CN103800318B - Brazilin is used for the application preventing and treating in the medicine of lesions of liver and kidney in preparation - Google Patents

Brazilin is used for the application preventing and treating in the medicine of lesions of liver and kidney in preparation Download PDF

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CN103800318B
CN103800318B CN201410044716.1A CN201410044716A CN103800318B CN 103800318 B CN103800318 B CN 103800318B CN 201410044716 A CN201410044716 A CN 201410044716A CN 103800318 B CN103800318 B CN 103800318B
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brazilin
preventing
injury
kidney
treating
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CN103800318A (en
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贾艳艳
赵瑾怡
文爱东
刘美佑
孙渊
鹿成韬
王珊
李健康
朱晓鹤
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Fourth Military Medical University FMMU
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Fourth Military Medical University FMMU
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Abstract

The invention discloses brazilin and prepare the application in the medicine preventing and treating lesions of liver and kidney, brazilin is the Chinese medicine ingredients that can be used for preventing liver kidney injury, its significant drug effect makes it have the potential developing into lesions of liver and kidney preventing and treating medicine, it is also possible to become the research direction of lesions of liver and kidney preventing and treating new drug.

Description

Brazilin is used for the application preventing and treating in the medicine of lesions of liver and kidney in preparation
Technical field
The present invention relates to brazilin and prepare the application in the medicine preventing and treating lesions of liver and kidney.
Background technology
Liver and kidney are that body weight for humans wants internal organs, its relevant disease serious threat human health.With injury of kidney disease it is Example, developed country's kidney disease sickness rate is 6.5%-10%, and selected areas of China sickness rate is up to 8%-12%.From 2005, the uremic patient of China's row renal replacement therapies there are about 60,000 examples, and with The annual speed more than 11% increases, and becomes clinical common critical illness, wherein acute injury of kidney case fatality rate Up to 30%.Therefore, the relevant disease that active development is safe and effective, with low cost prevents and/or curative Thing is significant.
Lignum Sappan is the dry duramen of leguminous plant Lignum Sappan (Caesalpinia sappan L.).It is distributed widely in The Guangxi of China, Guangdong, Taiwan, Guizhou, the ground such as Yunnan and Sichuan.There is " removing blood stasis evacuation of pus pain relieving " Effect, brazilin (Brasilin) is its main component, and structure is as follows:
Modern pharmacology research shows, brasilein all has preferably protection to apoplexy and myocardial ischemia And therapeutical effect, brasilein can protect cranial nerve, increase cerebral blood flow to suppress Na-K ATP simultaneously Enzymatic activity, reaches cerebral protection.At present, the curative effect of kidney and hepar damnification be there is no by brazilin Report.
There is no the medicine of clear and definite preventing and treating lesions of liver and kidney at present.As a example by injury of kidney, its therapeutic scheme includes: 1) Drug therapy of cylinder electrolyte balance is maintained;2) dialysis treatment;3) renal replacement therapy, due to Without clear and definite kidney injury treatment medicine, the implantation rate after injury of kidney is high.Simultaneously as without clear and definite pre- Anti-injury of kidney medicine, it is impossible to control the sickness rate of injury of kidney, increased the weight of injury of kidney further to human health Harm.
Summary of the invention
It is an object of the invention to provide brazilin preparing in the medicine preventing and treating lesions of liver and kidney Application.
For reaching above-mentioned purpose, present invention employs techniques below scheme:
Brazilin is used for the application preventing and treating in the medicine of hepatic injury or injury of kidney in preparation.
Preventing and treating to injury of kidney is presented as the improvement of serum creatinine.
Preventing and treating to injury of kidney is presented as the improvement of blood urea nitrogen.
Preventing and treating to hepatic injury is presented as the improvement of alanine aminotransferase.
Preventing and treating to hepatic injury is presented as the improvement of aspartate aminotransferase.
The dosage form of described medicine include powder, pill, capsule, tablet, microcapsule, soft microcapsule, The multiple interior external preparation such as membrane, suppository, injection, unguentum, tincture, powder, electuary or aerosol.
Beneficial effects of the present invention is embodied in:
1) brazilin of the present invention belongs to Chinese medicine ingredients, and toxic and side effects is low;
2) present invention can be effectively improved hepar damnification, maintains and repairs liver function;
3) present invention can be effectively improved kidney injury, maintains and repairs renal function;
4) brazilin of the present invention has the potential quality being developed into Liver and kidney protection medicine, or as base Plinth/prodrug, protects medicine for development of new Liver and kidney, for Liver and kidney protection medicine provide new thinking with Research structure.
Accompanying drawing explanation
Fig. 1 is the change of liver organization pathological section, A: sham operated rats pathological section after rat different disposal Figure;B: model group pathological section figure;C: brazilin administration group pathological section figure;
Fig. 2 be Scr (serum creatinine) after rat different disposal change (N=6), * represents with false Operation group compares P 0.05, and # represents P 0.05 compared with model group;
Fig. 3 be BUN (blood urea nitrogen) after rat different disposal change (N=6), * represent with Sham operated rats compares P 0.05, and # represents P 0.05 compared with model group;
Fig. 4 is the change of kidney tissue pathological slice, sham: sham operated rats pathology after rat different disposal Slice map;I/R: model group pathological section figure;I/R+Bra: brazilin administration group pathological section figure;
Fig. 5 be TNF-α (tumor necrosis factor-alpha) after rat different disposal change (N=6), * representing P 0.05 compared with sham operated rats, # represents P 0.05 compared with model group;
Fig. 6 be caspase 3 (glutathion desmoenzyme-3) after rat different disposal change ( N=6), * represents P 0.05 compared with sham operated rats, and # represents P 0.05 compared with model group.
Detailed description of the invention
With embodiment, the present invention is elaborated below in conjunction with the accompanying drawings.
In embodiment, brazilin is purchased from Shanghai Kemin Biological Technology Co., Ltd.。
Embodiment 1: the protective effect that rats'liver ischemia/reperfusion (LI/R) is damaged by brazilin
SD rat 30, body weight 220-280g, purchased from The Fourth Military Medical University's animal experimental center.Rat Sub-cage rearing (ambient temperature is 24 DEG C, and humidity is 60-70%).30 rats are randomly divided into following groups (n=6): sham operated rats, model group and brazilin administration group are (containing high, medium and low 3 dosage Group), preoperative 6d fasting, freely drink water.Each group rat is through 10% chloral hydrate intraperitoneal injection of anesthesia, so Rear brazilin administration group carries out rat tail vein injection brazilin aqueous solution (clarification, through filtering), Brazilin is administered by high, normal, basic 3 dosage levels (120,60,30mg/kg) respectively, sham-operation Group and model group injecting normal saline.
30min after administration, each group rat eye socket blood sampling 1.0mL;Then by prostrate for rat fixing, sham-operation Group is sewed up after opening abdomen;Brazilin administration group and model group open abdomen, ligature Hepatic artery, portal vein in the lump And bile duct, unclamp after ligation 30min, then carry out two-layered suture.Postoperative 4h, 10h respectively organize rat and enter Row eye socket blood sampling (about 1.0mL);Postoperative 24h respectively organizes rat and takes liver organization, and gathers blood sample 1.5mL, Hematometry alanine aminotransferase (ALT) and aspartic acid transamination is taken during Reperfu-sion 4,10,24h Enzyme (AST).
The results are shown in Table 1 and Fig. 1, in brazilin administration group, high, normal, basic 3 dosage waters averagely show Hepatocyte protection significantly, and there is concentration dependent;Pathological section shows simultaneously: brazilin is given Tissue necrosis area after medicine (30mg/Kg) is significantly less than model group, and inflammation damnification is the lowest simultaneously In model group.
Table 1 respectively organize rat blood serum ALT and AST change (N=6)
Note: sham: sham operated rats;LI/R: model group;High dose, middle dosage, low dosage: brazilin dosage is respectively For 120mg/kg, 60mg/kg, 30mg/kg.* represent that there is compared with sham significant difference, P 0.05;# represents and LI/R Compare and there is significant difference, P 0.05.
Embodiment 2: the protective effect that kidney of rats ischemia/reperfusion (RI/R) is damaged by brazilin
SD rat 30, body weight 220-280g, purchased from The Fourth Military Medical University's animal experimental center.Rat Sub-cage rearing (ambient temperature is 24 DEG C, and humidity is 60-70%), 30 rats are randomly divided into following groups (n=6): sham operated rats, model group and brazilin administration group are (containing high, medium and low 3 dosage Group), preoperative 6d fasting, freely drink water.Each group rat is through 10% chloral hydrate intraperitoneal injection of anesthesia, the back of the body Sleeping fixing, then to carry out rat tail vein injection brazilin aqueous solution (clear for brazilin administration group Clearly, through filtering), brazilin is respectively by high, normal, basic 3 dosage levels (120,60,30mg/kg) It is administered, sham operated rats and model group injecting normal saline.
30min after administration, each group rat eye socket blood sampling 1.0mL, then carry out Resection of right kidney art: rat carries on the back Otch at the right kidney in portion, finds out right kidney separation rear cutout and removes;Two-layered suture is carried out after excision;Brazilin is given Medicine group and model group carry out separating the left renal aorta of ligation and perform the operation: otch at the left kidney in back, find out left kidney, Separate left renal aorta, unclamp after ligaturing left renal aorta 30min, then carry out two-layered suture.Postoperative 4h, 10h respectively organize rat and carry out eye socket blood sampling (about 1.0mL);Postoperative 24h respectively organizes rat and wins left kidney, And gather blood sample 1.5mL.Left kidney is equally divided into two halves and preserves, and half makees tissue slice, and half censorship is done Pathological section.
Result is shown in Fig. 2-Fig. 4, and in brazilin administration group, high, normal, basic 3 dosage waters averagely show aobvious Write ground renal protection, there is concentration dependent.Under high dose level, the BUN of Reperfu-sion 24h is obvious Declining, Scr is on close level sham operated rats.Pathological section shows simultaneously: brazilin is administered (30mg/Kg) After tissue necrosis area significantly less than model group, inflammation damnification is also significantly lower than model group simultaneously.By scheming 5 and Fig. 6 understand, and brazilin is administered (30mg/Kg) can significantly reduce TNF-α and caspase 3, thus speculate, brazilin preventing and treating ischemia/reperfusion injury of kidney may by reduce inflammatory damage, Reduce apoptosis to realize.
Brazilin is the Chinese medicine ingredients that can be used for preventing liver kidney injury, and its significant drug effect makes it have There is the potential developing into lesions of liver and kidney preventing and treating medicine, it is also possible to become the research direction of lesions of liver and kidney preventing and treating new drug.

Claims (6)

1. brazilin is used for preventing and treating During Hepatic Ischemiareperfusion Injury or renal ischemia-reperfusion injury in preparation Medicine in application.
The most according to claim 1 brazilin preparation be used for preventing and treating During Hepatic Ischemiareperfusion Injury or Application in the medicine of renal ischemia-reperfusion injury, it is characterised in that: the preventing and treating to injury of kidney is presented as blood The improvement of creatinine.
The most according to claim 1 brazilin preparation be used for preventing and treating During Hepatic Ischemiareperfusion Injury or Application in the medicine of renal ischemia-reperfusion injury, it is characterised in that: the preventing and treating to injury of kidney is presented as urine The improvement of element nitrogen.
The most according to claim 1 brazilin preparation be used for preventing and treating During Hepatic Ischemiareperfusion Injury or Application in the medicine of renal ischemia-reperfusion injury, it is characterised in that: the preventing and treating to hepatic injury is presented as third The improvement of histidine amino group transferring enzyme.
The most according to claim 1 brazilin preparation be used for preventing and treating During Hepatic Ischemiareperfusion Injury or Application in the medicine of renal ischemia-reperfusion injury, it is characterised in that: the preventing and treating to hepatic injury is presented as sky The improvement of winter histidine amino group transferring enzyme.
The most according to claim 1 brazilin preparation be used for preventing and treating During Hepatic Ischemiareperfusion Injury or Application in the medicine of renal ischemia-reperfusion injury, it is characterised in that: the dosage form of described medicine selected from pill, Capsule, tablet, microcapsule, membrane, suppository, injection, unguentum, tincture, powder, electuary or Aerosol.
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CN112353834A (en) * 2020-12-03 2021-02-12 中国人民解放军空军军医大学 Application of two-component Shensu drink in preparation of medicine for preventing and treating chronic kidney injury

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Brazilin protects cultured rat hepatocytes from bromochloroform-induced toxicity;Moon C.K. 等;《Drug Chem Toxical》;19921231;第15卷(第1期);第81-91页 *
苏木水煎液对糖尿病佘冰大鼠血糖、肾功能和肾脏病理影响;张红等;《时珍国医国药》;20111231;第22卷(第5期);第1255-1256页 *
高效液相色谱法同时测定苏木中的巴西苏木素和原苏木素B;陈雪敏等;《分析试验室》;20120430;第31卷(第4期);第98-101页 *

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