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PubMed2006

When normal is not: the dilemma of interpreting laboratory averages of bioactive molecules subject to heterogeneous regulatory feedback and epigenetic mosaicism.

Complex regulatory systems control the levels of many bioactive molecules in the serum. These systems involve the integration of feedback responses from numerous tissues. End-organs and tissues can manifest epigenetic mosaicism, particularly with aging or disease states. We propose that an isolated lab value may reflect a blended average of inhomogeneous feedback responses from target tissues in various states of dysfunction. Reliance on such data may underestimate the state of systemic dysfunction. Yet in clinical practice, normal serum levels of a given molecule and its associated regulatory machinery are often assumed to reflect normal body homeostasis and tissue function. Organism-wide integration of abnormally high and low levels of bioactivity of a molecule in different tissues may yield apparently normal serum values of the bioactive molecule and known components of its regulatory system. We specifically discuss thyroid hormone regulation and function as a case example. Epigenetic reprogramming of either regulatory loops or tissue responses represents another way in which normal serum levels of the molecule may obscure target-organ dysfunction. The proposed idea has broad implications for disease pathogenesis, diagnosis, and therapies. A model where individual tissues employ illegitimate signaling to subvert the concerns of the organism as a whole is also proposed.

Animals↗

PubMed2005

Exploring novel bioactive compounds from marine microbes.

The historical paradigm of the deep ocean as a biological 'desert' has shifted to one of a 'rainforest' owing to the isolation of many novel microbes and their associated bioactive compounds. Recently, there has been an explosion of information about novel bioactive compounds that have been isolated from marine microbes in an effort to further explore the relatively untapped marine microbes and their secondary metabolites for drug discovery. The microbes are recovered and purified from the ocean by both conventional and innovative isolation methods to obtain those previously thought to be 'uncultivable'. To overcome the difficulties and limitations associated with cultivation techniques, several DNA-based molecular methods have been developed to bypass the culture-dependent bottleneck. Bioactive compounds isolated using the above strategies have not only shown importance in biotechnological and pharmaceutical applications but have also increased our understanding of the diversity of marine microbiota, ecosystem functions and the exploitable biology.

Anti-Infective Agents↗

PubMed2006

The formation of bioactive amyloid species by prion proteins in vitro and in cells.

Amyloid proteins are a group of proteins that can polymerize into cross beta-sheeted amyloid species. We have found that enhancing cellular 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) formazan exocytosis is a common property of bioactive amyloid species formed from all of the amyloid proteins tested to date. In this report, we show that the infectious amyloid species of the prion protein HET-s of the filamentous fungus Podospora anserina, like other amyloidogenic proteins, also enhances MTT formazan exocytosis. More strikingly, cellular MTT formazan exocytosis revealed the formation of bioactive amyloid species in prion-infected mouse N2a neuroblastoma cells. These findings suggest that cellular MTT formazan exocytosis can be useful for studying the roles of bioactive amyloid species in prion infectivity and prion-induced neurodegeneration.

Amyloid beta-Peptides↗

PubMed2005

Secretion of bioactive interleukin-6 and tumor necrosis factor-alpha proteins from primary cultured human fetal membrane chorion cells infected with influenza virus.

Influenza virus infection during pregnancy is implicated in one of the causes of premature delivery, abortion and stillbirth. Pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor (TNF)-alpha produced by fetal membranes, are postulated to facilitate premature delivery. We investigated the secretion of IL-6 and TNF-alpha from primary cultured human fetal membrane chorion and amnion cells infected with influenza virus at protein and bioactivity levels in order to understand the pathology of premature delivery during influenza virus infection. Concentrations of IL-6 and TNF-alpha proteins were significantly increased in culture supernatants of chorion cells by influenza virus infection. Culture supernatants of the virus-infected chorion cells stimulated the proliferation of IL-6-sensitive 7-TD-1 cells and induced the cytolysis of TNF-alpha-sensitive L929 cells, both activities of which were inhibited by the addition of respective antibody, whereas no such phenomena were observed in amnion cells. The results demonstrated that only chorion cells secreted significant amounts of bioactive IL-6 and TNF-alpha proteins responding to influenza virus infection. The present study suggests a possibility that the secretion of bioactive IL-6 and TNF-alpha proteins from fetal membrane chorion cells is implicated in the pathogenesis of premature delivery during influenza virus infection.

Adult↗

PubMed1998

Characterization of hamster recombinant monomorphic and polymorphic arylamine N-acetyltransferases: bioactivation and mechanism-based inactivation studies with N-hydroxy-2-acetylaminofluorene.

The purified hamster recombinant arylamine N-acetyltransferases (NATs), rNAT1-9 and rNAT2-70D, were characterized for their capabilities to bioactivate N-hydroxy-2-acetylaminofluorene (N-OH-AAF) to DNA binding reactants and for their relative susceptibilities to mechanism-based inactivation by N-OH-AAF. The rate of DNA adduct formation resulting from rNAT1-9 bioactivation of [14C]N-OH-AAF was more than 30 times greater than that of rNAT2-70D-catalyzed bioactivation of [14C]N-OH-AAF. This result is consistent with substrate specificity data indicating that N-OH-AAF is a much better acetyl donor for hamster NAT1 than NAT2. Previous studies indicated that N-OH-AAF is a mechanism-based inactivator of hamster and rat NAT1. In the presence of N-OH-AAF, both rNAT1-9 and rNAT2-70D underwent irreversible, time-dependent inactivation that exhibited pseudo first-order kinetics and was saturable at higher N-OH-AAF concentrations. The enzymes were partially protected from inactivation by the presence of cofactor and substrates. The limiting rate constants (ki) and dissociation constants (Ki) for inactivation by N-OH-AAF were determined. The second-order rate constants (ki/KI) were 22.1 min-1 mM-1 for rNAT1-9 and 1.0 min-l mM-1 for rNAT2-70D, indicating that rNAT1-9 is approximately 20 times more susceptible than rNAT2-70D to inactivation by N-OH-AAF. The kinetic parameters for rNAT1-9 were nearly identical to values previously reported for partially purified hamster NAT1. Partition ratios were 504 for inactivation of rNAT1-9 by N-OH-AAF and 137 for inactivation of rNAT2-70D. Thus, a turnover of almost 4 times as many N-OH-AAF molecules is required to inactivate each molecule of rNAT1-9 than is needed to inactivate rNAT2-70D. The partition ratio data are consistent with the finding that rNAT1-9 catalyzes a higher rate of DNA adduct formation by N-OH-AAF than rNAT2-70D. The combined results indicate that the recombinant enzymes are catalytically and functionally identical to hamster NATs and, therefore, will be a useful resource for studies requiring purified NATs.

Animals↗

PubMed1986

Correlation of the bioactivity of luteinizing hormone in follicular fluid with oocyte maturity in the spontaneous cycle.

This study was done to measure the bioactivity of luteinizing hormone (LH) in follicular fluid (FF) and to correlate this and other hormonal values with oocyte maturity in the spontaneous cycle. Twenty follicles (greater than 18 mm) from 18 ovulatory patients were obtained, and FF, according to oocyte maturity, was divided into three groups (I to III) of increasing maturity. FF progesterone correlated with maturity and was highest (P less than 0.01) in group III; estradiol, prolactin, and follicle-stimulating hormone were similar in the three groups. Immunoreactive LH was similar in groups I and II but was highest (30.5 +/- 7 mIU/ml) in group III (P less than 0.02). Bioactive (bio) LH was much higher in group III follicles (1307 +/- 387 mIU/ml); the bio:immunoreactive LH ratio also increased significantly (P less than 0.05). FF progesterone correlated positively with bio LH (r = 0.89, P less than 0.005) and the bio:immunoreactive LH ratio (r = 0.9, P less than 0.001); immunoreactive LH did not correlate. These data suggest that bioactivity of LH is an important correlate of oocyte maturity and that local ovarian factors may modulate these concentrations in FF.

Adult↗

PubMed1991

Luteinizing hormone pulse frequency and in vitro bioactivity in male idiopathic infertility.

We investigated 51 patients with idiopathic oligospermia and 10 control subjects. Blood samples were collected every 20 minutes from 10 P.M. to 10 A.M. and luteinizing hormone (LH) pulsatility was analyzed. A pool of all samples obtained from each subject was used to measure bioactive LH in an in vitro mouse Leydig cell bioassay and immunoactive LH in an immunoradiometric assay. Mean immunoactive LH pulse frequency was higher and mean bioactive to immunoactive LH ratio was lower in infertile men than in controls. There was a significant negative correlation between bioactive LH to immunoreactive LH ratio and LH pulse frequency. These data indicate that the defect in the gonadal axis in oligospermic men resides not in the hypothalamic-pituitary function but rather in the testis itself.

Adult↗

PubMed1988

Secretory dynamics of bioactive and immunoreactive prolactin in polycystic ovary syndrome.

To further investigate prolactin (PRL) secretion in polycystic ovary syndrome (PCO), the authors evaluated immunoreactive (immuno) and bioactive (bio) PRL levels in the basal state and in response to provocative testing with intravenous dopamine (DA), metoclopramide (MCP), and gonadotropin-releasing hormone (GnRH), before and after disulfiram. Basal measurements of immuno-PRL, bio-PRL, and the ratio of bio/immuno-PRL were similar in PCO and controls. The immuno-PRL decrement after DA was greater than that of bio-PRL in both groups (P less than 0.05). After MCP, immuno-PRL increased more than bio-PRL in PCO (P less than 0.01), and this immuno-PRL increment was greater than that of controls (P less than 0.05). Bio-PRL and immuno-PRL increased after GnRH in PCO, but not controls, and these responses were inhibited by disulfiram. These data confirm PRL hypersecretion in some women with PCO, which is better expressed by immunoreactivity than bioactivity. Given the assay systems and patients studied, bioactivity

Adult↗

PubMed2003

Rapid and simultaneous analysis of some bioactive components in Eucommia ulmoides by capillary electrophoresis.

A micellar electrokinetic chromatography method was established for the qualitative and quantitative determination of three groups of bioactive components, iridoids, flavonoids and phenolic compounds, in Eucommia ulmoides. Of the eleven bioactive components being studied, ten were successfully separated in 50 mM boric acid buffer at pH 9.5, with 50 mM sodium dodecylsulfate and 4% 1-butanol, at a voltage of 20 kV, temperature of 20 degrees C and injection under high pressure at 138 kPa for 5 s in a fused-silica capillary with peak detection at 214 nm. A high reproducibility and good linearity was obtained. The relative standard deviations of the migration times in eight injections of the standards ranged from 0.64 to 1.88% and those of the corrected peak area ranged from 2.79 to 6.62%. A good linearity, with correlation coefficients in the range of 0.995-1.000, was obtained in the calibration curves of each standard from 1 to 50 ppm. The amount of these bioactive components in the bark and leaves of Eucommia ulmoides were determined.

Calibration↗

PubMed1980

LH bioactivity increases more than immunoreactivity during puberty.

We have measured bioactive LH in the plasma of 60 normal boys and 45 normal girls throughout puberty because the rise in immunoreactive LH has seemed too small to account for the profound changes in sexual maturation during adolescence. Bioactive LH was determined using an in vitro bioassay (rat interstitial cell testosterone production); I-LH was measured by radioimmunoassay using the same LH standard, LER 907. Bioactive LH was measurable in all 270 plasma samples; I-LH in 218. In both boys and girls, B-LH rose more than I-LH when compared to chronological age, bone age, and pubertal stage. In boys, B-LH increased 8.2-fold (P < 0.001) from prepuberty to late puberty, whereas I-LH rose 3.0-fold (P < 0.001). Similarly, in girls B-LH increased 23.1-fold (P < 0.001) while I-LH increased 4.9-fold (P < 0.001). Between pubertal stages there was less overlap of individual values of B-LH, in comparison to those of I-LH. We conclude that B-LH increases more than I-LH during normal puberty and is a more discriminating measure of maturation. One implication of these findings is that a qualitative change in gonadotropin secretion may occur during puberty.

Adolescent↗

PubMed2001

Bioactivity of 25-hydroxy-, 26-hydroxy, 25,26-dihydroxy- and 25,26-epoxybrassinolide.

The bioactivity of 25-hydroxybrassinolide, (25S)- and (25R)-26-hydroxybrassinolide, (25S)- and (25R)-25,26-dihydroxybrassinolide, and of (25R)-25,26-epoxybrassinolide was tested in the rice leaf lamina inclination assay. The 25- and (25S)-26-hydroxy derivatives are known metabolites of the naturally-occurring phytohormone brassinolide, whereas the other compounds are novel, but closely related, congeners. When tested alone, all showed either no activity or only weak activity at relatively high doses. When coapplied with indole-3-acetic acid (IAA), an auxin that synergizes the effects of brassinosteroids, enhanced bioactivity was observed for each compound. However, even when applied together with IAA, none of the compounds proved more bioactive than brassinolide with or without IAA. We conclude from these results that enzymatic hydroxylation of endogenous brassinolide at C-25 and/or C-26 does not enhance brassinosteroid activity, and so does not comprise an activation pathway in brassinolide biosynthesis. Instead, these hydroxylations result in modest to appreciable metabolic deactivation.

Brassinosteroids↗

PubMed2002

Synthesis and bioactivity of C-2 and C-3 methyl ether derivatives of brassinolide.

The following six novel methyl ether derivatives of brassinolide were prepared and their brassinosteroid activity was measured by means of the rice leaf lamina inclination bioassay: 2-O-methylbrassinolide, 3-O-methylbrassinolide, 2,22,23-tri-O-methylbrassinolide, 3,22,23-tri-O-methylbrassinolide, 2-O-methyl-25-methoxybrassinolide and 3-O-methyl-25-methoxybrassinolide. Brassinolide was used as a standard for comparison. All six compounds were also tested in the presence of 1000 ng of indole-3-acetic acid (IAA), an auxin that synergizes the effects of brassinosteroids. The 2-O-methyl- and 3-O-methylbrassinolide derivatives showed weak activity at high doses, which was enhanced by IAA, especially in the case of the 3-O-methyl derivative. Similarly, the 2,22,23-tri-O-methyl- and 3,22,23-tri-O-methyl derivatives displayed weak bioactivity on their own, but significantly stronger activity when applied with IAA. The 3-O-methyl and 3,22,23-tri-O-methyl analogues plus IAA were comparable in bioacivity to brassinolide alone, but were less active than brassinolide plus IAA. In each case, O-methylation at C-2 resulted in a greater loss of activity than O-methylation at C-3 under the same conditions. The relatively strong activity of 3,22,23-tri-O-methylbrassinolide in the presence of IAA is especially noteworthy as it indicates that free hydroxyl groups at C-3, C-22, and C-23 are not essential for bioactivity. Finally, 2-O-methyl- and 3-O-methyl-25-methoxybrassinolide were essentially inactive alone, and showed only a modest increase in bioactivity when coapplied with IAA.

Biological Assay↗

PubMed2000

Biological and mechanical properties of PMMA-based bioactive bone cements.

We reported previously that a bioactive PMMA-based cement was obtained by using a dry method of silanation of apatite-wollastonite glass ceramic (AW-GC) particles, and using high molecular weight PMMA particles. But handling and mechanical properties of the cement were poor (Mousa et al., J Biomed Mater Res 1999;47:336-44). In the present study, we investigated the effect of the characteristics of PMMA powder on the cement. Different cements containing different PMMA powders (CMW1, Surgical Simplex, Palacos-R and other two types of PMMA powders with Mw 270,000 and 1,200,000) and AW-GC filler in 70 wt% ratio except Palacos-R (abbreviated as B-CMW1 and B-Surg Simp, B-Palacos 50 [50 wt% AW-GC filler] and B-Palacos 70 [70 wt% AW-GC filler], B-270 and B-1200) were made. Dough and setting times of B-CMW1, B-Surg Simp B-270 and B-1200 were similar to the commercial CMW1 cement which did not contain bioactive powder (C-CMW1), but B-palacos which contained large PMMA beads with high Mw had delayed setting time. B-270 had the highest bending strength among the tested cements. After 4 and 8 weeks of implantation in the medullary canals of rat tibiae, the bone-cement interface was examined using SEM. The affinity index of B-1200 was significantly higher than the other types of cements. B-270 showed good combination of handling properties, high mechanical properties and showed higher bioactivity with minimal soft tissue interposition between bone and cement compared with commercial PMMA bone cement. This may increase the strength of the bone-cement interface and increase the longevity of cemented arthroplasties.

Animals↗

PubMed2001

Influence of sol and stage of spinnability on in vitro bioactivity and dissolution of sol-gel-derived SiO2 fibers.

The ability of the sol-gel-derived green state silica fibers to induce the formation of bone-like calcium phosphate (HCA) on their surfaces has not been studied earlier. Bioactive silica fibers provide alternatives for the design of novel products, e.g., as implants used in tissue guiding or bone repairs. In this study, dry spinning was used to prepare the sol-gel fibers. Different fibers with different bulk structures were prepared by changing the composition and controlling the stage of spinnability. Additionally, the influence of the aging time of the fibers on the bulk structure of the samples was investigated. Furthermore, the ability to form calcium phosphate was investigated in vitro in the simulated body fluid (SBF). Transmission electron microscopy was used to illustrate the bulk structure of the green state fibers and scanning electron microscopy to illustrate the formed calcium phosphate layer on the fibers. The fibers were additionally characterized by measuring the dissolution of the silica in the SBF. In vitro bioactive silica fibers were successfully prepared. The calcium phosphate layer was formed within 1-5 days in the best case. The structural stability and the in vitro bioactivity varied with the aging time expect in one case where practically stable fibers could be prepared. The concentration of silica released in the SBF had no direct connection with the HCA formation. The silica-rich gel layer was not observed on the fibers, but the structure of the fibers was suggested to have an important role in the HCA formation.

Microscopy, Electron↗

PubMed2001

Role of acid attack in the in vitro bioactivity of a glass-ceramic of the 3CaO.P2O5-CaO.SiO2-CaO.MgO.2SiO2 system.

A non-bioactive glass-ceramic (GC13) that contains hydroxyapatite (Ca5(PO4)3OH), diopside (CaMg(SiO3)2) and althausite (Mg2 PO4OH) as crystalline phases has been obtained by thermal treatment of a parent bioactive glass (G13) of nominal composition (wt%) 40.0 CaO-34.5 SiO2-16.5 P2O5-8.5 MgO-0.5CaF2. To induce bioactivity, GC13 was chemically treated with 1 M HCl for different periods of time. After chemical etching the in vitro studies showed formation of an apatite-like surface layer. In this article the influence of etching time both on the surface composition of the glass-ceramic and on the growth rate of the apatite layer is studied. It is concluded that the presence of hydroxyapatite in the glass-ceramic, associated to microstructural fluctuations, can favour apatite deposition in vitro.

Apatites↗

PubMed2002

Preparation and in vitro bioactivity of hydroxyapatite/solgel glass biphasic material.

Hydroxyapatite/solgel glass biphasic material has been obtained in order to improve the bioactivity of the hydroxyapatite (OHAp). A mixture of stoichiometric OHAp and the precursor gel of a solgel glass, with nominal composition in mol% CaO-26, SiO2-70, P205-4, has been prepared. The amounts of components used have been selected to obtain a final relationship for OHAp/solgel glass of 60/40 on heating. Two different thermal treatments have been used: (i) 700 degrees C, temperature of solgel glass stabilisation and (ii) 1000 degrees C, lower temperature of hydroxyapatite sintering. The bioactivity of the resulting materials has been examined in vitro by immersion in simulated body fluid at 37 degrees C. The results obtained show that both materials are bioactive. The apatite-like layer grown is greater for the new materials than for the OHAp and the solgel glass themselves.

Calcium Compounds↗

PubMed2002

Development of a sensitive whole blood chemiluminescence method for assessing the bioactivity of calcium phosphate powders.

The development of simple, but highly sensitive and accurate in vitro methods for assessing the bioactivity of biomaterials is a key requirement for assuring their successful clinical application. Moreover, screening techniques that will allow various materials to be recommended, or otherwise, for further testing, have the potential to make appreciable savings in the time and expense associated with product development. This paper gives details of a novel whole blood chemiluminescence method, based on the photoprotein Pholasin, which emits light in the presence of the free radical superoxide. other reactive oxygen species and the enzyme myeloperoxidase. This whole blood assay may have the potential as a screening method for assessing calcium phosphate (Ca-P) bioceramic powders according to their relative bioactivity. The method employed involves exposure of samples of anti-coagulated (heparinised) blood to the various Ca-P materials and stimulating the contacted leukocytes in the blood with phorbol-12-myristate-13-acetate (PMA). PMA stimulates protein kinase C directly and sets in motion a cascade of events in the leukocytes leading to the activation of the superoxide generating NADPH oxidase system. PMA also promotes degranulation, which is the fusion of the granule membrane with the plasma membrane and the extracellular release of granule enzymes. Changes in the free radical and degranulation activity of the cells, as measured by the luminescent response of Pholasin to cells stimulated with PMA, after exposure to the Ca-P powders, are presented as percentage differences from the response to (control) blood samples not exposed to the powders. The resultant data clearly indicate significant differences in the light detected via Pholasin from the blood exposed to the bioceramic materials compared to that from the relevant controls. These differences correlate well with the ascribed bioactivity of the Ca-P powders. as assigned from the measured chemical and structural properties. Furthermore, the method can also be applied to samples of blood, which have been diluted in the ratio 1:100 in standard blood dilution buffer. The light output response in the diluted blood experiments is exactly the same as that observed with undiluted whole blood but occurs immediately as compared to the many minutes required to give response in the latter case. Thermally processed (800 degrees C) Ca-P materials have also been studied. A relationship between the heat-induced properties of the powders and the chemiluminescence responses recorded from blood cells stimulated with PMA has been established.

Biocompatible Materials↗

PubMed2002

Preparation of a bioactive and degradable poly(epsilon -caprolactone)/silica hybrid through a sol-gel method.

A bioactive and degradable poly(epsilon -caprolactone)/silica hybrid was synthesized for the application as a bone substitute. Triethoxysilane end capped polyepsilon -caprolactone) was prepared by the reaction with alpha,omega-hydroxyl poly(epsilon -caprolactone) and 3-isocyanatopropyl triethoxysilane using 1,4-diazabicyclo[2,2,2,]octane as a catalyst. It was then co-condensed with tetraethyl orthosilicate and calcium nitrate tetrahydrate via a sol-gel method. The bioactivity of the poly(epsilon -caprolactone)/silica hybrid was assessed using simulated body fluid and low crystalline apatite was successfully formed on its surface after soaking for 1 week at 36.5 degrees C. Its biodegradability was evaluated in the phosphate buffered saline and the degradability was mostly come from the poly(epsilon -caprolactone) phase in the hybrid. It means that this hybrid is likely to be applicable to a bioactive and degradable bone substitute.

Biocompatible Materials↗