Apoptosis-Inducing Effect of Artonin E in Breast Cancer

Etti, Imaobong Christopher; Abdullah, Rasedee; Kadir, Arifah Abdul

doi:10.5772/intechopen.79205

Cited by 2 publications

(1 citation statement)

References 22 publications

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“…22 Against MCF-7 breast cancer cells over 24, 48 and 72 h, inhibition based on IC50 values of artonin E were 6.9, 5.1 and 3.8 µM. [41][42][43] Inhibition was more potent than tamoxifen used as positive control. Values of tamoxifen were 24, 21 and 19 µM.…”

Section: Anti-cancer Activities Of Artonin Ementioning

confidence: 92%

Artonin E: A Short Review of its Chemistry, Sources, Anti-Cancer Activities and Other Pharmacological Properties

2023

TJNPR

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Among the prenylated flavonoids is a group known as artonins. To date, 24 of such compounds (artonins A-Y) have been recorded. 6 Pharmacological properties of artonins include anti-plasmodial, anticancer and antibacterial activities. In this article, the chemistry, sources, anti-cancer and other medicinal properties of artonin E from Artocarpus species are reviewed for the first time. A brief account on other artonins is included. Some prospects and future research on artonin E and other artonins are suggested. Chemistry of Artonin EArtonin E or 5'-hydroxymorusin from Artocarpus species (Moraceae) is a prenylated flavonoid with a molecular formula of C25H24O7 and molecular weight of 436.5 g/mol. 6,7 The molecular structure of artonin E has three aromatic rings (A-C) with three OH groups at C2', C4' and C5' of ring B, and one OH group at C5 of ring A (Figure 1). There are two prenyl units, one isoprenoid substituent at C3 of oxygenated ring C and one forming a dimethylpyrane ring D at C7 and C8. The presence of a double bond between C2 and C3, and a carbonyl group at C4 are essential for the bioactivities of artonin E. Morusin has a similar molecular structure as artonin E except that it lacks the OH group at C5'. For this reason, artonin E is sometimes called 5'-hydroxymorusin. 6 The structure of artonin E is a 3-isoprenyl 2',4',5'-trioxygenated flavone. 5,7 Other compounds with the same structural type are artoindonesianins L and U. Prenylated flavonoids also include 3isoprenyl 2',4'-dioxygenated flavones such as artocarpin 8 and morusin. 9Sources of Artonin E Artonin E was first isolated from the bark Artocarpus altilis (syn. A. communis) 10 (Figure 2). Subsequently, artonin E was reported in other Artocarpus species that include A. chama, A. elasticus, A. gomezianus, A. kemando, A. lanceifolius, A. lowii, A. nobilis, A. rigida, A. rigidus (syn. A. rotunda), A. scortechnii and A. teysmannii (Table 1). Plant part most reported are the root and bark, with no reports on the leaf.

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Section: Anti-cancer Activities Of Artonin Ementioning

confidence: 92%

Artonin E: A Short Review of its Chemistry, Sources, Anti-Cancer Activities and Other Pharmacological Properties

2023

TJNPR

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Small Molecules Inhibit Extranuclear Signaling by Estrogen: A Promising Strategy to Halt Breast Cancer Progression and Metastasis

Etti¹,

Nwafor²,

Essien³

2021

Reproductive Hormones

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The sex hormone estrogen plays critical roles in reproductive and sexual development. It regulates the expression and activity of key signaling molecules critical in various cellular signaling pathways. These signals are mediated by its binding to estrogen receptors alpha (ERα) and beta (ERβ). ERα has been shown to greatly participate in extranuclear signaling, inducing tumorogenesis and breast cancer metastasis. Small molecules from plants are reported with better selectivity toward tumorigenic cells with negligible toxicity when compared to their synthetic counterpart. The molecules used in this study were first probed for their drug-likeness and their pharmacokinetic profile was elucidated before docking them to the ligand binding domain of the human ERα followed by a post docking prime analysis. All tested molecules had good drug-like and pharmacokinetic properties when compared to about 95% of orally available drugs as predicted by qikprop. The docking results revealed a strong binding interaction with ERα, influenced mostly by the vicinal diol groups of the studied molecules. These resulted in a conformational change, inducing receptor dimerization and altering the interactions of the sex hormone with other proteins. The studied ligands are promising in strongly inhibiting the binding of estrogen to ERα, thus limiting its extranuclear signaling.

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Apoptosis-Inducing Effect of Artonin E in Breast Cancer

Cited by 2 publications

References 22 publications

Artonin E: A Short Review of its Chemistry, Sources, Anti-Cancer Activities and Other Pharmacological Properties

Artonin E: A Short Review of its Chemistry, Sources, Anti-Cancer Activities and Other Pharmacological Properties

Small Molecules Inhibit Extranuclear Signaling by Estrogen: A Promising Strategy to Halt Breast Cancer Progression and Metastasis

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