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Journal of Pharmaceutical Negative Results
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   2012| January-December  | Volume 3 | Issue 1  
    Online since August 11, 2012

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Insignificant anti-acne activity of Azadirachta indica leaves and bark
Pratibha Nand, Sushma Drabu, Rajinder K Gupta
January-December 2012, 3(1):29-33
Background and Aim: Azadirachta indica has a long history of medicinal usage in skin ailments due to its antibacterial and anti-inflammatory properties. The present study was undertaken to explore the potential of the leaves and bark of Azadirachta indica in the treatment of acne. Materials and Methods: Monographic analysis of the plant was carried out, followed by the phytochemical screening of the sequential extracts of leaves and bark of Azadirachta indica. The results indicated presence of alkaloids, flavonoids, saponins, terpenes, and tannins. Gas chromatography-mass spectrometry (GC/MS) analysis of the test extracts indicated the presence of many phytoconstituents in dichloromethane and methanolic extracts namely stigmasterol, nimbiol, sugiol, 4-cymene, α-terpinene terpinen-4-ol, and vitamin E. The test extracts were evaluated against acne causing bacteria, namely Staphylococcus aureus (MTCC 96), Staphylococcus epidermidis (MTCC 2639), and Propionibacterium acnes (MTCC *1951), for their in vitro antimicrobial activity, using agar disc diffusion method. Results: Dichloromethane and methanolic extracts of Azadirachta indica showed very little activity against S. aureus and S. epidermidis, but did not show any antimicrobial activity against P. acnes. Conclusion: Despite possessing antibacterial properties, Azadirachta indica showed insignificant effect against acne causing bacteria.
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Negative effect of Alocasia macrorrhizos on the lipid profile in hyperlipidemic rats
Ramya , SD Ullal, R Maskeri, MS Pradeepti, Habeeba Umma, S Rajeshwari
January-December 2012, 3(1):9-12
Introduction: Currently, there is considerable interest in the development of lipid-lowering agents from natural products. The purpose of this study was to evaluate the hypolipidemic activity of hydroalcoholic extract of leaves of Alocasia macrorrhizos (AM), which is known to have anti-oxidant activity. Materials and Methods: Cholesterol-rich high-fat-diet was used to induce hyperlipidemia. Rats were randomly assigned to five groups of six rats each. Groups 1 and 2 served as normal and high-fat-diet-fed control, respectively. Group 3 received the standard drug, atorvastatin, while groups 4 and 5 received AM 250 and 500 mg/kg, respectively. High-fat-diet was fed for 45 days and treatment/vehicle was administered during the latter 30 days, following which blood samples of anaesthetized rats obtained by cardiac puncture were sent for lipid profile. Results: High-fat-diet significantly increased (P < 0.05) all the parameters of lipid profile compared to group 1. Atorvastatin treatment significantly reduced total cholesterol (TC), LDL-C, VLDL-C (P < 0.001), and triglyceride (P < 0.05), however, there was no significant change in HDL-C compared to group 2. AM at both the doses significantly reduced triglyceride and VLDL-C levels compared not only to group 2, but also to group 3 (P < 0.05). There was no change in TC and HDL-C levels, however, there was a significant dose related rise in the LDL-C level in the AM-treated groups compared to group 2 (P < 0.05 at 250 mg/kg, P < 0.001 at 500 mg/kg). Conclusion: The hydroalcoholic extract of leaves of Alocasia macrorrhizos at the dose of 250 and 500 mg/kg in rats significantly reduced triglyceride and VLDL-C levels; however, it increased LDL-C. Hence, it may not be suitable as a lipid-lowering agent.
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Absence of antimicrobial activity of Euphorbia milii molluscicidal latex
Eduardo C Oliveira-Filho, Bianca F. G. Z. Alves, Jacyara C Lopes, Valdi L Tutunji
January-December 2012, 3(1):13-15
Introduction : Euphorbia milii latex has been used as herbal medicine and proved to be a potent plant molluscicide. Materials and Methods : The susceptibility of Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa to E. milii molluscicidal latex was evaluated by assays in the agar well diffusion method and tubes dilution, to determine the minimal inhibitory concentration and minimal bactericidal concentration. Results : Latex in natura (fresh) and lyophilized in a maximum viable concentration of 100 mg/L did not show any inhibitory effect on the growth of the bacterial strains tested. Conclusion : Although it has been effective as a molluscicide, this latex presented a total absence of antimicrobial activity in the two forms and concentrations tested.
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Unsuitability of pharmacopoeial dissolution conditions for entacapone: Effects of various dissolution parameters on dissolution profile
SK Pallewar, TA Premchandani, AM Pethe
January-December 2012, 3(1):49-53
Purpose: Entacapone, a catechol-O-methyltransferase inhibitor, is poorly water soluble (BCS class IV). The dissolution profile of pure Entacapone is improved in the presence of an alkaline buffer and after addition of a surfactant by facilitating the drug release process at the solid/liquid interface. Rationale: According to USP the best dissolution medium for Entacapone is phosphate buffer 5.8 in type II paddle-type apparatus with a paddle speed of 50 rpm. Materials and Methods: In this article an effect of various parameters (buffer, surfactant, and RPM) on the dissolution profile of Entacapone is studied by applying factorial design 33 (phosphate buffer- 5.3, 5.8, and 6.8; sodium lauryl sulfate- 0.5%, 1.0%, and 1.5%; rotation speed of paddle- 50, 75, and 100). Pure Entacapone pellets were formed using a hydraulic press. Conclusion: The release profile data revealed that the dissolution profile of Entacapone is remarkably improved in the alkaline medium (6.8), addition of surfactant does not affect the release profile, whereas increasing RPM of the paddle reduces the dissolution profile; hence it can be stated that Entacapone dissolution is pH dependent, showing maximum dissolution and pH 6.8 which is contradictory to the conditions specified in USP 2010.
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Mobile phone short messaging service for optimizing asthma treatment has no healthcare related effects: A controlled trial
Claus Møldrup, J Stein, B Søndergaard
January-December 2012, 3(1):1-8
Context: One important aspect of modern asthma care is self-management: Allowing the patients to monitor their disease severity continuously and to adjust the dose of inhaled corticosteroid based on the symptoms, lung function, and the use of rescue medication. The Short Messaging Service (SMS) is a convenient, reliable, affordable, and secure means of telemedicine that may improve asthma control. Aim: The objective of this study is to assess the health-related effects of an SMS compliance and monitoring system for optimized asthma treatment. Settings and Design: In total, 244 asthmatics participated in a prospective controlled randomized trial (114 interventions, 130 controls). Materials and Methods: The intervention consisted of sequences of SMS messages sent to the intervention group, each containing two or three monitoring questions and one reminder to take the preventive medication. Both the intervention and control groups received questionnaires on days 0, 45, and 90. The primary outcome measures were a self-assessed outcome questionnaire that included a five question asthma control test, EQ-5D, use of health services, and questions on the use of preventive medicine. Statistical Analysis Used: The Pearson Chi-Square test was used for categorical variables (or Fisher's Exact Test, if the expected count was less than five in one or more cells) and the two-sample t-test or Wilcoxon Rank Sum test was used for continuous variables, as appropriate. The distributional assumption was investigated using histograms and P-P plots. Results: The use of SMS monitoring yielded no health-related effects, no decrease in the use of healthcare services, and no change in the use of medicine between the control and intervention groups. The lack of outcomes for the intervention was neither due to recruitment or the randomizing of participants nor due to dropouts. This study furthermore supports other findings concerning the lack of asthma control in the asthma population. Conclusion: Short Messaging Service is a reliable, convenient, affordable, secure, widespread, and a feasible technology for communication between the patient and healthcare system. However, even given the poor level of asthma control determined at the baseline, this study clearly documents that an SMS compliance and monitoring intervention design, like the one presented in this article, does not improve asthma control, nor does it generate fewer contacts with the healthcare system or improve the use of medicines.
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Lack of anti-obesity effect of Mimosa pudica seed mucilage on mice fed on a high-fat diet
Neerja Rani, Surendra Kumar Sharma, Neeru Vasudeva
January-December 2012, 3(1):38-40
Objective: To investigate the anti-obesity potential of the mucilage of the Mimosa pudica Linn. seed on mice fed on a high-fat diet. Materials and Methods: Two in vivo, that is, lipid emulsion and high-fat diet models were used to investigate the anti-obesity effect in male Swiss albino mice. In the high-fat diet model, the mice were fed a high-fat diet, containing 60% fat, with or without mucilage, for six weeks. The time course of body weight, food intake, organ and fat pad weight (liver and parametrial fat), and serum parameters (triglyceride, total cholesterol, etc.) were measured. In the other model, lipid emulsion with or without mucilage was administered orally, and the plasma triacylglycerol level was measured at 0 to 5 hours. Results: No significant reduction in body weight, organ or fat pad weight (liver and parametrial fat) or serum parameters (triglyceride, total cholesterol) after treatment with mucilage in high-fat diet fed mice was observed. Furthermore the mucilage did not inhibit the elevation of the plasma triacylglycerol level at five hours after the oral administration of lipid emulsion. Conclusion: The present study indicated that the mucilage of the Mimosa pudica seed did not reveal significant anti-obesity action in high-fat diet fed mice.
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Absence of hypolipidemic effect of Holoptelea integrifolia leaf extract in tyloxapol-induced hyperlipidemic rats
S Baroda, N Chaturvedi, P Kumar, MD Gupta, SN Gaidhani, MM Wanjari
January-December 2012, 3(1):16-21
Objective: The leaves of Holoptelea integrifolia are used in the treatment of diabetes and lipid disorders. The present study demonstrates the influence of the aqueous extract of leaves of Holoptelea integrifolia (HIAE) on the lipid profile in normal and Tyloxapol-induced hyperlipidemic rats. Materials and Methods: The vehicle, the aqueous extract of leaves of Holoptelea integrifolia (250 and 500 mg / kg), and fenofibrate, reference standard (65 mg / kg), were administered orally for seven days to different groups of normal and Tyloxapol-induced hyperlipidemic rats. The lipid profile was assessed on the eighth day by estimating the plasma levels of total cholesterol, triglycerides, HDL-c, LDL-c, VLDL-c, and the corresponding atherogenic index and the LDL-c/HDL-c ratio. Results: Administration of the HIAE neither caused any significant effect on the lipid profile in normolipidemic rats nor attenuated tyloxapol-induced hyperlipidemia. Conclusion: The present investigations revealed that the aqueous extract of the leaves of Holoptelea integrifolia did not exhibit a hypolipidemic effect and did not substantiate its traditional use in lipid disorders and obesity.
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Insignificant antimicrobial activities and phytochemical screening in different extracts of indian Ginseng
Premlata Singariya, Padma Kumar, Krishan Kumar Mourya
January-December 2012, 3(1):41-45
Aim: The aim of present study is to investigate the antimicrobial activity of (Flower, Ripen fruit and calyx) of Withania somnifera (RUBL20668) extracts, in order to use them as a possible source of new antimicrobial substances against important human pathogens. Materials and Methods: Crude extracts of different parts of both species of W. somnifera were evaluated against some important bacteria (two Gram +ve and four Gram-ve bacteria). Staphylococcus aureus (Gram +ve), Bacillus Subtilis (Gram +ve), Escherichia coli (Gram-ve), Raoultella planticola (Gram-ve), Pseudomonas aeruginosa (Gram-ve), Enterobactor aerogens (Gram-ve), one yeast Candida albicans and one fungus Aspergillus flavus. The dried and powdered seeds were successively extracted with hexane, toluene, iso propyl alcohol, acetone and ethanol, using the soxhlet assembly. The antimicrobial activity assay was done by both disc diffusion and serial dilution methods. Result: The results indicate that all the extracts in different polar solvents did not show any antibacterial activity against S. aureus, E. coli, R. planticola or E. aerogens or any antifungal activity against A. flavus. Conclusion: All extracts in the different polar solvents did not have or had very less antibacterial and antifungal activities.
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Lack of analgesic property in xanthium strumarium Linn. Fruit's butanolic extracts
Deepak Jain, Shashi Bharti Shukla, Sofiya Verma
January-December 2012, 3(1):22-25
Objective: The objective of the present study is to investigate the analgesic activity profile of xanthium strumarium Linn. (Family: Asteraceae) in mice and rats, using various models. Materials and Methods: The effects of the butanolic extract were observed in three different dose levels 50, 100, and 150 mg / kg, as the extract did not show any sign of toxicity up to 500 mg / kg (p.o.) dose. The investigation was carried out for assessing the activity on thermal and chemical-induced pain reactions. Result: The Xanthium strumarium (XS) fruit's butanolic extract did not have any significant effect on the thermal pain reaction (hot plate method). The extract was devoid of any protective effect against acetic acid-induced writhing, at any of the tested doses. Conclusion: The Xanthium strumarium Fruits' butanolic extract lacked analgesic activity.
  3,290 446 -
Negative effect of noscapine on human serum albumin glycation
Alireza Ahmadzadeh
January-December 2012, 3(1):34-37
Introduction: Glycation, one of the post-translational modifications of proteins, is a nonenzymatic reaction initiated by the primary addition of sugar to the amino groups of proteins. In the early stage of glycation, the synthesis of intermediates leads to the formation of Amadori compounds. In the late stage, advanced glycation end products (AGE) are irreversibly formed after a complex cascade of reactions. It has recently become clear that glycation also affects diabetes-related complications and Alzheimer's disease. The main aim of this investigation is to provide direct evidence for the effects of Noscapine on HSA glycation. Materials and Methods: In this study human serum albumin (HSA) (10 mg / ml) was incubated in phosphate buffered saline (PBS) (50 mM) with Glucose (40 mM) and different concentrations of Noscapine (25, 100, 250, 500 μM), for 42 days, at 37°C, as also HSA was incubated alone (control or H), with Glucose (40mM) (glycated or H + G), respectively, under the same conditions. After incubation the samples were prepared for circular dichroism (CD) and Fluorescencetechniques. Statistical Analysis Used: The results were expressed as mean ± SEM and chi square test was significant at P < 0.05. Results: In glycated sample CD and Fluorescence showed more change relative to the control sample, but in the presence of different Noscapine concentrations and Glucose there were no significant changes relative to the glycated sample. Conclusions: Thus, this study suggests that Noscapine is not responsible for the antiglycation effect.
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Lack of diuretic activity of hot water extract of whole plant of Amaranthus viridis L. in rats
WD Ratnasooriya, M Obeysekera, J. R. A. C. Jayakody, C. D. T. Ratnasooriya, KR Weerasekera
January-December 2012, 3(1):26-28
Objective: To assess the diuretic potential of hot water extract (HWE) of a whole plant of Amaranthus viridis L. Materials and Methods: Different doses (25, 50, and 100 mg / kg) of HWE of the whole plant of A. viridis or vehicle or furosemide, reference drug, was orally administered to hydrated rats (n = six / group) and their cumulative urine output was monitored at hourly intervals for five hours. Result: The HWE of A.viridis does not possess significant (P > 0.05) diuretic activity. Conclusion : The HWE of the whole plant of A. viridis did not possess diuretic activity in rats, as was claimed in traditional and folkloric medicine.
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No evidence of antiprotozoal property of asteracid weeds Sphaeranthus indicus Linn
Namrata V Nemade, Manojkumar Z Chopda, Raghunath T Mahajan
January-December 2012, 3(1):46-48
Introduction: Sphaeranthus indicus Linn, an asteracid weed, has been studied by various researchers. The flower of S. indicus possesses biological activities like Nematicidal, Larvicidal, Piscicidal and others, for example, agricultural. Objective: The present investigation for the antiprotozoal activitiy of a methanolic extract (MeOHx) and the alkaloidal fraction (SAF) of the flowers of Sphaeranthus indicus Linn. has been undertaken. Materials and Methods: The study was carried out in seven groups of the Paramecium sp. by using the hemocytometer technique. Different concentrations of MeOHx (50 and 100 μg / ml) and SAF (20 and 40 μg / ml) were applied. The percent mortality was calculated and the results were expressed by using the probit analysis. Results: There was no significant activity against the tested protozoa. Conclusion: Thus, the results of the present investigation suggest that MeOHx and SAF are not responsible for the antiprotozoal property of S. indicus.
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Review of the pharmaceutical treatment outcome in cases of complicated systemic lupus erythematosus with aplastic anemia
Reza Karbasi-Afshar, Noushin Bayat, Amin Saburi
January-December 2012, 3(1):54-55
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