Molecular simulations probing Kushecarpin A as a new lipoxygenase inhibitor

Zizyphus oxyphylla Edgew is used in Pakistan as a folk medicinal remedy for inflammatory conditions, pains especially rheumatic pain, fevers, allergy and diabetes. The aim of the current study was to scientifically validate the folk use of Z. oxyphylla Edgew by using the isolated compound in vitro and in vivo levels. Kushecarpin A was isolated from ethyl acetate fraction of the plant crude extract. Molecular docking simulations predicted Kushecarpin A as a potential new lipoxygenase (LOX) inhibitor. Kushecarpin A showed significant lipoxygenase inhibition (IC50: 7.2 ± 0.02 μM) thus validated computational prediction. It also exhibited significant and highly significant inhibition (p < 0.05 and p < 0.01) of carrageenan-induced hind paw oedema at the doses of 5, 10 and 20 mg/kg. Kushecarpin A seems to be a potentially new anti-inflammatory compound responsible for anti-inflammatory activities of Z. oxyphylla Edgew. In vitro and in vivo anti-inflammatory inflammatory activities were found in good agreement with the folk medicinal use of Z. oxyphylla Edgew in inflammatory disorders.     

Two new benzofuran derivatives with anti-inflammatory activity from Liriope spicata var. prolifera

Two new benzofuran derivatives, 2-(4′-hydroxybenzyl)-5,6-methylenedioxy-benzofuran () and 2-(4′-hydroxybenzoyl)-5,6-methylenedioxy-benzofuran (), along with 8 known compounds were isolated from 60% EtOH extract of the fibrous roots of Liriope spicata var. prolifera. Their structures were elucidated on the basis of extensive spectroscopic analysis. In an in vitro bioactive assay, the two new benzofuran derivatives showed anti-inflammatory activity. Compounds 1 and 2 exhibited significant inhibitory activity against neutrophil respiratory burst stimulated by phorbol 12-myristate 13-acetate (PMA) with IC₅₀ value of 4.15 ± 0.07 and 5.96 ± 0.37 μM, respectively.     

复方牛山参口服液镇痛抗炎作用药化试验研究

[目的]为复方牛山参口服液的临床应用提供参考。[方法]以昆明种小白鼠为试验动物,10ml／kg生理盐水处理为空白对照,研究25ml／kg消炎痛及2．5、5．0、10、20g/kg复方牛山参口服液灌胃处理对小白鼠扭体反应和耳廓肿胀的影响,考察复方牛山参口服液镇痛抗炎作用的量效、时效关系。[结果]25ml／kg消炎痛及2．5、5．0、10、20g／kg复方牛山参口服液对小白鼠扭体次数的抑制率分别为81．73％、33．65％、38．46％、50．48％、76．73％,对小白鼠耳廓肿胀的抑制率分别为15．14％、6．23％、5．20％、18．20％、27．22％;5．0g／kg复方牛山参口服液灌胃处理0、1、2、3、6．5h后,扭体鼠发生率分别为50％、50％、10％、10％、0。[结论]复方牛山参口服液的镇痛作用较消炎痛稍差,但其对小白鼠耳廓肿胀的抑制作用优于消炎痛。     

慈姑中秋水仙碱的提取及抗炎作用研究

[目的]研究慈姑中秋水仙碱的最佳提取工艺及抗炎作用.[方法]考察乙醇浓度、提取时间、提取温度和料液比对慈姑中秋水仙碱提取率的影响,在单因素试验的基础上,采用L9(34)正交试验优化提取工艺参数.根据最佳提取工艺,采用高效液相色谱法,测定慈姑中秋水仙碱的含量.通过体外抗炎试验,来评价慈姑中秋水仙碱的抗炎能力.[结果]慈姑中秋水仙碱的最佳提取工艺条件为:乙醇浓度60％,提取温度50℃,提取时间30 min,料液比1:25 (g/ml).慈姑中秋水仙碱的含量为40.58 μ.g/100 mg.与模型对照组比较,慈姑中秋水仙碱(9.0,4.5g/kg)抑制胸腔液PGE2,TNF-α,IL-1β含量升高(P＜0.05).慈姑中秋水仙碱高剂量组能抑制肺组织TNF-α.IL-1β,MDA含量升高(P＜0.01),中剂量组抑制肺组织IL-1β含量升高(P＜0.01).[结论]慈姑中秋水仙碱具有良好的抗炎作用,抗炎机制可能与影响炎症介质产生和抗氧化作用有关.     

蒲公英提取物与狼毒素总黄酮主要药效作用研究

采用平板法、试管法测定两种蒲公英乙醇提取物与狼毒素总黄酮(TFC)对金黄色葡萄球菌、大肠杆菌、无乳链球菌体外抑制作用和最小抑菌浓度(MIC)以及最小杀菌浓度(MBC),利用二甲苯致小鼠耳廓肿胀试验、牛奶致热试验观察三者的抗炎、解热作用。结果表明,狼毒素总黄酮(TFC)与蒲公英40%乙醇提取物(40%HT)具有中度抑菌作用,且二者组合有显著的抑菌作用;狼毒素总黄酮40%乙醇提取物在500、250 mg/kg,90%乙醇提取物(90%HT)在500 mg/kg剂量下显著抑制二甲苯致小鼠耳廓的肿胀(P<0.01);狼毒素总黄酮不具有解热作用,两种蒲公英提取物均能显著抑制牛奶致热(P<0.01或P<0.05)。     

中药抗炎机理研究进展

中药对各种类型的炎症有不同程度的抑制效应,主要从调节下丘脑-垂体-肾上腺皮质轴功能,干扰花生四烯酸代谢,对炎症介质的作用,抑制白细胞趋化、移动和活化,抑制氧自由基的产生,影响细胞内第二信使以及抗血栓形成等方面抑制炎症。     

Prenylated phloroglucinol derivatives from Hypericum sampsonii

Six new acylphloroglucinol derivatives, sampsonols A-F (1–6), were isolated from the petroleum ether extract of the aerial parts of Hypericum sampsonii. The structures and relative configurations of sampsonols A-F were elucidated by extensive spectroscopic analyses. All these compounds were tested for their in vitro cytotoxic and anti-inflammatory activities. Sampsonols A and B (1 and 2) showed significant cytotoxicity against four human tumor cell lines with IC₅₀ values in the range of 13–28 μM, whereas sampsonols C and F (3 and 6) showed potent inhibitory activities against LPS-induced NO production in RAW 264.7 macrophages with IC₅₀ values of 27.3 and 29.3 μM, respectively.     

千年健镇痛抗炎药理研究

[目的]研究千年健药材水提物和醇提物的镇痛抗炎作用。[方法]采用二甲苯致小鼠耳廓肿胀模型观察千年健的抗炎作用;冰醋酸致小鼠扭体试验观察千年健的镇痛作用。[结果]与正常对照组相比,千年健水提和醇提部位的高、低剂量组能明显降低小鼠耳廓的耳肿胀度,且有显著性差异(P<0.05);千年健水提和醇提部位的高、低剂量组能明显减少0.7%冰醋酸致小鼠的扭体反应次数,且有极显著性差异(P<0.01)。[结论]千年健药材具有良好的镇痛抗炎作用。     

Non-steroidal anti-inflammatory drugs induce apoptosis in implanted hepatoma of mice

AIM: To study the mechanism of the effect of NSAIDs on apoptosis in mice hepatoma at anti-inflammatory doses. METHODS: Kunming breed mice were inoculated subcutaneously in the flank with mice hepatoma H22 cell line. The effects of ibuprofen, indomethacin, and nimesulide on apoptosis were determined by using electron microscopy, agarose gel electrophoresis, flow cytometry, and Western blot analysis of the expression of c-myc, bcl-x_L and bcl-2 proteins. RESULTS: NSAIDs induced apoptosis of mice implanted hepatoma, which includes the morphological changes such as reduction in the volume, and the nuclear chromatin condensation, as well as the "ladder pattern" revealed by agarose gel electrophoresis of DNA. The apoptotic index was increased to 15%±1.0%, 29.7%±1.5%, 46.3%±3.5% from 3.3%±0.6% by detecting Sub-G₁ peaks on flow cytometry. Western blot analysis showed that levels of bcl-2 and bcl-x_L were significantly reduced by treatment with nimesulide. Ibuprofen and indomethacin decreased bcl-2 expression but increased bcl-x_L expression. C-myc wasn't changed in these groups. CONCLUSION: These results suggest that NSAIDs induces apoptosis of mice hepatoma, which may be due to their regulation on the expressions of bcl-2 family genes.