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Review
. 2021 May 31;13(11):2733.
doi: 10.3390/cancers13112733.

Is Emodin with Anticancer Effects Completely Innocent? Two Sides of the Coin

Esra Küpeli Akkol  1 , Iffet Irem Tatlı  2 , Gökçe Şeker Karatoprak  3 , Osman Tuncay Ağar  4 , Çiğdem Yücel  5 , Eduardo Sobarzo-Sánchez  6   7 , Raffaele Capasso  8
Affiliations
Review

Is Emodin with Anticancer Effects Completely Innocent? Two Sides of the Coin

Esra Küpeli Akkol et al. Cancers (Basel). .

Abstract

Many anticancer active compounds are known to have the capacity to destroy pathologically proliferating cancer cells in the body, as well as to destroy rapidly proliferating normal cells. Despite remarkable advances in cancer research over the past few decades, the inclusion of natural compounds in researches as potential drug candidates is becoming increasingly important. However, the perception that the natural is reliable is an issue that needs to be clarified. Among the various chemical classes of natural products, anthraquinones have many biological activities and have also been proven to exhibit a unique anticancer activity. Emodin, an anthraquinone derivative, is a natural compound found in the roots and rhizomes of many plants. The anticancer property of emodin, a broad-spectrum inhibitory agent of cancer cells, has been detailed in many biological pathways. In cancer cells, these molecular mechanisms consist of suppressing cell growth and proliferation through the attenuation of oncogenic growth signaling, such as protein kinase B (AKT), mitogen-activated protein kinase (MAPK), HER-2 tyrosine kinase, Wnt/-catenin, and phosphatidylinositol 3-kinase (PI3K). However, it is known that emodin, which shows toxicity to cancer cells, may cause kidney toxicity, hepatotoxicity, and reproductive toxicity especially at high doses and long-term use. At the same time, studies of emodin, which has poor oral bioavailability, to transform this disadvantage into an advantage with nano-carrier systems reveal that natural compounds are not always directly usable compounds. Consequently, this review aimed to shed light on the anti-proliferative and anti-carcinogenic properties of emodin, as well as its potential toxicities and the advantages of drug delivery systems on bioavailability.

Keywords: anthraquinone; apoptosis; cancer; drug discovery; emodin; nano-drug delivery.

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Conflict of interest statement

The authors declare that they have no known competing financial interest or personal relationships that could have appeared to influence the work reported in this paper.

Figures

Figure 1
Figure 1
An overview of emodin’s anticancer efficacy.
Figure 2
Figure 2
Chemical structures of 9,10-anthracenedione and emodin.
Figure 3
Figure 3
DNA-intercalating anthraquinones of clinical use.
Figure 4
Figure 4
Chemical structures of emodin and its synthesizedderivatives.
Figure 5
Figure 5
Chemical structure of emodin azide methyl anthraquinone derivative.
Figure 6
Figure 6
Antitumoral mechanisms of emodin.
Figure 7
Figure 7
Chemical structure of compound 1.
Figure 8
Figure 8
Chemical structure of DK-V-47.
Figure 9
Figure 9
Chemical structures of synthesized emodin derivatives E-1 and FLE.
Figure 10
Figure 10
Chemical structure of new emodin derivatives I and II.
Figure 11
Figure 11
Chemical structure of potent targeted compound 6.
Figure 12
Figure 12
Chemical structure of emodin linked with 5-fluorouracil derivatives.
Figure 13
Figure 13
Chemical structure of some potent synthesized compounds.
See this image and copyright information in PMC

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