Search results for "Allium"
showing 10 items of 385 documents
Gallium modulates osteoclastic bone resorption in vitro without affecting osteoblasts.
2010
Gallium (Ga) has been shown to be effective in the treatment of disorders associated with accelerated bone loss, including cancer-related hypercalcemia and Paget's disease. These clinical applications suggest that Ga could reduce bone resorption. However, few studies have studied the effects of Ga on osteoclastic resorption. Here, we have explored the effects of Ga on bone cells in vitro.In different osteoclastic models [osteoclasts isolated from long bones of neonatal rabbits (RBC), murine RAW 264.7 cells and human CD14-positive cells], we have performed resorption activity tests, staining for tartrate resistant acid phosphatase (TRAP), real-time polymerase chain reaction analysis, viabili…
Bifunctional Gallium-68 Chelators: Past, Present, and Future
2016
This article reviews the development of bifunctional chelates for synthesising (68)Ga radiopharmaceuticals. It structures the chelates into groups of macrocycles, nonmacrocycles, and chimeric derivatives. The most relevant bifunctional chelates are discussed in chelate structure, parameters of (68)Ga-labeling, and stability of the (68)Ga-chelate complexes. Furthermore those derivatives are included, where (67)Ga was applied instead of (68)Ga. A particular feature discussed is the ability of certain bifunctional chelate structures to function in kit-type preparation of the (68)Ga radiopharmaceuticals. Currently, nonmacrocyclic and chimeric derivates attract particular attention such as THP-d…
Structure and cytotoxicity of steroidal glycosides from Allium schoenoprasum
2013
Abstract A phytochemical analysis of the whole plant of Allium schoenoprasum , has led to the isolation of four spirostane-type glycosides ( 1 – 4 ), and four known steroidal saponins. Their structures were elucidated mainly by 2D NMR spectroscopic analysis and mass spectrometry as (20 S ,25 S )-spirost-5-en-3β,12β,21-triol 3- O -α- l -rhamnopyranosyl-(1 → 2)-β- d -glucopyranoside ( 1 ), (20 S ,25 S )-spirost-5-en-3β,11α,21-triol 3- O -α- l -rhamnopyranosyl-(1 → 2)-β- d -glucopyranoside ( 2 ), laxogenin 3- O -α- l -rhamnopyranosyl-(1 → 2)-[β- d -glucopyranosyl-(1 → 4)]-β- d -glucopyranoside ( 3 ), and (25 R )-5α-spirostan-3β,11α-diol 3- O -β- d -glucopyranosyl-(1 → 3)-[β- d -glucopyranosyl-…
Cytotoxic steroidal glycosides from Allium flavum.
2014
Abstract Three new spirostane-type glycosides ( 1 – 3 ) were isolated from the whole plant of Allium flavum . Their structures were elucidated mainly by 2D NMR spectroscopic analysis and mass spectrometry as (20 S ,25 R )-2α-hydroxyspirost-5-en-3β-yl O -β- d -xylopyranosyl-(1 → 3)-[β- d -galactopyranosyl-(1→2)]-β- d -galactopyranosyl-(1→4)-β- d -galactopyranoside ( 1 ), (20 S ,25 R )-2α-hydroxyspirost-5-en-3β-yl O -β- d -xylopyranosyl-(1 → 3)-[β- d -glucopyranosyl-(1→2)]-β- d -galactopyranosyl-(1→4)-β- d -galactopyranoside ( 2 ), and (20 S ,25 R )-spirost-5-en-3β-yl O -α- l -rhamnopyranosyl-(1 → 4)-[β- d -glucopyranosyl-(1→2)]-β- d -glucopyranoside ( 3 ). The three saponins were evaluated f…
44Sc-DOTA-BN[2-14]NH2 in comparison to 68Ga-DOTA-BN[2-14]NH2 in pre-clinical investigation. Is 44Sc a potential radionuclide for PET?
2011
In the present study we demonstrate the in vitro and in vivo comparison of the (44)Sc and (68)Ga labeled DOTA-BN[2-14]NH(2). (44)Sc is a positron emitter with a half life of 3.92 h. Hence it could be used for PET imaging with ligands requiring longer observation time than in the case of (68)Ga.The binding affinity of (nat)Sc-DOTA-BN[2-14]NH(2) and (nat)Ga-DOTA-BN[2-14]NH(2) to GRP receptors was studied in competition to [(125)I-Tyr(4)]-Bombesin in the human prostate cancer cell line PC-3. A preliminary biodistribution in normal rats was performed, while first microPET images were assessed in male Copenhagen rats bearing the androgen-independent Dunning R-3327-AT-1 prostate cancer tumor.The …
Potential use of 68Ga-apo-transferrin as a PET imaging agent for detecting Staphylococcus aureus infection.
2010
Abstract Introduction 67 Ga citrate has been extensively used to detect infection and inflammation since 1971. However, its clinical utility is compromised due to several limitations. The present project explored whether 68 Ga- apo -transferrin ( 68 Ga-TF), when prepared in vitro, is a useful agent for positron emission tomography (PET) imaging of bacterial infection. Methods An infection was induced in male Wistar rats by injecting 5×10 5 CFU units of Staphyococcus aureus in the right thigh muscle. 68 Ga-TF was synthesized by mixing 68 GaCl 3 with apo -transferrin (TF, 2 mg) in sodium carbonate (0.1 M, pH 7.0) and incubating at 40°C for 1 h. Animals were injected with 10–15 MBq of 68 Ga-TF…
A DOTA based bisphosphonate with an albumin binding moiety for delayed body clearance for bone targeting
2016
Radiolabeled bisphosphonates are commonly used in the diagnosis and therapy of bone metastases. Blood clearance of bisphosphonates is usually fast and only 30%-50% of the injected activity is retained in the skeleton, while most of the activity is excreted by the urinary tract. A longer blood circulation may enhance accumulation of bisphosphonate compounds in bone metastases. Therefore, a chemically modified macrocyclic bisphosphonate derivative with an additional human albumin binding entity was synthesized and pharmacokinetics of its complex was evaluated. The DOTA-bisphosphonate conjugate BPAMD was compared against the novel DOTAGA-derived albumin-binding bisphosphonate DOTAGA(428-d-Lys)…
68Ga-BPAMD: PET-imaging of bone metastases with a generator based positron emitter
2012
Abstract Purpose Bone metastases are a serious aggravation for patients suffering from cancer. Therefore, early recognition of bone metastases is of great interest for further treatment of patients. Bisphosphonates are widely used for scintigraphy of bone lesions with 99m Tc. Using the 68 Ge/ 68 Ga generator together with a macroyclic bisphosphonate a comparable PET-tracer comes into focus. Procedures The bisphosphonate DOTA-conjugated ligand BPAMD was labelled with 68 Ga. [ 68 Ga]BPAMD was evaluated in vitro concerning binding to hydroxyapatite and stability. The tracer's in vivo accumulation was determined on healthy rats and bone metastases bearing animals by μ-PET. Results BPAMD was lab…
Radiolabelling and preliminary evaluation of 68Ga-tetrapyrrole derivatives as potential tracers for PET
2013
article i nfo Tetrapyrroles are multisided natural products which are of relevance in clinical medicine. Owing to their specific accumulation in tumour tissue, porphyrins, metalloporphyrins and chlorins have been used as in photodynamic therapy and optical imaging. Moreover, their specific uptake into inflammatory atheromatous plaques via LDL endocytosis has been reported. The present study is concerned with the synthesis of 68 Ga labelled porphyrin derivatives and an in vitro assessment of the utility of radiotracers in positron emission tomography. A set of five porphyrin derivatives were labelled using 68 Ga from a commercially obtained radionuclide generator. Dedicated post-processing o…
Liver subcellular fractions from rats treated by organosulfur compounds from Allium modulate mutagen activation
2000
The effects of in vivo administration of naturally occurring organosulfur compounds (OSCs) from Allium species were studied on the activation of several mutagens. Male SPF Wistar rats were given p.o. one of either diallyl sulfide (DAS), diallyl disulfide (DADS), dipropyl sulfide (DPS) or dipropyl disulfide (DPDS) during 4 consecutive days and the ability of hepatic S9 and microsomes from treated rats to activate benzo[a]pyrene (BaP), cyclophosphamide (CP), dimethylnitrosamine (DMN), N-nitrosopiperidine (N-PiP) and 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) was determined in the Ames test. Administration of DAS, DPS and DPDS resulted in a significant increase of the activation of…