Title:In Silico Validation, Fabrication and Evaluation of Nano-Liposomes of Bistorta amplexicaulis Extract for Improved Anticancer Activity Against Hepatoma Cell Line (HepG2)
Volume: 18
Issue: 7
Author(s): Salma Batool, Muhammad Javaid Asad, Muhammad Arshad, Warda Ahmed, Muhammad Farhan Sohail, Sumra Wajid Abbasi, Sajjad Ahmad, Rahman Shah Zaib Saleem*Muhammad Sheeraz Ahmed*
Affiliation:
- Department of Chemistry and Chemical Engineering, SBA School of Science and Engineering (SBASSE), Lahore University of Management Sciences (LUMS), Lahore, 54792,Pakistan
- Department of Biochemistry, Pir Mehr Ali Shah University of Arid Agriculture, Rawalpindi, 46300,Pakistan
Keywords:
Bistorta amplexicaulis, anticancer activity, HepG2, MCF-7, liposomes, HUVEC.
Abstract:
Background: Bistorta amplexicaulis of the genus Polygonum (Polygonaceae) has been
reported for its antioxidant and anticancer activities. However, the low cellular uptake of the compounds
in its extract limits its therapeutic application.
Objectives: The present study aimed at developing a nanoliposomal carrier system for B. amplexicaulis
extracts for improved cellular uptake, thus resulting in enhanced anticancer activity.
Methods: Ultra Pressure Liquid Chromatography (UPLC) was used to identify major compounds
in the plant extract. Nanoliposomes (NLs) were prepared by employing a thin-film rehydration
method using DPPC, PEG2000DSPE and cholesterol, followed by characterization through several
parameters. In vitro screening was performed against breast cancer cell line (MCF-7) and Hepatocellular
carcinoma cell line (HepG-2) using MTT-assay. Raw extract and nanoliposomes were tested
on Human Umbilical Vein Endothelial Cells (HUVEC). Moreover, molecular docking was performed
to validate the data obtained through wet lab.
Results: The UHPLC method identified gallic acid, caffeic acid, chlorogenic acid and catechin as
the major compounds in the extract. The NLs with a size ranging between 140-155 nm, zeta potential
-16.9 to -19.8 mV and good polydispersity index of < 0.1 were prepared, with a high encapsulation
efficiency of 81%. The MTT assay showed significantly (p > 0.05) high uptake and cytotoxicity
of NLs as compared to the plant extract. Moreover, reduced toxicity against HUVEC cells was
observed as compared to the extract. Also, the docking of identified compounds suggested a favorable
interaction with the SH2 domain of both STAT3 and STAT5.
Conclusion: Overall, the results suggest NLs as a potential platform that could be developed for
the improved intracellular delivery of plant extract, thus increasing the therapeutic outcomes.