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   Table of Contents - Current issue
July-December 2020
Volume 9 | Issue 2
Page Nos. 177-287

Online since Wednesday, October 7, 2020

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Synthesis and comparison of anti-Leishmania major activity of antimony and iron complexes of 3-hydroxypyran-4-one and 3-hydroxypyridine-4-one as bi-dentate ligands p. 177
Zeynab Zarrabi, Lotfollah Saghaie, Afshin Fassihi, Nader Pestechian, Sedigheh Saberi
Background: Leishmaniasis infection threatens millions of people in under developing and developing countries. Treatment of this neglected disease is very complicated. Subjects and Methods: A novel series of antimony (V) complexes using bidentate ligands of hydroxypyranones and hydroxypyridinones have been designed and synthesized. For the synthesis of the complexes, SbCl5 in water was added to the solution of each ligand at 60°C and the pH of mixture was adjusted to 8 using aqueous NaOH. After 24 h stirring, extraction of produced compound into acetone gave the desired complex. The structure of complexes was achieved by using FTIR, 1HNMR, and electron spin ionization mass spectroscopic techniques. All compounds were evaluated for in vitro anti amastogote form of Leishmania major. Results and Conclusion: The most potent antimony complexes against amastigotes were 5b (after 48 and 72 h) and 5a (after 72 h) with IC50 values of 24.4, 16.3, and 30.1 µg/mL, respectively. Furthermore, antimony and iron complexes were used together for in vitro anti amastigote form of L. major activity. These compounds were toxic for macrophages and destroyed them.
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Apoptotic effects of ginger extract (Zingiber officinale) on esophageal cancer cells ESO26: An in vitro study p. 183
Abbas Abbasi, Ali Azizi, Seidmostafa Nachvak, Elaheh Alizadeh, Rezvan Abbsavaran, Elham Mirtaheri, Mehdi Moradinazar, Mehrali Rahimi
Aim: Ginger is a natural dietary rhizome with antioxidant, anti-inflammatory, and anticarcinogenic properties. It has many medical beneficial properties such as anti-proliferation and antiapoptotic effects on cancerous esophageal cells. Materials and Methods: Esophageal cancer cells ESO26 were cultured in the presence and absence of ginger extract at various concentrations for 12, 18, and 24h. Then, the viability was determined by 3-(4,5-dimethylthiazol)-2,5-diphenyl tetrazolium bromide (MTT) assay. Western blot analysis of caspase-3 was performed to detect apoptosis. p21, Bax, and Bcl-2 gene expression was measured using quantitative polymerase chain reaction (PCR). Data were analyzed using one-way analysis of variance (ANOVA) followed by Tukey test. Results: The ginger extract increased the cleavage of caspase-3 in cells (P < 0.05). Results of real-time PCR have shown that ginger decreased the expression of Bcl-2 and increased Bax and p21 gene expression (P < 0.05). Conclusions: Results showed that the process of cell proliferation has been stopped. Also, this study indicated that ginger might exert a chemopreventive effect on esophageal cancer through the suppression of proliferation and the growth of tumor cells as well as the induction of apoptosis.
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Synthesis and evaluation of thiadiazole-based antileishmanial agents p. 189
Farshid Hassanzadeh, Elham Jafari, Mozhgan Saeedi, Sedigheh Saberi
Background and Objectives: The 1, 3, 4-thiadiazole scaffold is one of the principal structural components, in a variety of drug categories such as antimicrobial, anti-inflammatory, antineoplastic, and antileishmanial agents. Considering the reported antileishmanial effects of thiadiazole derivatives and the importance of this disease, some of the thiadiazole derivatives with modifications at sulfur atom or amine group attached to the 2-position were synthesized and evaluated for antileishmanial activity. Materials and Methods: Derivatives of 1,3,4-thiadiazole including 2-substituted-thio-1,3,4-thiadiazoles bearing (5-(4-nitrobenzylideneamino) or 5-amino (II, IV, V) and one derivative of 2-substituted-amino-1,3,4-thiadiazole bearing (5- (4-nitrophenyl) (VII) were synthesized and evaluated for their in vitro antileishmanial activity against promastigote and amastigote forms of the Leishmania major. Results: The most active compound was found to be compound II after 24-h incubation against promastigotes and amastigotes with the half maximal inhibitory concentration (IC50) values of 44.4 µM and 64.7 µM, respectively. Conclusion: All of the synthesized compounds showed good antileishmanial activity against both forms of L. major after 48 and 72h incubation.
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Repeated administration of fluvoxamine worsens gentamicin-induced nephrotoxicity in rats p. 196
Afshin Ramian, Iraj Javadi, Hossein Sadeghi, Heibatollah Sadeghi, Esmaeel Panahi Kokhdan, Amir Hossein Doustimotlagh, Reza Abbasi, Sadegh Alizadeh, Hamed Nikbakht
Background: Depression is one of the most prevalent and life-threatening forms of mental disorders in chronic kidney disease. Antidepressant agents such as fluvoxamine are broadly prescribed in this situation. This study investigated the effects of fluvoxamine on gentamicin (GEN)-induced nephrotoxicity in rats. Materials and Methods: Twenty-four male Wistar rats were randomly divided into four groups (n = 6) including (1) control group, (2) GEN group, (3) GEN + fluvoxamine (25 mg/kg) group, and (4) GEN + fluvoxamine (50 mg/kg) group. Fluvoxamine was orally given to animals 45 min before GEN was injected (100 mg/kg, intraperitoneally [i.p.]). Blood urea nitrogen (BUN), creatinine (Cr), sodium (Na+), potassium (K+), and malondialdehyde (MDA) levels in serum were measured. Moreover, the glucose (Glu) and protein (Pro) levels in urine and the ratio of kidney to body weight (g/100g body weight) were determined. Histopathological alterations in kidney were evaluated. Results: GEN significantly increased the Cr and BUN serum levels as well as urine Glu and Pro concentrations (P ≤ 0.001). Fluvoxamine exacerbated the elevation in the indicated parameters. GEN also significantly increased the serum MDA levels. Fluvoxamine had no effect on the elevated serum levels of MDA. GEN did not show any effect on the K+ and Na+ serum concentrations. Increased kidney-to-body weight ratio due to GEN nephrotoxicity was further exacerbated by 25 mg/kg of fluvoxamine (P ≤ 0.001). Pathologic findings also confirm the biochemical results. Conclusion: The data suggest that fluvoxamine worsens the nephrotoxicity of GEN. However, further clinical and animal investigations are required to elucidate the mechanism of this interaction.
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Hollow fiber-based liquid-phase microextraction and HPLC-UV determination of lovastatin in biological fluids p. 203
Fatemeh Bayat, Atefeh Hajiagha Bozorgi
In this study, a hollow fiber liquid-phase microextraction (HF-LPME) method coupled with high-performance liquid chromatography (HPLC) was successfully developed for the determination of trace levels of lovastatin in urine and plasma samples. Lovastatin was extracted from 15 mL of the acidic sample solution with a pH of 2 into an organic extracting solvent (n-octanol) impregnated in the pores of a hollow fiber and then back extracted into an acidified aqueous solution in the lumen of the hollow fiber. After extraction, 10 µL of the acceptor phase was injected into HPLC system. To obtain high extraction efficiency, the parameters affecting the HF-LPME, including pH of the sample and extractant phases, type of organic phase, ionic strength, stirring rate, extraction time, and temperature, were studied and optimized. Under the optimized conditions (solvent 1-octanol, pH = 2, 45 min stirring at 45°C with 750rpm), the relative recovery percentage was 85.2–97, which shows the capability of the method to analyze the analyte concentration. This technique provided preconcentration factor 199, 185, and 170 for water, urine, and plasma, respectively. Good precisions values (with relative standard division ≤ 10.5%) were obtained. The results indicated that the HF-LPME method has an excellent cleanup capacity and a high preconcentration factor and could serve as a simple and sensitive method for monitoring the drug in biological samples.
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Fosfomycin protects intestinal cells from nuclear changes suggestive of deoxynivalenol-induced apoptosis p. 209
Denisa Perez Gaudio, Joaquín Mozo, Guadalupe Martínez, María B Fernández Paggi, Julieta M Decundo, Agustina Romanelli, Susana Dieguez, Alejandro Soraci
Background: Fosfomycin (FOS) is a broad-spectrum antibiotic that inhibits cell wall synthesis. It has bactericidal activity against both gram-positive and gram-negative bacteria. FOS also promotes phagocytosis, has immunomodulatory effects, and protects against the toxicity caused by other drugs. On the contrary, deoxynivalenol (DON) causes cytotoxicity on tissues of rapid growth and fast turnover. Objectives: The aim of this study was to determine the percentage of nuclear changes indicative of DON-induced apoptosis on intestinal cell cultures (Caco-2) and to evaluate the protective effect of FOS on mycotoxin-exposed cells. Materials and Methods: Cell cultures were treated as follows: (1) DON: 2.8 µg/mL, (2) calcium FOS: 580 µg/mL, (3) DON 2.8 µg/mL + calcium FOS 580 µg/mL, and (4) negative control. Nuclear morphology was evaluated in fixed cells stained with 4′,6-diamino-2-phenylindol and then visualized under an immunofluorescence microscope. Results: Percentages of cells with nuclear changes were significantly higher in cells treated with DON (31.53% ± 4.17%) compared to those incubated with the antibiotic in conjunction with the mycotoxin (5.63% ± 4.23%). On the contrary, there were no significant differences between cells incubated with DON + FOS and cells incubated only with the antibiotic (1.10% ± 1.55%) when compared to the negative control (3.50% ± 0.09%). Conclusion: The results from this study showed that DON induces nuclear changes suggestive of apoptosis in intestinal cells and that FOS can protect cells from DNA damage. Further studies are needed to determine whether DON induces apoptosis only on cells of epithelial origin and to understand the implications of FOS protective effect under in vivo conditions.
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The role of duloxetine in changing the process of tolerance to morphine analgesic effects in male rats p. 215
Alireza Parvizpur, Kiarash Fekri, Laleh Fekri, Parvin Ghadimi, Mohammad Charkhpour
Introduction: Among various neurological systems involved in the development of morphine tolerance, serotonergic and adrenergic systems are very significant. In this study, we used duloxetine to further investigate the association between serotonergic and noradrenergic systems and the occurrence of opioid tolerance. Materials and Methods: Six groups of male Wistar rats were studied including saline, morphine, morphine + duloxetine (15, 30, and 60 mg.kg–1.day–1), and duloxetine-treated groups. Base latency time (BL) was determined using hot plate test (50 ± 0.5ºC). The latency times were reported as MPE% (maximum possible effect) and AUC (area under the curve) was calculated for each MPE%-Time curve (to evaluate global analgesic effect). Results: Morphine-treated group showed tolerance on the 9th day. As the same way, the groups treated with morphine and duloxetine (15, 30, 60 mg/kg) showed tolerance on the 13th, 17th, and 23rd days, respectively. Duloxetine-treated group was tolerated on the 11th day. There was a significant difference between the mean AUC in morphine + duloxetine (60 mg/kg-1/day–1) and morphine-treated groups. Conclusion: Previous studies revealed that chronic administration of morphine would reduce serotonin release in the central nervous system (CNS). This study showed the effective role of duloxetine and the serotonergic system in postponing the tolerance to analgesic effects of morphine.
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Cytotoxic, antimicrobial activities, and phytochemical investigation of three peach cultivars and acerola leaves p. 221
Seham S El-Hawary, Ola Mohamed Mousa, Rana Ahmed El-Fitiany, Rania A El Gedaily
Background: Phytoconstituents of Prunus persica Linn. (Peach) and Malpighia glabra Linn. (Acerola) leaves were not thoroughly studied, although they are commonly incorporated in the food industry. Aim: Our aim is to explore metabolites and vitamins in three peach cultivars leaves; Desert red, Florida prince, Swelling and acerola. Material and Methods: Analysis was done using GC/MS (gas chromatography–mass spectrometry), HPLC (high-performance liquid chromatography), and spectrophotometry. Cytotoxicity was performed using MTT assay. Results: Total phenolic and flavonoid content varied from 79.54 to 121.51 μg gallic acid equivalent/mg dry weight and 31.05 to 39.77 μg quercetin equivalent/mg dry weight, respectively. Twenty-four flavonoids were identified; hesperidin was the major flavonoid in peach cultivars (3863.4 mg/100 g in Desert red, 2971 mg/100 g in Swelling, and 2624 mg/100g in Florida prince). Glucuronic acid (33.04%) and vitamin C (34 mg/100 g) were major in acerola. Thirty-four metabolites including supraene and sitosterol as well as 24 fatty-acid esters including linoleic and oleic acids were detected in the unsaponifiable and saponifiable matter, respectively. Antimicrobial activity against bacterial and fungal strains was screened in comparison with ampicillin and amphotericin B. All tested extracts significantly decreased cell viability against breast (MCF-7) and colon cell lines (HCT-116). M. glabra showed no significant difference from standard doxorubicin (0.1 μg/mL) which may suggest a strong anticancer activity against colon cell line. Conclusion: This study may highlight the magnitude of the leaves of these plants as rich sources of important metabolites and vitamin C.
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Deciphering the in vitro antioxidant potential and mineral analysis of Fagopyrum species from Kashmir and Ladakh regions p. 235
Fayaz Ahmad Dar, Tanveer Bilal Pirzadah, Inayatullah Tahir, Reiaz Ul Rehman
Context: The Kashmir and Ladakh Himalayan regions are having a rich diversity of buckwheat germplasm, which is an excellent source of nutrition and functional food. The objective of this study was based on comparative in vitro flavonoid, antioxidant, and mineral analyses of Fagopyrum species grown in these regions. Materials and Methods: To achieve this goal, leaf samples from the four buckwheat species were subjected to antioxidant analysis. Besides, the mineral analysis of the groat samples of different buckwheat species was carried out by atomic absorption spectroscopy (AAS). Results: Results indicated that the methanolic extract shows higher total phenolic content (TPC) and total flavonoid content (TFC) in the samples of Fagopyrum sagittatum followed by Fagopyrum tataricum, Fagopyrum kashmirianum, and Fagopyrum esculentum. Total reducing power (TRP), ferric reducing antioxidant power (FRAP), 1,1-diphenyl-2-picrylhydrazyl (DPPH), superoxide anion radical (SOR), and hydrogen peroxide (H2O2) radical scavenging assays indicated excellent results from the leaf extracts of F. sagittatum. The results suggested that the crude methanolic extract of buckwheat species had effective reducing power, radical scavenging activity, and metal-chelating ability compared to other standard antioxidants. AAS analysis revealed that calcium content was higher in F. sagittatum (21,600 ppm), whereas the iron and zinc contents were higher in F. kashmirianum (1,122.5 ppm) and F. sagittatum (166.75 ppm), respectively. Conclusion: Our study suggested that methanolic extracts of Fagopyrum species could act as a potent source of natural antioxidants to the pharmaceutical and food industry. In addition, the study also revealed that the rich elemental profiles of buckwheat species specify their therapeutic value and thus could be used as a potential biofortification crop.
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Contribution of community pharmacy in treating tuberculosis: A pharmacy centric study from Belagavi district p. 246
Uday Kumar Rangaswamy, Madiwalayya S Ganachari
Introduction: Tuberculosis (TB) is an important global health problem, which is aimed to be eradicated by 2025 from India. Community pharmacists play a significant role in treating and eradication of TB. This study aimed to understand the contribution of community pharmacy and their potential role in RNTCP (Revised National TB Control Programme) functioning. Materials and Methods: The study was conducted at Belagavi, Karnataka, India on 312 community pharmacies. A structured interview form was used to assess several factors such as education, knowledge, anti-TB drug dispensing patterns, willingness to be trained, and become a DOTS (Directly Observed Treatment Short course) provider. Results: On an overall scale, we found that the majority of licensed community pharmacy was managed by D. Pharm holders with a limited knowledge of TB. It was also noted that there was a lack of willingness to be rigorously trained for updating their knowledge, although they were interested in being trained for being recognized as a DOTS center. Conclusion: There is a strong need for strengthening community pharmacy services in tune with RNTCP to achieve better efficiency in treating and eradication of TB.
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Antioxidant capacity and HPLC determination of phenolic in different organs of Calligonum polygonoides subspecies comosum p. 251
Hayam S Ahmed, Abeer S Moawad, Asmaa I Owis, Sameh F AbouZid
Background: Calligonum polygonoides subsp. comosum is a perennial desert plant. Most of the previous chemical investigation of this plant was performed on the whole herb but there were no data about quantification of active constituent in different organs of C. polygonoides. Materials and Methods: in vitro antioxidant activity, total phenolic, and total flavonoid contents of the different organs were determined using 2, 2-diphenyl-1-picrylhydrazyl (DPPH), Folin–Ciocalteu, and aluminum chloride (AlCl3) methods, respectively. Quantitative analysis of the phenolic compounds was determined in the different organs of the plant using high-performance liquid chromatography (HPLC). Results: Both bark and leaves showed the highest radical scavenging activity with the values of 450.30 and 398.10 μg/g ascorbic acid equivalent, respectively. The total phenolic content of the samples was in the range of 27.9–281.5 μg/g gallic acid equivalent and total flavonoid content of the samples was in the range of 53.9–257.4 μg/g rutin equivalent where the leaves and bark showed the highest contents. HPLC analysis showed that flavonol glycosides content was higher in all organs compared to the aglycones. Flowers and fruits were the richest organs in flavonols, whereas leaves, stems, and bark were the richest in taxifolin and catechin. Conclusion: Depending on the obtained results C. polygonoides is an excellent source of natural antioxidants.
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Cocrystallization: An innovative route toward better medication p. 256
Braham Dutt, Manjusha Choudhary, Vikaas Budhwar
Nowadays, poor solubility, lower bioavailability, and hindered physical, chemical, and biopharmaceutical properties of active pharmaceutical ingredients (APIs) become a very important matter of discussion for pharmaceutical scientists. It is a challenging task for pharmaceutical researchers and industry to develop a suitable formulation with improved physicochemical properties. The process of cocrystallization is long known; however, in the recent times, this approach has gained enormous importance in pharmaceuticals as a relatively new method for enhancement of solubility, bioavailability, stability, thermal properties, permeability, tablet ability, and other related physicochemical properties. Cocrystals are multicomponent systems in which two components, an API and a coformer, were present in stoichiometric ratio and bonded together with non-covalent interactions in the crystal lattice. Cocrystallization offers better optimization of not only physicochemical properties but also therapeutic response and pharmacological properties of APIs. The design of a cocrystallization experiment is based on robustness, hydrogen bonding rules, and potential intermolecular interactions. Various theoretical and experimental approaches increase the chances for selection of a suitable coformer, the most challenging step during the design of cocrystal formation. The present review covers classification of cocrystals, drug selection criteria for cocrystals, chemistry involved in cocrystal formation, methods of preparation, their characterizations, and various applications in pharmaceutical and biomedical fields.
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Recent advances in the development of the nanostructured lipid carriers for the topical fungal infections p. 271
Amandeep , Shailendra Bhatt, Manish Kumar, Sheetal Devi, Prabhat Kumar Upadhyay, Vipin Saini, Amit Mittal, Navneet Mehan, Anupam Saini
Topical fungal infections are one of the often faced diseases worldwide. The first choice for the treatment of fungal infection is topical therapy due to its advantages such as decreasing the risk of systemic side effects and targeting the drug at the site of fungal infection. The treatment of the fungal infection depends on the penetration of the drug molecules through the outermost layer of the skin (stratum corneum) at an effective concentration. The disadvantages of topical treatment are its lack of drug adherence at the site of application and bigger particle size of drug molecules. Nanostructured lipid carriers are the advanced form of lipid nanoparticles and carry the nano range of the drug molecules, which helps to achieve localized and slow release. The topical route is generally preferred due to the possible side effects of oral medication. Advances in the field of formulation may soon render outdated conventional products such as creams, ointments, and gels. Several carrier systems loaded with antifungal drugs have shown promising results in the treatment of skin fungal infections.
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Combinational treatments for breast cancer p. 279
Omid Tavallaei, Marzieh Marzbany, Mahsa Rasekhian
Heterogenicity is an indispensable element of breast cancer, which manifests itself on clinical, histopathological, and molecular levels. This heterogenicity could be a determinant factor of disease progression and drug resistance in the patients. Common therapies for metastatic breast cancer include surgery, radiotherapy, chemotherapy, and immunotherapy. On the introduction of biologic medicine, target therapy, and gene therapy, a potential has been reached to lower the rate of morbidity and mortality and also to improve the quality of life among patients with breast cancer. Although these treatments have been frequently proved by yielding promising results, a very few number of them have found their way into clinic settings due to progressive nature of these tumors, diversity of cancer populations and their microenvironments, genetic instability, and heterogenicity of breast cancers. As only minor advancements have been made in the case of recurrent metastatic breast cancer, handling this condition is now considered a medical necessity. According to genetic instability and heterogenicity of breast tumors, it is implausible to assume a single-targeted therapy could help treating most solid tumors. So, this review aimed to put together studies focused on combinational treatments targeting growth inhibition and apoptosis induction in breast cancer cells and comparing the results with monotherapies.
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