Search results for: wistar albino rats

Authors: V. A. Doss, R. Sowndarya, K. Juila Rose Mary

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Objective: Amino acid neurotransmitter system dysfunction plays a major role in the pathophysiology of depression. The objective of the present study was to identify the amino acids as possible metabolite biomarkers for depression using GCMS (Gas Chromatography Mass Spectrometry) before and after exercise regimen in brain samples of depression induced animal models. Methods: Depression-like behaviour was induced by Chronic Unpredictable mild stress (CUMS). Severity of depression was measured by forced swim test (FST) and sucrose consumption test (SCT). Swimming protocol was followed for 4 weeks of exercise treatment. Brain obtained from depressed and exercise treated rats were used for the metabolite analysis by GCMS. Subsequent statistical analysis obtained by ANOVA followed by post hoc test revealed significant metabolic changes. Results: Amino acids such as alanine, glycine, serine, glutamate, homocysteine, proline and branched chain aminoacids (BCAs) Leucine, Isoleucine, Valine were determined in brain samples of control, depressed and exercised groups. Among these amino acids, the levels of D-Serine and branched chain amino acids were found to be decreased in depression induced rats. After four weeks of swimming exercise regimen, there were improvements in the levels of serine and Branched chain amino acids. Conclusion: We suggest that Serine and BCAs may be investigated as potential metabolite markers using GCMS and their beneficial metabolic changes in Exercise.

Keywords: metabolomics, depression, forced swim test, exercise, amino acid metabolites, GCMS, biomarker

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Authors: Hanan F. Aly, Fateheya M. Metwally, Hanaa H. Ahmed

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The current study is undertaken to elucidate a possible neuroprotective role of dehydroepiandrosterone (DHEA) against the development of Alzheimer’s disease in experimental rat model. Alzheimer’s disease was produced in young female ovariectomized rats by intraperitoneal administration of AlCl3 (4.2 mg/kg body weight) daily for 12 weeks. Half of these animals also received orally DHEA (250 mg/kg body weight, three times weekly) for 18 weeks. Control groups of animals received either DHAE alone, or no DHEA, or were not ovariectomized. After such treatment the animals were analyzed for oxidative stress biomarkers such as hydrogen peroxide, nitric oxide and malondialdehyde, total antioxidant capacity, reduced glutathione, glutathione peroxidase, glutathione reductase, superoxide dismutase and catalase activities, antiapoptotic marker Bcl-2 and brain derived neurotrophic factor. Also, brain cholinergic markers (acetylcholinesterase and acetylcholine) were determined. The results revealed significant increase in oxidative stress parameters associated with significant decrease in the antioxidant enzyme activities in Al-intoxicated ovariectomized rats. Significant depletion in brain Bcl-2 and brain-derived neurotrophic factor levels were also detected. Moreover, significant elevations in brain acetylcholinesterase activity accompanied with significant reduction in acetylcholine level were recorded. Significant amelioration in all investigated parameters was detected as a result of treatment of Al-intoxicated ovariectomized rats with DHEA. These results were confirmed by histological examination of brain sections. These results clearly indicate a neuroprotective effect of DHEA against Alzheimer’s disease.

Keywords: Alzheimer’s disease, oxidative stress, apoptosis, dehydroepiandrosterone

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Authors: Amberkar Mohanbabu Vittalrao, Avin, Meena Kumari Kamalkishore, Padmanabha Udupa, Vinaykumar Bavimane, Honnegouda

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Objective: To evaluate the hepato-protective activity of Tinospora cordiofolia (Tc) against paracetamol induced hepatic damage in rats. Methods: The plant stem (test drug) was procured locally, shade dried, powdered and extracted with water. Silymarin was used as standard hepatoprotective drugs and 2% gum acacia as a control (vehicle) against paracetamol (PCT) induced hepatotoxicity. Results and Discussion: The hepato-protective activity of aqueous stem extract was assessed by paracetamol induced hepatotoxicity preventive model in rats. Alteration in the levels of biochemical markers of hepatic damage like AST, ALT, ALP and lipid peroxides were tested in both paracetamol treated and untreated groups. Paracetamol (3g/kg) had enhanced the AST, ALT, ALP and the lipid peroxides in the serum. Treatment of silymarin and aqueous stem extract of Tc (200 and 400mg/kg) extract showed significant hepatoprotective activity by altering biochemical marker levels to the near normal. Preliminary phytochemical tests were done. Aqueous Tc extract showed presence of phenolic compound and flavonoids. Our findings suggested that Tc extract possessed hepatoprotective activity in a dose dependent manner. Conclusions: Tc was found to possess significant hepatoprotective property when treated with PCT. This was evident by decreasing the liver enzymes significantly when treated with PCT as compared to PCT only treated group (P < 0.05). Hence Tinospora cardiofolia could be a good, promising, preventive agent against PCT induced hepatotoxicity.

Keywords: Tinospora cardiofolia, hepatoprotection, paracetamol, silymarin

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Authors: B. Sadek, N. Khan, D. Łażewska, K. Kieć-Kononowicz

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The effects of the non-imidazole histamine H3 receptor (H3R) antagonist DL77 in passive avoidance paradigm (PAP) and novel object recognition (NOR) task in MK801-induced cognitive deficits associated with schizophrenia (CDS) in adult male rats, and applying donepezil (DOZ) as a reference drug were investigated. The results show that acute systemic administration of DL77 (2.5, 5, and 10 mg/kg, i.p.) significantly improved MK801-induced (0.1 mg/kg, i.p.) memory deficits in PAP. The ameliorating activity of DL77 (5 mg/kg, i.p.) in MK801-induced deficits was partly reversed when rats were pretreated with the centrally-acting H2R antagonist zolantidine (ZOL, 10 mg/kg, i.p.) or with the antimuscarinic antagonist scopolamine (SCO, 0.1 mg/kg, i.p.), but not with the CNS penetrant H1R antagonist pyrilamine (PYR, 10 mg/kg, i.p.). Moreover, the memory enhancing effect of DL77 (5 mg/kg, i.p.) in MK801-induced memory deficits in PAP was strongly reversed when rats were pretreated with a combination of ZOL (10 mg/kg, i.p.) and SCO (1.0 mg/kg, i.p.). Furthermore, the significant ameliorative effect of DL77 (5 mg/kg, i.p.) on MK801-induced long-term memory (LTM) impairment in NOR test was comparable to the DOZ-provided memory-enhancing effect, and was abrogated when animals were pretreated with the histamine H3R agonist R-(α)-methylhistamine (RAMH, 10 mg/kg, i.p.). However, DL77(5 mg/kg, i.p.) failed to provide procognitive effect on MK801-induced short-term memory (STM) impairment in NOR test. In addition, DL77 (5 mg/kg) did not alter anxiety levels and locomotor activity of animals naive to elevated-plus maze (EPM), demonstrating that improved performances with DL77 (5 mg/kg) in PAP or NOR are unrelated to changes in emotional responding or spontaneous locomotor activity. These results provide evidence for the potential of H3Rs for the treatment of neurodegenerative disorders related to impaired memory function, e.g. CDS.

Keywords: histamine H3 receptor, antagonist, learning, memory impairment, passive avoidance paradigm, novel object recognition

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Authors: Hichem Sebai, Mohamed Amine Jabri, Kais Rtibi, Haifa Tounsi, Lamjed Marzouki

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Artemisia campestris has been widely used in Tunisian traditional medicine for its health beneficial effects. However, the present study aims at evaluating the antiulcer effects of Artemisia campestris aqueous extract (ACAE) as well as the mechanism of action involved in such gastroprotection. In this respect, male Wistar rats were divided into seven groups: control, aspirin (ASPR), ASPR + various doses of ACAE (100, 200 and 400 mg/kg, b.w.), ASPR+ famotidine and ASPR+ caffeic acid. Animals were pre-treated with ACAE extract during 10 days. We firstly showed that aspirin administration was accompanied by an oxidative stress status assessed by an increase of malondialdehyde (MDA) level, a decrease of sulfhydryl -(SH) groups content and depletion of antioxidant enzyme activities such as superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx). Pre-treatment with ACAE protected against aspirin-induced gastric oxidative stress. More importantly, aspirin administration increased plasma and tissue hydrogen peroxide (H₂O₂), free iron and calcium levels while the ACAE pre-treatment reversed all aspirin-induced intracellular mediators disturbance. The results of the present study clearly indicated that AEAC gastroprotection might be related, at least in part, to its antioxidant properties as well as to various gastric mucosal defense mechanisms, including the protection of gastric sulfhydryls and an opposite effect on some intracellular mediators such as free iron, hydrogen peroxide, and calcium. However, our data confirm the use of Artemisia campestris extracts in the Tunisian traditional folk medicine for the treatment of gastrointestinal diseases.

Keywords: gastric ulcer, Artemisia campestris, oxidative stress, sulfhydryl groups, Fenton reaction, rat

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Authors: Cansu Arslan Turan, Tuba Cimilli Ozturk, Ebru Unal Akoglu, Kemal Aygun, Ecem Deniz Kırkpantur, Ozge Ecmel Onur

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Although the mechanism of action is not well known, Intravenous Lipid Emulsion (ILE) has been shown to be effective in the treatment of lipophilic drug intoxications. It is thought that ILE probably separate the lipophilic drugs from target tissue by creating a lipid-rich compartment in the plasma. The second theory is that ILE provides energy to myocardium with high dose free fatty acids activating the voltage gated calcium channels in the myocytes. In this study, the effects of ILE treatment on digoxin overdose which are frequently observed in emergency departments was searched in an animal model in terms of cardiac side effects and survival. The study was carried out at Yeditepe University, Faculty of Medicine-Experimental Animals Research Center Labs in December 2015. 40 Sprague-Dawley rats weighing 300-400 g were divided into 5 groups randomly. As the pre-treatment, the first group received saline, the second group received lipid, the third group received DigiFab, and the fourth group received DigiFab and lipid. Following that, digoxin was infused to all groups until death except the control group. First arrhythmia and cardiac arrest occurrence times were recorded. As no medication causing arrhythmia was infused, Group 5 was excluded from the statistical analysis performed for the comparisons of first arrhythmia and death time. According to the results although there was no significant difference in the statistical analysis comparing the four groups, as the rats, only exposed to digoxin intoxication were compared with the rats pre-treated with ILE in terms of first arrhythmia time and cardiac arrest occurrence times, significant difference was observed between the groups. According to our results, using DigiFab treatment, intralipid treatment, intralipid and DigiFab treatment for the rats exposed to digoxin intoxication makes no significant difference in terms of the first arrhythmia and death occurrence time. However, it is not possible to say that at the doses we use in the study, ILE treatment might be successful at least as a known antidote. The fact that the statistical significance between the two groups is not observed in the inter-comparisons of all the groups, the study should be repeated in the larger groups.

Keywords: arrhytmia, cardiac arrest, DigiFab, digoxin intoxication

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Authors: Huma Shareef, Ghazala H. Rizwani, Ahsana Dar

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In traditional medicine Cardiospermum halicacabum L. (Sapindeaceae) is used against various ailments. In current investigation searching a new remedy that will available easily, non expensive, able to lower hypertension and standardize blood pressure, made us to develop an herbal medicine. Crude ethanol extract of C. halicacabum and its various fractions ethyl acetate and butanol showed a dose-dependent hypotensive effect in anaesthetized rats. The trachea was exposed and freed from connective tissue and incubated by cannula to facilitate spontaneous respiration. The right carotid artery and left jugular vein were cannulated with polyethylene tubing PE-50 for monitoring blood pressure changes via pressure transducer (Gould P23 ID) connected to a Grass model 79D polygraph and for i.v. injection, respectively. Drugs or the plant extracts were administered at a constant volume of 0.5 ml/kg, followed by injection of 0.2 ml of saline that flushed the cannula. Systolic, diastolic and mean arterial blood pressure (MABP) was measured in mm Hg and heart rate in beats/min. Ethanol extract of C. halicacabum showed a significant activity at 50 mg/kg dose. Ethyl acetate fraction (10, 20, 30, 40, and 50 mg/kg) induced dose dependent fall in systolic and diastolic blood pressure, heart rate of rats. At 10-30 mg/kg the hypotensive effect was non significantly reduced by 10 -15%. However, the extract at 40 mg/kg induced significant hypotensive effect calculated as 30.95±3.2% MABP and this effect persists till 50 mg/kg. The higher polar fraction (butanol) of the whole plant failed to produce any significant response against MABP at all the tested doses (10-50 mg/kg). C. halicacabum lowers blood pressure, exerts a dose-dependent hypotensive effect, can be used as hypotensor.

Keywords: cardiospermum halicacabum, calcium channel blocker, hypotensive, various extracts

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Authors: Ho Seong Shin

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Introduction: A research in relation to wound healing also showed that platelet-rich plasma (PRP) was effective on normal tissue regeneration. Nonetheless, there is no evidence that when platelet-rich plasma was applied on diabetic wound, it normalize diabetic wound healing process. In this study, we have analyzed matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-9 (MMP-9) expression to know the effect of PRP on diabetic wounds using Reverse transcription-polymerase chain reaction (RT-PCR) of MMP-2, MMP-9 mRNA. Materials and Methods: Platelet-rich plasma (PRP) was prepared from blood of 6 rats. The whole 120-mL was added immediately to an anticoagulant. Citrate phosphonate dextrose(CPD) buffer (0.15 mg CPDmL) in a ratio of 1 mL of CPD buffer to 5 mL of blood. The blood was then centrifuged at 220g for 20minutes. The supernatant was saved to produce fibrin glue. The participate containing PRP was used for second centrifugation at 480g for 20 minutes. The pellet from the second centrifugation was saved and diluted with supernatant until the platelet concentration became 900,000/μL. Twenty male, 4week-old OLETF rats were underwent operation; each rat had two wounds created on left and right sides. The each wound of left side was treated with PRP gel, the wound of right side was treated with physiologic saline gauze. Results: RT-PCR analysis; The levels of MMP-2 mRNA in PRP applied tissues were positively related to postwounding days, whereas MMP-2 mRNA expression in saline-applied tissues remained in 5day after treatment. MMP-9 mRNA was undetectable in saline-applied tissues for either tissue, except 3day after treatment. Following PRP-applied tissues, MMP-9 mRNA expression was detected, with maximal expression being seen at third day. The levels of MMP-9 mRNA in PRP applied tissues were reported high intensity of optical density related to saline applied tissues.

Keywords: diabetes, MMP-2, MMP-9, OLETF, PRP, wound healing MMP-9

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Authors: Pratibha Goyal, Nupur Mathur, Anuradha Singh

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Antibiotic resistance is the worldwide threat to human health in this century. Excessive use of antibiotic after their discovery in 1940 makes certain bacteria to become resistant against antibiotics. Most common antibiotic-resistant bacteria include Staphylococcus aureus, Salmonella typhi, E.coli, Klebsiella pneumonia, and Streptococcus pneumonia. Among all Staphylococcus resistant strain called Methicillin-resistant Staphylococcus aureus (MRSA) is responsible for several lives threatening infection in human commonly found in the hospital environment. Our study aimed to isolate bacteriophage against MRSA from the hospital sewage treatment plant and to analyze its efficiency In Vivo in Swiss albino mice model. Sewage sample for the isolation of bacteriophages was collected from SDMH hospital sewage treatment plant in Jaipur. Bacteriophages isolated by the use of enrichment technique and after characterization, isolated phages used to determine phage treatment efficiency in mice. Mice model used to check the safety and suitability of phage application in human need which in turn directly support the use of natural bacteriophage rather than synthetic chemical to kill pathogens. Results show the plaque formation in-vitro and recovery of MRSA infected mice during the experiment. Favorable lytic efficiency determination of MRSA and Salmonella presents a natural way to treat lethal infections caused by Multidrug-resistant bacteria by using their natural host-pathogen relationship.

Keywords: antibiotic resistance, bacteriophages, methicillin resistance Staphylococcus aureus, pathogens, phage therapy, Salmonella typhi

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Authors: Sabri Sudirman, Yuan-Hua Hsu, Zwe-Ling Kong

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Male reproductive dysfunction is predominantly due to insulin resistance and hyperglycemia result in inflammation and oxidative stress. Furthermore, nanotechnology provides an alternative approach to improve the bioavailability of natural active food ingredients. Therefore, the aim of this study were to investigate nanoencapsulated triterpenoids from petri-dish cultured Antrodia cinnamomea (PAC) nanoparticles whether it could increase the bioavailability; in addition, the anti-inflammatory and anti-oxidative effects could more effectively ameliorate the reproductive function of diabetic male rats. First, PAC encapsulated in chitosan-silica nanoparticles (Nano-PAC) were prepared by biosilicification method. Scanning electron micrographs confirm the average particle size is about 30 nm, and the encapsulation efficiency is 83.7% by HPLC. Diabetic male Sprague-Dawley rats were induced by high fat diet (40% kcal from fat) and streptozotocin (35 mg/kg). Nano-PAC was administered by oral gavage in three doses (4, 8 and 20 mg/kg) for 6 weeks. Besides, metformin (300 mg/kg) and nanoparticles (Nano) were treated as the positive and negative control respectively. Results indicated that 4 mg/kg Nano-PAC administration for 6 weeks improved hyperglycemia, insulin resistance, and also reduced advanced glycation end products in plasma. In addition, 8 mg/kg Nano-PAC ameliorated morphological of testicular seminiferous tubules, sperm morphology and motility, reactive oxygen species production and mitochondrial membrane potential. Moreover, 20 mg/kg Nano-PAC restored reproductive endocrine system function and increased KiSS-1 level in plasma. In plasma or testis anti-oxidant superoxide dismutase, glutathione peroxidase and catalase were increased whereas malondialdehyde, as well as pro-inflammatory cytokines tumor necrosis factor-α, interleukin-6, and interferon-gamma, decreased. Most importantly, 8 mg/kg Nano-PAC down-regulated the oxidative stress induced c-Jun N-terminal kinase (JNK) signaling pathway. Our study successfully nanoencapsulated PAC to form nanoparticles and low-dose Nano-PAC improved diabetes-induced hyperglycemia, inflammation and oxidative stress to ameliorate the reproductive function of diabetic male rats.

Keywords: Antrodia cinnamomea, diabetes mellitus, male reproduction, nanoparticles

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Authors: H. Sebai, M. A. Jabria, D. Wannes, H. Tounsi, L. Marzouki

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We aimed in the present study to investigate the protective effects of Tunisian Rosa canina aqueous extract (RCAE) against ethanol-induced gastric ulceration and oxidative stress in a rat model. In this respect, adult male Wistar rats were used and divided into six groups of ten each: control, EtOH, EtOH plus various doses of RCAE, EtOH plus famotidine and EtOH + gallic acid. Phytochemical and biochemical analysis were performed using colorimetric methods. We found that RCAE is rich in total polyphenols, total flavonoids, and condensed tannins, and exhibited an importance in vitro antioxidant activity on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. In vivo, the results showed that oral administration of EtOH caused macroscopic and histological changes in gastric mucosa. These injuries are accompanied by an oxidative stress status as assessed by an increase of lipid peroxidation as well as a decrease of antioxidant enzyme activities such as superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx). Alcohol intoxication also induced intracellular mediators deregulation as assessed by an increase of hydrogen peroxide (H2O2), calcium and free iron levels in gastric mucosa. More, importantly, RCAE pretreatment reversed all macroscopic, histological and biochemical changes induced by EtOH administration. In conclusion, we suggest that RCAE has potent protective effects on acute ethanol-induced gastric ulceration related in part in part its antioxidant properties and its opposite effect on intracellular mediators. Indeed, Rosa canina can be offered as a food additive to protect against alcohol consumption-induced gastric and oxidative damage.

Keywords: alcohol, antioxidant properties, food additive, gastric ulceration, rat model, Rosa canina

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Authors: Hanen Bouaziz-Ketata, Ghada Ben Salah, Hichem Ben Salah, Kamel Jamoussi, Najiba Zeghal

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The present study investigated the protective role of Hyparrhenia hirta on nitrate-induced liver damage. Experiments were carried out on adult rats divided into 3 groups, a control group and two treated groups. NaNO3 was administered daily by oral gavage at a dose of 400 mg/kg bw in treated groups either alone or coadministered with Hyparrhenia hirta methanolic extract via drinking water at a dose of 200 mg/kg bw for 50 days. Liver toxicity induced by NaNO3 was characterized by higher serum levels of glucose, total cholesterol and triglyceride and lower serum total protein than those of controls. Transaminases and lactate deshydrogenase activities in serum were elevated indicating hepatic cells’ damage after treatment with NaNO3. The hyperbilirubinemia and the increased serum gamma glutamyl transferase activities suggested the presence of cholestasis in NaNO3 exposed rats. In parallel, NaNO3 caused oxidant/antioxidant imbalance in the liver as reflected by the increased lipid peroxidation, the decreased total glutathione content and superoxide dismutase, catalase and glutathione peroxidase activities. Nitrate caused also a significant induction of DNA fragmentation as evidenced by the presence of a smear without ladder formation on agarose gel. Hyparrhenia hirta supplementation showed an improvement of all parameters cited above. We conclude that the present work provides ethnopharmacological relevance of Hyparrhenia hirta against the toxic effect of nitrate, suggesting its role as a potential antioxidant.

Keywords: Hyparrhenia hirta, liver, nitrate toxicity, oxidative stress, rat

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Authors: Esmaeil Biazar

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A nanofibrous PHBV nerve conduit has been used to evaluate its efficiency based on the promotion of nerve regeneration in rats. The designed conduits were investigated by physical, mechanical and microscopic analyses. The conduits were implanted into a 30-mm gap in the sciatic nerves of the rats. Four months after surgery, the regenerated nerves were evaluated by macroscopic assessments and histology. This polymeric conduit had sufficiently high mechanical properties to serve as a nerve guide. The results demonstrated that in the nanofibrous graft with cells, the sciatic nerve trunk had been reconstructed with restoration of nerve continuity and formatted nerve fibers with myelination. For the grafts especially the nanofibrous conduits with cells, muscle cells of gastrocnemius on the operated side were uniform in their size and structures. This study proves the feasibility of artificial conduit with Schwann cells for nerve regeneration by bridging a longer defect in a rat model.

Keywords: sciatic regeneration, Schwann cell, artificial conduit, nanofibrous PHBV, histological assessments

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Authors: Nandhakumar Elumalai, Purushothaman Ayyakannu, Sachidanandam T. Panchanatham

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Background: Understanding the basic mechanisms and factors underlying the tumor growth and invasion has gained attention in recent times. The processes of angiogenesis and apoptosis are known to play a vital role in various stages of cancer. The vascular endothelial growth factor (VEGF) is well established as one of the key regulators of tumor angiogenesis while MMPs are known for their exclusive ability to degrade ECM. Objective: The present study was designed to evaluate the pro apoptotic and anti angiogenic activity of the herbal formulation Shemamruthaa. The anticancer activity of Shemamruthaa was tested in breast cancer cell line (MCF-7). Results of MTT, trypan blue and flow cytometric analysis of apoptotis suggested that Shemamruthaa can induce cytotoxicity in cancer cells, in a concentration- and time dependent manner and induce apoptosis. With these results, we further evaluated the antiangiogenic and pro-apoptotic activities of Shemamruthaa in DMBA induced mammary carcinoma in Sprague Dawley rats. Flavono tumour was induced in 8-week-old Sprague-Dawley rats by gastric intubation of 25 mg DMBA in 1ml olive oil. After 90 days of induction period, the rats were orally administered with Shemamruthaa (400 mg/kg body wt) for 45 days. Treatment with the drug SM significantly modulated the expression of p53, MMP-2, MMP-3, MMP-9 and VEGF by means of its anti angiogenic and protease inhibiting activity. Conclusion: Based on these results, it might be concluded that the formulation, Shemamruthaa, constituted of dried flowers of Hibiscus rosa-sinensis, fruits of Emblica officinalis, and honey has been found to exhibit pronounced antiproliferative and apoptotic effects. This enhanced anticancer effect of Shemamruthaa might be attributed to the synergistic action of polyphenols such as flavonoids, tannins, alkaloids, glycosides, saponins, steroids, terpenoids, vitamin C, niacin, pyrogallol, hydroxymethylfurfural, trilinolein, and other compounds present in the formulation. Collectively, these results demonstrate that Shemamruthaa holds potential to be developed as a potent chemotherapeutic agent against mammary carcinoma.

Keywords: Shemamruthaa, flavonoids, MCF-7 cell line, mammary cancer

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Authors: Azza A. Ali, Asmaa Abdelaty, Mona G. Khalil, Mona M. Kamal, Karema Abu-Elfotuh

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Background: Aluminium (Al) is known as a neurotoxin environmental pollutant that can cause certain diseases as Dementia, Alzheimer's disease, and Parkinsonism. It is widely used in antacid drugs as well as in food additives and toothpaste. Stresses have been linked to cognitive impairment; Social isolation (SI) may exacerbate memory deficits while protein malnutrition (PM) increases oxidative damage in cortex, hippocampus and cerebellum. The risk of cognitive decline may be lower by maintaining social connections. Epigallocatechin-3-gallate (EGCG) is the most abundant catechin in green tea and has antioxidant, anti-inflammatory and anti-atherogenic effects as well as health-promoting effects in CNS. Objective: To study the influence of different stressful conditions as social isolation, electric shock (EC) and inadequate Nutritional condition as PM on neurotoxicity induced by Al in rats as well as to investigate the possible protective effect of EGCG in these stressful and PM conditions. Methods: Rats were divided into two major groups; protected group which was daily treated during three weeks of the experiment by EGCG (10 mg/kg, IP) or non-treated. Protected and non-protected groups included five subgroups as following: One normal control received saline and four Al toxicity groups injected daily for three weeks by ALCl3 (70 mg/kg, IP). One of them served as Al toxicity model, two groups subjected to different stresses either by isolation as mild stressful condition (SI-associated Al toxicity model) or by electric shock as high stressful condition (EC- associated Al toxicity model). The last was maintained on 10% casein diet (PM -associated Al toxicity model). Isolated rats were housed individually in cages covered with black plastic. Biochemical changes in the brain as acetyl cholinesterase (ACHE), Aβ, brain derived neurotrophic factor (BDNF), inflammatory mediators (TNF-α, IL-1β), oxidative parameters (MDA, SOD, TAC) were estimated for all groups. Histopathological changes in different brain regions were also evaluated. Results: Rats exposed to Al for three weeks showed brain neurotoxicity and neuronal degenerations. Both mild (SI) and high (EC) stressful conditions as well as inadequate nutrition (PM) enhanced Al-induced neurotoxicity and brain neuronal degenerations; the enhancement induced by stresses especially in its higher conditions (ES) was more pronounced than that of inadequate nutritional conditions (PM) as indicated by the significant increase in Aβ, ACHE, MDA, TNF-α, IL-1β together with the significant decrease in SOD, TAC, BDNF. On the other hand, EGCG showed more pronounced protection against hazards of Al in both stressful conditions (SI and EC) rather than in PM .The protective effects of EGCG were indicated by the significant decrease in Aβ, ACHE, MDA, TNF-α, IL-1β together with the increase in SOD, TAC, BDNF and confirmed by brain histopathological examinations. Conclusion: Neurotoxicity and brain neuronal degenerations induced by Al were more severe with stresses than with PM. EGCG can protect against Al-induced brain neuronal degenerations in all conditions. Consequently, administration of EGCG together with socialization as well as adequate protein nutrition is advised especially on excessive Al-exposure to avoid the severity of its neuronal toxicity.

Keywords: environmental pollution, aluminum, social isolation, protein malnutrition, neuronal degeneration, epigallocatechin-3-gallate, rats

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Authors: Ahmad Nazrun Shuid, Isa Naina Mohamed, Nurul Izzah Ibrahim, Norazlina Mohamed

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Studies have shown that oral tocotrienol, a potent vitamin E, promoted fracture healing of osteoporotic bone. In this study, tocotrienol was combined with a polymer carrier (PLGA), and injected to the fracture site. The slow and constant release of tocotrienol particles would promote fracture healing of post-menopausal osteoporosis rat model. Fracture healing was assessed using micro-CT. Twenty-four Sprague-Dawley rats were ovariectomised or sham-operated and the left tibiae were fractured and fixed with plate and screws. The fractures were created at the upper third of the left tibiae. The rats were divided into 3 groups: sham-operated (SO), ovariectomised-control (OVxC) and PLGA-incorporated tocotrienol treatment (OVx + TT) groups. After 4 weeks, the OVx + TT group showed significantly better callus fracture healing than the OVxC group. In conclusion, tocotrienol-incorporated PLGA was able to promote fracture healing of osteoporotic bone.

Keywords: osteoporosis, micro-CT, tocotrienol, PLGA, fracture

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Authors: Emielex M. Aguilar, Kristen Angela G. Cruz, Czarina Joie L. Rivera, Francis Dave C. Tan, Gavino Ivan N. Tanodra, Dianne Katrina G. Usana, Mary Grace T. Valentin, Nico Albert S. Vasquez, Edwin Monico C. Wee

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The risk of diabetes mellitus is increasing in the Philippines, with Metformin and Insulin as drugs commonly used for its management. The use of herbal medicines has grown increasingly, especially among the elderly population. Moringa oleifera or malunggay is one of the most common plants in the country, and several studies have shown the plant to exhibit a hypoglycemic property with its flavonoid content. This study aims to investigate the possible effects of concomitant use of Metformin and powdered M. oleifera leaves (PMOL) on blood glucose levels. Twenty male Sprague-Dawley rats were equally distributed into four groups. Fasting blood glucose levels of the rats were measured prior to experimentation. The following treatments were administered to the four groups, respectively: glucose only 2 g/kg; glucose 2 g/kg + Metformin 100 mg/kg; glucose 2 g/kg + PMOL 200 mg/kg; and glucose 2 g/kg + PMOL 200 mg/kg and Metformin 100 mg/kg. Blood glucose levels were determined on the 1st, 2nd, 3rd, and 4th hour post-treatment and compared between groups. Statistical analysis showed that the type of intervention did not show significance in the reduction of blood glucose levels when compared with the other groups (p=0.378), while the effect of time exhibited significance (p=0.000). The interaction between the type of intervention and time of blood glucose measurement was shown to be significant (p=0.024). Within each group, the control and PMOL-treated groups showed significant reduction in blood glucose levels over time with p-values of 0.000 and 0.000, respectively, while the Metformin-treated and the combination groups had p-values of 0.062 and 0.093, respectively, which are not significant. The descriptive data also showed that the mean total reduction of blood glucose levels of the Metformin and PMOL combination treatment group was lower than the PMOL-treated group alone, while the mean total reduction of blood glucose levels of the combination group was higher than the Metformin-treated group alone. Based on the results obtained, the combination of Metformin and PMOL did not significantly lower the blood glucose levels of the rats as compared to the other groups. However, the concomitant use of Metformin and PMOL may affect each other’s blood glucose lowering activity. Additionally, prolonged time of exposure and delay in the first blood glucose measurement after treatment could exhibit a significant effect in the blood glucose levels. Further studies are recommended regarding the effects of the concomitant use of the two agents on blood glucose levels.

Keywords: blood glucose levels, concomitant use, metformin, Moringa oleifera

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Authors: D. L. Tambe, S. Dighe Nachiket

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Objective: Depression is a common but serious illness and the phenothiazine derivatives shows prominent effect against the depression hence work was undertaken to validate this use scientifically. Material and Methods: Synthesis of phenothiazine derivatives are done by the substitution of various groups, but the basic scheme of synthesis is started with synthesis of 4-(Cyclohexylidene) Benzoic acid using PABA. After that with the further six step of synthesis of 3-(10H-phenothiazin-2-yl)-N, 5-diphenyl-4H-1, 2, 4-triazol-4-amine is done which is final product. Antidepressant activity of all the synthesized compounds was evaluated by despair swim test by using Sprague Dawley Rats. Standard drug imipramine was used as the control. In the despair swim test, all the synthesized derivatives showed antidepressant activity. Results: Among the all phenothiazine derivatives four compounds (6.6-7.2 (14H –phenyl ), 9.43 (1H OH), 8.50 (1H NH phenothiazine),6.85-8.21(14H phenyl), 8.50 (1H NH phenothiazine), 11.82 (1H – OH), 6.6-7.2 (8H –phenyl ), 9.43 (1H OH), 8.50 (1H NH phenothiazine), 4.2 (1H NH) and 6.85-8.21(8H phenyl), 8.50 (1H NH phenothiazine), 3.9 (1H NH) 11.82 (1H – OH) showed significant antidepressant activity comparing with control drug imipramine. Conclusion: Various Novel phenothiazine derivatives show more potent antidepressant activity and it plays more beneficial role in human health for the treatment of depression.

Keywords: antidepressant activities, despair swim test, phenothiazine, Sprague Dawley Rats

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Authors: S. Nurdiana, A. S. Nor Haziqah, M. K. Nur Ezwa Khairunnisa, S. Nurul Izzati, Y. Siti Amna M. J. Norashirene, I. Nur Hilwani

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Azadirachta excelsa or locally known as sentang are frequently used as a traditional medicine by diabetes patients in Malaysia. However, less attention has been given to their toxicity effect. Thus, the study is an attempt to examine the protective effect of A. excelsa on the pancreas and to determine possible toxicity mediated by the extract. Diabetes was induced experimentally in rats by high-fat-diet for 16 weeks followed by intraperitoneal injection of streptozotocin at dosage of 35 mg/kg of body weight. Declination of the fasting blood glucose level was observed after continuous administration of A. excelsa for 14 days twice daily. This is due to the refining structure of the pancreas. However, surprisingly, the plant extract reduced the leukocytes, erythrocytes, hemoglobin, MCHC and lymphocytes. In addition, the rat treated with the plant extract exhibited increment in AST and eosinocytes level. Overall, the finding shows that A. excelsa possesses antidiabetic activity by improving the structure of pancreatic islet of Langerhans but involved in ameliorating of hematology and biochemical parameters.

Keywords: Azadirachta excelsa, diabetes, pancreas, hemato-biochemical parameters

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Authors: Linda Blümel, Bettina Bert, Jan Brosda, Heidrun Fink, Melanie Hamann

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Age-related cognitive decline can eventually lead to dementia, the most common mental illness in elderly people and an immense challenge for patients, their families and caregivers. Cholinesterase inhibitors constitute the most commonly used antidementia prescription medication. The standardized Ginkgo biloba leaf extract EGb 761® is approved for treating age-associated cognitive impairment and has been shown to improve the quality of life in patients suffering from mild dementia. A clinical trial with 96 Alzheimer´s disease patients indicated that the combined treatment with donepezil and EGb 761® had fewer side effects than donepezil alone. In an animal model of cognitive aging, we compared the effect of combined treatment with EGb 761® or donepezil monotherapy and vehicle. We compared the effect of chronic treatment (15 days of pretreatment) with donepezil (1.5 mg/kg p. o.), EGb 761® (100 mg/kg p. o.), or the combination of the two drugs, or vehicle in 18 – 20 month old male OFA rats. Learning and memory performance were assessed by Morris water maze testing, motor behavior in an open field paradigm. In addition to chronic treatment, the substances were administered orally 30 minutes before testing. Compared to the first day and to the control group, only the combination group showed a significant reduction in latency to reach the hidden platform on the second day of testing. Moreover, from the second day of testing onwards, the donepezil, the EGb 761® and the combination group required less time to reach the hidden platform compared to the first day. The control group did not reach the same latency reduction until day three. There were no effects on motor behavior. These results suggest a superiority of the combined treatment of donepezil with EGb 761® compared to monotherapy.

Keywords: age-related cognitive decline, dementia, ginkgo biloba leaf extract EGb 761®, learning and memory, old rats

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Authors: Azza A. Ali, Hebatalla I. Ahmed, Asmaa Abdelaty

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Background: Manganese (Mn) is a naturally occurring element. Exposure to high levels of Mn causes neurotoxic effects and represents an environmental risk factor. Mn neurotoxicity is poorly understood but changing of AChE activity, monoamines and oxidative stress has been established. Bisphenol A (BPA) is a synthetic compound widely used in the production of polycarbonate plastics. There is considerable debate about whether its exposure represents an environmental risk. Caffeine is one of the major contributors to the dietary antioxidants which prevent oxidative damage and may reduce the risk of chronic neurodegenerative diseases. Epigallocatechin-3-gallate is another major component of green tea and has known interactions with caffeine. It also has health-promoting effects in CNS. Objective: To evaluate the potential protective effects of Caffeine and/or EGCG against Mn-induced neurotoxicity either alone or in the presence of BPA in rats. Methods: Seven groups of rats were used and received daily for 5 weeks MnCl2.4H2O (10 mg/kg, IP) except the control group which received saline, corn oil and distilled H2O. Mn was injected either alone or in combination with each of the following: BPA (50 mg/kg, PO), caffeine (10 mg/kg, PO), EGCG (5 mg/kg, IP), caffeine + EGCG and BPA +caffeine +EGCG. All rats were examined in five behavioral tests (grid, bar, swimming, open field and Y- maze tests). Biochemical changes in monoamines, caspase-3, PGE2, GSK-3B, glutamate, acetyl cholinesterase and oxidative parameters, as well as histopathological changes in the brain, were also evaluated for all groups. Results: Mn significantly increased MDA and nitrite content as well as caspase-3, GSK-3B, PGE2 and glutamate levels while significantly decreased TAC and SOD as well as cholinesterase in the striatum. It also decreased DA, NE and 5-HT levels in the striatum and frontal cortex. BPA together with Mn enhanced oxidative stress generation induced by Mn while increased monoamine content that was decreased by Mn in rat striatum. BPA abolished neuronal degeneration induced by Mn in the hippocampus but not in the substantia nigra, striatum and cerebral cortex. Behavioral examinations showed that caffeine and EGCG co-administration had more pronounced protective effect against Mn-induced neurotoxicity than each one alone. EGCG alone or in combination with caffeine prevented neuronal degeneration in the substantia nigra, striatum, hippocampus and cerebral cortex induced by Mn while caffeine alone prevented neuronal degeneration in the substantia nigra and striatum but still showed some nuclear pyknosis in cerebral cortex and hippocampus. The marked protection of caffeine and EGCG co-administration also confirmed by the significant increase in TAC, SOD, ACHE, DA, NE and 5-HT as well as the decrease in MDA, nitrite, caspase-3, PGE2, GSK-3B, the glutamic acid in the striatum. Conclusion: Neuronal degeneration induced by Mn showed some inhibition with BPA exposure despite the enhancement in oxidative stress generation. Co-administration of EGCG and caffeine can protect against neuronal degeneration induced by Mn and improve behavioral deficits associated with its neurotoxicity. The protective effect of EGCG was more pronounced than that of caffeine even with BPA co-exposure.

Keywords: manganese, bisphenol a, caffeine, epigallocatechin-3-gallate, neurotoxicity, behavioral tests, rats

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Authors: Tresna Lestari, Tita Nofianti, Ade Yeni Aprilia, Lilis Tuslinah, Ruswanto Ruswanto

Abstract:

Nanoparticle formulation is often used to improve drug absorptivity, thus increasing the sharpness of the action. Ginger torch flower extract was formulated into nanoparticle form using poloxamer 1, 3 and 5%. The nanoparticle was then characterized by its particle size, polydispersity index, zeta potential, entrapment efficiency and morphological form by SEM. The result shows that nanoparticle formulations have particle size 134.7-193.1 nm, polydispersity index less than 0.5 for all formulations, zeta potential -41.0 - (-24.3) mV and entrapment efficiency 89.93-97.99 against flavonoid content with a soft surface and spherical form of particles. Methanolic extract of ginger torch flower could enhance superoxide dismutase activity by 1,3183 U/mL in male rats. Nanoparticle formulation of ginger torch extract is expected to increase the capability of the drug to enhance superoxide dismutase activity.

Keywords: superoxide dismutase, ginger torch flower, nanoparticle, poloxamer

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Authors: Saylav Ejder Bora, Arife Erdogan, Mumin Alper Erdogan, Oytun Erbas, Ismet Parlak

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Objective: The aim of this study was to evaluate histological, electrical and biochemical effects of metoprolol, lipid emulsion and magnesium sulphate as an alternative method to be used in preventing long QT emergence, that is among the lethal consequences of amitryptiline toxicity. Methods: Thirty Sprague- Dawley male rats were included. Rats were randomly separated into 5 groups. First group was administered saline only while the rest had received amitryptiline 100 mg/kg + saline, 5 mg/kg metoprolol, 20 ml/kg lipid emulsion and 75 mg/kg magnesium sulphate (MgSO4) intraperitoneally. ECG at DI lead, biochemical tests following euthanasia were performed in all groups after 1 hour of administration. Cardiac tissues were removed, sections were prepared and examined. Results: QTc values were significantly shorter in the rest when compared to amitryptiline+ saline group. While lipid emulsion did not affect proBNP and troponin values biochemically as compared to that of the control group, histologically, it was with reduced caspase 3 expression. Though statistically insignificant in the context of biochemical changes, pro-BNP and urea levels were lower in the metoprolol group when compared to controls. Similarly, metoprolol had no statistically significant effect on histological caspase 3 expression in the group that was treated with amitryptiline+metoprolol. On the other hand, there was a statistically significant decrease in Troponin, pro-BNP and urea levels as well as significant decline in histological caspase 3 expression within the MgSO4 group when compared to controls. Conclusion: As still a frequent cause of mortality in emergency units, administration of MgSO4, lipid emulsion and metoprolol might be beneficial in alternative treatment of cardiovascular toxicity caused by tricyclic antidepressant overdose, whether intake would be intentional or accidental.

Keywords: amitryptiline, cardiovascular toxicity, long QT, Rat Model

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Authors: I-Han Hsiao, Chun-Ping Huang, Ching-Liang Hsieh, Yi-Wen Lin

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Epilepsy is chronic brain disorder that results in the sporadic occurrence of spontaneous seizures in the temporal lobe, cerebral cortex, and hippocampus. Clinical antiepileptic medicines are often ineffective or little benefits in the small amount of patients and usually initiate severe side effects. This inflammation contributes to enhanced neuronal excitability and the onset of epilepsy. Auricular electric-stimulation (AES) can increase parasympathetic activity and stimulate the solitary tract nucleus to induce the cholinergic anti-inflammatory pathway. Furthermore, it may be a therapeutic strategy for the treatment of epilepsy. In the present study, we want to investigate the effects of AES on inflammatory mediators in kainic acid (KA)-induced epileptic seizure rats. Experimental KA injection increased expression of TLR-2 pathway associated inflammatory mediators, were further reduced by either 2Hz or 15 Hz AES in the prefrontal cortex, hippocampus, and somatosensory cortex. We suggest that AES can successfully control the epileptic seizure by down-regulation of inflammation signaling pathway.

Keywords: auricular electric-stimulation, epileptic seizures, anti-inflammation

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Authors: Mehdi Sheikhi, Marjan Nassiri-Asl, Esmail Abbasi, Mahsa Shafiee

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Various synthetic derivatives of natural flavonoids are known to have neuroactive properties. The present study aimed to investigate the effects of vitexin (5, 7, 4-trihydroxyflavone-8-glucoside), a flavonoid found in such plants as tartary buckwheat sprouts, wheat leaves phenolome, Mimosa pudica Linn and Passiflora spp, on scopolamine-induced memory impairment in rats. To achieve this goal, we assessed the effects of vitexin on memory retrieval in the presence or absence of scopolamine using a step-through passive avoidance trial. In the first part of the study, vitexin (25, 50, and 100 μM) was administered intracerebroventricularly (i.c.v.) before acquisition trials. In the second part, vitexin, at the same doses, was administered before scopolamine (10 μg, i.c.v.) and before the acquisition trials. During retention tests, vitexin (100 μM) in the absence of scopolamine significantly increased the stepthrough latencies compared to scopolamine. In addition, vitexin (100 μM) significantly reversed the shorter step-through latencies induced by scopolamine (P < 0.05). These results indicate that vitexin has a potential role in enhancing memory retrieval. A possible mechanism is modulation of cholinergic receptors; however, other mechanisms may be involved in its effects in acute exposure.

Keywords: flavonoid, memory retrieval, passive avoidance, scopolamine, vitexin

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Authors: Nurul Izzah Ibrahim, Isa Naina Mohamed, Norazlina Mohamed, Ahmad Nazrun Shuid

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Osteoporosis disease delays fracture healing. Statins have shown potential for osteoporosis and to promote fracture healing. The effects of statin can be further potentiated by combining it with a carrier known as poly-(DL-lactide), which would provide persistent release of statin to the fracture site. This study was designed to investigate the effects of direct injection of poly-(DL-lactide)-incorporated lovastatin on fracture healing of postmenopausal osteoporosis rat model. Twenty-four Sprague-Dawley female rats were divided into 3 groups: sham-operated (SO), ovariectomized-control rats (OVxC) and poly-(DL-lactide)-incorporated lovastatin (OVx+Lov) groups. The OVx+Lov group was given a single injection of 750 µg/kg lovastatin particles incorporated with poly-(DL-lactide). After 4 weeks, the fractured tibiae were dissected out for biomechanical assessments of the callus. The OVx+Lov group showed significantly better callus strength than the OVxC group (p<0.05). In conclusion, a single injection of lovastatin-incorporated poly-(DL-lactide) was able to promote better fracture healing of osteoporotic bone.

Keywords: statins, fracture healing, osteoporosis, poly-(DL-lactide)

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Authors: Anshu Bahl, Saroj Kaler, Shivani Gupta, S B Ray

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Background: Somatostatin is an endogenous regulatory neuropeptide. Somatostatin and its analogues play an important role in neuropathic and inflammatory pain. Neuropeptide Y is extensively distributed in the mammalian nervous system. NPY has an important role in blood pressure, circadian rhythm, obesity, appetite and memory. The purpose was to investigate somatostatin and NPY expression in dorsal root ganglia during pain. The plantar incision model in rats is similar to postoperative pain in humans. Methods: 24 adult male Sprague dawley rats were distributed randomly into two groups – Control (n=6) and incision (n=18) groups. Using Hargreaves apparatus, thermal hyperalgesia behavioural test for nociception was done under basal condition and after surgical incision in right hind paw at different time periods (day 1, 3 and 5). The plantar incision was performed as per standard protocol. Perfusion was done using 4% paraformaldehyde followed by extraction of dorsal root ganglia at L4 level. The tissue was processed for immunohistochemical localisation for somatostatin and neuropeptide Y. Results: Post incisional groups (day 1, 3 and 5) exhibited significant decrease of paw withdrawal latency as compared to control groups. Somatostatin expression was noted under basal conditions. It decreased on day 1, but again gradually increased on day 3 and further on day five post incision. The expression of Neuropeptide Y was noted in the cytoplasm of dorsal root ganglia under basal conditions. Compared to control group, expression of neuropeptide Y decreased on day one after incision, but again gradually increased on day 3. Maximum expression was noted on day five post incision. Conclusion: Decrease in paw withdrawal latency indicated nociception, particularly on day 1. In comparison to control, somatostatin and NPY expression was decreased on day one post incision. This could be correlated with increased axoplasmic flow towards the spinal cord. Somatostatin and NPY expression was maximum on day five post incision. This could be due to decreased migration from the site of synthesis towards the spinal cord.

Keywords: dorsal root ganglia, neuropeptide y, postoperative pain, somatostatin

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Authors: Mohd Aslam Aslam

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Chronic renal failure is a debilitating condition responsible for high morbidity and mortality. Because of its costs and the complexity of its treatment, proper care is available to very few patients in India. According to researchers, the number of adults aged 30 or older who have chronic kidney disease is projected to increase from 13.2 percent currently, to 14.4 percent in 2020 and 16.7 percent in 2030. The aerial part of Aerva lanata (Busehri booti) have been used in kidney disorders by the Unani physicians. In the present study, the effect of extract of Aerva lanata was investigated on cisplatin-induced nephrotoxicity in rats. The renal effects of this drug was evaluated by monitoring levels of blood urea nitrogen (BUN), serum creatinine, serum uric acid in blood and histopathological examination of kidney. Aerva lanata was evaluated at two different doses (1400 mg/kg and 2800 mg/kg). The effect of higher dose was more pronounced in terms of inhibition in the rise of BUN, serum creatinine and uric acid. Higher dose show greater prevention in the rise of BUN, serum creatinine, and uric acid. The histopathological examination of the kidney tissue of the rats treated with aqueous methanolic extract of Aerva lanata (Higher dose-2800 mg/kg) showed marked inhibition of glomerular congestion, tubular casts, peritubular congestion, epithelial desquamation, blood vessel congestion, interstitial edema and inflammatory cells produced by the cisplatin-induced nephrotoxicity. This finding clearly indicates the protective role of Aerva lanata at higher dose. Present investigation validates the use of Aerva lanata in kidney disorders by Unani physicians.

Keywords: Aerva lanata, Busehri booti, nephroprotective, unani medicine

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Authors: Kalimullah Khan, Samina Roohi, Mohammad Rafi, Rizwana Zahoor

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Labeling of 5-Aminolevulinic acid (5-ALA) with 99 mTc was achieved by using tin chloride dihydrate (Sncl2.2H2O) as reducing agent. Radiochemical purity and labeling efficiency was determined by Whattman paper No.3 and instant thin layer chromatographic strips impregnated with silica gel (ITLC/SG). Labeling efficiency was dependent on many parameters such as amount of ligand, reducing agent, pH, and incubation time. Therefore, optimum conditions for maximum labeling were selected. Stability of 99 mTc- 5-ALA was also checked in fresh human serum. Tissue bio-distribution of 99 mTc-5-ALA was evaluated in Spargue Dawley rats. 5-ALA was 98% labeled with 99 mTc under optimum conditions, i.e. 100µg of 5-ALA, pH: 4, 10µg of Sncl2.2H2O and 30 minutes incubation at room temperature. 99 mTc labelled 5- ALA remained stable for 24 hours in human serum. Bio-distribution study (%ID/gm) in rats revealed that maximum accumulation of 99 mTc-5-ALA was in liver, spleen, stomach and intestine after half hour, 4 hours, and 24 hours. Significant activity in bladder and urine indicated urinary mode of excretion.

Keywords: 99mTc-ALA, aminolevulinic acid, quality control, radiopharmaceuticals

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Authors: Tita Nofianti, Tresna Lestari, Ade Y. Aprillia, Lilis Tuslinah, Ruswanto Ruswanto

Abstract:

Nanoparticle technology gives a chance for drugs, especially natural based product, to give better activities than in its macromolecule form. The ginger torch is known to have activities as an antioxidant, antimicrobial, anticancer, etc. In this research, ginger torch flower extract was nanoparticlized using poloxamer 1, 3, and 5%. Nanoparticle was charaterized for its particle size, polydispersity index, zeta potential, entrapment efficiency, and morphological form by SEM (scanning electron microscope). The result shows that nanoparticle formulations have particle size 134.7-193.1 nm, polydispersity index is less than 0.5 for all formulations, zeta potential is -41.0 to (-24.3) mV, and entrapment efficiency is 89.93 to 97.99 against flavonoid content with a soft surface and spherical form of particles. Methanolic extract of ginger torch flower could enhance superoxide dismutase activity by 1,3183 U/mL in male rats. Nanoparticle formulation of ginger torch extract is expected to increase the capability of drug to enhance superoxide dismutase activity.

Keywords: superoxide dismutase, ginger torch flower, nanoparticle, poloxamer

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