Displaying publications 1 - 20 of 76 in total

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  1. The influence of genetic polymorphisms on the efficacy and side effects of anastrozole in postmenopausal breast cancer patients
    Abubakar MB, Wei K, Gan SH
    Pharmacogenet Genomics, 2014 Dec;24(12):575-81.
    PMID: 25203739 DOI: 10.1097/FPC.0000000000000092
    Breast cancer is a common cause of cancer mortality among women. Several genetic factors have been implicated in its development. Current treatment guidelines for estrogen receptor-positive breast cancer recommend that anastrozole [or any of the other two aromatase inhibitors (letrozole and exemestane)] is used as an alternative to tamoxifen or following several years of tamoxifen treatment. Nevertheless, this approach is still associated with many challenges, ranging from the recurrence of breast cancer to considerable interindividual variability in the tolerability of anastrozole, which may cause adverse effects, such as musculoskeletal symptoms, and lead to the withdrawal of many patients from treatment. Variabilities in the genes encoding the drug target (aromatase) or its metabolizing enzymes (CYP3A and UGT1A) contribute toward the interindividual variability in anastrozole's pharmacokinetics and/or pharmacodynamics. This paper reviews the role of genetic polymorphisms of CYP19A1, CYP3A4, and UGT1A4 in the responses of female hormone receptor-positive postmenopausal breast cancer patients to anastrozole. Many reviews in the literature have suggested that the study of functional polymorphisms and investigation of relevant genetic markers may provide valuable information in predicting responses to anastrozole in terms of its therapeutic and adverse effects. Nevertheless, more studies are required before the knowledge of its pharmacogenomics can be applied to the individualization of treatment to ensure that patients receive the maximum benefits. Therefore, future analyses, including but not limited to genome-wide association studies, are encouraged to address some of the gray areas in the pharmacogenomics of anastrozole therapy in postmenopausal breast cancer cases; this will help in providing guidance for future pharmacogenomics protocols when anastrozole is utilized in patients' management.
    Matched MeSH terms: Triazoles/adverse effects; Triazoles/pharmacokinetics*
  2. Correlation of Serum Estradiol and Duration of Anastrazole Therapy with Treatment Related Adverse Effects Among Postmenopausal Breast Cancer Women: A Cross-sectional Study
    Abubakar MB, Gan SH
    Niger J Physiol Sci, 2017 Dec 30;32(2):219-225.
    PMID: 29485645
    Although anastrozole (Anas) plays a key role in the management of endocrine sensitive post-menopausal (PM) breast cancer (BC), there is much variability in its efficacy and tolerability. Anas-associated musculoskeletal symptoms (MS) and other adverse reactions, such as hot flashes (HF) and vaginal dryness/dyspareunia (VDD), are common and can affect the quality of life of BC patients, even sometimes leading to treatment withdrawal. The aim of this study was to determine the clinical and demographic factors associated with these adverse events. This is a cross-sectional study in estrogen receptor (ER) positive PM women (n = 92) with stages I to III BC receiving Anas. Multivariate analyses were performed to investigate the factors associated with Anas-induced adverse effects such as MS, HF and VDD. A serum estradiol concentration was undetectable (< 36.7 pmol/L) in 68.1% of patients but was detectable within a normal range (>36.7-88.1 pmol/L) in the other 31.9% of patients, and this group was found to have a lower odds of having at least one adverse effect (AE) compared to those with undetectable levels [adjusted odds ratio (AOR) 0.12, 95% confidence interval (CI) 0.02 to 0.64, p = 0.013]. Women with grades II and III tumors and a family history of BC had a higher odds of AE (grade II: AOR 12.22, CI 1.48 to 100.80, p = 0.020; grade III: AOR 12.95, CI 1.25 to 134.33, p = 0.032) and VDD (AOR 5.99, CI 1.30 to 27.52, p = 0.021), respectively. Patients who received Anas treatment for more than one year had a higher odds of VDD (one to three years: AOR 34.57, CI 3.86, 309.50, p = 0.002; more than 3 years: AOR 27.90, CI 2.21 to 351.84, p = 0.010). Advanced age also lowered the odds of HF (AOR 0.90, CI 0.83 to 1.00, p = 0.049). In conclusion, patients' hormonal environments and durations of Anas treatment may play a role in developing Anas-induced adverse effects.
    Matched MeSH terms: Triazoles/adverse effects*; Triazoles/pharmacology
  3. Fulltext Triazoloquinazolines as a new class of potent α-glucosidase inhibitors: in vitro evaluation and docking study
    Abuelizz HA, Anouar EH, Ahmad R, Azman NIIN, Marzouk M, Al-Salahi R
    PLoS One, 2019;14(8):e0220379.
    PMID: 31412050 DOI: 10.1371/journal.pone.0220379
    Previously, we synthesized triazoloquinazolines 1-14 and characterized their structure. In this study, we aimed to evaluate the in vitro activity of the targets 1-14 as α-glucosidase inhibitors using α-glucosidase enzyme from Saccharomyces cerevisiae type 1. Among the tested compounds, triazoloquinazolines 14, 8, 4, 5, and 3 showed the highest inhibitory activity (IC50 = 12.70 ± 1.87, 28.54 ± 1.22, 45.65 ± 4.28, 72.28 ± 4.67, and 83.87 ± 5.12 μM, respectively) in relation to that of acarbose (IC50 = 143.54 ± 2.08 μM) as a reference drug. Triazoloquinazolines were identified herein as a new class of potent α-glucosidase inhibitors. Molecular docking results envisaged the plausible binding interaction between the target triazoloquinazolines and α-glucosidase enzyme and indicated considerable interaction with the active site residues.
    Matched MeSH terms: Triazoles
  4. Fulltext Treated Rhizophora mucronata tannin as a corrosion inhibitor in chloride solution
    Agi A, Junin R, Rasol M, Gbadamosi A, Gunaji R
    PLoS One, 2018;13(8):e0200595.
    PMID: 30089104 DOI: 10.1371/journal.pone.0200595
    Treated Rhizopora mucronata tannin (RMT) as a corrosion inhibitor for carbon steel and copper in oil and gas facilities was investigated. Corrosion rate of carbon-steel and copper in 3wt% NaCl solution by RMT was studied using chemical (weight loss method) and spectroscopic (FTIR) techniques at various temperatures in the ranges of 26-90°C. The weight loss data was compared to the electrochemical by the application of Faraday's law for the conversion of corrosion rate data from one system to another. The inhibitive efficiency of RMT was compared with commercial inhibitor sodium benzotriazole (BTA-S). The best concentration of RMT was 20% (w/v), increase in concentration of RMT decreased the corrosion rate and increased the inhibitive efficiency. Increase in temperature increased the corrosion rate and decreased the inhibitive efficiency but, the rate of corrosion was mild with RMT. The FTIR result shows the presence of hydroxyl group, aromatic group, esters and the substituted benzene group indicating the purity of the tannin. The trend of RMT was similar to that of BTA-S, but its inhibitive efficiency for carbon-steel was poor (6%) compared to RMT (59%). BTA-S was efficient for copper (76%) compared to RMT (74%) at 40% (w/v) and 20% (w/v) concentration respectively. RMT was efficient even at low concentration therefore, the use of RMT as a cost effective and environmentally friendly corrosion inhibiting agent for carbon steel and copper is herein proposed.
    Matched MeSH terms: Triazoles/chemistry
  5. Fulltext Crystal structure of 3-(adamantan-1-yl)-4-(4-chloro-phen-yl)-1H-1,2,4-triazole-5(4H)-thione
    Al-Wabli RI, El-Emam AA, Alroqi OS, Chidan Kumar CS, Fun HK
    Acta Crystallogr E Crystallogr Commun, 2015 Feb 1;71(Pt 2):o115-6.
    PMID: 25878859 DOI: 10.1107/S2056989015000596
    The title compound, C18H20ClN3S, is a functionalized triazoline-3-thione derivative. The benzene ring is almost perpendic-ular to the planar 1,2,4-triazole ring [maximum deviation = 0.007 (1) Å] with a dihedral angle of 89.61 (5)° between them and there is an adamantane substituent at the 3-position of the triazole-thione ring. In the crystal, N-H⋯S hydrogen-bonding inter-actions link the mol-ecules into chains extending along the c-axis direction. The crystal packing is further stabilized by weak C-H⋯π inter-actions that link adjacent chains into a two-dimensional structure in the bc plane. The crystal studied was an inversion twin with a 0.50 (3):0.50 (3) domain ratio.
    Matched MeSH terms: Triazoles
  6. Fulltext Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
    Altamimi AS, Alafeefy AM, Balode A, Vozny I, Pustenko A, El Shikh ME, et al.
    J Enzyme Inhib Med Chem, 2018 Dec;33(1):147-150.
    PMID: 29199484 DOI: 10.1080/14756366.2017.1404593
    A series of symmetric molecules incorporating aryl or pyridyl moieties as central core and 1,4-substituted triazoles as a side bridge was synthesised. The new compounds were investigated as lactate dehydro-genase (LDH, EC 1.1.1.27) inhibitors. The cancer associated LDHA isoform was inhibited with IC50 = 117-174 µM. Seven compounds exhibited better LDHA inhibition (IC50 117-136 µM) compared to known LDH inhibitor - galloflavin (IC50 157 µM).
    Matched MeSH terms: Triazoles/pharmacology*; Triazoles/chemistry
  7. Thiadiazole-, selenadiazole- and triazole-fused anthraquinones as G-quadruplex targeting anticancer compounds
    Andreeva DV, Vedekhina TS, Gostev AS, Dezhenkova LG, Volodina YL, Markova AA, et al.
    Eur J Med Chem, 2024 Mar 15;268:116222.
    PMID: 38387333 DOI: 10.1016/j.ejmech.2024.116222
    G-quadruplex (G4) ligands attract considerable attention as potential anticancer therapeutics. In this study we proposed an original scheme for synthesis of azole-fused anthraquinones and prepared a series of G4 ligands carrying amino- or guanidinoalkylamino side chains. The heterocyclic core and structure of the terminal groups strongly affect on binding to G4-forming oligonucleotides, cellular accumulation and antitumor potency of compounds. In particular, thiadiazole- and selenadiazole- but not triazole-based ligands inhibit the proliferation of tumor cells (e.g. K562 leukemia) and stabilize primarily telomeric and c-MYC G4s. Anthraselenadiazole derivative 11a showed a good affinity to c-MYC G4 in vitro and down-regulated expression of c-MYC oncogene in cellular conditions. Further studies revealed that anthraselenadiazole 11a provoked cell cycle arrest and apoptosis in a dose- and time-dependent manner inhibiting K562 cells growth. Taken together, this work gives a valuable example that the closely related heterocycles may cause a significant difference in biological properties of G4 ligands.
    Matched MeSH terms: Triazoles/pharmacology
  8. Hypoglycemia in patients with type 2 diabetes from India and Malaysia treated with sitagliptin or a sulfonylurea during Ramadan: a randomized, pragmatic study
    Aravind SR, Ismail SB, Balamurugan R, Gupta JB, Wadhwa T, Loh SM, et al.
    Curr Med Res Opin, 2012 Aug;28(8):1289-96.
    PMID: 22738801 DOI: 10.1185/03007995.2012.707119
    To compare the incidence of symptomatic hypoglycemia between sitagliptin and sulfonylurea in Muslim patients with type 2 diabetes who fasted during Ramadan.
    Matched MeSH terms: Triazoles/adverse effects*; Triazoles/therapeutic use
  9. Synthesis, in vitro and in silico studies of S-alkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols as cholinesterase inhibitors
    Arfan M, Siddiqui SZ, Abbasi MA, Rehman A, Shah SAA, Ashraf M, et al.
    Pak J Pharm Sci, 2018 Nov;31(6 (Supplementary):2697-2708.
    PMID: 30587482
    The research was aimed to unravel the enzymatic potential of sequentially transformed new triazoles by chemically converting 4-methoxybenzoic acid via Fischer's esterification to 4-methoxybenzoate which underwent hydrazinolysis and the corresponding hydrazide (1) was cyclized with phenyl isothiocyanate (2) via 2-(4-methoxybenzoyl)-N-phenylhydrazinecarbothioamide (3); an intermediate to 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-thiol (4). The electrophiles; alkyl halides 5(a-g) were further reacted with nucleophilic S-atom to attain a series of S-alkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols 6(a-g). Characterization of synthesized compounds was accomplished by contemporary spectral techniques such as FT-IR, 1H-NMR, 13C-NMR and EI-MS. Excellent cholinesterase inhibitory potential was portrayed by 3-(n-heptylthio)-5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole; 6g against AChE (IC50; 38.35±0.62μM) and BChE (IC50; 147.75±0.67μM) enzymes. Eserine (IC50; 0.04±0.01μM) was used as reference standard. Anti-proliferative activity results ascertained that derivative encompassing long straight chain substituted at S-atom of the moiety was the most potent with 4.96 % cell viability (6g) at 25μM and with 2.41% cell viability at 50μMamong library of synthesized derivatives. In silico analysis also substantiated the bioactivity statistics.
    Matched MeSH terms: Triazoles/chemical synthesis*; Triazoles/metabolism
  10. AChE inhibitor: a regio- and stereo-selective 1,3-dipolar cycloaddition for the synthesis of novel substituted 5,6-dimethoxy spiro[5.3']-oxindole-spiro-[6.3″]-2,3-dihydro-1H-inden-1″-one-7-(substituted aryl)-tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole
    Ashraf Ali M, Ismail R, Choon TS, Kumar RS, Osman H, Arumugam N, et al.
    Bioorg Med Chem Lett, 2012 Jan 1;22(1):508-11.
    PMID: 22142546 DOI: 10.1016/j.bmcl.2011.10.087
    Pyrrolothiazolyloxindole analogues share vital pharmacological properties, considered useful in Alzheimer's disease (AD). The aim of this study was synthesis and evaluate pyralothiazolyloxindole analogues if possess acetyl cholinesterase (AChE) inhibitory activity. The easily accessible one-pot synthesis of these compounds resulted to be significantly less difficult and expensive than that of donepezil. Several compounds possess anti-cholinesterase activity in the order of micro and sub-micromolar. Particularly, compound was the most potent inhibitors of the series against acetyl cholinesterase enzyme with IC(50) 0.11μmol/L.
    Matched MeSH terms: Triazoles/chemical synthesis*; Triazoles/pharmacology
  11. Fulltext Novel rGO-T-C(n) Nanosheets developed via click chemistry as a lubricant anti-wear additive
    Bagheri S, Jamal N, Halilu A, TermehYousefi A
    Sci Rep, 2018 04 18;8(1):6221.
    PMID: 29670168 DOI: 10.1038/s41598-018-23898-y
    Process equipment and facilities are constantly facing the dilemmas of tear and wear. This manuscript introducing functionalized reduced graphene oxide with triazole moiety via click chemistry as a anti-wear additive. While this has been achieved successfully, full characterization of the new anti-wear additive material revealed it to be promising in ameliorating issues of wears. One of the merits of the synthesized material includes reduction of contact asperity as the lipophilic alkyl chain length increases. It has been tested to be functional when formulated as an additive in group III petroleum base oil. Accordingly, it shows an irregularity in renewable base oil. Following screening evaluations of the lipophilic alkyl chain lengths, the additive with twelve carbon atoms; functionalized reduced graphene oxide, rGO-T-C(12) was confirmed to stand out among others with the good reduction of friction coefficient and the least wear scar diameter of ~539.78 µm, compared to the base oil containing no additive.
    Matched MeSH terms: Triazoles
  12. Fulltext Crystal structure of 1-{1-[2-(phenyl-selan-yl)phen-yl]-1H-1,2,3-triazol-4-yl}cyclo-hexan-1-ol
    Camargo LR, Zukerman-Schpector J, Deobald AM, Braga AL, Tiekink ER
    Acta Crystallogr E Crystallogr Commun, 2015 Mar 1;71(Pt 3):o200-1.
    PMID: 25844248 DOI: 10.1107/S2056989015003242
    Two independent mol-ecules, A and B, comprise the asymmetric unit of the title compound, C20H21N3OSe. While the benzene ring directly bound to the central triazole ring is inclined to the same extent in both mol-ecules [dihedral angles = 40.41 (12) (mol-ecule A) and 44.14 (12)° (B)], greater differences are apparent in the dihedral angles between the Se-bound rings, i.e. 74.28 (12) (mol-ecule A) and 89.91 (11)° (B). Close intra-molecular Se⋯N inter-actions of 2.9311 (18) (mol-ecule A) and 2.9482 (18) Å (B) are noted. In the crystal, supra-molecular chains along the a axis are formed via O-H⋯N hydrogen bonding. These are connected into layers via C-H⋯O and C-H⋯N inter-actions; these stack along (01-1) without directional inter-molecular inter-actions between them.
    Matched MeSH terms: Triazoles
  13. Fulltext Effect of Tilt Angle and Pin Depth on Dissimilar Friction Stir Lap Welded Joints of Aluminum and Steel Alloys
    Chitturi V, Pedapati SR, Awang M
    Materials (Basel), 2019 Nov 26;12(23).
    PMID: 31779107 DOI: 10.3390/ma12233901
    Automobile, aerospace, and shipbuilding industries are looking for lightweight materials for cost effective manufacturing which demands the welding of dissimilar alloy materials. In this study, the effect of tool rotational speed, welding speed, tilt angle, and pin depth on the weld joint were investigated. Aluminum 5052 and 304 stainless-steel alloys were joined by friction stir welding in a lap configuration. The design of the experiments was based on Taguchi's orthogonal array for conducting the experiments with four factors and three levels for each factor. The microstructural analysis showed tunnel defects, micro voids, and cracks which formed with 0° and 1.5° tilt angles. The defects were eliminated when the tilt angle increased to 2.5° and a mixed stir zone was formed with intermetallic compounds. The presence of the intermetallic compounds increased with the increase in tilt angle and pin depth which further resulted in obtaining a defect-free weld. Hooks were formed on either side of the weld zone creating a mechanical link for the joint. A Vickers hardness value of HV 635.46 was achieved in the mixed stir zone with 1000 rpm, 20 mm/min, and 4.2 mm pin depth with a tilt angle of 2.5°, which increased by three times compared to the hardness of SS 304 steel. The maximum shear strength achieved with 800 rpm, 40 mm/min, and a 4.3 mm pin depth with a tilt angle of 2.5° was 3.18 kN.
    Matched MeSH terms: Triazoles
  14. Copper Catalysis in Living Systems and In Situ Drug Synthesis
    Clavadetscher J, Hoffmann S, Lilienkampf A, Mackay L, Yusop RM, Rider SA, et al.
    Angew Chem Int Ed Engl, 2016 12 12;55(50):15662-15666.
    PMID: 27860120 DOI: 10.1002/anie.201609837
    The copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction has proven to be a pivotal advance in chemical ligation strategies with applications ranging from polymer fabrication to bioconjugation. However, application in vivo has been limited by the inherent toxicity of the copper catalyst. Herein, we report the application of heterogeneous copper catalysts in azide-alkyne cycloaddition processes in biological systems ranging from cells to zebrafish, with reactions spanning from fluorophore activation to the first reported in situ generation of a triazole-containing anticancer agent from two benign components, opening up many new avenues of exploration for CuAAC chemistry.
    Matched MeSH terms: Triazoles
  15. Deferasirox in thalassemia: a comparative study between an innovator drug and its copy among a sample of Iraqi patients
    Daher AM, Al-Momen H, Jasim SK
    Ther Adv Drug Saf, 2019;10:2042098619880123.
    PMID: 31636883 DOI: 10.1177/2042098619880123
    Background: The health care industry is witnessing an increasing trend in the use of generic medicines because of their presumed low cost compared with innovator medicines. The aim of this study was to determine and compare the performance of the copy drug Osveral® and its innovator drug deferasirox (Exjade®).

    Methods: A prospective observational study including 223 patients receiving the branded medicine Exjade® and 101 patients receiving the copy Osveral® was carried out. Data were assessed for a 1-year period and included clinical symptoms, serum ferritin (SF), serum creatinine (SC), and alanine aminotransferase (ALT). Data were analyzed with SPSS version 22 software (SPSS, Chicago, IL, USA).

    Results: The median age of the sample was 8 years. There was no significant difference in gender distribution between the two groups (p = 0.625). Nausea was the most frequently reported adverse effect followed by diarrhea and abdominal pain in both groups. Patients receiving Exjade® had a higher relative reduction of SF at the end of the study compared with the Osveral® group (19.9% versus 9.93%, p = 0.028). SC was found to be significantly higher in the Osveral® group than in the Exjade® group throughout the study period. The mean platelet count was higher in the Exjade® group. ALT was significantly higher among patients receiving Osveral® over the last three months of the study.

    Conclusions: Exjade® showed a better ability to reduce SF, with less liver toxicity, and better hemostasis profile. No congenital anomalies associated with short-term use of both drugs during pregnancy were observed or reported.

    Matched MeSH terms: Triazoles
  16. Sequential synthesis of amino-1,4-naphthoquinone-appended triazoles and triazole-chromene hybrids and their antimycobacterial evaluation
    Devi Bala B, Muthusaravanan S, Choon TS, Ashraf Ali M, Perumal S
    Eur J Med Chem, 2014 Oct 6;85:737-46.
    PMID: 25129868 DOI: 10.1016/j.ejmech.2014.08.009
    A general method for the synthesis of a library of hitherto unreported amino-1,4-naphthoquinone-appended triazoles was accomplished via a sequential three-component reaction of substituted N-propargylaminonaphthoquinones with variously substituted alkyl bromides/2-bromonaphthalene-1,4-dione and sodium azide in the presence of Et3N/CuI in water. Aminonaphthoquinone-appended iminochromene-triazole hybrid heterocycles were also synthesized from the amino-1,4-naphthoquinone-appended-1,2,3-triazolylacetonitriles. All the triazole hybrids were screened for their in vitro activity against Mycobacterium tuberculosis H37Rv (MTB). Among the triazoles, 2-(((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)(4-(trifluoromethyl)phenyl)amino)naphthalene-1,4-dione (7d) emerged as the most active one with IC50 = 1.87 μM, being more potent than the anti-TB drugs, cycloserine (6 times), pyrimethamine (20 times) and equipotent as the drug ethambutol (IC50 
    Matched MeSH terms: Triazoles/chemistry*
  17. Fulltext Distribution of Silicified Microstructures, Regulation of Cinnamyl Alcohol Dehydrogenase and Lodging Resistance in Silicon and Paclobutrazol Mediated Oryza sativa
    Dorairaj D, Ismail MR
    Front Physiol, 2017;8:491.
    PMID: 28747889 DOI: 10.3389/fphys.2017.00491
    Lodging is a phenomenon that affects most of the cereal crops including rice, Oryza sativa. This is due to the fragile nature of herbaceous plants whose stems are non-woody, thus affecting its ability to grow upright. Silicon (Si), a beneficial nutrient is often used to toughen and protect plants from biotic and abiotic stresses. Deposition of Si in plant tissues enhances the rigidity and stiffness of the plant as a whole. Silicified cells provide the much needed strength to the culm to resist breaking. Lignin plays important roles in cell wall structural integrity, stem strength, transport, mechanical support, and plant pathogen defense. The aim of this study is to resolve effects of Si on formation of microstructure and regulation of cinnamyl alcohol dehydrogenase (CAD), a key gene responsible for lignin biosynthesis. Besides evaluating silicon, paclobutrazol (PBZ) a plant growth retartdant that reduces internode elongation is also incorporated in this study. Hardness, brittleness and stiffness were improved in presence of silicon thus reducing lodging. Scanning electron micrographs with the aid of energy dispersive x-ray (EDX) was used to map silicon distribution. Presence of trichomes, silica cells, and silica bodies were detected in silicon treated plants. Transcripts of CAD gene was also upregulated in these plants. Besides, phloroglucinol staining showed presence of lignified vascular bundles and sclerenchyma band. In conclusion, silicon treated rice plants showed an increase in lignin content, silicon content, and formation of silicified microstructures.
    Matched MeSH terms: Triazoles
  18. Electron microscopy studies of the effects of garlic extract against trichophyton rubrum
    FARZAD AALA, UMI KALSOM YUSUF, ROSIMAH NULIT
    Sains Malaysiana, 2013;42:1585-1590.
    Trichophyton rubrum is one of dermatophytes that penetrates keratinized tissues such as skin, hair and nail of human and animals. Recently, antifungal drugs such as imodazole and triazole was found to cause side effects, toxicity to patients and also not very efficient due to resistance to these drugs. As an alternative, some plants extract had been used to treat dermatophytes. This studies was done using Garlic extract (Allium sativum) to evaluate its effects on the growth of hypha of Trichophyton using Electron miscroscopy. Garlic had been known to posses antimicrobial, antiinflammatory, antithrombotic and antitumor activities. This studies found that garlic extract as low as 4 mg/mL inhibit the growth of hypha. Scanning electron microscopy studies revealed that hypha treated with garlic extract showed shrinkage, flat and cell wall demolition, similar to hypha treated with allicin (positive control) having rough surface, shrinkage and distortion. The tip of hypa became large after treatment with garlic extract. Transmission electron microscopy studies also found that hypha treated with allicin display cell wall thickening, local thickening, destruction of cytoplasmic content, mean while hypha treated with garlic extract exhibited cell wall thickening, disordered hyphal tip and desolution of cytoplasmic compartments and similar with hypha treated with allicin. These results showed that garlic extract and pure allicin could be use as an alternative to treat dermatophytes.
    Matched MeSH terms: Triazoles
  19. Fulltext The α6 subunit-containing GABAA receptor: A novel drug target for inhibition of trigeminal activation
    Fan PC, Lai TH, Hor CC, Lee MT, Huang P, Sieghart W, et al.
    Neuropharmacology, 2018 09 15;140:1-13.
    PMID: 30016665 DOI: 10.1016/j.neuropharm.2018.07.017
    Novel treatments against migraine are an urgent medical requirement. The α6 subunit-containing GABAA receptors (α6GABAARs) are expressed in trigeminal ganglia (TG), the hub of the trigeminal vascular system (TGVS) that is involved in the pathogenesis of migraine. Here we reveal an unprecedented role of α6GABAARs in ameliorating TGVS activation using several pharmacological approaches in an animal model mimicking pathological changes in migraine. TGVS activation was induced by intra-cisternal (i.c.) instillation of capsaicin in Wistar rats. Centrally, i.c. capsaicin activated the trigeminal cervical complex (TCC) measured by the increased number of c-Fos-immunoreactive (c-Fos-ir) TCC neurons. Peripherally, it elevated calcitonin gene-related peptide immunoreactivity (CGRP-ir) in TG and depleted CGRP-ir in the dura mater. Pharmacological approaches included a recently identified α6GABAAR-selective positive allosteric modulator (PAM), the pyrazoloquinolinone Compound 6, two α6GABAAR-active PAMs (Ro15-4513 and loreclezole), an α6GABAAR-inactive benzodiazepine (diazepam), an α6GABAAR-selective antagonist (furosemide), and a clinically effective antimigraine agent (topiramate). We examined effects of these compounds on both central and peripheral TGVS responses induced by i.c. capsaicin. Compound 6 (3-10 mg/kg, i.p.) significantly attenuated the TCC neuronal activation and TG CGRP-ir elevation, and dural CGRP depletion induced by capsaicin. All these effects of Compound 6 were mimicked by topiramate, Ro15-4513 and loreclezole, but not by diazepam. The brain-impermeable furosemide antagonized the peripheral, but not central, effects of Compound 6. These results suggest that the α6GABAAR in TG is a novel drug target for TGVS activation and that α6GABAAR-selective PAMs have the potential to be developed as a novel pharmacotherapy for migraine.
    Matched MeSH terms: Triazoles/pharmacology
  20. Fulltext Enhancement of mechanical properties of blended polyethylene radiation capsules for the triga mark II research reactor
    Fatema Anuar, Mohammed Iqbal Shueb, Ruzitah Mohd Salleh, Nazaratul Ashifa Abdullah Salim, Julia Abdul Karim
    Jurnal Sains Nuklear Malaysia, 2012;24(2):1-13.
    MyJurnal
    Mechanical properties of blended polyethylene (PE) containing the antioxidant Irganox 1010 and the UV-absorber Tinuvin 326 were studied for future use as radiation capsule material for the TRIGA Mark II research reactor. High density and low density polyethylene were blended with the additives and tested for elongation at break, impact strength and gel content, before and after irradiation inside the nuclear reactor. Characterization via FTIR as well as determination of crystallization and melt transition temperatures through DSC were also conducted. It was found that the addition of the antioxidant at different amounts (from 0 to 4 phr) had various effects on the properties of the blended PE, with 0 phr being the amount at which there was the biggest increase in elongation at break and impact strength, post-irradiation.
    Matched MeSH terms: Triazoles
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