scholarly journals Co-Crystals of Resveratrol and Polydatin with L-Proline: Crystal Structures, Dissolution Properties, and In Vitro Cytotoxicities

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5722
Author(s):  
Yijie Lou ◽  
Kaxi Yu ◽  
Xiajun Wu ◽  
Zhaojun Wang ◽  
Yusheng Cui ◽  
...  

Resveratrol (RSV) and polydatin (PD) have been widely used to treat several chronic diseases, such as atherosclerosis, pulmonary fibrosis, and diabetes, among several others. However, their low solubility hinders their further applications. In this work, we show that the solubility of PD can be boosted via its co-crystallization with L-proline (L-Pro). Two different phases of co-crystals, namely the RSV-L-Pro (RSV:L-Pro = 1:2) and PD-L-Pro (PD:L-Pro = 1: 3), have been prepared and characterized. As compared to the pristine RSV and PD, the solubility and dissolution rates of PD-L-Pro in water (pH 7.0) exhibited a 15.8% increase, whereas those of RSV-L-Pro exhibited a 13.8% decrease. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay of pristine RSV, PD, RSV-L-Pro, and PD-L-Pro against lung cancer cell line A549 and human embryonic kidney cell line HEK-293 indicated that both compounds showed obvious cytotoxicity against A549, but significantly reduced cytotoxicity against HEK-293, with PD/PD-L-Pro further exhibiting better biological safety than that of RSV/RSV-L-Pro. This work demonstrated that the readily available and biocompatible L-Pro can be a promising adjuvant to optimize the physical and chemical properties of RSV and PD to improve their pharmacokinetics.

Author(s):  
O. Pochapinskyi ◽  
◽  
G. Lavrenchuk ◽  
N. Atamaniuk ◽  
A. Chernyshov ◽  
...  

Objective: to investigate the structural and morpho-functional changes in test systems of malignant (A-549 cell line) and normal (fibroblasts of the 6th passage) human cells during incubation with gadolinium-containing photon-capture agent «Dotavist» and photosensitizer «Fotolon». Methods. The passaged (continuously interweaved) cell culture technique on normal human fibroblasts and malignant human cells; cytological, biophysical, statistical methods. Results. The cytotoxic properties of «Dotavist» gadolinium-containing photon-capturing agent and «Photolon» photosensitizer in a wide range of concentrations (5, 10, 25, 50, 100 and 200 μl/ml) were studied by the morphofunctional characteristics (growth kinetics, proliferative and mitotic activity, presence of atypical cells) in the in vitro test systems of malignant (non-small cell lung cancer cell line A-549) and normal (6th passage fibroblasts) human cells. It was found that the cytotoxic properties of «Dotavist» in test systems of malignant and normal cells are expressed under its administration in high concentrations (100 and 200 μl/ml). During incubation with «Photolon» photosensitizer the cytotoxic effect on malignant cells was determined at the lowest concentrations (5 and 10 μl/ml). Photosensitizer administration in the increasing concentrations has lead to genotoxic effects. Cytotoxic effect of photosensitizer on the normal human fibroblasts was evident in the 5-200 μl/ml concentration range. There was a moderate decrease in mitotic activity along with increasing concentration. Genotoxic properties of photosensitizer were evident at 25 μl/ml concentration and above. Conclusion. Study results of the effectiveness of neutron-capture and photon-capture technologies by the sensitivity assay in the in vitro test systems of human malignant cells (non-small cell lung cancer cell line A-549) and normal cells (transplantable human fibroblast culture, the 6th passage) to the gadolinium-containing photon-capture «Dotavist» agent and «Photolon» photosensitizer in different concentrations provide the basis for pre-clinical stage of evaluating the effectiveness of medications used in binary technologies. Key words: culture of human malignant cells, culture of human fibroblasts, neutron-capture agent, photon-capture agent, photosensitizer, proliferation, mitotic index.


2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Quang Trung Nguyen ◽  
Phuong Nam Pham Thi ◽  
Nguyen Van Tuyen

Six Fe(III) complexes bearing unsymmetrical salen-type ligands derived from 2-hydroxynaphthaldehyde and substituted salicylaldehydes were synthesized by coordinating the unsymmetrical salen-type ligands with FeCl3.6H2O. The synthetic complexes were characterized by electrospray ionization mass spectra (ESI-MS), effective magnetic moments (μeff), and infrared (IR) and ultraviolet-visible (UV-Vis) spectra. The spectroscopic data are in good agreement with the suggested molecular formulae of the complexes. Their cyclic voltammetric studies in acetonitrile solutions showed that the Fe(III)/Fe(II) reduction processes are electrochemically irreversible. The in vitro cytotoxicity of the obtained complexes was screened on human cancer cell lines KB (a subline of Hela tumor cell line) and HepG2 (a human liver cancer cell line) and a normal human cell line HEK-293 (Human Embryonic Kidney cell line). The results showed that the synthetic Fe(III) complexes are highly cytotoxic and quite selective. The synthetic complexes bearing unsymmetrical salen-type ligands with different substituted groups in the salicyl ring indicate different cytotoxicity.


2020 ◽  
Vol 12 (1) ◽  
pp. 14-19 ◽  
Author(s):  
Qotrunnada Fithrotunnisa ◽  
Ade Arsianti ◽  
Gerry Kurniawan ◽  
Fona Qorina ◽  
Nadzila Anindya Tejaputri ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document