Design, preparation and studies regarding cytotoxic properties of glycyrrhetinic acid derivatives

Qing Xuan Zheng; Rui Wang; Yan Xu; Chang Xin He; Cai Yun Zhao; Zhi Fang Wang; Rui Zhang; Wim Dehaen; Hui Jing Li; Qi Yong Huai

doi:10.1248/bpb.b19-00615

Design, preparation and studies regarding cytotoxic properties of glycyrrhetinic acid derivatives

Qing Xuan Zheng
, Rui Wang
, Yan Xu
, Chang Xin He
, Cai Yun Zhao
, Zhi Fang Wang
, Rui Zhang
, Wim Dehaen
, Hui Jing Li
, Qi Yong Huai^*

^*Corresponding author for this work

Shandong University
KU Leuven
School of Marine Science and Technology, Harbin Institute of Technology Weihai

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44% of MDA-MB-231 cells at 5, 10, and 20µM, respectively.

Original language	English
Pages (from-to)	102-109
Number of pages	8
Journal	Biological and Pharmaceutical Bulletin
Volume	43
Issue number	1
DOIs	https://doi.org/10.1248/bpb.b19-00615
State	Published - 2020
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Apoptosis
Cytotoxicity
Glycyrrhetinic acid
MDA-MB-231

Access to Document

10.1248/bpb.b19-00615

Cite this

@article{439e4fd210ad45e98aab56d7ced3325b,

title = "Design, preparation and studies regarding cytotoxic properties of glycyrrhetinic acid derivatives",

abstract = "Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44\% of MDA-MB-231 cells at 5, 10, and 20µM, respectively.",

keywords = "Apoptosis, Cytotoxicity, Glycyrrhetinic acid, MDA-MB-231",

author = "Zheng, \{Qing Xuan\} and Rui Wang and Yan Xu and He, \{Chang Xin\} and Zhao, \{Cai Yun\} and Wang, \{Zhi Fang\} and Rui Zhang and Wim Dehaen and Li, \{Hui Jing\} and Huai, \{Qi Yong\}",

note = "Publisher Copyright: {\textcopyright} 2020 The Pharmaceutical Society of Japan.",

year = "2020",

doi = "10.1248/bpb.b19-00615",

language = "英语",

volume = "43",

pages = "102--109",

journal = "Biological and Pharmaceutical Bulletin",

issn = "0918-6158",

publisher = "Pharmaceutical Society of Japan",

number = "1",

}

TY - JOUR

T1 - Design, preparation and studies regarding cytotoxic properties of glycyrrhetinic acid derivatives

AU - Zheng, Qing Xuan

AU - Wang, Rui

AU - Xu, Yan

AU - He, Chang Xin

AU - Zhao, Cai Yun

AU - Wang, Zhi Fang

AU - Zhang, Rui

AU - Dehaen, Wim

AU - Li, Hui Jing

AU - Huai, Qi Yong

PY - 2020

Y1 - 2020

N2 - Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44% of MDA-MB-231 cells at 5, 10, and 20µM, respectively.

AB - Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44% of MDA-MB-231 cells at 5, 10, and 20µM, respectively.

KW - Apoptosis

KW - Cytotoxicity

KW - Glycyrrhetinic acid

KW - MDA-MB-231

UR - https://www.scopus.com/pages/publications/85077480218

U2 - 10.1248/bpb.b19-00615

DO - 10.1248/bpb.b19-00615

M3 - 文章

C2 - 31902913

AN - SCOPUS:85077480218

SN - 0918-6158

VL - 43

SP - 102

EP - 109

JO - Biological and Pharmaceutical Bulletin

JF - Biological and Pharmaceutical Bulletin

IS - 1

ER -

Design, preparation and studies regarding cytotoxic properties of glycyrrhetinic acid derivatives

Abstract

UN SDGs

Keywords

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