Anti-inflammatory and related pharmacological activities of cultured mycelia and fruiting bodies of Cordyceps militaris

This study aimed to elucidate pharmacological activities of Cordyceps militaris. The 70% ethanolic extracts of cultured mycelia (CME) and fruiting bodies (FBE) of Cordyceps militaris were prepared. CME was able to directly scavenge the stable free radical diphenyl-2-picrylhydrazyl (DPPH), indicating its antioxidant activity. Both CME and FBE showed topical anti-inflammatory activity in the croton oil-induced ear edema in mice. CME was found to contain acute anti-inflammatory activity, which was evaluated using the carrageenin-induced edema, and also strong antinociceptive activity in writhing test. CME and FBE contain potent inhibitory activity on the chick embryo chorioallantoic membrane (CAM) angiogenesis in a dose-dependent manner. Cordycepin, a metabolite of Cordyceps militaris, appeared to be at least partly responsible for its anti-inflammatory and anti-angiogenic activities. CME concentration-dependently inhibited the NO production and iNOS expression upon stimulation by lipoposaccharide in RAW 264.7, a murine macrophage cell line. In brief, we demontrate that Cordyceps militaris possesses anti-inflammatory and antinociceptive activites, and related antioxidant, anti-angiogenic, and NO production-inhibitory activities.     

Heme oxygenase-1 mediates the anti-inflammatory effect of mushroom Phellinus linteus in LPS-stimulated RAW264.7 macrophages

This work aimed to elucidate the anti-inflammatory mechanism of the n-BuOH subfraction (PL) prepared from fruiting bodies of Phellinus linteus. PL induced heme oxygenase-1 (HO-1) of the RAW264.7 macrophages in concentration- and time-dependent manner. It suppressed induction of inducible nitric oxide synthase (iNOS) and subsequent production of nitric oxide (NO) through down-regulation of iNOS promoter activity in lipopolysaccharide (LPS)-stimulated macrophages. Zn(II) protoporphyrin IX (ZnPP), a specific inhibitor of HO-1, partly blocked suppression by PL on iNOS promoter activity and NO production, which were elevated in LPS-stimulated macrophages. LPS was able to enhance NO production via reactive oxygen species (ROS) generation, c-Jun NH(2)-terminal kinase (JNK) and c-Jun induction. ZnPP prevented PL from down-regulating ROS generation and JNK activation in LPS-stimulated macrophages. Taken together, PL shows its anti-inflammatory activity via mediation of HO-1 in an in vitro inflammation model.     

Phellinus linteus inhibits inflammatory mediators by suppressing redox-based NF-kappaB and MAPKs activation in lipopolysaccharide-induced RAW 264.7 macrophage

The mushroom Phellinus linteus has been known to exhibit potent biological activity. In contrast to the immuno-potentiating properties of Phellinus linteus, the anti-inflammatory properties of Phellinus linteus have rarely been investigated. Recently, ethanol extract and n-BuOH fractions from Phellinus linteus were deemed most effective in anti-inflammatory activity in RAW 264.7 macrophages. The regulatory mechanisms of Phellinus linteus butanol fractions (PLBF) on the pharmacological and biochemical actions of macrophages involved in inflammation have not been clearly defined yet. In the present study, we tested the role of PLBF on anti-inflammation patterns in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage cells. To investigate the mechanism by which PLBF inhibits NO and PGE2 production as well as inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression, we examined the activation of IkappaB and MAPKs in LPS-activated macrophages. PLBF clearly inhibited nuclear translocation of NF-kappaB p65 subunits, which correlated with PLBF's inhibitory effects on IkappaBalpha phosphorylation and degradation. PLBF also suppressed the activation of mitogen-activated protein (MAP) kinases including p38 and stress-activated protein kinase/c-Jun NH2-terminal kinase (SAPK/JNK). Furthermore, macrophages stimulated with LPS generated ROS via activation of membrane-bound NADPH oxidase, and ROS played an important role in the activation of nuclear factor-kappaB (NF-kappaB) and MAPKs. We demonstrated that PLBF directly blocked intracellular accumulation of reactive oxygen species in RAW 264.7 cells stimulated with LPS much as the NADPH oxidase inhibitors, diphenylene iodonium, and antioxidant pyrrolidine dithiocarbamate did. The suppression of NADPH oxidase also inhibited NO production and iNOS protein expression. Cumulatively, these results suggest that PLBF inhibits the production of NO and PGE2 through the down-regulation of iNOS and COX-2 gene expression via ROS-based NF-kappaB and MAPKs activation. Thus, PLBF may provide a potential therapeutic approach for inflammation-associated disorders.     

Anti-inflammatory and antinociceptive potential of Maclura pomifera (Rafin.) Schneider fruit extracts and its major isoflavonoids, scandenone and auriculasin

The aqueous, ethanolic and chloroform extracts and two prenylated isoflavones: scandenone (I) and auriculasin (II), isolated from the fruits of Maclura pomifera (Rafin.) Schneider, were investigated for their in vivo anti-inflammatory and antinociceptive activity. For the anti-inflammatory activity, both carrageenan-induced hind paw edema and 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema models and for the antinociceptive activity, p-benzoquinone-induced abdominal constriction test were used. Scandenone, the chloroform and the ethanolic extracts were shown to possess antinociceptive activity and anti-inflammatory activity on carrageenan-induced hind paw edema model at 100 mg/kg dose. The same compound and the extract were also found to be highly active in (TPA)-induced mouse ear edema model whereas auriculasin and the H(2)O extract showed to be inactive in all of the assays.     

Antinociceptive, anti-inflammatory and acute toxicity effects of Zataria multiflora Boiss extracts in mice and rats

Antinociceptive, anti-inflammatory and acute toxicity of the aqueous infusion and ethanolic maceration extracts of the aerial parts of Zataria multiflora Boiss were studied in mice and rats. Antinociceptive activity was done using hot-plate and writhing tests. The effect of the extracts against acute inflammation was studied by vascular permeability increased by acetic acid and xylene induced ear edema in mice. The activity of the extracts against chronic inflammation was assessed by the cotton pellet test in rats. LD50 of the infusion and maceration extract was 3.85 and 3.47 g/kg, respectively. Intraperitoneal injection of both extracts in mice showed significant and dose-dependent antinociceptive activity. Naloxone, an opioid antagonist, pretreatment inhibited the antinociceptive activity of the extracts. The extracts exhibited antinociceptive activity against acetic acid induced writhing which was partially blocked by naloxone. Both extracts did not show remarkable activity against acute inflammation induced by acetic acid in mice. In the xylene ear edema, Z. multiflora Boiss extracts showed significant activity in mice. In the chronic inflammation the efficacy of the extracts was more than in acute inflammation. It is concluded that aqueous infusion and maceration of the aerial parts of Z. multiflora Boiss have antinociceptive effect and this may be mediated by opioid receptors. The extracts showed also anti-inflammatory effect against acute and chronic inflammation.     

Anti‐Inflammatory,Antinociceptive and Cytotoxic Effects of the Methanol Extract of Cecropia pachystachya Trécul

Cecropia pachystachya is widely used in the traditional medicine as anti‐inflammatory, antitusive, expectorant, antiasthmatic and hypoglycemic. It is also commercially available to treat skin cancer. To validate some of the popular uses of this species, its methanol leaves extract (CPM) was tested for anti‐inflammatory, antinociceptive and cytotoxic effects. The anti‐inflammatory activity was evaluated by croton oil‐induced ear edema test. When used orally, the anti‐inflammatory effect of CPM at 300 mg/kg was similar to that of indomethacin with 53% inhibition of the ear edema. Also, results on topical treatment were similar to that of dexamethasone with 83% inhibition of the edema. To evaluate the antinociceptive activity, acetic acid‐induced writhing and formalin‐induced pain tests were employed. CPM (100 and 300 mg/kg) reduced the number of writhing by 61% and 67%, respectively. In both doses, the activity was comparable to the reference drug, indomethacin. The oral administration of CPM was ineffective in the first phase of formalin test but exhibited great effects on the second phase decreasing the licking time by 85% at 300 mg/kg. The cytotoxic potential of CPM was also investigated against HL60, HL60.bcl2 and Jurkat tumor cell lines and showed an inhibition of more than 50% of cell proliferation. The flavones orientin and isoorientin were detected in CPM. Copyright © 2012 John Wiley & Sons, Ltd.     

Assessment of anti-inflammatory and antinociceptive activities of Daphne pontica L. (Thymelaeaceae)

The n-hexane, diethylether, ethyl acetate and methanol extracts from roots, leaves, stems and flowers with young leaves of Daphne pontica L. (Thymelaeaceae) were investigated for their in vivo anti-inflammatory and antinociceptive activities. For the anti-inflammatory activity assessment, carrageenan-induced hind paw edema, PGE(2)-induced hind paw edema and 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema models and for the antinociceptive activity, p-benzoquinone-induced abdominal constriction test were used. Only ethyl acetate extracts of the roots showed significant anti-inflammatory activity on carrageenan-induced (22.7-32.0% inhibition) and PGE(2)-induced hind paw edema (3.2-27.3% inhibition) as well as 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema (47.8-43.3% inhibition) models at 50 mg/kg dose without inducing any apparent gastric lesion or acute toxicity, whereas the other extracts were shown to be ineffective. In addition to roots, ethyl acetate extracts of the stems exhibited 19.5-29.9%; 5.3-23.9%; 36.6-28.1% inhibition on carrageenan-induced and PGE(2)-induced hind paw edema as well as 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema models, respectively. On the other hand, none of the extracts showed any significant antinociceptive activity.     

The apoptosis effect of hispolon from Phellinus linteus (Berkeley & Curtis) Teng on human epidermoid KB cells

Phellinus linteus (Berkeley & Curtis) Teng, a well-known fungus of the genus Phellinus in the family of Hymenochaetaceae, is being increasingly used to treat a wide variety of disease processes such as oral ulcer, gastroenteric disorder, inflammation, lymphatic disease, and various cancers. However, the mechanism underlying its anti-oral cancer effect is poorly understood. In the present study, we prepared the ethanol extract of Phellinus linteus as a crude drug, and then obtained the active component hispolon by bioassay-guided isolation. Hispolon showed a dose-dependent inhibition of human epidermoid KB cell proliferation with IC50 of 4.62+/-0.16 microg/ml. Furthermore, it was revealed that hispolon could induce human epidermoid KB cell apoptosis with the characteristic of a DNA ladder, and with a significant increase of sub-G1. This process was accompanied by the collapse of mitochondrial membrane potential, the release of cytochrome c and the activation of Caspase-3. These results demonstrated that hispolon induced the death of KB cells through a mitochondria mediated apoptotic pathway. We propose that Phellinus linteus and its effective components could be used as an anti-oral cancer drug for future studies.     

The anti-inflammatory and hepatoprotective effects of fractions from Cudrania cochinchinensis var. gerontogea.

Various fractions of the ethanol extract from the root wood of Cudrania cochinchinensis var. gerontogea (Moraceae) were evaluated for their anti-inflammatory effects on carrageenan-induced edema and hepatoprotective activities on carbon tetrachloride (CCl4)-induced and D-galactosamine-(D-GalN) induced acute hepatotoxicity in rats. The fractions (n-hexane, CHCl3, EtOAc, n-BuOH, and H2O) displayed significant inhibitory activity against carrageenan-induced edema, and the active anti-inflammatory components were further localized in the n-BuOH fraction, which exhibited the greatest anti-inflammatory effect, an effect 5% greater than indomethacin (which was used as a standard reference substance). Each fraction exerted a significant hepatoprotective effect by reducing enzymatic alteration (sGOT and sGPT) and by improving hepatic lesions, including liver centrilobular inflammation, cell necrosis, fatty change, ballooning degeneration in CCl4-induced acute hepatitis; and necrosis of the portal area in D-GalN-induced acute liver injury. The n-BuOH and EtOAc fractions had the greatest hepatoprotective effects on CCl4-induced liver injury; in contrast, the CHCl3 fraction was most potent against D-GalN intoxication, which is comparable to silymarin, as a recognized hepatoprotective drug.     

Anti-inflammatory,antipyretic and antinociceptive activities of Tabernaemontana pandacaqui Poir

Studies on carrageenin-induced rat paw edema, yeast-induced hyperthermia in rat and writhing response induced by acetic acid in mice showed that the alcoholic extract of stems of Tabernaemontana pandacaqui (T. pandacaqui) has significant anti-inflammatory, antipyretic and antinociceptive activities. These activities are due to alkaloidal components since they were also observed when the crude alkaloidal (CA) fraction separated from alcoholic extract was tested in the same models.     

Topical anti-inflammatory activity of Serjania erecta Radlk (Sapindaceae) extracts

Serjania erecta Radlk (Sapindaceae), commonly called cinco-folhas or cipó-cinco-folhas in Brazil, is thought to be effective for treating several inflammatory diseases. In order to verify the topical anti-inflammatory effect of Serjania erecta, hydroalcoholic extract and fractions were obtained by extraction in solvents of increasing polarity and were tested in mouse models using croton-oil-induced inflammation. Our findings showed that topical application of Serjania erecta hydroalcoholic extract (0.01-3.0 mg/ear), and the dichloromethane (0.03-1.0 mg/ear), ethyl acetate (0.03-1.0 mg/ear), and hexane (0.003-1.0 mg/ear) fractions revealed significant activity, causing a dose-dependent reduction of croton-oil ear edema (ID(50)=0.14 mg/ear, 0.23 mg/ear, 0.14 mg/ear, 0.04 mg/ear, respectively). The extract and all tested fractions also decreased tissue myeloperoxidase activity (indicative of polymorphonuclear leukocytes influx) in mouse-ears treated with croton oil with a maximum inhibition of 72% at 3.0 mg/ear for the hydroalcoholic extract and 81%, 78%, and 83% at 1.0mg/ear for dichloromethane, ethyl acetate and hexane fractions, respectively. As expected, dexamethasone (0.05 mg/ear) was effective in inhibiting both edema and myeloperoxidase activity (99% and 82%, respectively). In conclusion, our results indicate a topical anti-inflammatory effect for the species of Serjania studied.     

麻疯树根提取物抗炎作用的实验研究

目的：研究麻疯树根提取物的抗炎作用。方法：采用二甲苯致小鼠耳廓肿胀法、鸡蛋清致大鼠足跖肿胀法和大鼠棉球肉芽肿法观察麻疯树根提取物的抗炎作用。结果：麻疯树根提取物能明显抑制二甲苯所致的小鼠耳廓肿胀和鸡蛋清所致的大鼠足跖肿胀,也能抑制大鼠棉球肉芽肿的形成。结论：麻疯树根提取物具有明显的抗炎作用。     

Appraisal of antinociceptive and anti-inflammatory potential of extract and fractions from the leaves of Torreya grandis Fort Ex. Lindl

Torreya grandis (Taxaceae) was studied for antinociceptive and anti-inflammatory effects. Leaves were extracted with 80% ethanol at 80 °C for 3 h and fractionated with petroleum ether, chloroform, ethylacetate and n-butanol. The aqueous ethanolic extract (aq.EE), ethylacetate fraction (EaF) and butanol fraction (BtF) at the doses of (100 and 200 mg/kg, i.g.) body weight were used for study. Evaluation of antinociceptive activity was carried out by acetic acid-induced writhing response and formalin-induced paw licking time in the first and second phases of mice. The paw edema induced by formalin- and xylene-induced ear edema were used to assess anti-inflammatory activity. It was found that Torreya grandis extract and fractions at the doses of (100 and 200 mg/kg, i.g.) were significantly attenuated the writhing responses induced by acetic acid and second phase of pain response induced by subplantar injection of formalin in mice. In addition, these extract and fractions inhibiting the formaldehyde-induced arthritis as well as xylene-induces edema prolifically. From acute oral toxicity studies no mortality was pragmatic even at highest dose (2500 mg/kg, i.g.). Furthermore, our phytochemical studies indicated that the aq. ethanolic extract of leaves contains alkaloids, flavonoids, tannins, terpenoids and saponins. The results provide justification for the folkloric uses of Torreya grandis in the treatment of analgesic and inflammatory-based diseases across the China.     

Anti-angiogenic activity of the methanol extract and its fractions of Ulmus davidiana var. japonica

This study aimed to elucidate anti-angiogenic activity of Ulmus davidiana var. japonica that has been widely used in folk medicine. The methanol extract (UDE) of Ulmus davidiana var. japonica concentration-dependently displayed a strong inhibition in the chick chorioallantoic membrane (CAM) angiogenesis. The n-butanol fraction of UDE and subsequent 30% MeOH subfraction were identified to be most responsible for the anti-angiogenic activity.     

Anti-inflammatory effect of Solanum lycocarpum fruits

The croton oil-induced mouse ear oedema test, acetic acid-induced abdominal writhing, and carrageenan-induced peritonitis were used to study the anti-inflammatory effects of the crude ethanol extract and its alkaloid fraction from Solanum lycocarpum fruits. The alkaloid fraction induced a dose-dependent reduction in ear oedema formation and leukocyte migration, suggesting that S. lycocarpum fruits may contain steroidal alkaloids accounting for the anti-inflammatory effect of the crude ethanol extract.     

盐地碱蓬幼苗和种子氯仿/甲醇提取物的化学组成及其抗炎作用(英)

目的 :阐明盐地碱蓬幼苗和种子氯仿 /甲醇提取物的化学组成及其抗炎作用。方法 :盐地碱蓬幼苗和种子分别用氯仿 /甲醇 (2∶1)提取并用甲醇 /氯乙酰 (5∶1)甲酯化。用GC MS分析甲酰化产物的化学组成。提取物对急性炎症的抑制作用采用巴豆油引起的正常小鼠和摘除肾上腺小鼠的耳肿胀、组胺引起的小鼠毛细管通透性以及角叉菜胶引起的大鼠足肿胀进行分析。对慢性炎症的抑制作用以巴豆油诱导的大鼠肉芽肿和福氏完全佐剂诱导的多发性关节炎进行分析。结果 :盐地碱蓬幼苗提取物的甲酰化产物中共检测出 14种脂肪酸甲酯 ,其中十六碳酸甲酯 (2 5 .9% ) ,9,12 十八碳二烯酸甲酯 (2 8.3% )及 9,12 ,15 十八碳三烯酸甲酯 (8.95 % )为主要成分。种子提取物的甲酰化产物中共检测出 10种脂肪酸甲酯 ,其中 9,12 十八碳二烯酸甲酯 (83.4 1% )为主要成分。两种提取物的甲酯化产物明显地抑制正常小鼠和摘除肾上腺小鼠的耳肿胀、降低毛细血管的通透性并抑制大鼠肉芽肿的形成 ,在 5 0～ 30 0mg·kg-1·d-1.剂量范围之内呈明显的剂量依赖关系 ,在 30 0mg·kg-1·d-1对佐剂性关节炎和大鼠足肿胀表现出显著的抑制作用。在 5 0～ 30 0mg·kg-1·d-1.剂量范围之内能显著地抑制炎症部位的PGE2 和MDA的形成和增加红细胞CAT的活力。     

短葶山麦冬水提物及其主要有效部位和成的抗炎活性(英文)

目的:研究短葶山麦冬水提物((Lm-a)、总皂苷(Lm-s)及主要成分Lm-3的抗炎活性,为其临床应用于治疗炎性疾病提供药理学依据。方法:采用二甲苯诱导小鼠耳廓肿胀和角叉菜胶或组胺诱导小鼠足跖肿胀模型,评价Lm-a,Lm-s和Lm-3灌胃给药的体内抗炎活性;采用肿瘤坏死因子(TNF-α)或佛波酯(PMA)诱导的髓样白血病细胞(HL-60)与人脐静脉内皮细胞(ECV304)黏附模型,考察Lm-3的体外抗炎活性。结果:单次灌胃给予Lm-a(336和672mg.kg-1)明显抑制二甲苯致小鼠耳廓肿胀和角叉菜胶致小鼠足跖肿胀;Lm-s和Lm-3(23.2和4.6mg.kg-1,相当于Lm-a672mg.kg-1)对上述炎症模型显示相似的抗炎活性;相当于短亭山麦冬4g.kg-1生药量的Lm-a、Lm-s及Lm-3均明显抑制组胺致小鼠足跖肿胀;Lm-3(0.01、0.1和1μmol.L-1)体外显著抑制TNF-α或PMA诱导的HL-60与ECV304细胞的粘附作用,提示其抗炎机制可能与调节蛋白激酶C通路等有关。结论:短葶山麦冬具有显著体内外抗炎活性,其主要活性部位和成分为总皂苷和Lm-3,为其临床应用于治疗炎性疾病提供药...     

Anti-inflammatory activity of Sedum kamtschaticum

Sedum kamtschaticum Fischer (Crassulaceae) has been used as a folk medicine in North-East Asia for treating inflammatory disorders. The present investigation was carried out to establish in vivo anti-inflammatory activity and cyclooxygenase-2 modulating activity of this plant material. The methanol extract of Sedum kamtschaticum significantly inhibited mouse croton oil-induced ear edema (24–47% inhibition at 50–400 mg/kg) and rat paw edema (24–30% inhibition at 400–800 mg/kg) by oral administration. Prednisolone (10 mg/kg) showed 54 and 36% inhibition in the same animal models, respectively. Sedum kamtschaticum also showed significant inhibitory activity against mouse ear edema induced by multiple treatment of phorbol ester for 3 days. In addition, Sedum kamtschaticum exhibited potent analgesic activity against mouse acetic acid-induced writhing (IC₅₀=125 mg/kg), while aspirin (200 mg/kg) showed 57% inhibition. Using lipopolysaccharide-treated RAW 264.7 cells, down-regulation of cyclooxygense-2 expression was found to be one of the cellular action mechanisms of anti-inflammation by Sedum kamtschaticum.     

Comparative evaluation of the anti-inflammatory and antinociceptive activity of Turkish Eryngium species

Extracts obtained from the root and aerial parts of various Eryngium (Apiaceae) species are used as folk remedy worldwide for the treatment of various inflammatory disorders. Ethanolic and aqueous extracts obtained from either aerial parts or roots of eight Eryngium species growing in Turkey, i.e., were evaluated for their in vivo anti-inflammatory and antinociceptive activities. Eryngium campestre, Eryngium creticum, Eryngium davisii, Eryngium falcatum, Eryngium isauricum, Eryngium kotschyi, Eryngium maritimum, and Eryngium trisectum. For the antinociceptive activity assessment p-benzoquinone-induced writhing test, and for anti-inflammatory activity carrageenan-induced hind paw oedema and TPA-induced ear oedema tests were employed in mice. According to the results of investigations, except Eryngium falcatum extracts, ethanol extracts either from the aerial parts or roots of Eryngium species showed apparent anti-inflammatory and antinociceptive activity. In spite of potent activity of the ethanol extract from Eryngium isauricum aerial parts was induced gastric damage. Aerial parts and roots of Eryngium maritimum and Eryngium kotschyi were found to possess most promising activities without including any apparent gastric damage.     

脊痛宁胶囊抗炎镇痛作用的实验研究

目的研究脊痛宁胶囊的抗炎、镇痛作用。方法以巴豆油致小鼠耳肿胀模型和角叉菜胶致大鼠足肿胀模型,观察脊痛宁胶囊的急性抗炎作用;以棉球植入小鼠腹腔致肉芽肿模型,观察脊痛宁胶囊的慢性抗炎作用;以醋酸法造成小鼠疼痛模型,观察脊痛宁胶囊的镇痛作用。结果脊痛宁胶囊对巴豆油致耳肿胀和角叉菜胶致大鼠足肿胀有显著的抑制作用,可显著抑制棉球所致肉芽肿形成,减少醋酸所致小鼠扭体次数。结论脊痛宁胶囊具有显著的抗炎、镇痛作用。