Synthesis of NG-061 and its analogs, and their biological evaluation as an enhancer of nerve growth factor.

A novel potentiator of nerve growth factor (NGF), NG-061, which had been isolated from the fermentation broth of Penicillium minioluteum F-4627, was synthesized from methoxybenzoquinone and phenylacetylhydrazine in a single step. A series of acyl hydrazone derivatives were also synthesized and their potentiator activity of neurotrophic effect of NGF on neurite outgrowth was evaluated by assay with a rat pheochromocytoma cell line PC12.

A new method for on-line measurement of diurnal change in potato tuber growth under controlled environments.

An on-line laser micrometer system was applied to measurement of diurnal change in potato (Solanum tuberosum L.) tuber growth. Diameters of the potato tuber were scanned by moving a laser micrometer along the longitudinal axis of the tuber at constant speed, and tuber volume was evaluated as an aggregate of thin discs. A single potato tuber, without competitive sink tubers in the plant, was grown in controlled air at 20 degrees C and 80% RH, and tuber volume was measured at 30 min intervals. During the growth experiment, the potato tuber increased in size without any inhibitory effect of periodical laser beam irradiation. Greatest expansion generally occurred during the early night, and transient contraction of the tuber occurred at the beginning of the light period.

The effect of lesionectomy and the perilesional GABAergic neuronal changes in alumina cream-induced focal motor epilepsy in cats.

The effect of lesionectomy depends on the reversibility of the epileptogenic changes in the perilesional cortex. We studied how the perilesional GABAergic neuronal changes are related to the effect of lesionectomy in the alumina cream-induced focal epilepsy model in cats. Sequential changes of GABAergic neurons and spike activities were measured after the micro-injections of alumina cream (AC). Alumina granulomas were excised 15 days and 40 days after the injections. At day 20 following the AC injection, GABAergic neurons were decreased 25 to 40% compared with those in the contralateral intact cortex. At day 40, a significant increase of spike activities occurred. GABA positive cells were decreased more than 50% compared with those in the contralateral cortex. At day 80, significant cell loss in perilesional cortex was demonstrated. The effect of lesionectomy was greater in the early excised group than in the late excised group. Decrease of GABAergic neuron was more severe in the late excised group compared to the early excised group. Our results indicate that more than 50% reduction of perilesional GABA neurons may be a critical point in epileptogenesis in this model. Lesionectomy alone prior to a 50% reduction in perilesional GABAergic neurons may be sufficient for seizure control. With these data it is still unclear whether these findings contribute to the choice between lesionectomy alone and lesionectomy with resection of the perilesional cortex. Further study is needed to understand the difference between the AC epilepsy model and human chronic epilepsy.

Secondary malignant lymphoma of the central nervous system with delayed high uptake on 123I-IMP single-photon emission computerized tomography. Case report.

A case of secondary central nervous system (CNS) lymphoma with high uptake in the delayed image of N-isopropyl-[123I]-p-iodoamphetamine (125I-IMP) single-photon emission computerized tomography (SPECT) is presented. Previous to this report, only six cases of brain tumor with high uptake on the delayed 123I-IMP SPECT scan have been reported, two of which were CNS malignant lymphomas. Of 19 brain tumors examined with 123I-IMP SPECT at Kameda General Hospital, this case was the only one that showed high uptake in the delayed image. These data imply that 123I-IMP SPECT, which has now become rather obsolete as a tumor-imaging method, can be useful in diagnosing CNS malignant lymphoma.

Synthesis and determination of configuration of natural 25-hydroxyvitamin D(3) 26,23-lactone.

The four stereoisomers of 25-hydroxyvitamin D(3) 26,23-lactone were synthesized by a stereoselective lactonization method. Natural 25-hydroxyvitamin D(3) 26,23-lactone was produced from 25-hydroxy-[3alpha-(3)H]vitamin D(3) by in vitro incubation of kidney homogenate prepared from vitamin D-supplemented chickens or was isolated from the serum of rats given 1,25-dihydroxyvitamin D(3) and 25-hydroxy-[3alpha-(3)H]vitamin D(3). The four synthetic isomers and the naturally produced 25-hydroxyvitamin D(3) 26,23-lactone were subjected to high-performance liquid chromatography in a system capable of separating the four isomers. The natural lactone comigrated with synthetic (23S,25R)-25-hydroxyvitamin D(3) 26,23-lactone, establishing it as the natural vitamin D(3) metabolite.

23,25-Dihydroxyvitamin D3: a natural precursor in the biosynthesis of 25-hydroxyvitamin D3-26,23-lactone.

To elucidate the biosynthesis of 25-hydroxyvitamin D3-26,23-lactone, two known metabolites of 25-hydroxyvitamin D3--23,25-dihydroxyvitamin D3 and 25,26-dihydroxyvitamin D3--were incubated individually with kidney homogenate prepared from vitamin D-supplemented chickens, a preparation known to produce the lactone from 25-hydroxyvitamin D3. The 25-hydroxyvitamin D3-26,23-lactone produced in vitro was then separated, purified, identified, and quantitated by consecutive straight-phase and reverse-phase high-performance liquid chromatography. 23,25-Dihydroxyvitamin D3 is a far better substrate for production of 25-hydroxyvitamin D3-26,23-lactone than is 25,26-dihydroxyvitamin D3. Production of lactone is highly selective for the natural 23(S)-hydroxy-23,25-dihydroxyvitamin D3 while both epimers of 25,26-dihydroxyvitamin D3 resulted in small amounts of product comigrating with natural lactone. It appears that 23(S),25-dihydroxyvitamin D3, but not 25,26-dihydroxyvitamin D3, is a natural precursor in the synthesis of 25-hydroxyvitamin D3-26,23-lactone; this result also implies that the configuration of the lactone at C-23 is S.