scholarly journals Perillaldehyde 1,2-epoxide Loaded SLN-Tailored mAb: Production, Physicochemical Characterization and In Vitro Cytotoxicity Profile in MCF-7 Cell Lines

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 161 ◽  
Author(s):  
Eliana B. Souto ◽  
Selma B. Souto ◽  
Aleksandra Zielinska ◽  
Alessandra Durazzo ◽  
Massimo Lucarini ◽  
...  

We have developed a new cationic solid lipid nanoparticle (SLN) formulation, composed of Compritol ATO 888, poloxamer 188 and cetyltrimethylammonium bromide (CTAB), to load perillaldehyde 1,2-epoxide, and surface-tailored with a monoclonal antibody for site-specific targeting of human epithelial growth receptor 2 (HER2). Perillaldehyde 1,2-epoxide-loaded cationic SLN (cPa-SLN), with a mean particle size (z-Ave) of 275.31 ± 4.78 nm and polydispersity index (PI) of 0.303 ± 0.081, were produced by high shear homogenization. An encapsulation efficiency of cPa-SLN above 80% was achieved. The release of perillaldehyde 1,2-epoxide from cationic SLN followed the Korsemeyer–Peppas kinetic model, which is typically seen in nanoparticle formulations. The lipid peroxidation of cPa-SLN was assessed by the capacity to produce thiobarbituric acid-reactive substances, while the antioxidant activity was determined by the capacity to scavenge the stable radical DPPH. The surface functionalization of cPa-SLN with the antibody was done via streptavidin-biotin interaction, monitoring z-Ave, PI and ZP of the obtained assembly (cPa-SLN-SAb), as well as its stability in phosphate buffer. The effect of plain cationic SLN (c-SLN, monoterpene free), cPa-SLN and cPa-SLN-SAb onto the MCF-7 cell lines was evaluated in a concentration range from 0.01 to 0.1 mg/mL, confirming that streptavidin adsorption onto cPa-SLN-SAb improved the cell viability in comparison to the cationic cPa-SLN.

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.


2021 ◽  
Vol 11 (19) ◽  
pp. 9066
Author(s):  
Ahmed A. H. Abdellatif ◽  
Mashari A. Aldhafeeri ◽  
Waleed H. Alharbi ◽  
Fahad H. Alharbi ◽  
Waleed Almutiri ◽  
...  

The aim of this study was to improve the solubility of etoposide–ethylcellulose (ET–ETO) microparticles using the freeze-drying technique. Ethylcellulose (EC) microparticles loaded with etoposide (ETO) were prepared with different drug–polymer molar ratios of 1:1, 1:3, 1:6, and 1:20 by the solvent evaporation method. The size of the prepared microparticles was 0.088 µm. The results showed that the amount of ETO encapsulated into the microparticles was 387.3, 365.0, 350.0, and 250 µg/50 mg microparticles for microparticles with drug–polymer ratios of 1:1, 1:3, 1:6, and 1:20, respectively. The FT-IR spectra showed no chemical interaction between ETO and the polymer in the solid state. The results obtained from the dissolution experiment showed that the freeze-dried microparticles were stable in 0.1 N HCl (gastric pH) for 2 h. At pH 7.4, the ETO release was 60 to 70% within the first 15 min and approximately 100% within 30 min. Results from the application of different dissolution models showed that the equations that best fit the dissolution data for the ET–ETO microparticles at pH 7.4 were the Higuchi and Peppas model equations. The in vitro cytotoxicity assay of free ETO and freeze-dried microspheres prepared in this study with a drug–polymer ratio of 1:1 was performed in two mammalian cancer cell lines, MCF-7 (for bone cancer of the mammary organ) and Caco-2 (for mammalian epithelial colorectal adenocarcinoma). The results showed that the half-maximal inhibitory concentrations (IC50 values) for ETO and freeze-dried ET–ETO microparticles were 18.6 µM and 27.1 µM, respectively. In conclusion, freeze-dried ET–ETO is a promising formulation for developing a fast-dissolving form of ETO with a significant antiproliferative activity against the tested cell lines used in this study. It is a promising formulation for local duodenal area targeting.


2020 ◽  
Vol 9 (5) ◽  
pp. 367-370
Author(s):  
BN Satish ◽  
◽  
Mallya Suma V ◽  
Vishwanatha ◽  
◽  
...  

About: Habenaria longicorniculata J. Graham are tuberous orchid, the tubers utilized by flok healers in cancer managemnet, as a rejuvenator. A study has been planned to evaluate In-vitro cytotoxicity of tuber extract against selected cell lines. Materials and Methods: H. longicorniculata J.Graham identified, uprooted during their flowering time. Tuber extract of this plant used for its In-vitro cytotoxicity against selected cell lines of Human Breast cancer (MCF 7), Human Liver carcinoma (HepG2), and Human cervix adenocarcinoma (HeLa) cells as per standard protocol. Results: Tuber Extract exhibited a CTC50 value of >1000 on MCF 7, HepG2 and HeLa cell lines. The results from the MTT assay indicate that 72hr extract incubation with the combined extracts is toxic to the cells and the level of damage is concentration dependent.


2016 ◽  
Vol 13 (3) ◽  
pp. 1633-1637 ◽  
Author(s):  
Arlene Thomas ◽  
Niraja Ranadive ◽  
Harisha Nayak ◽  
Sneha Surendran ◽  
Madhavan Nampoothiri ◽  
...  

Author(s):  
Lalitha Simon

  Objective: The objective of this study was to synthesize 7-amino-2-styrylchromone derivatives and evaluate their in vitro cytotoxic and antioxidant potential.Methods: 7-amino-2-styrylchromones were synthesized from 7-amino-2-methylchromone by condensing it with various substituted aromatic aldehydes. The cytotoxicity of the synthesized molecules was assessed against two cell lines, MCF-7 and HCT-116 by 3-(4,5-dimethyl thiazol-2-yl)-2,5- diphenyl tetrazolium bromide assay. Cell cycle analysis of the most potent molecule ASC-7 was carried out. The antioxidant studies were conducted by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide methods.Result: (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) with inhibitory concentration 50% (IC50) 56.0 μM was found to be the most potent molecule against MCF-7. ASC-7 induced G0/G1 phase arrest of MCF-7. Furthermore, (E)-7-amino-2-(3,4-methylenedioxystyryl)- 4H-chromen-4-one(ASC-7) showed good DPPH scavenging activity (IC50 54.6 μM). However, none of the tested compounds exhibited nitric oxide scavenging property.Conclusion: This study reports the synthesis of 7-amino-2-styrylchromones. Some of the synthesized compounds showed moderate cytotoxicity against the tested cell lines MCF-7 and HCT-116. (E)-7-amino-2-(3,4-methylenedioxystyryl)-4H-chromen-4-one (ASC-7) was found to be the best cytotoxic and antioxidant agent.


Planta Medica ◽  
2017 ◽  
Vol 84 (02) ◽  
pp. 129-134 ◽  
Author(s):  
Lien Do ◽  
Thammarat Aree ◽  
Pongpun Siripong ◽  
Nga Vo ◽  
Tuyet Nguyen ◽  
...  

AbstractFive new flavones possessing a fully substituted A-ring with C-6 and C-8 methyl groups, bougainvinones I – M (1–5), along with three known congeners, 2′-hydroxydemethoxymatteucinol (6), 5,7,3′,4′-tetrahydroxy-3-methoxy-6,8-dimethylflavone (7) and 5,7,4′-trihydroxy-3-methoxy-6,8-dimethylflavone (8), were isolated from the EtOAc extract of the stem bark of Bougainvillea spectabilis. Their structures were established by means of spectroscopic data (ultraviolet, infrared, high-resolution electrospray ionization mass spectrometry, and one-dimensional and two-dimensional nuclear magnetic resonance) and single-crystal X-ray crystallographic analysis. The in vitro cytotoxicity of all isolated compounds against five cancer cell lines (KB, HeLa S-3, MCF-7, HT-29, and HepG2) was evaluated. Compound 5 showed promising cytotoxic activity against the KB and HeLa S-3 cell lines, with IC50 values of 7.44 and 6.68 µM. The other compounds exhibited moderate cytotoxicity against the KB cell line.


Author(s):  
Asri Peni Wulandari ◽  
R. R. Indry Noviarin Examinati ◽  
Madihah . ◽  
Desi Harneti Putri Huspa ◽  
Poniah Andayaningsih ◽  
...  

Objective: To investigate the in vitro cytotoxicity effect of the crude ethyl acetate extract of Cladosporium sp. on MCF-7, HeLa, and DU-145 cell lines.Methods: In vitro cytotoxicity was evaluated by tetrazolium reduction assay. The percentage of cell inhibition was analyzed using probit analysis to obtain 50% inhibitory concentration (IC50). Morphological alteration of the cell lines after exposure with extract was observed under an inverted microscope.Results: The ethyl acetate extract of the metabolite performed an anticancer activity for cancer cell line MCF-7, HeLa, and DU-145 with IC50 respectively 8.46 μg/ml; 9.87 μg/ml; and 98.03 μg/ml. The extract shows greater the anticancer activity and has strong antiproliferative on MCF-7 and HeLa cell line than DU-145. Confirmation morphological were observed under the inverted microscope showed a morphological change in cancer cells when incubated with the extract.Conclusion: From the performed assay, the crude extract of Cladosporium sp. exhibit cytotoxic activity against MCF-7, HeLA, and DU-145.


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