The effect of C2-fluoro group on the biological activity of DC-81 and its dimers

C2-Fluoro substituted pyrrolobenzodiazepines (PBDs) have been synthesized that exhibit potential anticancer activity in a number of human tumour cell lines. These C2-fluoro substituted PBDs also exhibit significant DNA-binding ability.     

Synthesis,Reactions, and Antimicrobial Activity of Novel Heterocyclic Compounds Containing Cyclopenta[d]thieno[2,3-b]pyridine Moiety and Related Fused Heterocycles

Russian Journal of Bioorganic Chemistry - We describe a simple method to synthesize novel 4-cyano-1-morpholin-4-yl-6,7-dihydro-5H-cyclopenta[c]pyridine-3-thione by the reaction of...     

Effects of spermatozoa during in vitro meiosis progression in the porcine germinal vesicle oocytes

We have investigated the effect of co-culture with porcine spermatozoa on in vitro maturation of porcine germinal vesicle (GV) oocytes before fertilization. Most oocytes were arrested at the first prophase of meiosis when oocytes were cultured in TCM 199 alone, but the proportion of oocytes that reached metaphase II was significantly elevated by co-incubation with spermatozoa in vitro. The oocyte maturation effect was observed with intact and parts of spermatozoa (head and tail) collected from adult swine (regardless of source). However, gonocytes from the newborn porcine testis were not able to enhance in vitro maturation of porcine germinal vesicle oocytes. Interestingly, the oocyte maturation effect by spermatozoa was not decreased with heat treatment, but the maturation effect of oocyte treatment disappeared with exposure to detergent in sperm suspension. Porcine spermatozoa were also observed to stimulate meiosis of oocytes, which was maintained at meiotic arrest using dibutyryl cyclic AMP or forskolin. The study suggests that (i) membrane of porcine spermatozoa contains a substance(s) that can enhance in vitro maturation of oocytes prior to fertilization, (ii) the putative meiosis-enhancing substance(s) of spermatozoa from adult testes retains the oocyte maturation effect during transportation of spermatozoa through epididymis, and (iii) the putative meiosis-enhancing substance(s) is able to overcome the inhibitory effect of dibutyryl cyclic AMP or forskolin by inducing germinal vesicle breakdown of porcine cumulus-oocyte complexes maintained in meiotic arrest.     

Influence of nano‐zinc oxide on tropane alkaloid production,h6h gene transcription and antioxidant enzyme activity in Hyoscyamus reticulatus L. hairy roots

The use of nanotechnology and biotechnology to improve the production of plant bioactive compounds is growing. Hyoscyamus reticulatus L. is a major source of tropane alkaloids with a wide therapeutic use, including treatment of Parkinson's disease and to calm schizoid patients. In the present study, hairy roots were obtained from two‐week‐old cotyledon explants of H. reticulatus L. using the A7 strain of Agrobacterium rhizogenes. The effects of different concentrations of the signaling molecule nano‐zinc oxide (ZnO) (0, 50, 100 and 200 mg/L), with three exposure times (24, 48 and 72 h), on the growth rate, antioxidant enzyme activity, total phenol contents (TPC), tropane alkaloid contents and hyoscyamine‐6‐beta‐hydroxylase (h6h) gene expression levels were investigated. Growth curve analysis revealed a decrease in fresh and dry weight of ZnO‐treated hairy roots compared to the control. ANOVA results showed that the antioxidant activity of the enzymes catalase, guaiacol peroxidase and ascorbate peroxidase was significantly higher in the ZnO‐treated hairy roots than in the control, as was the TPC. The highest levels of hyoscyamine (37%) and scopolamine (37.63%) were obtained in hairy roots treated with 100 mg/L of ZnO after 48 and 72 h, respectively. Semi‐quantitative RT‐PCR analysis revealed the highest h6h gene expression was in hairy roots treated with 100 mg/L of ZnO after 24 h. It can be concluded that ZnO is as an effective elicitor of tropane alkaloids such as hyoscyamine and scopolamine due to its enhancing effect on expression levels of the biosynthetic h6h gene.     

Dot-enzyme-linked immunosorbent assay (dot-ELISA) for the rapid diagnosis of human fascioliasis

A dot-enzyme-linked immunosorbent assay (dot-ELISA) was developed as a fast and field applicable antibody detection tool for the diagnosis of human fascioliasis. The assay is performed using partially purified antigens from a species of Fasciola at 180 ng protein/dot (2 microliters) and serum samples at 1:20 dilution (1 microliter). Dot-ELISA results completely agreed with those of micro-ELISA. Antigen-coated nitrocellulose sheets stored for 3 mo at -20 C showed results identical to fresh sheets. Sera from patients with fascioliasis (n = 30) and other parasitic or viral infections (n = 120) were compared with sera from healthy controls (n = 14). Ninety samples can be tested within 90 min. The sensitivity, specificity, and speed of the assay may justify its use in laboratory and field studies.     

Species dependent influence of (-)-alpha-pinene on attraction of ambrosia beetles (Coleoptera: Curculionidae: Scolytinae) to ethanol-baited traps in nursery agroecosystems

Field-based trapping experiments were conducted in Ohio in 2003, 2004, and 2008 to determine the influence of (-)-alpha-pinene on the attraction of exotic and native ambrosia beetles (Coleoptera: Curculionidae: Scolytinae) to ethanol-baited traps. In 2003 and 2004, we determined the effect of adding an (-)-alpha-pinene ultrahigh release lure (UHR; 2 g/d at 20 degrees C) to traps baited with an ethanol UHR lure (0.39 g/d). FewerAnisandrus (Xyleborus) sayi (Hopkins) and Xyleborinus saxeseni (Ratzeburg) were collected in 2003 and 2004 from traps baited with ethanol UHR plus (-)-alpha-pinene UHR compared with ethanol UHR. (-)-alpha-Pinene also reduced the attraction of Xyloterinus politus (Say) to ethanol-baited traps in 2004. Total captures of Xylosandrus germanus (Blandford) in 2003 were higher in traps baited with ethanol UHR plus (-)-alpha-pinene UHR than in traps with ethanol UHR alone but not in 2004. In 2008, captures were compared among traps baited with eight combinations of ethanol and (-)-a-pinene at both UHR and low release (LR) rates. Release rates for ethanol LR and (-)-alpha-pinene LR were 0.027 and 0.0015 g/d, respectively. (-)-alpha-Pinene UHR and (-)-alpha-pinene LR reduced the attractiveness of ethanol UHR to A. sayi and X. saxeseni. Ethanol UHR was also more attractive than ethanol LR to A. sayi and X. germanus. These findings demonstrate traps baited with ethanol alone are more effective than ethanol plus (-)-alpha-pinene for monitoring ambrosia beetle flight activity in ornamental nurseries. Ethanol release rate is also an important consideration for monitoring purposes.     

Growth and physiochemical responses of <Emphasis Type="Italic">Camelina sativa</Emphasis> L. under UV-C stress

A study was conducted to estimate the effect of UV-C (200–280 nm) radiation stress on growth and physiochemical responses of Camelina sativa L. cv. Calina (EC643910; a potential bio-fuel crop) for its possible mass multiplication at high-altitude under high radiations. The germination percentage in terms of radicle protrusion and opening of cotyledonary leaves significantly decreased 13.98 and 27.8 %, respectively, as compared to control. However, no significant change was observed in growth parameters including root and shoot lengths and fresh biomass. The relative membrane leakage rate and lipid peroxidation as a malondialdehyde contents significantly increased with the value of ~99 % and 0.17 mM g^?1 FW, respectively, under UV-C stress. Also, the proline, glycine betaine and total soluble sugars contents increased by ~330, ~440, ~144 %, respectively, as compared to control. Among non-enzymatic antioxidants, the ascorbic acid and total phenol contents significantly increased by ~284 and ~537 %, respectively, as compared to control. Likewise, the activity of antioxidant enzyme, ascorbate peroxidase, guaiacol peroxidase and catalase increased under UV-C stress with the value of 1.03, 0.05 and 0.06 µmol mg protein^?1 min^?1, respectively. In addition, the chlorophyll a, b and total (a + b) contents decreased by ~180, ~151 and ~147 %, respectively, as compared to control. In contrast, the total carotenoids and anthocyanin contents increased by ~160 and ~184 %, respectively. Our findings suggest the adaptive growth and physiochemical responses of C. sativa under UV-C stress. Therefore, it may be recommended for large-scale cultivation at high-altitude under intense natural radiations for future bio-fuel production.     

A requirement for ankyrin binding to clathrin during coated pit budding

Recent studies suggest that the mobility of clathrin-coated pits at the cell surface are restricted by an actin cytoskeleton and that there is an obligate reduction in the amount of spectrin on membranes during coated pit budding. The spectrin-actin cytoskeleton associates with membranes primarily through ankyrins, which interact with the cytoplasmic region of numerous integral membrane proteins. We now report that the fourth repeat domain (D4) of ankyrin(R) binds to the N-terminal domain of clathrin heavy chain with high affinity. Addition of peptides containing the D4 region inhibited clathrin-coated pit budding in vitro. In addition, microinjection of D4 containing peptides blocked the endocytosis of fluorescent low density lipoprotein (LDL). Ankyrin(R) peptides that contained repeat domains other than D4 had no effect on either in vitro budding or internalization of LDL. Finally, immunofluorescence shows that ankyrin is uniformly associated with endosomes that contain fluorescent LDL. These results suggest that ankyrin plays a role in the budding of clathrin-coated pits during endocytosis.