Abstract
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: The present study evaluated the biological properties of Thottea siliquosa, belonging to the family Aristolochiaceae, which is a traditionally used Ayurvedic plant.
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: 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: 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.
Keywords: Anticancer activity, anti-inflammatory activity, antioxidant activity, polyphenols, Thottea siliquosa, EGFR, VEGFR, COX2.
Recent Patents on Anti-Cancer Drug Discovery
Title:Antioxidant, Anti-Inflammatory and Anticancer Activities of the Methanolic Extract of Thottea siliquosa: An In Vitro and In Silico Study
Volume: 16 Issue: 3
Author(s): Amrutha Koottasseri, Amal Babu, Anna Augustin, Joice Tom Job and Arunaksharan Narayanankutty*
Affiliation:
- Division of Cell and Molecular Biology PG & Research Department of Zoology, St. Joseph’s College (Autonomous), Devagiri, Calicut, Kerala,India
Keywords: Anticancer activity, anti-inflammatory activity, antioxidant activity, polyphenols, Thottea siliquosa, EGFR, VEGFR, COX2.
Abstract:
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: The present study evaluated the biological properties of Thottea siliquosa, belonging to the family Aristolochiaceae, which is a traditionally used Ayurvedic plant.
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: 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: 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.
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Koottasseri Amrutha , Babu Amal , Augustin Anna , Job Tom Joice and Narayanankutty Arunaksharan *, Antioxidant, Anti-Inflammatory and Anticancer Activities of the Methanolic Extract of Thottea siliquosa: An In Vitro and In Silico Study, Recent Patents on Anti-Cancer Drug Discovery 2021; 16 (3) . https://dx.doi.org/10.2174/1574892816666210401143750
DOI https://dx.doi.org/10.2174/1574892816666210401143750 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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