Browse publications by year: 2024

  1. Thapa R, Moglad E, Goyal A, Bhat AA, Almalki WH, Kazmi I, et al.
    EXCLI J, 2024;23:991-1017.
    PMID: 39253534 DOI: 10.17179/excli2024-7475
    One of the main causes of death worldwide is lung cancer, which is largely caused by cigarette smoking. The crucial transcription factor NF-κB, which controls inflammatory responses and various cellular processes, is a constitutively present cytoplasmic protein strictly regulated by inhibitors like IκB proteins. Upon activation by external stimuli, it undergoes phosphorylation, translocates into the nucleus, and modulates the expression of specific genes. The incontrovertible association between pulmonary malignancy and tobacco consumption underscores and highlights a public health concern. Polycyclic aromatic hydrocarbons and nitrosamines, potent carcinogenic compounds present in the aerosol emitted from combusted tobacco, elicit profound deleterious effects upon inhalation, resulting in severe perturbation of pulmonary tissue integrity. The pathogenesis of smoking-induced lung cancer encompasses an intricate process wherein NF-κB activation plays a pivotal role, triggered by exposure to cigarette smoke through diverse signaling pathways, including those associated with oxidative stress and pro-inflammatory cytokines. Unraveling the participation of NF-κB in smoking-induced lung cancer provides pivotal insights into molecular processes, wherein intricate crosstalk between NF-κB and pathways such as MAPK and PI3K-Akt amplifies the inflammatory response, fostering an environment conducive to the formation of lung cancer. This study reviews the critical function of NF-κB in the complex molecular pathways linked to the initiation and advancement of lung carcinogenesis as well as potential treatment targets. See also the graphical abstract(Fig. 1).
  2. Amin Hapis NAN, Nor Rashid N, Choo YM
    Curr Top Med Chem, 2024 Aug 27.
    PMID: 39253916 DOI: 10.2174/0115680266312717240821062535
    Dengue fever, caused by the Dengue virus (DENV) and transmitted by Aedes aegypti mosquitoes, has become endemic in over 100 countries. Despite considerable research, there is a lack of specific drugs for clinical use against dengue. Hence, further exploration to identify anti-- dengue compounds is essential. In recent years, natural products have gained attention for their antiviral properties. Plant-based medicines are particularly appealing due to their safety and low toxicity. This review summarizes natural compounds with potential antiviral activity against DENV, highlighting their mechanisms of action. Various compounds, from traditional herbal remedies to novel plant isolates, show promise against dengue, targeting crucial viral proteins like the envelope protein, proteases, and RNA polymerase. Exploring natural sources of antiviral agents against dengue is crucial. These compounds offer hope for effective treatments and mitigating dengue's global impact.
  3. Suleman M, Faizullah, Khan A, Mohammad Sayaf A, Alghamdi A, Alghamdi SA, et al.
    Curr Med Chem, 2024 Aug 27.
    PMID: 39253929 DOI: 10.2174/0109298673311962240815055821
    BACKGROUND: Colorectal cancer (CRC) stands as the third most widespread cancer worldwide in both men and women, witnessing a concerning rise, especially in younger demographics. Abnormal activation of the Non-Receptor Tyrosine Kinase c-Src has been linked to the advancement of several human cancers, including colorectal, breast, lung, and pancreatic ones. The interaction between c-Src and Hexokinase 2 (HK2) triggers enzyme phosphorylation, significantly boosting glycolysis, and ultimately contributing to the development of CRC.

    OBJECTIVES: The objectives of this study are to examine the influence of newly identified mutations on the interaction between c-Src and the HK2 enzyme and to discover potent phytocompounds capable of disrupting this interaction.

    METHODS: In this study, we utilized molecular docking to check the effect of the identified mutation on the binding of c-Src with HK2. Virtual drug screening, MD simulation, and binding free energy were employed to identify potent drugs against the binding interface of c-Src and HK2.

    RESULTS: Among these mutations, six (W151C, L272P, A296S, A330D, R391H, and P434A) were observed to significantly disrupt the stability of the c-Src structure. Additionally, through molecular docking analysis, we demonstrated that the mutant forms of c-Src exhibited high binding affinities with HK2. The wildtype showed a docking score of -271.80 kcal/mol, while the mutants displayed scores of -280.77 kcal/mol, -369.01 kcal/mol, -324.41 kcal/mol, -362.18 kcal/mol, 266.77 kcal/mol, and -243.28 kcal/mol for W151C, L272P, A296S, A330D, R391H, and P434A respectively. Furthermore, we identified five lead phytocompounds showing strong potential to impede the binding of c-Src with HK2 enzyme, essential for colon cancer progression. These compounds exhibit robust bonding with c-Src with docking scores of -7.37 kcal/mol, -7.26 kcal/mol, -6.88 kcal/mol, -6.81 kcal/mol, and -6.73 kcal/mol. Moreover, these compounds demonstrate dynamic stability, structural compactness, and the lowest residual fluctuation during MD simulation. The binding free energies for the top five hits (-42.44±0.28 kcal/mol, -28.31±0.25 kcal/mol, -34.95±0.44 kcal/mol, -38.92±0.25 kcal/mol, and -30.34±0.27 kcal/mol), further affirm the strong interaction of these drugs with c-Src which might impede the cascade of events that drive the progression of colon cancer.

    CONCLUSION: Our findings serve as a promising foundation, paving the way for future discoveries in the fight against colorectal cancer.

  4. Tjader NP, Beer AJ, Ramroop J, Tai MC, Ping J, Gandhi T, et al.
    Cancer Res Commun, 2024 Jun 27;4(6):1597-1608.
    PMID: 38836758 DOI: 10.1158/2767-9764.CRC-24-0026
    In breast tumors, somatic mutation frequencies in TP53 and PIK3CA vary by tumor subtype and ancestry. Emerging data suggest tumor mutation status is associated with germline variants and genetic ancestry. We aimed to identify germline variants that are associated with somatic TP53 or PIK3CA mutation status in breast tumors. A genome-wide association study was conducted in 2,850 women of European ancestry with breast cancer using TP53 and PIK3CA mutation status (positive or negative) as well as specific functional categories [e.g., TP53 gain-of-function (GOF) and loss-of-function, PIK3CA activating] as phenotypes. Germline variants showing evidence of association were selected for validation analyses and tested in multiple independent datasets. Discovery association analyses found five variants associated with TP53 mutation status with P values <1 × 10-6 and 33 variants with P values <1 × 10-5. Forty-four variants were associated with PIK3CA mutation status with P values <1 × 10-5. In validation analyses, only variants at the ESR1 locus were associated with TP53 mutation status after multiple comparisons corrections. Combined analyses in European and Malaysian populations found ESR1 locus variants rs9383938 and rs9479090 associated with the presence of TP53 mutations overall (P values 2 × 10-11 and 4.6 × 10-10, respectively). rs9383938 also showed association with TP53 GOF mutations (P value 6.1 × 10-7). rs9479090 showed suggestive evidence (P value 0.02) for association with TP53 mutation status in African ancestry populations. No other variants were significantly associated with TP53 or PIK3CA mutation status. Larger studies are needed to confirm these findings and determine if additional variants contribute to ancestry-specific differences in mutation frequency.

    SIGNIFICANCE: Emerging data show ancestry-specific differences in TP53 and PIK3CA mutation frequency in breast tumors suggesting that germline variants may influence somatic mutational processes. This study identified variants near ESR1 associated with TP53 mutation status and identified additional loci with suggestive association which may provide biological insight into observed differences.

    MeSH terms: Adult; Female; Humans; Middle Aged; Germ-Line Mutation*; Genetic Predisposition to Disease/genetics; Polymorphism, Single Nucleotide; European Continental Ancestry Group/genetics; Genome-Wide Association Study*
  5. King B, Greenhill SJ, Reid LA, Ross M, Walworth M, Gray RD
    Sci Rep, 2024 Jun 28;14(1):14967.
    PMID: 38942799 DOI: 10.1038/s41598-024-65810-x
    The Philippines are central to understanding the expansion of the Austronesian language family from its homeland in Taiwan. It remains unknown to what extent the distribution of Malayo-Polynesian languages has been shaped by back migrations and language leveling events following the initial Out-of-Taiwan expansion. Other aspects of language history, including the effect of language switching from non-Austronesian languages, also remain poorly understood. Here we apply Bayesian phylogenetic methods to a core-vocabulary dataset of Philippine languages. Our analysis strongly supports a sister group relationship between the Sangiric and Minahasan groups of northern Sulawesi on one hand, and the rest of the Philippine languages on the other, which is incompatible with a simple North-to-South dispersal from Taiwan. We find a pervasive geographical signal in our results, suggesting a dominant role for cultural diffusion in the evolution of Philippine languages. However, we do find some support for a later migration of Gorontalo-Mongondow languages to northern Sulawesi from the Philippines. Subsequent diffusion processes between languages in Sulawesi appear to have led to conflicting data and a highly unstable phylogenetic position for Gorontalo-Mongondow. In the Philippines, language switching to Austronesian in 'Negrito' groups appears to have occurred at different time-points throughout the Philippines, and based on our analysis, there is no discernible effect of language switching on the basic vocabulary.
    MeSH terms: Asian Americans; Bayes Theorem; Humans; Language*; Malaysia; Philippines; Phylogeny*; Polynesia; Taiwan; Asian Continental Ancestry Group; Human Migration*
  6. Yue S, Bajuri NH, Khatib SFA, Lee Y
    J Environ Manage, 2024 Nov;370:122423.
    PMID: 39243639 DOI: 10.1016/j.jenvman.2024.122423
    As new quality productivity (NQP) emerges as a rising star of productivity that can effectively leverage technological innovation and sustainability, this study aims to explore the relationship between NQP and environmental innovation, with a particular focus on the roles of managerial empowerment and board centralization within the context of China A-share listed companies. Utilizing the entire sample of China A-share market from 2013 to 2022, the study analyses the effectiveness of various dimensions reflecting innovation engagement among Chinese listed companies. For measuring NQP, the entropy method is employed to calculate the weights. By controlling for industry and year effects, the study examines both the main and moderating effects of managerial empowerment and board centralization. Additionally, heterogeneity tests, robustness checks, and two-stage least squares (2SLS) estimation were conducted to address endogeneity concerns. The results demonstrate that NQP significantly enhances environmental innovation, with managerial empowerment supporting this positive effect and board centralization obstructing it. The positive effect of NQP is particularly evident in state-owned enterprises, while in heavily polluting industries, the anticipated positive moderating effect of top managers disappears due to strict regulatory environments. Furthermore, board centralization negatively moderates environmental innovation, especially in lightly polluting sectors where internal governance is more sensitive. The study underscores the importance for policymakers to tailor regulations that balance managerial empowerment and board centralization to enhance the transformation of NQP into environmental innovation. Future research is needed to further investigate different background settings and the mechanisms through which NQP influences sustainability.
    MeSH terms: China; Efficiency; Humans; Industry; Inventions
  7. Muzammil K, Khaleel AQ, Merza MS, Kyada A, Ariffin IA, Verma S, et al.
    PMID: 39243880 DOI: 10.1016/j.prostaglandins.2024.106887
    BACKGROUND & AIMS: Taking into account the anti-inflammatory and antioxidant properties of omega-3 fatty acids and the evidence indicating the role of chronic inflammation and oxidative stress in the pathophysiology diabetes, this study aimed to determine the effect of ω-3 fatty acids on oxidative stress and inflammatory markers in Type 2 diabetes mellitus (T2DM) patients.

    METHODS: A systematic search up to July 30, 2023 was completed in Scopus, PubMed, Web of Science, and Embase databases, to identify eligible RCTs. Heterogeneity tests of the selected studies were performed using the I2. Random effects models were assessed and pooled data were determined as standardized mean differences (SMD) with a 95% CI.

    RESULTS: The meta-analysis of 23 trials, involving 1,523 patients, demonstrated a significant decrease in TNF-α (SMD: -1.62, 95% CI: -2.89 to -0.35, P= 0.013) and increase in TAC (SMD: 0.92, 95% CI: 0.33 to 1.52, P = 0.002) following ω-3 fatty acids administration. Meanwhile, supplementation did not have beneficial effects on malondialdehyde, C-reactive protein (CRP), superoxide dismutase (SOD), and interlukin-6 levels. The subgroup analysis revealed a significant decrease in CRP levels and an increase in SOD levels in studies with durations of less than 12 weeks.

    CONCLUSIONS: We found that ω-3 fatty acid intake can significantly decrease TNF-α and increase TAC levels, but this effect was not observed on other markers. Nevertheless, future well-designed with large sample size and long duration RCT studies with precise ω-3 fatty acids dose and ingredients are required to understand better the effects of these compounds and their constituents on oxidative stress and inflammatory markers in T2DM patients.

  8. Qutob M, Rafatullah M, Muhammad SA, Siddiqui MR, Alam M
    Chemosphere, 2024 Sep 06;364:143291.
    PMID: 39243904 DOI: 10.1016/j.chemosphere.2024.143291
    Nature iron is considered one of the promising catalysts in advanced oxidation processes (AOPs) that are utilized for soil remediation from polycyclic aromatic hydrocarbons (PAHs). However, the existence of anions, cations, and organic matter in soils considered impurities that restricted the utilization of iron that was harnessed naturally in the soil matrix and reduced the catalytic performance. In this regard, tropical soil naturally containing iron and relatively poor with impurities was artificially contaminated with 100 mg/50 g benzo[α]pyrene (B[α]P) and remediated using a slurry phase reactor supported with persulfate (PS). The results indicated that tropical soil containing iron and relatively poor with impurities capable of activating the oxidants and formation of radicals which successfully degraded B[α]P. The optimum removal result was 86% and obtained under the following conditions airflow = 260 mL/min, temperature 55 °C, pH 7, and [PS]0 = 1.0 g/L, at the same experimental conditions soil organic matter (SOM) mineralization was 48%. After the remediation process, there was a significant reduction in iron and aluminum contents, which considered the drawbacks of this system. Experiments to scavenge reactive species highlighted O2•- and SO4•- as the main radicals that oxidized B[α]P. Additionally, monitoring of by-products post-remediation aimed to assess toxicity and elucidate degradation pathways. Mutagenicity tests yielded positive results for two B[α]P by-products. The toxicity tests considered were the lethal concentration of 50% (LC50 96 h) for fat-head minnows revealed that all B[α]P by-products were less toxic than the parent pollutant itself. This research marks a significant advancement in soil remediation by advancing the use of the AOP method, removing the requirement for additional catalysts in the AOP system for the removal of B[α]P from soil.
  9. Kuwata K, Lum WM, Takahashi K, Benico G, Takahashi K, Lim PT, et al.
    Harmful Algae, 2024 Sep;138:102701.
    PMID: 39244236 DOI: 10.1016/j.hal.2024.102701
    Amphidoma languida, a marine thecate dinoflagellate that produces the lipophilic toxin azaspiracids (AZAs), is primarily found in the Atlantic. Although this species has not been recorded in the Asian Pacific, environmental DNAs related to Am. languida have been widely detected in the region by metabarcoding analysis. Their morphology and AZA production remain unclear. In this study, the morphology, ultrastructure, phylogeny, and AZA production of nine Amphidoma strains isolated from Japan, Malaysia, and Philippines were investigated. Phylogenetic trees inferred from rDNAs (SSU, ITS, and LSU rDNA) showed monophyly of the nine Pacific strains and were sister to the Am. languida clade, including the toxigenic strains from the Atlantic. Cells were ellipsoid, 8.7-16.7 µm in length and 7.4-14.0 µm in width, with a conspicuous apical pore complex. A large nucleus in the hyposome, parietal chloroplast with a spherical pyrenoid in the episome, and refractile bodies were observed. Thecal tabulation was typical of Amphidoma, Po, cp, X, 6', 6'', 6C, 5S, 6''', 2''''. A ventral pore was located on the anterior of 1' plate, beside the suture to 6' plate. The presence of a ventral depression, on the anterior of anterior sulcal plate, was different from Am. languida. A large antapical pore, containing approximately 10 small pores, was observed. Cells were apparently smaller than Am. trioculata, a species possessing three pores (ventral pore, ventral depression, and antapical pore). TEM showed the presence of crystalline structures, resembling guanine crystals, and cytoplasmic invaginations into the pyrenoid matrix. Flagellar apparatus lacking the striated root connective is similar to peridinioids and related dinoflagellates. AZAs were not detected from the Pacific strains by LC-MS/MS. This non-toxigenic Amphidoma species, here we propose as Amphidoma fulgens sp. nov., is widely distributed in the Asian Pacific. Moreover, molecular comparison also suggested that most of the environmental DNA sequences previously reported as Am. languida or related sequences from the Asian Pacific were attributable to Am. fulgens.
    MeSH terms: DNA, Ribosomal/genetics; Japan; Malaysia; Marine Toxins; Pacific Ocean; Philippines; Phylogeny*; Spiro Compounds
  10. Hashim NM, Mohd Husani NI, Wardani NI, Alahmad W, Shishov A, Madurani KA, et al.
    Anal Chim Acta, 2024 Oct 09;1325:342891.
    PMID: 39244296 DOI: 10.1016/j.aca.2024.342891
    Emerging pollutants pose an increasing threat to the environment and human well-being, requiring substantial progress in analytical methodologies. Dispersive micro-solid phase extraction (μ-dSPE) has proven successful in detecting and measuring these contaminants, particularly in trace quantities. However, challenges persist in achieving a uniform sorbent distribution and efficient separation from the sample matrix. To address these issues, effervescent-assisted dispersive micro-solid phase extraction (EA-μ-dSPE) was developed. This method uses on-site produced carbon dioxide as a dispersing agent, eliminating the need for vortexing or ultrasonication. Due to the sorbent dispersion in the sample solution, the contact surface between the analyte and the sorbent increases, resulting in increased extraction efficiency, reduced extraction time, and promotes of sustainability. Several parameters are critical to the successful execution of this procedure to extract the analytes, including the type and structure of sorbent, composition of dispersing agents, sorbent separation procedure, and type and properties of desorption solvents. The sorbent plays a critical role in successful extraction of emerging pollutants. It is clear that for the extraction of the analyte on the sorbent, proper interaction must be established between the analyte and the sorbent via physical and chemical interactions. This review thoroughly evaluates the underlying principles of the approach, its potential, and the significant advancements that have been documented. It explores the method's capacity to analyse and identify emerging pollutants, emphasising its potential across various sample matrices for enhanced pollutant identification and quantification.
  11. Sutin AR, Mansor N, Luchetti M, Stephan Y, Terracciano A
    Clin Gerontol, 2024 Sep 08.
    PMID: 39244651 DOI: 10.1080/07317115.2024.2400283
    OBJECTIVES: Evidence for the association between purpose in life and cognitive health is primarily from North American and European samples. This study evaluates this association in a large sample from Malaysia, an upper-middle-income country in Southeast Asia.

    METHODS: Participants (N = 5,579) from the Malaysian Ageing and Retirement Study reported on their purpose in life and subjective memory and were administered tasks that measured episodic memory, verbal fluency, and overall cognitive function.

    RESULTS: Purpose was associated with better subjective memory (β=.13), episodic memory (β=.06), verbal fluency (β=.12), and overall cognitive function (β=.07) (ps 

  12. Binti Md Bahar AN, Muhamad AN, Teh CSJ, Adnan MS, Adam S, Hng SY, et al.
    Pathog Glob Health, 2024 Sep 08.
    PMID: 39244781 DOI: 10.1080/20477724.2024.2400412
    INTRODUCTION AND AIM: In Malaysia, pertussis in children beyond infancy is underreported. This study aimed to determine the prevalence of Bordetella pertussis and the prevalence of pertussis-susceptible children aged ≥4 years who presented with acute respiratory infections.

    METHODS: This single-center, cross-sectional study conducted at the Paediatric Emergency Department from 1 October 2022, to 31 January 2023, included children aged 4 years and older with ARTIs symptoms and excluded those who were COVID-19 positive. B. pertussis was detected via quantitative Polymerase Chain Reaction on nasopharyngeal swabs and pertussis toxin (PT) IgG enzyme-linked immunosorbent assay.

    RESULTS: Children (n = 298) with a median (Interquartile range, [IQR]) age of 6.0 (5.0, 8.0) years old were recruited, and 98% were vaccinated adequately. Two cases of B. pertussis (n = 2/298, 0.67%) were detected. Both children were also co-infected with Bordetella spp. The majority of the patients (n = 246/296, 83.1%) had low protective antibodies against pertussis (anti-PT IgG <5 IU/ml), and children 5 years and older were more likely to have lower anti-PT Ig G levels of <5 IU/ml (odds ratio 2.02 [95% CI 1.04,3.90]) compared to children 4 years old.

    CONCLUSION: The prevalence of pertussis was low. However, there is significant waning immunity. Booster doses of pertussis vaccine should be given to all school-aged children.

  13. Mebarak M, Maïano C, Mendoza J, Zamora Á, Baños R, Desdentado L, et al.
    Body Image, 2024 Dec;51:101787.
    PMID: 39244790 DOI: 10.1016/j.bodyim.2024.101787
    The Functionality Appreciation Scale (FAS) is increasingly used in diverse national and linguistic contexts. However, limited work has assessed the extent to which the instrument demonstrates measurement invariance and differential item functioning (DIF) across nations and respondent characteristics. Here, we examined measurement invariance and DIF of the FAS using archival data from adults in Colombia (Mebarak et al., 2023) and Spain (Zamora et al., 2024). Participants included 1420 (women n = 804, men n = 616) respondents from Colombia and 838 (women n = 415, men n = 423) respondents from Spain who completed translations of the FAS. Confirmatory factor analysis supported a unidimensional structure of the FAS in both national groups. Additionally, the FAS achieved full measurement invariance (up to latent mean invariance) across both groups. We also found that the FAS lacked DIF as a function of age, body mass index (BMI), and gender identity across both national groups. Older participants (relative to younger participants), men (relative to women), and participants with lower BMIs (relative to those with higher BMIs) had higher FAS scores. These results support the notion that the FAS is measuring a common underlying construct across these national groups and respondent characteristics.
    MeSH terms: Adolescent; Adult; Aged; Body Image/psychology; Colombia; Factor Analysis, Statistical; Female; Gender Identity; Humans; Male; Middle Aged; Personal Satisfaction; Psychometrics*; Surveys and Questionnaires; Spain; Reproducibility of Results; Body Mass Index; Young Adult
  14. Mawazi SM, Fathima N, Mahmood S, Al-Mahmood SMA
    Am J Emerg Med, 2024 Sep 04;85:98-107.
    PMID: 39244809 DOI: 10.1016/j.ajem.2024.09.001
    The COVID-19 epidemic has become a major international health emergency. Millions of people have died as a result of this phenomenon since it began. Has there been any successful pharmacological treatment for COVID-19 since the initial report on the virus? How many searches are undertaken to address the impact of the infection? What is the number of drugs that have undergone investigation? What are the mechanisms of action and adverse effects associated with the investigated pharmaceuticals used to treat COVID-19? Has the Food and Drug Administration (FDA) approved any medication to treat COVID-19? To date, our understanding is based on a restricted corpus of published investigations into the treatment of COVID-19. It is important to note that no single study comprehensively encompasses all pharmacological interventions for COVID-19. This paper provides an introductory summary of a bibliometric analysis conducted on the data about COVID-19, sourced explicitly from two platforms, namely PubMed and ScienceDirect. The analysis encompasses the period spanning from 2019 to 2022. Furthermore, this study examines the published literature about the pharmacological interventions for the novel coronavirus disease 2019 (COVID-19), explicitly focusing on the safety and effectiveness of different medications such as Remdesivir (marketed as Veklury®), Lopinavir/Ritonavir (commercially known as Kaletra® or Aluvia®), Ribavirin, Favipiravir (marketed as Avigan®), Ivermectin, Casirivimab and Imdevimab (branded as Ronapreve®), Sotrovimab (marketed as Xevudy®), Anakinra, Molnupiravir, Nirmatrelvir/Ritonavir (marketed as Paxlovid®), and Galidesivir. Findings indicate that while Remdesivir and Nirmatrelvir/Ritonavir show significant efficacy in reducing hospitalization and severe outcomes, drugs like Lopinavir/Ritonavir and Ivermectin have inconsistent results. Our insights suggest a multifaceted approach incorporating these therapies can significantly improve patient outcomes. Repurposing drugs has been critical in rapidly responding to COVID-19, allowing existing medications to be used in new ways to combat the virus. Combination therapies and further research are essential to optimize treatment strategies.
  15. Lekkala R, Ng YH, Feroz SR, Norazmi NAZB, Ali AH, Hasbullah SA, et al.
    Eur J Med Chem, 2024 Sep 05;279:116828.
    PMID: 39244861 DOI: 10.1016/j.ejmech.2024.116828
    In this work, a series of nineteen novel pyrano[2,3-c]pyrazole-4-aminoquinoline hybrids were synthesized as potent antimalarial agents by covalently linking the scaffolds of 4-aminoquinoline and pyrano[2,3-c]pyrazoles via an ethyl linker and characterized using Fourier transform infrared spectroscopy (FTIR) and nuclear magnetic resonance spectroscopy (NMR). Molecular docking was used to test each hybrid's and standard chloroquine's ability to bind to Plasmodium falciparum lactate dehydrogenase enzyme (PfLDH), an important enzyme in the parasite's glycolytic pathway. The hybrid compounds had a stronger binding affinity than the standard chloroquine (CQ). The schizontical antimalarial test of pyrano[2,3-c]pyrazole-4-aminoquinoline hybrid compound shows that all nineteen hybrid compounds were potent with the IC50 values ranging from 0.0151 to 0.301 μM against the CQ-sensitive 3D7 P. falciparum strain, and were active against the CQ-resistant K1 P. falciparum strain with the IC50 values ranging from 0.01895 to 2.746 μM. All the tested hybrid compounds were less potent than the standard drug chloroquine dipaspate (CQDP) against the CQ-sensitive 3D7 strain. In contrast, nine of the nineteen hybrids (16d, 16g, 16h, 16i, 16l, 16n, 16o, 16r, and 16s) displayed superior antimalarial activity than the CQDP against the CQ-resistant K1 P. falciparum strain. Among all the tested hybrids, 16c against the 3D7 strain and 16h against the K1 strain were the most promising antimalarial agents with 0.0151 and 0.01895 μM of IC50 values, respectively. In addition, the compounds were selective, showing moderate to low cytotoxic activity against a human normal liver WRL68 cell line. The synthesis of pyrano[2,3-c]pyrazole-4-aminoquinoline hybrids introduces new chemical entities that have the potential to exhibit potent antimalarial activity. It could address the ongoing challenge of drug resistance in malaria treatment.
  16. Zhao Z, Qiao S, Jin Z, Li H, Yu H, Zhang C, et al.
    Int J Biol Macromol, 2024 Sep 07;279(Pt 3):135424.
    PMID: 39245128 DOI: 10.1016/j.ijbiomac.2024.135424
    Oral vaccines are generally perceived to be safe, easy to administer, and have the potential to induce both systemic and mucosal immune responses. However, given the challenges posed by the harsh gastrointestinal environment and mucus barriers, the development of oral vaccines necessitates the employment of a safe and efficient delivery system. In recent years, nanoparticle-based delivery has proven to be an ideal delivery vector for the manufacture of oral vaccines. Hence, considering the above, the sucralfate acidified (SA) encapsulated N-2-Hydroxypropyl trimethyl ammonium chloride chitosan (N-2-HACC)/N,O-carboxymethyl chitosan (CMCS) nanoparticles (SA@N-2-HACC/CMCS NPs) were prepared, and the BSA was used as a model antigen to investigate the immune responses. The SA@N-2-HACC/CMCS NPs had a particle size of 227 ± 7.0 nm and a zeta potential of 8.43 ± 2.62 mV. The NPs displayed slow and sustained release and high stability in simulated gastric juice and intestinal fluid. RAW 264.7 macrophage-like cell line demonstrated enhanced uptake of the SA@N-2-HACC/CMCS/BSA Nps. The vaccine via oral administration markedly enhanced the residence time of BSA in the intestine for more than 12 h and elicited the production of IgG and sIgA. The SA@N-2-HACC/CMCS NPs developed here for oral administration is an excellent technique for delivering antigens and provides a path of mucosal vaccine research.
  17. Kazim AR, Low VL, Houssaini J, Tappe D, Heo CC
    Acta Trop, 2024 Sep 06.
    PMID: 39245158 DOI: 10.1016/j.actatropica.2024.107383
    A Trypanosoma screening was conducted on 130 pools comprising 1,241 ticks, collected from 674 selected farm ruminants in Peninsular Malaysia. Of these, nine pools were tested positive for Trypanosoma. Subsequent BLAST searches revealed that the 18S rRNA gene sequences were closely related to Trypanosoma rhipicephalis isolate Chaco CB, with percentage similarities ranging from 95.56% to 99.84%. Phylogenetic analysis showed that three of the nine sequences formed a clade with Trypanosoma rhipicephalis. The remaining six Trypanosoma sequences formed a distinct clade, separate from T. rhipicephalis and other Trypanosoma species, with genetic distances of 4.34% and 4.33-4.58%, respectively. This study marks the first report of tick-associated Trypanosoma in Malaysia and underscores significant research gaps regarding trypanosome interactions with tick hosts in the region.
  18. Haryani Y, Halid NA, Guat GS, Nor-Khaizura MAR, Hatta MAM, Sabri S, et al.
    J Biotechnol, 2024 Sep 06.
    PMID: 39245212 DOI: 10.1016/j.jbiotec.2024.09.002
    Lactic acid bacteria (LAB) are known to exhibit various beneficial roles in fermentation, serving as probiotics, and producing a plethora of valuable compounds including compounds with antimicrobial activity including bacteriocin-like inhibitory substance (BLIS) that can be used as biopreservative to improve food safety and quality. However, the yield of BLIS is often limited, which poses a challenge to be commercially competitive with the current preservation practice. Therefore, the present work aimed to establish an optimised two-plasmid CRISPR/Cas9 system to redirect the carbon flux away from lactate towards compounds with antimicrobial activity by disrupting lactate dehydrogenase gene (ldh) on various strains of LAB. The lactic acid-deficient (ldhΔ) strains caused a metabolic shift resulting in increased inhibitory activity against selected foodborne pathogens up to 78% than the wild-type (WT) strain. The most significant effect was depicted by Enterococcus faecalis-ldh∆ which displayed prominent bactericidal effects against all foodborne pathogens as compared to the WT that showed no antimicrobial activity. The present work provided a framework model for economically important LAB and other beneficial bacteria to synthesise and increase the yield of valuable food and industrial compounds. The present work reported for the first time that the metabolism of selected LAB can be manipulated by modifying ldh to attain metabolites with higher antimicrobial activity.
  19. Dewika M, Markandan K, Ruwaida JN, Sara YY, Deb A, Irfan NA, et al.
    Sci Total Environ, 2024 Dec 01;954:176063.
    PMID: 39245389 DOI: 10.1016/j.scitotenv.2024.176063
    Microplastic pollution has become a major global environmental issue, negatively impacting terrestrial and aquatic ecosystems as well as human health. Tackling this complex problem necessitates a multidisciplinary approach and collaboration among diverse stakeholders. Within this context, the Quintuple Helix framework, which highlights the involvement of academia, government, industry, civil society, and the environment, provides a comprehensive and inclusive perspective for formulating effective policies to manage atmospheric microplastics. This paper discusses each helix's roles, challenges, and opportunities and proposes strategies for collaboration and knowledge exchange among them. Furthermore, the paper highlights the importance of interdisciplinary research, innovative technologies, public awareness campaigns, regulatory frameworks, and corporate responsibility in achieving sustainable and resilient microplastic management policies. The Quintuple Helix approach can mitigate microplastics, safeguard ecosystems, and preserve planetary health by fostering collaboration and coordination among diverse stakeholders.
    MeSH terms: Air Pollutants/analysis; Environmental Monitoring; Ecosystem; Environmental Policy*
External Links