Efficient chemical conversion of louisianin A to C and D, the inhibitor of angiogenesis.
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Allyl Compounds↗
Biomedical subjects
K Komiyama
Publications and source records attributed to K Komiyama.
Pyridindolols K1 and K2, new alkaloids from Streptomyces sp. K93-0711
Two new alkaloids with the beta-carboline skeleton, pyridindolols K1 (C18H18N2O5) and K2 (C16H16N2O4), were isolated from the culture broth of Streptomyces sp. K93-0711. The structure of pyridindolols were established by spectroscopic investigations and chemical transformations. Pyridindolol K2 inhibited the adhesion of HL-60 cells to LPS-activated HUVEC monolayer (IC50 = 75 micrograms/ml).
Journal Article↗
The effect of adriamycin against a liver metastatic model by encapsulation in liposomes.
Antitumor activities of liposomes containing adriamycin (L-ADM) and their distribution process into tumour cells were analysed. The lipid composition of the liposomes was dimyristoylphosphatidylglycerol (DMPG)/egg phosphatidylcholine/cholesterol/adriamycin (ADM) in a molar ratio of 11.4:2:12:1.3. Liver-metastasizing murine tumour models, M5076 and L5178Y-ML, were used. In vivo antitumour effect against these tumour models was assessed from increase in life span (ILS). The survival prolongation effect of L-ADM in mice with liver failure caused by M5076 was significantly higher than that of F-ADM. In contrast, significant enhancement of the effects by encapsulation in liposomes was not observed in L5178Y-ML-bearing mice. In vitro cytostatic activities of L-ADM against M5076 cells as well as against other tumour cell lines were lower than those of F-ADM. The in vitro kinetic study on the distribution of L-ADM to the tumour cells revealed that ADM in L-ADM was taken up into the tumour cells mainly after it was released from the liposomes rather than taken up as the liposomal form. Among the cell lines tested, M5076 cells had the highest phagocytic activity and therefore the highest uptake activity of ADM during incubation with L-ADM. These findings suggest that the augmented antitumour activity of L-ADM in M5076-bearing mice was the result of phagocytosis of L-ADM by M5076 cells as well as the reduction of toxicity, prolonged retention of ADM in systemic circulation, and liver accumulation of ADM after administration of L-ADM.
Animals↗
Madindoline, a novel inhibitor of IL-6 activity from Streptomyces sp. K93-0711. I. Taxonomy, fermentation, isolation and biological activities.
Selective growth inhibition against IL-6-dependent cells was detected in fermentation extracts of a microbial strain, K93-0711, which was characterized as Streptomyces species. Active metabolite, termed madindoline A and B, were isolated, and the structure was determined to be 3a-hydroxy-indoline with diketocyclopentene at the N position. Madindoline A and B displayed dose-dependent inhibition of MH60 cells, an IL-6-dependent cell line, in presence of 0.1 U/ml IL-6. The IC50 for madindoline A and B against this cell line was 8 microM and 30 microM, respectively. These compounds did not inhibit the growth of cell lines which are not IL-6 dependent and the growth inhibition of the MH60 cell line was reversed by addition of excess, 0.4 U/ml, of IL-6 to the culture media. These compounds did not show any antimicrobial activity at a concentration of 1,000 micrograms/ml.
Bridged Bicyclo Compounds, Heterocyclic↗
A new inhibitor of melanogenesis, albocycline K3, produced by Streptomyces sp. OH-3984.
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Anti-Bacterial Agents↗
Chlovalicin, a new cytocidal antibiotic produced by Sporothrix sp. FO-4649. I. Taxonomy, fermentation, isolation and biological activities.
Selective growth inhibition against IL-6 dependent cells was detected in fermentation extracts of a fungal strain FO-4649 which was characterized as Sporothrix species. An active metabolite (1) termed chlovalicin was isolated together with ovalicin and two other ovalicin derivatives (compounds 3 and 4). Chlovalicin, a ovalicin derivative with a chlorinated methylene moiety at the C-1 position of the cyclohexane ring, dose-dependently inhibited the growth of IL-6 dependent MH60 cells (IC50, 7.5 microM) in the presence of 0.2 U/ml IL-6 and, to a lesser extent, the growth of B16 melanoma cells (IC50, 38 microM). Among the other three compounds, only ovalicin showed inhibitory activity (IC50, 27 microM) against MH60 cells. These four compounds did not show any antimicrobial activity at a concentration of 1000 micrograms/ml.
Animals↗
Chlovalicin, a new cytocidal antibiotic produced by Sporothrix sp. FO-4649. II. Physicochemical properties and structural elucidation.
A new growth inhibitor of IL-6 responsive MH60 cells, chlovalicin (MW; 332, C16H25O5Cl), was found in cultures of Sporothrix sp. FO-4649, together with a known sesquiterpene, ovalicin. The structure of chlovalicin was elucidated by spectroscopic methods. Chlovalicin possesses a chlorinated methylene moiety at the C-1 position, and it corresponds to halogenated products derived from the epoxide ring attached to the C-1 position of ovalicin. The absolute configuration of chlovalicin was clarified as 1S, 2R, 3S, 1'S, 2'R by chemical transformation from ovalicin.
Anti-Bacterial Agents↗
Macrosphelide, a novel inhibitor of cell-cell adhesion molecule. II. Physiochemical properties and structural elucidation.
New anticell-adherence compounds, macrosphelides A and B, were isolated from the fermentation broth of Microsphaeropis sp. FO-5050, and their structures were elucidated by spectroscopic methods and chemical transformations. Macrosphelides A (M.W. 342, C16H22O8) and B (M.W. 340, C16H20O8) with three esters in their molecules were classified as 16-membered macrocyclic compounds. Macrosphelide B was found to be a corresponding oxidative product of macrosphelide A at the C-14 position.
Anti-Bacterial Agents↗
[Molecular aspects of secretory IgA (S-IgA) in gut-associated lymphoid tissues].
Secretory IgA, which plays an important role in the defense of the exocrine tissue, is composed of a polymeric IgA, joining (J) chain and secretory component (SC). Polymeric IgA and J chain are produced by plasma cells and SC by glandular epithelial cells. We here described the molecular aspects of J chain and SC. Study of the J chain has been confined to vertebrates which produce immunoglobulin (Ig) because the function of J chain is considered to be a polymerization of Ig. Recent molecular studies indicate that the role of J chain has been questioned. The J chain is expressed in invertebrates, as well as, representative species of vertebrates and that J chain is a primitive polypeptide that arose before the evolution of Ig molecules. SC is a 80 kDa glycoprotein functioning as a receptor for J chain-containing polymeric Ig. The expression of SC is regulated by various inflammatory cytokines such as, IL-1, IL-4, IL-6, IL-8, IFN-gamma and TNF-alpha, suggesting SC upregulation in vivo in inflammatory conditions. The human SC cDNA analysis reveals that it consisted of 11 exons with no functional TATA-box or CCAAT-box in the putative promoter region. Further upstream, there are several interesting motifs such as NF-kB and IFN-gamma response element, suggesting possible regulation of SC by cytokines through cellular signal transduction pathways.
Animals↗
Louisianins A, B, C and D: non-steroidal growth inhibitors of testosterone-responsive SC 115 cells. I. Taxonomy, fermentation, isolation and biological characteristics.
In the course of screening for non-steroidal growth inhibitors of testosterone-responsive Shionogi carcinoma 115 cells, louisianins A, B, C and D, were isolated from fermentation broth of Streptomyces sp. WK-4028. Louisianin A remarkably inhibited the growth of SC 115 cells in the presence of 10(-7) M testosterone at an IC50 value of 0.6 microgram/ml, whereas, no inhibition was observed on the other cell lines. Furthermore, inhibitory activity of testosterone 5 alpha-reductase and antimicrobial activity have not been observed at a concentration of 50 micrograms/ml and 1,000 micrograms/ml, respectively.
5-alpha Reductase Inhibitors↗
Louisianins A, B, C and D: non-steroidal growth inhibitors of testosterone-responsive SC 115 cells. II. Physico-chemical properties and structural elucidation.
New non-steroidal growth inhibitors of testosterone-responsive SC 115 cells, louisianins A (MW: 189; C11H11NO2), B (MW: 191; C11H13NO2), C (MW: 173; C11H11NO) and D (MW: 173; C11H11NO) were isolated from the cultured broth of Streptomyces sp. WK-4028. Their structures were determined on the basis of spectroscopic data. The structure of louisianin A in particular was confirmed by X-ray crystallographic analysis. The four compounds commonly possess a unique pyrindine skeleton in the molecule.
5-alpha Reductase Inhibitors↗
Phenopyrrozin, a new radical scavenger produced by Penicillium sp. FO-2047.
A new radical scavenger, named phenopyrrozin, was isolated from the culture broth of Penicillium sp. FO-2047. Phenopyrrozin was purified from whole broth solvent extraction, silica gel chromatography, and HPLC. The structure of phenopyrrozin was elucidated as 5,6,7,7a-tetrahydro-2-hydroxy-1-phenyl-3H-pyrrolizin-3-one. The IC50 of phenopyrrozin against lipid peroxidation induced by Cr2K2O7 was 73 micrograms/ml. Phenopyrrozin also reduced chromosomal aberrations induced by paraquat.
Animals↗
Macrosphelide, a novel inhibitor of cell-cell adhesion molecule. I. Taxonomy, fermentation, isolation and biological activities.
Potent anti-adherent activity was detected in fermentation extracts of microbial strain FO-5050. Active compounds designated macrosphelide A and B were isolated and the structure was determined to be 16-membered macrolide antibiotics possessing three ester bonds in the ring structure. Macrosphelide A dose-dependently inhibited the adhesion of HL-60 cells to LPS-activated HUVEC monolayer (IC50, 3.5 microM); macrophelide B also inhibited HL-60 adhesion but to a lesser extent (IL50, 36 microM). Macrosphelide A did not show any antimicrobial and cytocidal activities at the concentration of 1000 micrograms/ml and 100 micrograms/ml, respectively.
Anti-Bacterial Agents↗
Detection of hepatitis C virus (HCV)-RNA in saliva and gastric juice.
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Base Sequence↗
Antioxidative activity of tocotrienol in heterogeneous system: indication of restriction within membrane by fluorescence measurement.
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Antioxidants↗
Factors related to plaque distribution in a group of Canadian preschool children.
The purpose of this study was to identify factors that were related to plaque distribution in a group of preschool children. 153 children aged 3-5 years from seven randomly-selected preschool programmes in Saskatoon, Canada, were examined for plaque (Silness & Loe, 1964) and for dental caries (WHO, 1987). The subjects were divided into three groups according to age: 3, 4 and 5 years old. Plaque was assessed on the buccal and lingual surfaces of all teeth. The examinations were conducted in the morning or afternoon. No prior oral hygiene instructions were given to the children or parents. Teachers, however, were informed when the examinations would take place. The mean total plaque score was 0.51. There was no significant difference between the plaque scores for the different age groups. Total plaque score was significantly related to dft and dfs scores (P < 0.05). The mean dft was 0.68 and mean dfs was 1.18, and 80.4% of the subjects were caries-free and had no restored teeth or surfaces. There was significantly more plaque on posterior teeth than on anterior teeth (P < 0.0001), and on buccal surfaces than on lingual surfaces (P < 0.001) in both mandibular and maxillary arches. Significant differences in plaque distribution were also found between subjects examined in the morning or the afternoon.
Age Distribution↗
[Fluoroscopic contrast medium percutaneous ethanol injection therapy (FCM-PEIT): newly developed clinical useful method for injecting ethanol into nodules of hepatocellular carcinoma].
We have performed fluoroscopic contrast medium percutaneous ethanol injection therapy (FCM-PEIT) total 266 times to 82 hepatocellular carcinoma (HCC) nodules in 44 HCC cases: FCM-PEIT is the newly developed method that HCC nodules are punctured by a needle and injected with ethanol mixed with water-soluble contrast medium (Iopamidol containing 370 mg/ml iodine) (vol/vol: 7/3) under the fluoroscopic observation as well as ultrasonic diagnostic equipment (US). Autopsy analyses have demonstrated nearly complete tumor necrosis by FCM-PEIT. We analyzed the detectable rate (%) of the contrast medium-mixed ethanol (CME) leakage out of HCC nodules by US-alone, fluoroscope-alone, and US-fluoroscope observation. The detectable rate of the leakage was 63% by US-fluoroscope, while was only 32% by US-alone. Particularly, all leakages into intra hepatic bile duct were missed by US-alone. The maximal CME-amount for injection without any leakage was not uniform and not related to the size of HCC nodules. The present results suggest that FCM-PEIT is clinically more useful method for the treatment of HCC compared to general PEIT that HCC nodules are injected with ethanol under the US-alone observation, since it is easy to confirm whether ethanol can be sufficiently injected into HCC nodules without any leakage.
Carcinoma, Hepatocellular↗
Role of cations and IgA in saliva-mediated aggregation of Pseudomonas aeruginosa in cystic fibrosis patients.
Oral colonization by Pseudomonas aeruginosa possibly precedes the pulmonary infection process in cystic fibrosis (CF) patients. As bacterial aggregates may play a role in establishment of pulmonary infections, involvement of IgA and cations in CF patient saliva-mediated aggregation of P. aeruginosa was investigated. For colonized patients, P. aeruginosa aggregation correlated with bacterial-specific and total salivary IgA. Cation or IgA depletion reduced P. aeruginosa aggregation by saliva from all patients. However, if cations were removed before IgA, and saliva was then reconstituted with calcium, only colonized patient saliva showed reduced aggregation. Aggregation by IgA-depleted saliva was augmented by reconstituting with original IgA. CF patient saliva-mediated aggregation of P. aeruginosa thus is cation-dependent and enhanced by bacterial-specific IgA. Characterizing the interactions among bacterial aggregating factor(s), cations, and antibodies in CF saliva will help clarify the link between P. aeruginosa oral colonization and pulmonary infections in CF patients.
Adolescent↗