scholarly journals Small-Molecule Screens Reveal Novel Haustorium Inhibitors in the Root Parasitic PlantTriphysaria versicolor

2019 ◽  
Vol 109 (11) ◽  
pp. 1878-1887 ◽  
Author(s):  
Yaxin Wang ◽  
Daniel Steele ◽  
Maylin Murdock ◽  
Seigmund Lai ◽  
John Yoder
Keyword(s):  
Small Molecules ◽  
Small Molecule ◽  
Early Stage ◽  
Structural Analog ◽  
Parasitic Plant ◽  
In Vitro Assay ◽  
Vitro Assay ◽  
Transcript Levels ◽  
Parasitic Weeds

Root parasitic weeds in Orobanchaceae pose a tremendous threat to agriculture worldwide. We used an in vitro assay to screen libraries of small molecules for those capable of inhibiting or enhancing haustorium development in the parasitic plant Triphysaria versicolor. Several redox-modifying molecules and one structural analog of 2,6-dimethoxybenzoquine (DMBQ) inhibited haustorium development in the presence of the haustorium-inducing factor DMBQ, some of these without apparent growth inhibition to the root. Triphysaria seedlings were able to acclimate to some of these redox inhibitors. Transcript levels of four early-stage haustorium genes were differentially influenced by inhibitors. These novel haustorium inhibitors highlight the importance of redox cycling for haustorium development and suggest the potential of controlling parasitic weeds by interrupting early-stage redox-signaling pathways.

An In Vitro Assay for Evaluation of Small-Molecule Inhibitors of Cholesterol Absorption

2004 ◽  
Vol 116 (35) ◽  
pp. 4753-4756 ◽  
Author(s):  
Lisbet Kværnø ◽  
Tobias Ritter ◽  
Moritz Werder ◽  
Helmut Hauser ◽  
Erick M. Carreira
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Cholesterol Absorption ◽  
In Vitro Assay ◽  
Vitro Assay

scholarly journals Structure based virtual screening identifies small molecule effectors for the sialoglycan binding protein Hsa

2020 ◽  
Vol 477 (19) ◽  
pp. 3695-3707 ◽  
Author(s):  
Rupesh Agarwal ◽  
Barbara A. Bensing ◽  
Dehui Mi ◽  
Paige N. Vinson ◽  
Jerome Baudry ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Small Molecules ◽  
Small Molecule ◽  
Critical Role ◽  
Human Platelets ◽  
T Antigen ◽  
Bacterial Attachment ◽  
Vitro Assay ◽  
Native Ligand

Infective endocarditis (IE) is a cardiovascular disease often caused by bacteria of the viridans group of streptococci, which includes Streptococcus gordonii and Streptococcus sanguinis. Previous research has found that serine-rich repeat (SRR) proteins on the S. gordonii bacterial surface play a critical role in pathogenesis by facilitating bacterial attachment to sialylated glycans displayed on human platelets. Despite their important role in disease progression, there are currently no anti-adhesive drugs available on the market. Here, we performed structure-based virtual screening using an ensemble docking approach followed by consensus scoring to identify novel small molecule effectors against the sialoglycan binding domain of the SRR adhesin protein Hsa from the S. gordonii strain DL1. The screening successfully predicted nine compounds which were able to displace the native ligand (sialyl-T antigen) in an in vitro assay and bind competitively to Hsa. Furthermore, hierarchical clustering based on the MACCS fingerprints showed that eight of these small molecules do not share a common scaffold with the native ligand. This study indicates that SRR family of adhesin proteins can be inhibited by diverse small molecules and thus prevent the interaction of the protein with the sialoglycans. This opens new avenues for discovering potential drugs against IE.

An In Vitro Assay for Evaluation of Small-Molecule Inhibitors of Cholesterol Absorption

2004 ◽  
Vol 43 (35) ◽  
pp. 4653-4656 ◽  
Author(s):  
Lisbet Kværnø ◽  
Tobias Ritter ◽  
Moritz Werder ◽  
Helmut Hauser ◽  
Erick M. Carreira
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Cholesterol Absorption ◽  
In Vitro Assay ◽  
Vitro Assay

scholarly journals In vitro Assay Selection of Glyphosate Resistance in Lettuce

1999 ◽  
Vol 124 (1) ◽  
pp. 86-89 ◽  
Author(s):  
Antonio C. Torres ◽  
Russell T. Nagata ◽  
Robert J. Ferl ◽  
Thomas A. Bewick ◽  
Daniel J. Cantliffe
Keyword(s):  
Early Stage ◽  
Dry Weight ◽  
Glyphosate Resistance ◽  
In Vitro Assay ◽  
Vitro Assay ◽  
Leaf Discs ◽  
Epsps Gene ◽  
Resistance Trait ◽  
The Cost

Glyphosate-resistant plants of `South Bay' lettuce (Lactuca sativa L.) were produced by using Agrobacterium tumefaciens containing a plasmid carrying glyphosate oxidase and EPSPS gene. An in vitro assay was performed to determine the sensitivity of `South Bay' leaf discs and seedling explants to varying glyphosate concentrations. The I50 for glyphosate leaf discs was 53.8 μm and for glyphosate seedlings 7.6 μm. There was a high correlation between the response of leaf discs and seedlings to glyphosate based on dry weight. These findings will allow identification of glyphosate-resistant transformants in an early stage of plant development, saving time and reducing the cost in generating an improved cultivar with the glyphosate resistance trait.

In Vitro Assay of Platelet Adhesiveness with Washed and Tanned Human Red Cells

1968 ◽  
Vol 20 (03/04) ◽  
pp. 384-396 ◽  
Author(s):  
G Zbinden ◽  
S Tomlin
Keyword(s):  
Platelet Adhesion ◽  
Sodium Citrate ◽  
Blood Platelets ◽  
In Vitro Assay ◽  
Red Cells ◽  
Platelet Adhesiveness ◽  
Vitro Assay ◽  
In Vitro System ◽  
Human Red Cells

SummaryAn in vitro system is described in which adhesion of blood platelets to washed and tannic acid-treated red cells was assayed quantitatively by microscopic observation. ADP, epinephrine and TAME produced a reversible increase in platelet adhesiveness which was antagonized by AMP. With Evans blue, polyanetholsulfonate, phthalanilide NSC 38280, thrombin and heparin at concentrations above 1-4 u/ml the increase was irreversible. The ADP-induced increase in adhesiveness was inhibited by sodium citrate, EDTA, AMP, ATP and N-ethylmaleimide. EDTA, AMP and the SH-blocker N-ethylmaleimide also reduced spontaneous platelet adhesion to red cells. No significant effects were observed with adenosine, phenprocoumon, 5-HT, phthalanilide NSC 57155, various estrogens, progestogens and fatty acids, acetylsalicylic acid and similarly acting agents, hydroxylamine, glucose and KCN. The method may be useful for the screening of thrombogenic and antithrombotic properties of drugs.

Angiogenic Effect of Pravastatin Alone and with Sera from Healthy and Complicated Pregnancies Studied by in vitro Vasculogenesis/Angiogenesis Assay

2021 ◽  
pp. 1-9
Author(s):  
Anita Virtanen ◽  
Outi Huttala ◽  
Kati Tihtonen ◽  
Tarja Toimela ◽  
Tuula Heinonen ◽  
...  
Keyword(s):  
Direct Effect ◽  
Late Onset ◽  
Maternal Serum ◽  
In Vitro Assay ◽  
Serum Samples ◽  
Therapeutic Concentration ◽  
Tubule Formation ◽  
Vitro Assay ◽  
Angiogenesis Assay

<b><i>Objective:</i></b> To determine the direct effect of pravastatin on angiogenesis and to study the interaction between pravastatin and maternal sera from women with early- or late-onset pre-eclampsia (PE), intrauterine growth restriction, or healthy pregnancy. <b><i>Methods:</i></b> We collected 5 maternal serum samples from each group. The effect of pravastatin on angiogenesis was assessed with and without maternal sera by quantifying tubule formation in a human-based in vitro assay. Pravastatin was added at 20, 1,000, and 8,000 ng/mL concentrations. Concentrations of angiogenic and inflammatory biomarkers in serum and in test medium after supplementation of serum alone and with pravastatin (1,000 ng/mL) were measured. <b><i>Results:</i></b> Therapeutic concentration of pravastatin (20 ng/mL) did not have significant direct effect on angiogenesis, but the highest concentrations inhibited angiogenesis. Pravastatin did not change the levels of biomarkers in the test media. There were no changes in angiogenesis when therapeutic dose of pravastatin was added with maternal sera, but there was a trend to wide individual variation towards enhanced angiogenesis, particularly in the early-onset PE group. <b><i>Conclusions:</i></b> At therapeutic concentration, pravastatin alone or with maternal sera has no significant effect on angiogenesis, but at high concentrations the effect seems to be anti-angiogenic estimated by in vitro assay.

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