Synthesis of bioactive quinazolin-4(3H)-one derivatives via microwave activation tailored by phase-transfer catalysis.

A series of nine new 2,3-disubstituted 4(3H)-quinazolin-4-one derivatives was furnished starting from the 2-propyl-4(3H)-quinazo-line-4-one (2). The reinvestigation of the key starting quinazolinone 2 was performed under microwave irradiation (MW) and solvent-free conditions. Combination of MW and phase-transfer catalysis using tetrabutylammonium benzoate (TBAB) as a novel neutral ionic catalyst was used for carrying out N-alkylation and condensation reactions of compound 2 as a simple, efficient and eco-friendly technique. The structure of the synthesized compounds was elucidated using different spectral and chemical analyses. In vitro antimicrobial activity of the compounds was investigated against four bacterial and two fungal strains; very modest activity was achieved. Some of the synthesized compounds were screened for their antitumor activity against different human tumor cell lines. The screened compounds exhibited a significant antitumor activity on some of the cancer cell lines, melanoma (SK-MEL-2), ovarian cancer (IGROV1), renal cancer (TK-10), prostate cancer (PC-3), breast cancer (MCF7) and colon cancer (HT29). The most active, even more active than the reference 5-fluorouracil, were found to be ethyl 4-[(4-oxo-2-propylquinazolin-3(4H)-yl)methyl]benzoate (3c), 3-{2-[6-(pyrrolidin-1-yl-sulfonyl)-1,2,3,4-tetrahydroquinoline]-2-oxoethyl}-2-propylquinazolin--4(3H)-one (3e), N'-[(E)-(2H-1,3-benzodioxo-5-yl)methylidene]-2-(4-oxo-2-propylquinazolin-3(4H)-yl)acetohydrazide (10a), N'-[(E)-(4-hydroxyphenyl)methylidene]-2-(4-oxo-2-propylquinazo-lin-3(4H) -yl)acetohydrazide (10b) and N'-[(E)-(4-nitrophenyl)methyl idene]-2-(4-oxo-2-propylquinazolin-3(4H)-yl)acetohydrazide (10c).

Occupational infection and needle stick injury among clinical laboratory workers in Al-Madinah city, Saudi Arabia.

BACKGROUND: Clinical laboratory workers face biohazard such as needlestick injury and occupational infection on a daily basis. In this study, we examined self-reported frequency of occupational infection and needlestick injury among the clinical laboratory workers in Al- Madinah, Saudi Arabia. METHODS: A total of 234 clinical laboratory workers were recruited from private and government health sectors to answer a self-administered questionnaire that was prepared to achieve the aims of the study. RESULTS: The results showed that approximately 33% of the sample had an experienced occupational infection while 24% had experienced a needlestick injury. Approximately, 49% reported that they always recap needle after use, whereas 15% reported doing that most of the times. Occupational infection, needlestick injury and recapping needles after use were associated with lack of training on biosafety (P < 0.05). CONCLUSION: The frequency of occupational infection and needlestick injury among clinical laboratory workers in Al-Madinah is high. Interventions related to biosafety and infection control and the use of needlestick prevention devices might be useful in lowering such frequency.

Assessment of biosafety measures in clinical laboratories of Al-Madinah city, Saudi Arabia.

INTRODUCTION: Workers in clinical laboratories are exposed to occupational hazards on a daily basis and their health and safety may be threatened if appropriate protective standards are not implemented. The aim of this study was to assess the knowledge and practices of clinical laboratory workers towards biosafety measures, in Al-Madinah city, Saudi Arabia. METHODOLOGY: Clinical laboratory staff was recruited from both the public and private sectors. A structured self-administered questionnaire was used to achieve the aim of the study. RESULTS: A total of 208 workers participated in the study (64% were males, 57% were from the public sector and 71% held a BSc degree). About 68% of the workers were trained in laboratory safety. The majority (> 80%) followed guidelines for disposing medical wastes, decontamination of sample spills, and use of protective lab coats, gloves, etc. However, among participants, 24.2% used to eat, drink or use gum, 18.3% used cosmetics and 24.6% used the mobile phone in the lab. About 18.4% reported that they continued working with a finger cut, whereas 67% reported that they used to recap needles after blood withdrawal. These unacceptable behaviors were associated with lack of lab safety training (P < 0.05), biology degree holders (P < 0.05), and low experience (3 years and less, P < 0.01). With respect to facilities, most of the laboratories complied with standard safety measures. CONCLUSION: The majority of the sample showed good laboratory practices with respect to safety measures. However, some behaviors are not accepted and need interventions.

Dual Effect of Curcumin-Zinc Complex in Controlling Diabetes Mellitus in Experimentally Induced Diabetic Rats.

Ultrasound-assisted extraction of curcumin from Curcuma longa was performed in an ultrasonic bath at 30°C using ethanol for 40 min. A successful attempt has been made to prepare curcumin-zinc (Zn) complex using a simple chemical procedure. The complex formation and its stoichiometry were characterized using elemental analysis, Fourier transform (FT)-IR and UV spectroscopy which revealed the interaction of Zn(II) ion (M) with curcumin (ligand, L) to proceed via (ML) complex type formation. Oral administration of curcumin-Zn complex at a concentration of 150 mg/kg body weight/rat/d for 45 d in streptozotocin-induced diabetic rats in comparison to curcumin and/or Zn administration exerted a hypoglycemic effect. A significant reduction in blood glucose, glycosylated hemoglobin (Hb)A1c, and lipid profile parameters with an excellent improvement in plasma insulin levels have been attained. Also, the reduced activities of serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), urea, and creatinine in the diabetic rats treated with the complex exhibited the non-toxic nature of the curcumin-Zn complex. Finally, the larger extent of the complex in hyperglycemic improvement in comparison to curcumin and/or Zn supplementation was interpreted by its dual action on glucose and insulin maintenance.

Antimutagenic and anticancer activity of Al Madinah Alhasawy mint (Mentha longifolia) leaves extract.

Mentha is one of the genera of Lamiaceae family. The aim of the present study was to evaluate the antimutagenic and anticancer activity of the water and methanolic extract of Alhasawy mint (Mentha longifolia), that grown in Madina Province, western region, Saudi Arabia using three different bioassays namely; Brine shrimp bioassay, Ames mutagenicity bioassay using 3 Hist-Salmonella typhimurium strains of different mutations (TA98, TA97 and TA100) and 2 reference mutagenic drugs nitrosopiperidine (NP) and 2-amino-3-methylimidazo-quinolidine (IQ) and Mammalian cell lines bioassays using 2 different cell lines HepG2 and Vero cell lines. The plant extract showed an efficient antimutagenic activity against the studied bioassays in a directly proportional effect with concentration.

Molecular characterization of Leishmania infection in sand flies from Al-madinah Al-munawarah province, western Saudi Arabia.

Cutaneous leishmaniasis (CL) is caused by various species of the genus Leishmania. The disease is considered a major health problem in different areas of Saudi Arabia including Al-madinah Al-munawarah province. We aimed to identify Leishmania species isolated from sand fly vectors by molecular analysis. Sand fly sampling was carried out from May 2010 to October 2010 in province of Al-madinah Al-munawarah from four different localities. Female sand flies collected were subjected to DNA extraction followed by molecular analysis using the semi-nested PCR and conventional PCR protocols, respectively, against minicircle kDNA and ribosomal internal transcribed spacer 1 (ITS1-rDNA). The PCR positive specimens against ITS1-rDNA locus were digested for further confirmation of species identification. A total of 2910 sand flies were collected. Phlebotomus papatasi accounted for 93.8% (1673 males and 1057 females), however, the number of Phlebotomus sergenti was only 180 (109 males and 71 females). Sixty-two out of 250 (23.7%) female P. papatasi tested for Leishmania parasite were positive for Leishmania major using the semi-nested PCR method against kDNA. All of the 62 positive specimens produced a band size 650 bp. A 31% of female P. sergenti were positive against kDNA of Leishmania tropica and produced a 720 bp band. These positive P. sergenti for L. tropica DNA produced ITS1-PCR-RFLP profile showed two bands of ∼200 bp and 57 bp which are specific for L. tropica, confirming the presence of L. tropica in P. sergenti. However, the ITS1-PCR-RFLP profile showed two bands of ∼203 bp and 132 bp which are specific for L. major in P. papatasi. We concluded that, the semi-nested PCR method against kDNA and the ITS1-PCR-RFLP analysis are useful tools for molecular identification of both L. major and L. tropica. A multicenter study is necessary in order to evaluate the extent of the disease and functional analysis of new Leishmania genes.

Molecular characterization of cutaneous leishmaniasis in Al-Madinah Al-Munawarah province, western Saudi Arabia.

BACKGROUND: Leishmaniasis is a parasitic disease affecting a large number of people worldwide. In this study we carried out the molecular characterization of cutaneous leishmaniasis (CL) in Al-Madinah Al-Munawarah Province, Saudi Arabia, confirming Leishmania major and Leishmania tropica as the prevalent species using molecular techniques. METHODS: One hundred and five patients with suspected CL were identified from four different localities in Al-Madinah Al-Munawarah Province and Al-Miqat Hospital, Al-Madinah, Saudi Arabia. Thirty-four of the 105 patients were selected at random for molecular investigation. RESULTS: Characterization of CL species by internal transcribed spacer 1 (ITS1) PCR-restriction fragment length polymorphism (RFLP) and kinetoplast DNA (kDNA) PCR established L. major and L. tropica as the causative organisms. kDNA PCR had a sensitivity of 90.7%, whereas ITS1 PCR had a sensitivity of 70.1%, thus facilitating the diagnosis and species identification. Parasite culture alone detected 39.2% and smear alone 55.3% of the positive samples. With the exception of kDNA PCR, all other assays were 100% specific. CONCLUSIONS: This study provides the first findings for the comprehensive molecular characterization of CL in Saudi Arabia.

Cytotoxic activity of methanolic extract of Mentha longifolia and Ocimum basilicum against human breast cancer.

Labiatae family is represented in Saudi Arabia. The aim of the present study was to go insight to investigate the anticancer activity and antioxidative potentials of methanolic extracts of Mentha longifolia L. (ML) and Ocimum basilicum L. (OB) that grown in Madina province, western region, Saudi Arabia. OB exhibited the greater phenolic contents as mg gallic acid equivalent/g weight (mg GAE/g) for a value of 105 +/- 5.5 mg GAE/g. On the other hand, ML produced 29 +/- 3.12 mg GAE/g. The standard antioxidant vitamin E used in this experiment elicited a value of total phenolic contents equal 22 +/- 2.2 mg GAE/g. The percentage scavenging activity of against diphenylpicrylhydrazyl (DPPH) was 850 and 160% for OB and ML extracts, respectively. Vitamin E elicited% scavenging activity of against DPPH equal to 198%. Brine shrimp cytotoxic assay clearly indicated the cytotoxic effects of either ML or OB extract. The brine shrimp survival is inversely proportional to the concentration of either ML or OB extract used with LD50 191.23 and 235.50 ppm, respectively. Toxic effects on brine shrimps indicated the anticancer potential of ML or OB extract. The ML or OB extract was unable to produce pbluescript (pBS) plasmid DNA damage, while the plasmid DNA treated with EcoRI produced a single band as a result of DNA damage. Also, both ML and OB extract exhibited marked cytotoxic activity against MCF-7 cells at various concentrations (20, 40, 80, 160 and 320 microg mL(-1)). The 160 and 320 microg mL(-1) showed more cytotoxic effect against MCF-7 cells. Based on results achieved, we can concluded that, OB and ML extracts have the potency to act as powerful antioxidants and protect against DNA damage and have cytotoxic activity against MCF-7 cell line.

Fracture resistance of teeth obturated with RealSeal using two different chelating agents: an in vitro study.

OBJECTIVES: The aim of this study was to evaluate the fracture resistance of endodontically treated teeth filled with a resin-based obturation material using two different chelating agents. METHODS AND MATERIALS: Forty extracted single-canal human teeth were prepared, instrumented, and randomly divided into three groups: Group 1 (n=15) received a final flush with 10 ml of neutralized 17% EDTA, followed by 10 ml of sodium hypochlorite (NaOCl), then obturated using lateral condensation with RealSeal. Group 2 (n=15) received a final flush of BioPure MTAD, followed by 10 ml of NaOCl, then obturated using lateral condensation with RealSeal. Group 3, the control group (n=10), was instrumented but not obturated, then the root canal opening was sealed with a temporary filling material. The specimens were stored in 100% humidity for 10 days, mounted in polyester resin, and loaded to failure. RESULTS: The ANOVA revealed a significant difference between the control group and the experimental groups, although there was no statistically significant difference between Group 1 and Group 2 (p=0.05). The MTAD group displayed higher mean fracture load values than the EDTA group. CONCLUSIONS: It can be concluded that filling the root canals with RealSeal increased the in vitro resistance to fracture of single-canal extracted human teeth when compared to instrumented and unobturated teeth. Teeth treated with MTAD demonstrated high fracture-resistance values when compared to teeth treated with 17% EDTA, but they were not statistically significant. CLINICAL SIGNIFICANCE: Filling the root canals with RealSeal with increased bonding to roots will increase resistance to fracture of these teeth.

Effect of eugenol-based root canal sealers on retention of prefabricated metal posts luted with resin cement.

OBJECTIVE: This study evaluated the effect of two different eugenol-based root canal sealers on the retention of prefabricated metal posts luted with adhesive resin cement. MATERIALS AND METHODS: Thirty prefabricated ParaPosts randomly divided among three groups of 10 each were luted into extracted single-rooted teeth with adhesive resin cement. Two of the groups had been obturated with Gutta-Percha and one of two eugenol-based root canal sealers (Endofil and Tubli-Seal), respectively. The third group was not obturated and served as the control. The forces required for dislodgment of posts from their prepared post spaces were recorded using a universal testing machine. Data were statistically analyzed using one-way ANOVA and Tukey's multiple range test was used to determine the mean differences. RESULTS: Endofil and Tubli-Seal groups demonstrated significantly reduced retention compared to the unobturated (control) group (P < 0.05). CONCLUSION: Eugenol-based sealers significantly reduced the retention of prefabricated posts luted with adhesive resin cement.

Dimensions of metal framework components of metal-ceramic fixed partial dentures constructed in a dental school setting.

OBJECTIVES: The aims of this study were to measure the dimensions of connectors and retainer copings of metal-ceramic fixed partial denture (FPD) frameworks and to explore, by means of a questionnaire, the factors viewed by technicians as important in their planning and provision of such dimensions. METHOD AND MATERIALS: Using two calliper devices, measurements were made of 66 consecutive FPDs under production in a dental school-based laboratory. The dimensions of 176 connectors and 124 retainers were analyzed with reference to FPD length and to number of pontics in a span. Questionnaires were completed by all 14 technicians working in the fixed prosthodontics section of the laboratory. RESULTS: The largest mean vertical connector dimensions were in the anterior regions of both arches, while the largest mean horizontal dimensions were in the posterior regions. Dimensions were unrelated to FPD size and length of interabutment span. The minimum thickness of the retainer coping walls was generally below optimal recommendations. Available space was the factor most commonly cited by technicians as dictating the dimensions that they applied. CONCLUSION: Dimensions were generally smaller than current recommendations, which the questionnaire responses indicate are largely due to space constraints.

Influence of timing of coronal preparation on retention of cemented cast posts and cores.

PURPOSE: This study investigated the effect of coronal preparation by high-speed handpiece on the retention of cemented cast posts and cores. MATERIALS AND METHODS: Cast posts and cores were fabricated for 90 extracted single-rooted human teeth cemented with zinc-phosphate cement and randomly divided into six groups of 15 specimens each. The six groups were matched randomly two by two, such that one of each of the matched groups was subjected to a 4-minute period of high-speed preparation of the cores. Castings from the first pair (1 and 2) were subjected to an axially directed removal force using a universal testing machine 15 minutes from the start of cement mixing; castings from the second (3 and 4) and third (5 and 6) pairs were tested at 1 hour and 24 hours, respectively, having been stored in water at 37 degrees C for the waiting periods. The forces required for dislodgment of posts from their prepared spaces were recorded. Data were statistically analyzed using two- and one-way ANOVA and the Student's t test. RESULTS: The results showed increased mean retentive strengths of posts as the time to testing increased for both unprepared and prepared groups. Significantly higher mean retentive strengths of posts were recorded for unprepared compared to prepared groups tested at 15 minutes and 1 hour after cementation. CONCLUSION: High-speed preparation had a significant negative effect on the retentive strengths of posts tested at 15 minutes and 1 hour after cementation, but not on those tested at 24 hours.