CN109172577A - The anti-syndrome of blood stasis application of scirpusin ingredient C in trigone - Google Patents

The anti-syndrome of blood stasis application of scirpusin ingredient C in trigone Download PDF

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CN109172577A
CN109172577A CN201810975463.8A CN201810975463A CN109172577A CN 109172577 A CN109172577 A CN 109172577A CN 201810975463 A CN201810975463 A CN 201810975463A CN 109172577 A CN109172577 A CN 109172577A
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scirpusin
blood stasis
index
syndrome
drug
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CN109172577B (en
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梁生旺
冀苏龙
王淑美
许晓丽
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Guangdong Pharmaceutical University
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Guangdong Pharmaceutical 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Abstract

The invention discloses scirpusin ingredient C in a kind of trigone to synthesize the application in anti-syndrome of blood stasis drug.First demonstration that scirpusin C has significant anti-blood stasis drug action, can be used for preparing the drug for the treatment of syndrome of blood stasis, and demonstrated by pharmacological evaluation: scirpusin C can significantly reduce thromboxane B in blood stasis model mice serum2(Thromboxane B2, TXB2), fibrinogen (Fibrinogen, FIB), tissue fibers proenzyme inhibitor -1(Active Plasminogen Activator Inhibitor-1,) and body Endothelin (Endothelin 1 PAI-1, ET-1) horizontal, mouse thymus index (Thymus index, TI), index and spleen index (Spleen index, SI) and liver (Hepatic index can be improved, HI) index, clinical value with higher and development prospect in terms of the treatment of syndrome of blood stasis.

Description

The anti-syndrome of blood stasis application of scirpusin ingredient C in trigone
Technical field
The present invention relates to pharmaceutical technology field, the anti-syndrome of blood stasis for being specifically related to a kind of scirpusin ingredient (scirpusin C) is answered With.
Background technique
Trigone is the dry tuber of Sparganiaceae plant rhizoma scirpi Sparganium stoloni erum Buch.-Ham., It is recorded in all previous " Chinese Pharmacopoeias ", bitter, row is flat, enters liver, the spleen channel, has breaking blood and promoting the circulation of qi, the effect of clearing stagnation and killing pain.Three Rib can be applied alone health product, vinegar product, also can compatibility curcuma zedoary, Radix Astragali, heighten the effect of a treatment, clinic is mainly used for treating mullerianosis Disease, the gynecological diseases such as fibroid, and for treating the illnesss such as hepatopathy and cardiovascular and cerebrovascular disease.
The complex chemical composition of trigone contains flavonoids, volatile oil, Phenylpropanoid Glycosides class, organic acid, alkaloid, Anthraquinones, steroid The ingredients such as body class and polypeptide.Modern pharmacological research has illustrated the activity of part of compounds and its relationship between clinical application.But It is that part has whether the compound of external activity has drug action, needs further to study.This is for instructing clinical application Exploitation with new drug has great importance.
Summary of the invention
The technical problem to be solved by the present invention is to overcome not specific enough the defect of existing trigone effective component and deficiencies, for the first time Demonstrate the drug action that scirpusin A, scirpusin C have anti-blood stasis.The present invention proves scirpusin A, trigone by pharmacological evaluation Plain C can significantly reduce TXB in blood stasis model mice serum2, FIB, PAI-1, ET-1 is horizontal, while different degrees of can change Kind mouse thymus index, spleen index and the dirty index of liver have significant anti-blood stasis drug action, can be used for preparing treatment blood stasis The drug of card, clinical value with higher and development prospect.
The object of the present invention is to provide a kind of scirpusin ingredient scirpusin C to prepare the application in anti-syndrome of blood stasis drug.
Another object of the present invention is to provide a kind of anti-syndrome of blood stasis drug.
Above-mentioned purpose of the present invention is achieved through the following technical solutions:
First demonstration that scirpusin A, scirpusin C all have significant anti-blood stasis drug action, there is drop illness Body Endothelin (Endothelin 1, ET-1), -1 (Active of tissue fibers proenzyme inhibitor PlasminogenActivator Inhibitor-1, PAI-1), thromboxane B2(Thromboxane B2, TXB2), fiber egg White original (Fibrinogen, FIB) is horizontal, improves liver index (Hepatic index, HI), index and spleen index (Spleen Index, SI), the effect of thymus index (Thymus index, TI) provides strong foundation for the exploitation of anti-blood stasis natural drug.
Therefore, applying below should all be within protection scope of the present invention:
Scirpusin C is synthesizing the application in anti-syndrome of blood stasis drug.
Scirpusin C is in the drug that preparation can improve Patients with Blood Stasis Syndrome thymus index, spleen index and liver dirt index Application.
Scirpusin C can reduce the TXB in Patients with Blood Stasis Syndrome serum in preparation2, FIB, PAI-1, ET-1 level drug In application.
The scirpusin ingredient is scirpusin C, and structural formula is as follows:
In addition, the anti-syndrome of blood stasis drug containing scirpusin C also should be within protection scope of the present invention.
Preferably, the anti-syndrome of blood stasis drug further includes scirpusin A.
The anti-syndrome of blood stasis drug can also contain pharmaceutically acceptable carrier, be prepared into different dosage forms.
The invention has the following advantages:
First demonstration that scirpusin A, scirpusin C have significant anti-blood stasis drug action, it was proved that Scirpusin C has drop illness body Endothelin (Endothelin 1, ET-1), -1 (Active of tissue fibers proenzyme inhibitor Plasminogen Activator Inhibitor-1, PAI-1), thromboxane B2(Thromboxane B2, TB2), fiber egg White original (Fibrinogen, FIB) is horizontal, improves liver index (Hepatic index, HI), index and spleen index (Spleen Index, SI), the effect of thymus index (Thymus index, TI) provides a kind of new for the exploitation of anti-blood stasis natural drug Selection and strong foundation.
Detailed description of the invention
Fig. 1 is the scirpusin A of various dose to mouse body comprehensive drug Index Influence.
Fig. 2 is the scirpusin B of various dose to mouse body comprehensive drug Index Influence.
Fig. 3 is the scirpusin C of various dose to mouse body comprehensive drug Index Influence.
Specific embodiment
Further illustrate the present invention combined with specific embodiments below, but the present embodiment the present invention is not done it is any type of It limits.Unless stated otherwise, the present invention uses reagent, method and apparatus is the art conventional reagents, method and apparatus.
Unless stated otherwise, agents useful for same and material of the present invention are commercially available.
1 compound activating microcirculation and removing stasis medicinal functional experiment of embodiment
1, experimental material
(1) drug: experiment self-control scirpusin A, scirpusin B, scirpusin C, purity >=99%.
(2) animal: KM mouse, ♀, 25 ± 5g of weight are provided, credit number: SCK by Guangdong Province's Experimental Animal Center (Guangdong) 2013-0002.
(3) reagent
Adrenalin hydrochloride injection (Grandpharma (China) Co., Ltd., lot number: 20170214)；Visit aspirin intestines Molten (Bayer HealthCare Co, lot number: BJ32400)；Sodium carboxymethylcellulose (CMC-Na, the examination of Chinese medicines group chemistry Agent Co., Ltd, lot number: F20110915 is analyzed pure)；Sodium chloride (Tianjin Zhi Yuan chemical reagent Co., Ltd, lot number: 20160312, analyze pure)；Mouse thromboxane B2 (TXB2), Endothelin receptor A (ET-1), Plasminogen activator inhibitor 1 (PAI-1), fibrinogen (FIB) enzyme-linked immunologic detecting kit (Tianjin An Nuoruikang Bioisystech Co., Ltd)；Experiment It is pure water with water.
(4) laboratory apparatus
Test dedicated ultrapure water machine (Sichuan water that Water Management Equipment Ltd.) in WP-UP-WF-10 water Pu； ME204E a ten thousandth assay balance (Mettler-Toledo Instrument (Shanghai) Co., Ltd.)；Ten a ten thousandth assay balance of SQP (Sai Duolisi scientific instrument Co., Ltd)；YP502N type electronic balance (Shanghai Precision Scientific Apparatus Co., Ltd)；LBY-N6K Automatic blood rheometer (Pulisheng Instruments Co., Ltd., Beijing)；SIGMA2-16KL refrigerated centrifuge (SIGMA)；Thermo is micro- Biological temperature-constant incubator (4121)；DW-86L626 ultra-low temp；BIO-RAD iMark microplate reader；The ice making of IMS-20 snowflake Machine.
2, animal packet:
Mouse is grouped at random by weight, is respectively divided into blank group, model group, aspirin positive drug control group, scirpusin A Various dose group, dosage such as table 1.
The dosage of 1 various dose group of table
Note: A represents scirpusin A, and B represents scirpusin B, and it is dosage multiple in bracket that C, which represents scirpusin C,.
3, prepared by model:
Using subcutaneous injection mouse subcutaneous administration adrenalin hydrochloride injection 1mlkg-1, 0 DEG C of ice is put it into after 2h Water 3~5min of went swimming takes out, 1mlkg is subcutaneously injected again-1Adrenalin hydrochloride injection, after being spaced 2h, again by it It is placed in 0 DEG C of ice water 3~5min of went swimming, takes out, causes chmice acute blood stasis model.
4, sample preparation:
Blank group and model group intragastric administration on mice 0.5%CMC-Na solution, remaining each administration group intragastric administration on mice are given corresponding dense The drug of degree, dosage 0.1ml10g-1.Each group intragastric administration on mice 7 days, 1 times/day, after administration in the 6th day after 2h, to stasis syndrome Model is replicated.After 7th day administration 2h, blood is taken, is centrifuged 10min under 4 DEG C, 3000 × g, supernatant liquid is taken to manage in EP In, it lays in -80 DEG C of ultra low temperature freezers, it is to be measured.
5, sample detection
(1) sample detection:
Prepare liquid is melted again at room temperature, using enzyme linked immunosorbent assay, according to the detecting step in kit specification, strictly Operation, detects TXB respectively2, ET-1, PAI-1, FIB concentration；Mouse take blood put to death after, dissection, the liver of taking-up, spleen with And thymus gland physiological saline adsorption surface bloodstain is weighed with filter paper adsorption surface moisture with assay balance, and data are recorded, and is calculated Mice organs index (table 2)；Note: mice organs index=mice organs weight (mg)/mouse weight (g).
Integration processing is standardized to indices, sees formula 3-1；
VMarkization value=(VAdministration group-VModel group)/(VNormal group-VModel group) formula 3-1
The frequency and expert that weight coefficient occurs in nearly five yearly correlations document according to index provide opinion, obtain each index Weight coefficient.
149, document in terms of having consulted over nearly 5 years in relation to blood stasis, wherein 47 have detected ET-1,28 are had detected PAI-1,36 have detected TXB2, 38 have detected FIB.It is detected the frequency combination subject occurred in the literature according to each index The weight coefficient of expert opinion, i.e. ET-1 and FIB is 3, TXB2Weight coefficient with PAI-1 is 2, thymus index, index and spleen index Weight coefficient with liver index is 1.Total activating microcirculation and removing stasis medicinal effect value is the standardized value of each index multiplied by the product of weight coefficient Addition and value, i.e., effect value of always invigorating blood circulation, is specifically calculated according to formula 2.
Indices pass in and out markization according to formula 1 and formula 2 and integration is handled:
VMarkization value=(VAdministration group-VModel group)/(VNormal group-VModel group) formula 1
VTI、VHI、VSIRespectively liver index, thymus index, index and spleen index standardization effect value；
VPAI-1、VTXB2、VET-2、VFIBRespectively detect the standardization effect value of every Serum Indexes；
VtotalFor comprehensive effect value.
(2) evaluation of result:
The results show that aspirin positive drug and scirpusin A, scirpusin B, scirpusin C can significantly reduce by modeling Cause the raising of body ET-1, PAI-1, FIB, TXB2 level；HI, TI, SI of mouse can be improved simultaneously, it was demonstrated that scirpusin A, Scirpusin B, scirpusin C all have the effect of drop blood stasis.Compared with aspirin administration group, scirpusin A improves blood stasis model blood TXB2, FIB concentration effect in clear is significantly stronger；It is bright that scirpusin B improves TXB2, FIB concentration effect in blood stasis model serum It is aobvious relatively strong, TI value increasing action caused by modeling can be reduced better than ASP administration group；Scirpusin C is to improvement model Serum Indexes PAI-1 amount and the effect for increasing TI value are substantially better than ASP, to the ET-1 concentration for reducing model serum, improve the effect of SI, and two Person improves degree, and there are few differences.As a result see Table 2 for details respectively.
Table 2
Note: compared with model group*P < 0.05,**p<0.01；P < 0.05 compared with ASP group, p < 0.01.
The comprehensive effect value of each administration group enhances (table 3, Fig. 1) with the increase of dosage.
Table 3
Studies have shown that scirpusin A of the present invention, scirpusin B, scirpusin C all have significantly reduce ET-1, PAI-1, FIB, TXB2 is horizontal, and improves the effect of HI, TI, SI, demonstrates scirpusin A, scirpusin B, scirpusin C for the first time and all has anti-blood stasis Drug action provides strong foundation for the exploitation of anti-blood stasis natural drug.
The above embodiment is a preferred embodiment of the present invention, but embodiments of the present invention are not by above-described embodiment Limitation, other any changes, modifications, substitutions, combinations, simplifications made without departing from the spirit and principles of the present invention, It should be equivalent substitute mode, be included within the scope of the present invention.

Claims (6)

1. scirpusin C is preparing the application in anti-syndrome of blood stasis drug.
2. scirpusin C is in the drug that preparation can improve Patients with Blood Stasis Syndrome thymus index, spleen index and liver dirt index Using.
3. scirpusin C can reduce the TXB in Patients with Blood Stasis Syndrome serum in preparation2, FIB, PAI-1, ET-1 level drug in Using.
4. a kind of anti-syndrome of blood stasis drug, which is characterized in that contain scirpusin C.
5. anti-syndrome of blood stasis drug according to claim 4, which is characterized in that further include scirpusin A.
6. anti-syndrome of blood stasis drug according to claim 4 or 5, which is characterized in that also contain pharmaceutically acceptable carrier.
CN201810975463.8A 2018-08-24 2018-08-24 Application of burreed tuber component C in rhizoma sparganii in preparation of anti-blood stasis medicine Active CN109172577B (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113694066A (en) * 2021-08-13 2021-11-26 广东药科大学 Application of scirpusin C in preparation of medicine for treating cerebral ischemic stroke

Citations (2)

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CN103536899A (en) * 2013-10-17 2014-01-29 广东药学院 Application of active peptide compound in rhizoma sparganii
CN103550215A (en) * 2013-10-17 2014-02-05 广东药学院 Applications of peptides compound in rhizome sparganii

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Publication number Priority date Publication date Assignee Title
CN103536899A (en) * 2013-10-17 2014-01-29 广东药学院 Application of active peptide compound in rhizoma sparganii
CN103550215A (en) * 2013-10-17 2014-02-05 广东药学院 Applications of peptides compound in rhizome sparganii

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113694066A (en) * 2021-08-13 2021-11-26 广东药科大学 Application of scirpusin C in preparation of medicine for treating cerebral ischemic stroke
CN113694066B (en) * 2021-08-13 2023-02-17 广东药科大学 Application of scirpusin C in preparation of medicine for treating cerebral ischemic stroke

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