雷公藤中萜类成分药理作用的分子机制研究进展

雷公藤所含萜类单体,如雷公藤甲素、雷公藤氯内酯醇、雷公藤内酯酮、南蛇藤素、扁蒴藤素具有独特的药理学作用,近年来国内外学者对上述五种萜类成分在炎症及免疫反应、神经系统、心血管系统、呼吸系统和肿瘤抑制等方面的药理学作用进行了广泛深入的研究。本研究对上述五种萜类成分的药理作用及分子机制进行了综述。     

青藤碱及其新剂型治疗类风湿性关节炎的研究进展

类风湿性关节炎是一种长期性、顽固性、致残性的自身免疫性疾病。目前,临床上治疗类风湿性关节炎的药物主要包括非甾体类抗炎药、糖皮质激素、免疫调节剂等,但长期使用易产生恶心、胃肠道不适、肝损伤等不良反应。青藤碱是源于青风藤中的一种有效成分,具有镇痛、抗炎、抗菌、降血压等药理作用,临床可用来治疗类风湿性关节炎等疾病。目前,青藤碱尚存在半衰期短、生物利用度低、给药剂量大等不足之处,青藤碱新剂型的开发有望为类风湿性关节炎的治疗提供新的思路。基于近年来青藤碱的研究进展,对青藤碱治疗类风湿性关节炎的基本性质、临床应用、药理作用和新剂型研究进行了综述,为青藤碱新剂型开发及临床应用提供参考。     

Anti-inflammatory activities of Chinese herbal medicine sinomenine and Liang Miao San on tumor necrosis factor-α-activated human fibroblast-like synoviocytes in rheumatoid arthritis

Aim of the study

Sinomenine, an alkaloid isolated from the root of Sinomenium acutum, has been used to alleviate the symptoms of rheumatic diseases. Liang Miao San (LMS), composed of the herbs Rhizoma Atractylodis (Cangzhu) and Cotex Phellodendri (Huangbai), is another traditional Chinese medicine formula for rheumatoid arthritis (RA) treatment. Although numerous studies have demonstrated the potential anti-inflammatory activities of sinomenine and LMS, the underlying intracellular mechanisms regulating the anti-inflammatory activities of sinomenine and LMS on human primary fibroblast-like synoviocytes (FLS) from RA patients and normal control subjects have not been elucidated.

Materials and methods

We investigated the in vitro anti-inflammatory activity of sinomenine and LMS on inflammatory cytokine tumor necrosis factor (TNF)-α-mediated activation of human normal and RA-FLS. The underlying intracellular signaling molecules were analyzed quantitatively using flow cytometry.

Results

Sinomenine was found to significantly inhibit TNF-α induced cell surface expression of vascular cell adhesion molecule (VCAM)-1 and release of inflammatory cytokine and chemokine IL-6, CCL2 and CXCL8 from both normal and RA-FLS (all p < 0.05). Moreover, the suppression of sinomenine on TNF-α induced VCAM-1 expression and IL-6 release of RA-FLS was significantly higher than that of normal FLS (p < 0.05). LMS significantly inhibited TNF-α-induced inflammatory chemokines CXCL10 and CCL5 release from both normal and RA-FLS, with significantly higher suppression on CXCL10 secretion in RA-FLS than that of normal FLS (all p < 0.05). Further investigations showed that sinomenine and LMS could significantly suppress TNF-α-induced phosphorylation of inhibitor κBα and extracellular signal-regulated protein kinase, the central signaling molecules mediating TNF-α-induced VCAM-1 expression and chemokine production.

Conclusion

Our results therefore provide a new insight into the differential anti-inflammatory activities of sinomenine and LMS through the suppression of TNF-α-activated FLS by modulating distinct intracellular signaling pathways in RA.     

青藤碱研究新进展

查阅近10年来有关青藤碱的国内外文献资料,选取具有较大应用价值及学术意义的内容,从青藤碱的提取工艺、含量测定、药物化学研究、药理、毒理、药动学、临床应用等方面分别介绍,拟对青藤碱有进一步的认识。青藤碱是一种抗炎止痛效果好、副作用小的非甾体抗炎止痛药,并以期成为一种良好的戒毒药。     

Immunomodulatory effects and structure-activity relationship of botanical pentacyclic triterpenes: A review

Botanical pentacyclic triterpenes possessed a broad range of pharmacological activities such as antioxidant, anti-tumor, anti-microbial and anti-inflammatory activities. It is believed that the mechanisms involved in these bioactivities are due to the modulation of immune system. Recently, the pharmacological validation on immunomodulatory of pentacyclic triterpenes derived from higher plants is very limited and several existence review papers related for this group of compound have not been focused for this activity. In this review, we have highlighted several studies on immunomodulatory potential of botanical pentacyclic triterpenes isolated from wide array of different species of medicinal plants and herbs based on various preclinical in vitro and animal models. This review also attempts to discuss on bioactivities of compouns related with their structure-activity relationship. Hence, the evaluation of pentacyclic triterpenes offers a great opportunity to discover adjuvants and novel therapeutic agents that presented beneficial immunomodulatory properties.     

白术的化学成分与药理作用及复方临床应用进展

白术作为一味传统中药,在历代本草著作中广泛记载,其功效有一定演变。现代研究发现,其主要化学成分有挥发油、多糖、内酯类等,具有抗肿瘤、抗炎、调节消化系统等药理作用。临床以中药复方的形式应用于胃肠道疾病、心血管疾病、免疫系统疾病、肝脏疾病等治疗。对近5年SCI收录的白术相关文章进行分析,简述其化学成分,重点围绕着药理作用以及复方的临床应用展开论述,为其进一步开发利用提供参考。     

Mechanism of electroacupuncture on inflammatory pain: neural-immune-endocrine interactions

Nociceptive signals are transmitted by peripheral afferents to the central nervous system under pain condition, a process that involves various neurotransmitters and pathways.Electroacupuncture(EA) has been widely used as a pain management technique in clinical practice.Emerging studies have shown that EA can inhibit the induction and transmission of pain signals and, consequently, mediate anti-nociceptive and anti-inflammatory effects by rebalancing the neural-immune-endocrine interactions.This review summarizes the neural-immune-endocrine circuit including peripheral afferent and central efferent, contributing to EA-induced neuroimmune and neuroendocrine modulation in inflammatory pain models.The peripheral afferent circuit includes crosstalk among immune cells, inflammatory cytokines, peripheral nociceptors.In central efferent primarily involves the neuroinflammatory interactions between spinal nociceptive neurons and glial cells.Furthermore, the hypothalamic-pituitary-adrenal axis, sympathetic and vagal nervous may serve as an essential pathway involved in the mechanism of acupuncture-mediated analgesia within the interactions of the central, immune and endocrine systems.Overall, this review focuses on the interactions of neural-immune-endocrine in inflammatory pain, which may be underlying the mechanism of EA-induced anti-inflammatory and antinociceptive effect.     

Targeting immunometabolism by active ingredients derived from traditional Chinese medicines for treatment of rheumatoid arthritis

Rheumatoid arthritis (RA), the most common inflammatory arthropathy word wild, is a systemic autoimmune disease that mainly affects the synovium of joints with a high disability rate. Metabolic mis-regulation has emerged as a fundamental pathogenesis of RA linked to immune cell dysfunction, while targeting immunometabolism provides a new and effective approach to regulate the immune responses and thus alleviate the symptom of RA. Recently, natural active compounds from traditional Chinese medicines (TCMs) have potential therapeutic effects on RA and regulating immunometabolism. In this review, in addition to updating the connection between cellular metabolism and cell function in immune cells of RA, we summarized that the anti-inflammatory mechanisms of the potential natural compounds from TCM by targeting metabolic reprogramming of immune cells, and discusses them as a rich resource for providing the new potential paradigm for the treatment of RA.     

灵芝多糖在糖尿病及其并发症防治中的研究进展

糖尿病是一种血糖水平异常增高的内分泌系统疾病,糖尿病及其并发症的流行已经对全球健康构成了重大威胁.灵芝Ganoderma是我国珍贵的传统中药材,而灵芝多糖是灵芝的主要有效成分之一,具有多种药理作用,包括抗肿瘤、提高免疫、抗肥胖及降血糖等.就灵芝多糖对糖尿病的作用及分子机制,重点是灵芝多糖对改善糖尿病并发症的研究进展进行...     

云实属植物化学成分及药理作用研究进展

查阅文献,对云实属植物的化学成分进行系统归纳总结,并对其药理作用进行了详细介绍。该属植物中主要含有高异黄酮类、查尔酮类和萜类等化学成分,药理作用有抑制黑色素生成、抗炎、抗氧化、抗菌和免疫调节等,为该属植物的进一步研究提供参考。     

枸杞多糖的神经保护作用机制研究进展

枸杞多糖是从茄科枸杞属植物宁夏枸杞的果实中提取分离得到的多糖类化合物,是枸杞中的主要有效成分之一,具有增强免疫、抗氧化、抗衰老、抗肿瘤、保护视网膜、保护肝脏、保护神经系统、降血糖降血脂等多种药理作用。目前,枸杞多糖在临床上广泛用于多种疾病的治疗,包括肿瘤及免疫类疾病,高血压高血脂,急性肝损伤,脑缺血及脑中风等。尤其对于阿尔茨海默症,脑缺血等神经系统疾病的治疗具有显著的临床疗效,使枸杞多糖在中枢神经系统方面的应用受到越来越多的重视。近年来,有关枸杞多糖保护神经系统的研究成果不断涌现,为了推进枸杞多糖在防治中枢神经系统疾病方面的作用机制研究,本文结合国内外最新报道,对近年来枸杞多糖发挥神经保护作用的途径进行系统总结和陈述,主要包括改善神经退行性病变、视神经保护、抑制氧化应激、抑制细胞凋亡、抑制炎症反应、降低谷氨酸毒性作用、抑制神经细胞非正常分化等几个方面。虽然枸杞多糖保护神经系统的作用机制主要涉及以上几种途径,但对于枸杞多糖神经保护作用机制的某些部分研究不够深入,枸杞多糖的神经保护作用机制仍然非常复杂,需从现代分子生物学和基因分析技术入手,为枸杞多糖对神经系统保护作用的深入研究提供依据和思路。     

中药有机酸类成分的药理作用及在心血管疾病的应用

对中药有机酸类成分的药理作用及在心血管疾病的应用进行综述.查阅国内外相关文献并对其进行分析.中药有机酸类成分药理作用广泛,如抗炎症反应,抑制血小板聚集、抗血栓,抗氧化,诱导肿瘤细胞凋亡等,其中抗炎症反应,抑制血小板聚集、抗血栓,抗氧化的药理作用可能对心血管系统疾病具有潜在的临床应用价值.重视中药有机酸类成分在心血管系统疾病中的科学研究,对于中药作用药效物质基础的阐明有重要意义,同时也为心血管疾病的防治提供了新的思路.     

马鞭草化学成分及药理作用研究进展

马鞭草含有黄酮类、环烯醚萜类、苯乙醇苷类、三萜类、甾醇类、挥发油类等多种成分,药理活性和临床应用广泛,具有较好的抗肿瘤、抗炎镇痛、抗早孕、抗真菌、抗氧化等作用,且在调节免疫功能和神经保护方面亦有潜在优势。临床多用于治疗皮肤疾病、各种炎症和泌尿系统疾病,可获得良好疗效。然而,目前关于马鞭草的研究多处于基础研究阶段,对于马鞭草的提取物和活性单体的研究资料还比较少,尤其是其发挥药理作用的信号通路和分子机制尚不明确,在药理学、药动学及临床应用等方面还有待进一步深入探讨。     

青藤碱对家兔 C-BSA 肾炎模型影响的实验研究

目的：研究青藤碱对慢性肾炎的药理作用。方法：采用C－BSA复制家兔膜性肾小球炎模型,用青藤碱进行实验性治疗。结果：青藤碱能使模型动物尿蛋白、血Cr与BUN、徨环免疫复合物（CIC）、及血与尿中的β2微球蛋白（β2－MG）均明显降低。用青藤碱治疗的动物,肾小球平均直径和肾小球内细胞数低于模型组。结论：青藤碱在减轻肾小球免疫性炎症、改善肾功能方面有较好的作用。     

羟基酪醇的药理作用和药代动力学研究进展

羟基酪醇(HT)是以酯类形式广泛存在于木犀科植物油橄榄的枝叶和果实中的多酚类化合物,是天然的抗氧化剂之一。近年来,大量研究发现,HT在代谢综合征、心血管疾病、神经退行性疾病等方面均有较好的活性,能够有效抗癌、抗炎、抗抑郁等;此外,HT属于亲水亲油性物质,具有较高的生物利用度和细胞毒性小的特点,能够快速分布于各组织器官且易透过血脑屏障。因此,研究人员将其视为新药开发的重点研究对象;但该药物在体内半衰期短,靶向性差,临床应用往往受到限制,仍需更深入的研究。笔者查阅了近年来国内外有关HT的报道,并对其基本性质、药理作用及作用机制、药代动力学进行归纳总结,着重介绍了HT的抗氧化应激损伤、缓解心血管疾病、抑制神经退行性疾病等的药理活性及作用机制,并对其抗炎、抗肿瘤、抗抑郁等生物活性以及体内药代动力学的现有研究进行简要综述,同时对其未来研究方向提出建议,以期为HT的进一步开发、研究和临床应用提供参考。     

黄酮类化合物的构效关系及其在肺部炎症疾病中的应用

黄酮类化合物是自然界中存在的多酚类物质,根据化学结构可分为黄酮、二氢黄酮、黄酮醇、二氢黄酮醇、异黄酮、二氢异黄酮、黄烷-3-醇、花色素和查耳酮等类,且不同化学结构的黄酮类化合物多具有不同的生物活性。众多研究表明,黄酮类化合物具有抗氧化、抗突变、抗肿瘤、抗炎、抗菌、抗病毒和调节免疫等药理作用,其中抗炎和抗氧化特性使其成为预防和治疗肺部炎症疾病的潜在药物。重点综述了黄酮类化合物在肺部炎症疾病中的应用,并探讨了其抗炎和抗氧化特性的构效关系,以期为黄酮类化合物的开发利用提供参考。     

金莲花治疗鼻黏膜炎性疾病研究概况

金莲花的药理作用包括:抗菌、抗病毒、抗炎、解热镇痛、抗氧化等.目前研究证实,金莲花可以调节呼吸道黏膜免疫状态,增加机体的抗感染能力、改善炎症状态、促进炎症恢复.但还存在以下问题,金莲花药效成分种类较多,其治疗鼻黏膜炎性疾病的作用机制和靶点仍不明确,且缺乏多中心、大样本的临床研究.今后,应开展多中心、大样本的临床研究,为...     

白头翁汤化学成分及药理作用研究进展

综述白头翁汤化学成分、药理作用研究进展。白头翁汤的化学成分主要有生物碱类、香豆素类、皂苷类、柠檬苦素类等,具有抗炎、抗菌、免疫调节、抗肿瘤等药理作用。     

茯苓化学成分、药理作用及质量控制研究进展

中药材茯苓是真菌茯苓[Poria cocos(Schw)Wolf]的干燥菌核,来源于多孔菌科,是药食两用类中药,其有效成分和药理作用较多,现已在临床应用广泛。现对茯苓的化学成分、药理作用以及质量控制研究进行综述。发现茯苓主要化学成分为三萜类、二萜类、甾醇类、多糖类以及其他类化合物,其中研究最多的是三萜和多糖类化合物。茯苓的药理作用体现在机体多个方面,主要集中于泌尿系统、消化系统、中枢神经、免疫系统等,具有利尿、抗炎、镇静催眠、抗衰老等多种药理作用。质量控制方面,大部分文献报道主要集中于茯苓的指纹图谱和含量测定研究。     

百可利在帕金森病中的神经保护作用机制研究进展

百可利(baicalein)是一种重要的黄酮类化合物,主要存在于黄芩的根中。研究表明,百可利在帕金森病的细胞模型和动物模型中具有神经保护作用,其能够抑制α-synuclein蛋白聚集、抗炎作用、调控Nrf2/ARE抗氧化防御体系、抑制铁损伤和抑制脂氧合酶。百可利可作为治疗帕金森病的潜在药物,笔者就百可利在帕金森病中的神经保护作用及其分子机制进行了综述。