Dykellic acid inhibits cell migration and tube formation by RhoA-GTP expression.

Dykellic acid, a novel factor initially identified from the culture broth of Westerdykella multispora F50733, has been shown to inhibit matrix metalloprotease 9 activity, caspase-3 activity, B cell proliferation and LPS-induced IgM production, suggesting that this factor may have anti-cancer effects. In an effort to further address the possible anti-tumoral effects of dykellic acid, we used wound healing, invasion and RhoA-GTP assays to examine the effects of dykellic acid on cell migration, invasion and angiogenesis. Our results revealed that dykellic acid dose-dependently inhibits B16 cell migration and motility, and inhibits HUVEC tube formation.

Gelastatins and their hydroxamates as dual functional inhibitors for TNF-alpha converting enzyme and matrix metalloproteinases: synthesis, biological evaluation, and mechanism studies.

The hydroxamic acid analogues (2) of the natural product gelastatins (1) were prepared by 1 step conversion reaction. The synthetic analogues (2) showed potent enzymatic inhibitory activities against MMP-2, MMP-9, and TACE IC50's of 6, 23, and 28 nM, respectively. In addition, 2 were able to inhibit TNF-alpha production effectively in mice as well as in a macrophage cell line, RAW 264.

Tungtungmadic acid, a novel antioxidant, from Salicornia herbacea.

Tungtungmadic acid (3-caffeoyl-4-dihydrocaffeoyl quinic acid) is a new chlorogenic acid derivative that was isolated from the Salicornia herbacea. The structure of tungtungmadic acid was determined using chemical and spectral analysis. The antioxidant activity of tungtungmadic acid was evaluated using various antioxidant assays, including free radical scavenging, lipid peroxidation and hydroxyl radical-induced DNA strand breaks assays.

Enhancement of tyrosinase inhibition of the extract of Veratrum patulum using cellulase.

Inhibitors of melanin biosynthesis were screened by using three different methods. The extract of Veratrum patulum contains hydroxystilbene compounds that are potent tyrosinase inhibitors. We evaluated the enzyme inhibitory property on the mushroom tyrosinase of hydroxystilbene compounds including resveratrol, oxyresveratrol, and their analogs.

The coffee diterpene kahweol suppress the inducible nitric oxide synthase expression in macrophages.

Excessive nitric oxide production by inducible nitric oxide synthase (iNOS) in stimulated inflammatory cells is thought to be a causative factor of cellular injury in cases of inflammation. In recent studies, it has been shown that kahweol, coffee-specific diterpene, exhibit chemoprotective effects. In this study, we investigated the effects of kahweol on the production of and the expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-activated RAW 264.

Cytotoxic triterpenoids from the fruits of Zizyphus jujuba.

The following eleven triterpenoic acids were isolated from the fruits of Zizyphus jujuba (Rhamnaceae): colubrinic acid, alphitolic acid, 3-O-cis-p-coumaroylalphitolic acid (3), 3-O-trans-p-coumaroylalphitolic acid (4), 3-O-cis-p-coumaroylmaslinic acid, 3-O-trans-p-coumaroylmaslinic acid, betulinic acid (7), oleanolic acid, betulonic acid (9), oleanonic acid and zizyberenalic acid. The in vitro cytotoxicities of the triterpenoic acids against K562, B16(F-10), SK-MEL-2, PC-3, LOX-IMVI, and A549 tumor cell lines were investigated by the sulforhodamin B (SRB) method. Among these compounds, the lupane-type triterpenes, such as compounds 3, 4, 7, and 9, showed high cytotoxic activities.

New guaianolides from leaves and stems of Chrysanthemum boreale.

The 8-acetoxy-2-methoxy-10-hydroxy-3,11(13)-guaiaden-12,6-olide 1 and 8,10-diacetoxy-2-methoxy-3,11(13)-guaiadiene-12,6-olide 2 were isolated from Chrysanthemum boreale Makino. Compound 1 inhibited the etoposide-induced apoptosis in U 937 cells with an IC50 value 8.6 microg/mL.

Dykellic acid inhibits phorbol myristate acetate-induced matrix metalloproteinase-9 expression by inhibiting nuclear factor kappa B transcriptional activity.

Proteolytic degradation of the extracellular matrix and tumor metastasis correlate with expression of endopeptidases known as matrix metalloproteinases (MMPs). Expression of MMPs is regulated by cytokines and signal transduction pathways, including those activated by phorbol myristate acetate. We found that dykellic acid, a fungal metabolite, significantly inhibits the phorbol myristate acetate-induced increase in MMP-9 expression and activity.

Dykellic acid inhibits drug-induced caspase-3-like protease activation.

Dykellic acid is a novel microbial metabolite isolated from the broth of Westerdykella multispora F50733. Investigations on the molecular function of dykellic acid revealed that this compound partially inhibits calcium influx, resulting in a decrease in Ca(2+)-dependent endonuclease activation and DNA fragmentation induced by camptothecin. In our experiments, active caspase-3-like protease cleavage of procaspase-3, PARP, and cytosolic cytochrome c was inhibited by dykellic acid in a concentration-dependent manner when the apoptosis was induced by camptothecin as well as doxorubicin.

Brine shrimp lethality of the compounds from Phryma leptostachya L.

Brine shrimp assay-guided fractionation and isolation of the EtOAc soluble fraction of Phryma leptostachya L. (Phrymacaceae) gave two active compounds, phrymarolin II (1) and ursolic acid (2), which were identified by physicochemical and spectroscopic methods. Compound 1 exhibited potent lethality with LD50 value of 0.

Eucosterol oligoglycosides isolated from Scilla scilloides and their anti-tumor activity.

Two new eucosterol oligoglycosides, 15-deoxo-30-hydroxyeucosterol 3-O-alpha-L-rhamnopyranosyl-(1-->2)-[(beta-D-glucopyranosyl-(1-->3)]-beta-D-glucopyranosyl-(1-->2)-alpha-L-arabinopyranosyl-(1-->6)-beta-D-glucopyranoside (scillanoside L-1, 1) and 3beta,31-dihydroxy-17alpha,23-epoxy-5alpha-lanost-8-en-23,26-olactone 3-O-alpha-L-rhamnopyranosyl-(1-->2)-[beta-D-glucopyranosyl-(1-->3)]-beta-D-glucopyranosyl-(1-->2)-alpha-L-arabinopyranosyl-(1-->6)-beta-D-glucopyranoside (scillanoside L-2, 2), were isolated from the bulbs of Scilla scilloides, together with four that were known (3-6), have been isolated from the bulbs of Scilla scilloides. The structures of the new compounds were determined on the basis of spectroscopic and chromatographic methods, and some chemical transformations were discussed. Amongst the isolated compounds, 3 showed the most significant cytotoxicity against tumor cells tested several types with ED(50) value of 1.

Biological effects of G1 phase arrest compound, sesquicillin, in human breast cancer cell lines.

Sesquicillin, isolated from fungal fermentation broth, strongly induced G1 phase arrest in human breast cancer cells. During G1 phase arrest, the expression level of cyclin D1, cyclin A, and cyclin E was decreased, and the expression of CDK (cyclin-dependent-kinase) inhibitor, protein p21(Waf1/Cip1), was increased in a time-dependent manner in a breast cancer cell MCF-7. Interestingly, the G1 phase arrest induced by sesquicillin also occurred independently of the tumor suppressor protein, p53.

Paenibacillus chinjuensis sp. nov., a novel exopolysaccharide-producing bacterium.

A novel exopolysaccharide-producing bacterium (WN9T) was isolated from Chinju, Korea, and was identified as a member of the genus Paenibacillus on the basis of phenotypic characteristics and phylogenetic inference based on 16S rDNA sequence. This organism is a facultatively anaerobic, endospore-forming rod. The diamino acid found in the peptidoglycan is meso-diaminopimelic acid.

Halomonas alimentaria sp. nov., isolated from jeotgal, a traditional Korean fermented seafood.

A gram-negative, moderately halophilic bacterial strain, YKJ-16T, which was isolated from jeotgal, a traditional Korean food, was considered to be a member of the genus Halomonas. Cells of strain YKJ-16T are non-motile and cocci or short rods, unlike most Halomonas species. However, chemotaxonomic and phylogenetic analyses demonstrated that strain YKJ-16T belongs to the genus Halomonas.