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  1. Fulltext 4,4'-({[(Pyridine-2,6-di-yl)bis-(methyl-ene)]bis-(-oxy)}bis-(methyl-ene))dibenzo-nitrile
    Yamin BM, Kamalulazmy NA, Hassan NI
    Acta Crystallogr Sect E Struct Rep Online, 2014 Feb 1;70(Pt 2):o132.
    PMID: 24764859 DOI: 10.1107/S1600536814000245
    The complete title molecule, C23H19N3O2, is generated by a twofold axis passing through the central ring. The two oxymethyl-benzo-nitrile arms are attached at the meta positions of the central pyridine ring. The dihedral angle between the pyridine ring and benzene ring of both arms is 84.55 (6)° while the benzene rings make a dihedral angle of 46.07 (7)°. In the crystal, weak C-H⋯π inter-actions link the molecules sheets parallel to the ac plane.
  2. Fulltext A New and All-Solid-State Potentiometric Aluminium Ion Sensor for Water Analysis
    Ying KS, Heng LY, Hassan NI, Hasbullah SA
    Sensors (Basel), 2020 Dec 03;20(23).
    PMID: 33287113 DOI: 10.3390/s20236898
    An all-solid-state potentiometric electrode system for aluminium ion determination was developed with a new aluminium ion sensor as the working electrode based on a new ionophore for aluminium ion, 1,1'-[(methylazanediyl)bis(ethane-2,1-diyl)]bis[3-(naphthalen-1-yl)thiourea] (ACH). The reference electrode was a potassium ion sensor, which acts as a pseudo-reference. Both electrodes were made from Ag/AgCl screen-print electrodes fabricated from a non-plasticized and photocurable poly(n-butyl acrylate) membrane that contained various other membrane components. The pseudo-reference potential based on the potassium ion sensor was fixed in 0.050 M KNO3, and such concentration of K+ ion did not interfere with the measurement of the Al3+ ion using the aluminium sensor. With such a pseudo-reference and in the presence of 0.050 M KNO3 as a background medium, the aluminium sensor measured changes of aluminium ion concentrations linearly from 10-6 to 10-2 M Al3+ ion with a Nernstian response of 17.70 ± 0.13 mV/decade. A low detection limit of 2.45 × 10-7 M was achieved with this all-solid-state potentiometric system. The aluminium sensor was insensitive to pH effects from 2.0 to 8.0 with a response time of less than 50 s. Under optimum conditions, a lifetime of 49 days was achieved with good sensor selectivity, reversibility, repeatability, and reproducibility. The all-solid-state electrode system was applied to analyze the Al3+ ion content of water samples from a water treatment plant. Compared with the conventional potentiometric detection system for aluminium ions, the new all-solid-state aluminium ion sensor incorporating a pseudo-reference from the potassium sensor demonstrated similar analytical performance. It thus provided a convenient means of aluminium content analysis in water treatment plants.
  3. Fulltext Pyrazole and pyrazoline derivatives as antimalarial agents: A key review
    Ravindar L, Hasbullah SA, Rakesh KP, Hassan NI
    Eur J Pharm Sci, 2023 Apr 01;183:106365.
    PMID: 36563914 DOI: 10.1016/j.ejps.2022.106365
    Malaria poses a severe public health risk and a significant economic burden in disease-endemic countries. One of the most severe issues in malaria control is the development of drug resistance in malaria parasites. The standard treatment for malaria is artemisinin-combination therapy (ACT). Nevertheless, the Plasmodium parasite's extensive resistance to prior drugs and reduced ACT efficiency necessitates novel drug discovery. The progress in discovering novel, affordable, and effective antimalarial agents is significant in combating drug resistance, and the hybrid drug concept can be used to covalently link two or more active pharmacophores that may act on multiple targets. Pyrazole and pyrazoline derivatives are considered pharmacologically necessary active heterocyclic scaffolds that possess almost all types of pharmacological activities. This review summarized recent progress in antimalarial activities of synthesized pyrazole and pyrazoline derivatives. The studies published since 2000 are included in this systematic review. This review is anticipated to be beneficial for future study and new ideas in searching for rational development strategies for more effective pyrazole and pyrazoline derivatives as antimalarial drugs.
  4. Recent developments in antimalarial activities of 4-aminoquinoline derivatives
    Ravindar L, Hasbullah SA, Rakesh KP, Hassan NI
    Eur J Med Chem, 2023 Aug 05;256:115458.
    PMID: 37163950 DOI: 10.1016/j.ejmech.2023.115458
    Malaria is the fifth most lethal parasitic infection in the world. Antimalarial medications have played a crucial role in preventing and eradicating malaria. Numerous heterocyclic moieties have been incorporated into the creation of effective antimalarial drugs. The 4-aminoquinoline moiety is favoured in antimalarial drug discovery due to the diverse biological applications of its derivative. Since the 1960s, 4-aminoquinoline has been an important antimalarial drug due to its low toxicity, high tolerability, and rapid absorption after administration. This review focused on the antimalarial efficacy of the 4-aminoquinoline moiety hybridised with various heterocyclic scaffolds developed by scientists since 2018 against diverse Plasmodium clones. It could aid in the future development of more effective antimalarial agents.
  5. Triazole hybrid compounds: A new frontier in malaria treatment
    Ravindar L, Hasbullah SA, Rakesh KP, Hassan NI
    Eur J Med Chem, 2023 Nov 05;259:115694.
    PMID: 37556947 DOI: 10.1016/j.ejmech.2023.115694
    Reviewing the advancements in malaria treatment, the emergence of triazole hybrid compounds stands out as a groundbreaking development. Combining the advantages of triazole and other moieties, these hybrid compounds offer a new frontier in the battle against malaria. Their potential as effective antimalarial agents has captured the attention of researchers and holds promise for overcoming the challenges posed by drug-resistant malaria strains. We focused on their broad spectrum of antimalarial activity of diverse hybridized 1,2,3-triazoles and 1,2,4-triazoles, structure-activity relationship (SAR), drug-likeness, bioavailability and pharmacokinetic properties reported since 2018 targeting multiple stages of the Plasmodium life cycle. This versatility makes them highly effective against both drug-sensitive and drug-resistant strains of P. falciparum, making them invaluable tools in regions where resistance is prevalent. The synergistic effects of combining the triazole moiety with other pharmacophores have resulted in even greater antimalarial potency. This approach has the potential to circumvent existing resistance mechanisms and provide a more sustainable solution to malaria treatment. While triazole hybrid compounds show great promise, further research and clinical trials are warranted to fully evaluate their safety, efficacy and long-term effects. As research progresses, these compounds can potentially revolutionize the field and contribute to global efforts to eradicate malaria, ultimately saving countless lives worldwide.
  6. Cervicofacial actinomycosis: a key consideration in cases of submandibular swelling
    Cheng XL, Abu Hassan NI, Ng DC
    BMJ Case Rep, 2023 Dec 09;16(12).
    PMID: 38087483 DOI: 10.1136/bcr-2023-258129
  7. Fulltext Exploring Eating and Nutritional Challenges for Children with Autism Spectrum Disorder: Parents' and Special Educators' Perceptions
    Ismail NAS, Ramli NS, Hamzaid NH, Hassan NI
    Nutrients, 2020 Aug 20;12(9).
    PMID: 32825466 DOI: 10.3390/nu12092530
    Autism spectrum disorder (ASD) is a complex neurodevelopmental disability that is frequently associated with food refusal, limited food repertoire and high-frequency single food intake mainly among children with ASD. Provision of nutrition can be very challenging due to the fact of these behavioural problems, either for the parents or special educators. Healthy nutrition is associated with providing and consuming nutritious food with results being in a good state of health. Semi-structured focus group discussions (FGDs) were conducted among 20 participants at a National Autism Centre to explore their understanding towards healthy nutrition. They were parents and special educators who were actively involved with children with ASD. A series of discussions were transcribed verbatim, and four researchers examined each transcript. Inductive analysis linking codes into main thematic categories was conducted using the constant comparison approach across the full data set. The outcome suggested that participants had limited knowledge relating to the proper dietary and nutritional needs of the children. The key messages from the discussion provide a foundation on the development of a nutrition education module which involves primary caretakers of children with ASD.
  8. Transformation of crystalline starch nanoparticles into highly luminescent carbon nanodots: Toxicity studies and their applications
    Sonthanasamy RSA, Ahmad WYW, Fazry S, Hassan NI, Lazim AM
    Carbohydr Polym, 2016 Feb 10;137:488-496.
    PMID: 26686155 DOI: 10.1016/j.carbpol.2015.11.021
    Being abundant in many tropical part of the world, Dioscorea sp. as food is limited due to its toxicity. However polysaccharides derive from these tubers could be important for other applications. Here we developed a Highly Luminescent Carbon Nanodots (C-dots) via acid hydrolysis of Gadong starch (GS). The hydrolysis rate of GS increased from 49% to 86% within 7 days while the X-ray diffraction showed the native GS particle is a C-crystalline type. The GS particles were either round or oval with diameters ranging from 50-90 nm. Further acid dehydration and surface oxidation reduced the size of GS nanoparticles to 6-25 nm. The C-dots produced a fluorescent emission at wavelength 441 nm. Toxicity tests demonstrate that zebrafish embryo were able to tolerate the C-dots for 48 h after exposure. This study has successfully demonstrated a novel approach of converting GS into excellent fluorescent C-dot.
  9. Orthogonal Recognition Processes Drive the Assembly and Replication of a [2]Rotaxane
    Kosikova T, Hassan NI, Cordes DB, Slawin AM, Philp D
    J Am Chem Soc, 2015 Dec 30;137(51):16074-83.
    PMID: 26473285 DOI: 10.1021/jacs.5b09738
    Within a small, interconnected reaction network, orthogonal recognition processes drive the assembly and replication of a [2]rotaxane. Rotaxane formation is governed by a central, hydrogen-bonding-mediated binding equilibrium between a macrocycle and a linear component, which associate to give a reactive pseudorotaxane. Both the pseudorotaxane and the linear component undergo irreversible, recognition-mediated 1,3-dipolar cycloaddition reactions with a stoppering maleimide group, forming rotaxane and thread, respectively. As a result of these orthogonal recognition-mediated processes, the rotaxane and thread can act as auto-catalytic templates for their own formation and also operate as cross-catalytic templates for each other. However, the interplay between the recognition and reaction processes in this reaction network results in the formation of undesirable pseudorotaxane complexes, causing thread formation to exceed rotaxane formation in the current experimental system. Nevertheless, in the absence of competitive macrocycle-binding sites, realization of a replicating network favoring formation of rotaxane is possible.
  10. Fulltext Data on antiplasmodial and stage-specific inhibitory effects of Aromatic (Ar)-Turmerone against Plasmodium falciparum 3D7
    Ali AH, Agustar HK, Hassan NI, Latip J, Embi N, Sidek HM
    Data Brief, 2020 Dec;33:106592.
    PMID: 33318979 DOI: 10.1016/j.dib.2020.106592
    Aromatic (ar)-turmerone is one of the aromatic constituents abundant in turmeric essential oil from Curcuma longa. Ar-turmerone exhibited anti-inflammatory properties. So far, antiplasmodial data for ar-turmerone is still not reported. The data showed the in vitro antiplasmodial effect of ar-turmerone against Plasmodium falciparum 3D7 (chloroquine-sensitive) via Plasmodium lactate dehydrogenase assay (pLDH) and cytotoxic effect against Vero mammalian kidney cells using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) colourimetric assay. Selectivity indexes of ar-turmerone were calculated based on inhibition concentration at 50% of parasite growth (IC50) from MTT and pLDH assays and the effects of ar-turmerone were compared to the antimalarial reference drug chloroquine diphosphate. The inhibitory effect of ar-turmerone at the intraerythrocytic stages of plasmodial lifecycles was evaluated via a stage-dependant susceptibility test. The antiplasmodial and cytotoxic activities of ar-turmerone revealed IC50 values of 46.8 ± 2.4 μM and 820.4 ± 1.5 μM respectively. The selectivity index of ar-turmerone was 17.5. Ar-turmerone suppressed the ring-trophozoite transition stage of the intraerythrocytic life cycle of P. falciparum 3D7.
  11. Steroids from Diplazium esculentum: Antiplasmodial activity and molecular docking studies to investigate their binding modes
    Safar HF, Ali AH, Zakaria NH, Kamal N, Hassan NI, Agustar HK, et al.
    Trop Biomed, 2022 Dec 01;39(4):552-558.
    PMID: 36602215 DOI: 10.47665/tb.39.4.011
    Diplazium esculentum is an edible fern commonly consumed by the local community in Malaysia either as food or medicine. Isolation work on the ethyl acetate extract of the stem of D. esculentum resulted in the purification of two steroids, subsequently identified as stigmasterol (compound 1) and ergosterol5,8-endoperoxide (compound 2). Upon further testing, compound 2 displayed strong inhibitory activity against the Plasmodium falciparum 3D7 (chloroquine-sensitive) strain, with an IC50 of 4.27±1.15 µM, while compound 1 was inactive. In silico data revealed that compound 2 showed good binding affinity to P. falciparum-Sarco endoplasmic reticulum calcium-dependent ATPase (PfATP6); however, compound 1 did not show an antiplasmodial effect due to the lack of a peroxide moiety in the chemical structure. Our data suggested that the antiplasmodial activity of compound 2 from D. esculentum might be due to the inhibition of PfATP6, which resulted in both in vitro and in silico inhibitory properties.
  12. Fulltext An Electrochemical DNA Biosensor for Carcinogenicity of Anticancer Compounds Based on Competition between Methylene Blue and Oligonucleotides
    Md Sani ND, Ariffin EY, Sheryn W, Shamsuddin MA, Heng LY, Latip J, et al.
    Sensors (Basel), 2019 Nov 22;19(23).
    PMID: 31766637 DOI: 10.3390/s19235111
    A toxicity electrochemical DNA biosensor has been constructed for the detection of carcinogens using 24 base guanine DNA rich single stranded DNA, and methylene blue (MB) as the electroactive indicator. This amine terminated ssDNA was immobilized onto silica nanospheres and deposited on gold nanoparticle modified carbon-paste screen printed electrodes (SPEs). The modified SPE was initially exposed to a carcinogen, followed by immersion in methylene blue for an optimized duration. The biosensor response was measured using differential pulse voltammetry. The performance of the biosensor was identified on several anti-cancer compounds. The toxicity DNA biosensor demonstrated a linear response range to the cadmium chloride from 0.0005 ppm to 0.01 ppm (R2 = 0.928) with a limit of detection at 0.0004 ppm. The biosensor also exhibited its versatility to screen the carcinogenicity of potential anti-cancer compounds.
  13. Fulltext A Review of Food Texture Modification among Individuals with Cerebral Palsy: The Challenges among Cerebral Palsy Families
    Kamal S, Kamaralzaman S, Sharma S, Jaafar NH, Chern PM, Hassan NI, et al.
    Nutrients, 2022 Dec 09;14(24).
    PMID: 36558401 DOI: 10.3390/nu14245241
    Individuals with cerebral palsy (CP) frequently present with multiple feeding problems, which may require food texture modification to ensure safe feeding. This review aims to explore the challenges individuals with CP and their caregiver's face and recommend modified food textures to ensure safety and improve the quality of life and nutritional status. A systematic search was carried out through four databases (i.e., EBSCO (Medline), PubMed, Science Direct, and Web of Science) between January 2011 and May 2022. Out of 86 articles retrieved, seven were selected based on keywords and seven other studies through manual search-five cross-sectional studies, two qualitative studies, one correlational study, one mixed method study, one case-control study, two sections of books, and two educational materials. The findings suggest that preparation and intake of food with modified texture play a necessary role in the safety of swallowing in addition to physical, social, and environmental aspects. Safety was found to be the crucial part of the food texture modification provision besides considering the stress of the caregivers and the nutritional status of individuals with CP. Currently, there are no standard guidelines available pertaining to food texture modification. This led to uncertainties in the dietary provision among caregivers, which may lead to undernourishment. Hence, standard guidelines relating to food texture modification that focuses on food preparation and menus with calorie and nutrient information are timely to be developed.
  14. Fulltext Nutritional status as predictors for quality of life among caregivers of children with severe cerebral palsy
    Kamal S, Hamzaid NH, Kamaralzaman S, Sharma S, Jaafar NH, Chern PM, et al.
    Transl Pediatr, 2023 Sep 18;12(9):1601-1618.
    PMID: 37814717 DOI: 10.21037/tp-23-195
    BACKGROUND: Individuals with severe cerebral palsy (CP) often experience various health issues, including feeding difficulties, which can adversely affect their nutritional status and caregivers' quality of life, e.g., more time spent for feeding rather than own selfcare. This study aimed to determine the prevalence of poor nutritional status among individuals with severe CP and explore its role as predictors for caregivers' quality of life.

    METHODS: This cross-sectional study was conducted in a government hospital (Cheras Rehabilitation Hospital), Community-Based Rehabilitation (CBR) Program, and Spastic Centre [non-profit organization (NGO)] in Klang Valley, Malaysia. Seventy-one participants with Gross Motor Function Classification System (GMFCS) level IV and V were recruited. Sociodemographic data, health-associated data, and anthropometric data were collected. Caregivers' quality of life was assessed using the Pediatric Quality of Life Inventory (PedsQL) CP module version 3.0 which included domains such as Movement and Balance, Eating Activities, and School Activities.

    RESULTS: Most participants were males (60.6%), with 61 classified as level IV in the GMFCS classification. According to the Eating and Drinking Ability Classification System (EDACS), 59 children were at level IV. In total, 40.8% were underweight according to CP growth chart and 49.3% had mid-upper arm circumference (MUAC) readings below the 5th percentile. The lowest scores in the PedsQL CP module version 3.0 were observed in the Daily Activities (5.34±10.87), and School Activities domains (8.15±18.65). Sociodemographic and anthropometric data, including body mass index (BMI)-for-age, MUAC, body fat, triceps, and subscapular skinfold measurement, were predictors for the School Activities domain [F (11, 44)=3.981, P<0.005, R2=0.499].

    CONCLUSIONS: Poor nutritional status in individuals with severe CP has been shown to negatively impact caregivers' quality of life. Therefore, a multidisciplinary approach involving nutritional intervention is essential to improve dietary provision and the nutritional status of children with CP.

  15. Fulltext Zinc status in public health: exploring emerging research trends through bibliometric analysis of the historical context from 1978 to 2022
    Mohamad NS, Tan LL, Ali NIM, Mazlan NF, Sage EE, Hassan NI, et al.
    Environ Sci Pollut Res Int, 2023 Mar;30(11):28422-28445.
    PMID: 36680719 DOI: 10.1007/s11356-023-25257-5
    The current study aims to provide a roadmap for future research by analyzing the research structures and trends in scholarly publications related to the status of zinc in public health. Only journal articles published between 1978 and 2022 are included in the refined bibliographical outputs retrieved from the Web of Science (WoS) database. The first section announces findings based on WoS categories, such as discipline heterogeneity, times cited and publications over time, and citation reports. The second section then employs VoSViewer software for bibliometric analysis, which includes a thorough examination of co-authorship among researchers, organizations, and countries and a count of all bibliographic databases among documents. The final section discusses the research's weaknesses and strengths in zinc status, public health, and potential future directions; 7158 authors contributed to 1730 papers (including 339 with publications, more than three times). "Keen, C.L." is a researcher with the most publications and a better understanding of zinc status in public health. Meanwhile, the USA has been the epicenter of research on the status of zinc in public health due to the highest percentage of publications with the most citations and collaboration with the rest of the world, with the top institution being the University of California, Davis. Future research can be organized collaboratively based on hot topics from co-occurrence network mapping and bibliographic couplings to improve zinc status and protect public health.
  16. Exploring diverse frontiers: Advancements of bioactive 4-aminoquinoline-based molecular hybrids in targeted therapeutics and beyond
    Ravindar L, Hasbullah SA, Rakesh KP, Raheem S, Agustar HK, Ismail N, et al.
    Eur J Med Chem, 2024 Jan 15;264:116043.
    PMID: 38118392 DOI: 10.1016/j.ejmech.2023.116043
    Amongst heterocyclic compounds, quinoline and its derivatives are advantaged scaffolds that appear as a significant assembly motif for developing new drug entities. Aminoquinoline moiety has gained significant attention among researchers in the 21stcentury. Considering the biological and pharmaceutical importance of aminoquinoline derivatives, herein, we review the recent developments (since 2019) in various biological activities of the 4-aminoquinoline scaffold hybridized with diverse heterocyclic moieties such as quinoline, pyridine, pyrimidine, triazine, dioxine, piperazine, pyrazoline, piperidine, imidazole, indole, oxadiazole, carbazole, dioxole, thiazole, benzothiazole, pyrazole, phthalimide, adamantane, benzochromene, and pyridinone. Moreover, by gaining knowledge about SARs, structural insights, and molecular targets, this review may help medicinal chemists design cost-effective, selective, safe, and more potent 4-aminoquinoline hybrids for diverse biological activities.
  17. Fulltext Zerumbone Ameliorates Neuropathic Pain Symptoms via Cannabinoid and PPAR Receptors Using In Vivo and In Silico Models
    Chia JSM, Farouk AAO, Mohamad TAST, Sulaiman MR, Zakaria H, Hassan NI, et al.
    Molecules, 2021 Jun 24;26(13).
    PMID: 34202590 DOI: 10.3390/molecules26133849
    Neuropathic pain is a chronic pain condition persisting past the presence of any noxious stimulus or inflammation. Zerumbone, of the Zingiber zerumbet ginger plant, has exhibited anti-allodynic and antihyperalgesic effects in a neuropathic pain animal model, amongst other pharmacological properties. This study was conducted to further elucidate the mechanisms underlying zerumbone's antineuropathic actions. Research on therapeutic agents involving cannabinoid (CB) and peroxisome proliferator-activated receptors (PPARs) is rising. These receptor systems have shown importance in causing a synergistic effect in suppressing nociceptive processing. Behavioural responses were assessed using the von Frey filament test (mechanical allodynia) and Hargreaves plantar test (thermal hyperalgesia), in chronic constriction injury (CCI) neuropathic pain mice. Antagonists SR141716 (CB1 receptor), SR144528 (CB2 receptor), GW6471 (PPARα receptor) and GW9662 (PPARγ receptor) were pre-administered before the zerumbone treatment. Our findings indicated the involvement of CB1, PPARα and PPARγ in zerumbone's action against mechanical allodynia, whereas only CB1 and PPARα were involved against thermal hyperalgesia. Molecular docking studies also suggest that zerumbone has a comparable and favourable binding affinity against the respective agonist on the CB and PPAR receptors studied. This finding will contribute to advance our knowledge on zerumbone and its significance in treating neuropathic pain.
  18. Fulltext Comparison of sPLA2IIA performance with high-sensitive CRP neutrophil percentage PCT and lactate to identify bacterial infection
    Tan TL, Kang CW, Ooi KS, Tan ST, Ahmad NS, Nasuruddin DN, et al.
    Sci Rep, 2021 05 31;11(1):11369.
    PMID: 34059757 DOI: 10.1038/s41598-021-90894-0
    Early bacterial infection (BI) identification in resource-limiting Emergency Departments (ED) is challenging, especially in low- and middle-income counties (LMIC). Misdiagnosis predisposes to antibiotic overuse and propagates antimicrobial resistance. This study evaluates new emerging biomarkers, secretory phospholipase A2 group IIA (sPLA2-IIA) and compares with other biomarkers on their performance characteristic of BI detection in Malaysia, an LMIC. A prospective cohort study was conducted involving 151 consecutive patients admitted to the ED. A single measurement was taken upon patient arrival in ED and was analysed for serum levels of sPLA2-IIA, high-sensitive C-reactive protein (CRP), procalcitonin (PCT), neutrophil percentage (N%), and lactate. All biomarkers' performance was compared for the outcomes using area under the receiver operating characteristic curve (AUROC), sensitivity, and specificity. The performance of sPLA2-IIA (AUROC 0.93 [95% CI: 0.89-0.97]; Sn 80% [95% CI: 72-87]; Sp 94% [95% CI: 81-89]) was the highest among all. It was comparable with high-sensitive CRP (AUROC 0.93 [95% CI: 0.88-0.97]; Sn 75% [95% CI: 66-83]; Sp 91 [95% CI: 77-98]) but had a higher Sn and Sp. The sPLA2-IIA was also found superior to N%, PCT, and lactate. This finding suggested sPLA2-IIA was recommended biomarkers for BI detection in LMIC.
  19. Fulltext Synthesis, Molecular Docking, and Antimalarial Activity of Hybrid 4-Aminoquinoline-pyrano[2,3-c]pyrazole Derivatives
    Shamsuddin MA, Ali AH, Zakaria NH, Mohammat MF, Hamzah AS, Shaameri Z, et al.
    Pharmaceuticals (Basel), 2021 Nov 17;14(11).
    PMID: 34832956 DOI: 10.3390/ph14111174
    Widespread resistance of Plasmodium falciparum to current artemisinin-based combination therapies necessitate the discovery of new medicines. Pharmacophoric hybridization has become an alternative for drug resistance that lowers the risk of drug-drug adverse interactions. In this study, we synthesized a new series of hybrids by covalently linking the scaffolds of pyrano[2,3-c]pyrazole with 4-aminoquinoline via an ethyl linker. All synthesized hybrid molecules were evaluated through in vitro screenings against chloroquine-resistant (K1) and -sensitive (3D7) P. falciparum strains, respectively. Data from in vitro assessments showed that hybrid 4b displayed significant antiplasmodial activities against the 3D7 strain (EC50 = 0.0130 ± 0.0002 μM) and the K1 strain (EC50 = 0.02 ± 0.01 μM), with low cytotoxic effect against Vero mammalian cells. The high selectivity index value on the 3D7 strain (SI > 1000) and the K1 strain (SI > 800) and the low resistance index value from compound 4b suggested that the pharmacological effects of this compound were due to selective inhibition on the 3D7 and K1 strains. Molecular docking analysis also showed that 4b recorded the highest binding energy on P. falciparum lactate dehydrogenase. Thus, P. falciparum lactate dehydrogenase is considered a potential molecular target for the synthesized compound.
  20. Fulltext An Amperometric Biosensor for the Determination of Bacterial Sepsis Biomarker, Secretory Phospholipase Group 2-IIA Using a Tri-Enzyme System
    Nik Mansor NN, Leong TT, Safitri E, Futra D, Ahmad NS, Nasuruddin DN, et al.
    Sensors (Basel), 2018 Feb 26;18(3).
    PMID: 29495352 DOI: 10.3390/s18030686
    A tri-enzyme system consisting of choline kinase/choline oxidase/horseradish peroxidase was used in the rapid and specific determination of the biomarker for bacterial sepsis infection, secretory phospholipase Group 2-IIA (sPLA2-IIA). These enzymes were individually immobilized onto the acrylic microspheres via succinimide groups for the preparation of an electrochemical biosensor. The reaction of sPLA2-IIA with its substrate initiated a cascading enzymatic reaction in the tri-enzyme system that led to the final production of hydrogen peroxide, which presence was indicated by the redox characteristics of potassium ferricyanide, K₃Fe(CN)₆. An amperometric biosensor based on enzyme conjugated acrylic microspheres and gold nanoparticles composite coated onto a carbon-paste screen printed electrode (SPE) was fabricated and the current measurement was performed at a low potential of 0.20 V. This enzymatic biosensor gave a linear range 0.01-100 ng/mL (R² = 0.98304) with a detection limit recorded at 5 × 10-3 ng/mL towards sPLA2-IIA. Moreover, the biosensor showed good reproducibility (relative standard deviation (RSD) of 3.04% (n = 5). The biosensor response was reliable up to 25 days of storage at 4 °C. Analysis of human serum samples for sPLA2-IIA indicated that the biosensor has potential for rapid bacterial sepsis diagnosis in hospital emergency department.
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