关节炎丸对佐剂型关节炎大鼠关节的病理研究

目的：探讨关节炎丸对佐剂型关节炎大鼠关节病理改变的影响。方法：建立佐剂型关节炎大鼠动物模型,从关节肿胀度和病理改变观察关节炎丸的治疗作用。结果：关节炎丸能显著抑制大鼠足趾肿胀度、滑膜、骨和软骨组织的破坏,且其治疗作用呈现一定的量效关系。结论：关节炎丸有消肿和抑制滑膜增生的作用。     

挂金灯活性部位对佐剂诱导性大鼠类风湿关节炎症的影响

目的:研究挂金灯活性部位对佐剂诱导性大鼠类风湿关节炎症的影响。方法:采用大鼠足趾注射完全费氏佐剂复制大鼠类风湿关节炎模型,观察挂金灯活性部位对大鼠类风湿关节炎症的影响。结果:挂金灯活性部位高、中、低浓度组对大鼠体质量的影响相对都较轻,以高剂量组治疗效果明显;挂金灯活性部位高、中、低剂量组均可以减轻费氏完全佐剂引发的大鼠足趾肿胀,其中高剂量组抑制作用最强。结论:挂金灯活性部位对AA大鼠有明显的抗炎消肿作用,能减轻或减缓炎性反应,具有减轻关节肿胀、不良反应低的特点。     

滇桂艾纳香乙酸乙酯提取物中总黄酮的含量测定

目的:建立滇桂艾纳香乙酸乙酯提取物中总黄酮的含量测定方法,为其质量控制标准提供依据。方法:采用紫外-可见分光光度法,以芦丁为对照品,5%亚硝酸钠溶液-10%硝酸-4%氢氧化钠溶液为显色系统,测定滇桂艾纳香乙酸乙酯提取物中总黄酮的含量,测定波长为510nm。结果:芦丁在0.0108～0.0645mg/ml范围内呈良好的线性关系,其回归方程为:A=12.363C+0.0055(r=0.9996);平均加样回收率为99.17%(RSD为0.66%)。结论:该方法快速简便、结果准确,可作为滇桂艾纳香乙酸乙酯提取物中总黄酮含量测定的有效方法。     

大孔吸附树脂富集纯化艾纳香废渣中总黄酮的工艺研究

目的:探究大孔吸附树脂富集纯化艾纳香废渣总黄酮的最佳工艺。方法:采用UV法测定总黄酮含量,以吸附率和解吸率为指标,采用静态吸附试验对8种大孔树脂进行筛选,优选出吸附解吸性能最佳的大孔树脂,并优化纯化条件,确定最佳工艺参数。结果:LX-17型树脂对艾纳香废渣中总黄酮有较好的吸附和解吸附效果。最佳纯化工艺为:50%乙醇提取2次,上柱液总黄酮浓度为3.03 mg·m L-1,洗脱溶剂为50%乙醇,洗脱速度为2 BV·h-1,纯化后总黄酮量高达20.03%。结论:LX-17型树脂适合富集纯化艾纳香废渣中的总黄酮。     

鼠曲草乙酸乙酯部位化学成分研究

目的：研究鼠曲草中乙酸乙酯部位的化学成分。方法：采用硅胶柱色谱、Sephadex LH-20等分离手段结合对鼠曲草乙酸乙酯萃取部位的E₁~E₃进行分离纯化,通过波谱数据分析（¹H-NMR,¹³C-NMR）进行结构鉴定。结果：从乙酸乙酯萃取部位的Fr₁~Fr₃分离了8个化合物,分别鉴定为正三十四烷醇（1）、paoriscabratine（2）、单棕榈酸酯（3）、9,16-二羰基-10,12,14-三烯-十八碳酸（4）、tithoniamide B（5）、corchoionol C（6）、胡萝卜苷（7）、2,3,5,4-四羟基反式二苯乙烯-2-O-β-D-吡喃葡萄糖苷（8）。结论：化合物 3 为首次从鼠曲草属植物中分离到,化合物 1,2,4~6,8 为首次从菊科植物中分离到。     

白芍总甙治疗类风湿关节炎药理作用研究进展

白芍总甙(total glucosides of paeonia,TGP)是从白芍干燥根中提取的有效成分单体,有效部位含有芍药甙(paeoniflonn)、羟基芍药甙(hydroxy-paeoniflorin)、芍药花甙(paeonin)、芍药内酯甙(albiflorin)、苯甲酰芍药甙(benzoylpaeoniflorin)等.新近的研究表明,白芍总甙具有抗炎和免疫调节等药理作用,临床上用于类风湿性关节炎(RA)及系统性红斑狼疮(SLE)等自身免疫性疾病的治疗,效果较好.     

鸡眼睛乙酸乙酯部位化学成分研究

目的:研究鸡眼睛乙醇提取物中等极性的乙酸乙酯萃取部位的化学成分,为民族药鸡眼睛的开发应用提供科学依据。方法:通过各种色谱分离技术对鸡眼睛乙醇提取物乙酸乙酯萃取部位进行分离纯化,根据化合物的理化性质和波谱数据鉴定其结构。结果:从鸡眼睛乙醇提取物乙酸乙酯萃取部位分离得到7个化合物,分别鉴定为:香草醛(vanillin,1),香草酸(vanillic acid,2),5-羟甲基糠醛(5-hydroxymethylfurfural,3),芥子醛(sinapic aldehyde,4),齐墩果酸(oleanolic acid,5),没食子酸(gallic acid,6),原儿茶酸(protocatechuic acid,7)。结论:其中化合物2～7为首次从该属植物中分离得到。     

小红参乙酸乙酯部位抗心肌缺血活性研究

目的:筛选出小红参抗心肌缺血主要活性部位,研究其抗心肌缺血活性。方法:通过去甲肾上腺素(norepinephrine,NE)诱导大鼠离体主动脉环收缩试验筛选小红参石油醚、乙酸乙酯、正丁醇、水部位,以主动脉环张力为观测指标,供试物浓度依次为1.5×10-3,5×10-3,1.5×10-2,5×10-2,5×10-1 g.L-1,确定小红参抗心肌缺血活性部位为乙酸乙酯部位,进一步进行此部位小鼠常压耐缺氧试验、家兔血小板聚集试验和抗垂体后叶素(pituitrin,Pit)致大鼠心肌缺血试验。结果:小红参乙酸乙酯舒张主动脉环效应明显强于其他3个部位,可能是小红参抗心肌缺血主要部位;小红参乙酸乙酯部位有一定抗小鼠常压耐缺氧作用,可显著抑制家兔血小板聚集活性,改善Pit致大鼠心肌缺血程度,明显增强大鼠心肌缺血模型血清SOD活性,降低MDA含量;1.17 g.kg-1小红参乙酸乙酯能改善Pit致大鼠心肌缺血程度,缺血后5 min T波变化百分率为8.6%±3.6%,明显增强大鼠心肌缺血模型血清SOD活性,降低MDA含量。结论:小红参乙酸乙酯部位可能是小红参抗心肌缺血的主要活性部位。     

祖师麻抗类风湿性关节炎有效部位的药效学研究

目的 研究祖师麻抗类风湿性关节炎的有效部位.方法 采用系统溶剂提取法对祖师麻进行提取、分离得到不同部位的提取物.以抗炎镇痛、刺激性等为指标,通过动物实验确定了祖师麻治疗类风湿性关节炎的有效部位及不良反应的部位.结果 乙酸乙酯提取物和正丁醇提取物为祖师麻抗类风湿关节炎的有效部位,刺激性主要来源于石油醚部位.结论 初步确定...     

枳椇子乙酸乙酯部位化学成分的研究

目的:分离鼠李科植物枳椇子种子乙酸乙酯部位的化学成分。方法:运用柱色谱法对枳椇子乙酸乙酯部位进行分离,并根据理化性质及波谱数据对所分离的化合物进行结构鉴定。结果:从中分离得到3个化合物,鉴定为:hovenitinsⅠ(Ⅰ),laricetrin(Ⅱ),Dihydromyricetin(Ⅲ)。结论:乙酸乙酯部位是枳椇子解酒的活性提取部位,该化学成分研究分离得到的三个化合物均为黄酮类,为新药的研发提供了科学依据。     

Therapeutic effects of dichloromethane fraction of Securidaca inappendiculata on adjuvant-induced arthritis in rat

Ethnopharmacological relevance

Securidaca inappendiculata (SI) is a traditional antirheumatic medicine used in China. The present study was designed to investigate the therapeutic efficacy of dichloromethane fraction of SI (SID) at three different doses on adjuvant induced arthritis (AA) rats.

Methods

Arthritis severity was evaluated by arthritic score, body weight loss, paw circumference, histological changes and hyperplasia of lymphatic tissues. Serum samples were collected for estimation of superoxide dismutase (SOD), glutathione (GSH), hydroxy radical (OH·), nitric oxide (NO), malondialdehyde (MDA), N-acetyl glucosaminidase (NAG), sialic acid (SA), alkaline phosphatase (ALP), aspartate transaminase (AST) and alanine transaminase (ALT). The levels of GSH, MDA, NAG and SA in liver were also assessed. The levels of interleukin-1 (IL-1), tumor necrosis factor alpha (TNF-α), monocyte chemotactic protein 1 (MCP-1) and vascular endothelial growth factor (VEGF) were determined using ELISA method. Another portion of blood was used for total and differential leucocyte counts.

Results

Administration with SID (at high dose with 100 mg/kg) significantly ameliorated the AA severity, suggested by the modulatory effects on body weight loss, paw swelling, hyperplasia of lymphatic tissues and synovial membrane, neutrocytosis and lymphocytosis. It also decreased levels of NO, MDA and OH·, restored SOD and GSH levels in serum. The abnormal increased levels of AST, ALT, ALP, NAG and SA significantly were reverted (compared with AA rats, P<0.01). A similar result was observed in livers. Levels of IL-1, TNF-α, MCP-1 and VEGF were reduced dramatically by SID too.

Conclusion

The results suggest SID possesses substantial anti-arthritic activity. The therapeutic efficacy may be due to immumodepressive effects, cytokines regulation, increasing membrane stability and antioxidantive activity.     

The anti-inflammatory effects of Caragana tangutica ethyl acetate extract

Ethnopharmacological relevance

Caragana tangutica KOM has been used to treat arthritis, wounds, fever and other disease conditions in traditional Chinese medicine (TMC). To support the application of the plant in traditional Chinese medicine by investigating the anti-inflammatory effects of the ethyl acetate extract of Caragana tangutica.

Materials and methods

The anti-inflammatory activity was evaluated by animal models including xylene-induced ear edema in mice, carrageenan-induced paw edema in rats, acetic acid induced writhing in mice and LPS-induced acute lung injury (ALI). The anti-inflammatory mechanism was evaluated by detecting prostaglandin E₂ and immunohistochemistry expression of cyclooxygenase-2 (COX-2) using an EIA assay kit and immunohistochemistry, respectively.

Results

The results showed that the xylene-induced ear edema in mice was significantly reduced by the ethyl acetate extract at dosages of 100, 200 and 400 mg/kg, and the carrageenan-induced paw edema in rats was monitored to be reduced by the ethyl acetate extract 3 h after carrageenan injection. The ethyl acetate extract was also found to reduce the inflammation pain of acetic acid-induced writhing model in a dose-dependent manner and cause reduction of the ALI in mice through the inhibition of the release of PGE₂ and the LPS-induced COX-2 expression in the lung.

Conclusion

Our study demonstrates that the ethyl acetate extract of the plant can help to reduce inflammations by inhibiting the expression of COX-2.     

黄连解毒汤乙酸乙酯提取物对光滑念珠菌黏附作用的影响

目的:探讨黄连解毒汤乙酸乙酯提取物(ethyl acetate extract of Huanglian Jiedu decoction,EAHD)对光滑念珠菌Candida glabrata黏附作用的影响。方法:采用二倍稀释法测定黄连解毒汤乙酸乙酯提取物对光滑念珠菌的最低抑菌浓度(minimum inhibitory concentration,MIC);采用XTT还原法评价EAHD对光滑念珠菌黏附作用的影响;利用倒置显微镜、扫描电子显微镜与荧光显微镜观察EAHD对光滑念珠菌早期黏附形态学影响;采用半定量与实时荧光定量PCR检测其黏附相关基因EPA1,EPA6和EPA7的表达量。结果:EAHD对光滑念珠菌的MIC为320 mg·L-1,阳性对照药氟康唑对光滑念珠菌的MIC为1 mg·L-1;EAHD对光滑念珠菌2,4 h的黏附的干预作用较明显,其中对4 h效果优于2 h;PCR结果显示EAHD可显著抑制EPA1,EPA6和EPA7的表达。结论:EAHD可能通过抑制光滑念珠菌部分黏附基因的表达而抑制其早期黏附。     

Protective effect of ethyl acetate fraction of Acacia ferruginea DC. against ethanol-induced gastric ulcer in rats

Ethnopharmacological relevance

In traditional systems of medicine, stem bark of Acacia ferruginea DC. is used for the treatment of itching, leucoderma, ulcers, stomatitis and diseases of the blood. In the present study, we determined antioxidant and anti-ulcerogenic activities of Acacia ferruginea stem bark.

Materials and methods

Acetone extract and its sub-fractions of Acacia ferruginea stem bark were subjected to assess their antioxidant potential using various in vitro systems such as DPPH^•, ABTS^•+ scavenging, FRAP and phosphomolybdenum reduction activities. Based on the antioxidant potential, the ethyl acetate fraction was used to evaluate the protective effect of ethanol-induced gastric damage in rat model. Enzyme activities such as superoxide dismutase, glutathione, catalase and lipid peroxidation were also determined in the stomach tissues.

Results

Ethyl acetate fraction (AFE) of Acacia ferruginea stem bark registered higher antioxidant and free radical scavenging activities than the crude acetone extract and other fractions. In addition, AFE exhibited that the IC₅₀ values of DPPH (2.5 µg/ml) and ABTS (1.8 µg/ml) were lower when compared to the standard quercetin (12.4 µg/ml and 4.7 µg/ml, respectively). In ethanol induced gastric ulcer, administration of AFE at doses of 10 mg/kg, 50 mg/kg and 100 mg/kg body weight prior to ethanol ingestion significantly protected the stomach ulceration. Consequently significant changes were observed in enzyme activities such as SOD, CAT, GSH and LPO in the stomach tissues when compared with ethanol control group.

Conclusion

It is concluded that the ethyl acetate fraction of Acacia ferruginea stem bark possessed higher antioxidant and anti-ulcerogenic activities. Based on the results, we suggest that Acacia ferruginea stem bark has potential to provide a therapeutic approach to ethanol mediated ulcer as an effective anti-ulcer agent.     

Anti-inflammatory activity of ethyl acetate fraction of the seeds of Brucea Javanica

Ethnopharmacological relevance

The seeds of Brucea javanica (L.) Merr. (Yadanzi in Chinese) have been used for the treatment of inflammation, dysentery, malaria, and cancer in Chinese traditional medicine. However, the anti-inflammatory mechanism of Brucea javanica has not been fully elucidated. This study examined the anti-inflammatory activity of ethyl acetate fraction of the seeds of Brucea javanica (EA-BJ) in vitro and in vivo.

Materials and methods

The anti-inflammatory activity of EA-BJ and its ability to modulate the production of NO, PGE2, TNF-α, IL-1β, IL-6 and IL-10 inflammatory mediators in lipopolysaccharide-activated RAW 264.7 macrophage were evaluated. Moreover, the anti-inflammatory activity of EA-BJ was also in vivo assayed by carrageenan induced paw edema in mice.

Results

In vitro assays showed remarkable anti-inflammatory activity of EA-BJ, through the inhibition of production of NO, PGE2, TNF-α, IL-1β and IL-6 inflammatory mediators and induction of production of IL-10 anti-inflammatory cytokine. In vivo assays showed anti-inflammatory activity for decrement of the paw edema in carrageenan induced paw edema test.

Conclusion

The results obtained in vitro and in vivo showed that possible anti-inflammatory effects of EA-BJ may be attributed to inhibition pro-inflammatory mediators production, NO, PGE2, TNF-α, IL-1β and IL-6 and to increase production of IL-10 anti-inflammatory cytokine. The seeds of Brucea javanica may thus prove beneficial in the treatment of inflammatory diseases.     

虎耳草乙酸乙酯部位高效液相色谱指纹图谱研究

目的:建立虎耳草药材的乙酸乙酯部位HPLC指纹图谱分析方法.方法:以Diamonsil C18色谱柱(4.6 mm×250mm,5 μm),流动相乙腈(A)-0.05％磷酸水溶液(B),梯度洗脱,流速1.0 mL·min-1,检测波长256 nm,柱温30℃.结果:建立了虎耳草药材的乙酸乙酯部位指纹图谱,确定了15个共有峰,并用对照品指认了7个峰,精密度和重复性实验中各共有峰相对保留时间RSD均小于3％,11批不同产地虎耳草相似度存在差异.结论:虎耳草药材乙酸乙酯部位指纹图谱的建立为药材质量控制提供了科学依据.     

德国鸢尾化学成分研究

通过硅胶,Sephadex LH-20葡聚糖凝胶,ODS反相柱色谱等分离技术对鸢尾科Iridaceae植物德国鸢尾Iris germanica根茎的化学成分进行分离纯化,采用理化性质及波谱分析方法对分离得到的化合物进行结构鉴定。从该植物根茎中分离得到21个化合物,分别鉴定为商陆素（1）,5,3,3’-三羟基-7,4’-二甲氧基黄烷酮（2）,5,7,4’-三羟基双氢黄酮（3）,cirsiliol-4’-glucoside（4）,3β,4’-dihydroxy-7,3’-dimethoxy flavornone-5-O-β-D-glucopyranoside（5）,染料木素（6）,irilin D（7）,muningin（8）,5,7, 4’-三羟基-6,3’,5’-三甲氧基异黄酮（9）,鸢尾苷元（10）,野鸢尾苷元（11）,鸢尾苷（12）,野鸢尾苷（13）,芒果苷（14）,irisxanthone（15）,焦谷氨酸（16）,2,4’, 6-trihydroxy-4-methoxybenzophenone-2-O-β-D-glucoside（17）,茶叶花宁（18）,草夹竹桃苷（19）,β-谷甾醇（20）,胡萝卜苷（21）。其中化合物 1~9,16,17 为首次从德国鸢尾中分离得到,化合物 8,9 为首次从鸢尾属植物中分离得到,化合物 1,4,17 为首次从鸢尾科植物中获得。     

假地豆的化学成分

目的:对假地豆化学成分进行研究。方法:采用硅胶、Sephadex LH-20柱色谱等方法进行提取分离,利用理化数据及波谱技术鉴定结构。结果:从假地豆的乙醇提取物中分离得到8个化合物:白桦脂酸(1)、木栓酮(2)、正十六烷酸(3)、β-谷甾醇(4)、亚油酸(5)、正四十一烷醇(6)、正二十八烷(7)和牡荆素(8)。结论:所有化合物均是首次从该植物中分离得到。     

樱桃花青素对佐剂性关节炎大鼠自由基和炎症因子的影响

目的:观察樱桃花青素对佐剂性关节炎(AA)大鼠自由基和抗氧化功能以及炎症因子的影响.方法:将50只SD雄性大鼠随机分为5组即正常组、模型组、樱桃花青素高、中、低剂量组.对足爪肿胀进行测量,在光镜下观察各组组织形态学变化,用比色法检测了动物外周全血的谷胱甘肽过氧化物酶(GSH-PX)活性、血清超氧化物酶(SOD)活性、血清丙二醛(MDA)含量以及血清总抗氧化能力(T-AOC).用ELISA检测血清中TNF-α含量,用放射免疫法检测了足爪PGE2含量.结果:模型组和正常组相比GSH-PX,SOD活性和T-AOC能力下降,血清MDA含量升高,血清中TNF-α和足爪PGE2含量升高.樱桃花青素组能升高GSH-PX,SOD和T-AOC活力,降低血清MDA,TNF-α以及足爪PGE2含量.光镜下组织形态观察表明樱桃花青素各组能不同程度减轻滑膜增生,减少炎细胞浸润.结论:樱桃花青素能增强AA抗氧化能力,并能降低炎症细胞因子PGE2和TNF-α,从而减轻AA模型的关节炎损伤.     

新疆一枝蒿乙酸乙酯部位化学成分研究

研究新疆一枝蒿Artemisia rupestris全草的化学成分.采用硅胶、反相、凝胶等柱色谱分离技术,对新疆一枝蒿乙酸乙酯部位进行分离纯化,采用波谱技术分析和理化常数对照等方法进行结构鉴定.从新疆一枝蒿乙酸乙酯部位分离并鉴定了12个化合物,分别为5,4'-二羟基-3,6,7-三甲氧基黄酮(1)、R-(-)-vestitol(2)、小麦黄素(3)、金圣草黄素(4)、3-吲哚甲酸(5)、七叶内酯(6)、芹菜素(7)、木犀草素(8)、反式咖啡酸(9)、紫花牡荆素(10)、金腰乙素(11)和洋艾素(12).化合物2为首次从蒿属植物分离得到,化合物1～6,9为首次从本植物中分离得到.