Microfluidic arrays of dermal spheroids: a screening platform for active ingredients of skincare products

Lab on a Chip ◽  
2021 ◽  
Vol 21 (20) ◽  
pp. 3952-3962
Author(s):  
Zhengkun Chen ◽  
Sina Kheiri ◽  
Albert Gevorkian ◽  
Edmond W. K. Young ◽  
Valerie Andre ◽  
...  
Keyword(s):  
Active Ingredients ◽  
Screening Platform ◽  
Microfluidic Arrays

A novel microfluidic array of a spheroid-based dermis model enables time-efficient in vitro screening of active ingredients of skincare products.

Construction of lux-based promoter-reporter platforms in Mycobacterium bovis BCG for screening of drug repurposing small-molecule compounds as new anti-tuberculosis drugs

2021 ◽  
Author(s):  
Li Zhu ◽  
Annie Wing-tung Lee ◽  
Kelvin Ka-Lok WU ◽  
Peng GAO ◽  
Kingsley King-Gee Tam ◽  
...  
Keyword(s):  
Small Molecule ◽  
Drug Repurposing ◽  
Virulence Gene ◽  
Multidrug Resistant ◽  
Rapid Screening ◽  
Human Macrophage ◽  
Tuberculosis Complex ◽  
Low Cytotoxicity ◽  
Screening Platform

The emergence of multidrug-resistant strains and hyper-virulent strains of Mycobacterium tuberculosis are big therapeutic challenges for tuberculosis (TB) control. Repurposing bioactive small-molecule compounds has recently become a new therapeutic approach against TB. This study aimed to construct a rapid screening system to identify novel anti-TB agents from a library of small-molecule compounds. In this study, a total of 320 small-molecule compounds were used to screen for their ability to suppress the expression of a key virulence gene, phoP, of M. tuberculosis complex using luminescence (lux)-based promoter-reporter platforms. The minimum inhibitory and bactericidal concentrations on drug-resistant M. tuberculosis and cytotoxicity to human macrophage were determined. RNA-sequencing (RNA-seq) was conducted to determine the drug mechanisms of the selected compounds as novel antibiotics or anti-virulent agents against the M. tuberculosis complex. Six compounds displayed bactericidal activity against M. bovis BCG, in which Ebselen demonstrated the lowest cytotoxicity to macrophage and was considered as a potential antibiotic for TB. Another ten compounds did not inhibit the in vitro growth of the M. tuberculosis complex but down-regulated the expression of phoP specifically. Of them, ST-193 and ST-193 (hydrochloride) showed low cytotoxicity and could dysregulate the entire phoP-associated gene network, and thus identified as potential anti-virulence agents for M. tuberculosis. This study provides a rapid screening platform coupled with a systematic validation and eventually suggested one potential antibiotic and two anti-virulence agents for M. tuberculosis infections.

scholarly journals In vitro mycelial sensitivity of Macrophomina phaseolina to fungicides

2013 ◽  
Vol 43 (4) ◽  
pp. 460-466 ◽  
Author(s):  
Rosane Fátima Baldiga Tonin ◽  
Aveline Avozani ◽  
Anderson Luiz Durante Danelli ◽  
Erlei Melo Reis ◽  
Sandra Maria Zoldan ◽  
...  
Keyword(s):  
Mycelial Growth ◽  
Petri Dish ◽  
Macrophomina Phaseolina ◽  
Control Treatment ◽  
Active Ingredients ◽  
Ic50 Values ◽  
Growth Evaluation ◽  
Fungus Growth ◽  
Ic50 Concentration

Black root rot, caused by Macrophomina phaseolina (Tass.) Goid., is the most common root disease in soybean fields. This study aimed to determine the in vitro mycelial sensitivity, measured by the IC50 (concentration to inhibit 50% of the fungus mycelial growth) of a M. phaseolina isolate obtained from soybean, to different fungicides (thiram, iprodione, carbendazim, pyraclostrobin, fluquinconazol, tolyfluanid, metalaxyl and penflufen + trifloxystrobin), at six concentrations (0.01 mg L-1, 0.10 mg L-1, 1.00 mg L-1, 10.00 mg L-1, 20.00 mg L-1 and 40.00 mg L-1 of the active ingredient). The 0.00 mg L-1 concentration represented the control, without fungicide addition. The mycelial growth evaluation was performed with the aid of a digital pachymeter, by measuring the colonies diameter, when the fungus growth in the control treatment reached the Petri dish edge. The experimental design was completely randomized, with four replications. Concerning the fungitoxicity of active ingredients, a variation from non-toxic to highly fungitoxic was observed to the M. phaseolina isolate, with IC50 values ranging from 0.23 mg L-1 to > 40.00 mg L-1, being carbendazim the most efficient one (IC50 = 0.23 mg L-1). The fungus showed insensitivity to the active ingredients of fluquinconazole, metalaxyl, thiram and tolyfluanid.

scholarly journals MyoScreen, a High-Throughput Phenotypic Screening Platform Enabling Muscle Drug Discovery

2018 ◽  
Vol 23 (8) ◽  
pp. 790-806 ◽  
Author(s):  
Joanne Young ◽  
Yoran Margaron ◽  
Mathieu Fernandes ◽  
Eve Duchemin-Pelletier ◽  
Joris Michaud ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
High Throughput ◽  
Acetylcholine Receptors ◽  
Calcium Release ◽  
Screening Strategy ◽  
Adult Skeletal Muscle ◽  
New Chemical Entities ◽  
Drug Treatments ◽  
Screening Platform

Despite the need for more effective drug treatments to address muscle atrophy and disease, physiologically accurate in vitro screening models and higher information content preclinical assays that aid in the discovery and development of novel therapies are lacking. To this end, MyoScreen was developed: a robust and versatile high-throughput high-content screening (HT/HCS) platform that integrates a physiologically and pharmacologically relevant micropatterned human primary skeletal muscle model with a panel of pertinent phenotypic and functional assays. MyoScreen myotubes form aligned, striated myofibers, and they show nerve-independent accumulation of acetylcholine receptors (AChRs), excitation–contraction coupling (ECC) properties characteristic of adult skeletal muscle and contraction in response to chemical stimulation. Reproducibility and sensitivity of the fully automated MyoScreen platform are highlighted in assays that quantitatively measure myogenesis, hypertrophy and atrophy, AChR clusterization, and intracellular calcium release dynamics, as well as integrating contractility data. A primary screen of 2560 compounds to identify stimulators of myofiber regeneration and repair, followed by further biological characterization of two hits, validates MyoScreen for the discovery and testing of novel therapeutics. MyoScreen is an improvement of current in vitro muscle models, enabling a more predictive screening strategy for preclinical selection of the most efficacious new chemical entities earlier in the discovery pipeline process.

Ultradeformable vesicles: concepts and applications relating to the delivery of skin cosmetics

2021 ◽  
Author(s):  
Andang Miatmoko ◽  
Qurrota Ayunin ◽  
Widji Soeratri
Keyword(s):  
Skin Aging ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Active Ingredients ◽  
Self Confidence ◽  
Skin Delivery ◽  
Cosmetic Ingredients ◽  
Insight Into

Skin aging is a phenomenon resulting in reduced self-confidence, thus becoming a major factor in social determinants of health. The use of active cosmetic ingredients can help prevent skin aging. Transfersomes are well known to be capable of deeply penetrating the dermis. This scoping review provides an insight into transfersomes and their prospective use in anti-aging cosmetics. Numerous reports exist highlighting the successful skin delivery of therapeutic agents such as high-molecular-weight, poorly water soluble and poorly permeable active ingredients by means of transfersomes. Moreover, in vitro and in vivo studies have indicated that transfersomes increase the deposition, penetration and efficacy of active ingredients. However, the use of transfersomes in the delivery of active cosmetic ingredients is limited. Considering their similar physicochemical properties, transfersomes should possess considerable potential as a delivery system for anti-aging cosmetics.

Targeting FGL2, a molecular drug target for glioblastoma, with natural compounds through virtual screening method

2021 ◽  
Author(s):  
Fahad Hassan Shah ◽  
Song Ja Kim
Keyword(s):  
Virtual Screening ◽  
Active Site ◽  
Drug Target ◽  
Screening Method ◽  
Tumor Development ◽  
Pharmacokinetic Profile ◽  
Natural Compounds ◽  
Screening Platform ◽  
Proliferation In Vitro

Background: Fibroleukin-2 protein (FGL2) causes redevelopment of brain tumors. Inhibition of these proteins has shown to improve glioblastoma prognosis and treatment efficacy. Aim: The current study gathered recently exploited natural compounds that suppress glioblastoma proliferation in vitro, tested against FGL2 protein. Method: Twenty-five compounds were explored through a virtual screening platform. Results: Three natural compounds (betanine, hesperetin and ovatodiolide) hit the active site of FGL2. Furthermore, the influence of these compounds was also assessed using in silico gene expression, and ADMET tools showed downregulation of some genes, which caused rapid tumor development while possessing a moderate acute toxicity and pharmacokinetic profile. Conclusion: Our study presents three compounds that are good candidates for evaluation in FGL2 mutated glioblastoma animal models.

Prediction of the skin sensitization potential of didecyldimethylammonium chloride and 3,7-dimethyl-2,6-octadienal and mixtures of these compounds with the excipient ethylene glycol through the human Cell Line Activation Test and the Direct Peptide Reactivity Assay

2019 ◽  
Vol 35 (8) ◽  
pp. 507-519 ◽  
Author(s):  
JaeHee Lee ◽  
AhRang Cho ◽  
Ravi Gautam ◽  
YeonGyeong Kim ◽  
SoJung Shin ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Antimicrobial Agent ◽  
Cell Line ◽  
Human Cell ◽  
Human Cell Line ◽  
Skin Sensitization ◽  
Active Ingredients ◽  
Activation Test ◽  
Didecyldimethylammonium Chloride

In commercial products such as household deodorants or biocides, didecyldimethylammonium chloride (DDAC) often serves as an antimicrobial agent, citral serves as a fragrance agent, and the excipient ethylene glycol (EG) is used to dissolve the active ingredients. The skin sensitization (SS) potentials of each of these substances are still being debated. Moreover, mixtures of DDAC or citral with EG have not been evaluated for SS potency. The in vitro alternative assay called human Cell Line Activation Test (h-CLAT) and Direct Peptide Reactivity Assay (DPRA) served to address these issues. On three independent runs of h-CLAT, DDAC and citral were predicted to be sensitizers while EG was predicted to be a non-sensitizer and also by the DPRA. Mixtures of DDAC or citral with EG at ratios of 7:3 and 1:4 w/v were all positive by the h-CLAT in terms of SS potential but SS potency was mitigated as the proportion of EG increased. Citral and its EG mixtures were all positive but DDAC and its EG mixtures were all negative by the DPRA, indicating that the DPRA method is not suitable for chemicals with pro-hapten characteristics. Since humans can be occupationally or environmentally exposed to mixtures of excipients with active ingredients, the present study may give insights into further investigations of the SS potentials of various chemical mixtures.

Abstract 782: Development of a high throughput in vitro screening platform to identify novel inducers of immunological cell death

2018 ◽  
Author(s):  
Didier Grillot ◽  
Akanksha Gangar ◽  
Raphaelle Guillard-Huet ◽  
Eric Boursier ◽  
Florent Potvain ◽  
...  
Keyword(s):  
Cell Death ◽  
High Throughput ◽  
In Vitro Screening ◽  
Screening Platform

Predictive Modeling and Biomechanical Microengineering of Mesenchymal Stem Cells: A High Content Screening Platform to Enhance Lineage Specific Differentiation

2013 ◽  
Author(s):  
Amit Paul ◽  
David Franz ◽  
Sumaira Yahya ◽  
Shan Sun ◽  
Michael Cho
Keyword(s):  
Stem Cells ◽  
Mesenchymal Stem Cells ◽  
Stem Cell ◽  
Predictive Modeling ◽  
Stem Cell Differentiation ◽  
High Content Screening ◽  
Cell Behavior ◽  
Functional Changes ◽  
Screening Platform

Recent evidence suggests that stem cell differentiation can be regulated by modulation of the cell’s biomechanics. The cytoskeletal structures and arrangements in stem cells undergoing differentiation are dramatically altered, and these alterations vary by lineage. The complexity of events associated with the transformation of these precursor cells leaves many questions unanswered about morphological, structural, proteomic, and functional changes in differentiating stem cells. A thorough understanding of stem cell behavior, both experimentally and computationally, would allow for the development of more effective approaches to the expansion of stem cells in vitro and for the regulation of their commitment to a specific phenotype.

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