Effects and mechanism of astilbin on myocardial ischemia-reperfusion injury in rats / 中国药房

OBJECTIVE To investigate the effects of astilbin （AST） on myocardial ischemia-reperfusion injury （MIRI） in rats and its potential mechanism. METHODS SD male rats were randomly divided into sham operation group， model group， positive control group （Compound Salvia miltiorrhiza tablets， 240 mg/kg）， AST low-dose and high-dose groups （30， 90 mg/kg）， and high- dose of AST+hypoxia-inducible factor-1α（HIF-1α） inhibitor group （AST 90 mg/kg+2ME2 15 mg/kg）， with 25 rats in each group. Except for sham operation group， MIRI model was induced in other groups， and then given relevant drug or normal saline intragastrically or intraperitoneally， for consecutive 28 d. Serum contents of cardiac troponin I （cTnI） and creatine kinase isoenzyme （CK-MB） were detected； volume ratio of myocardial infarction was measured； the pathological changes of myocardium， the apoptotic rate of myocardial cells and ultrastructure of mitochondria in myocardial tissue were all observed. The contents of tumor necrosis factor α （TNF-α）， interleukin 6 （IL-6） and malondialdehyde （MDA）， the activity of superoxide dismutase （SOD）， the expressions of HIF-1α， adenovirus E1B interacting protein 3 （BNIP3） and myosin-like Bcl-2 interacting protein （Beclin1） were determined in myocardium. The ratio of microtubule-associated protein light chain 3 （LC3） Ⅱ to Ⅰ （LC3 Ⅱ/Ⅰ） in rat myocardium was calculated. RESULTS Compared with model group， no obvious swelling was found in the myocardial tissue of rats in positive control group， AST low-dose and high-dose groups， and the myocardial fibers were arranged regularly； the volume ratio of myocardial infarction， the contents of cTnI， CK-MB， TNF-α， IL-6 and MDA， the apoptotic rate were decreased significantly （P＜0.05）， while SOD activity， protein expressions of HIF-1α， BNIP3 and Beclin1， LC3Ⅱ/Ⅰ were increased significantly （P＜0.05）. HIF-1α inhibitor could significantly weaken the improvement effect of AST on the above indicators in MIRI model rats （P＜0.05）. CONCLUSIONS AST enhances mitochondrial autophagy by activating HIF-1α/BNIP3 signaling pathway， thereby reducing MIRI in rats.

Microwave-assisted extraction and content determination of astilbin in Lysiphyllum strychnifolium stems

Abstract Lysiphyllum strychnifolium (Craib) A. Schmitz. (in Thai name, Ya nang daeng) has been traditionally used to treat fever, alcohol intoxication, cancer, allergies, and blood toxins. It can be used as a health-promoting herbal tea and contains hydroalcoholic extracts. The purpose of the present study was to develop a microwave-assisted extraction method for astilbin in L. strychnifolium stems. HPLC was used to determine astilbin content. Three extraction conditions were optimized: types of solvent, microwave power levels, and the number of extraction cycles. Water:methanol (40:60) was the best solvent for astilbin extraction from L. strychnifolium stems using 450 watts and six microwave-assisted extraction cycles. This technique offers important advantages over conventional methods, such as shorter extraction times, substantial energy savings, and a reduced environmental burden.

Ethyl acetate extract of Smilax glabra Roxb roots and its major active compound astilbin promote osteoblastogenesis in vitro by upregulating bone cell differentiation- associated genes

Objective: To investigate the osteoblastogenic activity of the ethyl acetate (EtOAc) extract of Smilax glabra Roxb roots and its major active compound astilbin. Methods: Astilbin was isolated from EtOAc extract using silica gel chromatography combined with fraction crystallization. Chemical structure of astilbin was determined by analysis of the spectroscopic data in comparison with the literature. MTT method was used to detect the toxicity. Alkaline phosphatase (ALP) activity was determined by the spectrophotometric method at 405 nm using p-nitrophenyl phosphate as a substrate. Calcium deposition was stained with alizarin red-S, distained with cetylpyridium chloride, and quantified at 562 nm. In silico model for astilbin-ALP interaction was analyzed using AutoDock 4.2.6. The changes in expression of osteoblast differentiation related genes were determined using quantitative real-time PCR. Results: Both the EtOAc extract and astilbin had no toxicity toward osteoblast MC3T3-E1 cells at 5.0, 10, 25, and 50 μg/mL. At 25 μg/ mL, they enhanced ALP activity and mineralization of osteoblasts up to 30% and 55% for the EtOAc extract and 22% and 41% for astilbin, respectively. Molecular docking analysis of astilbin-ALP interaction revealed Arg167, Asp320, His324, and His437 were key residues participating in hydrophobic interaction; meanwhile, His434 and Thr436 residues were involved in hydrogen bond formation in the active site of human tissue-nonspecific ALP. Moreover, the expression level of genes opn, col1, osx, and runx2 were up-regulated in astilbin treated samples with the fold changes as 2.2; 3.7; 4.1; 2.3, respectively at 10 μg/mL (P<0.05). Conclusions: The EtOAc extract and its major compound astilbin exhibit osteoblastogenic activity by up-regulating important markers for bone cell differentiation. It could be a new and promising osteogenic agent with dual actions for therapeutic applications.

Optimization of processing technology of Sarcandra glabra based on multi-index evaluation method / 中草药

Objective: Analytic hierarchy process (AHP) was used to establish a comprehensive evaluation method of multiple indexes of traditional Chinese medicine, and the best processing technology of Sarcandra glabra was optimized. Methods: On the basis of single factor experiment, the comprehensive score of neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, caffeic acid, isofraxidin, astilbin and rosmarinic acid content was used as evaluation index by AHP, and drying temperature and drying time were used as influencing factors. The purification process of S. glabra leaves was determined by single factor investigation. Taking soaking time, soaking time, cutting length and drying temperature as influencing factors, the optimal cutting process of S. glabra stems was optimized by central composite design-response surface method. Multi-index analytic hierarchy process (AHP) was used to analyze and verify the optimal process. Results: The best processing technology of S. glabra stems was as follows: stem Rob water washed once, soaked in 12 times of water for 1 h, moistened and softened for 3 h, cut into 15 mm segments after taking out, and baked at 50 ℃ for 2 h; The processing method of leaves was as follows: leaf Rob water washed once and dried at 50 ℃ for 4 h; Then mixed the processed stems and leaves of S. glabra at 2:1. The deviation between the verification value and the prediction value of the comprehensive score of the optimal S. glabra stem by softening and cutting method was 4.70%. Conclusion: The processing technology is simple, stable and feasible. The obtained parameters can provide scientific basis for the research and production of S. glabra, and AHP can provide reference for the multi-index evaluation of traditional Chinese medicine.

Effects of Crystal Form on in vivo and in vitro Behavior of Astilbin Nanosuspensions / 中国药房

OBJECTIVE： To investigate the effects of crystal form on in vivo and in vitro behavior of Astilbin nanosuspensions （AT-NS）. METHODS： AT-NS1 and AT-NS2 were prepared by precipitation method and miniaturized media milling method respectively. The particle size and polydispersity index （PDI） were determined by laser particle size analyzer. X-ray diffraction （XRD）， scanning electron microscopy （SEM）， HPLC and paddle method were used to analyze and compare the structure characteristics， appearance morphology and in vitro dissolution of AT raw material， AT-NS1 and AT-NS2. Totally 15 healthy male SD rats were randomly divided into AT raw material， AT-NS1 and AT-NS2 group， with 5 rats in each group. They were given relevant medicine suspension 120 mg/kg （using water as solvent） intragastrically； blood samples  were collected from orbit before medication （0 min） and 5， 10， 20， 30， 60， 120， 240， 480 min after medication. Using rutin as internal standard， HPLC method was used to determine plasma concentration of AT in rats. Pharmacokinetic parameters were calculated by using DAS 2.0 software and then compared. RESULTS： The particle sizes of AT-NS1 and AT-NS2 were （212.48±0.32） nm and （226.36±2.29） nm， respectively； PDI were 0.129 3±0.026 3 and 0.254 7±0.012 4. XRD analysis showed AT-NS1 was amorphous， and AT-NS2 was crystalline. Diffraction peaks of both were different from those of AT raw material. SEM analysis showed that AT-NS1 and AT-NS2 were similar in morphology， and they were spherical and uniform in size； AT raw material was lump with large particle size and different sizes. Results of dissolution tests showed that accumulative dissolution of AT raw material， AT-NS1 and AT-NS2 were 4.54％， 35.01％， 12.22％ at 1 h； accumulative dissolution of them were 24.01％， 81.14％， 64.69％ at 12 h； accumulative dissolution of them were 36.04％， 84.47％， 85.86％ at 24 h， respectively. Results of pharmacokinetic study showed， compared with AT raw material group， cmax and AUC0-∞ of AT-NS1 and AT-NS2 groups as well as t1/2z of AT-NS1 group were increased significantly， while tmax of AT-NS1 group was significantly reduced significantly （P＜0.05）. Compared with AT-NS2 goup， cmax， AUC0-∞ and t1/2z of AT-NS1 group were increased significantly， while tmax was reduced significantly （P＜0.05）. CONCLUSIONS： When AT is prepared into NS， dissolution in vitro and oral absorption in vivo of AT are increased significantly. In a short time， the dissolution/absorption of amorphous NS is faster than crystalline NS.

Astilbin reduces ROS accumulation and VEGF expression through Nrf2 in psoriasis-like skin disease

Background: Psoriasis is a common and intractable skin disease affecting the physical and mental health of patients. The accumulation of ROS is involved in the pathogenesis of psoriasis and antioxidants are believed to be therapeutic. This study aimed to investigate the therapeutic efficacy of astilbin on ROS accumulation in psoriasis. Results: The study showed that 50 μg/ml astilbin could inhibit the growth and reduce the accumulation of ROS in HaCaT cells stimulated by IL-17 and TNF-α. Astilbin could elevate the Nrf2 accumulation in the nuclei, eventually leading to the transcriptional activation of various antioxidant proteins and reducing the expression of VEGF. Conclusions: Our results collectively suggest that astilbin could induce Nrf2 nucleus translocation, which is contribute to reduce the ROS accumulation and VEGF expression, and inhibit the proliferation of HaCaT cells.

Preparation of astilbin amorphous nanosuspension and its evaluation / 中国中药杂志

Astilbil nanosuspension (AT-NS) was prepared by an antisolvent precipitation method. The formula and process of AT-NS were optimized by the single factor experiment. AT-NS was prepared under the optimal conditions, and its morphology and crystallinity were characterized. In vitro release of AT-NS was also determined. The particle size of AT-NS stabilized by PVP K30 was (149±3) nm, and the polydispersity index (PDI) and stability index (SI) were 0.137±0.014 and 0.940±0.012, respectively. The results of SEM showed that AT-NS was spherical. Both XRD and DSC showed that AT was amorphous in nanosuspension. In the release test, AT-NS showed a significantly increased dissolution. This simple low-cost approach could prepare AT-NS successfully. AT-NS could significantly improve the dissolution of AT and provide the reference to break the limitation on the clinical application of AT.

Content changes regularity of flavonoids in Smilax glabra by QAMS method / 中草药

Objective: To establish a method of quantitative analysis of multi-components by single-marker (QAMS) for simultaneously determination of neoastilbin, astilbin, neoisoastilbin, isoastilbin, and engeletin in Smilax glabra, and research the tendency of content changes in different growth years by QAMS. Methods: An HPLC method was established to determine the relative correction factors of four other flavonoids by using astilbin as the internal reference standard. Then the method was used to determine the various content of five flavonoids in different growth years and validate the feasibility and accuracy by comparing the content results determined by the external standard method with QAMS. The dynamic change regularity of flavonoids in S. glabra was investigated. Results: A total of 23 samples from five batches in different growth years were simultaneously determined by external standard method and QAMS, the results deviation were all less than 1.0%. The content of five flavonoids in different growth years was different, astilbin decreased with the increase of growth years, neoastilbin, neoisoastilbin and isoastilbin had the reverse trend. Conclusion: The established QAMS method is feasible and accurate for the simultaneous determination of five flavonoids in S. glabra. Growth years have a certain impact on the content of each component.

Effect of astilbin on cerebral monoamine mediators dopamine and 5-hydroxytryptamine in depression mice / 新乡医学院学报

Objective To evaluate the anti-depression effect of astilbin on mice with depressive disorder and to explore its mechanism of action.Methods Seventy-two male mice (C57BL/6J type) were randomly divided into control group,model group,low,middle,high dose of astilbin group and imipramine(IMI) group,with 12 mice in each group.The mice in the control group were adopted in a normal way.The rats in the model group,low,middle,high dose of astilbin group and IMI group were adopted in chronic unexpected mild stress (CUMS) to establish depression model,and the stress was continuously kept for three weeks and daily medicine with physiological saline,10,20,40 mg · kg-1 astilbin and 10 astilbin imipramine were provided in the way of intraperitoneal injection.Examination for behavioural changes of animals was implemented via tail suspension test,forced swimming test,sucrose preference test,open field test.High performance liquid chromatography (HPLC) was adopted to examine the level of dopamine (DA) and 5-hydroxytryptamine(5-HT)in prefrontal cortex.Results There was no significant difference in the number of horizontal movement and vertical movement among the control group,model group,IMI group and low,middle,high dose of astilbin group(P ＞ 0.05).Compared with the control group,the dead time of tail suspension test and forced swimming test in the model group was longer (P ＜ 0.05),and sugar preference,DA and 5-HT in prefrontal cortex decreased dramatically (P ＜ 0.05).Compared with the model group,the dead time of tail suspension test and forced swimming test in the low,middle,high dose of astilbin group was shorter (P ＜ 0.05),and sugar preference and DA level in prefrontal cortex increased dramatically (P ＜ 0.05).The 5-HT level in prefrontal cortex in the middle,high dose of astilbin group and IMI group was higher than that in the model group (P ＜ 0.05),but there was no significant difference in the 5-HT level in prefrontal cortex between low dose of astilbin group and model group (P ＞ 0.05).There was no significant difference in the dead time of tail suspension test and forced swimming test and sugar preference among the control group,IMI group and low,middle,high dose of astilbin group (P ＞ 0.05).Conclusion Astilbin works excellently in anti-depression,and the major mechanism may involve in up-regulating the level of DA and 5-HT in prefrontal cortex.

Determination of astilbin and engelitin in Baqia-Sanyu granules / 国际中医中药杂志

Objective To establish HPLC-DAD method for determination of 2 components in Baqia-sanyu granules.Methods The HPLC system consisted of the Fortis Cortecstm C18 column (4.6 mm× 250 mm, 5 μm), the mobile phase consisted of 0.05%KH2PO4and acetonitrile, gradient elution flow rate was 1.0 ml/min, the column temperature was 30 ℃, and the UV detector was set at 290 nm. Results The linear response range of astilbin and engelitin were 0.002 2-0.044 μg and 0.012 4-0.248 μg(r=0.999 9). The average recovery were 97.0% and 97.8%. RSD were 1.61% and 1.65%. Conclusions The method high sensitive, accurate, repeatable and high specifid. It could be an important method to control the standard of this preparations.

Optimization of Extraction and Purification Technology of Total Flavonoids from Engelhardia roxburghi-ana and Content Determination of 3 Kinds of Effective Components / 中国药房

OBJECTIVE:To optimize the extraction and purification technology of total flavonoids from Engelhardia roxburghi-ana,and to establish the method for the content determination of 3 kinds of effective components. METHODS:Using the extrac-tion transfer rate of astilbin as index,single factor test was used to investigate extraction solvent,extraction method,volume frac-tion of percolation solvent ethanol,percolation material-liquid ration,soaking time before percolation and percolation rate of extrac-tion technology,and volume fraction of eluant ethanol in AB-8 resin purification technology. The contents of 3 effective compo-nents as astilbin,texifolin and engelitin in total flavonoids from E. roxburghiana were determined by HPLC. RESULTS:The opti-mal extraction technology was using 70% ethanol as extraction and percolation solvent,percolation extraction,soaking for 8 h be-fore percolation,percolation material-liquid ratio of 1∶16(g/ml),percolation rate of 30 ml/(min·kg). The purification technology was diluting the solution to 0.5 g (crude drug)/ml with water,ethyl acetate extraction,dissolved extract with 50% ethanol after evaporated to dryness,AB-8 resin for sampling,eluted with 50% ethanol,concentrating and drying. In verification test,extraction transfer rate of astilbin was more than 80%(RSD=0.42%,n=3). The contents of astilbin,taxifolin and engeletin in total flavo-noids from E. roxburghiana by purified were 57.94%,3.72% and 2.83%,respectively;the contents of 3 components accounted for 64.00% of total flavonoids. CONCLUSIONS:The extraction and purification technology is stable,rational and reliable;the content determination method of 3 effective components in total flavonoids of E. roxburghiana is accurate,simple and producible.

Mechanism research of alleviating rat liver ischemia-reperfusion injury by Astilbin / 国际外科学杂志

Objective To explore the protective effect of astilbin in hepatic ischemia-reperfusion injury (HIRI).Methods SD rats were divided into Sham group (control group),HIRI group (ischemia-reperfusion group),astilbe (low dose group,middle dose group,high dose group),and estabilished the model of rat HIRI.After liver were reperfused with blood (in 4 h,8 h,16 h),collecting the specimens of blood and liver tissues.Detection of serum alanine aminotransferase (ALT),aspertate aminotransferase (AST);Then observed the changes of liver cell microstructure;Western blot analysised the expression of HMGB1,TLR4,NF-kB,TNF-α in liver tissue.Results The serum ALT levels of Sham group in 4 h,8 h,16 h were (58.11 ±4.81) U/L,(57.12 ± 5.33) U/L,(57.63 ±4.54) U/L,the serum ALT levels of HIRI group in 4 h,8 h,16 h were (540.38 ± 21.41) U/L,(831.21 ± 20.11) U/L,(191.95 ± 15.35) U/L.Compared with Sham group,the serum ALT levels of HIRI group were significantly increased(P ＜ 0.01).Compared with HIRI group,The serum ALT levels of three dose groups in 4 h,8 h,16 h were significantly declined,including high dose group lower the most obvious (The serum ALT levels of high dose group in 4 h,8 h,16 h were (223.75 ± 10.53) U/L,(412.14 ±23.59) U/L,(205.25 ± 15.48) U/L (P ＜0.01).The results of light microscope indicated that drug groups significantly reduce the liver cell damage.The results of Western blot displayed that High dose group of HMGB1,TLR4 protein expression in 4 h,8 h,16 h drop significantly than HIRI group(P ＜0.05).High dose group of NFkB,TNF-α protein expression in postoperative 8 h,16 h decrease significantly than HIRI group (P ＜ 0.05),but in postoperative 8 h,there was no statistically significant difference compared with group HIRI (P＞0.05).Conclusion Astilbe pretreatment can reduce HIRI and its mechanism may be associated with downregulating the axis of HMGB1/TLR4/NF-kB/TNF-α,proceed to the next inhibiting the inflammatory response.

Optimization of the Extraction Technology of Astilbin in Puling Penyankang Capsules by Orthogonal Test / 中国药房

OBJECTIVE:To optimize the extraction technology of astilbin from medicinal herbs in Puling penyankang cap-sules. METHODS:The extraction technology of astilbin from ingredients(Smilacis glabrae rhizoma,chuanxiong rhizoma,Eucom-miae cortex,notoginseng radix et rhizoma,Plantaginis semen)of Puling penyankang capsules was optimized with concentration of ethanol,immersion time and percolation speed as factors,and using the yield of extractum and the extraction amount of astilbin as index. RESULTS:The optimized extraction technology was as follows as 2-fold 70% ethanol,immersed for 24 h,percolated with 70% ethanol with percolation speed of 3 ml/min,10-fold percolate volume was colleted. In verification test,the yield of extractum were 6.79%,6.92% and 6.84%,respectively,with average value of (6.85 ± 0.96)%(n=3);the extraction amounts of astilbin were 39.23,39.67 and 39.69 mg,with average value of (39.53 ± 0.66) mg (n=3). CONCLUSIONS:The optimized extraction technology of astilbin in Puling penyankang capsules is stable and practical.

Chemical constituents of Ardisia faberi / 中草药

Objective: To investigate the chemical constituents of Adisia faberi. Methods: Compounds were isolated and purified by the normal phase silica gel, Sephadex LH-20, MCI gel, and ODS-A-HG packing material. Their structures were identified by the methods of MS, 1H-NMR, and 13C-NMR combined with physicochemical property. Results: Eleven compounds were isolated and their structures were elucidateasbauerenol (1), oleic acid (2), (Z)-10-heneicosenoic acid (3), grasshopper ketone (4), bergenin (5), mallonanoside A (6), ethyl gallate (7), astilbin (8), quercitrin (9), ardisiacrispin B (10), and ardicrenin (11). Conclusion: Compounds 2, 7, 9-11 are isolated from this plant for the first time; Compounds 3, 4, 6, and 8 are isolated from plants in genus Ardisia Swartz for the first time.

Astilbin Inhibits Proliferation of Rat Aortic Smooth Muscle Cells Induced by Angiotensin Ⅱ and Down-regulates Expression of Protooncogene / 华中科技大学学报（医学）（英德文版）

This study examined the effect of astilbin on the proliferation of rat aortic smooth muscle cells (RASMCs) induced by angiotensin Ⅱ (Ang Ⅱ) and explored the possible mechanisms.Cell proliferation model of RASMCs was induced by treatmente with Ang Ⅱ.Cells were randomly divided to 8 groups.Normally cultured VSMCs serves as blank control group; in Ang Ⅱ model group,cells were treated with AngⅡ at 10-7 mol/L; in three astilbin groups,cells were treated with 10,15,30 mg/L of astilbin; in three Ang Ⅱ +astilbin groups,cells were treated with Ang Ⅱ (at 1 0-7 mol/L) and astilbin at 10,15,30 mg/L.Cell proliferation ability was detected by MTT method and the cell cycles and proliferation index were flow cytometrically determined.The expression of c-myc mRNA was assessed by using reverse transcription polymerase chain reaction (RT-PCR),and the expression of NF-κB in RASMCs was immunocytochemically observed.Our results showed that MTT metabolism in RASMCs in the basic and Angll stimulated situation was inhibited by astilbin,and the cells numbers of G0/G1 phase were increased and that of G2/S phase were decreased markedly.Not only highly expression of c-myc gene stimulated by Ang Ⅱ could be inhibited by Astilbin significantly,but also the expression of NF-κB protein can be down regulated by Astilbin.We are led to conclude that astilbin astilbin can inhibit the Ang Ⅱ -mediated proliferation of RASMCs by blocking the transition of RASMCs from Go/G1 phase to S phase and by down-regulating the expression of NF-κB,c-mvc gene.

Protective effect of astilbin on ischemia reperfusion-induced liver injury through increasing IL-10 expression / 第二军医大学学报

Objective: To investigate the protective effect of astilbin on warm ischemia/reperfusion-induced liver injury and to study the related mechanism. Methods: C57BL/6 mice were randomly divided into four groups (n=8): sham-operated group (Sham), model control group (I/R), low dose astilbin treatment group (10 mg/kg) and high dose astilbin (40 mg/kg) treatment group. Mice in the two treatment groups were intraperitoneally injected with astilbin 24 hours and one hour before ischemia. Then 70% hepatic ischemia/reperfusion model (the left and middle hepatic lobe) was established. Mice in the I/R model control group and the sham operation group were administered with the same volume of normal saline. The blood sample and liver tissue samples were collected 90 min after ischemia and 6 h after reperfusion. Serum ALT activity was detected as an indicator of liver function damage and the content of MPO in liver tissues were detected by ELISA. The pathological changes of the liver were observed. The expression of IL-10 in liver tissues was detected by Western blotting and the expression of IL- 10 mRNA was detected by semi-quantitative RT-PCR. Results: Astilbin treatment can effectively lower the serum ALT level and MPO level in the liver tissues in some I/R mice. It could also improve the pathological manifestations of the liver. Compared with the I/R model control group, IL-10 protein levels gradually increased in the two treatment groups, which was consistent with the result of RT-PCR (low dose group P<0.05; high dose group, P<0.01). Conclusion: Astilbin can effectively reduce the inflammatory response after liver warm ischemia-reperfusion induced injury, effectively improve the mouse liver function and pathological damage, which might be related to the upregulation of IL-10 expression in the liver tissues.

Inhibition of peroxidase activity and scavenging of reactive oxygen species by astilbin isolated from Dimorphandra mollis (Fabaceae, Caesalpinioideae)

Astilbin (5,7,3’,4’-tetrahydroxy-2,3-dihydroflavonol-3-ß-o-rhamnoside), a flavonoid with a large range of biological activities, was isolated from Dimorphandra mollis, a shrub common to the Brazilian Cerrado. The purpose of this study is to verify the effects of astilbin on myeloperoxidase (MPO) and horseradish peroxidase (HRP), and its antioxidant activity against hypochlorous acid (HOCl) and total antioxidant activity (TAC) by the 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation (ABTS•+). Astilbin inhibited MPO and HRP activities in a concentration-dependent relationship and effectively scavenged HOCl. The TAC by ABTS•+ of astilbin (IC50 ~ 20 mM) was higher than that of uric acid, which was used as a positive control. These data demonstrate that astilbin is a potent antioxidant and that it inhibits MPO and HRP activities efficiently.

The Inhibitory Effect of Astilbin on the Arteriosclerosis of Murine Thoracic Aorta Transplant / 华中科技大学学报（医学）（英德文版）

The inhibitory effect of astilbin on transplant arteriosclerosis in murine model of thoracic aorta transplantation was examined.Model of rat thoracic aorta transplantation was established.Ninety rats were divided into three groups.In isograft group,the thoracic aorta of Brown Norway (BN) rat was anastomosed with the abdominal aorta of another BN rat.In allograft group,the thoracic aorta of BN rat was anastomosed with the abdominal aorta of Lewis rat.In astilbin group,the rats receiving allo-transplantation were given astiibin 5 mg/kg per day for a time of 28 days.The donor thoracic aorta and the recipient abdominal aorta were anastomosed by means of a polyethylene cannula (inner diameter:1.5 mm,length:3 mm length).The grafts were histologically examined for structural changes.The areas of arterial lumen and endatrium were calculated.Our results showed that,in the allograft group,28 days after aliografting,conspicuous proliferation of smooth muscles and infiltration with a great number of inflammatory cells were found in the tunica intima and tunica media.Astilbin significantly inhibited the proliferation of smooth muscles and ameliorated the infiltration of inflammatory cells thereyby prevent against the development of transplant arteriosclerosis.It is concluded that asltilbin can effectively prevent the development of arteriosclerosis in allotrausplant by inhibiting the proliferation of smooth muscles and inhibit the proliferation of smooth muscles in tunica of intima and media and reducing infiltration of the inflammatory cells.

Effect of Astilbin on expression of CTLA-4 in activated T cells of mouse heart transplantation model with acute rejection / 中华器官移植杂志

Objective To investigate the effect of astilbin on expression of CTLA-4 in activated T cells of mouse heart transplantation model with acute rejection.Methods Cardiomyocytes of BALB/ c mouse and spleen cells of C57BL/6 mouse were separated.The cardiomyocytes(2?10~5/ml)as irri- tation cells and spleen cells(1?10~6/ml)as responsers were mixed and cultured.The model of mouse heart transplantation with acute rejection in vitro was established.Three groups were set up:control group,Astilbin(15/?g/ml) group,Astilbin+anti-CTLA-4 mAb 9H10 (30?g/ml)group.Apoptosis of T cells was observed by TUNEL.The expression of CTLA-4 in activated T cells was detected by RT-PCR and Western blot.Results Apoptosis indexes of activated T cells in Astilbin group were sig- nificantly higher than those in the control group(73.4%?12.5% vs 35.1%?9.2%,P＜0.01). The expression of CTLA-4 in Astilbin group was significantly higher than control group(P＜0.01), but there was no apparently difference between control group and Astilbin+CTLA-4 mAb group(P＞0.05).Conclusion Astilbin induces apoptosis of activated T cells in heart transplantation,which may be partially related to its enhanced expression of CTLA-4.