外用中药止血散的药效学研究

为探讨自制外用中药止血散(简称止血散)的止血和抗炎作用,通过小鼠断尾模型、药物吸附及粘稠性试验、二甲苯致小鼠耳廓肿胀试验及抑菌试验对其药效学进行评价,通过大鼠皮肤刺激性试验和豚鼠皮肤过敏性试验考察其安全性。结果表明,自制中药止血散对大鼠完整皮肤和破损皮肤均无刺激性,对豚鼠皮肤无致敏性。在止血时间方面,止血散组和云南白药对照组较空白对照组明显缩短(P0.01),止血散组与云南白药组无显著差异(P0.05);在血液吸附能力及粘稠性方面,止血散显著好于云南白药(P0.01);二甲苯致小鼠耳肿胀试验中,止血散组与红霉素软膏组小鼠耳肿胀度均显著低于模型组(P0.01),止血散组与红霉素软膏组无显著性差异(P0.05);止血散对大肠杆菌和金黄色葡萄球菌的最小抑菌浓度(MIC)均为5 g·L~(-1),对枯草芽孢杆菌的MIC为10 g·L~(-1)。     

Anti-Inflammatory Polyketide Derivatives from the Sponge-Derived Fungus Pestalotiopsis sp. SWMU-WZ04-2

Five undescribed polyketide derivatives, pestaloketides A–E (1–5), along with eleven known analogues (6–16), were isolated from the sponge-derived fungus Pestalotiopsis sp. Their structures, including absolute configurations, were elucidated by analyses of NMR spectroscopic HRESIMS data and electronic circular dichroism (ECD) calculations. Compounds 5, 6, 9, and 14 exhibited weak cytotoxicities against four human cancer cell lines, with IC₅₀ values ranging from 22.1 to 100 μM. Pestaloketide A (1) is an unusual polyketide, featuring a rare 5/10/5-fused ring system. Pestaloketides A (1) and B (2) exhibited moderately inhibited LPS-induced NO production activity, with IC₅₀ values of 23.6 and 14.5 μM, respectively, without cytotoxicity observed. Preliminary bioactivity evaluations and molecular docking analysis indicated that pestaloketides A (1) and B (2) had the potential to be developed into anti-inflammatory activity drug leads.     

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.