In Silico Validation, Fabrication and Evaluation of Nano-Liposomes of Bistorta amplexicaulis Extract for Improved Anticancer Activity Against Hepatoma Cell Line (HepG2)

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.

Cite this article as:

Batool Salma , Asad Javaid Muhammad, Arshad Muhammad , Ahmed Warda , Sohail Farhan Muhammad , Abbasi Wajid Sumra, Ahmad Sajjad , Saleem Shah Zaib Rahman*, Ahmed Sheeraz Muhammad *, In Silico Validation, Fabrication and Evaluation of Nano-Liposomes of Bistorta amplexicaulis Extract for Improved Anticancer Activity Against Hepatoma Cell Line (HepG2), Current Drug Delivery 2021; 18 (7) . https://dx.doi.org/10.2174/1567201818666210316113640