Anti-lipid peroxidation, α-glucosidase and α-amylase inhibitory effects of the extract of capitula of Coreopsis tinctoria Nutt. and protection effects on high-fat/high-sugar and streptozotocin-induced type 2 diabetes in mice.
This study evaluated the anti-lipid peroxidation, α-glucosidase and α-amylase inhibitory effects of CTC extracts, and analyze its chemical composition by HPLC. Moreover, the antioxidant activity and protection effects of CTC extracts were investigated on high-fat/high-sugar and streptozotocin-induced T2DM mice. In vitro study, the ethyl acetate extract (EAE) and n-butanol extract (BE) of CTC exhibited anti-lipid peroxidation (IC 50 : BHA> BE or EAE> ascorbic acid, p EAE, p
Source: Chemistry and Biodiversity - October 14, 2019 Category: Biochemistry Authors: Zhang Y, Luo L, Li Z, Li H, Yao X, Luo R Tags: Chem Biodivers Source Type: research

Synthesis and evaluation of aminothiazole derivatives as hedgehog pathway inhibitors.
Abstract A series of aminothiazole derivatives bearing the benzimidazole moiety were synthesized, and evaluated in Gli luciferase reporter assays. Lead optimization led to the discovery of potent hedgehog pathway antagonist 18, with IC 50 values in nanomolar range. The molecular basis ascribed to hindering sonic hedgehog-driven Smoothened (Smo) localization within the primary cilium (PC). Moreover, compound 18 inhibited Gli1 mRNA expression in mutant Smo cell line and displayed moderate cytotoxicity against DAOY cancer cell. PMID: 31609078 [PubMed - as supplied by publisher] (Source: Chemistry and Biodiversity)
Source: Chemistry and Biodiversity - October 14, 2019 Category: Biochemistry Authors: Sun C, Zhang Y, Lin L, Liu S, Wang R, Zang W, Meng W, Chen X Tags: Chem Biodivers Source Type: research

A new pimarane diterpenoid from the Botryotinia f.eliana fungus isolated from deep-sea water.
Abstract A new pimarane diterpenoid, named botryopimarene A ( 1 ), was discovered from a fungus Botryotinia f.eliana MCCC 3A00494 isolated from the deep-sea water, together with ten known compounds. The planar structure of 1 was established based on the extensive spectroscopic analyses. The absolute configurations of tricyclic system in 1 were resolved by the theoretical ECD calculation, while the 15,16-diol moiety in the side chain was resolved by the Mo 2 (OAc) 4 -induced ECD spectrum. Compound 1 , featuring a Δ 9,11 double bond, was rarely discovered in pimarane family. Compounds 1-11 were tested their cy...
Source: Chemistry and Biodiversity - October 9, 2019 Category: Biochemistry Authors: Niu S, Peng G, Xia JM, Xie CL, Li Z, Yang XW Tags: Chem Biodivers Source Type: research

CF3-pyridinyl substitution on anti-malarial therapeutics: Probing differential ligand binding and dynamical inhibitory effects of a novel triazolopyrimidine-based inhibitor on Plasmodium falciparum Dihydroorotate dehydrogenase.
Abstract The quest for reliable Dihydroorotate dehydrogenase (DHODH) inhibitors has engendered the discovery of potential therapeutic compounds at different stages of clinical trials. Although promising, high attrition rates and unfavorable bioactivities have limited their drug developmental progress. A recent structural modification of DSM265, a triazolopyrimidine-based inhibitor, yielded DSM421, derived by the substitution of the SF5-aniline group on DSM265 with a CF3-pyridinyl moiety. Consequently, DSM421 exhibited improved pharmacological and pharmacokinetics attributes relative to DSM265. The improved bioacti...
Source: Chemistry and Biodiversity - October 7, 2019 Category: Biochemistry Authors: Agoni C, Salifu EY, Munsamy G, Olotu FA, Soliman M Tags: Chem Biodivers Source Type: research

Natural monoterpenes: much more than only a scent.
Abstract Terpenes are a widespread group of secondary metabolites that can be found in various family plants such as the Lamiaceae. In view of their numerous valuable biological activities, the industrial production of concrete terpenes and essential oils rich in the substances is intensively studied. Monoterpenes constitute a significant part of the whole group of the aforementioned secondary metabolites. This is due to their numerous biological activities and their ability to permeate the skin. Despite the fact that these substances have gain popularity, they are not comprehensive characterized. The presented re...
Source: Chemistry and Biodiversity - October 6, 2019 Category: Biochemistry Authors: Wojtunik-Kulesza K, Kasprzak K, Oniszczuk T, Oniszczuk A Tags: Chem Biodivers Source Type: research

Antioxidant and Cytotoxic Activities of Distillates Purified by Means of Molecular Distillation from Ginger Extract Obtained with Supercritical CO2 Fluid.
Abstract The ginger extract obtained with supercritical CO 2 fluid was purified by molecular distillation (MD), and the chemical compositions, antioxidant and cytotoxic activities of ginger extract and its distillates were investigated. Analysis revealed that the ginger extract was rich in terpene hydrocarbons, along with oxygenated terpenes and other non-volatile compounds. The MD distillates were prepared in a series of stages and the active compounds like terpenes and gingerols could be separated by MD. The major compounds of the distillates purified by MD at 40 ℃, 80 Pa and 60 ℃, 80 Pa were terpene hydroca...
Source: Chemistry and Biodiversity - October 1, 2019 Category: Biochemistry Authors: Wang L, Zhao W, Lu Y, Wang C Tags: Chem Biodivers Source Type: research

Caffeic acid alkyl amide derivatives ameliorate oxidative stress and modulate ERK1/2 and Akt signaling pathways in a rat model of diabetic retinopathy.
Abstract The purpose of this study was to examine the neuroprotective effects of caffeic acid hexyl (CAF6) and dodecyl (CAF12) amide derivatives on the early stage of retinopathy in streptozotocin-induced diabetic rats. Animals were divided in 5 groups (n = 8/group); One group consisted of control non-diabetic rats, while the other 4 were diabetic animals either non-treated or treated with CAF6, CAF12 or resveratrol intravitreally for 4 weeks. Retinal superoxide dismutase (SOD) activity and 8- iso prostaglandin F 2α (iPF 2α ) levels were evaluated by an ELISA assay. Phosphorylation of ERK1/2 and AKT we...
Source: Chemistry and Biodiversity - September 30, 2019 Category: Biochemistry Authors: Fathalipour M, Eghtedari M, Borges F, Silva T, Moosavi F, Firuzi O, Mirkhani H Tags: Chem Biodivers Source Type: research

A Theoretical Study of the Molecular Coupled Structures of Aristolochic Acids and Humic Acid, Potential Environmental Contaminants.
Abstract An understanding of the fate of organic compounds originating from plants in soil is crucial for determining their persistence and concentrations in the environment. Aristolochic acids are believed to be the causal agents that induce Balkan endemic nephropathy by food contamination through soil adsorption of humic acids, major components of soil. Aristolochic acids are active chemicals in Aristolochia plant species found in endemic villages. In this article, molecular structure interactions between 18 structures of aristolochic acids with an inserted humic acid structure were studied. These structures wer...
Source: Chemistry and Biodiversity - September 30, 2019 Category: Biochemistry Authors: Petrescu AM, Lukinich-Gruia AT, Paunescu V, Ilia G Tags: Chem Biodivers Source Type: research

Protective Effect of the Traditional Chinese Patent Medicine Qing-Xuan Granule against Bleomycin-Induced Pulmonary Fibrosis in mice.
This study was designed to investigate the effects of QX and possible   molecular mechanisms for bleomycin-induced PF. The work used western blotting and Q-PCR to explore the vitro and vivo mechanisms of QX treatment, while using HPLC-TOF/MS to explore the composition of QX. QX was given daily orally for two weeks after bleomycin intratracheal instillation. The protective effects of QX on lung function, inflammation, growth factors, hydroxyproline content and deposition of extracellular matrix were investigated. QX decreased expression of Col I and α-SMA in lung tissues by down-regulating TGF-β1-Smad2/3 sig...
Source: Chemistry and Biodiversity - September 26, 2019 Category: Biochemistry Authors: Liu B, Lv W, Ge H, Tang H, Li R, Zhang C Tags: Chem Biodivers Source Type: research

Fibrous Aggregates of Short Peptides Containing Two Distinct Aromatic Amino Acid Residues.
Abstract TThe aim of the study was the assessment of the ability of short peptides to form ordered fibrous aggregates under physiological conditions. Dipeptides were derived from different aromatic amino acids (heteroaromatic peptides) and tripeptides were obtained from two distinct aromatic amino acids with cysteine or methionine residue in the C-terminal, N-terminal, or central position. The ability of the peptides to form fibrous aggregates under physiological conditions was evaluated using three independent methods: the Congo Red assay, the Thioflavine T assay, and microscopic examinations using normal and pol...
Source: Chemistry and Biodiversity - September 26, 2019 Category: Biochemistry Authors: Kolesinska B, Lipinski W, Wasko J, Walczak M, Fraczyk J, Kamiński ZJJ, Galecki K, Draczynski Z, Krucinska I, Kaminska M Tags: Chem Biodivers Source Type: research

Synthesis of Disulfide-Bridged N-Phenyl-N'-(Alkyl/Aryl/Heteroaryl)Urea Derivatives and Evaluation of Their Antimicrobial Activities.
S, Sriram D Abstract The recognition of new antimicrobial agents is extremely needed to overcome multidrug-resistant bacterial and tuberculosis infections. In the present study, eight novel substituted urea derivatives containing disulfide bond ( 10a-h ) were designed, synthesized and screened for their in vitro antimicrobial activities on standard strains of Gram-positive and Gram-negative bacteria as well as on Mycobacterium tuberculosis . According to the obtained results, antibacterial effects of the compounds were found to be considerably better than their antimycobacterial activities along with their weak cy...
Source: Chemistry and Biodiversity - September 26, 2019 Category: Biochemistry Authors: Doğan ŞD, Buran S, Gündüz MG, Özkul C, Krishna VS, Sriram D Tags: Chem Biodivers Source Type: research

Chemical composition and antimicrobial activity of Achillea tenuifolia Lam. essential oil at different phenological stages from Khoy.
In this report, we extracted the essential oil from the aerial parts of the A. tenuifolia (collected from Khoy), at various developmental stages (i.e. vegetative, flowering and fruiting), characterize them and study their antibacterial activities. Of 46, 51 and 38 components found in the vegetative, flowering, and fruiting stages, respectively, 35 were present in all three stages, including oxygenated terpenes such as carvacrol (30.85-34.11), germacrene-C (17.87-16.21), spathulenol (8.96-7.26), β-sesquiphellandrene 4.25-4.11), t-muurolol (3.25-2.27) and α-cadinol (3.29-2.01). We witnessed that the composition of...
Source: Chemistry and Biodiversity - September 24, 2019 Category: Biochemistry Authors: Aminkhani A, Sharifi R, Dorosti R Tags: Chem Biodivers Source Type: research

Volatile and Sensory Profiles of Algerian Extra-virgin Olive Oil from Souidi and Zeletni Cultivars.
In this study, the volatile and sensory profiles of monovarietal extra-virgin olive oil (EVOO) from two less widespread Algerian autochthonous cultivars (Souidi and Zeletni) were obtained using headspace solid-phase microextraction coupled to gas chromatography-mass spectrometry and a panel test, respectively. A total of 14 and 10 volatile compounds belonging to different chemical classes were identified and quantified in the Souidi and Zeletni EVOOs, respectively. Zeletni EVOO contains 2.07 times more (E)-2-hexenal than Souidi EVOO. In addition, the amounts of C6 compounds from LA and LnA, as well as the total amount of t...
Source: Chemistry and Biodiversity - September 23, 2019 Category: Biochemistry Authors: Cherfaoui M, Cecchi T, Keciri S, Boudriche L Tags: Chem Biodivers Source Type: research

Antibiotic-potentiating activity of the Phanostenine isolated from Cissampelos sympodialis Eichl.
Abstract Cissampelos sympodialis is well studied and investigated for its antiasthmatic properties, but there are no data in the literature describing antibacterial properties of alkaloids isolated from this botanical species. This work reports the isolation and characterization phanostenine obtained from roots of C. sympodialis and describes for the first time its antimicrobial and antibiotic modulatory properties. Phanostenine was first isolated from Cissampelos sympodialis and its antibacterial activities were determined. Chemical structures of the alkaloid isolate were determined using spectroscopic and chemic...
Source: Chemistry and Biodiversity - September 23, 2019 Category: Biochemistry Authors: Martins da Costa JG, Cunha WEM, Camilo CJ, Nonato CFA, Mendes JWS, de Carvalho NKG, Coutinho HDM, Menezes IRA, de Lemos TLG, Braz-Filho R, Rodrigues FFG, Matias EFF, Zengin G Tags: Chem Biodivers Source Type: research

In vitro Trypanocidal and Antibacterial Activities of Essential Oils from Four Species of the Family Annonaceae.
The objective of this study was to evaluate the chemical composition, and the trypanocidal and antibacterial activities of the essential oils from four species of Annonaceae: Bocageopsis multiflora R.E.Fr., Duguetia quitarensis Benth., Fusaea longifolia Saff., and Guatteria punctata (Aubl.) RAHoward. The chemical composition of the essential oils from the aerial parts yielded 23, 20, 21 and 23 constituents, respectively, which were identified by GC-MS. The trypanocidal activity was evaluated against the amastigote and trypomastigote forms of T. cruzi. The antibacterial activity was evaluated by the microdilution method aga...
Source: Chemistry and Biodiversity - September 22, 2019 Category: Biochemistry Authors: Bay M, de Oliveira JVS, Sales Junior PA, Murta SMF, Dos Santos AR, Bastos IDS, Orlandi PP, de Sousa Junior PT Tags: Chem Biodivers Source Type: research

Synthesis and relaxometric characterization of new Poly[N,N-bis(3-AminoPropyl)Glycine] (PAPGly) dendrons Gd-based contrast agents and their in-vivo study by using the Dynamic Contrast-Enhanced MRI technique at Low field (1 T).
Abstract The synthesis of poly[N,N-bis(3-aminopropyl)glycine] (PAPGly) dendrons Gd-based contrast agents (GdCAs) via an orthogonal protection of the different functional groups and an activation/coupling strategy wherein a specific number of synthetic steps adds a generation to the existing dendron have been described. The aim of this protocol is to build up two different generations of dendrons (G-0 or dendron's core, and G-1) with peripheral NH2-groups to conjugate a 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid (DO3A) derivative and after to chelate with Gd3+ paramagnetic ions. These complexes, which have...
Source: Chemistry and Biodiversity - September 22, 2019 Category: Biochemistry Authors: Laurent S, Granato L, Longo D, Vander Elst L, Henoumont C, Aime S, Muller RN Tags: Chem Biodivers Source Type: research

Comparative Analyses on the Bioactive Compounds and in vitro Antioxidant Capacity of Tea Infusions Prepared from the Selected Medicinal Fruits.
This study was conducted to analyze the bioactive compounds and in vitro , antioxidant capacity of tea infusions prepared from whole and ground medicinal fruits, including gardenia, jujube, magnolia, quince, and wolfberries. The dried medicinal fruit samples were ground, and then passed through a 60-mesh sieve (pore size, 250 µm). Hot water (80 ℃) infusions of whole and ground fruits were examined. In average of both whole and ground tea infusions, the maximum bioactive compounds were found in gardenia (β-carotene, lycopene and vitamin C), magnolia (total chlorophyll and anthocyanin), quince (flavonoid), and w...
Source: Chemistry and Biodiversity - September 19, 2019 Category: Biochemistry Authors: Islam MZ, An HG, Lee YT Tags: Chem Biodivers Source Type: research

Design and Construction of Aroyl-Hydrazone Derivatives: Synthesis, Crystal Structure, Molecular Docking and Their Biological Activities.
Abstract Here, we report synthesis and characterization of four new aroyl-hydrazone derivatives; L 1 -L 4 and their structural as well as biological activities have been explored. In addition to docking with Bovine serum albumin (BSA) and duplex DNA, the experimental results demonstrate the effective binding of  L 1 -L 4   with BSA protein and calf thymus DNA (ct-DNA) which is in agreement with the docking results. Further biological activities of  L 1 -L 4 have been examined through molecular docking with different proteins which are involved in the propagation of viral or cance...
Source: Chemistry and Biodiversity - September 18, 2019 Category: Biochemistry Authors: Kumari P, Ansari SN, Kumar R, Saini AK, Mobin SM Tags: Chem Biodivers Source Type: research

Epigallocatechin Exerts Anti-Obesity Effect in Brown Adipose Tissue.
Abstract Catechins in green tea are well-known to be effective in reducing the risk of obesity. The purpose of this study was to elucidate the effects of catechins present in green tea on adipocyte differentiation and mature adipocyte metabolism. Treatment of 3T3-L1 mouse adipocyte during differentiation adipocytes with (-)-epigallocatechin (EGC) and gallic acid (GA) resulted in dose-dependent inhibition of adipogenesis. Specifically, EGC increased adiponectin and uncoupling protein 1 (UCP1) transcription in mature adipocytes. Transcription levels of adipose triglyceride lipase (ATGL) and hormone-sensitive lipase ...
Source: Chemistry and Biodiversity - September 18, 2019 Category: Biochemistry Authors: Kim HS, Jae-Hak M, Kim YM, Huh JY Tags: Chem Biodivers Source Type: research

Effect of seasonal and regional variations on Phenolic compounds of Deverra Scoparia (flowers/seeds) methanolic extract and the evaluation of its in-vitro antioxidant activity.
Abstract The widespread use of Deverra Scoparia in Algerian folk-medicine as a remedy, can be relatively attributed to their total phenolic compounds. The current study aimed to provide a scientific basis for optimal collection and usage of Deverra Scoparia plant. Hence, thirty-seven samples were gathered from nine sites in Algeria during two seasons 2016 and 2017, then exposed to a green extraction. Total phenolic (TPC), Flavonoid (FC) and Condensed Tannins (CTC) Content were estimated spectrophotometrically. Whereas, the antioxidant activity was measured using five different methods, DPPH˙, ABTS •+ , FRAP,...
Source: Chemistry and Biodiversity - September 17, 2019 Category: Biochemistry Authors: Benarfa A, Gourine N, Mahfoudi R, Harrat M, Yousfi M Tags: Chem Biodivers Source Type: research

Optimization the cellulase - ultrasounic synergistic extraction conditions of polysaccharides from Lenzites betulina.
In this study, cellulase - ultrasounic synergistic extraction method was applied to extract polysaccharides from L.betulina , and the response surface methodology was used to optimize the extraction conditions. The eight basic factors affecting extraction yield were evaluated by Plackett-Burman design (PBD). Then the four important factors significantly affecting the yield of polysaccharides from L.betulina , including enzymolysis temperature, enzymolysis time, ultrasound time and ultrasound temperature, were optimized by Box-Behnken design (BBD). Maximum extraction yield of L.betulina polysaccharides was 13.64 ± 0....
Source: Chemistry and Biodiversity - September 17, 2019 Category: Biochemistry Authors: Guo L, Tan DC, Hui FY, Gu F, Xiao KM, Wang JM, Hua Y Tags: Chem Biodivers Source Type: research

Design, synthesis, molecular docking, and cholinesterase inhibitory potential of phthalimide-dithiocarbamate hybrids as new agents for treatment of Alzheimer's disease.
Abstract A novel series of phthalimide-dithiocarbamate hybrids was synthesized and evaluated for inhibitory potentials against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The anti-cholinesterase results indicated that among the synthesized compounds, the compounds 7g and 7h showed the most potent anti-AChE and anti-BuChE activities, respectively. In silico docking study of the compounds 7g and 7h, respectively in the active site of AChE and BuChE revealed that these compounds bound to important residues. The compound 7g also showed remarkable neuroprotective activity comparable to the standard a...
Source: Chemistry and Biodiversity - September 15, 2019 Category: Biochemistry Authors: Mahdavi M, Asadi M, Ebrahimi M, Mohammadi-Khanaposhtani M, Azizian H, Sepehri S, Nadri H, Biglar M, Amanlou M, Larijani B, Mirzazadeh R, Edraki N Tags: Chem Biodivers Source Type: research

Isolation and antimacrofouling activity of indole and furoquinoline alkaloids from 'guatamb ú' trees (Aspidosperma australe and Balfourodendron riedelianum).
Isolation and antimacrofouling activity of indole and furoquinoline alkaloids from 'guatambú' trees (Aspidosperma australe and Balfourodendron riedelianum). Chem Biodivers. 2019 Sep 13;: Authors: Pérez M, Pis Diez CM, Valdez MB, García M, Paola A, Avigliano E, Palermo JA, Blustein G Abstract In this work the antifouling activity was studied of five alkaloids isolated from trees of the Atlantic rainforest. The tested alkaloids were: olivacine ( 1 ), uleine ( 2 ) and N -methyltetrahydroellipticine ( 3 ) from Aspidosperma australe ('yellow guatambú') and the furoquinoline alka...
Source: Chemistry and Biodiversity - September 13, 2019 Category: Biochemistry Authors: Pérez M, Pis Diez CM, Valdez MB, García M, Paola A, Avigliano E, Palermo JA, Blustein G Tags: Chem Biodivers Source Type: research

Synthesis, Structural Characterization and Antimicrobial Evaluation of Ruthenium Complexes with Heteroaromatic Carboxylic Acids.
Abstract The ability of two new ruthenium complexes to show antibacterial and antibiofilm activities against E. coli, S. aureus, P. aeruginosa PAO1 (laboratory strain) and P. aeruginosa LES B58 (clinical strain) in this paper were evaluated. Complexes, mer-[RuIII(2-bimc)3]·H2O (1) and cis-[RuIVCl2(2,3-pydcH)2]·4H2O (2), were obtained using aromatic carboxylic acid ligands, namely, 1H-benzimidazole-2-carboxylic acid (2-bimcH) and pyridine-2,3-dicarboxylic acid (2,3-pydcH2). Compounds were physico-chemically characterized using X-ray diffraction, Hirshfeld surface analysis, IR and UV-Vis spectroscopies...
Source: Chemistry and Biodiversity - September 13, 2019 Category: Biochemistry Authors: Jabłońska-Wawrzycka A, Rogala P, Czerwonka G, Michałkiewicz S, Hodorowicz M, Barszcz B Tags: Chem Biodivers Source Type: research

Synthesis, Characterization and Evaluation of Cytotoxic Activity of Novel Aziridinyl Phosphonic Acid Derivatives.
e S Abstract New aziridine 2-phosphonic acids were prepared by mono hydrolysis of the aziridine 2-phosphonates that were obtained by the modified Gabriel-Cromwell reaction of vinyl phosphonate or alpha-tosylvinyl phosphonate with a primary amine or a chiral amine. The cellular cytotoxicity of these compounds was tested against the HCT-116 colorectal cancer cell line and the CCD-18Co normal colon fibroblast line using the MTT assay.  Three of the synthesized phosphonic acid derivatives 2e, 2h and 2i showed higher cytotoxicity than the reference cancer treatment agent etoposide. Cell death was through a robust ...
Source: Chemistry and Biodiversity - September 12, 2019 Category: Biochemistry Authors: Dogan Ö, Khan R, Ulusan S, Banerjee S Tags: Chem Biodivers Source Type: research

Synthesis and Antioxidant Activity of Carane and Pinane Based Sulfenimines and Sulfinimines.
Abstract The synthesis of sulfenimines and sulfinimines has been carried out with 10-hydroxyisocamphylthiol. The stereochemistry of the compounds has been deduced by methods of NMR, DFT calculations and X-ray diffraction analysis. The cytotoxic, antioxidant and membrane-protective activity of the synthesized compounds as well as of the previously obtained sulfenimines and sulfinimines based on 4-caranethiol have been determined. PMID: 31503399 [PubMed - as supplied by publisher] (Source: Chemistry and Biodiversity)
Source: Chemistry and Biodiversity - September 10, 2019 Category: Biochemistry Authors: Sudarikov DV, Krymskaya YV, Shevchenko OG, Slepukhin PA, Rubtsova SA, Kutchin AV Tags: Chem Biodivers Source Type: research

Cornusglucosides A and B, two new iridoid glucosides from the fruit of Cornus officinalis Sieb. et Zucc.
Abstract Phytochemical investigation of the fruit of Cornus officinalis led to the isolation and characterization of two new iridoid glucosides, named cornusglucoside A (1) and cornusglucoside B (2). Their structures were elucidated by means of spectroscopic methods (UV, IR, HR-ESI-MS, 1D and 2D NMR) and chemical evidence, as well as by comparison with known analogues in the literature. Additionally, their abilities to inhibit the activation of IL-6-induced STAT3 in HepG2 cells were assessed. PMID: 31487435 [PubMed - as supplied by publisher] (Source: Chemistry and Biodiversity)
Source: Chemistry and Biodiversity - September 5, 2019 Category: Biochemistry Authors: Zhang WK, He J, Xu Y, Xu JK, Ye XS, Zhang XX Tags: Chem Biodivers Source Type: research

Recent Advances of Natural Polyphenols Activators for Keap1-Nrf2 Signaling Pathway.
Abstract The dysregulation of Keap1-Nrf2/ARE signaling pathway is associated with many diseases Over the years, a wide range of natural products has provided sufficient resources for the discovery of potential therapeutic drugs. Among them, polyphenols possess Nrf2 activation not only inhibit the production of ROS, inhibit Keap1-Nrf2 protein-protein interaction, but also degrade Keap1 and regulate the Nrf2 related pathway. In fact, with the continuous improvement of natural polyphenols separation and purification technology and further studies on the Keap1-Nrf2 molecular mechanism, more and more natural polyphenol...
Source: Chemistry and Biodiversity - September 3, 2019 Category: Biochemistry Authors: Zhou Y, Jiang Z, Jia G, Shi J Tags: Chem Biodivers Source Type: research

New 2-Oxoimidazolidine Derivatives: Design, Synthesis and Evaluation of Anti-BK Virus Activities in Vitro.
Abstract A series of novel 2-oxoimidazolidine derivatives were synthesized and their antiviral activities against BK human polyomavirus type 1 (BKPyV) were evaluated in vitro. Bioassays showed that the synthesized compounds 1-((5-(dichloromethylene)-2-oxoimidazolidin-4-ylidene)amino)sulfonylpiperidine-4-carboxylic acid and 4-(dichloromethylene)-5-(cyclobutylsulfamoylimino)-2-oxoimidazo¬lidine exhibited moderate activities against BKPyV (EC50 = 5.4 and 5.5 μM, respectively) that are comparable to the standard drug cidofovir. The first compound exhibited the same cytotoxicity in HFF cells and selectivity inde...
Source: Chemistry and Biodiversity - September 3, 2019 Category: Biochemistry Authors: Kornii Y, Chumachenko S, Shablykin O, Prichard MN, James SH, Hartline C, Zhirnov V, Brovarets V Tags: Chem Biodivers Source Type: research

Comparison of Chemical Composition of the Essential Oils from Different Botanical Organs of Pinus mugo Growing in Poland.
Abstract The essential oils from needles, twigs, bark, wood, cones and young shoots of Pinus mugo were analyzed by GC, GC/MS and 1H-NMR spectroscopy. More than 130 compounds were identified. The oils differed in the quantitative composition. The principal components of the oil from twigs with needles were 3-carene (23.8%) myrcene (22.3%) and α-pinene (10.3%). The needle oil contained mainly α-pinene (18.6%), 3-carene (11.3%) and bornyl acetate (8.3%). The oils from twigs without needles, young shoots, bark and wood were dominated by 3-carene (28.6%, 15.0%, 18.5% and 34.6%, respectively) and myrcene (23...
Source: Chemistry and Biodiversity - September 2, 2019 Category: Biochemistry Authors: Lis A, Lukas M, Mellor K Tags: Chem Biodivers Source Type: research

Chemodiversity and Antiproliferative Activity of the Essential Oil of Schinus molle L.Growing in Jordan.
Abstract The leaves and unripe and fully-grown fruits of Schinus molle were collected from three geographical regions of Jordan:Amman (the Mediterranean), Madaba (Irano-Turanean), and Sahab (Saharo-Arabian).The hydro-distilled volatile oils of fresh and driedleaves and fruits were analyzed by gas chromatography-mass spectrometry (GC/MS).The actual composition of the emitted volatiles was determined using Solid Phase Micro-Extraction (SPME). Alphaand β- phellandrenes were the majorcomponents in all the analyzed samples. Quantitative differences were observed in the obtained essential oils (0.62 - 5.25%).Additi...
Source: Chemistry and Biodiversity - September 1, 2019 Category: Biochemistry Authors: Afifi F, Aboalhaija NH, Awwad O, Khalil E, Abbassi R, Abaza IF Tags: Chem Biodivers Source Type: research

Synthesis of amido sulfonamido heteroaromatics under ultrasonication and their antimicrobial activity.
Abstract A convenient and facile methodology for N-sulfonylation of heteroaryl amines with ethyl chlorosulfonylacetate in the presence of dispersed sodium in THF under ultrasonication is reported. The corresponding heteroaryl sulfonamido esters are directly condensed with heteroaryl amines to get amido sulfonamido heteroaromatics in the presence of mild base in THF under ultrasonication. Utilization of easy reaction conditions, shorter reaction times, and isolation of products in high yields under ultrasonication makes this process as an economically viable. The compounds 12c, 12d, 12f and 13f are potential antiba...
Source: Chemistry and Biodiversity - August 30, 2019 Category: Biochemistry Authors: Divya KRG, Teja GL, Yamini G, Padmaja A, Padmavathi V Tags: Chem Biodivers Source Type: research

An ent-kaurane diterpenoid isolated from Isodon excia (Maxim.) Hara Suppresses Bcr-Abl Protein Expression In Vitro and In Vivo and Induces Apoptosis of CML Cells.
Abstract Chronic myelogenous leukemia (CML) is a disease of the blood stem cells that features the oncoprotein Bcr-Abl. Tyrosine kinase inhibitors (TKIs) are used to treat CML patients, but these have limited efficacy due to the emergence of resistance via genetic mutation. Kamebakaurin is an ent-kaurane diterpenoid that has been isolated from Isodon excia (maxim.) hara. Herein, we investigate the potential of kamebakaurin as a chemotherapy reagent for the treatment of CML. We conducted in vitro and in vivo biological experiments and found that kamebakaurin potently inhibits cell proliferation, mainly by enhancing...
Source: Chemistry and Biodiversity - August 29, 2019 Category: Biochemistry Authors: Xia Y, Feng M, Wang E, Chen L, Wang J, Hou R, Zhao Y Tags: Chem Biodivers Source Type: research

Phytochemical content, Antidiabetic, Anticholinergic, Antioxidant Activities of Endemic Lecokia cretica Extracts.
ccedil;in İ, Köksal E Abstract The aim of this work was to investigate the enzyme inhibition, antioxidant activity, and phenolic compounds of Lecokia cretica (Lam.) DC. Acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase enzymes were strongly inhibited by the L. cretica extracts. IC 50 values for the three enzymes were found as 3.21 mg/mL, 2.1 mg/mL, and 2.07 mg/mL respectively. Antioxidant activities were examined in both aqueous and ethanol (EtOH) extracts using CUPRAC, FRAP, and DPPH method. Also, the phenolic compounds of the endemic plant were identified and quantified by ...
Source: Chemistry and Biodiversity - August 29, 2019 Category: Biochemistry Authors: Aras A, Bursal E, Türkan F, Tohma H, Kılıç Ö, Gülçin İ, Köksal E Tags: Chem Biodivers Source Type: research

Essential Oil Compositions and Antibacterial and Antioxidant Activities of Five Lavandula stoechas Cultivars Grown in Thailand.
Abstract The essential oils of five Lavandula stoechas cultivars grown in Thailand were characterized for their volatile compounds using GC-FID and GC-MS methods as well as screened for antibacterial and antioxidant activities. Dried aerial parts, including flowers and stems from each cultivar, were subjected to hydrodistillation for 4 h. The essential oil yields were 0.18%-0.82% w/w. Of the 95 compounds detected and identified, 1,8-cineole, fenchone, and camphor were considered the major compounds. Essential oil from each cultivar demonstrated different patterns of antibacterial activity and a variety of antioxid...
Source: Chemistry and Biodiversity - August 28, 2019 Category: Biochemistry Authors: Insawang S, Pripdeevech P, Pripdeevech C, Pripdeevech S, Pripdeevech S, Nakham T, Artrod A, D'Souza PE, Panuwet P Tags: Chem Biodivers Source Type: research

Phytotoxic Diterpenoids from Plants and Microorganisms.
This article argues that the phytotoxic diterpenoids isolated from the plants and microorganisms can either inhibit the seed germination and the growth of plant seedlings or lead to some disease symptoms on the tested plant tissues and plant seedlings. PMID: 31456316 [PubMed - as supplied by publisher] (Source: Chemistry and Biodiversity)
Source: Chemistry and Biodiversity - August 27, 2019 Category: Biochemistry Authors: Wei W, Li Y, Li H, Ma K, Wang L, Gao K Tags: Chem Biodivers Source Type: research

Chemosensitizing effect of cernumidine extracted from Solanum cernuum Vell. on bladder cancer cells in vitro.
Abstract Cernumidine (CER) is a guanidinic alkaloid isolated from Solanum cernuum's leaves. In this work, we investigated the cytotoxicity, chemosensitizing effect of cernumidine to cisplatin (cDDP) and the possible mechanism of action of the combination on bladder cancer cells. Cernumidine showed cytotoxicity and could sensitize bladder cancer cells to cisplatin. The combination of CER+cDDP inhibited cell migration on T24 cells. CER+cDDP down-regulated MMP-2/9 and p-ERK1/2, while it increased EGFR activity corroborating the observed cell migration inhibition. Down-regulation of Bcl-2 and up-regulation pro-apoptot...
Source: Chemistry and Biodiversity - August 25, 2019 Category: Biochemistry Authors: Bastos J, Miranda MA, Mondal A, Sachdeva M, Cabral H, Neto YAAH, Khan I, Groppo M, McChesney JD Tags: Chem Biodivers Source Type: research

Chemical Analysis of Selected Seaweeds and Seagrass from the Adriatic Coast of Montenegro.
Abstract The three seaweeds (Halimeda tuna, Codium bursa and Cystoseira barbata) and one seagrass (Cymodocea nodosa) were collected from the Coast of Montenegro, Gulf of Boka Kotorska and their chemical analysis was performed. In seagrass C. nodosa, three phenolic compounds were identified (diosmetin 7- sulphate, caphtaric and coutaric acid). The content of β-glucan, fatty acids, sterols and micro- and macro-elements were investigated among all samples. The highest content of β-glucan was detected in C. nodosa seagrass (13.04 ± 0.42 g/100 g). The highest polyunsaturated fatty acids (PUFAs) level, ...
Source: Chemistry and Biodiversity - August 23, 2019 Category: Biochemistry Authors: Milović S, Stanković I, Radović J, Kolundžić M, Nikolić V, Stanojković T, Nikolić D, Petović S, Kundaković T Tags: Chem Biodivers Source Type: research

Interference of seasonal variation on the antimicrobial and cytotoxic activities of the essential oils from the leaves of Iryanthera polyneura Ducke in the Amazon rain forest.
ni IB Abstract The essential oils (EOs) obtained from the leaves of Iryanthera polyneura Ducke trees was chemically assessed and tested for the ability of inhibit the growth of Candida albicans, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus mutans and S. sanguis. The oil was also tested against breast (MCF-7) and prostate (PC-3) cancer cell lines. Minimum bactericidal concentrations (MBCs) and inhibitory concentrations 50 (IC50) values were obtained. EOs were active against Gram positive bacteria. Spathulenol, α-cadinol and τ-muurolol were major com...
Source: Chemistry and Biodiversity - August 22, 2019 Category: Biochemistry Authors: Martins ER, Díaz IEC, Paciencia MLB, Frana SA, Morais D, Eberlin MN, Silva JS, Silveira ER, Barros MP, Suffredini IB Tags: Chem Biodivers Source Type: research

Synthesis and antibacterial evaluation of Mannich bases derived from 1,2,4-triazole.
Abstract The series of novel Mannich bases were synthesized and evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative bacterial strains. The results showed that all compounds were less active than the drugs used as reference, but some of them had moderate potency against Staphylococcus epidermidis ATCC 12228 and Bacillus subtilis ATCC 6633. The presence of a phenyl ring in the position 4 of piperazine seems to be a necessary for antibacterial activity in this class of compounds. PMID: 31436917 [PubMed - as supplied by publisher] (Source: Chemistry and Biodiversity)
Source: Chemistry and Biodiversity - August 22, 2019 Category: Biochemistry Authors: Wujec M, Paneth A, Trotsko N, Popiołek Ł, Grzegorczyk A, Krzanowski T, Janowska S, Malm A Tags: Chem Biodivers Source Type: research

Mechanistic Insight into the Photodynamic Effect Mediated by Neutral Red and a New Azine Compound in Staphylococcus aureus Cells.
Abstract The photodynamic activity of Neutral Red and the new monobrominated Neutral Red was studied in suspensions of Staphylococcus aureus. The effect of mannitol and sodium azide in the presence of 25 µM photosensitizer on lethal photosensitization were investigated. The results of the mechanistic evaluation of Neutral Red showed that both mannitol and sodium azide produced a completed protective effect after irradiation without significant differences between them. The evaluation of monobromated Neutral Red also showed a protective effect of microorganisms with the addition of mannitol. Although sodium a...
Source: Chemistry and Biodiversity - August 19, 2019 Category: Biochemistry Authors: Urrutia MN, Ortiz CS, Alovero FL Tags: Chem Biodivers Source Type: research

Headspace solid phase microextraction coupled to GC-MS for the analysis of volatiles of honeys from arid and Mediterranean areas of Algeria.
Abstract The volatile composition of seven honey samples collected from various regions of Algeria and feeding on different plants have been determined. The Headspace Solid-Phase MicroExtraction (HS-SPME) coupled with Gas Chromatography-Mass Spectrometry (GC-MS) was used to achieve the purpose. In this work, different parameters of the HS-SPME analytical method were investigated in order to reach maximal sensitivity, and thus to obtain maximum information about the volatile profile of Algerian honey. These parameters include saline medium, HS extraction temperature, and the nature of the fibre used. The results sh...
Source: Chemistry and Biodiversity - August 16, 2019 Category: Biochemistry Authors: Neggad A, Benkaci-Ali F, Alsafra Z, Eppe G Tags: Chem Biodivers Source Type: research

Caffeic Acid Inhibits the Formation of Advanced Glycation End Products (AGEs) and Mitigates the AGEs-Induced the Oxidative Stress and Inflammation Reaction in Human Umbilical Vein Endothelial Cells (HUVECs).
Abstract The advanced glycation end products (AGEs) are the products of non-enzymatic glycation reaction of proteins and sugars, which can induce the generation of free radicals and the expression of inflammatory factors, thereby playing an important role in vascular dysfunction in diabetes. To investigate the effects of caffeic acid (CA) on glycation formed by glucose and protein, various spectroscopic techniques and molecular docking methods were carried out. Furthermore, the protective effects of CA on human umbilical vein endothelial cells (HUVECs) damaged by AGEs were explored. The results indicated that CA i...
Source: Chemistry and Biodiversity - August 16, 2019 Category: Biochemistry Authors: Cao X, Xia Y, Zeng M, Wang W, He Y, Liu J Tags: Chem Biodivers Source Type: research

Extraction of natural fragrance ingredients: history overview and future trends.
The objective of this review is to draw a clear picture of where those technological advances are today and to assess the ones that may be effectively transposed at the industrial scale tomorrow. PMID: 31419369 [PubMed - as supplied by publisher] (Source: Chemistry and Biodiversity)
Source: Chemistry and Biodiversity - August 16, 2019 Category: Biochemistry Authors: Burger P, Plainfossé H, Brochet X, Chemat F, Fernandez X Tags: Chem Biodivers Source Type: research

Variation of Chemical Constituents and Antiradical Capacity of Nine Ferulago angulata (Schltdl.) Boiss Populations from Iran.
Abstract The present study was designed to assess the influence of geographical factors on essential oil (EO) composition, along with antiradical potential and phytochemical contents of Ferulago angulata (Schltdl.) Boiss (Apiaceae) extracts for the first time. The aerial parts were hydro-distilled by Clevenger apparatus and subjected to gas chromatography coupled with flame ionization detector (GC/FID) and mass spectroscopy (GC/MS). The EO yields were significantly different from populations "Mongar" (south-slope, 3000 m) with 1.34 ± 0.06% and "Male-Amiri" (north slope, 2600 m) with 0.18...
Source: Chemistry and Biodiversity - August 15, 2019 Category: Biochemistry Authors: Bagherifar S, Sourestani MM, Zolfaghari M, Mottaghipisheh J, Zomborszki ZP, Csupor D Tags: Chem Biodivers Source Type: research

Enhancement of the Amazonian A çaí Waste Fibers through Variations of Alkali Pretreatment Parameters.
Enhancement of the Amazonian Açaí Waste Fibers through Variations of Alkali Pretreatment Parameters. Chem Biodivers. 2019 Aug 13;: Authors: de Oliveira DNPS, Claro PIC, de Freitas RR, Martins MA, Souza TM, da S E Silva BM, Mendes LM, Bufalino L Abstract The açaí fruit depulping produces large amounts of long lignocellulosic fiber bundles that are disposed in the environment. Chemical pretreatments may improve açaí fibers favoring their usage in advanced materials. This work aimed to define optimal alkali reaction parameters to improve the properties of a&ccedi...
Source: Chemistry and Biodiversity - August 13, 2019 Category: Biochemistry Authors: de Oliveira DNPS, Claro PIC, de Freitas RR, Martins MA, Souza TM, da S E Silva BM, Mendes LM, Bufalino L Tags: Chem Biodivers Source Type: research

Variability in the phytochemical contents and free radical-scavenging capacity of Capsicum annuum var. glabriusculum (Wild Piquin Chili).
This study aimed to determine the variations in the phytochemical and antioxidant contents of the wild Piquin chili. The total flavonoid content of hydroalcoholic extracts (0.06 to 0.70 mg equivalent of quercetin per gram of dry weight (mg QE/g DW)), free radical-scavenging capacity for 2,2-Diphenyl-1-picrylhydrazyl (DPPH·) radicals (0.55 to 8.55 mM TE/g DW), amount of 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) in aqueous extracts (18.13 to 107.6 mM TE/g DW) and pungency (21,760 to 88,476 Scoville heat units) were highly variable. By analyzing the spatial distribution using the first three princi...
Source: Chemistry and Biodiversity - August 12, 2019 Category: Biochemistry Authors: Moreno-Ramírez YDR, Hernández-Bautista A, López PA, Vanoye-Eligio V, Torres-Rodríguez ML, Torres-Castillo JA Tags: Chem Biodivers Source Type: research

Synthesis and Antioxidant Ability of Novel Derivatives Based on para-Coumaric Acid Containing Isobornyl Groups.
Abstract A series of novel esters and amides was synthesized on the basis of para-coumaric acid containing isobornyl groups in ortho-positions relative to the phenolic hydroxyl. Antioxidant properties of the obtained compounds were evaluated and compared on in vitro models: radical-scavenging ability, antioxidant activity on a substrate containing the lipids of animal brain, cytotoxicity of red blood cells, antioxidant and membrane-protective properties on the model of oxidative red blood cells hemolysis. Statistically significant relationship was established between the antioxidant activity of the studied compoun...
Source: Chemistry and Biodiversity - August 10, 2019 Category: Biochemistry Authors: Buravlev EV, Dvornikova IA, Schevchenko OG, Kutchin AV Tags: Chem Biodivers Source Type: research

Polyphenol characterization, antioxidant and skin whitening properties of Alnus cordata (Loisel.) Duby stem bark.
In conclusion, results show that A. cordata stem bark may be considered a potential source of agents for the treatment of skin disorders due to its bleaching properties and favourable safety profiles, associated to a good antioxidant power. PMID: 31397975 [PubMed - as supplied by publisher] (Source: Chemistry and Biodiversity)
Source: Chemistry and Biodiversity - August 9, 2019 Category: Biochemistry Authors: Smeriglio A, D'Angelo V, Denaro M, Trombetta D, Raimondo FM, Germanò MP Tags: Chem Biodivers Source Type: research

Profiles of the Essential Oils and Headspace Analysis of Volatiles from Mandragora autumnalis Bertol. Growing Wild in Tunisia.
This study characterizes and distinguishes M. autumnalis from Tunisia and attributes the compounds responsible for the intoxicating and particular odour of fruits. PMID: 31390142 [PubMed - as supplied by publisher] (Source: Chemistry and Biodiversity)
Source: Chemistry and Biodiversity - August 7, 2019 Category: Biochemistry Authors: Arbi F, Ayari-Gribaa O, Souilem F, Chiboub W, Zardi-Berguaoui A, Ben Jannet H, Ascrizzi R, Flamini G, Harzallah-Skhiri F Tags: Chem Biodivers Source Type: research