紫甘蓝花色苷及其复合体的抗炎活性研究

为了探究紫甘蓝花色苷—3-二糖-5-D-吡喃葡糖苷矢车菊素(cyanidin-3-diglcoside-5-glcoside,Cy)及其复合体对鼠源单核-巨噬细胞RAW264.7的抗炎活性,首先采用紫甘蓝花色苷碱水解产物中的Cy为原料,模拟天然蓝花中结构相对稳定的花色苷复合体存在形式,与芦丁(rutin)及2种不同金属离子(Mg~(2+)和Fe~(3+))构建5种Cy复合体;然后通过建立脂多糖(LPS)诱导的鼠源单核-巨噬细胞RAW264.7炎症模型,评价Cy复合体构建前后对Cy抗炎活性的影响。结果表明,Cy可以显著性抑制RAW264.7细胞上清液中NO释放及细胞内炎症相关基因iNOS、IL-1β、IL-6和TNF-α的mRNA的表达(P0.05)。在构建的复合体中,与Cy相比,Cy-Fe~(3+)、Cy-rutin-Fe~(3+)、Cy-Mg~(2+)和Cy-rutin-Mg~(2+)复合体的抗炎活性均显著提高(P0.05)。其中,Cy-Mg~(2+)和Cy-rutinMg~(2+)复合体的抗炎活性高于Cy-Fe~(3+)和Cy-rutin-Fe~(3+)复合体,而Cy-Mg~(2+)复合体的抗炎活性最强。由这些结果可以得出Cy及其复合体均具有显著的抗炎活性,且Cy复合体的抗炎活性高于Cy。Cy复合体有望开发成为一种新型食品添加剂,辅助干预炎症反应及其引起的相关疾病。     

中药生物碱的提取及抗炎作用研究

为探讨自拟中药复方"宫炎净"总生物碱、简化复方总生物碱以及益母草生物碱对小鼠的抗炎作用,将实验小鼠分为生理盐水、地塞米松、复方"宫炎净"总生物碱、简化复方总生物碱以及益母草生物碱组,依据建立小鼠耳廓肿胀、腹腔毛细血管通透性、足趾肿胀以及肉芽肿炎症模型来评估各组药物的抗炎效果。结果表明,复方"宫炎净"总生物碱组与简化复方总生物碱能够显著抑制二甲苯所致小鼠耳廓肿胀率、降低小鼠腹腔毛细血管通透性、抑制蛋清所致小鼠足趾肿胀率、降低棉球所致小鼠肉芽组织增生,均与益母草生物碱组差异显著(P0.05),并与地塞米松组差异不显著(P0.05)。结果显示,复方"宫炎净"总生物碱组与简化复方总生物碱抗炎效果相差不大,简化复方可作为临床用药组方使用。     

抗菌消炎胶囊中知母薄层鉴别方法的改进

[目的]改进抗菌消炎胶囊中知母的薄层鉴别方法。[方法]以知母阴性、菝葜皂苷元为对照品,采用不同展开溶剂系统进行薄层色谱鉴别。[结果]改进后方法薄层色谱斑点清晰,重现性好,专属性好,阴性对照无干扰。[结论]改进后的方法快捷简便、重复性好、毒性小,可作为抗菌消炎胶囊中知母的鉴别方法。     

Topical anti-inflammatory plant species: Bioactivity of Bryonia dioica, Tamus communis and Lonicera periclymenum fruits

The practice of rubbing different plant material juices or extracts into the skin to relieve pain and rheumatic symptoms is deeply rooted in folk medicine and has been used for a long time. Several common species, usually available in agroecosystems of the Iberian Peninsula, were/are used for topical medicinal preparations as reported in recent ethnobotanical surveys. Based on these studies, the fruits of three relevant species (Bryonia dioica or white-bryony, Lonicera periclymenum or common honeysuckle and Tamus communis or black-bryony) were gathered and different analyses and assays were performed in order to characterize their phytochemical composition and to find biologically active compounds for pharmaceutical application. Black-bryony ripened fruits revealed the highest antioxidant properties which are in agreement to its highest concentration in phenolics, flavonoids, ascorbic acid, tocopherols and lycopene. The studied fruits revealed interesting antioxidant properties and bioactive phytochemicals that could provide scientific evidence for their folk uses as anti-inflammatory species.     

Chlamydia trachomatis evokes a relative anti-inflammatory response in a free Ca dependent manner in human macrophages

Chlamydia trachomatis infections manifest as unique, chronic inflammatory diseases, indicating a relative compromise in the capacity of early immune responders such as macrophages to resolve the infection. We decided to investigate whether or not the chronic inflammatory manifestations are influenced by a disturbance in the pattern of inflammatory:anti-inflammatory cytokine elaboration early in the infection cycle in macrophages and assess the possible modulatory role of Ca²⁺ signals in the process. Although the basal and functional levels of IL-12 and IL-10 are not identical in concentration, chlamydia initiated a significant decline in IL-12. This led to a difference in the ratio of time-course decline in IL-12 compared with IL-10 in a Ca²⁺-poor medium, while there was significant increase in IL-10 in a Ca²⁺-rich medium. Also, when macrophages were infected after treatment with drugs that either facilitated Ca²⁺ influx into cells or inhibited efflux from intracellular stores into cytosol, there was a significant enhancement of the elaboration of IL-10 compared with IL-12. The immobilization of cytosolic Ca²⁺ by BAPTA-AM resulted in the decline of macrophage IL-12 and IL-10 in both infected and uninfected cases. There was evidence that infectivity and status of chlamydial elementary bodies harvested from macrophages during these experiments were consistent with chronic forms as assessed by HSP-60:MOMP ratio. The implication of these findings is that chlamydia infection of macrophages, together with its capacity to moderate macrophage intracellular Ca²⁺ levels, may evoke a net anti-inflammatory response that presumably favors chronic chlamydia infections.     

Anti-Inflammatory and Analgesic Effects of the Marine-Derived Compound Excavatolide B Isolated from the Culture-Type Formosan Gorgonian Briareum excavatum

In recent years, several marine-derived compounds have been clinically evaluated. Diterpenes are secondary metabolites from soft coral that exhibit anti-inflammatory, anti-tumor and cytotoxic activities. In the present study, we isolated a natural diterpene product, excavatolide B, from cultured Formosan gorgonian Briareum excavatum and investigated its anti-inflammatory activities. We found that excavatolide B significantly inhibited the mRNA expression of the proinflammatory mediators, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), in lipopolysaccharide (LPS)-challenged murine macrophages (RAW 264.7). We also examined the anti-inflammatory and anti-nociceptive effects of excavatolide B on intraplantar carrageenan-induced inflammatory responses. Excavatolide B was found to significantly attenuate carrageenan-induced nociceptive behaviors, mechanical allodynia, thermal hyperalgesia, weight bearing deficits and paw edema. In addition, excavatolide B inhibited iNOS, as well as the infiltration of immune cells in carrageenan-induced inflammatory paw tissue.     

Bioactive Steroids from the Formosan Soft Coral Umbellulifera petasites

Three new steroids, petasitosterones A and B (1 and 2) and a spirosteroid petasitosterone C (3), along with eight known steroids (4–11), were isolated from a Formosan marine soft coral Umbellulifera petasites. The structures of these compounds were elucidated by extensive spectroscopic analysis and comparison of spectroscopic data with those reported. Compound 3 is a marine steroid with a rarely found A/B spiro[4,5]decane ring system. Compounds 1–3 and 5 displayed inhibitory activity against the proliferation of a limited panel of cancer cell lines, whereas 2 and 5 exhibited significant anti-inflammatory activity to inhibit nitric oxide (NO) production. The inhibitory activities for superoxide anion generation and elastase release of compounds 1–11 were also examined to evaluate the anti-inflammatory potential, and 2–4 were shown to exhibit significant activities.     

Anti-Inflammatory Activity of Tanzawaic Acid Derivatives from a Marine-Derived Fungus Penicillium steckii 108YD142

Chemical investigation of a marine-derived fungus, Penicillium steckii 108YD142, resulted in the discovery of a new tanzawaic acid derivative, tanzawaic acid Q (1), together with four known analogues, tanzawaic acids A (2), C (3), D (4), and K (5). The structures of tanzawaic acid derivatives 1–5 were determined by the detailed analysis of 1D, 2D NMR and LC-MS data, along with chemical methods and literature data analysis. These compounds significantly inhibited nitric oxide (NO) production and the new tanzawaic acid Q (1) inhibited the lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins and mRNA expressions in RAW 264.7 macrophages. Additionally, compound 1 reduced the mRNA levels of inflammatory cytokines. Taken together, the results of this study demonstrated that the new tanzawaic acid derivative inhibits LPS-induced inflammation. This is the first report on the anti-inflammatory activity of tanzawaic acid Q (1).     

岗梅根醇提物抗炎活性的实验研究

为了研究岗梅根醇提物的抗炎活性,采用二甲苯致小鼠耳廓肿胀法、鸡蛋清致大鼠足跖肿胀法、大鼠棉球肉芽肿法和醋酸致小鼠毛细血管通透性增高法观察岗梅根醇提物的抗炎作用。结果表明,岗梅根醇提物对炎症早期的渗出和后期结缔组织增生均有较明显的抑制作用(P0.05)。结论:岗梅根醇提物具有显著的抗炎活性。