Title:In-vitro Antioxidant, In-vitro and In-silico Ovarian Anticancer Activity (Ovarian Cancer Cells-PA1) and Phytochemical Analysis of Cissus quadrangularis L. Ethanolic Extract
Volume: 27
Issue: 10
Author(s): Xuejing Zhao, Yinghui Wang, Zhaohui Zhang, Periyannan Velu and Runping Liu*
Affiliation:
- Department of Obstetrics and Gynecology, Hanzhong People’s Hospital, 723000, Hanzhong, Shaanxi, China
Keywords:
C. quadrangularis L, ethanolic extract, phytochemical analysis, ovarian cancer PA1 cells, anticancer activity, antioxidant activity.
Abstract:
Background: Cissus quadrangularis is a valuable natural source of traditional medicines.
Objective: An in vitro investigation was performed to determine whether the ethanolic extract
from the whole portions of C. quadrangularis had anticancer and free radical scavenging activities
against ovarian cancer cells-PA1. C. quadrangularis is a herb collected from rural areas in
Andhra Pradesh, India.
Materials and Methods: C. quadrangularis was air-dried and crushed, and the powder and ethanol
(0.5 kg) were used in a Soxhlet device for continuous extraction. Phytochemical analysis of
the extracts was performed using a standard procedure. The antioxidant activity of the ethanolic
extract of C. quadrangularis was evaluated using DPPH. An in vitro anticancer study used an
ethanolic extract against the PA1 cell line. Apoptosis of ovarian cancer cells was studied using
DAPI and carboxy-H2DCFDA staining. From LC-MS analysis, quercetin-3-O-alpha-Lrhamnopyranoside
and erucic acid were docked with the threonine tyrosine kinase (TTK) enzyme
using auto docking.
Results: The ethanolic extract of C. quadrangularis demonstrated significant dose-dependent antioxidant
activity compared to ascorbic acid. The ethanolic extract of C. quadrangularis was found to
have high anticancer activity against ovarian cancer cell lines (PA1), with an IC50 value of 482.057 ±
113.857 μg/ml. DAPI and carboxy-H2DCFDA staining confirmed that C. quadrangularis ethanolic
extract induced apoptosis in ovarian cancer cells (p < .001). Molecular docking studies helped identify
the binding affinities between the protein and ligand complexes, such as Quercetin-3-O-alpha-Lrhamnopyranoside
binding sites of target proteins 5N7V (MET602, GLN672) and erucic acid 5N7V
(GLY354). Quercetin-3-O-alpha-L-rhamnopyranoside was reported to bind with 5N7V by hydrogen
bonding at MET602 and GLN672 amino acids with 2.02, 2.99 Å bonding length distance and binding
affinity of -7.9 kcal/mol. Erucic acid was reported to bind with 5N7V by hydrogen bonding at
GLY354 amino acid with 3.18, 2.93 Å bonding length (Å) distance and binding affinity of -4.3
kcal/mol. The current analysis showed that the ethanolic extracts of C. quadrangularis L. exhibited
antioxidant and anticancer properties against ovarian PA1 cells.
Conclusion: The experimental results confirmed that C. quadrangularis L. is a promising, safe
chemotherapeutic plant for ovarian cancer PA1 cells. The docking results demonstrated that
Quercetin-3-O-alpha-L-rhamnopyranoside strongly binds threonine tyrosine kinase at the
MET602 and GLN672 positions. This study showed that the C. quadrangularis ethanolic extract
has Quercetin-3-O-alpha-L-rhamnopyranoside, which can be used as an anticancer agent.