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PubMed1990

A bioactive glass powder-ammonium hydrogen phosphate composite for repairing bone defects.

Bioactive glass powder (AW-G) was made into a rigid compound by mixing with ammonium hydrogen phosphate and was evaluated as a bone-defect filler. The proximal metaphysis of the rat tibia was drilled and packed with (a) polymethyl-methacrylate (PMMA) bone cement, (b) AW-G powder, (c) AW-G powder with ammonium hydrogen phosphate (AW-G)-(A-P), or (d) nothing, as a control. The animals, with different implantation periods up to 24 weeks, were sacrificed and the defective sites were histologically analyzed. The results revealed direct bonding between the bone tissue and the (AW-G)-(A-P). The general inflammatory reaction of (AW-G)-(A-P) was less than that of PMMA bone cement. The compressive strength of (AW-G)-(A-P) implanted subcutaneously into rats was measured chronologically and deterioration did not occur during a period of 24 weeks. The rigidity increased to 1.6 times 6 months after implantation as compared with the initial value. This compound can be used as paste and is transformed into a rigid compound in about 4 min without noticeable elevation of the temperature. Thus, this (AW-G)-(A-P) composite can be used as a bone defect filler, and there is a possibility that it can even be used as a bone cement if higher rigidity can be attained.

Animals↗
PubMed2007

Experimental approaches for studying uptake and action of herbal medicines.

In order to gain wider credibility, herbal medicines must go through the rigorous scientific scrutiny to which synthetic drugs are subjected, and this includes investigating their absorption, bioavailability and metabolism. This review describes approaches for determining how active compounds in herbal formulations enter the systemic circulation. To assess how bioactive molecules enter the target organs and cells, specific cell lines and organ culture models can be used, followed by in vitro models to show how they may regulate digestion, energy balance and metabolism. This could lead to a better understanding of how herbal medicines affect digestion and absorption; fundamental questions which should be answered in addition to their mechanism of action.

Biological Availability↗
PubMed2004

Mastrus ridibundus parasitoids eavesdrop on cocoon-spinning codling moth, Cydia pomonella, larvae.

Cocoon-spinning larvae of the codling moth, Cydia pomonella L. (Lepidoptera: Olethreutidae) employ a pheromone that attracts or arrests conspecifics seeking pupation sites. Such intraspecific communication signals are important cues for illicit receivers such as parasitoids to exploit. We tested the hypothesis that the prepupal C. pomonella parasitoid Mastrus ridibundus Gravenhorst (Hymenoptera: Ichneumonidae) exploits the larval aggregation pheromone to locate host prepupae. In laboratory olfactometer experiments, female M. ridibundus were attracted to 3-day-old cocoons containing C. pomonella larvae or prepupae. Older cocoons containing C. pomonella pupae, or larvae and prepupae excised from cocoons, were not attractive. In gas chromatographic-electroantennographic detection (GC-EAD) analyses of bioactive Porapak Q extract of cocoon-derived airborne semiochemicals, ten compounds elicited responses from female M. ridibundus antennae. Comparative GC-mass spectrometry of authentic standards and cocoon-volatiles determined that these compounds were 3-carene, myrcene, heptanal, octanal, nonanal, decanal, (E)-2-octenal, (E)-2-nonenal, sulcatone, and geranylacetone. A synthetic 11-component blend consisting of these ten EAD-active compounds plus EAD-inactive (+)-limonene (the most abundant cocoon-derived volatile) was as effective as Porapak Q cocoon extract in attracting both female M. ridibundus and C. pomonella larvae seeking pupation sites. Only three components could be deleted from the 11-component blend without diminishing its attractiveness to M. ridibundus, which underlines the complexity of information received and processed during foraging for hosts. Mastrus ridibundus obviously "eavesdrop" on the pheromonal communication signals of C. pomonella larvae that reliably indicate host presence.

Animals↗
PubMed2006

Astonishing diversity of natural surfactants: 7. Biologically active hemi- and monoterpenoid glycosides.

This review article presents 90 hemi- and 188 monoterpenoid glycosides, isolated and identified from plants and microorganisms, that demonstrate different biological activities. These natural bioactive glycosides are good prospects for future chemical preparations from these compounds as antioxidants and as anticancer, antimicrobial, and antibacterial agents. These glycosidic compounds have been subdivided into several groups, including hemiterpenoids; acyclic, monocyclic, and bicyclic monoterpenoids; and iridoid monoterpenoids.

Biological Products↗
PubMed1996

A low-cost UV laser for flash photolysis of caged compounds.

Photolysis of caged compounds has become a standard tool for the rapid application of bioactive molecules. In principle this technique also allows to apply substances in a spatially very restricted manner. An important practical limitation for such experiments, however, is the high cost of UV lasers. Here we describe the assembly of an inexpensive pulsed nitrogen laser which is suitable for photolysis experiments. The laser which can be constructed in less than 1 week and for less than US$ 500 emits light pulses with a duration of approximately 5 ns, an energy of up to 200 microJ (= 40 kW) and a wavelength of 337 nm. Its beam can be focused to roughly 30 microns, a firing frequency of up to 50 Hz can be achieved, and electrical artifacts are minimal. These specifications make the laser optimally suited for most photolysis experiments. Its low price and ease of use should make the technique of spatially restricted flash photolysis amenable to many laboratories.

Animals↗
PubMed1993

Pyrazine CH- and NH-acids. Antithrombotic activity and chromatographic behaviour.

1. A series of newly synthesized pyrazine CH- and NH-acids was subjected to analytical and pharmacological studies. 2. The compounds were chromatographed in HPLC systems employing three reversed-phase columns and methanol-buffer solvents of various composition at acidic, neutral and alkaline pH. 3. Chemometrical analysis by the principal component method allowed for ordering of the compounds on a plane determined by the first two principal component axes. 4. Pharmacological tests were done for representatives of the series of compounds. 5. An in vivo antithrombotic assay on mice proved diversified bioactivity within the group of agents. 6. Attempts were undertaken to relate chromatographic behaviour to antithrombotic activity. 7. Based on the results obtained, an approach was proposed to reduce the number of pharmacological tests in selecting the most promising agents.

Adenosine Diphosphate↗
PubMed1982

Microsomal bioactivation and covalent binding of aliphatic halides to DNA.

Studies were carried out on the in vitro covalent binding of a series of 14C-labeled aliphatic halides to calf thymus DNA following bioactivation by hepatic microsomes isolated from phenobarbital-treated rats. Six compounds were shown to exhibit binding to DNA of greater than 0.3 nmol/mg DNA (1,2-dibromoethane, bromotrichloromethane, trichloroethylene, carbon tetrachloride, chloroform, and 1,1,2-trichloroethane). Covalent binding of the aliphatic halides to the nucleic acids was confirmed by sedimentation of the DNA-organohalogen adduct in a cesium chloride gradient and Sephadex LH-20 chromatography of the nucleosides released by enzymatic hydrolysis.

Animals↗
PubMed2005

Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.

N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC50 values ranging from 0.95 to 17.50 microM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.

Binding Sites↗
PubMed2004

Involvement of proapoptotic Bcl-2 family members in parthenolide-induced mitochondrial dysfunction and apoptosis.

Parthenolide is a sesquiterpene lactone responsible for the bioactivities of Feverfew. Besides its potent anti-inflammatory effect, this compound has recently been reported to induce apoptosis in cancer cells, possibly through mitochondrial dysfunction. In the present study, we attempted to examine parthenolide-mediated cell death signaling pathway by focusing on the involvement of Bcl-2 family members. Using a human colorectal cancer cell line COLO205, we first demonstrated that parthenolide acted through the cell death receptor pathway to activate caspase 8. Following caspase 8 activation, Bid, a proapoptotic Bcl-2 member, was cleaved and this cleavage then triggered Bax conformational changes and Bax translocation from cytosol to mitochondrial membrane. Meanwhile, another proapoptotic protein, Bak, was up-regulated and oligomerized on the mitochondrial membrane. All these alterations were found to be prerequisite for the subsequent release of proapopototic mitochondrial proteins, including cytochrome c and Samc, in parthenolide-treated cells. Moreover, selective inhibition of caspase 8 activity by a synthetic caspase inhibitor (IETD-FMK) or overexpression of a viral protein (CrmA) suppressed the cleavage of Bid, conformational changes of Bax, cytochrome c release, and apoptosis. Therefore, the proapoptotic Bcl-2 family members are important mediators relaying the cell death signaling elicited by parthenolide from caspase 8 to downstream effector caspases such as caspase 3, and eventually to cell death.

Apoptosis↗
PubMed2006

Quality evaluation of Platycladus orientalis (L.) Franco through simultaneous determination of four bioactive flavonoids by high-performance liquid chromatography.

Platycladus orientalis (L.) Franco (Cupressaceae), a traditional Chinese herb and food additive, has been used for treatments of gout, rheumatism, diarrhoea and chronic tracheitis. To evaluate the quality of P. orientalis (L.) Franco, a sensitive, simple and accurate reversed-phase high-performance liquid chromatographic (RP-HPLC) separation method with a photodiode array detector (DAD) was developed for the determination of four main bioactive flavonoids, rutin, quercitrin, quercetin and amentoflavone. Separation of the four compounds was achieved by the HPLC assay (Agilent Eclipse XDB-C 18 column with mobile phase, methanol-acetonitrile-18 mM sodium acetate buffer (pH 3.5) and recorded at UV 356 nm). This method showed good linear relation in the range of 0.8-80 microg/ml for rutin, 1.84-184 microg/ml for quercitrin, 0.72-72 microg/ml for quercetin and 0.72-72 microg/ml for amentoflavone. The correlation coefficients of the calibration curve for the analysis were all higher than 0.999. In addition, the contents of those four flavonoids in P. orientalis (L.) Franco growing in 12 different locations in China were compared to establish the effectiveness of the method.

Biflavonoids↗
PubMed2003

Solid-phase microextraction of volatile compounds from the chopped leaves of three species of Eucalyptus.

Headspace solid-phase microextraction (HS-SPME) coupled with gas chromatography and ion-trap mass spectrometry has been used to identify biogenic volatile organic compounds present in the headspace of chopped leaves of Eucalyptus (E.) dunnii, E. citriodora, and E. saligna. A simple HS-SPME method entailing 30 min of extraction at 30 degrees C was developed for this purpose. Thirty compounds were identified in the headspace of 60 juvenile chopped Eucalyptus leaves, and another 30 were tentatively identified. The presence of compounds such as (E)-4,8-dimethyl-1,3,7-nonatriene (DMNT), (E,E)-4,8,12-trimethyl-1,3,7,11-tridecatetraene (TMNT), (E,E)-alpha-farnesene, (E,E,E)-3,7,11,15-tetramethyl-1,3,6,10,14-hexadecapentaene (TMHP), beta-caryophyllene, alpha-humulene, germacrene D, and beta-cubebene in the headspace of the leaves but not in the essential oils from the same Eucalyptus trees and information about the infochemical roles of some of these compounds in other living plant systems suggest they might play a bioactive role in Eucalyptus leaves.

Eucalyptus↗
PubMed2005

Isolation and identification of antifungal and antialgal alkaloids from Haplophyllum sieversii.

Bioassay-guided fractionation of the hexane/ethyl acetate/water (H/EtOAc/H2O) crude extract of the aerial parts of Haplophyllum sieversii was performed because of preliminary screening data that indicated the presence of growth inhibitory components against Colletotrichum fragariae, Colletotrichum gloeosporioides, and Colletotrichum acutatum. Fractionation was directed using bioautographical methods resulting in the isolation of the bioactive alkaloids flindersine, anhydroevoxine, haplamine, and a lignan eudesmin. These four compounds were evaluated for activity against C. fragariae, C. gloeosporioides, C. acutatum, Botrytis cinerea, Fusarium oxysporum, and Phomopsis obscurans in a dose-response growth-inhibitory bioassay at 50.0, 100.0, and 150.0 microM. Of the four compounds tested, flindersine demonstrated the highest level of antifungal activity. Additionally, flindersine, eudesmin, and haplamine were screened against the freshwater phytoplanktons Oscillatoria perornata, Oscillatoria agardhii, Selenastrum capricornutum, and Pseudanabaena sp. (strain LW397). Haplamine demonstrated selective inhibition against the odor-producing cyanobacterium O. perornata compared to the activity against the green alga S. capricornutum, with lowest observed effect concentration values of 1.0 and 10.0 microM, respectively.

Alkaloids↗
PubMed2003

Isolation of homodolastatin 16, a new cyclic depsipeptide from a Kenyan collection of Lyngbya majuscula.

An examination of an organic extract of the cyanobacterium Lyngbya majuscula, collected from Wasini Island off the southern Kenyan coast, led to the isolation of the known cyclic depsipeptide antanapeptin A (1), recently isolated from a Madagascan collection of L. majuscula, and a new bioactive cyclic depsipeptide, homodolastatin 16 (2). The structures of these two compounds were determined from NMR and mass spectrometry data. Homodolastatin 16, a higher homologue of the potential anticancer agent dolastatin 16, exhibited moderate activity against oesophageal and cervical cancer cell lines.

Antineoplastic Agents↗
PubMed2003

Potent mammalian cerebroprotection and neuronal cell death inhibition are afforded by a synthetic antioxidant analogue of marine invertebrate cell protectant ovothiols.

Implicit strategies for neuroprotection in the adult brain include GABAA receptor activation, N-methyl-d-aspartate receptor and sodium voltage-gated channel inhibition. Ironically, these same targets may be harmful to the immature or developing brain. Protection has been demonstrated for both immature and mature brain with the use of a synthetic ovothiol analogue. The following beneficial effects have been demonstrated in mice: protection against audiogenic seizures, brain structures with clear-cut delineation of ibotenate-challenged white and grey matter lesions along with exceptional early and delayed protections, and potent cerebral cell death inhibition. The compound lacks both GABAergic activity and sodium channel blocker properties, which may help explain the lack of toxicity normally expressed in an immature brain utilizing these agents [J.W. Olney (2002) Neurotoxicology, 93, 1-10]. The oxidized form of the compound is virtually devoid of antioxidant activity. In vivo it exhibits cerebroprotective properties similar to those of reduced compounds endowed with antioxidant properties. This unexpected finding has prompted an extensive in vitro exploration of underlying molecular mechanisms that have led to the identification of several recycling mechanisms consistent with non rate-limiting conversion of oxidized to reduced compound forms. Taken as a whole, this work offers an unique combined in vitro and in vivo support that: (i). antioxidant therapy, here engineered from marine invertebrate egg protectants, may be a valuable strategy in protecting both mammalian adult and developing brain; and (ii). recycling (thiol-disulphide exchange) properties of the oxidized form of an antioxidant compound are as important as the antioxidant potential exhibited by a bioactive reduced antioxidant in certain neuroprotective processes.

Animals↗
PubMed2003

Gene expression changes in the human fibroblast induced by Centella asiatica triterpenoids.

The molecular pathways underlying the diverse biological activity of the triterpeniod compounds isolated from the tropical medicinal plant Centella asiatica were studied with gene microarrays and real-time reverse transcription polymerase chain reaction (real-time RT-PCR) to quantify the expression of 1053 human genes in human fibroblasts. Fibroblast cells grown in culture were used as a model system to evaluate the stimulation of wound healing by titrated extract from Centella asiatica (TECA) as well as by the four principal triterpenoid components of Centella. TECA treatment effects the expression of genes involved in angiogenesis and the remodeling of extracellular matrix, as well as diverse growth factor genes. The extent of expression change of TNFAIP6, an extracellular hyaluronan binding protein, was found to be largely dose-dependent, to respond most strongly to the free acids asiatic acid and madecassic acid, and to increase in expression over 48 hours of treatment. These results show that Centella triterpenes evoke a gene-expression response consistent with their prevailing medical uses in the treatment of connective tissue disorders such as wound healing and microangiopathy. The identification of genes modulated by these compounds provides the basis for a molecular understanding of Centella's bioactivity, and opportunities for the quantitative correlation of this activity with clinical effectiveness at a molecular level.

Cell Line↗
PubMed2004

New Polyacetylenes, DGAT inhibitors from the roots of Panax ginseng.

The petroleum ether extract of Panax ginseng showed a significant inhibition of the diacylglycerol acyltransferase (DGAT) enzyme from rat liver microsomes. Bioactivity-guided fractionation led to the isolation of two new polyacetylenic compounds, (9 R,10 S)-epoxyheptadecan-4,6-diyn-3-one ( 1) and 1-methoxy-(9 R,10 S)-epoxyheptadecan-4,6-diyn-3-one ( 2). Their chemical structures were elucidated on the basis of spectroscopic evidence and asymmetric synthesis. IC50 values of 9 microg/mL ( 1) and 32 microg/mL ( 2) were obtained.

Acetylene↗
PubMed1990

Studies on the induction of gene mutations in bacterial and mammalian cells by the ring-opened benzene metabolites trans,trans-muconaldehyde and trans,trans-muconic acid.

t,t-Muconaldehyde and t,t-muconic acid have been investigated for the induction of gene mutations in Salmonella typhimurium (reversion of the his- strains TA97, TA98, TA100, TA102, TA104 and TA1535), Escherichia coli (reversion of the trp- strain WP2 uvrA) and Chinese hamster V79 cells (acquisition of resistance toward 6-thioguanine). t,t-Muconaldehyde proved weakly mutagenic in strain TA104 in the presence and absence of NADPH-fortified postmitochondrial fraction from rat liver homogenate (S9 mix). In strains TA97, TA100 and TA102, weak positive responses were observed only in the presence of S9 mix. In strains TA98, TA1535 and WP2 uvrA, the result was negative. In V79 cells, the mutation frequency was increased from approximately 7 X 10(-6) to 90 X 10(-6) in cultures exposed to t,t-muconaldehyde at optimal concentration (1.7-3 microM in separate experiments). The concentration-response curve showed pronounced hyperlinearity, with no mutagenic effect being observed at a third of the optimal concentration. t,t-Muconic acid was greater than 100 times less toxic than t,t-muconaldehyde in both bacteria and mammalian cells, and it did not show any mutagenic effect. These results complete a previous mutagenicity study, carried out on benzene and 13 metabolites. It is concluded that the newly investigated metabolites cannot account for the bacterial mutagenicity of bioactivated benzene and benzene-trans-1,2-dihydrodiol, since these compounds exhibited their strongest response in strain TA1535. t,t-Muconaldehyde showed similarities in its mutagenicity to p-benzoquinone and hydroquinone. All three compounds showed, at most, weak effects in bacteria, but were strongly mutagenic in V79 cells.(ABSTRACT TRUNCATED AT 250 WORDS)

Aldehydes↗
PubMed2005

Gene expression profiling of nephrotoxicity from the sevoflurane degradation product fluoromethyl-2,2-difluoro-1-(trifluoromethyl)vinyl ether ("compound A") in rats.

The major degradation product of the volatile anesthetic sevoflurane, the haloalkene fluoromethyl-2,2-difluoro-1-(trifluoromethyl)vinyl ether (FDVE or "compound A"), is nephrotoxic in rats. FDVE undergoes complex metabolism and bioactivation, which mediates the nephrotoxicity. Nevertheless, the molecular and cellular mechanisms of FDVE toxification are unknown. This investigation evaluated the gene expression profile of kidneys in rats administered a nephrotoxic dose of FDVE. Male Fischer 344 rats (five per group) received 0.25 mmol/kg intraperitoneal FDVE or corn oil (controls) and were sacrificed after 24 or 72 h. Urine output and kidney histological changes were quantified. Kidney RNA was extracted for microarray analysis using Affymetrix GeneChip Rat Expression Array 230A arrays. Quantitative real-time PCR confirmed the modulation of several genes. FDVE caused significant diuresis and necrosis at 24 h, with normal urine output and evidence of tubular regeneration at 72 h. There were 517 informative genes that were differentially expressed >1.5-fold (p < 0.05) versus control at 24 h, of which 283 and 234 were upregulated and downregulated, respectively. Major classes of upregulated genes included those involved in apoptosis, oxidative stress, and inflammatory response (mostly at 24 h), and regeneration and repair; downregulated genes were generally associated with transporters and intermediary metabolism. Among the quantitatively most upregulated genes were kidney injury molecule, osteopontin, clusterin, tissue inhibitor of metalloproteinase 1, and TNF receptor 12, which have been associated with other forms of nephrotoxicity, and angiopoietin-like protein 4, glycoprotein nmb, ubiquitin hydrolase, and HSP70. Microarray results were confirmed by quantitative real-time PCR. FDVE causes rapid and brisk changes in gene expression, providing potential insights into the mechanism of FDVE toxification, and potential biomarkers for FDVE nephrotoxicity which are more sensitive than conventional measures of renal function.

Anesthetics, Inhalation↗