黄藤合剂的急性毒性和药效学研究

用热板法和扭体法研究黄藤合剂镇痛效果,测定毛细血管通透性和炎症组织PGE2含量以研究其抗炎活性及机理.小鼠灌胃给予黄藤合剂最大给药量76.8 g/kg后,7天内未见明显异常变化.黄藤合剂8mg/kg即能明显提高小鼠对热刺激的痛阈值,减少醋酸引起的扭体次数,降低毛细血管通透性,减少炎症组织PGE2的含量.16 g/kg,还能推迟疼痛反应出现的时间,延长潜伏期.黄藤合剂具有镇痛抗炎作用,最大给药量为76.8 g/kg,其作用机理可能与减少PGE2含量有关.     

草苁蓉多糖的体内抗炎作用

用二甲苯致小鼠耳肿胀、急性腹腔炎症模型对PBR抑制小鼠急性炎症作用进行研究,采用右旋糖酐致大鼠足肿胀模型探讨其亚急性抗炎作用。结果发现,1.6 g·kg-1的PBR能有效抑制二甲苯致小鼠耳肿胀,并能显著抑制小鼠体内白细胞及中性粒细胞的渗出,与PBS组相比差异显著（P〈0.05）。不同浓度的PBR在给药1h后可不同程度地抑制右旋糖酐所致大鼠足跖肿胀,其中140 mg·kg-1的PBR在给药4h后抑制作用更明显,与PBS组相比差异极显著（P〈0.01）。这表明,PBR具有一定的抗急性和亚急性炎症作用,其机理很可能是抑制血管内白细胞和中性粒细胞的渗出。该研究为进一步研究开发PBR提供了实验依据。     

酢浆草对小鼠急性腹膜炎的抗炎镇痛作用研究

目的:研究酢浆草对醋酸所致急性腹膜炎小鼠的抗炎镇痛作用。方法:腹腔注射醋酸制备小鼠急性腹膜炎模型,观察酢浆草乙醇提取物对醋酸所致小鼠扭体反应的影响;观察酢浆草乙醇提取物对醋酸所致小鼠腹腔毛细血管通透性增高的影响。结果:酢浆草乙醇提取物能使小鼠扭体反应次数减少;能降低小鼠腹腔毛细血管的通透性。结论:酢浆草对醋酸所致小鼠急性腹膜炎具有一定的抗炎镇痛作用。     

泻心汤不同剂量配伍的抗炎作用比较研究

目的不同剂量配伍时泻心汤的抗炎作用的对比分析,其抗炎作用有何影响。方法采用角叉菜胶导致小鼠炎症模型,经口灌胃小鼠不同剂量配伍的泻心汤水提液,连续灌胃给药5 d后,测定足肿胀度;试验测定丙二醛(MDA)含量和一氧化氮(NO)含量,查看其抗炎作用的活性。结果对比模型炎症对照组,生理盐水组、地塞米松组及各个剂量配伍组的足肿胀度均比模型对照组低,差异有统计学意义(P0.05);与剂量配伍4组相比较,剂量配伍2组足肿胀度下降,差异有统计学意义(P0.05)。与模型对照组比较,生理盐水组、地塞米松组及各个剂量配伍组MDA含量和NO含量均低于模型对照组组,差异有统计学意义(P0.05);与剂量配伍4组进行对比,剂量配伍2组NO含量和MDA的含量均下降,差异有统计学意义(P0.05)。结论三黄泻心汤的不同剂量配伍时抗炎作用不一样。     

Luffolide,a novel anti-inflammatory terpene from the spongeLuffariella sp.

Summary Luffolide (4) is a minor metabolite of the spongeLuffariella sp. from Palau. The structure of luffolide was determined by single crystal X-ray analysis. Luffolide is relatively unstable and undergoes a complex cyclization reaction to give the hexacyclic products5 and6. Luffolide (4) has some of the anti-inflammatory properties of manoalide (1): this may help to define the chemical reaction between manoalide (1) and phospholipase A₂.All crystallographic calculations were done on a PRIME 9950 computer operated by the Cornell Chemistry Computing Facility. Principal programs employed were: FOBS, a data reduction program by G.D. Van Duyne, Cornell University, 1987; MULTAN 80, and RANTAN 80, systems of computer programs for the automatic solution of crystal structures from X-ray diffraction data (locally modified to perform all Fourier calculations including Patterson syntheses) written by P. Main, S. E. Hull, L. Lessinger, G. Germain, J. P. Declercq and M. M. Woolfson, University of York, England, 1980 BDLS, an, anisotropic block diagonal least squares refinement written by K. Hirotsu, E. Arnold, and G. D. Van Duyne, Cornell University, 1987; PLUTO 78, a locally modified crystallographic illustration program by W. D. S. Motherwell, Cambridge Crystallographic Data Centre, 1978; and BOND, a program to calculate molecular parameters and prepare tables written by K. Hirotsu and G. Van Duyne, Cornell University, 1985.Acknowledgment. We thank the Government of the Republic of Palau for a scientific research permit. We thank Dr Klaus Rützler, Smithsonian Institution, Washington, D.C. for identifying the sponge and Mary Kay Harper for performing additional bioassays. This research was supported by grants from the Sea Grant College Programs of California [Projects R/MP-30 to DJF) and R/MP-31 (to RSJ)] and New York (to JC) and the National Institutes of Health (CA 24487 to JC).     

红土沉香的化学成分及其抗炎活性研究

综合运用多种柱色谱技术从越南红土沉香乙醇提取物中分离得到13个化合物,经过现代波谱学技术鉴定其结构为：7-甲氧基-2-[2-(4-甲氧基苯基)乙基]色酮(1),6-甲氧基-2-(2-苯乙基)色酮(2),6,7-二甲氧基-2-(2-苯乙基)色酮(3),6-甲氧基-2-[2-(4-甲氧基苯基)乙基]色酮(4),6-甲氧基-2-[2-(3-甲氧基苯基)乙基]色酮(5),5-羟基-6-甲氧基-2-[2-(4-甲氧基苯基)乙基]色酮(6),6,8-二羟基-2-(2-苯乙基)色酮(7),(1β,3α,4aβ,5β,8aα)-4a,5-dimethyl-3-(prop-1-en-2-yl)octahydronaphthalene-1,8a(1H)-diol(8),rel-(4S,5R,7R,8R,11R)-eremophil-9-en-12,8-olide(9),cyclodebneyol(10),柯拉斯那酸甲酯(11),白木香醇(12)和4-表-15-羟基菖蒲螺烯酮(13).其中,化合物1为新天然产物,所有化合物均为首次从红土沉香中分离得到.以上化合物的抗炎活性测试结果表明,化合物3、8和13具有一定的抗炎活性,IC50值分别为81.23 ± 2.83、39.55 ± 3.75和72.63 ± 2.87 μmol·L－1.     

非甾体类抗炎药的临床应用研究

目的阐述非甾体抗炎药物的临床应用.方法通过对国内外文献的比较分析,概述非甾体抗炎药作用机制、发展进程及发展趋势.结果非甾体抗炎药物是通过抑制花生四烯酸代谢而发挥作用,但对花生四烯酸代谢酶的选择性差异造成其严重的不良反应,使非甾体抗炎药临床应用受限.结论为了降低药物的不良反应,选择性COX-2/5-LO双重抑制剂及一氧化氮释放型非甾体抗炎药是临床用药的发展趋势.     

Aspirin-like drugs may block pain independently of prostaglandin synthesis inhibition

Summary Using flurbiprofen, a chiral anti-inflammatory and analgesic 2-arylpropionic acid derivative, the enantiomers of which are not converted to each other (less than 5%) in rats or man, we obtained evidence that prostaglandin synthesis inhibition is primarily mediating the anti-inflammatory activity but prostaglandin synthesis independent mechanisms contribute to the analgesic effects. Thus, the S-form inhibited prostaglandin synthesis, inflammation and nociception in rats. The R-form had much less effect on prostaglandin synthesis and did not affect inflammation. It did, however, block nociception in rats almost as potently as the S-form. S-flurbiprofen, in contrast to the R-form, was clearly ulcerogenic in the gastrointestinal mucosa. These results indicate additional molecular mechanisms of analgesia and suggest the use of R-arylpropionic acids as analgesics.     

CD1d and natural T cells: how their properties jump-start the immune system

Cellular and humoral immune mechanisms recruited to defend the host from infectious agents depend upon the early immune events triggered by antigen. The cytokine milieu within which the immune response matures is the most important of many factors that govern the nature of the immune response. Natural T cells, whose function is controlled by CD1d molecules, are an early source of cytokines that can bestow type 1 or type 2 differentiative potential upon helper T lymphocytes. This review attempts to illuminate the glycolipid antigen presentation properties of CD1d, how CD1d controls the function of natural T cells and how CD1d and natural T cells interact to jump start the immune system. CD1d is postulated to function as a sensor, sensing alterations in cellular lipid content by virtue of its affinity for such ligands. The presentation of a neo-self glycolipid, presumably by infectious assault of antigen-presenting cells, activates natural T cells, which promptly release pro-inflammatory and anti-inflammatory cytokines and jumpstart the immune system. Received 10 July 2000; received after revision 16 October 2000, accepted 16 November 2000     

扁担杆正丁醇提取物抗炎作用及机制研究

采用化学方法制备扁担杆正丁醇提取物．采用二甲苯致小鼠耳郭肿胀法及角叉菜胶致小鼠足肿胀法观察抗炎作用,采用酶联免疫吸附法（ELISA）测定血清IL-1β和TNF-α含量,分析抗炎机制．与对照组比较,高浓度扁担杆正丁醇提取物对二甲苯致小鼠耳郭肿胀及角叉菜胶致小鼠足肿胀均具有显著的抑制作用（P＜0．05）,并可不同程度降低角叉菜胶致炎小鼠血清IL-1β和TNF-α的含量（P＜0．05）．扁担杆正丁醇提取物具有一定的抗炎作用,其抗炎作用机制可能与降低TNF-α和IL-1β的表达有关．