A series of twenty four newly synthesized 1-aroyl-3-aryl-5-hydroxy-5-(2,4-dichloro-5-fluorophenyl) pyrazolines (3) and 1H-3-aryl-5-hydroxy-5-(2,4-dichlore-5-fluorophenyl)-pyrazoles (6) were tested for cytostatic and cytotoxic effects on in a primary three cell line-one dose anticancer assay against NCI-H 460 (Lung), MCF 7(Breast) and SF 268 (CNS). Proliferation of these cancer cell lines was strongly inhibited by eleven compounds. These eleven compounds were then passed on for evaluation in the full panel of 60 cell lines derived from seven cancer types namely, Lung, Colon, Melanoma, Renal, Ovarian, CNS and Leukemia. These compounds showed antiproliferative activity on the whole cell panel. Compound 1H-pyrazole, 6d [3,4-methylenedioxy at C 3] showed highest activity with Growth Inhibition (GI50 value <10 μ M against all tested 60 cell lines except for Leukamia CCRF-CEM, HL-60TB, K-562 cell lines. Whereas hydroxypyrazolines 3i, 3k 3m, 3o, 3p and 3q showed moderate activity with GI50 value <50 μM against all tested 60 cell lines. Compounds 3h, 3c, 6c appear to be less active with GI50 value >100μM for some of the tested cell lines. Compound 6a appears to be least active with GI50 value >100 μM for almost all the tested cell lines. The Total Growth Inhibition (TGI) and Lethal Concentration (LC50) values for the most active compound [6d] found to be >100 μM for Leukemia cell lines and for the other cell lines these values remain <20 μM and hence prove to be a cytostatic and cytotoxic for these lines. Henco these newly synthesized pyrazole and pyrazoline derivatives showed promising antiproliferative property.
Antitubercular activity of 7-methyljuglone derivatives series were subjected to quantitative structure activity relationship analysis with an attempt to derive and understand a correlation between the biological activity as dependent variable and various descriptors as independent variables. Several statistical regression expressions were obtained using multiple linear regression analysis. The QSAR models were generated using 19 compounds. The predictive ability of the resulting QSAR models was evaluated employing the leave one-out method of cross validation. Several statistical regression expressions were obtained using multiple linear regression analysis. The analysis of best resulted in the following 2-D model which suggests that pIC50 = [-0.025] MR+[0.278] StrE+[0.028] p+[3.04459] HOMO, n = 19, r2= 0.87961, r2 = 0.81048, variance = 0.0805, SD = 0.4324, F = 85.78. The study suggested that substitution of group at Rl and R3 position on naphthoquinones ring with hydrophobic nature and low bulkiness are favorable for the antitubercular activity in the concerned microbes. The quantitative structure activity relationship study provides important structural insights in designing of potent antitubercular agents.
Joloo is a traditional herbal formulation used in the management of tumour of the breast in southwestern Nigeria. The acute and subchronic toxicity studies of Joloo have been reported previously but the chronic toxicity has not been investigated. The study was undertaken to evaluate the long-term toxic effect of Joloo on mice. Ethanolic extract of Joloo was administered to four groups of mice weighing 27.5±1.4 (N = 10/group) Repeated doses (400, 800 and 1600 mg kg -1 b.wt.) were administered orally for 91 days. Parameters observed include, body and relative organ weights, haematology, biochemical analysis, antioxidant activities and histologic studies. There were no adverse effects on the generał condition, body and relative organ weight, red blood cells and white blood celi. However there were significant increase in leucocytes, GPx, CAT and SOD at 800 and 1600 mg kg -1 b.wt. The histoarchitecture of the liver, heart and the spleen revealed slight alteration (mild necrosis) and there was dose-dependent though insignificant increase in some of the biochemical analytes (ALT and AST) at 1600 mg kg -1 b.wt. Based on these findings it can be inferred that Joloo is devoid of toxicity at 400 and 800 mg kg -1 b.wt. and possess strong antioxidant activities, whereas high dose (1600 mg kg -1 b.wt.) may be associated with some toxicity concerns.
The objective of the present study is to evaluate the antioxidant potential of ethanolic extract of Murraya koenigii leaf on enzymatic, non enzymatic antioxidants and ultrastructural changes in liver of streptozotocin (STZ) induced diabetic rats. Effect of oral administration of M. koenigii leaves extract (200 mg kg-1 body weight) on the levels of blood glucose, plasma insulin glycosylated hemoglobin, Thiobarbituric Acid Reactive Substances (TBARS), hydroperoxides, enzymatic and non-enzymatic antioxidants were estimated in STZ induced diabetic rats. Ultrastructural changes in the liver were also examined. Glibenclamide was used as a standard drug. The elevated levels of blood glucose, glycosylated hemoglobin, TBARS, hydroperoxides and decreased level of insulin observed in diabetic rats were significantly altered after treatment with the M. koenigii. The altered enzymatic and non-enzymatic antioxidants in the liver of streptozotocin induced diabetic rats, were restored to near normal levels by treatment with the M. koenigii leaves extract. Ultrastructure analysis of the liver of diabetic rat revealed a reduction in the Rough Endoplasmic Recticulum (RER) and swelling of mitochondria in the hepatocytes and these abnormalities were restored to near normal morphology by the treatment of rats with M. koenigii leaf extract. Our results suggested that the ethanolic extract of M. koenigii possess potent antioxidant properties which may be due to the presence of biologically active ingredients such as carbazole alkaloids, glycosides, triterpenoids and phenolic compounds. Thus the hepatoprotective and antidiabetic properties of M. koenigii leaves were probably of its antioxidant property.
Cyclophosphamide (CP) is one among the important therapeutic chemotherapy drug used worldwide. Damage to normal tissues due to toxic metabolites limits the usage of CP efficiently for treating various cancers. In the present study, hepatoprotective effect of Momordica charantia Linn. (Cucurbitaceae) against CP induced hepatotoxicity in rats was evaluated. Hepatocellular damage in rats was induced by injecting CP i.p. (total of 200 mg kg -1, b.wt.) for 2 days. Momordica charantia fruit aqueous extract (MCE) (300 mg kg -1 b.wt.) was administered orally for 12 days for treatment. Protective effect of MCE was evaluated by assessing the liver marker enzymes such as AST, ALT, ALP, LDH and γ-GT in serum, AST and ALT in Hver tissues and biochemical parameters such as total protein, urea, creatinine, uric acid, total and direct bilirubin. Liver marker enzymes and clinical chemistry parameters were significantly altered in CP intoxication. These alterations were significantly normalized in animals administered with MCE. Protective effect of MCE could be due to radical-scavenging and antioxidant properties of the MCE. MCE could had been demonstrated these properties due to the presence of phytochemical components that include polyphenols, alkaloids, terpenoids, glycosides and tannins. Present findings supported that the treatment with MCE could be helpful against hepatocellular damage, owing to its hepatoprotective property.
Abrus precatorius Linn, is a leguminous plant of the fabaceae family whose stem, bark, leave and roots are widely used for medicinal purposes in tropical and subtropical regions of the world. The plant parts are purgative, emetic, tonic, anti-phlogistic, aphrodisiac and anti-ophthalmic agents. The purpose of the present investigation was to study antioxidant, anti-inflammatory and analgesic activity of Abrus precatorius Linn, ethanolic seed extracts by soxhlet method. The free radical scavenging activity of extract was carried out by 1,1-diphenyl-2-picrylhydrazyl method and anti-inflammatory activity by carrageenan induced rat paw edema and analgesic activity carried out by tail flick and tail immersion method. The extract showed significant activity i.e., 80.1±0.34% at 300 μg mL-1. The extract was evaluated for its anti-inflammatory activity it showed significant anti-inflammatory activity i.e., 62.68% at 375 mg kg-1 by carrageen induced method. Further, the extract was evaluated for analgesic activity and the extract showed significant activity at 300 mg kg-1 after 90 min interval by tail flick and tail immersion method. As ethanolic extract of Abrus precatorius Linn, was found to have potent antioxidant, anti-inflammatory and analgesic potential. The present study concludes that seeds of Abrus precatorius Linn, can be used as good natural antioxidant to treat free radical induced disease.
N-nitrosamines are human carcinogens that may form in the environment by both natural and anthropogenic actions. Edible tissues of aquatic organisms are susceptible to contamination due to exposure from water, sediment and food processing methods; therefore, possible health risk may exist. The purpose of this study was to examine absorption and metabolism patterns of seven N-nitros amine compounds in various compartments of commercially-a vail able Red Swamp crayfish. Crayfish samples were purchased from a wholesale dealer and exposed to N-nitrosamines at varying concentrations (0 (control), 10, 20, 40, 80 ng mL-1). Samples were washed in tap water and boiled for 7-10 min at 100°C. Crayfish were dissected into shell, hepatopancreas and tail meat. N-nitrosamines were extracted using standard solid-phase extraction protocol with Extrelut and Florisil cartridges. N-nitrosamines were identified and quantified using GC-FID. N-nitrosamines were not detected in control samples. Absorption of the various N-nitrosamines depended on treatment concentration, duration and compartment. At higher concentrations, NDBA (N-nitrosodibutylamine) concentrations could be used as an indicator of NPIP, NPYR, NDPA and NMEA levels. NPIP could be used to predict the levels of NDMA, NDPA, NPYR and NMEA when crayfish are exposed to N-nitrosamines for 6 and 24 h periods. NPYR had the highest rate of metabolism while NDMA had the slowest. Understanding absorption and metabolism patterns can help determine possible health risk due to consumption of crayfish.
Aggression is a common adverse effect in Anabolic Androgenic Steroids (AASs) abusers. The present study aimed to investigate possible interaction between nandrolone decanoate and amino acids on behavior and neurotransmitters. Rats received repeated injections of nandrolone (10 mg kg-1, i.m., once weekly), amino acids mixture (0.8 g kg-1, p.o., once daily) and their combination for eight weeks. Defensive aggression, open field and hot plate tests were measured at the end of experiments. Serotonin (5-HT), Dopamine (DA), Norepinephrine (NE) and glutamate were measured in specific brain regions. Analysis of data showed that nandrolone, amino acids and their combination increased aggression and differentially affected brain neurotransmitters. Nandrolone decreased rearing, while amino acids decreased ambulation, increased rearing and grooming frequencies. Taken together, our data indicate that treatment with nandrolone decanoate, amino acids mixture and their combination may induce neurochemical alterations in brain regions regulating aggressive behavior.
Donor blood represents one of the most important sources of therapeutic preparations required for various cases necessitating transfusions of plasma or erythrocytes. While, thorough screening tests for, for example, syphilis and other infectious agents are conducted (as a routine test), other analytical tests aiming at the detection of drug residues are rare (if at all) performed. The present study was designed-as a preliminary study-to discover drugs of abuse in blood in donating King Abdul-Aziz Hospital (Makkah, Saudi Arabia). A total of 300 EDTA plasma samples (approximately 1.5 mL each) was obtained from a King Abdul-Aziz Hospital blood bank from voluntary blood donors after regular whole blood donation. Immediately after sampling, the plasma was separated in a centrifuge, transferred to a 2 mL Eppendorf tube and frozen until analysis. All donors were males; in the preliminary test, 28 cases (9.3%) were positive for one of screened substance (1 case; 0.3% were positive for amphetamine, 7 cases (2.3%) were positive for tricyclic antidepressants TCA and 20 cases (6.7%) were positive for tetrahydrocannabinol (THC). On the second screen, confirmed cases were 20 cases (6.7%), 1 case (0.3%) was positive for amphetamine, 2 cases (0.7%) were positive for TCA and 17 cases (5.7%). Positive cases were significantly younger than negative cases (25.80±2.58 vs. 27.34±3.08 years, respectively). The present study sheds light on the importance of screening blood and blood products in blood banks for commonly abused drugs, besides regular checkup for infectious diseases. It is advised to put this step as a routine in blood screening as much as the facilities permit to do so.
In the present study Acacia catechu-Catechin (CTN) was evaluated for antiamnesic and antioxidant activity using various in vivo models. Scopolamine and natural aging were used to induce experimental amnesia in mice. The tested does of CTN (40, 20 and 10 mg kg-1) significantly enhanced the learning capacity and retention of memory in Passive Shock Avoidance and Spatial Water cage exteroceptive behavioural models. Pre-treatment with CTN restored the increased levels of lipid peroxidation and reduced glutathione due to scopolamine and natural aging. A dose dependent CTN (40, 20 and 10 mg kg-1) antioxidant activity of Thiobarbituric acid reactive substances (TBARS) and reduced glutathione (GSH) in whole brain was seen, which were comparable to Standard Piracetam (400 mg kg-1). Hence, it is worthwhile to explore the potential of this Acacia catechu-Catechin in the management of Neurodegenerative disorders of the type Alzheimer's disease.
The aim of this study was to evaluate the efficacy and safety of newer drug Aceclofenac 100 mg BD compared to Diclofenac Sodium 50 mg three times daily tid in post extraction dental pain. A total number of 100 patients posted for third molar extraction were recruited for the study. Those who met the inclusion criteria (n = 51) were randomized into two treatment groups A and B. Group A received T. Diclofenac Sodium and Group B received T. Aceclofenac. On the day of surgery patients were given the study drugs and Visual Analog Scales (VAS) to assess the pain intensity for 5 days. Baseline pain intensity immediately after surgery and at 8 h was recorded on the day of surgery. On day 5 evaluated statistically using one way analysis of variance. The statistical analysis of pain intensity using VAS showed that 78% of patients showed severe baseline pain intensity and at the end of 8 h on the first day of surgery, Diclofenac group showed 27% reduction in pain intensity and 40% reduction in Aceclofenac group (p<0.05). On day 5 pain reduction was 95% and 100% in Diclofenac and Aceclofenac group, respectively. Global assessment and safety assessment showed better gastrointestinal profile for the Aceclofenac than Diclofenac sodium. It proves that Aceclofenac has a rapid onset and prolonged pain relief and statistically significant analgesic effect in the immediate postoperative period of 8 h in comparison to Diclofenac sodium.
The present study was undertaken to investigate hepatoprotective activity of Clitoria ternatea seed and root and Vigna mungo seed against acetaminophen- and carbon tetrachloride-intoxicated rats. The liver functioning was evaluated by measuring serum marker enzymes and hepatic fibrosis was accessed by measuring collagen content in terms of p-hydroxyproline levels. Mast cell infiltration and potentiation of phenobarbitone-induced sleeping time were also measured. In addition, serum bilirubin, creatinine, lipid peroxidation and antioxidant parameters were also estimated. C. ternatea and V. mungo seed extracts significantly (p<0.05) decreased SGOT, SGPT, ALP and total bilirubin in both acetaminophen and CCl 4 - intoxicated rats. The C. ternatea root extract, showed similar results only in CCl 4 - intoxicated rats. These findings were further supplemented by histopathological studies of liver tissues. Hepatic collagen content as evident from decreased (p<0.05) hydroxyproline levels and hepatic mast cell infiltration were significantly decreased in extracts pre-treated animals. In addition, C. ternatea and V. mungo seed extracts significantly (p<0.05) reduced hepatic lipid peroxidation as evident from the decreased MDA, increased antioxidant enzymes activities and GSH levels in the liver tissues. The V. mungo seed extract significantly potentiated barbiturate-induced sleeping time. The findings of study suggested that C. ternatea and V. mungo possess potent hepatoprotective activity. The hepatoprotective activity of C. ternatea could be attributed to antioxidant properties and prevention of pre-inflammatory changes. The hepatoprotective activity of V. mungo could be attributed partly to the hepatic microsomal enzyme inhibition and partly to the antioxidant properties.
The present study evaluated the hepatoprotective effects and anti-oxidant activities of methanol leaf extract of Senna occidentalis against acetaminophen-induced hepatic injury in rats. The plant was extracted by cold maceration in 80% methanol for 48 hours. Acute toxicity test was done in rats orally. Hepatoprotective activity of the extract was investigated in rats challenged with acetaminophen (2000 mg kg-1). Twelve hours post challenge, extract at 75, 150 and 300 mg kg-1 (per os) were administered to rats for 4 days. Silymarin was used as positive control. Serum (alanine aminotransaminase) ALT, (aspartate aminotransferase) AST, (alkaline phosphatase) ALP, total bilirubin and total protein levels were assayed. Pentobarbitone-induced sleeping time was carried out on day 4. The effect of the extract on erythrocyte membrane stability was determined. Concentrations ranging from 10-400 μg mL-1 were assayed (in vitro) for antioxidant activities using the DPPH and FRAP spectrophotometric methods. The extract at 150 and 300 mg kg-1 doses significantly (p<0.05) reduced acetaminophen-mediated increase in serum transaminases (AST, ALT and ALP) and bilirubin with increase in total serum protein values. The extract exerted maximal effect at 300 mg kg-1. Acetaminophen-induced prolonged pentobarbitone sleeping time was significantly (p<0.05) reduced in the groups treated with 150 and 300 mg kg-1 of the extract. Using the DPPH assay, the extract showed 60% antioxidant activity when compared with ascorbic acid (79%) at 400 μg mL-1. FRAP assay gave 1.7 FRAP value compared to 2.0 from ascorbic acid at 400 μg mL-1. The extract markedly stabilized rat erythrocyte cell membranes. The findings suggest that the methanol leaf extract of S. occidentalis may be useful in the protection of the hepatocytes from toxins.
Hippocampal formation is involved in learning and memory and has also been reported to be sensitive to neurotoxic insults. However, little has been reported on the chronic simultaneous intake of ethanol and acetaminophen despite their degrees of abuse and misuse as regards hippocampus. In this study, forty adult wistar rats of average weight 150±20.2 g were randomly distributed into four groups of treatments T1; T2, Tg and control C (N = 10). For a period of six weeks, animals in group T: received 100 mg kg-1 b.wt. acetaminophen and 25% ethanol in 2% sucrose solution while group T2 animals received 25% ethanol in 2% sucrose solution. Tg animals were given 100 mg kg-1 b.wt. acetaminophen and group C animals were given only distilled water. The animals were sacrificed by whole body intracardiac perfusion fixation and the regions of hippocampus were dissected out using Paxinos stereotaxic coordinate method. Brain specimens were processed for routine histological techniques, sectioned at 6 ^ and stained for nissl's substance. Significantly reduced neuronal density (p>0.05) of 44 and 38% neuronal loss in CA3 subfield, respectively in treatment groups T1 and T2 compared to control group was recorded. Also, marked degeneration of pyramidal neurons in the regions of CA1 and CA3 of treatment groups that received 100 mg kg-1 b.wt. acetaminophen and 25% ethanol in 2% sucrose solution as well as animals that received 25% ethanol in 2% sucrose solution, respectively with mild degenerative effects in the group that took 100 mg kg-1 b.wt. acetaminophen compared to the control group was also observed. These alterations observed following exposure to chronic simultaneous administration of ethanol and acetaminophen point to possibilities of higher memory impairments and learning deficits which are of very strong public health concern.
In the systematic screening programme for cytotoxic compound from marine actinomycetes, the compound furan-2-yl acetate (F2A) from Streptomyces VITSDK1 spp. The structure of the compound was unequivocally determined by spectral studies. It was previously found that F2A has potential antiviral activity against fish nodavirus. In the present study, the cytotoxicity of F2A was studied using (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay which showed the IC50 values were less than 15 μg mL-1 against various tumor cell lines, whereas it was >25 μg mL-1 against non-tumor cell lines. F2A inhibited the cell proliferation in a dose-and time-dependent manner. Furthermore, the cytotoxic mechanism was determined in HeLa cells. The morphological analysis, Hoechst staining and DNA fragmentation studies revealed the apoptosis mediated cell death. The cytosolic protein analysis of F2A treated HeLa cells by immunoblotting showed the mitochondrial cytochrome c release, increased expression of caspase 3 and caspase 9 with PARP cleavage. There was no change in the caspase-8 levels. The Bcl-2 was found to be down regulated and Bax was up regulated in the F2A treated cells. Further, the apoptosis induction and cell death was found to be mediated by Reactive Oxygen Species (ROS) and lipid peroxidation. A molecular docking study of F2A with 28 selected cancer drug target enzymes provides some insight on mode of activity of the compound. The findings showed that the F2A exhibits selective cytotoxicity towards tumor cells at a lower concentration via apoptosis.
This study evaluated the central action of Waltheria indica extract. Aqueous ethanolic extract of the plant showed bioactivity in acetic-acid induced stretches in animal model. The central effects of the most biologically active fraction (ethyl acetate) of extract of Waltheria indica was evaluated in mice using the elevated plus maze paradigm and the strychnine and leptazol-induced convulsions. Sedative effect was studied using the amylobarbitone-induced sleeping time. The extract fraction significantly (p<0.05) increased the amylobarbitone sleepirg time and protected (100%) mice from death due to pentylenetetrazole convulsion. The extract failed to protect mice against strychnine convulsion, even though it delayed 1he time of onset of death. The exploratory activity was also significantly (p<10.05) decreased in the extract treated mice. The extract blocked leptazole-induced convulsion, potentiated amylobarbitone sleeping time and decreased exploratory activity, indicating anticonvulsant and sedative actions.
Many people in rural Bangladesh use a traditional contraceptive pill, "Shanti Bori" to control fertility in which Tragia involucrata is one of the components. The aim of the present study was to evaluate the validity of antifertility effect of this plant. The hexane (HE) and ethyl acetate extracts (EAE) of the aerial parts of T. involucrata have been evaluated for the anti-fertility activity in proven fertile female rats at dose of 200 mg kg-1 body weight. Preliminary phytochemical analysis showed the presence of phytosterols, triterpenes and flavonoids in the extracts. HE and EAE showed significant anti-fertility activity. It was found that the extracts reduced the number of litters born significantly at the dose of 200 mg kg-1 body weight. HE and EAE exhibited 81 and 50% antiimplantation potency respectively at the tested dose. The extracts also showed the estrogenic activity and potentiated the action of the standard drug ethanyl estradiol. All these observations suggest that extracts have antiimplantation as well as the abortifacient activity and are safe at the effective antifertility doses employed in this study
In the present study the prophylactic effects of the antioxidants, β-carotene and/or N-acetyl cysteine (NAC) in ameliorating the metabolic abnormalities and oxidative damage induced cardiopathy under the effect of the flavor enhancers, monosodium glutamate (MSG) toxicity were studied. Animals were divided into 5 groups; G1: normal control, G2: MSG-treated group, Gs 3,4 and 5: animals pretreated with either NAC or β-carotene or their combination prior MSG administration, respectively. The present results revealed that, chronic administration of MSG caused metabolic dysfunction characterized by significant increases in the levels of serum glucose, total lipids, triglycerides (TG), total cholesterol (TCh) and Low Density Lipoprotein (LDL) and a decrease in the high density lipoprotein (HDL), parameters have important role in MSG induced cardiovascular disorders. The adverse effects of MSG may be related to an imbalance between the oxidant and antioxidant systems. This was indicated by marked increased levels of serum nitric oxide (NO) accompanied by pronounced increased level of thiobarbituric acid reactive substances (TBARS, marker of lipid peroxidation) and decreased levels of the antioxidants, L-ascorbic acid, glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT) in cardiac tissue versus normal animals. Significant inhibition in cardiac Na+/K+ ATPase with increase in serum activities of creatine phophokinase (CPK) and aspartate aminotransferase (AST) were also observed in MSG treated animals as biomarker enzymes of cardiac tissue damage. This result was supported by myocardial infarction (necrotic lesion) observed by histopathological examination. Administration of either β-carotene or NAC prior MSG injection significantly modulated the alteration in most of the previously mentioned parameters to near their normal levels. Administration of synergistic combination of the these antioxidants showed the most significant effect as it has the ability to restore all of the studied parameters to their normal levels. The biochemical results were supported by the improvement in histological architecture of heart tissue, implicating that these antioxidants either alone or their combination may protect heart from the harmful effects of cardio-toxic agents.
Hymenocardia acida leaf extract is used folklorically as remedy for fever, pain and respiratory diseases. It has also been shown to possess antisickling, antioxidant, antiulcer, anti-arthritic and mutagenic properties, among others. This study was undertaken to ascertain the acute and sub chronic toxicity profile of H. acida ethanol leaf extract administered orally in rats. Acute toxicity test was carried out using modified Lorke's method. Four groups of seven rats each were used for sub chronic toxicity evaluation. The first group served as control, while groups two, three and four received 25, 50 and 100 mg kg -1 extract respectively for twenty-nine days. In the acute toxicity test, the extract did not cause any signs of toxicity or produce mortality in rats. Results also showed that sub chronic administration of the extract did not significantly (p>0.05) affect food consumption, body weight and haematological parameters at the doses used. Water intake was observed to increase significantly (p<0.01) in the groups administered 25 and 50 mg kg -1 extract during the first and fourth weeks of administration. Relative spleen weights were significantly (p<0.05) lowered in groups given 50 and 100 mg kg -1 extract while relative brain weight reduced significantly (p<0.05) in the group administered 100 mg kg -1 extract. Serum triglyceride levels were also significantly (p<0.01) elevated in 50 and 100 mg kg -1 extract-treated groups, without significant alterations of other biochemical parameters. Microscopically, mild cortical-tubular cellular oedema in kidneys of extract-treated groups was observed. This study shows that although H. acida leaf extract is safe acutely, its long-term use of may be associated with mild renal toxicity.
In the present study, the effects of combined metabolites produced by lactic acid bacteria were tested on food pathogenic and contaminant microorganisms. Totally, eight strains of Lactobacillus acidophilus (FTDC 2804, FTDC 0785, FTDC 8592, FTDC 1295, FTDC 4793, FTDC 4462, FTDC 0582 and FTDC 2916) were used which cultivated in four types of agro waste substrates including pineapple waste, soy whey, cabbage and molasses. The inhibitory effects of L. acidophilus metabolites (lactic acid, hydrogen peroxide, acetaldehyde, diacetyl and bacteriocin) were determined by agar well diffusion method on two pathogenic bacteria; Staphylococcus aureus and Escherichia coli. Metabolites of different L. acidophil us strains cultured in different agro waste substrates showed diverse inhibitory effects. Among all, the highest inhibition zone was obtained with the strains cultivated in pineapple waste, such as, L. acidophilus FTDC 4462 strain (1O.57±0.1O mm for S. aureus and 1l.13±0.45 mm for E. coli). It can be concluded that L. acidophilus species has the ability to grow in agro waste materials and produce beneficial metabolites with antibacterial activities.
N-nitrosamines are considered human carcinogens and have been found in cured meats, seafood, vegetables, apples, beer, drinking water, waste water, tobacco products and rubber products. Limited studies exist on the effects of low dose exposure to multiple N-nitrosamines compounds. The objectives of this study were to investigate the cellular mechanisms of action by which N-nitrosamines exhibit toxicity resulting in liver tumors and other effects. Hep2G human liver cells (ATCC HTB-37) was obtained from the American Type Culture Collection (ATCC, Manassas, VA). For assay, 5xl0 4 Hep2G cells/well were seeded in a 24 well culture plate and incubated at 37°C and 7% C0 2 until development of a monolayer. Cells were incubated with a combination of selected N-nitrosamines at selected concentrations (0, 4, 8, 16, 32, 64 mM) for 12 and 24 h. Lactate dehydrogenase (LDH) release (% cytotoxicity), histone-related DNA fragmentation and detoxification enzymes were determined. After 12 and 24 h incubation with N-nitrosamines,% cytotoxicity in Hep2G cells displayed a dose-dependent relationship at concentrations of 4, 8 and 16 mM. Cytotoxicity peaked at 16 mM for both time periods and then decreased with increasing concentration (64 mM) to 19.46 (12 h) and 55.73 (24 h). Overall, levels of glutathione-S-transferase (GST), glutathione peroxidase (GPx), Glutathione Reductase (GR) and Superoxide Dismutase (SOD) were higher with control compared to N-nitrosamines-treated cells. Histone-related DNA fragmentation was highest in cells treated with 8 mM (24 h). Possible mechanisms of action may be due to lower detoxification enzymes and/or an increase in H 20 2 production, leading to cell death.
Nature has been a source of medicinal agents for thousands of years and an impressive number of modern drugs have been isolated from natural sources, many based on their use in traditional medicine. Therapeutically interesting and important drugs can be developed from plant sources which are used in traditional systems of medicines. Indian traditional system of medicine is based on empirical knowledge of the observations and the experience over millennia and more than 5000 plants are used by different ethnic communities in India. The present communication constitutes a review on the medicinal properties and pharmacological actions of Cassia auriculata L. and Cissus quadrangularis Wall. used in Indian traditional medicine. These plants are known to contain various active principles of therapeutic value and to possess biological activity against a number of diseases.
Ixora coccinea L. (Rubiaceae) possess anti-inflammatory and antitussive properties. It is traditionally used for various respiratory ailments including catarrhal bronchitis cough and asthma. In the present study we investigated anti-asthmatic properties of an hydro alcoholic leaf extract of I. coccinea in an ovalbumin (OVA)-induced asthmatic rat model. We also evaluated the anti-allergic property of the extract by Abdominal Wall (AW) method and histamine-induced cutaneous reaction. Rats were sensitized with intraperitoneal (i.p.) ovalbumin and challenged by OVA intranasally to induce chronic airway inflammation. Randomized treatment groups of sensitized rats received I. coccinea extract or distilled water. I. coccinea extract at doses of 1000 and 1500 mg kg-1 suppressed eosinophilia and significantly inhibited AHR in rat with OVA-induced asthma. Based on lung histopathological study using hematoxylin and eosin I. coccinea reduced inflammatory cell infiltration and repaired epithelial cells damaged. In addition the extract at the same doses significantly decreased the diameter of the blue spot (16 and 55%, respectively) compared with the controls and inhibited the skin reactions induced by histamine (23.55 and 53.36%, respectively). In conclusion our results provide evidence that I. coccinea has anti-asthmatic properties and then can support its use in folk medicine to treat asthma.
The present study was designed to investigate the antioxidant, analgesic and anti-inflammatory potential of the methanolic extract along with its organic soluble fractions of the herb Eclipta prostrata. In addition, total phenolic and flavonoid content and total antioxidant capacity were also determined. Antioxidant potential of the extract/fractions was evaluated by DPPH (1,1diphenyl-2-picrylhydrazyl), NO (nitric oxide) and ONOO- (peroxynitrite) scavenging assay method. Ethyl acetate fractions (EtOAc) showed highest scavenging activity in all the methods with IC50 value of 12.98±0.08, 45.98±0.07 and 14.45±0.18 μg mL-1 for DPPH, NO and ONOO- assay method, respectively. In reducing power assay, EtOAc fraction also showed significant (p<0.001) activity. Further, the extract/fractions were studied for their analgesic (hot plate, tail immersion and acetic acid induced writhing test) and anti-inflammatory (carrageenan induced paw edema in rats) activities at a dose level of 200 and 400 mg kg-1 body weight. Among all the extract/fractions, EtOAc fraction showed a dose dependent and significant (p<0.005, p<0.05) analgesic activity in all the tested method. EtOAc fractions also reduced the paw edema considerably (86.80% inhibition after 3 h, p<0.005, p<0.05) in dose dependent manner compared to carrageenan induced rat. Altogether, these results suggest that the MeOH extract and its organic soluble fractions could be used as a potential antioxidant, analgesic and anti-inflammatory agent