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Anticancer Activity (anticancer + activity)
Selected AbstractsFacile Synthesis and Antibacterial, Antitubercular, and Anticancer Activities of Novel 1,4-DihydropyridinesARCHIV DER PHARMAZIE, Issue 6 2010Kalam Sirisha Abstract A series of twenty new 4-substituted-2,6-dimethyl-3,5-bis- N -(heteroaryl)-carbamoyl-1,4-dihydropyridines have been prepared from a three-component one-pot condensation reaction of N -heteroaryl acetoacetamide, an aromatic/heteroaromatic aldehyde, and ammonium acetate under four different experimental conditions. Except for the conventional method, all the experimental conditions were simple, eco-friendly, economical, and the reactions were rapid and high-yielding. The methods employed have been compared in terms of yields, cost, and simplicity. The synthesized compounds were characterized by different spectroscopic techniques and evaluated for their in-vitro anticancer, antibacterial, and antitubercular activities. Amongst the compounds tested, compound 25 exhibited the highest anticancer activity while compounds 14 and 18 exhibited significant antibacterial and antitubercular activities. [source] Immunomodulatory and Anticancer Activities of Some Novel 2-Substituted-6-bromo-3-methylthiazolo[3,2- a]benzimidazole DerivativesARCHIV DER PHARMAZIE, Issue 4 2009Hatem A. Abdel-Aziz Abstract Ethyl 6-bromo-3-methyl-1,3-thiazolo[3,2- a]benzimidazole-2-carboxylate 2 was prepared by the ambient temperature bromination of ethyl 3-methyl-1,3-thiazolo[3,2- a]benzimidazole-2-carboxylate 1. The acid hydrazide 4 was obtained by the reaction of ester 2 with hydrazine hydrate. Treatment of compound 4 with benzaldehyde or 2-thiophenaldehyde yielded the corresponding hydrazones 6a and 6b, respectively, while the reaction of acid hydrazide 4 with ethoxymethylene malononitrile (7a) or with ethyl ethoxymethylene cyanoacetate (7b) in refluxing ethanol afforded pyrazole derivatives 9a and 9b, respectively. Taken together, from the biological investigations compounds 9a and 9b were the most significant inhibitors of LPS-stimulated NO generation from Raw murine macrophage 264.7, and, as another result, compounds 2 and 4 had a weak radical scavenging activity against DPPH radicals. Moreover, 2, 4, and 9a had a concomitant strong cytotoxicity against both colon carcinoma cells (HCT-116) and hepatocellular carcinoma cells (Hep-G2) while 9b showed specific cytotoxicity only against colon carcinoma cells. [source] ChemInform Abstract: 1-Toluene-sulfonyl-3- [(3,-hydroxy-5,-substituted)-,-butyrolactone]-indoles: Synthesis, COX-2 Inhibition and Anticancer Activities.CHEMINFORM, Issue 25 2008Palwinder Singh 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, Photophysical Studies and Anticancer Activity of a New Halogenated Water-Soluble PorphyrinPHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 4 2007Janusz M. D, browski ABSTRACT A water-soluble halogenated porphyrin, namely 5,10,15,20 -tetrakis(2-chloro-3-sulfophenyl)porphyrin (TCPPSO3H), was prepared and evaluated as sensitizer for photodynamic therapy (PDT). Photophysical properties of TCPPSO3H, such as high photostability, long triplet lifetime and high singlet oxygen quantum yield suggest high effectiveness of this class of halogenated porphyrins in PDT. TCPPSO3H is non-toxic in the dark and causes a significant photodynamic effect examined against MCF7 (human breast carcinoma), SKMEL 188 (human melanoma) and S91(mouse melanoma) cell lines upon red light irradiation (cutoff < 600 nm) at low light doses. Time-dependent cellular uptake of TCPPSO3H reached plateau at 120 min and was the highest for S91, 20% lower for MCF7 and 70% lower for SKMEL 188. Our results show that this halogenated water-soluble porphyrin is an efficient photosensitizer and reveal the potential of this class of compounds as PDT agents. [source] Innentitelbild: Discovery, Structure, and Anticancer Activity of an Iridium Complex of Diselenobenzoquinone (Angew. Chem.ANGEWANDTE CHEMIE, Issue 41 201041/2010) Das erste Diselenobenzochinon wurde in Form des stabilen Komplexes [Cp*Ir(,4 -C6H4Se2)] isoliert; eine Röntgenstrukturanalyse bestätigte die Struktur. H. Amouri et,al. beschreiben in ihrer Zuschrift auf S.,7692,ff. außerdem die Antitumoraktivität dieses Komplexes: Der Diselenokomplex zeigt eine ähnliche cytotoxische Aktivität wie Cisplatin. [source] Discovery, Structure, and Anticancer Activity of an Iridium Complex of Diselenobenzoquinone,ANGEWANDTE CHEMIE, Issue 41 2010Dr. Hani Amouri [Cp*Ir(,4 -C6H4Se2)] wurde als erster beständiger ,4 -Diseleno- p -benzochinon-Komplex isoliert. Eine Röntgenstrukturanalyse bestätigt die Koordination des bislang nicht ermittelbaren Diselenobenzochinon-Intermediats (siehe Bild; Ir,magenta, Se,gelb). Bei einem gemeinsamen Test auf Antikrebsaktivität mit seinen Sauerstoff- und Schwefelanaloga wirkte nur der Diselenokomplex zytotoxisch; seine Aktivität war derjenigen von Cisplatin vergleichbar. [source] Synthesis and Anticancer Activity of Novel Betulinic acid and Betulin DerivativesARCHIV DER PHARMAZIE, Issue 8 2010Harish Kommera Abstract A series of novel betulinic acid derivatives 3,11 and betulin derivatives 12,17 were synthesized. The compounds were characterized by the means of 1H- and 13C-NMR spectroscopy as well as mass spectrometry. The compounds have been tested on ten tumor cell lines of different histogenic origin. The most active derivatives, containing a chloroacetyl group on C-3 in betulinic acid 9 and C-28 in betulin 15, were up to ten times more cytotoxic and many fold more selective towards tumor cells in comparison to normal cells (fibroblasts) than betulinic acid. Furthermore, compound 15 was found to possess cell growth inhibition even when treated for a short time on anaplastic thyroid cancer cells (SW1736). [source] Relationship Between Anticancer Activity and Stereochemistry of Saldach Ligands and their Iron(III) ComplexesARCHIV DER PHARMAZIE, Issue 11 2009Annegret Hille Abstract (R,R)-, (S,S)- and (R,S)- N,N,-bis(salicylidene)-1,2-diaminocyclohexane (saldach) and their iron(III) complexes were screened for anticancer activity against MCF-7 and MDA-MB 231 breast cancer as well as HT-29 colon carcinoma cells. Antiproliferative effects depended on the presence of the central atom iron but were independent on the configuration at the saldach ligand. While the free ligands were inactive, the iron(III) derivatives displayed anticancer activity within a concentration range of 1 to 5 ,M irrespective of the used cell line. At 5 ,M they were even more active than cis -platin. A mode of action comparable to cis -platin can be excluded because it is very likely that the DNA is not the primary target of [FeIII (saldach)] complexes. [source] Amidrazones as Precursors of Biologically Active Compounds , Synthesis of Diaminopyrazoles for Evaluation of Anticancer ActivityARCHIV DER PHARMAZIE, Issue 1 2006Maria Teresa Cocco Abstract The regioselectivity of coupling phenyl isocyanate to 3-(2-acylhydrazino)-3-aminopropenenitriles and ethyl 3-(2-acylhydrazino)-3-aminopropenoates as simple access to aminopyrazole derivatives, endowed with potential antitumoral activity, is reported. 3-(2-Acylhydrazino)-3-aminopropenenitriles react with phenyl isocyanate to afford 3-amino-3-(2-acylhydrazino)-2-phenylaminocarbonyl-2-propenenitriles. These key intermediates were cyclized into 3,5-diaminopyrazole-4-carboxamide derivatives. Preliminary results of poor antiproliferative activities of these compounds are also reported. [source] Synthesis of 5-Substituted 2-Methylbenzimidazoles with Anticancer ActivityARCHIV DER PHARMAZIE, Issue 1 2003Sh. I. El-Naem Abstract A series of compounds comprising the thiocarboximidopyrazolyl 5, the phenylpyrazolyl 6, the dimethylpyrazolyl 7, the nitrophenylpyrazolyl 8, the dimethyloxazolyl 9, the benzoxazepinyl 10, and pyrimidyl 11 a,c derivatives of 3-(2-methyl-1H -benzimidazol-5-ylazo)pentane-2, 4-dione was synthesized. Moreover, 5-amino-2-methylbenzimidazole (3) was reacted with phthalic anhydride or maleic anhydride in acetic acid or in toluene to produce 12,15. Treating 5, 6-diamino-2-methylbenzimidazole (16) with ethyl cyanoacetate or diethyl malonate or acetyl acetone leads to the formation of the benzodiazepine derivatives 17,20. The cytotoxic activity of the compounds 2, 7, 9, 10, and 11 was tested against 60 types of human cancer cell lines. Compounds 7 and 9 were found to be the most potent. [source] ChemInform Abstract: An Expeditious Synthesis and Anticancer Activity of Novel 4-(3,-Indolyl)oxazoles.CHEMINFORM, Issue 28 2010Dalip Kumar 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] ChemInform Abstract: Synthesis and Anticancer Activity of New 1-Substituted-6H-pyrido[4,3-b]carbazole Derivatives.CHEMINFORM, Issue 41 2008Beata Tylinska 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 of Novel 4,6-Disubstituted Quinazoline Derivatives, Their Antiinflammatory and Anticancer Activity (Cytotoxic) Against U937 Leukemia Cell Lines.CHEMINFORM, Issue 35 2008P. Mani Chandrika 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, Structure and Anticancer Activity of Novel Alkenyl-1,3,5-triazine Derivatives.CHEMINFORM, Issue 43 2006F. Saczewski 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, Crystal Structure and Anticancer Activity of Novel Derivatives of Ethyl 1-(4-Oxo-8-aryl-4,6,7,8-tetrahydroimidazo[2,1-c] [1,2,4]triazin-3-yl)formate.CHEMINFORM, Issue 38 2006Krzysztof Sztanke 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 Anticancer Activity of Some Novel 5-Azacytosine Nucleosides.CHEMINFORM, Issue 16 2004Kamal N. Tiwari Abstract For Abstract see ChemInform Abstract in Full Text. [source] Potential of resveratrol in anticancer and anti-inflammatory therapyNUTRITION REVIEWS, Issue 8 2008Chibuike C Udenigwe Phytochemicals present in food have shown significant prospects in the treatment and management of a vast array of human diseases. Resveratrol is a stilbene-type aromatic phytoalexin predominantly found in grapes, peanuts, berries, turmeric, and other food products. Resveratrol has been reported to exhibit several physiological activities including anticancer and anti-inflammatory activities in vitro and in experimental animal models, as well as in humans. Anticancer activity of this compound is mainly due to induction of apoptosis via several pathways, as well as alteration of gene expressions, all leading to a decrease in tumor initiation, promotion, and progression. Resveratrol exhibits anti-inflammatory activity through modulation of enzymes and pathways that produce mediators of inflammation and also induction of programmed cell death in activated immune cells. Resveratrol has been shown to produce no adverse effects, even when consumed at high concentrations. Hence, resveratrol possesses good potential to be used as an adjunctive or alternative therapy for cancer and inflammatory diseases. [source] Anticancer activity of hydrophobic peptides from soy proteinsBIOFACTORS, Issue 1-4 2000Song E Kim Abstract An anticancer peptide from soy protein was purified and isolated. Defatted soy protein was hydrolyzed with thermoase and hydrophobic peptides were extracted with ethanol. The peptide extract was fractionated by XAD-2 hydrophobic, gel filtration chromatography, and different C18 HPLCs. Anticancer activity of each fraction was assayed by measuring in vitro cytotoxicity on P388D1, a mouse monocyte macrophage cell line. IC50 value of a peptide fraction from Sephadex G-25 chromatography was 0.16 mg/ml. This peptide fraction at 1 mg/ml significantly affected cell cycle progression by arresting P388D1 at G2/M phases. Finally purified peptide from analytical C18 HPLC was nonapeptide of which molecular weight was 1157 Da and the sequence was X-Met-Leu-Pro-Ser-Tye-Ser-Pro-Tyr. [source] Molecular Interaction between a Gadolinium,Polyoxometalate and Human Serum AlbuminEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 34 2009Li Zheng Abstract Polyoxometalates (POMs) show promising antibacterial, antiviral (particularly anti-HIV), antitumor, and anticancer activities, but the mechanism of these potential therapeutic effects remains to be elucidated at the molecular level. The interaction between the Gd-containing tungstosilicate [Gd(,2 -SiW11O39)2]13, and human serum albumin (HSA) was studied by several techniques. Fluorescence spectroscopy showed an energy transfer between the single tryptophan residue of HSA and the POM. Circular dichroism led to the conclusion that the POM significantly altered the secondary structure of HSA. Isothermal titration calorimetry revealed an enthalpy-driven binding reaction between HSA and the POM, resulting in the formation of a 1:1 complex.(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009) [source] NF- ,B in liver diseases: a target for drug therapyJOURNAL OF APPLIED TOXICOLOGY, Issue 2 2009Pablo Muriel Abstract There are five nuclear factor- ,B (NF- ,B) transcription factors with important roles in innate immunity, liver inflammation, fibrosis and apoptosis prevention. Several inhibitors of NF- ,B, like caffeic acid, captopril, curcumin, pyrrolidine dithiocarbamate, resveratrol, silymarin and thalidomide, have demonstrated antinecrotic, anticholestatic, antifibrotic and anticancer activities in the liver. A link between inflammation and hepatocellular carcinoma through the NF- ,B pathway has been observed, providing ample experimental support for the tumor-promoting function of NF- ,B in various models of cancer. NF- ,B has been associated with the induction of proinflammatory gene expression and has attracted interest as a target for the treatment of inflammatory disease. However, despite much attention being focused on the deleterious effects of NF- ,B, activation of this factor during the resolution of inflammation is associated with the production of antiinflammatory molecules like interleukin (IL)-10 and the onset of apoptosis. This suggests that NF- ,B has an antiinflammatory role in vivo involving the regulation of the resolution of inflammation. Also, NF- ,B promotes liver regeneration by upregulating IL-6 and other molecules like hepatocyte growth factor. It has been postulated that the beneficial properties of NF- ,B are due to p50 homodimers, whose activation prevents cholestatic and chronic liver injury. More basic understanding on the function of the diverse NF- ,B factors is urgently needed in different physiological and pathological conditions, because depending on the subunit composition of the dimmer, the disease and the stage of the illness, inhibition of the factor may result in a beneficial or in a deleterious response. Copyright © 2008 John Wiley & Sons, Ltd. [source] Structures, Components and Functions of Secretory Tissues in Houttuynia cordataJOURNAL OF INTEGRATIVE PLANT BIOLOGY, Issue 12 2007Xi-Lu Ni Abstract Houttuynia cordata Thunb., traditionally used as a therapeutic plant in folk medicine, has shown antioxidant and anticancer activities. The species, as a core component of paleoherbs, is normally characterized based on the presence of different types of secretory tissue: oil cells, three types of secretory cells and glandular hairs. The aim of this work was to study the structural, componential, and the functional characteristics of the secretory tissues in both the floral and vegetative parts. The results indicate that oil cells and secretory cells are distributed in all organs of the plant, while glandular hairs are situated on the aerial stems and leaves. Both oil cells and glandular hairs initiate from the protoderm, but their developmental processes are different. Although three types of secretory cells initiate from different primary meristems, the developmental patterns of different secretory cells are the same. Also, although the origins of secretory cells are different from oil cells, their early developmental processes are the same. Histochemical results show that oil cells, secretory cells and glandular hairs produce flavonoids, phenolic compounds, tannins, lipids, aldehyde and ketone-compounds. In addition, there are terpenoids and pectic-like substances in oil cells, alkaloids in secretory cells of aerial stems, and terpenoids and alkaloids in glandular hairs. These compounds play very important roles in protecting plants from being eaten by herbivores (herbivory) and infected by microbial pathogens. The oil cell and secretory cell, as unicellular secretory tissues, are intermediates between the primitive surface glandular and secretory cavity and canal during the evolution of secretory structures. [source] Antiviral and anticancer activities of 13(E)-labd-13-ene-8,,15-diol isolated from Brachyglottis monroiPHYTOTHERAPY RESEARCH, Issue 2 2010Hwa Jung Choi Abstract The antiviral activity of 13(E)-labd-13-ene-8,,15-diol (1), isolated from Brachyglottis monroi, was examined against human rhinovirus 2 (HRV2) and 3 (HRV3), and the anticancer activity on human cancer cells (A549 and Hep2). Compound (1) showed strong anti-HRV2 and HRV3 activity with a 50% inhibitory concentration (IC50) of 2.68 and 0.87,µg/mL, respectively, and a 50% cytotoxicity concentration (CC50) of 59.45,µg/mL. Ribavirin only showed anti-HRV3 activity with an IC50 of 30.48,µg/mL and a CC50 > 100,µg/mL. The addition of compound (1) to HRV-infected HeLa cells directly reduced the formation of visible cytopathic effect (CPE) and it directly interacted with HRV particles. Furthermore, A549 and Hep2 cells incubated with 32,µg/mL of compound (1) for 48,h exhibited antilung and antilaryngeal cancer activities, with a viability of less than 50%. These results suggest that compound (1) may be used as a potential antiviral and anticancer agent. Copyright © 2009 John Wiley & Sons, Ltd. [source] Recent developments in bisintercalator natural productsBIOPOLYMERS, Issue 9 2010Olga E. Zolova Abstract The bisintercalator natural products are a family of nonribosomal peptides possessing a range of biological properties that include antiviral, antibiotic, and anticancer activities. The name bisintercalator is derived from the ability to directly bind to duplex DNA through two planar intercalating moieties. Although 19 members of this family of compounds have been identified over the past 50 years, the biosynthetic genes responsible for the formation of four of these molecules (thiocoraline, SW-163, triostin A, and echinomycin) were identified only recently. This recent progress opens an avenue towards understanding how Nature produces these bisintercalating products and provides the potential to develop and identify novel potent analogous lead compounds for clinical applications. This review discusses the mode of action of bisintercalators and summarizes recent genetic and biochemical insights into their biosynthetic production, analog formation, and possible mechanisms by which resistance to these compounds is achieved by their producing organisms. © 2010 Wiley Periodicals, Inc. Biopolymers 93: 777,790, 2010. [source] Isothiocyanate E-4IB induces MAPK activation, delayed cell cycle transition and apoptosisCELL PROLIFERATION, Issue 3 2007J. Bodo Methods and results: In the current investigation, we examined the consequence of activating of signalling pathways during the release the cells from the block at G1/S boundary by synthetic isothiocyanate E-4IB. Using synchronized leukaemic HL60 cells, we show that activation of mitogen-activated protein kinases ERK1/2, c-Jun N-terminal kinase and p38 signalling pathways by E-4IB are coupled with delayed transition through the cell cycle and rapid cell cycle arrest resulted in diminished mitochondrial membrane potential culminating in apoptosis. These events were accompanied by histone deacetylase inhibition, increase of double strand DNA breaks detected by histone H2AX phosphorylation and up-regulation of cell cycle regulatory protein p21 and phosphorylation of CDC25C phosphatase. Conclusion: These findings suggest that the activation of mitogen-activated protein kinases signalling pathways, followed by the induction cell cycle arrest and apoptosis, might be responsible for anticancer activities of E-4IB. [source] Aryloxy Phosphoramidate Triesters: a Technology for Delivering Monophosphorylated Nucleosides and Sugars into CellsCHEMMEDCHEM, Issue 11 2009Youcef Mehellou Dr. Abstract Prodrug technologies aimed at delivering nucleoside monophosphates into cells (protides) have proved to be effective in improving the therapeutic potential of antiviral and anticancer nucleosides. In these cases, the nucleoside monophosphates are delivered into the cell, where they may then be further converted (phosphorylated) to their active species. Herein, we describe one of these technologies developed in our laboratories, known as the phosphoramidate protide method. In this approach, the charges of the phosphate group are fully masked to provide efficient passive cell-membrane penetration. Upon entering the cell, the masking groups are enzymatically cleaved to release the phosphorylated biomolecule. The application of this technology to various therapeutic nucleosides has resulted in improved antiviral and anticancer activities, and in some cases it has transformed inactive nucleosides to active ones. Additionally, the phosphoramidate technology has also been applied to numerous antiviral nucleoside phosphonates, and has resulted in at least three phosphoramidate-based nucleotides progressing to clinical investigations. Furthermore, the phosphoramidate technology has been recently applied to sugars (mainly glucosamine) in order to improve their therapeutic potential. The development of the phosphoramidate technology, mechanism of action and the application of the technology to various monophosphorylated nucleosides and sugars will be reviewed. [source] Amido-Functionalised Prodigiosenes: Synthesis and Anticancer PropertiesCHEMMEDCHEM, Issue 5 2009Abstract Prodigiosin: Amido-functionalised prodigiosin-derived compounds were synthesised via a robust and efficient synthetic route. These compounds were then evaluated against 60 human cell lines consisting of nine diverse tumour cell types and their anticancer activities were assessed. [source] Determination of xanthohumol in hops (Humulus lupulus L.) by nonaqueous CEELECTROPHORESIS, Issue 6 2007Javor Kac Dr. Abstract Xanthohumol (XN) is a prenylated chalcone with antimutagenic and anticancer activity from hops. A nonaqueous reverse polarity capillary electrophoretic method for the determination of XN in hop extract was developed and validated. The optimal parameters were a 64.5,cm long fused-silica capillary with 50,,m id at 25°C; 30,kV negative voltage (anode at detector side of the capillary); nonaqueous buffer with 75,mM NaOH and 50,mM boric acid in methanol; hydrodynamical injection with 10,mbar for 40,s; and detection at 440,nm. XN, isoxanthohumol (IX), colupulone, adlupulone, and n -lupulone were well resolved on the electropherogram. The LOD for XN was 0.05,mg/L and RSD for peak area was below 3%. The amount of XN in different samples of hop pellets varied from 0.14 to 0.42%. [source] Human telomeric G-quadruplex: The current status of telomeric G-quadruplexes as therapeutic targets in human cancerFEBS JOURNAL, Issue 5 2010Stephen Neidle The 3,-ends of human chromosomal DNA terminate in short single-stranded guanine-rich tandem-repeat sequences. In cancer cells, these are associated with the telomere-maintenance enzyme telomerase together with the end-binding protein hPOT1. Small molecules that can compete with these proteins and induce the single-stranded DNA to form quadruplex,ligand complexes are, in effect, able to expose these 3,-ends, which results in the activation of a DNA damage response and selective inhibition of cell growth. Several of these G-quadruplex binding molecules have shown promising anticancer activity in tumour xenograft models, which indicate that the approach may be applicable to the treatment of a wide range of human cancers. This minireview summarizes the available data on these compounds and the challenges posed for drug discovery. [source] The components and anticancer activity of the volatile oil from Streblus asperFLAVOUR AND FRAGRANCE JOURNAL, Issue 5 2004Weerachai Phutdhawong Abstract The volatile oil from fresh leaves of Streblus asper Lour. was isolated by hydrodistillation and analysed through a combination of gas chromatography with FID (GC,FID) and gas chromatography,mass spectrometry (GC,MS). The essential oil was obtained in 0.005% yield as a brown liquid. The major constituents of the volatile oil of S. asper were phytol (45.1%), , -farnesene (6.4%), trans -farnesyl acetate (5.8%), caryophyllene (4.9%) and trans-trans-, -farnesene (2.0%). In addition, the volatile oil showed signi,cant anticancer activity (ED50 << 30 µg/ml) from cytotoxicity primary screening tests with P388 (mouse lymphocytic leukaemia) cells but no signi,cant antioxidant activity (IC50 values of >>100 µg/ml) in a DPPH radical scavenging assay. Copyright © 2004 John Wiley & Sons, Ltd. [source] Ginkgo biloba extracts and cancer: a research area in its infancyFUNDAMENTAL & CLINICAL PHARMACOLOGY, Issue 4 2003Francis V. DeFeudis Abstract Recent studies conducted with various molecular, cellular and whole animal models have revealed that leaf extracts of Ginkgo biloba may have anticancer (chemopreventive) properties that are related to their antioxidant, anti-angiogenic and gene-regulatory actions. The antioxidant and associated anti-lipoperoxidative effects of Ginkgo extracts appear to involve both their flavonoid and terpenoid constituents. The anti-angiogenic activity of the extracts may involve their antioxidant activity and their ability to inhibit both inducible and endothelial forms of nitric oxide synthase. With regard to gene expression, a Ginkgo extract and one of its terpenoid constituents, ginkgolide B, inhibited the proliferation of a highly aggressive human breast cancer cell line and xenografts of this cell line in nude mice. cDNA microarray analyses have shown that exposure of human breast cancer cells to a Ginkgo extract altered the expression of genes that are involved in the regulation of cell proliferation, cell differentiation or apoptosis, and that exposure of human bladder cancer cells to a Ginkgo extract produced an adaptive transcriptional response that augments antioxidant status and inhibits DNA damage. In humans, Ginkgo extracts inhibit the formation of radiation-induced (chromosome-damaging) clastogenic factors and ultraviolet light-induced oxidative stress , effects that may also be associated with anticancer activity. Flavonoid and terpenoid constituents of Ginkgo extracts may act in a complementary manner to inhibit several carcinogenesis-related processes, and therefore the total extracts may be required for producing optimal effects. [source] | ||||||||||||||||||||||||||||||||||||||||