Design and synthesis of new anticancer glycyrrhetinic acids and oleanolic acids

Rui Wang; Qing-Xuan Zheng; Wei Wang; Ling Feng; Hui-Jing Li; Qi-Yong Huai

doi:10.1248/bpb.b17-00016

Design and synthesis of new anticancer glycyrrhetinic acids and oleanolic acids

Rui Wang, Qing-Xuan Zheng, Wei Wang, Ling Feng, Hui-Jing Li^*, Qi-Yong Huai^*

^*Corresponding author for this work

Research output: Journal Publications and Reviews › RGC 21 - Publication in refereed journal › peer-review

10 Citations (Scopus)

Abstract

A series of new glycyrrhetinic acids and oleanolic acids has been designed and synthesized based on the principles of combinatorial chemical synthesis. Their anticancer activities were further studied by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method with hepatocellular carcinoma (Hep-G2), breast cancer (MCF-7) cell lines and a normal hepatic cell (LO2). Cytotoxicity tests (in vitro) indicated that compound 6a showed the highest cytotoxicity with the lowest IC₅₀ values of 23.34 μM on Hep-G2 cells, 12.23 μM on MCF-7 cells, and 44.47 μM on LO2, which would widen the structural diversity of these anticancer targets and confirm the perspectives of further investigations.

Original language	English
Pages (from-to)	703-710
Journal	Biological and Pharmaceutical Bulletin
Volume	40
Issue number	5
DOIs	https://doi.org/10.1248/bpb.b17-00016
Publication status	Published - Feb 2017

Research Keywords

Anticancer
Glycyrrhetinic acid
Oleanolic acid
Synthesis

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title = "Design and synthesis of new anticancer glycyrrhetinic acids and oleanolic acids",

abstract = "A series of new glycyrrhetinic acids and oleanolic acids has been designed and synthesized based on the principles of combinatorial chemical synthesis. Their anticancer activities were further studied by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method with hepatocellular carcinoma (Hep-G2), breast cancer (MCF-7) cell lines and a normal hepatic cell (LO2). Cytotoxicity tests (in vitro) indicated that compound 6a showed the highest cytotoxicity with the lowest IC50 values of 23.34 μM on Hep-G2 cells, 12.23 μM on MCF-7 cells, and 44.47 μM on LO2, which would widen the structural diversity of these anticancer targets and confirm the perspectives of further investigations.",

keywords = "Anticancer, Glycyrrhetinic acid, Oleanolic acid, Synthesis",

author = "Rui Wang and Qing-Xuan Zheng and Wei Wang and Ling Feng and Hui-Jing Li and Qi-Yong Huai",

year = "2017",

month = feb,

doi = "10.1248/bpb.b17-00016",

language = "English",

volume = "40",

pages = "703--710",

journal = "Biological and Pharmaceutical Bulletin",

issn = "0918-6158",

publisher = "Pharmaceutical Society of Japan",

number = "5",

}

TY - JOUR

T1 - Design and synthesis of new anticancer glycyrrhetinic acids and oleanolic acids

AU - Wang, Rui

AU - Zheng, Qing-Xuan

AU - Wang, Wei

AU - Feng, Ling

AU - Li, Hui-Jing

AU - Huai, Qi-Yong

PY - 2017/2

Y1 - 2017/2

N2 - A series of new glycyrrhetinic acids and oleanolic acids has been designed and synthesized based on the principles of combinatorial chemical synthesis. Their anticancer activities were further studied by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method with hepatocellular carcinoma (Hep-G2), breast cancer (MCF-7) cell lines and a normal hepatic cell (LO2). Cytotoxicity tests (in vitro) indicated that compound 6a showed the highest cytotoxicity with the lowest IC50 values of 23.34 μM on Hep-G2 cells, 12.23 μM on MCF-7 cells, and 44.47 μM on LO2, which would widen the structural diversity of these anticancer targets and confirm the perspectives of further investigations.

AB - A series of new glycyrrhetinic acids and oleanolic acids has been designed and synthesized based on the principles of combinatorial chemical synthesis. Their anticancer activities were further studied by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method with hepatocellular carcinoma (Hep-G2), breast cancer (MCF-7) cell lines and a normal hepatic cell (LO2). Cytotoxicity tests (in vitro) indicated that compound 6a showed the highest cytotoxicity with the lowest IC50 values of 23.34 μM on Hep-G2 cells, 12.23 μM on MCF-7 cells, and 44.47 μM on LO2, which would widen the structural diversity of these anticancer targets and confirm the perspectives of further investigations.

KW - Anticancer

KW - Glycyrrhetinic acid

KW - Oleanolic acid

KW - Synthesis

UR - http://www.scopus.com/inward/record.url?scp=85019209037&partnerID=8YFLogxK

UR - https://www.scopus.com/record/pubmetrics.uri?eid=2-s2.0-85019209037&origin=recordpage

U2 - 10.1248/bpb.b17-00016

DO - 10.1248/bpb.b17-00016

M3 - RGC 21 - Publication in refereed journal

SN - 0918-6158

VL - 40

SP - 703

EP - 710

JO - Biological and Pharmaceutical Bulletin

JF - Biological and Pharmaceutical Bulletin

IS - 5

ER -

Design and synthesis of new anticancer glycyrrhetinic acids and oleanolic acids

Abstract

Research Keywords

UN SDGs

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