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Published on: February 9, 2021
Synthesis, In Vitro Anticancer, Anti-Inflammatory and DNA Binding Activity of Thiazolidinedione Derivatives
Nadine Uwabagira1, Balladka K Sarojini1,2, Ashwini Prabhu3
1Division of Biochemistry, Department of Studies in Chemistry, Mangalore University, Karnataka, India
Background:
Cancer is the second leading cause of mortality worldwide. Despite several advances made in the treatment strategies, the cure for cancer remains still a challenge. Currently used treatment modalities pose several side effects and remain ineffective in the later stages. Thiazolidinediones (TZDs) have been shown to possess anti-cancer activity in several in vitro models.
Objectives:
The objective of this study was to assess the effect of novel synthesized thiazolidinedione derivatives on three selected cancer cell lines viz., human breast adenocarcinoma cell line (MCF-7), lung adenocarcinoma (A549) and colorectal carcinoma (HT29). This study also aimed to evaluate the anti-inflammatory and DNA binding activity of the synthesized derivatives.
Methods:
The synthesized thiazolidinedione derivatives were screened for their in vitro anti-cancer activity on the human breast adenocarcinoma cell line (MCF-7), lung adenocarcinoma (A549) and colorectal carcinoma (HT29) using the Methyl Thaizolyl Tetrazolium (MTT) Assay. They were also evaluated for in vitro antiinflammatory activity using albumin denaturation method, DNA binding activity and hemocompatibility.
Results:
Compounds 5a, 5b, 5d, 6c and 6d showed IC50 of 30.19, 41.56, 65.97, 60.16 and 50.41μM respectively on breast adenocarcinoma (MCF-7), IC50 of 49.75, 51.42, 65.43, 61.94 and 56.80μM on lung adenocarcinoma (A549) and 38.11, 45.58, 71.24, 53.15 and 51.25μM on colorectal carcinoma (HT29). In the hemolysis assay, compounds 5a and 5b were found to be nontoxic and nonhemolytic to human erythrocytes. Five compounds possessed significant anticancer and anti-inflammatory activity. Three of them are Mannich bases, whereas the remaining two are aryl acyl derivatives.
Conclusion:
The in vitro results (anticancer and anti-inflammatory) showed that the 4-chloro anilinomethyl substitution at third position and thiophenoethenyl at the fifth position of thiozolidinedione (5a) emerged as the most effective derivative on all the tested cancer cell lines. A higher DNA binding affinity of the test compounds was also found.
Insights
Novel thiazolidinedione derivatives show potent anticancer and anti-inflammatory effects against breast, lung, and colorectal cancer cell lines. Compound 5a demonstrated the highest efficacy and good hemocompatibility, indicating therapeutic potential.
Area of Science:
- Medicinal Chemistry
- Oncology
- Pharmacology
Background:
- Cancer remains a leading cause of mortality worldwide, with current treatments facing limitations and significant side effects.
- Thiazolidinediones (TZDs) are a class of compounds recognized for their potential anticancer properties in preliminary studies.
Purpose of the Study:
- To synthesize and evaluate novel thiazolidinedione derivatives for their in vitro anticancer activity against human breast (MCF-7), lung (A549), and colorectal (HT29) cancer cell lines.
- To assess the anti-inflammatory and DNA binding capabilities of these synthesized derivatives.
Main Methods:
- Synthesized thiazolidinedione derivatives were screened for in vitro anticancer activity using the MTT assay on MCF-7, A549, and HT29 cell lines.
- Anti-inflammatory activity was assessed via albumin denaturation, and DNA binding affinity and hemocompatibility were also evaluated.
Main Results:
- Several derivatives exhibited significant anticancer activity, with compounds 5a, 5b, 5d, 6c, and 6d showing varying IC50 values across the tested cancer cell lines.
- Compounds 5a and 5b demonstrated non-toxic and non-hemolytic profiles in hemolysis assays.
- Five compounds displayed notable anticancer and anti-inflammatory effects, including Mannich bases and aryl acyl derivatives.
Conclusions:
- The thiazolidinedione derivative 5a, featuring specific substitutions, was the most effective against all tested cancer cell lines.
- The synthesized compounds also exhibited promising anti-inflammatory activity and significant DNA binding affinity.
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