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Chemistry & Biodiversity

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https://www.readbyqxmd.com/read/29325229/dual-drug-targeting-of-mutant-bcr-abl-induces-inactive-conformation-new-strategy-for-the-treatment-of-chronic-myeloid-leukemia-and-overcoming-monotherapy-resistance
#1
Ahmed A El Rashedy, Fisayo A Olotu, Mahmoud E S Soliman
Bcr-Abl is an oncogenic fusion protein which expression enhances tumorigenesis, and has been highly associated with chronic myeloid leukemia (CML). Acquired drug resistance in mutant Bcr-Abl has enhanced pathogenesis with the use of single therapy agents such as Nilotinib. Moreover, allosteric targeting has been identified to consequentially inhibit Bcr-Abl activity, which led to the recent development of ABL-001 (asciminib) that selectively binds the myristoyl pocket. Experimental studies have revealed that the combination of Nilotinib and ABL-001 induced a "bent" conformation in the C-terminal helix of Bcr-Abl; a benchmark of inhibition, thereby exhibiting a greater potency in the treatment of CML, surmounting the setbacks of drug resistance, disease regression and relapse...
January 11, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29325221/naphthalene-derivatives-and-quinones-from-ventilago-denticulata-and-their-nitric-oxide-radical-scavenging-antioxidant-cytotoxic-antibacterial-and-phosphodiesterase-inhibitory-activities
#2
Wannapha Molee, Anuchit Phanumartwiwath, Chatchai Kesornpun, Sanya Sureram, Nattaya Ngamrojanavanich, Kornkanok Ingkaninan, Chulabhorn Mahidol, Somsak Ruchirawat, Prasat Kittakoop
New naphthalene derivatives (1 and 2) and a new isomer (3) of ventilagolin, together with known anthraquinones, chrysophanol (4), physcion or emodin 3-methyl ether (5), and emodin (6), were isolated from vines of Ventilago denticulata. The isolated compounds exhibited cytotoxic activity with IC50 values of 1.15-40.54 μg/mL. Compounds 1-3 selectively exhibited weak antibacterial activity (MIC values of 200.0-400.0 μg/mL), while emodin (6) displayed moderate antibacterial activity with MIC values of 25.0 μg/mL...
January 11, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29325215/oplopane-sesquiterpenes-from-ligularia-knorringiana-and-their-anti-complementary-activity
#3
Wei Dai, Chuang-Qi Lu, Yan Wang, Yan Lu, Dao-Feng Chen, Qi Wang
Three new oplopane sesquiterpenes, knorringianalarins D - F (1 - 3, resp.), and five known analogues (4 - 8, resp.) were isolated from the roots and rhizomes of Ligularia knorringiana. The structures of three new compounds were identified as 4-acetoxy-2β-hydroxy-3β-(2-methylbutyryloxy)-9α-(4-methylsenecioyloxy)-11α,12-epoxyoplop-10(14)-ene (1), 3β,4-diacetoxy-8α-(2-methylbutyryloxy)-9α-(4-acetoxy-4-methylsenecioyloxy)-11α,12-epoxyoplop-10(14)-ene (2), and (1R,5R,6R,7R,9R)-5,9,11-trihydroxy-4,15-dinor-10(14)-oplopen-3-one (3) based on spectroscopic methods including 1D, 2D NMR, mass spectrometry, and CD spectroscopy techniques...
January 11, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29292595/hybrid-pharmacophore-design-molecular-docking-synthesis-and-biological-evaluation-of-novel-aldimine-type-schiff-base-derivatives-as-tubulin-polymerization-inhibitor
#4
Alieh Ameri, Ghadamali Khodarahmi, Hamid Forootanfar, Farshid Hassanzadeh, Gholam-Hosein Hakimelahi
A series of hybrid Aldimine-type Schiff base derivatives including trimethoxyphenyl ring and 1,2,4-triazle-3-thiol/thione were designed as tubulin inhibitors. The molecular docking simulations on tubulin complex (PDB: 1SA0) revealed that derivatives with nitro and /or chloro or dimethylamine substitutes (4-Nitro, 2-Nitro, 3-Nitro, 4-Cl-3-nitro, and 4-N(CH3 )2 ) on the aldehyde ring were the best compounds with remarkable binding energies (-9.09, -9.07, -8.63, -8.11, and -8.07 kcalmol-1 , respectively) compared to Colchicine (-8...
January 1, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29292594/chemical-composition-antioxidant-and-anti-melanogenic-activities-of-essential-oils-from-chrysanthemum-boreale-makino-at-different-harvesting-stages
#5
Do-Yoon Kim, Kyung-Jong Won, Dae Il Hwang, Soo Min Park, Bokyung Kim, Hwan Myung Lee
In the present study, the chemical compositions and skin whitening-related anti-oxidant and anti-melanogenic effect of essential oils (EOs) extracted from Chrysanthemum boreale MAKINO (CBM) (CBMEOs) at vegetative, pre-flowering and full-flowering are investigated and contrasted among the three stages. The yields and components of the CBMEOs were different at each stage. The CBMEOs increased DPPH and ABTs scavenging activities and attenuated the α-melanocyte stimulating hormone (α-MSH)-induced tyrosinase activity and melanin synthesis in B16BL6 cells...
January 1, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29282856/chemical-composition-of-essential-oils-from-thymus-vulgaris-cymbopogon-citratus-and-rosmarinus-officinalis-and-their-effects-on-the-hiv-1-tat-protein-function
#6
Feriotto Giordana, Marchetti Nicola, Costa Valentina, Beninati Simone, Tagliati Federico, Mischiati Carlo
New drugs would be beneficial to fight resistant HIV strains, in particular those capable of interfering with essential viral functions other than those targeted by highly active antiretroviral therapy drugs. Despite the central role played by Tat protein in HIV transcription, a search for vegetable extracts able to hamper this important viral function was never carried out. In this work, we evaluated the chemical composition and possible interference of essential oil from Thymus vulgaris, Cananga odorata, Cymbopogon citratus and Rosmarinus officinalis with the Tat/TAR-RNA interaction and with Tat-induced HIV-1 LTR transcription...
December 28, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29278459/antiviral-activity-of-faramea-hyacinthina-and-faramea-truncata-leaves-on-dengue-virus-type-2-and-their-major-compounds
#7
Rodolfo S Barboza, Ligia M M Valente, Thiago Wolff, Iranaia Assunção-Miranda, Rômulo S L Neris, Iris P Guimarães-Andrade, Mário Gomes
The defatted fractions of the Faramea hyacinthina and F. truncata (Rubiaceae) leaf MeOH extracts showed in vitro non-cytotoxic and anti-dengue virus serotype 2 (DENV2) activity in human hepatocarcinoma cell lineage (HepG2). Submitting these fractions to the developed RP-SPE method allowed isolating the antiviral flavanone (2S)-isosakuranetin-7-O-β-D-apiofuranosyl(1→6)-β-D-glucopyranoside (1) from both species and yielded less active sub-fractions. The new diasteroisomeric epimer pair 2S + 2R of 5,3',5'-trihydroxy-flavanone-7-O-β-D-apiofuranosyl(1→6)-β-D-glucopyranoside (2a/2b) from F...
December 26, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29266741/reaction-product-variability-and-biological-activity-of-the-lactoperoxidase-system-depending-on-medium-ionic-strength-and-ph-and-on-substrate-relative-concentration
#8
Françoise Bafort, Christian Damblon, Nicolas Smargiasso, Edwin De Pauw, Jean-Paul Perraudin, M Haïssam Jijakli
The potential of ions produced in water by the lactoperoxidase system against plant pests has shown promising results. We tested the bioactivity of ions produced by the lactoperoxidase oxidation of I- and SCN- in several buffers or in tap water and characterized the ions produced. In vitro biological activity was tested against Penicillium expansum, the causal agent of mold in fruits, and the major cause of patulin contamination of fruit juices and compotes. In buffers, the ionic concentration was increased 3-fold, and pathogen inhibition was obtained down to the 1/15 dilution...
December 20, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29239523/iridoides-of-chemotaxonomy-relevance-a-new-antirrhinoside-ester-and-other-constituents-from-kickxia-spuria%C3%A2-subsp-integrifolia-brot-r-fern
#9
Alessandro Venditti, Claudio Frezza, Ilaria Serafini, Alessandro Ciccòla, Fabio Sciubba, Mauro Serafini, Armandodoriano Bianco
In this work, the secondary metabolite content of the ethanolic extract of Kickxia spuria subsp. integrifolia (Brot.) R. Fern. is reported. Fourteen compounds were isolated and identified by means of Column Chromatography and NMR and MS spectrometric techniques, respectively. Among these compounds, the chemotaxonomic markers of the species were evidenced whereas others were reported for the first time in the genus. Among these a new antirrhinoside derivative (12) was recognized. The iridoid content show a molecular pattern very similar to those reported for other taxa comprised in the Antirrhinae tribe of Plantaginaceae, thus providing an additional evidence to support the current botanical classification of the Kickxia genus...
December 14, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29236361/new-metabolites-produced-by-cylindrocarpon-sp-sy-39-from-a-driftwood
#10
Takuma Suzuki, Seiya Yoshida, Takuya Koseki, Takako Aboshi, Tetsuya Murayama, Unang Supratman, Yoshihito Shiono
Four novel cylindropyrone A (1), 10'-hydroxyilicicolinic acid D (3), cylindrolactones A (4) and B (5), together with known dihydroinfectopyrone (2) were isolated from the culture of Cylindrocarpon sp. SY-39 from a driftwood. Their structures were elucidated using 1D- and 2D-NMR spectroscopy. Compound 3 showed antimicrobial activity against Staphylococcus aureus with MIC value of 5.0 μg/ml. This article is protected by copyright. All rights reserved.
December 13, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29224253/phytochemical-composition-and-biological-activities-of-dyssodia-tagetiflora-lag
#11
Ana María García-Bores, Amira Arciniegas-Arciniegas, Alma Reyna Campos, Carlos Céspedes-Acuña, Betsaida Avila-Suárez, Julio Alarcón-Enos, Saul Flores-Maya, Adriana Montserrat Espinosa-González, Alfonso Romo de Vivar-Romo, Carlos Pérez Plasencia, José Guillermo Avila-Acevedo
While plants of the genus Dyssodia are used by man to a certain extent, few phytochemical and pharmacological studies have been performed with species of this genus. D. tagetiflora is an endemic plant of Mexico and has been used as fodder. The aim of this research was to isolate and identify the main bioactive components and evaluate the insecticidal, antioxidant, genotoxic and cytoprotective activities of D. tagetiflora. The isolated substances included an essential oil composed of six monoterpenes, and extracts containing two flavonols, three flavonol-glycosides and four thiophenes...
December 10, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29194948/chagosendines-a-c-new-metal-complexes-of-imidazole-alkaloids-from-the-calcareous-sponge-leucetta-chagosensis
#12
Bang An, Fuling Yin, Nicole J de Voogd, Xiaoguang Chen, Wei Cheng, Wenhan Lin
Chemical examination of the bright yellow sponge Leucetta chagosensis resulted in the isolation of three new imidazole-based alkaloid complexes namely chagosendines A-C (1-3), together with known analogues pyronaamidine, naamidine J, and naamine C. Their structures were determined on the basis of extensive spectroscopic (IR, MS, NMR and single-crystal X-ray diffraction) analysis in association with the chemical conversion. The isolated alkaloids together with three synthesized new homodimer complexes were evaluated for the antitumor activities...
November 30, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29178537/chemical-composition-and-in-vitro-anthelmintic-activity-of-extracts-of-tagetes-patula-against-a-multidrug-resistant-isolate-of-haemonchus-contortus
#13
Flávio Augusto Sanches Politi, Amauri Alves Souza, Rafaela Regina Fantatto, Rosemeire Cristina Linhari Rodrigues Pietro, Waldomiro Barioni, Márcio Dias Rabelo, Humberto Ribeiro Bizzo, Ana Carolina de Souza Chagas, Maysa Furlan
Sheep breeding has suffered economic losses due to parasitism by gastrointestinal nematodes, particularly Haemonchus contortus. The use of natural products, specifically Tagetes patula, has been suggested as an alternative method of combatting this issue. Chemical analyses of the extracts of this species described in the literature report the presence of important classes of secondary metabolites such as thiophenes, flavonoids, alkaloids and benzofurans, some of which were identified and isolated in this study...
November 27, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29168349/bioactive-pimarane-diterpenes-from-the-arctic-fungus-eutypella-sp-d-1
#14
Xiaoli Wang, Kunlai Sun, Bin Wang
Two new pimarane diterpenes, libertellenone M (1) and libertellenone N (2), together with five known compounds were isolated from the culture extract of Eutypella sp. D-1 derived from high-latitude soil of the Arctic. The structures of these compounds were determined by spectroscopic data as well as experimental and calculated electronic circular dichroism (ECD) analysis. Antimicrobial and cytotoxic activities of the isolated compounds were evaluated. Compound 3 exhibited weak antibacterial activity against Escherichia coli, Bacillus subtilis, and Vibrio vulnificus, each with MIC values of 16 μg/mL...
November 23, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29164821/cytotoxic-triterpenoids-from-roots-of-actinidia-chinensis
#15
Liu-Bin Wei, Si-Yuan Ma, Hong-Xing Liu, Chu-Sheng Huang, Na Liao
Phytochmical investigation of roots of Actinidia chinensis PLANCH led to the isolation triterpenoids 1 - 16, including a new compound 2α,3α,23,24-tetrahydroxyurs-12,20(30)-dien-28-oic acid (1). Their structures were identified on the basis of spectroscopic analysis, including 1D- and 2D-NMR, HR-ESI mass spectrometry, and by comparison with the literatures. The cytotoxicities of triterpenoids 1 - 16 against a panel of cultured human cancer cell lines (HepG2, A549, MCF-7, SK-OV-3, and HeLa) were evaluated. The new compound 1 exhibited moderate antitumor activities with IC50 values of 19...
November 21, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29164813/chemical-polymorphism-of-essential-oils-of-artemisia-vulgaris-growing-wild-in-lithuania
#16
Asta Judzentiene, Jurga Budiene
Compositional variability of mugwort (Artemisia vulgaris L.) essential oils has been investigated in the study. Plant material (over ground parts at full flowering stage) was collected from forty-four wild populations in Lithuania. The oils from aerial parts were obtained by hydrodistillation and analyzed by GC(FID) and GC/MS. In total, up to 111 components were determined in the oils. As the major constituents were found: sabinene, 1,8-cineole, artemisia ketone, both thujone isomers, camphor, cis-chrysanthenyl acetate, davanone and davanone B...
November 21, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29164812/inter-and-intraspecific-variability-of-nitrogenated-compounds-in-gorgonian-corals-via-application-of-a-fast-one-step-analytical-protocol
#17
Chiara Samorì, Federica Costantini, Paola Galletti, Emilio Tagliavini, Marco Abbiati
Gorgonian corals play a structural role in temperate and tropical biogenic reefs, forming animal forests and creating biodiversity hot spots. In the Mediterranean Sea, slow-growing and long-lived gorgonian species are threatened by human disturbances and global environmental changes and concern about their conservation is rising. Alkaloid metabolites have proven to be essential in protecting these species from environmental stressors.. Traditional profiling methodologies to detect these metabolites require a large quantity of living tissue...
November 21, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29164790/comparative-study-of-fatty-acids-profile-in-eleven-wild-mushrooms-of-boletacea-and-russulaceae-families
#18
Marija V Dimitrijevic, Violeta D Mitic, Olga P Jovanovic, Vesna P Stankov Jovanovic, Jelena S Nikolic, Goran M Petrovic, Gordana S Stojanovic
Eleven species of wild mushrooms which belong to Boletaceae and Russulaceae families were examined by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) analysis for the presence of fatty acids. As far as we know, the fatty acid profiles of B. purpureus and B. rhodoxanthus were described for the first time. Twenty-six fatty acids were determined. Linoleic (19.5 - 72%), oleic (0.11 - 64%), palmitic (5.9 - 22%) and stearic acids (0.81 - 57%) were present in the highest contents. In all samples, unsaturated fatty acids dominate...
November 21, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29164786/four-new-acylated-iridoid-glycosides-from-the-aerial-part-of-veronicastrum-sibiricum-and-their-antioxidant-response-element-inducing-activity
#19
Myeong Il Kim, Chul Young Kim
Four new (1 - 4) and one known (5) acylated iridoid glycosides were isolated from aerial parts of Veronicastrum sibiricum (L.) Pennell. The chemical structures of isolated compounds were determined to be 3'',4''-dicinnamoyl-6-O-rhamnopyranosyl-10-O-bergaptol-5,7-bisdeoxycynanchoside (1), 3'',4''-dicinnamoyl-6-O-rhamnopyranosylpaulownioside (2), 2'',4''-dicinnamoyl-6-O-rhamnopyranosylcatalpol (3), 3'',4''-dicinnamoyl-6-O-rhamnopyranosylaucubin (4), and 3'',4''-dicinnamoyl-6-O-rhamnopyranosylcatalpol (5) using spectroscopic techniques...
November 21, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29161468/the-relationship-between-endogenous-%C3%AE-glucuronidase-activity-and-biologically-active-flavones-aglycone-contents-in-hairy-roots-of-baikal-skullcap
#20
V S Dikaya, A I Solovyeva, R A Sidorov, P A Solovyev, A Yu Stepanova
Here we examine the relationship between contents of principal flavones in hairy roots of Scutellaria baicalensis with the activity of the β-glucuronidase (sGUS) enzyme during a culturing cycle. Using RP-HPLC, we show that the highest contents of aglycones, baicalin and wogonin is observed at the growth days 8, 14 and 71 and reach 45, 41 and 62% (based on the total weight of hairy roots of the Baikal skullcap), correspondingly. Their accumulation is accompanied by increase of the sGUS activity, which we determined fluorometrically...
November 21, 2017: Chemistry & Biodiversity
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