A synergistic approach for management of lung carcinoma through folic acid functionalized co-therapy of capsaicin and gefitinib nanoparticles: Enhanced apoptosis and metalloproteinase-9 down-regulation.

BACKGROUND: Lung cancer is one of the most lethal cancers and lacks effective treatment strategy. Therapeutic efficacy can be improved through active targeting approach utilizing surface engineered nanoparticles (NPs) for cancer therapy. PURPOSE: The present study envisioned development of Folic acid (FA) functionalized NPs for co-administration of gefitinib (Gnb) and capsaicin (Cap) respectively to enhance the therapeutic outcome by disabling the barriers related to tumors extracellular matrix. RESEARCH METHODS AND PROCEDURE: The FA conjugated Gnb/Cap polymeric (PLGA-PEG) NPs were prepared using oil in water emulsion technique and methodically developed using Quality by Design (QbD) concept employing central composite design. The developed formulations were subjected to various in vitro (A549 cell lines) and in vivo evaluations in urethane-induced lung cancer. RESULTS: The modified NPs displayed particle sizes of 217.0 ±â€¯3.2 nm and 213.0 ±â€¯5.2 nm and drug release of 85.65 ±â€¯3.21% and 81.43 ±â€¯4.32% for Gnb and Cap respectively. Higher cellular uptake and lower cell viability in A549 cell line was displayed by functionalized NPs compared to free drug. Co administration of Gnb and Cap NPs displayed significant targeting potential, reduction in tumor volume while restoring the biochemical parameters viz., SOD, catalase, TBARS and protein carbonyl, towards normal levels when compared with toxic group. Significant down regulation was observed for anti-apoptotic proteins (MMP-9) and up regulation of pro-apoptotic proteins (caspase-3, caspase-9 and MMP-9) with co-therapy of Gnb and Cap NPs, when compared with individual therapy through Gnb/Cap. CONCLUSION: Potentiation of the action of Gnb when co administered with Cap NPs can be a promising breakthrough for developing safe, effective and targeted delivery for lung carcinoma therapy.

Modulation of oxidative stress response by flaxseed oil: Role of lipid peroxidation and underlying mechanisms.

Polyunsaturated fatty acids (PUFA's) are majorly classified as ω-3 and ω-6 fatty acids. The eicosapentaenoic acid (EPA, ω-3:20-5), docosahexaenoic acid (DHA, ω-3:22-6) and alpha-linolenic acid (ALA, ω-3:18-3) are known ω-3 fatty acids, extracted from animal (e.g fish oil) and plant sources (e.g flaxseed oil). Furthermore, linoleic acid (LA, ω-6:18-2) is recognized as ω-6 fatty acid and the most prominent biological fatty acid with a pro-inflammatory response. Flaxseed oil has variety of biological roles, due to the significant amount of ω-3/ω-6 fatty acids. Numerous studies have reported that ALA (ω-3:18-3) and LA (ω-6:18-2) has diverse pharmacological activities. The ALA (ω-3:18-3) and LA (ω-6:18-2) are recognised to be the pharmacological antagonist. For example, ALA (ω-3:18-3) is recognised as anti-inflammatory, whereas LA (ω-6:18-2) is considered to be pro-inflammatory. PUFA's get oxidized in three ways; firstly, free radical-mediated pathway, secondly non-free radical non-enzymatic metabolism, and lastly enzymatic degradation. The present report is an attempt to summarize various modes of PUFA's metabolism and elaborate biological effects of the associated metabolites concerning flaxseed oil.

GLA supplementation regulates PHD2 mediated hypoxia and mitochondrial apoptosis in DMBA induced mammary gland carcinoma.

The aim of the present study is to evaluate the effect of gamma linolenic acid (GLA) on mitochondrial mediated death apoptosis, hypoxic microenvironment and cholinergic anti-inflammatory pathway against 7, 12-dimethylbenz (a) anthracene (DMBA) induced mammary gland carcinoma. The effects of GLA were evaluated morphologically and biochemically against DMBA induced mammary gland carcinoma. The metabolic study was done for evaluation of biomarkers using 1H NMR. The present study was also verified through immunoblotting and qRT-PCR studies for the evaluation of various pathways. GLA treatment has a delineate implementation upon morphology of the tissues when evaluated through carmine staining, hematoxyline and eosin staining and scanning electron microscopy. GLA also demarked a commendatory proclamation of the fifteen key serum metabolites analogous with amino acid metabolism and fatty acid metabolism when recognized through1H NMR studies. The immunoblotting and qRT-PCR studies accomplished that GLA mediated mitochondrial death apoptosis, curtail hypoxic microenvironment along with hindrance of de novo fatty acid synthesis and also mediate the cholinergic anti-inflammatory pathway to proclaim its anticancer effects.

Comparative efficacy of alpha-linolenic acid and gamma-linolenic acid to attenuate valproic acid-induced autism-like features

The present study was undertaken to elucidate the effect of alpha-linolenic acid (ALA, 18:3, ω-3) and gamma-linolenic acid (GLA, 18:3, ω-6) on experimental autism features induced by early prenatal exposure to valproic acid (VPA) in albino wistar pups. The pups were scrutinized on the accounts of behavioral, biochemical, and inflammatory markers, and the results suggested that the GLA can impart significant protection in comparison to ALA against VPA-induced autism features. When scrutinized histopathologically, the cerebellum of the GLA-treated animals was evident for more marked protection toward neuronal degeneration and neuronal loss in comparison to ALA. Concomitant administration of ALA and GLA with VPA demonstrated a marked cutdown in the Pgp 9.5 expression with GLA having more pronounced effect. Henceforth, it can be concluded that ALA and GLA can impart favorable protection against the VPA-induced autism-like features with GLA having pronounced effect (AU)

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Novel glycoside from Wedelia calendulacea inhibits diethyl nitrosamine-induced renal cancer via downregulating the COX-2 and PEG2 through nuclear factor-κB pathway.

A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13)-ene-28-oic acid-3-O-ß-D-glucopyranoside (HEG) was isolated from whole plant of Wedelia calendulacea (Compositae). The structure was elucidated and established by standard spectroscopy approaches. Diethylnitrosamine (DEN) (200 mg/kg) and ferric nitrilotriacetate (Fe-NTA) (9 mg/kg) were used for induction of renal cell carcinoma (RCC) in the rats. The rats were further divided into different groups and were treated with HEG doses for 22 weeks. Anti-cancer effect in RCC by HEG was dose dependent to restrict the macroscopical changes as compared to DEN + Fe-NTA-control animals. Significant alteration in biochemical parameters and dose-dependent alleviation in Phase I and Phase II antioxidant enzymes were responsible for its chemo-protective nature. HEG in dose-dependent manner was significant to alter the elevated levels of pro-inflammatory cytokines and inflammatory mediators during RCC. The histopathological changes were observed in the HEG pre-treated group, which was proof for its safety concern as far as its toxicity is concerned. The isolated compound HEG can impart momentous chemo-protection against experimental RCC by suppressing the cyclooxygenase (COX-2) and prostaglandin E2 (PGE2) expression via nuclear factor-kappa B (NF-κB) pathway.

Comparative efficacy of alpha-linolenic acid and gamma-linolenic acid to attenuate valproic acid-induced autism-like features.

The present study was undertaken to elucidate the effect of alpha-linolenic acid (ALA, 18:3, ω-3) and gamma-linolenic acid (GLA, 18:3, ω-6) on experimental autism features induced by early prenatal exposure to valproic acid (VPA) in albino wistar pups. The pups were scrutinized on the accounts of behavioral, biochemical, and inflammatory markers, and the results suggested that the GLA can impart significant protection in comparison to ALA against VPA-induced autism features. When scrutinized histopathologically, the cerebellum of the GLA-treated animals was evident for more marked protection toward neuronal degeneration and neuronal loss in comparison to ALA. Concomitant administration of ALA and GLA with VPA demonstrated a marked cutdown in the Pgp 9.5 expression with GLA having more pronounced effect. Henceforth, it can be concluded that ALA and GLA can impart favorable protection against the VPA-induced autism-like features with GLA having pronounced effect.

Melastoma malabathricum Linn attenuates complete freund's adjuvant-induced chronic inflammation in Wistar rats via inflammation response.

BACKGROUND: Natural products use for arthritis treatment is gaining importance in the medical worldt. Various studies reports medical importance of Melastoma malabathricum Linn. (MM) (Melastomataceae), also known as "putki," has a broad range of health benefits, for its free radical scavenging constituents. The current investigation scrutinizes the antioxidant and anti-inflammatory effect of MM against adjuvant-induced arthritis in experimental rats. METHODS: High-performance thin layer chromatography (HPTLC) was used for estimation of phytochemical-constituents present in the MM extract. Protective effect of MM extract in Wistar rats was estimated using CFA-induced model. The rats were divided into different groups with six rats in each group. All animals received oral administration of MM and indomethacin for 28 days. The body weight and arthritic score were scrutinized at regular intervals. At the end of experimental protocol, the rats were sacrificed, and blood samples were used for antioxidant, hematological parameters, pro-inflammatory and inflammatory mediator, respectively. Histopathological observation was used to evaluate the protective effect of MM extract. RESULT & DISCUSSION: Current study confirmed the preventive effect of MM against adjuvant-induced paw edema, paw redness and arthritic progression. MM significantly (P < 0.001) modulated the oxidative stress parameters as well as hematological parameter induced by CFA. The result also altered the distorted level of proinflammatory mediators and inflammatory mediator, which further reinforce the implication of MM in CFA induced arthritis. Histological analyses of joints of rats showed a reduction in the synovial hyperplasia and mononuclear infiltration in the MM treated group which provides evidence for the antiarthritic effect of MM. CONCLUSION: From above parameters our study states that the MM is capable of restraining the alteration produced via adjuvant-induced arthritis in aminals. The repressing effect of MM could be attributed, at least in part, to antioxidant, hematological and anti-inflammatory effect. Figure Caption: Melastoma Malabathricum Linn Attenuates Complete Freund's Adjuvant-Induced Chronic Inflammation in Wistar rats by Inflammation Response.

Chemomodulatory effect Melastoma Malabathricum Linn against chemically induced renal carcinogenesis rats via attenuation of inflammation, oxidative stress, and early markers of tumor expansion.

Melastoma malabathricum Linn (MM) has high valued for its commercial significance. Indian market (northeast) has great demand for the plants, which extended, its use as a traditional home remedy due to its anti-inflammatory effects. In this study, we scrutinize the therapeutic and protective effect of MM against diethylnitrosamine (DEN) and ferric nitrilotriacetate (Fe-NTA)-induced renal carcinogenesis, renal hyperproliferation, and oxidative stress in rats. Liquid chromatography mass spectroscopy (LC-MS) was used for identification of phytoconstituents. Administration of DEN confirmed the initiation the renal carcinogenesis via enhancing the expansion of tumor incidence. Intraperitoneally, administration of Fe-NTA boost the antioxidant enzymes (phase I), viz., superoxide dismutase (SOD), catalase (CAT), glutathione reductase (GR), glutathione peroxidase (GPx) and phase II, viz., quinone reductase (QR) and glutathione-S-transferase (GST). It also increased the content of renal lipid peroxidation (LPO), hydrogen peroxidase (H2O2) with decrease content in glutathione content (GSH). It also increased the renal biochemical and non-biochemical parameter. It also confirmed the augment the level of thymidine [3H] incorporation into renal DNA, ornithine decarboxylase (ODC) activity and increased the generation of proinflammatory (TNF-α, IL-6 and IL-ß) and inflammatory mediator (PGE2). We also analyzed the macroscopic and histologic of renal tissue. In addition, the effect of phytoconstituent of MM extract was evaluated in silico and free radical scavenging activity against the DPPH and ABTS free radicals. LC-MS confirmed the presence of quercetin >gallic acid in MM extract. Renal carcinogenesis rats treated with MM (100, 250, and 500 mg/kg) confirmed the significantly (P < 0.001) protective effect via reduction the antioxidant (phase I and phase II) enzymes, biochemical parameter and restore the proinflammatory and inflammatory mediator at dose dependent manner. MM altered the ODC and thymidine activity in renal DNA. The chemoprotective effect of MM was confirmed via decreased the renal tumor incidence, which was confirmed by the macroscopic and histopathological observation. Consequently, our result suggests that MM is a potent chemoprotective agent and suppresses DEN+ Fe-NTA-induced renal carcinogenesis, inflammatory reaction, and oxidative stress injury in Wister rats.

α-Chymotrypsin regulates free fatty acids and UCHL-1 to ameliorate N-methyl nitrosourea induced mammary gland carcinoma in albino wistar rats.

This study was undertaken to investigate the effect of α-chymotrypsin on methyl nitrosourea (MNU) induced mammary gland carcinoma in albino wistar rats. Animals were randomized into four groups (six animals in each). Group I (sham control 0.9 % normal saline p.o.); Group II (toxic control, MNU 47 mg/kg, i.v.); Group III (α-chymotrypsin, 5 mg/kg, p.o.); Group IV (α-chymotrypsin, 10 mg/kg p.o.). Toxicity was induced by single i.v. injection of MNU followed by α-chymotrypsin supplementation therapy for 100 days. MNU treatment was evident with increased alveolar bud count, differentiation score, upregulated inflammatory enzymes markers (COX, LOX and NO) antioxidative stress markers (TBARs, SOD, catalase and GSH).MNU associated toxicity was also ascertained by PGP 9.5 and NF-κB expression in the mammary gland tissue followed by FAME analysis for fatty acid profiling. α-chymotrypsin afforded significant protection against the deleterious effects of MNU.

Effect of ß-sitosterol against methyl nitrosourea-induced mammary gland carcinoma in albino rats.

BACKGROUND: The present study was in quested to study the effects of ß-sitosterol on methyl nitrosourea (MNU) induced mammary gland carcinoma in albino wistar rats. METHODS: Animals were randomized and divided into four groups of eight animals each. Group I (sham control 1 % CMC in normal saline p.o.); Group II (toxic control, MNU 47 mg/kg, i.v); Group III (MNU 47 mg/kg, i.v + ß-sitosterol, 10 mg/kg, p.o); Group IV (MNU 47 mg/kg, i.v + ß-sitosterol, 20 mg/kg, p.o). Toxicity was induced by single i.v. injection of MNU followed by ß-sitosterol supplementation therapy for 115 days at the dose mentioned above. RESULTS: Treatment with ß-sitosterol evidenced decrease in the alveolar bud and lobule score in the whole mount of the mammary gland. ß-sitosterol exhibited diminishing effect on oxidative stress through synchronizing lipid and enzymatic antioxidant defense. A significant decrease in the saturated and unsaturated fatty acid was evident with the MNU treatment and ß-sitosterol demonstrated a marked effect on it. Pgp 9.5 expression was dose dependently upregulated by ß-sitosterol treatment in comparison to MNU treatment. On the contrary, downregulated NF-kB expression was perceived, when ß-sitosterol was concomitantly administered with MNU. CONCLUSION: ß-sitosterol afforded significant protection against the deleterious effects of MNU.

Rutin attenuates intestinal toxicity induced by Methotrexate linked with anti-oxidative and anti-inflammatory effects.

BACKGROUND: Methotrexate (MTX) is recognized as an anti-metabolite in cancer chemotherapy and is associated with various toxicities assigned to inflammation and oxidative stress. Rutin has been reported to have significant anti-inflammatory, antioxidant along with antiulcer properties. The present study was undertaken to corroborate the effect of rutin against MTX induced intestinal toxicity in experimental animals. METHOD: Six groups of rats (n = 6) were dosed with normal saline (3 ml/kg,i.p.); MTX (2.5 mg/kg,i.p.); rutin (50 and 100 mg/kg,i.p.); rutin + MTX (50 mg/kg + 2.5 mg/kg,i.p.); rutin + MTX (100 mg/kg + 2.5 mg/kg,i.p.) for seven consecutive days and sacrificed on eighth day. The intestinal contents were scrutinized physiologically (pH, total acidity, free acidity, CMDI), biochemically (TBARS, protein carbonyl, SOD, catalase and GSH) and for immunoregulatory cytokines (IL-2, IL-4 and IL-10). RESULTS AND DISCUSSION: The administration of rutin demonstrated significant protection against intestinal lesions damaged by MTX. The treatment with rutin elicited noticeable inhibition of free acidity (26.20%), total acidity (22.05%) and CMDI (1.16%) in the experimental animals similar to control. In MTX treated toxic group, the levels of oxidative markers and immunoregulatory cytokines significantly increased in comparison to control, which was subsequently restored after rutin treatment. Rutin also demonstrated 75.63, 81.00 and 80.43% inhibition of cyclooxygenase-1 and 2, and 15-lipoxygenase respectively. CONCLUSION: The positive modulation of MTX toxicity could be attributed to the free radical scavenging and anti-inflammatory (dual inhibition of arachidonic acid pathways) potential of rutin.

Effect of lycopene against gastroesophageal reflux disease in experimental animals.

BACKGROUND: Lycopene is a robust antioxidant with significant antiulcer activity. Henceforth, the present study was ventured to elucidate the effect of lycopene on experimental esophagitis. METHODS: Groups of rats were subjected to forestomach and pylorus ligation with subsequent treatment with lycopene (50 and 100 mg/kg, po) and pantoprazole (30 mg/kg, po). RESULTS: Treatment with lycopene evidenced sententious physiological protection when scrutinized for pH, acidity (total and free), volume of gastric juices and esophagitis index. Lycopene further embarked diminishing effect on oxidative stress through synchronising lipid and protein peroxidation along with regulating the enzymatic activity of SOD and catalase. Lycopene also modified the levels of immunoregulatory cytokines (IL- 1ß and IL-6) favourably. The dose dependent efficacy of lycopene in the current experimental condition was also attested when exemplified morphologically through scanning electron microscopy. CONCLUSION: From the current line of evidences, it was concluded that lycopene can impart momentous protection against experimental esophagitis by wrapping up the reactive oxygen species and through dual inhibition of the arachidonic acid pathway.

Dual inhibition of arachidonic acid pathway by mulberry leaf extract.

The present work investigates the anti-inflammatory, analgesic and antipyretic activity of methanolic extract of mulberry leaves of variety S-1, S-13 and S-146. The S-146 extract was further evaluated for its efficacy against adjuvant arthritis in albino rats followed by inhibitory potential for COX 1, COX 2 and 5 LOX. The HPLC analysis enumerated the presence of morin, reversterol, scopoletin and 7-hydroxy coumarin as the major constituents. The anti-inflammatory, antipyretic and analgesic activity observed in the present experiment could be accredited to the dual inhibition in the AA pathway. The inhibition of COX and LOX enzymes could be imparted to the presence of resveraterol, morin, scopoletin and 7-hydroxy coumarin.

Effect of standardized fruit extract of Luffa cylindrica on oxidative stress markers in hydrogen peroxide induced cataract.

OBJECTIVE: The ability of Luffa cylindrica Roem fruit extract (LCE) to modulate biochemical parameters was investigated by in vitro studies for its role in hydrogen peroxide induced cataract on isolated goat lenses which were incubated for 72 h at 37°C. MATERIALS AND METHODS: Test groups contained 5, 10, 15, 20, 25, and 30 µg/ml of LCE along with 1 ml of H2O2 (0.5 mM) as cataract inducer. Lenses were examined for morphological variation and transparency periodically during the incubation. Biochemical parameters such as superoxide dismutase (SOD), reduced glutathione (GSH), total protein content (TPC), and malondialdehyde (MDA) were estimated. RESULTS: SOD, GSH, and TPC levels were found to increase proportionally with the concentration of LCE. However, MDA levels were found to be inversely proportional to the concentration of LCE. Opacity was graded as per "lens opacities classification system III." Morphological examination suggested that LCE (25 µg/ml) maintained a vision for 44 h. No lens in LCE dose groups developed dense nuclear opacity after 24 h as opposed to 80% in negative control. CONCLUSION: The results suggest that LCE can delay the onset and/or prevent the progression of cataract which can be attributed to the presence of adequate phenolics, flavonoids, and Vitamin A and its high nutritional value. This preliminary study can be further synergized by testing LCE against other in vivo and in vitro models of cataract.

Anti-inflammatory potential of alpha-linolenic acid mediated through selective COX inhibition: computational and experimental data.

The present work investigates the anti-inflammatory activity of alpha-linolenic acid (ALA) and linoleic acid (LA) using computational and experimental analysis. The binding affinity of ALA and LA was appraised for cyclooxygenase 1 (COX-1), cyclooxygenase 2 (COX-2), and 5-lipoxygenase (5-LOX) using AutoDock 4.2 and AutoDock Vina 1.1.2. Anti-inflammatory activity of ALA (2 and 4 ml/kg, i.p.) (55.65 % v/v) and LA (2 and 4 ml/kg, i.p.) (55 % v/v) was further assayed using the rat paw edema test against a variety of phlogistic agents including carrageenan, arachidonic acid, prostaglandin, and leukotriene, respectively. ALA (2 and 4 ml/kg, i.p.) and LA (2 and 4 ml/kg, i.p.) were further tested for their efficacy against complete Freund's adjuvant (CFA)-induced (0.05 ml) arthritis in albino rats. Following CFA-induced arthritis, ALA and LA were tested for their inhibitory proficiency against COX-1, COX-2, and 5-LOX in vitro. The present study commends that the anti-inflammatory potential of ALA could be attributed to COX inhibition, in particular, COX-2.

Effect of Perilla frutescens fixed oil on experimental esophagitis in albino Wistar rats.

The present study was undertaken to elucidate the effect of Perilla frutescens fixed oil on experimental esophagitis in albino rats. A group of rats (n = 6), treated with control vehicle (0.9% NaCl in double distilled water, 3 mL/kg, i.p.) and Perilla frutescens fixed oil (100%) (1, 2, and 3 mL/kg, i.p.), or pantoprazole (30 mg/kg, i.p.), were subjected to pylorus and forestomach ligation. Animals were sacrificed after 6 h and evaluated for the gastric pH, volume of gastric juices, total acidity, esophagitis index and free acidity. Esophageal tissues were further subjected to estimations of TBARS, GSH, catalase, and SOD. Treatment with fixed oil significantly inhibited the gastric secretion, total acidity, and esophagitis index. The oil also helped to restore the altered levels of oxidative stress parameters to normal. The present study also makes evident the in vitro antihistaminic and anticholinergic activity of alpha linolenic acid (ALA) (18 : 3, n - 3) on isolated rat ileum preparation. The lipoxygenase inhibitory, histamine antagonistic, antisecretory (anticholinergic), and antioxidant activity of the oil was attributed for its efficacy in reflux esophagitis.

Antiarthritic effects of Ajuga bracteosa Wall ex Benth. in acute and chronic models of arthritis in albino rats.

OBJECTIVE: To evaluate the antiarthritic activity of Ajuga bracteosa using albino rats. METHODS: The antiarthritic activity of 70% ethanolic extract of Ajuga bracteosa (EEAB) was evaluated against turpentine oil- and formaldehyde- induced acute non immunological and complete freund's adjuvant (CFA)-induced chronic immunological arthritis in albino rats. RESULTS: EEAB showed a significant (P<0.05) and dose dependent inhibitory effect against acute and chronic models of arthritis. EEAB exhibited better antiarthritic activity than the standard aspirin. CONCLUSIONS: EEAB exhibits a significant and promising antiarthritic activity against acute and chronic arthritis and supports the traditional use of Ajuga bracteosa for rheumatism and other inflammatory diseases.

Effect of aloe vera (Aloe barbadensis Miller) gel on doxorubicin-induced myocardial oxidative stress and calcium overload in albino rats.

Administration of a single dose of doxorubicin (DOX) (7.5 mg/kg, i.v.) produces cardiotoxicity, manifested biochemically by significant decrease in blood glutathione (GSH) and tissue GSH along with elevated levels of serum lactate dehydrogenase (LDH) and serum creatine phosphokinase (CPK). In addition, cardiotoxicity was further confirmed by significant increase in lipid peroxides expressed as malondialdehyde (MDA, secondary indicator of lipid peroxidation), tissue catalase and tissue superoxide dismutase (SOD). Administration ofA. vera gel (100 and 200 mg/kg) orally for 10 days produced a significant protection against cardiotoxicity induced by DOX evidenced by significant reductions in serum LDH, serum CPK, cardiac lipid peroxides, tissue catalase and tissue SOD along with increased levels of blood and tissue GSH. The results revealed that A. vera gel produced a dose dependent protection against DOX induced cardiotoxiaty.

Linum usitatissimum (linseed/flaxseed) fixed oil: antimicrobial activity and efficacy in bovine mastitis.

PURPOSE: In vitro antimicrobial activity and in vivo therapeutic efficacy of L. usitatissimum (linseed/flaxseed) fixed oil in bovine mastitis were investigated. METHOD: In vitro antimicrobial activity of L. usitatissimum fixed oil was evaluated against a number of microorganisms by disc diffusion method and MIC determination. The in vivo efficacy of the oil was evaluated in nine mastitis-affected cows divided into three groups (three in each group), following once-a-day intramammary infusion of oil, cefoperazone or an oil-cefoperazone combination for 7 days and by monitoring the California mastitis test score, somatic cell count and microbial count in milk samples. RESULTS: The in vitro antimicrobial activity of the oil against Staphylococcus aureus, Streptococcus agalactiae and Escherichia coli was comparable to that of cefoperazone while the antimicrobial activity against Enterococcus faecalis, Micrococcus luteus and Candida albicans, was greater than that of cefoperazone. In the in vivo study, the oil exhibited significant reduction in the California mastitis test score and somatic cell count in milk samples from infected udders following 7 days of intramammary administration suggesting its anti-inflammatory effect. The microbial count in milk samples was also reduced significantly following oil treatment. The effects were comparable to the treatment by cefoperazone (Mastiwock) alone or in combination with the oil. Apparently, the anti-inflammatory and antimicrobial properties of the oil contribute to its therapeutic efficacy in mastitis; the oil could be used as an alternative treatment for bovine mastitis CONCLUSION: The results suggest possible therapeutic potential of L. usitatissimum fixed oil in bovine mastitis.

Anti-inflammatory, analgesic and antipyretic activities of Linum usitatissimum L. (flaxseed/linseed) fixed oil.

The fixed oil of L. usitatissimum (flaxseed/linseed) inhibited PGE2-, leukotriene-, histamine- and bradykinin-induced inflammation. The oil also inhibited arachidonic acid-induced inflammation, suggesting its capacity to inhibit both cyclooxygenase and lipoxygenase pathways of arachidonate metabolism. In tail immersion model, the oil raised the pain threshold to a lesser extent than morphine but showed excellent peripherally acting, analgesic activity comparable to aspirin, against acetic acid-induced writhing in mouse. In typhoid paratyphoid A/B vaccine-induced pyrexia, the oil showed antipyretic activity comparable to aspirin. The oil contains 57.38% alpha-linolenic acid. Dual inhibition of arachidonic acid metabolism, antihistaminic and antibradykinin activities of the oil could account for the biological activity and the active principle could be alpha-linolenic acid an omega-3 (18:3, n-3) fatty acid.