A new irregular monoterpene acetate along with eight known compounds with antifungal potential from the aerial parts of Artemisia incisa Pamp (Asteraceae).

A new compound named as santolinylol-3-acetate (4-(2-hydroxypropan-2-yl)-2-methylhexa-1,5-dien-3-yl acetate) (3), along with seven known compounds; linoleic acid (1), benzoic acid (2), santolinylol (4), ethyl-(E)-p-hydroxy cinnamate (5), scopoletin (6), esculetin (7) isofraxidin (8) and eupatorin (9), were isolated from the aerial parts (ethanolic extract) of endangered species: Artemisia incisa Pamp (Asteraceae). The compounds' structures were determined through modern spectroscopic techniques, and comparison of data (physicochemical constants) with the literature. The relative stereochemistry of santolinylol-3-acetate (3) was determined by comparing its data of NOESY, and specific rotation with its diol analogue; santolinylol (4), isolated from the same plant; A. incisa. The results of the antifungal activity showed that coumarins are as whole less active compounds. Compounds 3 (25 and 300 µg/mL), and 4 (12.5 and 300 µg/mL), showed good activities against Candida albicans, and Aspergillus flavus, respectively, which justifies A. incisa as a traditional medicine for curing the said fungal infections.

Synthesis of (99m)TcN-clinafloxacin Dithiocarbamate Complex and Comparative Radiobiological Evaluation in Staphylococcus aureus Infected Mice.

Clinafloxacin dithiocarbamate (CNND) preparation and radiolabeling through [(99m)Tc ≡ N](2+) core with the gamma (γ) emitter ((99m)Tc) was assessed. The potentiality of the (99m)Tc(V) ≡ N-CNND complex was investigated as perspective a Staphylococcus aureus (S.a.) in vivo infection radiotracer in terms of radiochemical stability in normal saline (n.s.), human serum (h.s.), binding efficacy with live and heat killed S.a. and biodistribution in female nude mice model (FNMD). More than 90% stability was observed in n.s. for 4 h with the highest yield of 98.70 ± 0.26% at 30 min after reconstitution. In h.s., the (99m)Tc(V) ≡ N-CNND complex was found stable up to 16 h with 15.35% side products. Maximum in vitro binding (68.75 ± 0.80%, 90 min) with S.a. was observed after 90 min of incubation. In FNMD, (infected with live strain) approximately six-fold higher uptakes was noted in the infected to inflamed and normal muscles. The higher stability in n.s., h.s., higher S.a. (live) up take with specific and targeted in vivo distribution confirmed potentiality of the (99m)Tc(V) ≡ N-CNND complex as perspective S.a. in vivo infection radiotracer.

(99m)Tc(CO)(3)-Ibritumomab tiuxetan; a novel radioimmunoimaging (RII) agent of B cell non-Hodgkin's lymphoma (NHL).

To exploit the B-lymphocyte antigen-CD20 binding capacity of the Ibritumomab tiuxetan (IBTN) monoclonal antibody (mAb) for imaging, the over-expression of B cells in non-Hodgkin's lymphoma (NHL) (a myeloproliferative disorder of the lymphatic system) was investigated. In the current investigation, we present the labeling of the IBTN with technetium-99m ((99m)Tc) through [(99m)Tc(CO)(3)](+) precursor for radioimmunoimaging (RII) of the tumor prior to its treatment with (90)Y labeled IBTN. Labeled IBTN was radiobiologically characterized in terms of radiochemical purity, in vitro stability in human plasma, immunoreactivity, binding with Raji and Ramos cells and biodistribution in a female nude mouse (FNM) model. It was observed that the reduced IBTN (rIBTN) showed more promising radiobiologic characteristics than the nonreduced IBTN. Significantly higher transchelation was seen in excess cysteine compared with histidine. The radioconjugate showed higher saturated binding affinity with CD20 antigen. Significantly higher target (tumor) to background ratios were observed 1 h post-injection (p.i.). Based on radiochemical purity, in vitro stability, immunoreactivity, binding and biodistrubtion in the FNM model, we recommend the radiolabeling of the rIBTN using tricarbonyl technique as a potential RII agent.

New anthraquinone dimer from the root bark of Cassia artemisioides (Gaudich. Ex. DC) Randell.

The phytochemical investigation of the root bark of Cassia artemisioides (Gaudich. Ex. DC) Randell resulted in the isolation of one new anthraquinone 1,1'-dihydroxy-3,3'-dimethyl-8,8'-dimethoxy-6,6'-O-bianthraquinone (1) along with four known anthraquinones 1,6-dihydroxy-8-methoxy-3-methylanthraquinone (2), 1-hydroxy-8-methoxy-3-methylanthraquinone (3), 1,8-dihydroxy-6-methoxy-3-methylanthraquinone (4), and 1,6,8-trihydroxy-3-methylanthraquinone (5). The structures of the compounds were elucidated using spectroscopic techniques including 1D and 2D NMR. The compounds were evaluated for antioxidant activity. 1,6,8-Trihydroxy-3-methyl anthraquinone (5) showed good activity among the tested compounds.

Radiosynthesis of (99m)Tc(CO)3-Clinafloxacin Dithiocarbamate and Its Biological Evaluation as a Potential Staphylococcus aureus Infection Radiotracer.

BACKGROUND: Clinafloxacin dithiocarbamate (CNND) was radiolabeled with technetium-99m ((99m)Tc) using [(99m)Tc(CO)3(H2O)3](+) and assessed for its radiochemical stability in saline and serum, its in vitro binding with methicillin-resistant Staphylococcus aureus (MRSA) and biodistribution in female nude mice (FNM) artificially infected with live and heat-killed MRSA. METHODS: In normal saline (NS) the (99m)Tc(CO)3-clinafloxacin dithiocarbamate ((99m)Tc(CO)3-CNND) showed radiochemical stability with a maximum value of 99.10 ± 0.20% and remained stable up to 4 h (92.65 ± 0.18%). RESULTS: In human serum at 37°C within 16 h of incubation, 14.85% side products as a result of de-tagging developed. Incubation with MRSA gave saturated binding with a maximum value of 72.75 ± 1.20%. Almost six-fold higher uptake was seen in the infected muscle of the FNM as compared to the inflamed and normal muscle. The (99m)Tc(CO)3-CNND complex showed a normal route of excretion from the body of the FNM model. CONCLUSION: The higher stability in NS, HS, saturated in vitro binding with a live strain of MRSA and six-fold higher uptake in the target organ showed the (99m)Tc(CO)3-CNND complex to be a potential MRSA infection radiotracer.