Displaying publications 21 - 40 of 51 in total

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  1. First isolation of Candida wangnamkhiaoensis from the blood of immunocompromised paediatric patient
    Tap RM, Ho Betty LS, Ramli NY, Suppiah J, Hashim R, Sabaratnam P, et al.
    Mycoses, 2016 Nov;59(11):734-741.
    PMID: 27427490 DOI: 10.1111/myc.12509
    Candida wangnamkhiaoensis is a species clustered under the Hyphopichia clade has not ever been isolated from any clinical specimens. To the best of our knowledge, this is the first report of C. wangnamkhiaoensis associated with fungaemia in immunocompromised paediatric patient. The isolate was assigned a strain name as UZ1679/14, in which the identification was confirmed by a polymerase chain reaction-sequencing of the internal transcribed spacer (ITS) and large subunit (LSU) regions of the rRNA gene. Antifungal susceptibility pattern showed that the isolate was sensitive to anidulafungin, caspofungin, fluconazole and voriconazole. The patient clinically improved after the antifungal treatment with caspofungin.
    Matched MeSH terms: Fluconazole/pharmacology
  2. Hepatotoxicity induced by antifungal drugs itraconazole and fluconazole in rats: a comparative in vivo study
    Somchit N, Norshahida AR, Hasiah AH, Zuraini A, Sulaiman MR, Noordin MM
    Hum Exp Toxicol, 2004 Nov;23(11):519-25.
    PMID: 15625777
    Itraconazole and fluconazole are oral antifungal drugs, which have a wide spectrum antifungal activity and better efficacy than the older drugs. However, both drugs have been associated with hepatotoxicity in susceptible patients. The mechanism of antifungal drug-induced hepatotoxicity is largely unknown. Therefore, the aim of this present study was to investigate and compare the hepatotoxicity induced by these drugs in vivo. Rats were treated intraperitoneally with itraconazole or fluconazole either single (0, 10, 100 and 200 mg/kg) or subchronic (0, 10, 50 and 100 mg/kg per day for 14 days) doses. Plasma and liver samples were taken at the end of the study. A statistically significant and dose dependent increase of plasma alanine aminotransferase (ALT) and alkaline phosphatase (ALP) activities were detected in the subchronic itraconazole-treated group. In addition, dose-dependent hepatocellular necrosis, degeneration of periacinar and mizonal hepatocytes, bile duct hyperplasia and biliary cirrhosis and giant cell granuloma were observed histologically in the same group. Interestingly, fluconazole treated rats had no significant increase in transaminases for both single and subchronic groups. In the subchronic fluconazole treated rats, only mild degenerative changes of centrilobular hepatocytes were observed. These results demonstrated that itraconazole was a more potent hepatotoxicant than fluconazole in vivo in rats.
    Matched MeSH terms: Fluconazole/administration & dosage; Fluconazole/toxicity*
  3. Fulltext Rare Kodamaea ohmeri keratitis following a trivial vegetative trauma
    Saud Al-Abbas AH, Ling JL, Muhammed J, Hussein A
    BMJ Case Rep, 2019 Jun 22;12(6).
    PMID: 31229985 DOI: 10.1136/bcr-2019-229660
    Kodamaea ohmeri keratitis is an opportunistic pathogen seen in patients who have undergone invasive procedures and immunocompromised state. It has been identified in septicemia patients, resulting in mortality. To the best of our knowledge, we identified the first case of K. ohmeri keratitis following an injury with vegetative material. A 57-year-old woman with underlying, poorly controlled diabetes mellitus was gardening when a tree leaf accidentally poked her in the eye. Two weeks later, the patient presented with right eye pain, redness and progressive blurring of vision due to a traumatised right cornea. Slit-lamp examination showed a small inferior paracentral corneal stromal infiltrate with overlying epithelial defect. A corneal scraping sample yielded K. ohmeri from Analytical Profile Index (API) 20C yeast identification system. She was treated with intensive topical amphotericin B and fluconazole. After 6 weeks of treatment, the keratitis resolved with faint scar tissue, and her visual acuity improved.
    Matched MeSH terms: Fluconazole/administration & dosage; Fluconazole/therapeutic use
  4. Intravenous fluconazole for bilateral endogenous Candida endophthalmitis
    Annamalai T, Fong KC, Choo MM
    J Ocul Pharmacol Ther, 2011 Feb;27(1):105-7.
    PMID: 21235384 DOI: 10.1089/jop.2010.0117
    To report a case of bilateral endogenous candida endophthalmitis treated with intravenous fluconazole.
    Matched MeSH terms: Fluconazole/administration & dosage*
  5. Fulltext An unusual cause of haemoptysis and headache: cryptococcosis
    How SH, Kuan YC, Ng TH, Ramachandram K, Fauzi AR
    Malays J Pathol, 2008 Dec;30(2):129-32.
    PMID: 19291924 MyJurnal
    Pulmonary cryptococcosis can be clinically silent in non-HIV infected patients but can also present as nodules and masses on the chest radiograph, which can be mistaken for tuberculosis or lung cancer. Common symptoms include fever and cough, and uncommonly haemoptysis. This report illustrates a non-HIV infected patient whose main complaint was haemoptysis and headache. He was diagnosed with pulmonary cryptococcosis from biopsy of an endobronchial mass found on flexible bronchoscopy. Disseminated cryptoccoccal infection should be considered as a differential diagnosis in non-HIV infected patients presenting with haemoptysis and headache. Early recognition and administration of appropriate therapy will improve clinical outcome in these patients.
    Matched MeSH terms: Fluconazole/therapeutic use
  6. Fulltext Cryptococcal meningitis in an immunocompetent child: a case report and literature review
    Othman N, Abdullah NA, Wahab ZA
    Southeast Asian J. Trop. Med. Public Health, 2004 Dec;35(4):930-4.
    PMID: 15916093
    An immunocompetent 5 year-old girl presented with pyrexia of unknown origin associated with headache. Initial investigations showed leukocytosis and an increased erythrocyte sedimentation rate. A Widal-Weil Felix test, blood film for malarial parasites, mycoplasma IgM antibody, cultures from blood and urine, full blood picture, Mantoux test, and chest x-ray were all negative. A lumbar puncture was done as part of a work-up for pyrexia of unknown origin. Cryptococcus neoformans was seen on India ink examination and confirmed on culture. She was treated with 10 weeks of intravenous amphotericin B and 8 weeks of fluconazole. Further immunological tests did not reveal any defect in the cell-mediated immune system. C. neoformans meningitis may present with non-specific symptoms and should be considered in a work-up for pyrexia of unknown origin.
    Matched MeSH terms: Fluconazole/therapeutic use
  7. Prevalence of albicans and non-albicans candiduria in a Malaysian medical centre
    Ding CH, Wahab AA, Muttaqillah NA, Tzar MN
    J Pak Med Assoc, 2014 Dec;64(12):1375-9.
    PMID: 25842581
    To determine the proportion of albicans and non-albicans candiduria in a hospital setting and to ascertain if fluconazole is still suitable as empirical antifungal therapy based on antifungal susceptibility patterns of Candida species.
    Matched MeSH terms: Fluconazole/therapeutic use
  8. Recurrent candidaemia in a neonate with Hirschsprung's disease: fluconazole resistance and genetic relatedness of eight Candida tropicalis isolates
    Chong PP, Chieng DC, Low LY, Hafeez A, Shamsudin MN, Seow HF, et al.
    J Med Microbiol, 2006 Apr;55(Pt 4):423-428.
    PMID: 16533990 DOI: 10.1099/jmm.0.46045-0
    The incidence of candidaemia among immunocompromised patients in Malaysia is increasing at an alarming rate. Isolation of clinical strains that are resistant to fluconazole has also risen markedly. We report here the repeated isolation of Candida tropicalis from the blood of a neonatal patient with Hirschsprung's disease. In vitro fluconazole susceptibility tests of the eight isolates obtained at different time points showed that seven of the isolates were resistant and one isolate was scored as susceptible dose-dependent. Random amplification of polymorphic DNA fingerprinting of the isolates using three primers and subsequent phylogenetic analysis revealed that these isolates were highly similar strains having minor genetic divergence, with a mean pairwise similarity coefficient of 0.893+/-0.041. The source of the infectious agent was thought to be the central venous catheter, as culture of its tip produced fluconazole-resistant C. tropicalis. This study demonstrates the utility of applying molecular epidemiology techniques to complement traditional mycological culture and drug susceptibility tests for accurate and appropriate management of recurrent candidaemia and highlights the need for newer antifungals that can combat the emergence of fluconazole-resistant C. tropicalis strains.
    Matched MeSH terms: Fluconazole/pharmacology*
  9. Fulltext Efficacy and safety of posaconazole for the prevention of invasive fungal infections in immunocompromised patients: a systematic review with meta-analysis and trial sequential analysis
    Wong TY, Loo YS, Veettil SK, Wong PS, Divya G, Ching SM, et al.
    Sci Rep, 2020 09 03;10(1):14575.
    PMID: 32884060 DOI: 10.1038/s41598-020-71571-0
    Invasive fungal infections are a potentially life-threatening complication in immunocompromised patients. The aim of this study was to assess the efficacy and safety of posaconazole as compared with other antifungal agents for preventing invasive fungal infections in immunocompromised patients. Embase, CENTRAL, and MEDLINE were searched for randomized conweekmonthtrolled trials (RCTs) up to June 2020. A systematic review with meta-analysis of RCTs was performed using random-effects model. Trial sequential analysis (TSA) was conducted for the primary outcome to assess random errors. A total of five RCTs with 1,617 participants were included. Posaconazole prophylaxis was associated with a significantly lower risk of IFIs (RR, 0.43 [95% CI 0.28 to 0.66, p = 0.0001]) as compared to other antifungal agents. No heterogeneity was identified between studies (I2 = 0%). No significant associations were observed for the secondary outcomes measured, including risk reduction of invasive aspergillosis and candidiasis, clinical failure, all-cause mortality, and treatment-related adverse events, except for infection-related mortality (RR, 0.31 [95% CI 0.15 to 0.64, p = 0.0001]). Subgroup analysis favoured posaconazole over fluconazole for the prevention of IFIs (RR, 0.44 [95% CI 0.28 to 0.70, p = 0.0004]). TSA confirmed the prophylactic benefit of posaconazole against IFIs. Posaconazole is effective in preventing IFIs among immunocompromised patients, particularly those with hematologic malignancies and recipients of allogenic hematopoietic stem cell transplantation.
    Matched MeSH terms: Fluconazole/therapeutic use*
  10. Efficacy of modified Leeming-Notman media in a resazurin microtiter assay in the evaluation of in-vitro activity of fluconazole against Malassezia furfur ATCC 14521
    Far FE, Al-Obaidi MMJ, Desa MNM
    J Mycol Med, 2018 Sep;28(3):486-491.
    PMID: 29753721 DOI: 10.1016/j.mycmed.2018.04.007
    BACKGROUND: Malassezia furfur is lipodependent yeast like fungus that causes superficial mycoses such as pityriasis versicolor and dandruff. Nevertheless, there are no standard reference methods to perform susceptibility test of Malassezia species yet.

    AIMS: Therefore, in this study, we evaluated the optimized culture medium for growth of this lipophilic yeast using modified leeming-Notman agar and colorimetric resazurin microtiter assay to assess antimycotic activity of fluconazole against M. furfur.

    RESULTS: The result showed that these assays were more adjustable for M. furfur with reliable and reproducible MIC end-point, by confirming antimycotic activity of fluconazole with MIC of 2μg/ml.

    CONCLUSION: We conclude that this method is considered as the rapid and effective susceptibility testing of M. furfur with fluconazole antifungal activity.

    Matched MeSH terms: Fluconazole/pharmacology*
  11. Combination Therapy of Clinically Approved Antifungal Drugs Is Enhanced by Conjugation with Silver Nanoparticles
    Hussain MA, Ahmed D, Anwar A, Perveen S, Ahmed S, Anis I, et al.
    Int Microbiol, 2019 Jun;22(2):239-246.
    PMID: 30810990 DOI: 10.1007/s10123-018-00043-3
    Silver nanoparticles (SN) have been recently developed as a new class of antimicrobial agents against numerous pathogenic microorganisms. SN have also been used as efficient drug delivery systems and have been linked with increasing drug potency. Here, we demonstrated the enhanced antifungal efficacy of nystatin (NYT) and fluconazole (FLU) after conjugation with SN. The antifungal bioactivity of NYT- and FLU-coated SN was evaluated against Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404 by the agar tube dilution method. The aim of this study was to determine and compare the antifungal efficacy of NYT and FLU with their SN and, finally, the combination of both nanoparticles as NYT-SN + FLU-SN against pathogenic fungi. The results indicated that all test samples showed a dose-dependent response against tested fungi. SN significantly enhanced the antifungal effects of NYT and FLU as compared to drugs alone. We observed a remarkable increase in the percent inhibition of both fungi (90-100%) when treated with a combination of both nanoparticles NYT-SN + FLU-SN at 200 μg/mL only. Furthermore, the morphological modifications occurred at the surface of fungal species were also analyzed by atomic force microscopy (AFM) and scanning electron microscopy (SEM). While tested against primary human cell line, all SN showed negligible cytotoxicity. Hence, these results suggest that the combination of SN with NYT and FLU may have clinical implications in the treatment of fungal infections. However, in vivo studies are needed before recommending the use of these nanoparticles safely in clinical situations.
    Matched MeSH terms: Fluconazole/pharmacology*
  12. Comparative Study of the Effects of Fluconazole and Voriconazole on Candida glabrata, Candida parapsilosis and Candida rugosa Biofilms
    Madhavan P, Jamal F, Pei CP, Othman F, Karunanidhi A, Ng KP
    Mycopathologia, 2018 Jun;183(3):499-511.
    PMID: 29380188 DOI: 10.1007/s11046-018-0243-z
    Infections by non-albicans Candida species are a life-threatening condition, and formation of biofilms can lead to treatment failure in a clinical setting. This study was aimed to demonstrate the in vitro antibiofilm activity of fluconazole (FLU) and voriconazole (VOR) against C. glabrata, C. parapsilosis and C. rugosa with diverse antifungal susceptibilities to FLU and VOR. The antibiofilm activities of FLU and VOR in the form of suspension as well as pre-coatings were assessed by XTT [2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide] reduction assay. Morphological and intracellular changes exerted by the antifungal drugs on Candida cells were examined by scanning electron microscope (SEM) and transmission electron microscope (TEM). The results of the antibiofilm activities showed that FLU drug suspension was capable of killing C. parapsilosis and C. rugosa at minimum inhibitory concentrations (MICs) of 4× MIC FLU and 256× MIC FLU, respectively. While VOR MICs ranging from 2× to 32× were capable of killing the biofilms of all Candida spp tested. The antibiofilm activities of pre-coated FLU were able to kill the biofilms at ¼× MIC FLU and ½× MIC FLU for C. parapsilosis and C. rugosa strains, respectively. While pre-coated VOR was able to kill the biofilms, all three Candida sp at ½× MIC VOR. SEM and TEM examinations showed that FLU and VOR treatments exerted significant impact on Candida cell with various degrees of morphological changes. In conclusion, a fourfold reduction in MIC50 of FLU and VOR towards ATCC strains of C. glabrata, C. rugosa and C. rugosa clinical strain was observed in this study.
    Matched MeSH terms: Fluconazole/pharmacology*
  13. Fulltext Successful treatment of Candida albicans endocarditis in a child with leukemia--a case report and review of the literature
    Ariffin H, Ariffin W, Tharam S, Omar A, de Bruyne J, Lin HP
    Singapore Med J, 1999 Aug;40(8):533-6.
    PMID: 10572495
    Candida species is now being increasingly recognised as an important cause of endocarditis especially in immunocompromised patients. A case of Candida albicans endocarditis in a child with acute lymphoblastic leukemia (ALL) is reported. The child did not have a central venous catheter at any time. Treatment consisted of intravenous amphotericin B and fluconazole for 3 weeks followed by oral fluconazole for 2 weeks. No surgical resection was necessary. We highlight here the importance of echocardiography in the management of prolonged febrile neutropenia and discuss the dilemma of continuing chemotherapy in such patients.
    Matched MeSH terms: Fluconazole/administration & dosage*
  14. Fulltext Synthesis and biological profile of substituted benzimidazoles
    Vashist N, Sambi SS, Narasimhan B, Kumar S, Lim SM, Shah SAA, et al.
    Chem Cent J, 2018 Dec 01;12(1):125.
    PMID: 30506405 DOI: 10.1186/s13065-018-0498-y
    BACKGROUND: A series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties. The synthesized compounds were screened for their antimicrobial and antiproliferative activities.

    RESULTS AND DISCUSSION: The synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug.

    CONCLUSION: Antimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole. The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC50 values were more potent than 5-fluorouracil.

    Matched MeSH terms: Fluconazole
  15. Fulltext Biofilm architecture of Candida rugosa and effect of amphotericin b, caspofungin, fluconazole and voriconazole on its structure
    Sri Raja Rajeswari Mahalingam, Priya Madhavan, Chong, Pei Pei
    Malaysian Journal of Medicine and Health Sciences, 2019;15(102):2-2.
    MyJurnal
    Introduction: One of the most common aetiology of opportunistic fungal infections in humans is Candida species. The virulence of Candida species is due to repertoire of factors, specifically, the ability to form biofilms. Medical devices such as intravenous catheters, prosthetic heart valves and surgical interventions provide pathogenic microorganisms with a surface to adhere to form biofilm. Fungi present as biofilms are often resistant to antifungal treatment because these biofilms offer a protective barrier that prohibits the drugs to get to the active site of the fungi. The objective of this study is to investigate the biofilm architecture of Candida rugosa (C.rugosa) at different developmental phases and to identify Sessile Minimum Inhibition Concentrations (SMICs) of amphotericin B, caspofungin, fluconazole, and voriconazole for the biofilm of C. rugosa. Methods: Confocal scanning laser microscopy (CSLM) and scanning electron microscopy (SEM) were used to visualize C. rugosa biofilms at different developmental phases. The antifungal susceptibility test was performed using serial doubling dilution. The growth kinetics of Candida biofilms was quantified using XTT reduction assay and crystal violet assay. Results: From the antifungal susceptibility test, the biofilms had SMIC of >16μg/mL for amphotericin B, 6µg/mL for caspofungin, >64μg/mL for fluconazole and >16μg/ mL for voriconazole. From the SEM micrographs, C. rugosa biofilm have a structure composed of an adherent yeast cells and blastopores with hyphal elements. There were significant alterations in the morphology after exposure to antifungal agents. The quantitative measurement of the matrix thickness of embedded yeast cells were obtained from CLSM micrographs. Conclusion: In conclusion, the ability of C. rugosa to form biofilms may attribute to one of the virulence factors that causes reduced susceptibility to antifungal agents.
    Matched MeSH terms: Fluconazole
  16. Fulltext Epidemiology and outcomes of candidaemia among adult patients admitted at Hospital Universiti Sains Malaysia (HUSM): a 5-year review
    Haydar, A.
    International Medical Journal Malaysia, 2018;17(1):3-12.
    MyJurnal
    Candida organisms are opportunistic fungal pathogens that have become a major cause of nosocomial infections worldwide. We investigated the clinical characteristics and outcomes of hospitalized patients with candidaemia caused by Candida albicans and non-albicans Candida spp at HUSM. Materials and Methods: We retrospectively evaluated all hospitalized patients with candidaemia from January 2010 till December 2014 based on inpatient hospital records and laboratory data. Results: A total of 134 patients with candidaemia were enrolled. Candida albicans and non-albicans Candida spp were responsible for 20% (27/134) and 80% (107/134) of candidaemia cases, respectively. Hospitalized patients with diabetes mellitus, surgical conditions, or concomitant septicaemia and those who received instrumentations such as CVC or CBD, and those admitted under medical settings were prone to develop candidaemia caused by either C. albicans or non-albicans Candida spp. All isolates were susceptible to Fluconazole except for C. krusei isolates. All-cause mortality within 30 days post diagnosis of candidaemia was 59%. Factors associated with mortality were solid tumor (p =0.014), surgical illness (p=0.128), central venous catheterization (p= 0.096) and leucocytosis (p=0.116). Only solid tumor was an independent contributory factor for mortality among patients with C. albicans candidaemia in the multivariate analyses (OR 5.09, 95% CI 1.38,18.74, p=0.014). Conclusions: The patients’ clinical characteristics were fairly comparable between Candida albicans and non-albicans candidaemia. The changing epidemiology of candidaemia at this centre was in fact alarming. The outcome associated with candidaemia was poor.
    Matched MeSH terms: Fluconazole
  17. Fulltext A catheter-related bloodstream infection caused by the yeast Kodamaea ohmeri
    Ding, C.H., Tzar M.N., Biswas S., Muttaqillah N.A.S., Wahab A.A.
    International Medical Journal Malaysia, 2018;17(2):135-138.
    MyJurnal
    Catheter-related bloodstream infections caused by Kodamaea ohmeri are generally not considered due to the relative scarcity of reported cases. This is a case of an 85-year-old man with poorly controlled diabetes mellitus who was initially admitted to our hospital for diabetic ketoacidosis. An internal jugular catheter was inserted as part of the initial management. A week later the patient developed a temperature spike and a yeast identified as Kodamaea ohmeri by ID 32 C (bioMérieux, France) was isolated from both his central and peripheral blood cultures. The catheter was removed and the patient was treated with fluconazole despite the organism’s relatively high minimum inhibitory concentration (2 μg/mL) to this antifungal. The fungemia resolved following a 2-weeks course of fluconazole.
    Matched MeSH terms: Fluconazole
  18. Fulltext In silico identification of novel tuberculosis drug targets in mycobacterium tuberculosis P450 enzymes by interaction study with azole drugs
    Suresh Kumar
    Malaysian Journal of Medicine and Health Sciences, 2020;16(101):24-30.
    MyJurnal
    Introduction: Tuberculosis (TB) is one of the utmost serious infectious diseases worldwide. The emergence of multi- drug resistance demands the development of better or new putative drug targets for tuberculosis. Recent studies sug- gest Mycobacterium tuberculosis cytochrome P450 enzymes as promising drug targets and azole drugs as potential inhibitors. Methods: Various computational tools, like Expasy Protparam, Swiss model, RaptorX and Phyre2 were used to analyze 12 Mycobacterium tuberculosis P450 enzymes and determine their three-dimensional structure. The structural validation was done through a Ramachandran plot using RAMPAGE server. The docking of P450 enzymes with azole drugs was done with autodock ver 4.2.6. Results: Based on sub-cellular localization prediction using CEL- LO tool, P450 enzymes CYP123A1, CYP132A1, CYP135A1, CYP136A1, CYP140A1, and CYP143A1 were predicted to be in the cytoplasm. Through structure assessment by Ramachandran plot, the best homology modelled proteins were docked with azole drugs like clotrimazole, croconazole, econazole, fluconazole, itraconazole, itraconazole, ketaconazole and micronazole by using autodock. By docking method it is identified that ketaconazole drug has a high affinity towards most of the mycobacterium P450 enzymes followed by the itrconazole drug. CYP123A1 enzyme is preferable as a drug target due to high binding affinity towards ketoconazole followed by CYP135A1, CYP140A1 enzymes. Conclusion: This study would help in identifying putative novel drug targets in Mycobacterium tuberculosis, which can lead to promising candidates for the optimization and development of novel anti-mycobac- terial agents.
    Matched MeSH terms: Fluconazole
  19. Fulltext Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
    Kumar S, Lim SM, Ramasamy K, Mani V, Shah SAA, Narasimhan B
    Chem Cent J, 2018 Jun 25;12(1):73.
    PMID: 29938365 DOI: 10.1186/s13065-018-0440-3
    BACKGROUND: Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and cytotoxicity studies.

    RESULTS: The structures of synthesized bis-pyrimidine molecules were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity using tube dilution method and anticancer activity against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B assay.

    CONCLUSIONS: The biological study demonstrated that compounds s7, s8, s11, s14, s16, s17 and s18 have shown more promising antimicrobial activity with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compound s3 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line.

    Matched MeSH terms: Fluconazole
  20. Fulltext Comparison between efficacy of allicin and fluconazole against Candida albicans in vitro and in a systemic candidiasis mouse model
    Khodavandi A, Alizadeh F, Harmal NS, Sidik SM, Othman F, Sekawi Z, et al.
    FEMS Microbiol Lett, 2011 Feb;315(2):87-93.
    PMID: 21204918 DOI: 10.1111/j.1574-6968.2010.02170.x
    The efficacy of allicin compared with fluconazole in alleviating systemic Candida albicans infections was evaluated both in vitro and in vivo through a systemic candidiasis mouse model. Determination of in vitro minimum inhibitory concentrations (MICs) for different C. albicans isolates revealed that both allicin and fluconazole showed different MICs that ranged from 0.05 to 12.5 μg mL(-1) and 0.25 to 16 μg mL(-1) , respectively. A time-kill study showed a significant effect of allicin (P<0.01) against C. albicans, comparable to that of fluconazole. Scanning electron microscopy observation revealed that, similar to fluconazole, allicin produced structural destruction of C. albicans cell surface at low MIC and lysis or puncture at high MIC concentrations. Treatment of BALB/c mice systemically infected with C. albicans showed that although the allicin treatment (at 5 mg kg(-1) day(-1) ) was slightly less efficacious than fluconazole treatment in terms of the fungal load reduction and host survival time, it was still effective against C. albicans in terms of mean survival time, which increased from 8.4 to 15.8 days. These results demonstrate the efficacy of anticandidal effects of allicin both in vitro and in an animal model of candidiasis and affirm the potential of allicin as an adjuvant therapy to fluconazole.
    Matched MeSH terms: Fluconazole/pharmacology*; Fluconazole/therapeutic use*
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