PubMed Health⌕ Search

SEARCH · PubMed Health

Results for “Bioactivation”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 865 records · Page 48Linked to original sources

Reaction of organic nitrate esters and S-nitrosothiols with reduced flavins: a possible mechanism of bioactivation.

Organic nitrate esters, such as glyceryl trinitrate and isosorbide dinitrate, are a class of compounds used to treat a variety of vascular ailments. Their effectiveness relies on their ability to be bioactivated to nitric oxide (NO) which, in turn, relaxes vascular smooth muscle. Although there have been many biological studies that indicate that NO can be formed from organic nitrate esters in a biological environment, the chemical mechanism by which this occurs has yet to be established. Previous studies have implicated both flavins and thiols in organic nitrate ester bioactivation. Thus, we examined the chemical interactions of flavins and thiols with organic nitrate esters as a means of determining the role these species may play in NO production. Based on these studies we concluded that a reasonable chemical mechanism for organic nitrate ester bioactivation involves reduction to the organic nitrite ester followed by conversion to a nitrosothiol. The release of NO from nitrosothiols can occur via a variety of processes including reaction with dihydroflavins and NADH.

Biotransformation↗

Effective stimulation for IL-12 p35 mRNA accumulation and bioactive IL-12 production of antigen-presenting cells interacted with Th cells.

Bioactive IL-12 is composed of two subunits, p35 and p40. In the APC-Th cell interaction, p40 mRNA accumulation in APC was shown to be up-regulated by stimulation with CD40 ligand (CD40L) on Th cells. However, the CD40-CD40L interaction scarcely induced p35 mRNA accumulation in APC. In the present experiments, p35 mRNA accumulation was induced in splenic macrophages/dendritic cells by the interaction with paraformaldehyde-fixed Th1 cells in the presence of Ag, and the p35 mRNA accumulation was abrogated by the inclusion of anti-I-A in cultures to block TCR/MHC class II interaction. The accumulation was also induced by the stimulation with agonistic anti-I-A. These results indicate that the interaction of the MHC class II molecule with TCR evokes an activation signal for p35 mRNA accumulation in APC. Furthermore, the production of bioactive IL-12 in macrophages/dendritic cells stimulated with CD40L was enhanced by the inclusion of agonistic anti-I-A. The p35 mRNA accumulation and IL-12 production of macrophages/dendritic cells induced by stimulation with OVA-specific fixed Th1 clone expressing CD40L were also enhanced by adding OVA in cultures. These results indicate that the p35 mRNA accumulation induced by MHC class II stimulation plays a role in bioactive IL-12 production.

Animals↗

Nutritional and biochemical properties of human milk: II. Lipids, micronutrients, and bioactive factors.

Human milk lipids contain preformed LCPUFA in considerable amounts, which serve as precursors for the formation of prostaglandins, prostacyclins, and other lipid mediators, as well as essential components in membrane-rich tissues (such as the brain and the retina), thus affecting functional outcomes. Besides a balanced nutrient composition and a number of conditionally essential nutrients, human milk provides different types and classes of bioactive factors, such as enzymes, hormones, and growth factors, many of which appear to have a role in supporting infantile growth and development. The bioactive agents include antimicrobial factors (e.g., secretory IgA, oligosaccharides, FA); anti-inflammatory agents; transporters (e.g., lactoferrin); and digestive enzymes (e.g., BSSL). Several nonpeptide hormones (thyroid hormones, cortisol, progesterone, pregnanediol, estrogens, and artificial contraceptive) and peptide hormones and growth factors (erythropoietin, hHG, gonadotropin-releasing hormone, epidermal growth factor insulin, insulin-like growth factor-I, nerve growth factor, transforming growth factor-alpha, gastrointestinal regulatory peptides and thyroid-parathyroid hormones) have been isolated and quantitated in human milk. Some of these components are also involved in the maturation of the gastrointestinal tract of the infant. In addition to the passive benefits provided by human milk, several data support the hypothesis that breastfeeding promotes the development of the infant's own immune system, which might confer long-term benefits for the newborn infant. The risk of IDDM, Crohn's disease, and atopic disease is lower in individuals who had been breastfed during infancy. Areas of major interest in human milk research include the study of human milk synthesis and the contributions of dietary composition and maternal metabolism to human milk composition, infantile utilization of human milk components, and the study of bioactive components, such as oligosaccharides, proteins and peptides, and lipids and their in vivo fate and biologic effects in the recipient infant.

Female↗

Early renal ischemia, with or without reperfusion, activates NFkappaB and increases TNF-alpha bioactivity in the kidney.

PURPOSE: Acute tubular necrosis (ATN) and the ensuing renal failure induced by ischemia and reperfusion injury (I/R) remain a major cause of morbidity and mortality among patients in the intensive care unit. Although it is well established that exogenous tumor necrosis factor-alpha (TNF) induces renal injury, it remains unknown whether ischemia and/or reperfusion activates the signaling mechanisms required for renal TNF production. We hypothesized that ischemia and/or reperfusion would activate the oxidant sensitive TNF transcription factor, nuclear factor kappa B (NFkappaB), and thereby lead to renal TNF production. MATERIALS AND METHODS: Male Sprague-Dawley rats were anesthetized with sodium pentobarbital, after which various periods of renal ischemia, with or without reperfusion, were induced in rats. At different time intervals, kidneys were harvested and NFkappaB activation (electrophoretic mobility shift assay), TNF mRNA content (RT-PCR), and TNF bioactivity (WEHI-164 cell clone cytotoxicity assay) were determined. RESULTS: Results indicate that 15 minutes of ischemia alone activates NFkappaB, whereas peak activation occurred at 30 minutes of ischemia alone. NFkappaB remained activated through 60 minutes reperfusion. Thirty minutes of ischemia is required to induce renal TNF mRNA production; however, renal TNF protein expression and bioactivity peaked following 1 hour of ischemia and 2 hours reperfusion. CONCLUSIONS: These results are the initial demonstration that renal ischemia, with or without reperfusion, activates the TNF transcription factor NFkappaB and increases TNF bioactivity in the kidney.

Animals↗

Secretion of bioactive interleukin-1beta by dendritic cells is modulated by interaction with antigen specific T cells.

The role of interleukin-1beta (IL-1beta) as a regulator of the immune response, although extensively investigated, is still debated. We then studied the expression of IL-1beta by human dendritic cells (DCs), the professional antigen presenting cells, and its modulation during immune reactions in vitro. Our results show that, on maturation or tetanus toxoid presentation to specific CD4(+) CD40L(+) T lymphocytes, DCs begin to accumulate IL-1beta precursor (pro-IL-1beta) but do not secrete bioactive IL-1beta. In contrast, interaction with alloreactive T cells results in both stimulation of pro-IL-1beta synthesis and secretion of processed isoforms of the cytokine, that display biologic activity. Both CD4(+) and CD8(+) subsets of allospecific T lymphocytes are required: CD4(+) T cells drive the synthesis of pro-IL-1beta through CD40 engagement but have no effects on pro-IL-1beta processing; CD8(+) T cells, unable to induce synthesis of pro-IL-1beta per se, are responsible for the generation of mature IL-1beta by pro-IL-1beta-producing DCs. Interleukin-1beta-converting enzyme (ICE) inhibitors do not prevent the recovery of IL-1beta bioactivity after allorecognition, indicating that allospecific CD8(+) T cells may induce the release of bioactive IL-1beta via mechanism(s) other than ICE activation. Altogether, these findings suggest that CD4(+) and CD8(+) T-lymphocyte subsets have distinct roles in the induction of IL-1beta secretion by DCs and support the hypothesis that IL-1beta plays a role in cell-mediated immune responses. (Blood. 2000;95:3809-3815)

CD4-Positive T-Lymphocytes↗

Retro-inverso prosaptide peptides retain bioactivity, are stable In vivo, and are blood-brain barrier permeable.

Prosaptide (trademark of Myelos Corporation, San Diego, CA) peptides are based on the 14-amino-acid neurotrophic sequence of human prosaposin and, like the parent protein, have potent neurotrophic and neuroprotective properties. We previously examined the in vivo stability of a series of bioactive Prosaptide peptides and designed peptides with increased enzymatic stability in the central and peripheral nervous systems. In this article, we examined the stability, biological activity, and permeability of the blood-brain barrier to retro-inverso Prosaptide peptidomimetics. Retro-inversion both reverses the primary sequence and replaces L-amino acids with D-amino acids. We examined the bioactivity of five peptidomimetics, Prosaptides D1-D5. Prosaptide D1, a peptide containing all D-amino acids with the primary sequence intact, was inactive. However, four retro-inverso peptidomimetics, Prosaptides D2-D5 retained bioactivity in neurite outgrowth and [(35)S]GTPgammaS binding assays. We focused on Prosaptide D4 as a prototypical retro-inverso Prosaptide peptidomimetic for further study. (125)I-Prosaptide D4 remained intact in brain or serum for 60 min after i.v. administration and was transported across the blood-brain barrier with a unidirectional influx constant of 2.5 x 10(-4) ml. g(-1). min(-1). We conclude that retro-inverso Prosaptide peptidomimetics are excellent candidates for development as therapeutics for central nervous system neurodegeneration.

Amino Acid Sequence↗

The role and clinical applications of bioactive lysolipids in ovarian cancer.

OBJECTIVE: To review the current understanding of the role of bioactive lysolipids in ovarian cancer and their potential clinical applications. METHODS: A MEDLINE search and our own work, including some unpublished work, are the major sources of the review. The MEDLINE search terms used included lysophosphatidic acid, lysophophatidylcholine (LPC), lysophosphatidylinositol (LPI), sphingosine-1-phosphate, and sphingosylphosphorylcholine (SPC). RESULTS: Elevated lysolipid levels were detected in plasma and ascites samples from patients with ovarian cancer compared with samples from healthy controls or patients with nonmalignant diseases. These lysolipids regulate growth adhesion, production of angiogenic factors, and chemotherapeutic drug resistance in ovarian cancer cells. Ovarian cancer cells were likely to be at least one of the sources for elevated lysolipid levels in the blood and ascites of patients with ovarian cancer. CONCLUSIONS: Bioactive lysolipid levels might be sensitive markers for detecting gynecologic cancers, particularly ovarian cancer. The prognostic value of lysolipids in ascites is worth further investigation. Bioactive lysolipid molecules can affect both the proliferative and metastatic potentials of ovarian cancer cells; therefore, regulation of the production or degradation of these lipids and interception of the interaction between these lipids and their receptors could provide novel and useful preventative or therapeutic measures.

Cell Adhesion↗

[Effect of fibrin on osseointegration of bioactive glass-ceramic materials--experimental study].

PURPOSE OF THE STUDY: The aim of the experimental study is to find out how fibrin influences the speed of osteiontegration of bioactive glass-ceramic materials BAS-O, BAS-HA, BAS-R (LASAK Prague, Czech Republic) and how it influences the response of live tissue at the implant-bone interface in the interval of 1-8 weeks. MATERIAL: Dense materials BAS-0 (glass-ceramics), BAS-HA (hydroxyapatite) and BAS-R (beta tricalcium phosphate) in the form of 0.6-1 mm granules were implanted in artificially created defects in tibia of an experimental animal with the addition of 0.1 ml of fibrin adhesive system Beriplast. Control implantation was performed with the addition of physiological solution. Materials BAS-HA and BAS-R were implanted in the same way in the ratio of 7:3, 8:2 and 9:1. Duration of exposure was 1-8 weeks. Radiographs of samples were taken by Mammograph and decalcified sections were coloured by toluidine blue and examined at 60 times and 120 times magnification. RESULTS: Surgical wounds were healed per primam. Radiographs of materials with the fibrin system showed clearly after one week defects and implants, after the third week part of the materials penetrated above the bone surface, after the fourth week there were evident signs of bone tissue formation between particles of BAS-HA, BAS-R and their mixtures. The most marked bone formation took place in the seventh and eighth weeks. With the use of glass-ceramics without fibrin the particles were after three weeks less clear, after the fourth week BAS-HA and BAS-R penetrated above the surface. A significant bone formation was obvious after the sixth and seventh weeks. There were no signs of resorption or fibrous encapsulating. Microscopic examination proved enveloping of particles of BAS-0 by fibrous tissue which was evident partially also after the eight week. With the use of fibrin the situation was analogical. In BAS-HA and BAS-R the finding in the first week was similar. With fibrin, there was after the third week a mature lamellar bone in the vicinity of granules and the fibrous interlayer disappeared. Neither positive nor negative impact of fibrin on the process of healing was found. With the application of BAS-R and fibrin system the bone tissue was after the third week more significant and trabeculae more bulky. The final result after eight weeks was the same: Ingrowth of the mixtures of the given materials proceeded in the same way. DISCUSSION: The applied glass-ceramic materials are used in the clinical practice. The speed of osteointegration depends on the quality of the bone bed, and on the tolerance of these materials by live tissue. Osteintegration can be accelerated by the use of growth factors or stem cells cultivated in the tissue culture. Fibrin which creates a network along which osteoblasts can migrate should have a similar quality. It seems that of decisive importance is the thickness of the fibrin layer around the implants. If this layer is thick glass-ceramics is enveloped more probably to fibrous tissue. In a thin layer the process is accelerated within the first three weeks. After a longer exposure the differences are not evident. Samples of BAS-HA and BAS-R, both applied separately and in a mixture, showed a marked bioactivity in the experiment. During eight weeks no signs were found of resorption which is typical of tricalcium phosphate in a longer time interval. CONCLUSION: In the experiment on an animal the fibrin adhesive system accelerated osteointegration of bioactive materials BAS-HA, BAS-R and their mixtures until the third week after the implantation. Small differences with the use of fibrin were adjusted within six weeks. Materials BAS-HA, BAS-R and their mixtures were completely osteointegrated. Glass-ceramics BAS-0 was partially enveloped by fibrous tissue, even with the use of fibrin adhesive system. During eight weeks no resorption of materials was found. The process of ingrowth can be seen on radiographs. X-ray picture of bone formation in BAS-HA, BAS-R correlates with the histological finding. The fibrin adhesive system facilitates manipulation with fine granules.

Animals↗

Apatite formation on bioactive zirconium metal prepared by chemical treatment.

Bioactive metallic materials, which can directly bond to living bone, are badly needed in dental and orthopedic implants for better long-term results. Forming a layer of bone-like apatite on the surface of the metal is one of the most promising methods to increase its bioactivity. This study creates a new chemical treatment for zirconium metal to induce apatite formation in a simulated body fluid (SBF), and analyzes the apatite layer by using scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDS), and Fourier transform infrared spectroscopy (FTIR). Zirconium samples were soaked in 10% CuCl2 aqueous solution at 80 degrees C for 72 hours, heat-treated at 500 degrees C for one hour and soaked in SBF for various periods. An apatite-like layer appeared on the zirconium surface as early as three days in SBF, and increased with immersion time. EDS and FTIR confirmed that the deposited layer was apatite. This implies that bioinert zirconium metal can become bioactive by forming an apatite layer in a simulated body fluid after a suitable chemical treatment. The ZrOOH+ hydrogel layer produced on the zirconium surface by CuCl2 and heat-treatments is thought to induce the apatite formation.

Apatites↗

Curcumin activates the aryl hydrocarbon receptor yet significantly inhibits (-)-benzo(a)pyrene-7R-trans-7,8-dihydrodiol bioactivation in oral squamous cell carcinoma cells and oral mucosa.

The development of oral squamous cell carcinoma (SCC) shows a positive correlation with the carcinogen exposure that occurs during tobacco and alcohol use. The purpose of this study was to investigate whether the naturally occurring chemopreventive agent, curcumin, modulates expression and function of carcinogen- metabolizing enzymes in human keratinocytes isolated from oral SCC tumors. Dose-response studies demonstrated that curcumin concentrations of >or=25 micro M were cytotoxic for oral SCC cells. Curcumin increased both expression (reverse transcription-PCR analyses) and function (high-performance liquid chromatography determination of ethoxyresorufin metabolism) of cytochrome P-450 (CYP) 1A1 and/or CYP1B1. The aryl hydrocarbon receptor (AhR), which up-regulates a battery of genes associated with carcinogen metabolism, is activated by polycyclic aromatic hydrocarbons such as the tobacco-associated carcinogen benzo(a)pyrene. Electromobility shift assays demonstrated that similar to the established AhR ligand 2,3,7,8,-tetrachlorodibenzo-p-dioxin, curcumin inclusion resulted in AhR nuclear translocation and formation of the transcriptionally active AhR-aryl hydrocarbon receptor nuclear translocator complex. Cellular capacity to bioactivate the tobacco-associated carcinogen (-)-benzo(a)pyrene-7R-trans-7,8-dihydrodiodiol was determined by evaluating conversion of the carcinogenic metabolite diol epoxide to stable tetrols via high-performance liquid chromatography. Results of our metabolism studies showed that curcumin significantly inhibited CYP1A1-mediated benzo(a)pyrene diol bioactivation in both oral SCC cells and intact oral mucosa. Because CYP1A1 is one of the primary carcinogen-activating enzymes in oral mucosa, the use of curcumin as an oral cavity chemopreventive agent could have significant clinical impact via its ability to inhibit carcinogen bioactivation.

Adult↗

[Synthesis of droloxifene citrate and its new bioactivity].

AIM: To investigate a feasible synthetic procedure of droloxifene and study on its new bioactivities. METHODS AND RESULTS: Droloxifene was synthesized using methoxybenzene and phenylacetic acid as starting materials, via Friedel-Crafts acylation, alkylation, demethylation, etherification, Grignard addition, elimination-dehydration, conversing configuration and forming citrate, totally 8 steps, overall yield 14.7% (9.2%). By pharmacological test, droloxifene citrate shows two new bioactivities: (1) obvious effect on reversing the MDR of K562/A02 cells and modulating mdrl, GST pi and TopoII alpha expression. (2) inducing apoptosis in cultured rat luteal cell. CONCLUSION: The improved synthetic procedure is shorter than the reported method by two steps and has advantages of simple separation, purification and conversion of configuration; easily available starting materials and reagents; concise operation. Two new bioactivities on reversing MDR and inducing apoptosis of luteal cell offered a clue in new drugs research and widened clinic application of droloxifene.

Animals↗

Clinical and histologic evaluation of bone-replacement grafts in the treatment of localized alveolar ridge defects. Part 2: bioactive glass particulate.

The purpose of this study was to evaluate the feasibility of using a bioactive alloplast and a physical barrier to augment localized alveolar ridge defects for the subsequent placement of dental implants. Twelve systemically healthy patients (aged 29 to 55 years) with inadequate dental alveolar ridge widths were selected for study. All patients completed initial therapy, which included scaling, root planing, and oral hygiene instruction. All ridge defects were augmented with a bioactive glass alloplast and a titanium-reinforced e-PTFE barrier. Vertical (height) and horizontal (width) hard tissue measurements were taken the day of ridge augmentation surgery (baseline) and at the 6-month reentry surgery. The change in ridge width varied from a loss of 1 mm to a gain of 4.5 mm, with a mean gain of 1.1 mm (P < .03). Eight of the 12 sites gained 1 mm or less. The difference in mean ridge width gain between maxillary and mandibular sites was not statistically significant (P > .08). Mean ridge width gain was 1.1 mm for both maxillary and mandibular sites. There was a loss in bone height of 0.3 mm from baseline. Four implants in four patients could not be placed because of inadequate ridge width augmentation. Histologic examination of the grafted sites revealed connective tissue encapsulation of most residual graft particles. In this study, bioactive glass particulate and an e-PTFE barrier did not consistently augment localized ridge defects for dental implant placement.

Adult↗

Identification of cytochrome P-450IIB1 as a cocaine-bioactivating isoform in rat hepatic microsomes and in cultured rat hepatocytes.

Induction of cytochrome P-450-dependent monooxygenases with phenobarbital (PB) or other hepatic drug-metabolizing enzyme inducers in the rat is associated with enhanced cocaine hepatotoxicity both in vivo and in cultured rat hepatocytes. To demonstrate whether the major PB-inducible P-450 subfamily (P-450IIB) could be involved in the metabolic activation of cocaine, rates of cocaine N-demethylation (the first step of cocaine bioactivation) and the rate of irreversible (covalent) binding of tritiated cocaine to hepatic microsomal proteins (a measure for the overall bioactivation) were determined in microsomes from saline or PB-pretreated rats. PB pretreatment augmented Vmax (6-fold), but not KM, of cocaine N-demethylation. Similarly, the rate of irreversible protein binding was 3-fold increased in microsomes from PB-pretreated rats as compared with those from saline controls. Addition of benzphetamine, a substrate of P-450IIB, markedly inhibited cocaine irreversible binding. In addition, various concentrations of cocaine inhibited microsomal pentoxyresorufin O-depentylase activity in a competitive-type pattern. A polyclonal antibody raised against purified rat P-450IIB1 markedly inhibited cocaine N-demethylation as compared with control incubations with preimmune IgG. Finally, pretreatment of rats with PB potentiated cocaine-induced cytotoxicity in primary, short-term cultured hepatocytes, assessed as lactate dehydrogenase release into the culture medium. This enhancing effect of PB became even more evident in glutathione-depleted cells. These results suggest that cocaine is metabolized and bioactivated by P-450IIB1 in the rat liver, and that induction of this isoform with various agents may be associated with enhanced lethal hepatocyte injury in the rat.

Animals↗

[Expression and bioactivity analysis of the fusion protein GFP-V(L) of the neutralizing monoclonal antibody MA18/7 against HBV].

AIM: To express the fusion protein of enhanced green fluorescent protein (EGFP) with the light chain variable domain of the neutralizing monoclonal antibody MA18/7 (mAb) against hepatitis B virus in E.coli, and determine its bioactivity. METHODS: The EGFP gene was cloned into vector pTO-T7 to construct an expression vector. And then according to ORF gene, MA18/7-V(L) was inserted into the 5' terminal of EGFP gene free of terminal code TAA to construct expression vector of fusion protein. The fusion protein was expressed in E.coli and its bioactivity was detected with ELISA and relative fluorescence intensity. RESULTS: The expression vector EGFP-V(L) was constructed. SDS-PAGE analysis showed that expressed fusion protein was mainly in the form of inclusion body. The fusion protein retained the property of EGFP and it could bind to V(H) to form Fv which had binding activity to pre-S1. CONCLUSION: The obtained fusion protein had good bioactivity and could be applied to further studies.

Antibodies, Monoclonal↗

Bioactivation of 1,1-dichloroethylene to its epoxide by CYP2E1 and CYP2F enzymes.

1,1-Dichloroethylene (DCE) exposure to mice elicits lung toxicity that selectively targets bronchiolar Clara cells. The toxicity is mediated by DCE metabolites formed via cytochrome P450 metabolism. The primary metabolites formed are DCE epoxide, 2,2-dichloroacetaldehyde, and 2-chloroacetyl chloride. The major metabolite detected is 2-S-glutathionyl acetate [C], a putative conjugate of DCE epoxide with glutathione. In this investigation, studies were undertaken to test the hypothesis that CYP2E1 and CYP2F2 are involved in bioactivation of DCE to the epoxide in murine lung. We have developed a method using liquid chromatography/mass spectrometry (LC/MS) to evaluate the kinetics of the rates of production of conjugate [C] by recombinant CYP2E1 and CYP2F enzymes and lung microsomes. Concentration-dependent formation of conjugate [C] was found in incubations of DCE with recombinant CYP2E1 and CYP2F enzymes and lung microsomes from CD-1, wild-type (mixed 129/Sv and C57BL), and CYP2E1-null mice. Recombinant rat CYP2E1 exhibited greater affinity and catalytic efficiency for DCE metabolism than did recombinant human CYP2E1, mouse CYP2F2, goat CYP2F3 or rat CYP2F4. In the lung microsomal incubations, the rates of conjugate [C] production were higher in CD-1 mice than in either wild-type or CYP2E1-null mice; the level of [C] in CYP2E1-null mice was about 66% of that in wild-type mice. These results demonstrated that LC/MS analysis is a suitable method for detection and quantitation of conjugate [C], and that CYP2E1 and CYP2F2 catalyze the bioactivation of DCE to the epoxide in murine lung. The results also demonstrated that CYP2E1 is the high-affinity enzyme involved in DCE bioactivation.

Acetaldehyde↗

[Treatment of juvenile bone cysts by curettage and filling of the cavity with BAS-0 bioactive glass-ceramic material].

PURPOSE OF THE STUDY: The aim of the study was to evaluate the long-term results of using the bioactive, glass-ceramic material BAS-0 for bone tissue replacement after removal of juvenile bone cysts by curettage. MATERIAL: Between 1990 and 2000, BAS-0 material was used to fill the cavity after removal of a juvenile bone cyst in 21 patients, 15 males and 6 females, with an average age of 15 years (range 4 to 44 years). Surgical treatment was indicated only in juvenile bone cysts meeting the following criteria: 1) subjective complaints, i. e., pain at activity; 2) X-ray findings of either a) thinning cortical layer with a potential for pathological fracture, particularly in the proximal femur, b) recurrent pathological fractures without apparent healing of the cyst or c) increase in cyst size by 25% within 6 months. In all patients, the diagnosis of a juvenile bone cyst was confirmed by histological examination. Cyst localization was as follows: eight in the humerus, eight in the femur, two in the fibula and one in the ulna, iliac bone and tibia each. METHODS: After careful curettage of a soft tissue lining from the inner surface of the cystic cavity, the space was filled completely with 2- to 4-mm BAS-0 granules in 15 patients; in the rest granules were applied in a mixture with cancellous bone graft, which was either autologous or allogenic. The former was implanted in one patient, the latter, taken from either the mother or father, was used in four and one patients, respectively. All patients were clinically and radiologically examined during the follow-up period of 3 to 12 years, with an average of 7 years. The clinical evaluation was based on subjective complaints, and on the state of soft tissues in the region of lesion, range of motion in the adjacent joints and the loading capacity of the limb treated. Radiological evaluation was based on standard X-ray images assessed according to the classification system of Neer. RESULTS: The clinical examination showed that 10 patients were free from subjective complaints, one patient had rest pain, three patients experienced pain when using the limb, four patients reported mild and intermittent pain, two patients were in pain when the whether changed and one patient complained of pain during pregnancy. Objectively, no inflammatory changes of soft tissues were found. Both passive and active motion of the adjacent joints was possible in the full range and the treated limb retained its complete function in all patients. X-ray examination showed excellent results, i. e., no residuum or cysts recurrence, in 16 patients. A residual lesion was present in one patient and cyst recurrence was recorded in four patients. DISCUSSION: The currently used methods of treatment include corticoid instillation in the cyst, injection of autologous bone marrow, multiple drilling and drainage of the cyst and removal of the cyst with subsequent filling of the cavity with bone graft. In our patients, the bioactive, glass-ceramic material BAS-0 was used to replace either autogenous or allogenic bone grafts. Complete healing of the cyst was achieved in 76% of our patients, which is the result comparable with the literature data. CONCLUSIONS: Although the therapy of juvenile bone cysts has changed from extensive surgical procedures to less invasive techniques, the curettage of a cyst with subsequent filling of the residual cavity still remains the method of choice in selected patients. Instead of autogenous cancellous bone grafts or allogenic grafts predominantly used for this procedure, the bioactive, glass-ceramic material BAS-0 can be recommended, particularly when the cavity to be filled is located in the metaphysis of a long bone, i. e., in the region subject to great compression.

Adolescent↗

[Review of bioactivities of natural cycloartane triterpenoids].

Cycloartane triterpenoids, which exist widely in nature, are mainly distributed in Astragalus (Leguminosae) species, Trib. Cimicifuga (Ranunculaceae) and Thalictrium (Ranunculaceae) species and possess various bioactivities. Along with the development of isolation techniques of phytochemistry, more and more this kind of compounds are isolated and identified. However, bioactivity researches on the compounds are relatively lagged behind. Most researches are still in screening level, deficient in mechanism elucidation, short of action proven in vivo and SAR analysis. The author summarized the bioactivity of this kind of compounds from all aspects: anti-tumor, anti-virus, antibacterial, anti-inflammation, immune-regulatory, cardiovascular system, hepatic protection and so forth. This will be benefit for the further research and development of the compounds.

Animals↗

[Establishment of a novel preliminary screening model for bioactive parts of folium of Isatis indigotica based on biothermodynamics].

OBJECTIVE: To apply a novel method for screening the bioactive parts and substances of traditional Chinese medicines (TCM) based on biothermodynamic theories. METHOD: The power-time curves of Escherchia coli proliferation at different concentrations of decoction and its five bioactive parts of folium of Isatis indigotica (FII) were determined by TAM Air Isothermal Calorimeter. The growth rate constants of promotive and inhibitory actions were calculated. Moreover, the potential pharmacological action of FII was analyzed from the point of view of TCM theory. RESULT: The growth rate constant k1 and Pm of the studied bacterium in the presence of the decoction of FII were concentration-dependant. The k1 and Pm increased with the mass increase of the decoction and its water-extract of FII. However, the value of k1 and Pm decreased with the increasing concentrations of its other four organic solvent parts. The experimental results revealed that the sequence of inhibitory activity of different extracts was n-BuOH extract > EtOAc extract > chloroform extract > PE extract. CONCLUSION: The decoction and its water-extract of FII stimulated the metabolism of E. coli. While the other four organic solvent extracts of the total decoction inhibited the growth of tested bacterium. The microcalorimetric method has many virtues such as extensive applicability, convenience, etc, and provides a new and useful means for primary screening the bioactive parts and substances of TCM.

Anti-Bacterial Agents↗