Biomedical subjects

M Fujimaki

Publications and source records attributed to M Fujimaki.

232 records · Page 13Linked to original sources

PubMedDate not supplied

Diverse biological activity of polycaphenol.

Millimolar concentrations of alkaline extract of Cacao husk (polycaphenol) were more cytotoxic to human oral tumor cells (human oral squamous cell carcinoma HSC-2, human salivary gland tumor HSG), than to human gingival fibroblast (HGF), suggesting its tumor-specific action. Polycaphenol enhanced the radical intensity and cytotoxic activity of vitamin K3 more effectively than that of sodium ascorbate (vitamin C). Polycaphenol effectively scavenged the superoxide anion, produced by the hypoxanthine-xanthine oxidase reaction, indicating bimodal (prooxidant and antioxidant) action of polycaphenol. Polycaphenol inhibited the cytopathic effect of HIV (human immunodeficiency virus) infection in MT-4 cells, to a comparable extent as that achieved by lignin. Pretreatment of mice with polycaphenol protected them from lethal infection of Eschericia coli. These data suggest the medicinal efficacy of polycaphenol.

Animals↗

PubMedDate not supplied

Diverse biological activities of moxa extract and smoke.

Diverse biological activities of moxa extracts and smoke (gas phase) were investigated. Moxa was extracted with hot water (Fr. I), or ethanol (Fr. II), or extracted with hot water after ethanol wash (Fr. III) and then lyophilized to obtain the dried powders. Moxa smoke (containing a lot of gaseous components obtained by burning Moxa) (Fr. IV) was collected into phosphate-buffered saline and quantified spectrophotometrically. These extracts and Moxa smoke showed comparable cytotoxic activity against human oral tumor cell lines (HSC-2, HSG). Human gingival fibroblasts (HGF) were more resistant to any Moxa fractions. Neither of the extracts showed anti-HIV activity. Pretreatment of mice with Fr. I significantly reduced the lethal effect of E. coli infection. All extracts produced radicals under alkaline condition, with a maximum intensity at pH 10.5, and enhanced the radical intensity of sodium ascorbate. It was unexpected that these extracts show significant O2- scavenging activities. These data suggest the medicinal efficacy of Moxa extracts and smoke.

Animals↗

PubMedDate not supplied

Induction of anti-Escherichia coli activity in mice by phenothiazines, benzo[a]phenothiazines and benz[c]acridines.

The abilities of 14 phenothiazines, 8 benzo[a]phenothiazines and 12 benz[c]acridines to induce anti-Escherichia coli activity in mice were compared. Pretreatment with several benzo[a]phenothiazines or benz[c]acridines protected mice from lethal infection of Escherichia coli in a dose-dependent manner, whereas most of the phenothiazines induced much weaker anti-Escherichia coli activity. However, direct contact of Escherichia coli with these compounds or their administration just after bacterial inoculation were ineffective. These data suggest the immunopotentiation activity of benzo[a]phenothiazines and benz[c]acridines.

Acridines↗

PubMedDate not supplied

Effects of Catuaba extracts on microbial and HIV infection.

Pretreatment of mice with hot water and alkaline extracts of Catuaba casca (Erythroxylum catuaba Arr. Cam.) effectively protected them from lethal infection of Escherichia coli and Staphylococcus aureus. The extracts significantly inhibited both the human immunodeficiency virus (HIV)-induced cytopathic effect and the expression of HIV antigen in HIV-1HTLV-IIIB or HIV-2ROD infected human lymphotropic virus type I (HTLV-1) positive MT-4 cells. The 50% effective concentrations of the active fractions (21-263 micrograms/ml) were 1/4 - 1/43 of their 50% cytotoxic concentrations. Their anti-HIV activity was shown to be induced, at least in part, via the inhibition of HIV adsorption to the cells. The data suggest a medicinal potential of Catuaba extracts against opportunistic infection in HIV patients.

Animals↗

PubMedDate not supplied

Effect of pine seed shell extract on microbial and viral infection.

Pretreatment of mice with ammonia extract of seed shell of Pinus Koraicenis, via the intraperitoneal or intravenous route, effectively protected them from lethal infection of Escherichia coli, Klebsiella pneumoniae and Staphylococcus aureus. The pine seed shell extract also moderately inhibited syncytium formation and cytopathogenic effect induced by human immunodeficiency virus (HIV) infection in cultured human lymphotropic virus type I (HTLV-1) positive MT-4 cells. These data suggest a medicinal potential of pine seed shell extract against opportunistic infection in HIV patients.

Animals↗

PubMedDate not supplied

Stereoselective metabolism of carvedilol in the rat. Use of enantiomerically radiolabeled pseudoracemates.

14C-Labeled R(+)- and S(-)-carvedilol enantiomers were prepared by direct resolution of 14C-labeled racemic carvedilol on a chiral HPLC column. Two enantiomerically radiolabeled carvedilol pseudoracemates, 14C-labeled R(+)/unlabeled S(-)-carvedilol and 14C-labeled S(-)/unlabeled R(+)-carvedilol, were reconstituted and administered orally and iv to separate groups of bile duct-cannulated rats to determine the biliary excretion of carvedilol enantiomers and the stereochemical composition of metabolites excreted into the bile. The respective biliary excretions of the radioactivity derived from the radiolabeled R(+)- and S(-)-enantiomers accounted for 41.4 +/- 0.9 and 41.5 +/- 1.9% of the oral racemic dose, and 43.7 +/- 2.4 and 40.0 +/- 0.9% of the iv dose. Oral administration of these pseudoracemates produced no enantiomeric difference in the biliary excretion of the radioactivity derived from the enantiomers, whereas iv administration did result in an enantiomeric difference: the biliary excretion rate of the radioactivity derived from R(+)-enantiomer was higher than that from S(-)-enantiomer. After administration by the two routes, two carbazole ring-hydroxylated glucuronides, 1-hydroxycarvedilol O-glucuronide (1-OHCG) and 8-hydroxycarvedilol O-glucuronide (8-OHCG), were detected as the major metabolites in the bile. The S/R enantiomer ratios of 1-OHCG were 0.59 for oral dosing and 0.43 for iv dosing, suggesting that the formation of 1-OHCG is selective for R(+)-enantiomer, while the S/R ratios of 8-OHCG showed values of 3.29 and 2.63 for oral and iv administrations, respectively, favoring S(-)-enantiomer. Since corresponding hydroxylated metabolites are rapidly biotransformed to glucuronides that are excreted predominantly in the bile, the stereoselectivity of these glucuronides presumably reflects that of carbazole ring hydroxylation.

Administration, Oral↗

PubMedDate not supplied

Macrophage stimulation activity of antimicrobial N,N-dimethylaminoethyl paramylon.

Pretreatment with N,N-dimethylaminoethyl (DMAE) paramylon significantly protected mice from infection by various microorganisms. When mouse peritoneal macrophages were cultured with DMAE-paramylon, they showed morphological change (spreading) and elevated NBT-reducing activity. Macrophages prepared from DMAE-paramylon-treated mice had higher NBT-reducing activity than those from control mice. On the other hand, carboxymethyl paramylon and paramylon sulfate, which did not induce appreciable antimicrobial activity, failed to stimulate macrophage functions. The data suggest a significant role of macrophages in antimicrobial activity induction by cationized glucans.

Animals↗

PubMedDate not supplied

Surgical treatment of carcinoma of the esophagogastric junction.

Forty-seven patients with carcinomas of the esophagogastric junction were operated. In acquiring complete dissection of lymph nodes located at the splenic hilus and along the splenic artery, splenectomy with or without caudal hemipancreatectomy was performed in 29 of 47 patients. To avoid leaving carcinoma cells behind in the remaining esophagus margin of resection, 20 patients underwent left thoracophrenicolaparotomy and 14 patients received blunt dissection of the intrathoracic esophagus. Five-year survival of 55.6% was observed in curative groups of the present study. No operative mortality was present.

Adenocarcinoma↗

PubMedDate not supplied

Lignified materials as potential medicinal resources. II. Prevention of pathogenic bacterial infections in mice.

Antibacterial activity was demonstrated when ddY mice were intraperitoneally infected with E. coli or P. aeruginosa two days after a single ip-injection of a hot-water or alkaline extract obtained from lignified materials, such as chips of slash pine, Douglas fir, tallow wood, and two shelf fungi. Lignified material is a promising medicinal resource for the prevention and/or treatment of pathogenic microbial infection.

Animals↗

PubMedDate not supplied

Antimicrobial spectrum of lignin-related pine cone extracts of Pinus parviflora Sieb. et Zucc.

Pine cones of Pinus parviflora Sieb., et Zucc, were extracted successively with 5% NaHCO3, 3% NH4OH, 1% NaOH and 4% NaOH, and the extracts were tested for ability to induce antimicrobial activity in mice infected with Staphylococcal aureus. Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Candida albicans, or Salmonella enteritidis. These alkaline extracts were potent against the first 5 of these strains of microorganisms, and the activity was recovered mostly from their acid-precipitates at pH 5. After further fractionation on a Sephadex LH-60 column, the highest molecular weight fraction was most potent. Chemical structures in these bioactive fractions were assumed to be lignin-related structures, based on spectral data from UV, NMR and IR spectroscopy.

Anti-Bacterial Agents↗

PubMedDate not supplied

Chemical modification potentiates paramylon induction of antimicrobial activity.

Induction of antimicrobial activity by two water-insoluble polysaccharides, paramylon and TAK, was significantly potentiated by introduction of positively charged groups (such as N,N-dimethylaminoethyl; N,N-diethylaminoethyl; and 2-hydroxy-3-trimethylammoniopropyl), but not by introduction of negatively charged groups (such as carboxymethyl or sulfate). Cross-linking of these derivatives with epichlorohydrin did not increase their potentiating activity. The effects of these derivatives did not always correlate with their ability to accumulate polymorphonuclear cells and to stimulate the generation of luminol-dependent chemiluminescence by peritoneal exudate cells.

Animals↗

PubMedDate not supplied

Induction of antimicrobial activity by antitumor substances from pine cone extract of Pinus parviflora Sieb. et Zucc.

Pretreatment with two distinct antitumor substances extracted from pine cone of Pinus parviflora Sieb. et Zucc. protected mice from the lethal effects of E. coli infection. Intraperitoneal administration of these fractions transiently induced differentiation-inducing factor (DIF) with a peak at 1-2hr. The rapid decay of DIF activity from the peritoneal cavity was followed by polymorphonuclear cell (PMN) accumulation and enhancement of superoxide generation (assayed with luminol-dependent chemiluminescence (LDCL] by peritoneal exudate cells. The superoxide generation by adherent cells was similarly enhanced by pretreatment, but was only 10-20% of that of the peritoneal exudate cells. Fractions that showed comparable antitumor/antimicrobial activity were also obtained from seed shells and cones of other pine trees of Japanese and foreign origin. On the other hand, a neutral polysaccharide fraction from Pinus parviflora Sieb. et Zucc. that lacked any of these activities did not induce PMN accumulation, DIF activity or LDCL generation. The results suggest a significant role in PMN activation for the expression of antimicrobial activity induced by pine cone extracts.

Animals↗

PubMedDate not supplied

Cranberry juice and its impact on peri-stomal skin conditions for urostomy patients.

In urostomy patients, peristomal skin problems are common and may stem from alkaline urine. Cranberry juice appears to acidify urine and has bacteriostatic properties, and is widely recommended for the reduction of urinary tract infections. Therefore, it is hypothesized that drinking cranberry juice might also prevent and/or improve skin complications for urostomy patients. To test this hypothesis, pH measurements of the skin around the stoma and of the urine of 13 urostomy patients were taken before and after instituting a regimen of drinking 160 to 320 g of cranberry juice each day for an average period of six months. Results showed an improvement in skin condition from 6 patients with erythema, maceration or pseudoepithelial hyperplasia at the beginning of the study to 2 patients with maceration or PEH. The average pH of the urine taken from the patients' pouches decreased a statistically significant amount from 8.0 to 7.3 (p = 0.0277), yet unexpectantly, the average pH of the fresh urine increased a statistically significant amount from 5.8 to 6.2 (p = 0.0178). Other results were not statistically significant. The authors conclude that while drinking cranberry juice did not appear to acidify the urine as expected, improvements were still seen in the skin conditions of the study participants, suggesting that drinking cranberry juice does positively impact the incidence of skin complications for these patients.

Aged↗

PubMedDate not supplied

Oxidation of R(+)- and S(-)-carvedilol by rat liver microsomes. Evidence for stereoselective oxidation and characterization of the cytochrome P450 isozymes involved.

Incubation of R(+)- and S(-)-carvedilol with rat liver microsomes showed the formation of four oxidative metabolites: 1-hydroxycarvedilol (1-OHC), 8-hydroxycarvedilol (8-OHC), 4'-hydroxycarvedilol (4'-OHC), and O-desmethylcarvedilol (DesC). The structures of these metabolites were confirmed by cochromatography with the authentic metabolites and by thermospray ms. As expected from in vivo metabolism studies, 1-OHC and 8-OHC were the major products for both enantioners used as a substrate. The S/R enantiomeric ratios for intrinsic clearance (Vmax/KM) of 1-OHC, 8-OHC, DesC, and 4'-OHC were 0.40, 1.99, 0.77, and 2.71, respectively, showing that stereoselective oxidation occurs in this species. These findings strongly suggest that the stereoselective biliary excretion of the two major carbazole ring-hydroxylated glucuronides, 1-hydroxycarvedilol O-glucuronide, and 8-hydroxycarvedilol O-glucuronide observed previously in rats can be explained by stereoselective hydroxylation in liver. The cause of the difference in intrinsic clearance for 1-OHC and 8-OHC between the two enantiomers was based on the difference in affinity to the catalyzing enzyme. The main enzyme concerned in the 1- and 8-hydroxylation of both enantiomers is considered to be CYP2D1 from the following observation: the marked strain differences between Sprague-Dawley and Dark Agouti rats and competitive inhibition by quinine. In the O-demethylation of both enantiomers, CYP2C11 is probably the major catalyzing enzyme, because sex differences, but no strain difference, were observed in both Sprague-Dawley and Dark Agouti rats, and also anti-CYP2C11 strongly inhibited this demethylation.

Adrenergic beta-Antagonists↗

PubMedDate not supplied

Induction of a protective immunity in mice against Escherichia coli by phenothiazines, 10-[n-(phthalimido)alkyl]-2-substituted-10H-phenothiazines and 1-(2-chloroethyl)-3-(2-substituted-10H-phenothiazines-10-yl)alkyl-1 -ureas .

Abilities of five phenothiazines, six 10-[n-(phthalimido)alkyl]-2-substituted-10H-phenothiazines and six 1-(2-chloroethyl)-3-(2-substituted-10H-phenothiazines-10-yl)alkyl-1- ureas to induce anti-Escherichia coli activity in mice were compared. Seventeen compounds tested in this study had no antibacterial effect in direct contact with Escherichia coli using the disk diffusion method except chlorpromazine (4) with low growth inhibitory action. The pretreatment of mice with several phenothiazines, 10-[n-(phthalimido)alkyl]-2-substituted-10H-phenothiazines or 1-(2-chloroethyl)-3-(2-substituted-10H-phenothiazines-10-yl)alkyl-1- ureas protected the animals from lethal infection of Escherichia coli to various extents. On the basis of these experiments, we assume that the protective effect against Escherichia coli infection might be due to the immunopotentiation or macrophage inducing activity by the compounds, or inactivation of lymphokines induced by the bacteria. Since the infection preventing effect of the tested phenothiazines depends on the chemical structures, the specificity of the biological process can be assumed.

Animals↗

PubMedDate not supplied

Radical modulation activity of lignins from a mangrove plant, Ceriops decandra (Griff.) Ding Hou.

The radical modulation activity of hot water and alkaline extracts from leaf of Ceriops decandra, a mangrove plant, was investigated using ESR spectroscopy. IR and NMR analyses demonstrate that the leaf extracts have a lignin-like polyphenolic structure. All these extracts produced radical(s) under alkaline conditions. The radical intensity of sodium ascorbate was slightly reduced at lower concentrations of the extracts, but it was synergistically enhanced at higher concentrations. All the extracts effectively scavenged superoxide anion, produced by hypoxanthine-xanthine oxidase reaction. Pretreatment of mice with the extracts significantly protected them from the lethal infection by E. coli. Similar activity was found in lignins from pine seed shell of Pinus parviflora Sieb. et Zucc. These data further support the medicinal efficacy of plant extracts.

Animals↗