فهرست مطالب

Journal of Reports in Pharmaceutical Sciences
Volume:9 Issue: 2, Jul-Dec 2020

  • تاریخ انتشار: 1399/08/18
  • تعداد عناوین: 14
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  • Zeynab Zarrabi, Lotfollah Saghaie, Afshin Fassihi, Nader Pestechian, Sedigheh Saberi* Pages 177-182
    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.

    Keywords: Anti-leishmania activity, antimony (V) complexes, iron complexes, Leishmania major
  • Abbas Abbasi, Ali Azizi, Seidmostafa Nachvak, Elaheh Alizadeh, Rezvan Abbsavaran, Elham Mirtaheri, Mehdi Moradinazar, Mehrali Rahimi* Pages 183-188
    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 24 h. 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.

    Keywords: Apoptosis, caspase-3, esophageal cancer, ginger
  • Farshid Hassanzadeh, Elham Jafari*, Mozhgan Saeedi, Sedigheh Saberi Pages 189-195
    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-amino1,3,4-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.

    Keywords: Amastigote, antileishmanial activity, leishmania major, promastigote, thiadiazole
  • Afshin Ramian, Iraj Javadi, Hossein Sadeghi*, Heibatollah Sadeghi, Esmaeel PanahiKokhdan, Amir Hossein Doustimotlagh, Reza Abbasi, Sadegh Alizadeh, Hamed Nikbakht Pages 196-202
    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 (25mg/kg) group, and (4) GEN + fluvoxamine (50mg/kg) group. Fluvoxamine was orally given to animals 45min before GEN was injected (100mg/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/100 g 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 25mg/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.

    Keywords: Fluvoxamine, gentamicin, nephrotoxicity, rat
  • Fatemeh Bayat, Atefeh Hajiagha Bozorgi* Pages 203-208

    In this study, a hollow fiber liquid-phase microextraction (HF-LPME) method coupled with highperformance liquid chromatography (HPLC) was successfully developed for the determination of trace levels of lovastatin in urine and plasma samples. Lovastatin was extracted from 15mL 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, 45min stirring at 45°C with 750 rpm), 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.

    Keywords: Biological sample, drug analysis, high-performance liquid chromatography, hollow fiber
  • Denisa Pérez Gaudio*, Joaquín Mozo, Guadalupe Martínez, María B.Fernández Paggi, Julieta M.Decundo, AgustinaRomanelli, Susana Dieguez, _ Alejandro Soraci Pages 209-214
    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 DONinduced 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.

    Keywords: Apoptosis, deoxynivalenol, fosfomycin, intestinal cells, protective effect
  • Alireza Parvizpur, Kiarash Fekri, Laleh Fekri, Parvin Ghadimi, Mohammad Charkhpour* Pages 215-220
    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 60mg.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, 60mg/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 (60mg/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.

    Keywords: Analgesic, duloxetine, morphine, rat, tolerance
  • Seham S.El-Hawary, Ola MohamedMousa, Rana Ahmed El-Fitiany*, Rania A. El Gedaily Pages 221-234
    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.

    Keywords: Acerola, antimicrobial, cytotoxicity, GC, MS, HPLC, peach
  • Fayaz Ahmad Dar, Tanveer BilalPirzadah, Inayatullah Tahir, Reiaz Ul Rehman* Pages 235-245
    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 (H2 O2 ) 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 (1,122.5ppm) and F. sagittatum (166.75ppm), 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.

    Keywords: 1.1-diphenyl-2-picrylhydrazyl, antioxidants, atomic absorption spectroscopy, buckwheat, ferric reducing antioxidant power, functional food, hydrogen peroxide
  • Uday Kumar Rangaswamy*, Madiwalayya S.Ganachari Pages 246-250
    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.

    Keywords: Community pharmacy, DOTS, RNTCP, tuberculosis
  • Hayam S. Ahmed*, Abeer S. Moawad, Asmaa I. Owis, Sameh F. AbouZid Pages 251-255
    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.

    Keywords: Antioxidant, Calligonum polygonoides, HPLC analysis, total flavonoid, total phenolic
  • Braham Dutt, Manjusha Choudhary, Vikaas Budhwar* Pages 256-270

    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.

    Keywords: Cocrystallization, cocrystals, coformer, polymorphs, salts
  • Amandeep, Shailendra Bhatt, Manish Kumar*, Sheetal Devi, Prabhat Kumar Upadhyay, Vipin Saini, Amit Mittal, Navneet Mehan, Anupam Saini Pages 271-278

    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.

    Keywords: Fungal infection, lipid nanoparticles, nanostructured lipid carriers, topical
  • Omid Tavallaei, Marzieh Marzbany, Mahsa Rasekhian* Pages 279-287

    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.

    Keywords: breast cancer, combinational treatment, combinatorial treatment