scholarly journals Enantioselective and Synergistic Herbicidal Activities of Common Amino Acids Against Amaranthus tricolor and Echinochloa crus-galli

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 2071
Author(s):  
Nawasit Chotsaeng ◽  
Chamroon Laosinwattana ◽  
Patchanee Charoenying
Keyword(s):  
Amino Acids ◽  
Biological Activities ◽  
Racemic Mixture ◽  
Amaranthus Tricolor ◽  
Pigment Synthesis ◽  
Barnyard Grass ◽  
Chemical Structures ◽  
Natural Substances ◽  
Wide Range ◽  
Acid Herbicides

Amino acids have a wide range of biological activities, which usually rely on the stereoisomer presented. In this study, glycine and 21 common α-amino acids were investigated for their herbicidal property against Chinese amaranth (Amaranthus tricolor L.) and barnyard grass (Echinochloa crus-galli (L.) Beauv.). Both d- and l-isomers, as well as a racemic mixture, were tested and found that most compounds barely inhibited germination but moderately suppressed seedling growth. Various ratios of d:l-mixture were studied and synergy between enantiomers was found. For Chinese amaranth, the most toxic d:l-mixtures were at 3:7 (for glutamine), 8:2 (for methionine), and 5:5 (for tryptophan). For barnyard grass, rac-glutamine was more toxic than the pure forms; however, d-tryptophan exhibited greater activity than racemate and l-isomer, indicating the sign of enantioselective toxicity. The mode of action was unclear, but d-tryptophan caused bleaching of leaves, indicating pigment synthesis of the grass was inhibited. The results highlighted the enantioselective and synergistic toxicity of some amino acids, which relied upon plant species, chemical structures, and concentrations. Overall, our finding clarifies the effect of stereoisomers, and provides a chemical clue of amino acid herbicides, which may be useful in the development of herbicides from natural substances.

scholarly journals Biological Activity of Bicyclic and Tricyclic Diterpenoids from Salvia Species of Immediate Pharmacological and Pharmaceutical Interest

2011 ◽  
Vol 6 (8) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Maria Carmela Bonito ◽  
Carla Cicala ◽  
Maria Carla Marcotullio ◽  
Francesco Maione ◽  
Nicola Mascolo
Keyword(s):  
Biological Activities ◽  
Folk Medicine ◽  
Plant Defence ◽  
Experimental Studies ◽  
Scientific Basis ◽  
Chemical Structures ◽  
Wide Range ◽  
Real Value ◽  
Antimicrobic Activity ◽  
Cyclic Compounds

Diterpenoids are a class of compounds that derive from the condensation of four isoprene units that leads to a wide variety of complex chemical structures, including acyclic bi-, tri-and tetra-cyclic compounds; in Salvia species, only bi-, tri-and tetra-cyclic compounds have been found. This review covers a wide range of biological activities and mode of action of diterpenoids isolated from Salvia species that might raise some pharmacological and pharmaceutical interest. We have produced a synoptic table where the biological activities of the main active principles are summarized. Our analysis emphasizes that diterpenoids from Salvia species continue to be a plant defence system since their antimicrobic activity. Experimental studies show that most of diterpenoids considered have cytotoxic and / or antiproliferative activity. Some of them have also cardiovascular and central effects. In a less extended manner, diterpenoids from Salvia species show gastrointestinal, urinary, antinflammatory, antidiabetic, ipolipidemic and antiaggregating effects. In the last decade, several clinical trials have been developed in order to investigate the real value of Salvia extracts treatment; results obtained are promising and confer scientific basis in the use of medicinal plants from folk medicine.

scholarly journals Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N-Diethyl-Substituted Amido Moieties

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Olayinka O. Ajani ◽  
Oluwole B. Familoni ◽  
Feipeng Wu ◽  
Johnbull O. Echeme ◽  
Zheng Sujiang
Keyword(s):  
Antibacterial Activity ◽  
Mass Spectra ◽  
Room Temperature ◽  
Biological Activities ◽  
Chemical Structures ◽  
Wide Range ◽  
Synthetic Routes ◽  
Mic Value ◽  
C Nmr

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1–11 and their substituted N,N-diethyl-2-(phenylmethylsulfonamido) alkanamide derivatives, 12–22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1–22 were confirmed by analytical and spectral data such as IR, 1H- and 13C-NMR, and mass spectra. The in vitro antibacterial activity of these compounds along with standard clinical reference, streptomycin, was investigated on two key targeted organisms. It was observed that 1-(benzylsulfonyl)pyrrolidine-2-carboxylic acid, 2 emerged as the most active compound against Staphylococcus aureus at MIC value of 1.8 μg/mL while 4-(3-(diethylamino)-3-oxo-2-(phenylmethylsulfonamido) propyl)phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL.

scholarly journals New Scabimycins A-C Isolated from Streptomyces acidiscabies (Lu19992)

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5922
Author(s):  
Constanze Paulus ◽  
Josef Zapp ◽  
Andriy Luzhetskyy
Keyword(s):  
Natural Products ◽  
Bioactive Peptides ◽  
Biological Activities ◽  
Powerful Source ◽  
Drug Candidates ◽  
Chemical Structures ◽  
Wide Range ◽  
Streptomyces Acidiscabies ◽  
New Compounds ◽  
Important Drug

Peptide natural products displaying a wide range of biological activities have become important drug candidates over the years. Microorganisms have been a powerful source of such bioactive peptides, and Streptomyces have yielded many novel natural products thus far. In an effort to uncover such new, meaningful compounds, the metabolome of Streptomyces acidiscabies was analyzed thoroughly. Three new compounds, scabimycins A–C (1–3), were discovered, and their chemical structures were elucidated by NMR spectroscopy. The relative and absolute configurations were determined using ROESY NMR experiments and advanced Marfey’s method.

scholarly journals Mining of Cyanobacterial Genomes Indicates That Plasmids Are Involved in the Production of Natural Products

2020 ◽  
Author(s):  
Rafael Popin ◽  
Danillo Alvarenga ◽  
Raquel Castelo-Branco ◽  
David Fewer ◽  
Kaarina Sivonen
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Biological Activities ◽  
Gene Clusters ◽  
Biosynthetic Pathways ◽  
Biosynthetic Gene ◽  
Biosynthetic Gene Clusters ◽  
Chemical Structures ◽  
Wide Range ◽  
Genes Encoding

Abstract Background Microbial natural products have unique chemical structures and diverse biological activities. Cyanobacteria commonly possess a wide range of biosynthetic gene clusters to produce natural products. Several studies have mapped the distribution of natural product biosynthetic gene clusters in cyanobacterial genomes. However, little attention has been paid to natural product biosynthesis in plasmids. Some genes encoding cyanobacterial natural product biosynthetic pathways are believed to be dispersed by plasmids through horizontal gene transfer. Thus, we examined complete cyanobacterial genomes to assess if plasmids are involved in the production and dissemination of natural products by cyanobacteria.Results The 185 analyzed genomes possessed 1 to 42 gene clusters and an average of 10. In total, 1816 biosynthetic gene clusters were found. Approximately 95% of these clusters were present in chromosomes. The remaining 5% were present in plasmids, from which homologs of the biosynthetic pathways for aeruginosin, anabaenopeptin, ambiguine, cryptophycin, hassallidin, geosmin, and microcystin were manually curated. The cryptophycin pathway was previously described as active while the other gene cluster include all genes for biosynthesis. Approximately 12% of the 424 analyzed cyanobacterial plasmids contained homologs of genes involved in conjugation. Large plasmids, previously named as “chromids”, were also observed to be widespread in cyanobacteria. Sixteen cryptic natural product biosynthetic gene clusters and geosmin biosynthetic gene clusters were located in those mobile plasmids.Conclusion Homologues of genes involved in the production of toxins, protease inhibitors, odorous compounds, antimicrobials, antitumorals, and other unidentified natural products are located in cyanobacterial plasmids. Some of these plasmids are predicted to be conjugative. The present study provides in silico evidence that plasmids are involved in the distribution of natural product biosynthetic pathways in cyanobacteria.

scholarly journals Synthesis, Characterization and Biological Studies of Some Organotin Compounds: (A-Review)

2020 ◽  
Vol 36 (05) ◽  
pp. 871-878
Author(s):  
Priyanka Siwacha ◽  
Surbhi Soni ◽  
Harish Kumar Sharmaa ◽  
Manoj Kumara
Keyword(s):  
Amino Acids ◽  
Biological Activities ◽  
Organometallic Compounds ◽  
Molecular Structures ◽  
Organotin Compounds ◽  
Single Source ◽  
Biological Studies ◽  
Hybrid Complex ◽  
Wide Range ◽  
Significant Attention

Significant attention has been given to organotin (IV) amino acids compounds in recent years. Organometallic compounds are better known for their potentiality to stabilize peculiar stereochemistry of their complexes and application in agriculture, catalysis and as single source precursors. Due to the better stability and diverse molecular structures the complexes own a wide range of biological activities. These individual properties create an alliance of action in the hybrid complex. In this review, we discuss the chemistry of organotin (IV) complexes and their different aspects in various fields. The aim of the present review is to evaluate the synthesis, characterization and biological activities of organotin compounds.

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL (2-OXO-3-(ARYLIMINO) INDOLIN-1-YL)-N-ARYL PROPANAMIDES AS ANTI-HUMAN IMMUNODEFICIENCY AGENTS

2018 ◽  
Vol 11 (12) ◽  
pp. 318
Author(s):  
Biplab Debnath ◽  
Ping Wang ◽  
Liu-meng Yang ◽  
Yong-tang Zheng ◽  
Swastika Ganguly
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Western World ◽  
Mass Tourism ◽  
Chemical Structures ◽  
Wide Range ◽  
Endogenous Compound ◽  
Acquired Immunodeficiency ◽  
Modern Mass ◽  
Immunodeficiency Syndrome

Objective: Acquired immunodeficiency syndrome (AIDS) was first identified in the Western world in 1981. Since then, AIDS has been increasingly wide spreading, its rapid worldwide dissemination brought about by modern mass tourism. Isatin (1 H-indole-2, 3-Dione), an endogenous compound identified in many organisms, shows a wide range of biological activities. In view of the above details, we wish to report the synthesis and evaluation of novel isatin analogs, as promising anti-human immunodeficiency (HIV) agents.Methods: A series of novel isatin analogs (3a-3p) were synthesized, and their chemical structures were confirmed by nuclear magnetic resonance:1H, 13C, ESI-MS spectral data, and CHNS.Results: The compounds were evaluated as inhibitors of HIV type-1 in MT-4 cell cultures. Of these sixteen compounds, only 5 compounds showed potent anti-HIV activity.Conclusion: Evaluation of compound properties in silico showed that they possess significant drug-like characteristics.

scholarly journals New Eunicellin-Type Diterpenes from the Panamanian Octocoral Briareum asbestinum

Marine Drugs ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 84 ◽  
Author(s):  
Marcelino Gutiérrez ◽  
Ricardo Santamaría ◽  
José Félix Gómez-Reyes ◽  
Héctor M. Guzmán ◽  
Javier Ávila-Román ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Biological Activities ◽  
Chemical Study ◽  
Inflammatory Activity ◽  
Bocas Del Toro ◽  
Chemical Structures ◽  
Wide Range ◽  
Marine Compounds ◽  
Anti Inflammatory ◽  
New Compounds

Gorgonian octocorals are considered a prolific source of secondary metabolites with a wide range of biological activities, including anti-inflammatory activity. In particular, the genus Briareum is known for producing a wealth of diterpenes with complex chemical structures. The chemical study of the methanolic extract of Briareum asbestinum collected in Bocas del Toro, on the Caribbean side of Panama, led to the isolation of three new eunicellin-type diterpenes: briarellin T (1), asbestinin 27 (2), asbestinin 28 (3) and the previously described asbestinin 17 (4). The structures of the new compounds were determined by extensive NMR analyses and HRMS. Anti-inflammatory activity assays showed a significant reduction of the pro-inflammatory cytokines TNF-α, IL-6, IL-1β and IL-8 as well as a downregulation of COX-2 expression in LPS-stimulated THP-1 macrophages. These findings support the potential use of these marine compounds as therapeutic agents in the treatment of inflammatory diseases.

New chalcone derivatives having pyrazole and sulfonamide pharmacophores as carbonic anhydrase inhibitors

2020 ◽  
Vol 17 ◽  
Author(s):  
Mehtap Tugrak ◽  
Halise Inci Gul ◽  
Hulya Akincioglu ◽  
Ilhami Gulcin
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Activities ◽  
Drug Candidate ◽  
Carbonic Anhydrase Inhibitors ◽  
Reference Drug ◽  
Lead Compounds ◽  
Chemical Structures ◽  
Ic50 Value ◽  
Wide Range ◽  
Ic50 Values

Background: Sulfonamide, pyrazole and chalcone pharmacophores are an important compounds in medicinal chemistry. They have wide range of biological activities including carbonic anhydrase (CA) inhibitory activities. Introduction: Carbonic anhydrase I and II inhibitors are used for the treatment of some disease such as retinal and cerebral edema (CAI), edema, epilepsy, and glaucoma (CA II). The available drugs in market have some limitations or side effect problems. So, there is a need to develop new drug candidate compound/s to overcome the problems at issue. In this study, a series of compounds MS4-MS10, (E)-4-(4-(3-aryl)-3-oxoprop-1-en-1-yl)-3-phenyl-1H-pyrazol-1-yl) benzenesulfonamides, were designed to discover new carbonic anhydrase inhibitors using hibryd approach. Methods: The compounds MS4-MS10 were synthesized as shown in Scheme 1 and their chemical structures were confirmed by 1H NMR, 13C NMR and HRMS spectra. Carbonic anhydrase (CAs, E.C.4.2.1.1) inhibitory effects of MS4-MS10 were tested on the hCA I and II isoenzymes by previously reported procedures. Results and Discussons: Carbonic anhydrase inhibitors results of the MS4-MS10 were presented in Table 1 as IC50 values (nM). They were inhibition range of 27.8-87.3 towards hCA I and 24.4-54.8 towards hCA II while reference drug AAZ IC50 values were 384.2 (hCA I) and 36.9 (hCA II). MS7 and MS9 had 13.8 (hCA I) and 1.5 (hCA II) times more potent CA inhibition than reference compound AAZ, respectively. Conclusion: MS7 (Ar: 2,4,5-trimethoxy phenyl) towards hCA I and MS9 (Ar: 3,4-dimethoxy phenyl) towards hCA II were the lead compounds of our series with the lowest IC50 value and can be considered for further studies.

scholarly journals Antiparasitic effects of selected isoflavones on flatworms

2021 ◽  
Vol 58 (1) ◽  
pp. 1-16
Author(s):  
D. Faixová ◽  
G. Hrčková ◽  
T. Mačák Kubašková ◽  
D. Mudroňová
Keyword(s):  
Secondary Metabolites ◽  
Biological Activities ◽  
Plant Secondary Metabolites ◽  
Therapeutic Effects ◽  
Dependent Manner ◽  
Biologically Relevant ◽  
Chemical Structures ◽  
Antiparasitic Drug ◽  
Wide Range

SummaryMedicinal plants have been successfully used in the ethno medicine for a wide range of diseases since ancient times. The research on natural products has allowed the discovery of biologically relevant compounds inspired by plant secondary metabolites, what contributed to the development of many chemotherapeutic drugs. Flavonoids represent a group of therapeutically very effective plant secondary metabolites and selected molecules were shown to exert also antiparasitic activity. This work summarizes the recent knowledge generated within past three decades about potential parasitocidal activities of several flavonoids with different chemical structures, particularly on medically important flatworms such as Schistosoma spp., Fasciola spp., Echinococcus spp., Raillietina spp., and model cestode Mesocestoides vogae. Here we focus on curcumin, genistein, quercetin and silymarin complex of flavonolignans. All of them possess a whole spectrum of biological activities on eukaryotic cells which have multi-therapeutic effects in various diseases. In vitro they can induce profound alterations in the tegumental architecture and its functions as well as their activity can significantly modulate or damage worm´s metabolism directly by interaction with enzymes or signaling molecules in dose-dependent manner. Moreover, they seem to differentially regulate the RNA activity in numbers of worm´s genes. This review suggests that examined flavonoids and their derivates are promising molecules for antiparasitic drug research. Due to lack of toxicity, isoflavons could be used directly for therapy, or as adjuvant therapy for diseases caused by medically important cestodes and trematodes.

The utilization by preruminant lambs of isolated soya bean protein in low protein milk replacers

1975 ◽  
Vol 26 (6) ◽  
pp. 1037 ◽  
Author(s):  
DM Walker ◽  
RD Kirk
Keyword(s):  
Amino Acids ◽  
Nitrogen Balance ◽  
Biological Activities ◽  
Soya Bean ◽  
Low Protein ◽  
Wide Range ◽  
Ad Libitum ◽  
Protein Milk ◽  
Milk Replacers ◽  
Bean Protein

Preruminant male crossbred lambs, aged 2–5 days at the start of the experiment, were used in five experiments with low protein milk replacers (0.10 of total energy as protein). Experiment 1. A diet with isolated soya bean protein (ISP) as the sole source of protein was supplemented with different amounts of DL-methionine. The ISP contained 1.06 g methionine (M) and 1.04 g cystine (C) per 16 g nitrogen (equivalent to 9.1 mg M + C per 100 kJ diet). Maximum nitrogen balance was achieved when the M + C concentration was 15.3 ? 3.7 mg per 100 kJ (equivalent to 3.8 g M + C per 16 g nitrogen). Experiment 2. The ISP diet (plus DL-methionine), was supplemented with L-valine, or L-threonine, or L-isoleucine, or L-lysine monohydrochloride, or a mixture of essential amino acids, to raise their concentration in rsp to those in whole egg proteins (g per 16 g nitrogen). There was no significant improvement in nitrogen balance as aresult of adding amino acids other than DL-methionine. Experiment 3. The ISP diet was supplemented with either DL-methionine (2.4 and 14.8 mg/100 kJ), or L-methionine (2.4 and 1 4 8 mg/100 kJ), or methionine hydroxy analogue (MHA) (14.8 mg/100 kJ), or L-cystine (14 8 mg/100 kJ). Nitrogen balances were determined. It was concluded that the Dand L-isomers of methionine had similar biological activities when used to supplement ISP, and that MHA was as effective as DL-methionine. There was no significant increase in nitrogen balance with the L-cystine supplement. Experiment 4. The ISP diet (plus DL-methionine) was given to three lambs continuously for 33 days. There was no significant change in nitrogen balance with increasing age. Experiment 5. The ISP diet (diet A) and a diet of equivalent protein content based on cows' milk proteins (diet B) were supplemented with DL-methionine and given to groups of lambs over a wide range of intakes of gross energy (GE). The maximum intake of GE by lambs given the ISP diet ad libitum was 1147 kJ/day per kg0.73, an intake far lower than that which would have been taken by lambs given the cows' milk diet ad libitum. The apparent digestibilities of nitrogen and DM in diet A were significantly lower than those in diet B and, at the mean intake of apparently digested nitrogen of 538 mg/day per kg0.73, there were significant differences in the nitrogen balances: the values were 362 and 255 mg nitrogen/day per for the cows' milk and ISP diets respectively.

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