Loading of capsaicin-in-cyclodextrin inclusion complexes into PEGylated liposomes and the inhibitory effect on IL-8 production by MDA-MB-231 and A549 cancer cell lines

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Hiba Abdelnabi ◽  
Walhan Alshaer ◽  
Hanan Azzam ◽  
Dana Alqudah ◽  
Ali Al-Samydai ◽  
...  

Abstract Capsaicin (CAP) is an active component in Capsicum annuum L. known to have anti inflammatory and anticancer activity. CAP is highly lipophilic and suffers low bioavailability. Therefore, developing delivery systems that enhance solubility and bioavailability can provide more promising therapeutic applications for CAP. In the current work, CAP was complexed with β-cyclodextrin (βCD) to form capsaicin-in-β-cyclodextrin (CAP-in-βCD) inclusion complexes. Then, the CAP-in-βCD inclusion complexes were characterized and loaded into PEGylated liposomes using the thin-film hydration extrusion method. The size, charge, and polydispersity index (PDI) of the PEGylated liposomes were characterized. The levels of IL-8 production were quantified after treatment using array beads. The results of this work showed that the successful formation of inclusion complexes at 1:5 M ratio of CAP to βCD respectively. PEGylated liposomes loaded with βCD/CAP inclusion complexes (CAP-in-βCD-in-liposomes) have a hydrodynamic diameter of (181 ± 36) nm, zeta potential of (−2.63 ± 4.00) mV, encapsulation efficiency (EE) of (38.65 ± 3.70)%, drug loading (DL) of (1.65 ± 0.16)%, and a stable release profile. Both free CAP and liposomal CAP showed a significant reduction in the IL-8 production by the MDA-MB-231 and A549 cancer cell lines after treatment. In conclusion, a liposomal-based drug delivery system for CAP was achieved.

2020 ◽  
Vol 21 (2) ◽  
pp. 439-447
Author(s):  
Samaneh Mansouri-Fard ◽  
Mojgan Ghaedi ◽  
Mohammad-Reza Shokri ◽  
Tannaz Bahadori ◽  
Jalal Khoshnoodi ◽  
...  

Author(s):  
ANANTHALAKSHMI R ◽  
XAVIER RAJARATHINAM SR ◽  
Mohamed Sadiq A ◽  
MOHAMED SADIQ A

Objective: The objective of the study was to access the anticancer activity of the biosynthesized ZnO nanoparticles against Huh7 liver cancer cell lines. Methods: The study was carried in vitro using Huh7 cell lines. The ZnO nanoparticles (ZnO NPs) were synthesized using Luffa acutangula peel extract and subjected to characterization by X-ray powder diffraction and transmission electron microscopy. The Huh7 cell lines were treated with ZnO NPs and done 3-(4, 5-dimethylthiazol- 2-yl)-2, 5-diphenyltetrazolium bromide assay. For live and dead assay, the cell lines treated with ZnO NPs were subjected to acridine orange/ethidium (AO/ET) bromide assay. Results: The ZnO NPs synthesized show spherical structure with 10–20 nm size. The 50% of Huh7 proliferation were inhibited at the concentration (IC50) of 40 μg/ml. The AO/ET assay shows compact nucleus and fine cytoplasmic morphology in control cells and apoptotic stage in treated cells Conclusion: This study suggests that ZnO NPs can be prepared in environment-friendly method using aqueous extract of L. acutangula and can be used in cancer treatment effectively.


2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984581
Author(s):  
Thana Juckmeta ◽  
Weerachai Pipatrattanaseree ◽  
Wuttichai Jaidee ◽  
Bhanuz Dechayont ◽  
Jitpisute Chunthorng-Orn ◽  
...  

A Thai traditional remedy called Benchalokawichian (BLW) consists of 5 plant species, Ficus racemosa, Capparis micracantha, Clerodendrum petasites, Harrisonia perforata, and Tiliacora triandra. It has long been used in Thai traditional medicine to reduce fever in respiratory tract infection, but there is no report on either cytotoxicity against cancer cell lines of the respiratory tract system or anti-inflammatory effect. Thus, the objectives of this research were to investigate the cytotoxic activity of the ethanolic and water extracts of BLW, its single plant ingredients and its isolated compounds against 5 cancer cell lines of the respiratory tract, by SRB assay. Anti-inflammatory activity of all extracts and compounds was also tested by using lipopolysaccharide-induced nitric oxide (NO) in RAW 264.7 cells. The main compounds were isolated by high-performance liquid chromatography and compared with BLW and plant ingredients. A major compound of BLW and H. perforata ethanolic extracts is perforatic acid, which inhibited the growth of 2 lung cancer cell lines, A549 and H226, with IC50 values of 6.7 and 13.2 µg/mL. The ethanolic extract of BLW and T. triandra showed cytotoxic activity against all cancer cell lines with IC50 values in the range of 10.1 to 45.2 µg/mL. In contrast, all EtOH extracts showed moderate anti-inflammatory activity, but the water extract had no inhibitory effect on either activity. Pectolinarigenin and O-methyllaloptaeroxyrin, 2 minor compounds, exhibited NO inhibitory effect with IC50 values of 7.1 and 7.9 µg/mL, respectively, whereas perforatic acid was inactive (>50 µg/mL). Moreover, pectolinarigenin showed high cytotoxic activity against all cancer cell lines of the respiratory system with IC50 values in the range of 1.9 to 9.1 µg/mL. As a result, these 2 minor compounds can be used as markers for quality control of BLW for anti-inflammatory activity. Perforatic acid and pectolinarigenin are of interest for further study on their cytotoxic mechanism. Remarkably, T. triandra, one of the plant components of BLW, is possibly the source of the active cytotoxic compounds.


2008 ◽  
Vol 61 (12) ◽  
pp. 975 ◽  
Author(s):  
Guo-Liang Lu ◽  
Cheuk-Lam Ho ◽  
Qiwei Wang ◽  
Wai-Yeung Wong ◽  
Chung-Hin Chui ◽  
...  

Three new transition metal complexes of 4,5-diazafluoren-9-one, [(DAFO)PdCl2], [(DAFO)PtCl2], and [(DAFO)ZnCl2], were prepared in good yields by the reactions between appropriate metal chloride precursors and 4,5-diazafluoren-9-one under ambient conditions. The structures of these metal complexes were established by spectroscopic (Fourier-transform IR, NMR, and fast-atom bombardment mass spectrometry) techniques. The possible biological activity of these compounds on three human cancer cell lines including Hep3B, MDAMB-231, and SKHep-1 was investigated. The results obtained showed that both zinc- and platinum-containing compounds exhibit a similar growth inhibitory effect on these three cancer cell lines when compared with the prototypical cis-platin. In contrast, the corresponding palladium congener is virtually biologically inactive in these trials.


2019 ◽  
Author(s):  
Macarena Siri ◽  
Maria Julieta Fernandez Ruocco ◽  
Estefanía Achilli ◽  
Malvina Pizzuto ◽  
Juan F. Delgado ◽  
...  

AbstractA γ–irradiated bovine albumin serum based nanoparticle was characterised structurally, and functionally. The nanoparticle was characterised by A.F.M, D.L.S, zeta potential, T.E.M., gel-electrophoresis, spectroscopy (UV-Vis, Fluorescence, FT-IR, and CD). Its stability was studied under adverse experimental conditions: pH values, chaotropic agents, and ionic strength and stability studies against time were mainly carried out by fluorescence spectroscopy following the changes in the tryptophan environment in the nanoparticle. Its function was studied by the interaction of the NP with the hydrophobic drug Emodin was studied. The binding and kinetic properties of the obtained complex were tested by biophysical methods as well as its toxicity in tumour cells.According to its biophysics, the nanoparticle is a spherical nanosized vehicle with a hydrodynamic diameter of 70 nm. Data obtained describe the nanoparticle alone as nontoxic for cancer cell lines. When combined with Emodin, the bioconjugate proved to be more active on MCF-7 and PC-3 cancer cell lines than the nanoparticle alone. No haemolytic activity was found when tested against ex vivo red blood cells. The stability of the albumin nanoparticle is based on a competition between short-range attraction forces and long-range repulsion forces. The nanoparticle showed similar behaviour as albumin against pH while improving its stability in urea and tween 80. It was stable up to 15 days and presented no protein degradation in solutions up to 2 M salt concentration. Significantly, the albumin aggregate preserves the main activity-function of albumin and improved characteristics as an excellent carrier of molecules.Graphical Abstract


2021 ◽  
Vol 22 (19) ◽  
pp. 10491
Author(s):  
Mohammed S. Abdel-Maksoud ◽  
Ahmed A. B. Mohamed ◽  
Rasha M. Hassan ◽  
Mohamed A. Abdelgawad ◽  
Garri Chilingaryan ◽  
...  

A new series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives 12a–n was designed and synthesized according to the structure of well-established V600EBRAF inhibitors. The terminal sulfonamide moiety was linked to the pyrimidine ring via either ethylamine or propylamine bridge. The designed series was tested at fixed concentration (1 µM) against V600EBRAF, finding that 12e, 12i and 12l exhibited the strongest inhibitory activity among all target compounds and 12l had the lowest IC50 of 0.49 µM. They were further screened on NCI 60 cancer cell lines to reveal that 12e showed the most significant growth inhibition against multiple cancer cell lines. Therefore, cell cycle analysis of 12e was conducted to investigate the effect on cell cycle progression. Finally, virtual docking studies was performed to gain insights for the plausible binding modes of vemurafenib, 12i, 12e and 12l.


Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
ED Spyrelli ◽  
C Virgiliou ◽  
AE Koletti ◽  
H Gika ◽  
G Mossialos ◽  
...  

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