PubMed HealthSearch

Biomedical subjects

D Vanden Berghe

Publications and source records attributed to D Vanden Berghe.

At least 19 recordsLinked to original sources

Complement-inhibiting cucurbitacin glycosides from Picria fel-terrae.

Four cucurbitacin glycosides were isolated from Picriafel-terrae and identified by MS and NMR spectroscopy as picfeltarraenin IA (1), picfeltarraenin IB (2), picfeltarraenin IV (4), and a new compound picfeltarraenin VI (3) (picfeltarraegenin I 3-O-beta-D-xylopyranoside). All four compounds acted as inhibitors on both the classical and alternative pathways of the complement system, with compound 3 exhibiting the highest inhibitory activity (IC50 29 +/- 2 microM and 21 +/- 1 microM, respectively). Compounds 1-4 showed no antiviral, antibacterial, or antifungal activities. Picfeltarraenin IA and IB were tested in an in vitro human tumor cell line panel, but displayed no cytotoxic activity.

Anti-Infective Agents

Structure-activity relationship and classification of flavonoids as inhibitors of xanthine oxidase and superoxide scavengers.

The structure-activity relationship of flavonoids as inhibitors of xanthine oxidase and as scavengers of the superoxide radical, produced by the action of the enzyme xanthine oxidase, was investigated. The hydroxyl groups at C-5 and C-7 and the double bond between C-2 and C-3 were essential for a high inhibitory activity on xanthine oxidase. Flavones showed slightly higher inhibitory activity than flavonols. All flavonoid derivatives except isorhamnetin (30) were less active than the original compounds. For a high superoxide scavenging activity on the other hand, a hydroxyl group at C-3' in ring B and at C-3 were essential. According to their effect on xanthine oxidase and as superoxide scavengers, the flavonoids could be classified into six groups: superoxide scavengers without inhibitory activity on xanthine oxidase (category A), xanthine oxidase inhibitors without any additional superoxide scavenging activity (category B), xanthine oxidase inhibitors with an additional superoxide scavenging activity (category C), xanthine oxidase inhibitors with an additional pro-oxidant effect on the production of superoxide (category D), flavonoids with a marginal effect on xanthine oxidase but with a prooxidant effect on the production of superoxide (category E), and finally, flavonoids with no effect on xanthine oxidase or superoxide (category F).

Enzyme Inhibitors

Complement-modulating properties of a kaempferol 7-O-rhamnosylsophoroside from the leaves of Morinda morindoides.

A kaempferol 7-O-rhamnosylsophoroside isolated from the leaves of Morinda morindoides showed dose-dependent complement-modulating properties towards both the classical (inhibiting effect) and alternative (activating effect) pathways of the complement system. Its structure was elucidated by chemical and spectroscopic methods as kaempferol 7-O-[alpha-L-rhamnopyranosyl-(1-->6)]-[beta-D-glucopyranosyl-(1-->2)]-be ta-D-glucopyranoside, a new natural product which was named morindaoside.

Carbohydrate Sequence

Inhibition of bacterial mutagenesis by Citrus flavonoids.

The antimutagenicity of the Citrus flavonoids naringin, hesperidin, nobiletin, and tangeretin against the mutagens benzo[a]pyrene, 2-aminofluorene, quercetin, and nitroquinoline N-oxide was investigated in the Salmonella/microsome assay. Naringin and hesperidin showed a weak antimutagenic activity against benzo[a]pyrene. Tangeretin was antimutagenic against all indirectly-acting mutagens tested, but in general a large molar excess was necessary. Liquid preincubation increased the antimutagenicity of tangeretin against 2-aminofluorene. Nobiletin acted as an antimutagen against benzo[a]pyrene, but it enhanced the mutagenicity of 2-aminofluorene. However, in a liquid preincubation assay nobiletin also exhibited antimutagenicity against 2-aminofluorene. Both tangeretin and nobiletin inhibited the mutagenicity of quercetin. Quercetin itself acted as an antimutagen against 2-aminofluorene in a Salmonella strain (TA1538) where its mutagenicity was not expressed. Quercetin should not merely be regarded as a genotoxic risk factor in the human diet, since its mutagenicity may be inhibited by accompanying compounds including other flavonoids, and since quercetin itself also exhibits an antimutagenic action. Because of the antimutagenic properties the Citrus flavonoids tested, especially tangeretin and nobiletin, might play a role in the chemoprevention of cancer.

Anticarcinogenic Agents

Screening of hundred Rwandese medicinal plants for antimicrobial and antiviral properties.

A series of 100 Rwandese medicinal plants (267 plant extracts), used by traditional healers to treat infections, were screened for antibacterial, antifungal and antiviral properties. The results of the testing showed that 45% were active against Staphylococcus aureus, 2% against Escherichia coli, 16% against Pseudomonas aeruginosa, 7% against Candida albicans, 80% against Microsporum canis and 60% against Trichophyton mentagrophytes. Not less than 27% of the plant species exhibited prominent antiviral properties against one or more test viruses, more specifically 12% against poliomyelitis, 16% against coxsackie, 3% against Semliki forest, 2% against measles and 8% against herpes simplex virus.

Anti-Bacterial Agents

In vitro anticomplementary activity of constituents from Morinda morindoides.

In a screening program for complement classical pathway modulation, an 80% MeOH extract of the leaves of Morinda morindoides showed potent dose-dependent anticomplementary activity. Bioassay-guided chromatographic separation of the active constituents led to the isolation of ten flavonoids of which two were aglycones. The compounds were tested in vitro for their putative complement-inhibiting properties on the classical (CP) and the alternative (AP) pathways of the complement system. The results indicated that quercetin [1], quercetin 3-O-rhamnoside (quercitrin) [5], and quercetin 3-O-rutinoside (rutin) [7] showed similar anticomplementary activities (inhibition) on the CP of complement. A mixture of two kaempferol triglycosides isolated and denoted as M(015), also had a good inhibitory effect. The effects of these compounds were dose-dependent for this pathway. On the AP of complement, quercetin [1] and M(015) had, respectively, more pronounced inhibitory and activatory effects than the other tested flavonoids, but their effects were not dose-dependent for this pathway. The other isolated flavonoids showed weak effects or were inactive for both pathways.

Animals

Antibacterial and molluscicidal phenolic acids from Spondias mombin.

Spondias mombin L. (Anacardiaceae), used in traditional medicine because of its antimicrobial properties, was found to contain a series of 6-alkenyl-salicylic acids. They were isolated from the ethanolic extract of leaves and stems of Spondias mombin by a combination of chromatographic methods. Their structure was determined by NMR and MS techniques as (17:3), (17:2) and (17:1) pelandjuaic acid [or 6-(8'Z,11'Z,14'Z-heptadecatrienyl)-salicylic acid, 6-(8'Z,11'Z-heptadecadienyl)-salicylic acid, and 6-(10'Z-heptadecenyl)-salicylic acid, respectively], 6-(12'Z-non-adecenyl)-salicylic acid, and 6-(15'Z-heneicosenyl)-salicylic acid, the two last compounds being new ones. These phenolic acids were shown to have a pronounced antibacterial effect against Bacillus cereus, Streptococcus pyogenes, and Mycobacterium fortuitum (minimal bactericidal concentration in a concentration range of 3-25 micrograms/ml), and a molluscicidal effect against the snail Biomphalaria glabrata, an intermediate host in the schistosome life cycle. Because of their high molluscicidal activity (LC90 down to 1-3 ppm), these long-chain salicylic acid derivatives may be important tools in the prevention of schistosomiasis.

Animals

Selenium deficiency triggering intractable seizures.

Two children with severe neurodevelopmental retardation and elevated liver function tests developed intractable seizures during the first year of life. Detectable neurometabolic conditions have been ruled out. At the time of seizures evidence for systemic selenium deficiency could be documented. The youngest patient, who manifested intractable fits from the fourth day of life, died at the age of ten months. Neuropathologic examination was consistent with Progressive Neuronal Degeneration of Childhood (PNDC) with liver disease or formerly known as Alpers disease. In the oldest child, whose diet was normally balanced, fits started from the age of 11 months and features of long-standing selenium deficiency became apparent from the age of 1 1/2 years and consisted of liver function disturbances, depigmented hair and osteoarthropathy. Oral substitution with selenium supplements in both children (3-5 micrograms/kg body weight) resulted in reduction of seizures and improvement of the EEG recordings after two weeks while liver function became normal. Two of the seleno-dependent enzymes Glutathione Peroxidase (GPX) and Phospholipid Hydroperoxide Glutathione Peroxidase (PHGPX) are speculated to play a key-role in the defence of neuronal cells against oxygen radical formation and peroxidative processes. Our findings support the hypothesis that the presence of selenium depletion in the brain amongst patients with epilepsy constitutes an important triggering factor for the origin of intractable seizures and subsequent neuronal damage.

Atrophy

Human retinal pigment epithelial cells from different donors continuously produce a vascular endothelial cell-stimulating factor into serum-free medium.

Mitogenic activities of human retinal pigment epithelial cell-conditioned medium (HRPE-CM) with different effects, such as inhibition, stimulation or no effect, on the proliferation of vascular endothelial cells (EC) in vitro have been reported. In this study, 14 HRPE cell lines were established from normal human eyes. Human umbilical vein endothelial cells (HUVEC) in the early passages were used as target cells to detect the mitogenic activity of HRPE-CM on the growth of vascular EC. Our results confirm that HRPE cells in culture continuously synthesize and secrete HUVEC growth substance(s) into a serum-free medium. The ability of HRPE cell lines to produce this mitogen seem unrelated either to in vivo donor factors or to in vitro cell life span. Using an enzyme-linked immunosorbance assay, we demonstrated that only HRPE cell extract, not HRPE-CM, can be recognized by basic fibroblast growth factor (bFGF)-specific antibody, though identical bioactivities on the growth of HUVEC were found in both preparations. The active component in HRPE-CM was heat- and trypsin-sensitive, and stable at extremes of pH (2.5 to 10.0). In addition, the bioactive molecule could not pass through a M(r) 30,000 cut-off membrane, suggesting that it is a fairly high molecular mass polypeptide. These observations suggest that the EC growth factor in HRPE-CM is distinct from fibroblast growth factors (FGFs).

Cell Division

Lack of evidence for strand-specific inhibition of poliovirus RNA synthesis by 3-methylquercetin.

Buffalo Green Monkey cells were infected with poliovirus-1 in the presence of 3-methylquercetin or guanidine, and the formation of positive- and negative-strand viral RNA was monitored using single-stranded RNA probes. Both 3-methylquercetin and guanidine prevented the formation of plus-strand as well as minus-strand viral RNA, although, due to the high multiplicity of infection used, a high number of genomic viral RNA was always present in the cells.

Animals

The use of iodinated density gradient media for the isolation of rod outer segments.

Sucrose, nycodenz, metrizamide and a mixture of equal volumes of sucrose and metrizamide were used as density gradient media for the isolation of retinal rod outer segments. The high osmolarity of sucrose had a strongly negative effect on the nature of the rod outer segments, whereas they were much better preserved using iodinated density gradient media such as nycodenz and metrizamide for their isolation.

Animals

3-Methylquercetin is a potent and selective inhibitor of poliovirus RNA synthesis.

3-Methylquercetin (3MQ) is a natural compound isolated from Euphorbia grantii that selectively inhibits poliovirus replication, but has no effect on encephalomyocarditis virus. When the compound is present from the beginning of infection, the bulk of viral protein synthesis is prevented, but the shut-off of host protein synthesis still occurs. Addition of 3MQ 3 hr after infection has a slight effect on viral protein synthesis, suggesting that this compound blocks a step of viral replication different from translation. Indeed, poliovirus RNA synthesis is potently blocked by 3MQ, i.e., 50% inhibition at 2 micrograms/ml (6.3 X 10(-6) M). No effect on encephalomyocarditis, nor on cellular RNA synthesis is observed even at 20 micrograms/ml. The inhibitory effect of 3MQ is reversible, since cells treated with this compound from the beginning of infection start to synthesize viral RNA and proteins when the compound is removed. Strikingly, other natural compounds structurally related to 3-methylquercetin such as quercetin, naringenin, naringin, morin, catechin, kaempferol, myricetin, phloretin, phlorizdin, and rutin do not block poliovirus replication.

Animals

Antimicrobial activity of seven metallic compounds against penicillinase producing and non-penicillinase producing strains of Neisseria gonorrhoeae.

The in vitro activity of seven metallic compounds was tested against penicillinase (beta lactamase) producing strains of Neisseria gonorrhoeae (PPNG) and non-PPNG strains. On a weight basis, the mercurials showed the greatest in vitro activity. Phenylmercuric borate, thiomersal, and mercuric chloride inhibited 90% of all strains at concentrations of 5 mg/l, 5 mg/l, and 20 mg/l respectively. Silver nitrate inhibited 90% of the strains at 80 mg/l and the MIC90 for mild silver protein was 200 mg/l. Copper and selenium salts had lower in vitro activities, inhibiting 90% of all the strains at 320 mg/l and 640 mg/l respectively. Silver nitrate and the six other compounds tested showed equal activities against PPNG and non-PPNG strains. This finding supports the recommendation for prophylaxis of gonococcal conjunctivitis of the newborn with 1% silver nitrate eye drops.

Copper

Characterization and assembly of poliovirus-related 45 S particles.

Using detergents, 45 S particles could be extracted from poliovirus-infected Vero and human embryonic kidney monolayer cells, but not from HeLa suspension cells. They were composed of the capsid proteins VP0, VP1, and VP3, devoid of RNA, and extremely sensitive to heat or to a slightly alkaline pH. The 45 S particles possessed neutralization epitopes of the N1 and N2 classes, as well as a VP3-linked epitope. The N2 epitopes were lost upon denaturation. In the presence of cell extracts 45 S particles were, like 14 S subunits, assembled to 71 S empty capsids expressing the N1 and N2 epitopes.

Animals

Selenium in environmental and drinking waters of Belgium.

The tetravalent and hexavalent selenium content of water samples can be determined by conventional energy-dispersive X-ray fluorescence after different preconcentration steps. Selenium values of nearly three-hundred different environmental and drinking water samples in Belgium are reported. The results are quite low, ranging from the detection limits up to 1 microgram 1-1. The concentration levels are compared to literature data and the speciation is discussed. The contribution of drinking water to the daily intake of selenium in Belgium ranges from less than 0.2 to 5%.

Belgium