Design and synthesis of bile acid derivatives and their activity against colon cancer

Wang, Zongyuan; xin, qiang; yijie, peng; wang, yanni; He, Deqin; Zhao, Quanyi

doi:10.1039/d2md00220e

Cited by 3 publications

(1 citation statement)

References 42 publications

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“…These compounds downregulated the expression of Bcl-2 and p-STAT3, contributing to their apoptotic and anti-proliferative effects. Interestingly, these compounds also exhibited anti-inflammatory activity by inhibiting the production of nitric oxide (NO) and downregulating the expression of TNF-alpha, both of which are associated with inflammation in colon cancer ( Wang et al, 2022 ).…”

Section: Synthetic Ba Derivatives Against Cancermentioning

confidence: 99%

The anticancer activity of bile acids in drug discovery and development

Li,

Zou,

Huang

et al. 2024

Front. Pharmacol.

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Bile acids (BAs) constitute essential components of cholesterol metabolites that are synthesized in the liver, stored in the gallbladder, and excreted into the intestine through the biliary system. They play a crucial role in nutrient absorption, lipid and glucose regulation, and the maintenance of metabolic homeostasis. In additional, BAs have demonstrated the ability to attenuate disease progression such as diabetes, metabolic disorders, heart disease, and respiratory ailments. Intriguingly, recent research has offered exciting evidence to unveil their potential antitumor properties against various cancer cell types including tamoxifen-resistant breast cancer, oral squamous cell carcinoma, cholangiocarcinoma, gastric cancer, colon cancer, hepatocellular carcinoma, prostate cancer, gallbladder cancer, neuroblastoma, and others. Up to date, multiple laboratories have synthesized novel BA derivatives to develop potential drug candidates. These derivatives have exhibited the capacity to induce cell death in individual cancer cell types and display promising anti-tumor activities. This review extensively elucidates the anticancer activity of natural BAs and synthetic derivatives in cancer cells, their associated signaling pathways, and therapeutic strategies. Understanding of BAs and their derivatives activities and action mechanisms will evidently assist anticancer drug discovery and devise novel treatment.

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Section: Synthetic Ba Derivatives Against Cancermentioning

confidence: 99%

The anticancer activity of bile acids in drug discovery and development

Li,

Zou,

Huang

et al. 2024

Front. Pharmacol.

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Magnetic particles with polymeric shells bearing lithocholic and folic acid moieties: Nano-warriors to fight colon cancer

Szymczuk,

Markiewicz,

Niemirowicz-Laskowska

et al. 2024

International Journal of Pharmaceutics

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Ursodeoxycholic Acid Platinum(IV) Conjugates as Antiproliferative and Antimetastatic Agents: Remodel the Tumor Microenvironment through Suppressing JAK2/STAT3 Signaling

Chen,

Zhang,

Liu

et al. 2024

J. Med. Chem.

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Tumor microenvironment (TME) is a pivotal factor driving the tumor metastasis and leading to the failure of tumor therapy. Here, a series of ursodeoxycholic acid platinum(IV) conjugates with potency in remodeling the TME through suppressing JAK2/STAT3 signaling was developed. A candidate was screened out, which displayed potent antiproliferative and antimetastatic performance both in vitro and in vivo. It displayed superior pharmacokinetic properties compared to cisplatin. Serious DNA injury was induced, and then mitochondriamediated apoptosis was initiated through the Bcl-2/Bax/Caspase3 pathway. The JAK2/STAT3 and TGF-β1 signaling pathways were remarkably inhibited, and prodeath autophagy was subsequently promoted. The inflammatory and hypoxic TME was suppressed by downregulating COX-2, MMP9, and HIF-1α, which resulted in inhibited angiogenesis in tumors by inhibiting the HIF-1α/VEGFA axis. Additionally, the immunosuppressive TME was reversed by blocking the immune checkpoint PD-L1, further improving the density of CD3 + and CD8 + tumor-infiltrating lymphocytes, and promoting macrophage polarization from M2-to M1-type.

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Design and synthesis of bile acid derivatives and their activity against colon cancer

Abstract: Bile acids (BAs) containing both hydrophilic hydroxyl and carboxyl groups and hydrophobic methyl and steroid nuclei can promote the absorption of fat and other substances in the intestine，and they are...

Cited by 3 publications

References 42 publications

The anticancer activity of bile acids in drug discovery and development

The anticancer activity of bile acids in drug discovery and development

Magnetic particles with polymeric shells bearing lithocholic and folic acid moieties: Nano-warriors to fight colon cancer

Ursodeoxycholic Acid Platinum(IV) Conjugates as Antiproliferative and Antimetastatic Agents: Remodel the Tumor Microenvironment through Suppressing JAK2/STAT3 Signaling

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