Journal of Applied Pharmaceutical Science (JAPS)
Permanent URI for this collection
Editor: Dr. Khalid Akhter Ansari
ISSN: 2231-3354; (Print)
Frequency: 12 issues a year
Language: Englishh
An Official Publication of Open Science Publishers
Open Access Peer-reviewed journal
Web site: https://www.japsonline.com/
Browse
Browsing Journal of Applied Pharmaceutical Science (JAPS) by Title
Now showing 1 - 20 of 2398
Results Per Page
Sort Options
Item 14, 15-epoxygeranylgeraniol and extracts isolated from Pterodon emarginatus Vog. fruits: antitumor activity on glioblastoma cells.(2012-09) Hansen, Daiane; Nakahata, Adriana Miti; Haraguchi, Mitsue; Okamoto, Oswaldo Keith; Goncalez, Edlayne; Alonso, AntonioPlant-derived substances have traditionally played important roles in the treatment of human diseases, including of great significance to cancer therapy. Plants of the genus Pterodon (Fabaceae, Leguminosae), commonly known as ‘sucupira’, are disseminated throughout the central region of Brazil and have been used frequently in popular medicine. In recent years, interest in these plants has increased considerably. The biological effects of their extracts and pure metabolites have been investigated in several experimental models in vivo and in vitro. Until the present day, the antitumor effect of Pterodon plants on brain tumors is unknown. Therefore, the aim of this work was to investigate the action of P. emarginatus Vogel extracts and its fractions on glioblastoma cells. The hexane (HE), dichloromethane (DE) and ethanol (EE) extracts were obtained from seeds powder in each solvent. The diterpene 14,15-epoxygeranylgeraniol was obtained from HE fractionation. For tumorigenic assays, the extracts and fractions were added to U87MG, a human glioblastoma cells line. The cell viability assay showed that the proliferation of U87MG was inhibited by both extracts and the 14,15- epoxygeranylgeraniol. Further trials in vivo will help to confirm these results, and may contribute to generate natural compounds for the treatment of this type of cancer.Item 15N-NMR spectroscopic studies and investigation of spectral data property relationships of proton pump inhibitors(Open Science Publishers LLP, 2019-06) NC, Bhanumathi Devi; N., Someswara Rao; Ghosh, Tamal; Mukerjee, AlokIn this study, the relationships between 15N-NMR and 13C-NMR chemical shifts of omeprazole, lansoprazole, ilaprazole,pantoprazole, and rabeprazole and their physicochemical and pharmacokinetic properties, namely, pKa, half-life,tmax, logP, and protein binding were investigated. This study also presents the first report of 15N-NMR spectroscopicstudies of lansoprazole, pantoprazole, and ilaprazole. It was found that 15N-NMR chemical shifts of the doubly bondedbenzimidazole nitrogen of proton pump inhibitors showed correlation with pKa2, protein binding and logP, while 15NNMR chemical shifts of the pyridine nitrogen correlate with protein binding and tmax. Sum of 15N-NMR chemical shiftsand sum of 13C-NMR chemical shifts, both, exhibit correlation with half-life, logP, and tmax. The sum of 13C chemicalshifts of the pyridine moiety exhibits correlation with pKa1, while the sum of 13C chemical shifts of the benzimidazolemoiety exhibits correlation with half-life. NMR chemical shifts may, hence, be useful as molecular descriptors in thedevelopment of Quantitative Structure/Spectral Data Property Relationship models.Item 2, 3, 7, 8-tetrachloro-dibenzo-p-dioxin induced testicular toxicity in rats and the protective effect of quercetin: Biochemical, histopathological and immunohistochemical studies.(2015-01) El-Gerbed, Mohamed S A; El-Saad, Ahmed M Abu; Haussein, Abdullah BedeerHumans and animals are most sensitive to toxicant exposure during development. Dioxin, as an endocrine disruptor, is known to impair testicular functions and fertility. The present study was carried out to investigate the effects of quercetin on TCDD-induced toxicity in the testicular tissue of rats. Forty male albino rats were randomly divided into four groups (n = 10/group). Group I represent the control group; Group II administrated TCDD (27.5 μg/kg) via gavage for four week; Group III received quercetin (20 mg/kg bw.) Via gavage before TCDD administration; Group IV received quercetin alone (20 mg/kg bw). Biochemical markers included levels of testicular malondialdehyde formation and reduced glutathione as well as monitoring the activities of testicular superoxide dismutase, catalase, glutathione peroxidase, glutathione S-transferase were studied. Also, serum hormonal profiles of luteinizing hormone and testosterone were reported. Our results show that administration of TCDD induces testicular damage concerning oxidative stress parameters, serum hormone level and sperm parameters. In addition, the microscopic structures of the testis, including histological and immunohistochemical studies were evaluated. Exposure to TCDD induces histopathological changes in rats testis including degeneration of seminiferous tubules, tubular necrosis, intratubular vacuolization, widened lumen and deshaped germ cells. Marked increase of apoptotic activity was observed. Also, our results clearly demonstrate the ameliorative potential of quercetin in dioxin induced testicular damage.Item 2, 4-Di-tert-butylphenol, the bioactive compound produced by Streptomyces sp. KB1.(2015-11) Chawawisit, Kittisak; Bhoopong, Phuangthip; Phupong, Worrapong; Lertcanawanichakul, MonthonStreptomyces sp. KB1(TISTR 2304), identified by 16S rDNA gene, was collected from the air sample at Ao-nang, Krabi province, Thailand and deposited in the GeneBank database (accession number KF939581.1). It could produce bioactive compounds and excrete into liquid culture medium within 4 days of incubation period at 30 °C, 200 rounds per minute in shaking incubator. Bioactive compounds in culture broth supernatant were extracted with 3-times of ethyl acetate (EA), evaporated by rotary evaporator at 45 °C under reduced pressure, purified by silica gel column chromatography and eluted by gradient solvent system of ethyl acetate: hexane at ratio of 1:9, 3:7, 4:6, 6:4 and 10:0, v/v. Eight pooled fractions were obtained, name PF1 - PF8, from basis of their TLC profile. Only PF4 displayed as purified active compound which showed anti-methicillin resistant Staphylococcus aureus (MRSA) activity. The PF4 was predicted as 2, 4-Di-tert-butylphenol (C14H22O) with molecular weight 206.2.Item 2-Methoxy-1,4-Naphthoquinone (MNQ) Suppresses Protein Kinase C βI, δ, and ζ Expression in Raji Cells.(2015-08) Yew, Wong Teck; Kitson, Liew; Hock, Anthony Ho Siong; Chiew, Gan Seng; Mooi, Lim YangProtein Kinase C (PKC) is widely documented to be involved in the regulation of cancer cell growth, proliferation, survival, inflammation and apoptosis. This study evaluates the capability of 2-Methoxy-1,4- Naphthoquinone (MNQ) in regulating PMA-induced PKC expression in human Burkitt’s lymphoma cell line (Raji cells). MNQ exhibited stronger anti-tumour-promoting activity than genistein based on the inhibitory assay of Epstein-Barr virus (EBV) activation. The IC50 values attained were 2.92 and 7.40 μM, respectively. The suppressive effects of MNQ on PKC expression was determined by using the PepTag® non-radioactive detection of PKC assay. The IC50 values achieved for staurosporine and rottlerin (standard control), and MNQ were 0.01, 6.38, and 13.13 μM, respectively. These preliminary results indicate that MNQ specifically suppressed the expression of PKC βI, δ, and ζ in a concentration-dependent manner in Raji cells.Item 3D QSAR and docking studies on benzoylsulfonohydrazides as histone acetyltransferase KAT6A inhibitors(Open Science Publishers LLP, 2020-05) MD., Muzaffar-Ur-Rehman; Akbar, Syed; Bahazeq, Asra AliSixty-one analogs of benzoylsulfonohydrazides were subjected to 3D QSAR studies using CoMFA and CoMSIAtechniques followed by docking studies to develop a correlation of the structure with their respective activities. Thegenerated model had shown good predictability and the contour analysis followed by docking study has provided aninsight to develop new inhibitors. The cross-validation values corresponding to CoMFA and COMSIA were observedto be within the acceptable criterion (q2 > 0.5). The docking analysis of the best active compound shown was −41.81kcal/mol. From the obtained analysis results of CoMFA as well as CoMSIA, the data can be useful to develop morepotent histone acetyltransferase inhibitors.Item 3D QSAR and Pharmacophore Modelling on Chalcones as Antileishmanial Agents potential Trypanothione reductase Inhibitors.(2013-12) Desai, Sujit Arun; Kumbhar, Santosh Sahedeo; Katti, Vishal Shankar; Choudhari, Prafulla Balkrishna; Bhatia, Manish SudeshChalcones is an important auxiliary having various important clinical applications. A series of Chalcones as antileishmanial agents by were reported. Three dimensional quantitative structure-activity relationship (3DQSAR), including, were performed to elucidate the 3D structural features which are important for the antileishmanial activity. The results of 3D QSAR model (q2 = 0.8100, r2 = 0.9355,) exhibited the highly degree of statistical significance and good predictive ability. The results generated 3D QSAR can provide important information about the structural characteristics which are contributors of the inhibitory potency of chalcones. In addition, docking analysis and pharmacophore mapping was applied to identify the binding modes between the ligands and the Trypanothione reductase and structural features of the ligands which are important for the biological activity of the molecules. The information obtained from this study could provide vital information for future development of potent instructions for the further development of potent antileishmanial agents as trypanothione reductase inhibitors.Item 3D-QSAR, molecular docking and dynamics simulation of difluorophenol pyridine derivatives as RSK2 inhibitor(Open Science Publishers LLP, 2019-06) Arba, Muhammad; Hamzah, Azali; Ombe, Sabarudin; Armid, Alrum; Ida, UsmanGiven the increasing role of P90 Ribosomal S6 Kinase 2 (RSK2) as an anticancer drug target, we performed3D-Quantitative structure–activity relationship, including comparative molecular field analysis (CoMFA) andcomparative molecular similarity indices analysis (CoMSIA) on difluorophenol pyridine derivatives as the inhibitorof RSK2. CoMFA model with q2 of 0.597 and R2 of 0.993, while CoMSIA model with q2 of 0.563 and R2 of 0.993,were obtained. The predictive ability of both models was assured using a test set compound with R2pred values of 0.996each. Using the validated models, novel compound was proposed and its interaction with RSK2 was investigatedemploying molecular docking and molecular dynamics simulation of 50 ns. Furthermore, molecular-mechanicsPoisson–Boltzmann surface area calculation was performed. The result showed that the newly designed compoundhas a comparable binding free energy with the known RSK2 inhibitor, indicating its potential as a new RSK2 inhibitor.Item 3D-QSAR, molecular docking, and dynamics simulation of quinazoline–phosphoramidate mustard conjugates as EGFR inhibitor(Open Science Publishers LLP, 2019-01) Ruslin, Ruslin; Amelia, Resky; Yamin, Yamin; Megantara, Sandra; Chun Wu; Arba, MuhammadTo develop novel and more potent quinazoline–phosphoramidate mustard conjugates as epidermal growth factorreceptor (EGFR) inhibitor, three-dimensional quantitative structure-activity relationship [comparative molecularfield analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA)] combined with moleculardocking were performed. A series of 13 compounds in the training set gave q2 values of 0.577 and 0.537, as well as r2values of 0.926 and 0.921 for CoMFA and CoMSIA models, respectively. The contour maps that were produced by theCoMFA and CoMSIA models revealed that steric, electrostatic, and hydrophobic fields were crucial in the inhibitoryactivity of quinazoline–phosphoramidate derivatives. Based on the CoMFA and CoMSIA models, several novel EGFRinhibitors were designed, which established crucial interactions at the ligand binding domain of EGFR. Nearly, 100ns MD simulation indicated the stability of the designed compounds at 100 ns, while molecular mechanics-PoissonBoltzmann surface area calculation showed that the designed compound had a higher affinity than that of the parentcompound.Item 3’,4’-Dimethoxy quercetin, a flavonol compound isolated from Kalanchoe Pinnata.(2013-01) Darmawan, Akhmad; Megawati; Fajriah, SofaFrom methanol extract of Kalanchoe pinnata (Lam.) Pers. leaves, a flavonol compound has been isolated. Fractionation of the methanol extract with ethyl acetate, followed by ethyl acetate fraction purification using column chromatography method with ethyl acetate : n-hexane as mobile phase gave a yellow crystal compound (A). Further analysis using 1D- and 2D-nuclear magnetic resonance (NMR), confirmed with mass spectrometer (LC-MS), compound A identified as 3’,4’-dimethoxy quercetin.Item Ability of scavenging free radicals and preventing lipid peroxidation of some phenols and ascorbic acid.(2015-08) Badanai, Jaqueline; Silva, Celi; Martins, Denise; Antunes, Dulce; Miguel, Maria GraçaThe capacity for scavenging free radicals and preventing lipid peroxidation of gallic, caffeic, and p-coumaric acids, thymol, eugenol and ascorbic acid were evaluated. The capacity for scavenging DPPH free radicals were performed in ethanol 96% and ethanol 70%. In the same assay, the activity estimation was followed at 10, 20 and 30 minutes. In this assay, eugenol presented the best activity (IC50 ranging from 2.10 mg/mL to 9.74 mg/mL. In the opposite site, p-coumaric had the lowest activity, in which the IC50 values were not possible to determine. Generally, 10 minutes of reaction provided lower scavenging activities than 30 minutes. The sole exception was ascorbic acid in which the activities were independent on the time of reaction. Ascorbic acid, eugenol and thymol possessed higher ability for scavenging DPPH free radicals in ethanol 70% than in ethanol 96%. Gallic and p-coumaric acids as well as thymol revealed to be the best scavengers of ABTS+ free radicals in contrast to ascorbic acid. The capacity for preventing lipid peroxidation was dependent on the concentration of samples. The assay showed that higher concentrations of gallic acid, thymol and p-coumaric acid added to sunflower oil (from 0.3 to 0.6%) induced higher lipid peroxidation with higher peroxide values. In contrast, increasing the percentages of caffeic acid and eugenol induced lower peroxidation of the sunflower oil. The percentage of samples added to this fat did not influence the index of p-anisidine. In this test, gallic acid had the best capacity for preventing the formation of 2,4-dienals and 2-alkenals decadienals able to react with p-anisidine.Item Accelerated stability and antimicrobial sensitivity studies of amoxicillin dry suspensions marketed in Bangladesh.(2011-11) Haider, Syed Shabbir; Nasrin, Nishat; Apu, Apurba Sarker; Asaduzzaman, MuhammadSince its introduction, amoxicillin dry suspension has been the mainstay for the antibacterial therapy for paediatric patients. But use of substandard preparation of antibiotic is one of the most important causes of microbial resistance. The present study has been carried out to evaluate the quality and stability status of 10 marketed amoxicillin dry suspensions of Bangladesh. All the brands were analyzed for their potency using chemical and microbiological methods described in the United States Pharmacopoeia and British Pharmacopoeia. Potency determination was done at three controlled temperatures - refrigerated, room and elevated (40C) showed that two samples were over potent but one sample was substandard out of the 10 samples. The initial potencies of the two samples were within USP range when freshly reconstituted but after 7 days, at room temperature, potencies deteriorated and came down to 90%. In refrigerated condition, all the samples remained in good condition and at 40C, a considerable loss of potencies in all the samples were observed. Results of microbiological assay also support the results of chemical assay. The study emphasizes the necessity of routine inspection, monitoring and evaluation of quality of formulations containing amoxicillin dry syrup.Item Access to Essential Medicines in Ghana: A Survey of Availability of Children’s Medicines in Medicine Outlets in the Ashanti Region.(2016-10) Frimpong, Grace; Ofori-Kwakye, KwabenaThe objective of this study was to assess the availability of 42 children’s essential medicines contained in the Standard Treatment Guidelines (STG) of Ghana in the 27 districts of Ashanti Region. Five hundred medicine outlets comprising of hospitals/health centers/clinics, community pharmacies and chemical shops were surveyed using a validated structured questionnaire. The results were analysed and the availability of the 42 medicines in each district was determined. The average availability of children’s medicines across the region was 41.3% (range: 26.4-52%), with the Kumasi Metropolis (KM) and Bosome Freho (BF) district having the highest and lowest availabilities, respectively. Six (14.3%) of the medicines, omeprazole, tinidazole, furosemide and spironolactone suspensions, and praziquantel and thiabendazole syrups had zero availability in the Region while ferrous sulphate syrup (95%), albendazole suspension (90%) and paracetamol syrup (88.8%) had the highest availabilities. Three hundred and twenty three different formulations of the 42 medicines were identified with foreign and local manufacturers accounting for 198 (61.3%) and 125 (38.7%) formulations, respectively. India (38.7%) and United Kingdom (35.5%) were the major foreign manufacturers. The duration of stock-outs was shorter for private than public/government facilities and generally ranged from up to one week (68.4 %) to over one month (3%). Reasons for the low or non-availability of children’s medicines included the lack of funds, non-prescription by physicians, unavailability of medicines at wholesalers and lack of awareness of medicine outlets staff.Item Acetylcholinesterase: Inhibitory activity of some Indonesian vegetables and fraction of selected plants(Open Science Publishers LLP, 2020-01) Nuria, Maulita Cut; Suganda, Asep Gana; Sukandar, Elin Yulinah; Insanu, MuhamadDementia is a global health problem that requires severe treatment. People with dementia who consume vegetablesevery day can reduce the risk of dementia. Alzheimer’s is one of the diseases that are characterized by dementia, whichresults in decreased neurotransmitter acetylcholine. This study was to investigate the acetylcholinesterase (AChE)enzyme inhibitory activity of various vegetables that are widely used by Indonesian Sundanese and Javanese ethnics. Inthis study, total phenolic and flavonoid content were analyzed for the determination of active compounds of the extracts.Ethanol extracts of 13 vegetables have been tested for AChE inhibitory activity using Ellman's colorimetric method in96-well plate. Four types of extracts (Cosmos caudatus, Nasturtium officinale, Nothopanax fruticosus, and Ocimumamericanum) had higher total phenolic and flavonoid content than other extracts. Vegetable extracts that had IC50 valuesof less than 1,000 µg/ml were C. caudatus and O. americanum. Both of these extracts were partitioned with n-hexaneand water. The IC50 values of water fraction of C. caudatus and n-hexane fraction of O. americanum were 325.0 ± 18.3and 374.4 ± 42.1 µg/ml, respectively. These results showed that fractions had a potential inhibitor of AChE, and thechemical components (phenolic, flavonoid, and terpenoid) can be isolated to find the active compound.Item Acid and Alkaline Hydrolysis Studies of Stevioside and Rebaudioside A.(2011-10) Chaturvedula, Venkata Sai Prakash; Prakash, IndraHydrolysis studies of the two diterpene glycosides stevioside and rebaudioside A that were isolated from Stevia rebaudiana were performed using acid and alkaline conditions. Acid hydrolysis was carried out using H2SO4 whereas alkaline hydrolysis was performed using NaOH. Using these methods, partial hydrolyzed glycosides of stevioside and rebaudioside A and their sugar residues were identified from the alkaline and acid hydrolysis studies respectively. The structures of the acid and alkaline hydrolysis products were achieved on the basis of extensive NMR and high resolution mass spectral data, and in comparison with the data reported in the literature as well as TLC comparison with their corresponding standard compounds.Item Acrylic hydrogels modified with bee pollen for biomedical applications.(2015-11) Tyliszczak, Bożena; Walczyk, Dorota; Wilczyński, SławomirThe focus of this paper is to present the effect of bee pollen on the structure and properties of acrylic hydrogels, often used as materials for wound dressings. Honey, propolis and bee pollen have been very well known for their extraordinary healing and medical properties for thousands of years. Ancient Egyptians, Greeks and Romans have reportedly used bee pollen as a drug, especially for a number of skin diseases and lesions. Acrylic hydrogels are, on the other hand, rather recently discovered materials used for novel wound dressings. The idea of our research was to combine a synthetic polymer matrix with bee pollen, in order to obtain innovative materials which could be used as wound dressings exhibiting new properties. The obtained acrylic hydrogels containing bee pollen were investigated towards swelling ability in distilled water and different fluids, including pseudo-extracellular fluid, simulated body fluid and Ringer’s solution. Moreover, incubation in water and simulated body fluids (SBF) and Ringer’s solution was carried out. The morphologies of bee pollen and obtained acrylic hydrogels modified with bee pollen were characterized by means of scanning electron microscopy (SEM). The chemical structure of the polymer matrix was confirmed by ATR-FT-IR spectra.Item Activated charcoal for oral medicinal purposes: Is it really activated.(2015-10) ZAINI Muhammad, Abbas AHMAD; MOHAMAD, Nur AtikaItem An active learning assignment to improve pharmacy students’ knowledge of herbal medicine.(2015-03) AbouZid, SamehMedicinal plant courses represent an essential part of the applied sciences component in the curriculum of pharmacy education in Egypt. One of the intended learning outcomes of these courses is to demonstrate knowledge and understanding in the theory and practice of herbal medicine. The aim of the current work was to improve pharmacy students' knowledge and understanding of the herbs used for medicinal purposes. The students, in groups, conducted direct interviews with staff members of the university using a semi-structured questionnaire. The questionnaire included questions about medicinal herbs used by the participants, purpose for use, method of preparation, and sources to obtain. The educational impact of this assignment was evaluated by a questionnaire distributed to the participated students. The majority of students agreed that carrying out the assignment helped them in improving their knowledge and understudying about medicinal herbs. Moreover, their oral communications skills were improved. The described active-learning assignment offered a great opportunity for the students to improve their communication skills and to gain knowledge about the commonly used medicinal herbs in their community.Item The Activity of Cedar Leaf oil Vapor against Respiratory Viruses: Practical Applications.(2013-11) Selvarani, Vimalanathan; James, HudsonRespiratory viruses continue to cause frequent acute and chronic infections, for which few satisfactory treatments are available. Some essential oils possess antiviral properties, but these have usually been tested as liquids, which have limited applications. In this study the vapor of cedar leaf oil (CLO vapor) was evaluated for antiviral activity, in addition to its possible anti-inflammatory activity. The viruses tested, Influenza viruses, Rhinovirus, Adenovirus, and Herpes simplex viruses 1 and 2, in the form of dried films, were all inactivated by exposure to CLO vapor. In assays for influenza viral hemagglutinin (HA) the HA activity was inhibited by CLO vapor. Exposure of human lung epithelial cell monolayers to the vapor showed inhibition of rhinovirus virus-induced cytokine IL-6, but the cells themselves were not adversely affected by short exposure to the vapor. However the two major volatile components of CLO, thujone and - pinene, did not show activity against influenza viral infectivity or hemagglutinin, indicating possible synergistic effects of the whole vapor. We conclude that CLO vapor has potential applications in the control of viral respiratory infections.Item Activity of Oxalis barrelieri aqueous extract on rat secretory diarrhea and intestine transit.(2015-01) Tagne, Michel Archange Fokam; Kamgang, René; Noubissi, Paul Aimé; Oyono, Jean-Louis EssameOxalis barrelieri is used in the folk medicine for diarrhea treatment. The effects of the aqueous extract of Oxalis barrelieri on castor oil-induced diarrhea and intestine transit were investigated in rats. To induce the diarrhea and enteropooling, animals orally received castor oil (1 mL/100 g bw). Each rat received 30 minutes after, one of the single oral doses of O. barrelieri aqueous extract: 0, 25, 50, 100, 200 and 250 mg/kg bw or loperamide (5 mg/kg bw). The frequency and the total diarrheal weight for diarrhea and the intestine content for enteropooling were measured. To value the extract effect on intestine transit, normal rats received or not acetylcholine 0.1 mg/kg bw i.p. and then different dose of plant extract 50 and 100 mg/kg bw. The extract produced significant (p<0.01) decrease: respectively 95 %, 96.36 %, 99 % and 100 % in the severity of diarrhea. The 50 and 100 mg/kg bw extract produced remarkable (p<0.01) decrease in castor oil-induced enteropooling (59 % and 71.43%), intestine transit (42.12 % and 46.50 %), and reduced acetylcholine action (-65.90 % and -53.73 %) respectively. The results provide evidence that the aqueous extract of O. barrelieri could act on secretory diarrhea and intestinal motility, and thus could justify its traditional use.