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Published on: September 22, 2019
Dihydropyridine Derivatives as Cell Growth Modulators In Vitro
Imanta Bruvere1, Egils Bisenieks1, Janis Poikans1
1Latvian Institute of Organic Synthesis, 21 Aizkraukles Str., Riga LV-1006, Latvia.
Abstract:
The effects of eleven 1,4-dihydropyridine derivatives (DHPs) used alone or together with prooxidant anticancer drug doxorubicin were examined on two cancer (HOS, HeLa) and two nonmalignant cell lines (HMEC, L929). Their effects on the cell growth (3H-thymidine incorporation) were compared with their antiradical activities (DPPH assay), using well-known DHP antioxidant diludine as a reference. Thus, tested DHPs belong to three groups: (1) antioxidant diludine; (2) derivatives with pyridinium moieties at position 4 of the 1,4-DHP ring; (3) DHPs containing cationic methylene onium (pyridinium, trialkylammonium) moieties at positions 2 and 6 of the 1,4-DHP ring. Diludine and DHPs of group 3 exerted antiradical activities, unlike compounds of group 2. However, novel DHPs had cell type and concentration dependent effects on 3H-thymidine incorporation, while diludine did not. Hence, IB-32 (group 2) suppressed the growth of HOS and HeLa, enhancing growth of L929 cells, while K-2-11 (group 3) enhanced growth of every cell line tested, even in the presence of doxorubicin. Therefore, growth regulating and antiradical activity principles of novel DHPs should be further studied to find if DHPs of group 2 could selectively suppress cancer growth and if those of group 3 promote wound healing.
Insights
Novel 1,4-dihydropyridine derivatives (DHPs) show varied effects on cancer and nonmalignant cells. Some DHPs exhibit antioxidant and growth-suppressing properties, suggesting potential for cancer therapy or wound healing applications.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Cancer Biology
Background:
- 1,4-dihydropyridine derivatives (DHPs) are investigated for their biological activities.
- Understanding DHP effects on cancer and normal cells is crucial for therapeutic development.
- Antioxidant and cytotoxic properties of DHPs are key areas of interest.
Purpose of the Study:
- To evaluate the effects of eleven novel 1,4-dihydropyridine derivatives (DHPs) on cancer and nonmalignant cell lines.
- To compare the antiradical activities of these DHPs with their effects on cell growth.
- To explore the potential of specific DHP groups for selective cancer growth suppression or wound healing.
Main Methods:
- Tested eleven 1,4-dihydropyridine derivatives (DHPs) on HOS, HeLa (cancer), and HMEC, L929 (nonmalignant) cell lines.
- Assessed cell growth inhibition using 3H-thymidine incorporation.
- Measured antiradical activity via DPPH assay, using diludine as a reference antioxidant.
Main Results:
- DHPs were categorized into three groups based on their chemical structure.
- Diludine and Group 3 DHPs demonstrated antiradical activity, unlike Group 2 DHPs.
- Novel DHPs exhibited cell type and concentration-dependent effects on cell proliferation; IB-32 (Group 2) suppressed cancer cell growth, while K-2-11 (Group 3) enhanced growth in all cell lines.
Conclusions:
- Novel DHPs display diverse biological activities, including antioxidant and differential growth modulation.
- Group 2 DHPs warrant further investigation for selective anticancer efficacy.
- Group 3 DHPs show potential for applications in wound healing due to their growth-promoting effects.
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