Intestinal anti-inflammatory activity of the Serpylli herba extract in experimental models of rodent colitis

IntroductionNowadays, there is an increasing interest for alternative options in the treatment of inflammatory bowel diseases (IBDs) that combine efficacy and an adequate safety profile.MethodsThe intestinal anti-inflammatory effects of Serpylli herba, the officinal drug in the European Pharmacopeia composed by the aerial parts of wild thyme (Thymus serpyllum), were evaluated in the trinitrobenzenesulfonic acid (TNBS)-induced rat colitis and dextran sodium sulfate (DSS)-induced mouse colitis, which are well characterized experimental models with some resemblance to human IBD.ResultsS. herba extract exerted an intestinal anti-inflammatory effect in both experimental models of colitis, as evidenced both histologically, since it facilitated the tissue recovery of the damaged colon, and biochemically as showed by the improvement of the different inflammatory markers evaluated, including myeloperoxidase activity, glutathione content, and leukotriene B₄ levels as well as the expression of the inducible proteins iNOS and COX-2. This beneficial effect was associated with the reduction in the expression of different cytokines, like TNFα, IL-1β, IFNγ, IL-6 and IL-17, the chemokine MCP-1, and the adhesion molecule ICAM-1, thus ameliorating the altered immune response associated with the colonic inflammation.ConclusionS. herba extract displays an anti-inflammatory effect on different models of rodent colitis that could be attributed to its immunomodulatory properties.     

Vernonia Amygdalina Del. stimulated glucose uptake in brain tissues enhances antioxidative activities; and modulates functional chemistry and dysregulated metabolic pathways

Brain glucose uptake is usually reduced in type 2 diabetes owing to downregulation of brain glucose transporters. The ability of Vernonia amygdalina to stimulate glucose uptake as well as ameliorate glucose-induced oxidative stress and proinflammation were investigated in rat brain. Hot infusion of V. amygdalina leaves was incubated with rat brain tissues for 2 h in the presence of glucose. Another incubation with glucose only, served as negative control while metformin served as positive control. Incubation of brain tissues with V. amygdalina led to significant (p?<?0.05) increase in glucose uptake, reduced glutathione, nitric oxide and non-thiol proteins levels, superoxide dismutase, catalase and ATPase activities, while concomitantly decrease in myeloperoxidase activity and malondialdehyde level compared to the negative control. Incubation with glucose only, led to the development of nitrate, amide II and amide I functional groups which were removed on incubation with the infusion. LC-MS analysis revealed depletion of oxidative stress-induced 2-keto-glutaramic acid and cysteinyl-tyrosine metabolites in brain tissues, with concomitant generation of S-formylglutathione and adenosine tetraphosphate by the infusion. Pathway analysis of the metabolites revealed an activation of pyruvate metabolism pathway in the negative control, with the infusion reducing the intensity fold. LC-MS analysis of the infusion revealed the presence of l–serine, l-cysteine, l-proline, nicotinic acid, cumidine, salicylic acid, isoquinoline, 3-methyl-, and γ-octalactone. Except for l–serine, l-cysteine and l-proline, the other compounds were predicted to be permeable across the blood brain barrier. These results indicate the brain glucose uptake stimulatory and neuroprotective effect of V. amygdalina.

     

Phytochemical screening and evaluation of anti-inflammatory activity of methanolic extract of Abroma augusta Linn

ObjectiveTo evaluate the Phytochemical and anti-inflammatory property of the different parts of methanolic extracts of Abroma augusta Linn.Materials and methodsAbroma augusta Linn (Family-Malvaceae) commonly known as Ulatkambal in Hindi and Devil's cotton in English, found in tropical Asia, South and eastern Africa, and Australia. It is mainly used for dysmenorrhoea, ammenorrhoea, sterlilty and other menstrual disorder. The present study aimed at evaluation of Phytochemical and anti-inflammatory study of different parts of Abroma augusta Linn methanolic extract by the carrageenan induced rat paw oedema method.ResultsThe result showed significant anti-inflammatory property of different parts of Abroma augusta Linn methanolic extract.ConclusionsThe methanolic extract of different parts of Abroma augusta Linn showed potent activity comparing with the standard drug diclofenac sodium perhaps due to the alkaloids and flavonoids present in the plant.     

Evaluation of in vivo and in vitro anti-inflammatory activity of Ajuga bracteosa Wall ex Benth

Ethnopharmacological relevance: Ajuga bracteosa Wall Ex Benth. (Labiateae) is described in Ayurveda for the treatment of rheumatism, gout, palsy and amenorrhea.ObjectivePresent study was aimed to investigate the in vivo and in vitro anti-inflammatory activity of Neelkanthi (whole plant) and to support its traditional use.MethodsMethanolic extract of plant Ajuga bracteosa (ABE) was investigated for its anti-inflammatory activity in carrageenan induced rat paw oedema, egg albumin induced inflammation in rats and the study was further supported with in vitro anti-inflammatory study by using Human red blood cell membrane stabilization (HRBC) method. Three doses of the extract (ABE-250, 500 and 750 mg/kg, i.p.) were used in the study and diclofenac sodium (5mg/kg, i.p.) was used as standard.ResultsABE (500 and 750 mg/kg, i.p.) significantly (P < 0.05) reduced increased in paw volume induced by carrageenan and egg albumin. ABE also showed significant stabilization toward HRBC membrane.ConclusionsABE at the dose of 500 and 750 mg/kg showed potent action on comparison with the standard drug diclofenac sodium.     

Antigonadotropic activity of hop extract.

Biological activity of water soluble fractions F-1 and F-2, which were extracted from hop, was studied and its action mechanism was speculated using the immature female SD rats. Administration of the substance significantly inhibited the effects of pregnant mare serum gonadotropin (PMSG) on 22-day-old female rats. Thus, PMSG-induced increases in ovarian weight, estrogen secretion, number of ovulated egg, progesterone production, uterine thymidine kinase activity, and plasma LH level were suppressed significantly. Furthermore, addition of the substance to incubated ovarian cells of the second day after PMSG injection resulted in suppression of FSH-induced estradiol secretion in vitro, probably via cAMP-dependent mechanism. But addition of the substance to incubated pituitary cells from ovariectomized rats did not change in LH secretion.     

红松针叶提取物抗氧化活性研究

目的 探讨红松针叶提取物的抗氧化活性.方法 采用无水乙醇和蒸馏水分别对红松针叶进行提取,观察其对于1,1-二苯基-2-苦基苯肼(DPPH)自由基的清除作用,.以及对β-胡萝卜素-亚油酸氧化体系的抑制作用,以此来评价红松针叶提取物的抗氧化活性.结果 红松针叶醇提物和水提取物对DPPH自由基有较好的清除作用,其IC 50值分别为2.03 g/L和6.49 g/L.而对β-胡萝卜素-亚油酸氧化体系有明显的抑制作用,其IC 50值分别为3.14 g/L和9.14 g/L.乙醇提取物的抗氧化活性明显高于水提取物.结论 红松针叶的乙醇提取物及水提取物在抗衰老、抗炎症等方面有广泛的应用前景.     

Evaluation of the anti-diabetic properties of Mucuna pruriens seed extract

ObjectiveTo explore the antidiabetic properties of Mucuna pruriens(M. pruriens).MethodsDiabetes was induced in Wistar rats by single intravenous injection of 120 mg/kg of alloxan monohydrate and different doses of the extract were administered to diabetic rats. The blood glucose level was determined using a glucometer and results were compared with normal and untreated diabetic rats. The acute toxicity was also determined in albino mice.ResultsResults showed that the administration of 5, 10, 20, 30, 40, 50, and 100 mg/kg of the crude ethanolic extract of M. pruriens seeds to alloxan-induced diabetic rats (plasma glucose > 450 mg/dL) resulted in 18.6%, 24.9%, 30.8%, 41.4%, 49.7%, 53.1% and 55.4% reduction, respectively in blood glucose level of the diabetic rats after 8h of treatment while the administration of glibenclamide (5 mg/kg/day) resulted in 59.7% reduction. Chronic administration of the extract resulted in a significant dose dependent reduction in the blood glucose level (P<0.001). It also showed that the antidiabetic activity of M. pruriens seeds resides in the methanolic and ethanolic fractions of the extract. Acute toxicity studies indicated that the extract was relatively safe at low doses, although some adverse reactions were observed at higher doses (8-32 mg/kg body weight), no death was recorded. Furthermore, oral administration of M. pruriens seed extract also significantly reduced the weight loss associated with diabetes.ConclusionsThe study clearly supports the traditional use of M. pruriens for the treatment of diabetes and indicates that the plant could be a good source of potent antidiabetic drug.     

Antioxidant and anti-inflammatory activity of Polygonatum sibiricum rhizome extracts

Objective

To investigate the antioxidant and anti-inflammatory activities of distilled water extract of fresh Polygonatum sibiricum (P. sibiricum) rhizome.

Methods

: The extracts were tested for antioxidant activity by using DPPH (1,1-diphenyl-2-picryl-hydrazyl), and hydroxyl (OH•) radicals scavenging activity. The level of intracellular reactive oxygen species (ROS) was determined in H₂O₂ treated chang liver cells. Anti-inflammatory activity was evaluated by the inhibition of nitric oxide (NO), inducible nitric oxide synthase (iNOS), as well as tumor necrosis factor-alpha (TNF-α) protein expression in a lipopolysaccharide stimulated Raw 264.7 murine macrophages cell line.

Results

: P. sibiricum water extracts scavenged DPPH, OH• radicals and decreased the level ROS. The extracts reduced NO reduction and inhibited the expression of iNOS and TNF-α proteins.

Conclusions

: The findings indicate that water extracts of P. sibiricum could be considered as natural antioxidants and anti-inflammatory agents for food and drug industries.     

Evaluation of antipyretic activity of ethyl acetate extract of Adenema hyssopifolium G. Don in a rat model

ObjectiveTo evaluate the effect of ethyl acetate extract of Adenema hyssopifolium (AHEAE) on normal body temperature and brewer's yeast-induced pyrexia rats.MethodsPreliminary phytochemical tests, acute toxicity tests and antipyretic evaluation were carried out in ethyl acetate extract of Adenema hyssopifolium. Two doses of the extract (300 or 600 mg/kg orally) and standard antipyretic agent, paracetamol at a dose of 150 mg/kg were administered to various group of the rats. Mean rectal temperature before and after treatment was noted.ResultsThe phytochemical analysis of AHEAE revealed the presence of flavonoid and iridoid glycosides as major phytoconstituents. The administration of AHEAE at a dose of 300 or 600 mg/kg produced significant reduction (P<0.001 and P<0.01) of the body temperature in normal and pyrexia rats on a dose dependent manner. The antipyretic influence of AHEAE was comparable to that of standard antipyretic agent, paracetamol (150 mg/kg), and onset of action and reduction in pyrexia towards normal body temperature was delayed when compared to paracetamol treatment. At dose of 600 mg/kg, AHEAE reduced pyrexia to normal body temperature at 4 h after its administration compared to reduction of pyrexia to normal body temperature at 2 h by standard drug. The reduction of fever was consistent in paracetamol group from 2 to 4 h after its administration to normal body temperature compared to AHEAE treatments.ConclusionsOur present results corroborate with the traditional notion of Adenema hyssopifolium G. DON that is being used as an effective cure of fever and add authenticity to claim of indigenous healers that the taxon is a potential antipyretic agent.     

Gelatinase activity in Mycobacterium bovis protein extract

Proteases are well-recognized as virulence factors in different pathologies, resulting in tissue damage potential. Despite efforts over the past few years to identify mycobacterial protein antigens, there is little information regarding the role of mycobacterial proteinase activities. In this study, by zymography techniques, we have detected and partially studied some biochemical properties of Mycobacterium bovis proteases, such as pH dependency of activity and susceptibility to classical proteinase inhibitors. We observed optimal proteolytic activity at pH 8. Some proteinases were inhibited by classic inhibitors of serine proteases, such as PMSF, AEBSF, and 3-4 DCI. In some AEBSF pre-treated preparations we observed residual gelatinase activity in Rf 0.32. This gelatinase was stimulated by Zn2+ and inhibited by OPA (1 mM). This last effect was reversed by exposure to equimolar quantitative OPA/Zn+2 (1 mM/1 mM). These results suggest the existence of serine proteinase and metalloproteinase types in protein extracts of Mycobacterium bovis.     

The extract of Mucuna pruriens possesses histamine activity

ObjectiveTo investigate the activity of the active principle in the spines of the seed pods of Mucuna pruriens using contraction of guinea pig ileum as index of pharmacological activity.MethodsThe active principle was extracted with 0.0015 M NaCl. Muscle strips of guinea pig ileum were prepared and contractile responses were measured using a Kymograph. Two sets of experiment were conducted: (1). The contraction of the ileum in presence of different concentrations of histamine, 2-methylhistamine and the extract of Mucuna pruriens. (2). The contractile response of the ileum in presence of different concentrations of the extract and antagonists including diphenhydramine, atropine and methysergide.Results(1) The extract of Mucuna pruriens hair, 2-methylhistamine and histamine produced dose dependent contraction of guinea pig ileum (Extract ED₅₀ = 13.0 μg/mL, 2-methylhistamine ED₅₀ = 8.5 μg/mL and histamine ED₅₀ = 10.0 μg/mL). (2) Diphenhydramine, an H₁ antagonist competitively blocked the contractile response of the Mucuna pruriens extract. (3) Coadminstration of the Mucuna pruriens extract either with different doses of antimuscarinic agent atropine or 5-hydroxytryptamine blocking agent methysergide did not alter the extract induced contractile response of the guinea pig ileum.ConclusionThese results demonstrate that the spines of Mucuna pruriens possess histamine activity which may contribute to its itching and painful irritation effects.     

Superoxide dismutase activity of Ginkgo biloba extract]

The Ginkgo biloba extract is obtained from green leaves of the Ginkgo biloba tree. Preparations with this active substance are among others used for the treatment of disturbances of the cerebral function and arteriosclerotic diseases. In in-vitro and in-vivo studies antagonistic effects of radical scavenger and PAF (platelet activating factor) were described. In this study a concentration-depending superoxide dismutase activity of the Ginkgo biloba extract r?kan liquid could be made evident.     

Carcinogenic activity in mice of diftalone,an anti-inflammatory agent

Summary The anti-inflammatory agent diftalone was administered in the diet to male and female BALB/c mice at 300-, 600-, and 1200-ppm dose levels for 80 weeks, starting at 8 weeks of age. The animals were kept under observation until 126–128 weeks of age, when the experiment was terminated. Diftalone treatment at the highest dose was hepatotoxic and induced hepatocellular tumors in females, angiomas of the liver in males, and angiosarcomas of the liver in male and female mice. The 300- and 600-ppm dose levels were not carcinogenic. The compound was not mutagenic for Salmonella typhimurium.     

The influence of nonsteroidal anti-inflammatory drugs on deaminase adenosine activity

The aim of the study was to evaluate the influence ofnonsteroidal anti-inflammatory drugs on deaminase adenosine activity using animal model. 70 rats of Wistar breed was divided into equal groups of ten. Animals were given intragastrically for three weeks: acetylsalicylic acid (ASA) at doses of 2 and 10 mg/kg bw/day, diclofenac at doses of 1 and 5 mg/kg bw/day, nimesulide at doses of 2.5 mg and 12.5 mg/kg bw/day. Control group received only water. After 21 days rats were decapitated and blood was collected to assess deaminase adenosine activity in plasma and erythrocytes. It was found that all investigated drugs inhibit ADA activity in plasma and ADA2 isoenzyme is responsible for this inhibition. Deaminase adenosine activity in erythrocytes is inhibited by ASA and diclofenac but increased by nimesulide.     

Doxycycline exhibits anti-inflammatory activity in CF bronchial epithelial cells

A hallmark of cystic fibrosis is the massive recruitment of neutrophils into the lung compartment in response to chronic Pseudomonas aeruginosa infection. The overexuberant neutrophilic response results in release of proteases (e.g. neutrophil elastase and matrix metalloproteinase-9) leading to matrix breakdown, airway remodeling, and progressive loss of lung function. Doxycycline is used clinically for the management of periodontitis due to its potent direct inhibition of matrix metalloproteinases; however, little is known regarding its potential anti-inflammatory properties and clinical utility in the context of cystic fibrosis airway disease. CF (IB3-1) and corrected (S9) bronchial epithelial cell lines were used to determine the cytotoxicity and anti-inflammatory effects of doxycycline in-vitro. Exposure to doxycycline, at low concentrations, resulted in minimal cell death and dose dependent reductions in release of CXCL-8 and MMP-9 protein. To confirm these findings, mechanistic analysis revealed ERK 1/2, p38, and JNK, but not NF-κB p65 dependent cell signaling inhibition with doxycycline treatment. These findings indicate that doxycycline exhibits anti-inflammatory activity in CF lung epithelial cells at concentrations below the cytotoxic potential. These data are encouraging and indicate in-vivo studies are warranted.