Displaying publications 1 - 20 of 62 in total

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  1. Tayyeb JZ, Priya M, Guru A, Kishore Kumar MS, Giri J, Garg A, et al.
    Mol Biol Rep, 2024 Mar 15;51(1):423.
    PMID: 38489102 DOI: 10.1007/s11033-024-09407-7
    BACKGROUND: Oral health remains a significant global concern with the prevalence of oral pathogens and the increasing incidence of oral cancer posing formidable challenges. Additionally, the emergence of antibiotic-resistant strains has complicated treatment strategies, emphasizing the urgent need for alternative therapeutic approaches. Recent research has explored the application of plant compounds mediated with nanotechnology in oral health, focusing on the antimicrobial and anticancer properties.

    METHODS: In this study, curcumin (Cu)-mediated zinc oxide nanoparticles (ZnO NPs) were synthesized and characterized using SEM, EDAX, UV spectroscopy, FTIR, and XRD to validate their composition and structural features. The antioxidant and antimicrobial activity of ZnO-CU NPs was investigated through DPPH, ABTS, and zone of inhibition assays. Apoptotic assays and gene expression analysis were performed in KB oral squamous carcinoma cells to identify their anticancer activity.

    RESULTS: ZnO-CU NPs showcased formidable antioxidant prowess in both DPPH and ABTS assays, signifying their potential as robust scavengers of free radicals. The determined minimal inhibitory concentration of 40 µg/mL against dental pathogens underscored the compelling antimicrobial attributes of ZnO-CU NPs. Furthermore, the interaction analysis revealed the superior binding affinity and intricate amino acid interactions of ZnO-CU NPs with receptors on dental pathogens. Moreover, in the realm of anticancer activity, ZnO-CU NPs exhibited a dose-dependent response against Human Oral Epidermal Carcinoma KB cells at concentrations of 10 µg/mL, 20 µg/mL, 40 µg/mL, and 80 µg/mL. Unraveling the intricate mechanism of apoptotic activity, ZnO-CU NPs orchestrated the upregulation of pivotal genes, including BCL2, BAX, and P53, within the KB cells.

    CONCLUSIONS: This multifaceted approach, addressing both antimicrobial and anticancer activity, positions ZnO-CU NPs as a compelling avenue for advancing oral health, offering a comprehensive strategy for tackling both oral infections and cancer.

    Matched MeSH terms: Benzothiazoles*
  2. Ravikumar OV, Marunganathan V, Kumar MSK, Mohan M, Shaik MR, Shaik B, et al.
    Mol Biol Rep, 2024 Feb 24;51(1):352.
    PMID: 38400866 DOI: 10.1007/s11033-024-09289-9
    BACKGROUND: Oral diseases are often attributed to dental pathogens such as S. aureus, S. mutans, E. faecalis, and C. albicans. In this research work, a novel approach was employed to combat these pathogens by preparing zinc oxide nanoparticles (ZnO NPs) capped with cinnamic acid (CA) plant compounds.

    METHODS: The synthesized ZnO-CA NPs were characterized using SEM, FTIR, and XRD to validate their composition and structural features. The antioxidant activity of ZnO-CA NPs was confirmed using DPPH and ABTS free radical scavenging assays. The antimicrobial effects of ZnO-CA NPs were validated using a zone of inhibition assay against dental pathogens. Autodock tool was used to identify the interaction of cinnamic acid with dental pathogen receptors.

    RESULTS: ZnO-CA NPs exhibited potent antioxidant activity in both DPPH and ABTS assays, suggesting their potential as powerful antioxidants. The minimal inhibitory concentration of ZnO-CA NPs against dental pathogens was found 25 µg/mL, indicating their effective antimicrobial properties. Further, ZnO-CA NPs showed better binding affinity and amino acid interaction with dental pathogen receptors. Also, the ZnO-CA NPs exhibited dose-dependent (5 µg/mL, 15 µg/mL, 25 µg/mL, and 50 µg/mL) anticancer activity against Human Oral Epidermal Carcinoma KB cells. The mechanism of action of apoptotic activity of ZnO-CA NPs on the KB cells was identified through the upregulation of BCL-2, BAX, and P53 genes.

    CONCLUSIONS: This research establishes the potential utility of ZnO-CA NPs as a promising candidate for dental applications. The potent antioxidant, anticancer, and effective antimicrobial properties of ZnO-CA NPs make them a valuable option for combating dental pathogens.

    Matched MeSH terms: Benzothiazoles*
  3. Benjamin MAZ, Ng SY, Saikim FH, Rusdi NA
    Molecules, 2022 Sep 30;27(19).
    PMID: 36234995 DOI: 10.3390/molecules27196458
    The therapeutic potential of bamboos has acquired global attention. Nonetheless, the biological activities of the plants are rarely considered due to limited available references in Sabah, Malaysia. Furthermore, the drying technique could significantly affect the retention and degradation of nutrients in bamboos. Consequently, the current study investigated five drying methods, namely, sun, shade, microwave, oven, and freeze-drying, of the leaves of six bamboo species, Bambusa multiplex, Bambusa tuldoides, Bambusa vulgaris, Dinochloa sublaevigata, Gigantochloa levis, and Schizostachyum brachycladum. The infused bamboo leaves extracts were analysed for their total phenolic content (TPC) and total flavonoid content (TFC). The antioxidant activities of the samples were determined via the 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assays, whereas their toxicities were evaluated through the brine shrimp lethality assay (BSLA). The chemical constituents of the samples were determined using liquid chromatography−tandem mass spectrometry (LC-MS/MS). The freeze-drying method exhibited the highest phytochemical contents and antioxidant activity yield, excluding the B. vulgaris sample, in which the microwave-dried sample recorded the most antioxidant and phytochemical levels. The TPC and TFC results were within the 2.69 ± 0.01−12.59 ± 0.09 mg gallic acid equivalent (GAE)/g and 0.77 ± 0.01−2.12 ± 0.01 mg quercetin equivalent (QE)/g ranges, respectively. The DPPH and ABTS IC50 (half-maximal inhibitory concentration) were 2.92 ± 0.01−4.73 ± 0.02 and 1.89−0.01 to 3.47 ± 0.00 µg/mL, respectively, indicating high radical scavenging activities. The FRAP values differed significantly between the drying methods, within the 6.40 ± 0.12−36.65 ± 0.09 mg Trolox equivalent (TE)/g range. The phytochemical contents and antioxidant capacities exhibited a moderate correlation, revealing that the TPC and TFC were slightly responsible for the antioxidant activities. The toxicity assessment of the bamboo extracts in the current study demonstrated no toxicity against the BSLA based on the LC50 (lethal concentration 50) analysis at >1000 µg/mL. LC-MS analysis showed that alkaloid and pharmaceutical compounds influence antioxidant activities, as found in previous studies. The acquired information might aid in the development of bamboo leaves as functional food items, such as bamboo tea. They could also be investigated for their medicinal ingredients that can be used in the discovery of potential drugs.
    Matched MeSH terms: Benzothiazoles
  4. Lai MY, Ooi CH, Lau YL
    Malar J, 2021 Mar 25;20(1):166.
    PMID: 33766038 DOI: 10.1186/s12936-021-03707-0
    BACKGROUND: As an alternative to PCR methods, LAMP is increasingly being used in the field of molecular diagnostics. Under isothermal conditions at 65 °C, the entire procedure takes approximately 30 min to complete. In this study, we establish a sensitive and visualized LAMP method in a closed-tube system for the detection of Plasmodium knowlesi.

    METHODS: A total of 71 malaria microscopy positive blood samples collected in blood spots were obtained from the Sarawak State Health Department. Using 18s rRNA as the target gene, nested PCR and SYBR green I LAMP assay were performed following the DNA extraction. The colour changes of LAMP end products were observed by naked eyes.

    RESULTS: LAMP assay demonstrated a detection limit of 10 copies/µL in comparison with 100 copies/µL nested PCR. Of 71 P. knowlesi blood samples collected, LAMP detected 69 microscopy-positive samples. LAMP exhibited higher sensitivity than nested PCR assay. The SYBR green I LAMP assay was 97.1% sensitive (95% CI 90.2-99.7%) and 100% specific (95% CI 83.2-100%). Without opening the cap, incorporation of SYBR green I into the inner cap of the tube enabled the direct visualization of results upon completion of amplification. The positives instantaneously turned green while the negatives remained orange.

    CONCLUSIONS: These results indicate that SYBR green I LAMP assay is a convenient diagnosis tool for the detection of P. knowlesi in remote settings.

    Matched MeSH terms: Benzothiazoles/chemistry*
  5. Mohd Syukri MS, A Rahman R, Mohamad Z, Md Illias R, Nik Mahmood NA, Jaafar NR
    Int J Biol Macromol, 2021 Jan 01;166:876-883.
    PMID: 33144251 DOI: 10.1016/j.ijbiomac.2020.10.244
    Enzyme immobilization has been known to be one of the methods to improve the stability and reusability of enzyme. In this study, a strategy to optimize laccase immobilization on polyethylene terephthalate grafted with maleic anhydride electrospun nanofiber mat (PET-g-MAH ENM) was developed. The development involves the screening and optimization processes of the crucial factors that influence the immobilization yield such as enzyme concentration, pH values, covalent bonding (CV) time, CV temperature, crosslinking (CL) time, CL temperature and glutaraldehyde concentration using two-level factorial design and Box-Behnken design (BBD), respectively. It was found that laccase concentration, pH values and glutaraldehyde concentration play important role in enhancing the immobilization yield of laccase on PET-g-MAH ENM in the screening process. Subsequently, the optimization result showed at 0.28 mg/ml laccase concentration, pH 3 and 0.45% (v/v) glutaraldehyde concentrations gave the highest immobilization yield at 87.64% which was 81.2% increment from the immobilization yield before optimization. Under the optimum condition, the immobilized laccase was able to oxidize 2, 2-azino-bis 3-ethylbenzothiazoline-6- sulfonic acid (ABTS) in a broad range of pH (pH 3-6) and temperature (20- 70 °C). Meanwhile, the kinetic parameters for Km and Vmax were 1.331 mM and 0.041 mM/min, respectively. It was concluded that the optimization of immobilized laccase on PET-g-MAH ENM enhance the performance of this biocatalyst.
    Matched MeSH terms: Benzothiazoles/chemistry
  6. Nallappan D, Fauzi AN, Krishna BS, Kumar BP, Reddy AVK, Syed T, et al.
    Biomed Res Int, 2021;2021:5125681.
    PMID: 34631882 DOI: 10.1155/2021/5125681
    Studies on green biosynthesis of newly engineered nanoparticles for their prominent medicinal applications are being the torch-bearing concerns of the state-of-the-art research strategies. In this concern, we have engineered the biosynthesized Luffa acutangula silver nanoparticles of flavonoid O-glycosides in the anisotropic form isolated from aqueous leave extracts of Luffa acutangula, a popular traditional and ayurvedic plant in south-east Asian countries. These were structurally confirmed by Ultraviolet-visible (UV-Vis), Fourier transform infrared spectroscopy accessed with attenuated total reflection (FTIR-ATR) spectral analyses followed by the scanning electron microscopic (SEM) and the X-ray diffraction (XRD) crystallographic studies and found them with the face-centered cubic (fcc) structure. Medicinally, we have explored their significant antioxidant (DPPH and ABTS assays), antibacterial (disc diffusion assay on E. coli, S. aureus, B. subtilis, S. fecilis, and S. boydii), and anticancer (MTT assay on MCF-7, MDA-MB-231, U87, and DBTRG cell lines) potentialities which augmented the present investigation. The molecular docking analysis of title compounds against 3NM8 (DPPH) and 1DNU (ABTS) proteins for antioxidant activity; 5FGK (Gram-Positive Bacteria) and 1AB4 (Gram-Negative Bacteria) proteins for antibacterial activity; and 4GBD (MCF-7), 5FI2 (MDA-MB-231), 1D5R (U87), and 5TIJ (DBTRG) proteins for anticancer activity has affirmed the promising ligand-protein binding interactions among the hydroxy groups of the title compounds and aspartic acid of the concerned enzymatic proteins. The binding energy varying from -9.1645 to -7.7955 for Cosmosioside (1, Apigenin-7-glucoside) and from -9.2690 to -7.8306 for Cynaroside (2, Luteolin-7-glucoside) implies the isolated compounds as potential bioactive compounds. In addition, the performed studies like QSAR, ADMET, bioactivity properties, drug scores, and toxicity risks confirmed them as potential drug candidates and aspartic acid receptor antagonists. This research auxiliary augmented the existing array of phytological nanomedicines with new drug candidates that are credible with multiple bioactivities.
    Matched MeSH terms: Benzothiazoles/chemistry
  7. John CM, Khaddaj Mallat R, Mishra RC, George G, Singh V, Turnbull JD, et al.
    Pharmacol Res, 2020 01;151:104539.
    PMID: 31707036 DOI: 10.1016/j.phrs.2019.104539
    Aging represents an independent risk factor for the development of cardiovascular disease, and is associated with complex structural and functional alterations in the vasculature, such as endothelial dysfunction. Small- and intermediate-conductance, Ca2+-activated K+ channels (KCa2.3 and KCa3.1, respectively) are prominently expressed in the vascular endothelium, and pharmacological activators of these channels induce robust vasodilation upon acute exposure in isolated arteries and intact animals. However, the effects of prolonged in vivo administration of such compounds are unknown. In our study, we hypothesized that such treatment would ameliorate aging-related cardiovascular deficits. Aged (∼18 months) male Sprague Dawley rats were treated daily with either vehicle or the KCa channel activator SKA-31 (10 mg/kg, intraperitoneal injection; n = 6/group) for 8 weeks, followed by echocardiography, arterial pressure myography, immune cell and plasma cytokine characterization, and tissue histology. Our results show that SKA-31 administration improved endothelium-dependent vasodilation, reduced agonist-induced vascular contractility, and prevented the aging-associated declines in cardiac ejection fraction, stroke volume and fractional shortening, and further improved the expression of endothelial KCa channels and associated cell signalling components to levels similar to those observed in young male rats (∼5 months at end of study). SKA-31 administration did not promote pro-inflammatory changes in either T cell populations or plasma cytokines/chemokines, and we observed no overt tissue histopathology in heart, kidney, aorta, brain, liver and spleen. SKA-31 treatment in young rats had little to no effect on vascular reactivity, select protein expression, tissue histology, plasma cytokines/chemokines or immune cell properties. Collectively, these data demonstrate that administration of the KCa channel activator SKA-31 improved aging-related cardiovascular function, without adversely affecting the immune system or promoting tissue toxicity.
    Matched MeSH terms: Benzothiazoles/pharmacology*
  8. Nor Hafiza Sayuti, ‘Ammar Akram Kamarudin, Nor Asma Ab. Razak, Norazalina Saad, Mohd Sabri Pak Dek, Norhaizan Mohd Esa
    MyJurnal
    Introduction: There are numerous studies on the therapeutic properties of Artocarpus heterophyllus. However, stud- ies on the aqueous extraction of A. heterophyllus leaves are limited. This present study was conducted to optimize the extraction conditions of A. heterophyllus leaves to yield the highest phenolic, flavonoids and antioxidant contents. Methods: Response surface methodology (RSM) was employed to obtain a higher phenolic extraction parameter(s) of A. heterophyllus leaves using Central Composite Design (CCD). The antioxidant activity was then determined via ABTS (2,29-azinobis (3 ethylbenzothiazoline-6-sulfonic acid)) and DPPH (2,2-Diphenyl-1-picrylhydrazyl) assay and analysis of the individual phenolics was performed by high performance liquid chromatography (HPLC). Results: The optimum extraction conditions with higher phenolics content and antioxidant activity was achieved at 81°C, 100 min and 40 mL/g sample with a good desirability value of 0.87. Under these optimized parameters, total phenolics and flavonoids were 174.48 ± 4.05 mg GAE/g sample and 21.44 ± 0.05 mg RE/g sample, respectively. Meanwhile, antioxidant activity via ABTS and DPPH assays were 90.88% ± 0.09 and 87.22% ± 0.62, respectively. Finally, under optimal extraction conditions revealed 4 compounds identified as chlorogenic acid, quercetin, rutin and kaempferol. Conclusion: The optimisation are promising to improve phenolic yield and antioxidant activity in A. heterophyllus leaves. It also proved that A. heterophyllus leaves can be used as an alternative natural antioxidant especially in medicinal applications since all identified compound possess significant biological activities for human health.
    Matched MeSH terms: Benzothiazoles
  9. Hussin M, Abdul Hamid A, Abas F, Ramli NS, Jaafar AH, Roowi S, et al.
    Molecules, 2019 Sep 03;24(17).
    PMID: 31484470 DOI: 10.3390/molecules24173208
    Herbs that are usually recognized as medicinal plants are well known for their therapeutic effects and are traditionally used to treat numerous diseases, including aging. This study aimed to evaluate the metabolite variations among six selected herbs namely Curcurmalonga, Oenanthejavanica, Vitex negundo, Plucheaindica, Cosmoscaudatus and Persicariaminus using proton nuclear magnetic resonance (1H-NMR) coupled with multivariate data analysis (MVDA). The free radical scavenging activity of the extract was measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azinobis(3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) and oxygen radical absorbance capacity (ORAC) assay. The anti-aging property was characterized by anti-elastase and anti-collagenase inhibitory activities. The results revealed that P. minus showed the highest radical scavenging activities and anti-aging properties. The partial least squares (PLS) biplot indicated the presence of potent metabolites in P. minus such as quercetin, quercetin-3-O-rhamnoside (quercitrin), myricetin derivatives, catechin, isorhamnetin, astragalin and apigenin. It can be concluded that P. minus can be considered as a potential source for an anti-aging ingredient and also a good free radical eradicator. Therefore, P. minus could be used in future development in anti-aging researches and medicinal ingredient preparations.
    Matched MeSH terms: Benzothiazoles
  10. Dzulkharnien NSF, Karim MR, Zahid NI, Rahman NMMA, Abdullah I, Salleh NM
    J Fluoresc, 2019 Jul;29(4):1049-1056.
    PMID: 31338718 DOI: 10.1007/s10895-019-02418-9
    The optical properties of a series of side chain liquid crystalline polymers (P1-P3) containing azo-benzothiazole mesogen with different terminal substituents (-H, -CH3 and -OCH2CH3) in four organic solvents of varying polarity have been investigated by absorption and fluorescence spectral analysis. Solvatochromic studies of P1-P3 did not show any regular variation on the absorption and emission intensities with changing the polarity of solvent. Theoretical studies were performed based on different solvent correlation methods such as Dimroth-Reichardt and Kamlet-Taft methods to investigate the solute-solvent interactions. Both absorption and emission maxima of investigated polymers were bathochromically shifted with the replacement of sixth position hydrogen atom by electron donating groups in benzothiazole moiety. The emission intensities of the studied polymers showed decreasing trend with increasing temperature.
    Matched MeSH terms: Benzothiazoles
  11. K R, G B, Banat F, Show PL, Cocoletzi HH
    Int J Biol Macromol, 2019 Apr 01;126:1234-1243.
    PMID: 30584938 DOI: 10.1016/j.ijbiomac.2018.12.196
    Health hazards associated with usage of plastic films for food preservation demands for development of active films from non-toxic and antioxidant rich bio-sources. The reported work highlights the development, characterization and application studies of chitosan films enhanced for their antioxidant activity by mango leaf extract (MLE) incorporation. Effect of MLE variation (1-5%) on the morphology, optical nature, water exposure and mechanical characteristics of the chitosan-MLE composite films was studied. Increase in the MLE concentration resulted in films with increased thickness and decreased moisture content. Contact angle, water solubility and vapor permeability analysis demonstrated the reduced hydrophilicity and water vapor penetrability of the films due to MLE inclusion. MLE films possessed better tensile strength (maximum of 23.06 ± 0.19 MPa) with reduced elongation ratio than the pure chitosan film (18.14 ± 0.72 MPa). Antioxidants assessment in terms of total phenolic content, DPPH radical scavenging, ferric reducing power and ABTS radical scavenging showed improved antioxidant activity with the incremental amounts of MLE in the chitosan films. Microscopic studies revealed the smooth, compact and dense nature of the MLE-chitosan films favouring low oxygen transport rates. Application studies to cashew nuts preservation for 28 days storage indicated 56% higher oxidation resistance for the 5% MLE film than a commercial polyamide/polyethylene film. Results highlight the potential and promising nature of MLE impregnated chitosan films as suitable alternative for active packaging films for food preservation.
    Matched MeSH terms: Benzothiazoles
  12. Hussain S, Ullah F, Ayaz M, Ali Shah SA, Ali Shah AU, Shah SM, et al.
    Drug Des Devel Ther, 2019;13:4195-4205.
    PMID: 31849451 DOI: 10.2147/DDDT.S228971
    Background: Cancer is one of the chronic health conditions worldwide. Various therapeutically active compounds from medicinal plants were the current focus of this research in order to uncover a treatment regimen for cancer. Anchusa arvensis (A. anchusa) (L.) M.Bieb. contains many biologically active compounds.

    Methods: In the current study, new ester 3-hydroxyoctyl -5- trans-docosenoate (compound-1) was isolated from the chloroform soluble fraction of A. anchusa using column chromatography. Using MTT assay, the anticancer effect of the compound was determined in human hepatocellular carcinoma cells (HepG-2) compared with normal epithelial cell line (Vero). DPPH and ABTS radical scavenging assays were performed to assess the antioxidant potential. The Molecular Operating Environment (MOE-2016) tool was used against tyrosine kinase.

    Results: The structure of the compound was elucidated based on IR, EI, and NMR spectroscopy technique. It exhibited a considerable cytotoxic effect against HepG-2 cell lines with IC50 value of 6.50 ± 0.70 µg/mL in comparison to positive control (doxorubicin) which showed IC50 value of 1.3±0.21 µg/mL. The compound did not show a cytotoxic effect against normal epithelial cell line (Vero). The compound also exhibited significant DPHH scavenging ability with IC50 value of 12 ± 0.80 µg/mL, whereas ascorbic acid, used as positive control, demonstrated activity with IC50 = 05 ± 0.15 µg/mL. Similarly, it showed ABTS radical scavenging ability (IC50 = 130 ± 0.20 µg/mL) compared with the value obtained for ascorbic acid (06 ± 0.85 µg/mL). In docking studies using MOE-2016 tool, it was observed that compound-1 was highly bound to tyrosine kinase by having two hydrogen bonds at the hinge region. This good bonding network by the compound might be one of the reasons for showing significant activity against this enzyme.

    Conclusion: Our findings led to the isolation of a new compound from A. anchusa which has significant cytotoxic activity against HepG-2 cell lines with marked antioxidant potential.

    Matched MeSH terms: Benzothiazoles/antagonists & inhibitors*
  13. Arumugam B, Palanisamy UD, Chua KH, Kuppusamy UR
    Mol Vis, 2019;25:47-59.
    PMID: 30820141
    Purpose: Oxidative stress is implicated in the etiology of diabetes and its debilitating complications, such as diabetic retinopathy (DR). Various flavonoids have been reported to be useful in reducing DR progression. Myricetin derivatives (F2) isolated from leaf extract of Syzygium malaccense have the potential to serve as functional food as reported previously. The present study was performed with the aim of determining the antioxidant potential and protective effect of myricetin derivatives (F2) isolated from leaf extract of S. malaccense against glucose oxidase (GO)-induced hydrogen peroxide (H2O2) production that causes oxidative stress in ARPE-19 (RPE) cells.

    Methods: Antioxidant properties were assessed through various radical (DPPH, ABTS, and nitric oxide) scavenging assays and determination of total phenolic content and ferric reducing antioxidant power level. ARPE-19 cells were preincubated with samples before the addition of GO (to generate H2O2). Cell viability, change in intracellular reactive oxygen species (ROS), H2O2 levels in cell culture supernatant, and gene expression were assessed.

    Results: F2 showed higher antioxidant levels than the extract when assessed for radical scavenging activities and ferric reducing antioxidant power. F2 protected the ARPE-19 cells against GO-H2O2-induced oxidative stress by reducing the production of H2O2 and intracellular reactive oxygen species. This was achieved by the activation of nuclear factor erythroid 2-related factor 2 (Nrf2/NFE2L2) and superoxide dismutase (SOD2), as well as downregulation of nitric oxide producer (NOS2) at the transcriptional level.

    Conclusions: The results showed that myricetin derivatives from S. malaccense have the capacity to exert considerable exogenous antioxidant activities and stimulate endogenous antioxidant activities. Therefore, these derivatives have excellent potential to be developed as therapeutic agents for managing DR.

    Matched MeSH terms: Benzothiazoles/antagonists & inhibitors
  14. Zengin G, Rodrigues MJ, Abdallah HH, Custodio L, Stefanucci A, Aumeeruddy MZ, et al.
    Comput Biol Chem, 2018 Dec;77:178-186.
    PMID: 30336375 DOI: 10.1016/j.compbiolchem.2018.10.005
    The genus Silene is renowned in Turkey for its traditional use as food and medicine. Currently, there are 138 species of Silene in Turkey, amongst which have been several studies for possible pharmacological potential and application in food industry. However, there is currently a paucity of data on Silene salsuginea Hub.-Mor. This study endeavours to access its antioxidant, enzyme inhibitory, and anti-inflammatory properties. Besides, reversed-phase high-performance liquid chromatography-diode array detector (RP-HPLC-DAD) was used to detect phenolic compounds, and molecular docking was performed to provide new insights for tested enzymes and phenolics. High amounts of apigenin (534 μg/g extract), ferulic acid (452 μg/g extract), p-coumaric acid (408 μg/g extract), and quercetin (336 μg/g extract) were detected in the methanol extract while rutin (506 μg/g extract) was most abundant in the aqueous extract. As for their biological properties, the methanol extract exhibited the best antioxidant effect in the DPPH and CUPRAC assays, and also the highest inhibition against tyrosinase. The aqueous extract was the least active enzyme inhibitor but showed the highest antioxidant efficacy in the ABTS, FRAP, and metal chelating assays. At a concentration of 15.6 μg/mL, the methanol extract resulted in a moderate decrease (25.1%) of NO production in lipopolysaccharide-stimulated cells. Among the phenolic compounds, epicatechin, (+)-catechin, and kaempferol showed the highest binding affinity towards the studied enzymes in silico. It can be concluded that extracts of S. salsuginea are a potential source of functional food ingredients but need further analytical experiments to explore its complexity of chemical compounds and pharmacological properties as well as using in vivo toxicity models to establish its maximum tolerated dose.
    Matched MeSH terms: Benzothiazoles/antagonists & inhibitors
  15. Taha M, Arbin M, Ahmat N, Imran S, Rahim F
    Bioorg Chem, 2018 04;77:47-55.
    PMID: 29331764 DOI: 10.1016/j.bioorg.2018.01.002
    Due to the great biological importance of β-glucuronidase inhibitors, here in this study, we have synthesized a library of novel benzothiazole derivatives (1-30), characterized by different spectroscopic methods and evaluated for β-glucuronidase inhibitory potential. Among the series sixteen compounds i.e.1-6, 8, 9, 11, 14, 15, 20-23 and 26 showed outstanding inhibitory potential with IC50 value ranging in between 16.50 ± 0.26 and 59.45 ± 1.12 when compared with standard d-Saccharic acid 1,4-lactone (48.4 ± 1.25 µM). Except compound 8 and 23 all active analogs showed better potential than the standard. Structure activity relationship has been established.
    Matched MeSH terms: Benzothiazoles/chemical synthesis; Benzothiazoles/pharmacology*; Benzothiazoles/chemistry
  16. Wun FML, Muhd Hafizi Zainal, Syahidah Mohd Tahir, Ishak B. Ahmad, Mohammad B. Kassim
    Sains Malaysiana, 2018;47:923-929.
    The presence of two different chromophores in benzothiazole molecule namely benzothiazole and aromatic rings lead to
    interesting chemical and biological properties that attract more researches on the compounds. Three new benzothiazolylbenzoythiourea
    compounds namely 1-(1,3-benzothiazol-2-yl)-3-(benzoylthiourea) (BBT), 1-(1,3-benzothiazol-2-yl)-3-
    (4-chlorobenzoylthiourea) (BBT-4Cl) and 1-(1,3-benzothiazol-2-yl)-3-(4-methoxybenzoylthiourea) (BBT-4OCH3
    ) with
    different electron withdrawing substituents (R) at the para positions on the benzene ring of benzoylthiourea ring have
    been synthesized from the reaction of R-benzoyl isothiocyanate (R= H, Cl, and OCH3
    ) and 2-aminobenzothiazole. The
    compounds were characterized by spectroscopic techniques (infrared, 1
    H proton NMR and UV-Vis). The IR spectra showed
    the frequency signals of n (C=O), n (C=S), n (N-H) at 1664-1673, 1238-1249 and 3031-3055 cm-1, respectively. The 1
    H
    proton NMR spectra showed the presence of N-H amine and amide signals in the region of (12.14-12.35) and (14.17-14.43)
    ppm, respectively. The proton signals of the two benzothiazole and benzoylthiourea moieties appear at 7.08-8.16 ppm.
    A theoretical study based on Density Functional Theory (DFT) and Time-Dependent (TD) DFT was conducted to optimize
    the geometrical structure and investigate the electronic properties of title compounds. The highest occupied molecular
    orbital (HOMO) was found on the benzothiazole moiety; while, the lowest-unoccupied molecular orbital (LUMO) was
    located at the benzoylthiourea fragment. The DFT optimized structures possessed an intramolecular hydrogen bonding
    and the types of para substituents used influenced the properties of hydrogen bonding.
    Matched MeSH terms: Benzothiazoles
  17. Chigurupati S, Shaikh SA, Mohammad JI, Selvarajan KK, Nemala AR, Khaw CH, et al.
    Indian J Pharmacol, 2017 10 17;49(3):229-235.
    PMID: 29033482 DOI: 10.4103/ijp.IJP_293_16
    OBJECTIVES: In this study, three (CS-1 to CS-3) azomethine derivatives of cinnamaldehyde were green synthesized, characterized, and their antioxidant and antidepressant activities were explored.

    MATERIALS AND METHODS: The antioxidant effect of these compounds was initially performed in vitro using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay methods before subjecting them to in vivo experiments. Compounds showing potent antioxidant activity (CS-1 and CS-2) were investigated further for their antidepressant activity using the forced swim test (FST) and tail suspension test (TST). Ascorbic acid (AA) and fluoxetine (20 mg/kg, p.o) were used as reference drugs for comparison in the antioxidant and antidepressant experiments, respectively.

    RESULTS: It was observed that CS-2 and CS-3 exhibited highest DPPH (half maximal inhibitory concentration [IC50]: 16.22 and 25.18 μg/mL) and ABTS (IC50: 17.2 and 28.86 μg/mL) radical scavenging activity, respectively, compared to AA (IC50: 15.73 and 16.79 μg/mL) and therefore, both CS-2 and CS-3 were tested for their antidepressant effect using FST and TST as experimental models. Pretreatment of CS-2 and CS-3 (20 mg/kg) for 10 days considerably decreased the immobility time in both the FST and TST models.

    CONCLUSION: The antioxidant and antidepressant effect of CS-2 and CS-3 may be attributed to the presence of azomethine linkage in the molecule.

    Matched MeSH terms: Benzothiazoles/chemistry
  18. Abdullah SA, Jamil S, Basar N, Abdul Lathiff SM, Mohd Arriffin N
    Nat Prod Res, 2017 May;31(10):1113-1120.
    PMID: 27564208 DOI: 10.1080/14786419.2016.1222387
    A new dihydrochalcone, 2',4'-dihydroxy-3,4-(2″,2″-dimethylchromeno)-3'-prenyldihydrochalcone (1) together with 4-hydroxyonchocarpin (2), isobavachalcone (3), 4',5-dihydroxy-6,7-(2,2-dimethylpyrano)-2'-methoxy-8-γ,γ-dimethylallyflavone (4), artocarpin (5) and cycloheterophyllin (6) were successfully isolated from the leaves and heartwoods of Artocarpus lowii King (Moraceae). The structures of these compounds were fully characterised using spectroscopic methods and by direct comparison with published data. These compounds were tested for their antioxidant and tyrosinase inhibitory activities. Compound (1) displayed moderate antioxidant activity towards DPPH and tyrosinase inhibitory activities with SC50 value of 223.8 μM and IC50 value of 722.5 μM, respectively. Among the isolated compounds, cycloheterophyllin (6) showed the most potential antioxidant activity with SC50 value of 320.0 and 102.8 μM for ABTS and DPPH radicals scavenging activities, respectively, and also exhibited highest FRAP equivalent value of 4.7 ± 0.09 mM. Compound (6) showed tyrosinase inhibitory activity with the IC50 value of 104.6 μM.
    Matched MeSH terms: Benzothiazoles
  19. Normah, I., Nurul Fasihah, R.
    MyJurnal
    Angelwing clam (Pholas orientalis) hydrolysate was prepared by hydrolysis using bromelain. The hydrolysate named as bromelain hydrolysate (BH) was then treated with β-cyclodextrin in the ratio of 1:0.8 (v/w) by physical mixing and kneading methods producing the physical mixed hydrolysate (PMH) and kneaded method hydrolysate (KMH), respectively. The masking effect of β-cyclodextrin on bitterness was evaluated based on sensory analysis, amino acid analysis and determination of flavor compound by gas chromatography- mass spectrometry (GC-MS) and field emission scanning electron microscope (FESEM). Sensory analysis showed that KMH has least bitter taste compared to BH. Amino acids analysis showed that hydrophobic amino acids content that contributed to the bitter taste were lower in KMH and PMH compared to BH. GC-MS analysis also showed that benzothiazole compounds were present in KMH. The absence of benzene, 1-phenyl-4-2-(2-cyano-2-phenylethyl) in KMH and PMH indicated that phenylalanine in BH had been masked by β-cyclodextrin. FESEM showed that the new solid phase formed by kneading method has a crystal structure which was completely different from the original morphology of BH and β-cyclodextrin. Therefore, the bitterness in BH had successfully been masked by β-cyclodextrin, thus indicates its potential to be used as food ingredient..
    Matched MeSH terms: Benzothiazoles
  20. Abu F, Mat Taib CN, Mohd Moklas MA, Mohd Akhir S
    PMID: 28761496 DOI: 10.1155/2017/2907219
    Antioxidant properties of crude extract, partition extract, and fermented medium from Dendrobium sabin (DS) flower were investigated. The oven-dried DS flower was extracted using 100% methanol (w/v), 100% ethanol (w/v), and 100% water (w/v). The 100% methanolic crude extract showed the highest total phenolic content (40.33 ± mg GAE/g extract) and the best antioxidant properties as shown by DPPH, ABTS, and FRAP assays. A correlation relationship between antioxidant activity and total phenolic content showed that phenolic compounds were the dominant antioxidant components in this flower extract. The microbial fermentation on DS flower medium showed a potential in increasing the phenolic content and DPPH scavenging activity. The TPC of final fermented medium showed approximately 18% increment, while the DPPH of fermented medium increased significantly to approximately 80% at the end of the fermentation. Dendrobium sabin (DS) flower showed very good potential properties of antioxidant in crude extract and partition extract as well as better antioxidant activity in the flower fermented medium.
    Matched MeSH terms: Benzothiazoles
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