Antiproliferative Activity of Cissus quadrangularis L. Extract Against Human Cervical Cancer Cells: In Vitro and In Silico Analysis

Abstract

Background: Ce rvical cancer is the second leading cause of cancer in women, which necessitates safe and potential therapeutic agents. Objective: This study was designed to investigate the antiproliferative effect of ethanolic extract of Cissus quadrangularis L. (CQ) against human cervical adenocarcinoma HeLa cell line and in silico analysis of selected active agents against apoptosis executioner enzyme caspase-3. Methods: Cell viability was analyzed in HeLa cells at different concentrations (25-300 μg/ml) of CQ extract. Reactive oxygen species (ROS) generation, cellular apoptosis, cell cycle analysis and caspases-3 activation were evaluated. In silico structure-based virtual screening analysis was carried out using AutoDock Vina and iGEMDOCK. Results: Cell viability of HeLa cells was reduced significantly (p ˂ 0.05) in a dose-dependent manner, however, CQ extract showed non-toxic to normal kidney epithelial NRK-52E cells. CQ extract induced the intracellular ROS level, nuclear condensation and reduced the mitochondrial membrane potential (MMP) with the induction of annexin V-FITC positive cells. CQ extract arrested cells in G0/G1 and G2/M checkpoints and activated caspase-3 activity significantly in HeLa cells. The molecular docking study showed a strong binding affinity of CQ phytocomponents against the caspase-3 (PDB ID: 1GFW) protein of human apoptosis. PASS analyses of selected active components using Lipinski’s Rule of five showed promising results. Further, drug-likeness and toxicity assessment using OSIRIS Data Warrior V5.2.1 software exhibited the feasibility of phytocomponents as drug candidates with no predicted toxicity. Conclusion: This study suggested that active constituents in CQ extract can be considered as potential chemotherapeutic candidates in the management of cervical cancer.

Assessment of Anticancer Activity and Gene Expression in P53 Gene of Cissus Quadrangularis L. Stem Mediated Silver Nanoparticles

“…This is confirmed by the IC50 values of 56.74 µg/ml in the AgNPs, which is considered moderate in cytotoxicity by the National Cancer Institute. Siddiqui et al (2021) also established the anticancer potential of the ethanolic extract of Cissus quadrangularis against the human cervical HeLa cell lines.…”

In vitro anti-inflammatory, anti-diabetic and antioxidant potential of Cissus quadrangularis along with its orexigenic activity in Drosophila melanogaster

“…This plant is rich in flavonoids, triterpenoids, stilbene derivatives and phytosterols with antioxidant potential, but more studies are needed to clarify pharmacological mechanisms of action. Bioactive components of C. quadrangularis have been used for cancer, obesity, antioxidant, anti-inflammatory disorders (Chatree et al, 2021;Siddiqui et al, 2021;Sundaran et al, 2020;Zaki et al, 2020;Stohs and Ray, 2013;Srisook et al, 2011). The plant also has hypoglycemic and anti-glycation activity (Chaudhari et al, 2013;Lekshmi and Mini, 2013).…”