Antioxidant, Anti-Inflammatory and Anticancer Activities of the Methanolic Extract of Thottea siliquosa: An In Vitro and In Silico Study.
Anti-Inflammatory Agents
/ pharmacology
Antioxidants
/ chemistry
Apoptosis
/ drug effects
Aristolochiaceae
Cell Line, Tumor
Cell Survival
/ drug effects
Computer Simulation
Cyclooxygenase 2
/ metabolism
Drug Screening Assays, Antitumor
ErbB Receptors
/ metabolism
Female
Flavonoids
/ chemistry
HeLa Cells
Humans
In Vitro Techniques
Lipoxygenase
/ metabolism
MCF-7 Cells
Molecular Docking Simulation
Phenols
/ chemistry
Plant Extracts
/ pharmacology
Receptors, Vascular Endothelial Growth Factor
/ metabolism
Anticancer activity
COX2.
EGFR
Thottea siliquosa
VEGFR
anti-inflammatory activity
antioxidant activity
polyphenols
Journal
Recent patents on anti-cancer drug discovery
ISSN: 2212-3970
Titre abrégé: Recent Pat Anticancer Drug Discov
Pays: United Arab Emirates
ID NLM: 101266081
Informations de publication
Date de publication:
2021
2021
Historique:
received:
21
09
2020
revised:
02
02
2021
accepted:
03
02
2021
pubmed:
3
4
2021
medline:
10
2
2022
entrez:
2
4
2021
Statut:
ppublish
Résumé
Oxidative stress and inflammation are the predominant cause of chronic diseases, including multiple forms of cancers. Prevention of oxidative stress and inflammation is considered to be a target for preventing these disorders due to their significant roles in various degenerative diseases. Various natural products and plant extracts prevent the process of free radical- induced damages. The present study evaluated the biological properties of Thottea siliquosa, belonging to the family Aristolochiaceae, which is a traditionally used Ayurvedic plant. Antioxidant assays carried out were DPPH, FRAP, hydrogen peroxide scavenging, and hemolysis inhibition assay; nitric oxide and lipoxygenase inhibition assays were used for anti-inflammatory studies. Anticancer activity was evaluated using human endometrial and breast cancer cells by MTT assay. Bioactive compounds present in T. siliquosa were identified by LCMS and each was docked with various cancer targets, including EGFR, VEGFR, GST, COX2, and Lipooxygenase. The results of the present study showed antioxidant properties of the methanolic crude extract of T. siliquosa as DPPH radical scavenging (110.40 ± 4.5 μg/mL), FRAP capacity (41.1 ± 6.2), and peroxide scavenging (233.4 ± 14.2 μg/mL). Besides, anti-inflammatory properties were also evident in terms of nitric oxide radical scavenging (28.76± 3.9 μg/mL) and lipoxygenase inhibition (39.2 ± 3.2 μg/mL) assays. In silico analysis confirmed the inhibitory potential of the bioactive compounds of T. siliquosa against cancer drug targets such as EGFR, VEGFR, and inflammatory enzymes cyclooxygenase as well as lipooxygenase. Further, the anticancer activity of the extract has been identified against human endometrial and breast cancer cells. The possible mechanism of anticancer action of the extract is mediated through the apoptosis induction mechanism acting through increased caspase and APAF-1 expressions. The study thus concludes that T. siliquosa showed significant antioxidant, anti-inflammatory and anticancer properties. Further studies together with a bioassay-guided fractionation may identify possible bioactive compounds.
Sections du résumé
BACKGROUND
BACKGROUND
Oxidative stress and inflammation are the predominant cause of chronic diseases, including multiple forms of cancers. Prevention of oxidative stress and inflammation is considered to be a target for preventing these disorders due to their significant roles in various degenerative diseases. Various natural products and plant extracts prevent the process of free radical- induced damages.
OBJECTIVE
OBJECTIVE
The present study evaluated the biological properties of Thottea siliquosa, belonging to the family Aristolochiaceae, which is a traditionally used Ayurvedic plant.
METHODS
METHODS
Antioxidant assays carried out were DPPH, FRAP, hydrogen peroxide scavenging, and hemolysis inhibition assay; nitric oxide and lipoxygenase inhibition assays were used for anti-inflammatory studies. Anticancer activity was evaluated using human endometrial and breast cancer cells by MTT assay. Bioactive compounds present in T. siliquosa were identified by LCMS and each was docked with various cancer targets, including EGFR, VEGFR, GST, COX2, and Lipooxygenase.
RESULTS
RESULTS
The results of the present study showed antioxidant properties of the methanolic crude extract of T. siliquosa as DPPH radical scavenging (110.40 ± 4.5 μg/mL), FRAP capacity (41.1 ± 6.2), and peroxide scavenging (233.4 ± 14.2 μg/mL). Besides, anti-inflammatory properties were also evident in terms of nitric oxide radical scavenging (28.76± 3.9 μg/mL) and lipoxygenase inhibition (39.2 ± 3.2 μg/mL) assays. In silico analysis confirmed the inhibitory potential of the bioactive compounds of T. siliquosa against cancer drug targets such as EGFR, VEGFR, and inflammatory enzymes cyclooxygenase as well as lipooxygenase. Further, the anticancer activity of the extract has been identified against human endometrial and breast cancer cells. The possible mechanism of anticancer action of the extract is mediated through the apoptosis induction mechanism acting through increased caspase and APAF-1 expressions.
CONCLUSION
CONCLUSIONS
The study thus concludes that T. siliquosa showed significant antioxidant, anti-inflammatory and anticancer properties. Further studies together with a bioassay-guided fractionation may identify possible bioactive compounds.
Identifiants
pubmed: 33797378
pii: PRA-EPUB-115143
doi: 10.2174/1574892816666210401143750
doi:
Substances chimiques
Anti-Inflammatory Agents
0
Antioxidants
0
Flavonoids
0
Phenols
0
Plant Extracts
0
Lipoxygenase
EC 1.13.11.12
Cyclooxygenase 2
EC 1.14.99.1
ErbB Receptors
EC 2.7.10.1
Receptors, Vascular Endothelial Growth Factor
EC 2.7.10.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
436-444Informations de copyright
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