异喹啉类生物碱的免疫调节作用*

异喹啉类生物碱是自然界存在的种类最多的一大类生物碱,具有抗肿瘤、抗炎、免疫调节和镇痛等多种生物活性。本文综述了阿朴菲类、双苄基异喹啉类、小檗碱类、吗啡类和苯菲啶类异喹啉生物碱对机体免疫应答的调节作用和机制,为其深入研究与开发提供参考。     

异喹啉类生物碱的生理活性及研究进展

异喹啉类生物碱是生物碱类成分的重要组成部分,该类生物碱数量多(目前发现有1000多种),结构类型复杂,药用价值大,具有多方面的生理活性.     

四氢异喹啉类生物碱的生物活性多样性及其作用机制

四氢异喹啉类生物碱在自然界中分布广泛, 有些药物在临床上已广泛应用。随着对四氢异喹啉类生物碱研究的深入, 越来越多新的生物活性、新的作用机制和靶点被发现和揭示, 此类生物碱生物活性的多样性受到人们广泛关注。本文综述了近五年来四氢异喹啉类化合物在抗肿瘤、抗菌、抗病毒、抗炎、抗凝血、支气管扩张及中枢神经系统作用等方面的活性及机制研究的新进展, 旨在为四氢异喹啉类生物碱的活性研究提供思路和启示, 为寻找先导化合物、合理设计药物分子提供依据。     

苯酞异喹啉类生物碱构型研究

本文论述了利用~1H核磁共振谱推定苯酞异喹啉类生物碱的相对构型,再以其比族光度确定其绝对构型的有关问题。     

紫堇属植物中异喹啉类生物碱的综述

紫堇属植物在自然界中分布广泛,其所含成分多为异喹啉类生物碱,具有多种药理作用。这些异喹啉类生物碱的核磁共振化学位移具有一定特征。     

锥花黄堇中的异喹啉生物碱

锥花黄堇(Corydalis thyrsiflora Prain)系罂粟科(Papaveraceae)紫堇属(Corydalis)植物,在西藏地区以其全草入药,藏药名“抓桑”,用于镇痛。其化学成分未见文献报道。我们用离子交换树脂法从该植物全草中提出总生物碱,通过柱层析及制备薄层层析分离,得到12个化合物并鉴定了结构,均为异喹啉生物碱(见图1),分别为原阿片碱     

某些异喹啉类生物碱对大鼠脑内单胺的影响

1-四氢巴马汀(1-THP)和四氢小檗碱(THB)与dl-THP一样都能降低脑内单胺和升高酸性代谢产物DOPAC,HVA和5-HIAA。它们作用的强弱次序为dl-THP<1-THP相似文献   

异喹啉生物碱对心血管药理作用的研究与临床

<正> 异喹啉生物碱为中药黄连等植物中的主要有效成份,常用制品有小檗碱(即黄连素)和小檗胺。该类药物可用于抗菌、抗病毒、抗原虫、利胆、止血、升白细胞、治疗矽肺等。近年来发现对心血管系统具有多种作用,通过药理学实验研究,基本明确了小檗碱和小檗胺对心血管的某些作用机制,并成功地应用于临床。1 降血压作用小檗胺的降压作用国外已有报道.国内经实验证明,小檗胺与小檗碱能使多种动物(狗、猫、兔)的血压下降,其降压强     

某些异喹啉类生物碱对大鼠脑内单胺的影响

1-四氢巴马汀(1-THP)和四氢小檗碱(THB)与dl-THP一样都能降低脑内单胺和升高酸性代谢产物DOPAC,HVA和5-HIAA。它们作用的强弱次序为dl-THP<1-THP相似文献   

Synthesis and Comparative Inotropic Effects of Several Isoquinoline Alkaloids

Pharmaceutical Chemistry Journal - Compounds 3a [1-(3′,4′-methylenedioxyphenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline] and 3b...     

Immunomodulatory effect of nonsteroidal anti-inflammatory drugs (NSAIDs) at the clinically available doses

Non-steroidal anti-inflammatory drugs (NSAIDs) with cyclooxygenase (COX) inhibitory activity are commonly used in various inflammatory diseases. In this study, to examine the immunomodulatory effects of well known NSAIDs at clinically available doses, macrophage- and T cell-mediated immune responses such as tumor necrosis factor (TNF)-alpha release and nitric oxide (NO) production, cell-cell adhesion, phagocytic uptake and lymphocyte proliferation were investigated. NSAIDs tested significantly enhanced TNF-alpha release from lipopolysaccharide (LPS)-activated RAW264.7 cells at certain concentrations (fenoprofen, indomethacin, piroxicam, aceclofenac, diclofenac and sulindac) or in a dose-dependent manner (aspirin and phenylbutazone). Of NSAIDs, phenylbutazone and aspirin most potently attenuated NO production, although sulindac was the only compound with cytoprotective activity against LPS-induced cytotoxicity. Most NSAIDs used displayed weak or no modulatory effects on phagocytic uptake and CD29- or CD43-mediated cell-cell adhesion. Interestingly, however, phenylbutazone itself triggered cell-cell clustering under normal culture conditions and enhanced the phagocytic activity. Aspirin and phenylbutazone also dose-dependently attenuated CD4+ T cell proliferation stimulated by concanavalin A (Con A) and CD8+ CTLL-2 cell proliferation induced by interleukin (IL)-2. Sulindac only blocked CTLL-2 cell proliferation. These results suggest that NSAIDs may differentially exert immunomodulatory effects on activated macrophages and lymphocytes, and some of the effects may enforce NSAID's therapeutic effect against inflammatory symptoms.     

异喹啉类心血管药物研究进展

本文报道了以中草药有效成分为先导物，设计合成了111个异喹啉衍生物包括双苄基异喹啉、苄基异喹啉、原小檗碱等类型化合物，对所合成衍生物进行α-受体，腺苷A1，A2，DHP钙通道放射受体分析以及其它的心血管活性研究，发现化合物VI19具有α1－受体拮抗作用新的钾通道阻滞剂，V9和V21可降低多种动物模型的血压，而无反射性加速心律的副作用，VI13具有抗心律失常和抗室颤作用，该化合物有可能进入临床试验。本文总结了部分化合物的构效关系为进一步研究新化合物提供理论基础。     

Immunomodulatory biomaterials

Vaccination is one of the most successful medical interventions for the prevention of disease in the twentieth century. However, with the development of new and less reactogenic vaccine antigens, which take advantage of molecular recombinant technologies, comes the need for more effective adjuvants that will facilitate the induction of adaptive immune responses. In this context, immunomodulatory biomaterials, particularly the ones based on biodegradable polymers, show great promise. This article discusses the various classes of immunomodulatory biomaterials and advocates a cross-disciplinary approach that brings together molecular concepts from various fields to rationally design vaccine adjuvants with immunomodulatory properties.     

茶碱在哮喘中的免疫调节作用

目的　探讨茶碱在哮喘治疗中的免疫调节作用。方法　观察 10例哮喘患者在每天口服 40 0mg的茶碱缓释片治疗 6周后 ,其血清T淋巴细胞亚群和IgE水平的变化。 结果　茶碱能显著提高哮喘患者外周血中的CD8T淋巴细胞数 (从治疗前的 18 9%± 4 4%提高到治疗后的 2 5 8%±5 9% ,P <0 0 5 )。并有降低哮喘患者外周血中IgE水平的趋势。结论　茶碱具有免疫调节作用 ,为重新评价茶碱在哮喘治疗中的作用提供了依据。     

黄连素的临床应用研究进展

黄连素长久以来一直作为广谱抗菌药物使用,具有显著的抑菌作用,原是治疗肠炎、痢疾的经典中药。近年来发现黄连素在降糖调脂、治疗心内科疾病、肿瘤科疾病等众多方面也有重要作用。现将其在这些方面的临床应用作一综述。     

北豆根总碱对环磷酰胺模型小鼠的免疫调节作用

从非特异性免疫功能及特异性免疫功能方面研究了北豆根总碱对环磷酰胺所致的免疫功能低下模型小鼠的免疫调节作用．实验结果表明,北豆根总碱２５ｍｇ／ｋｇ、５０ｍｇ／ｋｇ腹腔注射能显著增强模型小鼠单核巨噬细胞吞噬功能、迟发型超敏反应及增加其外周血淋巴细胞ＡＮＡＥ阳性百分率;北豆根总碱２５ｍｇ／ｋｇ腹腔注射能显著提高模型鼠血清溶血素生成能力．初步机理研究表明,北豆根总碱５０ｍｇ／ｋｇ腹腔注射能显著拮抗环磷酰胺对小鼠胸腺ＤＮＡ含量的抑制作用,提示北豆根总碱可能通过促进ＤＮＡ合成而达到增强免疫功能的作用．     

Immunomodulatory activities on macrophage of a polysaccharide from Sipunculus nudus L.

A water-soluble polysaccharide, named as SNP, was extracted and fractioned from the body wall of Sipunculus nudus L. by DEAE-Sepharose anion exchange and Sepharose CL-6B column chromatography. The structural characteristics of SNP investigated by high performance size exclusion chromatography (HP-SEC), Fourier transform infrared spectroscopy (FT-IR) and gas chromatography-mass spectrometry (GC-MS) indicated that SNP was a homogeneous polysaccharide with a molecular mass of 350 kD and the monosaccharide composition was determined to be rhamnose (28%), fucose (16%) and galactose (56%). SNP was able to upregulate the expression of cytokines (IL-6 and TNF-α), but did not affect IL-10 secretion by murine macrophages and human peripheral blood mononuclear cells. RT-PCR analysis demonstrated that the SNP also induced the expression of iNOS and COX-2, responsible for the induction of NO and PGE2 respectively, and SNP suppressed the arginase activity. These results suggest that the polysaccharide isolated from S. nudus activates macrophages and has potent immunostimulating activity.