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At least 613 records · Page 34Linked to original sources
PubMed2004

Transmission electron microscopy of Schistosoma mansoni cercariae treated with hinokitiol (beta-thujaplicin), a compound for potential skin application against cercarial penetration.

Since skin is the only route of entry of the parasite in schistosomiasis patients, intervention at the level of skin penetration should control the infection. Several compounds were screened for their ability to protect against cercarial penetration. Hinokitiol (beta-thujaplicin) was found to have a significant cercaricidal effect in vitro, although there is no information on its cercaricidal mechanisms. To study the kinetics of morphological changes in Schistosoma mansoni associated with exposure to hinokitiol in vitro, cercariae were incubated in media containing hinokitiol at different concentrations and examined by transmission electron microscopy (TEM). TEM revealed that ultrastructural changes occurred by 15 minutes post exposure, at a concentration of 25 microg/ml. Degenerative changes involving both tegument and deeper parenchymal structures were progressive with duration of exposure at the concentration of 50 microg/ml. These structural changes may account for the inability of hinokitiol-treated cercariae to infect the host.

Animals↗
PubMed2006

Lack of hinokitiol (beta-thujaplicin) carcinogenicity in F344/DuCrj rats.

Chronic toxicity and carcinogenicity of hinokitiol (beta-thujaplicin), used as an antibiotic and fungicidal agent of a food additive, was examined in both sexes of F344/DuCrj (F344) rats. In this chronic toxicity study, groups of 10 rats of each sex were given a diet containing hinokitiol at doses of 0, 0.005, 0.015 and 0.05% for 52 weeks. No treatment-related adverse effects were noted in the survival rate, general condition, body weights, food consumption, urinalysis, hematology and clinical chemistry. Slight but significant elevation of spleen and liver weights was noted in both sexes given 0.05% hinokitiol, along with an increase in hemosiderin deposits in male spleens, related to chelator binding of iron, together with slight centrilobular hypertrophy of male hepatocytes. However, these alterations were negligible and not toxicologically significant. In the carcinogenicity study, groups of 50 female and 50 male rats were given a diet containing hinokitiol at doses of 0, 0.005, 0.015 and 0.05% (excluding 0.005% in females). No treatment-related changes in survival rate, general condition, body weight, food consumption, hematology and organ weights were noted. Detailed histopathological examination revealed no treatment-related increase in the incidences of any neoplastic lesions. The results demonstrate that hinokitiol is not carcinogenic in F344 rats of either sex.

Animals↗
PubMed2005

Mosquito larvicidal activity of active constituent derived from Chamaecyparis obtusa leaves against 3 mosquito species.

Mosqutio larvicidal activity of Chamaecyparis obtusa leaf-derived materials against the 4th-stage larvae of Aedes aegypti (L.), Ochlerotatus togoi (Theobald), and Culex pipiens pallens (Coquillett) was examined in the laboratory. A crude methanol extract of C. obtusa leaves was found to be active (percent mortality rough) against the 3 species larvae; the hexane fraction of the methanol extract showed a strong larvicidal activity (100% mortality) at 100 ppm. The bioactive component in the C. obtusa leaf extract was characterized as beta-thujaplicin by spectroscopic analyses. The LC50 value of beta-thujaplicin was 2.91, 2.60, and 1.33 ppm against Ae. aegypti, Oc. togoi, and Cx. pipiens pallens larvae. This naturally occurring C. obtusa leaves-derived compound merits further study as a potential mosquito larval control agent or lead compound.

Aedes↗
PubMed1991

Radionuclide detection of occult infection: current strategies.

A number of new radionuclide techniques are available for diagnosing infection. These include the radiolabeling of neutrophils and lymphocytes with a variety of chelating agents and isotopes, and the use of antibodies directed against bacteria in the inflammatory exudate. Other new techniques include radiolabeled nanocolloids, chemotactic peptides, and liposomes. This article reviews the evolving role of these techniques in the detection of sites of occult infection.

Animals↗
PubMed2006

The excellence of Aomori Hiba (Hinokiasunaro) in its use as building materials of Buddhist temples and Shinto shrines.

Five hinokitiol-related compounds (hinokitiol (beta-thujaplicin), beta-dolabrin, gamma-thujaplicin, 4-acetyltropolone and alpha -thujaplicin) isolated from the acid oil of Aomori Hiba (Thujopsis dolabrata Sieb. et Zucc. var hondai MAKINO) showed clear antifungal activity against wood-rotting fungi. These compounds have obvious insecticidal effects on termites. They also exhibited potent acaricidal activity against mites. The above-mentioned features suggest that Konjiki-do, a well known national treasure, one of the buildings in Chuson-ji Temple of Iwate Prefecture, Japan, which was built of wood from the tree containing these five compounds, was kept from harm against noxious insects and wood-rotting fungi for a long time of about 840 years, until it was extensively repaired in 1962. In addition to Konjiki-do, there are some old famous Buddhist temples and Shinto shrines using Aomori Hiba. From the results, it was found that Aomori Hiba (Hinokiasunaro) is excellent for use as building materials.

Buddhism↗
PubMed1982

Synthesis and characterization of a novel inhibitor of an aminoglycoside-inactivating enzyme.

A novel low-molecular weight inhibitor of an aminoglycoside-inactivating enzyme, initially isolated from fermentation broths of Streptomyces neyagawaensis, was determined to be 7-hydroxytropolone. Its structure was confirmed by synthesis. In vitro synergy was demonstrated between 7-hydroxytropolone and certain aminoglycosides against bacteria which were resistant to those aminoglycosides by virtue of a 2"-O-adenylyltransferase. The synthesis and characterization of some analogs of 7-hydroxytropolone is also described.

Anti-Bacterial Agents↗
PubMed1986

Studies on lipoxygenase inhibitors. I. MY3-469 (3-methoxytropolone), a potent and selective inhibitor of 12-lipoxygenase, produced by Streptoverticillium hadanonense KY11449.

Streptoverticillium hadanonense KY11449 was found to produce a 12-lipoxygenase inhibitor MY3-469. The compound was purified by chromatography on Diaion HP-10, charcoal, Sephadex LH-20 and crystallization. The chemical structure of MY3-469 was determined to be 3-methoxytropolone on the basis of its physico-chemical properties. The half maximal inhibitory concentration (IC50) of MY3-469 against bovine platelet 12-lipoxygenase was 1.8 X 10(-6)M. The compound did not inhibit bovine platelet cyclooxygenase at 10(-3)M and showed weak inhibition (IC50 2.8 X 10(-4)) against 5-lipoxygenase of rat basophilic leukemia cells. The results indicate that MY3-469 is a potent and selective inhibitor of 12-lipoxygenase.

Actinomycetales↗
PubMed1988

BMY-28438 (3,7-dihydroxytropolone), a new antitumor antibiotic active against B16 melanoma. I. Production, isolation, structure and biological activity.

A new antitumor antibiotic BMY-28438 was isolated from the cultured broth of Streptomyces tropolofaciens No. K611-97. The antibiotic showed potent cytotoxicity against cultured B16 melanoma cells and remarkable prolongation of life span of mice bearing B16 melanoma. The structure of BMY-28438 was determined as 3,7-dihydroxytropolone on the basis of spectral analyses and direct comparison with the authentic compound synthesized.

Animals↗
PubMed1993

Eupenifeldin, a novel cytotoxic bistropolone from Eupenicillium brefeldianum.

Eupenifeldin was isolated from cultures of Eupenicillium brefeldianum ATCC 74184 by extraction and crystallization. The compound was identified as a pentacyclic bistropolone on the basis of spectral data and its complete structure was established by single-crystal X-ray analysis. The compound is cytotoxic against the HCT-116 cell line and has in vivo antitumor activity in the P388 leukemia model.

Animals↗
PubMed2003

[Antimicrobial activity of hinokitiol against Legionella pneumophila].

Antimicrobial activity of hinokitiol (beta-thujaplicin), which is a major component of the essential oil of Chamaecyparis obtuse, against Legionella pneumophila was investigated experimentally. The quantitative antibacterial assay of hinokitiol was carried out by the disk-diffusion method. The test concentrations of hinokitiol were 0.39 to 25.0 micrograms/disk, and the lowest concentrations of hinokitiol that showed growth inhibition against L. pneumophila were 1.56 micrograms/disk on B-SYE agar and 0.39 microgram/disk on B-SYE agar without iron.

Anti-Bacterial Agents↗
PubMed1999

Induction of apoptosis by hinokitiol, a potent iron chelator, in teratocarcinoma F9 cells is mediated through the activation of caspase-3.

Hinokitiol, a potent iron chelator, has been reported to induce differentiation in teratocarcinoma F9 cells with a reduction of viable cells. In this study, we examined the steps leading to eventual cell death by hinokitiol during differentiation. Hinokitiol induced DNA fragmentation of F9 cells in a concentration- and time-dependent manner. This effect was also observed in a cell-free system using the nuclei from intact cells and the cytosols from hinokitiol-treated cells. In contrast, hinokitiol methyl ether and hinokitiol-Fe (III) complex, which are deficient in iron-chelating activity, showed no DNA fragmentation activity in both cell culture and cell-free systems. These results suggest that iron deprivation by hinokitiol may be involved in the induction of apoptosis of F9 cells. Caspase-3, one of the key enzymes in the apoptotic cascade, was specifically activated by hinokitiol treatment, but not by the other two derivatives. In addition, its specific inhibitor, benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone, strongly blocked hinokitiol-induced DNA fragmentation. These results indicate that iron deprivation by hinokitiol can induce apoptosis of F9 cells through the activation of caspase-3.

Amino Acid Chloromethyl Ketones↗
PubMedDate not supplied

[Effect of the novel aminoadamantane derivative A-7 on Parkinsonian syndrome induced by systemic administration of neurotoxin MPTP].

A new antiparkinsonian drug, N-(2-adamantyl)hexamethyleneimine hydrochloride (A-7), was studied on the model of parkinsonism syndrome (PS) induced by MPTP neurotoxin. A-7 (5-20 mg/kg) attenuated the MPTP induced akinesia and rigidity manifestations in C57B1/6 mice, the effect being more pronounced than that of cyclodol and levodopa and comparable to that of midantane (amantadine). A-7 also decreased the PS manifestations in rats: removed tremor, rigidity, and oligokinesia, normalized the MPTP-violated bioelectrical activity of nucleus caudatus, sensomotor cortex, and dorsal hippocamp, and eliminated pathologic slow activity, paroxysmal discharges, and high-frequency activity discharges. The activity of A-7 exceeded that of levodopa (enhancing tremor) and cyclodol (not eliminating the pathologic slow activity).

Amantadine↗
PubMed2002

Diagnostic value of (111)In-granulocyte scintigraphy in patients with fever of unknown origin.

UNLABELLED: 111In-granulocyte scintigraphy is often used as a diagnostic tool in patients with fever of unknown origin (FUO). However, its diagnostic performance has been studied in only a limited number of investigations, with most having been published more than 10 y ago; in addition, a broad range of sensitivities and specificities has been reported. Therefore, the aim of this study was to investigate the diagnostic value of granulocyte scintigraphy in patients fulfilling the criteria of FUO. Also studied was whether increased peripheral leukocyte count or C-reactive protein (CRP) level could be used to select patients for scintigraphy to raise the diagnostic value. METHODS: For 31 patients with true FUO who underwent granulocyte scintigraphy at a third-line referral hospital between 1995 and 2000, the files and scintigraphy findings were reviewed retrospectively to test the ability of scintigraphy to identify infection or chronic inflammatory bowel disease as the cause of FUO. In addition, leukocyte counts and CRP values were recorded. RESULTS: Scintigrams were true-positive in 6 cases, false-positive in 4 cases, true-negative in 19 cases, and false-negative in 2 cases. Sensitivity was 75%, specificity was 83%, the predictive value of a scintigram showing positive findings was 60%, and the predictive value of a scintigram showing negative findings was 90%. Leukocyte counts did not differ between patients with true-positive and true-negative scintigrams. In contrast, CRP was elevated in all patients with true-positive scintigrams but in only half the patients with true-negative scintigrams. However, if only patients with elevated CRP were used for calculation of test performance, the test performance was not improved. CONCLUSION: (111)In-granulocyte scintigraphy seems to have a reasonable sensitivity and specificity in cases of FUO, when one takes into account that (111)In-granulocyte scintigraphy is not a first-line test. The high predictive value of a scintigram showing negative findings may be especially valuable for ruling out an infectious cause of FUO. Neither peripheral leukocyte count nor CRP levels seem useful for selection of patients on whom scintigraphy should be performed.

Adolescent↗