Embelin – a drug of antiquity: shifting the paradigm towards modern medicine

Abstract

Embelin is the only known non-peptide small-molecule X-linked inhibitor of the apoptosis protein (XIAP) - an anti-apoptotic protein considered a promising cancer therapeutic target. Embelin acts as an NF-κB blocker and potential suppressor of tumorigenesis. It also exhibits potent cytotoxic, antioxidant and cancer chemopreventive effects. Given the potential uses of embelin, it is recommended that further investigations take place to properly explore its pharmacological and clinical effects.

Chemical Control of Fertility in Male Dogs: A Review

“…Embelin is the major active constituent in the fruits commonly known as vidanga which was first chemically investigated by Scott in 1888 (Poojari, 2014). Embelin, at an oral dose of 80 mg/kg every alternate day for 100 days caused significant reduction in the weight of testes and epididymis, the diameter of the seminiferous tubule and Leydig cells and biochemical changes in testes and epididymis of male dogs.…”

Emerging Epigenetic Therapies

“…Embelin treatment leads to the downregulation of genes involved in cell proliferation (COX-2, cyclin-D1, c-Myc) and tumor metastasis (VEGF, ICAM-1, MMP-9) as well as XIAP [157,158]. The pro-apoptotic, anti-tumorogenic, and anti-cancer activities of embelin have been attributed to its inhibitory effect on X-linked Inhibitor of Apoptosis Protein (XIAP).…”

Embelin-Induced Phosphatidylserine Translocation in the Erythrocyte Cell Membrane

“…Embelin (2,5-dihydroxy-3-undecyl-1,4-benzoquinone), a phytochemical isolated from Embelia ribes [1], has antihelminthic [2], contraceptive [2], anti-inflammatory [3][4][5][6] and anticancer [1][2][3][4][6][7][8][9][10][11] potency, as well as photosensitizing [1] and radiation sensitizing [12] property. Embelin has further been shown to decrease cardiac injury following experimental myocardial infarction [13] and to protect cells against UVB-induced oxidative damage [14], but to aggravate the encephalopathy following neonatal hypoxia-ischemia [15].…”

“…Mechanisms mediating the effects of embelin include mitochondrial depolarization [22,23,27,29,31], induction of oxidative stress [17], inhibition of X-linked inhibitor of the apoptosis protein (XIAP) [3,5,10,11,16,19,20,24,30,[32][33][34][35][36], of PTEN/ Akt/mTOR/S6K1 signaling [37,38] and of the transcription factors NF-κB [2,11,16,25,39] and STAT3 [3,6,18,37], increase of intracellular free Ca 2+ concentration ([Ca 2+ ] i ) [40], upregulation of TRAIL receptors DR4/DR5 [19] and Bax [7,23,31], as well as activation of p38 kinase [17,32], Jun kinase [17], p53 transcription factor [6,22,28,32] and caspases [7,8,11,…”