Anti‐inflammatory activity of Rhodiola rosea – “a second‐generation adaptogen”

Rhodiola rosea (golden root), a unique phytoadaptogen grown in high‐altitude regions has gained attention for its various therapeutic properties. In India, this plant is found in the Himalayan belt and has not been completely explored for its beneficial health effects. The present study was undertaken to evaluate the anti‐inflammatory efficacy of the tincture extract of Rhodiola rosea roots (RTE). The anti‐inflammatory activity was determined through carrageenan‐induced paw oedema, formaldehyde‐induced arthritis and nystatin‐induced paw oedema in rat model. The tincture extract exhibited inhibitory effect against acute and subacute inflammation at a dose of 250 mg/kg body weight. Inhibition of nystatin‐induced oedema was also observed in a dose‐dependent manner. The in vitro inhibitory effects of the tincture extract from R. rosea roots was evaluated against the enzymes relating to inflammation. The enzymes include cyclooxygenase‐1 (COX‐1), cyclooxygenase‐2 (COX‐2) and Phospholipase A₂ (PLA₂). The extract showed varying inhibitory activities against these enzymes depending on the concentrations. A potent inhibition was observed against Cox‐2 and PLA₂. Inhibition of nystatin induced oedema and phospholipase A₂ suggested that membrane stabilization could be the most probable mechanism of action of RTE in anti‐inflammation. The findings in this study may provide the use of R. rosea root extract in the treatment of inflammatory conditions. Copyright © 2009 John Wiley & Sons, Ltd.     

Prophylactic and Therapeutic Effects of Acanthopanax senticosus Harms Extract on Murine Collagen‐induced Arthritis

Evidences are accumulating that extract of Acanthopanax senticosus Harms (ASH; syn Eleutherococcus senticosus [Rupr. & Maxim.] Maxim), a shrub native to Northeastern Asia, has antiinflammatory effects. In this study, we examined prophylactic and therapeutic effects of ASH extract (ASHE) on rheumatoid arthritis using collagen‐induced arthritis (CIA) mouse model. Acanthopanax senticosus Harms extract was administered before the onset of arthritis in the prophylaxis model. In the therapeutic model, ASHE was administered after the onset of arthritis with or without anti‐TNF‐α antibody. The ASHE treatment showed efficacy before onset of CIA but there was no effect after CIA was established. The ASHE treatment delayed the onset and decreased severity of CIA. In vitro examinations showed that ASHE is an antioxidant and that ASHE suppresses TNF‐α and interleukin‐6 production in human peripheral blood mononuclear cells. The combination therapy with ASHE and anti‐TNF‐α antibody reduced the severity of arthritis compared with anti‐TNF‐α antibody alone. The present study shows that ASHE has prophylactic effect against CIA and support therapeutic effect of anti‐TNF‐α antibody. © 2014 The Authors. Phytotherapy Research published by John Wiley & Sons Ltd.     

Aqueous Extract of Rosmarinus officinalis L. Inhibits Neutrophil Influx and Cytokine Secretion

Rosmarinus officinalis L. phenolic compounds have attracted considerable attention because of their antioxidant and antimicrobial properties, including its ability to treat inflammatory disorders. In this work, we investigated the in vivo and in vitro effects of R. officinalis aqueous extract on neutrophil trafficking from the blood into an inflamed tissue, on cell‐derived secretion of chemical mediators, and on oxidative stress. Anti‐inflammatory activity was investigated using carrageenan‐induced inflammation in the subcutaneous tissue of male Wistar rats orally treated with the R. officinalis extract (100, 200, or 400 mg/kg). The leukocyte influx (optical microscopy), secretion of chemical mediators (prostaglandin E2 (PGE2), TNF‐α, interleukin 6 (IL‐6), leukotriene B4 (LTB4), and cytokine‐induced neutrophil chemoattractant 1 by enzyme‐linked immunosorbent assay), and the anti‐oxidative profile (super oxide dismutase (SOD), glutathione peroxidase, and thiobarbituric acid reactive substance (TBARS) spectrophotometry) were quantified in the inflamed exudate. N‐Formyl‐methionine‐leucine‐phenylalanine‐induced chemotaxis, lipopolysaccharide‐induced NO₂^? production (Greiss reaction), and adhesion molecule expression (flow cytometry) were in vitro quantified using oyster glycogen recruited peritoneal neutrophils previous treated with the extract (1, 10, or 100 µg/mL). Animals orally treated with phosphate‐buffered saline and neutrophils incubated with Hank's balanced salt solution were used as control. R. officinalis extract oral treatment caused a dose‐dependent reduction in the neutrophil migration as well as decreased SOD, TBARS, LTB4, PGE2, IL‐6, and TNF‐α levels in the inflamed exudate. In vitro treatment with R. officinalis decreased neutrophil chemotaxis, NO₂^? production, and shedding of L‐selectin and β2 integrin expressions. Results here presented show that R. officinalis aqueous extract displays important in vivo and in vitro anti‐inflammatory actions by blocking pathways of neutrophil migration and secretion, suggesting its therapeutic application to acute inflammatory reactions. Copyright © 2014 John Wiley & Sons, Ltd.     

Isolation of Anti‐Inflammatory Fractions and Compounds from the Root of Astragalus membranaceus

Foot ulceration, if not treated properly, will eventually result in amputation. Inflammation may impede the wound healing process if not properly controlled. The root of Astragalus membranaceus (AR) is one of the Chinese herbs commonly found in Chinese herbal formulae used for treating foot ulcer. In this study, we aimed to identify the active fractions and/or compounds from AR aqueous extract, which are responsible for the anti‐inflammatory effect using in vitro bioassay‐guided fractionation. The anti‐inflammatory effect was monitored by the inhibition of nitric oxide (NO) released from lipopolysaccharide‐stimulated mouse macrophage RAW 264.7 cells after treated with AR aqueous extract or its fractions and isolated components. Two major active fractions (P2‐3‐2‐2‐2 and P2‐3‐2‐2‐3) were found to significantly inhibit NO production at 0.156 mg/mL (p < 0.01). In addition, three chemical components (formononetin, calycosin and astragaloside IV) were successfully isolated from P2‐3‐2‐2‐3. Only formononetin could significantly inhibit NO production (p < 0.01), whereas the other two components had no significant effects at concentrations ranging from 0.039 to 0.156 mg/mL. In conclusion, two major anti‐inflammatory active fractions that may enhance wound healing were identified, and formononetin was one of the active ingredients in the active fractions. Copyright © 2012 John Wiley & Sons, Ltd.     

The anti‐hepatitis B virus therapeutic potential of anthraquinones derived from Aloe vera

Although the approved hepatitis B virus (HBV)‐polymerase inhibitors (e.g., lamivudine) often lead to drug‐resistance, several natural products have shown promising efficacies. Though Aloe vera (AV) gel and its constituents are shown inhibitors of many viruses, their anti‐HBV activity still remains elusive. We therefore, tested the anti‐HBV potential of AV extract and its anthraquinones in hepatoma cells, including molecular docking, high‐performance thin layer chromatography (HPTLC), and cytochrome P450 (CYP3A4) activation analyses. Our anti‐HBV assays (HBsAg/HBeAg Elisa) showed maximal inhibition of viral antigens production by aloe‐emodin (~83%) > chrysophanol (~62%) > aloin B (~61%) > AV extract (~37%) in HepG2.2.15 cells. Interestingly, the effect of aloe‐emodin was comparable with lamivudine (~86%). Moreover, sequential treatment with lamivudine (pulse) followed by aloe‐emodin (chase) enhanced the efficacy of monotherapy by ~12%. Docking (AutoDock Vina) of the anthraquinones indicated strong interactions with HBV‐polymerase residues that formed stable complexes with high Gibbs's free energy. Further, identification of aloe‐emodin and aloin B by validated HPTLC in AV extract strongly endorsed its anti‐HBV potential. In addition, our luciferase‐reporter gene assay of transfected HepG2 cells showed moderate induction of CYP3A4 by aloe‐emodin. In conclusion, this is the first report on anti‐HBV potential of AV–derived anthraquinones, possibly via HBV‐polymerase inhibition. Of these, although aloin B exhibits novel antiviral effect, aloe‐emodin appears as the most promising anti‐HBV natural drug with CYP3A4 activating property towards its enhanced therapeutic efficacy.     

Anti‐Inflammatory Sesquiterpene Lactones from Lychnophora trichocarpha Spreng. (Brazilian Arnica)

The aerial parts of Lychnophora trichocarpha Spreng. (Asteraceae) are used macerated in water or ethanol to treat inflammation, pain, rheumatism, contusions, bruises and insect bites in Brazilian traditional medicine. In this study, anti‐inflammatory activity of ethanol extract from aerial parts of L. trichocarpha and its ethyl acetate fraction was investigated. Sesquiterpene lactones, lychnopholide (Lyc) and eremantholide C (EreC), isolated of ethyl acetate fraction, were also assayed for in vitro and in vivo anti‐inflammatory activity. Topical treatment with ointments containing ethanol extract, its ethyl acetate fraction and sesquiterpene lactones significantly reduced carrageenan‐induced mice paw oedema. In vitro assays demonstrated that Lyc inhibited interferon ‐γ/lipopolysaccharide ‐stimulated nitric oxide (NO) production in J774A.1 macrophages and increased production of IL‐10 anti‐inflammatory cytokine. The reduction of tumor necrosis factor‐α (TNF‐α) production by EreC was accompanied by an increased production of IL‐10 in a concentration‐dependent manner in J774A.1 macrophages. The anti‐inflammatory effect of Lyc seems to involve the inhibition of production of NO and increased production of IL‐10. The mechanism of the effect of EreC on the reduction of carrageenan‐induced paw oedema may be attributed to inhibition of production of TNF‐α and stimulation of IL‐10 production. The results corroborate the use of ethanol extract from Lychnophora trichocarpha in folk medicine for anti‐inflammatory action and indicate that the topical route is suitable for use. Copyright © 2012 John Wiley & Sons, Ltd.     

Therapeutic effect of Northern Labrador tea extracts for acute myeloid leukemia

Acute myeloid leukemia (AML) is an aggressive hematological malignancy that is one of the more common pediatric malignancies in addition to occurring with high incidence in the aging population. Unfortunately, these patient groups are quite sensitive to toxicity from chemotherapy. Northern Labrador tea, or Rhododendron tomentosum Harmaja (a.k.a. Ledum palustre subsp. decumbens) or “tundra tea,” is a noteworthy medicinal plant used by indigenous peoples in Alaska, Canada, and Greenland to treat a diversity of ailments. However, laboratory investigations of Northern Labrador tea, and other Labrador tea family members, as botanical sources for anticancer compounds have been limited. Utilizing an AML cell line in both in vitro and in vivo studies, as well as in vitro studies using primary human AML patient samples, this study demonstrated for the first time that Northern Labrador tea extracts can exert anti‐AML activity and that this may be attributed to ursolic acid as a constituent component. Therefore, this medicinal herb holds the potential to serve as a source for further drug discovery efforts to isolate novel anti‐AML compounds.     

Anti‐inflammatory Activities of Eleven Centaurea Species Occurring in the Carpathian Basin

Our study aimed at the identification of anti‐inflammatory activities of different fractions of C. sadleriana extract after per os administration in rats, the identification of the active compounds of the plant and the investigation of the in vitro anti‐inflammatory activities of Centaurea species native to or cultivated in the Carpathian Basin. The aerial parts of Centaurea sadleriana Janka have been used in Hungarian folk medicine to treat the wounds of sheep. Methanol extract of C. sadleriana was fractioned by solvent‐solvent partitioning. The n‐hexane fraction was further fractionated and the anti‐inflammatory activities of certain subfractions were confirmed in vivo in rats. The n‐hexane and chloroform fraction of the methanol extract of C. sadleriana exhibited remarkable COX‐1 and COX‐2 inhibiting effects in vitro. Chromatographic separation of the fractions led to the identification of the active subfractions and 11 compounds (α‐linolenic acid, γ‐linolenic acid, stigmasterol, β‐sitosterol, campesterol, vanillin, pectolinarigenin, salvigenin, hispidulin, chrysoeriol and apigenin). The in vitro screening for anti‐inflammatory activities of further Centaurea species occurring in the Carpathian Basin (C. adjarica, C. bracteata, C. cataonica, C. cynaroides, C. dealbata, C. indurata, C. macrocephala, C. melitensis, C. nigrescens, C. ruthenica) revealed considerable COX‐1 and COX‐2 inhibitory activities. Because C. sadleriana is an endangered species native only to the Carpathian Basin, the investigation of more prevalent species is reasonable. Copyright © 2012 John Wiley & Sons, Ltd.     

Anti‐Angiogenic Activity of Herba Epimedii on Zebrafish Embryos In Vivo and HUVECs In Vitro

Herba Epimedii, an herb commonly used in East Asian medicine, is commonly used for treatment of impotence, osteoporosis and many inflammatory conditions in traditional Chinese medicine. Recent studies revealed that Herba Epimedii also has anti‐tumor or anti‐cancer activities, which may possibly be mediated through anti‐angiogenesis. This study aims to examine and confirm the anti‐angiogenic activity in the herb using both in vivo and in vitro approaches. The 95% ethanol extract and four subsequent fractions (n‐hexane, ethyl acetate (EA), n‐butanol and aqueous fractions) of Herba Epimedii were tested on the zebrafish model by the quantitative assay for endogenous alkaline phosphatase; then, the active fraction was further tested on Tg(fli1a:EGFP)y1 zebrafish embryos and human umbilical vein endothelial cells (HUVECs) for the anti‐angiogenic effects. In addition, the action mechanism of Herba Epimedii was further investigated on wild‐type zebrafish embryos and HUVECs. The EA fraction showed anti‐angiogenic effects in both in vivo and in vitro models. Further experiments demonstrated that it might affect angiogenesis by acting on multiple molecular targets in zebrafish embryos and ERK signaling pathway in HUVECs. In conclusion, Herba Epimedii can inhibit angiogenesis, which may be the mechanism for its anti‐inflammatory, anti‐tumor and anti‐cancer actions. Copyright © 2012 John Wiley & Sons, Ltd.     

Phenolic‐Linked Biochemical Rationale for the Anti‐Diabetic Properties of Swertia chirayita (Roxb. ex Flem.) Karst.

The crude extract of Swertia chirayita, an important medicinal plant of Nepal, is locally used for many diseases including type 2 diabetes. In this study, crude aqueous and 12% ethanol solution extracts of S. chirayita collected from nine districts of Nepal were analyzed for anti‐diabetic‐linked anti‐hyperglycemia potential using in vitro biochemical assays. There was moderate‐to‐high positive correlation between antioxidant activity and total phenolic content of both extracts and moderate‐to‐high α‐glucosidase inhibitory activity. Although the anti‐diabetic property of S. chirayita is mainly attributed to the phytochemical swerchirin present in its hexane fraction, we propose that the crude extract of this plant used in local healing also has anti‐hyperglycemia potential. The crude extracts indicated the presence of three main phytochemicals mainly mangiferin, swertiamarin, and amarogentin and their derivatives. Among the standard compounds (mangiferin, swertiamarin, and amarogentin), mangiferin showed α‐glucosidase and 2,2‐diphenyl‐1‐picrylhydrazyl radical inhibitory activity indicating anti‐hyperglycemia potential. Copyright © 2012 John Wiley & Sons, Ltd.     

Pycnogenol® inhibits immunoglobulin E‐mediated allergic response in mast cells

IgE‐dependent mast cell activation is known to be associated with the allergic diseases. Pycnogenol^® (PYC) is a standardized extract of the bark of French maritime pine containing bioflavonoids with a potent antioxidant activity. The antiallergic activity of PYC was evaluated using both in vivo and in vitro experimental models. Oral administration of PYC significantly inhibited anti‐dinitrophenyl (DNP) IgE‐mediated passive cutaneous anaphylaxis in rats. In an in vitro study, PYC dose‐dependently reduced histamine release from rat peritoneal mast cells (RPMC) triggered by anti‐DNP IgE. PYC inhibited the protein expression and secretion of tumor necrosis factor‐α and interleukin‐6 in anti‐DNP IgE‐stimulated RPMC. Moreover, PYC decreased anti‐DNP IgE‐induced calcium uptake into RPMC. Furthermore, PYC suppressed nuclear factor‐kappa B activation. From these results, the clinical use of PYC in the mast cell‐mediated immediate‐type allergic diseases is proposed. Copyright © 2009 John Wiley & Sons, Ltd.     

Inhibition of Prostaglandin D2 Production by Trihydroxy Fatty Acids Isolated from Ulmus davidiana var. japonica

The stem and root barks of Ulmus davidiana var. japonica (Ulmaceae) have been used to treat inflammatory diseases including mastitis, rhinitis, sinusitis, and enteritis. In an ongoing study focused on the discovery of natural anti‐inflammatory compounds from natural products, a methanol extract of the stem and root barks of U. davidiana var. japonica showed anti‐inflammatory activities. Activity‐guided fractionation of the methanol extract yielded a new trihydroxy fatty acid, 9,12,13‐trihydroxyoctadeca‐10(Z),15(Z)‐dienoic acid (1), and a known compound, pinellic acid (2). These two trihydroxy fatty acids 1 and 2 inhibited prostaglandin D₂ production with IC₅₀ values of 25.8 and 40.8 μM, respectively. These results suggest that 9,12,13‐trihydroxyoctadeca‐10(Z),15(Z)‐dienoic acid (1) and pinellic acid (2) are among the anti‐inflammatory principles in this medicinal plant. Copyright © 2012 John Wiley & Sons, Ltd.     

Diarylheptanoids Rich Fraction of Alnus nepalensis Attenuates Malaria Pathogenesis: In‐vitro and In‐vivo Study

Diarylheptanoids from Alnus nepalensis leaves have been reported for promising activity against filariasis, a mosquito‐borne disease, and this has prompted us to investigate its anti‐malarial and safety profile using in‐vitro and in‐vivo bioassays. A. nepalensis leaf extracts were tested in‐vitro against chloroquine‐sensitive Plasmodium falciparum NF54 by measuring the parasite specific lactate dehydrogenase activity. Among all, the chloroform extract (ANC) has shown promising anti‐plasmodial activity (IC₅₀ 8.06 ± 0.26 µg/mL). HPLC analysis of ANC showed the presence of diarylheptanoids. Efficacy and safety of ANC were further validated in in‐vivo system using Plasmodium berghei‐induced malaria model and acute oral toxicity in mice. Malaria was induced by intra‐peritoneal injection of P. berghei infected red blood cells to the female Balb/c mice. ANC was administered orally at doses of 100 and 300 mg/kg/day following Peter's 4 day suppression test. Oral administration of ANC showed significant reduction of parasitaemia and increase in mean survival time. It also attributed to inhibition of the parasite induced pro‐inflammatory cytokines as well as afford to significant increase in the blood glucose and haemoglobin level when compared with vehicle‐treated infected mice. In‐vivo safety evaluation study revealed that ANC is non‐toxic at higher concentration. Copyright © 2016 John Wiley & Sons, Ltd.     

Spirulina extract enriched for Braun‐type lipoprotein (Immulina®) for inhibition of 4T1 breast tumors' growth and metastasis

Spirulina platensis extracts have exhibited considerable anti‐cancer effects. To investigate the efficacy of the Spirulina extract enriched for Braun‐type lipoprotein (Immulina®) for breast cancer treatment, 4T1 breast tumor‐bearing mice were treated with 40 mg/kg Immulina® daily and the tumors' growth and metastasis were assessed. Also, CD4, CD8, and CD56 staining were performed to investigate the Immulina® effect on the immune cells' recruitment to the tumors by immunohistochemistry. Immulina® could significantly (P < 0.001) inhibit 4T1 breast tumors' growth. Immulina®‐treated group exhibited a 63% decrease in the tumors' volume in comparison with control (P < 0.001). Also, Immulina® could significantly (P < 0.001) decrease metastatic burden at the vital organs as 68% and 61% decrease in the liver and lungs metastatic colonies were observed, respectively. Also, Immulina® could increase mean survival time of the tumor‐bearing mice for 29 days. The Spirulina‐treated mice tumors contained significantly more infiltrated NK, CD4+, and CD8+ T lymphocytes in comparison with control. Taking together, Immulina® can be a safe anti‐cancer supplement with the ability to cause direct apoptosis to the cancer cells and activate the immune system against tumor. This supplement with natural origin seems to have bright future to help breast cancer patients.     

Ginger's (Zingiber officinale Roscoe) inhibition of rat colonic adenocarcinoma cells proliferation and angiogenesis in vitro

Ginger's (Zingiber officinale Roscoe) natural bioactives, specifically ginger extract and 6‐gingerol, were measured for their in vitro inhibition of two key aspects of colon cancer biology – cancer cell proliferation and angiogenic potential of endothelial cell tubule formation. Ginger extract was obtained via column distillation, while the 6‐gingerol was purchased from Calbiochem. Antiproliferation activity was assessed through tritiated thymidine ([³H]Tdr) incorporation studies of YYT colon cancer cells; the anti‐angiogenic ability of gingerol was assessed by a Matrigel assays using MS1 endothelial cells. These selected ginger bioactives had: 1) a direct effect on YYT rat cancer cell proliferation (6–1.5% ginger extract; 100–4 µM 6‐gingerol); 2) an indirect effect on MS1 endothelial cell function either at the level of endothelial cell proliferation or through inhibition of MS1 endothelial cell tube formation (100–0.8 µM). Compound 6‐gingerol was most effective at lower doses in inhibiting endothelial cell tube formation. These in vitro studies show that 6‐gingerol has two types of antitumor effects: 1) direct colon cancer cell growth suppression, and 2) inhibition of the blood supply of the tumor via angiogenesis. Further research is warranted to test 6‐gingerol in animal studies as a potential anticancer plant bioactive in the complementary treatment of cancer. Copyright © 2008 John Wiley & Sons, Ltd.     

Protective Effects of Turbinaria ornata and Padina pavonia against Azoxymethane‐Induced Colon Carcinogenesis through Modulation of PPAR Gamma,NF‐κB and Oxidative Stress

The aim of this study was to investigate the antiproliferative and protective effects of the brown seaweeds, Turbinaria ornata and Padina pavonia, against azoxymethane (AOM)‐induced colon carcinogenesis in mice. Both algal extracts showed anti‐proliferative effects on the human carcinoma cell line HCT‐116 in vitro, with T. ornata demonstrating a more potent effect. Male albino Swiss mice received intraperitoneal injections of AOM (10 mg/kg) once a week for two consecutive weeks and 100 mg/kg of either T. ornata or P. pavonia extracts. AOM‐induced mice exhibited alterations in the histological structure of the colon, elevated lipid peroxidation and nitric oxide, declined glutathione content and reduced activity of superoxide dismutase and glutathione peroxidase. In addition, AOM induced downregulation of peroxisome proliferator activated receptor gamma (PPARγ) and p53 mRNA expression, with concomitant upregulation of nuclear factor‐kappa B (NF‐κB) in colon tissue. Administration of either algal extract markedly alleviated the recorded alterations. In conclusion, the current study suggests that T. ornata and P. pavonia, through their antioxidant and anti‐inflammatory effects, are able to attenuate colon inflammation by downregulating NF‐κB expression. Furthermore, the protective effects of both algae against AOM‐initiated carcinogenesis were attributed, at least in part, to their ability to upregulate colonic PPARγ and p53 expression. Copyright © 2015 John Wiley & Sons, Ltd.     

In Vitro Inhibition of the Transcription Factor NF‐κB and Cyclooxygenase by Bamboo Extracts

Several bamboo species have been used in traditional medicine for the treatment of inflammatory conditions. The present study evaluates the in vitro anti‐inflammatory properties of the traditionally used bamboo species Phyllostachys nigra (Lodd.) Munro and Sasa veitchii (Carr.) Rehder to explore their future research opportunities and therapeutic potential as anti‐inflammatory agents. The extracts were evaluated for their potential inhibitory activity at the level of NF‐κB‐induced gene expression and suppression of cyclooxygenase (COX)‐1 and COX‐2 enzyme activities, representative pharmacological targets for the anti‐inflammatory action of glucocorticoids and non‐steroidal anti‐inflammatory drugs, respectively. The activity of P. nigra (Lodd.) Munro and S. veitchii (Carr.) Rehder was compared with bamboo species without traditional anti‐inflammatory indications. High‐performance liquid chromatography with diode‐array detection and liquid chromatography–tandem mass spectrometry analyses were performed to phytochemically characterize the extracts. P. nigra (Lodd.) Munro leaf extract potently inhibited NF‐κB‐induced gene expression, while S. veitchii (Carr.) Rehder leaf extract exerted a selective COX‐2 inhibition. The crude extracts consistently showed a more potent bioactivity than the solid phase extraction fractions. P. nigra (Lodd.) Munro and S. veitchii (Carr.) Rehder both exert anti‐inflammatory properties, but act via a different molecular mechanism. Copyright © 2013 John Wiley & Sons, Ltd.     

Boswellia frereana (frankincense) suppresses cytokine‐induced matrix metalloproteinase expression and production of pro‐inflammatory molecules in articular cartilage

The aim of this study was to assess the anti‐inflammatory efficacy of Boswellia frereana extracts in an in vitro model of cartilage degeneration and determine its potential as a therapy for treating osteoarthritis. Cartilage degradation was induced in vitro by treating explants with 5 ng/ml interleukin1α (IL‐1α) and 10 ng/ml oncostatin M (OSM) over a 28‐day period, in the presence or absence of 100 μg/ml B. frereana. Treatment of IL‐1α/OSM stimulated cartilage explants with B. frereana inhibited the breakdown of the collagenous matrix. B. frereana reduced MMP9 and MMP13 mRNA levels, inhibited MMP9 expression and activation, and significantly reduced the production of nitrite (stable end product of nitric oxide), prostaglandin E2 and cycloxygenase‐2. Epi‐lupeol was identified as the principal constituent of B. frereana. This is the first report on the novel anti‐inflammatory properties of Boswellia frereana in an in vitro model of cartilage degradation. We have demonstrated that B. frereana prevents collagen degradation, and inhibits the production of pro‐inflammatory mediators and MMPs. Due to its efficacy we propose that B. frereana should be examined further as a potential therapeutic agent for treating inflammatory symptoms associated with arthritis. Copyright © 2009 John Wiley & Sons, Ltd.     

Acetonic Extract from the Feijoa sellowiana Berg. Fruit Exerts Antioxidant Properties and Modulates Disaccharidases Activities in Human Intestinal Epithelial Cells

Feijoa sellowiana fruit has been shown to possess various biological activities, such as anti‐bacterial and anti‐cancer properties, in a variety of cellular models, but its activity on human intestinal epithelial cells has never been tested. The purpose of this study was to investigate the effects of the acetonic extract of F. sellowiana fruits on the viability, membrane peroxidation, disaccharidases activities and proliferation of in vitro models of human intestinal epithelial cells. To obtain this goal, Caco‐2 and HT‐29 cells were exposed to the acetonic extract for 24 h. Cell proliferation, viability, lactase and sucrase‐isomaltase activity and H₂O₂‐induced membrane lipid peroxidation were tested. We found that, compared to control conditions, the acetonic extract significantly increased lactase and sucrase‐isomaltase activity in Caco‐2, but not HT‐29, cells, decreased proliferation, had no effects on viability and restored lipid peroxidation in both cell models. This study suggests that the acetonic extract improves lactase and sucrase‐isomaltase activity, inhibits cell proliferation, have no cytotoxic effects and prevent lipid peroxidation of intestinal epithelial cells. These effects may be exploited in case of disaccharidases deficit and also as an adjuvant treatment of diseases related to oxidative stress. Copyright © 2016 John Wiley & Sons, Ltd.