benzofurans and Hemolysis

Ultrasound- and microwave-assisted green synthetic strategies were applied to furnish benzofuran-oxadiazole

Topics: A549 Cells; Antineoplastic Agents; Benzofurans; Cell Survival; Chemistry Techniques, Synthetic; Hemolysis; Humans; Microwaves; Molecular Docking Simulation; Neoplasms; Oxadiazoles; Triazoles

Combination of photodynamic therapy (PDT) and photothermal therapy (PTT) generally requires different components to build a composite irradiated with different excitation lights. One component photoactive agent for enhanced combination of PDT and PTT under the excitation of a single wavelength light source is more urgent in tumor phototherapy via adjusting spatial arrangement of photoactive units. Herein, porphyrin-based covalent organic framework nanoparticles (COF-366 NPs) were synthesized to control the orderly spatial arrangement of the photoactive building units and firstly used for antitumor therapy in vivo. COF-366 NPs provide the simultaneous therapy of PDT and PTT under a single wavelength light source with the monitoring of photoacoustic (PA) imaging, which makes the operation simpler and more convenient. COF-366 NPs had achieved good phototherapy effect even in the face of large tumors. The prepared multifunctional COF-366 NPs open up a new avenue to phototherapeutic materials and expand the application range of covalent organic framework.

Topics: Animals; Benzofurans; Cell Line, Tumor; Combined Modality Therapy; Female; Hemolysis; Magnetic Resonance Spectroscopy; Mice; Mice, Inbred BALB C; Mice, Nude; Nanoparticles; Neoplasm Transplantation; Neoplasms; Neoplasms, Experimental; Organic Chemicals; Photoacoustic Techniques; Phototherapy; Porphyrins; Rabbits; Reactive Oxygen Species

The intention of present research work is to formulate usnic acid (UA) loaded heparin modified gellan gum (HAG) nanoparticles (NPs). HAG copolymer based conjugation was synthesized and characterized by

Topics: A549 Cells; Adipates; Animals; Antineoplastic Agents; Apoptosis; Benzofurans; Cell Cycle; Drug Carriers; Drug Liberation; Erythrocytes; Hematologic Tests; Hemolysis; Heparin; Humans; Male; Nanoparticles; Polysaccharides, Bacterial; Rats

Synthesis of natural products has speeded up drug discovery process by minimizing the time for their purification from natural source. Several diseases like Alzheimer's disease (AD) demand exploring multi targeted drug candidates, and for the first time we report the multi AD target inhibitory potential of synthesized dihydroactinidiolide (DA). Though the activity of DA in several solvent extracts have been proved to possess free radical scavenging, anti bacterial and anti cancer activities, its neuroprotective efficacy has not been evidenced yet. Hence DA was successfully synthesized from β-ionone using facile two-step oxidation method. It showed potent acetylcholinesterase (AChE) inhibition with half maximal inhibitory concentration (IC

Topics: Acetylcholinesterase; Amyloid beta-Peptides; Animals; Benzofurans; Catalytic Domain; Cell Line, Tumor; Cholinesterase Inhibitors; Free Radical Scavengers; Hemolysis; Humans; Mice; Molecular Docking Simulation; Molecular Dynamics Simulation; Neuroprotective Agents; Peptide Fragments; Protein Multimerization; Reactive Oxygen Species

Leishmaniasis is an infectious disease complex caused by protozoa from the Leishmania genus, which presents a broad spectrum of clinical manifestations: cutaneous, mucocutaneous and visceral forms. The current treatments are unsatisfactory considering that few drugs are available and present some level of toxicity. Many lignans and neolignans have been used for the development of new antileishmania drugs. The capability in vitro of the neolignan 2,3-dihydrobenzofuran (2,3-DBF), a commonly found constituent of propolis and other plants, to inhibit the growth of promastigote and macrophage-internalized amastigote forms of Leishmania amazonensis was investigated. The cytotoxicity of this compound was assessed by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) test in BALB/c murine macrophages and human erythrocyte lysis assay. The 2,3-DBF was active against promastigote (IC

Topics: Animals; Antiprotozoal Agents; Benzofurans; Erythrocytes; Hemolysis; Humans; Hydroxylation; Inhibitory Concentration 50; Leishmania; Lignans; Lysosomes; Macrophage Activation; Macrophages, Peritoneal; Mice, Inbred BALB C; Nitric Oxide; Osmolar Concentration; Phagocytosis

Usnic acid (UA) has been associated with chronic diseases through its antioxidant action. Its main target is the cell membrane; however, its effect on that of human erythrocytes has been scarcely investigated. To gain insight into the molecular mechanisms of the interaction between UA and cell membranes human erythrocytes and molecular models of its membrane have been utilized. Dimyristoylphosphatidylcholine (DMPC) and dimyristoylphosphatidylethanolamine (DMPE) were chosen as representative of phospholipid classes located in the outer and inner monolayers of the erythrocyte membrane, respectively. Results by X-ray diffraction showed that UA produced structural perturbations on DMPC and DMPE bilayers. DSC studies have indicated that thermotropic behavior of DMPE was most strongly distorted by UA than DMPC, whereas the latter is mainly affected on the pretransition. Scanning electron (SEM) and defocusing microscopy (DM) showed that UA induced alterations to erythrocytes from the normal discoid shape to echinocytes. These results imply that UA molecules were located in the outer monolayer of the erythrocyte membrane. Results of its antioxidant properties showed that UA neutralized the oxidative capacity of HClO on DMPC and DMPE bilayers; SEM, DM and hemolysis assays demonstrated the protective effect of UA against the deleterious oxidant effects of HClO upon human erythrocytes.

Topics: Antioxidants; Benzofurans; Cell Shape; Cells, Cultured; Dimyristoylphosphatidylcholine; Dose-Response Relationship, Drug; Erythrocyte Membrane; Erythrocytes; Hemolysis; Humans; Hypochlorous Acid; Lipid Bilayers; Microscopy; Microscopy, Electron, Scanning; Models, Molecular; Molecular Structure; Phosphatidylethanolamines; X-Ray Diffraction

The misfolding of human islet amyloid polypeptide (hIAPP) is regarded as one of the causative factors of type 2 diabetes mellitus (T2DM). Salvia miltiorrhiza (Danshen), one of the most commonly used of traditional Chinese medicines, is often used in Compound Recipes for treating diabetes, however with unclear mechanisms. Since salvianolic acid B (SalB) is the most abundant bioactive ingredient of salvia miltiorrhiza water-extract. In this study, we tested whether SalB has any effect on the amyloidogenicity of hIAPP. Our results clearly suggest that SalB can significantly inhibit the formation of hIAPP amyloid and disaggregate hIAPP fibrils. Furthermore, photo-crosslinking based oligomerization studies suggest SalB significantly suppresses the toxic oligomerization of hIAPP monomers. Cytotoxicity protection effects on pancreatic INS-1 cells by SalB were also observed using MTT-based assays, potentially due to the inhibition on the membrane disruption effects and attenuated mitochondria impairment induced by hIAPP. These results provide evidence that SalB may further be studied on the possible pharmacological treatment for T2DM.

Topics: Amino Acid Sequence; Amyloid; Benzofurans; Cell Line; Cell Survival; Diabetes Mellitus, Type 2; Drugs, Chinese Herbal; Erythrocytes; Hemolysis; Humans; Insulin-Secreting Cells; Islet Amyloid Polypeptide; Mitochondria; Molecular Sequence Data; Protein Structure, Secondary; Salvia miltiorrhiza

Viper envenomation undeniably induces brutal local manifestations such as haemorrhage, oedema and necrosis involving massive degradation of extracellular matrix at the bitten region and many a times results in dangerous systemic haemorrhage including pulmonary shock. Snake venom metalloproteases (SVMPs) are being considered to be the primary culprits for the venom-induced haemorrhage. As a consequence, the venom researchers and medical practitioners are in deliberate quest of SVMP inhibitors. In this study, we evaluated the inhibitory effect of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran-5-carbonitrile (DFD) on viper venom-induced haemorrhagic and PLA(2) activities. DFD effectively neutralized the haemorrhagic activity of the medically important viper venoms such as Echis carinatus, Echis ocelatus, Echis carinatus sochureki, Echis carinatus leakeyi and Crotalus atrox in a dose-dependent manner. The histological examinations revealed that the compound DFD effectively neutralizes the basement membrane degradation, and accumulation of inflammatory leucocytes at the site of Echis carinatus venom injection further confirms the inhibition of haemorrhagic activity. In addition, DFD dose dependently inhibited the PLA(2) activities of Crotalus atrox and E. c. leakeyi venoms. According to the docking studies, DFD binds to hydrophobic pocket of SVMP with the ki of 19.26 × 10(-9) (kcal/mol) without chelating Zn(2+) in the active site. It is concluded that the clinically approved inhibitors of haemorrhagins could be used as a potent first-aid agent in snakebite management. Furthermore, a high degree of structural and functional homology between SVMPs and their relatives, the MMPs, suggests that DFD analogues may find immense value in the regulation of multifactorial pathological conditions like inflammation, cancer and wound healing.

Topics: Animals; Benzofurans; Citalopram; Dose-Response Relationship, Drug; Enzyme Inhibitors; Erythrocytes; Hemolysis; Hemorrhage; Humans; Male; Mice; Phospholipases A; Protein Binding; Skin; Viper Venoms

The rhodamine B (RhB) covalently grafted SBA-15-structured mesoporous silica nanoparticles (MSNs-RhB) of high surface area (750 m(2) g(-1)), large pore volume (0.7 cm(3) g(-1)), uniform particle size (about 400 nm) and positively charged surface (29.6 +/- 5.0 mV), has been developed as a drug delivery system (SAB@MSNs-RhB) for anti-ROS (reactive oxygen species)/hepatic fibrosis by loading a negatively charged drug salvianolic acid B (SAB). The dosage formulation SAB@MSNs-RhB effectively protected the loaded drug SAB from decomposition. The multi-release experimental results showed that SAB@MSNs-RhB exhibited an outstanding SAB sustained-release property, and relatively high SAB release rates and concentrations in a long term after the consumption of previously released SAB as compared to SAB loaded MSNs (SAB@MSNs) of negatively charged surface (-31.1 +/- 2.6 mV). The influences of the drug concentration, incubation time, drug formula and drug carrier on the ROS level, proliferative activity and cytotoxicity of LX-2 cells were evaluated. The results showed that the inhibiting effect of SAB@MSNs-RhB on the ROS level and proliferative activity of LX-2 cells was more remarkable than free SAB in a long term (72 h), and became more intensive with the increase of the sample concentration and the incubation time. SAB@MSNs-RhB enhanced the cellular drug uptake, the drug bioaccessability and efficacy for anti-ROS/hepatic fibrosis via the nanoparticles-mediated endocytosis and the sustained release of the drug. There was no visible cytotoxicity of free SAB, MSNs-RhB and SAB@MSNs-RhB against LX-2 cells in a broad concentration range (0.5-100 microm) and incubation time periods up to 72 h. The blood compatibility of the carrier MSNs-RhB was evaluated by investigating the hemolysis and coagulation behaviors in a broad concentration range (50-500 microg mL(-1)) under in vitro conditions. The results suggested that MSNs-RhB possessed good blood compatibility.

Topics: Benzofurans; Biocompatible Materials; Cell Line; Cell Proliferation; Drug Carriers; Drug Delivery Systems; Drugs, Chinese Herbal; Fluorescent Dyes; Hemolysis; Humans; Liver Cirrhosis; Materials Testing; Molecular Structure; Nanoparticles; Particle Size; Porosity; Reactive Oxygen Species; Rhodamines

Six 3H-spiro[benzofuran-2,1'-cyclohexane] derivatives were synthesized from naturally occurring filifolinol, and their classical complement pathway inhibitory activity was determined. IC(50) values of the most potent compounds were comparable to the activity of the natural complement inhibitor K76-COOH and some synthetic tricyclic analogs of it.

Topics: Animals; Benzofurans; Complement Pathway, Classical; Cyclohexanes; Hemolysis; Heterocyclic Compounds, 3-Ring; Humans; Inhibitory Concentration 50; Plant Extracts; Sesquiterpenes; Sheep; Spiro Compounds; Structure-Activity Relationship; Tritium

The present study was designed to examine whether lithospermic acid B (LSB) isolated from Salvia miltiorrhiza has an ameliorative effect on renal functional parameters in association with the expression of aquaporin 2 (AQP 2) and Na,K-ATPase in the ischemia-reperfusion induced acute renal failure (ARF) rats. LSB showed strong antioxidant activity against production of reactive oxygen species (ROS), ROS-induced hemolysis, and production of lipid peroxide in a dose-dependent manner. Polyuria caused by down-regulation of renal AQP 2 in the ischemia-reperfusion induced ARF rats was partially restored by administration of LSB (40 mg/kg, i.p.), restoring expression of AQP 2, in renal inner and outer medulla. The expression of Na,K-ATPase alpha1 subunit in outer medulla of the ARF rats was also restored in the ARF rats by administration of LSB, while beta1 subunit level was not altered. The renal functional parameters including creatinine clearance, urinary sodium excretion, urinary osmolality, and solute-free reabsorption were also partially restored in ischemia-ARF rats by administration of LSB. Histological study also showed that renal damages in the ARF rats were abrogated by administration of LSB. Taken together, these data indicate that LSB ameliorates renal defects in rats with ischemia-reperfusion induced ARF, most likely via scavenging of ROS.

Topics: Acute Kidney Injury; Animals; Aquaporin 2; Aquaporins; Benzofurans; Blotting, Western; Depsides; Enzyme Inhibitors; Erythrocytes; Free Radical Scavengers; Hemolysis; Hydroxyl Radical; In Vitro Techniques; Kidney; Kidney Function Tests; Lipid Peroxidation; Male; Oxidants; Plant Roots; Proteins; Rats; Rats, Sprague-Dawley; Reperfusion Injury; Salvia miltiorrhiza; Sodium-Potassium-Exchanging ATPase; Superoxides

Topics: Amiodarone; Benzofurans; Cell Survival; Erythrocytes; Hemolysis; Humans; Lymphocytes; Ultraviolet Rays

Topics: Adult; Benzofurans; Depression, Chemical; Deuterium; Erythrocytes; Hemolysis; Histidine; Humans; Kynurenic Acid; Oxidation-Reduction; Oxygen; Silicon Dioxide; Solvents; Stimulation, Chemical; Ultraviolet Rays; Water; Xenon