荆芥挥发油对白三烯拮抗活性的实验研究

目的：观察剂芥挥发油（Sto）对白三烯类炎症介质的影响，探讨其抗炎作用机理。方法：角又菜胶制备大鼠急性胸膜炎炎症模型，剂芥挥发油连续预防给药7走，ELISA法测定模型大鼠血清中LTB。含量；大鼠连续灌胃给予剂芥挥发油7天。制备腹腔白细胞悬液。加入外源性花生四烯酸，RP—HPLC法测定LTB4和LTC4的生成含量。结果：剂芥挥发油0．2、0．1mL／kg能明显降低模型大鼠血清LTB4含量，0．2mL/kg能显著减少花生四烯酸代谢产物LTB4和LTC4的生成。结论：剂芥挥发油具有拮抗白三烯活性的作用，是其良好抗炎作用的机制之一。     

清金化痰颗粒对慢性阻塞性肺疾病加重期(痰热郁肺)大鼠白三烯B4、白三烯C4及肺组织病理形态的影响

目的:清金化痰颗粒对慢性阻塞性肺疾病加重期(痰热郁肺)大鼠血清及支气管肺泡灌洗液(BALF)白三烯B4、白三烯C4及肺组织病理形态的影响。方法:采用脂多糖(LPS)加烟雾染毒制备COPD痰热郁肺证大鼠模型(正常组除外),随机分为正常组、模型组、罗红霉素组(0.0315 g·kg-1)、清金化痰颗粒低、高剂量组(9.40,37.6 g·kg-1),每日灌胃给药1次,分别于给药后p第7天、第14天每组分别处死8只大鼠,酶联免疫法(ELISA)测定血清及(BALF)白三烯B4、白三烯C4的含量及HE染色观察肺组织病理变化情况。结果:给药至第7天、第14天模型组大鼠血清及BALF中LTB4、LTC4含量较正常组明显升高(P<0.01),罗红霉素组、清金化痰颗粒低剂量组及高剂量组较模型组均显著下降(P<0.01)。第7天和第14天罗红霉素组与清金化痰颗粒高剂量组血清和BALF中LTB4和LTC4含量均明显下降,两者无明显差异(P>0.05),清金化痰颗粒低剂组血清和BALF中LTB4和LTC4含量降低低于罗红霉素组与清金化痰颗粒高剂量组血清和BALF中LTB4和LTC4含量(P<0.05)。与第7天比较,第14天罗红霉素组、清金化痰颗粒高剂量及低剂量组血清和BALF中LTB4和LTC4含量均明显下降(P<0.01)。结论:清金化痰颗粒可明显减轻COPD肺组织损伤,其作用机制与抑制LTB4和LTC4的释放有关。     

芒果苷对花生四烯酸代谢产物的影响

目的:研究芒果苷对花生四烯酸(AA)代谢产物的影响,以阐明其抗炎机理。方法:分别以反相高效液相法和放射性免疫法测定大鼠胸腔渗出液中性白细胞中白三烯B4(LTB4)、LTC4S水平和6-酮-前列腺素1a(6-keto-PGFla)含量。结果:高、中剂量的芒果苷可明显降低6-keto-PGFla的含量;而高、中、低剂量的芒果苷对LTB4、LTC4的水平则无影响。结论:芒果苷的抗炎机制可能与其抑制花生四烯酸代谢通路中6-keto-PGFla的释放有关。     

辛夷挥发油体外干预大鼠胸腔炎性白细胞5-LO活性的研究

目的:观察辛夷挥发油体外对大鼠胸腔炎性白细胞脂氧酶(5-LO)活性的影响,探讨其干预花生四烯酸代谢的抗炎机制。方法:以角叉菜胶所致急性胸膜炎模型大鼠的胸腔炎性白细胞为基本反应体系,分别加入CaCl2、MgCl2、花生四烯酸(AA)、A23187以及辛夷挥发油(0.011、0.044、0.088、0.132mg/ml)或齐留通(0.625μg/ml),提取完整白细胞的5-LO代谢产物白三烯B4(LTB4)和5-羟基二十碳四烯酸(5-HETE),运用反相高效液相色谱(RP-HPLC)紫外检测分离测定LTB4和5-HETE的合成水平,来反映5-LO的活性。结果:辛夷挥发油在0.011~0.132mg/ml浓度范围内,对大鼠胸腔白细胞LTB4与5-HETE的生物合成呈现抑制趋势。结论:辛夷挥发油体外可抑制大鼠胸腔白细胞花生四烯酸代谢酶5-LO的活性,降低LTB4与5-HETE合成水平,提示其抗炎作用可能与抑制5-LO活性,减少致炎代谢产物的生成有关。     

荆芥挥发油抗炎作用机理的实验研究

目的:观察并探讨荆芥挥发油(Sto)的抗炎作用及作用机理。方法:角叉菜胶制备大鼠气囊滑膜炎炎症模型,荆芥挥发油连续给药3天。取模型大鼠气囊灌洗液,检测蛋白质含量及WBC计数;测定气囊灌洗液中磷脂酶A2(PLA2)活性、TNF活性及PGE、MDA含量;并取炎症模型动物脾细胞及腹腔巨噬细胞检测细胞因子IL-1、IL-2活性。结果:荆芥挥发油能降低模型大鼠气囊灌洗液中蛋白质渗出量及WBC计数;降低磷脂酶A2(PLA2)活性、TNF活性及PGE、MDA含量;能抑制细胞因子IL-1活性,调节IL-2活性。结论:进一步证实了荆芥挥发油良好的抗炎作用,且提示其抗炎作用与抑制花生四烯酸代谢途径、影响致炎细胞因子及抗氧化作用有关。     

喘宁软胶囊对多形核粒细胞生成和释放白三烯的抑制作用

目的：探讨喘宁软胶囊（简称喘宁）平喘作用机制。方法：分别采用生物检定法、HPLC法、免疫ELISA法离体测试大鼠多形核粒细胞（PMNs)生成和释放慢反应物质（SRS－A）、白三烯B4（LTB4）、白三烯C4（LTC4）。结果：在离体试验中，喘宁0．1，0．4，1．6，6．4g/L浓度及喘宁4g/kg ig 20d所得血清能明显抑制大鼠PMNs生成和释放SRS－A；喘宁0．025，0．05，0．1g/L及0．1，0．4，1．6g/L浓度呈量效关系分别抑制大鼠PMNs生成和释放LTB4，LTC4。结论：初步证明喘宁有平喘作用，其机制与抑制花生四烯酸（AA）生成和释放白三烯有关。     

六味地黄颗粒对哮喘大鼠炎症介质白三烯β4、白三烯C4及5-脂氧合酶影响的研究

目的 探讨六味地黄颗粒对哮喘大鼠炎症介质白三烯β4(LTB4)、白三烯C4(LTC4)及5-脂氧合酶(5-LO)含量的影响.方法 将SFP级SD大鼠160只随机分为8组,每组20只.除空白对照组和生理盐水组外,其余各组均以卵蛋白(OVA)辅以氢氧化铝凝胶为佐剂注射致敏,2周后雾化吸入2%OVA激发哮喘,建立哮喘模型,从实验第8天,各组分别用药干预,生理盐水组用生理盐水腹腔注射及吸入代替,空白对照组不予处理,造模时间共28d,取材后,高倍镜下观察各组大鼠肺及支气管的病理学改变;采用ELISA法检测肺组织匀浆中LTB4、LTC4的浓度.对大鼠肺组织中5-LO含量进行免疫组化评估.结果 六味地黄颗粒组、六味地黄颗粒辅助地塞米松组、六味地黄颗粒辅助布地奈德组肺组织中LTB4、LTC4的浓度明显低于哮喘模型组(P＜0.05).各用药组肺组织中5-LO含量与哮喘模型组比较并无明显差异(P＞0.05).结论 六味地黄颗粒在治疗哮喘过程中可能抑制肺组织中LTB4、LTC4 分泌,这可能是其治疗哮喘的作用靶点之一.     

六种苦豆子生物碱对炎症介质白三烯的影响

目的：研究苦参碱(matrine MT)、氧化苦参碱(oxymatrine OMT)、槐果碱(sophocarpine SC)、氧化槐果碱(oxysophocarpine OSC)、槐定碱(sophoridine SRI)、氧化槐定碱(oxysophoridine OSRI)6种苦豆子类生物碱对炎症介质白三烯巴和白三烯134的影响，来研究其抗炎作用机制。方法：以大鼠腹腔白细胞为材料，采用高效液相色谱法(HPLC)测定白细胞内白三烯C4和白三烯B4水平。结果：SRI对LTC4的生物合成影响很小，但对LTB4的生物合成有明显的抑制作用。其余5种生物碱对LTC4和LTB4的生物合成均有明显的抑制作用，且有良好的剂量-效应关系。结论：6种苦豆子生物碱对白三烯(LTC4和LTB4)的生物合成均具有不同程度的抑制作用，这可能是它们抗炎作用的机制之一。     

荆芥挥发油对大鼠胸腔白细胞5-脂氧酶活性的影响

目的：探讨荆芥挥发油对5-脂氧酶(5-LO)活性的影响，以期进一步阐明其干预花生四烯酸代谢的抗炎机制。方法：以角叉菜胶急性胸膜炎模型大鼠的胸腔白细胞为基本反应体系，分别加入外源性花生四烯酸(AA)与不同质量浓度的荆芥挥发油(0.011，0.022，0.043，0.087，0.179，0.255，0.364 g·L^-1)、齐留通(0.625×10^-3 g·L^-1)，在钙离子载体A₂₃₁₈₇诱导下，提取完整白细胞的5-LO代谢产物白三烯B₄(LTB₄)和5-羟基二十碳四烯酸(5-HETE)，运用反相高效液相色谱(RP-HPLC)紫外检测分离测定LTB₄和5-HETE水平。结果：荆芥挥发油在0.022～0.364 g·L^-1内，对大鼠胸腔白细胞LTB₄与5-HETE的生物合成均呈现显著性的抑制作用(P<0.05或P<0.001)，并表现出剂量依赖性，其对LTB₄与5-HETE生成的IC₅₀分别为0.124 g·L^-1和0.142 g·L^-1。结论：荆芥挥发油体外可剂量依赖性地抑制大鼠胸腔白细胞花生四烯酸代谢酶5-LO的活性，表明其良好的抗炎作用与抑制5-LO活性，减少致炎物质LTB₄的生成有关。     

犀角地黄汤合消风散对慢性皮炎湿疹模型小鼠血清LTB4、LTC4水平的影响

目的：观察犀角地黄汤合消风散对慢性皮炎湿疹模型小鼠血清LTB4、LTC4水平的影响。方法：50只小鼠随机分为5组,致敏小鼠,实验组采用犀角地黄汤合消风散煎剂给药17天,末次激发后24h处死小鼠,使用酶联免疫吸附试验对小鼠血清LTB4、LTC4进行检测。结果：犀角地黄汤合消风散中药干预1、2组LTB4检测结果分别为0.282ng/ml、0.313ng/ml,与模型组相比有非常显著和明显的差异（P〈0.001和P〈0.05）,LTC4检测结果中药干预组分别为1.509ng/ml、1.602ng/ml,与模型组比较显著的差异（P〈0.01）。结论：犀角地黄汤合消风散对慢性皮炎湿疹模型小鼠血清LTB4、LTC4水平有显著的调节作用。     

芒果苷对脂多糖诱导慢性炎症的抗炎作用

目的:探讨芒果苷对脂多糖(LPS)诱导慢性炎症的抗炎作用及其机制。方法:90只SD大鼠随机分为正常组、模型组、泼尼松5 mg/kg组与芒果苷200、100、50 mg/kg组。以LPS间断尾静脉注射建立慢性炎症模型,进行大鼠全血白细胞计数,ELISA测定血清超敏C反应蛋白(hs-CRP)、肿瘤坏死因子(TNF-α)、白细胞介素6(IL-6)、可溶性细胞间粘附分子1(sICAM-1),RT-PCR检测白细胞核转录因子κB(NF-κB)基因表达。结果:与模型组比较,芒果苷200 mg/kg组全血白细胞总数与血清hs-CRP、TNF-α、IL-6、sICAM-1水平明显降低(P<0.05),白细胞NF-κB基因表达下调(P<0.05)。结论:芒果苷可显著抑制LPS诱导的慢性炎症,其作用机制与其下调白细胞NF-κB基因表达而降低炎症因子水平有关。     

复方栀子注射液解热抗炎作用的研究

目的研究复方栀子注射液解热抗炎的作用。方法通过家兔细菌内毒素发热、大鼠干酵母发热实验观察其解热作用;通过大鼠角叉菜胶所致足肿胀、小鼠二甲苯耳肿胀模型观察其抗炎作用。结果复方栀子注射液2mL/kg剂量组能明显减轻细菌内毒素所致家兔发热反应和干酵母所致大鼠发热反应;2、4mL/kg剂量组能显著抑制角叉菜胶所致大鼠足肿胀和二甲苯所致小鼠耳廓肿胀。结论复方栀子注射液具有明显的解热、抗炎作用。     

电针对角叉菜胶致炎大鼠的治疗作用和对COX蛋白表达的影响

目的:观察电针对角叉菜胶致炎大鼠的抗炎效应及其对环氧合酶(COX)蛋白表达的干预作用,以探讨电针抗急性炎症作用及其部分机理。方法:大鼠右后足跖皮下注射2%角叉菜胶诱导急性炎症模型,分别采用电针、消炎痛和罗非昔布治疗。采用毛细管放大法、放射免疫分析法和Western Blotting法分别检测足跖肿胀度、血清PGE2含量和足爪炎症组织及脾脏组织COX-1/-2蛋白表达水平。结果:电针可有效抑制角叉菜胶致炎大鼠足跖肿胀,尤以造模后3 h最为显著;与模型对照组比较,电针可有效降低血清中的PGE2含量;电针对环氧合酶蛋白表达无显著影响。结论:电针对角叉菜胶致炎大鼠急性炎症具有良好的抗炎效应,并通过抑制血清中PGE2含量控制炎症进一步的发展。在急性炎症过程中,电针尚未对环氧合酶蛋白表达起干预作用,其具体的抗炎机制还有待于进一步深入研究。     

Anti-inflammatory activity of Salacia oblonga Wall. and Azima tetracantha Lam.

The anti-inflammatory activity of Salacia oblonga rootbark powder and Azima tetracantha leaf powder was assayed in male albino rats using carrageenan-induced rat paw oedema (acute inflammation) and cotton pellet granuloma (chronic inflammation) methods. Both the crude drugs were maximally active at a dose of 1000 mg/kg. In the cotton pellet granuloma assay, these drugs were able to suppress the transudative, exudative and proliferative components of chronic inflammation. Furthermore, these drugs were able to lower the lipid peroxide content of exudate and liver, γ-glutamyl transpeptidase activity in the exudate of cotton pellet granuloma. The increased acid and alkaline phosphatase activity and decreased serum albumin in cotton pellet granulomatous rats were normalised after treatment with these drugs. It is likely that these drugs may exert their activity by antiproliferative, antioxidative and lysosomal membrane stabilization.     

Hypocholesterolemic and antioxidant effects of aqueous extracts from the dried calyx of Hibiscus sabdariffa L. in hypercholesterolemic rats

The present study was designed to investigate the hypolipidemic effects and antioxidant effects of Hibiscus sabdariffa L. (roselle) with regard to protection of LDL oxidation in vivo and ex vivo in rats made hypercholesterolemic by continuous cholesterol feeding. Administering the dried calyx extracts of roselle at doses of 500 and 1,000 mg/kg together with continuous cholesterol feeding to hypercholesterolemic rats for 6 weeks significantly decreased serum cholesterol level by 22% and 26%, respectively (p<0.001); serum triglycerides level by 33% and 28%, respectively (p<0.05); serum LDL level by 22% and 32%, respectively (p<0.05). However, serum HDL level was not affected. LDL was extracted from plasma of the hypercholesterolemic rats and the effects of the dried calyx extracts of roselle on the oxidation of LDL in vivo and ex vivo were examined. Six-week treatment with 250, 500 and 1,000 mg/kg of the extracts significantly decreased thiobarbituric acid reactive substances (TBARs) formation (p<0.05) while the formation of conjugated dienes during the oxidation of LDL induced by CuSO(4) was reduced, but not significantly different. These lines of evidence suggest that the aqueous extracts from the dried calyx of roselle possess both antioxidant effects against LDL oxidation and hypolipidemic effects in vivo. However, its mechanism(s) of action remains to be elucidated.     

麦冬多糖MDG-1对鼠实验性心肌缺血的保护作用

目的研究麦冬多糖（MDG-1）对鼠离体心脏缺血再灌注损伤和皮下注射异丙肾上腺素致急性心肌缺血的保护作用。方法在离体实验中,采用Langendorff豚鼠离体心脏缺血再灌注模型,将豚鼠随机分为缺血再灌注损伤组（IRI）、阳性对照组（果糖二磷酸钠,FDP）和MDG-1给药组。阳性对照组和MDG-1给药组各设10^-6～10^-4g／mL3个剂量,分别测定缺血再灌注后不同时间的心脏收缩幅度、心率、冠脉流量。在整体动物实验中,采用大鼠皮下注射异丙肾上腺素致急性心肌缺血的模型,分别给予大鼠口服MDG-110、20、40mg／kg,以普奈洛尔为阳性对照,分别设置模型组和正常对照组,观察心电图ST段位移和血浆乳酸脱氢酶（LDH）的活性。结果在离体实验中,不同剂量的MDG-1可以增加离体心脏缺血再灌注后的冠脉流量（P〈0．01）,较快恢复心脏收缩幅度（P〈0．01）,抑制由缺血再灌注引起的心率加快（P〈0．01）。在整体实验中,给予大鼠口服40mg／kgMDG-1可以抑制异丙肾上腺素导致的心肌缺血大鼠血浆LDH活性的升高（P〈0．05）,而对心电图ST段位移无显著的影响（P〉0．05）。结论MDG-1具有拮抗豚鼠离体心脏缺血再灌注损伤的作用,口服MDG-1对异丙肾上腺素所致大鼠心肌缺血损伤具有一定的保护作用。     

Anti-inflammatory activity of Bacopa monniera in rodents

The ethanol extract of Bacopa monniera (Scrophulariaceae) exhibited marked anti-inflammatory activity against carrageenan-induced paw edema in mice and rats, an acute inflammatory model. To assess the possible mechanism of anti-inflammatory action against carrageenan, the ethanol extract was treated with chemical mediators (histamine, serotonin, bradykinin, prostaglandin E(2) and arachidonic acid)-induced edema in rats. The extract selectively inhibited prostaglandin E(2)-induced inflammation. Thus, it may be inferred that B. monniera possesses significant anti-inflammatory activity that may well be relevant for its effectiveness in the healing of various inflammatory conditions in traditional medicine.     

Analgesic, anti-inflammatory and antioxidant properties of Buddleja globosa, Buddlejaceae

ETHNOPHARMACOLOGICAL RELEVANCE: Buddleja globosa, known as "matico", is employed in Chile for wound healing. AIM OF THE STUDY: To validate the traditional use of the crude drug through in vivo and in vitro evaluation of the anti-inflammatory, analgesic and antioxidant properties of its extracts. MATERIALS AND METHODS: Sequential hexane, dichloromethane, methanol and total methanol extracts were studied using bioguided fractionation. The following activities were investigated: analgesic (writhing test), oral and topic anti-inflammatory (paw- and ear-induced edema), free radical scavenging and antioxidant activities (1,1-diphenyl-2-picrylhydrazyl, DPPH, superoxide anion, lipid peroxidation and xanthine oxidase inhibition). Sodium naproxen, nimesulide, indomethacin were used as reference drugs for in vivo, quercetin and allopurinol for in vitro assays. RESULTS: A mixture of alpha- and beta-amyrins was isolated from the hexane extract that showed 41.2% of analgesic effect at 600 mg/kg, inhibited by 47.7 and 79.0% the arachidonic acid (AA) and 12-deoxyphorbol-13-decanoate (TPA)-induced inflammation at 3mg/20 microL/ear, respectively. A mixture of beta-sitosterol, stigmasterol, stigmastenol, stigmastanol and campesterol was isolated from the fraction CD4-N and beta-sitosterol-glycoside from the fraction CD5-N, reducing TPA-induced inflammation by 78.2 and 83.7% at 1mg/20 microL/ear, respectively. The fraction CD4-N at 300 mg/kg also showed analgesic activity (38.7%). The methanol extract at 600mg/kg per os showed anti-inflammatory effect (61.4%), topic anti-inflammatory (56.7% on TPA) and analgesic activity (38.5%). Verbascoside and luteolin-7-O-glucoside were the major components of the methanol extract; apigenin 7-O-glucoside was also detected. Inhibition of superoxide anion, lipoperoxidation, and DPPH bleaching effect was found in the methanol serial and global extracts. CONCLUSIONS: The present report demonstrate the analgesic and anti-inflammatory properties of Buddleja globosa and validate its use in Chilean traditional medicine.     

活血接骨丹药效作用观察

给动物灌胃活血接骨丹（２．４ｇ／ｋｇ,４．８ｇ／ｋｇ）可显著对抗。甲苯所致小鼠耳廓炎症,产生良好的抗炎作用。该药（２．４ｇ／ｋｇ）在热板镇痛实验中显示有镇痛作用。其对股骨骨折大鼠可加速骨折愈合,同时降低血清ＡＬＰ及升高血清Ｃａ,且有增加家兔动脉血流量的作用倾向。该药对小鼠急性毒性作用极小。     

Anti-inflammatory and anti-nociceptive activities of the stem bark extracts from Allanblackia monticola STANER L.C. (Guttiferae)

THE AIM OF THIS STUDY: was to assess the anti-inflammatory and mechanism of action of Allanblackia monticola (Guttiferae). The anti-inflammatory activity "in vivo" of the methylene chloride/methanol extract, methanol and methylene chloride fractions of stem barks of Allanblackia monticola, administered orally at doses of 37.5; 75; 150 and 300 mg/kg, was evaluated on carrageenan-induced oedema in rats to determine the most active fraction. Indomethacin, inhibitor of cyclo-oxygenase was used as reference drug. The effects of the most active fraction were then examined on the rat paw oedema caused by histamine, serotonin, arachidonic acid and dextran followed by its ulcerogenic effect. The results showed that the methylene chloride fraction of Allanblackia monticola was more effective on the oedema caused by the carrageenan. The anti-nociceptive activity of the methylene chloride fraction was assessed using the acetic acid-induced abdominal constriction model, formalin test and hot plate test. At 150 mg/kg, Allanblackia monticola caused maximum inhibitions of inflammation induced by carrageenan (83.33%), by histamine (42.10%), by dextran (40.29%) and by arachidonic acid (64.28%). Allanblackia monticola (75-300 mg/kg) did not cause significant modification of the oedema induced by serotonin. Concerning the anti-nociceptive properties of the plant, the methylene chloride fraction (75-300 mg/kg) caused a dose-dependent inhibition on abdominal contractions induced by acetic acid (32.34-77.37%) and significantly inhibited the inflammatory pain caused by formalin (40.71-64.78%). Allanblackia monticola did not increase the latency time in the hot plate test. Like indomethacin (10mg/kg), the fraction at the dose of 150 mg/kg caused ulceration of the gastric mucous membrane in treated rats. These results show that Allanblackia monticola has an anti-inflammatory and analgesic activities with gastric ulcerative side effects.