28-day oral toxicity study of the aqueous extract from spider brake (Pteris multifida Poiret) in rats.

Spider brake (Pteris multifida Poiret) is a very important folk herb and a constituent in most of the traditional herbal beverage formulas in Taiwan; however, little toxicological information is available regarding the safety following repeated exposure. The present study was conducted to evaluate the toxicity of aqueous extract from spider brake (SB) in Sprague-Dawley rats on dietary oral gavage at concentrations of 100, 500, and 1000 mg/kg b.w. day for 28 days. There were no adverse effects on general condition, growth, feed and water consumption, feed conversion efficiency, red blood cell and clotting potential parameters, clinical chemistry values, and organ weights except for neutrophils and lymphocytes being slightly diminished in male and female rats at the highest dose, respectively. Necropsy and histopathology findings revealed no treatment-related changes in any of the organs. The results obtained in this study allowed us to conclude that the SB properly utilized in the traditional oral administration could be devoid of any toxic risk.

Free radical-scavenging activity of aqueous extract of Pteris multifida Poiret.

Aqueous extract of Pteris multifida showed scavenging activities on DPPH, hydroxyl radicals and reducing power.

Efficacy of caspofungin against Aspergillus flavus, Aspergillus terreus, and Aspergillus nidulans.

The echinocandin caspofungin is a potent inhibitor of the activity of 1,3-beta-D-glucan synthase from Aspergillus flavus, Aspergillus terreus, and Aspergillus nidulans. In murine models of disseminated infection, caspofungin prolonged survival and reduced the kidney fungal burden. Caspofungin was at least as effective as amphotericin B against these filamentous fungi in vivo.

Anti-oxidant activity and effect of Pinus morrisonicola Hay. on the survival of leukemia cell line U937.

The free radical scavenging and anti-cancer activites of Pinus morrisonicola Hay. were studied using different parts of the pine, namely, needle, bark and cone. Results showed that pine needle water extract has the highest scavenging superoxide anion activity and the lowest IC50 value in inhibiting superoxide anion formation; however, the bark water extract showed the best anti-lipid peroxidation activity. Additionally, needle water extract displayed the highest inhibition of leukemia cell line U937 growth. The results indicated that P. morrisonicola Hay. possesses potential chemopreventative and therapeutic properties.

BMS-201620: a selective beta 3 agonist.

A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human beta3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent beta3 full agonist (Ki = 93 nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation.

Beta 3 agonists. Part 1: evolution from inception to BMS-194449.

Screening of the BMS collection identified 4-hydroxy-3-methylsulfonanilidoethanolamines as full beta 3 agonists. Substitution of the ethanolamine nitrogen with a benzyl group bearing a para hydrogen bond acceptor promoted beta(3) selectivity. SAR elucidation established that highly selective beta(3) agonists were generated upon substitution of C(alpha) with either benzyl to form (R)-1,2-diarylethylamines or with aryl to generate 1,1-diarylmethylamines. This latter subset yielded a clinical candidate, BMS-194449 (35).(1)

BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.

A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human beta(3) adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 (25), a potent beta(3) full agonist (K(i)=21 nM, 95% activation) with partial agonist (45%) activity at the beta(1) receptor. Based on its desirable in vitro and in vivo properties, BMS-196085 was chosen for clinical evaluation.

CT myelography for differential diagnosis between intramedullary and intradural-extramedullary spinal tumors in the region of the conus medullaris.

We reviewed the myelograms and computed tomographic myelograms of 12 cases of intraspinal tumor with a "cupping sign" on the myelogram in the region of the conus medullaris from 1986 to 1988. There were 5 intramedullary tumors, 4 of them having an exophytic component, and 7 intradural-extramedullary tumors. The myelograms revealed that 4 of the 5 intramedullary tumors showed expansion and the outline of the conus medullaris was irregular, whereas 1 of the tumors showed smooth compression (crescent-shaped) and displacement of the conus medullaris. Six of the 7 intradural-extramedullary tumors showed smooth compression and displacement of the conus medullaris, while 1 of the tumors had caused expansion of the conus medullaris. Complete blockage of the passage of the contrast medium was noted in 3 of the 5 intramedullary tumors, while a partial block was noted in 3 of the 7 intradural-extramedullary tumors. Two of the 7 intradural-extramedulllary tumors showed an extradural tumor component, such as a dumb-bell tumor and a enlarged intervertebral neural foramen. Tumor calcification was noted in 1 of the 7 intradural-extramedullary tumors. Dural ectasia was noted in 2 of the 7 intradural-extramedullary tumors which were later proven to be neurofibromatosis. We conclude that smooth compression (crescent-shaped) and displacement of the conus medullaris, existence of an extradural tumor component, and eroded intervertebral neural foramina favor intradural-extramedullary tumors, while expansion and a conus medullaris with an irregular outline favors intramedullary tumors.