Types A and D Trichothecene Mycotoxins from the Fungus Myrothecium roridum

Planta Medica ◽  
2019 ◽  
Vol 85 (09/10) ◽  
pp. 774-780 ◽  
Author(s):  
Waranya Lakornwong ◽  
Kwanjai Kanokmedhakul ◽  
Kasem Soytong ◽  
Arm Unartngam ◽  
Sarawut Tontapha ◽  
...  
Keyword(s):  
Fungal Biomass ◽  
Macrocyclic Lactone ◽  
Antimalarial Activity ◽  
Pathogenic Fungus ◽  
The Other ◽  
Spectroscopic Methods ◽  
Type D ◽  
Vero Cell Line ◽  
Type A Trichothecenes ◽  
Myrothecium Roridum

AbstractChromatographic separation of extracts from the fungal biomass of a plant pathogenic fungus, Myrothecium roridum, yielded 8 trichothecene toxins including 6 type D trichothecenes (1–6) and 2 type A trichothecenes (7–8). 6′,12′-Epoxymyrotoxin A (1) and 7′-hydroxymytoxin B (2) were new macrocyclic trichothecenes, while the other trichothecenes were identified as myrotoxin B (3), myrotoxin D hydrate (4), 2′,3′-epoxymyrothecine A (5), miotoxin A (6), and 2 trichothecenes lacking the macrocyclic lactone system, roridin L-2 (7) and trichoverritone (8). The structures of these mycotoxins were characterized using spectroscopic methods. The absolute configurations of 1 and 2 were determined by NOESY and a comparison of their experimental and calculated ECD spectra. Most of these mycotoxins (1–4 and 6) exhibited highly potent antimalarial activity against Plasmodium falciparum. They also showed strong cytotoxicity towards KB and NCI-H187 cell lines (IC50 0.60 – 112.28 nM), as well as the Vero cell line (IC50 1.50 – 46.51 nM).

Antimalarial activity of the bisquinoline trans-N1,N2-bis (7-chloroquinolin-4-yl)cyclohexane-1,2-diamine: comparison of two stereoisomers and detailed evaluation of the S,S enantiomer, Ro 47-7737.

1997 ◽  
Vol 41 (3) ◽  
pp. 677-686 ◽  
Author(s):  
R G Ridley ◽  
H Matile ◽  
C Jaquet ◽  
A Dorn ◽  
W Hofheinz ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Ex Vivo ◽  
The Other ◽  
Parasite Resistance ◽  
Curative Effect ◽  
Specific Process ◽  
Terminal Half Life ◽  
Detailed Evaluation ◽  
Oral Doses

The S,S enantiomer of the bisquinoline trans-N1,N2-bis(7-chloroquinolin-4-yl)cyclohexane-1,2-diamine, Ro 47-7737, is significantly more potent against chloroquine-resistant Plasmodium falciparum than the R,R enantiomer and the previously described racemate. Both the enantiomers and the racemate are more potent inhibitors of heme polymerization than chloroquine, and their activities are probably mediated by inhibition of this parasite-specific process. The S,S enantiomer, Ro 47-7737, was studied in more detail and proved to be a potent antimalarial in the treatment of P. vivax ex vivo and P. berghei in vivo. Its suppression of P. berghei growth in a mouse model (50% effective dose, 2.3 mg/kg of body weight) was equal to that of chloroquine and mefloquine, and Ro 47-7737 was found to be more potent than these two drugs in the Rane test, in which the curative effect of a single dose is monitored. The dose at which 50% of animals were permanently cured (34 mg/kg) was markedly superior to those of chloroquine (285 mg/kg) and mefloquine (> 250 mg/kg). When administered orally at 50 mg/kg, Ro 47-7737 also showed a faster clearance of parasites than either chloroquine or mefloquine, and unlike the other two compounds, Ro 47-7737 showed no recrudescence. In a study to compare prophylactic efficacies of oral doses of 50 mg/kg, Ro 47-7737 provided protection for 14 days compared to 3 days for mefloquine and 1 day for chloroquine. The good curative and prophylactic properties of the compound can be explained in part by its long terminal half-life. The ability to generate parasite resistance to Ro 47-7737 was also assessed. With a rodent model, resistance could be generated over eight passages. This rate of resistance generation is comparable to that of mefloquine, which has proved to be an effective antimalarial for many years. Toxicity liabilities, however, ruled out this compound as a candidate for drug development.

scholarly journals Two New Polyiodides in the 4,4´-Bipyridinium Diiodide/Iodine System

2012 ◽  
Vol 67 (1) ◽  
pp. 5-10
Author(s):  
Guido J. Reiss ◽  
Martin van Megen
Keyword(s):  
Hydrogen Bonding ◽  
Hydrogen Bonds ◽  
Complex I ◽  
The Other ◽  
Cyclic Dimer ◽  
Water Molecules ◽  
Spectroscopic Methods ◽  
Halogen Bonds ◽  
One Dimensional ◽  
Hydroiodic Acid

The reaction of bipyridine with hydroiodic acid in the presence of iodine gave two new polyiodide-containing salts best described as 4,4´-bipyridinium bis(triiodide), C10H10N2[I3]2, 1, and bis(4,4´-bipyridinium) diiodide bis(triiodide) tris(diiodine) solvate dihydrate, (C10H10N2)2I2[I3]2 · 3 I2 ·2H2O, 2. Both compounds have been structurally characterized by crystallographic and spectroscopic methods (Raman and IR). Compound 1 is composed of I3 − anions forming one-dimensional polymers connected by interionic halogen bonds. These chains run along [101] with one crystallographically independent triiodide anion aligned and the other triiodide anion perpendicular to the chain direction. There are no classical hydrogen bonds present in 1. The structure of 2 consists of a complex I144− anion, 4,4´-bipyridinium dications and hydrogen-bonded water molecules in the ratio of 1 : 2 : 2. The I144− polyiodide anion is best described as an adduct of two iodide and two triiodide anions and three diiodine molecules. Two 4,4´-bipyridinium cations and two water molecules form a cyclic dimer through N-H· · ·O hydrogen bonds. Only weak hydrogen bonding is found between these cyclic dimers and the polyiodide anions.

Synthesis, thermal stability, electronic features, and antimicrobial activity of phenolic azo dyes and their Ni(II) and Cu(II) complexes

2014 ◽  
Vol 68 (3) ◽  
Author(s):  
Selma Bal ◽  
Sedat Bal ◽  
Abdullah Erener ◽  
Hatice Halipci ◽  
Seyhan Akar
Keyword(s):  
Thermal Stability ◽  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Azo Dyes ◽  
Coordination Compounds ◽  
Decomposition Temperature ◽  
Water Soluble ◽  
The Other ◽  
Spectroscopic Methods ◽  
Antimicrobial And Antifungal Activity

AbstractFour water soluble azo dyes, 4-(isopropyl)-2-[(E)-(4-chlorophenyl)diazenyl]phenol (L 1), 4-(isopropyl)-2-[(E)-(2,4-dichlorophenyl)diazenyl]phenol (L2), 4-(sec-butyl)-2-[(E)-(4-chlorophenyl) diazenyl]phenol (L 3), 4-(sec-butyl)-2-[(E)-(2,4-dichlorophenyl)diazenyl]phenol (L 4), and their Cu(II) and Ni(II) complexes were synthesized and characterized using spectroscopic methods. Examination of their thermal stability revealed similar decomposition temperature of approximately 260–300°C and that they were more thermally stable than their metal complexes. Ni(II) complexes of ligands L2 and L4 were more stable than the other coordination compounds. Among the synthesized ligands, L2 and the complexes Cu(L3)2 and Ni(L4)2 showed both antimicrobial and antifungal activity. However, the other ligands and the complexes were poorly active against selected microorganisms.

scholarly journals Bioxanthracenes from the Insect Pathogenic Fungus Cordyceps pseudomilitaris BCC 1620. I. Taxonomy, Fermentation, Isolation and Antimalarial Activity.

2001 ◽  
Vol 54 (1) ◽  
pp. 29-35 ◽  
Author(s):  
AMONLAYA JATURAPAT ◽  
MASAHIKO ISAKA ◽  
NIGEL L. HYWEL-JONES ◽  
YUWAPIN LERTWERAWAT ◽  
SUMALEE KAMCHONWONGPAISAN ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Pathogenic Fungus

Microbial Hydroxylation of Hydroxyprogesterones and α-Glucosidase Inhibition Activity of Their Metabolites

2007 ◽  
Vol 62 (4) ◽  
pp. 593-599 ◽  
Author(s):  
Muhammad Iqbal Choudhary ◽  
Muhammad Nasir ◽  
Shamsun N. Khan ◽  
Muhammad Atif ◽  
Rahat A. Ali ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Inhibitory Activity ◽  
Microbial Transformation ◽  
The Other ◽  
Gibberella Fujikuroi ◽  
Spectroscopic Methods ◽  
Cunninghamella Elegans ◽  
Inhibition Activity ◽  
Microbial Hydroxylation ◽  
Other Hand

Microbial transformation of 11α-hydroxyprogesterone (1) with Cunninghamella elegans, Gibberella fujikuroi, Fusarium lini, and Candida albicans yielded 11α,15α,16α-trihydroxypregn-4- ene-3,20-dione (3), 11α-hydroxy-5α-pregnane-3,20-dione (4), 6β ,11α-dihydroxypregn-4-ene-3,20- dione (5), 11α-hydroxypregna-1,4-diene-3,20-dione (6), 11α,17β -dihydroxyandrost-4-en-3-one (7), and 11α,15α-dihydroxypregn-4-ene-3,20-dione (8). On the other hand, microbial transformation of 17α-hydroxyprogesterone (2) with Cunninghamella elegans and Fusarium lini yielded 11α,17α- dihydroxypregn-4-ene-3,20-dione (9), and 17α-hydroxypregna-1,4-diene-3,20-dione (10). The structures of the metabolites 3 - 10 were deduced on the basis of spectroscopic methods. Compound 3 was identified as a new metabolite, which exhibited a promising inhibitory activity against the α-glucosidase enzyme.

scholarly journals Crossings and Nestings in Set Partitions of Classical Types

10.37236/392 ◽  
2010 ◽  
Vol 17 (1) ◽  
Author(s):  
Martin Rubey ◽  
Christian Stump
Keyword(s):  
Type A ◽  
The Other ◽  
Type B ◽  
Set Partition ◽  
Set Partitions ◽  
Type D ◽  
Other Hand ◽  
The One

In this article, we investigate bijections on various classes of set partitions of classical types that preserve openers and closers. On the one hand we present bijections for types $B$ and $C$ that interchange crossings and nestings, which generalize a construction by Kasraoui and Zeng for type $A$. On the other hand we generalize a bijection to type $B$ and $C$ that interchanges the cardinality of a maximal crossing with the cardinality of a maximal nesting, as given by Chen, Deng, Du, Stanley and Yan for type $A$. For type $D$, we were only able to construct a bijection between non-crossing and non-nesting set partitions. For all classical types we show that the set of openers and the set of closers determine a non-crossing or non-nesting set partition essentially uniquely.

scholarly journals Investigation of antimalarial activity and cytotoxicity profiling of a Bangladeshi plant Syzygium cymosum

2020 ◽  
Vol 14 (08) ◽  
pp. 924-928
Author(s):  
Muhammad Riadul Haque Hossainey ◽  
Saiful Arefeen Sazed ◽  
Maisha Khair Nima ◽  
Mohammad Saydur Rahman ◽  
Tanvir Ashraf ◽  
...  
Keyword(s):  
Vero Cell ◽  
Cell Line ◽  
Crude Extract ◽  
Antimalarial Drug ◽  
Methanolic Extract ◽  
Antimalarial Activity ◽  
Chloroform Fraction ◽  
Moderate Activity ◽  
Plant Materials ◽  
Vero Cell Line

Introduction: The persistent increase of resistance to existing antimalarials underscores the needs for new drugs. Historically, most of the successful antimalarial are derived from plants. The leaves of the S. cymosum is one of the plant materials used by traditional healers in malaria-endemic areas in Bangladesh for treatment of malaria. Here, we investigated the crude extract and its fractions against chloroquine (CQ)-sensitive 3D7, CQ-resistant Dd2, and artemisinin (ART)-resistant IPC 4912 Mondulkiri strains of Plasmodium falciparum. Methodology: The antimalarial activities were tested using HRP II based in-vitro antimalarial drug sensitivity ELISA described by WWARN and half inhibitory concentrations (IC50) were calculated by non-linear regression analysis using GraphaPad Prism. The cytotoxicity of the crude methanolic extract was assessed using the MTT assay on Vero cell line. Results: The methanolic crude extract revealed promising activity against 3D7 (IC50 6.28 µg/mL), Dd2 (IC50 13.42 µg/mL), and moderate activity against IPC 4912 Mondulkiri (IC50 17.47 µg/mL). Among the fractionated portions, the chloroform fraction revealed highest activity against IPC 4912 Mondulkiri (IC50 1.65 µg/mL) followed by Dd2 (1.73 µg/mL) and 3D7 (2.39 µg/mL). The crude methanolic extract also demonstrated good selectivity with the selectivity indices of > 15.92, > 7.45, and > 6.91 against 3D7, Dd2, and IPC 4912, respectively when tested against Vero cell line. Conclusions: This is the first report on S. cymosum for its putative antimalarial activity, and is imperative to go for further phytochemical analyses in order to investigate possible novel antimalarial drug compound(s).

scholarly journals The cluster and dual canonical bases of Z[x(11), ..., x(33)] are equal

2010 ◽  
Vol Vol. 12 no. 5 (Combinatorics) ◽  
Author(s):  
Brendon Rhoades
Keyword(s):  
Quantum Group ◽  
Polynomial Ring ◽  
Geometric Model ◽  
Cluster Algebra ◽  
Canonical Basis ◽  
The Other ◽  
Monomial Basis ◽  
Type D ◽  
Dual Canonical Basis ◽  
International Audience

Combinatorics International audience The polynomial ring Z[x(11), ..., x(33)] has a basis called the dual canonical basis whose quantization facilitates the study of representations of the quantum group U-q(sl(3) (C)). On the other hand, Z[x(1 1), ... , x(33)] inherits a basis from the cluster monomial basis of a geometric model of the type D-4 cluster algebra. We prove that these two bases are equal. This extends work of Skandera and proves a conjecture of Fomin and Zelevinsky.

scholarly journals Effect of bismuth and bore content in glass system inhibitor on the corrosion behavior of mild steel in 1M hydrochloric acid solution

2019 ◽  
Vol 8 (4) ◽  
pp. 328-337 ◽  
Author(s):  
Azeddine Elbadaoui ◽  
Galai Mouhsine ◽  
Soumya Ferraa ◽  
Hanane Barebita ◽  
Mohammed Cherkaoui Cherkaoui ◽  
...  
Keyword(s):  
Hydrochloric Acid ◽  
Acid Solution ◽  
Mild Steel ◽  
Corrosion Behavior ◽  
Steel Surface ◽  
Inhibition Efficiency ◽  
The Other ◽  
Spectroscopic Methods ◽  
Electrochemical Polarization ◽  
Inhibitor Type

The influence of (0.90-x) Bi2O3-xB2O3-0.10 (Ta2O5-Nb2O5) on the corrosion behavior of mild steel in 1M hydrochloric acid was studied. Electrochemical polarization and impedance spectroscopic methods measurements were used. The inhibition efficiency increases with S1 concentration to reach 79% at 150 ppm. Polarization curves show that our inhibitors. S1 is a cathodic inhibitor type. The increase in temperature leads to a decrease in the inhibition efficiency of the used inhibitor. The thermodynamic study showed that the film was formed at the steel surface by physisorption in the presence of inhibitor. Moreover, in this study, the results showed that the inhibition efficiencies depend on the B2O3 andBi2O3 content in the glass. it is observed that the value at 50% of B2O3 in the glass provided better protection than the other content.

SYNTHESIS, ANTIMALARIAL ACTIVITY AND QSAR STUDIES OF CHALCONES,N-BENZYLIDENESULFONAMIDES AND CHALCONESULFONAMIDES

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (05) ◽  
pp. 20-34
Author(s):  
A. H. More ◽  
◽  
S. J Raul ◽  
S. S Mahajan
Keyword(s):  
Antimalarial Activity ◽  
Qsar Model ◽  
The Other ◽  
Acute Oral Toxicity ◽  
Microwave Irradiation Method ◽  
Oral Toxicity ◽  
Training Set ◽  
Test Set ◽  
Qsar Studies ◽  
Life Threatening

Malaria remains the major cause of human morbidity and mortality worldwide. Malaria, caused byPlasmodium species, is potentially life threatening, increasing in prevalence and becoming evenmore resistant to in-use drugs. In this article, synthesis of compounds from the series of chalcones,benzylidenesulfonamides and chalconesulfonamides, by the conventional and microwave-irradiationmethods is discussed. The microwave-irradiation method was convenient, rapid and high yielding ascompared to the conventional method of synthesis. The acute oral toxicity studies indicated that all thecompounds were safe for administration up to 2000 mg/kg body weight of a mouse. The compoundswere screened for their antimalarial activity. Two chalcones, five benzylidenesulfonamides and threechalconesulfonamides showed antimalarial activity equivalent to chloroquine. Benzylidenesulfonamidesshowed better antimalarial activity compared to the compounds from the other two series.Chalconesulfonamides showed better antimalarial activity than chalcones. The QSAR studies werecarried out by correlating antimalarial activity of all the compounds with their physicochemical descriptors.Validation of the best QSAR model was carried out using the training set and the test set method. Thesestudies provided guidance for the development of novel antimalarials from these series.

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