Search results for "Biological activity"
showing 10 items of 465 documents
A review of the biological and pharmacological activities of saponins.
1996
Summary This paper reviews the important biological and pharmacological activities of saponins reported over the last few years. These include cancer-related activity, as well as antiphlogistic and antiallergic, immunomodulating, antihepatotoxic, antiviral, hypoglycemic, antifungal and molluscicidal activities. The action of saponins on the cardiovascular, central nervous, and endocrine systems and other miscellaneous effects are also discussed.
Design, Synthesis and Biological Evaluation of Novel Pyrazolo[1,2,4]triazolopyrimidine Derivatives as Potential Anticancer Agents
2021
Three novel pyrazolo-[4,3-e][1,2,4]triazolopyrimidine derivatives (1, 2, and 3) were designed, synthesized, and evaluated for their in vitro biological activity. All three compounds exhibited different levels of cytotoxicity against cervical and breast cancer cell lines. However, compound 1 showed the best antiproliferative activity against all tested tumor cell lines, including HCC1937 and HeLa cells, which express high levels of wild-type epidermal growth factor receptor (EGFR). Western blot analyses demonstrated that compound 1 inhibited the activation of EGFR, protein kinase B (Akt), and extracellular signal-regulated kinase (Erk)1/2 in breast and cervical cancer cells at concentrations…
Transport, stability, and biological activity of resveratrol
2011
Numerous studies have reported interesting properties of trans-resveratrol, a phytoalexin, as a preventive agent of several important pathologies: vascular diseases, cancers, viral infections, and neurodegenerative processes. These beneficial effects of resveratrol have been supported by observations at the cellular and molecular levels in both cellular and in vivo models, but the cellular fate of resveratrol remains unclear. We suggest here that resveratrol uptake, metabolism, and stability of the parent molecule could influence the biological effects of resveratrol. It appears that resveratrol stability involves redox reactions and biotransformation that influence its antioxidant properti…
Crystal structure of the chalcone (E)-3-(furan-2-yl)-1-phenylprop-2-en-1-one
2015
The crystal packing of the compound is described by an intermolecular arrangement with the molecules as interlaced layers in a zigzag fashion, denoting interacting self-complementary dimers mainly by the localization of weak hydrogen bonds in a head-to-tail arrangement.
Isolation, identification and toxicological characterization of TSS 1, a new mycotoxin of the rosenane class.
1990
11-β-hydroxy-7-deoxy-rosenonolactone (TSS1), a product of the pathogenic fungusTrichothecium roseum (Moniliaceae) was isolated from culture medium extracts and completely described in its structure by spectroscopical methods.TSS 1 was classified as a representative of the lactone series of the rosenane class and as a structural isomer to Rosenololactone (1) and Rosololactone (2, 3).TSS1 showed toxic effects in the growth inhibition test toE coli (EC 50: lOμg/mL) andB subtil is (EC 50: 17μg/mL), inhibited fermentation of yeast (EC 50: 2.8μg/mL) and suppressed motility ofAnemia satina larvae (EC 50: 45/μg/mL).Rosenonolactone, the best known representative of that mycotoxin class, showed only …
2-Aryl-substituted 4H-3,1-benzoxazin-4-ones as novel active substances for the cardiovascular system
1991
4H-3,1-Benzoxazin-4-ones of the structural types 3 and 4 are accessible by cyclization reactions. The introduction of the phosphonate group was achieved by way of Wohl-Ziegler bromination and subsequent Michaelis-Arbuzow reaction with a trialkyl phosphite. Pharmacological investigations on isolated left atria, ileum specimens, and Langendorff hearts as well as in vivo circulatory studies on anesthetized rats revealed that the phosphonates 4 exert calcium antagonistic effects. Whereas 2-(arylvinyl)benzoxazinones gave rise to pronounced negative inotropic effects, compound 3e exhibited relaxing effects on smooth musculature in particular and markedly increased the coronary flow through Langen…
Convenient Synthesis of Biologically Important Retinoids
1995
The toxic and teratogenic effects caused by the highly biologically active (all-E)-retinoic acid and its derivatives prompted us to synthesize a number of retinoids. We developed synthetic approaches to (all-E)-retinyl β-D-glucuronide 3, methyl (retinoyl β-D-glucopyranoside)uronate 5, (all-E)-retinoic acid β-D-glucopyranosyl ester 8 and (all-E)-retinoyl β-D-glucuronide 6 in high purity and yield. Compound 3 was synthesized under Koenigs-Knorr conditions from (all-E)-retinol and an α-halogenose. Compounds 5 and 8 were prepared by esterification of a silver salt of (all-E)-retinoic acid with an α-glycosyl halide in pyridine. (all-E)-Retinoyl β-D-glucuronide 6 was prepared by reaction of (all-…
Oligosaccharide recognition by selectins: Synthesis and biological activity of multivalent sialyl lewis-X ligands
1995
Abstract Trivalent sialyl Lewis-X ligands 6–8 anchored onto flexible templates have been synthesized and evaluated as inhibitors of E-selectin and P-selectin mediated cell adhesion in cell culture assays and in vivo. Biological activities in vitro correlated with spacer length and lead to ligands with 3-fold (E-selectin) and 5-fold (P-selectin) improved receptor binding avidity per single tetrasaccharide moiety.
Synthesis, structural aspects and bioactivity of the marine cyclopeptide hymenamide C
2001
Abstract Head-to-tail proline containing cyclopeptide hymenamide C [cyclo(Leu-Trp-Pro 3 -Phe-Gly-Pro 6 -Glu); 1 ], isolated from a marine sponge and for which a preliminary immunomodulating activity was reported, was efficiently synthesized by a three-dimensional orthogonal solid-phase strategy (Fmoc/tBu/Allyl) via anchoring the ω -carboxyl function of the glutamic acid to the solid support (PAC–PEG–PS). The linear precursor was entirely assembled and subsequently cyclized on resin, yielding a major product identical to the natural hymenamide C and a minor one, a geometric isomer of hymenamide C ( 2 ), differing for the geometry of peptide linkages at Pro residues. Both the ‘proline-rich’ c…
Chromatographic quantitation of the hydrophobicity of ionic compounds by the use of micellar mobile phases
1998
Abstract Many biologically active compounds of interest in structure–activity relationships are ionic at physiological pH. However, ionic organic compounds are only weakly or not retained in conventional RPLC which impedes the chromatographic estimation of their hydrophobicity and the development of quantitative retention–activity relationship studies. The use of micellar mobile phases allows the retention of ionic compounds. Hydrophobic and electrostatic forces govern the retention of ionic compounds in micellar liquid chromatography. In this paper three different retention models log k–log P for ionic compounds are tested (P=partition coefficient). The retention model (log k=a log P+bα+c)…