In the present study, antihyperglycemic and hypolipidemic effects of stem extract of Euphorbia hirta were studied in albino mice by administering graded oral doses (250 and 500 mg/kg body weight) of the extract for 21 days. The ethanolic and petroleum ether extracts of stems of the E. hirta were orally tested for 21 days in alloxan induced diabetic mice and blood glucose level was measured with glucometer. Administration of extract resulted in significant reduction in serum cholesterol, triglycerides, creatinine, urea, alkaline phosphatase levels but HDL levels and total proteins were found to be increased after treatments. The antioxidant activity of extracts were also evaluated by various antioxidant assays, including DPPH free radical scavenging activity, superoxide anion radical scavenging, nitric oxide scavenging and reducing power assay. The various antioxidant activities were compared to standard antioxidants such as butylated hydroxyl anisole and ascorbic acid. All the extracts showed antioxidant activity in all the tested methods.
The present study was carried out to determine the effect of hydroalcoholic extract of Semecarpus anacardium nut (SANE) and the possible interaction with propranolol (PRO) on experimentally induced myocardial infarction (MI) in rats. Isolated rat hearts were infused with propranolol 10 µg/ml (PRO), SANE 1 µg/ml (SANE 1), SANE 10 µg/ml (SANE 10), SANE 25 µg/ml (SANE 25), SANE 50 µg/ml (SANE 50) and SANE 10 + PRO dissolve in KH solution using modified Langendorff’s apparatus through the aorta and subjected to ischemic reperfusion injury (IRI) by stopping the KH flow. The influence of different treatment was analysed by quantification of % recovery in terms of heart rate and force of contraction, biomarkers and antioxidants in post ischemic condition and histopathological studies. The superoxide dismutase and catalase activities were reduced in the heart tissue of isolated heart perfused with PRO, SANE 1, SANE 10, SANE 25, SANE 10 +PRO compared with IRI control. The biomarker LDH activity decreases in perfusate with PRO, SANE 1, SANE 10, SANE 25, SANE 10+PRO treatment and rises in heart tissue homogenate (HTH) of SANE 10 and SANE 10+PRO group compared with IRI control. CKMB activity decreases significantly in perfusate of SANE 10 and SANE 10+PRO groups and elevated in HTH in the groups PRO, SANE 10, SANE 25, SANE 10+PRO as compared with IRI control. Significant level of % recovery in terms of heart rate and developed tension were observed in groups infused with SANE 10 and SANE 10+PRO compared with IRI control. Histopathological studies reported SANE 10+PRO as a best protective group. To conclude, perfusion of SANE 10 with PRO in combination demonstrated most significant cardioprotective efficacy in isolated rat heart subjected to ischemia reperfusion injury.
In present work was designed to develop suitable transdermal matrix patches of Lovastatin (LS), using hydroxy propyl methyl cellulose (HPMC) and Eudragit RL 100 with Triethyl citrate as a plasticizer. A 32 full factorial design was employed, the amount of HPMC( X1) and Eudragit RL- 100( X2), was used as independent variables. The folding endurance, tensile strength, moisture content, moisture uptake and diffusion of drug were selected as dependent variables. The Casting solvent technique was employed for the preparation of HPMC, ERL-100 film. The dry films were evaluated for Physical appearance, thickness uniformity, moisture content, moisture uptake, tensile strength, flatness and folding endurance. In vitro diffusion studies were performed using cellulose acetate membrane (pore size 0.45 µ) in a Franz’s diffusion cell. The concentration of diffused drug was measured using UV-visible spectrophotometer (Jasco V-530) at λ max 254 nm. The experimental results shows that the patch containing HPMC in higher proportion gives increase in the release of drug. It indicates that as the concentration of X2 (Eudragit RL 100) increase, the drug release from the matrix was decrease. The present study has demonstrated the potential of the fabricated matrix film for prolonged release of Lovastatin.
The aim of present work was to improve the solubility of a poor water soluble drug, cinnarizine, by using solid dispersion technique. Cinnarizine is a H1-receptor antagonist and widely used in the treatment of motion sickness, vomiting and vertigo. In the present work solid dispersion of cinnarizine were prepared with a polyethylene glycol 4000 and polyvinyl pyrrolidone K30 by using solvent evaporation and fusion method in the 1:1, 1:2 and 1:3 ratio of drug and carrier respectively. Solid dispersion of cinnarizine was evaluated for drug content, Infrared spectroscopy and In vitro dissolution study. The solid dispersion with PEG and PVP exhibited enhanced dissolution rate of cinnarizine. IR spectra revealed no chemical incompatibility between drug and carrier. The dissolution of the solid dispersion was carried out in 0.1N HCl. The In vitro dissolution study showed a significant increase in the release rate of cinnarizine in solid dispersion of cinnarizine with polyvinyl pyrrolidone K30 in the ratio 1:3 prepared by solvent evaporation method.
A number of pieces of evidence suggest a role of the serotonin in cognitive function. Early studies failed to distinguish between the roles of the many 5-HT receptor subtypes due to the lack of selectivity of the ligands used in these studies. Recently, the role of the neurotransmitter serotonin (5-HT) and its receptor subtypes in cognition has emerged and with the availability of Antisense oligonucleotides, antipeptide antibodies, selective radioligands, knockout mice, and selective antagonists of the 5-HT6 receptor, the focus on 5-HT receptor subtypes as targets for memory enhancement has increased. This article will focus on the role of the most recently identified 5-HT receptor subtype, i.e. the 5-HT6 receptor and its antagonists present in various clinical and preclinical phases in modulating cognitive function.
The pharmaceutical industry is under extraordinary strain. Facing the wrath of consumers because of the cost of products, constantly answering the questions of state and federal legislators looking to control health care costs, and losing value in the marketplace, the industry’s hands are more than full. A less discussed but substantial problem impacts all of pharmaceutical industry’s other problems, counterfeiting. The World Health Organization estimates that counterfeit drugs make up about 10 percent of the global medicine market, and more than 25 percent in developing countries. With counterfeit drugs increasingly finding their way into global distribution chains and ultimately into patients' mouths, it is essential that pharmaceutical companies have effective enforcement strategies to combat the manufacture and distribution of counterfeit drugs.
Emerging as an epidemic of the 21st century type II diabetes has become a major health problem throughout the globe. Known treatments of type II diabetes mellitus have limitations such as weight gain and hypoglycaemias. A new perspective is the use of incretin hormones and incretin enhancers. Incretin mimetics are a new class of pharmacological agents with multiple antihyperglycemic actions that mimic the actions of incretin hormones such as glucagon-like peptide (GLP)-1. DPP-4, a protease that specifically cleaves dipeptides from proteins and oligopeptides after a penultimate N-terminal proline or alanine, is involved in the degradation of a number of neuropeptides, peptide hormones and cytokines, including the incretins GLP-1 and GIP. Based on preliminary clinical data, incretin mimetics and DPP-IV inhibitors show potential for treating type II diabetes.
In the present work attempts were made to prepare fast-dispersible tablets of Sertraline by direct compression method with a view to enhance patient compliance. The three superdisintegrants used in this study were Crosscarmellose sodium, Crospovidone and Sodium starch glycolate. Tablets having superdisintegrant at different concentration (8, 10 and 12 mg) level were prepared. The prepared batches of tablets were evaluated for uniformity of weight, thickness, hardness, friability, in-vitro dispersion time and in-vitro dissolution study. Tablet containing crosscarmellose sodium showed excellent in vitro dispersion time and drug release as compared to other formulations. After study, formulation N6 shows short dispersion time with maximum drug release in 40 minutes.
Free radicals are implicated for many diseases including Diabetes mellitus, arthritis, cancer, ageing etc. In treatment of these diseases, antioxidant therapy has gained utmost importance. Antioxidants can also help to repair damage already sustained by cells. Randia dumetorum Lamk. is a plant of medicinal important belongs to the family Rubiaceae. Polyphenols are good antioxidant. Fruits consist of Phenolic in large amount. It is traditionally used to cure diseases but no scientific data is available. Thus the objective of present study was aimed to check the antioxidant potential of Aqueous extract of Randia dumetorum fruits using different models viz. DPPH radical scavenging, iron chelating activity and nitric oxide scavenging assay. The results were analyzed statistically by regression method. The % scavenging activity at different concentrations was determined and the IC50 value of the extracts was compared with that of standard, ascorbic acid. Its antioxidant activity was estimated by IC50 value and the values are 45.02 μg/ml (reducing power assay), 66 μg/ml, (DPPH scavenging assay) and 79.09 μg/ml (nitric oxide scavenging assay). In all the testing, a significant correlation existed between concentrations of the extract and percentage inhibition of free radicals, metal chelation. According to these results, it may be hypothesized that antioxidant effect of fruits could be related to presence of polyphenolic compounds. These results clearly indicate that Randia dumetorum is effective against free radical mediated diseases.
The purpose of this prospective randomized single blind study was to determine the anesthetic efficacy of combination of 2 % Lidocaine with 1 : 80,000 Epinephrine and 0.5 mol / L Mannitol in Inferior Alveolar Nerve (IAN) Blocks in patients with symptomatic irreversible pulpitis. 60 subjects randomly received IAN Blocks using the following two anesthetic formulations: one formulation comprised of 2.5 ml of 2 % Lidocaine with 1 : 80,000 Epinephrine and the other formulation comprised of 1.6 ml of 2 % Lidocaine with 1 : 80,000 Epinephrine and 0.9 ml of 0.5 mol / L Mannitol. The pain response of the patient was recorded on endodontic access and initial instrumentation using the Heft-Parker Visual Analogue Scale. From the statistical analysis obtained following this study the addition of 0.5 mol / L Mannitol to lidocaine with epinephrine formulations significantly improved effectiveness in achieving a greater percentage of total pulpal anesthesias compared with a lidocaine formulation without Mannitol for IAN blocks. There is a significant improvement in the efficacy of IAN blocks when 2 % Lidocaine with 1 : 80,000 Epinephrine is administered in combination with 0.5 mol / L Mannitol. Based on the results of this study we can conclude that this combination of local anesthetic should be used on a regular basis to obtain successful anesthesia. However there is a need for more research as there are very few studies done on this aspect.
Antioxidants have gained importance as pharmacological agents and have been consumed in various forms mainly as fruits, vegetables and dietary supplements. These antioxidants are majorly obtained from plant source or have been synthesized chemically. This study concentrated on the in vitro evaluation of antioxidant property of a water soluble metabolite from Streptomyces species KSRO-04. The antioxidant activity was evaluated by Total phenolic content, total flavonoid content, total antioxidant activity, DPPH assay, lipid peroxidation inhibition assay, nitric oxide scavenging activity, Super oxide anion scavenging activity, Metal ion chelating activity and total reductive capability. The metabolite was characterised using TLC and purity was assessed by HPLC. The UV absorption indicated absorption maximum of 360nm suggesting a polyene nature of the metabolite. The metabolites showed a moderate antioxidant activity with good nitric oxide scavenging activity and also hinted that the anti oxidant activity is not solely due to the phenolic compounds. The metabolite from the Streptomyces species KSRO-04 is a potent antioxidant agent which suggests its beneficiary role as a pharmacological agent.
Free radicals are molecules containing unpaired electrons so that they are not stable and very reactive to other molecules. ROS/RNS radicals have physiological function, but the overproduction of free radicals can initiate oxidative/nitrosative stress that contributes to a high number of diseases. Body has an ability to neutralize the free radicals by forming the endogenous antioxidant. Environmental changes, living style, certain pathological conditions can cause the shift of prooxidant-antioxidant equilibrium. Thus, endogenous antioxidant intake is needed, particularly that originating from natural materials. One of the plants believed to have antioxidant activity is sesewanua (Clerodendrum fragrans [Vent.] Willd.) leaf. This study was aimed to evaluate the antioxidant activity of ethanol extract, hexane fraction, ethyl acetate fraction, and water fraction of the sesewanua leaf using DPPH and nitrate-oxide free radical scavenging method. The study is a laboratory experiment. The sample was sesewanua (Clerodendrum fragrans) obtained from East Malalayang I village, Malalayang district, Manado city, North Sulawesi. The antioxidant activity testing utilized 1,1-Diphenyl-2-Picrylhydrazyl (DPPH) and nitrate-oxide free radical scavenging method. Data included percent inhibition of free radicals and were analyzed using linear regression to determine 50% inhibition concentration (IC50) of DPPH and nitrate-oxide free radicals. As conclusion, the ethanol extract, hexane fraction, ethyl acetate fraction, and water fraction of the sesewanua leaf had antioxidant activity through DPPH free antiradical activity, but not active as antiradical NO.
Colorectal cancer is increasingly common nowadays in Asian countries and still remains the second leading cause of cancer death in the United States. The chemopreventive and hypolipidemic effect of Caralluma adscendens (Roxb.), an edible succulent, was studied in 1,2-dimethylhydrazine (DMH)-induced colon cancer. Rats were given a weekly subcutaneous injection of DMH (20 mg/kg body weight), a known colon carcinogen, in the groin for 16 weeks. Caralluma adscendens (Roxb.) (50 & 100 mg/kg body weight P.O.) was given at the initiation stage of carcinogenesis. The animals were sacrificed at the end of the experimental period of 30 weeks. The tissue lipid profile was evaluated using various biochemical estimations. The levels of cholesterol, HMG CoA reductase, free fatty acids, and triglycerides were significantly increased, whereas the levels of tissue phospholipids were decreased in DMH-treated rats as compared to control rats. On administering caralluma adscendens (Roxb.) at the initiation stage of colon carcinogenesis, the levels of tissue cholesterol, HMG CoA reductase, free fatty acids, triglycerides were significantly decreased, whereas the levels of phospholipids were increased as compared to unsupplemented DMH treated rats in dose dependent manner. Thus, Caralluma adscendens (Roxb.) supplementation was found to reduce the risk of colon cancer markedly by virtue of its hypolipidemic and antioxidative effects.
Different heterocyclic analogues were evaluated for their diverse biological activities. Out of them, the 1,2,4-triazole nucleus is an ubiquitous structural feature of many synthetic compounds with diversified therapeutic efficacy. A large volume of published literature over the last few decades precludes a comprehensive review. The triazole moiety seems to be very small but its broad biological profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. This article presents a comprehensive review on the pharmacological activities of some novel derivatives of the 1,2,4-triazole moiety.
(PDF) 1,2,4-TRIAZOLE: A REVIEW OF PHARMACOLOGICAL ACTIVITIES. Available from: https://www.researchgate.net/publication/318895777_124-TRIAZOLE_A_REVIEW_OF_PHARMACOLOGICAL_ACTIVITIES [accessed Oct 06 2020].
Resistance to bacteria is a growing threat to human health worldwide. The rate of discovery of new antibacterial is far outshined by the rate at which resistance is spreading. Therefore, there remains a pressing need for the development of new antibacterial drugs. Recent alarm estimates that deaths due to antimicrobial resistance may increase from 700,000 million lives annually by 2050. Glucosamine-6-phosphate (GlcN-6-P) synthase represents an interesting protein target because it plays an essential role in the protection of cell wall. The primary aim and objective of this study is to identify lead molecules as promising antibacterial agents by inhibiting Glucosamine-6-phosphate (GlcN-6-P) synthase enzyme. Autodock 4. 2, the effective tool for exploring the binding affinity of small molecule to enzyme target was used to study the interactions between the oxazine derivatives and the GlcN-6-P synthase binding site. The ligands were optimized for improving their efficacy and safety. Lead optimization was performed using Molinspiration server and the ligands were optimized for evaluating their oral bioavailability. With Glucosamine 6 phosphate synthase receptor, the binding energy was found to be best for 5 compounds SZ-3 (-5.27 kcal/mol), SZ-4 (-6.02 kcal/mol), SZ-5 (-5.35 kcal/mol), SZ-8 (-5.62kcal/mol), SZ-10 (-5.29 kcal/mol) when compared to the standard ligand, Ciprofloxacin (-5.09 kcal/mol) and were interacting well with the key residues TYR 304, GLU 438, LEU 484. Docking study strongly enhanced the activity of oxazine derivatives as new discovered hits.