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   Table of Contents - Current issue
Coverpage
January-March 2023
Volume 14 | Issue 1
Page Nos. 1-62

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GUEST EDITORIAL  

Design of experiments: A design to improve pharmaceutical research p. 1
Bhaswat S Chakraborty
DOI:10.4103/japtr.japtr_690_22  
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ORIGINAL ARTICLES Top

The knowledge and anxiety toward the implementation of COVID-19 vaccination Highly accessed article p. 2
Lintje Boekoesoe, Nur Ayini S. Lalu, K Sarinah Basri, Zul Fikar Ahmad, Andi Nirmasita
DOI:10.4103/japtr.japtr_614_22  
The aim of the study was to analyze the relationship between the level of knowledge and anxiety regarding the implementation of the COVID-19 vaccination in the community. The research was conducted in the Dulupi Health Center work area from March to April 2022, with an analytical observational research design using a cross-sectional approach. The research population is the Dulupi Public Health Center work area community, with a total sample of 297 people taken using the cluster random sampling technique and calculated by Slovin's formula. Data were collected through a questionnaire which were then analyzed by univariate and bivariate. The knowledge variable, most of them had less knowledge (91.9%), and in the anxiety variable, most of the respondents experienced mild anxiety (55.2%). In the implementation variable, most of the respondents were not vaccinated, 245 people (82.5%), while those who were vaccinated were 52 people (17.5%). The level of knowledge and anxiety is primarily related to the implementation of COVID-19 vaccination, with P-values of (0.047) and (0.000) <P (0.05). There is a significant correlation between knowledge and anxiety regarding implementing COVID-19 vaccination in the Dulupi Health Center work area, Boalemo Regency.
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Synthesis of nitrogen mustard-based fluorophores for cell imaging and cytotoxicity studies p. 6
Yuanwei Liang, Maojun Liang, Cuiyu Li, Daini Wang, Xiaoxuan Gong, Kaiji Zheng
DOI:10.4103/japtr.japtr_574_22  
Nitrogen mustards are important alkylating anticancer drugs used for neoplasms treatment. However, little research about the integration of luminophore into nitrogen mustard-based compounds for both imaging and therapeutic application was reported. In this study, we report a series of novel nitrogen mustard-containing 1-furyl-2-en-1-one and 1-thienyl-2-en-1-one derivatives as intramolecular charge transfer-based luminophore for research in both imaging subcellular localization and antiproliferation toward lung cancer cells. The target products were prepared by Knoevenagel condensation and characterized by nuclear magnetic resonance and high-resolution mass spectrometer. The absorption and fluorescence studies were carried out by ultraviolet-visible and fluorescence spectrophotometers, respectively. Cell morphology was observed under an inverted microscope. Cytotoxicity test was detected by MTT assay. Cellular localization was observed by a confocal laser scanning microscope. Colony formation ability was carried out by colony formation assay. Cell migration ability was detected by transwell migration assay. Differences between the two groups were analyzed by two-tailed Student's t-test. The difference with P < 0.05 (*) was considered statistically significant. The compounds were synthesized in high yield. The λmax and Stokes shift of these compounds reach up to 567 and 150 nm, respectively. These compounds exhibited good antiproliferative activity against lung cancer cells, with compound 3h exhibiting the best IC50 of 13.1 ± 2.7 μM. Furthermore, the selected compound 3h is located preferentially in lysosomes and a small amount in nuclei, effectively inhibiting cell colony formation and migration abilities toward A549 cells. These findings suggested that nitrogen mustard-based fluorophores might be a potential effective chemotherapeutic agent in lung cancer therapy.
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Investigations of chemical compositions and antioxidative potential of essential oils isolated from the leaves of two Garcinia species p. 12
Shanthirasekaram Kokilananthan, Vajira P Bulugahapitiya, Harshi Manawadu, Chinthaka Sanath Gangabadage
DOI:10.4103/japtr.japtr_570_22  
Garcinia quaesita and Garcinia zeylanica are Sri Lankan endemic plants with significant therapeutic potential and numerous health-care applications. Despite this, there are no adequate literatures reported on the chemical compositions (CCs) and antioxidative potential (AP) of leaves' essential oils (EOs). The purpose of this study was to extract EOs from the leaves and investigate the CCs and AP of the extracted EOs. The hydro-distillation technique was used to extract the EOs, and the CCs of the EOs were identified through gas chromatography–mass spectrometry analysis. Only those compounds that had a matching value of more than 90% were taken into consideration, and the AP of the extracted EOs was determined using the ferric-reducing antioxidant power (FRAP) assay. Hydro-distillation process yielded EOs in the same quantity, 0.12% (v/w) on a fresh weight basis for two varieties. About 33 CCs that were found in the extracted EOs were mainly sesquiterpenes. The most prevalent substances in the EOs were copaene (19.39%), caryophyllene (12.94%), alloaromadendrene (12.12%), α-humulene (11.24%), and α-cubebene (9.38%). It is interesting to note that copaene and alloaromadendrene were only found in G. quaesita, whereas α-cubebene was only found in G. zeylanica. Caryophyllene and α-humulene were identified in both EOs at different concentrations. The EO from G. quaesita showed high AP, presenting FRAP values 274.74 ± 1.32 μL Trolox Eq/L. This study is recognized as being the first to examine the CCs and AP of EOs, and the results may inspire the creation of new uses and high-value leaf products.
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Computational approach in searching for dual action multitarget inhibitors for osteosarcoma p. 18
Maria Apriliani Gani, Ahmad Dzulfikri Nurhan, Bulan Rhea Kaulika Hadinar Putri, Andhi Suyatno, Shakil Ahmed Khan, Chrismawan Ardianto, Fedik Abdul Rantam, Junaidi Khotib
DOI:10.4103/japtr.japtr_541_22  
Osteosarcoma is a common primary malignant bone tumor that typically manifests in the second decade of life. This study aimed to identify osteogenic compounds that potentially serve as multitarget inhibitors for osteosarcoma. The study was a molecular docking study of nine Food and Drug Administration-approved compounds with osteogenic properties to the key membrane proteins of osteosarcoma. The ligands used were raloxifene, simvastatin, dexamethasone, risedronate, ibandronate, zoledronic acid, ascorbic acid, alendronate, and β-glycerophosphate, whereas the target proteins used were RET, fibroblast growth factor receptor 1, KIT, PDGFRA, VEGFR1, and VEGFR2. Chem3D version 15.0.0.106 was used for ligand preparation, and AutoDockTools version 1.5.6 was used for protein preparation, whereas molecular docking was conducted using AutoDock Vina. Raloxifene, simvastatin, and dexamethasone had the lowest binding activity to the target proteins. The binding affinity of raloxifene was from −8.4 to −10.0 kcal mol−1, that of simvastatin was −8.3 to −9.2 kcal mol−1, whereas dexamethasone ranged from −6.9 to −9.1 kcal mol−1. Most types of interactions were hydrophobically followed by hydrogen bonding. The current study suggests that raloxifene, simvastatin, and dexamethasone have the potential to act as multitarget inhibitors for osteosarcoma with the ability to induce bone remodeling.
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Increasing the stability of incense gum extract (Styrax benzoin) with a mixture of surfactants p. 24
Nora Susanti, Jamalum Purba, M Yosia Gopas Oetama
DOI:10.4103/japtr.japtr_539_22  
Styrax benzoin is a type of incense produced in North Tapanuli, Indonesia. The content of metabolite compounds provides wide use in pharmaceuticals. The occurrence of deposits in the extract makes this preparation unstable; this instability creates problems, especially in the concentration of the extract and is impractical so it needs to be redissolved. The method of using surfactants can be used as a suspending agent, a mixture of two types of surfactants gives variations in hydrophilic and lipophilic balance (HLB), by finding the optimum HLB value to create optimum solution stability and organoleptic, various mixture ratios were carried out with test parameters such as organoleptic, pH, viscosity, particle size, and components of chemical compounds. The results show that the optimum HLB of S. benzoin is 12.7 in surfactants Tween 80 and Span 80.
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Bioactive phytoconstituents of ethanolic extract from Chromolaena odorata leaves interact with vascular endothelial growth factor and cyclooxygenase-2: A molecular docking study p. 29
TR Teuku Husni, Darmawi Darmawi, Azwar Azwar, Kurnia Fitri Jamil
DOI:10.4103/japtr.japtr_520_22  
Chromolaena odorata is an invasive plant with a broad spectrum of medicinal properties, including wound healing. This study aimed to evaluate the interaction of the already identified bioactive phytoconstituents from ethanolic extracts of C. odorata leaves with two angiogenesis-related proteins – vascular endothelial growth factor (VEGF) and cyclooxygenase-2 (COX-2) in silico. A molecular docking protocol was performed on AutoDock Vina employing the molecular structure of VEGF (3HNG) and COX-2 (3LN1) downloaded from the Protein Data Bank. The results reveal that most of the phytoconstituents possess strong binding affinity, where β-tocopherol and squalene have the highest values. In conclusion, it is highly possible that the phytoconstituents of C. odorata from the ethanolic leaf extract perform an interaction with VEGF and COX-2 and affect their activities.
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Prevalence of panton–Valentine leukocidin and toxic shock syndrome toxin-1 genes in methicillin-resistant Staphylococcus aureus isolated from nose of restaurant workers in Kirkuk city p. 34
Najdat Bahjat Mahdi
DOI:10.4103/japtr.japtr_508_22  
Staphylococcus aureus resides naturally in the nasal cavity of healthy individuals, including those working in restaurants, so they may be a source for spreading this bacterium to restaurant customers directly or indirectly through cooked meals. This bacterium has several virulence factors enabling it to cause many diseases in different parts of the body. It has also the capability to resist conventional antibiotics including methicillin. To investigate methicillin-resistant S. aureus (MRSA), 170 nasal swabs were collected from food preparation workers in 30 restaurants (5–6 workers in each restaurant) in Kirkuk city. After collection, the samples were directly transferred to the laboratory and cultured on selective media like mannitol salt agar (MSA). Microbiological examination including morphological, biochemical, and confirmatory tests showed that 24/170 of collected samples were positive for S. aureus with a rate of 14.12%. Among 24 isolates, 20 (83.3%) belonged to MRSA. All isolates were resistant to oxacillin and penicillin (100%), whereas sensitive to other antibiotics (gentamicin, chloramphenicol, and rifampicin). Polymerase chain reaction exhibited that 13 (65%) of MRSA isolates have toxic shock syndrome toxin-1 gene and only 4 (20%) have Panton–Valentine leukocidin gene.
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In silico identification of natural compounds from virgin coconut oil as potential ligand peroxisome proliferator-activated receptor-gamma as preventive food leads against colitis: Is it really work? p. 39
Ni Made Rika Trismayanti, Kusworini , Handayani Dian
DOI:10.4103/japtr.japtr_505_22  
Ulcerative colitis (UC) is an inflammation of the large intestine characterized by diarrhea with blood. UC has a more extensive manifestation in children. Current therapy has not given satisfactory results. This is the basis for the need for preventive therapy to reduce the morbidity and mortality of UC in children. Virgin coconut oil (VCO) is a viable dietary supplement option due to its ability to act as a peroxisome proliferator-activated receptor (PPAR) ligand, inhibiting the release of pro-inflammatory cytokines. The aim of this study was to determine natural compounds from VCO that have the potential to prevent colitis using a docking-based virtual screening approach. Quantitative structure-activity relationship analysis was used to find out how similar the input compounds and the database were. Docking is done using AutoDockTools 1.5.6. The algorithm used is the Lamarckian Genetic Algorithm (4.2). PPAR-gamma (PPAR-γ) was used as the target protein in a complex with rosiglitazone (ID PDB: 7AWC). PyMol 2.5.1 was used to prepare and visualize three-dimensional data, and the amino acid interactions were visualized using Discovery Studio 2021 Clients. It was found that linoleic acid and oleic acid in VCO have anti-inflammatory effects with predictive values of 0.73 and 0.614, respectively, and that they stop tumor necrosis factor (TNF) expression with predictive values of 0.751 and 0.724. The result of molecular docking showed that the VCO compound was able to interact with the same residue as the control. VCO reduces inflammation by acting as a PPAR-γ and TNF expression inhibitor.
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Prevalence and pattern of third molars impaction: A retrospective radiographic study p. 46
Ramizu Bin Shaari, Mohamad Arif Awang Nawi, Ameera Kamal Khaleel, Ali Sultan AlRifai
DOI:10.4103/japtr.japtr_489_22  
Third molar impaction is considered a prevalent issue. The research aimed to study the pervasiveness and pattern of impaction in Karbala/Iraqi population. Orthopantomograms were studied regarding its angulation, impaction depth, and correlation with ramus. The outcomes manifested that the prevalence of 3rd impacted molars was 34.71%, with the proportion of male to female as 0.83:1. Impacted mandibular 3rd molars were significantly encountered. The prevalence of vertical angulation, mesioangular, horizontal, and inverted were significantly associated with the impacted mandibular 3rd molars (P < 0.05). However, the prevalence of distoangular and bucco/lingual was significantly associated (P < 0.05) with the upper impacted 3rd molars. Level C of impaction was significantly (P < 0.05) the most typical level in the maxilla impacted the 3rd molar, and level A and level B of impaction were significantly (P < 0.05) the most prevalent level correlated with the mandibular 3rd molar impaction. Class II was significantly (P < 0.05) the frequently occurring condition subsequent to Classes III and I. In conclusion, the impaction of 3rd molars was significantly predominant in females and lower jaw. The vertical angulation, level C of impaction associated with maxillary 3rd molars and levels A and B of impaction related with mandibular 3rd molars, and Class II are the most encountered conditions.
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Bioassay for total serum bioactivity of Atractylodes lancea p. 51
Kesara Na-Bangchang, Anurak Cheoymang, Nadda Muhamad, Inthuon Kulma
DOI:10.4103/japtr.japtr_431_22  
The study aimed to establish a bioassay for total bioactivity of Atractylodes lancea (AL) in human serum samples. Inhibition of bacterial growth (Staphylococcus aureus ATCC 25923) was assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The calibration curve (0, 0.39, 0.78, 1.56, 3.13, 2.56, and 50 ng/ml) was linear with correlation coefficients >0.990. The limit of quantification (LOQ) was 1.66 mg/ml using 20-ml serum sample. The developed bioassay method meets the standard of the bioanalytical method for determination of serum bioactivity of AL.
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The effect of additional sucrose on the value of tensile strength and elongation of chicken legs gelatin film p. 56
Begum Fauziyah, Dyah Fatimatussholichah, Aldila Raudatus Syarifah, Burhan Ma'arif
DOI:10.4103/japtr.japtr_388_22  
Gelatin is a clear, flavorless, and colorless biopolymer formed by the denaturation of collagen protein in animal tissues. Gelatin is an important ingredient in the manufacture of capsule shell films. The tensile strength and elongation values of gelatin film indicate its quality. Sucrose is one of the ingredients that can affect the tensile strength and elongation of the gelatin film. To determine the effect of adding sucrose on the tensile strength and elongation of the chicken leg skin gelatin film. To extract the gelatin, clean, sliced chicken leg skin was freeze-dried, ground into powder, and extracted. The characteristics of chicken skin gelatin were measured using Fourier-transform infrared, and the data were read in the 4000–400 cm − 1 range for 32 scans. Pouring the solution into a mold, flattening it, and drying it at 40°C results in a film that has been tested for tensile strength and elongation. Gelatin films with a 30% sucrose addition had the best tensile strength and elongation values, with a tensile strength of 3.03 MPa and an elongation of 152.02%. Sucrose alters the tensile strength and elongation of chicken leg gelatin film. 30% sucrose provides better tensile and elongation strength.
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ERRATUM Top

Erratum: Formulation and characterization of orodispersible tablet of glimepiride p. 62

DOI:10.4103/2231-4040.368254  
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