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Extracts from powders of geminated brown rice (Oryza sativa L.), Moringa oleifera, and Cordyceps militaris were combined in various ratios and their health-beneficial properties were investigated. All combined extracts exerted the synergistic effects on antioxidant activity as well as inhibitions against α-amylase and α-glucosidase. Extract formulas T4 (70% germinated brown jasmine rice, 20% M. oleifera dry leaves, and 10% C. militaris) and T2 (80% germinated brown jasmine rice, 10% M. oleifera dry leaves, and 10% C. militaris) elicited the significantly highest antioxidant activity and the significantly highest inhibition against α-glucosidase, respectively. Both formulas exhibited the significantly highest inhibition against α-amylase. As compared to each other, extract formulas T4 and T2 possessed the higher glucose consumption-promoting and antiinflammatory activities, respectively. Both formulas were not toxic to normal RAW-264.7 and SW-480 human colon cancer cells. Bioactive compounds with health-supporting properties were identified using UHPLC-QTOF-MS/MS. These combined extracts can be promising therapeutic food. [ABSTRACT FROM AUTHOR]

Plant chemodiversity is a helpful tool for disease prevention and a basis for adjuvant treatments to conventional therapies. In this regard, the extract of Polypodium leucotomos rhizomes, PLE, has shown benefits fighting inflammation and recurrent infections but its molecular mechanism is poorly undersood. This work shows that Plesinox 3A, containing PLE, Vitamins A, C, and selenium, helps modulate the initial inflammatory response triggered by bacterial LPS through the upregulation of IL8 and IL10, together with downregulation of COX2, IL1B and TNF, in a more efficient manner than PLE alone. Additionally, this formulation enhances the antiviral response through the upregulation of MX1, IFNA1 and IFNG in different cell types. Finally, the addition of vitamins and selenium to PLE in Plesinox 3A greatly boosts the anti-bacterial properties of PLE alone. Overall, these findings support the combined use of PLE, vitamins, and selenium, in the form of Plesinox 3A as an immune booster to prevent recurrent infections, highlighting a gene set potentially involved in its beneficial effect, as well as showing its direct anti-bacterial properties, which are greater than those of PLE alone. [ABSTRACT FROM AUTHOR]

Context: Ganoderma lucidum polysaccharides (GLP), from Ganoderma lucidum (Leyss. ex Fr.) Karst. (Ganodermataceae), are reported to have anti-inflammatory effects, including anti-neuroinflammation and anti-colitis. Nevertheless, the role of GLP in acute pneumonia is unknown. Objective: To explore the protective role of GLP against LPS-induced acute pneumonia and investigate possible mechanisms. Materials and methods: GLP were extracted and used for high-performance liquid chromatography (HPLC) analysis after acid hydrolysis and PMP derivatization. Sixty C57BL/6N male mice were randomly divided into six groups: Sham, Model, LPSþGLP (25, 50 and 100mg/kg/d administered intragastrically for two weeks) and LPSþdexamethasone (6mg/kg/d injected intraperitoneally for one week). Acute pneumonia mouse models were established by intratracheal injection of LPS. Haematoxylin and eosin (H&E) staining was examined to evaluate lung lesions. ELISA and quantitative real-time PCR were employed to assess inflammatory factors expression. Western blots were carried out to measure Neuropilin-1 expression and proteins related to apoptosis and autophagy. Results: GLP suppressed inflammatory cell infiltration. In BALF, cell counts were 1.1x106 (model) and 7.1x105 (100 mg/kg). Release of GM-CSF and IL-6 was reduced with GLP (25, 50 and 100mg/kg) treatment. The expression of genes IL-1b, IL-6, TNF-a and Saa3 was reduced. GLP treatment also suppressed the activation of Neuropilin-1 (NRP1), upregulated the levels of Bcl2/Bax and LC3 and led to downregulation of the ratio C-Caspase 3/Caspase 3 and P62 expression. Discussion and conclusions: GLP could protect against LPS-induced acute pneumonia through multiple mechanisms: blocking the infiltration of inflammatory cells, inhibiting cytokine secretion, suppressing NRP1 activation and regulating pneumonocyte apoptosis and autophagy. [ABSTRACT FROM AUTHOR]

Context: Accumulated experimental evidence suggests that resveratrol (RSV) may have an effect on acute kidney injury (AKI) by inhibiting inflammation. However, the credibility of the evidence for this practice is unclear. Objective: This study investigated the effect of RSV on AKI and the underlying mechanism. Methods: We searched PubMed, EMBASE, and Web of Science from 2005 to April 2022 for controlled animal trials assessing the effect of conventional resveratrol versus placebo on renal function outcome after AKI. This study was registered within the International Prospective Register of Systematic Reviews (PROSPERO) as number CRD42022329596. Results: We retrieved 455 studies, 25 studies comprising data of 436 animals that met the inclusion criteria. Our meta-analysis suggested that RSV treatment was significantly associated with lower levels of serum creatinine (Scr) and blood urea nitrogen (BUN). The greatest effects were recorded in low-dose (<20mg/kg/day) groups rather than in high-dose (> 20 mg/kg/day) groups. For time-response effects, subgroup analysis indicated that intervention duration of RSV can influence the treatment effect, and more beneficial effects were observed when studies had a drug administration time of <2weeks. Discussion and conclusions: This systematic review of animal AKI studies showed a consistently favourable effect of RSV as compared to placebo on renal function outcomes that increased with lower TNF-α, IL-6, and IL-1β. RSV has a more beneficial effect on SA-AKI animal models than the others. When the RSV intervention dose was low (< 20mg/kg/day) and the intervention time was <2 weeks, more benefits could be observed. [ABSTRACT FROM AUTHOR]

Context: Pinus densiflora Siebold & Zucc. (Pinaceae) needle extracts ameliorate oxidative stress, but research into their anti-inflammatory effects is limited. Objective: To investigate antioxidant and anti-inflammatory effects of a Pinus densiflora needles (PINE) ethanol extract in vitro and in vivo. Materials and methods: We measured levels of reactive oxygen species (ROS), superoxide dismutase (SOD) and inflammatory mediators in lipopolysaccharide (LPS)-stimulated RAW264.7 cells at various PINE concentrations (25, 50 and 100 lg/mL; but 6.25, 12.5 and 25 lg/mL for interleukin-1b and prostaglandin E2 (PGE2)). Thirty ICR mice were randomized to six groups: vehicle, control, PINE pre-treatment (0.1, 0.3 and 1 mg/left ear for 10 min followed by arachidonic acid treatment for 30 min) and dexamethasone. The posttreatment ear thickness and myeloperoxidase (MPO) activity were measured. Results: PINE 100 lg/mL significantly decreased ROS (IC50, 70.93 lg/mL, p<0.01), SOD (IC50, 30.99 lg/mL, p<0.05), malondialdehyde (p<0.01), nitric oxide (NO) (IC50, 27.44 lg/mL, p<0.01) and tumour necrosis factor-alpha (p<0.05) levels. Interleukin-1b (p<0.05) and PGE2 (p<0.01) release decreased significantly with 25 lg/mL PINE. PINE 1mg/ear inhibited LPS-stimulated expression of cyclooxygenase-2 and inducible NO synthase in RAW264.7 macrophages and significantly inhibited ear oedema (36.73-15.04% compared to the control, p<0.01) and MPO activity (167.94-105.59%, p<0.05). Discussion and conclusions: PINE exerts antioxidant and anti-inflammatory effects by inhibiting the production of inflammatory mediators. Identified flavonoids such as taxifolin and quercetin glucoside can be attributed to effect of PINE. [ABSTRACT FROM AUTHOR]

Context: Deer antler based active ingredients are known to have certain anti-inflammatory and antioxidant activities. However, its potential hepatoprotective effect remains unclear. Objective: This article reports the hepatoprotective effect of protein components in deer antler bases (R1) on lipopolysaccharide/D-galactosamine (LPS/D-GalN)-induced acute liver injury (ALI) in mice, and explores its possible mechanism. Materials and methods: The four separated and purified protein components of deer antler bases were screened and verified by the RAW264.7 cell inflammation model. In the in vivo experiment of LPS/D-GalNinduced ALI in mice, ALT, AST, SOD, CAT, GSH and MDA were detected. The liver histopathology was analysed, the COX-2 and iNOS proteins were analysed by immunohistochemistry, and 4-HNE was analysed by immunofluorescence staining. In addition, the effects on the MAPK pathway and NF-jB/IjB-a pathway in liver proteins were explored. Results: With isolated RA protein fraction pre-treated RAW264.7 cells, NO production decreased by 35.3% compared with the model group. The experimental results of ALI in mice induced by LPS/D-GalN show that R1 protein components can protect mice from ALI through anti-inflammatory and anti-oxidative stress effects and reduce liver pathological damage in mice. The results also indicate that the R1 protein component may protect the liver by inhibiting the activation of the MAPK pathway and the NF-jB/IjB-a pathway induced by LPS/D-GalN. Conclusions: The separated and purified R1 protein component of deer antler base has a good protective effect on LPS/D-GalN-induced liver injury, and may become a potential material for protecting against liver injury. [ABSTRACT FROM AUTHOR]

Context: Developing effective drugs to treat myocardial ischaemia-reperfusion (MI/R) injury is imperative. Traditional Chinese medicines (TCMs) have had considerable success in the treatment of cardiovascular diseases. Elucidating the mechanisms by which TCMs improve MI/R injury can supplement the literature on MI/R prevention and treatment. Objective: To summarise TCMs and their main protective mechanisms against MI/R injury reported over the past 40 years. Methods: Relevant literature published between 1980 and 2020 in Chinese and English was retrieved from the Web of Science, PubMed, SpringerLink, PubMed Central, Scopus, and Chinese National Knowledge Infrastructure (CNKI) databases. Search terms included 'medicinal plants', 'myocardial ischaemia reperfusion injury', 'Chinese medicine prescriptions', 'mechanisms', 'prevention', 'treatment' and 'protection'. For inclusion in the analysis, medicinal plants had to be searchable in the China Medical Information Platform and Plant Database. Results: We found 71 medicinal species (from 40 families) that have been used to prevent MI/R injury, of which Compositae species (8 species) and Leguminosae species (7 species) made up the majority. Most of the effects associated with these plants are described as antioxidant and anti-inflammatory. Furthermore, we summarised 18 kinds of Chinese compound prescriptions, including the compound Danshen tablet and Baoxin pill, which mainly reduce oxidative stress and regulate mitochondrial energy metabolism. Discussion and conclusions: We summarised TCMs that protect against MI/R injury and their pharmacological mechanisms. This in-depth explanation of the roles of TCMs in MI/R injury protection provides a theoretical basis for the research and development of TCM-based treatment drugs. [ABSTRACT FROM AUTHOR]

Context: Amauroderma rugosum (Blume & T. Nees) Torrend (Ganodermataceae) is an edible mushroom with medicinal properties. However, the effects of A. rugosum on gastric ulcer remain unclear. Objective: To investigate the gastroprotective efficacy of water extract of A. rugosum (WEA) on gastric ulcer. Materials and methods: Sprague-Dawley rats were randomly grouped as control, model, lansoprazole and 200, 100 and 50 mg/kg of WEA. After pre-treatment for seven days, ethanol- and indomethacininduced gastric ulcer models were established. The gastric ulcer and histopathology were investigated. Enzyme-linked immunosorbent assay (ELISA), quantitative polymerase chain reaction (Q-PCR) and Western blot assays were conducted to explore the potential anti-inflammatory effect and mechanism of WEA. Additionally, the pyloric ligation model was used to explore the influence of WEA on gastric acid and mucus. Results: Pre-treatment with WEA (200, 100 and 50mg/kg) effectively reduced ulcerous area in both ethanol-induced (71%, 88% and 71%) and indomethacin-induced (77%, 65% and 86%) gastric ulcer model. The gastric levels of tumour necrosis factor-alpha (TNF-a) (34% and 50mg/kg), interleukin-6 (IL-6) (32% and 100mg/kg) and interleukin-1b (IL-1b) (36%, 45% and 41%) were reduced significantly (p<0.05) by WEA. Serum nitric oxide was decreased significantly (p<0.05) at 200 and 50mg/kg and PGE2 concentration was increased remarkably (p<0.05) at 100 mg/kg. Gene expression of inflammasome Nlrp3, and the nuclear translocation of nuclear factor-jB (NF-jB) P65 were significantly decreased by WEA pre-treatment. However, the pH of gastric acid and secretion of mucus did not show any significant change. Conclusions: The gastroprotective effect of WEA on gastric damage is attributed to anti-inflammation through the inhibition on NF-jB P65 nuclear migration and Nlrp3 gene expression. [ABSTRACT FROM AUTHOR]

Context: Ranunculus ternatus Thunb (Ranunculaceae), (RTT) is used clinically for the treatment of tuberculosis or as tumour adjuvant therapy, but its potential effect on diabetic nephropathy (DN) has not been studied. Objective: To investigate the effect of RTT extract in renal fibrosis of DN. Materials and methods: C57BL/6 mice were randomly divided into four groups (n = 12). Diabetes mellitus (DM) mice were induced by streptozotocin (STZ, 55 mg/kg/day) for five consecutive days and treated by RTT extract (2 g/kg). Afterward, blood glucose, HE and Masson staining were assayed. The expression levels of Vimentin, ɑ-SMA, TNF-ɑ, NF-κB p-p65, NF-κB p65, SMYD2, H3K36me3, H3K4me3 were determined by western blots. Firbronectin was respectively assayed by western blot and immunofluorescent staining. Results: RTT extract significantly ameliorated renal injury and renal fibrosis in the renal tissue of STZ-induced diabetic mice as demonstrated by the decreased expression level of Fibronectin (65%), Vimentin and α-SMA (75% & 53%). In addition, the levels of TNF-α (57%), NF-κB p-p65 and NF-κB p65 (35% & 25%) were elevated in the DN mice. Importantly, these were alleviated after RTT extract treatment. Moreover, we observed that the protein levels of SMYD2 (30%), H3K36me3 and H3K4me3 (53% & 75%) were reduced in DN mice after treatment with RTT extract. Discussion and conclusions: RTT extract mediates antifibrotic effects and anti-inflammatory responses in STZ-induced DN mainly through suppressing SMYD2 activation and H3K36me3 and H3K4me3 protein expression. RTT extract might have therapeutic potential against high glucose-induced nephropathy. [ABSTRACT FROM AUTHOR]

A novel ent-pimarane-type diterpenoid, sigesbeckia J (1), along with two known diterpenoids, siegesbeckia acid (2) and ent-18-acetoxy-16R,17-dihydroxykauran-19-oic acid (3), were isolated from the aerial parts of Sigesbeckia glabrescens Makino. Their chemical structures were elucidated based on extensive spectroscopic interpretation. The absolute configuration of ent-pimaranetype diterpenoid (1) was determined by comparing experimental and calculated ECD spectra. Compared with the positive control minocycline (IC50 32.84 ΞM), compound 1 exhibited moderate cell growth anti-inflammatory activities in vitro by testing their inhibition of LPS-induced NO production in BV2 microglial cells, with IC50 value of 58.74Ξ. [ABSTRACT FROM AUTHOR]

Lipids are complex organic compounds made up of carbon, oxygen, and hydrogen. These play a diverse and intricate role in cellular processes like membrane trafficking, protein sorting, signal transduction, and bacterial infections. Both Gram-positive bacteria (Staphylococcus sp., Listeria monocytogenes, etc.) and Gram-negative bacteria (Chlamydia sp., Salmonella sp., E. coli, etc.) can hijack the various host-lipids and utilize them structurally as well as functionally to mount a successful infection. The pathogens can deploy with various arsenals to exploit host membrane lipids and lipid-associated receptors as an attachment for toxins' landing or facilitate their entry into the host cellular niche. Bacterial species like Mycobacterium sp. can also modulate the host lipid metabolism to fetch its carbon source from the host. The sequential conversion of host membrane lipids into arachidonic acid and prostaglandin E2 due to increased activity of cPLA-2 and COX-2 upon bacterial infection creates immunosuppressive conditions and facilitates the intracellular growth and proliferation of bacteria. However, lipids' more debatable role is that they can also be a blessing in disguise. Certain host-lipids, especially sphingolipids, have been shown to play a crucial antibacterial role and help the host in combating the infections. This review shed light on the detailed role of host lipids in bacterial infections and the current understanding of the lipid in therapeutics. We have also discussed potential prospects and the need of the hour to help us cope in this race against deadly pathogens and their rapidly evolving stealthy virulence strategies. [ABSTRACT FROM AUTHOR]

Background: Resolvin D1 (RvD1) is a soluble mediator, which is the metabolite of docosahexaenoic acid (DHA), an omega-3 fatty acid. It is thought that RvD1 may contribute to the etiology of bipolar disorder (BD) because of its anti-inflammatory and antidepressant effect. In this study, it was aimed to compare the serum RvD1 levels of patients with BD diagnosed manic-depressive-euthymic episodes with those of healthy subjects. The secondary objective of this study is to investigate the relationship between RvD1 measures and inflammatory markers. Methods: We included 121 male patients with BD type I, 44 in a mania, 35 in depression and 42 in euthymic state, and 41 healthy controls. Serum RvD1 levels and inflammation indicators (CRP, neutrophil, leukocyte, and albumin) were measured. Results: When the RvD1 values of patients were compared, the median (interquartile range) RvD1 value was 11.2 (5.2) for manic patients, 11.2 (6.6) for depressive patients, 9.6 (5.6) for euthymic patients and 8.4 (7.7) for the control group. There were statistically significant differences between the groups in terms of RvD1 values (p <.001). After adjustment for age and current state with ANCOVA, there were statistically significant differences between manic vs. control groups and depression vs. control groups (p <.001, p=.047). Also mean CRP measures (p=.029) and neutrophil counts (p=.009) were significantly correlated with log transformed RvD1 levels. Conclusions: Our results of increased anti-inflammatory RvD1 during manic and depressive states suggest RvD1 may serve as a delayed resolvent possibly improving inflammatory imbalance. Further research is needed to confirm our findings. [ABSTRACT FROM AUTHOR]

A new trienic α-pyrone derivative asteltoxin G (1) bearing a tetrahydrofuran ring and a new ochratoxin derivative named ochratoxin A1 (5), along with seven known compounds, were isolated from a sponge-derived fungus Aspergillus ochraceopetaliformis. The compounds (1'9) were evaluated on the basis of spectroscopic analyses and comparison with those of the reported data. The new compound ochratoxin A1 (5) exhibited anti-inflammatory activity against IL-6 and TNF-α expression of the LPS-induced THP-1 cells with inhibitory rates of 74.4 and 67.7% at concentration of 10 μM, respectively. [ABSTRACT FROM AUTHOR]

Context:Gymnosperma glutinosum(Spreng.) Less. (Asteraceae) is a bush used for the empirical treatment of pain, fever, and cancer. Anent-neo-clerodane diterpene (2-angeloylent-dihydrotumanoic acid; ADTA) was isolated fromG. glutinosum. Objective:This study evaluates the cytotoxic, anti-inflammatory, and antinociceptive effects of ADTA. Materials and methods:The cytotoxic effects of ADTA (1–350 μM) were evaluated using the MTT assay with human tumorigenic (SW-620, MDA-MB231, SKLU1, SiHa, and PC-3), and non-tumorigenic (HaCaT) cells for 48 h. Thein vitroanti-inflammatory effects of ADTA (0.23–460 μM) were assessed using murine peritoneal macrophages stimulated with LPS and estimating the levels of pro-inflammatory mediators for 48 h. The antinociceptive effects of ADTA (25–100 mg/kg p.o.) were evaluated using twoin vivomodels of chemical-induced nociception during 1 h. Results:ADTA lacked cytotoxic activity (IC50> 100 μM) on tumorigenic cells. In non-tumorigenic cells (HaCaT), ADTA exerted low cytotoxic effects (IC50 = 273 μM). ADTA, at concentrations of 115 μM or higher, decreased the release of pro-inflammatory mediators. The maximum antinociceptive effects of ADTA in the acetic acid-induced abdominal constrictions by ADTA was found at 100 mg/kg (63%), whereas in the formalin test at phase 1 and phase 2, ADTA (100 mg/kg) decreased the licking time by 47 and 71%, respectively. Conclusion:The results indicate that ADTA, obtained fromG. glutinosum, exerts moderatein vitroanti-inflammatory andin vivoantinociceptive effects, but lacks cytotoxic effects on human cancer cells. [ABSTRACT FROM PUBLISHER]

Perilla frutescens(L.) Britt Labiatae (Pl), known as “Zi-So” and widely grown in China (red cultivar, Rpl) and Japan (green cultivar, Gpl), is frequently served on “Sa-Shi-Mi” dishes. Considering whether the perilla leaves substantially possess antimicrobial activity, we prepared the essential oils (EO: EOr and EOg), the pentane and ether [E: E(rp) and E(gp)] subfractions, the aqueous [Rpl(w) and Gpl(w)] and ethanolic extracts [pl(E), Rpl(E) and Gpl(E)] to compare their biological activities. Results indicated Gpl(E) and Rpl(E) contained huge amount (in mg/100 g) of polyphenoilcs (1472±1.0 vs. 1269.8±1.7), rutin (20.8±0.8 vs. 11.4±0.6), quercetin (29.8±0.9 vs. 13.6±0.6), and lutein (13.9±0.7 vs. 14.2±0.8). The total number of volatile constituents present in EOr and EOg were 27 in each but different phytochemicals. The top five major constituents (in %) in EOr were perilla aldehyde (54.35%), limonene (23.81%),trans-caryophyllene (7.2%),cis,trans-α-farnescene (7.02%), and linalool (2.40%); that in EOg were perilla aldehyde (65.26%), limonene (12.49%),cis,trans-α-farnescene (7.31%),trans- caryophyllene (5.91%), and linalool (2.75%); The top two constituents in E(rp) were perilla aldehyde (93.19%) and linalool (4.02%); that of E(gp) were perilla aldehyde (84.40%) and linalool (5.03%). EO and E showed moderate DPPH free radical scavenging-, ferrous ion chelating-, superoxide anion- and H2O2-scavenging capabilities. At 1.0 mg/mL the Es always revealed to be superior to EOs againstE. coli,S. aureus,V. parahemolyticus, andT. mentagrophytes. Amazingly, E was stronger than perilla aldehyde againstS. typhimurium,. The cytotoxicity test indicated Gpl(E) was more toxic than Rpl(E) and the pl(E)s were more toxic than pl(w)s. Conversely, the pl(w)s showed stronger TNF-α suppressing activity than pl(E)s. The pentane subfractions were entirely ineffective. Conclusively, the Perilla EOs contain huge amount of polyphenoilcs, the Es exhibit the rather good antimicrobial and cytotoxic effects, while the pl(w)s possess rather promising anti-inflammatory effect, underlying the promising antimicrobial and antiinflammtory effects of perilla leaves. [ABSTRACT FROM AUTHOR]

A phytochemical investigation on the 5-lipoxygenase (5-LOX) inhibitory methanolic extract of Rudbeckia hirta L. flowers yielded 10 phenolic metabolites, including three phenolic acids, two phenolic acid esters, four flavonol glycosides and a trimethylated flavonol. The structures of the isolated metabolites were determined on the basis of spectroscopic analyses and by comparison with the literature data. Seven of these metabolites were isolated for the first time from the genus Rudbeckia. The in vitro 5-LOX inhibitory, immunomodulatory and antioxidant (oxygen radical absorbance capacity) activities of the isolated compounds were evaluated, and the results provided a new scientific evidence for the ethnopharmacological use of the herb in inflammatory conditions. [ABSTRACT FROM AUTHOR]

Context: Cyclophosphamide (CP) causes lung injury in rats through its ability to generate free radicals with subsequent epithelial and endothelial cell damage. Objective: This study was conducted to assess whether allicin can ameliorate CP-induced early lung injury in rats. Materials and methods: Male Sprague Dawely rats were divided into four groups. Group I was the control group. Group II received allicin (50 mg/kg/d, p.o.) for 14 consecutive days. Group III was injected once with CP (150 mg/kg, i.p.). Group IV received allicin for seven consecutive days, before and after CP injection (150 mg/kg, i.p.). The parameters of study were serum biomarkers, lung tissue antioxidant profile and histopathological changes in lung tissue. Results: A single intraperitoneal injection of CP markedly altered the levels of several biomarkers in lung homogenates. Significant increases in lung content of lipid hydroperoxides were seen that paralleled the decreased levels of total reduced glutathione. Superoxide dismutase activity (SOD) was significantly increased. CP increased the level of serum biomarkers; total protein, lactate dehydrogenase (LDH) and tumor necrosis factor-alpha (TNF-α). Pretreatment of rats daily with oral allicin seven days prior to and seven days after CP inject significantly inhibited the development of lung injury, prevented the alterations in lung and serum biomarkers associated with inflammatory reactions, with less lipid peroxidation (LP) and restoration of antioxidants. Moreover, allicin attenuated the secretion of proinflammatory cytokine, TNF-α expression in rat serum. In addition, allicin effectively blunted CP-induced histopathological changes in lung tissue. Discussion and conclusion: Our results suggest that allicin is efficient in blunting CP-induced pulmonary damage. [ABSTRACT FROM AUTHOR]

Many algal species contain relatively high concentrations of polysaccharide substances, a number of which have been shown to have anti-inflammatory and/or immunomodulatory activity. In this study, we evaluated the anti-inflammatory and antinociceptive effects in mice of a sulfated polysaccharide fraction (PLS) extracted from the algae Gracilaria caudata. The antiinflammatory activity of PLS was evaluated using several inflammatory agents (carrageenan, dextran, bradykinin, and histamine) to induce paw edema and peritonitis in Swiss mice. Samples of the paw tissue and peritoneal fluid were removed to determine myeloperoxidase (MPO) activity or TNF-α and IL-1β levels, respectively. Mechanical hypernociception was induced by subcutaneous injection of carrageenan into the plantar surface of the paw. Pretreatment of mice by intraperitoneal administration of PLS (2.5, 5, and 10 mg/kg) significantly and dose-dependently reduced carrageenan-induced paw edema ( p < 0.05) compared to vehicle-treated mice. Similarly, PLS 10 mg/kg effectively inhibited edema induced by dextran and histamine; however, edema induced by bradykinin was unaffected by PLS. PLS 10 mg/kg inhibited total and differential peritoneal leukocyte counts following carrageenan-induced peritonitis. Furthermore, PLS reduced carrageenan-increased MPO activity in paws and reduced cytokine levels in the peritoneal cavity. Finally PLS pretreatment also reduced hypernociception 3-4 h after carrageenan. We conclude that PLS reduces the inflammatory response and hypernociception in mice by reducing neutrophil migration and cytokines concentration. [ABSTRACT FROM AUTHOR]

Context: Medicinal plants are a largely unexplored source of drug repository. Urtica dioica L. (Urticaceae) is used in traditional medicine to treat diverse conditions. Objective: The present study describes the antidiabetic, antiinflammatory, antibacterial activity, and toxicological studies of Urtica dioica. Materials and methods: U. dioica leaves were subjected to solvent extraction with hexane, chloroform, ethyl acetate, methanol, and aqueous, respectively, and screened for antidiabetic (300 mg/kg bw by glucose tolerance test; GTT), antiinflammatory (200 mg/kg bw by rat paw edema assay) and antibacterial activities [by disc-diffusion and minimum inhibitory concentration (MIC) assays]. Toxicological studies were carried on Artemia salina and Wistar rats; phytochemical analyses were carried out, using chromatographic and spectroscopic techniques. Results: The aqueous extract of U. dioica ( AEUD) significantly ( p < 0.001; 67.92%) reduced the blood glucose level during GTT in Wistar rats with an effective dose of 300 mg/kg bw in dose-dependent studies. High-performance liquid chromatography with photodiode-array detection (HPLC-DAD) analysis showed the presence of hydroxycinnamic acid derivatives and flavonoids in AEUD. Hexane Fraction-2 (HF2) exhibited both antiinflammatory activity (48.83% after 3 h), comparable to that of indomethacin (53.48%), and potent antibacterial activity with MIC values ranging from 31.25-250 µg/mL against all the tested strains. Gas chromatography-mass spectrometry (GC-MS) analysis showed fatty acid esters and terpenes as the major constituents of HF2. Toxicity tests showed higher safety margin of all the solvent extracts with LC50 > 1000 μg/mL each on A. salina. Discussion and conclusion: Our results showed that the U. dioica leaves are an interesting source of bioactive compounds, justifying their use in folk medicine, to treat various diseases. [ABSTRACT FROM AUTHOR]

Spices and aromatic herbs have been used since antiquity as preservatives, colorants, and flavor enhancers. Spices, which have long been the basis of traditional medicine in many countries, have also been the subject of study, particularly by the chemical, pharmaceutical, and food industries, because of their potential use for improving health. Both in vitro and in vivo studies have demonstrated how these substances act as antioxidants, digestive stimulants, and hypolipidemics and show antibacterial, anti-inflammatory, antiviral, and anticancerigenic activities. These beneficial physiological effects may also have possible preventative applications in a variety of pathologies. The aim of this review is to present an overview of the potential of spices and aromatic herbs as functional foods. [ABSTRACT FROM AUTHOR]

1. The purpose was to investigate whether the pharmacokinetics and pharmacodynamics of prednisolone in the non-human primate was an appropriate surrogate for man. 2. After single intravenous doses of 0.03, 0.3, and 3 mg kg-1, prednisolone demonstrated a dose-dependent clearance and volume of distribution. When corrected for concentration-dependent protein binding, the free clearance was linear at the tested dose levels. The protein binding-corrected volume of distribution was similar across doses. The serum half-life was estimated as being between 2 and 4 h. Prednisolone exhibits near complete inhibition of the cytokines TNF-α, IL-1β, IL-6 and IL-8 with very similar IC50 estimates from 0.09 to 0.16 μg ml-1 (from 0.24 to 0.44 μM). 3. The monkey demonstrated a similar pharmacokinetics-pharmacodynamics profile of prednisolone when compared with man (from the literature). [ABSTRACT FROM AUTHOR]

Promising antiinflammatory activity together with low ulcerogenic properties of some Michael addition products of thiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones which have been synthesized in our previous study, prompted us to investigate their antioxidant properties. Since compound Ib has both antioxidant and antiinflammatory activities beside the lowest ulcerogenic incidence, it was selected for investigation of its inhibitory effect on various cyclooxygenase ezymes. It was found that while it did not inhibit cyclooxygenase-1 (COX-1) enzyme, there was a small inhibitory effect (17%) on COX-2 enzyme. We concluded that the diminished harmful effects on the stomach of this novel antiinflammatory compound were related to its antioxidant properties since it is ineffective on COX-1 enzyme. In conclusion, the compounds having both antioxidant and antiinflammatory activities with a lack of COX-1 enzyme inhibitory effect may improve the gastrointestinal safety profile of such compounds. [ABSTRACT FROM AUTHOR]

Despite marked improvements in the treatment of diabetes and its retinal complications, diabetic retinopathy remains a leading cause of blindness and vision impairment in working-age adults. Control of blood glucose and blood pressure will remain important means to prevent the onset and progression of diabetic retinopathy. Current and improved surgical treatments, such as laser therapy and vitrectomy, have also proved highly effective in preventing major visual loss in advanced stages of retinopathy. In this review, emerging drug-based therapies (corticosteroids, somatostatin analogues, anti-VEGF agents, a specific PKCβ1/2 inhibitor [ruboxistaurin]), more effective inhibitors of aldose reductase, inhibitors of the renin-angiotensin system and anti-inflammatory agents that could help to preserve sight in the growing population of diabetic patients into the 21st Century are discussed. [ABSTRACT FROM AUTHOR]

Echinacea is one of the most popular herbs in modem Europe and United States marketplaces. Unfortunately, most of the Echinacea consumed is misused, based on its misrepresentation as an effective cold and flu remedy. Throughout the later part of the nineteenth century and the first thirty years of the twentieth century, Echinacea was the preferred treatment for infections. The introduction of antibiotics resulted in the eclipse of Echinacea, along with the professional medical doctors, known as the "Eclectics," who based their treatment on the use of herbs. [ABSTRACT FROM AUTHOR]

The petroleum ether, ethyl acetate, and methanol extracts of Phyllanthus reticulatus Poir. (Euphorbiaceae) were chosen for pharmacological screening. In the acetic acid-induced writhing test, the ethyl acetate extract in doses of 150 and 300 mg/kg showed 51.23 and 65.12% inhibition of writhing, respectively. A significant elongation of tail-flick time was evident both in the ethyl acetate and the methanol extracts (42.38 and 60.49%) only at the 300 mg/kg dose level. In carrageenan-induced rat paw edema model, the methanol extract at the 300 mg/kg dose level showed 40.03% inhibition of edema at the end of 4 h. These results demonstrated that the extracts of P. reticulatus possess significant analgesic and anti-inflammatory properties. [ABSTRACT FROM AUTHOR]

Some new 3',5'-substituted-5H,3'H-spirodibenzo[a, d]cycloheptene-5,2'-[1,3,4]thiadiazole and 10,11-dihydro-5H,3' H-spirodibenzo[a, d]cycloheptene-5,2'-[1,3,4]thiadiazole derivatives 3a-n were regioselectively synthesized under 1,3-dipolar cycloaddition of 5-thiooxo-5H-dibenzo[a, d]cyclo-heptene and 5-thiooxo-10,11-dihydro-5H-dibenzo[a, d]cycloheptene with a variety of nitrilimines (generated in situ via dehydrohalogenation of the corresponding hydrazonoyl chlorides in the presence of triethylamine). The new products were tested for antiinflammatory, analgesic, and ulcerogenic score activities comparable to Indomethacin. Compounds 3i-l showed significant activity compared to Indomethacin. [ABSTRACT FROM AUTHOR]

The ethanol extract of Achillea nobilis L. subsp. neilreichii (Kerner) Formanék (Asteraceae) flower heads was investigated for its antinociceptive and anti-inflammatory activities and for acute toxicity in mice and rats. While the extract exhibited an antinociceptive effect during the late phase of the formalin test (100, 200, and 400 mg/kg, i.p.) and an anti-inflammatory effect in the paw edema test (100 and 200 mg/kg, i.p.), it did not exert any significant antinociceptive effect in the tail-flick test. Furthermore, administration of 400 mg/kg extract increased the latency to hot-plate test at 60 and 90 min. No significant change was detected in sensory motor performance. The acute LC50 value of the extract was 4456 mg/kg (i.p.) in mice. The current results demonstrate that an ethanol extract of A. nobilis L. subsp. neilreichii exerts anti-inflammatory activity. [ABSTRACT FROM AUTHOR]

The antiinflammatory activity of 22 plants used in folk medicine, or indigenous in the United Arab Emirates, was tested using the carrageenan-induced rat paw edema method. Three plants (Citrullus colocynthis, Hammada elegans and Rhazya stricta) showed such activity. Activity-guided fractionation of Hammada elegans extract led to the isolation of a single active compound which was identified as piperidine hydrochloride. Citrullus colocynthis-m^aced antiinflammatory activity may by due to loss of body water. [ABSTRACT FROM AUTHOR]

IL-1 cytokines are mainly responsible for controlling a series of pro-inflammatory reactions induced in response to pathogen mediated tissue injury. Among the IL-1 cytokine family, IL-1 β results in upregulation of genes responsible for boosting immune system reactivity and inflammatory response. With growing pathophysiological relevance of IL-1β in a myriad of disease pathogenesis, new biological drugs have been developed in recent years. One such drug, Canakinumab, targeting IL-1β has been recently approved for clinical use. The recent results from the CANTOS (Canakinumab Anti-Inflammatory Thrombosis Outcome Study) trial are encouraging in this aspect. The results suggest that anti-inflammatory therapy using canakinumab at a dose of 150 mg every 3 months led to significantly lower recurrent cardiovascular events than the placebo drug. These results were independent of lipid-lowering effects of these drugs. If the results are widely applicable, the CANTOS trial would reaffirm the hypothesis of atherothrombosis due to inflammation, hence supporting the need for a cytokine-based therapy for the secondary prevention of cardiovascular diseases. Moreover, the potential benefits of the phenomenal reduction in the inflammatory cascade induced by canakinumab should be carefully balanced against its long-term safety profile which is yet unknown. However, the inflammatory hypothesis of atherothrombosis supports a cytokine-based therapy for the secondary prevention of cardiovascular disease. Furthermore, the potential benefits from the reduction in inflammatory markers induced by canakinumab should be carefully balanced against its unknown long-term safety profile. [ABSTRACT FROM AUTHOR]