Abstract

Cancers of the gastrointestinal (GI) tract are often life-threatening malignancies, which can be a severe burden to the health care system. Globally, the mortality rate from gastrointestinal tumors has been increasing due to the lack of adequate diagnostic, prognostic, and therapeutic measures to combat these tumors. Coumarin is a natural product with remarkable antitumor activity, and it is widely found in various natural plant sources. Researchers have explored coumarin and its related derivatives to investigate their antitumor activity, and the potential molecular mechanisms involved. These mechanisms include hormone antagonists, alkylating agents, inhibitors of angiogenesis, inhibitors of topoisomerase, inducers of apoptosis, agents with antimitotic activity, telomerase inhibitors, inhibitors of human carbonic anhydrase, as well as other potential mechanisms. Consequently, drug design and discovery scientists and medicinal chemists have collaborated to identify new coumarin-related agents in order to produce more effective antitumor drugs against GI cancers. Herein, we summarize the therapeutic effects of coumarin and its derivatives against GI cancer.

Highlights

  • Cancer accounts for about 13% of all deaths globally (~7.9 million per year) and is considered a major cause of mortality [1]

  • Perumalsamy et al performed an in silico and in vitro study to investigate whether substituted biscoumarin (SSBC) could induce apoptosis and inhibit proliferation of tumor cells [84]

  • Coumarin compounds have a broad range of biological activity, and for decades many scientists have investigated these compounds, and some have devised new related structures to potentially treat cancer, as well as a plethora of other diseases

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Summary

INTRODUCTION

Cancer accounts for about 13% of all deaths globally (~7.9 million per year) and is considered a major cause of mortality [1]. Carcinogenesis of the GI tract is influenced by many intrinsic and Coumarin and Gastrointestinal Cancer external risk factors, including alcohol use, being overweight, genetic mutations, as well as infection with specific bacteria such as Helicobacter pylori [8]. The most common symptoms are epigastric pain, upper abdominal bloating, and a palpable abdominal mass [9] These tumors put a pressing load on health care providers and are considered a public health issue [8]. Coumarins can exert a wide range of pharmaceutical functions, including activity against bacteria, viral infections, and fungal infections. It has anti-cancer, anti-inflammatory, anticoagulant, and anti-hypertensive activity [13, 14]. We summarize some therapeutic effects of coumarin against GI cancer

PHARMACOKINETICS OF COUMARIN
COUMARINS AND GASTRIC CANCER
COUMARINS AND COLON CANCER
Coumarin compound
Quenched organic hydroperoxides and hydrogen peroxide
Coumarins and Pancreatic Cancer
Coumarin derivatives
Induced apoptosis and necroptosis
Coumarins and Hepatocellular Carcinoma
Coumarin and Esophageal Cancer
Isoprenylated coumarins
Hydroxypyridinonecoumarin Furanocoumarin
Anticancer activity
In vitro In vitro In vitro In vitro In vitro
CONCLUSIONS
Findings
AUTHOR CONTRIBUTIONS

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