Percentage Protection Research Articles

ANTIULCER ACTIVITY OF AQUEOUS EXTRACT OF FRESH LEAF OF BRASSICA OLERACEAE LINN. VAR. ACEPHALA (D.C) ALEF) (BRASSICACEAE)

Brassica o leraceae (BOL) is the common cabbage and a familiar garden plant, widely used as spice all over the world. Cabbage is an excellent sou rce of Vitamin C and has been widely employed locally to treat acute inflammation and peptic ulcers. The present study aim ed at evaluating the anti ulcer activity of Brassica oleraceae , while identifying the phytoconstituents responsible for the observed effects and exploring some of the possible mechanisms of its anti ulcer activity, using standard laboratory procedures. Dos es of 100, 300 and 750 mg / kg of Brassica oleraceae were separately administered to groups of overnight fasted rats, with appropriate standard drugs using Ethanol / HCl, Indomethacin and Cysteamine models to explore anti ulcer property of BOL on the stoma ch and duodenum respectively. The extract in a dose dependent fashion, offered better protection against the ulcerogens in the gastric ulcer models, when compared with the positive control groups. However, the smallest dose of 100 mg / kg recorded the hig hest percentage protection in the cysteamine group. Up to 1200 mg / kg i.p and 10,000 mg / kg oral doses of Brassica oleraceae did not produce any mortality in mice. Phytochemical constituents identified included alkaloids, tannins, cardiac glycosides, fla vonoids, phlobatannins, anthraquinones and saponins. The pH was 8.5. The present study ha s validated the local use of Brassica oleraceae in the treatment of peptic ulcer and the speculated mechanisms of action could be through acid neutralization, cytoprot ection and antioxidation by flavonoids.

Characterization of Indian beers: chemical composition and antioxidant potential.

Chemical composition, antioxidant potential and corresponding lipid preoxidation of Indian commercial beers were evaluated. The presence of polyphenolic compounds such as tannic acid, gallic acid, catechol, vanillin, caffeic acid, quercetin, p-coumaric acid and rutin was quantified using LC-MS while the organic acids including tartaric, malic, acetic, citric and succinic acids were analysed using HPLC. Beer sample B8 had the greatest concentration of phenolic and flavonoid components (0.620 ± 0.084mg/mL and 0.379 ± 0.020mg/mL respectively) among the beer samples studied. The DPPH radical scavenging activity was observed in the range of 68.34 ± 0.85% to 89.90 ± 0.71% and ABTS radical cation scavenging activity was in the range of 59.75 ± 0.20% to 76.22 ± 0.50%. Percent protection in lipid peroxidation was quantified to be maximum (54.45 ± 3.39%) in sample B5. Total phenolic content positively correlates with antioxidant assays, DPPH and ABTS (r = 0.35 and r = 0.58 respectively) with p < 0.001 and also with lipid peroxidation (r = 0.04) with p < 0.001. Negative correlation was observed between total flavonoid content with ABTS and lipid peroxidation (r = -0.1 and r = -0.05) respectively. The process of brewing warrants additional research to determine how the concentration of selected phenolic compounds can be increased.

ANTIULCER ACTIVITY OF PREMNA SERRATIFOLIA AGAINST ASPIRIN INDUCED GASTRIC ULCER MODEL

The present study was carried out to investigate antiulcer activity of methanolic bark extract of Premna serratifolia against aspirin induced gastric ulcer models of male wistar rats. In aspirin induced pylorus ligation model, various parameters were s tudied viz. volume and pH of gastric juice, total acidity, free acidity, ulcer score, ulcer index and percentage protection was determined. Ulcer score, ulcer index and percentage inhibition of ulceration was determined for ulcer model . Ranitidine (50 mg/kg p.o.) was used as the standard drug. Pretreatment with the extracts (200 & 400 mg/kg p.o.) showed significant protection against ulcer model . In aspirin induced pylorus liga ted model, the methanolic bark extract showed significant decrease in the volume of gastric juice, free and total acidity, ulcer score, ulcer index and increase in pH of gastric juice as compared to the toxicant control group. In conclusion, Premna serratifolia possess significant anti - ulcer and cytoprotective effect.

Analysis of Time of Measurement and Modes of Administration of Some Medicinal Plants Additives on Mercury Accumulation in the Liver

Mercury toxicity leads to cell damage in many organs of the body. The authors comparatively examined the ability of different food additives with medicinal properties to protect against mercury (Hg) accumulation in the liver following different treatment interventions and modes of administration. Rats were fed on either 7% w/w Zingiber officinale, 7% w/w Garlic, 10% w/w Lycopersicon esculentum, or 5%, w/w Garcinia kola (all in rat chow), while Hg (10 ppm) was given in drinking water. The additives were administered together with the metals (group 2), a week after (group 3) or a week before metal exposure (group 4) for a period of six weeks. The metal accumulations in the liver were determined using an Atomic Absorption Spectrophotometer (AAS). All the additives significantly (p&lt;0.05) reduced the accumulation of mercury in the liver, percentage protection being lowest for ginger as an additive and highest for garlic. Percentage protection was significantly higher at weeks 4 (P&lt;0.01) and 6 (P&lt;0.001), compared to week 2. The mode of administration did not interact significantly with either time or additive in their relationship to percentage protection. Each additive provided significant protection from mercury and protection generally varied with time, but variations were not modified by mode of administration.

ANALGESIC, ANTI-INFLAMMATORY AND ANTI-ULCER ACTIVITY OF ETHANOL AND ETHYL ACETATE EXTRACTS OF TECOMARIA CAPENSIS LEAVES

In the present study ethyl acetate and ethanol extracts of leaves of Tecomaria capensis were screened for analgesic, anti - inflammatory and anti - ulcer activity. The analgesic activity was perfor med by two thermal models. One is hot plate method and another one is tail flick method. The two extracts of Tecomaria capensis leaves have showed analgesic activity in both methods . The anti - inflammatory activity was investigated by two methods. One is ca rrageenan induced paw edema method ( in - vivo ) and other is HRBC stabilization method ( in - vitro ). In both method s ethyl acetate and ethanol extracts sho wed anti - inflammatory activity. Anti - ulcer activity was done by aspirin induced method. In this, various b iochemical parameters like ulcer index, gastric juice, pH , free acidity, total acidity and percentage protection has been investigated. Further, histopathological studies have also been examined. Ethyl acetate and ethanol extracts have showed anti - ulcer ac tivity. In all the activities ethyl acetate showed a comparable activity to that of standard.

Hepatoprotective and antioxidant capacity of Melochia corchorifolia extracts

ObjectiveTo evaluate hepato protective and antioxidant capacity of Melochia corchorifolia (M. corchorifolia) aerial part extracts. MethodsAntioxidant activity was evaluated by using three free radicals (Superoxide, Hydroxyl and DPPH) and hepatoprotective activity was assessed against CCl4 induced liver intoxication in rats. ResultsThe extracts produced concentration dependent percentage protection in decrease of serum enzymes and percentage inhibition on free radicals. Among all extracts methanol extract showed better activity with percentage protection of SGOT (78.98%), SGPT (79.65%), ALP (82.48%) and total bilirubin (80.0%) levels against CCl4 liver intoxication and also methanolic extract showed better activity with IC50 values on superoxide, hydroxyl and DPPH radicals were 127 μ g, 240 μ g and 179 μ g. ConclusionsFrom the results obtained during the study it could be concluded that M. corchorifolia aerial part extracts have antioxidant and hepatoprotective components. Further study is necessary for isolation and characterization of bioactive molecules which are responsible for hepatoprotective and antioxidant activity.

The role of potassium BK channels in anticonvulsant effect of cannabidiol in pentylenetetrazole and maximal electroshock models of seizure in mice

Cannabidiol is a nonpsychoactive member of phytocannabinoids that produces various pharmacological effects that are not mediated through putative CB1/CB2 cannabinoid receptors and their related effectors. In this study, we examined the effect of the i.c.v. administration of potassium BK channel blocker paxilline alone and in combination with cannabidiol in protection against pentylenetetrazol (PTZ)- and maximal electroshock (MES)-induced seizure in mice. In the PTZ-induced seizure model, i.c.v. administration of cannabidiol caused a significant increase in seizure threshold compared with the control group. Moreover, while i.c.v. administration of various doses of paxilline did not produce significant change in the PTZ-induced seizure threshold in mice, coadministration of cannabidiol and paxilline attenuated the antiseizure effect of cannabidiol in PTZ-induced tonic seizures. In the MES model of seizure, both cannabidiol and paxilline per se produced significant increase in percent protection against electroshock-induced seizure. However, coadministration of cannabidiol and paxilline did not produce significant interaction in their antiseizure effect in the MES test. The results of the present study showed a protective effect of cannabidiol in both PTZ and MES models of seizure. These results suggested a BK channel-mediated antiseizure action of cannabidiol in PTZ model of seizure. However, such an interaction might not exist in MES-induced convulsion.

Screening of the Anticonvulsant Activity of Some Isatin Derivatives in Experimental Seizure Models and Its Effect on Brain GABA Levels in Mice

The modern therapeutic approaches of antiepileptic agents against epileptic patients are showing many side effects, dose related effects and chronic toxicity. The aim of our present work is to evaluate anticonvulsant activity of isatin derivatives (<b>Ia-Ij</b>) to reduce the side-effects and increase the percentage protection from various stages of convulsions. No animals showed toxic effects even up to 2000mg/kg. It is evident that <b>Ib, Ie, Ih, Ii </b>and<b> Ij </b>showed anticonvulsant effect at the dose levels of 10 and 100mg/kg in MES test and except <b>Ij</b> all other derivatives exhibited antiepileptic effect at 10 and 100mg/kg in PTZ induced convulsions test. The isatin derivatives<b> </b>(<b>Ib, Ie, Ih </b>and<b> Ii</b>) which proved antiepileptic effect in both MES and PTZ induced convulsion models are selected and GABA levels in brain were estimated. They showed significant increase of GABA levels in brain.

Abstract 4797: The antioxidation microsphere flow cytometer assay.

Abstract Increased production of reactive oxygen species is a feature of most, if not all, human disease, including cardiovascular disease and cancer. Dietary antioxidants may be especially important in protecting against human diseases associated with free radical damage to cellular DNA, lipids, and proteins. Yet, present data are not sufficient to quantify micronutrient requirements needed to protect against oxidative damage. The antioxidant roles of many food constituents, including herbs and spices, have not been clarified. The AMFC assay measures the oxidation of R-Phycoerythrin attached to microspheres via a protein coupling linker. A 25mM stock solution of ABTS.+ [2,2’-Azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) free radical], prepared during a 12 hour, 4 °C incubation with potassium persulfate to cause removal of one electron generating a metastable ABTS. This stock solution was diluted to 100μM in 150μl, which resulted in 80% quenching of 15μl of 104 PE microspheres. The antioxidant effects were measured by first incubating 50μl the 80 % quenching ABTS.+ with 100μl portions of serial diluted antioxidants for 30 min. at 22 °C to determine the antioxidants neutralize the ABTS.+. Subsequently, 15μl of PE-tagged microspheres were added to each sample and incubated one hour at 22 °C. The peak fluorescent channel number was determined for 5,000 microspheres. The typical percentage protection by the antioxidant standard at 500 ng/ml for Trolox (water soluble Vitamin E derivative) was 8, while 500 ng/ml of Vitamin C restored 78% The range of 500-5,000 ng/ml showed the protective effects of Trolox and Vitamin C remained constant. On the average, equivalent percentage protection for both the hydrophilic and lipid soluble fractions of 14 spices (courtesy of McCormick Science Institute) was not achieved until the 20-50 μg/ml concentration of the spices with Turmeric, Cinnamon, Oregano and Cloves, showing the highest antioxidant protection. Interestingly, Rosemary, Sage, Thyme and Turmeric revealed a significant reduction in antioxidant activity at 200 μg/ml. These are still significant antioxidant levels that show a secondary reason besides flavoring to use spices for achieving clinically important antioxidant activity. The AMFC assay is very sensitive to the effects of oxidants, functions under physiological conditions, requires little sample and allows application to the study of serum samples. Thus, one may monitor antioxidant activity in healthy volunteers taking compounds to boost the antioxidant activity to offset the long-term effects of oxidative radiation and chemotherapy. Citation Format: Jerry T. Thornthwaite, Hare R. Shah. The antioxidation microsphere flow cytometer assay. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 4797. doi:10.1158/1538-7445.AM2013-4797 Note: This abstract was not presented at the AACR Annual Meeting 2013 because the presenter was unable to attend.

Deletion of 12/15-lipoxygenase alters macrophage and islet function in NOD-Alox15(null) mice, leading to protection against type 1 diabetes development.

AimsType 1 diabetes (T1D) is characterized by autoimmune depletion of insulin-producing pancreatic beta cells. We showed previously that deletion of the 12/15-lipoxygenase enzyme (12/15-LO, Alox15 gene) in NOD mice leads to nearly 100 percent protection from T1D. In this study, we test the hypothesis that cytokines involved in the IL-12/12/15-LO axis affect both macrophage and islet function, which contributes to the development of T1D.Methods12/15-LO expression was clarified in immune cells by qRT-PCR, and timing of expression was tested in islets using qRT-PCR and Western blotting. Expression of key proinflammatory cytokines and pancreatic transcription factors was studied in NOD and NOD-Alox15null macrophages and islets using qRT-PCR. The two mouse strains were also assessed for the ability of splenocytes to transfer diabetes in an adoptive transfer model, and beta cell mass.Results12/15-LO is expressed in macrophages, but not B and T cells of NOD mice. In macrophages, 12/15-LO deletion leads to decreased proinflammatory cytokine mRNA and protein levels. Furthermore, splenocytes from NOD-Alox15null mice are unable to transfer diabetes in an adoptive transfer model. In islets, expression of 12/15-LO in NOD mice peaks at a crucial time during insulitis development. The absence of 12/15-LO results in maintenance of islet health with respect to measurements of islet-specific transcription factors, markers of islet health, proinflammatory cytokines, and beta cell mass.ConclusionsThese results suggest that 12/15-LO affects islet and macrophage function, causing inflammation, and leading to autoimmunity and reduced beta cell mass.

Discovery of some novel imines of 2-amino, 5-thio, 1,3,4-thiadiazole as mucomembranous protector. Synthesis, anti-oxidant activity and in silico PASS approach

A series of some novel imines (6a–f) of 2-amino, 5-thio 1,3,4-thiadiazole connected to benzimidazole chalcones were prepared. The structures of the final imines were ascertained by IR, 1HNMR, mass and elemental analyses. Predicted activity spectra of all the final derivatives were determined in the category of mucomembranous protector nature with a Pa value more than 0.7. All the newly synthesized compounds were screened for their antiulcer activity in the pylorus-ligated rats. Free radical scavenging activity of all final derivatives was determined by DPPH method.Compounds 6e, 6a and 6b showed a percentage protection of (73.47, 72.17 and 70.43 at a dose of 10mg/kgb.w.) when compared to standard omeprazole (77.37%, 2mg/kgb.w.). Compounds 6e, 6a and 6b showed free radical scavenging activity with an IC50 of 0.32, 0.39 and 0.49mM respectively. Scanning of stomach specimens using electron microscope revealed that the mice treated with standard and synthetic derivatives had no injury observed in stomach mucosa, which is identical to that of the control animal. It has been concluded that ulcer healing properties of the imines are probably due to their antioxidant action.

Experimental evaluation of anticonvulsant effect of human placental extract in pentylenetetrazole induced convulsions in mice

Background: Human placental extract (HPE) is used in different clinical conditions. Human placental extract (HPE), a folklore medicine, prepared from fresh, healthy human placenta has been in use, as single dose therapy in the treatment of epilepsy in some parts of India. Hence, present study was carried out to explore anticonvulsant property of Human placental extract (HPE) in Pentylenetetrazole (PTZ) induced convulsions in albino mice. Methods: Effects of human placental extract (HPE) (1.0, 1.2 and 1.4 ml / 100 gm body weight) as test drug, sodium valproate (150 mg / kg body weight) as standard and distilled water as control were studied in pentylenetetrazole (PTZ) induced convulsions in albino mouse model. Failure to observe even a single episode of tonic spasm for 5 sec. duration for 1 hour was taken as index of anticonvulsant activity. Onset, duration, complete recovery from convulsion and percent protection was calculated and statistical analysis was carried out using student ‘t’ test. Results: Pretreatment with human placental extract (HPE) administered in the dose of 1.0 ml / 100 gm body weight provided 33.33% and in the doses of 1.2 and 1.4 ml / 100 gm body weight and sodium valproate provided 100% protection from convulsions induced by Pentylenetetrazole in albino mice. Conclusion: Human placental extract (HPE) has shown promising anticonvulsant effect on Pentylenetetrazole induced mouse model.

Synthesis and PASS-assisted in silico approach of some novel 2-substituted benzimidazole bearing a pyrimidine-2, 4, 6(trione) system as mucomembranous protector

Purpose:The present paper demonstrates the utility of PASS computer-aided program and makes a clear comparison of predicted and observed pharmacological properties of some novel 5-[(2E)-1-(1H-benzimidazol-2-yl)-3-substituted phenylprop-2-en-1-ylidene] pyrimidine-2, 4, 6 (1H, 3H, 5H)-triones (5a–f).Materials and Methods:The synthesis of the titled derivatives were achieved by the reaction between 2E)-1-(1H-benzimidazol-2-yl)-3-phenylprop-2-en-1-ones (4a–f) and barbituric acid in the presence of catalytic amount of acetic acid medium. All the final structures were assigned on the basis of IR, 1HNMR and mass spectra analysis. All the newly synthesized compounds were screened for their antiulcer activity in the pylorus-ligated rats.Results:Compounds 5b, 5e and 5c showed a percentage protection of (69.58, 69.56 and 67.17 at a dose of 50 mg/kg b.w.) when compared to standard omeprazole (77.37%, 2 mg/kg b.w.).Conclusion:Scanning of stomach specimens using electron microscope revealed that the mice treated with standard and synthetic derivatives had no injury observed in stomach mucosa, which is identical to that of the control animal.

Efficacy of DEET and non‐DEET‐based insect repellents against bites of Simulium damnosum vectors of onchocerciasis

Coping strategies including smoke screens are used against nuisance bites of Simulium damnosum Theobald (Diptera:Simuliidae) in onchocerciasis endemic communities. To find more effective alternatives, the efficacy of commercially available N,N-diethyl-3-methylbenzamide (DEET) products with active concentrations of 9.5, 13, 25, 50 and 98.1-100% and 'NO MAS,' (active component: para-menthane-3,8-diol and lemon grass oil) were tested at Bui-Agblekame, Ghana. A Latin square study design was implemented using eight groups of two vector collectors each, who used repellents (treatment), mineral oil or nothing each day until the end of the study. Flies were caught and their numbers each hour recorded using the standard methods for onchocerciasis transmission studies. T-tests were used to compare the mean duration of protection and a one-way analysis of variance controlling for catchers and repellents was performed. Tukey's test was used to compare protection by repellents and mineral oil. The highest percentage protection was 80.8% by NO MAS and the least 42.5% by the 13% DEET product. The period of absolute protection was 5 h by NO MAS and 1 h by 50% DEET product. No significant increase in protection was offered beyond 25% active DEET products and no significance was observed in terms of catcher × repellent effect (F = 1.731, d.f. = 48, P = 0.209).

Synthesis and evaluation of bipyrazolic derivatives as inhibitors of corrosion of C38 steel in molar hydrochloric acid

Methyl 2-(bis((3,5-dimethyl-1H-pyrazol-1-yl)methyl)amino) acetate, BT36, and methyl 2-(bis((3,5-dimethyl-1H-pyrazol-1-yl)methyl)amino)-3-(1H-indol-3-yl)propanoate, BT 43, have been synthesized. Investigation by weight-loss measurement and use of electrochemical techniques revealed the compounds are very effective inhibitors of corrosion of C38 steel in 1 M HCl solutions—percentage protection exceeded 95 % for BT43 at concentrations as low as 10−2 M. An impedance study in the absence and presence of these compounds revealed the mechanism of protection was cathodic inhibition by polarization and charge-transfer. The Langmuir adsorption isotherm was obeyed. Quantum chemical data calculated by use of DFT at the B3LYP/6-31G* level of theory revealed a good correlation between inhibition efficiency and the molecular structure of BT36 and BT43. The highest occupied molecular orbital, the lowest unoccupied molecular orbital, the separation energy (ΔE), and the dipole moment (μ) from the inhibitor to the metal surface explain the experimental data well.

Studies on wheat bran Arabinoxylan for its immunostimulatory and protective effects against avian coccidiosis

Wheat (Triticum aestivum) bran derived polysaccharides, Arabinoxylans (AXs), were evaluated for their immunostimulatory and protective efficacy against Eimeria infection in chickens. Humoral response revealed significantly higher (P<0.05) total Igs, IgG and IgM titers at days 7th and 14th post primary and secondary injections of sheep red blood cells in the experimental chickens administered with AXs as compared to those of control group. The percent protection and daily weight gains were significantly higher (P<0.05) in the chickens of experimental groups as compared to control; whereas, mean oocyst per gram of droppings and lesion scores were significantly higher (P<0.05) in control group as compared to chickens in the experimental groups. The differences in organ body weight ratio of all the lymphoid organs were statistically non-significant (P>0.05) between experimental and control groups except thymus and cecal tonsils. In conclusion, AXs showed both immunostimulatory and protective effects against coccidiosis in broiler chickens.

Gastroprotective effect of leaf extracts of Basella alba var. alba against experimental gastric ulcers in rats

The aqueous and ethanol extracts of the leaves of Basella alba L. var. alba Wight, Basellaceae, were investigated for antiulcer activity on rats employing the pylorus ligation and ethanol induced ulcer models. The various gastric secretion parameters such as total acidity, free acidity, gastric acid volume, pH and histopathological parameters such as ulcer index and percent protection were comparatively examined between control, test and standard groups. The antiulcer activity of aqueous extract of B. alba (AEBA) and ethanol extract of B. alba (EEBA) were studied in rats treated with the doses of 1 mL/kg of absolute ethanol, 200 and 400 mg of test extracts and 20 mg/kg of famotidine for control, test and standard groups respectively in both the models. The animals pretreated with AEBA and EEBA showed a dose-dependent protection against gross damaging action of ethanol and pylorus ligation on gastric mucosa of animals. Histopathological evaluation also revealed that Group I treated with absolute ethanol showed severe gastric mucosal damage. The AEBA and EEBA showed 68.25 and 58.11% protection in gastric mucosal damage as compared to control group. Both the extracts of B. alba var. alba were able to decrease the gastric acidity and increase the mucosal defense in the gastric mucosal area. This study indicate that B. alba var. alba possesses significant gastroprotective effect and the same is substantiated by the histopathological examination of the ulcerated stomachs of the animals.

Design, synthesis and H1-antihistaminic activity of novel 1-substituted-4-(3-chlorophenyl)-[1,2,4] triazolo [4,3-a] quinazolin-5(4H)-ones

In the present study a series of 1-substituted-4-(3-chlorophenyl)-[1,2,4] triazolo [4,3-a] quinazolin-5(4H)-ones were synthesized and screened for their H1-antihistaminic activity. The synthesized compounds were characterized by IR, 1H-NMR, mass spectral data and purity of the compounds was determined by elemental analysis. Antihistaminic activity of the title compounds was evaluated by histamine induced bronchoconstriction method in guinea pigs. Among the series, 4-(3-chlorophenyl)-1-methyl-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one (S5) was the most potent with the percentage protection of 69.65% and its potency is comparable to the reference drug chlorpheniramine maleate (70.09% protection). Interestingly the sedative property of compound S5 was found to be negligible (5.36%) when compared to chlorpheniramine maleate (34.92%).

Pyrazole incorporated 1,2-diazanaphthalene derivatives: Synthesis and in- vivo pharmacological screening as anti-inflammatory and analgesic agents

In the present study, a new series of compounds (3 to 22) containing pyrazole moiety clubbed with 1,2-diazanaphthalene ring, structurally related to celecoxib and naproxen was synthesized. The compounds were evaluated for anti-inflammatory activity using carrageenan induced rat paw edema bioassay. Compounds showing marked anti-inflammatory activity were further tested for their analgesic, ulcerogenic and lipid peroxidation effect using naproxen as reference drug. The results showed that compounds 6, 13 and 14 exhibited good anti-inflammatory and analgesic activity with minimum gastric irritation. Compounds 13 and 14 emerged as potent anti-inflammatory (with percentage inhibition of 79.23 and 76) and analgesic agent (with percentage protection of 68.72 and 67.68) in the present study. Key words: Cinnoline, pyrazole, anti-inflammatory activity, analgesic activity, lipid peroxidation.

Protective immunization of hamsters against Opisthorchis viverrini infection is associated with the reduction of TGF-β expression

Opisthorchis viverrini infection is a significant health problem in Thailand and other countries in Southeast Asia. There is little known about the mechanisms of the immune response to O. viverrini in immunoprotection. However, it has been reported that this parasite can suppress both cell and antibody mediated immune responses. The TGF-β and IL-10 are immunosuppressive cytokines that play an important role in inhibition of host immune response leading to worm survival. In this study, we immunized hamsters to protect against O. viverrini infection and the IL-4, IL-10, TGF-β and IFN-γ expression in spleen was investigated by real time PCR analysis. An O. viverrini-crude somatic antigen preparation (CSAg) administered with complete Freund's adjuvant (CFA) or with alum was used to stimulate immune responses in O. viverrini-primed hamsters. The greatest percent protection (48.4%) was seen following immunization with CSAg plus alum. The mean number±SD of worms recovered in the PBS control, CFA alone, CSAg plus CFA, alum alone and CSAg plus alum was 17.4±2.3, 17.1±3.3, 14.5±3.8, 14.5±2.3 and 9±2.7, respectively. Significant protection correlated with the reduction of TGF-β and IL-10, but not IL-4, IFN-γ expressions. Since TGF-β expression is significantly increased in the spleens of hamsters with opisthorchiasis, stimulation of this cytokine by parasite antigens was confirmed by using CSAg and primary hamster spleen cells. Antigen fractions with molecular masses of 81–92, 64–72 and 19–21.4kDa were found to significantly induce TGF-β production. Our results suggested that TGF-β induction by O. viverrini may have an important role in parasite survival.