Abstract
Cancer is one of the most common causes of disease-related deaths worldwide. Despite the discovery of many chemotherapeutic drugs that inhibit uncontrolled cell division processes for the treatment of various cancers, serious side effects of these drugs are a crucial disadvantage. In addition, multi-drug resistance is another important problem in anticancer treatment. Due to problems such as cytotoxicity and drug resistance, many investigations are being conducted to discover and develop effective anticancer drugs. In recent years, researchers have focused on the anticancer activity coumarins, due to their high biological activity and low toxicity. Coumarins are commonly used in the treatment of prostate cancer, renal cell carcinoma and leukemia, and they also have the ability to counteract the side effects caused by radiotherapy. Both natural and synthetic coumarin derivatives draw attention due to their photochemotherapy and therapeutic applications in cancer. In this review, a compilation of various research reports on coumarins with anticancer activity and investigation and a review of structure-activity relationship studies on coumarin core are presented. Determination of important structural features around the coumarin core may help researchers to design and develop new analogues with a strong anticancer effect and reduce the potential side effects of existing therapeutics.
Highlights
Coumarins are polyphenolic compounds belonging a group of colorless and crystalline oxygenated heterocyclic compounds first isolated from the plant named Dipteryx odorata Willd. (Fabaceae) known locally as “coumaroun” by Vogel in 1820 [1,2]
Studies conducted on the anticancer activity of coumarin and its derivatives revealed that the mechanism of action of these compounds is generally caspase dependent apoptosis
Studies on human and cynomolgus monkey liver fragments and/or hepatocytes have identified a relative resistance to coumarin toxicity, and this was associated with coumarin 7-hydroxylation, which is the main route of coumarin metabolism
Summary
Coumarins are polyphenolic compounds belonging a group of colorless and crystalline oxygenated heterocyclic compounds first isolated from the plant named Dipteryx odorata Willd. (Fabaceae) known locally as “coumaroun” by Vogel in 1820 [1,2]. Most natural coumarins are isolated from vascular plants, some coumarins such as novobiocin, coumermycin and aflatoxin are isolated from microbial sources [7,8] These compounds have become of importance in recent years due to their various biological activities. The usage of some coumarin derivatives as a tobacco flavor, which are used as fixative and flavoring agents, has been regulated by the FDA because of its negative effects, such as mild nausea, diarrhea and hepatotoxicity [23,24,25,26] Besides their medical use, coumarins are used in the cosmetic industry and agrochemical industry, as well as optical brightening agents [27,28]. Determination of important structural features around the coumarin core may help researchers to design and develop new analogues with a strong anticancer effect and reduce the potential side effects of existing therapeutics
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