C4261

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A case of coumarin necrosis with penile and pedal involvement.

Y Harmanyeri et al.

Journal of the European Academy of Dermatology and Venereology : JEADV, 10(3), 248-252 (1998-06-27)

A 57-year-old male patient with advanced adenocarcinoma of the lung, who was administered oral anticoagulant therapy because of pulmonary embolism, developed coumarin necrosis confined to the penis and feet. To our knowledge, this patient showing acral involvement is the seventh

Ultrasound accelerated gelation of novel L-lysine based hydrogelators.

Shangfeng Pan et al.

Chemical communications (Cambridge, England), 49(73), 8045-8047 (2013-08-02)

We reported a novel hydrogelator with L-lysine as a linker to connect 7-carboxyl methoxycoumarin and hydrazine as lipophilic and water-soluble moieties. Ultrasound accelerated the gelation and induced homogenous self-assembly of fibrils into entangled 3D networks. The hydrogel exhibits great potential

Reduction of lipid peroxidation products and advanced glycation end-product precursors by cyanobacterial aldo-keto reductase AKR3G1—a founding member of the AKR3G subfamily.

Jan Hintzpeter et al.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 29(1), 263-273 (2014-11-08)

The purpose of this study was to investigate the origin and function of the aldo-keto reductase (AKR) superfamily as enzymes involved in the detoxification of xenobiotics. We used the cyanobacterium Synechocystis sp. PCC 6803 as a model organism and sequence

Species differences in the metabolism of ritobegron in vitro and assessment of potential interactions with transporters and cytochrome P450 enzymes.

Y Abe et al.

Die Pharmazie, 70(1), 38-46 (2015-05-16)

Ritobegron, a selective β3-adrenoceptor agonist, is the prodrug of the active compound, KUC-7322. We investigated species differences in its metabolism in vitro and the potential for drug-drug interactions with ritobegron. In rat, dog, monkey, and human liver microsomes, ritobegron was

New Coumarin Derivatives as Potent Selective COX-2 Inhibitors: Synthesis, Anti-Inflammatory, QSAR, and Molecular Modeling Studies.

Dina H Dawood et al.

Archiv der Pharmazie, 348(12), 875-888 (2015-10-16)

Two new series of coumarin derivatives incorporating thiazoline and thiazolidinone moieties were designed, synthesized, and investigated in vivo for their anti-inflammatory activities using the carrageenan-induced rat paw edema model and in vitro for their inhibitory activities against the human cyclooxygenase

An updated review of the clinical development of coumarin (1,2-benzopyrone) and 7-hydroxycoumarin.

M E Marshall et al.

Journal of cancer research and clinical oncology, 120 Suppl, S39-S42 (1994-01-01)

Several authors have demonstrated that coumarin (1,2-benzopyrone) in combination with cimetidine can produce objective antitumor responses in some patients with advanced renal cell carcinoma. The purpose of this report is to review the clinical development of coumarin, with or without

Characterization of laminar extrudates manufactured at room temperature in the absence of solvents for the delivery of drugs.

G Oliveira et al.

International journal of pharmaceutics, 454(1), 90-98 (2013-07-13)

Extrudates with laminar shape for delivery of drugs were manufactured at room temperature and without solvents. Different lipidic materials, formulations and extrusion conditions were studied, as well as the influence of the size of particles of coumarin on the release

High-throughput fluorescence assay of cytochrome P450 3A4.

Qian Cheng et al.

Methods in molecular biology (Clifton, N.J.), 987, 157-162 (2013-03-12)

Microtiter plate-based fluorescence assays allow rapid measurement of the catalytic activities of cytochrome P450 oxygenases (P450s). We describe a high-throughput fluorescence assay of P450 3A4, one of the key enzymes involved in xenobiotic metabolism. The assay involves the oxidative debenzylation

Synthesis and biological evaluation of novel coumarin-pyrazoline hybrids endowed with phenylsulfonyl moiety as antitumor agents.

Kamilia M Amin et al.

European journal of medicinal chemistry, 60, 187-198 (2013-01-08)

Two groups of coumarin-pyrazoline hybrids were synthesized. The target compounds were obtained by cyclization of the coumarin chalcones with various substituted hydrazines to produce the corresponding pyrazolines through 1,4-addition on α,β-unsaturated carbonyl system. Selected compounds were investigated for their anticancer

Azorella compacta methanolic extract induces apoptosis via activation of mitogen-activated protein kinase.

Min Hee Sung et al.

Molecular medicine reports, 12(5), 6821-6828 (2015-09-24)

Azorella compacta Phil. (AC) is an alpine medicinal plant used traditionally for antibacterial treatment. Recent studies have revealed that this plant also has anti‑diabetic effects, but that it is toxic. The present study investigated the underlying mechanisms of action of

Toxicology and risk assessment of coumarin: focus on human data.

Klaus Abraham et al.

Molecular nutrition & food research, 54(2), 228-239 (2009-12-22)

Coumarin is a secondary phytochemical with hepatotoxic and carcinogenic properties. For the carcinogenic effect, a genotoxic mechanism was considered possible, but was discounted by the European Food Safety Authority in 2004 based on new evidence. This allowed the derivation of

The Japanese toxicogenomics project: application of toxicogenomics.

Takeki Uehara et al.

Molecular nutrition & food research, 54(2), 218-227 (2009-12-31)

Biotechnology advances have provided novel methods for the risk assessment of chemicals. The application of microarray technologies to toxicology, known as toxicogenomics, is becoming an accepted approach for identifying chemicals with potential safety problems. Gene expression profiling is expected to

Ectopic expression of a stress-inducible glycosyltransferase from saffron enhances salt and oxidative stress tolerance in Arabidopsis while alters anchor root formation.

Oussama Ahrazem et al.

Plant science : an international journal of experimental plant biology, 234, 60-73 (2015-03-26)

Glycosyltransferases play diverse roles in cellular metabolism by modifying the activities of regulatory metabolites. Three stress-regulated UDP-glucosyltransferase-encoding genes have been isolated from the stigmas of saffron, UGT85U1, UGT85U2 and UGT85V1, which belong to the UGT85 family that includes members associated

Autoimmune disease-associated variants of extracellular endoplasmic reticulum aminopeptidase 1 induce altered innate immune responses by human immune cells.

Yasser A Aldhamen et al.

Journal of innate immunity, 7(3), 275-289 (2015-01-17)

Endoplasmic reticulum aminopeptidase 1 (ERAP1) gene polymorphisms have been linked to several autoimmune diseases; however, the molecular mechanisms underlying these associations are not well understood. Recently, we demonstrated that ERAP1 regulates key aspects of the innate immune response. Previous studies

Fluorescent protein-tagged Vpr dissociates from HIV-1 core after viral fusion and rapidly enters the cell nucleus.

Tanay M Desai et al.

Retrovirology, 12, 88-88 (2015-10-30)

HIV-1 Vpr is recruited into virions during assembly and appears to remain associated with the viral core after the reverse transcription and uncoating steps of entry. This feature has prompted the use of fluorescently labeled Vpr to visualize viral particles

The antitumor activity of PNA modified vinblastine cationic liposomes on Lewis lung tumor cells: In vitro and in vivo evaluation.

Xue-Tao Li et al.

International journal of pharmaceutics, 487(1-2), 223-233 (2015-04-22)

Non-small cell lung cancer (NSCLC) is one of the frequently-occurring disease in the world, and the treatment effects are usually unsatisfactory. Vinblastine is an anti-microtubule drug in clinic. In this study, a nanostructured liposome was designed and prepared for treating

Expression and function of aminopeptidase N/CD13 produced by fibroblast-like synoviocytes in rheumatoid arthritis: role of CD13 in chemotaxis of cytokine-activated T cells independent of enzymatic activity.

Rachel Morgan et al.

Arthritis & rheumatology (Hoboken, N.J.), 67(1), 74-85 (2014-09-16)

Aminopeptidase N/CD13 (EC 3.4.11.2) is a metalloproteinase expressed by fibroblast-like synoviocytes (FLS). It has been suggested that CD13 can act chemotactically for T cells in rheumatoid arthritis (RA). We undertook this study to measure CD13 in vivo and in vitro

3-Phenylcoumarin derivatives selectively modulate different steps of reactive oxygen species production by immune complex-stimulated human neutrophils.

Micássio F Andrade et al.

International immunopharmacology, 15(2), 387-394 (2013-01-22)

Immune complex (IC) deposition in tissues triggers the release of harmful oxidant and lytic compounds by neutrophils. We examined how ten 3-phenylcoumarin derivatives affect the reactive oxygen species (ROS) production by IC-stimulated human neutrophils. Most of the 3-phenylcoumarins inhibited the

Quercetin and Coumarin Inhibit Dipeptidyl Peptidase-IV and Exhibits Antioxidant Properties: In Silico, In Vitro, Ex Vivo.

Anand-Krishna Singh et al.

Biomolecules, 10(2) (2020-02-07)

Quercetin and coumarin, two naturally occurring phytochemicals of plant origin, are known to regulate hyperglycemia and oxidative stress. The present study was designed to evaluate the inhibitory activity of quercetin and coumarin on dipeptidyl peptidase-IV (DPP-IV) and their antioxidant potential.

2-Phenylethynesulfonamide (PES) uncovers a necrotic process regulated by oxidative stress and p53.

Paolo Mattiolo et al.

Biochemical pharmacology, 91(3), 301-311 (2014-08-21)

2-Phenylethynesulfonamide (PES) or pifithrin-μ is a promising anticancer agent with preferential toxicity for cancer cells. The type of cell death and the molecular cascades activated by this compound are controversial. Here, we demonstrate PES elicits a caspase- and BAX/BAK-independent non-necroptotic

Photo responsive monoolein cubic phase containing coumarin-Tween 20 conjugates.

Jing Dai et al.

Drug development and industrial pharmacy, 39(9), 1457-1463 (2013-08-02)

Photo-responsive monoolein (MO) cubic phase was developed by incorporating coumarin-Tween 20 conjugate in the cubic phase. 7-chlorocarbonylmethoxycoumarin was obtained from 7-hydroxycoumarin through three-step reactions with the yield of 19.8% and it was conjugated to the head group of Tween 20.

Extension of a dynamic headspace multi-volatile method to milliliter injection volumes with full sample evaporation: Application to green tea.

Nobuo Ochiai et al.

Journal of chromatography. A, 1421, 103-113 (2015-08-16)

An extension of multi-volatile method (MVM) technology using the combination of a standard dynamic headspace (DHS) configuration, and a modified DHS configuration incorporating an additional vacuum module, was developed for milliliter injection volume of aqueous sample with full sample evaporation.

Anti-inflammatory actions of herbal formula Gyejibokryeong-hwan regulated by inhibiting chemokine production and STAT1 activation in HaCaT cells.

Soo-Jin Jeong et al.

Biological & pharmaceutical bulletin, 38(3), 425-434 (2015-03-12)

Gyejibokryeong-hwan (GJBRH; Keishi-bukuryo-gan in Japan and Guizhi Fuling Wan in China) is a traditional herbal formula comprising five medicinal herbs and is used to treat climacteric syndrome. GJBRH has been shown to exhibit biological activity against diabetes, diabetic nephropathy, atherosclerosis

A review of coumarin derivatives in pharmacotherapy of breast cancer.

Musiliyu A Musa et al.

Current medicinal chemistry, 15(26), 2664-2679 (2008-11-11)

The coumarin (benzopyran-2-one, or chromen-2-one) ring system, present in natural products (such as the anticoagulant warfarin) that display interesting pharmacological properties, has intrigued chemists and medicinal chemists for decades to explore the natural coumarins or synthetic analogs for their applicability

Low cost referenced luminescent imaging of oxygen and pH with a 2-CCD colour near infrared camera.

Josef Ehgartner et al.

The Analyst, 139(19), 4924-4933 (2014-08-07)

A low cost imaging set-up for optical chemical sensors based on NIR-emitting dyes is presented. It is based on a commercially available 2-CCD colour near infrared camera, LEDs and tailor-made optical sensing materials for oxygen and pH. The set-up extends

Metabolic drug-drug interaction potential of macrolactin A and 7-O-succinyl macrolactin A assessed by evaluating cytochrome P450 inhibition and induction and UDP-glucuronosyltransferase inhibition in vitro.

Soo Hyeon Bae et al.

Antimicrobial agents and chemotherapy, 58(9), 5036-5046 (2014-06-04)

Macrolactin A (MA) and 7-O-succinyl macrolactin A (SMA), polyene macrolides containing a 24-membered lactone ring, show antibiotic effects superior to those of teicoplanin against vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus. MA and SMA are currently being evaluated as antitumor agents

Mitochondrial targeting of bilirubin regulatory enzymes: An adaptive response to oxidative stress.

Siti Nur Fadzilah Muhsain et al.

Toxicology and applied pharmacology, 282(1), 77-89 (2014-12-06)

The intracellular level of bilirubin (BR), an endogenous antioxidant that is cytotoxic at high concentrations, is tightly controlled within the optimal therapeutic range. We have recently described a concerted intracellular BR regulation by two microsomal enzymes: heme oxygenase 1 (HMOX1)

In Vitro Inhibition of Human Placental Glutathione S-Transferase by 3-Arylcoumarin Derivatives.

Mustafa Muhlis Alparslan et al.

Archiv der Pharmazie, 348(9), 635-642 (2015-07-25)

Glutathione S-transferases (EC: 2.5.1.18, GSTs) are phase II detoxification enzymes that catalyze the conjugation of various electrophilic compounds to glutathione (GSH), thus usually producing less reactive and more water soluble compounds. However, there is evidence that elevated expression of GSTs

In silico methods for physiologically based biokinetic models describing bioactivation and detoxification of coumarin and estragole: implications for risk assessment.

Ivonne M C M Rietjens et al.

Molecular nutrition & food research, 54(2), 195-207 (2009-11-28)

In chemical safety assessment, information on adverse effects after chronic exposure to low levels of hazardous compounds is essential for estimating human risks. Results from in vitro studies are often not directly applicable to the in vivo situation, and in

Gemcitabine-coumarin-biotin conjugates: a target specific theranostic anticancer prodrug.

Sukhendu Maiti et al.

Journal of the American Chemical Society, 135(11), 4567-4572 (2013-03-07)

We present here, the design, synthesis, spectroscopic characterization, and in vitro biological assessment of a gemcitabine-coumarin-biotin conjugate (5). Probe 5 is a multifunctional molecule composed of a thiol-specific cleavable disulfide bond, a coumarin moiety as a fluorescent reporter, gemcitabine (GMC)

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