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Journal of Pharmaceutical Negative Results
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   Table of Contents - Current issue
January-December 2018
Volume 9 | Issue 1
Page Nos. 1-60

Online since Tuesday, August 21, 2018

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Comparison of spectrophotometric methods of total flavonoid assay based on complex formation with aluminum chloride as applied to multicomponent herbal drug angionorm Highly accessed article p. 1
Petr Struchkov, Vladimir Beloborodov, Vladimir Kolkhir, Inna Voskoboynikova, Alexey Savvateev
Objective: The objective was to compare the complex formation of flavones (luteolin, apigenin), flavonols (morin, quercetin, and rutin), flavanones (naringenin), flavanonols (dihydroquercetin), caffeic, and ferulic acids with aluminum ion using two spectrophotometric methods and the application of these methods to estimate the flavonoid content in the angionorm herbal product. Materials and Methods: Method 1 included direct complex formation with aluminum chloride, and Method 2 involved preliminary nitrozation and subsequent complex formation of nitroso-derivatives with aluminum chloride. 2,4-dinitrophenylhydrazine method was also tested. Results: The conjugation system increase in the chromophore structure of nitroso derivatives is reflected by the hyperchromic effect of all substances (from 1.4 to 4-fold). The largest bathochromic shift of nitroso derivatives was seen for rutin, luteolin, and dihydroquercetin (to 510–530 nm). The total flavonoids estimation in the extract of the four herbs mixture, which constitute angionorm preparation active ingredient, depends on the chosen reference substance (3.49% calculated as luteolin when measured by Method 1 or 8.71% by Method 2; 7.97% calculated as dihydroquercetin when measured by Method 1 and 4.14% by Method 2. Conclusion: The complex formation according to Methods 1 and 2 does not allow the identification of the selective spectral regions typical for the certain flavonoids subgroups and hydroxycinnamic acids. Neither method of complex formation is suitable for the assay of total flavonoids in unknown samples or for the flavonoid content comparison in the different herbal material.
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Matrix tablet-containing solid dispersion is not suitable for sustained release delivery of beclomethasone dipropionate p. 8
GS Ravi, C Sathwik Krishna, R Narayana Charyulu, Akhilesh Dubey, Srinivas Hebbar
Objective: In the present study, an attempt was made to enhance the solubility of beclomethasone dipropionate by solid dispersion method followed by formulating and evaluating the sustained release matrix tablets-containing solid dispersion of beclomethasone dipropionate to overcome its lacuna of short elimination half-life. Materials and Methods: Solid dispersion was prepared by using β-cyclodextrin and polyethylene glycol 6000 as a carrier by physical mixture, solvent evaporation, and kneading methods and evaluated for percentage yield, drug content, and in vitro dissolution studies. The selected formulation of solid dispersion was subjected for preparation of sustained release tablets by direct compression method using matrix polymers hydroxypropyl methyl cellulose (HPMC) K 15 and guar gum and evaluated for thickness, weight variation, hardness, friability, drug content, and in vitro drug release studies. Results: The Fourier-transform infrared spectroscopy study revealed no interaction between the drug and polymers. The powder possessed good flow properties before the compression. The results of in vitro dissolution studies were not satisfactory to achieve sustained release of the drug from the formulation. Conclusion: The aim was to formulate sustained release matrix tablets of beclomethasone dipropionate which was not achieved, hence it was concluded that the matrix tablets prepared using HPMC K 15 and guar gum-containing solid dispersion of beclomethasone dipropionate is not a suitable approach for the sustained release delivery of beclomethasone dipropionate.
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Tetrandrine beads using alginate/polyvinyl alcohol and alginate-carboxymethyl cellulose: Not ideal as colon-targeted dosage form p. 14
Raditya Iswandana, Ertika Festya Amangkoe, Runia Aisyah Isnaini
Objectives: Colon drug delivery system should be able to maintain drug release until the system reaches its target. In this study, beads were selected as drug carrier system to deliver tetrandrine to colon using a combination of two polymers, alginate and polyvinyl alcohol (PVA) and also alginate and carboxymethyl cellulose (CMC). It was hypothesized that alginate/PVA beads and alginate-CMC beads may be able to protect the drug effectively while in the gastrointestinal tract and may deliver the drug at colon under the influence of colonic pH. Materials and Methods: Beads were formulated into six formulae with different concentrations of polymer. Beads were characterized and evaluated for in vitro drug release using dissolution method. Results: Beads' Formula 3 (alginate and PVA 2:1) and Formula 6 (alginate and CMC 2:1.5) were the best formulae with entrapment efficiency 32.12% and 39.83%, respectively. The drug release test was performed first in hydrochloric acid (HCl) medium for 2 h, then in phosphate-buffered pH 7.4 + 2% Tween 80 for 3 h, and finally in phosphate-buffered pH 6.8 + 2% Tween 80 medium for 3 h, successively. The results of drug release in HCl pH 1.2 were 84.13%, 73.12%, 66.57%, 85.59%, 78.26%, and 69.56%, for Formula 1, 2, 3, 4, 5, and 6, respectively. Conclusion: All type of beads showed the high release of tetrandrine in HCl; hence, it is not ideal yet as a colon-targeted dosage form.
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Evaluation of the activity of Tontelea micrantha extracts against bacteria, Candida and Mayaro virus p. 21
Waleska Stephanie Cruz, Ariane Coelho Ferraz, William Gustavo Lima, Thaís Fátima Silva Moraes, Fernanda Lopes Ferreira, Jaqueline Maria Siqueira Ferreira, Cintia Lopes De Brito Magalhães, Lucienir Pains Duarte, Sidney Augusto Vieira Filho, José Carlos De Magalhães
Objectives: This work aimed to evaluate the antibacterial, antifungal, and anti-Mayaro virus(MAYV) activity of leaf and branch extracts from Tontelea micrantha. Materials and Methods: T. micrantha extracts were prepared through the partition of the leaf and branch samples in different solvents. Then, the antibacterial and antifungal activity was assessed against bacterial pathogens and Candida sp. by the determination of the minimum inhibitory concentration (MIC) by the broth microdilution method. The activity against anti-MAYV was evaluated through the quantification of the extract concentration that promoted the protection of 50% of the cells after the viral infection. Results: The extracts of T. micrantha were inactive (MIC >500 μg/mL) against Gram-positive, Gram-negative and Candida species at the highest concentration tested (500 μg/mL). Anti-MAYV activity was also not detected, with SI <10, ranging from 1.2 to 3.6. Conclusion: Although it is used in traditional medicine, Leaf and branch extracts from T. micrantha did not present antimicrobial activity, which could be caused by the antagonistic effect of the compounds present in the extract.
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Absence of antibacterial, anti-candida, and anti-dengue activities of a surfactin isolated from Bacillus subtilis p. 27
William Gustavo Lima, Adriano Guimarães Parreira, Lídia Anitta Alves Nascimento, Camyla Alves Leonel, Jéssica Tauany Andrade, Juliana Maria Campos Palumbo, Adriana Cristina Soares, Paulo Afonso Granjeiro, Jaqueline Maria Siqueira Ferreira
Background: Biosurfactants are biological compounds that possess many pharmacological proprieties. Among them, surfactin is one of the most active against pathogens of medical interest, such as fungi, bacteria, and enveloped viruses. Objectives: In this study, we aim to evaluate the antibacterial anti-Candida, and anti-dengue potential of a surfactin biosynthesized by Bacillus subtilis ATCC 6633. In addition, the fractional inhibitory concentration (FIC) was calculated to determine the behavior of this biosurfactant in association with antibacterial and antifungal drugs of clinical use. Materials and Methods: B. subtilis ATCC 6633 culture was maintained on nutrient agar plates, and biosurfactant production was carried out in mineral salt medium with 2% glucose. The isolated and purified surfactin was used for determination of antibacterial and antifungal effects by the broth microdilution method. A checkerboard assay was performed to determine the potential synergic effect of surfactin with gentamicin, penicillin, and nystatin. Finally, the activity against Dengue virus (DENV) was evaluated through quantification of cell viability after viral infection. Results: Although it had low cytotoxicity (CC50 >400 μg/mL), surfactin was inactive against Gram-negative and Gram-positive bacteria, Candida species, and DENV at the highest concentration tested (500 μg/mL). According to FIC values, none of the antimicrobials tested showed a synergistic association with surfactin. Conclusions: Surfactin produced by B. subtilis ATCC 6633 is not a promising antimicrobial agent, and its combination with clinically available antibiotics does not lead to a synergic effect.
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Inappropriate of In vitro antimicrobial and anticancer activities from cashew (Anacardium occidentale L.) nut shell extracts p. 33
Yuttana Sudjaroen, Kanittada Thongkao, Kowit Suwannahong
Objective: Cashew nut is one of the major agriculture products in Southern of Thailand, and the volume of cashew nut shell is become increase as a by-product. Thus, cashew nut shell is attractive source for evaluation of antimicrobial activities as inexpensive source. This study was aimed to evaluates in vitro antimicrobial properties of the water extract (CW) and ethanol extract (CE) from cashew nut shell and to evaluate anticancer activity and cytotoxicity of extracts by in vitro screening test against cell lines and normal mammalian cells, respectively. Materials and Methods: CW and CE extracts were determined total phenolic compound by Folin-Ciocalteu reagent. Antibacterial activity of CW and CE against Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Acinetobacter baumannii were evaluated by resazurin microplate assay (REMA). Antimicrobial activities of both extracts against herpes simplex virus Type I and Mycobacterium tuberculosis were tested according by green fluorescent protein (GFP)-based assay; Candida albicans was tested according by REMA; and Plasmodium falciparum was tested according by microculture radioisotope techniques. Anticancer activities of CW and CE were tested with MCF7, NCI-H187, HepG2-, and Caco2 cell lines; and cytotoxicity test was used Vero and human dermal fibroblasts, neonatal (HDFn) cells. Results: CW and CE were lack of in vitro antibacterial (maximum concentration = 100 μg/ml), antimicrobial, and anticancer activities (maximum concentration = 50 μg/ml). CW and CE (0-50 μg/ml) were lack of cytotoxicity against Vero cells and HDFn-neonatal dermal fibroblast. Conclusions: CW and CE extracts of cashew nut shell had no significant in vitro anticancer and antimicrobial activities with noncytotoxicity.
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Triazole-chalcones: Lack of antibacterial, anti-candida, and anti-dengue virus activities p. 39
Michelli dos Santos, Felipe Rocha Da Silva Santos, Ariane Coelho Ferraz, Jéssica Tauany Andrade, Karina Marjorie Silva Herrera, William Gustavo Lima, Lailah Horácio Sales Pereira, Marina Goulart da Silva, José Augusto Ferreira Perez Villar, José Carlos de Magalhães, Alex Gutterres Taranto, Luciana Lara dos Santos, Jamária Adriana Pinheiro Soares-Martins, Jaqueline Maria Siqueira Ferreira
Background: The need to identify new antimicrobial drugs that present different mechanisms of action is urgent. The variety of biological properties of chalcones give them a potential therapeutic compounds. Chalcones' synthetic manipulations are investigated worldwide in search of more powerful and efficient drugs to several infectious diseases' treatment. Objective: The purpose of this work was to evaluate the potential antibacterial, antifungal, and anti-dengue virus (DENV) of new ten triazole chalcones. Materials and Methods: Triazole chalcones were used to determine its antibacterial activity against Gram-positive bacteria (Staphylococcus aureus and Staphylococcus epidermidis), Gram-negative bacteria (Klebsiella pneumoniae, Enterobacter cloacae, Acinetobacter baumannii, and Pseudomonas aeruginosa) species, and anti-Candida activity (Candida albicans) by the broth microdilution assay. The anti-DENV activity was evaluated by cell viability quantification after viral infection by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide colorimetric assay. Results: Although Triazole chalcones have shown a low cytotoxicity concentration (with CC50of 47.21–192.51 μg/mL), these compounds did not exhibit antimicrobial activity against Gram-negative and Gram-positive bacteria, C. albicans neither DENV, even in the highest concentration tested. Triazole chalcones had no activity against all tested microorganisms, except for Gram-positive S. epidermidis bacteria when a poor antimicrobial effect was observed (125 μg/mL). Conclusion: The results suggest that triazole chalcones investigated in this study are not promising antimicrobial agents.
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Lack of antibacterial activity of aqueous and ethanolic leaf extracts of Ziziphus talanai (Blanco) Merr. p. 44
Angelico Garcia Reyes, Adrian Eustrace P Miclat, Angelo B Bañares, Renato A Dela Peña
Objective: The objective of the study is to investigate the phytochemicals and potential antibacterial activity of aqueous and ethanolic leaf extracts of Ziziphus talanai. Materials and Methods: Aqueous and ethanolic crude leaf extracts were subjected to phytochemical screening and assayed for their antimicrobial activities via paper disc diffusion method against Escherichia coli and Staphylococcus aureus. Results: Glycosides, condensed tannins, and saponins were found present in the two extracts; however, leucoanthocyanins were additionally detected in the aqueous extract. Both extracts exhibited no antibacterial activity against E. coli and S. aureus as indicated by the absence of a zone of inhibition. Conclusion: The results of the present study suggest a limited presence of phytochemicals in the crude aqueous and ethanolic leaf extracts of Z. talanai. Water can extract more phytochemicals from Z. talanai leaves than ethanol. However, the results further suggest that the phytochemicals from the leaves extracted using water and ethanol do not have antibacterial activities against E. coli and S. aureus. The negative results of the antimicrobial assay using the crude leaf extracts may not be generalized as lack of bioactivity of the other parts of Z. talanai.
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Lack of antidiabetic effect of ethanolic extract of leaves of Solanum trilobatum Linn (Solanaceae) p. 49
Subramani Parasuraman, Siaw Sze Hoong, Lim Nian Zou, David Lim De Wei, Sunderesan Loshini
Objective: The objective was to study the antidiabetic properties of ethanolic extract of the leaves of Solanum trilobatum (EEST) in streptozocin (STZ)-induced diabetics in Sprague-Dawley (SD) rats. Materials and Methods: EEST was prepared by using hot percolation method and the extract was used for antidiabetic screening. The SD rats were divided into six groups each of six animals, namely normal control, diabetic control, glibenclamide and EEST-treated groups at 125, 250, and 500 mg/kg. Except normal control animals, all the other animals were induced diabetes with intraperitoneal injection of STZ (55 mg/kg). The control and diabetic animals were treated with respective assigned treatment once daily for 21 consecutive days. The blood glucose was monitored at regular intervals and biochemical parameters such as aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, urea, and creatinine were measured with terminal sample. At the end of the study, the animals were sacrificed; lung, heart, stomach, liver, and kidney were harvested and absolute organ weight was measured. Results: The rats administrated with the extracts at dose of 500 mg/kg body weight (BW)/day showed significant antidiabetic activity and this effect was comparable with that of glibenclamide. The diabetic control animals showed significant increased levels of total cholesterol, high-density lipoprotein (HDL), HDL ratio, very-low-density lipoprotein, and glibenclamide, and EEST prevented STZ-induced cholesterol impairments. EEST did not show any significant antidiabetic effect at 125 and 250 mg/kg BW/day treated rats. Conclusion: EEST showed significant antidiabetic activity at 500 mg/kg and prevented STZ-induced metabolic changes in experimental animals. EEST did not show any antidiabetic activity in diabetic animals treated with 125 and 250 mg/kg of EEST.
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The effectiveness of Melissa officinalis on sleep problem in patients with chronic heart failure p. 55
Fatemeh Aliakbari, Mahmoud Rafieian
Background: Numerous studies have documented high prevalence rate of major depression in patients with heart failure. The aim of the present study was to evaluate the effectiveness of Melissa officinalis on sleep problem in patients with chronic heart failure (CHF). Materials and Methods: In a randomized, controlled trial study, eighty patients (40 in each group) with CHF experiencing insomnia were allocated randomly into intervention and control groups. The patients in intervention group received 12 ml M. officinalis syrup in addition to conventional treatment 1 h before going to bed for 4 weeks. A demographic questionnaire and the Pittsburgh Sleep Quality Index were used to collect data. Questionnaires were completed by all individuals before and after the intervention. Results: The time duration of waiting for falling into sleep in intervention group was significantly less than control group (P = 0.001). The hours during which the individuals were fully asleep were significantly more than control group (P < 0.05). Conclusion: M. officinalis may improve the quality of sleep in patients with CHF who experience insomnia.
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Adverse events during plateletpheresis donation p. 59
Viroj Wiwanitkit
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Self-medication with herbal medicines, an untamed threat to global health p. 60
Enegide Chinedu, Dabum Luka Jacob
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