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Cytotoxic and Antioxidant Activity of a Set of Hetero Bicylic Methylthiadiazole Hydrazones: A Structure-Activity Study.

Kodisundaram P, Duraikannu A, Balasankar T, Sundarao Ambure P, Roy K - Int J Mol Cell Med (2015)

Bottom Line: Compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects.The free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis.Docking studies revealed interactions of compound 10 with p38α MAP kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

View Article: PubMed Central - PubMed

Affiliation: Department of Chemistry, Annamalai University, Annamalai Nagar-608002, Tamilnadu, India.

ABSTRACT
The current study highlights the in vitro antioxidant and antitumor activity of the previously-synthesized hydrazone derivatives against various free radicals and human cancer cell lines, respectively. The anticancer efficacies of the compound were tested by measuring cytotoxicity in cancer cell lines HeLa, A549, and non-cancerous NL20 cells. Compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects. The free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis. The results from cytotoxicity and cell migration assay showed that the substitution of electron-withdrawing fluoro, chloro and bromo functional groups induced a significant (P< 0.001) loss of cell viability and inhibited the invasive potential of the human cancer cells. Additionally, these compounds showed significantly (P< 0.05) a less toxicity toward non-cancerous NL20 cells. Docking studies revealed interactions of compound 10 with p38α MAP kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

No MeSH data available.


Related in: MedlinePlus

Antiproliferative effects of synthetic compounds 10, 12 and 13 at 8µM in HeLa A549 and NL20 cells by crystal blue staining method. * Significantly different from untreated control cells (P<0.05). ** Significantly different from untreated control cells (P<0.01). *** Significantly different from untreated control cells (P<0.001).   Significantly different from untreated NL20 cells (P<0.05).    Significantly different from untreated control cells (P<0.001).
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Figure 3: Antiproliferative effects of synthetic compounds 10, 12 and 13 at 8µM in HeLa A549 and NL20 cells by crystal blue staining method. * Significantly different from untreated control cells (P<0.05). ** Significantly different from untreated control cells (P<0.01). *** Significantly different from untreated control cells (P<0.001).   Significantly different from untreated NL20 cells (P<0.05).    Significantly different from untreated control cells (P<0.001).

Mentions: Of the several synthetic compounds, compo-unds containing electron withdrawing functional groups (-F, -Cl and -Br) that were demonstrated to exert potent cytotoxic effects were used for testing their antiproliferative effects by crystal violet blue staining assay in comparison (Figure 3). Compo-unds 10 and 12 showed significantly (P< 0.001) greater inhibitory effect on HeLa and A549 cells compared to untreated control cells, whereas compound 13 displayed significantly (P< 0.01) higher cytotoxicity against tested cancer cells compared to untreated cells. The cytotoxicity of 10, 12 and 13 was also tested in normal lung epithelial cells (NL-20) near to the corresponding IC50 values. Accordingly, 10 and 13 displayed significant (P< 0.05) cytotoxic effect on cell viability in NL20 cells as compared to cancer cell lines (Figure 3) and untreated cells. However, no significant difference was observed in NL20 cells treated with compound 12.


Cytotoxic and Antioxidant Activity of a Set of Hetero Bicylic Methylthiadiazole Hydrazones: A Structure-Activity Study.

Kodisundaram P, Duraikannu A, Balasankar T, Sundarao Ambure P, Roy K - Int J Mol Cell Med (2015)

Antiproliferative effects of synthetic compounds 10, 12 and 13 at 8µM in HeLa A549 and NL20 cells by crystal blue staining method. * Significantly different from untreated control cells (P<0.05). ** Significantly different from untreated control cells (P<0.01). *** Significantly different from untreated control cells (P<0.001).   Significantly different from untreated NL20 cells (P<0.05).    Significantly different from untreated control cells (P<0.001).
© Copyright Policy
Related In: Results  -  Collection

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Show All Figures
getmorefigures.php?uid=PMC4499575&req=5

Figure 3: Antiproliferative effects of synthetic compounds 10, 12 and 13 at 8µM in HeLa A549 and NL20 cells by crystal blue staining method. * Significantly different from untreated control cells (P<0.05). ** Significantly different from untreated control cells (P<0.01). *** Significantly different from untreated control cells (P<0.001).   Significantly different from untreated NL20 cells (P<0.05).    Significantly different from untreated control cells (P<0.001).
Mentions: Of the several synthetic compounds, compo-unds containing electron withdrawing functional groups (-F, -Cl and -Br) that were demonstrated to exert potent cytotoxic effects were used for testing their antiproliferative effects by crystal violet blue staining assay in comparison (Figure 3). Compo-unds 10 and 12 showed significantly (P< 0.001) greater inhibitory effect on HeLa and A549 cells compared to untreated control cells, whereas compound 13 displayed significantly (P< 0.01) higher cytotoxicity against tested cancer cells compared to untreated cells. The cytotoxicity of 10, 12 and 13 was also tested in normal lung epithelial cells (NL-20) near to the corresponding IC50 values. Accordingly, 10 and 13 displayed significant (P< 0.05) cytotoxic effect on cell viability in NL20 cells as compared to cancer cell lines (Figure 3) and untreated cells. However, no significant difference was observed in NL20 cells treated with compound 12.

Bottom Line: Compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects.The free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis.Docking studies revealed interactions of compound 10 with p38α MAP kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

View Article: PubMed Central - PubMed

Affiliation: Department of Chemistry, Annamalai University, Annamalai Nagar-608002, Tamilnadu, India.

ABSTRACT
The current study highlights the in vitro antioxidant and antitumor activity of the previously-synthesized hydrazone derivatives against various free radicals and human cancer cell lines, respectively. The anticancer efficacies of the compound were tested by measuring cytotoxicity in cancer cell lines HeLa, A549, and non-cancerous NL20 cells. Compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects. The free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis. The results from cytotoxicity and cell migration assay showed that the substitution of electron-withdrawing fluoro, chloro and bromo functional groups induced a significant (P< 0.001) loss of cell viability and inhibited the invasive potential of the human cancer cells. Additionally, these compounds showed significantly (P< 0.05) a less toxicity toward non-cancerous NL20 cells. Docking studies revealed interactions of compound 10 with p38α MAP kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

No MeSH data available.


Related in: MedlinePlus