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... (+)- and (−)-Ganodilactone (1), a pair of novel meroterpenoid dimers possessing a unique 5′H-spiro[chroman-4,2′-furan]-2,5′-dione ring system, along with their biogeneticly-related compound, ganomycin I (2), were discovered from the fruiting bodies of Ganoderma leucocontextum. The structures and absolute configurations were assigned with the aid of 1D and 2D NMR spectra, HRESIMS analysis and ECD c ...
... BACKGROUND: Organophosphorus pesticides (OP’s) are heavily constituted in agriculture, gardens, home and veterinary and although it is useful, there are concerns about the environment, safety and health of human and animals. In this study, we investigated the effects of a new oxime, (3Z)-5-Chloro-3-(Hydroxyimino)indolin-2-one (OXIME) against the alterations induced by malathion, an OP insecticide, ...
... Bioassay-guided fractionation of the ethanolic extract from the whole plants of Pteridium aquilinum has resulted in the isolation of a new pterosin glycoside, (‒)-pteroside N (1), and a new seco-illudoid sesquiterpene, pterosinone (2). Their structures were identified by analysis of the spectroscopic data including extensive 2D NMR. All of the isolates were evaluated for the anti-Alzheimer disease ...
... The yeast Torula corallina is a strong erythritol producer that is used in the industrial production of erythritol. However, melanin accumulation during culture represents a serious problem for the purification of erythritol from the fermentation broth. Melanin biosynthesis inhibitors such as 3,4-dihydroxyphenylalanine and 1,8-dihydroxynaphthalene (DHN)-melanin inhibitors were added to the T. cora ...
... 1-Deoxynojirimycin (1-DNJ), an iminosugar rich in mulberry, has been shown to possess antimetastatic potential. The antimetastatic mechanisms of 1-DNJ in melanoma B16F10 cells were studied, as were the antimetastatic activity (cell adhesion, migration, and invasion) of 1-DNJ, matrix metalloproteinases (MMP-2 and MMP-9), tissue inhibitors of metalloproteinase (TIMP-1 and TIMP-2) mRNA, and flow cyto ...
... To investigate the effects of postharvest application of 1-MCP on ethylene production and fruit softening, activities of ethylene biosynthesis and fruit softening enzymes were measured during postharvest ripening of plum (Prunus salicina Lindl. cv. Tegan Blue) fruit after being exposed to 1-MCP (0, 0.5, 1.0 or 2.0 microliter L⁻¹) at 20 ± 1 °C for 24 h. Following the treatments, fruit were allowed ...
... Aim of the study: Rheumatoid arthritis synovial fibroblasts (RASFs) are known to produce matrix metalloproteinases (MMPs) and cause joint destruction. The purpose of this study is to develop a potential medicine for rheumatoid arthritis (RA). Materials and methods: To this end, first, the MMPs inhibition factor was purified from an alkali-solubilized fraction of RJ (Apis mellifera) by C18 reverse- ...
... Schistosomiasis, caused by trematodes of the genus Schistosoma, remains an important public health issue. Adult schistosomes can survive in the definitive host for several decades, although they are subject to the host immune response. Consequently, understanding the mechanism underlying worm survival in the definitive hosts could aid in developing novel strategies against schistosomiasis. We prev ...
... Culinary herbs and spices are widely used ethnomedically across Africa. They are traditionally employed in the treatment of several ailments including inflammation disorders, pain alleviation and infectious diseases. Pharmacological studies are necessary to provide a scientific basis to substantiate their traditional use and safety. In this study, the 15-lipoxygenase inhibitory, antioxidant, antim ...
... To evaluate the 15-lipoxygenase inhibitory activity of the methanol leaf extracts of Commelina benghalensis, Tradescantia fluminensis (T. fluminensis) and Tradescantia zebrina.The inhibitory activity was evaluated using a spectrophotometric assay by observing the increase in absorbance at 234 nm due to the formation of the product 13-hydroperoxyoctadecadienoic acid. The extracts were also tested f ...
... Ring D-modified gibberellin (GA) A5 and A20 derivatives are structurally similar to GA20 and GA9 (the precursors to growth-active GA1 and GA4) and, when applied to higher plants, especially grasses, can reduce shoot growth with concomitant reductions in levels of growth-active GAs and increases in levels of their immediate 3-deoxy precursors. The recombinant Arabidopsis GA 3-hydroxylase (AtGA3ox1) ...
RNA interference; apoptosis; autophagosomes; autophagy; cathepsin D; cell lines; cell viability; children; children at risk; enzyme inhibition; flow cytometry; fluorescent antibody technique; gene expression; gene targeting; heat stress; heat-shock protein 90; image analysis; immunoblotting; lymphocytic leukemia; lysosomes; messenger RNA; neoplasm cells; patients; pharmacology; protein synthesis; staining; water solubility
Abstract:
... B-lineage acute lymphoblastic leukemia (B-ALL) is most common in children. We had reported heat shock protein 90 (Hsp90) over-expressed in high risk B-ALL children. 17-DMAG is a water soluble Hsp90 inhibitor, which was proved to be effective for advanced solid tumors and hematological malignancy. However, there is little research on its application in newly diagnosed B-ALL. And the detailed mechan ...
... 20(S)-Protopanaxadiol [20(S)-PPD], one of the metabolites of ginsenosides, was investigated to determine its potential mechanism for targeting to epidermal growth factor receptor (EGFR) pathway in lung cancer cell A549. Results of kinase inhibitory assay showed that 20(S)-PPD was an EGFR tyrosine kinase inhibitor. By binding to EGFR, 20(S)-PPD disrupted the EGFR/MAPK signaling. The expression of g ...
... A 20-kDa protein (p20) with a GTP binding activity was purified from the cultured cells of Glycine max (soybean). The amino acid sequence of p20 showed 65% identity in a 23 amino acid overlap against the Kunitz-type trypsin inhibitor of soybean reported. Furthermore, it was found that a Kunitz-type soybean trypsin inhibitor of commercial origin also binds GTP. ...
... Semen cryopreservation is critical for appropriate planning of both AI and IVF trials, improving the benefit:cost ratio. However, cryopreservation induces damage in mammalian spermatozoa, resulting in decreased fertility (Medeiros et al. 2002 Theriogenology 57, 327-344). It is known that cryopreservation and thawing induce apoptosis in a variety of cells, including bovine sperm (Anzar et al. 2002 ...
... Trypsin from the pyloric ceca of Atlantic bonito (Sarda sarda) was purified and characterized with respect to its purity; molecular weight; sensitivity to temperature, pH, and inhibition; and N-terminal sequence. The purified trypsin had a molecular weight of 29 kDa as per sodium dodecyl sulfate polyacrylamide gel electrophoresis, and optimal activity was observed at pH 9 and 65 °C with BAPNA as a ...
... Avian influenza is a serious zoonotic infectious disease with huge negative impacts on local poultry farming, human health and social stability. Therefore, the design of new compounds against avian influenza has been the focus in this field. In this study, computational methods were applied to investigate the compounds with neuraminidase inhibitory activity. First, 2D-SAR model was built to recogn ...
... The naturally occurring (6Z)‐(±)‐2‐methoxy‐6‐hexadecenoic acid (1) and (6Z)‐(±)‐2‐methoxy‐6‐octadecenoic acid (2) were synthesized in 7–8 steps with 38 and 13% overall yields, respectively, by using an acetylide coupling approach, which made it possible to obtain a 100% cis‐stereochemistry for the double bonds. In a similar fashion, the acetylenic analogs (±)‐2‐methoxy‐6‐hexadecynoic acid (3) and ...
... This study evaluated the hypolipidemic and antiobesity effects of phloroacetophenone (2′,4′,6′-trihydroxyacetophenone, THA) isolated from Myrcia multiflora and their relationship with triglyceride (TG) intestinal absorption and pancreatic lipase activity inhibition. The hypolipidemic effect of THA was evaluated by acute (Triton WR-1339 treatment) and chronic assay (high-fat diet treatment), the an ...
... To observe the direct effects of 3,4,5,6-tetrahydroxyxanthone on connexin43 (Cx43) expression in cultured endothelial cells, cells were treated with lysophosphatidylcholine (LPC, 10 mg/l) for 24 h in the presence or absence of different concentrations of 3,4,5,6-tetrahydroxyxanthone (1, 3, or 10 μmol l⁻ ¹). The reactive oxygen species (ROS) production, cell viability, asymmetric dimethylarginine ( ...
... DNA is considered to be one of the most promising targets for anticancer agents. Acridine analogues have anticancer activity based on DNA binding and topoisomerases inhibition. However, due to the side effects, resistance and low bioavailability, a few have entered into clinical usage and the mechanisms of action are not fully understood. Novel acridine derivatives are needed for effective cancer ...
... Tyrosinase is one of the key enzymes in mammalian melanin biosynthesis. Decreasing tyrosinase activity has been targeted for the prevention of conditions related to the hyperpigmentation of the skin, such as melasma and age spots. This paper is devoted to the engineering of vesicle formulations loaded with 3-hydroxycoumarin for topical pharmaceutical applications. At first, it was demonstrated the ...
... It is recognized that the air pollution is associated with the pathogenesis of airway diseases. This study aims to elucidate the role of the 3-methyl-4-nitrophenol (PNMC), one of the components of diesel-exhaust particles, in compromising the airway epithelial barrier integrity.A549 cells, an airway epithelial cell line, were cultured to monolayers to be used as an in vitro epithelial barrier mode ...
... Curcumin derivatives have been shown to inhibit replication of human influenza A viruses (IAVs). However, it is not clear whether curcumin and its derivatives can inhibit neuraminidase (NA) of influenza virus. In this study, a meaningful 3D quantitative structure–activity relationship model (comparative molecular field analysis R² = 0.997, q² = 0.527, s = 0.064, F = 282.663) was built to understan ...
DNA; DNA damage; DNA topoisomerase; Euphorbia kansui; Western blotting; apoptosis; caspase-3; cell cycle; cell proliferation; enzyme activity; enzyme inhibition; gene expression regulation; medicinal plants
Abstract:
... We have previously reported that many ingenol compounds derived from Euphorbia kansui exhibit topoisomerase (topo) II inhibitory activity. Of these compounds, 3EZ,20Ac-ingenol inhibited topo I activity. Camptothecin, which inhibits the religation activity of topo I without interfering with the binding of topo I to DNA and induces topo I-mediated DNA cleavage, was used as a positive control. In thi ...
... Telomere and telomerase were closely related to the occurrence and development of some cancers. After the key active site of telomerase was identified, to enhance the ability of dihydropyrazole derivatives to inhibit telomerase, we designed a series of novel 4,5-dihydropyrazole derivatives containing heterocyclic oxygen moiety based on previous studies. The telomerase inhibition assay showed that ...
... Corneal endothelial cells serve as a limiting factor in the ability to preserve whole cornea for proper utilization, such as transplantation. Previous reports have demonstrated the importance of proper endothelial maintenance during preservation for improved corneal function. As such, analyses into the modes of cell death will allow for future in-depth investigations of the complex stresses and re ...
Marie E. Migaud; Rupert C. Wilmouth; Gary I. Mills; Gareth J. Wayne; Catherine Risley; Christopher Chambers; Simon J. F. Macdonald; Christopher J. Schofield
... Staphylococcus epidermidis (S. epidermidis) is a common bacterial colonizer on the surface of human skin. Lactate is a natural constituent of skin. Here, we reveal that S. epidermidis used sodium l-lactate as a carbon source to undergo fermentation and yield malodors detected by gas colorimetric tubes. Several furan compounds such as furfural originating from the fermentation metabolites play a ro ...
... Five tannin-related compounds – gallic acid, flavogallonic acid dilactone, valoneic acid dilactone, gallagyldilactone, ellagic acid – were isolated from the heartwood of Shorea laeviforia, and the inhibitory activity of each against rat liver 5Α-reductase was evaluated. Valoneic acid dilactone and gallagyldilactone exhibited positive inhibitory activity, but gallic acid and ellagic acid did not. F ...
Carthamus tinctorius; Phyllanthus emblica; alopecia; enzyme inhibition; ethanol; growth promotion; herbs; loss prevention; mechanism of action; mice; rats
Abstract:
... ETHNOPHARMACOLOGICAL RELEVANCE: Many Thai traditional herbs have been used for hundreds of years for hair treatment and nourishment, including hair loss. However, scientific evidence about their mechanisms of action has not yet been elucidated. AIMS OF THE STUDY: The purpose of this research is to define the possible mechanisms involved in hair loss treatment of the selected plants by determining ...
... Exactly how failure through conceptus-endometrial signalling on Day 16 of pregnancy causes early embryo mortality (EM) is yet unknown. It was hypothesised that EM pregnancies are associated with an impaired endocrine action of interferon tau (IFNT) from the conceptus on the corpus luteum (CL) and peripheral blood mononuclear cells (PBMC), in addition to paracrine failure in preventing the upregula ...
... Supplementation of glutamine to porcine embryo culture medium improves blastocyst development, increases leucine consumption, and enhances mitochondrial activity. In cancer cells, glutamine has been implicated in the phosphorylation and activation of mechanistic target of rapamycin (MTOR) to support rapid cellular proliferation. The objective of this study was to determine if phosphorylation of MT ...
... Alpha amylases are hydrolytic enzymes that are widespread in nature, being found in animals, microorganisms, and plants. These enzymes hydrolyze starch molecules into reducing sugars. Alpha amylases from microbial sources have several applications in industrial sectors. This enzyme is an effective target for the development of anti‐fungal agents. The binding affinity and enzyme inhibitory properti ...
... A series of 3H-1,2-benzoxathiepine 2,2-dioxides incorporating 7-acylamino moieties were obtained by an original procedure starting from 5-nitrosalicylaldehyde, which was treated with propenylsulfonyl chloride followed by Wittig reaction of the bis-olefin intermediate. The new derivatives, belonging to the homosulfocoumarin chemotype, were assayed as inhibitors of the zinc metalloenzyme carbonic an ...
... Decapping scavenger (DcpS) enzymes catalyze the cleavage of a residual cap structure following 3′ → 5′ mRNA decay. Some previous studies suggested that both m⁷GpppG and m⁷GDP were substrates for DcpS hydrolysis. Herein, we show that mononucleoside diphosphates, m⁷GDP (7-methylguanosine diphosphate) and m₃²,²,⁷GDP (2,2,7-trimethylguanosine diphosphate), resulting from mRNA decapping by the Dcp1/2 c ...
... 9,10-Phenanthrenequinone (9,10-PQ), a major quinone in diesel exhaust particles, induces apoptosis via the generation of reactive oxygen species (ROS) because of 9,10-PQ redox cycling. We have found that intratracheal infusion of 9,10-PQ facilitates the secretion of surfactant into rat alveolus. In the cultured rat lung, treatment with 9,10-PQ results in an increase in a lower-density surfactant b ...
... A library of 2(a),3(a/e)-difluorosialic acids and their C-5 and/or C-9 derivatives were chemoenzymatically synthesized. Pasteurella multocida sialic acid aldolase (PmAldolase), but not its Escherichia coli homologue (EcAldolase), was found to catalyze the formation of C5-azido analogue of 3-fluoro(a)-sialic acid. In comparison, both PmAldolase and EcAldolase could catalyze the synthesis of 3-fluor ...
Laura Micheli; Elena Lucarini; Elena Trallori; Carmen Avagliano; Carmen De Caro; Roberto Russo; Antonio Calignano; Carla Ghelardini; Alessandra Pacini; Lorenzo Di Cesare Mannelli
... To examine the effects of the alpha-amylase inhibitor isoform 1 called phaseolamin, a standardized extract from white kidney beans (Phaseolus vulgaris L.) was tested against the hallmarks of metabolic syndrome. The efficacy of a per os repeated treatment with P. vulgaris extract (500 mg/kg) was compared with metformin (100 mg/kg) and atorvastatin (10 mg/kg) in a model of metabolic syndrome evoked ...
Mansour Sobeh; Mona F. Mahmoud; Samar Rezq; Amira E. Alsemeh; Omar M. Sabry; Islam Mostafa; Mohamed A. O. Abdelfattah; Khadija Ait El-Allem; Assem M. El-Shazly; Aziz Yasri; Michael Wink
... Patients with neuropathic pain experience chronic painful tingling, burning, and prickling sensations accompanied with hyperalgesia and/or allodynia. In this study, 38 secondary metabolites of a methanol extract from Salix tetrasperma flowers were identified by liquid chromatography-mass spectrometry (HPLC-MS/MS). The extract showed substantial anti-inflammatory, central and peripheral anti-nocice ...
abiotic stress; abscisic acid; dephosphorylation; electrophysiology; enzyme inhibition; gene expression; genes; ion channels; pathogens; phosphoprotein phosphatase; protein kinases; receptors; seed dormancy; seed germination; seedlings; signal transduction; stomatal movement; stress response
Abstract:
... The plant hormone abscisic acid (ABA) is involved in regulating a number of major processes such as seed dormancy, seedling development, and biotic and abiotic stress responses. The function and effect of ABA on pathogens are still unclear, but the roles of ABA in seed germination and abiotic stress responses have been well characterized. Abiotic stresses elevate ABA levels and activate ABA signal ...
... In this study, via a bioactivity-guided fractionation of MeOH extracts of the fruits of Piper nigrum, alkamide (5) and five previously-identified alkamides were isolated. Their structures were elucidated via spectroscopic analysis (1H, 13C NMR and ESI-MS), as follows: retrofractamide A (1), pipercide (2), piperchabamide D (3), pellitorin (4), dehydroretrofractamide C (5) and dehydropipernonaline ( ...
... Amaranth seed is a valuable source of dietary protein with very high nutritional quality, and recently its potential as a nutraceutical has been proposed. The aim of this work was to provide experimental evidence for the presence of anti-hypertensive peptides in globulin 11S, one of the major constituents of the seed, by means of an in-silico based peptide library screening method. A three-dimensi ...
... In this work, the angiotensin-converting enzyme (ACE)-inhibitory and radical-scavenging activities of the β-lactoglobulin (β-Lg)-derived peptides WY f(19-20), WYS f(19-21), WYSL f(19-22), WYSLA f(19-23), WYSLAM f(19-24), and WYSLAMA f(19-25) have been determined. The ACE-inhibitory activity (IC50) varied from 38.3 to 90.4 micromolar, with the exception of WYS (>500 micromolar). All β-Lg-derived pe ...
... Some of the most potent ACE-inhibitory peptides described in food have a proline at the end of their sequence, a characteristic that can cause problems in the synthesis procedures. In this work, we studied two different preparations of peptide Asp-Lys-Ile-His-Pro (DKIHP), which were obtained by two different synthetic procedures (Boc and Fmoc). The peptide synthesized by the Boc method yielded a u ...
... In this study, the in vitro angiotensin-converting enzyme (ACE)-inhibitory (ACE-I) activity of peptide fractions from different yoghurt batches was assessed. Inhibition of ACE activity resulted in an overall antihypertensive effect. Yoghurts were prepared either using a sole yoghurt culture including Lactobacillus delbrueckii ssp. bulgaricus Lb1466 and Streptococcus thermophilus St1342, or L. acid ...
... Fish processing wastes can be used for preparing bioactive peptides with various functionalities. Our objective was to evaluate the in vitro angiotensin converting enzyme (ACE) inhibitory activity of tilapia protein hydrolysates and its corresponding fractionates. Tilapia protein was alkali-solubilised at pH 11.0 and recovered at pH 5.5 to obtain a stable substrate. This substrate was hydrolysed u ...
... No new therapy for acute myeloid leukemia (AML) has been approved for more than 30 years. To effectively treat AML, new molecular targets and therapeutic approaches must be identified. In silico analysis of several databases of AML patients demonstrated that the expression of alkaline ceramidase 3 (ACER3) significantly inversely correlates with the overall survival of AML patients. To determine wh ...
... Endemic Alkanna cappadocica was used to isolate novel antitumor molecules from Turkish landscapes in our previous studies. In this study, deoxyalkannin (ALCAP1), β,β-dimethylacrylalkannin (ALCAP2), acetylalkannin (ALCAP3), and alkannin (ALCAP4) as well as the novel isolated compounds 5-methoxydeoxyalkannin (ALCAP5), 8-methoxydeoxyalkannin (ALCAP6), 5-methoxyacetylalkannin (ALCAP7), 5-methoxy-β,β-d ...
... Marbling, or i.m. fat, is an important factor determining beef quality. Both adipogenesis and hypertrophy of existing adipocytes contribute to enhanced marbling. We hypothesized that the fetal stage is important for the formation of i.m. adipocytes and that AMP-activated protein kinase (AMPK) has a key role in adipogenesis during this stage. The objective of this study was to assess the role of AM ...
... The adverse outcome pathway (AOP) framework can be used to help support the development of alternative testing strategies aimed at predicting adverse outcomes caused by triggering specific toxicity pathways. In this paper, we present a case-study demonstrating the selection of alternative in chemico assays targeting the molecular initiating events of established AOPs, and evaluate use of the resul ...
adipocytes; adipogenesis; adiponectin; autophagy; body fat distribution; brown adipose tissue; cAMP-dependent protein kinase; enzyme inhibition; heat production; insulin; insulin resistance; lipolysis; noninsulin-dependent diabetes mellitus; obesity; peroxisome proliferator-activated receptor gamma; proteasome inhibitors; protein content
Abstract:
... Adipocyte dysfunction is closely associated with the development of obesity, insulin resistance, and type 2 diabetes. In addition to having a positive effect on adiponectin pathway and insulin signaling through direct and/or indirect mechanisms, adapter protein APPL1 has also been reported to regulate body weight, brown fat tissues thermogenesis, and body fat distribution in diabetic individuals. ...
... Atg4 is essential for autophagosome formation and Atg8 recycle with the function of processing the precursor and the lipidated Atg8-family proteins. Abnormal autophagic activity is involved in a variety of pathophysiological diseases and ATG4B is of interest as a potential therapeutic target due to its key roles in autophagy process. So ATG4B inhibitors are highly needed. FMK-9a is the most potent ...
... Incubation of Escherichia coli γ-glutamylcysteine synthetase with L-glutamic acid γ-monohydroxamate and ATP caused slow but irreversible inhibition of the enzyme, and more than 90% activity was lost in three days. The enzyme was not inactivated when ATP was absent or L-aspartic acid β-monohydroxamate was substituted for L-glutamic acid γ-monohydroxamate, suggesting that the inactivation process re ...
DNA damage; DNA replication; cell cycle; cell nucleolus; chromatin; cytoplasm; enzyme activity; enzyme inhibition; eukaryotic cells; mortality; phosphorylation
Abstract:
... In eukaryotes, in response to replication stress, DNA damage response kinase, ATR is activated, whose signalling abrogation leads to cell lethality due to aberrant fork remodelling and excessive origin firing. Here we report that inhibition of ATR kinase activity specifically during replication stress recovery results in persistent ATR signalling, evidenced by the presence of ATR-dependent phospho ...
Abeliophyllum distichum; acetates; actin; animal models; animal ovaries; antioxidants; bone resorption; diarrhea; dose response; enzyme inhibition; female genital diseases; femur; genes; indigenous species; leaves; mitogen-activated protein kinase; morphometry; oral administration; osteoporosis; ovariectomy; postmenopause; protective effect; rats; traditional medicine; women; South Korea
Abstract:
... Abeliophyllum distichum Nakai (AD), called Miseon, is one of Korea's monotypic endemic species. As a folk remedy, the AD has been used to treat inflammatory disease, stomachaches, diarrhea, and gynecologic disease in Korea. Some researchers have reported that the AD has anti-cancer, anti-inflammatory, and anti-oxidant effects. But the protective effect of AD leaf for osteoporosis has not been repo ...
... Abrus agglutinin (AGG), a heterotetrameric type II ribosome inactivating protein isolated from the seeds of Abrus precatorius shows potent antitumor activity in different cancer models. We examined the role of antioxidant system in modulation of the anticancer activity of AGG in in vitro and in hamster model of oral cancer. AGG promotes apoptosis through accumulation of ROS in CAL33 cells. Interes ...
... The role of hydrogen peroxide (H2O2) in abscisic acid (ABA)-induced anthocyanin accumulation in detached and intact leaves of rice seedlings was investigated. Treatment with ABA resulted in an accumulation of anthocyanins in detached rice leaves. Dimethylthiourea, a chemical trap for H2O2, was observed to be effective in inhibiting ABA-induced accumulation of anthocyanins. Inhibitors of NADPH oxid ...
... Caspase-3 displays a pivotal role as an executioner of apoptosis, hydrolyzing several proteins including the nuclear enzyme poly(ADP-ribose)polymerase (PARP). Ac-Asp-Glu-Val-Asp-H (Kᵢ° = 2.3 × 10⁻¹⁰M at pH 7.5 and 25.0 °C), designed on the basis of the cleavage site of PARP, has been reported as a highly specific human caspase-3 inhibitor. Here, di- and tri-peptidyl aldehydes 11–13 and 27–29 have ...
... Plant essential oils and its chemical compositions are commonly applied in medicinal and other industries due to their broad advanced pharmacological activities. In the present study, we systematically evaluated the acaricidal activities of twelve compounds of essential oils against Psoroptes cuniculi in vitro and in vivo. In addition, to support the clinic uses, their toxicities against immortali ...
... In spring 2005, a downy brome population with possible resistance to fluazifop-P, an acetyl-CoA carboxylase (ACCase) inhibitor (group 1) herbicide was found in a commercial creeping red fescue seed production field, near La Grande, OR, where fluazifop-P had been used to control downy brome repeatedly over 7 yr. Greenhouse experiments were conducted to confirm resistance to a number of group 1 herb ...
... Lifestyle interventions and physical activity remain the cornerstone of obesity management, as pharmacological therapies (orlistat) are associated with gastrointestinal (GI) side effects. Combining orlistat with fibers can reduce side effects, improving compliance. Therefore, a fiber that inhibits lipase without side effects could help treat obesity.The aims of the present work were to assess whet ...
... Betalain pigments are water soluble natural pigments that contain nitrogen. Betacyanin have been reported to possess several biological properties In the present work, the pigment from the rind of Hylocereus undatus was analyzed for its stability upon elevated temperature, pH, time, light period, and metal ions. Further, the effect of betacyanin pigment on xanthine oxidase enzyme inhibition was st ...
... Biosynthesis of hydroxybenzoates even at enzymatic level is poorly understood. In this report, effect of feeding of putative biosynthetic precursors and pathway-specific enzyme inhibitors of early phenylpropanoid pathway on p-hydroxybenzoic acid accumulation in chitosan-elicited hairy roots of Daucus carota was studied. Three selective metabolic inhibitors of plant phenylpropanoid pathway, namely, ...
... A mutant strain of Fusarium sporotrichioides NRRL 3299 produced by disruption of Tri11, a gene encoding a cytochrome P-450 monooxygenase, was shown to be altered in its ability to biosynthesize T-2 toxin. This mutant strain produced four trichothecenes that were not observed in cultures of the parent strain. The compounds were identified as isotrichodermin, 8-hydroxyisotrichodermin, 8-hvdroxyisotr ...
... Casein was hydrolyzed by alcalase to a degree of hydrolysis of 10.9% to obtain a hydrolysate having ACE-inhibition in vitro with an IC ₅₀ value of 52.6 μ g/mL. The prepared hydrolysate was modified by alcalase-catalyzed plastein reaction with extrinsic proline added at 0.4 mol/mol free amino groups (on the basis of the hydrolysate), and fractionated by ethanol- or methanol-water solvents in propor ...
... To elucidate the mechanism underlying the action of dietary vinegar on antithrombotic activity, acetic acid, the main acidic component of dietary vinegar, was used to determine antiplatelet and fibrinolytic activity. The results revealed that acetic acid significantly inhibits adenosine diphosphate (ADP)-, collagen-, thrombin-, and arachidonic acid (AA)-induced platelet aggregation. Acetic acid (2 ...
... ALS inhibitor-resistant biotypes are the fastest growing class of herbicide-resistant (HR) weeds. A Canadian ALS inhibitor-resistant biotype of Russian thistle was first reported in 1989. The molecular basis for ALS-inhibitor resistance is unknown for Canadian populations of this polyploid weed species, and was determined in this study for one Alberta and two Saskatchewan HR Russian thistle popula ...
... To date, almost all the established photoelectrochemical (PEC) enzymatic biosensors require the surface-confinement procedure to immobilize enzyme as biorecogniton element for probing various analytes of interest. This Letter develops a novel example without such necessity. Specifically, we first prepared a BiOI nanoflakes (NFs)/TiO₂ nanoparticles (NPs) p–n heterojunction as the photoelectrode, on ...
... Huernia species are typical famine‐food plants consumed in southern Ethiopia. H. hystrix is a heavily exploited ethnomedicinal succulent plant traded in traditional medicine systems especially on South Africa's eastern seaboard. This study investigated the acetylcholinesterase (AChE) inhibition, antioxidant, antiinflammatory and antimicrobial properties of extracts obtained from the stems and root ...
... Malathion, under in vitro laboratory conditions, is readily degraded by an Arthrobacter species to four metabolites—malathion half-ester, malathion dicarboxylic acid, potassium dimethyl phosphorothioate, and potassium dimethyl phosphorodithioate. However, it is not clear whether or not this degradation represents a simultaneous detoxication of the malathion molecule. With this in mind, the relativ ...
water pollution; water quality; chlorpyrifos; methomyl; Gammarus; aquatic arthropods; acetylcholinesterase; enzyme inhibition; feeding behavior; locomotion; enzyme activity; toxicity testing
Abstract:
... Relations between whole-body acetylcholinesterase (AChE) inhibition and changes in feeding and locomotor behaviours were investigated in adult male Gammarus fossarum during short-term exposure (96h) to the organophosphorous pesticide chlorpyrifos (CPE) and the carbamate pesticide methomyl (MT). AChE activity was measured after 24, 48 and 96h of exposure. The feeding rate was assessed after 48 and ...
... Crude oil and its derivatives are primary energy resources for humans, and processes involving these materials could affect aquatic environments. Acetyl cholinesterase (AChE) activity is a suitable biomarker for exposure to organophosphate pesticides. Under controlled conditions, fish exposed to polycyclic aromatic hydrocarbons (PAHs), such as benzo[a]pyrene, pyrene and anthracene, showed inhibiti ...
Artemia; Euphorbiaceae; Fourier transform infrared spectroscopy; X-radiation; acetylcholinesterase; active sites; chemical composition; chemical constituents of plants; cytotoxicity; density functional theory; enzyme inhibition; leaves; molecular models; mortality; nuclear magnetic resonance spectroscopy; spectral analysis
Abstract:
... Phytochemical investigations of the ethanolic extract of leaves of Clutia lanceolata (Family: Euphorbiaceae) resulted in the isolation of four compounds viz. 3,4-dihydroxy-2-methylbenzoic acid (1), 2,2′-dihydroxy-1,1′-binaphthyl (2), 1,3,8-trihydroxy-6-methylanthracene-9,10-dione (3) and 5-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,4,6-trien-3-one (4). Although all the isolated compounds we ...
... The use of chemogenomics techniques applied to a marine natural products database has pointed out halogenated sesquiterpenes present in red alga Laurencia dendroidea as potential acetylcholinesterase inhibitors. Therefore, in this work five metabolites were studied using molecular docking and enzymatic inhibition assays. According to the results the most promising metabolite in relation to acetylc ...
Meloidogyne javanica; Heterodera avenae; Tylenchulus semipenetrans; plant parasitic nematodes; acetylcholinesterase; enzyme activity; organophosphorus compounds; carbamates; kinetics; in vitro studies; protein content; enzyme inhibition; Saudi Arabia
Abstract:
... The in vitro inhibition potency of some organophosphates (OPs) and carbamates (CAs) which are widely used to control plant-parasitic nematodes on acetylcholinesterase (AChE) of Meloidogyne javanica, Heterodera avenae and Tylenchulus semipenetrans, the major pathogens responsible for the damage of a wide range of crops in Al-Qassim region, Saudi Arabia was examined. AChE of H. avenae activity was 1 ...
... Anthocleista vogelii (Planch) is used in folk medicine in conditions related to inflammation and oxidative stress. This suggests that some of its constituents could possess ability to reduce oxidative damage to cells and ameliorate inflammatory conditions which are two prominent features in the brain of a person suffering from Alzheimer’s disease.The leaf extracts were investigated for their bioac ...
... An endophytic fungus, Chaetomium sp. YMF432, was isolated from Huperzia serrata (Thunb. ex Murray) Trev. and subjected to phytochemical investigation based on its special environment. From the extracts of fermentation solid of strain YMF 432, eight compounds including 1-O-methylemodin (1), 5-methoxy-2-methyl-3-tricosyl-1,4-benzoquinone (2), 4,8-dihydroxy-1-tetralone (3), (3β,5α,6α, 22E)-3-hydroxy- ...
... In this study, demethylcurcumin (DC), a minor constituent in curcuminoids, showed better anti-acetylcholinesterase (anti-AChE) activities, anti-amyloid β peptide aggregation, neuroprotective activities in 6-hydroxydopamine-treated SH-SY5Y cell models, and anti-nitric oxide production in lipopolysaccharide-treated RAW 264.7 macrophages than those of curcumin. Based on molecular docking analyses wit ...
Alzheimer disease; Scyphozoa; acetylcholinesterase; alkaloids; amino acids; aquatic organisms; enzyme inhibition; fractionation; gas chromatography-mass spectrometry; gel chromatography; hydrophobicity; inhibitory concentration 50; nuclear magnetic resonance spectroscopy; reference standards; spectral analysis; venoms
Abstract:
... Natural compounds from marine organisms have been rarely studied for their acetylcholinesterase inhibitory activities. The aim of this study was to isolate novel compounds with antiAChE activity from the venom of upside-down jellyfish Cassiopea andromeda Forskål, 1775. The compounds of the fractionated venom on gel filtration chromatography were identified by analyzing gas chromatography–mass spec ...
... Acetylcholinesterase (AChE) inhibition is one of insect toxicity mechanisms found in many plants. Stemona collinsiae Craib, a traditional insecticidal plant, has been of interest for its AChE inhibitory activity.Powdered roots of S. collinsiae were successively extracted with hexane, dichloromethane, and methanol. The contents of major active insecticidal components, didehydrostemofoline and stemo ...
acetylcholinesterase; enzyme inhibition; Rhodiola rosea; rhizomes; plant extracts; hydroquinone; chemical constituents of plants; Alzheimer disease
Abstract:
... An activity-directed fractionation and purification process was used to identify the acetylcholinesterase inhibitory-active components of Rhodiola rosea L. (RR). Dried rhizome of RR was extracted with boiled ethanol. After removal of tannins, the extract was separated into chloroform, ethyl acetate, n-butanol and water fractions. Among these, chloroform and n-butanol fractions showed stronger acti ...
... Two strains of Cydia pomonella (L.) (Lepidoptera: Tortricidae) were selected in the lab by exposure to increasing concentrations of diflubenzuron (Rdfb strain) or azinphos-methyl (Raz strain). Insecticide bioassays showed that the adults of the Rdfb strain exhibited a 2.6-fold and a 7.7-fold resistance ratio to azinphos-methyl and carbaryl, respectively compared to a susceptible strain (S) whereas ...
... BACKGROUND: Millions of people and domestic animals around the world are affected by leishmaniasis, a disease caused by various species of flagellated protozoans in the genus Leishmania that are transmitted by several sand fly species. Insecticides are widely used for sand fly population control to try to reduce or interrupt Leishmania transmission. Zoonotic cutaneous leishmaniasis caused by L. ma ...
Adriana M. Dos Santos; Ariele C. Moreira; Bianca Rebelo Lopes; Mariana F. Fracola; Fernando G. de Almeida; Odair C. Bueno; Quezia B. Cass; Dulce Helena F. Souza
Atta sexdens; acetates; acetylcholine; acetylcholinesterase; ammonium; batch systems; choline; colorimetry; death; enzyme inhibition; hydrolysis; ion exchange chromatography; leaf-cutting ants; neurotransmitters; pH; phylogeny; sulfates; tandem mass spectrometry
Abstract:
... Acetylcholinesterase (AChE) is responsible for catalyzing the hydrolysis of the neurotransmitter acetylcholine (ACh) leading to acetate and choline (Ch) release. The inhibition of AChE produces a generalized synaptic collapse that can lead to insect death. Herein we report for the first time the isolation of two AChEs from Atta sexdens which were purified by sulphate ammonium precipitation followe ...
CD29 antigen; adenocarcinoma; adenoma; apoptosis; colorectal neoplasms; drug therapy; enzyme inhibition; human cell lines; humans; mucosa; neoplasm cells; patients; protein content; protein-glutamine gamma-glutamyltransferase; resistance mechanisms; transcription factor NF-kappa B
Abstract:
... Acid ceramidase (ASAH1) has been implicated in the progression and chemoresistance in different cancers. Its role in colon cancer biology and response to standard chemotherapy has been poorly addressed so far. Here, we have investigated ASAH1 expression at the protein level in human colon cancer cell lines and tissues from colon cancer patients, and have examined in vitro the possible link between ...
... Numerous studies have reported that the glycaemic response to starch-rich meals can be reduced by 20–50% with acidic drinks or foods. A number of candidate explanations have been put forward, but this phenomenon still remains vaguely understood. This study intends to demonstrate the remarkable effect of acid inhibition of salivary α-amylase during oro-gastric hydrolysis of starch, shedding light o ...
Sabine Kahlau; Florian Schröder; Jörg Freigang; Bernd Laber; Gudrun Lange; Daniel Passon; Sabrina Kleeßen; Marc Lohse; Arno Schulz; Pascal von Koskull‐Döring; Sebastian Klie; Sascha Gille
... BACKGROUND: Aclonifen is a unique diphenyl ether herbicide. Despite its structural similarities to known inhibitors of the protoporphyrinogen oxidase (e.g. acifluorfen, bifenox or oxadiazon), which result in leaf necrosis, aclonifen causes a different phenotype that is described as bleaching. This also is reflected by the Herbicide Resistance Action Committee (HRAC) classification that categorizes ...
... This paper presents the effect of acrolein on three dehydrogenases and proposes a fast spectrometric method for acrolein analysis. We have found that alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (AlDH) are inhibited by low acrolein concentrations (0.2 mM) while inhibition of glutamate dehydrogenase (GDH) is not observed even at higher acrolein concentrations (1 mM). Acrolein is a suicide ...
... The mechanism of action of pyroxasulfone was studied by examination of the inhibitory effects of this herbicide on the biosynthesis of very-long-chain fatty acids (VLCFAs) both in vivo and in vitro. Pyroxasulfone treatment drastically reduced the biosynthesis of VLCFAs and caused a buildup of fatty acid precursors in cultured rice cells. Pyroxasulfone specifically inhibited the elongation steps fr ...