中兽药复方“连藤”的抗炎作用及安全性评价

试验选择中草药连翘、青风藤等配伍组成复方制剂“连藤”,采用水煎醇提法提取该复方制刑有效成分,通过急性毒性试验、最大耐受量试验、异常毒性试验对复方“连藤”的安全性进行评价,经二甲苯致小鼠耳廓肿胀试验检测复方“连藤”的抗炎作用。结果表明,复方“连藤”为实际无毒,其最大耐受量为18g／（kg·bw）;在体内抗炎试验中,复方“连藤”的高[10．0g／（kg·bw）]、中[5．0g／（kg·bw）]剂量组的肿胀抑制作用明显高于阳性对照（地塞米松）组。复方“连藤”安全、无毒且有良好的抗炎作用,具有开发潜力。     

穿心莲抗炎作用的药物动力学研究

采用药理效应方法,选择大鼠炎症模型对穿心莲进行了药物动力学探讨.结果表明:其体存生物相当药量的表观药动学过程符合二室模型,其Ka=0.734 h-1,K10=0.030 h-1,t1/2(Ka)=0.944 h,t1/2(α)=0.956 h,t1/2(β)=24.869 h,AUC=95.001 g·h/ml.     

Regulating autonomic nerve system: a new field of anti-inflammatory therapy for cardiovascular diseases

The role of chronic inflammation and autonomic neuropathy in the crucial underlying process contributing to the initiation and the progression of various cardiovascular diseases is well established. It is well known that the immune system is innervated by the autonomic nervous system, and the inflammatory reaction and immune reaction are re-gulated by the autonomic nerve system. Vagus nerve depresses inflammatory reaction via cholinergic anti-inflammatory pathway(CAP), while sympathetic nervous system has bidirectional regulation of pro-inflammation and anti-inflammation, which are affected by several factors such as the concentration of neurotransmitters or types of receptors. In this paper, we reviewed different effects of CAP and sympathetic nervous system on cardiovascular inflammatory reaction. Activation of CAP and regaining normal sympathetic function will improve the chronic inflammation in the process of cardiovascular diseases. Low-toxic and selective α7nAchR agonist is expected to be applied in cardiovascular diseases to alleviate chronic inflammation.     

Non-steroidal anti-inflammatory drugs in equine orthopaedics

Orthopaedic disorders are commonly encountered in equine veterinary medicine, and non-steroidal anti-inflammatory drugs (NSAIDs) play an important role in the management of many equine orthopaedic disorders. There are multiple NSAIDs available for use in horses, including both non-selective and selective NSAIDS, and the body of literature evaluating the efficacy of these medications, their effects on normal and inflamed musculoskeletal tissues, and their side effects is broad. This review aims to summarise the current literature on the use of NSAIDs for equine orthopaedic disorders and examines new and future avenues for the management of inflammation in equine orthopaedics.     

New Briarane Diterpenoids from Taiwanese Soft Coral Briareum violacea

Ten new briarane diterpenoids, briaviolides A–J (1–10), together with six known briaranes, solenolides A and D, excavatolide A, briaexcavatolide I, 4β-acetoxy-9-deacetystylatulide lactone and 9-deacetylstylatulide lactone, were isolated from the Taiwanese soft coral, Briareum violacea. Their structures were determined on the basis of spectroscopic data (¹H- and ¹³C-NMR, ¹H–¹H COSY, HSQC, HMBC and NOESY), HR-MS and chemical methods. The absolute configuration of briaviolide A (1) was determined by X-ray crystallographic analysis. Compounds 5, 9 and derivative 11 showed moderate inhibitory activities on superoxide-anion generation and elastase release by human neutrophils in response to N-formyl-methionyl-leucyl-phenylalanine/Cytochalasin B (fMLP/CB).     

Four New Briarane Diterpenoids from Taiwanese Gorgonian Junceella fragilis

Four new 8-hydroxybriarane diterpenoids, frajunolides P–S (1–4), together with umbraculolide A, juncenolide C, junceellonoid A and juncin R, were isolated from the acetone extract of the gorgonian Junceella fragilis, collected from the southeast coast of Taiwan. Compound 1 contains an unusual pivaloyloxy group at C-2, while 3 is a rare compound having a chlorine atom on the olefinic carbon (C-6). The structures of the isolated compounds were established by extensive spectroscopic analysis, including 1D- and 2D-NMR, as well as HRMS data. Compound 1 was further confirmed by X-ray crystallographic analysis. In the anti-inflammatory test, compounds 1 and 2 exhibited moderate inhibition on superoxide anion generation and elastase release by human neutrophils in response to formylmethionylleucyl-phenylalanine/dihydrocytochalasin B (fMLP/CB).     

五谷虫粗提物的抗炎效果及对小鼠免疫调节的影响

为探讨五谷虫粗提物对急性炎症的抑制效果以及对机体免疫机能的影响,利用耳肿胀法判断五谷虫粗提物对小鼠的抗炎效果,通过免疫器官指数、血清部分生化指标、血清溶血素含量及碳廓清指数的测定来考察五谷虫粗提物对小鼠免疫功能的影响。结果表明：五谷虫粗提物能够明显降低小鼠的耳肿胀程度,显著提高小鼠脾和胸腺指数,能够提高血清中球蛋白的含量,同样能够显著提高小鼠半数溶血值及吞噬指数。由此可以推断,五谷虫粗提物有抗炎作用,且能够提高小鼠的免疫功能。     

Anti-Inflammatory and Analgesic Effects of TRPV1 Polypeptide Modulator APHC3 in Models of Osteo- and Rheumatoid Arthritis

Arthritis is a widespread inflammatory disease associated with progressive articular surface degradation, ongoing pain, and hyperalgesia causing the development of functional limitations and disability. TRPV1 channel is one of the high-potential targets for the treatment of inflammatory diseases. Polypeptide APHC3 from sea anemone Heteractis crispa is a mode-selective TRPV1 antagonist that causes mild hypothermia and shows significant anti-inflammatory and analgesic activity in different models of pain. We evaluated the anti-inflammatory properties of APHC3 in models of monosodium iodoacetate (MIA)-induced osteoarthritis and complete Freund’s adjuvant (CFA)-induced rheumatoid monoarthritis in comparison with commonly used non-steroidal anti-inflammatory drugs (NSAIDs) such as diclofenac, ibuprofen, and meloxicam. Subcutaneous administration of APHC3 (0.1 mg/kg) significantly reversed joint swelling, disability, grip strength impairment, and thermal and mechanical hypersensitivity. The effect of APHC3 was equal to or better than that of reference NSAIDs. Protracted treatment with APHC3 decreased IL-1b concentration in synovial fluid, reduced inflammatory changes in joints, and prevented the progression of cartilage degradation. Therefore, polypeptide APHC3 has the potential to be an analgesic and anti-inflammatory substance for the alleviation of arthritis symptoms.     

Bioactive Lipids of Marine Microalga Chlorococcum sp. SABC 012504 with Anti-Inflammatory and Anti-Thrombotic Activities

Microalgae are at the start of the food chain, and many are known producers of a significant amount of lipids with essential fatty acids. However, the bioactivity of microalgal lipids for anti-inflammatory and antithrombotic activities have rarely been investigated. Therefore, for a sustainable source of the above bioactive lipids, the present study was undertaken. The total lipids of microalga Chlorococcum sp., isolated from the Irish coast, were fractionated into neutral-, glyco-, and phospho-lipids, and were tested in vitro for their anti-inflammatory and antithrombotic activities. All tested lipid fractions showed strong anti-platelet-activating factor (PAF) and antithrombin activities in human platelets (half maximal inhibitory concentration (IC₅₀) values ranging ~25–200 μg of lipid) with the highest activities in glyco- and phospho-lipid fractions. The structural analysis of the bioactive lipid fraction-2 revealed the presence of specific sulfoquinovosyl diacylglycerols (SQDG) bioactive molecules and the HexCer-t36:2 (t18:1/18:1 and 18:2/18:0) cerebrosides with a phytosphingosine (4-hydrosphinganine) base, while fraction-3 contained bioactive phosphatidylcholine (PC) and phosphatidylethanolamine (PE) molecules. These novel bioactive lipids of Chlorococcum sp. with putative health benefits may indicate that marine microalgae can be a sustainable alternative source for bioactive lipids production for food supplements and nutraceutical applications. However, further studies are required towards the commercial technology pathways development and biosafety analysis for the use of the microalga.