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Allylthiopyridazine derivatives were synthesized and evaluated for anti-proliferative activities in the previous study. In this study, selected two allylthiopyridazine derivatives (compound I, 3-heptylamino-6-allylthiopyridazine and compound II, 3-dipentylamino-6-allylthiopyridazine) were assessed for cytotoxicity and chronic proliferation in human colon carcinoma RKO cells. Two derivatives dose-dependently inhibited cell viability and proliferation. To elucidate the anticancer mechanism of two derivatives, we investigated the expression level of apoptosis-related proteins in RKO cells. Compound I induced the activation of JNK and expression of p53 and p21. On the other hand, compound II showed no change of p53 level. Interestingly, compound II inhibited the nuclear translocation of NF-${\kappa}B$. This result suggested that compound II suppressed cell proliferation. These different mechanisms of these compounds might have occurred through different steric conformation.
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참고문헌 (18)
참고문헌 신청
Wallock-Richards, D / 2014 / Garlic revisited: Antimicrobial activity of allicin-containing garilic extracts against Burkholderia cepacia complex / PLoS ONE 9:e112726
Tao, M / 2014 / Study on the inhibitory effect of allicin on human gastric cancer cell line SGC-7901 and its mechanism / Afr. J. Tradit. Complement Altern. Med 11:176
Xu, L / 2014 / Role of JNK activation and mitochondrial bax translocation in allicin-induced apoptosis in human ovarian cancer SKOV3 cells. Evid. Based Complement / Alternat. Med
Feldberg, R. S / 1988 / In vitro mechanism of inhibition of bacterial cell growth by allicin / Antimicrob. Agents Chemother 32:1763
Borlinghaus, J / 2014 / Allicin: Chemistry and biological properties / Molecules 19:12591
Tao, M / 2014 / Study on the inhibitory effect of allicin on human gastric cancer cell line SGC-7901 and its mechanism / Afr. J. Tradit. Complement Altern. Med 11:176
Xu, L / 2014 / Role of JNK activation and mitochondrial bax translocation in allicin-induced apoptosis in human ovarian cancer SKOV3 cells. Evid. Based Complement / Alternat. Med
Feldberg, R. S / 1988 / In vitro mechanism of inhibition of bacterial cell growth by allicin / Antimicrob. Agents Chemother 32:1763
Borlinghaus, J / 2014 / Allicin: Chemistry and biological properties / Molecules 19:12591
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