2. Academic Validation
  3. Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity

Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity

  • Bioorg Med Chem Lett. 2016 Aug 1;26(15):3464-7. doi: 10.1016/j.bmcl.2016.06.043.
Chao Yang 1,  Hui Chen 2,  Shihai Lu 1,  Meng Zhang 1,  Wei Tian 1,  Mingping Wang 3,  Ling Zhang 1,  Yunlong Song 1,  Aijun Shen 4,  Youjun Zhou 5,  Ju Zhu 6,  Canhui Zheng 7
Affiliations

Affiliations

  • 1 School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
  • 2 Changhai Hospital, Second Military Medical University, Shanghai 200433, China.
  • 3 School of Pharmacy, Second Military Medical University, Shanghai 200433, China; Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
  • 4 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • 5 School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: zhouyoujun@smmu.edu.cn.
  • 6 School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: zhuju@smmu.edu.cn.
  • 7 School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: canhuizheng@smmu.edu.cn.
PMID: 27353532 DOI: 10.1016/j.bmcl.2016.06.043
Abstract

The luteolin from Flos Chrysanthemi was found to directly bind to the Bcl-2 protein and inhibit the tumor cell growth in our previous study. However, it has been shown to possess wide and week biological activities. In this study, a series of derivatives of luteolin were designed and synthesized, and their tumor cell growth inhibitory activities were evaluated against human leukemia cell line HL-60. The results showed that compounds 1B-2, 2A-3, and 2B-5, with hydrophobic substituted benzyl groups introduced to B ring and hydrogen or methyl introduced to 7-OH group of luteolin, exhibited the strongest inhibitory activity with the IC50 lower than 10μM, which were significantly more potent than luteolin. The studies presented here offer a good example for modifications of Flavones to improve their tumor cell growth inhibitory activities.

Keywords

Anti-tumor; Bcl-2 protein; Flos Chrysanthemi; Luteolin; Structural modification.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z