Joseph Litty, Srinivasan K K
Department of Pharmaceutical Sciences, Centre for Professional and Advanced studies, Cheruvandoor Campus, Ettumanoor PO, Kottayam, 686 631, Kerala, India.
Department of Chemistry, Shri Madhwa Vadiraja Institute of Technology and Management, Bantakal, Udupi, 574 115, Karnataka, India.
Toxicol Rep. 2019 Oct 31;6:1198-1205. doi: 10.1016/j.toxrep.2019.10.015. eCollection 2019.
Triacontanoic ester of 5"-hydroxyjustisolin, a lignan from D. Don, possesses antitumor activity. However, the molecular mechanism underlying this is not yet clearly understood. The present study showed significant inhibition in cell viability on HeLa cell line and induced minor toxicity in normal cells. This compound induced mitotic arrest at G0/G1 phase followed by apoptosis in human cervical cancer cells and was accompanied by the upregulation of BAX, caspase-3 and downregulation of Bcl-2. Taken together, these data reveal that the title compound acts through multiple cellular/molecular pathways, which strongly suggest the role of pro and antiapoptotic Bcl-2 family proteins. Triacontanoic ester of 5''-hydroxyjustisolin may be a potential agent for the cervical cancer treatment.
5”-羟基异落叶松脂素的三十烷酸酯是一种从D. Don中提取的木脂素,具有抗肿瘤活性。然而,其潜在的分子机制尚未完全明确。本研究表明,该化合物对HeLa细胞系的细胞活力有显著抑制作用,且对正常细胞产生轻微毒性。该化合物可诱导人宫颈癌细胞在G0/G1期发生有丝分裂停滞,随后引发凋亡,同时伴随着BAX、caspase-3的上调以及Bcl-2的下调。综上所述,这些数据表明该标题化合物通过多种细胞/分子途径发挥作用,这强烈提示了促凋亡和抗凋亡Bcl-2家族蛋白的作用。5”-羟基异落叶松脂素的三十烷酸酯可能是一种治疗宫颈癌的潜在药物。