Novel Calcium Aminoclay (CaAC)-Vitamin C Hybrid: In-Vitro Cytotoxicity Assessment in HaCaT Cells and In-Vivo Embryotoxicity Assay in Zebrafish

2021 ◽  
Vol 21 (7) ◽  
pp. 3667-3672
Author(s):  
Vinh Van Tran ◽  
Vu Khac Bui Hoang ◽  
Hang-Suk Chun ◽  
Ju-Young Moon ◽  
Young-Chul Lee
Keyword(s):  
Vitamin C ◽  
Cell Viability ◽  
Hacat Cell ◽  
In Vitro Cytotoxicity ◽  
Hatching Rate ◽  
Hacat Cells ◽  
Promising Candidate ◽  
Cytotoxicity Assessment

Vitamin C (VC) is well-known as a hydrophilic antioxidant commonly used in cosmeceutical formulations due to its protection and maintenance of youthful skin. Aminoclay (AC), a synthetic organic-nanoclay, has shown great potential for delivery of VC. However, the practical cosmeceutical applications of aminoclay for delivery of VC are severely limited due to the paucity of reported research on its cytotoxicity to human skin. Therefore, in the present study, we evaluated the biosafety of a calcium aminoclay-vitamin C (CaAC-VC) hybrid through an In-Vitro cytotoxicity assessment in HaCaT cells and an In-Vivo embryotoxicity assay in zebrafish. HaCaT cell viability and changes in the morphology and hatching rate of the zebrafish were investigated. The results indicated that the CaAC-VC hybrid showed a lower cytotoxicity relative to pure VC and that as such, it should be considered to be a promising candidate for VC-delivery applications.

Two zinc-aminoclays’ in-vitro cytotoxicity assessment in HeLa cells and in-vivo embryotoxicity assay in zebrafish

2017 ◽  
Vol 137 ◽  
pp. 103-112 ◽  
Author(s):  
Hang-Suk Chun ◽  
Duckshin Park ◽  
Song Eun Lim ◽  
Kwang-Hun Jeong ◽  
Ji-Seon Park ◽  
...  
Keyword(s):  
Hela Cells ◽  
In Vitro Cytotoxicity ◽  
Cytotoxicity Assessment

scholarly journals Phytochemical Profile, Antioxidant Activity, and Cytotoxicity Assessment of Tagetes erecta L. Flowers

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1201
Author(s):  
Ana Flavia Burlec ◽  
Łukasz Pecio ◽  
Solomiia Kozachok ◽  
Cornelia Mircea ◽  
Andreia Corciovă ◽  
...  
Keyword(s):  
Biological Activities ◽  
In Vitro Cytotoxicity ◽  
In Vitro Assays ◽  
Tagetes Erecta ◽  
Phytochemical Analysis ◽  
Total Extract ◽  
Tagetes Erecta L ◽  
Cytotoxicity Assessment

Tagetes erecta L. is a popular ornamental plant of the Asteraceae family, which is widely cultivated not only for its decorative use, but also for the extraction of lutein. Besides carotenoid representatives, which have been extensively studied, other important classes of secondary metabolites present in the plant, such as polyphenols, could exhibit important biological activities. The phytochemical analysis of a methanolic extract obtained from T. erecta inflorescences was achieved using liquid chromatography–mass spectrometry (LC-MS) techniques. The extract was further subjected to a multistep purification process, which allowed the separation of different fractions. The total extract and its fractions contain several polyphenolic compounds, such as hydroxybenzoic and hydroxycinnamic acid derivatives, flavonols (especially quercetagetin glycosides), and several aglycons (e.g., quercetin, patuletin). One of the fractions, containing mostly quercetagitrin, was subjected to two different antioxidant assays (metal chelating activity and lipoxygenase inhibition) and to in vitro cytotoxicity assessment. Generally, the biological assays showed promising results for the investigated fraction compared to the initial extract. Given the encouraging outcome of the in vitro assays, further purification and structural analysis of compounds from T. erecta extracts, as well as further in vivo investigations are justified.

Yangambin and Epi-yangambin Isomers: New Purification Method from Ocotea fasciculata and First Cytotoxic Aspects Focusing on In Vivo Safety

Planta Medica ◽  
2020 ◽  
Vol 86 (06) ◽  
pp. 415-424
Author(s):  
Júlia Martins ◽  
Joana Coelho ◽  
Maraine Catarina Tadini ◽  
Rebeca Oliveira de Souza ◽  
Sonia Aparecida Figueiredo ◽  
...  
Keyword(s):  
Cell Viability ◽  
In Vitro Cytotoxicity ◽  
In Vivo Studies ◽  
Albumin Concentration ◽  
Purification Method ◽  
Preparative Scale ◽  
Cytotoxicity Studies ◽  
First Time

Abstract Ocotea fasciculata presents yangambin (YAN) and its isomer epi-yangambin (EPI-YAN) as major lignans, which are employed as the plant markers for quality control purposes and as potential pharmacological compounds. However, a gap between the pure isomers and safety and efficacy protocols is faced by the scientific community. In this context, this work aimed to report (i) a new and advantageous purifying process in a semi-preparative scale for YAN and EPI-YAN isolation from Ocotea fasciculata, and (ii) an in vitro cytotoxicity study to estimate, for the first time, the LD50 values of the isolated epimers, as well as the influence of albumin concentration in cell culture medium. The best condition for epimers isolation was achieved in normal-phase liquid chromatography. The lignan fraction (LF), previously obtained from the plant ethanolic extract, was purified yielding 17% and 29% of YAN and EPI-YAN, respectively. The in vitro study demonstrated that YAN and EPI-YAN were safe, and only at the highest concentration studied, a decrease on cell viability was observed. The estimated LD50 value was higher than 1612 mg/kg for both epimers. The LF, on the other hand, demonstrated an estimated LD50 of 422 mg/kg. Lignan cytotoxicity studies also evidenced that the higher cell viability was related to the higher concentration of fetal bovine serum as a source of albumin in medium. This is the first time the LD50 and safety of the isolated epimers were estimated, opening up great perspectives of success in in vivo studies.

scholarly journals Preparation and Evaluation of the Effect of Acetyl Hexapeptide-8 Ampoule for Scalp Treatment

2021 ◽  
Vol 19 (3) ◽  
pp. 435-444
Author(s):  
Hae-Won Jo ◽  
Kyung-Hee Lee ◽  
Jeong-Hee Kim
Keyword(s):  
In Vitro Cytotoxicity ◽  
Integrin Subunit ◽  
Mrna Levels ◽  
Dependent Manner ◽  
Hacat Cells ◽  
Skin Reactions ◽  
In Vivo Experiments ◽  
Irritation Test

Purpose: The topical application of scalp-care cosmetics, infused with functional ingredients, can offer an optimal cosmetic approach to prevent problems associated with aging. In terms of the development of anti-aging cosmetics, we studied the use of acetyl hexapeptide-8 (AH-8) for improving elasticity of the scalp.Methods: Ampoules containing 3% and 5% concentrations of AH-8 as an active ingredient were prepared and their safety and efficacy were evaluated. HaCaT cells were used to evaluate the safety of AH-8 ampoules by measurement of in vitro cytotoxicity. In in vivo experiments, we tested the AH-8 ampoules by cumulative irritation test (CIT) on healthy adults, 20–50 years of age. Relative expressions of superoxide dismutase 2 (SOD2), forkhead box O1 (FOXO1), actinin alpha 1 (ACTN1), collagen type XVII alpha 1 chain (COL17A1), and integrin subunit beta 4 (ITGB4) were assessed using quantitative real-time PCR (Q-PCR).Results: AH-8 ampoules showed significant cytotoxicity to HaCaT cells in a dose-dependent manner. CIT assessment in 30 adults revealed no skin reactions to both 3% and 5% AH-8 ampoules. After treatment of HaCaT cells with the AH-8 ampoules, mRNA levels of SOD2 and FOXO1, which are directly implicated as antioxidant factors, were increased. Of the factors that improve elasticity, ACTN1 mRNA levels had the greatest increase when treated with the 5% AH-8 ampoules (1.75 µg/mL). Also, the AH-8 ampoules increased mRNA levels of COL17A1, and ITGB4 in HaCaT cells.Conclusions: In this study, we proved that 3% and 5% AH-8 ampoules are safe for use as a scalp-care cosmetic. AH-8 ampoule had efficacy in anti-aging and improving elasticity of the scalp. This comprehensive test showed that AH-8 can be developed as a cosmetic for anti-aging and improvement of scalp elasticity.

Mixed Micelles as Nano Polymer Therapeutics of Docetaxel: Increased In vitro Cytotoxicity and Decreased In vivo Toxicity

2018 ◽  
Vol 15 (4) ◽  
pp. 564-575 ◽  
Author(s):  
Arehalli S. Manjappa ◽  
Popat S. Kumbhar ◽  
Prajakta S. Khopade ◽  
Ajit B. Patil ◽  
John I. Disouza
Keyword(s):  
Mixed Micelles ◽  
In Vitro Cytotoxicity ◽  
Polymer Therapeutics ◽  
In Vivo Toxicity

Mannose Conjugated Starch Nanoparticles for Preferential Targeting of Liver Cancer

2020 ◽  
Vol 17 ◽  
Author(s):  
Akhlesh Kumar Jain ◽  
Hitesh Sahu ◽  
Keerti Mishra ◽  
Suresh Thareja
Keyword(s):  
Side Effects ◽  
Liver Cancer ◽  
Entrapment Efficiency ◽  
Xrd Analysis ◽  
In Vitro Cytotoxicity ◽  
Physical Interaction ◽  
Scanning Calorimetry ◽  
Starch Nanoparticles

Aim: To design D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for site specific delivery. Background: Liver cancer is the third leading cause of death in world and fifth most often diagnosed cancer is the major global threat to public health. Treatment of liver cancer with conventional method bears several side effects, thus to undertake these side effects as a formulation challenge, it is necessary to develop novel target specific drug delivery system for the effective and better localization of drug into the proximity of target with restricting the movement of drug in normal tissues. Objective: To optimize and characterize the developed D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for effective treatment of liver cancer. Materials and methods: 5-FU loaded JFSSNPs were prepared and optimized formulation had higher encapsulation efficiency were conjugated with D-Mannose. These formulations were characterized for size, morphology, zeta potential, X-Ray Diffraction, and Differential Scanning Calorimetry. Potential of NPs were studied using in vitro cytotoxicity assay, in vivo kinetic studies and bio-distribution studies. Result and discussion: 5-Fluorouracil loaded NPs had particle size between 336 to 802nm with drug entrapment efficiency was between 64.2 to 82.3%. In XRD analysis, 5-FU peak was diminished in the diffractogram, which could be attributed to the successful incorporation of drug in amorphous form. DSC study suggests there was no physical interaction between 5- FU and Polymer. NPs showed sustained in vitro 5-FU release up to 2 hours. In vivo, mannose conjugated NPs prolonged the plasma level of 5-FU and assist selective accumulation of 5-FU in the liver (vs other organs spleen, kidney, lungs and heart) compared to unconjugated one and plain drug. Conclusion: In vivo, bio-distribution and plasma profile studies resulted in significantly higher concentration of 5- Fluorouracil liver suggesting that these carriers are efficient, viable, and targeted carrier of 5-FU treatment of liver cancer.

Formulation, Characterization and In vitro Cytotoxicity of 5-Fluorouracil Loaded Polymeric Electrospun Nanofibers for the Treatment of Skin Cancer

2019 ◽  
Vol 13 (2) ◽  
pp. 114-128 ◽  
Author(s):  
Gayatri Patel ◽  
Bindu K.N. Yadav
Keyword(s):  
Skin Cancer ◽  
Basal Cell Carcinoma ◽  
Cell Viability ◽  
Cell Carcinoma ◽  
Basal Cell ◽  
Fiber Diameter ◽  
Electrospun Nanofibers ◽  
In Vitro Cytotoxicity ◽  
Fractional Factorial

Background: The purpose of this study was to formulate, characterize and conduct in vitro cytotoxicity of 5-fluorouracil loaded polymeric electrospun nanofibers for the treatment of skin cancer. The patents on electrospun nanofibers (US9393216B2), (US14146252), (WO2015003155A1) etc. helped in the selection of polymers and method for the preparation of nanofibers. Methods: In the present study, the fabrication of nanofibers was done using a blend of chitosan with polyvinyl alcohol and processed using the electrospinning technique. 5-fluorouracil with known chemotherapeutic potential in the treatment of skin cancer was used as a drug carrier. 24-1 fractional factorial screening design was employed to study the effect of independent variables like the concentration of the polymeric solution, applied voltage (kV), distance (cm), flow rate (ml / hr) on dependent variables like % entrapment efficiency and fiber diameter. Results: Scanning electron microscopy was used to characterize fiber diameter and morphology. Results showed that the fiber diameter of all batches was found in the range of 100-200 nm. The optimized batch results showed the fiber diameter of 162.7 nm with uniform fibers. The tensile strength obtained was 190±37 Mpa. Further in vitro and ex vivo drug release profile suggested a controlled release mechanism for an extended period of 24 hr. The 5-fluorouracil loaded electrospun nanofibers were found to decrease cell viability up to ≥50% over 24 hr, with the number of cells dropping by ~ 10% over 48 hr. As the cell viability was affected by the release of 5-fluorouracil, we believe that electrospun nanofibers are a promising drug delivery system for the treatment of Basal Cell Carcinoma (BCC) skin cancer. Conclusion: These results demonstrate the possibility of delivering 5-Fluorouracil loaded electrospun nanofiber to skin with enhanced encapsulation efficiency indicating the effectiveness of the formulation for the treatment of basal cell carcinoma type of skin cancer.

scholarly journals EXTH-46. ARTIFICIAL INTELLIGENCE-BASED IDENTIFICATION OF COMBINED VANDETANIB AND EVEROLIMUS IN THE TREATMENT OF ACVR1-MUTANT DIFFUSE INTRINSIC PONTINE GLIOMA

2020 ◽  
Vol 22 (Supplement_2) ◽  
pp. ii97-ii97
Author(s):  
Diana Carvalho ◽  
Peter Richardson ◽  
Nagore Gene Olaciregui ◽  
Reda Stankunaite ◽  
Cinzia Emilia Lavarino ◽  
...  
Keyword(s):  
Artificial Intelligence ◽  
Cell Viability ◽  
Xenograft Model ◽  
Diffuse Intrinsic Pontine Glioma ◽  
Pontine Glioma ◽  
Serine Threonine Kinase ◽  
Orthotopic Xenografts ◽  
Extended Survival

Abstract Somatic mutations in ACVR1, encoding the serine/threonine kinase ALK2 receptor, are found in a quarter of children with the currently incurable brain tumour diffuse intrinsic pontine glioma (DIPG). Treatment of ACVR1-mutant DIPG patient-derived models with multiple inhibitor chemotypes leads to a reduction in cell viability in vitro and extended survival in orthotopic xenografts in vivo, though there are currently no specific ACVR1 inhibitors licensed for DIPG. Using an Artificial Intelligence-based platform to search for approved compounds which could be used to treat ACVR1-mutant DIPG, the combination of vandetanib and everolimus was identified as a possible therapeutic approach. Vandetanib, an approved inhibitor of VEGFR/RET/EGFR, was found to target ACVR1 (Kd=150nM) and reduce DIPG cell viability in vitro, but has been trialed in DIPG patients with limited success, in part due to an inability to cross the blood-brain-barrier. In addition to mTOR, everolimus inhibits both ABCG2 (BCRP) and ABCB1 (P-gp) transporter, and was synergistic in DIPG cells when combined with vandetanib in vitro. This combination is well-tolerated in vivo, and significantly extended survival and reduced tumour burden in an orthotopic ACVR1-mutant patient-derived DIPG xenograft model. Based on these preclinical data, three patients with ACVR1-mutant DIPG were treated with vandetanib and everolimus. These cases may inform on the dosing and the toxicity profile of this combination for future clinical studies. This bench-to-bedside approach represents a rapidly translatable therapeutic strategy in children with ACVR1 mutant DIPG.

scholarly journals Impact of RARα and miR-138 on retinoblastoma etoposide resistance

Tumor Biology ◽  
2021 ◽  
Vol 43 (1) ◽  
pp. 11-26
Author(s):  
Maike Busch ◽  
Natalia Miroschnikov ◽  
Jaroslaw Thomas Dankert ◽  
Marc Wiesehöfer ◽  
Klaus Metz ◽  
...  
Keyword(s):  
Cell Viability ◽  
Cell Lines ◽  
Cancer Progression ◽  
Treated Patient ◽  
Luciferase Reporter ◽  
Luciferase Reporter Gene ◽  
Gene Assay ◽  
The Impact

BACKGROUND: Retinoblastoma (RB) is the most common childhood eye cancer. Chemotherapeutic drugs such as etoposide used in RB treatment often cause massive side effects and acquired drug resistances. Dysregulated genes and miRNAs have a large impact on cancer progression and development of chemotherapy resistances. OBJECTIVE: This study was designed to investigate the involvement of retinoic acid receptor alpha (RARα) in RB progression and chemoresistance as well as the impact of miR-138, a potential RARα regulating miRNA. METHODS: RARα and miR-138 expression in etoposide resistant RB cell lines and chemotherapy treated patient tumors compared to non-treated tumors was revealed by Real-Time PCR. Overexpression approaches were performed to analyze the effects of RARα on RB cell viability, apoptosis, proliferation and tumorigenesis. Besides, we addressed the effect of miR-138 overexpression on RB cell chemotherapy resistance. RESULTS: A binding between miR-138 and RARα was shown by dual luciferase reporter gene assay. The study presented revealed that RARα is downregulated in etoposide resistant RB cells, while miR-138 is endogenously upregulated. Opposing RARα and miR-138 expression levels were detectable in chemotherapy pre-treated compared to non-treated RB tumor specimen. Overexpression of RARα increases apoptosis levels and reduces tumor cell growth of aggressive etoposide resistant RB cells in vitro and in vivo. Overexpression of miR-138 in chemo-sensitive RB cell lines partly enhances cell viability after etoposide treatment. CONCLUSIONS: Our findings show that RARα acts as a tumor suppressor in retinoblastoma and is downregulated upon etoposide resistance in RB cells. Thus, RARα may contribute to the development and progression of RB chemo-resistance.

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