Antiinflammatory activity of methanol extract isolated from stem bark of Magnolia kobus

The present study reports the antiinflammatory activity of a methanol extract isolated from the stem bark of Magnolia kobus (MK). MK potently inhibited lipopolysaccharide (LPS)-induced production of nitric oxide and interleukin-1beta (IL-1beta) in RAW 264.7 cells, a murine macrophage-like cell line. The secretion of tumor necrosis factor-alpha (TNF-alpha) was also suppressed in LPS-stimulated RAW 264.7 cells although the magnitude of inhibition was weaker than that of nitric oxide and IL-1beta. The mRNA expressions of inducible nitric oxide synthase (iNOS), IL-1beta and TNF-alpha were also suppressed by MK in LPS-stimulated RAW 264.7 cells. Further study demonstrated that LPS-induced DNA binding of AP-1 and phosphorylation of c-jun N-terminal kinase (JNK) were inhibited by MK treatment in RAW 264.7 cells, whereas phosphorylation of p38 mitogen-activated protein kinase was unaffected. Moreover, topical application of MK suppressed ear swelling in 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced skin inflammation model. Collectively, these results suggest that MK exerts antiinflammatory effects in vitro and in vivo and this might be mediated, at least in part, by blocking AP-1 and JNK activation.     

Attenuation of colitis injury in rats using Garcinia cambogia extract

Inflammatory bowel disease (IBD), Crohn's disease and ulcerative colitis are chronic enteropathies that probably result from a dysregulated mucosal immune response. These pathologies are characterized by oxidative and nitrosative stress, leukocyte infiltration and up-regulation of pro-inflammatory substances. Current IBD treatment presents limitations in both efficacy and safety that stimulated the search for new active compounds. Garcinia cambogia extract has attracted interest due to its pharmacological properties, including gastroprotective effects. In this study, the antiinflammatory activity of a garcinia extract was assessed in TNBS-induced colitis rats. The results obtained revealed that garcinia administration to colitic rats significantly improved the macroscopic damage and caused substantial reductions in increases in MPO activity, COX-2 and iNOS expression. In addition, garcinia extract treatment was able to reduce PGE(2) and IL-1beta colonic levels. These antiinflammatory actions could be related to a reduction in DNA damage in isolated colonocytes, observed with the comet assay. Finally, garcinia extract caused neither mortality nor toxicity signals after oral administration. As such, the antiinflammatory effects provided by the Garcinia cambogia extract result in an improvement of several parameters analysed in experimental colitis and could provide a source for the search for new antiinflammatory compounds useful in IBD treatment.     

Protective effects of sugar cane extract on endotoxic shock in mice

Sugar cane extract (SCE) has been shown to have an immunostimulating effect in chickens. This study evaluated the effect of SCE on Salmonella Abortusequi lipopolysaccharide (LPS)-induced lethal shock in d-galactosamine (GalN)-sensitized mice. Mice were administered intraperitoneally SCE (500 mg/kg) or phosphate buffered saline before or after injection of LPS and GalN. All the mice injected with LPS and GalN (control group) died of histopathologically congestive and hemorrhagic hepatic insufficiency within 24 h, showing significantly increased activities of plasma aspartate aminotransferase (AST; 380 IU/mL) and alanine aminotransferase (ALT; 130 IU/mL). Pretreatment of mice with SCE at 3 h before challenge with LPS and GalN (SCE treated group) resulted in significantly improved survival rates (92.3%) and a decrease in liver injury. These surviving mice in the SCE treated group showed no changes in the mean levels of plasma AST (60 IU/mL) and ALT (18 IU/mL). However, the level of tumor necrosis factor-alpha in the SCE treated group was not significantly different when compared with that in the control group challenged with LPS and GalN. These results suggest that SCE has protective effects on LPS-induced mortality in this mouse model.     

Effects of baicalein isolated from roots of Scutellaria baicalensis Georgi on interleukin 1β- and tumour necrosis factor α-induced tissue-type plasminogen activator and plasminogen activator inhibitor-1 production in cultured human umbilical vein endothelial cells

The effects were examined of baicalein on tissue-type plasminogen activator (t-PA) and plasminogen activator inhibitor-1 (PAI-1) production stimulated by interleukin-1α (IL-1β) and tumour necrosis factor-α (TNF-α) in cultured human vein umbilical endothelial cells (HUVECs). IL-1β and TNF-α increased PAI-1 production, but they decreased t-PA production. Baicalein isolated from the roots of Scutellaria baicalensis Georgi, inhibited the PAI-1 production stimulated by IL-1β and TNF-α, but it had no effect on the t-PA. In addition, protein kinase C (PKC) inhibitors such as H7 and sphingosine decreased the reduction of t-PA and the increase of PAI-1 by IL-1β and TNF-α. On the other hand, dibutryl cAMP and forskolin had no effect on the t-PA reduction and PAI-1 increase by IL-1β and TNF-α. Moreover, IL-1β and TNF-α did not cause [Ca²⁺] elevation. These results suggest that the inhibitory action of baicalein on the PAI-1 production by both cytokines might be directly mediated through PKC inhibition. © 1997 John Wiley & Sons, Ltd.     

Protective effects of an herbal formulation of Radix Astragali, Radix Codonopsis and Cortex Lycii on streptozotocin-induced apoptosis in pancreatic beta-cells: an implication for its treatment of diabetes mellitus

Hyperglycemia is one of the main causes of oxidative stress in type 2 diabetes mellitus. During hyperglycemia, the increased level of various reducing sugars in the blood enhances the production of reactive oxygen species (ROS) and triggers tissue damage, especially in pancreatic beta-cells. Streptozotocin (STZ) is a diabetogen that causes diabetes mellitus via ROS-induced apoptosis in beta-cells. In this study, SR10, an herbal formulation consisting of the aqueous extracts of Radix Astragali, Radix Codonopsis and Cortex Lycii was examined for its antidiabetic effects in vitro. SR10 treatment resulted in significant enhancement of survival rate of rat pancreatic beta-cells which were treated by streptozotocin. SR10 apparently reduced apoptosis of streptozotocin-treated beta-cells by decreasing DNA fragmentation, sub-G(1) peak area and percentage of apoptotic cells. Nitric oxide (NO) production in streptozotocin-treated cells was inhibited by SR10 via the suppression of the expression of inducible nitric oxide synthase (iNOS). The implication of SR10 in treating type 2 diabetes mellitus was discussed.     

Phlomis umbrosa root inhibits mast cell-dependent allergic reactions and inflammatory cytokine secretion

The effect of an aqueous extract of Phlomis umbrosa Turcz. (Labiatae) root (PUAE) on mast cell-dependent allergic reactions and inflammatory cytokine secretion were investigated. PUAE (0.01-1 g/kg) inhibited compound 48/80-induced systemic allergic reaction. When PUAE was employed in a systemic allergic reaction test, the plasma histamine levels were reduced in a dose-dependent manner. PUAE (0.1 and 1 g/kg) also significantly inhibited the local allergic reaction activated by anti-dinitrophenyl (DNP) IgE. PUAE (0.001-1 mg/mL) dose-dependently inhibited the histamine release from rat peritoneal mast cells activated by compound 48/80 or anti-DNP IgE. PUAE (0.01-1 mg/mL) inhibited the secretion of interleukin (IL)-1beta in phorbol 12-myristate 13-acetate plus calcium ionophore A23187-stimulated human mast cell line (HMC-1) cells. PUAE (1 mg/mL) inhibited the gene expression and production of the main inflammatory cytokine, TNF-alpha, in HMC-1 cells. These results provide evidence that PUAE may be beneficial in the treatment of allergic diseases.     

SunghyangJungki-San Ga Pogongyoung inhibits IL-1 mediated tumour necrosis factor-alpha secretion in astrocytes

Astrocytes play an important role in initiating and modulating inflammatory responses within the central nervous system (CNS). Extensive studies in rodents have shown that substance P induces inflammatory cytokine production in astrocytes. In this study we have examined whether an aqueous extract of SunghyangJungki-San Ga Pogongyoung (SSGP) inhibits the secretion of TNF-alpha from primary cultures of rat astrocytes. SSGP (10-1,000 microg/mL) significantly inhibited the TNF-alpha secretion by astrocytes stimulated with lipopolysaccharide (LPS) and substance P (SP). Interleukin-1 (IL-1) has been shown to elevate TNF-alpha secretion from LPS-stimulated astrocytes while having no effect on astrocytes in the absence of LPS. We therefore examined whether IL-1 mediated inhibition of TNF-alpha secretion from primary astrocytes by SSGP. Treatment with SSGP (10-1,000 microg/mL) to astrocytes stimulated with both LPS and SP decreased IL-1 secretion significantly. Moreover, the secretion of TNF-alpha by LPS and SP in astrocytes was progressively inhibited with an increasing amount of IL-1 neutralizing antibody. Our results suggest that SSGP may inhibit TNF-alpha secretion by inhibiting IL-1 secretion and that SSGP has an antiinflammatory activity in the CNS.     

Evidence that the marine-derived multi-mineral Aquamin has anti-inflammatory effects on cortical glial-enriched cultures

It is well established that neuroinflammation contributes to brain aging, and that cortical cells are particularly vulnerable. Lipopolysaccharide stimulates the release of the pro-inflammatory cytokines, tumor necrosis factor-alpha and interleukin-1beta from glial cells which consequently induces an impairment in neuronal cell function. The food supplement, Aquamin, is a natural, multi-mineral derived from the red algae Lithothamnion corallioides, rich in calcium, magnesium and 72 other trace minerals. The aim of this study was to evaluate the anti-inflammatory potential of Aquamin in lipopolysaccharide-stimulated, glial-enriched primary cultures of rat cortex. It is reported that Aquamin prevented lipopolysaccharide-induced secretion of tumor necrosis factor-alpha and interleukin-1beta from cortical glia. These data suggest that nutritional supplements such as Aquamin may play an important role in impeding the detrimental effects of excessive inflammation in the brain.     

Protective effect of Astragalus polysaccharides on ATP binding cassette transporter A1 in THP‐1 derived foam cells exposed to tumor necrosis factor‐alpha

Astragalus polysaccharide (APS), the main extract from the traditional Chinese medicinal herb Astragalus membranaceus, has been reported to benefit the treatment of immune‐inflammatory diseases and metabolic disorders. In atherosclerotic plaques, proinflammatory cytokines exert adverse effects on lipids thereby aggravating atherosclerosis. Recent evidence shows that tumor necrosis factor‐alpha (TNF‐α) can down‐regulate the expression of ATP‐binding cassette transporter A1 (ABCA1), which plays a vital role in reverse cholesterol transport and determines the process of atherosclerosis. In the present study, the effects of APS on ABCA1 expression, cholesterol effluent rate and total cholesterol content of THP‐1 derived foam cells exposed to TNF‐α were investigated. Compared with the foam cells exposed to TNF‐α, ABCA1 expression was promoted in the presence of APS. Consequently the cholesterol effluent rate increased and the total cholesterol content decreased significantly. TNF‐α could enhance the activity of nuclear factor‐kappa B (NF‐κB) in the foam cells. This effect could be attenuated by APS. These findings suggest that APS could protect ABCA1 against the lesion of TNF‐α in THP‐1 derived foam cells, which may contribute to its antiatherosclerotic properties. Copyright © 2009 John Wiley & Sons, Ltd.     

Protective effect of Moutan Cortex extract on acetaminophen-induced hepatotoxicity in mice

Previously, we demonstrated that Moutan Cortex prevents acetaminophen (AAP)-induced cytotoxicity in vitro. The present study examined the protective effect of Moutan Cortex on AAP induced hepatotoxicity and the possible mechanisms underlying this effect in mice. When Montan Cortex was administered to ICR mice, followed by hepatotoxic dose of AAP (400 mg/kg, i.p.), Moutan Cortex pre-exposure prevented liver injury as indicated by the decrease of serum alanine aminotransferase level. Moutan Cortex also protected AAP-induced hepatic glutathione depletion. Cytochrome P450 2E1-dependent aniline and p-nitrophenol hydroxylases activities in microsomal incubations were significantly inhibited by Moutan Cortex. Abrogation of toxicity was also mirrored in DNA fragmentation. These observations demonstrate that Moutan Cortex pre-exposure may attenuate AAP-induced GSH depletion, cytochrome P450 2E1 activity, and hepatic DNA damage in vivo.     

Effect of Ginkgo biloba extract on beta-adrenergic receptors in different rat brain regions

The effect of oral administration of Ginkgo biloba extract at a dose of 90 mg/kg for 7 consecutive days on rat brain beta-adrenergic receptors in the frontal cortex, hippocampus, striatum and hypothalamus was studied. Ginkgo biloba treatment induced a significant decrease in the density (B(max)) of beta-adrenoreceptors in the frontal cortex and hippocampus. It has been suggested that modulation of the beta-adrenergic system is implicated in the favourable effects of Ginkgo biloba extracts on learning and memory.     

Antiinflammatory effect of the ethanol extract of Berberis koreana in a gerbil model of cerebral ischemia/reperfusion

Berberis koreana extract (BE) has a strong neuroprotective effect after ischemic stroke in gerbils, which is associated with the inhibition of the N-methyl-d-aspartate receptor. The present study examined the antiinflammatory mechanism of BE after ischemic damage in vitro and in vivo. The BE used contained on average 7.39 +/- 0.78 mg/g of berberine. In PC12 cells with inflammation, prostaglandin E2 (PGE2) production was significantly reduced by BE. About 75% of pyramidal cells in the hippocampal CA1 region of gerbils exposed to 5 min of transient ischemia were protected from ischemic damage by BE. Cyclooxygenase-2 (COX-2) immunoreactivity and its protein level in the CA1 region of vehicle-treated animals exposed to an ischemic insult increased with time post-ischemia, whereas no such changes were observed in BE-treated animals exposed to ischemia. PGE2 production in BE-treated ischemic animals was significantly lower than that observed in vehicle-treated ischemic animals. Summarizing, the potent neuroprotective effect of BE was found to be due to the inhibitions of COX-2 expression and PGE2 production and its antiinflammatory activity.     

Action of Rubus coreanus extract on systemic and local anaphylaxis

The effect was investigated of the aqueous extract of Rubus coreanus Miq. (Rosaceae) fruits (RCAE) on systemic and local anaphylaxis. RCAE (0.01-1 g/kg) dose-dependently inhibited systemic anaphylaxis induced by compound 48/80 in mice. RCAE (1 g/kg) also significantly inhibited local anaphylaxis activated by anti-DNP IgE. Pretreatment with RCAE at the same concentration before systemic anaphylaxis reduced the plasma histamine levels in a dose-dependent manner. RCAE (0.001-1 mg/mL) dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-DNP IgE. The level of cAMP in RPMC, when RCAE was added, significantly increased, compared with that of the normal control. Moreover, RCAE (0.01-1 mg/mL) had a significant inhibitory effect on anti-DNP IgE-induced tumour necrosis factor-alpha production from RPMC. These results indicate that RCAE may possess antianaphylactic action.     

Drug interaction potential of the seed extract of Urtica urens L. (dwarf Nettle)

Dwarf nettle (Urtica urens) seed extract was examined in vivo in the rat for its potential to modulate drug metabolizing enzymes including aminopyrine N‐demethylase (APND; CYP2C6), aniline 4‐hydroxylase (A4H; CYP2E1), nitrosodimethylamine N‐demethylase (NDMA‐ND; CYP2E1) erythromycin N‐demethylase (ERND; CYP3A1) CYP2D1/2 and glutathione S‐transferase (GST). RT‐PCR data and western blotting studies clearly demonstrated that CYP2C6 and CYP2E1 mRNA levels were substantially increased after Urtica treatment, while the level of CYP3A1 mRNA decreased and that of CYP2D1/2 remained unchanged. Urtica treatment significantly induced GST activity in the liver, lung and kidney (66‐, 46‐ and 31‐fold, respectively) while decreasing that of APND (35‐, 61‐ and 94‐fold) and NDMA‐ND (23, 28 and 54‐fold). ERND activity in liver was reduced 45‐fold, but increased in the lung and kidney (78‐ and 144‐fold) after Urtica treatment. These results indicate that Urtica seed extract may have the potential to inhibit and/or induce the metabolism of certain co‐administered drugs. Copyright © 2009 John Wiley & Sons, Ltd.     

1-hydroxy-2,3,4,6-tetramethoxy-xanthone对大鼠局灶性脑缺血再灌注损伤的保护作用

目的 :研究 1 hydroxy 2 ,3 ,4,6 tetramethoxy xanthone对大鼠局灶性脑缺血再灌注损伤的保护作用。 方法 :采用线栓法阻断大脑中动脉 (MCA)血流 ,造成局灶性脑缺血再灌注模型 (MCAO) ;评价大鼠神经行为功能、测定脑梗塞体积及血清中丙二醛(MDA)含量、超氧化物歧化酶 (SOD)和谷胱甘肽过氧化物酶 (GSH Px)活性。结果 :与大鼠脑缺血再灌注模型组相比 ,1 hydroxy 2 ,3 ,4,6 tetramethoxy xanthone能明显降低脑缺血再灌注大鼠的神经行为学评分分值 (P <0 .0 5 ) ,缩小脑梗塞灶体积 (P <0 .0 1) ,显著提高SOD、GSH Px的活力 (P <0 .0 5 ) ,降低MDA含量 (P <0 .0 5 )。结论 :1 hydroxy 2 ,3 ,4,6 tetramethoxy xanthone对大鼠脑缺血再灌注损伤具有保护作用 ,其作用机制可能与提高SOD、GSH Px的活性 ,减少脂质过氧化有关。     

黄芪提取物对四氯化碳致大鼠肝纤维化的保护作用

目的:研究黄芪提取物对四氯化碳(CCl4)致大鼠肝纤维化的保护作用及其机制。方法:取一批大鼠,其中10只为正常组,除正常组sc等体积生理盐水外,其他大鼠均从第1 d开始颈背部sc CCl4原液(5 mL.kg-1)。以后每周2次sc 40%CCl4花生油(3 mL.kg-1)7周,以复制大鼠肝纤维化模型。选造模好的肝纤维化大鼠,随机分为黄芪提取物(4,2 g.kg-1)组,CCl4模型组,每组10只。造模结束第2 d开始给药。正常组和CCl4模型组ig蒸馏水,药物组ig黄芪提取物(4,2 g.kg-1),每天1次,连续ig给药30 d。用赖氏法测定大鼠血清丙氨酸转氨酶(ALT)和天冬氨酸转氨酶(AST)的活性,用放免法测定大鼠血清透明质酸(HA)和肿瘤坏死因子(TNF-α)的含量,并观察肝脏病理变化。结果:黄芪提取物(4,2 g.kg-1)组ALT和AST活性为(36.82±7.25),(48.83±17.55)U.L-1,(75.87±15.04),(96.69±34.56)U.L-1与模型组相比,黄芪提取物可明显降低CCl4致大鼠肝纤维化血清ALT和AST活性;HA和TNF-α含量为(211.88±72.77),(300.00±142.83)μg.L-1,(0.91±0.20),(1.00±0.11)μg.L-1与模型组相比,黄芪提取物可明显降低HA和TNF-α含量;黄芪提取物可明显减轻大鼠肝纤维化的程度。结论:黄芪提取物有明显地保肝和抗肝纤维化作用,其作用机制可能与降低HA和TNF-α含量有关。     

Administration of Cyperus rotundus tubers extract prevents weight gain in obese Zucker rats

Cyperus rotundus L. (Cyperaceae; C. rotundus) is an Indian medicinal plant demonstrated to exert multiple health benefits. The purpose of the present study was to test the biological efficacy of C. rotundus tubers extract on weight control in obese Zucker rats. It was demonstrated that administration of 45 or 220 mg/kg/day of C. rotundus tubers hexane extract for 60 days in Zucker rats induced a significant reduction in weight gain without affecting food consumption or inducing toxicity. In vitro, 250 microg/mL of this extract was able to stimulate lipolysis in 3T3-F442 adipocytes suggesting that this medicinal plant contains activators of beta-adrenoreceptors (AR). The binding assay performed on the rat beta3-AR isoform, known to induce thermogenesis, demonstrated that C. rotundus tubers extract can consistently and effectively bind to this receptor. These data suggest that the effect on weight gain exerted by C. rotundus tubers extract may be mediated, at least partially, through the activation of the beta3-AR. In conclusion, C. rotundus tubers extract prove to be a new herbal supplement for controlling body weight preferentially in beta3-AR sensitive species.