Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
156
163
10.12991/jrp.2019.120
658
Synthesis, characterization and antitubercular evaluation of some new isoxazole appended 1-carboxamido-4,5-dihydro-1h-pyrazoles
Kishor PALLEAPATI
Venkata Ramana KANCHARLAPALLI
Afzal Basha SHAIK
Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis. TB is a global problem and is one of the major culprits responsible for the death of many in the developing world despite the availability of more than 20 drugs. Hence, there is an imperative need for the development of novel antitubercular drugs. To develop better agents against tuberculosis, we synthesized a series of dihydropyrazole-1-carboxamides by the base-catalyzed condensation of isoxazolyl chalcones with semicarbazide. The compounds were purified by column chromatography and characterized by spectral methods including IR, 1H NMR, 13C NMR and elemental analysis. The antitubercular activity was screened against Mycobacterium tuberculosis by MABA assay where isoniazid was used as positive control for comparing the activity. The studies revealed that isoxazole-1-carboxamides were more active compared to the corresponding chalcones. Substituents on the phenyl ring at position-5 of isoxazole ring played a crucial role in determining the antitubercular potency. The compounds 4n and 4o containing a blend of halogen and methoxyl groups at ortho and para positions of phenyl ring showed potency greater than the standard, isoniazid with MIC of 0.1 μg/mL and emerged as promising leads against TB. Further, 4n and 4o were assessed for their cytotoxic effects on L02 (human normal cell line) by using MTT assay. The compounds showed no cytotoxicity and established the safety of these compounds.
https://jrespharm.com/abstract.php?id=658
Isoxazolyl Chalconesdihydropyrazole-1-carboxamidesantitubercular activityMycobacterium tuberculosisMABA assayMTT assay
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
164
169
10.12991/jrp.2019.121
668
Anti-inflammatory properties of the ruthenium polypyridyl complex, k314, on the in vitro activated macrophages
Furkan AYAZ
Ruthenium polypyridyl complex derivatives find applications in the solar cells. They are mostly used as photosensitizers in solar cells for energy production. In our study we examined their activities on the immune system cells. At cellular level metabolic activities are shaped by the electron transfer reactions and ruthenium polypyridyl complexes can very well interfere this process and alter the outcome. A change in the cell’s metabolism would lead to a change in the cell’s activity. Depending on the functional group types attached to the ruthenium complex there can be changes in their biological function. Therefore our group has been screening their different derivatives’ effects on the immune system cells inflammatory activity. We primarily focus on macrophages that are crucial cells of the innate immunity. In order to measure the activity of the macrophage cell line we detected the changes in the pro-inflammatory TNFα, IL1β and IL6 cytokine levels by ELISA. Our in vitro results support that K314 can be used as an anti-inflammatory drμg candidate in autoimmune diseases or inflammatory disorders. Furthermore, K314 can also be used as a surface coating material on the patches to prevent the inflammation in the area; as well as organ and tissue transplants, especially bone tissue, to suppress the inflammation mediated rejection of the transplant.
https://jrespharm.com/abstract.php?id=668
TNFαIL-6IL-1βinflammationmacrophageimmunomodulationanti-inflammatory moleculesinnate immunity
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
170
176
10.12991/jrp.2019.122
670
The development of forced degradation studies for the determination of daptomycin in urine at various conditions by using rp-lc method
Bediha AKMEŞE
Nurgül K. BAKIRHAN
Tuğçe GÖVER
Sibel A. ÖZKAN
Daptomycin is known as the first lipopeptide antibiotic shows activity against gram-positive bacteria. A
fast, simple and repeatabile RP-LC method has been developed for the determination of daptomycin in mobile phase
solution and human urine. This drug was exposed to various stress conditions such as hydrolytic, oxidative, thermal
and photolytic and the stressed samples were detected by the proposed method. Daptomycin was well separated on a
X-Terra RP-18 column using the mobile phase consisting of a mixture of acetonitrile:water (45:55 v/v) at a flow rate of
1 mL min-1. The system operates at 222 nm for daptomycin and 319 nm and tinidazole was used as internal standard
under these conditions. The linearity of daptomycin was obtained between 0.50 and 12 μg mL<sup>-1<sup> concentration range.
Limits of detection was determined as 0.1176 and 0.1412 μg mL<sup>-1</sup> and the limits of quantification was obtained as 0.3563
and 0.4277 μg mL<sup>-1</sup> in the mobile phase and urine, respectively. Hydrochloric acid, sodium hydroxide, hydrogen
peroxide affected response of daptomycin under stress degradation conditions.
https://jrespharm.com/abstract.php?id=670
Drugdaptomycindegradation conditionshigh performance liquid chromatography
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
177
186
10.12991/jrp.2019.123
671
Spectrophotometry, potentiometry and hplc in determination of acidity constant for cabergoline and tadalafil
Merve Banu POLAT
Ayşegül DOĞAN
Nursabah E. BAŞCI
Acidic dissociation constant (pKa) is an important physicochemical parameter in absorption, dissociation and elimination mechanisms of drugs in body. Various analytical methods are utilized for the determination of pKa values of pharmaceutical active ingredients, and potentiometry, spectrophotometry and HPLC are the most common methods. Cabergoline is dopaminergic ergoline derivative having a powerful and long-term prolactin reducing effect, which is used for the treatment of Parkinson disease. Tadalafil leads an increasing cGMP level in Corpus cavernous, during secretion of nitric oxide in sexual arousal. In the presented study, detection of pKa values for Cabergoline and Tadalafil by using potentiometry, spectrophotometry and HPLC was investigated. The pKa value for Cabergoline was respectively found to be 6.42, 6.05 and 6.20 by spectrophotometry, potentiometry and HPLC. Spectrophotometric pKa value was significantly different (p>0.05) from others, and potentiometry and spectrophotometry were appropriate for pKa value determination of Cabergoline. The pKa values for Tadalafil by potentiometry and spectrophotometry were found to be 3.52 and 3.44, respectively. But, in HPLC, no differentiation was observed in retention times of Tadalafil by increasing pH value of mobile phase. Developed methods for determination of pKa values for Cabergoline and Tadalafil demonstrated high repeatability values (RSD<%1). In this study, experimental pKa values for Cabergoline and Tadalafil from developed methods were compared with the values calculated by the common softwares and high-level divergences were observed.
https://jrespharm.com/abstract.php?id=671
Acidity constantpKaphysicochemical parameterCabergolineTadalafil
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
187
197
10.12991/jrp.2019.124
661
Antioxidant and anti-inflammatory potentials of solanum pubescens willd an ethnomedicinal plant of south western andhra pradesh, india
Haseebur RAHMAN
Nazneen RAHMAN
Mir HARIS
Riaz MAHMOOD
Solanum pubescens Willd is an essential ethnomedicinal plant in treatment of hemorrhoids, inflammation, cancer, whooping cough, rheumatoid arthritis, liver disorders, diarrhea, headache, menstrual pain, tuberculosis, ulcers, and belongs to Southern states of India. Henceforth, to validate its medicinal uses concerning the inflammation management the current study aims to evaluate the acute toxicity, in vitro antioxidant efficacy and in vivo anti-inflammatory action of hexane and chloroform extracts of S. pubescens fruits and stem in carrageenan and cotton pellet-induced inflammation in rats. The investigations revealed that the S. pubescens fruit essential oil (SPFO), S. pubescens fruit chloroform extract (SPFC), S. pubescens stem hexane extract (SPSH) and S. pubescens stem chloroform extract (SPSC) demonstrated substantial 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl radicles (OH•), superoxide anion radicles (SOR), nitric oxide radicles (NOR), 2,4,6-tripyridyl-s-triazine (TPTZ) radicle scavenging effect, lipid peroxidation inhibition, total reducing power and total antioxidant activity. The extracts treatment (200 mg/ kg) exhibited significant in vivo anti-inflammatory impact by inhibiting carrageenan-induced paw edema and the weight of cotton pellet-induced granuloma in rats. The current observations might be valuable in strengthening the ethnomedicinal use and considering S. pubescens as a pool of novel anti-inflammatory agents.
https://jrespharm.com/abstract.php?id=661
Solanum pubescens Willdantioxidantanti-inflammationcarrageenangranuloma
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
198
207
10.12991/jrp.2019.125
675
Analgesic, anti-inflammatory and anti-pyretic activities of methanolic extract of cordyline fruticosa (l.) a. chev. leaves
Sharmin NAHER
Md. Abdullah AZIZ
Mst. Irin AKTER
S.M. Mushiur RAHMAN
Sadiur Rahman SAJON
Traditionally Cordyline fruticosa (L.) A. Chev. is being used for the treatment of various disorders, such as
fever, headache, diarrhea, coughs, haemoptysis, small pox, madness, skin eruptions, joint pains, rheumatic bone pains,
swelling pain and it is also used for abortion. The aim of our study wast o evaluate analgesic, anti-inflammatory and
anti-pyretic activities of methanolic extract of C. Fruticosa leaves (MCFL). Analgesic effect of MCFL was investigated by
using acetic acid induced writhing test, formalin-induced paw licking test, tail immersion test and hot plate test. The
anti-inflammatory activity was assessed by using xylene induced ear edema test and cotton pellet induced granuloma
test, whereas antipyretic effect was observed by utilizing Brewer’s yeast-induced pyrexia test. In analgesic test, MCFL
significantly (∗p< 0.05, vs. control) reduced paw licking and abdominal writhing of mice in a dose dependent manner.
MCFL at a dose of 800 mg/kg body weight, significantly increased pain threshold in tail immersion test and hot plate
test. Significant anti-inflammatory effect was produced by MCFL by reducing xylene induced air edema and cotton
pellet induced granuloma in a dose dependent manner. In anti-pyretic test, after 4th hour of respective treatment, MCFL
at all doses exhibited anti-pyretic activity, when compared with control (∗p < 0.05, vs. control). The results obtained
demonstrate that C. fruticosa may provide a source of plant compounds with analgesic, anti-inflammatory and
antipyretic activities.
https://jrespharm.com/abstract.php?id=675
Cordyline fruticosaanalgesicanti-inflammatoryanti-pyretic
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
208
216
10.12991/jrp.2019.126
669
Elucidation of biological properties of some commercial anthraquinones: mutagenic / antimutagenic and antimicrobial activity approaches
Ahmet UYSAL
Erdoğan GÜNEŞ
Yusuf DURAK
Anthraquinones (AQ) are the most common group of naturally occurring quinones. Both natural and synthetic AQs have been used as colorants in food, drugs and cosmetic industries. The aim of this study was to evaluate the mutagenic/antimutagenic potentials of some AQs (Alizarin, quinizarin, purpurin, and 1,8-dihydroxy anthraquinone) with Salmonella typhimurium TA98 and TA100 strains by Ames test and antimicrobial activity by broth microdilution method. So, AQs were tested for their toxicity and nontoxic doses of the chemicals were used. The results manifested that none of the chemicals were mutagenic for TA98 and TA100 strains both with and without metabolic activation enzymes (S9 mix). Purpurin and alizarin exhibited strong antimutagenic effects against 4-nitrophenylendiameine and 2-aminoflourene at all test doses (1000, 500 and 250 μg/plate) for TA98; and against sodium azide and 2-aminoanthracene for TA100. Alizarin showed the highest inhibition rate (93%) against sodium azide at a concentration of 1000 μg/plate. While 1,8-dihydroxy anthraquinone and quinizarin revealed strong antimutagenicity at 10000 μg/plate without S9 mix, they exhibited excellent antimutagenic action after addition of S9 enzymes for TA98 strain at all test doses. Similarly, 1,8-dihydroxy anthraquinone and quinizarin were moderate antimutagenic against sodium azide at all test doses without S9 mix, their antimutagenicity increased and they ameliorated the mutagenic action of 2-aminoanthracene by the addition of S9 for TA100. These two chemicals were strong antimutagenic against promutagens activated by S9 mix. Also it was defined that purpurin and alizarin have antimicrobial capacity against MRSA strains.
https://jrespharm.com/abstract.php?id=669
Alizarinquinizarinpurpurin1,8-dihydroxy anthraquinoneAmes testantimicrobial
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
217
223
10.12991/jrp.2019.127
649
Oxoaporphine alkaloids from the barks of platymitra siamensis craib (annonaceae) and their cytotoxicity against mcf-7 cancer cell line
Shieh Ting KAN
Mohamad Syahrizal AHMAD
Saripah Salbiah SYED ABDUL AZZIZ
Khalijah AWANG
Yuhanis MHD BAKRI
Mohd Azlan NAFIAH
Phirdaous ABBAS
Yumi Zuhanis Has-Yun HASHIM
Study on the chemical constituents of the dichloromethane (DCM) crude extract of Platymitra siamensis Craib has led to the isolation of four oxoaporphine alkaloids. The compounds were identified as liriodenine (1), O-methylmoschatoline (2), lysicamine (3) and cepharadione-A (4) which were isolated first time from this species. The structures of the isolated compounds were elucidated based on their spectral data (1H, 13C and LCMS) and reports in the literature. Here we observed that, only alkaloid 1 exhibited obvious cytotoxic effects against MCF-7 human breast cancer cells line with IC<sub>50</sub> value of 31.26 μM. This work is the first attempt on phytochemical and bioactivity study on the genus of Platymitra.
https://jrespharm.com/abstract.php?id=649
Platymitra siamensisAnnonaceaeoxoaporphine alkaloidsMCF-7cytotoxic activity
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
224
234
10.12991/jrp.2019.128
652
Zingiber officinale mitigates diazinon-induced testicular toxicity via suppression of oxidative stress and apoptosis in mice model
Saeed YAGHUBI BEKLAR
Maedeh HAMZEH
Abbasali KARIMPOUR
Fereshteh Talebpour AMIRI
Diazinon (DZN), as an organophosphate insecticide, induces testicular toxicity through oxidative stress. Ginger, a herbal medicine, has antioxidant and anti-inflammatory properties. This study was designed to investigate the effects of ginger against DZN-induced testicular toxicity. In this experimental study, thirty-two adult male mice were randomly divided into four groups. The control group; ginger group (100 mg/kg); DZN group (10 mg/kg); ginger + DZN group. Ginger and DZN received for 30 consecutive days by gavage, and DZN has been treated one hour after receiving ginger. Sperm parameters (including motility, sperm count, sperm viability rate and morphological sperm abnormalities), biochemical (MDA and GSH), testosterone levels, histopathological and immunohistochemical assays of testis were evaluated. The results revealed that treatment with DZN caused significant damage of sperm parameters (sperm motility, count, viability rate and abnormalities), increased oxidative stress (increased MDA and decreased GSH level), significant histopathological changes and decreased Johnsen’s Score, testosterone level and increased caspase-3 immunoreactivity. Ginger preserved sperm parameters and mitigated the toxic effects of DZN. Also, treatment with ginger significantly reduced caspase-3 immunoreactivity. Our results concluded that the ginger with anti-apoptotic and antioxidant activity and with scavenging free radicals protect testis against DZN-induced toxicity.
https://jrespharm.com/abstract.php?id=652
Organophosphate insecticidediazinongingeroxidative stresstesticular toxicitycaspase-3
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
235
241
10.12991/jrp.2019.129
654
Effect of aerial part and root extracts from ferulago mughlae peșmen and ferulago sandrasica peșmen & quézel growing in turkey on erectile dysfunction in streptozotocin-induced diabetic rats
Songül KARAKAYA
Fatmagül DELİMUSTAFAOĞLU-BOSTANLIK
Didem YILMAZ-ORAL
Serap GÜR
Ceyda Sibel KILIÇ
Ferulago species have been utilised since ancient times as antihelmentic, peptic, sedative and aphrodisiac, and as the seasoning in view of their special odors. In Turkish traditional medicine, the roots from some members of this genus are utilized as aphrodisiac, so we determined to show in vitro relaxant effect of F. mughlae Peșmen and F. sandrasica Peșmen & Quézel species extracts on corpus cavernosum (CC). A totality of 20 adult male Sprague-Dawley rats (diabetic and control groups) were induced by single intraperitoneal injection of 40 mg/kg of Streptozotocin. In vitro organ bath tests were carried out on rats to evaluate isometric pressure. Tissues were stretched with phenylephrine (Phe), and relaxation responses relevant to acetylcholine (ACh, 1 mM ), sodium nitroprusside (SNP 0.1 μM ) and electrical field stimulation (EFS, frequency 20 Hz) were gained. Whole these concentration-response curves were replicated with aqueous extracts obtained from the aerial parts and roots. The extracts were active in both groups. It was found that root extracts of F. mughlae and F. sandrasica yielded 97.80% and 97.55% relaxation. Among the extracts of roots (especially roots of F. mughlae) showed the best activity. On the other hand, lyophilized aqueous extracts of aerial part (especially F. sandrasica) showed the worst activity. Based on this findings, the roots of this species deserve further in vivo assessments for their aphrodisiac potential.
https://jrespharm.com/abstract.php?id=654
AphrodisiacsApiaceaeFerulagoerectile function
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
242
248
10.12991/jrp.2019.130
651
Water fraction of sonchus arvensis (linn.) leaves protects heart upon isoproterenol-induced myocardial infarction in rats and promotes survival of cardiomyocytes in vitro
Neng Fisheri KURNIATI
Elin Yulinah SUKANDAR
Rahmayati RUSNEDY
Dhyan Kusuma AYUNINGTYAS
Nova SULISKA
Yasushi FUJIO
The study aimed to evaluate the cardioprotective role of Sonchus arvensis (Linn.) leaves in isoproterenol
(ISO)-induced myocardial infarction (MI) in Wistar rats and in the survival of cardiomyocytes in vitro upon starvation
challenge. Fractions of an ethanolic extract of S. arvensis leaves (100 and 200 mg/kg bw) were administered orally to
Wistar rats (250–300 g) for 14 days. Isoproterenol 85 mg/kg bw was given at day 13 and 14. The rats were then sacrificed
on the next day. Serum activities of aspartate transferase (AST), alanine transferase (ALT), creatine kinase (CK), creatine
kinase-MB (CK-MB) and lactate dehydrogenase (LDH) were measured using standard commercial kits. The protective
effect of S. arvensis on damaged cardiomyocytes was investigated by examining the cell survival. Furthermore, the
Tumor Necrosis Factor-α (TNF-α) serum level of the MI rats was also determined. The results show that pretreatment
with n-hexane and ethyl acetate fractions of S. arvensis for a period of 14 days could not attenuate the increase of AST,
ALT, CK, CK-MB, and LDH levels upon isoproterenol administration. Moreover, viability of the fractions pretreatedcardiomyocytes
showed a cardiotoxic effect. However, pretreatment with the water fraction significantly attenuated the
increase of AST, ALT, CK, CK-MB, and LDH levels in isoproterenol-induced MI rats and increased the survival of
cardiomyocytes upon starvation challenge. The increase of the TNF-α level upon ISO administration in rats was not
observed in the water fraction pre-treatment group. In conclusion, the water fraction of Sonchus arvensis L. leaves at a
dose of 100 mg/kg bw protects the myocardium and exerts cardioprotective effects, probably by inhibiting TNF-α
production.
https://jrespharm.com/abstract.php?id=651
Sonchus arvensis L.isoproterenolmyocardial infarctioncardiomyocytesTNF-α.
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
249
258
10.12991/jrp.2019.131
655
Blood pressure lowering effect of scopoletin on oxidative stress-associated hypertensive rats
Armenia ARMENIA
Rahmat HIDAYAT
Meiliani MEILIANI
Yori YULIANDRA
Scopoletin is a coumarin derivative known for its antioxidant capacity. The present study was undertaken to investigate the blood pressure lowering effect of scopoletin in multiple models of hypertensive rats. To obtain animal models of hypertension, a number of 18 Wistar-Kyoto male rats were divided into two groups receiving a combination of oral prednisone and salt for 14 days (PN group, the endocrine hypertension model) while another half received the same inducers with an additional Nω-nitro-L-arginine methyl ester (L-NAME) for 2 days (PNL group, oxidative stress-associated hypertension model). The rats were anesthetized with propofol and subdivided into 3 groups receiving control, scopoletin 10 mg/kg, and tempol 100 μmol/kg. The systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial blood pressure (MAP) and heart rate (HR) were recorded for 120 minutes after a single dose of drug commencement. The serum concentration of nitric oxide (NO) was measured before and at the end of the experiment. The data were analyzed using two-way ANOVA followed by Tukey’s HSD with 95% confidence interval. The results showed that scopoletin decreased the SBP, DBP, and MAP of the rats significantly (p<0.05) without any significant effect on the animal HR (p>0.1). The concentration of NO in animals receiving scopoletin and tempol was greater as compared control, but there was no significant difference in blood NO between both hypertensive models (p>0.1). The study concludes that scopoletin is effective as blood pressure lowering agent on oxidative stress-associated hypertensive rats.
https://jrespharm.com/abstract.php?id=655
scopoletinantihypertensiveheart ratenitric oxideoxidative stressL-NAME
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
259
266
10.12991/jrp.2019.132
659
Scylla serrata forskal as natural source of glucosamine hydrochloride
Muammar FAWWAZ
Pipin VEMILIA
Indah MUTMAINNAH
Muzakkir BAITS
Glucosamine (GlcN) has great application in the food, cosmetic, pharmaceutical, and biomaterial areas; it is typically produced by hydrolysis in the exoskeletons of marine animals, one of the types of mud crab (Scylla serrata Forskal). Mud crab shells contain chitin and chitosan compounds which can be further derivatives for the production of GlcN HCl. The purpose of this study is to isolate and determine the level of GlcN HCl by hydrolysis of chitin and chitosan from mud crab shell. GlcN HCl was characterized by Fourier Transform Infra-Red (FT-IR) spectrophotometry, and its quantity was analyzed by UV-Vis spectrophotometry. Both methods used GlcN HCl as a standard for comparison and calculation of match factor (MF). The results of this study showed that the samples contain GlcN HCl either chitin or chitosan. FT-IR spectrum of chitin sample appears at wave number 1033 cm-1, 1532 cm-1, 3415 cm-1 whereas for chitosan at 1033 cm-1, 1532 cm-1, 3356 cm-1. Both sample spectrums showed vibration corresponding to ether (-O-), ethyl (CH2) and amine group (NH). The MF value of sample chitin and chitosan is 933 and 974, respectively; it shows that the resulting spectra are identical with the standard. The GlcN HCl level of sample chitin and chitosan was 553 and 993 mg/g, respectively. It can be concluded that the waste of mud crab shell has high potential as a natural source of GlcN HCl.
https://jrespharm.com/abstract.php?id=659
Chitinchitosanglucosamine HClmud crab shell
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
267
274
10.12991/jrp.2019.133
663
Modeling to predict the cytotoxicity of sio2 and tio2 nanoparticles
Samira JAFARI
Ali SHAYANFAR
The objective of the current study was to design a suitable model to predict the cytotoxicity induced by SiO<sub>2</sub> and TiO<sub>2</sub> nanoparticles in different conditions using computational models. To achieve this, we employed various statistical approaches such as linear regression, as well as artificial neural networks and support vector machine (non-linear models). The effective input parameters of the SiO<sub>2</sub> nanoparticles were particle size, particle concentration, and cell exposure time. In the case of the TiO<sub>2</sub> nanoparticles, the particle size and concentration served as input variables. Cell viability was considered the output response for both nanoparticles. The modeling was performed using both linear and non-linear methods. In addition, an external validation analysis was conducted to evaluate the predictability of the models by splitting the data into training and test data. The best models to predict cell viability were the models developed by artificial neural network. The results of this investigation indicate that non-linear models could be superior to linear models in predicting cell viability for SiO<sub>2</sub> and TiO<sub>2</sub> nanoparticles.
https://jrespharm.com/abstract.php?id=663
Artificial neural networkcytotoxicitymodelingnanoparticles
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
275
283
10.12991/jrp.2019.134
674
The influence of melatonin supplementation against aluminum-induced toxicity in brains of male rats
Ömür KARABULUT BULAN
Bertan Boran BAYRAK
Güner SARIKAYA-ÜNAL
Refiye YANARDAĞ
Aluminum (Al), an ubiquitous element in nature, enters the body primarily through gastrointestinal tract, respiratory system and skin. Being a powerful neurotoxin for human brain, Al was reported to be involved in the etiology of Alzheimer's disease due to its easy access and accumulation in the central nervous system. Melatonin (Mel) is a tryptophan-derived neurohormone in animals and plants, and produced in the pineal gland of all mammalian species. The present study examines the effects of Mel on Al-induced oxidative stress, inflammation, tissue factor production and brain damage in rat brain. Wistar albino rats were divided into four groups. Group I: control animals; Group II: rats injected with 10 mg/kg Mel; Group III: rats injected with 5 mg/kg Al<sub>2</sub>(SO<sub>4</sub>)3; and Group IV: rats injected combination of Al and Mel (5 mg/kg Al<sub>2</sub>(SO<sub>4</sub>)3 and 10 mg/kg Mel). Animals were injected three times a week for one month. At the end of the month, rats were sacrificed, their brains were removed. It was found that lipid peroxidation, protein carbonyl, advanced oxidation protein products, hydroxyproline levels, tissue factor, catalase, superoxide dismutase, glutathione peroxidase, glutathione reductase, myeloperoxidase, acetylcholine esterase, alkaline phosphatase, acid phosphatase and glucose-6-phosphate dehydrogenase activities were increased, while paraoxonase, arylesterase, sodium potassium ATPase activities and glutathione levels were decreased in the Al-treated group. Mel treatment reversed these changes by demonstrating significant antioxidant effects. Results indicated that Mel has potential therapeutic value against Al-induced oxidative stress in the rat brain tissue and these effects may be related to its antioxidant activities.
https://jrespharm.com/abstract.php?id=674
Aluminummelatoninbrainoxidative stresstissue factor levels
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
284
291
10.12991/jrp.2019.135
665
Peruvian pharmacist employment and wage: gender, university and type of job influences
Luz CHACALTANA
Josefa PARI
Pompeyo CUBA
Luzmila HERNANDEZ
Juana LA ROSA
Cecilia SOLANO
Melisa QUISPE
Alfredo OYOLA
Wage is a key element for the performance of the health professional. Because of that, an observational study was carried out based on the secondary analysis of the main results from the "National Survey of University Graduates and Universities (NSUGU), 2014" to identify the conditioning factors of inequality in accessing to the labor market and low wage of Peruvian pharmacists. Chi square, crude Odds Ratio (cOR) and adjusted Odds Ratio (aOR) with 95% confidence interval were calculated. In the bivariate analysis the work not related to pharmaceutical training exposed pharmacists to almost four and a half times the risk of a remuneration lower than 1000 PEN compared to those who had a job related to their professional training (cOR=4.473) and it increased to six times in the multivariate analysis (cOR=5.938). Women were less likely to have this remuneration than men (cOR = 0.544) and maintained this characteristic in the multivariate analysis. The graduation from a public university was a protective factor of remuneration lower than 1000 PEN in the multivariate analysis, but not in the bivariate analysis. Women and graduates from public universities are more likely to be unemployed, while exposure to low income is measured by occupation not related to professional training.
https://jrespharm.com/abstract.php?id=665
Pharmacystwageemploymentinequality
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
292
297
10.12991/jrp.2019.136
662
The percentage of depressive symptoms in patients with type 2 diabetes mellitus in m djamil general hospital padang, indonesia
Eva DECROLI
Alexander KAM
Dwisari DILLASAMOLA
The objectives of this study are to find the percentage of depressive symptoms and the most appeared clinical manifestation of depressive symptoms. A total of 2016 patient with type 2 diabetes from M Djamil General Hospital had fulfilled the questionnaire we administered. Demographic and clinical data were determined from the patient’s medical records. Depressive symptoms defined by The Center for Epidemiologic Studies Depression Scale-Revised (CESD-R) score of 16 or higher. CESD-R consisted of nine symptoms group and a 20-item questionnaire. These symptoms groups in patients with depressive symptoms will be counted. Patients with depressive symptoms were grouped based on a type of diabetic medication they consumed (diet only, oral antidiabetic, and insulin) and diabetic complication. From 2016 patients participated in this study, we found 235 (11.7%) patients were having depressive symptoms. The most appeared clinical manifestation in 235 patients with depressive symptoms is fatigue (88.08%), loss of interest (52.34%), sadness (41.7%), poor concentration (40.42%), and agitation (23.83%). There are more depressive symptoms in patients consuming oral antidiabetic drug than patients using insulin and diet only (70.2 vs. 28.1 vs 1.7%). More depressive symptoms are also found in patients with diabetic nephropathy than patients with diabetic neuropathy and heart disease (52.8 vs. 27.7 vs. 19.6%). These findings showed that there are many depressive symptoms in patients with T2DM, and some of most appeared clinical manifestation in depressive symptoms should be considered.
https://jrespharm.com/abstract.php?id=662
Diabetesdepressive symptomsoral antidiabeticinsulinclinical manifestation
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
298
303
10.12991/jrp.2019.137
667
Patient counseling, risk factors and comorbidity assessment in diabetic foot ulcer
Smithamol SUNNY
Swathy PRADEEP
Anita ANN SUNNY
Rama PARTHASARATHY
Shanmugasundaram RAJESHKUMAR
Sankar VEINTRAMUTHU
Diabetic foot ulcer usually develops due to lack of knowledge and awareness regarding the consequences of the disease progression and poor foot care among diabetics. The objective of the study is to enhance knowledge, attitude and clinical practice among diabetic foot ulcer patients through pharmacist counseling, and to assist physician in the selection of cost effective antibiotics. Data on the disease condition such as duration of illness, type of diabetes, category of infections, classification of foot ulcer, risk factors, comorbidities and antibiotics used were collected and analyzed. Additionally, the details of culture sensitivity report for sensitive and resistant microorganisms with respect to antibiotics were recorded. Appropriate patient education on diabetic foot ulcer helps to improve their knowledge, attitude, and practice significantly. The commonest microbial isolates identified in diabetic foot ulcer patients were Klebsiella pneumonia, Pseudomonas aeruginosa and Staphylococcus aureus. Culture sensitive drugs found were meropenem, amoxicillin with clavulanic acid, clindamycin and the resistant drugs were cefepime, levofloxacin and penicillin.
https://jrespharm.com/abstract.php?id=667
Diabetic foot ulcerpatient counselingrisk factorscomorbidityculture sensitivity
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
304
314
10.12991/jrp.2019.138
666
Comorbidities and its relation to performance status and estimated survival rate among cancer patients
Sankar VEINTRAMUTHU
Rama PARTHASARATHY
Sangeetha MATHEW
Subash JOHN
Vignesh KANDA KUMAR
Prudence Attilade RODRIGUES
Many studies report the presence of comorbidities, which have a consequential impact on the management and survival of cancer patients. The aim of the present study is to assess the prevalence of comorbidities and their influence on overall management, estimated survival, and performance of cancer patients. A hospital based prospective study was conducted at a multi-specialty teaching hospital for a period of 10 months. Out of a sample of 140 cancer patients, 70 were diagnosed with comorbidities. Estimated survival rates and comorbidity scores were assessed using the Charlson Comorbidity Index (CCI). Performance scores were observed using the Eastern Cooperative Oncology Group (ECOG) performance score. CCI and performance score were statistically analyzed by SPSS Version 19. Hypertension (40%) was the leading comorbidity, followed by diabetes (25.71%). Those women with high (>5) CCI score (57.14%, p=0.04) had significantly decreased estimated survival rates of less than or equal to 2 months compared to those having less than (<) 2 CCI score and who reached estimated survival rates of more than or equal to 7 months. The performance score (2.065±0.81) was significantly (P=0.0001) increased after treatment of the comorbidity compared to the performance score (1.125±1.27) of patients without comorbidity. Only alkylating agents (cyclophosphamide p=0.003, Carboplatin & Oxaliplatin p= 0.007, Cisplatin p= 0.0001), and folic acid analogues (Leucovorin p=0.01) showed significant differences in the management of cancer between groups. This study suggests that breast cancer is associated with increased comorbidity burden compared to other types of cancer. Also, comorbidity is associated with overall decreased estimated survival rate and performance status among cancer patients.
https://jrespharm.com/abstract.php?id=666
Cancercomorbidityestimated survival ratetreatment patternperformance statusCCIECOG
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
315
325
10.12991/jrp.2019.139
672
Dissolution enhancement and physicochemical characterization of fenofibric acid in surface solid dispersion with croscarmellose sodium
Yulias Ninik WINDRIYATI
Yeyet Cahyati SUMIRTAPURA
Jessie Sofia PAMUDJI
The dissolution enhancement of the water-insoluble drug fenofibric acid (FA) was conducted by the surface solid dispersion (SSD) technique with croscarmellose sodium (CS) as a carrier. The SSD formulations of FA were prepared by the solvent evaporation method in three different drug-to-carrier weight ratios, evaluated for the dissolutions, and compared to the physical mixtures (PMs). The optimum SSD formulation and its corresponding PM were characterized by Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Thermal Analysis (DTA), and Fourier Transform Infrared Spectroscopy (FTIR) and were compressed into tablets to evaluate the dissolution after compression. The best dissolution was obtained from the SSD 1:1. The recrystallization of FA in the SSD preparation could change the crystal habit of FA and deposited it on the surface of CS. İn addition, there was no chemical interaction observable between both FA and CS in the SSD formulation. No chemical interaction between FA and CS in the SSD. However, a slight reduction was noticed in the crystallinity of FA if compared to that of the pure drug. This study showed that the SSD formulation had the best dissolution compared to the PM, the conventional direct compression, and the reference formulation of FA in its commercial tablets. The SSD preparation with CS could enhance the dissolution of FA from its tablet dosage form.
https://jrespharm.com/abstract.php?id=672
Fenofibric acidsurface solid dispersioncroscarmellose sodiumdissolutionphysicochemical characterization
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
326
335
10.12991/jrp.2019.140
688
In vitro bioavailability studies on phytochemical profile and antioxidant activity potential of clematis viticella l.
Esra ACAR-ŞAH
Engin CELEP
Erdem Yeşilada
Since biotransformation processes generally affect the biological activities of phytochemical compounds, bioavailability is one of the primary steps in determining the potency of the activity. Previous studies have shown that in vitro antioxidant capacity of phytochemicals cannot completely reflect real health benefits. Clematis species (Ranunculaceae) are used to eliminate the symptoms of many diseases including particularly in the treatment of rheumatic diseases in Turkey, however the number of studies conducted is limited. In the light of this information, the total phytochemical profile of the extract of aerial parts of C. viticella prepared with 80% methanol and the gastrointestinal digestion products and the antioxidant activity profile were evaluated by subjecting them to the in vitro simulation model of the human digestive tract in the study. It was observed that both total phytochemical content and antioxidant activity decreased after simulated human digestion. Moreover, this study was shown potential bioaccessibility and bioavailability of total phenol, phenolic acid, flavonoid, and saponin content found in the aerial parts of Clematis viticella were reduced. Consequently, these indicate that it can result from the complicated interaction of compounds in the plant matrix in an in vitro simulated human digestion.
https://jrespharm.com/abstract.php?id=688
Clematis viticella L.Ranunculaceaephenolic profileantioxidant activityin vitro digestion simulation modelbioavailabilitybioaccessibility
Marmara Üniversitesi
Journal of Research in Pharmacy
2630-6344
2019
23
2
336
343
10.12991/jrp.2019.141
608
Biological activity and chemical composition of the essential oil of nepeta cataria l.
Behnam ASHRAFI
Parvin RAMAK
Behrouz EZATPOUR
Gholam Reza TALEI
In this study, chemical composition, antioxidant and antimicrobial activity of the essential oil of Nepeta cataria L., a native plant that grows in Lorestan region of Iran, were studied. Chemical constituents of the essential oil were identified by means of gas chromatography/mass spectrometry (GC/MS) and the relative content of each constituent was determined by area normalization. Disc diffusion and broth microdilution assays were used for in vitro antimicrobial screening. Antioxidant activity was employed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging. The predominant bioactive ingredients with high percentage in N. Cataria essential oil was 4a-α, 7-α, 7a-β-Nepetalactone (53.87%). The essential oil’s IC<sub>50</sub> value of 80.62 μg / mL in the DPPH assay, could be regarded as its strong antioxidant potential. The antibacterial activities of the essential oil were screened and compared against dozen important human pathogens. The essential oil showed good antibacterial activity, especially on Salmonella spp.. The biggest diameters of inhibition zones (29 mm) was recorded for Salmonella typhi and Salmonella paratyphi A showed the lowest MIC (160 μg / mL).
https://jrespharm.com/abstract.php?id=608
Antimicrobialantioxidant, Nepeta cataria L.essential oil