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扁柏酚通过抑制肿瘤细胞增殖和诱导凋亡来抑制结直肠癌生长。

Obovatol inhibits colorectal cancer growth by inhibiting tumor cell proliferation and inducing apoptosis.

作者信息

Lee Su-Kyung, Kim Hye-Nan, Kang Yeong-Rim, Lee Chang Woo, Kim Hwan-Mook, Han Dong Cho, Shin Jongheon, Bae Kihwan, Kwon Byoung-Mog

机构信息

Korea Research Institute of Bioscience and Biotechnology, University of Science and Technology, 52 Uendong, Yuseonggu, Daejon 305-600, Republic of Korea.

出版信息

Bioorg Med Chem. 2008 Sep 15;16(18):8397-402. doi: 10.1016/j.bmc.2008.08.033. Epub 2008 Aug 19.

Abstract

Neolignans such as obovatol, honokiol, and magnolol have been previously reported to show various biological activities including anti-inflammation and antitumor effects. This is the first demonstration on the in vivo antitumor effect of obovatol on human colorectal carcinoma SW620 cells. Nude mice were implanted with SW620 cells and fed with vehicle or 5mg/kg/d dose of obovatol for 20 days. Obovatol inhibited tumor growth that accounted for 50% decrease in tumor volume and 44.6% decrease in tumor weight at the end of the experiment without any adverse health effect. In nude mice bearing SW620-incubated tumor, obovatol exhibited more potent antitumor activity than honolkiol. In addition, DNA flow cytometric analysis shows that obovatol progresses to apoptosis as detected by flow cytometry after double staining with annexin V and propidium iodide. Thus, we suggest that obovatol is a potent inducer of cell apoptosis in SW620 cells, and a potent antitumor agent.

摘要

先前已有报道称,诸如奥巴托醇、厚朴酚和和厚朴酚等新木脂素具有多种生物活性,包括抗炎和抗肿瘤作用。这是首次证明奥巴托醇对人结肠直肠癌SW620细胞具有体内抗肿瘤作用。将SW620细胞接种到裸鼠体内,并给其喂食溶媒或5mg/kg/d剂量的奥巴托醇,持续20天。奥巴托醇抑制了肿瘤生长,在实验结束时,肿瘤体积减少了50%,肿瘤重量减少了44.6%,且对健康没有任何不良影响。在携带SW620培养肿瘤的裸鼠中,奥巴托醇表现出比厚朴酚更强的抗肿瘤活性。此外,DNA流式细胞术分析表明,在用膜联蛋白V和碘化丙啶双重染色后,通过流式细胞术检测发现奥巴托醇可促使细胞凋亡。因此,我们认为奥巴托醇是SW620细胞中一种有效的细胞凋亡诱导剂,也是一种有效的抗肿瘤药物。

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