Research in Pharmaceutical Sciences
Volume:8 Issue: 3, Aug 2013

The six elements commonly known as metalloids are boron, silicon, germanium, arsenic, antimony, and tellurium. Metalloid containing compounds have been used as antiprotozoal drugs. Boron-based drugs, the benzoxaboroles have been exploited as potential treatments for neglected tropical diseases. Arsenic has been used as a medicinal agent and arsphenamine was the main drug used to treat syphilis. Arsenic trioxide has been approved for the treatment of acute promyelocytic leukemia. Pentavalent antimonials have been the recommended drug for visceral leishmaniasis and cutaneous leishmaniasis. Tellurium (IV) compounds may have important roles in thiol redox biological activity in the human body, and ammonium trichloro (dioxoethylene-O,O’-)tellurate (AS101) may be a promising agent for the treatment of Parkinson’s disease. Organosilicon compounds have been shown to be effective in vitro multidrug-resistance reverting agents.

Turnips with a long history of usage, are helpful in preventing breast and prostate cancer, inflammation and body`s immune system dysfunction. In this study, we investigated the effects of chloroform, ethyl acetate and methanolic extracts of Brassica rapa L. on cell-mediated immune response in mice. Chloroform, ethyl acetate and methanolic extracts of B. rapa glands were prepared by maceration method. To study the effects of B. rapa on acquired immunity, groups of Balb/c mice (n=8) were used. Sheep red blood cell (SRBC) was injected (s.c., 1×108 cells/ml, 0.02 ml) and 5 days later, different extracts (10, 100 and 500 mg/kg), betamethasone (4 mg/kg) and Levamisol (4 mg/kg) as a positive control and normal saline as a negative control were given i.p. After 1 h SRBC was injected to footpad (s.c., 1×108 cells/ml, 0.02 ml) and footpad swelling was measured up to 72 h. To investigate the effects of B. rapa on innate immunity the same procedure was used, but animals only received one injection of SRBC 1 h after i.p. injection of test compounds. Our findings showed that SRBC induced an increase in paw swelling with maximum response at 6-8 and 2-4 h for innate and acquired immunity, respectively. Betamethasone inhibited and levamisol increased paw thickness in both models. In both innate and acquired immunity models, chloroform, ethyl acetate and methanolic extracts of B. rapa glands significantly and dose-dependently reduced paw thickness. Ethyl acetate extract showed better effect. As glucosinolates are better extracted by ethyl acetate, it may be concluded that they are contributed in the more pronounced effects of ethyl acetate extract.

DNA methylation plays an important role in carcinogenesis through epigenetic silencing of tumor suppressor genes. Aberrant methylation usually results from changes in the activity of DNA methyltransferases (DNMTs). Some studies show that the overexpression of the DNMTs may lead to aberrant methylation of tumor suppressor genes. Also the overexpression of DNMTs may be related to methylation status of their genes. Due to limited number of studies on DNMT3B promoter methylation, this study was performed to quantitatively measure the methylation level of DNMT3B gene in archival formalin fixed paraffin embedded (FFPE) tissues from breast cancer patients. Using differential high resolution melting analysis (D-HRMA) technology, the methylation level of DNMT3B gene promoter was quantified in 98 breast cancer FFPE tissues and also 10 fresh frozen normal tissue samples. Statistical analyses used for analyzing the correlation between the methylation and clinical variables. All the normal samples were found to be methylated at the DNMT3B promoter (the average methylation level 3.34%). Patients were identified as hypo-methylated (mean methylation level 0.8%), methylated (mean methylation level 2.48%) and hyper-methylated (mean methylation level 10.5%). Statistical analysis showed a significant correlation between the methylation status and the sample type, cancer type and tumor size. Also the methylation level was significantly associated with histologic grade. It is concluded that quantification of DNMT3B promoter methylation might be used as a reliable and sensitive diagnostic and prognostic tool in breast cancer. Also D-HRMA is demonstrated as a rapid and cost effective method for quantitative evaluation of promoter methylation.

In this study، the aim was the evaluation of effect of intravenous (IV) administration of ketamine، peritonsillar infiltration of tramadol and their combination for control of post-operative pain in comparison with single use of each drug in children undergoing tonsillectomy. One hundred and twenty children، aged 2-15 years، selected for elective adenotonsillectomy were enrolled in the study. We divided the patients into four groups of 30 each، Group I: received IV ketamine 0. 5 mg/kg، Group II: received peritonsillar infiltration of tramadol 2 mg/kg، Group III: received IV ketamine 0. 5 mg/kg added to peritonsillar tramadol 2 mg/kg and Group IV: received IV and peritonsillar infiltration of 0. 9% saline. We utilized the Children’s Hospital of Eastern Ontario Pain Scale (CHEOPS) recorded each 15 min after surgery to the first h and then each 2، 4، 6، 8، 16، 24 h to assess pain levels postoperatively. The analysis of data showed that Group III had significantly lower CHEOPS scores than another three groups (P<0. 001)، while both Groups I and II had the same ranged scores، which were not statistically significant (P>0. 05). During 24 h after surgery، the first time for analgesic requirement was higher in Group III in comparison with other groups (P<0. 001). Combined use of IV ketamine 0. 5 mg/kg with peritonsillar infiltration of tramadol 2 mg/kg provided better and more prolong analgesic effects compared with using each drug alone in patients undergoing tonsillectomy.

A range of iron bidentae ligands containing the chelating moiety 3-hydroxypyridin-4-ones (HPOs) have been synthesized via a single or a three-step synthetic pathway. In the single-step reaction, maltol was directly reacted by suitable primary amine and in the second synthetic method; benzylated maltol was reacted with related amines to give 1-substuted-2-methyl-3-benzyloxypyridin-4-one derivatives. Finally, removal of the benzyl group under acidic conditions was performed by catalytic hydrogenation to yield the favored bidentate chelators as HCl salt. The partition coefficient of the free ligands and their iron (III) complexes between an aqueous phase buffered at pH 7.4 and 1-octanol were also determined. The cytotoxic effects of these iron chelators against HeLa and K562 cell lines were evaluated using MTT assay and the results showed that cytotoxicity was closely related to the lipophilicity of compounds so that the most lipophilic compound (4g) revealed the highest activity and compound 4e as a more hydrophilic agent (Kpart; 0.05) showed the lowest cytotoxic effect.\

This study was conducted to evaluate the burn wound healing and antioxidant activity of methanolic and aqueous extracts of Galium odoratum (L.) Scop. in rats. Second degree burn wounds were induced in six groups of six rats each. Groups 1 and 2 received eucerin and silver sulfadiazine as control and reference standard and groups 3, 4, 5 and 6 were given methanolic and aqueous extracts of 15% and 30% (w/w in eucerin base) respectively. The topical treatment was done daily for 14 days. The percentage of wound contraction and histology parameters of healed wounds were observed. The antioxidant potential of both extracts was assessed by 1, 1-diphenyl-2-picryl-hydrazyl (DPPH) assay. There was statistically significant improvement in wound contraction of animals treated with extracts in comparison to control (p < 0.001). The healed wounds in extracts-treated animals contained less inflammatory cells and had better re-epithelialization. Wound contraction and histology parameters were relatively better in aqueous extract (90.68 ± 6.13% and 97.18 ± 4.37% for aqueous extracts of 15% and 30% in comparison to 79.29 ± 9.16% and 91.94 ± 4.14% for methanolic extracts of 15% and 30% respectively). In DPPH assay, both methanolic and aqueous extracts displayed significant antioxidant activity with IC50 values of 148 µg/ml and 83 µg/ml, respectively. In conclusion, both extracts had desirable antioxidant potential plus experimentally and histologically ascertained burn wound healing activity, relatively better for aqueous extract.

Dried aceton-chloroform extract of aerial parts of Euphorbia spinidens Bornm. ex Prokh. endemic to Iran, yielded two new triterpenoids, lup-20(29)-ene-33, 28 diol commonly known as betulin and (3β,23E)-Cycloarta-23-ene-3,25-diol. The structures of the isolated compounds were elucidated by 13C- and 1H-NMR as well as 2D-NMR, IR and by the aid of mass fragmentation pattern. In phagocyte chemiluminescence assay, different concentrations of compounds were incubated with the human whole blood in triplicate and the chemiluminescence activity of phagocytic cells were measured by using serum opsonized zymosan and luminol. For lymphocyte proliferation assay, peripheral human blood lymphocytes were incubated with different concentrations of the test compound in supplemented Roswell Park Memorial Institute (RPMI) 1640 medium along with 5.0 µg/ml phytohemagglutinin (PHA) at 37ºC in CO2 environment for 72 h and proliferation level was determined by Beta-scintillation counter. In phagocyte chemiluminescence assay, betulin showed moderate inhibitory effect on the oxidative burst in the neutrophils, while addition of betulin triterpene was able to stimulate the proliferation of the phytohemagglutinin (PHA) treated human peripheral blood lymphocytes (hPBLs).

Cell lines derived from mammalian are dominant systems for the production of recombinant therapeutic proteins because of their capacity for correct protein folding, assembly and post-translational modification. In the search of an efficient method for the production of a recombinant protein using animal cell culture, we investigated the effects of different treatment including fetal calf serum concentration, glycerol and culture temperature on a Chinese hamster ovary (CHO) cell line on the production of recombinant human growth hormone (rhGH) and recombinant Chinese hamster ovary (rCHO) viability. The GH production was assessed using ELISA and western blotting methods and cell viability was determined by flow cytometry. The production of recombinant protein increased by 2-fold when stimulatory chemical such as glycerol was added in two stages, first cells were cultured without glycerol for a period of time in order to obtain enough cell density and then glycerol was added to achieve high specific productivity.. Moreover, glycerol addition increased cell viability. Low culture temperature (below 37ºC) led to enhanced cellular productivity of the rhGH by 3-fold but decreased cell viability. These findings indicate that quite simple factors such as culture temperature and addition of simple chemicals may lead to the improvement of industrial process for the production of recombinant proteins such as rhGH.