Oneilsimon2005

The assay has been standardized using known eukaryotic protein kinase inhibiting anticancer agents like AG-490, AG-1295, AG-1478, Flavopiridol and Imatinib as positive controls, at a concentration ranging from 10 μg/well to 100 μg/well. Anti-infective compounds which are not reported to inhibit eukaryotic protein kinases were used as negative controls. A number of microbial cultures have been screened for novel eukaryotic protein kinase inhibitors. Further these microbial extracts were tested in various cancer cell lines like Panel, HCT116, Calul, ACHN and H460 at a concentration of 10 μg/mL/ well. The anticancer data was seen correlating well with the Streptomyces kinase assay thus validating the assay.We have previously reported a wide range of components from Cissus quadrangularis with in vitro effects on lipases and glycosidases. We now report that a preparation of the plant (CQR-300) administered at 300 mg daily was effective in reducing weight, as well as improving blood parameters associated with metabolic syndrome, as well as serotonin levels in obese and overweight individuals.The same propolis sample that was analyzed by GC-MS in 1997 and 2012 was examined again after being frozen for 15 years. No qualitative changes were seen in its composition; artepilin C, prenyl-p-coumaric acid, dihydrocinnamic acid, caffeic acid were the major compounds.(-)-(10E,15S)-10,11-Dehydrocurvularin (1), produced from an associated-fungus of Scolopendra subspinipes mutilans on a gram scale, was microbiologically converted to curvularin (2) and 5-methoxycurvularin (3) by Antrodiella semisupina in 61% totally isolated yield. The structures of these compounds were elucidated on the basis of spectroscopic and mass spectrometric analysis. The undescribed assignments of 1H and 13C NMR spectral data for 5-methoxycurvularin (2) has now been explicitly provided. The cytotoxic activities of compounds 1-3 against four human cancer cell lines were evaluated. Dehydrocurvularin (1) showed moderate cytotoxicity against Caski and Hep-G2, and curvularin (2) was selectively cytotoxic against MDA-MB-231.Our research was focused on the evaluation of bergenin content and free radical scavenging activity of extracts prepared from three different species of Bergenia - B. crassifolia (L.) Fritsch., B. ciliata (Haw.) Sternb. and B. x ornata Stein. collected during different seasons. Using an HPLC method, the highest total amount of bergenin was revealed in the leaves of B. x ornata and B. crassifolia (4.9 - 5.1 mg x g(-1)). Free radical scavenging power was determined by two methods--FRAP and NADH. The best free radical scavengers were B. crassifolia (FRAP 6.7 - 15.9 mg GAE. 100g(-1); NADH 20.3 - 50.9%) and B. ornata (FRAP 13.7 - 15.2 mg GAE. 100g(-1); NADH 29.3 - 31.1%). The lowest content of bergenin and the weakest radical scavenger was B. P505-15 purchase ciliata (bergenin 3.1 mg x g(-1); FRAP 5.5 - 11.0 mg GAE.100g(-1); NADH 23.2 - 25.6%). The presence of a large percentage of bergenin is responsible for the radical scavenging activity, as shown by the results from the FRAP and NADH assays. Significant, positive correlation was found between bergenin content and radical scavenging activity in both methods.Lavandin is a well-known aromatic plant cultivated mainly for its valuable essential oil. Nonetheless, little attention has been paid so far to the quantification of other natural products such as polyphenols. Accordingly, we examined the effect of increasing doses of UV-B radiation on the main phenolic content, antioxidant activity and estimated biomass of one year old lavandin pots compared with pots grown outdoors. Significantly higher total phenolic content and concentration of main polyphenols have been found in outdoor plants. Rosmarinic acid has been described as the major phenolic compound in methanolic extracts (max. 25.9 ± 9.7 mg/g(-1) DW). Furthermore, we found that increasing doses of UV-B promote the plant growth of this species as well as the accumulation of phenolic compounds although with less antioxidant capacity in scavenging DPPH radicals. On the other hand, our results showed a remarkable variability among individual plants regarding the content of major phenolic acids. The application of UV-B doses during plant growth could be a method to promote biomass in this species along with the promotion of higher content of valuable secondary metabolites.Red clover (Trifolium pratense) contains soluble phenolic compounds with roles in inhibiting proteolysis and ammonia production. Alfalfa (Medicago sativa) has been found to have a low phenolic content, but few alfalfa and red clover cultivars have been compared for phenolic content. Total soluble phenolics were quantified by a Folin-Ciocalteu colorimetric assay in nine red clover and 27 alfalfa cultivars. Mean total phenolic contents of red clover and alfalfa were 36.5 ± 4.3 mg/gdw and 15.8 ± 1.4 mg/gdw, respectively, with the greater standard deviation of red clover possibly indicating more diversity in phenolic content. Because different phenolic standards had different response factors in the colorimetric assay, the red clover and 11 alfalfa cultivars were analyzed by HPLC to determine if the differences in total soluble phenolics between genera reflected differences in the amounts of phenolics or in the classes of phenolics responding to the colorimetric assay. Two red clover cultivars differed in total phenolics and phaselic acid. Alfalfa produced different phenolic compounds from red clover, at lower concentrations. Extracts of two red clover cultivars were separated by thin-layer chromatography (TLC), and the bands were assayed for activity against Clostridium sticklandii, a bovine ruminal hyper ammonia-producing bacterium (HAB). Only biochanin A had anti-HAB activity. Inhibitory amounts indicated that five red clover cultivars could be suitable sources of anti-HAB activity.A series of structurally simple compounds belonging to thestilbene family were synthesized by means of a Ti(III)-mediated methodology that allows access, in an efficient manner, to derivatives of dihydrostilbene, E-stilbene, and stilbene oxide, with high yields. The antioxidant activity of these compounds has been evaluated by means of two electrochemical assays, which provide complementary information, showing that the majority of these stilbene analogs exhibit significant antioxidant activity dependent on the electronic structure and functionalization of the molecule in each case.Morus alba L. has been used in Asian traditional medicine as an anti-inflammatory, anti-asthmatic, anthelmintic and as a whitening agent in cosmetic products. Mulberroside A is the major active compound from M. alba root bark. In this study, cell suspension and root cultures of M. alba were established, and the effect of the elicitors on the enhancement of mulberroside A production in M. alba was investigated. The cell suspension and root cultures of M. alba were exposed to elicitors and then mulberroside A contents were determined by an indirect competitive ELISA method. High levels of mulberroside A were obtained by addition of 100 and 200 μM salicylic acid with 24 h exposure time in cell suspension cultures (37.9 ± 1.5 and 34.0 ± 4.7 mg/g dry wt., respectively). Furthermore, addition of yeast extract at 2 mg/mL with 24 h exposure time can significantly increase mulberroside A contents from both cell suspension (3.2-fold) and root cultures (6.6-fold). Mulberroside A contents from both cell suspension and root cultures after treatment with elicitors are similar or higher than those found in the intact root and root bark of several years old M. alba. These results indicate that mulberry tissue cultures using the elicitation method are interesting alternative sources for mulberroside A production.One new phenyl ethyl glycoside, 2-(4-hydroxyphenyl)ethyl-O-α-L-arabinofuranosyl-(1 --> 6)-O-β-D-glucopyranoide (1) and 11 known compounds (2-12) were isolated from the twigs of Acer tegmentosum. Compound 6 showed potent anti-neuroinflammatory activity against the LPS-stimulated BV-2 microglial cells with tNO production of 25.0 ± 2.5 μM and TNF-α concentration of 617.6 ± 47.1 pg/mL at 30 μM.A new polyketide 1 and a new decaline derivative 2 were isolated from a sediment-derived fungus Aspergillus carneus Blochwitz, together with one known bisabolane sesquiterpenoid and seven known polyketide metabolites. The structures of the isolated compounds were established by HR-MS, and 1D and 2D NMR spectroscopy. The cytotoxic and antiradical activities of the isolated compounds were evaluated.6,8,9-Trihydroxy-2-methyl-2H-naphtho[2,3-b]pyran-5,10-dion, a pigment of the sea urchin Echinothrix diadema, and six analogs were synthesized. The cytotoxic activity and contraceptive properties of the synthesized pyranonaphthazarins have been investigated using the sperm and eggs of the sea urchin Strongylocentrotus intermedius.The constituents of walnut (Juglans regia L.) leaves are represented by tannins, phenolics, and naphthoquinones, the characteristic compound being juglone. The content of juglone in the methanolic extract of the leaves determined by the GC/MS method was 9.9 ± 0.2 mg/100 g; small amounts (1.3 ± 0.02 mg/100 g) were recorded in the infusion, whereas in the decoction it was not detected. As some studies indicate toxicity of juglone, only decoctions should be recommended for therapeutic use.2-Acetyl-1-hydroxynaphthalene was converted into 1,4-dimethoxy-2-naphthoxyacetic acid in seven steps (methylation, Bayer-Villiger oxidation, hydrolysis, bromination, methylation, alkylation and hydrolysis). 2-Hydroxy-1,4-naphthoquinone on acetylation, aromatization, methylation and hydrolysis, respectively, also yielded the title compound.A detailed phytochemical investigation of the dichloromethane extract of the aerial parts of Hypericum maculatum Crantz. led to the isolation of four new (2-5) and six known (1a/b, 6-10) polyprenylated phloroglucinol derivatives. The new compounds were identified by means of spectral methods (MS, NMR, IR, UV) as (E)-4-(3,7-dimethylocta-2,6-dien-1-yl)-5-hydroxy-2-(3-methylbut-2-en-1-yl)-3,6-dioxocyclohexa-1,4-dien-1-yl isobutyrate (2), (E)-2-(3,7-dimethylocta-2,6-dien-1-yl)-5-hydroxy-4-(3-methylbut-2-en-1-yl)-3,6-dioxocyclohexa-1,4-dien-1-yl isobutyrate (3), (E)-4-(3,7-dimethylocta-2,6-dien-1-yl)-5-hydroxy-2-(3-methylbut-2-en-1-yl)-3,6-dioxocyclohexa-1,4-dien-1-yl 2-methylbutanoate (4) and (E)-2-(3,7-dimethylocta-2,6-dien-1-yl)-5-hydroxy-4-(3-methylbut-2-en-1-yl)-3,6-dioxocyclohexa-1,4-dien-1-yl 2-methylbutanoate (5). The known compounds have been identified as hyperpolyphyllirin/hyperibine J (1a/b), erectquione A (6), (E)-1-(3-(3,7-dimethylocta-2,6-dien--yl)-2,4,6-trihydroxyphenyl)-2-methylpropan-1-one (7), (E)-1-(3-(3,7-dimethylocta-2,6-dien-1-yl)- 2,4,6-trihydroxyphenyl)-2-methylbutan-1-one (8), 1-(5,7-dihydroxy-2-methyl-2-(4-methylpent-3-en-1-yl)chroman-8-yl)-2-methylpropan-1-one (9) and 1-(6,8-dihydroxy-1,1,4a-trimethyl-2,3,4,4a,9,9a-hexahydro-1H-xanthen-5-yl)-2-methylpropan-1-one (10). The stereochemistry of 1a is described for the first time. The cytotoxicity of 1-6 on SKW-3, BV-173 and K-562 tumor cell lines was determined using MTT based assays.