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J Ethnopharmacol [journal]
- Hispolon inhibition of inflammatory apoptosis through reduction of iNOS/NO production via HO-1 induction in macrophages. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 13.
Phellinus linteus (Berkeley & Curtis), a well-known medical fungus, has long been used as a traditional medicine in Oriental countries to treat various diseases, and hispolon (HIS) is one of its bioactive components. HIS is known to possess potent antineoplastic and antiviral properties; however, its effect on inflammatory apoptosis is still undefined.RAW264.7 macrophages were incubated with HIS for 30min followed by LPS, LTA, or PGN stimulation for 12h. The expression of indicated proteins AP-1 and NF-κB transcriptional activities was examined by Western blotting using specific antibodies. Levels of NO and ROS were examined by Griess reaction, and DCHF-DA staining via flow cytometric analysis, respectively. AP-1 and NF-κB transcriptional activities were detected by luciferase reporter assay. Knockdown of HO-1 protein expression was performed by transfection of macrophages with HO-1 siRNA. Pharmacological inhibitors including ROS scavenger NAC, JNK inhibitor SP600125, NF-κB inhibitor BAY117082 were applied for mechanism study.HIS showed concentration-dependent inhibition of LPS, LTA, and PGN-induced iNOS protein expressions and NO production by RAW264.7 macrophages. Accordingly, HIS protected RAW264.7 cells from LPS-, LTA-, and PGN-induced apoptosis. Increased HO-1 by HIS was detected at both protein and mRNA levels along with an increase in intracellular peroxide, and this was inhibited by the translational inhibitor, cycloheximide (CHX), the transcriptional inhibitor, actinomycin D (Act D), and the reactive oxygen species scavenger, N-acetylcysteine (NAC). A mechanistic study indicated that inhibition of c-Jun N-terminal kinase (JNK) protein phosphorylation, and activator protein (AP)-1 and nuclear factor (NF)-κB activation were involved in the anti-inflammatory actions of HIS in macrophages. A structure-activity relationship analysis showed that HIS expressed the most potent effect of inhibiting iNOS and apoptosis elicited by LPS, LTA, and PGN with a significant increase in HO-1 protein in macrophages.Evidence supporting HIS prevention of inflammatory apoptosis via blocking NO production and inducing HO-1 protein expression in macrophages is provided, and the hydroxyl at position C3 is a critical substitution for the anti-inflammatory actions of HIS.
- Quantification of polyphenols and evaluation of antimicrobial, analgesic and anti-inflammatory activities of aqueous and acetone-water extracts of Libidibia ferrea, Parapiptadenia rigida and Psidium guajava. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 11.
Vast numbers of plant species from northeastern Brazil have not yet been phytochemically or biologically evaluated.The goal of this work was to obtain, characterize and show the antimicrobial, analgesic and anti-inflammatory activities of aqueous and acetone-water extracts of Libidibia ferrea, Parapiptadenia rigida and Psidium guajava.The plant material (100g) was dried, and the crude extracts were obtained by using turbo-extraction (10%; w/v) using water or acetone:water (7:3, v/v) as the extraction solvent. High-performance liquid chromatography (HPLC) methods were used to screen the crude extracts for hydrolysable tannins (gallic acid) and condensed tannins (catechins). The antibacterial activity was evaluated by agar-diffusion and microdilution methods against Gram-positive strains (Staphylococcus aureus ATCC 25923, Staphylococcus epidermidis INCQS 00016, Enterococcus faecalis ATCC 29212 and a clinical isolate of methicillin-resistant S. aureus) as well as Gram-negative strains (Escherichia coli ATCC 25922, Salmonella enteritidis INCQS 00258, Shigella flexneri and Klebsiella pneumoniae). To evaluate the anti-inflammatory activity, a leukocyte migration model was used. Analgesic activity was determined by the hot plate test and the acetic acid-induced abdominal writhing test. Data were analysed by analysis of variance (ANOVA) at a significance level of 5%.P. rigida presented the highest amount of total polyphenols (35.82±0.20%), while the greatest catechin content was found in the acetone-water extract of P. guajava (EAWPg; 1.04μg/g). The largest amounts of catechins were found in the aqueous extract of L. ferrea (EALf; 1.07μg/g) and the acetone-water extract of P. rigida (EAWPr; 1.0μg/g). All extracts showed activity against Gram-positive bacteria. The aqueous and acetone-water extracts of P. guajava showed the greatest inhibition zones in the agar diffusion tests. In the evaluation of the minimum inhibitory concentration (MIC), the most susceptible Gram-positive bacterium was S. epidermidis and the most susceptible Gram-negative bacterium was Shigella flexneri. EAPg and EAWPg showed the greatest MIC values. All extracts were significant inhibitors of leukocyte migration (p<0.05). Using the writhing test, significant analgesic activity was found for EAPr (50mg/kg), EAWPr (100mg/kg and 200mg/kg) and EAWPg (50mg/kg) (p<0.05).Thus, the appropriate extraction procedure preserves the chemical components such as gallic acid and quercetin, and showed antimicrobial, anti-inflammatory and analgesic properties.
- Attenuation of inflammatory mediators, oxidative stress and toxic risk evaluation of Aporosa lindleyana Baill bark extract. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 11.
Traditionally, Aporosa lindleyana Baill. has been used against various ailments viz. jaundice, fever, headache, seminal loss and insanity. The present study aims to evaluate the anti-inflammatory and anti-oxidant activity of the ethanolic extract of Aporosa lindleyana Baill. bark and its fractions.The anti-inflammatory activity of ethanolic extract of Aporosa lindleyana Baill. bark and its various fractions at doses of 200mg/kg and 300mg/kg b.w. has been carried out by carrageenan induced hind paw edema method. To establish the probable mechanism of action, TNF-α and NO levels have been estimated by ELISA method and the effect of active fraction on COX-2 and NF-κB expressions has been evaluated. The effect on the levels of anti-oxidative enzymes (CAT, SOD & GPX) by the ethanolic extract and its fractions has also been investigated. Furthermore, peptic ulcer and hepatotoxic risk evaluation has also been carried out at three times higher dose than that used in inflammatory in vivo model.Among the extract and its various fractions tested for anti-inflammatory activity, the methanolic fraction at a dose of 300mg/kg showed significant inhibition in paw edema by 73% as compared to Indomethacin which showed 77% inhibition after 5h. The same dose of methanolic fraction also caused significant reduction in TNF-α (59.27%) and NO concentration (57.12%) while Indomethacin showed inhibition of 63.91% and 60.12%, respectively. The active methanolic fraction was also found to inhibit the expression of NF-κB and COX-2 induced by carrageenan. Histological studies showed that the ethanolic extract and its fractions did not cause any damage to the stomach as well as to liver. Moreover, the active fractions also decreased lipid peroxidation levels and increased the antioxidant enzyme activities (SOD, CAT, GPX).The results of present study demonstrated that significant anti-inflammatory activity of methanolic fraction of A. lindleyana may be attributed to the modulation of pro-inflammatory mediators. Same fraction was also found to be effective against oxidative stress as it was found to elevate the levels of anti-oxidative enzymes. It can therefore be concluded that the methanolic fraction could be explored as a disease modifying agent against inflammation and oxidative stress.
- Effects of ethanolic dried leaf extract of lecaniodiscus cupanioides on antioxidant enzymes and biochemical parameters in rats. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 8.
Lecaniodiscus cupanioides is widely used in West African folk medicine for the treatment of inflammatory conditions, fevers and bacterial infections.To evaluate the potential toxic effects of the ethanolic dried leaf extract of Lecaniodiscus cupanioides (LC) on antioxidant enzymes in selected organs and biochemical parameters.Crude ethanolic extract of LC dried leaves was prepared. A 90-day sub-chronic toxicity studies was conducted using albino rats. Reconstituted LC was administered at a dosage of 400, 800 and 1600mg/kg (high dose) with a control group receiving 10ml/kg orally. Histopathological studies of major organs and blood chemistry analysis were performed on blood obtained via cardiac puncture after euthanization. Selected organs (liver, kidney and brain) were harvested for antioxidant and histopathological assessments.The extract produced significant (p<0.05) increases in the weights of liver, kidney and brain at 800mg/kg and 1600mg/kg compared to the control. Biochemical analysis showed significant increase in Alanine transferase (ALT) at 800mg/kg and 1600mg/kg. Assay for antioxidant enzymes showed a reversible decrease in the activity of Catalase (CAT), Superoxide dismutase (SOD) and Glutathione (GSH) with an increase in Malondialdehyde (MDA) at 800mg/kg and 1600mg/kg LC. Histopathological study showed reversible congestion in the brain, liver, and kidney at 800mg/kg and 1600mg/kg.Findings in this study reveal that the ethanolic dried leaf extract of LC has the potential for inhibiting in vivo antioxidant enzymes activity and causing hepatotoxicity after prolonged exposure.
- Salvia miltiorrhiza: An ancient Chinese herbal medicine and a new source for innovative anti-osteoporotic drugs. [REVIEW]
- J Ethnopharmacol 2014 Aug 7.
Red sage (Salvia miltiorrhiza Bunge), also known as Danshen in Chinese, is a member of the genus, Salvia, that has been historically used and currently exploited in combination with other herbs to treat skeletal diseases in traditional Chinese medicine (TCM). With the advance of modern analytical technology, a multitude of bone-targeting, pharmaceutically active, compounds has been isolated and characterized from various sources of TCM including those produced in S. miltiorrhiza root. The aim of the review is to provide a comprehensive overview about the historical TCM interpretation of the action of S. miltiorrhiza in osteoporosis, its use clinical trials, its main phytochemical constituents, and its action on bone-resorptive and bone formation-stimulating mechanisms in in vitro and in vivo studies.Literature sources used were Pubmed, CNKI.net, Cqvip.com, PubChem, and the Web of Science. For the inquiry, keywords such as Salvia, danshen, osteoporosis, bone, osteoclast, osteoblast were used in various combinations. About 130 research papers and reviews were consulted.In TCM, the anti-osteopororotic effect of S. miltiorrhiza is ascribed to its action on liver and blood stasis as main therapeutic targets defining osteoporosis. 36 clinical trials were identified which used S. miltiorrhiza in combination with other herbs and components to treat post-menopausal, senile, and secondary osteoporosis. On average the trials were characterized by high efficacy (>80%) and low or lack toxicity problems. However, various limitations such as small patient samples, short treatment duration, frequent lack of detailed numerical data, and no clear endpoints must be taken into consideration. To date, more than 100 individual compounds have been isolated from this plant and tested in various animal models and biochemical assays. Compounds display anti-resorptive and bone formation-stimulating features targeting different pathways in the bone remodeling cycle. Pathways affected include the activation of osteoblasts, the modulation of osteoclastogenesis, and the inhibition of collagen degradation by cathepsin K.The inclusion of S. miltiorrhiza in more than 30% of all herbal clinical trials successfully targeting osteoporosis has stimulated significant interest in the identification and characterization of individual constituents of this herb. The review highlights the anti-osteoporotic potential of S. miltiorrhiza in clinical applications and the potential of the herb to provide potent compounds targeting specific pathways in bone resorption and bone formation.
- Discovery of N-methyltetrahydroprotoberberines with k-opioid receptor agonist activities from corydalis yanhusuo W. T. Wang by using two-dimensional liquid chromatography. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 5.
The need for an efficacious analgesic without unwanted side effects is urgent. κ-opioid receptor agonists are known to exhibit potent analgesic effects and elicited fewer side effects than other opioid agonists. Thus in this study we chose the κ-opioid receptor as the target to identify the active components from traditional Chinese medicines (TCMs).The κ-opioid receptor was expressed in human embryonic kidney-293 T cells (HEK293T). Fluorometric Imaging Plate Reader (FLIPR) assay was used for the determination of Ca(2+) response when κ-opioid receptor was activated. A novel 2D separation system employing C18HCE as the first dimension and a strong cation exchange column (SCX) as the second dimension was conducted for the purification of the active principles.With the aid of HPLC-based activity profiling, activities could be linked to two peaks from Corydalis yanhusuo W. T. Wang (C. yanhusuo) extract. Two N-methyltetrahydroprotoberberines with κ-opioid receptor agonist activities were isolated for the first time from C. yanhusuo by using 2D-LC.Our study suggests that N-methyltetrahydroprotoberberines may serve as a new scaffold for κ-opioid receptor ligands. The strategy that we adopted can be applied to other naturally-occurring active alkaloids acting at different receptors.
- Mechanisms of the dilator action of the Erigerontis Herba on rat aorta. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 4.
Erigerontis Herba is widely used as traditional Chinese medicine and is commonly used for neuroprotection and vascular protection.In this study, the vasodilator effects of Erigerontis Herba (DZXX) were investigated using rat isolated aorta rings.The involvement of endothelium in the vasorelaxation was studied by comparing response of endothelium-intact and endothelium-denuded aorta rings which precontracted with U46619. The involvement of K(+) channels was studied by pretreatment of the aorta rings with various K(+) channel inhibitors. The involvement of Ca(2+) channel was studied by incubating aorta rings with Ca(2+)-free solution, primed with U46619 prior to elicit contraction by addition of Ca(2+) solution.DZXX (0.2-2mg/ml) induced a concentration-dependent relaxation on U44619-precontracted aorta rings with EC50 of 0.354±0.036mg/ml. Removal of endothelium or pretreatment with the BKCa inhibitor iberiotoxin, KIR inhibitor barium chloride or Kv inhibitor 4-aminopyridine produced no effect on the DZXX-induced vasorelaxation. However, pretreatment with the KATP inhibitor glibenclamide or a non-selective K(+) channel inhibitor tetraethylammonium produced significant inhibition on the DZXX-induced vasorelaxation by 29.9% and 21.3%, respectively. Pretreatment with DZXX (0.4, 1.2 and 2mg/ml) produced a concentration-dependent inhibition on Ca(2+)-induced vasoconstriction.These results suggest the vasodilator effect of DZXX was endothelium-independent, mediated by decreasing the influx of Ca(2+) by calcium channel inhibition and increasing the influx of K(+) by opening of KATP channel.
- Anti-inflammatory activity of omphalocarpin isolated from radix Toddaliae Asiaticae. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 4.
Radix Toddaliae Asiaticae has long been used as a traditional ethnic Chinese medicine for the treatment of inflammation and rheumatism. In our earlier communication we have reported the anti-arthritic activity of the ethyl alcohol extract and ethyl acetate fraction from Radix Toddaliae Asiaticae. This study was to examine the anti-inflammatory activity of prenylcoumarin omphalocarpin isolated from the ethyl acetate extract with the bioassay-guided methods.Cultured macrophage RAW 264.7 cells were used for the experiments. The ability of omphalocarpin to modulate the production of nitric oxide (NO), tumor necrosis factor alpha (TNF-α), interleukin-6 (IL-6), inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) was evaluated. Western blot was used to detect the expression of iNOS and COX-2 and the translocation of nuclear factor kappa B (NF-κB) to the nucleus. Meanwhile, the anti-inflammatory activity of omphalocarpin in vivo was also assayed by xylene induced ear edema in mice.It has been shown that omphalocarpin inhibited lipopolysaccharide (LPS)-stimulated NO production and pro-inflammatory mediators secretion, including TNF-α, IL-6 in a dose-dependent manner. Omphalocarpin also strongly suppressed the expression and enzymatic activity of iNOS and COX-2 and the translocation of NF-κB to the nucleus. In vivo assays omphalocarpin exhibited anti-inflammatory activity for alleviation of the ear swelling in xylene induced ear edema test.These results obtained in vitro and in vivo showed that the anti-inflammatory mechanism of omphalocarpin might be attributed to the inhibition of pro-inflammatory mediators including nitric oxide, IL-6 and TNF-α. Omphalocarpin decreased the overproduction of NO through down-regulation of the expression and enzymatic activity of iNOS and COX-2 in LPS-stimulated macrophage, which was due to the suppression of NF-κB activation in the transcriptional level. This is the first report of the anti-inflammatory activity of omphalocarpin.
- The total alkaloids of Aconitum tanguticum protect against lipopolysaccharide-induced acute lung injury in rats. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 4.
The whole plant of Aconitum tanguticum has been widely used as a remedy for infectious diseases in traditional Tibetan medicine in China. The total alkaloids of Aconitum tanguticum (TAA) are the main active components of Aconitum tanguticum and have been demonstrated to be effective in suppressing inflammation. The aim of the present study was to investigate the protective effects of TAA on acute lung injury (ALI) induced by lipopolysaccharide (LPS) in rats.TAA was extracted in 95% ethanol and purified in chloroform. After vacuum drying, the TAA powder was dissolved in dimethyl sulfoxide. Adult male Sprague-Dawley rats were randomly divided into six groups. Rats were given dexamethasone (DXM, 4mg/kg) or TAA (60mg/kg, 30mg/kg) before LPS injection. The PaO2 and PaO2/FiO2 values, lung wet/dry (W/D) weight ratio and histological changes in lung tissue were measured. The cell counts, protein concentration, tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and interleukin-1β (IL-1β) in bronchoalveolar lavage fluid (BALF), and myeloperoxidase (MPO) activity in lung tissue were determined at 6, 12 or 24h after LPS treatment. In addition, the NF-κ B activation in lung tissue was analyzed by western blot.In ALI rats, TAA significantly reduced the lung W/D ratio and increased the value of PaO2 or PaO2/FiO2 at 6, 12 or 24h after LPS challenge. TAA also reduced the total protein concentration and the number of total cells, neutrophils or lymphocytes in BALF. In addition, TAA decreased MPO activity in the lung and attenuated histological changes in the lung. Furthermore, TAA inhibited the concentration of TNF-α, IL-6 and IL-1β in BALF at 6, 12 or 24h after LPS treatment. Further study demonstrated that TAA significantly inhibited NF-κ B activation in lung tissue.The current study proved that TAA exhibited a potent protective effect on LPS-induced ALI in rats through its anti-inflammatory activity.
- Prevention of pulmonary fibrosis with salvianolic acid A by inducing fibroblast cell cycle arrest and promoting apoptosis. [JOURNAL ARTICLE]
- J Ethnopharmacol 2014 Aug 4.
Danshen (Salvia miltiorrhiza Bunge) is widely used in traditional Chinese medicine (TCM), often in combination with other herbs, to treat a diversity of ailments. More recent studies have focused on its possible roles in the treatment of respiratory diseases (pneumonia and pulmonary fibrosis) and found that it has pharmacological activity that protects pulmonary morphology and function. However, the mechanism underlying this activity has not yet been clarified.The purpose of this study was to investigate the anti-pulmonary fibrosis effects exerted by salvianolic acid A (SAA), the ingredient responsible for the pharmacological activity of Danshen, and the underlying mechanisms. Bleomycin (BLM)-induced rat pulmonary fibrosis was used to evaluate the antifibrotic role of SAA, and fibroblast cells were used to study the mechanism involved.BLM-treated rats exhibited increased alveolar wall thickness and collagen deposition in lung tissues, but these pathologies were greatly attenuated by daily administration of SAA. We also found that SAA significantly inhibited the proliferation, adhesion and migration of fibroblasts in vitro. This was partly due to a strong induction of cell cycle arrest and apoptosis upon SAA treatment. Consistent with these phenotypes, we observed decreased expression of the cell cycle-related proteins cyclin D1, cyclin E1, and cyclin B1, and increased expression of p53 and p21 in SAA-treated cells. In addition, the anti-apoptotic Bcl-2 protein decreased in a dose-dependent manner, while cleaved caspase-3 protein increased upon SAA treatment.These results suggest that the alleviation of rat pulmonary fibrosis by SAA is due to the inhibition of fibroblast proliferation and induction of apoptosis, which occurs mainly through p53-dependent growth arrest and apoptosis. We suggest that SAA should be considered as a potential novel therapeutic agent for the treatment of fibrotic lung diseases.