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Biological Activity (biological + activity)
Kinds of Biological Activity Selected AbstractsEVALUATION OF EXTRACTS FROM BAMBOO FOR BIOLOGICAL ACTIVITY AGAINST CULEX PIPIENS PALLENSINSECT SCIENCE, Issue 4 2004Hai-qun Cao Abstract The extracts from 7 species of bamboo were tested for larvicidal activity against Culex pipiens pallens. At the tested concentration, the extracts of selected bamboo had different degree of toxic effects on the fourth instar larvae of Culex pipiens pallens. Among them, the extracts of Pleioblastus juxianensis, Brachystachyum albostriatum, Phyllostachys platyglossa and Pleioblastus amarus were found to be effective with LC50values at 24 h of 30.65 mg/L, 53.94 mg/L, 41.21 mg/L and 54.49 mg/L respectively, against Culex pipiens pallens larvae. The extract of Pleioblastus juxianensis by Soxhlet method showed stronger activity than the extract obtained by interval-shaking, the LC50 of which were 30.65 mg/L and 48.34 mg/L, respectively. The diethyl ether extract of Pleioblastus juxianensis exhibited better larvicidal activity than the methanol extract and the petroleum ether extract. The results would help to provide the basis for the study of environment acceptable pesticide for mosquito control, and also help to comprehensively utilize the source of bamboo. [source] BIOLOGICAL ACTIVITY OF EXTRACT OF STELLERA CHAMAEJASME AGAINST FIVE PEST INSECTSINSECT SCIENCE, Issue 3 2002WANG Ya-wei Abstract Biological activity of an extract of the root of Stellera chameajasme with ethanol by dip (SCEE) against 5 insect pests, Pieris rapae, Plutella xylostella, Spodoptera litura, Myzus persicae, and Ostrina fumalis as tested. The LD, of stomach poison of SCEE against the fifth instar larvae of P. rapae was 12. 32 ,arvae day 2 after treatment. With SCEE at concentration of 5, 2. 5 and 50 mg/mL, the fifth instar larvae of P. rapae, the third instar larvae of P. xylostella, and the third instar larvae of S. litura by disc leaf dipped method, had corrected mortalities of 100%, 31. 03 % and 16. 67 % 7 days after treatment respectively. The LC50 of SCEE against M. persicae was 0. 599 2 mg/mL after day 2 treatment by leaf dipped method. With SCEE at 10 mg/mL for the third instar larvae of O. furnucalis by mixture pesticide method, the corrected mortalities of 65. 52% and 85. 72% days 7 and day 14 after treatments respectively. The results showed that SCEE possessed strong biological activity to P. rapae, O. furnacalis, and M. persicae, while possessed weak biological activity to S. litura and P. xylostella. [source] Synthesis and Biological Activities of 2,4-Diaminopteridine DerivativesARCHIV DER PHARMAZIE, Issue 5 2009Fei Ma Abstract Substituted 2,4-diaminopteridine derivatives 10a,10l were prepared in moderate to good yield. Their structures were confirmed by 1H-NMR and MS spectroscopy, as well as by elemental analysis. Their inhibitory properties against inducible nitric oxide synthase (iNOS) were evaluated in vitro. Biological tests indicated that compound 10a, 10d, 10e, 10h, 10i, and 10l showed potent inhibitory activities similar to that of methotrexate (MTX), while the activities of compound 10b, 10c, 10f, 10g, 10j, and 10k are stronger than MTX. Two compounds, i. e., 10b (IC50 = 18.85 ,M) and 10i (IC50 = 24.08 ,M) were further studied for their effect on septic shock in rats and immunologically liver injured mice (in vivo). The results demonstrated that 10b and 10i had the capacity to increase the blood pressure in septic shock and showed notable protective activities on immunological hepatic injury. [source] ChemInform Abstract: Novel Acyl Coenzyme A: Diacylglycerol Acyltransferase 1 Inhibitors , Synthesis and Biological Activities of N-(Substituted heteroaryl)-4-(substituted phenyl)-4-oxobutanamides.CHEMINFORM, Issue 43 2010Yoshihisa Nakada Abstract A series of novel N-(substituted hetaryl)-4-aryl-4-oxobutanamides are designed, synthesis and evaluated for their activity against DGAT-1 enzyme. [source] ChemInform Abstract: Synthesis and Biological Activities of Some Novel Triazoloquinazolines and Triazinoquinazolines Containing Benzenesulfonamide Moieties.CHEMINFORM, Issue 33 2010Mostafa M. Ghorab Abstract New compounds (IVb), (VIIIc) and (X) exhibit good antipyretic activities compared to the reference drug acetaminophen, whereas compounds (VIb), (VIIIb) and (XIV) show promising antiinflammatory activities compared to indomethacin. [source] ChemInform Abstract: Synthesis and Biological Activities of Some Schiff,s Bases from 4-Amino-3-(3-hydroxybutyl)-1H-1,2,4-triazole-5-thione.CHEMINFORM, Issue 38 2009Jing Zhang Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis, Structure and Biological Activities of Some Novel Anthranilic Acid Esters Containing N-Pyridylpyrazole.CHEMINFORM, Issue 32 2009Weili Dong Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis, Structure and Biological Activities of Some Novel N-(4,6-Disubstituted-pyrimidin-2-yl)-N,- (trifluoromethylphenyl)guanidine Derivatives.CHEMINFORM, Issue 49 2008Feng-Qi He Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Syntheses and Biological Activities of Benzimidazolo[2,1-b]benzo[e]thiazepin-5(10H)-ones.CHEMINFORM, Issue 19 2008Noushin Rastkari Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Synthesis, Structures, and Biological Activities of New 1H-1,2,4-Triazole Derivatives Containing Pyridine Unit.CHEMINFORM, Issue 38 2007Jian-Bing Liu Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis and Biological Activities of cis and trans 5-Amino-3- [(6-chloro-3-pyridyl)methyl] amino-1-(5,5-dimethyl-2-oxo-4-substitutedphenyl-1,3,2-dioxaphosphinan-2- yl)-4-cyano(ethoxycarbonyl)-1H-pyrazoles.CHEMINFORM, Issue 1 2007Zai-Gang Luo Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Rubriflordilactones A (I) and B (II), Two Novel Bisnortriterpenoids from Schisandra rubriflora and Their Biological Activities.CHEMINFORM, Issue 29 2006Han-Dong Sun Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Study on Structure and Biological Activities of Novel Triazole Compounds Containing 1,3-Dithiolane Ring.CHEMINFORM, Issue 10 2006Liang-Zhong Xu Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis and Biological Activities of Aryl-Ether-, Biaryl-, and Fluorene-Aspartic Acid and Diaminopropionic Acid Analogues as Potent Inhibitors of the High-Affinity Glutamate Transporter EAAT-2.CHEMINFORM, Issue 8 2006Alexander Greenfield Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access the actual ChemInform Abstract, please click on HTML or PDF. [source] Synthesis and Biological Activities of Novel Aryl Indole-2-carboxylic Acid Analogues as PPAR, Partial Agonists.CHEMINFORM, Issue 7 2006James F. Dropinski Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access the actual ChemInform Abstract, please click on HTML or PDF. [source] Tetrahydrofuranylmethylamines: An Efficient and Simple One-Step Synthesis and Biological Activities.CHEMINFORM, Issue 10 2004Marcus Limbeck Abstract For Abstract see ChemInform Abstract in Full Text. [source] Studies on Synthesis and Biological Activities of Novel Triazole Compounds Containing N,N-Dialkyldithiocarbamate.CHEMINFORM, Issue 17 2003L. Z. Xu Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Novel, Potent, and Selective Phosphodiesterase 5 Inhibitors: Synthesis and Biological Activities of a Series of 4-Aryl-1-isoquinolinone Derivatives.CHEMINFORM, Issue 41 2001Tatsuzo Ukita Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Total Synthesis of the Cyclodepsipeptide Apratoxin A and Its Analogues and Assessment of Their Biological ActivitiesCHEMISTRY - A EUROPEAN JOURNAL, Issue 29 2006Dawei Ma Prof. Dr. Abstract A novel total synthesis of apratoxin A is described, with key steps including the assembly of its ketide segment through a D -proline-catalyzed direct aldol reaction and Oppolzer's anti aldol reaction and the preparation of its thiazoline unit in a biomimetic synthesis. An oxazoline analogue of apratoxin A has also been elaborated by a similar approach. This compound has a potency against HeLa cell proliferation only slightly lower than that of apratoxin A, whilst a C(40)-demethylated oxazoline analogue of apratoxin A displays a much lower cytotoxicity and the C(37)-epimer and C(37) demethylation product of this new analogue are inactive. These results suggest that the two methyl groups at C(37) and C(40) and the stereochemistry at C(37) are essential for the potent cellular activity of the oxazoline analogue of apratoxin A. Further biological analysis revealed that both synthetic apratoxin A and its oxazoline analogue inhibited cell proliferation by causing cell cycle arrest in the G1 phase. [source] Synthesis and Biological Activities of AzalamellarinsCHEMISTRY - AN ASIAN JOURNAL, Issue 9 2010Sasiwadee Boonya-udtayan Abstract The synthesis of azalamellarins, a new series of lactam analogues of biologically active lamellarins, was achieved using CuI -mediated and microwave-assisted CNamide bond formation. Seventeen azalamellarins, including N -allylazalamellarins and N -propylazalamellarins ,-D, L -N, and J-dehydro J, were synthesized and evaluated for their cytotoxicity against the cancer cell lines HuCCA-1, A-549, HepG2, and MOLT-3. The results showed that certain azalamellarins exhibited good activities in the micromolar IC50 value range (IC50=the drug concentration that causes 50,% of cell-growth inhibition after 72,h of continuous exposure to the test molecule), comparable to their parent lamellarin analogue. [source] Syntheses, Characterizations, and Biological Activities of Tetradeca-4,8-dien-1-yl Acetates as Sex Attractants of Leaf-Mining Moth of the Genus Phyllonorycter (Lepidoptera: Gracillariidae)CHEMISTRY & BIODIVERSITY, Issue 9 2009Ilme Liblikas Abstract The four possible isomers of tetradeca-4,8-dien-1-yl acetate and corresponding alcohols were synthesized stereoselectively by synthetic routes employing Wittig coupling reaction for the preparation of (Z,E)- and (Z,Z)-isomers, and alkylation of terminal alkynes for the preparation of (E,E)- and (E,Z)-isomers as the key steps. Synthetic products were characterized by 13C- and 1H-NMR spectroscopy as well as mass-spectrometric methods. All four isomers gave distinctive mass spectra where m/z 81 fragments clearly dominated. Elution order, followed by retention index presented in parenthesis, of tetradeca-4,8-dien-1-ols was determined as (Z,Z) (2082.1), (Z,E) (2082.8), (E,E) (2083.1), and (E,Z) (2083.2) from unpolar SPB-1 column, and as (E,E) (2210.2), (Z,E) (2222.1), (E,Z) (2223.4), and (Z,Z) (2224.7) from polar DB-WAX column. The isomers of tetradeca-4,8-dien-1-yl acetates eluted in the order of (Z,Z) (2176.1), (Z,E) (2178.4), (E,Z) (2185.9), and (E,E) (2186.4) from SPB-1, and (Z,E) (2124.3), (E,E) (2157.7), (Z,Z) (2128.9), and (E,Z) (2135.9) from DB-WAX columns. Field-screening tests for attractiveness of tetradeca-4,8-dien-1-yl acetates revealed that (4Z,8E)-tetradeca-4,8-dien-1-yl acetate significantly attracted Phyllonorycter coryli and Chrysoesthia drurella males. (4E,8E)-Tetradeca-4,8-dien-1-yl acetate was the most efficient attractant for Ph. esperella and Ph. saportella males, and (4E,8Z)-tetradeca-4,8-dien-1-yl acetate was attractive to Ph. cerasicolella males. [source] Study on Structure and Biological Activities of Novel Triazole Compounds Containing 1,3-Dithiolane RingCHINESE JOURNAL OF CHEMISTRY, Issue 10 2005Liang-Zhong Xu Abstract Seven novel triazole compounds containing 1,3-dithiolane groups were synthesized according to the biological isosterism. Their structures were confirmed by means of elemental analysis, MS, 1H NMR, IR and X-ray crystallography. The results of preliminary biological tests showed that all of these compounds possess some antifungal and plant growth regulatory activities. [source] Synthesis, Structure and Biological Activities of Novel Triazole Compounds Containing Thioamide GroupCHINESE JOURNAL OF CHEMISTRY, Issue 7 2005Liu Fa-Qian Abstract Two compounds 2-benzoyl- N -phenyl-2-(1,2,4-triazol-1-yl)thioacetamide (1) and 2-(4-chlorobenzoyl)- N -phenyl- 2-(1,2,4-triazol-1-yl)thioacetamide (2) were synthesized from substituted acetophenone, triazole and phenyl isothiocyanate by several step reactions. The structure of compound 1 was determined by single-crystal X-ray diffraction analysis. It crystallizes in monoclinic system with space group P21/c, a=0.8806(2) nm, b=1.2097(2) nm,c=1.4809(3) nm, ,=105.88°, Z=4, V=1.5173(6) nm3, Dc=1.411 Mg/m3, ,=0.22 mm -1, F(000)=672, finalR1=0.040 and Rw=0.103. There is obvious potentially weak CH···N intermolecular interaction in the crystal, which stabilizes the structure. The results of biological test show that the two compounds have antifungal and plant growth regulating activities. [source] Synthesis, Solution Structure and Biological Activity of Val-Val-Pro-Gln,a Bioactive Elastin PeptideEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 8 2005Caterina Spezzacatena Abstract Val-Val-Pro-Gln (valyl-valyl-prolyl-glutamine) is a small but highly conserved sequence present in all elastins. We describe its synthesis by mixed anhydride solution chemistry as an alternative to solid-phase peptide synthesis (SPPS). The molecular structure of the tetrapeptide in solution was investigated by classical spectroscopy, such as circular dichroism (CD), nuclear magnetic resonance (NMR) and Fourier Transform Infrared Spectroscopy (FTIR). The biological activity of Val-Val-Pro-Gln was evaluated by a bromodeoxyuridine (BrdU) incorporation assay with normal human dermal fibroblasts. This small peptide may play a critical role in control of matrix metabolism through its release from the elastin polypeptide chain during periods of tissue breakdown and remodelling. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005) [source] Second-Generation Inhibitors for the Metalloprotease Neprilysin Based on Bicyclic Heteroaromatic Scaffolds: Synthesis, Biological Activity, and X-Ray Crystal-Structure AnalysisHELVETICA CHIMICA ACTA, Issue 4 2005Stefan Sahli A new class of nonpeptidic inhibitors of the ZnII -dependent metalloprotease neprilysin with IC50 values in the nanomolar activity range (0.034,0.30,,M) were developed based on structure-based de novo design (Figs.,1 and 2). The inhibitors feature benzimidazole and imidazo[4,5- c]pyridine moieties as central scaffolds to undergo H-bonding to Asn542 and Arg717 and to engage in favorable , - , stacking interactions with the imidazole ring of His711. The platform is decorated with a thiol vector to coordinate to the ZnII ion and an aryl residue to occupy the hydrophobic S1, pocket, but lack a substituent for binding in the S2, pocket, which remains closed by the side chains of Phe106 and Arg110 when not occupied. The enantioselective syntheses of the active compounds (+)- 1, (+)- 2, (+)- 25, and (+)- 26 were accomplished using Evans auxiliaries (Schemes,2, 4, and 5). The inhibitors (+)- 2 and (+)- 26 with an imidazo[4,5- c]pyridine core are ca. 8 times more active than those with a benzimidazole core ((+)- 1 and (+)- 25) (Table,1). The predicted binding mode was established by X-ray analysis of the complex of neprilysin with (+)- 2 at 2.25-Å resolution (Fig.,4 and Table,2). The ligand coordinates with its sulfanyl residue to the ZnII ion, and the benzyl residue occupies the S1, pocket. The 1H -imidazole moiety of the central scaffold forms the required H-bonds to the side chains of Asn542 and Arg717. The heterobicyclic platform additionally undergoes ,-, stacking with the side chain of His711 as well as edge-to-face-type interactions with the side chain of Trp693. According to the X-ray analysis, the substantial advantage in biological activity of the imidazo-pyridine inhibitors over the benzimidazole ligands arises from favorable interactions of the pyridine N-atom in the former with the side chain of Arg102. Unexpectedly, replacement of the phenyl group pointing into the deep S1, pocket by a biphenyl group does not enhance the binding affinity for this class of inhibitors. [source] Chemical Characterization and Biological Activity of Macfadyena unguis-cati (Bignoniaceae)JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 3 2000D. S. DUARTE Macfadyena unguis-cati (L.) has been widely used in folk medicine as an anti-inflammatory, antimalarial and antivenereal. The purpose of this study was to chemically characterize the main plant components, and to evaluate the biological properties of some of the fractions derived from leaves (MACb) and liana (MACa) of this plant. Chemical characterization allowed the identification of the compounds corymboside, vicenin-2, quercitrin, chlorogenic acid, isochlorogenic acid, lupeol, ,-sitosterol, ,-sitosterylglucoside, allantoin and lapachol. The biological screening of fractions and/or purified substances derived from fractions revealed antitumoral and antitrypanosomal activities in fractions MACa/lapachol and MACb/MACb21, respectively. The anti-lipoxygenase and anti-cyclooxygenase effect seen in fractions MACa and MACb showed a partial correlation with the anti-inflammatory property attributed to this plant. [source] Development of a Lyophilization Formulation that Preserves the Biological Activity of the Platelet-inducing Cytokine Interleukin-11 at Low ConcentrationsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 1 2000CHRISTOPHER PAGE Recombinant human interleukin-11 (rhIL-11) is a licensed biological therapeutic product in at least one country and is used to combat thrombocytopenia during chemotherapeutic regimens, as well as undergoing clinical trials for a range of other disorders. Following attempts to lyophilize IL-11 at low concentrations, it was clear that a significant loss of recoverable biological activity occurred. Investigation of a variety of factors, including the type of container in which the rhIL-11 was lyophilized, revealed that surface adsorption to glass was a major factor resulting in loss of activity of rhIL-11 in solution (> 40% reduction after 3 h at room temperature), in addition to losses of activity post-lyophilization. To overcome this problem, different formulations containing combinations of human serum albumin (HSA), trehalose and Tween-20 have been investigated. Two formulations were successful in entirely preserving the biological activity of rhIL-11 through lyophilization and subsequent reconstitution (potency estimates of formulated relative to original material being ,0.97). Accelerated degradation studies, performed at intervals over a six-month period, demonstrated the stability of freeze-dried rhIL-11 using these formulations (predicted annual reduction in potency after storage at ,20°C ,1.4%). In conclusion, we have developed a working combination of excipients (0.5% HSA, 0.1% trehalose and 0.02% Tween-20 in potassium phosphate buffer (pH 7.4)) to formulate a stable rhIL-11 freeze-dried product in glass containers, with no loss in potency. These findings should facilitate development of low dose rhIL-11 products and be an indicator of caution to those using this and other material with similar physical properties, without taking appropriate precautions to avoid losses through adsorption. [source] Molecular Diversity of VEGF-A as a Regulator of Its Biological ActivityMICROCIRCULATION, Issue 7 2009Jeanette Woolard ABSTRACT The vascular endothelial growth factor (VEGF) family of proteins regulates blood flow, growth, and function in both normal physiology and disease processes. VEGF-A is alternatively spliced to form multiple isoforms, in two subfamilies, that have specific, novel functions. Alternative splicing of exons 5,7 of the VEGF gene generates forms with differing bioavailability and activities, whereas alternative splice-site selection in exon 8 generates proangiogenic, termed VEGFxxx, or antiangiogenic proteins, termed VEGFxxxb. Despite its name, emerging roles for VEGF isoforms on cell types other than endothelium have now been identified. Although VEGF-A has conventionally been considered to be a family of proangiogenic, propermeability vasodilators, the identification of effects on nonendothelial cells, and the discovery of the antiangiogenic subfamily of splice isoforms, has added further complexity to their regulation of microvascular function. The distally spliced antiangiogenic isoforms are expressed in normal human tissue, but downregulated in angiogenic diseases, such as cancer and proliferative retinopathy, and in developmental pathologies, such as Denys Drash syndrome and preeclampsia. Here, we examine the molecular diversity of VEGF-A as a regulator of its biological activity and compare the role of the pro- and antiangiogenic VEGF-A splice isoforms in both normal and pathophysiological processes. [source] Synthesis and Biological Activity of Some 1,3-Dihydro-2H -3-benzazepin-2-ones with a Piperazine Moiety as Bradycardic AgentsARCHIV DER PHARMAZIE, Issue 2 2010Hong-Yu Liang Abstract A series of 1,3-dihydro-2H -3-benzazepin-2-ones with a piperazine moiety were designed and synthesized by treating the common intermediate of 1,3-dihydro-7,8-dimethoxy-3-[3-(1-piperazinyl)propyl]-2H -3-benzazepin-2-ones with a variety of N -aryl-2-chloroacetamides and acyl chlorides. Their structures have been characterized by 1H-NMR, MS, and elemental analysis. The title compounds were evaluated for their bradycardic activity in vitro. Most of the synthesized compounds exhibited some vasorelaxant activity and heart-rate-reducing activity with bradycardic potency. [source] Novel l,-Methylcarbapenems Having Cyclic Sulfonamide Moieties: Synthesis and Evaluation of in-vitro Biological Activity , Part IIARCHIV DER PHARMAZIE, Issue 9 2009Seong Jong Kim Abstract The synthesis of a new series of 1,-methylcarbapenems having cyclic sulfonamide moieties is described. Their in-vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of a substituent on the pyrrolidine ring was investigated. One particular compound IIIe having a [1,2,5]thiadiazolidin 1,1-dioxide moiety showed the most potent antibacterial activity. [source] | |||||||||||||||||||||||||||||||||||||||||||||||||