined using q It tests.It is that difference is statistically significant with P < 0.05.
Three, experimental result
1, squalene expression comparison result in each group mouse liver tissue
Compared with model group, tea seed cake is low, squalene mRNA expressions significantly reduce (P < in high dose group liver organization 0.05), and degree and the certain dependence of tea seed cake dosage presentation are reduced.It the results are shown in Table 1 (note:The * p compared with blank control group< 0.05, * * p<0.01, * * * p<0.001;Compared with model control group#p<0.05,##p<0.01,###p<0.001)。
Squalene mRNA relative expression levels compare in 1 each group mice serum of table and liver organization
2, the horizontal comparison result of each group lipid of mice
Compared with model group, tea seed cake is low, high dose group total plasma cholesterol, triglycerides significantly reduce, and reduces degree Certain dependence is presented with tea seed cake dosage.It the results are shown in Table 2 (notes:The * p compared with blank control group<0.05, * * p< 0.01, * * * p<0.001;Compared with model control group#p<0.05,##p<0.01,###p<0.001)。
2 each group lipid of mice of table is horizontal
The above results show the camellia meiocarpa dregs of rice by inhibiting the expression of squalene to significantly reduce the total of high blood lipid model mouse Cholesterol, triglycerides can be prepared into food, drug or the health products of prevention high blood ester.In addition, the camellia meiocarpa dregs of rice can be with As the positive drug for screening other inhibitor for squalene synthetic enzyme.
The effect of above-described embodiment is specifically to introduce the essentiality content of the present invention, but those skilled in the art should know Protection scope of the present invention should not be confined to the specific embodiment by road.

Claims (7)

1. the tea seed cake of camellia meiocarpa is used as the purposes of inhibitor for squalene synthetic enzyme.
2. the tea seed cake of camellia meiocarpa is used to prepare the purposes of the food, drug or health products that reduce cholesterol levels.
3. the tea seed cake of camellia meiocarpa is used to prepare the purposes of the food, drug or health products that reduce triglyceride levels.
4. the tea seed cake of camellia meiocarpa is used to prepare the purposes of the food of lipid-loweringing, drug or health products.
5. the tea seed cake of camellia meiocarpa is used to prepare the use of the food of prevention hyperlipidemia and its caused disease, drug or health products On the way.
6. purposes according to claim 5, it is characterised in that:Disease caused by hyperlipidemia includes hyperlipidemia, artery congee Sample hardening, nonalcoholic fatty liver.
7. a kind of inhibitor for squalene synthetic enzyme, it is characterised in that:Tea seed cake containing camellia meiocarpa, also contain food, drug or Acceptable dosage form in food, drug or health products is made in acceptable carrier or excipient in health products.
CN201810769428.0A 2018-07-13 2018-07-13 A kind of tea seed cake is used as inhibitor for squalene synthetic enzyme and the purposes for lipid-loweringing Pending CN108524678A (en)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1475249A (en) * 2002-08-13 2004-02-18 田维熙 Fatty acid synthetic enzyme inhibitor and its production method and application
US20070128300A1 (en) * 2004-01-29 2007-06-07 Nam Jong H Natural tea having effects of hangover relief and liver function recovery and method for preparing the same

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1475249A (en) * 2002-08-13 2004-02-18 田维熙 Fatty acid synthetic enzyme inhibitor and its production method and application
CN1332687C (en) * 2002-08-13 2007-08-22 田维熙 Fatty acid synthetic enzyme inhibitor and its production method and application
US20070128300A1 (en) * 2004-01-29 2007-06-07 Nam Jong H Natural tea having effects of hangover relief and liver function recovery and method for preparing the same

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
李梦丹: "茶油籽粕的综合利用", 《粮食与油脂》 *
顾觉奋: "角鲨烯合成酶抑制剂降血脂作用及机制的研究进展", 《药学进展》 *
龚吉军: "油茶粕多肽降血脂活性研究", 《食品研究与开发》 *

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