Protective effects of Foeniculum vulgare root bark extract against carbon tetrachloride-induced hepatic fibrosis in mice

AIM To investigate the protective effects of Foeniculum vulgare root bark (FVRB), a traditional Uyghur medicine, against carbon tetrachloride (CCl4)-induced hepatic fibrosis in mice. METHODS Mice were randomly divided into eight groups (n = 20 each). Except for the normal control group, mice in the rest groups were intraperitoneally injected (i.p.) with 0.1% CCl4-olive oil mixture at 10 mL/kg twice a week to induce liver fibrosis. After 4 wk, mice were treated concurrently with the 70% ethanol extract of FVRB (88, 176, 352 and 704 mg/kg, respectively) daily by oral gavage for 4 wk to evaluate its protective effects. Serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), triglyceride (TG), hexadecenoic acid (HA), laminin (LN), glutathione (GSH), superoxide dismutase (SOD), and malondialdehyde (MDA) in liver tissues were measured. Hematoxylin-eosin (H and E) staining and Masson trichrome (MT) staining were performed to assess histopathological changes in the liver. The expression of transforming growth factor beta 1 (TGF-beta 1), matrix metalloprotein 9 (MMP-9) and metallopeptidase inhibitor 1 (TIMP-1) was detected by immunohistochemical analysis. Additionally, TGF-beta 1 and alpha-smooth muscle actin (alpha-SMA) protein expression was measured by Western blot. RESULTS A significant reduction in serum levels of AST, ALT, TG, HA and LN was observed in the FVRB-treated groups, suggesting that FVRB displayed hepatoprotective effects. Also, the depletion of GSH, SOD, and MDA accumulation in liver tissues was suppressed by FVRB. The expression of TGF-beta 1, MMP-9 and TIMP-1 determined by immunohistochemistry was markedly reduced in a dose-dependent manner by FVRB treatment. Furthermore, protective effects of FVRB against CCl4-induced liver injury were confirmed by histopathological studies. Protein expression of TGF-beta 1 and alpha-SMA detected by Western blot was decreased by FVRB treatment. CONCLUSION Our results indicate that FVRB may be a promising agent against hepatic fibrosis and its possible mechanisms are inhibiting lipid peroxidation and reducing collagen formation in liver tissue of liver fibrosis mice.

Optimization of Polysaccharide Extraction from Radix Glehniae Root Bark by Response Surface Methodology and Anti-immunosuppressive Activity Analysis

[ Objective ] This study aimed to establish and optimize the extraction technology of polysaccharides from Radix Glehniae root bark, and to explore the processing methods of Radix Glehniae in producing areas. [ Method ] Based on the single-factor experiment, with polysaccharide content and polysaccharide yield as indices, various factors affecting polysaccharide yield from Radix Glehniae root bark were investigated by central composite design-response surface method. Mo- reover, immune functions of cyclophosphamide-induced blood-deficient mice in various polysaccharide groups were compared to investigate the effects of root bark removal of Radix Glehniae on medicinal quality. [ Result] Ultrasonic extraction was the appropriate extraction technology of polysaccharides from Radix Glehniae root bark. The optimal ultrasonic extraction conditions were ultrasonic time 36 min, ultrasonic power 460 W, solid-liquid ratio 1： 10, ethanol concentration 80%, under which polysaccharide yield reached 16.08%. Polysaccharides extracted from Radix Glehniae root （ALP） and Radix Glehniae root bark （BLP） could effec- tively improve immune function of blood-deficient mice with no significant differences. [ Conclusion] Radix Glehniae could be used without removal of root bark. The optimized extraction process was stable and feasible, which laid a solid foundation for further comprehensive development and utilization of Radix Glehniae root bark.

Study on the Mechanism of Mulberry Root Bark Decoction in the Treatment of Chronic Obstructive Pulmonary Disease based on Network Pharmacology

Objective:Study the mechanism of Mulberry Root Bark Decoction in the treatment of COPD based on network pharmacology.Methods:The active components and predictive targets of Mulberry Root Bark Decoction were screened by TCMSP database.The disease targets of COPD were collected by searching GeneCards,DisGeNET,PhamGKB and TTD databases.Using R language to draw Venn diagram,and get the key target of Mulberry Root Bark Decoction in the treatment of COPD.Cytoscape was used to construct the regulatory network of drug active ingredient disease target.The key targets were imported into string database to construct protein-protein interaction network,and the core targets were obtained by network topology analysis with Cytoscape software.Finally,the Bioconductor platform and R language were used for GO and KEGG enrichment analysis・Results:There were 142 active components and 255 drug targets in Mulberry Root Bark Decoction.1941 COPD targets were retrieved.There were 129 common targets of Mulberry Root Bark Decoction and COPD;Eight core targets of PPI network were obtained.GO function analysis is involved in oxidative stress,cellular chemical stress and other biological processes.Cell components such as cell membrane raft and membrane region involve molecular functions such as ubiquitin like protein ligase and DNA binding transcription factor.KEGG mainly includes PI3K-Akt signal pathway,tumor necrosis factor signal pathway,IL-17 signal pathway,etc.Conclusion:Quercetin,luteolin,kaempferol,wogonin and other active components in Mulberry Root Bark Decoction act on PI3K/Akt,TNF,IL-17,TCR and other signal pathways through Jun,TP53,MAPK1,IL6 and other targets to play an anti-inflammatory and reduce oxidative stress response role.The results of this study can provide a reference for further study on the mechanism of Mulberry Root Bark Decoction in the treatment of chronic obstructive pulmonary disease.

Evaluation of antitumour activity of Calotropis gigantea L.root bark against Ehrlich ascites carcinoma in Swiss albino mice

Objective:To investigate experimentally the possible antitumor effect of methanol extract(ME) of Calotropis gigantea L.(C.gigantean) root bark and its petroleum ether(PEF) and chloroform(CF) soluble fractions against Ehrlich ascites carcinoma(EAC) in Swiss albino mice.Methods:The effects of ME(10 and 20 mg/kg),PEF(40 and 80 mg/kg) and CF(20 and 40 mg/kg) on the growth of EAC and life span of EAC bearing mice were studied.Hematological profile and biochemical parameters(SAI.P,SGPT and SCOT) were also estimated.Results:Results of in vivo study showed a significant decrease in viable tumor cell count and a significant increase of life span in the ME and CF treated group compared to untreated one.The life span of ME and CF treated animals was significandy(P【0.05) increased by 43.90%(20 mg ME/kg) and 57.07%(40 mg CF/kg).ME and CF brought back the hematological parameter more or less normal level.ME and CF also restored the altered levels of serum alkaline phosphatase(SALP) and serum glutamate oxaloacetate transaminase(SGOT).Conclusions:Methanol extract(ME) of C.gigantea root bark and its chloroform soluble fraction(CF) possesses significant antitumor activity.

Evaluation of in-vitro antibacterial activity and anti-inflammatory activity for different extracts of Rauvolfia tetraphylla L.root bark

Objective:To assess the in-vitro antihacterial activity and anti-inflammatory activity of orally administered different extracts(Hydro-alcoholic,methanolic,ethyl acetate and hexane)of Rauvolfia tetraphylla(R.tetraphylla)root bark in Carrageetiaii induced acute inflammation in rats.Methods:In-vitro antibacterial activity was evaluated for extracts against four Gram positive and four Gram negative bacteria by using cylinder plate assay.Hydro-alcoholic extract(70%v/v ethanol)at 200,400 and 800 mg/kg doses and methanolic,ethyl acetate and hexane extracts at doses 100,200 and 400 mg/kg were tested for anti-inflammatory activity in Carrageenan induced rat paw oedema model and paw thickness was measured every one hour up to 6 hrs.Results:All extracts of R.tetraphylla root bark showed good zone of inhibition against tested bacterial strains.In Carrageenan induced inflammation model,hydro-alcoholic and methanolic extract of R.tetraphylla root bark at three different doses produced significant(P<0.00l)reduction when compared to vehicle treated control group and hexane,ethyl acetate extracts.Conclusions:In the present study extracts of R.tetraphylla root bark shows good in-vitro antibacterial activity and in-vivo anti-inflammatory activity in rats.

Separation and Purification of Acetophenones from Cynanchum bengei Decne Root Bark by Combination of Silica Gel and High-speed Counter-current Chromatography

[Objectives] To develop a method for separation and purification of acetophenones from Cynanchum bengei Decne root bark by combination of silica gel and high-speed counter-current chromatography( HSCCC). [Methods]The crude extract of Cynanchum bengei Decne root bark was separated by silica gel column chromatography,and parts A and B containing acetophenones were obtained. Then,parts A and B were separated by HSCCC with a two-phase solvent system composed of petroleum ether-ethyl acetate-methanol-water( 4∶ 6∶ 4. 5∶ 5. 5 and4∶ 6 ∶ 3 ∶ 7, V/V), respectively. [Results] From 260 mg of part A, four compounds with p-dihydroxybenzene 3. 9 mg(Ⅰ),4-hydroxyacetophenone 17. 1 mg( Ⅱ),2,5-di-hydroxyacetophenone 13. 3 mg(Ⅲ) and 2,4-dihydroxyaceto-phenone 21. 0 mg(Ⅳ) were obtained. And from 300 mg of part B,136 mg of Radix Cynanchi Bungei benzophenone(Ⅴ) was obtained. The purity of compounds determined by HPLC was 97. 0%,96. 6%,99. 2%,99. 7%,99. 5%,respectively. [Conclusions] The established method is simple and efficient. It can be used for separation of acetophenones from Cynanchum bengei Decne root bark and has better practical value,which could provide a reference basis for development and utilization of Cynanchum bengei Decne root bark.

Cytotoxicity and anti-inflammatory effects of root bark extracts of Acanthopanax henryi

AIM: To investigate the cytotoxicity, anti-inflammatory activity, and action mechanism of root bark extracts of Acanthopanax henryi. METHOD: The hot methanol extract of the root bark of A. henryi was subjected to XAD-4 column chromatography eluting with a gradient of methanol in water. The cytotoxicity and anti-inflammatory effects of the MeOH fractions were evaluated on the inhibition on lipopolysaccharide(LPS)-induced nitric oxide, prostaglandin E2, interleukin-1β, and interleukin-6 production in RAW 264.7 macrophages. RESULTS: The 80% MeOH fraction was a better inhibitor of LPS-induced NO, PGE2, IL-1β, and IL-6 production, and expression of inducible nitric oxide synthase(iNOS) at the protein levels in a concentration-dependent manner. CONCLUSION: The 80% MeOH fraction of A. henryi root bark has significant anti-inflammatory activity. This provides a pharmacological basis for clinical application for the treatment of inflammation.

桑源药材的化学成分及治疗2型糖尿病的作用机制研究进展

桑叶、桑枝、桑白皮、桑葚等药材源于桑科植物桑Morus alba L,具有良好的生理活性。桑源药材中含有黄酮类、生物碱类、多糖类、酚酸类、Diels-Alder型和香豆素类等多种化学成分,其中黄酮类化合物、多糖或生物碱是其特征性活性成分。桑叶、桑枝、桑白皮、桑葚及其有效成分可能通过抑制α-葡萄糖苷酶的活性、保护胰岛β细胞、改善炎症反应、抗氧化应激、调节线粒体代谢、调节肠道菌群、改善糖尿病并发症等途径达到防治2型糖尿病的作用。本文对桑源药材的化学成分及其在2型糖尿病防治中的应用及作用机制进行了系统综述,以期为桑源药材的开发及临床合理应用提供指导。

仝小林应用桑白皮、地骨皮、白鲜皮治疗老年皮肤瘙痒症经验

仝小林院士认为老年皮肤瘙痒症发病往往由于老年阴分不足,郁生内热,煎灼上焦发为肺热,并生温燥扰动皮毛。临床常在滋阴润燥的基础上,加用桑白皮、地骨皮、白鲜皮组成的三皮止痒方清热养阴止痒。方中桑白皮清泻肺热,善治浮风燥痒;地骨皮常与桑白皮同用,滋阴降火解决老年患者阴虚体态,且平肺气、除郁热,使肺热宣泄而皮毛开;白鲜皮清热燥湿、祛风解毒,为治皮肤瘙痒之靶药。三者配伍,态靶结合,既合老年皮肤瘙痒症的病机特点,又能针对性减轻患者瘙痒症状,临床常用剂量均为15~30 g。

重构本草——白鲜皮

通过古籍文献调研、中药现代研究进展及其研究成果的梳理,结合中医临床及中药学等学科领域内专家学者的认识及应用经验,经讨论认为:白鲜皮的功效主要为清热燥湿,祛风解毒。症靶为瘙痒。现代药理发现,白鲜皮及其有效成分具有抗过敏、抗真菌、抗炎、抗氧化、抗肿瘤、止血、神经保护等作用。本品内服有肝损伤可能,注意合理用药。临床煎服剂量多为5~30 g,外用剂量为15~100 g,勿大剂量久服。

牡丹根皮提取物对D-半乳糖致小鼠衰老模型的影响

利用D-半乳糖诱导的皮肤衰老模型,评估了牡丹根皮提取物对多种生物标志物的影响,以及对皮肤含水量和水分散失量的影响。结果表明,牡丹根皮提取物能够显著改善皮肤的丙二醛(MDA)水平和过氧化氢酶(CAT)活性,有效降低晚期糖基化终末产物(AGEs)和白介素1β(1L-1β)的水平,同时对小鼠皮肤病理有显著的改善效果。此外,牡丹根皮提取物还能降低皮肤炎症因子,增加皮肤中的总超氧化物歧化酶(SOD),改善羟脯氨酸(HYP)水平和Ⅲ型胶原蛋白(COLⅢ)水平。然而,对谷胱甘肽(GSH)、肿瘤坏死因子-α(TNF-α)、皮肤含水量和皮肤水分散失的影响较小。总的来说,牡丹根皮提取物在一定程度上展现了优秀的抗衰老效果,这为其在抗衰老产品中的应用提供了科学依据。

丹皮的化学成分研究

目的 研究中药丹皮 Paeonia suffruticosa的化学成分。方法 利用反复硅胶柱层析进行分离纯化 ,通过波谱分析鉴定化合物结构。结果 分离得到 9个化合物 ,分别鉴定为白桦脂酸 (betulinic acid, ) ,白桦脂醇 (betulin, ) ,齐墩果酸 (oleanolic acid, ) ,3β,2 3- dihydroxy- 30 - norolean- 12 ,2 0 (2 9) - dien- 2 8- oic acid ( ) ,芍药苷元(paeoniflorigenone, ) ,3- O- m ethylpaeonisuffral( ) ,牡丹酚 (paeonol, ) ,6 -羟基香豆素 (6 - hydroxycoum arin, )和没食子酸 (gallic acid, )。结论 化合物 ～ 和 为首次从该植物中分离得到。

6种宁神类药物抗抑郁作用动物实验研究

目的 探讨石菖蒲、酸枣仁、朱砂、远志、茯神、合欢花等6种宁神类药物的抗抑郁作用.方法 采用旷场试验评价药物对小鼠自发活动的影响,强迫游泳和强迫悬尾实验评价药物对小鼠不动时间的影响,Western-blot免疫印迹检测胶质纤维酸性蛋白的表达.结果 与对照组比,旷场试验中各实验组动物活动总路径差异无统计学意义（P＞0.05）,强迫游泳实验中石菖蒲、朱砂、远志、茯神、合欢花组不动时间显著缩（P＜0.05～0.01）,悬尾实验中石菖蒲、朱砂、远志和茯神组不动时间显著缩短（P＜0.05～0.01）,各组GFAP蛋白表达差异无统计学意义（P＞0.05）.结论 石菖蒲、朱砂、远志、茯神、合欢花具有抗抑郁作用.

榆树根皮的化学成分

目的研究榆科植物榆树 (UlmuspumilaL )根皮中的化学成分。 方法利用硅胶柱色谱、凝胶柱色谱、制备薄层色谱以及半制备HPLC进行分离纯化 ;根据理化性质和光谱数据进行结构鉴定。结果从榆树根皮的乙酸乙酯提取物中共分离得到 7个化合物 ,经鉴定分别为mansononeE(UE Ⅰ )、滨蒿内酯 (UE Ⅱ )、mansononeF(UE Ⅲ )、齐墩果酸 (UE Ⅳ )、1 亚油酸甘油单酯 (UE Ⅴ )、maslinicacid(UE Ⅵ )和 β 谷甾醇 (UE Ⅶ )。 结论化合物UE Ⅱ、UE Ⅳ～Ⅵ为从榆属植物内首次分离 ;UE Ⅰ、UE

榆树根皮的化学成分(Ⅱ)

目的研究榆树(Ulmus pumilaL.)根皮中的化学成分。方法采用反复硅胶柱色谱法,凝胶柱色谱法等进行分离纯化;通过理化常数测定和光谱分析鉴定其化学结构。结果分离得到了8个化合物,即1十七烷酸甘油单酯(1 heptadecanoyl glycerol,1)、花生酸(eicosanoic acid,2)、1十六烷酸甘油单酯(1 hexadecanoyl glycerol,3)e、pifriedelanol(4)、无羁萜(friedelin,5)c、amaldulenic acid(6)、arjunolic acid(7)、异莨菪亭(isoscopoletin,8)。结论化合物1为首次从自然界分离得到,化合物2、3、6、7、8为属内首次分离得到,化合物4、5为种内首次分离得到。

白鲜皮抗内毒素活性物质的分离提取与活性研究

提要:目的筛选与类脂A(lipidA)具有较高结合活性的中药,从中提取具有拮抗内毒素(lipopolysaccharide,LPS)活性的物质。方法采用生物传感技术,以lipidA为靶点,检测42种中药的水提物与lipidA的结合活性;以白鲜皮为研究对象,通过大孔吸附树脂、溶剂萃取、聚酰胺柱层析和高效液相色谱(HPLC)法,分离提取与lipidA结合活性较高的组分;动态比浊法鲎试验检测HPLC产物DPR-1～3对LPS(0.1ng/ml)的中和作用;ELISA法检测DPR-2对LPS(100ng/ml)刺激的RAW264.7细胞释放肿瘤坏死因子-α(TNF-α)及白细胞介素-6(IL-6)的影响。结果8种中药水提物与lipidA具有较高的结合活性(RU>100arc/s);从白鲜皮中逐步分离出与lipidA结合活性较高的组分,经HPLC法获得3种物质DPR-1～3;DPR-2对LPS具有一定的中和作用,在8μg/ml浓度以上可显著抑制LPS诱导的RAW264.7细胞释放TNF-α和IL-6(P<0.05),并具有剂量效应关系。结论从42种中药中筛选出与lipidA具有较高结合活性的中药白鲜皮,并从中分离提取出抗LPS活性物质DPR-2,其抗LPS活性可能与DPR-2对LPS的中和活性有关。

白鲜皮化学成分的研究

目的研究白鲜皮Dictamni Cortex的化学成分。方法该植物乙醇提取液的乙酸乙酯部位经硅胶、Sephadex LH-20凝胶、制备HPLC柱分离纯化,所得化合物的结构通过各种光谱方法进行鉴定。结果从中分离得到10个化合物,分别鉴定为异阔戴明(1)、尼克酰胺(2)、丁香酸(3)、白鲜碱(4)、柠檬苦素(5)、吴茱萸苦素(6)、梣酮(7)、黄柏酮(8)、大叶桉亭(9)、β-谷甾醇(10)。结论化合物1为首次从芸香科植物中分得,化合物2为首次从白鲜属植物中分得,化合物3为首次从该植物中分得。

高效液相色谱法测定棉根皮中棉酚含量

目的 :建立棉根皮中主要有效成分棉酚的含量测定方法。方法 :丙酮超声提取 ,C18柱 ,乙腈 0 .2 %磷酸水 (85∶15 )为流动相 ,检测波长 2 35nm。结果 :平均回收率 97.6 % ,RSD为 1.5 9% (n =5 )。结论 :此方法适用于棉根皮中棉酚的含量测定 ,并测定了 3种棉根皮中棉酚含量。

紫荆皮、紫金皮、昆明山海棠镇痛作用比较研究

[目的]观察紫荆皮、紫金皮、昆明山海棠外用的镇痛作用,为指导临床合理用药和开发新药提供科学依据。[方法]采用小鼠醋酸扭体法、小鼠热板法和大鼠热辐射法比较3种药物外用的镇痛效果。[结果]紫荆皮、紫金皮、昆明山海棠均能延长热板法小鼠舔足时间。显著减少醋酸所致的小鼠扭体次数,镇痛率可达30%以上,显著提高大鼠痛阈值。[结论]紫荆皮、紫金皮、昆明山海棠均具有明显的镇痛作用,其中以昆明山海棠效果最佳。

桑白皮的化学成分研究

采用硅胶和凝胶柱层析方法对桑白皮(Cortex Mori)的化学成分进行分离纯化,并根据理化性质和光谱数据分析鉴定得到11个化合物,分别是:羟基白藜芦醇(Hydroxyresveratrol,1),桑叶苷A(mulberroside A,2),熊果酸(ursolic acid,3),3-乙酰基-α-香树酯醇(3-acetyl-α-amyranol,4),熊果烷(ursane,5),β-谷甾醇(β-sitosterol,6),胡萝卜苷(daucosterol,7),十六碳烷酸(palmitic acid,8),十八碳烷酸(stearic acid,9),二十六烷酸-α-单甘油酯(α-glycerol monohexacosanoate,10),二十八烷酸-α-单甘油酯(α-glycerol monooctacosanoate,11)。其中化合物5、8～11均为首次从桑白皮中获得。