The synthesis and antitumor activity of lithocholic acid and its derivatives

Xiao Long He; Yajing Xing; Xiang Zhong Gu; Jie Xin Xiao; Ying Ying Wang; Zhengfang Yi; Wen Wei Qiu

doi:10.1016/j.steroids.2017.06.009

The synthesis and antitumor activity of lithocholic acid and its derivatives

Xiao Long He
, Yajing Xing
, Xiang Zhong Gu
, Jie Xin Xiao
, Ying Ying Wang
, Zhengfang Yi
, Wen Wei Qiu^*

^*Corresponding author for this work

East China Normal University
Jiangsu Jiaerke Pharmaceuticals Group Co., Ltd.

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

27 Scopus citations

Abstract

In this paper, a new and concise synthetic route of lithocholic acid (LCA) using commercially available steroid source deoxycholic acid is reported. A series of amide derivatives of LCA were also synthesized and investigated for their activity against the growth of MCF-7 and MCF-7/ADR cells using the sulforhodamine B assay. For MCF-7, the most potent compound 20 showed a 20-fold higher antitumor activity than LCA. For MCF-7/ADR, the most potent compound 24 showed a 22-fold higher antitumor activity than LCA. The transwell migration assay of 20 was evaluated on MDA-MB-231 cells. The colony formation and apoptosis assays of 20 were performed on MCF-7 and MCF-7/ADR cell lines.

Original language	English
Pages (from-to)	54-60
Number of pages	7
Journal	Steroids
Volume	125
DOIs	https://doi.org/10.1016/j.steroids.2017.06.009
State	Published - 2017

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

Antitumor
Apoptosis
Breast cancer
Lithocholic acid
Migration

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10.1016/j.steroids.2017.06.009

Cite this

@article{c10bf21bb05a4c8abe60185bc7c31cd5,

title = "The synthesis and antitumor activity of lithocholic acid and its derivatives",

abstract = "In this paper, a new and concise synthetic route of lithocholic acid (LCA) using commercially available steroid source deoxycholic acid is reported. A series of amide derivatives of LCA were also synthesized and investigated for their activity against the growth of MCF-7 and MCF-7/ADR cells using the sulforhodamine B assay. For MCF-7, the most potent compound 20 showed a 20-fold higher antitumor activity than LCA. For MCF-7/ADR, the most potent compound 24 showed a 22-fold higher antitumor activity than LCA. The transwell migration assay of 20 was evaluated on MDA-MB-231 cells. The colony formation and apoptosis assays of 20 were performed on MCF-7 and MCF-7/ADR cell lines.",

keywords = "Antitumor, Apoptosis, Breast cancer, Lithocholic acid, Migration",

author = "He, \{Xiao Long\} and Yajing Xing and Gu, \{Xiang Zhong\} and Xiao, \{Jie Xin\} and Wang, \{Ying Ying\} and Zhengfang Yi and Qiu, \{Wen Wei\}",

note = "Publisher Copyright: {\textcopyright} 2017 Elsevier Inc.",

year = "2017",

doi = "10.1016/j.steroids.2017.06.009",

language = "英语",

volume = "125",

pages = "54--60",

journal = "Steroids",

issn = "0039-128X",

publisher = "Elsevier Inc.",

}

TY - JOUR

T1 - The synthesis and antitumor activity of lithocholic acid and its derivatives

AU - He, Xiao Long

AU - Xing, Yajing

AU - Gu, Xiang Zhong

AU - Xiao, Jie Xin

AU - Wang, Ying Ying

AU - Yi, Zhengfang

AU - Qiu, Wen Wei

PY - 2017

Y1 - 2017

N2 - In this paper, a new and concise synthetic route of lithocholic acid (LCA) using commercially available steroid source deoxycholic acid is reported. A series of amide derivatives of LCA were also synthesized and investigated for their activity against the growth of MCF-7 and MCF-7/ADR cells using the sulforhodamine B assay. For MCF-7, the most potent compound 20 showed a 20-fold higher antitumor activity than LCA. For MCF-7/ADR, the most potent compound 24 showed a 22-fold higher antitumor activity than LCA. The transwell migration assay of 20 was evaluated on MDA-MB-231 cells. The colony formation and apoptosis assays of 20 were performed on MCF-7 and MCF-7/ADR cell lines.

AB - In this paper, a new and concise synthetic route of lithocholic acid (LCA) using commercially available steroid source deoxycholic acid is reported. A series of amide derivatives of LCA were also synthesized and investigated for their activity against the growth of MCF-7 and MCF-7/ADR cells using the sulforhodamine B assay. For MCF-7, the most potent compound 20 showed a 20-fold higher antitumor activity than LCA. For MCF-7/ADR, the most potent compound 24 showed a 22-fold higher antitumor activity than LCA. The transwell migration assay of 20 was evaluated on MDA-MB-231 cells. The colony formation and apoptosis assays of 20 were performed on MCF-7 and MCF-7/ADR cell lines.

KW - Antitumor

KW - Apoptosis

KW - Breast cancer

KW - Lithocholic acid

KW - Migration

UR - https://www.scopus.com/pages/publications/85021388780

U2 - 10.1016/j.steroids.2017.06.009

DO - 10.1016/j.steroids.2017.06.009

M3 - 文章

C2 - 28648585

AN - SCOPUS:85021388780

SN - 0039-128X

VL - 125

SP - 54

EP - 60

JO - Steroids

JF - Steroids

ER -

The synthesis and antitumor activity of lithocholic acid and its derivatives

Abstract

UN SDGs

Keywords

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