Displaying publications 41 - 51 of 51 in total

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  1. Design, Synthesis and Therapeutic Potential of Some 6, 6'-(1,4- phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine)analogues
    Kumar S, Narasimhan B, Lim SM, Ramasamy K, Mani V, Shah SAA
    Mini Rev Med Chem, 2019;19(7):609-621.
    PMID: 30526456 DOI: 10.2174/1389557519666181210162413
    BACKGROUND: A series of 6, 6'-(1,4-phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine) derivatives has been synthesized by Claisen-Schmidt condensation and its chemical structures was confirmed by FT-IR, 1H/13C-NMR spectral and elemental analyses. The molecular docking study was carried out to find the interaction between active bis-pyrimidine compounds with CDK-8 protein. The in vitro antimicrobial potential of the synthesized compounds was determined against Gram-positive and Gram-negative bacterial species as well fungal species by tube dilution technique. Antimicrobial results indicated that compound 11y was found to be most potent one against E. coli (MICec = 0.67 µmol/mL) and C. albicans (MICca = 0.17 µmol/mL) and its activity was comparable to norfloxacin (MIC = 0.47 µmol/mL) and fluconazole (MIC = 0.50 µmol/mL), respectively.

    CONCLUSION: Anticancer screening of the synthesized compounds using Sulforhodamine B (SRB) assay demonstrated that compounds 2y (IC50 = 0.01 µmol/mL) and 4y (IC50= 0.02 µmol/mL) have high antiproliferative potential against human colorectal carcinoma cancer cell line than the reference drug (5- fluorouracil) and these compounds also showed best dock score with better potency within the ATP binding pocket and may also be used lead for rational drug designing.

    Matched MeSH terms: Candida albicans/drug effects
  2. Design, Synthesis, SAR Study, Antimicrobial and Anticancer Evaluation of Novel 2-Mercaptobenzimidazole Azomethine Derivatives
    Tahlan S, Narasimhan B, Lim SM, Ramasamy K, Mani V, Shah SAA
    Mini Rev Med Chem, 2020;20(15):1559-1571.
    PMID: 30179132 DOI: 10.2174/1389557518666180903151849
    BACKGROUND: Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2- (1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized.

    RESULTS AND DISCUSSION: The synthesized analogues were characterized by FT-IR, 1H/13C-NMR and MS studies as well C, H, N analysis. All synthesized compounds were evaluated for in vitro antibacterial activity against Gram-positive (B. subtilis), Gram-negative (E. coli, P. aeruginosa, K. pneumoniae and S. typhi) strains and in vitro antifungal activity against C. albicans and A. niger strains by serial dilution method, the minimum inhibitory concentration (MIC) described in μM/ml. The in vitro anticancer activity of synthesized compounds was determined against human colorectal carcinoma cell line (HCT- 116) using 5-fluorouracil as standard drug.

    CONCLUSION: In general, most of the synthesized derivatives exhibited significant antimicrobial and anticancer activities. Compounds 8, 10, 15, 16, 17, 20 and 22 showed significant antimicrobial activity towards tested bacterial and fungal strains and compound 26 exhibited significant anticancer activity.

    Matched MeSH terms: Candida albicans/drug effects
  3. Fulltext Growth profile and SEM analyses of Candida albicans and Escherichia coli with Hymenocallis littoralis (Jacq.) Salisb leaf extract
    Rosli N, Sumathy V, Vikneswaran M, Sreeramanan S
    Trop Biomed, 2014 Dec;31(4):871-9.
    PMID: 25776614 MyJurnal
    Hymenocallis littoralis (Jacq.) Salisb (Melong kecil) commonly known as 'Spider Lily' is an herbaceous plant from the family Amaryllidaceae. Study was carried out to determine the effect of H. littoralis leaf extract on the growth and morphogenesis of two pathogenic microbes, Candida albicans and Escherichia coli. The leaf extract displayed favourable anticandidal and antibacterial activity with a minimum inhibition concentration (MIC) of 6.25 mg/mL. Time kill study showed both microbes were completely killed after treated with leaf extract at 20 h. Both microbes' cell walls were heavily ruptured based on scanning electron microscopy (SEM) analysis. The significant anticandidal and antibacterial activities showed by H. littoralis leaf extract suggested the potential antimicrobial agent against C. albicans and E. coli.
    Matched MeSH terms: Candida albicans/drug effects*
  4. The antifungal agent of silver nanoparticles activated by diode laser as light source to reduce C. albicans biofilms: an in vitro study
    Astuti SD, Puspita PS, Putra AP, Zaidan AH, Fahmi MZ, Syahrom A, et al.
    Lasers Med Sci, 2019 Jul;34(5):929-937.
    PMID: 30413898 DOI: 10.1007/s10103-018-2677-4
    Candida albicans is a normal flora caused fungal infections and has the ability to form biofilms. The aim of this study was to improve the antifungal effect of silver nanoparticles (AgNPs) and the light source for reducing the biofilm survival of C. albicans. AgNPs were prepared by silver nitrate (AgNO3) and trisodium citrate (Na3C6H5O7). To determine the antifungal effect of treatments on C. albicans biofilm, samples were distributed into four groups; L + P+ was treatment with laser irradiation and AgNPs; L + P- was treatment with laser irradiation only; L - P+ was treatment with AgNPs only (control positive); L - P- was no treatment with laser irradiation or AgNPs (control negative). The growth of fungi had been monitored by measuring the optical density at 405 nm with ELISA reader. The particle size of AgNPs was measured by using (particle size analyzer) and the zeta potential of AgNPs was measured by using Malvern zetasizer. The PSA test showed that the particle size of AgNPs was distributed between 7.531-5559.644 nm. The zeta potentials were found lower than - 30 mV with pH of 7, 9 or 11. The reduction percentage was analyzed by ANOVA test. The highest reduction difference was given at a lower level irradiation because irradiation with a density energy of 6.13 ± 0.002 J/cm2 resulted in the biofilm reduction of 7.07 ± 0.23% for the sample without AgNPs compared to the sample with AgNPs that increased the biofilm reduction of 64.48 ± 0.07%. The irradiation with a 450-nm light source had a significant fungicidal effect on C. albicans biofilm. The combination of light source and AgNPs provides an increase of biofilm reduction compared to the light source itself.
    Matched MeSH terms: Candida albicans/drug effects
  5. Antimicrobial activity of tiger's betel (Piper porphyrophyllum N.E. Br., Piperaceae)
    Wiart C, Hannah NA, Yassim M, Hamimah H, Sulaiman M
    Phytother Res, 2004 Sep;18(9):783-4.
    PMID: 15478188
    The ethanol extract of leaves of Piper porphyrophyllum N.E. Br. showed a broad spectrum of antibacterial activity. The activity was increased on fractionation (hexane, dichloromethane and aqueous), particularly in the aqueous fraction. No activity was shown against tested Candida albicans.
    Matched MeSH terms: Candida albicans/drug effects
  6. Fungicidal effect and oral acute toxicity of Cassia spectabilis leaf extract
    Sangetha S, Zuraini Z, Sasidharan S, Suryani S
    Nihon Ishinkin Gakkai Zasshi, 2008;49(4):299-304.
    PMID: 19001757
    The fungicidal activity of Cassia spectabilis leaf extracts was investigated using the disk diffusion technique and the broth dilution method. The extract showed a favorable antimicrobial activity against Candida albicans with a minimum inhibition concentration(MIC) value of 6.25 mg / ml. Apart from the fungicidal effects, imaging using scanning electron microscopy (SEM) was done to determine the major alterations in the microstructure of the C. albicans. The main abnormalities noted in the SEM studies were the alterations in morphology and complete collapse of the yeast cells after 36 h of exposure to the extract. The in vitro time-kill study performed using the leaf extract at 1/2, 1 or 2 times of the MIC significantly inhibited the yeast growth with a noticeable drop in optical density (OD) of yeast culture, thus confirming the fungicidal effect of the extract on C. albicans. In addition, in vivo antifungal activity studies on candidiasis in mice showed a 5-fold decrease in Candida in kidneys and blood samples in the groups of animals treated with the extract (2.5 g / kg body weight). In an acute toxicity study using mice, the acute minimum fatal dose of the extract was greater than 2000 mg / kg, and we found no histopathological changes in macroscopic examination by necropsy of mice treated with extract. We conclude that the extract may be safely used as an anticandidal agent.
    Matched MeSH terms: Candida albicans/drug effects
  7. Isolation and bioactivities of constitutents of the roots of Garcinia atroviridis
    Permana D, Lajis NH, Mackeen MM, Ali AM, Aimi N, Kitajima M, et al.
    J Nat Prod, 2001 Jul;64(7):976-9.
    PMID: 11473441
    Two new prenylated compounds, the benzoquinone atrovirinone (1) and the depsidone atrovirisidone (2), were isolated from the roots of Garcinia atroviridis. Their structures were determined on the basis of the analysis of spectroscopic data. While compound 2 showed some cytotoxicity against HeLa cells, both compounds 1 and 2 were only mildly inhibitory toward Bacillus cereus and Staphylococcus aureus.
    Matched MeSH terms: Candida albicans/drug effects
  8. A study on Candida biofilm growth characteristics and its susceptibility to aureobasidin A
    Munusamy K, Vadivelu J, Tay ST
    Rev Iberoam Micol, 2018 03 12;35(2):68-72.
    PMID: 29544734 DOI: 10.1016/j.riam.2017.07.001
    BACKGROUND: Biofilm is known to contribute to the antifungal resistance of Candida yeasts. Aureobasidin A (AbA), a cyclic depsipeptide targeting fungal sphingolipid biosynthesis, has been shown to be effective against several Candida species.

    AIMS: The aim of this study was to investigate Candida biofilm growth morphology, its biomass, metabolic activity, and to determine the effects of AbA on the biofilm growth.

    METHODS: The biofilm forming ability of several clinical isolates of different Candida species from our culture collection was determined using established methods (crystal violet and XTT assays). The determination of AbA planktonic and biofilm MICs was performed based on a micro-broth dilution method. The anti-biofilm effect of AbA on Candida albicans was examined using field emission scanning electron microscope (FESEM) analysis.

    RESULTS: A total of 35 (29.7%) of 118 Candida isolates were regarded as biofilm producers in this study. Candida parapsilosis was the largest producer, followed by Candida tropicalis and C. albicans. Two morphological variants of biofilms were identified in our isolates, with 48.6% of the isolates showing mainly yeast and pseudohyphae-like structures, while the remaining ones were predominantly filamentous forms. The biofilm producers were divided into two populations (low and high), based on the ability in producing biomass and their metabolic activity. Candida isolates with filamentous growth, higher biomass and metabolic activity showed lower AbA MIC50 (at least fourfold), compared to those exhibiting yeast morphology, and lower biomass and metabolic activity. The observation of filament detachment and the almost complete removal of biofilm from AbA-treated C. albicans biofilm in FESEM analysis suggests an anti-biofilm effect of AbA.

    CONCLUSIONS: The variability in the growth characteristics of Candida biofilm cultures affects susceptibility to AbA, with higher susceptibility noted in biofilm cultures exhibiting filamentous form and high biomass/metabolic activity.

    Matched MeSH terms: Candida albicans/drug effects
  9. Pink oyster mushroom Pleurotus flabellatus mycelium produced by an airlift bioreactor-the evidence of potent in vitro biological activities
    Klaus A, Wan-Mohtar WAAQI, Nikolić B, Cvetković S, Vunduk J
    World J Microbiol Biotechnol, 2021 Jan 04;37(1):17.
    PMID: 33394203 DOI: 10.1007/s11274-020-02980-6
    Four types of mycelial extracts were derived from the airlift liquid fermentation (ALF) of Pleurotus flabellatus, namely exopolysaccharide (EX), endopolysaccharide (EN), hot water (WE), and hot alkali (AE) extracts. Such extracts were screened for their active components and biological potential. EN proved to be most effective in inhibition of lipid peroxidation (EC50 = 1.71 ± 0.02 mg/mL) and in Cupric ion reducing antioxidant capacity (CUPRAC) assay (EC50 = 2.91 ± 0.01 mg TE/g). AE exhibited most pronounced ability to chelate ferrous ions (EC50 = 4.96 ± 0.08 mg/mL) and to scavenge ABTS radicals (EC50 = 3.36 ± 0.03 mg TE/g). β-glucans and total phenols contributed most to the chelating ability and quenching of ABTS radicals. Inhibition of lipid peroxidation correlated best with total glucans, total proteins, and β-glucans. Total proteins contributed most to CUPRAC antioxidant capacity. Antifungal effect was determined against Candida albicans ATCC 10231 (MIC: 0.019-0.625 mg/mL; MFC: 0.039-2.5 mg/mL), and towards C. albicans clinical isolate (MIC and MFC: 10.0-20.0 mg/mL). Comparison of cytotoxicity against colorectal carcinoma HCT 116 cells (IC50: 1.8 ± 0.3-24.6 ± 4.2 mg/mL) and normal lung MRC-5 fibroblasts (IC50: 17.0 ± 4.2-42.1 ± 6.1 mg/mL) showed that EN, and especially AE possess selective anticancer activity (SI values 3.41 and 9.44, respectively). Slight genotoxicity was observed only for AE and EX, indicating the low risk concerning this feature. Notable antioxidative and anticandidal activities, selective cytotoxicity against colorectal carcinoma cells, and absence/low genotoxicity pointed out that ALF-cultivated P. flabellatus mycelium could be considered as a valuable source of bioactive substances.
    Matched MeSH terms: Candida albicans/drug effects
  10. Fulltext Composition and Bioactivity of Essential Oil from Citrus grandis (L.) Osbeck 'Mato Peiyu' Leaf
    Tsai ML, Lin CD, Khoo KA, Wang MY, Kuan TK, Lin WC, et al.
    Molecules, 2017 Dec 05;22(12).
    PMID: 29206180 DOI: 10.3390/molecules22122154
    'Mato Peiyu' pomelo (Citrus grandis (L.) Osbeck 'Mato Peiyu') leaves from pruning are currently an agricultural waste. The aim of this study was to isolate essential oils from these leaves through steam distillation (SD) and solvent-free microwave extraction (SFME) and to evaluate their applicability to skin care by analyzing their antimicrobial, antioxidant (diphenyl-1-picrylhydrazyl scavenging assay, β-carotene/linoleic acid assay, and nitric oxide scavenging assay), anti-inflammatory (5-lipoxygenase inhibition assay), and antityrosinase activities. The gas chromatography-mass spectrometry results indicated that the main components of 'Mato Peiyu' leaf essential oils were citronellal and citronellol, with a total percentage of 50.71% and 59.82% for SD and SFME, respectively. The highest bioactivity among all assays was obtained for 5-lipoxygenase inhibition, with an IC50 value of 0.034% (v/v). The MIC90 of the antimicrobial activity of essential oils against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Candida albicans ranged from 0.086% to 0.121% (v/v). Citronellal and citronellol were the main contributors, accounting for at least 54.58% of the essential oil's bioactivity. This paper is the first to report the compositions and bioactivities of 'Mato Peiyu' leaf essential oil, and the results imply that the pomelo leaf essential oil may be applied in skin care.
    Matched MeSH terms: Candida albicans/drug effects
  11. Synthesis and antimicrobial properties of some new thiazolyl coumarin derivatives
    Arshad A, Osman H, Bagley MC, Lam CK, Mohamad S, Zahariluddin AS
    Eur J Med Chem, 2011 Sep;46(9):3788-94.
    PMID: 21712145 DOI: 10.1016/j.ejmech.2011.05.044
    Two novel series of hydrazinyl thiazolyl coumarin derivatives have been synthesized and fully characterized by IR, (1)H NMR, (13)C NMR, elemental analysis and mass spectral data. The structures of some compounds were further confirmed by X-ray crystallography. All of these derivatives, 10a-d and 15a-h, were screened in vitro for antimicrobial activity against various bacteria species including Mycobacterium tuberculosis and Candida albicans. The compounds 10c, 10d and 15e exhibited very good activities against all of the tested microbial strains.
    Matched MeSH terms: Candida albicans/drug effects
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