Displaying publications 721 - 740 of 1094 in total

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  1. Fulltext Nutraceuticals and mitochondrial oxidative stress: bridging the gap in the management of bronchial asthma
    Allam VSRR, Paudel KR, Gupta G, Singh SK, Vishwas S, Gulati M, et al.
    Environ Sci Pollut Res Int, 2022 Sep;29(42):62733-62754.
    PMID: 35796922 DOI: 10.1007/s11356-022-21454-w
    Asthma is a chronic inflammatory disease primarily characterized by inflammation and reversible bronchoconstriction. It is currently one of the leading causes of morbidity and mortality in the world. Oxidative stress further complicates the pathology of the disease. The current treatment strategies for asthma mainly involve the use of anti-inflammatory agents and bronchodilators. However, long-term usage of such medications is associated with severe adverse effects and complications. Hence, there is an urgent need to develop newer, novel, and safe treatment modalities for the management of asthma. This has therefore prompted further investigations and detailed research to identify and develop novel therapeutic interventions from potent untapped resources. This review focuses on the significance of oxidative stressors that are primarily derived from both mitochondrial and non-mitochondrial sources in initiating the clinical features of asthma. The review also discusses the biological scavenging system of the body and factors that may lead to its malfunction which could result in altered states. Furthermore, the review provides a detailed insight into the therapeutic role of nutraceuticals as an effective strategy to attenuate the deleterious effects of oxidative stress and may be used in the mitigation of the cardinal features of bronchial asthma.
  2. Fulltext Synthesis and docking studies of 2,4,6-trihydroxy-3-geranylacetophenone analogs as potential lipoxygenase inhibitor
    Ng CH, Rullah K, Aluwi MF, Abas F, Lam KW, Ismail IS, et al.
    Molecules, 2014;19(8):11645-59.
    PMID: 25100256 DOI: 10.3390/molecules190811645
    The natural product molecule 2,4,6-trihydroxy-3-geranyl-acetophenone (tHGA) isolated from the medicinal plant Melicope ptelefolia was shown to exhibit potent lipoxygenase (LOX) inhibitory activity. It is known that LOX plays an important role in inflammatory response as it catalyzes the oxidation of unsaturated fatty acids, such as linoleic acid to form hydroperoxides. The search for selective LOX inhibitors may provide new therapeutic approach for inflammatory diseases. Herein, we report the synthesis of tHGA analogs using simple Friedel-Craft acylation and alkylation reactions with the aim of obtaining a better insight into the structure-activity relationships of the compounds. All the synthesized analogs showed potent soybean 15-LOX inhibitory activity in a dose-dependent manner (IC50 = 10.31-27.61 μM) where compound 3e was two-fold more active than tHGA. Molecular docking was then applied to reveal the important binding interactions of compound 3e in soybean 15-LOX binding site. The findings suggest that the presence of longer acyl bearing aliphatic chain (5Cs) and aromatic groups could significantly affect the enzymatic activity.
  3. The potential hazards of Aspergillus sp. in foods and feeds, and the role of biological treatment: a review
    Sheikh-Ali SI, Ahmad A, Mohd-Setapar SH, Zakaria ZA, Abdul-Talib N, Khamis AK, et al.
    J Microbiol, 2014 Oct;52(10):807-18.
    PMID: 25269603 DOI: 10.1007/s12275-014-4294-7
    The contamination of food and feed by Aspergillus has become a global issue with a significant worldwide economic impact. The growth of Aspergillus is unfavourable to the development of food and feed industries, where the problems happen mostly due to the presence of mycotoxins, which is a toxic metabolite secreted by most Aspergillus groups. Moreover, fungi can produce spores that cause diseases, such as allergies and asthma, especially to human beings. High temperature, high moisture, retarded crops, and poor food storage conditions encourage the growth of mold, as well as the development of mycotoxins. A variety of chemical, biological, and physical strategies have been developed to control the production of mycotoxins. A biological approach, using a mixed culture comprised of Saccharomyces cerevisiae and Lactobacillus rhamnosus resulted in the inhibition of the growth of fungi when inoculated into fermented food. The results reveal that the mixed culture has a higher potential (37.08%) to inhibit the growth of Aspergillus flavus (producer of Aflatoxin) compared to either single culture, L. rhamnosus NRRL B-442 and S. cerevisiae, which inhibit the growth by 63.07% and 64.24%, respectively.
  4. Fulltext Advancements in transmitters and sensors for biological tissue imaging in magnetic induction tomography
    Zakaria Z, Abdul Rahim R, Mansor MS, Yaacob S, Ayub NM, Muji SZ, et al.
    Sensors (Basel), 2012;12(6):7126-56.
    PMID: 22969341 DOI: 10.3390/s120607126
    Magnetic Induction Tomography (MIT), which is also known as Electromagnetic Tomography (EMT) or Mutual Inductance Tomography, is among the imaging modalities of interest to many researchers around the world. This noninvasive modality applies an electromagnetic field and is sensitive to all three passive electromagnetic properties of a material that are conductivity, permittivity and permeability. MIT is categorized under the passive imaging family with an electrodeless technique through the use of excitation coils to induce an electromagnetic field in the material, which is then measured at the receiving side by sensors. The aim of this review is to discuss the challenges of the MIT technique and summarize the recent advancements in the transmitters and sensors, with a focus on applications in biological tissue imaging. It is hoped that this review will provide some valuable information on the MIT for those who have interest in this modality. The need of this knowledge may speed up the process of adopted of MIT as a medical imaging technology.
  5. Successful treatment of very large congenital infantile fibrosarcoma
    Hamidah A, Reena M, Halim ARA, Ibrahim S, Eguchi M, Zarina AL, et al.
    Pediatr Int, 2011 Oct;53(5):768-770.
    PMID: 21955012 DOI: 10.1111/j.1442-200X.2011.03358.x
  6. Breast Cancer Survival at a Leading Cancer Centre in Malaysia
    Abdullah MM, Mohamed AK, Foo YC, Lee CM, Chua CT, Wu CH, et al.
    Asian Pac J Cancer Prev, 2015;16(18):8513-7.
    PMID: 26745110
    BACKGROUND: GLOBOCAN12 recently reported high cancer mortality in Malaysia suggesting its cancer health services are under-performing. Cancer survival is a key index of the overall effectiveness of health services in the management of patients. This report focuses on Subang Jaya Medical Centre (SJMC) care performance as measured by patient survival outcome for up to 5 years.

    MATERIALS AND METHODS: All women with breast cancer treated at SJMC between 2008 and 2012 were enrolled for this observational cohort study. Mortality outcome was ascertained through record linkage with national death register, linkage with hospital registration system and finally through direct contact by phone or home visits.

    RESULTS: A total of 675 patients treated between 2008 and 2012 were included in the present survival analysis, 65% with early breast cancer, 20% with locally advanced breast cancer (LABC) and 4% with metastatic breast cancer (MBC). The overall relative survival (RS) at 5 years was 88%. RS for stage I was 100% and for stage II, III and IV disease was 95%, 69% and 36% respectively.

    CONCLUSIONS: SJMC is among the first hospitals in Malaysia to embark on routine measurement of the performance of its cancer care services and its results are comparable to any leading centers in developed countries.

  7. Potential anti-epileptic phytoconstituents: An updated review
    Kaur J, Famta P, Famta M, Mehta M, Satija S, Sharma N, et al.
    J Ethnopharmacol, 2021 Mar 25;268:113565.
    PMID: 33166627 DOI: 10.1016/j.jep.2020.113565
    ETHNOPHARMACOLOGICAL RELEVANCE: Epilepsy is one of the most commonly occurring non-communicable neurological disorder that affects people of all age groups. Around 50 million people globally are epileptic, with 80% cases in developing countries due to lack of access to treatments determined by high cost and poor availability or it can be defined by the fraction of active epileptic patients who are not appropriately being treated. The availability of antiepileptic drugs and their adjuvant therapy in such countries is less than 50% and these are highly susceptible to drug interactions and severe adverse effects. As a result, the use of herbal medicine is increasingly becoming popular.

    AIM OF THE STUDY: To provide pharmacological information on the active constituents evaluated in the preclinical study to treat epilepsy with potential to be used as an alternative therapeutic option in future. It also provides affirmation for the development of novel antiepileptic drugs derived from medicinal plants.

    MATERIALS AND METHODS: Relevant information on the antiepileptic potential of phytoconstituents in the preclinical study (in-vitro, in-vivo) is provided based on their effect on screening parameters. Besides, relevant information on pharmacology of phytoconstituents, the traditional use of their medicinal plants related to epilepsy and status of phytoconstituents in the clinical study were derived from online databases, including PubMed, Clinicaltrial. gov, The Plant List (TPL, www.theplantlist.org), Science Direct. Articles identified using preset searching syntax and inclusion criteria are presented.

    RESULTS: More than 70% of the phytoconstituents reviewed in this paper justified the traditional use of their medicinal plant related to epilepsy by primarily acting on the GABAergic system. Amongst the phytoconstituents, only cannabidiol and tetrahydrocannabinol have been explored for clinical application in epilepsy.

    CONCLUSION: The preclinical and clinical data of the phytoconstituents to treat epilepsy and its associated comorbidities provides evidence for the discovery and development of novel antiepileptic drugs from medicinal plants. In terms of efficacy and safety, further randomized and controlled clinical studies are required to understand the complete pharmacodynamic and pharmacokinetic picture of phytoconstituents. Also, specific botanical source evaluation is needed.

  8. Drug delivery advances in mitigating inflammation via matrix metalloproteinases in respiratory diseases
    Mehta M, Paudel KR, Panth N, Xenaki D, Macloughlin R, Oliver BG, et al.
    Nanomedicine (Lond), 2021 03;16(6):437-439.
    PMID: 33599533 DOI: 10.2217/nnm-2021-0016
  9. Targeting Cancer using Curcumin Encapsulated Vesicular Drug Delivery Systems
    Hardwick J, Taylor J, Mehta M, Satija S, Paudel KR, Hansbro PM, et al.
    Curr Pharm Des, 2021;27(1):2-14.
    PMID: 32723255 DOI: 10.2174/1381612826666200728151610
    Curcumin is a major curcuminoid present in turmeric. The compound is attributed to various therapeutic properties, which include anti-oxidant, anti-inflammatory, anti-bacterial, anti-malarial, and neuroprotection. Due to its therapeutic potential, curcumin has been employed for centuries in treating different ailments. Curcumin has been investigated lately as a novel therapeutic agent in the treatment of cancer. However, the mechanisms by which curcumin exerts its cytotoxic effects on malignant cells are still not fully understood. One of the main limiting factors in the clinical use of curcumin is its poor bioavailability and rapid elimination. Advancements in drug delivery systems such as nanoparticle-based vesicular drug delivery platforms have improved several parameters, namely, drug bioavailability, solubility, stability, and controlled release properties. The use of curcumin-encapsulated niosomes to improve the physical and pharmacokinetic properties of curcumin is one such approach. This review provides an up-to-date summary of nanoparticle-based vesicular drug carriers and their therapeutic applications. Specifically, we focus on niosomes as novel drug delivery formulations and their potential in improving the delivery of challenging small molecules, including curcumin. Overall, the applications of such carriers will provide a new direction for novel pharmaceutical drug delivery, as well as for biotechnology, nutraceutical, and functional food industries.
  10. Advancing of Cellular Signaling Pathways in Respiratory Diseases Using Nanocarrier Based Drug Delivery Systems
    Mehta M, Dhanjal DS, Satija S, Wadhwa R, Paudel KR, Chellappan DK, et al.
    Curr Pharm Des, 2020;26(42):5380-5392.
    PMID: 33198611 DOI: 10.2174/1381612826999201116161143
    Cell Signaling pathways form an integral part of our existence that allows the cells to comprehend a stimulus and respond back. Such reactions to external cues from the environment are required and are essential to regulate the normal functioning of our body. Abnormalities in the system arise when there are errors developed in these signals, resulting in a complication or a disease. Presently, respiratory diseases contribute to being the third leading cause of morbidity worldwide. According to the current statistics, over 339 million people are asthmatic, 65 million are suffering from COPD, 2.3 million are lung cancer patients and 10 million are tuberculosis patients. This toll of statistics with chronic respiratory diseases leaves a heavy burden on society and the nation's annual health expenditure. Hence, a better understanding of the processes governing these cellular pathways will enable us to treat and manage these deadly respiratory diseases effectively. Moreover, it is important to comprehend the synergy and interplay of the cellular signaling pathways in respiratory diseases, which will enable us to explore and develop suitable strategies for targeted drug delivery. This review, in particular, focuses on the major respiratory diseases and further provides an in-depth discussion on the various cell signaling pathways that are involved in the pathophysiology of respiratory diseases. Moreover, the review also analyses the defining concepts about advanced nano-drug delivery systems involving various nanocarriers and propose newer prospects to minimize the current challenges faced by researchers and formulation scientists.
  11. Fulltext Fabrication of Gum Arabic-Graphene (GGA) Modified Polyphenylsulfone (PPSU) Mixed Matrix Membranes: A Systematic Evaluation Study for Ultrafiltration (UF) Applications
    Ali AM, Rashid KT, Yahya AA, Majdi HS, Salih IK, Yusoh K, et al.
    Membranes (Basel), 2021 Jul 16;11(7).
    PMID: 34357192 DOI: 10.3390/membranes11070542
    In the current work, a Gum, Arabic-modified Graphene (GGA), has been synthesized via a facile green method and employed for the first time as an additive for enhancement of the PPSU ultrafiltration membrane properties. A series of PPSU membranes containing very low (0-0.25) wt.% GGA were prepared, and their chemical structure and morphology were comprehensively investigated through atomic force microscopy (AFM), Fourier transforms infrared spectroscopy (FTIR), X-ray diffraction (XRD), and field emission scanning electron microscopy (FESEM). Besides, thermogravimetric analysis (TGA) was harnessed to measure thermal characteristics, while surface hydrophilicity was determined by the contact angle. The PPSU-GGA membrane performance was assessed through volumetric flux, solute flux, and retention of sodium alginate solution as an organic polysaccharide model. Results demonstrated that GGA structure had been successfully synthesized as confirmed XRD patterns. Besides, all membranes prepared using low GGA content could impart enhanced hydrophilic nature and permeation characteristics compared to pristine PPSU membranes. Moreover, greater thermal stability, surface roughness, and a noticeable decline in the mean pore size of the membrane were obtained.
  12. Fulltext Phytochemical Constituents and Allelopathic Potential of Parthenium hysterophorus L. in Comparison to Commercial Herbicides to Control Weeds
    Motmainna M, Juraimi AS, Uddin MK, Asib NB, Islam AKMM, Ahmad-Hamdani MS, et al.
    Plants (Basel), 2021 Jul 15;10(7).
    PMID: 34371648 DOI: 10.3390/plants10071445
    The allelopathic effect of various concentrations (0, 6.25, 12.5, 50 and 100 g L-1) of Parthenium hysterophorus methanol extract on Cyperus iria was investigated under laboratory and glasshouse conditions. No seed germination was recorded in the laboratory when P. hysterophorus extract was applied at 50 g L-1. In the glasshouse, C. iria was mostly injured by P. hysterophorus extract at 100 g L-1. The phytochemical constituents of the methanol extract of P. hysterophorus were analyzed by LC-ESI-QTOF-MS=MS. The results indicated the presence of phenolic compounds, terpenoids, alkaloids, amino acids, fatty acids, piperazines, benzofuran, indole, amines, azoles, sulfonic acid and other unknown compounds in P. hysterophorus methanol extract. A comparative study was also conducted between P. hysterophorus extract (20, 40 and 80 g L-1) with a synthetic herbicide (glyphosate and glufosinate ammonium at 2 L ha-1) as a positive control and no treatment (negative control) on Ageratumconyzoides, Oryzasativa and C. iria. The growth and biomass of test weeds were remarkably inhibited by P. hysterophorus extract. Nevertheless, no significant difference was obtained when P. hysterophorus extract (80 g L-1) and synthetic herbicides (glyphosate and glufosinate ammonium) were applied on A.conyzoides.
  13. Emerging trends in nanomedicine for topical delivery in skin disorders: Current and translational approaches
    Pandey P, Satija S, Wadhwa R, Mehta M, Purohit D, Gupta G, et al.
    Dermatol Ther, 2020 05;33(3):e13292.
    PMID: 32126154 DOI: 10.1111/dth.13292
  14. In vitro evaluation of the involvement of Nrf2 in maslinic acid-mediated anti-inflammatory effects in atheroma pathogenesis
    Ooi BK, Phang SW, Yong PVC, Chellappan DK, Dua K, Khaw KY, et al.
    Life Sci, 2021 Aug 01;278:119658.
    PMID: 34048809 DOI: 10.1016/j.lfs.2021.119658
    AIMS: Maslinic acid (MA) is a naturally occurring pentacyclic triterpene known to exert cardioprotective effects. This study aims to investigate the involvement of nuclear factor erythroid 2-related factor 2 (Nrf2) for MA-mediated anti-inflammatory effects in atheroma pathogenesis in vitro, including evaluation of tumor necrosis factor-alpha (TNF-α)-induced monocyte recruitment, oxidized low-density lipoprotein (oxLDL)-induced scavenger receptors expression, and nuclear factor-kappa B (NF-ĸB) activity in human umbilical vein endothelial cells (HUVECS) and human acute monocytic leukemia cell line (THP-1) macrophages.

    MATERIALS AND METHODS: An in vitro monocyte recruitment model utilizing THP-1 and HUVECs was developed to evaluate TNF-α-induced monocyte adhesion and trans-endothelial migration. To study the role of Nrf2 for MA-mediated anti-inflammatory effects, Nrf2 inhibitor ML385 was used as the pharmacological inhibitor. The expression of Nrf2, monocyte chemoattractant protein-1 (MCP-1), vascular cell adhesion molecule 1 (VCAM-1), cluster of differentiation 36 (CD36), and scavenger receptor type A (SR-A) in HUVECs and THP-1 macrophages were investigated using RT-qPCR and Western blotting. The NF-κB activity was determined using NF-κB (p65) Transcription Factor Assay Kit.

    KEY FINDINGS: The results showed opposing effects of MA on Nrf2 expression in HUVECs and THP-1 macrophages. MA suppressed TNF-α-induced Nrf2 expression in HUVECs, but enhanced its expression in THP-1 macrophages. Combined effects of MA and ML385 suppressed MCP-1, VCAM-1, and SR-A expressions. Intriguingly, at the protein level, ML385 selectively inhibited SR-A but enhanced CD36 expression. Meanwhile, ML385 further enhanced MA-mediated inhibition of NF-κB activity in HUVECs. This effect, however, was not observed in THP-1 macrophages.

    SIGNIFICANCE: MA attenuated foam cell formation by suppressing VCAM-1, MCP-1, and SR-A expression, as well as NF-κB activity, possibly through Nrf2 inhibition. The involvement of Nrf2 for MA-mediated anti-inflammatory effects however differs between HUVECs and macrophages. Future investigations are warranted for a detailed evaluation of the contributing roles of Nrf2 in foam cells formation.

  15. Fulltext Physiological and Biochemical Responses of Ageratum conyzoides, Oryza sativa f. spontanea (Weedy Rice) and Cyperus iria to Parthenium hysterophorus Methanol Extract
    Motmainna M, Juraimi AS, Uddin MK, Asib NB, Islam AKMM, Ahmad-Hamdani MS, et al.
    Plants (Basel), 2021 Jun 14;10(6).
    PMID: 34198474 DOI: 10.3390/plants10061205
    The current study was designed to investigate the effect of Parthenium hysterophorus L. methanol extract on Ageratum conyzoides L., Oryza sativa f. spontanea (weedy rice) and Cyperus iria L. in glasshouse condition. Here, Parthenium hysterophorus methanol extract at 20, 40, and 60 g L-1 concentrations was applied on the test species to examine their physiological and biochemical responses at 6, 24, 48 and 72 h after spraying (HAS). The phytotoxicity of P. hysterophorus was strong on A. conyzoides compared to weedy rice and Cyperus iria at different concentrations and exposure times. There was a reduction in photosynthesis rate, stomatal conductance, transpiration, chlorophyll content and carotenoid content when plants were treated with P. hysterophorus extract concentrations. Exposure to P. hysterophorus (60 g L-1) at 24 HAS increased malondialdehyde (MDA) and proline content by 152% and 130%, respectively, in A. conyzoides compared with control. The activities of antioxidant enzymes (superoxide dismutase (SOD), catalase (CAT) and peroxidase (POD)) were also increased in the presence of P. hysterophorus extract. Present findings confirm that the methanol extract of P. hysterophorus can disrupt the physiological and biochemical mechanism of target weeds and could be used as an alternative to chemical herbicides.
  16. Fulltext Axial Compressive Strength Models of Eccentrically-Loaded Rectangular Reinforced Concrete Columns Confined with FRP
    Isleem HF, Abid M, Alaloul WS, Shah MK, Zeb S, Musarat MA, et al.
    Materials (Basel), 2021 Jun 23;14(13).
    PMID: 34201659 DOI: 10.3390/ma14133498
    The majority of experimental and analytical studies on fiber-reinforced polymer (FRP) confined concrete has largely concentrated on plain (unreinforced) small-scale concrete columns, on which the efficiency of strengthening is much higher compared with large-scale columns. Although reinforced concrete (RC) columns subjected to combined axial compression and flexural loads (i.e., eccentric compression) are the most common structural elements used in practice, research on eccentrically-loaded FRP-confined rectangular RC columns has been much more limited. More specifically, the limited research has generally been concerned with small-scale RC columns, and hence, the proposed eccentric-loading stress-strain models were mainly based on the existing concentric-loading models of FRP-confined concrete columns of small scale. In the light of such demand to date, this paper is aimed at developing a mathematical model to better predict the strength of FRP-confined rectangular RC columns. The strain distribution of FRP around the circumference of the rectangular sections was investigated to propose equations for the actual rupture strain of FRP wrapped in the horizontal and vertical directions. The model was accomplished using 230 results of 155 tested specimens compiled from 19 studies available in the technical literature. The test database covers an unconfined concrete strength ranging between 9.9 and 73.1 MPa, and section's dimension ranging from 100-300 mm and 125-435 mm for the short and long sides, respectively. Other test parameters, such as aspect ratio, corner radius, internal hoop steel reinforcement, FRP wrapping layout, and number of FRP wraps were all considered in the model. The performance of the model shows a very good correlation with the test results.
  17. Utilization of solar energy for wastewater treatment: Challenges and progressive research trends
    Pandey AK, Reji Kumar R, B K, Laghari IA, Samykano M, Kothari R, et al.
    J Environ Manage, 2021 Nov 01;297:113300.
    PMID: 34293672 DOI: 10.1016/j.jenvman.2021.113300
    This article offers a trend of inventions and implementations of photocatalysis process, desalination technologies and solar disinfection techniques adapted particularly for treatment of industrial and domestic wastewater. Photocatalysis treatment of wastewater using solar energy is a promising renewable solution to reduce stresses on global water crisis. Rendering to the United Nation Environment Programme, 1/3 of world population live in water-stressed countries, while by 2025 about 2/3 of world population will face water scarcity. Major pollutants exhibited from numerous sources are critically discussed with focus on potential environmental impacts & hazards. Treatment of wastewater by photocatalysis technique, solar thermal electrochemical process, solar desalination of brackish water and solar advanced oxidation process have been presented and systematically analysed with challenges. Both heterogenous and homogenous photocatalysis techniques employed for wastewater treatment are critically reviewed. For treating domestic wastewater, solar desalination technologies adopted for purifying brackish water into potable water is presented along with key challenges and remedies. Advanced oxidation process using solar energy for degradation of organic pollutant is an important technique to be reviewed due to their effectiveness in wastewater treatment process. Present article focused on three key issues i.e. major pollutants, wastewater treatment techniques and environmental benefits of using solar power for removal of pollutants. The review also provides close ideas on further research needs and major concerns. Drawbacks associated with conventional wastewater treatment options and direct solar energy-based wastewater treatment with energy storage systems to make it convenient during day and night both listed. Although, energy storage systems increase the overall cost of the wastewater treatment plant it also increases the overall efficiency of the system on environmental cost. Cost-efficient wastewater treatment methods using solar power would significantly ensure effective water source utilization, thereby contributing towards sustainable development goals.
  18. Advanced drug delivery systems targeting NF-κB in respiratory diseases
    Prasher P, Sharma M, Chellappan DK, Gupta G, Jha NK, Singh SK, et al.
    Future Med Chem, 2021 07;13(13):1087-1090.
    PMID: 33947226 DOI: 10.4155/fmc-2021-0013
  19. Fulltext Peroxisome proliferator-activated receptor gamma: promising target in glioblastoma
    Gupta G, Singhvi G, Chellappan DK, Sharma S, Mishra A, Dahiya R, et al.
    Panminerva Med, 2018 Sep;60(3):109-116.
    PMID: 30176701 DOI: 10.23736/S0031-0808.18.03462-6
    Glioblastoma, also known as glioblastoma multiforme, is the most common and worldwide-spread cancer that begins within the brain. Glioblastomas represent 15% of brain tumors. The most common length of survival following diagnosis is 12 to 14 months with less than 3% to 5% of people surviving longer than five years. Without treatment, survival is typically 3 months. Among all receptors, special attention has been focused on the role of peroxisome proliferator-activated receptors (PPARs) in glioblastoma. PPARs are ligand-activated intracellular transcription factors. The PPAR subfamily consists of three subtypes encoded by distinct genes named PPARα, PPARβ/δ, and PPARγ. PPARγ is the most extensively studied subtype of PPAR. There has been interesting preliminary evidence suggesting that diabetic patients receiving PPARγ agonists, a group of anti-diabetics, thiazolidinedione drugs, have an increased median survival for glioblastoma. In this paper, the recent progresses in understanding the potential mechanism of PPARγ in glioblastoma are summarized.
  20. Novel 9-(2-(1-arylethylidene)hydrazinyl)acridine derivatives: Target Topoisomerase 1 and growth inhibition of HeLa cancer cells
    Haider MR, Ahmad K, Siddiqui N, Ali Z, Akhtar MJ, Fuloria N, et al.
    Bioorg Chem, 2019 07;88:102962.
    PMID: 31085373 DOI: 10.1016/j.bioorg.2019.102962
    A series of 9-(2-(1-arylethylidene)hydrazinyl)acridine and its analogs were designed, synthesized and evaluated for biological activities. Various biochemical assays were performed to determine the free radical scavenging capacity of synthesized compounds (4a-4j). Anticancer activity of these compounds was assessed against two different human cancer cell lines viz cervical cancer cells (HeLa) and liver cancer cells (HepG2) as well as normal human embryonic kidney cell line (HEK 293). Compounds 4b, 4d and 4e showed potential anti-proliferative effects on HeLa cells. Based on results obtained from antioxidant and cytotoxicity studies, 4b, 4d and 4e were further studied in detail for different biological activities. 4b, 4d and 4e reduced the cell growth, inhibited metastatic activity and declined the potential of cell migration in HeLa cell lines. Topoisomerase1 (Top1) treated with compounds 4b, 4d and 4e exhibited inhibition of Top1 and prevented DNA replication. Molecular docking results validate that interaction of compounds 4b, 4d and 4e with Top1-DNA complex, which might be accountable for their inhibitory effects. Further it was concluded that compounds 4b, 4d and 4e arrests the cells at S phase and consequently induces cell death through DNA damage in HeLa cells.
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