Purpurins are potent hydrophobic photosensitizers in vivo. Cremopfore EL is an important vehicle for the administration of hydrophobic drugs. Mode-delivery-effects on the binding of etiopurpurin (ET2) to human plasma (LDL, HDL, and high density proteins, HDP) is studied for delivery in CRMaq and...

A pilot study was undertaken to determine the effect of transurethral light on photosensitized periurethral prostatic tissue in the dog. Initial studies demonstrated that a sufficient level of the photosensitizer tin (II) etiopurpurin dichloride, SnET2, was present in the canine prostate 24 hour...

Current local treatments for cutaneous human immunodeficiency virus—associated Kaposi's sarcoma lesions can be less than ideal. Photodynamic therapy (PDT) consisting of a photoreactive drug and a laser light source has been used to treat a variety of neoplasms. This paper presents the case...

Study Objective. To evaluate endometrial ablation in the rat using photodynamic therapy and the photosensitizer tin ethyl etiopurpurin (SnET2).Design. Laboratory research.Setting. A pharmaceutical and device manufacturing company.Materials. Forty-five healthy female rats (age 8–10 wks).Interven...

PurposePrevious studies have demonstrated the technical feasibility of destroying prostate tissue using photodynamic therapy for benign and malignant disease. A series of canine studies was performed to evaluate the systemic uptake and distribution of the photosensitizer tin ethyl etiopurpurin (...

Tin ethyl etiopurpurin is a promising second generation photosensitizer for photodynamic treatment of cancer. This compound is only poorly soluble in aqueous media and, therefore, needs a delivery system for administration to animals. Successful tumor eradication has previously been reported, fo...

ABSTRACTPurpose:Photodynamic therapy (PDT) is an emerging, minimally invasive therapy for prostate cancer that depends on the sequestration of a photosensitizing drug within targeted tissue. The photosensitizer is subsequently activated by light of a specific wavelength, resulting in destruction...

A series of novel 5-methyl-2-phenylthiazole-4-substituted-heteroazole derivatives (6–15) have been synthesized. The structures of these compounds were established by IR, 1HNMR, Mass spectral data and elemental analyses. Compounds were evaluated for their anti-inflammatory and analgesic activiti...

Several new 1-methyl-5-[substituted-4-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic acids and their ethyl ester derivatives were prepared. The compounds were tested for analgesic and antiinflammatory activities, acute toxicity, ulcerogenic effect, and as in vitro inhibitors of 3α-hydroxyste...

Ion-supported Ph3P, 4-(diphenylphosphino)benzyltrimethylammonium bromide (IS-Ph3P), could be used for the facile amidation of a wide range of carboxylic acids with amines in the presence of bromotrichloromethane to provide the corresponding amides in good yields. In the present reaction, the des...

In order to explain the difficulty in hydrolysing the lactam linkage of 1-benzyl-2-oxo-5-ethyl-4-piperidineacetic acid (XIV) under acid conditions, several model compounds such as 1-benzyl-2-piperidone (X), 1-benzyl-5-ethyl-2-piperidone (XI), 1-benzyl-4-ethyl-2-piperidone (XII) and 1-benzyl-2-ox...

The free radical trapping nitrone compounds α-phenyl-N-tert-butylnitrone (PBN), 2-sulfophenyl-N-tert-butylnitrone (S-PBN) and disodium 2,4-disulfophenyl-N-tert-butyl nitrone (NXY-059) are effective neuroprotective agents in experimental models of both transient and permanent focal ischemia. A r...

Oxygen free radical generation may have important secondary damaging effects after the onset of cerebral ischemia. Free radical scavengers have been used successfully in attenuating neuronal damage in the reperfusion period in transient forebrain ischemia. There are limited data on effectiveness...

The status epilepticus (SE) induced in rats by lithium-pilocarpine (Li-pilo) shares many common features with soman-induced SE including extensive limbic neuropathology. Reactive oxygen species are hypothesized to play a role in the SE induced neuropathology and we propose that the free radical ...

Primycin, an antibiotic isolated from a species ot Actinomycetes, inhibits the growth of Euglena gracilis and Astasia longa, but adaptation occurs after a lag whose duration depends sensitively on primycin concentration. A low concentration of actinomycin D, which by itself scarcely inhibits gro...

Primycin is a natural complex, a mixture of homologous antibiotics. On thin-layer chromatography in neutral solvent systems the co-crystallizing components exhibit the phenomenon of secondary adsorption. The complex can be separated in n-butanol or chloroform solvent systems containing a high pe...

Using energy-dispersive X-ray microanalytic and interference microscopic techniques, the intracellular concentration of the monovalent ions (Na+, K+, Cl+) as well as the intracytoplasmic and intracellular water contents were studied in normal and adrenalectomized rat hepatocytes with and without...

1. In the liver of adrenalectomized rats a subtoxic dose of primycin inhibits the synthesis of tryptophan pyrrolase induced by hydrocortisone.2. Primycin does not substantially affect the enhancement of the activity of TP observed in the liver of adrenalectromized animals after administration of...

Primycin, a mixture of macrolide antibiotic agents, on treatment with nucleophiles is transformed in a reversible reaction into water-soluble compounds with the same molecular weights as that of the starting materials. Detailed 2D NMR spectroscopic studies of the separated components revealed th...

The macrolide antibiotic primycin is shown to consist of more than twenty compounds. Nine components, representing about 90 % of the total, have been isolated and their structures elucidated by spectroscopic methods. Molecular weights were determined by FAB mass spectrometry. The components stud...