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

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

26 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

Keywords

Antitumor
Apoptosis
Breast cancer
Lithocholic acid
Migration

UN SDGs

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

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10.1016/j.steroids.2017.06.009

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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

Keywords

UN SDGs

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