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European chemical bulletinVol. 11., No. 9. (2022.)

Tartalom

Original Article

  • Salma Sherif Ahmed Mohamed Ahmed Hassan ,
    Shaiful Azuar Mohamad ,
    Rozila Ismail ,
    Shamima Abdul Rahman :

    context: pleurotus species (oyster mushroom) have been used by people worldwide for their medicinal properties, dietary benefit and other purposes. They contain various compounds which biologically active with therapeutic effects. Pleurotus florida which also known as white oyster mushroom is an edible mushroom that is popular due to its low production cost, nutritional contents and easy cultivation method. Aims: this study was designed to evaluate the potential antioxidant and antimicrobial properties of pleurotus florida exopolysaccharide and endopolysaccharide extracts to be an alternative source for existing antioxidant and antimicrobial agent. Methods: In this study, the antioxidant activities of different concentrations of Pleurotus florida extracts were evaluated using total phenolic content (TPC), DPPH radical scavenging activity and ferric reducing antioxidant power (FRAP) assay and the antimicrobial activities were evaluated using agar disk-diffusion method. Results: Out of the 5 concentrations tested for antioxidant properties for both extracts, concentration of 1mg/ml of the IPS extract showed the highest TPC and FRAP activity, while for the DPPH radical scavenging activity concentration of 0.2mg/ml of IPS extract showed the highest scavenging activity. For the antimicrobial evaluation, all the 3 concentrations that were used showed no antimicrobial activity against E. coli, S.aureus and P. aeruginosa. Conclusion: In conclusion, white oyster mushroom has shown potent antioxidant effects which makes it a good antioxidant candidate that can be incorporated in medicine and diet, and as the concentration of Pleurotus florida mushroom increases the antioxidant effects increase. However, both exo-and endopolysaccharide extract doesn’t exhibit any antimicrobial activity in low concentrations.

    Keywords: Antioxidant; Antimicrobial; Endopolysaccharide; Exopolysaccharide; Mushrooms; Pleurotus florida

  • Aqilah Salim ,
    Shamima Abdul Rahman ,
    Shafii Khamis ,
    Hazlina Ahmad Masalli ,
    Mohamed Zafar Ali Mohamed Amiroudine ,
    Daryl Jesus Arapoc :

    Pomegranate or Punica granatum is a fruit that is known for its various pharmacological activities such as antioxidant and cytotoxic activities. Commercial Punica granatum in Malaysia are mostly imported but there are pomegranates that are grown locally. Many studies and research have been done on imported Punica granatum but very little is done on locally grown Punica granatum. This study aims to evaluate and compare the antioxidant and cytotoxic activities of methanolic pulp and peel extract of both local and imported Punica granatum through in vitro studies. The antioxidant study was done by evaluating the Total Phenolic Content (TPC) and 2, 2- diphenyl-1-picrylhydrazyl (DPPH) assay. TPC was done using Folin-Ciocalteu assay and DPPH assay was done using 2, 2- diphenyl-1-picrylhydrazyl. The standards used in these assays were gallic acid, quercetin and ascorbic acid respectively. Cytotoxic study was conducted through MTT (3 (4, 5- dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay against MCF-7 and MDA-MB 231 breast cancer cell lines, head and neck tumour HTB-143 cell line and 3T3 normal cell line. This study revealed that peel extracts have a higher content of phenol and the anticancer analysis shows that the peel extract of local Punica granatum has cytotoxic activity against all cell lines including 3T3 normal cell line.

  • Sumathi D/O Govindasamya ,
    Nurdiana Jamil ,
    Wan Rosalina Wan Rosli :

    CYP3A4 enzyme metabolises more than half of all marketed medicine and is regarded as a major enzyme as it is involved in majority of phase I metabolism. Apart from that CYP3A4 has also been implicated in food-drug interactions such as grapefruit-CYP3A4 and St John’s wort-CYP3A4. Traditional vegetables termed “ulam” is widely consumed in Malaysia, either in raw form or cooked. This is especially due to the people’s increasing awareness of healthy lifestyle which makes vegetable consumption a big part of their diet. Therefore, knowledge regarding inhibitory potentialof ulam constotuents toward the CYP3A4 is important so that informed choices could be made in order to manage the risk of food-drug interactions. Therefore, this study wants to investigate the potential of CYP3A4 inhibition by active constituents of ulam to determine the existence of ulam-drug interaction. Methods: Four types of ulam was investigated that include Melicope ptelefolia (“tenggek burung”), Cosmos caudatus (“ulam raja”), Oenanthe javanica (“selom”) and Centella asiatica (“pegaga”). The plant’s active constituents were extracted using methanol and then its inhibition activity was determined using luminescence assay with ketoconazole as controls. Results: The enzyme CYP3A4 was found to be inhibited by ulam extracts and Centella asiatica (pegaga) was found to have the highest inhibition (IC50 value 23.99 μg mL-1). Then Melicope ptelefolia (IC50 value 34.67 μg mL-1), Cosmos caudatus (IC50 value 52.48 μg mL-1), and Oenanthe javanica (IC50 value 107.15μg mL-1). Conclusion: Ulam was found to have CYP3A4 inhibitory properties, especially Centella asiatica, Melicope ptelefolia and Cosmos caudatus. Therefore consumption of ulam may have potential for food-drug interactions and caution may be exercised when consuming ulam together with CYP3A4-metabolised drugs. What this paper adds: Ulam is a popular traditional food. This paper investigates the food-drug interaction that may be affect the outcome of CYP 3A4-metabolised drugs and found possible interaction in case the ulam is consumed excessively and taken together with the CYP 3A4-metabolised drugs.

    Keywords: traditional vegetable, ulam, CYP 3A4, enzyme inhibition, food-drug interaction

  • Liew Kai Bin ,
    Fariz Haiqal Bin Ruslan ,
    A.B.M. Helal Uddin ,
    Zaidul Islam Sarker ,
    Ashok Kumar Janakiraman :
    Orally disintegrating film: a revisit of its two decades development16-20en [264.80 kB - PDF]EPA-02286-00102-0040

    For the last two decades, oral drug delivery system was extensively discussed in the pharmaceutical field which includes Orally Disintegrating Film (ODF) due to its advantages over other oral dosage form such as tablet and capsule. ODF can be taken without water and classified as patient friendly dosage form especially for geriatric and pediatric who affected the most with swallowing disorder. ODF manufactured by various methods such as solvent casting method, semi solid casting method, hot melting extrusion, solid dispersion extrusion, rolling method and spraying method. ODF formulated using several chemicals like hydrophilic polymers, plasticizer, saliva stimulating agent, surfactant, sweeteners, API, coloring, and flavoring agents. Validation tests such as thickness test, folding endurance, tensile strength, young modulus, disintegration, and dissolution test performed to analyze the mechanical properties, disintegration, and dissolution profile of the film. Some challenges will be encountered in the process of formulating ODF such as API insolubility, unpleasant taste of API, stability issue, and dose uniformity. Those challenges can be overcome with great formulations, high standard manufacturing methods and ideal storage management. In general, ODF have great potential in pharmaceutical market and can be a good tool to enhance the therapeutic convenient of patient which then lead to advancement of healthcare system.

  • Muhammad Mirza Ismat Muzamil ,
    A.B.M. Helal Uddin ,
    Zaidul Islam Sarker ,
    Ashok Kumar Janakiraman ,
    Liew Kai Bin :

    Naringenin is a natural flavonoid which is commonly found in large amounts of natural plants including citrus fruits, tomatoes, cherries, cocoa and grapefruit. Naringenin has a molecular weight of 272.26 and is described as poorly soluble in water. Due to its poor solubility, it will lead to low bioavailability. The aim of this study is to determine the efficiency of using solid lipid nanoparticles (SLN) method in improving solubility of Naringenin. Other than that, concentration of lipid and temperature were studied as well to determine the optimum formation of NRG-SLNs. Solubility of Naringenin is enhance by method of solid lipid nanoparticles. Materials that were used is Naringenin as active ingredient, stearic acid as lipid phase, Tween 80 as non-ionic surfactant and olive oil. As for the oil selection test, the naringenin was determined in several types of oils such as sunflower oil, eucalyptus oil, coconut oil and olive oil. The Naringenin-Solid Lipid Nanoparticles (NRG-SLNs) were prepared by separately two beakers with label of lipid phase and aqueous phase. These different beakers will be mix through some process and will be sonicate and temperature must be maintained at 85°C. On the other hand, the concentration of lipid and temperature are highlighted as the parameter in this study. Evaluation of the prepared SLNs inclusive of drug content uniformity, solubility studies, in vitro dissolution, transmission electron microscopy (TEM) and short-term stability studies. Based on the particle characterization, the particle size of NRG-SLNs ranging from 144 – 648 nm. The polydispersity index (PDI) showed values of 0.609 – 0.721. PDI is indicator if size distribution homogeneity. Zeta potential result was -0.112 mV which is nearly neutral. Other than that, the encapsulation efficiency of Naringenin encapsulated by SLNs method ranging from 77% - 82%. The solid lipid nanoparticles method was proven to significantly improve solubility and enhance stability profile of naringenin compared to the pure naringenin

    Keywords: Naringenin, solid lipid nanoparticles, concentration of lipid, temperature

  • Nur Syafiqah Mohd Asri ,
    Najwa Mohamad ,
    Waheedah Abdul Hakeem :

    Previous studies on university waste have shown that paper products constitute a large proportion of the solid waste generated. Hence, to reduce paper wastage, wastepaper can be reused for the extraction of cellulose for other application such as biomaterial for the production of biodegradable products. This study is aimed to extract and characterize cellulose from wastepaper collected in University of Cyberjaya (UoC). Pre-treatment with sonicator, alkaline and bleaching treatments were employed for the extraction of cellulose. The functional group present in the extracted wastepaper cellulose (WPC) was determined using fourier transform infrared spectroscopy (FT-IR). Thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) were carried out to characterize its thermal stability. The hydration property of WPC was evaluated by water retention capacity (WRC). All the characterization analyses of WPC were compared to commercialized microcrystalline cellulose (MCC). 53.1% of WPC was successfully extracted with some extent of lignin and its purity was supported by the FT-IR findings where the functional groups of cellulose were detected. In thermal analysis, WPC has lower thermal stability than MCC due to its lesser crystalline structure. WPC has higher WRC than MCC because of its bigger particle size. The results obtained in this study reflect the effectiveness of the methods applied in extracting WPC. Extraction of WPC for the utilization in biomaterial production is definitely a practical way to reduce paper waste.

    Keywords: Cellulose, Extraction, Wastepaper

  • Nurul Atikah Musa ,
    Masliana binti Hassan ,
    Imtiaz Khalid Mohammed ,
    Najwa Mohamad :

    Objective of this study was to determine cytotoxicity and antimicrobial effects of SA-PEG, SA-PEG-OCT, CMC-PEG, CMC-PEG-OCT, SA-CMC-PEG and SA-CMC-PEG-OCT hydrogels for wound healing application. In this study, the cytotoxicity effect were observed using human foreskin fibroblast (HS-27) cell that is treated with concentration of hydrogels’ extract of 25%, 50% and 100% for 24 hours. The cytotoxic activity was determined via CellTiter®-Blue cell viability assay. Meanwhile, disk diffusion method was used using Staphylococcus aureus to observe the Zone of Inhibition (ZOI) of hydrogels for antimicrobial study. Cell viability assay revealed that the results of mean cell viability for 100% hydrogel concentration according to decreasing order are as follow: SA-PEG-OCT > SA-CMC-PEG-OCT > SA-PEG > SA-CMC-PEG > CMC-PEG > CMC-PEG-OCT. All hydrogels loaded with OCT showed ZOIs that manifested antimicrobial effects against S. aureus. However, there is no ZOIs observed for hydrogels without OCT. The observed SA-PEG-OCT hydrogel, CMC-PEG-OCT hydrogel and SA-CMC-PEG-OCT hydrogel that contain approximately 0.5% OCT each demonstrated antimicrobial activity against S. aureus without undesirable cytotoxicity on fibroblast cell. Thus, SA/CMC based hydrogel loaded with OCT may be suitable for the use in wound healing management.

    Keywords: hydrogel, cytotoxicity, antimicrobial, sodium alginate, carboxymethyl cellulose, octenidine dihydrochloride, antiseptic

  • Imtiaz Khalid Mohammed ,
    Waheedah Abdul Hakeem ,
    Nurkhalida Kamal ,
    Noorazura Ashikeen Ahmad :

    The spawn of antimicrobial resistance (AMR) era has started ever since the past few decades, and it has caused a great concern especially by healthcare providers. The importance of a new class of novel antibiotics is very much needed to overcome this AMR. Fortunately, through computer aided drug design (CADD) and various other in silico methods, it allows scientists to create new potent ligands as potential drugs. Methodologies: Herein, 156 novel aminoalkylnaphthols are examined for the first time in this molecular docking study against two metalloenzymes; UDP-3-O-[R-3-hydroxymyrisoyl]-N-acetylglusomaine deactylase of pseudomonas aeruginosa (PaLpxC) and peptide deformylase of staphylococcus aureus (SaPDF). Results: The novel ligands are reported to have satisfactory inhibition constant (Ki). The best docked ligand against PaLpxC is 4y with Ki of 1.71 and 4u with a Ki of 14.73 against SaPDF. This indicates the potency of the novel ligands. Besides that, after further graphical analyses, the novel aminoalkylnaphthols are found to bind at a new binding site in PaLpxC as compared to reported inhibitors in literatures, which might suggest a new promising binding site has been found. Conclusion: Therefore, this new class of novel ligands are promising potent inhibitors against these two important enzymes.

  • Nurul Najihah Bahrin ,
    Abd Almonem Doolaanea ,
    Batoul Alallam ,
    Mohamed Awang ,
    Fashli Syafiq Abd Razak :

    The use of nanotechnology in drug delivery could improve treatment by allowing targeted delivery and fewer adverse effects. The application of tailored nanomaterials as well as the development of delivery systems from nanoscale molecules are examples of nanotechnology drug delivery applications. Leeches have been chosen in this study as it has historically been shown to be a beneficial therapy for a variety of diseases, including war wound care. Leech saliva extract (LSE) contains complex mixture of different biologically and pharmacologically active substances which are beneficial for the mankind. Objective: This study was designed to encapsulate Leech Saliva Extract (LSE) in nanoparticles and to evaluate the effect of process parameters on the nanoparticle size, zeta potential, encapsulation efficiency and in vitro release profile. Methodology: Electrospray technique was used to fabricate the nanoparticles. The process parameters, namely applied voltage and flow rate were adjusted. The fabricated nanoparticles undergone characterization to evaluate how the process parameters affect the particle size, zeta potential, encapsulation efficiency and in vitro release profile. Results and discussion: LSE ALG nanoparticles have shown mean particle size and zeta potential of 205 nm and -7.32 mV respectively. Encapsulation efficiency (EE) of over 87% was obtained while maintaining payload integrity. In vitro release profile showed initial burst drug release (42%) was observed up to 6 hour and a constant slow LSE release was observed up to 48 hour. Conclusion: Adjustment of electrospray process parameters yielded optimum result of standard nanoparticles. LSE-loaded in alginate nanoparticles were successfully prepared using one-step-method.

    Keywords: encapsulation; leech saliva extract (LSE); alginate; nanoparticles

Original Article

  • Nurhabibah,
    A.K. Nugroho ,
    Ronny Martien ,
    Endang Lukitaningsih :

    This study aimed to investigate the formulation and characterization of Lovastatin in an L-SNEDDS. The selected is composed of L-SNEDDS based on a solubility study of lovastatin in many oils, surfactants, and co-surfactants. Ternary phase diagrams were constructed based on lovastatin solubility to determine lower limit and high limit of oil, surfactant, and co-surfactant selected further to optimize the system using a D-Optimal mixture design. The optimized S of lovastatin was evaluated, including size particle, polydisperse index, and emulsification time. The optimal formula of L-SNEDDS was verified and determined size particle, polydisperse index, emulsification time, drug content, and dissolution of lovastatin. The results showed that the best formula is the composition of oleic acid 5,2%; tween 80 79,5%, and PEG 400 15,8%. The particle size is below 100 nm, the polydisperse index is below 0,5, and the emulsification time is below 20 seconds. The loading of SNEDDS lovastatin is 97,01%, and the SNEDDS of lovastatin composed of oleic acid, tween 80, and PEG 400 showed increasing dissolution of lovastatin than pure lovastatin

    Keywords: L-SNEDDS, lovastatin, solubility, evaluation, dissolution

  • Nabil A. Alhemiary :

    The zileuton was determined utilizing the differential pulse voltammetry (DPV) approach employing a modified molecularly imprinted carbon paste electrode (CPE) containing BiOCl/CuS@SnO2NPs nanocomposite The BiOCl/CuS@SnO2NPs/CPE exhibits a strong and well-defined peak for the oxidation of zileuton at 640 mV in phosphate buffer solution pH = 8. With a linear range of 4-75 μM and a low detection limit of 0.0.7 μM, DPV was used to measure zileuton. BiOCl/CuS@SnO2NPs/CPE was tested for repeatability, reproducibility, and stability, and the results support the sensor's good characteristics. The selectivity of the proposed method was studied, and the results showed that there was no disruption in the detection of zileuton, and that the peak current changed by less than 5%. Finally, BiOCl/CuS@SnO2NPs/CPE was successfully used to determine zileuton in pharmaceutical formulations and human serum samples, with recovery rates ranging from 98.3% percent to 103.6% percent and an RSD of less than 5%.

    Keywords: Nanocomposite, Zileuton, Carbon Paste Electrode, modified

Original Article

  • Mahani Mahadi ,
    Mohamad Syawal Mohd Zawawi ,
    Zauyah Yusuf :

    Kombucha tea is generally known as a fermented tea beverage yielded by fermenting sugar and black tea with a kombucha culture known as a mushroom. Due to its health benefit, this fermented tea had become one of popular drink world-wide. Kombucha tea has been reported to increase energy, promote detoxification, act as probiotic, possess anti-cancer, antioxidant, and anti-microbial properties. Therefore, this research aims to investigate the presence of phytochemical compounds and its anti-oxidant properties. In this study, green tea, black tea, sugar solution, black kombucha tea, green kombucha tea, and sugar kombucha solution as the tested group. All group was fermented in an incubator for 14 days and proceed for phytochemical screening and antioxidant analysis on day 0, 7 and 14. Identification alkaloids, flavonoids, phenol, saponin, tannin and glycosides were measured in each group. From the phytochemical analysis, black kombucha tea contain phenol, flavonoid and saponin meanwhile green kombucha tea contained phenol, flavonoid and tannin. Green and black tea contained phenol, flavonoid, saponin and tannin while sugar solution and sugar kombucha solution do not contain any phytochemical compound. Two antioxidant tests performed which are 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) scavenging assay and total phenolic compound (TPC). The result showed black and green kombucha tea, and sugar kombucha solution had the highest percentage of scavenging activity on day 7 and 14 compared to black and green tea and sugar solution. Similar to DPPH, highest TPC was observed in both black and green kombucha tea compared to other solutions. In conclusion, kombucha green and black tea contained several phytochemical com-pounds that may enhanced their antioxidant activity.

    Keywords: Kombucha tea; antioxidant activity, metabolite profile

  • Aina Shafia Hashim ,
    Najwa Mohamad ,
    Mahani Mahadi :

    High exposure to bioaerosols may promotes range of infection. Bioaerosols causes air pollutants in indoor or outdoor environment. Teaching laboratories, one the facility that commonly used by the student and staff designed to have a control indoor environment to minimise level of bioaerosol that may affect health and contaminate the experimental results. Hence, this study investigated the indoor air quality by measuring the bacterial and fungal bioaerosol in 4 different teaching laboratories in University of Cyberjaya. Settle plate and contact plate method were used for passive air and surface sampling. Colonies were counted after 48 hours incubation and identified based on morphology characteristic. Bacterial identifications were evaluated using streak plate and Gram-staining method. Results showed that Pharmacognosy Laboratory has the highest number of bacterial and fungal bioaerosols with 124.00 and 38.00 CFU/m3 respectively compared to Medical Science Laboratory 1 and Clean Room. The lowest number of bacterial and fungal bioaerosols measured in Medical Science Laboratory 2 with 12 CFU/m3 and 16 CFU/m3 respectively. Culturable bacterial bioaerosol showed a variety colour of colonies, with different morphological characteristic. Gram stain of the bacteria from all four laboratories revealed that 62.5% was gram positive cocci, 18.75% was gram negative cocci and 18.75% was gram negative coccobacilli. This study found the indoor air quality of laboratories of University of Cyberjaya is within the standard level and the bioaerosol is considerably low, hence it is safe to students and staffs. However, proper maintenance is needed to prevent bioaerosol emission.

    Keywords: bioaerosols; bacterial bioaerosols; fungal bioaerosols

  • Naveen Pathakala ,
    Mohammed Sayeed ,
    Ram Mohan Manda ,
    Himabindu Peddapalli ,
    Rajendra Kumar Jadi ,
    Vasudha Bakshi ,
    Narender Boggula :

    High Performance Liquid Chromatography (HPLC) is one of the effective separation analytical tools to determine and quantitate the impurities. By using HPLC, we can separate a mixture of compounds to identify and quantify into individual components. In literature survey, various quantification methods are available for the determination of dolutegravir in combined dosage form. The present research paper describes a simple, accurate and precise reversed-phase high performance liquid chromatography (RP-HPLC) method for quantification of dolutegravir in bulk and pharmaceutical dosage form (tablets). This method is validated for different analytical performance parameters like linearity, precision, accuracy, limit of detection, limit of quantification, and robustness were determined according to the International Conference of Harmonization (ICH) Q2B guidelines. Detection was carried out at 256 nm. The mobile phase used as pH-3.6 phosphate buffer:acetonitrile in ratio of (40:60) v/v with flow rate of 1 ml/min. All the parameters of validation were found in the acceptance range of ICH guidelines. The method was found to be linear and correlation coefficient obtained was 0.9996. The system suitability parameters were found to be within the limits. The proposed method was validated in terms of linearity, range, accuracy, precision, specificity, robustness and stability studies and the method is successfully applies to the estimation of dolutegravir in tablet dosage form. Hence the developed method can be adapted to regular quality control analysis.

    Keywords: Reversed-Phase High-Performance Liquid Chromatography, dolutegravir, validation, linearity, accuracy

  • Since November 2019, no cost-effective and potential small drug molecule has been discovered against the SARS-CoV-2 pandemic. The major disadvantage of conventional synthesis is the laborious research time for discovery and development with a huge economy that is not easily met by current pandemic conditions. The main aim of this study is to discover and identify the most effective and promising molecules against the three targets of SARS-CoV-2, such as protease, spike protein and RdRp, via molecular docking screening of various phytochemicals from Rosa Centifolia. The binding affinities were studied using a structure-based drug design of molecular docking. The study results showed that most constituents possess good affinity towards the target than standard drug N3 inhibitor. Among 27 compounds, multiflorin B showed the highest binding energies of -6.975, and -5.471 kcal/mol against protease and RdRp targets, respectively. The compound sabinene showed good interaction with spike protein with a docking score of -4.449 kcal/mol. Molecular ADMET profile estimation showed that the docked phytochemicals are safe. The present study indicates that the various active phytochemical constituents of Rosa Centifolia could inhibit SARS-CoV-2.

    Keywords: Rosa Centifolia, Mpro-target, Insilico docking studies, SARS-CoV-2, ADMET