N,N-Didesmethylgrossularine-1 (DDMG-1), a compound with a rare alpha-carboline structure, was isolated from an Indonesian ascidian Polycarpa aurata as responsible for the observed inhibitory activity against TNF-alpha production in lipopolysaccharide-stimulated murine macrophage-like RAW264.7 cells. DDMG-1 inhibited the mRNA level of mTNF-alpha, IkappaB-alpha degradation, and binding of NF-kappaB to the target DNA site in LPS-stimulated RAW 264.
View Article and Find Full Text PDFEight sesquiterpene quinones: ilimaquinone (1), smenospongidine (3), smenospongiarine (5), smenospongine (7), and their corresponding 5-epimers 2, 4, 6, and 8, isolated from the Palauan marine sponge Hippospongia sp., were examined regarding their effects on TNF-α production in LPS-stimulated RAW 264.7 cells.
View Article and Find Full Text PDFWe have recently isolated four new melophlins P (1), Q (2), R (3), and S (4) together with seven known melophlins A (5), D (6), E (7), G (8), H (9), I (10), and O (11) from two marine sponges of the genus Melophlus collected in Palau. In this study, the influence of these compounds on the colony formation of Chinese hamster V79 cells and the production of IL-8 in PMA-stimulated HL-60 cells were examined. These 11 compounds did not show any effect on IL-8 production.
View Article and Find Full Text PDFThree new sesquiterpenes, 2-deoxy-7-O-methyllemnacarnol (1), 2-deoxy-12 alpha-ethoxy-7-O-methyllemnacarnol (2), and 2-deoxy-12 alpha-methoxy-7-O-methyllemnacarnol (3), were isolated from a soft coral Nephthea sp. collected in Indonesia, together with five known sesquiterpenes. The structures of the new compounds were assigned on the basis of their spectroscopic data.
View Article and Find Full Text PDFFour new polysulfur aromatic alkaloids, lissoclibadins 4 (1), 5 (2), 6 (3), and 7 (4), were isolated from the ascidian Lissoclinum cf. badium collected in Indonesia, together with seven known alkaloids, lissoclibadins 1 (5), 2 (6), and 3 (7), lissoclinotoxins E (8) and F (9), 3,4-dimethoxy-6-(2'-N,N-dimethylaminoethyl)-5-(methylthio)benzotrithiane (10), and N,N-dimethyl-5-(methylthio)varacin (11). Compounds 1-11 were isolated from the ascidian collected in March (wet season), while 5-11 have been obtained previously from the organism collected in September (dry season) at the same site.
View Article and Find Full Text PDFThe in vitro growth inhibitory activity of lissoclibadins and lissoclinotoxins isolated from the tropical ascidian Lissoclinum cf. badium against nine human cancer cell lines was examined to evaluate their potential anticancer efficacy. Lissoclibadins 1 (1) and 2 (2), and lissoclinotoxin F (4) showed the strongest activity of the six compounds tested, which were more potent than the anticancer drug cisplatin.
View Article and Find Full Text PDFThree new macrocyclic trichothecenes, named 12'-hydroxyroridin E (1), roridin Q (2), and 2',3'deoxyroritoxin D (3), were isolated from the marine-derived fungus Myrothecium roridum TUF 98F42, and a new macrocyclic trichothecene, named roridin R (4), was isolated from Myrothecium sp. TUF 02F6 together with roridins A and H and isororidin E. The structures of new compounds were determined on the basis of their spectral data.
View Article and Find Full Text PDFJ Antibiot (Tokyo)
February 2006
Griseofulvin may combine with tubulin as a component of microtubules and, at high doses, inhibits microtubule formation in mammalian cells. In this study, the author examined the effects of three various 2'-substitutive derivatives of griseofulvin on microtubule distribution in Chinese hamster V79 cells. The results showed that 2'-demethoxy-2'propoxygriseofulvin was the strongest inhibitor of a normal cytoplasmic microtubule network, unlike findings in previous in-vitro studies.
View Article and Find Full Text PDFThe biosynthetic origin of the C-12 methyl group in homoanatoxin-a (1) was identified by the feeding experiment of L-[methyl-13C]-methionine in the culture of the cyanobacterium Raphidiopsis mediterranea Skuja strain LBRI 48. Remarkably high incorporation (80%) of 13C was observed at C-12. The in vivo enzymatic transformation of 1 was also examined by the prolonged culture of strain LBRI 48.
View Article and Find Full Text PDFA neurotoxin, homoanatoxin-a, was identified from a toxic strain of the cyanobacterium Raphidiopsis mediterranea Skuja (strain LBRI 48) isolated from Lake Biwa, Japan, as the major toxin component (0.57% of dry cell-weight). This cyanobacterium produced anatoxin-a and a new homoanatoxin-a derivative as minor components (0.
View Article and Find Full Text PDFWe examined the effects of (+/-)-indenestrol A (IA), an antioxidative and superoxide-producing metabolite of diethylstilbestrol (DES), on the activation of murine macrophages (RAW 264.7 cells) in vitro, particularly with regard to interferon (IFN)-gamma-induced nitric oxide (NO) production. (+/-)-IA inhibited NO production more strongly than DES as assessed by a nitrite assay.
View Article and Find Full Text PDFPreviously, we reported that (+/-)-IA but not DES produces O2- spontaneously in PBS. We are interested in the possibility that these compounds might produce active oxygen species under mild cell culture conditions. On incubation of RAW 264.
View Article and Find Full Text PDFAlprazolam is a hypnotic/tranquilizer that has been shown to specifically inhibit the platelet-activating factor (PAF)-induced aggregation of human platelets. The goal of this study was to elucidate whether alprazolam modulates IL-1alpha-initiated responses. For this purpose we investigated the effects of alprazolam on the IL-1alpha-induced production of inflammatory cytokines (IL-8 and monocyte chemoattractant protein 1 (MCP-1)) in a human glioblastoma cell line, T98G, and explored the signaling pathways involved.
View Article and Find Full Text PDFRecently, we investigated the inhibitory effects of 17 beta-estradiol and diethylstilbestrol on microtubule assembly, cytotoxicity, and aneuploidy in V79 cells. The present study analyzes the effects of equilin and equilenin (amongst the natural estrogens originally isolated from the urine of pregnant horses) and their related compounds, on the relative plating efficiency of Chinese hamster V79 cells. The results showed that a hydroxyl group on 17-C and a methoxyl group on 3-C of the estrogen skeleton were important for cytotoxicity.
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