Showing papers in "Indian Journal of Pharmaceutical Sciences in 2014"
TL;DR: The use of Triphala and its three individual constituents as potential immunostimulants and/or immunosuppressants further suggests them to be a better alternative for allopathic immunomodulators.
Abstract: The role of plant extracts and Ayurvedic polyherbal preparations in treating various ailments has been acknowledged since time immemorial. Studies based on the effect of these extracts in treatment of different diseases have also been well documented. Indian medicinal literature also emphasizes the synergistic effect of polyherbal drugs in restoring and rejuvenating immune system. This review focuses on the immunomodulatory potential of the polyherbal preparation, Triphala and its three constituents, Terminalia bellerica, Terminalia chebula and Emblica officinalis. The role of Triphala and its extract has been emphasized in stimulating neutrophil function. Under stress condition such as noise, Triphala significantly prevents elevation of IL-4 levels as well as corrects decreased IL-2 and IFN-γ levels. Under the condition of inflammatory stress its immunosuppressive activity is attributed to its inhibitory action on complement system, humoral immunity, cell mediated immunity and mitogen-induced T-lymphocyte proliferation. The aqueous and alcoholic extracts of the individual constituents reportedly enhance especially the macrophage activation due to their free radical scavenging activity and the ability to neutralize reactive oxygen species. This study thus concludes the use of Triphala and its three individual constituents as potential immunostimulants and/or immunosuppressants further suggests them to be a better alternative for allopathic immunomodulators.
69 citations
TL;DR: In this article, the authors investigated in vitro antimycobacterial activity as well as anti-bacterial activity of various extracts rich in specific phytoconstituents from garlic.
Abstract: Tuberculosis is one of the major public health problems faced globally. Resistance of Mycobacterium tuberculosis to antitubercular agents has called for an urgent need to investigate newer drugs to combat tuberculosis. Garlic (Allium sativum) is an edible plant which has generated a lot of curiosity throughout human history as a medicinal plant. Garlic contains sulfur compounds like allicin, ajoene, allylmethyltrisulfide, diallyltrisulfide, diallyldisulphide and others which exhibit various biological properties like antimicrobial, anticancer, antioxidant, immunomodulatory, antiinflammatory, hypoglycemic, and cardiovascular effects. According to various traditional systems of medicine, garlic is one of the established remedies for tuberculosis. The objective of the current study was to investigate in vitro antimycobacterial activity as well as anti-bacterial activity of various extracts rich in specific phytoconstituents from garlic. Preparation of garlic extracts was done based on the chemistry of the constituents and their stability. The estimation of in vitro antimycobacterial activity of different garlic extracts was done using Resazurin microtire plate assay technique whereas activity of garlic oil was evaluated by colony count method. The antibacterial activity of extracts and oil was estimated by zone of inhibition method. Extracts of garlic rich in allicin and ajoene showed appreciable antimycobacterial activity as compared to standard drugs. Garlic oil demonstrated significant antibacterial activity, particularly against methicillin-resistant Staphylococcus aureus.
59 citations
TL;DR: A green chemistry approach for organic synthesis is described here, which involves microwave exposure of reactants in presence or absence of solvents and suggests that microwave-assisted syntheses lead to higher yields within very short reaction times.
Abstract: A green chemistry approach for organic synthesis is described here, which involves microwave exposure of reactants in presence or absence of solvents. A novel and simple method has been developed for the synthesis of some benzotriazole derivatives under microwave irradiation. In addition, these compounds were synthesised also by conventional heating procedures for comparison. All the compounds synthesised were characterised by melting point, TLC, IR and (1)H NMR spectroscopy. Comparison between conventional and microwave-assisted synthesis was done by comparing total reaction time and percentage yield. The results suggest that microwave-assisted syntheses lead to higher yields within very short reaction times. On antifungal evaluation by cup plate method, all compounds showed antifungal activity. One compound showed activity similar to and two compounds showed better activity than standard antifungal drug flucanazole.
42 citations
TL;DR: It is suggested that adult zebrafish produce the expected anticonvulsive and proconvulsive effects and could potentially be used as a screen in future epilepsy research.
Abstract: Recently zebrafish larvae have emerged as a high-throughput model for screening pharmacological activities. The present study was undertaken to investigate the effect of established anticonvulsants, such as valproic acid, carbamazepine, gabapentin, diazepam, lacosamide and pregabalin against pentylenetetrazole (6 mM) seizures in adult zebrafish. Different phases of seizures (increase swim activity, rapid whirlpool-like circling swim behaviour and brief clonus-like seizures leading to loss of posture) were elicited in zebrafish on exposure for 15 min to 6 mM pentylenetetrazole. The exposure of zebrafish to an increasing concentration of the anticonvulsants alongside 6 mM pentylenetetrazole showed concentration-dependent elevation of seizure latency against pentylenetetrazole-induced seizures except for pregabalin, which failed to produce any anticonvulsant activity in zebrafish. Moreover the proconvulsant activity of caffeine was also evaluated using suboptimal concentration (4 mM) of pentylenetetrazole in adult zebrafish. Decrease in seizure latency of different phases of seizures was observed with increasing concentration of caffeine compared with its respective control group. In view of the above findings, the results of the present study suggested that adult zebrafish produce the expected anticonvulsive and proconvulsive effects and could potentially be used as a screen in future epilepsy research.
37 citations
TL;DR: A novel, simple, accurate and reproducible high performance thin layer chromatographic method was developed, which would be of use in quality control of these tablets, and appeared to have significant effect on robustness.
Abstract: High performance thin layer chromatographic method for simultaneous estimation of olmesartan medoxomil, amlodipine besylate and hydrochlorothiazide was developed and validated as per ICH guidelines. Moreover, robustness testing was performed applying a central composite design with k factor having 2 k factorial runs, 2k axial experiments and two center points. High performance thin layer chromatographic separation was performed on aluminium plates precoated with silica gel 60F 254 and toluene:chloroform:methanol:acetonitrile:formic acid (2:7:1.8:0.8:0.2% v/v) as optimized mobile phase. The detection wavelength for simultaneous estimation of three drugs was 232nm. The R f values for olmesartan medoxomil, amlodipine besylate and hydrochlorthiazide were 0.78, 0.20 and 0.45, respectively. Percent recoveries in terms of accuracy for the marketed formulation was found to be 101.3-104.4, 100.7-104 and 101.5-103.9 for, olmesartan medoxomil, amlodipine besylate and hydrochlorthiazide, respectively. The pooled %relative standard deviation values for repeatability studies and intermediate precision studies was found to be less than 2% for olmesartan medoxomil, amlodipine besylate and hydrochlorthiazide, respectively. All the three factors evaluated in the robustness testing by central composite design were found to have an insignificant effect on the retention factor. However, methanol content in total mobile phase as a factor appeared to have significant effect on robustness, compared to band size and developing distance and hence it is important to be carefully controlled. In summary, a novel, simple, accurate and reproducible high performance thin layer chromatographic method was developed, which would be of use in quality control of these tablets.
28 citations
TL;DR: It is found that recovery of cognitive function in the resveratrol group (15 mg/kg/day), was significantly better than that of either the untreated or the vehicle groups, and S100B protein levels in cerebral spinal fluid and serum of rats treated with resver atrol were significantly reduced compared with the untreated and vehicle groups.
Abstract: S100B protein in serum and cerebral spinal fluid is increasingly used as a biochemical marker in early examinations after seizure to assess brain damage. Resveratrol, a nonflavonoid polyphenol, has been identified as a potent antiepileptic agent. However, a potential association between epilepsy with S100B protein in the cerebral spinal fluid and the sera of animal models lacks investigation. In this study, we evaluated the effects of resveratrol on behaviour and S100B protein levels in cerebral spinal fluid and serum in a rat model of chronic epilepsy induced via pentylenetetrazole kindling. By Morris water maze experiment analysis, we found that recovery of cognitive function in the resveratrol group (15 mg/kg/day), was significantly better than that of either the untreated or the vehicle groups. Further Nissl staining revealed that resveratrol significantly reduced pentylenetetrazole-induced death of neurons in the CA1 and CA3 regions of the hippocampus. Moreover, S100B protein levels in the cerebral spinal fluid and serum of rats treated with resveratrol were significantly reduced compared with the untreated and vehicle groups. These novel findings suggest an important mechanism of resveratrol and contribute to the treatment of epilepsy.
26 citations
TL;DR: An attempt has been made to review various natural substances with aldose reductase inhibitory activity and their role in management of diabetic complications.
Abstract: Diabetes is a disease, which has assumed vital public health importance because of the complications associated with it Various mechanisms including polyol pathway along with a complex integrating paradigm have been implicated in glucose-mediated complications Though polyol pathway was established as a major mechanism, precise pathogenesis of these complications is not yet completely elucidated Thus research focus was shifted towards key enzyme, aldose reductase in the pathway Even though various compounds with aldose reductase inhibitory activity were synthesised, a very few compounds are under clinical use However, studies on these compounds were always under conflicting results and an attempt has been made to review various natural substances with aldose reductase inhibitory activity and their role in management of diabetic complications
26 citations
TL;DR: The potential biological activities of camellia assamica and Camellia sinensis having massive phytochemical constituents and trace elements are revealed and the presence of active biological compounds such as flavonoids, proteins, phenols, alkaloids and glycosides also exhibited strong activity against tested bacterial strains.
Abstract: This study was carried out as a prerequisite to evaluate the therapeutic potential of Camellia varieties. The crude extracts of six different plants of green tea Camellia assamica and Camellia sinensis were tested against three Gram-positive and four Gram-negative bacteria using agar disk diffusion method at 50 mg/ml concentration. 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) and diphenyl-(2,4,6-trinitrophenyl)iminoazanium free radical scavenging methods were performed to evaluate the antioxidant potential. Phytochemical constituents and trace metals were detected through thin layer chromatography and Inductively Coupled Plasma Atomic Emission Spectrophotometer, respectively. The maximum inhibition of Staphylococcus aureus was recorded by dimethyl sulphoxide extracts of green tea varieties. The measured zone of inhibition of dimethyl sulphoxide extracts by Qimen was (10.00±0.0 mm), Japanese (10.00±0.0 mm), Turkish (10.00±0.0 mm), Indonesian (8.33±1.0 mm), P3 clone (10.00±0.0 mm) and Sri Lankan (10.00±0.0 mm). Maximum scavenging potential activity was found with ethanol, methanol and dimethyl sulphoxide extracts. Spot screening of TLC-developed plates indicated that the presence of active biological compounds such as flavonoids, proteins, phenols, alkaloids and glycosides also exhibited strong activity against tested bacterial strains. This study reveals the potential biological activities of Camellia assamica and Camellia sinensis having massive phytochemical constituents and trace elements.
25 citations
TL;DR: A simple, specific, accurate and rapid reversed phase high performance liquid chromatographic method was validated for the determination of the content of ciprofloxacin in three pharmaceuticals forms: generic, similar and compounded and showed that the method was highly efficient for quantification in the matrices evaluated.
Abstract: A simple, specific, accurate and rapid reversed phase high performance liquid chromatographic method was validated for the determination of the content of ciprofloxacin in three pharmaceuticals forms: generic, similar and compounded. The results of the validation showed that the method was highly efficient for quantification of ciprofloxacin in the matrices evaluated. The recovery rates were between 97.4 to 104.3 %, and the relative standard deviations were lower than 5 % for repeatability, and lower than 5.15 % for intermediate precision. The limits of detection, quantification and practical, were 0.11, 0.35 and 1.56 μg/ml, respectively. All compounded samples were approved with in the quality control; however, one generic and one similar sample presented above allowed level.
25 citations
TL;DR: Limiting the use of newer and costlier antibiotics, branded drugs and number of drugs per prescription could be considered as targets to cut down the cost of drug therapysignificantly.
Abstract: Drug therapy accounts for a major portion of health expenditure. A useful strategy for achieving cost efficient healthcare is drug utilisation research as it forms the basis for making amendments in drug policies and helps in rational drug use. The present observational study was conducted to generate data on drug utilization in inpatients of our tertiary care hospital to identify potential targets for improving drug prescribing patterns. Data was collected retrospectively from randomly selected 231 medical records of patients admitted in various wards of the hospital. WHO Anatomical Therapeutic Chemical/Defined Daily Dose methodology was used to assess drug utilisation data and drug prescriptions were analysed by WHO core drug indicators. Antibiotics were prescribed most frequently and also accounted for majority of drug costs. The prescribed daily dose for most of the antibiotics corresponded to defined daily dose reflecting adherence to international recommendations. Brand name prescribing and polypharmacy was very common.78% of the total drugs prescribed were from the National List of Essential Medicines 2003. Restricting the use of newer and costlier antibiotics, branded drugs and number of drugs per prescription could be considered as targets to cut down the cost of drug therapysignificantly.
25 citations
TL;DR: It is suggested that ethanol extract of Oroxylum indicum might have potential chemical constituents that could be used in the future for the development of novel analgesic agent.
Abstract: We aimed to study phytochemical screening and analgesic activity of ethanol extract of Oroxylum indicum. The dried powder of the barks of the plant was extracted with 95% ethanol and was subjected to various phytochemical tests to ascertain the principle constituents contained in the extract. The result revealed the presence of alkaloids, flavonoids, tannins, glycosides in the ethanol extract of Oroxylum indicum. The extract was screened for analgesic activity by using hot plate, acetic acid-induced writhing and formalin test. The ethanol extract of the plant at two different doses (250 and 500 mg/kg) showed significant (P<0.05) analgesic effect in all test methods (hot plate, acetic acid-induced writhing and formalin). The analgesic activity was compared with a standard drug (ketorolac at 10 mg/kg). Based on the present findings and previous literature review it can be concluded that flavonoids and tannins might be responsible for the analgesic activity. We suggest that ethanol extract of Oroxylum indicum might have potential chemical constituents that could be used in the future for the development of novel analgesic agent.
TL;DR: Among the chemical induced model, antimycin mediated cell injury was more reliable for ischemia reperfusion study and enzymatic model was found to be best among the three approaches as it can create injury in short experimental time and are reproducible.
Abstract: Renal ischemia reperfusion injury contributes patho-physiological imbalance of acute renal failure that comprises of generation of reactive oxygen species, nitric oxide and peroxynitrite and inflammation involving cytokine/adhesion molecule cascade, finally leads to cell death. Oxygen deprival associated with ischemia that in turn lead to decline ATP production is the characteristic feature usually addressed in the development of in vitro cell based ischemic model. In order to create oxygen deficit in the cell lines different approaches like chemical induction, enzymatic induction and anaerobic chamber models are widely used. However efficiencies of these models were varied and the present study was aimed to compare the suitability of these models in creating in vitro ischemia reperfusion in cell culture. In the chemical induced method we used different concentrations of rotenone, antimycin and sodium azide to inhibit electron transport chain and thereby reduced the ATP production, measured indirectly by cell viability assay. Among the chemical induced model, antimycin mediated cell injury was more reliable for ischemia reperfusion study. In the enzymatic model, comprises of glucose oxidase (3mM/s) and catalase (998 s(-1) at 10:1 ratio) was used and found to be best among the three approaches as it can create injury in short experimental time and are reproducible. However anaerobic chamber method was not suitable for ischemia reperfusion study as it need more time to induce significant cell injury.
TL;DR: There is a need for interventions focusing on HIV/AIDS prevention and management, optimum resource allocation and development of antiAIDS campaigns to reduce the infection rate.
Abstract: HIV/AIDS has reached a pandemic level across the world with more than 33 million people who are living with HIV. In the United States, more than half a million people have been victims of AIDS. This study investigates the most vulnerable racial minority population (the African Americans) in the United States and the second least affected (the Caucasians) in order to predict the trends of the epidemic. A Markov chain analysis was used to model the progression of the disease among vulnerable people, infective people and AIDS cases for the two races separately, based on the 2009 Centers of Disease Control and Prevention HIV/AIDS Surveillance Report. Based on the Markov model, our study predicts that the number of African American people living with AIDS diagnosis and HIV infection and dead due to HIV/AIDS will be 662.2, 1225.3 and 62.9 in 2015 and 794.9, 1566.5 and 79.2 in 2030, respectively. The number of Caucasian people living with AIDS diagnosis and HIV infection and dead due to HIV/AIDS will be 96.4, 160 and 6.5 in 2015 and 118.6, 206.9 and 8.3 in 2030, respectively. The numbers of deaths due to HIV/AIDS are quite stable over the years in both the races. There is an increasing trend in the number of people living with HIV infection and AIDS diagnosis in Caucasians compared with African Americans. The absolute number of Caucasians living with AIDS diagnosis and HIV infection is quite smaller compared with African Americans. The results reveal discrepancy in HIV infection, AIDS diagnosis and deaths due to HIV/AIDS among the African Americans and the Caucasians races. There is a need for interventions focusing on HIV/AIDS prevention and management, optimum resource allocation and development of antiAIDS campaigns to reduce the infection rate.
TL;DR: The binding potential of four flavanone glycosides such as naringin, hesperidin, poncirin and sakuranin against acetylcholinesterase was analysed by using the method of molecular modeling and docking to determine the activity of the top scored compound.
Abstract: Acetylcholinesterase hydrolyzes the neurotransmitter called acetylcholine and is crucially involved in the regulation of neurotransmission. One of the observable facts in the neurodegenerative disorders like Alzheimer's disease is the decrease in the level of acetylcholine. Available drugs that are used for the treatment of Alzheimer's disease are primarily acetylcholinesterase inhibitors with multiple activities. They maintain the level of acetylcholine in the brain by inhibiting the acetylcholinesterase function. Hence acetylcholinesterase inhibitors can be used as lead compounds for the development of drugs against AD. In the present study, the binding potential of four flavanone glycosides such as naringin, hesperidin, poncirin and sakuranin against acetylcholinesterase was analysed by using the method of molecular modeling and docking. The activity of the top scored compound, naringin was further investigated by enzyme inhibition studies and its inhibitory concentration (IC50) towards acetylcholinesterase was also determined.
TL;DR: The results of previous investigations on extracts of selected marine algae showed that Caulerpa peltata and Padina gymnospora had more promising antiproliferative and antioxidant activities than Gelidiella acerosa and Sargassum wightii, and these extracts were further analyzed for their constituents by using gas chromatography in tandem with mass spectrometry.
Abstract: The results of our previous investigations on extracts of selected marine algae showed that Caulerpa peltata and Padina gymnospora had more promising antiproliferative and antioxidant activities than Gelidiella acerosa and Sargassum wightii. Based on these results, the more active chloroform extract of C. peltata and ethyl acetate extract of P. gymnospora were further analyzed for their constituents by using gas chromatography in tandem with mass spectrometry. The GC-MS analysis (GC % peak area given in parentheses) showed that fucosterol (12.45%) and L-(+)-ascorbic acid 2, 6-dihexadecanoate (8.13%) were the major compounds present in P. gymnospora ethyl acetate extract. On the other hand, C. peltata chloroform extract had 1-heptacosanol (10.52%), hexacosanol acetate (9.28%), tetradecyl ester of chloroacetic acid (7.22%), Z,Z-6, 28-heptatriactontadien-2-one (6.77%) and 10, 13-dimethyl-methyl ester of tetradecanoic acid (5.34%) as major compounds. Also described in the report are the beta-carotene bleaching inhibitory and total reducing activities of the chloroform and ethyl acetate extracts of C. peltata and P. gymnospora, respectively, relative to the other three extracts (aqueous, methanol, chloroform or ethyl acetate) of the two algae.
TL;DR: Synthesised compounds synthesised by cyclisation of corresponding 3-(heteroaryl)-1(2-hydroxyphenyl) prop-2-en-1-one with sodium acetate in alcohol–water exhibited significant in vitro anticancer potential.
Abstract: A few flavanones were synthesised by cyclisation of corresponding 3-(heteroaryl)-1(2-hydroxyphenyl) prop-2-en-1-one with sodium acetate in alcohol-water and evaluated for activity. Synthesised compounds were assayed for their in vitro anticancer activity against three human cancer cell lines, mammary adenocarcinoma (MCF7), human colon adenocarcinoma (HT29) and human kidney adenocarcinoma (A498) using sulforhodamine B dye. Results indicated that most of the compounds exhibited significant in vitro anticancer potential. Among them, compound having furan ring showed most potent activity against all the tested cell lines.
TL;DR: It can be concluded that ozonated oil can be of potential therapeutic use for healing wounds because of its higher tensile strength, collagen content and superoxide dismutase activity than that of vehicle treated wounds.
Abstract: The hypothesis that ozonated oil has wound healing property was investigated in an excision wound model using Sprague Dawley rats. The animals were divided into four groups, which were treated with sesame oil (vehicle), framycetin (standard), or two doses of ozonated sesame oil (peroxide values 500 and 700 mEq/1000 g, respectively). The formulations were topically applied on the excision wounds once daily for 11 consecutive days and the animals were euthanized on the 12(th) day. Wound healing was assessed by measuring the wound contracture, tensile strength, collagen content and superoxide dismutase activity of skin of the excised wound area. On the terminal day, areas of the wounds of the group receiving high dose ozonated oil were significantly smaller than those of the group treated with vehicle. Ozonated oil treated wounds had significantly higher tensile strength, collagen content and superoxide dismutase activity than that of the vehicle treated wounds. Histopathological analysis of skin of the excised wound area treated with ozonated oil revealed better healing activity vis-a-vis vehicle-treated wounds. Thus, it can be concluded that ozonated oil can be of potential therapeutic use for healing wounds.
TL;DR: A simple, precise and specific reversed phase HPLC method for the simultaneous determination of 22 components present in different essential oils namely cinnamon bark oil, caraway oil and cardamom fruit oil was developed and validated and demonstrated to be applicable to the determination of the ingredients in commercial sample of essential oil.
Abstract: The aim of the present study was the development and validation of a simple, precise and specific reversed phase HPLC method for the simultaneous determination of 22 components present in different essential oils namely cinnamon bark oil, caraway oil and cardamom fruit oil. The chromatographic separation of all the components was achieved on Wakosil-II C18 column with mixture of 30 mM ammonium acetate buffer (pH 4.7), methanol and acetonitrile in different ratio as mobile phase in a ternary linear gradient mode. The calibration graphs plotted with five different concentrations of each component were linear with a regression coefficient R(2) >0.999. The limit of detection and limit of quantitation were estimated for all the components. Effect on analytical responses by small and deliberate variation of critical factors was examined by robustness testing with Design of Experiment employing Central Composite Design and established that this method was robust. The method was then validated for linearity, precision, accuracy, specificity and demonstrated to be applicable to the determination of the ingredients in commercial sample of essential oil.
TL;DR: Quality of life, symptoms of patients affected by breast, head and neck, cervical and stomach cancers, and in stomach cancer patients, nausea and vomiting, dysphagia, reflex symptoms and eating restrictions were significantly affected.
Abstract: Over the last decade, quality of life investigations of cancer patients' have became a critical evaluation parameter in the clinical cancer research and treatment evaluation programs. This study was carried out in a 1200 bed tertiary care teaching hospital, MGM Hospital, located at Warangal, India. Present study assessed the overall quality of life, symptoms of patients affected by breast, head and neck, cervical and stomach cancers by using guidelines and modules of The European Organisation for Research and Treatment of Cancer. The assessment was carried out in two phases, as review I at ≤2 cycles and review II at ≥5 cycles of treatment. Data were analyzed for 104 individuals with the mean age of 46.1I�11.2 years. The evaluation was characterised as functional scale and symptom scale. In the functional scale physical, and role functions were significant (P<0.05) in all the 4 types of cancers studied. Additional, future perspective, social and emotional functions were observed to be significant in breast cancer, head and neck cancer and cervical cancer, respectively. Where as in symptom scale pain was observed to be significant for all cancers studied. Individually, breast cancer patient also showed significant parameters like fatigue, arm symptoms, and upset by hair loss. Head and neck cancer patients had insomnia and diarrhoea as additional significant symptom scale parameters. In cervical cancer patients, fatigue, insomnia, menopausal symptoms, and in stomach cancer patients, nausea and vomiting, dysphagia, reflex symptoms and eating restrictions were significantly affected. Most of the findings are similar to past studies in the respective type of cancer patients which shows that, quality of life was mostly influenced by the above mentioned factors and have some interesting implications for management and treatment of cancer.
TL;DR: The results support the claim for the preparation of nanosuspensions with enhanced solubility and bioavailability of nevirapine so as to improve the dissolution rate of neirapine.
Abstract: The objective of this study was to prepare and characterise nevirapine nanosuspensions so as to improve the dissolution rate of nevirapine. Nevirapine is a nonnucleoside reverse transcriptase inhibitor of immunodeficiency virus type-1 and it is poorly water-soluble antiretroviral drug. The low solubility of nevirapine can lead to decreased and variable oral bioavailability. Nanosuspension can overcome the oral bioavailability problem of nevirapine. Nevirapine nanosuspensions were prepared using nanoedge method. The suspensions were stabilised using surfactants Lutrol F 127 or Poloxamer 407 and hydroxypropyl methyl cellulose. The nanosuspension was characterised for particle size, polydispersibility index, crystalline state, particle morphology, in vitro drug release and pharmacokinetics in rats after oral administration. The results support the claim for the preparation of nanosuspensions with enhanced solubility and bioavailability.
TL;DR: The antimicrobial effect of 24 different hydroalcoholic extracts obtained from four parts (leaf+stem (aerial), peel, pulp and seed) of Momordica charantia L. were investigated against five Gram-positive, six Gram-negative and four fungal strains.
Abstract: The antimicrobial effect of 24 different hydroalcoholic extracts (100, 75, 50 and 25% methanol and water) obtained from four parts (leaf+stem (aerial), peel, pulp and seed) of Momordica charantia L. were investigated against five Gram-positive, six Gram-negative and four fungal strains. The extraction was done by individual cold percolation method using hexane, different hydroalcoholic solvent (100, 75, 50 and 25% methanol) and water. The antimicrobial activity was done by agar well diffusion assay. The extracts, which showed >15 mm zone of inhibition, were further screened to determine minimum inhibitory concentration and minimum bactericidal concentration using a broth dilution method performed in 96-well microtitre plate. The extractive yield was highest in aqueous extracts of all the four parts closely followed by 25% methanol. Micrococcus flavus was the most susceptible Gram-positive bacteria and Pseudomonas testosteroni was the most susceptible Gram-negative bacteria. The highest antibacterial activity was shown by 100% methanol. The Gram-negative Pseudomonas spp. was more susceptible towards all the extracts than the Gram-positive bacteria or fungal strains investigated. One hundred percent and 50% methanol extracts of seed showed lowest minimum inhibitory concentration and minimum bactericidal concentration values, that is <39 and 625 μg/ml, respectively, against Pseudomonas pictorum. Therefore, these extracts would be of interest in the control of Pseudomonas spp. in food industry as well as used for therapeutic purposes.
TL;DR: Simulated projections of metabolic syndrome patients predict serious life-threatening cardiovascular consequences in the representative cohort of patients in western India.
Abstract: Long-term cardiovascular complications in metabolic syndrome are a major cause of mortality and morbidity in India and forecasted estimates in this domain of research are scarcely reported in the literature. The aim of present investigation is to estimate the cardiovascular events associated with a representative Indian population of patients suffering from metabolic syndrome using United Kingdom Prospective Diabetes Study risk engine. Patient level data was collated from 567 patients suffering from metabolic syndrome through structured interviews and physician records regarding the input variables, which were entered into the United Kingdom Prospective Diabetes Study risk engine. The patients of metabolic syndrome were selected according to guidelines of National Cholesterol Education Program - Adult Treatment Panel III, modified National Cholesterol Education Program - Adult Treatment Panel III and International Diabetes Federation criteria. A projection for 10 simulated years was run on the engine and output was determined. The data for each patient was processed using the United Kingdom Prospective Diabetes Study risk engine to calculate an estimate of the forecasted value for the cardiovascular complications after a period of 10 years. The absolute risk (95% confidence interval) for coronary heart disease, fatal coronary heart disease, stroke and fatal stroke for 10 years was 3.79 (1.5-3.2), 9.6 (6.8-10.7), 7.91 (6.5-9.9) and 3.57 (2.3-4.5), respectively. The relative risk (95% confidence interval) for coronary heart disease, fatal coronary heart disease, stroke and fatal stroke was 17.8 (12.98-19.99), 7 (6.7-7.2), 5.9 (4.0-6.6) and 4.7 (3.2-5.7), respectively. Simulated projections of metabolic syndrome patients predict serious life-threatening cardiovascular consequences in the representative cohort of patients in western India.
TL;DR: Multivariate analysis reveals that younger patients (≥45 years) were more likely and absence of comorbidities and shorter hospital stay were associated with less likelihood of prescribing multiple antimicrobial drugs, andEstimating antimicrobial drug use by defined daily dose method will remain open to criticism.
Abstract: Widespread overuse and inappropriate use of antimicrobial drugs continues to fuel an increase in antimicrobial resistance and leads to consequent treatment complications and increased healthcare costs. In the present study we aimed to describe antimicrobial drug consumption and predictors and to identify potential targets for antimicrobial stewardship. This was a prospective observational study conducted at adult medicine wards of tertiary care teaching hospital over the period of five months. Antimicrobial drug consumption was measured using days of therapy per 1000 patient days and defined daily dose per 1000 patient days. Additionally, predictors of multiple antimicrobial prescribing were also analyzed. Seven hundred thirty patients were screened and 550 enrolled, receiving 1,512 courses of antimicrobial therapy, mainly intravenously (66%). Most frequently prescribed agents were artesunate (13%), ceftriaxone (11%) and metronidazole (10.5%). Overall consumption was 1,533 days of therapy per 1000 patient days and was mainly attributed to antibiotics (98.3%) for empirical therapy (50%). Median days of antimicrobial drugs prescribing were 3 (inter quartile range 2-5). Most commonly consumed antimicrobials were ceftriaxone (31%, 248.8 g) and artesunate (26%, 29 g). Antimicrobials contributed to 72.5% expense of the total incurred. Multivariate analysis reveals that younger patients (≥45 years) (odds ratio: 1.59, 95% CI 1.14-2.21) were more likely and absence of comorbidities (odds ratio: 0.58, 95% CI 0.42-0.79) and shorter hospital stay (≥6 days)(odds ratio: 0.44, 95% CI 0.32-0.60) were associated with less likelihood of prescribing multiple antimicrobial drugs. Estimating antimicrobial drugs use by defined daily dose method will remain open to criticism because the prescribed dosage is not often in agreement with the "usual" daily dose, which depends on location of and susceptibility of pathogenic organisms and metabolic status of the patient.
TL;DR: Houttuynia cordata Thunb extract exhibited significant hepatoprotective property in carbon tetrachloride-induced hepatotoxicity in mice and showed significant antioxidant actions by scavenging the alkyl and hydroxyl free radicals.
Abstract: Houttuynia cordata Thunb (Saururaceae) is a traditional medicinal herb used to treat several disease symptoms. The present study was focused on the hepatoprotective effects of H. cordata ethyl acetate extract in experimental mice. Further the antioxidant potential of the extract was also evaluated to substantiate its hepatoprotective properties. Carbon tetrachloride-induced hepatic damage in mice was used to measure the serum biochemical parameters. Morphological changes in hepatocyte architecture were studied by haematoxylin and eosin staining. In vitro alkyl and hydroxyl free radical scavenging assays were performed to evaluate the antioxidant effect. Administration of H. cordata extract significantly reduced the elevated serum levels and regulated the altered levels of serum cholesterol in carbon tetrachloride-treated mice (P<0.05). The morphological changes in hepatocyte architecture were also reversed by H. cordata treatment. Further, the extract showed significant antioxidant actions by scavenging the alkyl and hydroxyl free radicals. The concentration of the extract necessary for 50% scavenging of alkyl and hydroxyl radicals was 15.5 and 410 μg/ml, respectively. H. cordata extract exhibited significant hepatoprotective property in carbon tetrachloride-induced hepatotoxicity in mice. The strong antioxidant activities possessed by the extract might be responsible for such actions.
TL;DR: The result of the present study demonstrates Tribulus terrestris has a protective effect against haloperidol-induced catalepsy, which is comparable to the standard drug used for the same purpose.
Abstract: Haloperidol, an antipsychotic drug, leads to the development of a behavioural state called catalepsy, in which the animal is not able to correct an externally imposed posture. In the present study we have attempted to evaluate the anticataleptic effect of Tribulus terrestris on haloperidol-induced catalepsy in albino mice. Mice were allocated to four groups, each group containing six animals. Both, the test drug, Tribulus terrestris and the standard drug trihexyphenidyl were uniformly suspended in 1% gum acacia solution. Catalepsy was induced in mice with haloperidol (1.0 mg/kg, intraperitoneally). The first group received the vehicle (10 ml/kg, orally), the second group received trihexyphenidyl (10 mg/kg, orally) and the remaining two groups received Tribulus terrestris (100, 200 mg/kg, orally). The animals were assessed after single and repeated dose administration for ten days, 30 min prior to haloperidol, using standard bar test. The result of the present study demonstrates Tribulus terrestris has a protective effect against haloperidol-induced catalepsy, which is comparable to the standard drug used for the same purpose. Our study indicates Tribulus terrestris can be used to prevent haloperidol-induced extrapyramidal side effects.
TL;DR: The present study compares the drug safety monitoring systems in the developed countries such as the USA and UK and provides implications for developing a system that can ensure the safety and efficacy of drugs in India.
Abstract: Pharmacovigilance is useful in assuring the safety of medicines and protecting the consumers from their harmful effects. A number of single drugs as well as fixed dose combinations have been banned from manufacturing, marketing and distribution in India. An important issue about the availability of banned drugs over the counter in India is that sufficient adverse drug reactions data about these drugs have not been reported. The most common categories of drugs withdrawn in the last decade were nonsteroidal antiinflammatory drugs (28%), antidiabetics (14.28%), antiobesity (14.28%), antihistamines (14.28%), gastroprokinetic drugs (7.14%), breast cancer and infertility drugs (7.14%), irritable bowel syndrome and constipation drugs (7.14%) and antibiotics (7.14%). Drug withdrawals from market were made mainly due to safety issues involving cardiovascular events (57.14%) and liver damage (14.28%). Majority of drugs have been banned since 3-5 years in other countries but are still available for sale in India. The present study compares the drug safety monitoring systems in the developed countries such as the USA and UK and provides implications for developing a system that can ensure the safety and efficacy of drugs in India. Absence of a gold standard for a drug safety surveillance system, variations in culture and clinical practice across countries makes it difficult for India to completely adopt another country's practices. There should be a multidisciplinary approach towards drug safety that should be implemented throughout the entire duration spanning from drug discovery to usage by consumers.
TL;DR: Its activity was twice that of diclofenac in inhibiting thermal protein denaturation taken as a measure of in vitro antiinflammatory activity; it enhanced the bioavailability of curcumin by more than five folds, and significantly alleviated the symptoms of arthritis in streptococcal cell wall-induced arthritis model as compared to both diccumin.
Abstract: Curcumin-diclofenac conjugate as been synthesized by esterification of phenolic group of curcumin with the acid moiety of diclofenac, and characterized by mass spectrometry, NMR, FTIR, DSC, thermogravimetric analysis and X-ray diffraction analysis. The relative solubility of curcumin-diclofenac conjugate, curcumin and diclofenac; stability of curcumin-diclofenac conjugate in intestinal extract; permeability study of curcumin-diclofenac conjugate using the everted rat intestinal sac method; stability of curcumin-diclofenac conjugate in gastrointestinal fluids and in vitro efficacy have been evaluated. In vivo bioavailability of curcumin-diclofenac conjugate and curcumin in Sprague-Dawley rats, and antiarthritic activity of curcumin-diclofenac conjugate, curcumin and diclofenac in modified streptococcal cell wall-induced arthritis model in Balb/c mice to mimic rheumatoid arthritis in humans have also been studied. In all of the above studies, curcumin-diclofenac conjugate exhibited enhanced stability as compared to curcumin; its activity was twice that of diclofenac in inhibiting thermal protein denaturation taken as a measure of in vitro antiinflammatory activity; it enhanced the bioavailability of curcumin by more than five folds, and significantly (P<0.01) alleviated the symptoms of arthritis in streptococcal cell wall-induced arthritis model as compared to both diclofenac and curcumin.
TL;DR: The fresh and dry herbage and oil yield of the aerial parts showed greater response in H3 i.e. harvesting at 160 days after planting, followed by H2 harvesting time and the quality of essential oil was evaluated using GC and GC-MS analysis.
Abstract: A field experiment on the effect of time of harvesting on yield and quality of Melissa officinalis L. was conducted under the agroclimatic conditions of Doon valley, Uttarakhand in order to assess the performance of four harvesting times (H1-120 days, H2-140 days, H3-160 days and H4-180 days after planting). The fresh and dry herbage and oil yield of the aerial parts showed greater response in H3 i.e. harvesting at 160 days after planting, followed by H2 harvesting time. The quality of essential oil was evaluated using GC and GC-MS analysis. Geranial (24.53 %) and neral (18.80 %) were the major constituents found in the essential oil followed by trans-caryophyllene (7.70 %).
TL;DR: It is demonstrated that antidiarrhoeal plants could control diarrhoea caused by heat-stable toxin-producing enterotoxigenic E. coli through their immunomodulatory effect.
Abstract: Diarrhoeal diseases due to enterotoxigenic Escherichia coli continue to be a cause of global concern. Medicinal plants have been gaining popularity as promising antidiarrhoeal agents. In the present study, four antidiarrhoeal plants, viz. Aegle marmelos, Cyperus rotundus, Psidium guajava and Zingiber officinale were screened against a heat-stable toxin-producing enterotoxigenic E. coli strain. Decoctions of these plants were studied for their effect on intracellular killing of the bacterial strain using murine monocytic cell line, J774. [ 3 H] thymidine release assay was used to evaluate the apoptotic/necrotic effect. All plants at concentrations <1% enhanced intracellular killing of the bacteria by J774 cells. However, at higher concentrations, the decoctions induced apoptosis in J774 cells. The study demonstrates that these plants could control diarrhoea caused by heat-stable toxin-producing enterotoxigenic E. coli through their immunomodulatory effect.
TL;DR: The microcapsules were found to be stable under accelerated stability conditions, which suggest them as better alternative delivery systems for enhanced therapeutic efficacy of antidepressant drug, venlafaxine HCl.
Abstract: The objective of present research work was to design and characterize the venlafaxine HCl-loaded sodium alginate-based mucoadhesive microcapsules by ionic gelation technique using HPMC K100M as mucoadhesive polymer. The Placket-Burman Design was applied for preliminary screening of the formulations and systematic optimization by using Box-Behnken Design. The prepared microcapsules were characterized for drug content, entrapment efficiency, micromeritic properties, particle size, swelling index, mucoadhesive strength, in vitro drug release and in vivo antidepressant activity. FTIR and differential scanning calorimetry studies showed no incompatibility. Surface morphology studies revealed spherical nature of the prepared microcapsules. In vitro drug release studies revealed sustained release by diffusion mechanism. Further, the microcapsules were effective in reducing the depression induced by forced swimming test in Sprague-Dawley rats compared to the pure drug. The microcapsules were found to be stable under accelerated stability conditions, which suggest them as better alternative delivery systems for enhanced therapeutic efficacy of antidepressant drug, venlafaxine HCl.