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Journal of Pharmaceutical Negative Results
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   2014| January-December  | Volume 5 | Issue 1  
    Online since July 16, 2014

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Absence of anthelmintic activity of hydroalcoholic leaf extracts of Artabotrys hexapetalus (Linn.f)
M Vasundhara, YP Karthik, KR Anjali, C Chithra, Priyanka Gupta, C Roopa
January-December 2014, 5(1):1-3
Objective: To study the anthelmintic activity of Artabotrys hexapetalus (Linn.f) leaves. Materials and Methods: The extraction was made using the hydroalcohol with soxhlet extraction system. The hydroalcoholic extract of varying concentration was used for conducting anthelmintic activity (12.5, 25, 50 and 100 mg/ml). Eudrilus eugeniae (African adult earthworm) was used as the test organism. Result: The time of paralysis and death of the earthworms, the positive control (albendazole) was more effective and no effect was shown by the hydroalcoholic extract of varying concentrations. Conclusion: Hydroalcoholic extract of Artabotrys hexapetalus, didn't show any anthelmintic activity at the concentration of 12.5, 25, 50 and 100 mg/ml.
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Absence of anxiolytic activity of Sarcocephalus latifolius fruit extract
David Arome, Chinedu Enegide, Solomon Fidelis Ameh, Amarachi Agbafor, Esenju Rose Mbonne, Itinegbedia Monica
January-December 2014, 5(1):4-7
Introduction: The use of pharmacological agents in the treatment of anxiety disorders have fallen out of favor as their unwanted side-effects have become evident. These presenting challenges call for an inward look into harnessing the full potential of medicinal plants that abound around us. Aim: This study aimed at evaluating the anxiolytic activity of ethanolic fruit extract of Sarcocephalus latifolius in mice. Materials and Methods: The prepared extract at 200, 400, and 600 mg/kg as well as 2.5 mg/kg of diazepam reference standard was administered orally. Anxiolytic activity of the extract was explored using elevated plus-maze and open-field models. Result: In the elevated plus-maze, the extract possessed insignificant (P > 0.05) anxiolytic effect by decreasing the time spent in open arms and entries into the open arms. However, the time spent in the closed arms increased significantly in the extract treated groups compared to the reference standard. In the open-field model, no significant (P > 0.05) locomotor activity was observed in the extract groups. The number of locomotion was less in the extract groups compared the reference standard having the highest locomotive activity. Furthermore, there were reduction in the number of rearing at extract doses of 400 and 600 mg/kg compared with the normal saline and reference standard. Conclusion: The results of this study showed that the ethanolic fruit extract of S. latifolius lack anxiolytic activity.
  5,039 2,409 2
Unsatisfied processing conditions in making ifosfamide nanostructured lipid carriers: Effects of various formulation parameters on particle size, entrapment efficiency, and drug loading capacity
Ramaiyan Velmurugan, Subramanian Selvamuthukumar
January-December 2014, 5(1):8-12
Introduction: The objectives of the present investigation were to develop an optimized formulation of ifosfamide (IF) nanostructured lipid carrier (NLC) to sustain the release, to overcome the instability of the drug in an acidic environment during oral administration, drug leakage during storage, drug expulsion, and low drug loading (DL). Materials and Methods: The IF NLC was prepared by solvent diffusion technique. Response surface methodology was applied to optimize the formulation. Drug/lipid ratio, organic/aqueous phase ratio, and concentration of surfactant were considered as the formulation variables that mainly affects the particle size (PS), entrapment efficiency (EE) and DL of the NLC. A total of 20 sets of formulations were performed with different ratios of drug/lipid, organic/aqueous phase volume and various concentration of the surfactant. The formulation was evaluated for PS, EE, and DL, differential scanning calorimetry, Fourier transform infrared and in vitro dissolution. Results: Increasing the aqueous phase volume results in an increase of EE and a decrease in loading capacity. PS also decreases to extent. Increasing the lipid concentration, EE increases and as well the PS. An increase in the concentration of the surfactant resulted in a decrease in PS and a slight increase in encapsulation efficiency and loading capacity. Conclusion: The positive impact on the response variables (PS, EE and DL capacity) of the formulation of IF NLC would be obtained only if the processing conditions could be followed.
  4,528 1,258 1
Inefficiency of ethanolic extract of Glycyrrhiza glabra and Ziziphus mauritiana roots on androgenic alopecia
Sukirti Upadhyay, AK Ghosh, Vijender Singh
January-December 2014, 5(1):25-28
Aim: To study the air growth promoting effect of roots of G. glabra and Z. mauritiana in androgen (testosterone) induced male pattern baldness (androgenic alopecia). Materials and Methods: Animals were divided into four groups and they were attempted to made alopecic by treatment with testosterone for 3 weeks. Group 1 (control), 2 (standard), 3 and 4 animals (test) were also treated topically with vehicle, finasteride and ethanolic extract of Z. mauritiana roots and G. glabra roots respectively. Animals were observed for signs of alopecia and after treatment period one animal from each group was euthanized randomly and the skin sections from the treated area was examined for changes in follicular morphology. Statistical Analysis: Statistical analysis of data was carried out by one-way ANOVA. Using Instat version 2.1 software. Results: The Group 1, 3 and 4 animals develop alopecia and their skin section also shows bulbous and miniaturized hair follicles and prominent sebaceous gland while Group 2 (standard antiandrogenic drug finasteride treated) animals does not develop alopecia and skin samples also shows well-formed follicles and normal sebaceous gland. Conclusion: This experiments shows incapability of ethanolic extract of Z. mauritiana and G. glabra combating androgenic alopecia.
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Long-term ethanol diet (based on waste powder as vehicle) does not cause liver injury in C57BL/6 and A/J mice
Lorena Bavia
January-December 2014, 5(1):39-44
Background: Alcohol abuse is increasing worldwide in the human population and causes severe damage such as steatosis, hepatitis, and cirrhosis. Alcoholic individuals recurrently are more susceptible to infectious diseases since alcohol metabolites affect the innate and acquired immune responses. Hence, there is a need for animal models to study alcohol-induced pathologies. Materials and Methods: In order to establish an alternative and cheaper protocol to perform mice alcohol feeding, powder from regular chow CR-1 was mixture with water and agar generating a semi-solid vehicle-diet in which ethanol was added. As pair-fed control glucose was equicalorically added to the semi-solid vehicle-diet. Results: Four weeks later, both ethanol and glucose diets did not cause hematological, physiological and pathological changes in C57BL/6 and A/J mice. Conclusions: Our results contributed to development of a new chow approach as vehicle-diet for substances soluble in ethanol or water. In addition, our results propose an alternative to powder chow destination.
  4,143 268 1
Lack of in vitro anticancer and antimicrobial activities in Suaeda maritima (seablite) crude extracts
Yuttana Sudjaroen
January-December 2014, 5(1):45-49
Aims: The aim was to determine antimicrobial and anticancer activities for water and ethanol extracts of leaves and shooting parts of seablite. Materials and Methods: Anticancer activity tests of seablite extracts were performed by resazurin microplate assay (REMA) and tested with 3 cell lines including KB cell line, epidermoid carcinoma of the oral cavity (American Type Culture Collection [ATCC] CCL-17), MCF-7 cell line, breast adenocarcinoma (ATCC HTB-22) and NCI-H187 cell line, and small cell lung carcinoma (ATCC CRL-5804). Antimicrobial activities of seablite water and ethanol extracts against herpes simplex virus type-I (HSV-1) and Mycobacterium tuberculosis H 37 Ra strain were tested according by green fluorescent protein-based assay; Candida albicans (ATCC 90028) and Bacillus cereus (ATCC 11778 or TISTR 687) were tested according by REMA; and Plasmodium falciparum, K1 strain was tested according by micro-culture radioisotope techniques. Results: Both extracts were not possessed anticancer activity to KB-oral cavity cancer, MCF7-breast cancer and NCI-H187-small lung cancer cell lines at maximum concentration = 50 μg/mL. In the same way to anticancer activity assays, both extracts were not inhibited HSV-1, P. falciparum K1 strain, M. tuberculosis H 37 Ra strain and B. cereus at the same concentration. Conclusions: Ethanol and water extracts of leaves and shooting parts of seablite had no significant anticancer and antimicrobial activities.
  3,927 392 1
Insignificant antidermatophytic activity of Brassica campestris oil
Neetu Jain, Meenakshi Sharma
January-December 2014, 5(1):22-24
Introduction: The aim of the present study was to investigate the antidermatophytic activity of Brassica campestris oil against selected dermatophytes through a disc diffusion technique. Materials and Methods : Four concentrations of mustard oil, 100%, 75%, 50%, and 25%, were screened against Trichophyton rubrum, Trichophyton simii, Chrysosporium indicum, and Chrysosporium tropicum through the disc diffusion technique. Results : The result showed that 25% and 50% concentrations of oil did not show any zone of inhibition. 75% and 100% concentration showed very poor activity against T. rubrum, T. simii, and C. indicum but in the case of C.tropicum, no zone of inhibition was observed . Conclusion: The mustard oil does not exhibited significant antidermatophytic activity in the disc diffusion method.
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Lack of hypoglycemic activity in total flavonoid fraction of Wrightia tinctoria on alloxan induced hyperglycemia
AK Shukla, Papiya Bigoniya
January-December 2014, 5(1):34-38
Objective: The objective of this study was to investigate the hypoglycemic activity of Wrightia tinctoria (Roxb) (R. Br. Linn., Family- Apocynaceae) total flavonoid (WTTF) fraction on alloxan induced hyperglycemia. Materials and Methods: Total flavonoid fraction from WTTF seed was separated and LD 50 calculated as 1006.93 mg/kg, i.p., following Organization for Economic Co-operation and Development guideline 423. The effect of total flavonoid fraction was observed in three different dose levels 50, 75, and 100 mg/kg. Hypoglycemic activity was carried out using alloxan induced hyperglycemia model. The parameters observed were body weight, blood glucose, total cholesterol, triglycerides (TG), low density lipoprotein, high density lipoprotein, urea and creatinine along with relative organ weight of liver, kidney, and pancreas. Results: Total flavonoid fraction of W. tinctoria did not have any significant effect on reducing glucose level. WTTF had significantly reduced creatinine (P < 0.001), TG (P < 0.05) level and relative weight of liver in diabetic rat at the dose of 100 mg/kg. Conclusion: All the findings indicate absence of antidiabetic activity in W. tinctoria seed but possible presence of liver and kidney protective property.
  3,742 254 -
Lack of alpha amylase inhibitory activity of monoammonium glycyrrhizinate
Harish Chandra Rodda, Ramya Bubuk, Fathima Kaneez-e-Kubra
January-December 2014, 5(1):13-14
Introduction: Monoammonium glycyrrhizinate (MAG) is used as a sweetener and also as a flavoring agent to enhance the flavor of dairy products, confectioneries, baked foods and beverages. It is used in cough drops, cough syrups and cosmetics. It is reported to have antioxidant, antitussive and antiviral activities. Materials and Methods: The in-vitro α - amylase inhibitory activity was performed using 3,5-dinitrosalicylic acid assay. Different concentrations (1 μg/ml, 3 μg/ml, 5 μg/ml, 10 μg/ml, 30 μg/ml and 50 μg/ml) of MAG were analyzed for the α - amylase inhibitory potential. Results: The results of this study revealed that MAG lacks α - amylase inhibitory potential. Conclusion: Documentation of pharmacological activities of phytochemicals, which have either positive or negative outcome, is required to create a database for phytopharmacological research. The result of this study can serve as one of the components of phytochemical research database.
  3,610 305 -
Incidence of new onset of type-2 diabetes with the use of atenolol for treatment of hypertension in north indian population: No role of irs-1 and kir 6.2 Gene polymorphism
Sudeep Bhardwaj, Praveen P Balgir, Rajesh K Goel
January-December 2014, 5(1):50-55
Introduction: Previous research has suggested that β1 adreno-receptor blockers commonly used for management of hypertension may promote new onset of type-2 diabetes mellitus. The objective of this study is to evaluate the role of insulin receptor substrate-1 (IRS-1) gene and pancreatic ATP-sensitive potassium inward rectifying channel (Kir 6.2) genetic polymorphism in induction of diabetes mellitus with chronic use of β1 blocker. Materials and Methods: A total of 150 patients with essential hypertension aged between 17 and 65 years who were diagnosed with essential hypertension and prescribed atenolol therapy, were recruited. Of these, only 100 patients responding to atenolol were followed-up for 12 months for monitoring blood glucose level every month. The IRS-1 and pancreatic ATP-sensitive potassium channel Kir 6.2 (E23K) gene polymorphism were genotyped using genomic DNA extracted from the whole blood of the recruited patients by polymerase chain reaction and restriction fragment length polymorphism. Results: This study revealed that among the 100 patients responding to atenolol 27% showed a significant increase in the fasting blood sugar. Genotyping study of the recruited patients revealed a difference in allelic frequencies for IRS-1 (Gly972Arg) and pancreatic ATP-sensitive potassium channel Kir 6.2 (E23K) variants. However, allelic distribution between the hypertensive patients on atenolol showing hyperglycemia and normoglycemia was not significantly different for these genes. Conclusion: Thus, showing no correlation, for incidence of diabetes post atenolol therapy in the studied population with these gene polymorphisms.
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No impact of neuropathy on pharmacokinetic of lamotrigine in rat model
Prameela Rani Avula, Hema Veesam
January-December 2014, 5(1):15-18
Purpose: The aim of the present research is to monitor any alteration in the serum concentrations of lamotrigine (LMT) in peripheral neuropathic conditions compared with normal conditions in a rat model. Materials and Methods: LMT concentrations were established at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 h post dose by high performance liquid chromatography-ultraviolet. After per oral administration of 10 mg/kg drug, pharmacokinetic parameters were determined from plasma drug concentration. Later pharmacokinetic parameters of neuropathic pain induced rats were calculated in order to estimate the possible effect of neuropathic pain on pharmacokinetic parameters. Results: The regression coefficient determined for LMT calibration curve was 0.99 ± 0.001. The working range for LMT was 0.5 to 2.5 μg/ml Limit of Detection (LOD 0.2 μg/ml). The maximum drug concentration was found at 2 h. Conclusion: However, none of the pharmacokinetic parameter showed statistically significant alteration where the results were quite stimulating for the development of clinically useful oxcarbazepine dosage form to explore its activity on neuropathic pain.
  3,594 299 2
Insignificant influence of test order on cognitive behavior in Wistar rats
Yow Hui-Yin, Nurulumi Ahmad, Norazrina Azmi, Mohd Makmor-Bakry
January-December 2014, 5(1):29-33
Objectives: The aim was to evaluate the effects of test order in behavioral performance of Wistar rats in cognitive performance tasks. Materials and Methods: The rats were tested with both object recognition and object location tasks in different test orders with an inter-test interval of 1-day. Results: An open field box sized 60 × 60 × 40 cm was associated with better experimental outcome compared with box sized 100 × 100 × 50 cm. Test order has insignificant effects on the exploration activity of rats with the 1-day inter-test interval. Conclusion: Test order of the cognitive performance tasks with inter-test interval of 1-day did not influence the performance of Wistar rats.
  3,502 296 1
Lack of diuretic activity of water extract of leaves of Pongamia pinnata L. in rats
SA Deraniyagala, WD Ratnasooriya, S Priyadharshini, TRK Perera
January-December 2014, 5(1):19-21
Objective : To assess the diuretic potential of water extract (WE) of leaves of Pongamia pinnata L. Materials and Methods : Different doses (500, 1000, 1500, and 3000 mg/kg) of WE of the leaves of P. pinnata or vehicle or furosemide, reference drug was orally administered to hydrated rats (n = 6/group) and their cumulative urine output was monitored at hourly intervals for 6 h. Result : The WE of P. pinnata does not possess significant (P > 0.05) diuretic activity. Conclusion : The WE of the leaves of P. pinnata did not possess diuretic activity in rats as was claimed in traditional and folkloric medicine.
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