Antitumor, Anti-Inflammatory and Analgesic Property of Embelin, a Plant Product

Chitra, M.; Sukumar, E.; Suja, V.; Devi, C. S. Shyamala

doi:10.1159/000239181

Cited by 164 publications

(121 citation statements)

References 5 publications

(5 reference statements)

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“…17 Embelin has been shown to have anti-tumor, anti-inflammatory, and analgesic properties. 30 Our study showed that embelin counteracted the glucose-related stimulatory effect on the proliferation and production of VEGF in Mü ller cells, supporting the use of embelin in the treatment of diabetic retinopathy. In fact, recent animal studies have shown that embelin has a strong antidiabetic effect in alloxan-induced diabetic rats, as evident by a reduction in fasting blood glucose levels, significant improvement in body weights, and restoration of biochemical parameters.…”

Section: Discussionsupporting

confidence: 67%

“…The results showed 42-fold increase at 25 mM glucose and 43-fold increase at 50 mM glucose of both proteins in a dose-dependent manner, respectively (Figure 3a). This relationship was further examined by incubation of Mü ller cells with high-glucose conditions (50 mM) and various concentrations of embelin (15,30, and 60 mM) for 72 h. The results showed that the decrease of XIAP expression by embelin led to a decrease of VEGF expression (Figure 3b).…”

Section: Embelin Reversed the Proliferation And Protein Expression Almentioning

confidence: 92%

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Elevated cell proliferation and VEGF production by high-glucose conditions in Müller cells involve XIAP

Sun

et al. 2013

Eye

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Purpose Mü ller cells have important roles in the pathogenesis of diabetic retinopathy by promoting cell proliferation and inducing the production of vascular endothelial growth factor (VEGF) under hyperglycemic conditions. The objective of this study was to determine the potential mechanism of Mü ller cell proliferation and VEGF production due to high-glucose conditions. Methods Primary cultured rat Mü ller cells were incubated with medium containing variable concentrations of glucose and/or embelin, a specific inhibitor of X-linked inhibitor of apoptosis protein (XIAP), for 72 h. The proliferation of Mü ller cells was assessed by the MTT assay. The expression and/or phosphorylation of 146 proteins were assessed using protein pathway array. Results High concentrations of glucoseinduced Mü ller cell proliferation and altered expression and/or phosphorylation of 47 proteins that have been identified to have key roles in several important signaling pathways (XIAP, VEGF, HIF1a, NFkB, etc) and are involved in the regulation of cell survival, proliferation, or apoptosis. However, Mü ller cell alterations induced by highglucose conditions were counteracted by the XIAP inhibitor embelin, and 26 proteins/ phosphorylations (out of 47) were restored to their normal levels. Nine proteins, including NFkB p65, p-p38, tumor necrosis factor-a, urokinase-type plasminogen activator, CREB, IL-1b, HCAM, estrogen receptor-a, and p-Stat3, were involved in regulatory networks between XIAP and VEGF. Conclusions The current study suggests that XIAP may be a potential regulator that can mediate a series of pathological changes induced by high-glucose conditions in Mü ller cells. Therefore, embelin could be a potential agent for the prevention and treatment of diabetic retinopathy.

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Section: Discussionsupporting

confidence: 67%

Section: Embelin Reversed the Proliferation And Protein Expression Almentioning

confidence: 92%

Elevated cell proliferation and VEGF production by high-glucose conditions in Müller cells involve XIAP

Sun

et al. 2013

Eye

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“…Prior studies of embelin and related analogues have demonstrated its antitumor effects in xenograft models. 66 In studies in mice, rats and dogs embelin was safe, but produced a reversible decrease in testosterone and infertility. 67,68 Thus, given the prior pharmacokinetic and toxicity data, embelin could be rapidly advanced into clinical trials for the treatment of solid tumors and hematologic malignancies.…”

Section: Bir 3 Inhibitorsmentioning

confidence: 99%

Targeting XIAP for the treatment of malignancy

et al. 2005

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X-linked inhibitor of apoptosis protein (XIAP) is a member of the inhibitor of apoptosis proteins family of caspase inhibitors that selectively binds and inhibits caspases-3, -7 and -9, but not caspase-8. As such, XIAP blocks a substantial portion of the apoptosis pathway and is an attractive target for novel therapeutic agents for the treatment of malignancy. Antisense oligonucleotides directed against XIAP are effective in vitro and are currently being evaluated in clinical trials. Small molecule XIAP inhibitors that target the baculovirus IAP repeat (BIR) 2 or BIR 3 domain are in preclinical development and are advancing toward the clinic. This review will discuss the progress being made in developing antisense and smallmolecule XIAP inhibitors.

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“…Embelin (2,5-dihydroxy-3-undecil-1,4-benzoquinone) was obtained from Oxalis erythrorhiza Gillies ex Hooker et Arnott (Oxalidaceae) 12,21 collected in the province of San Juan, Argentina, following the procedure described by Feresin et al 14 Figure 1 shows the chemical structure of embelin. Its empirical formula is C 17 H 26 O 4 , and its molecular weight is 294.39 g mol À1 .…”

Section: Experimental Procedures Materialsmentioning

confidence: 99%

Dispersion and release of embelin from electrospun, biodegradable, polymeric membranes

Tornello

Feresin

Tapia

et al. 2012

Polym J

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In this work, microfiber meshes containing embelin, a poorly water-soluble bioactive agent, were prepared by solubilizing embelin in a biodegradable and biocompatible polymer matrix of poly(e-caprolactone) (PCL). Plain or drug-loaded, highly porous, fibrous membranes with a high area-to-volume ratio were obtained by electrospinning. Non-woven microfibrous meshes were formed by uniform bead-free fibers with a mean diameter of 1.2 lm. Non-porous films were obtained by solution casting, and were used for comparison. The drug-loading content of the prepared systems was appropriate for topical applications. The thermal properties revealed that the crystallinity of embelin significantly decreased, the drug having almost completely dissolved in the PCL fibers. The in situ bioavailability of embelin, an antimycotic agent, is an important aspect to consider in topical drug applications. The drug-loaded systems presented different contact areas with the biological environment. When comparing the ability to expose embelin with the biological environment of the prepared systems, drug-loaded fibrous scaffolds showed a higher bioavailability of the bioactive agent because of an increase by 86% in the area-to-volume ratio, providing an effective area per unit mass that was 5.8-fold higher than that of the film. For the meshes, 90% embelin release was observed after 12 h of exposure to phosphate-buffered saline, whereas for the films a comparable level of release occurred only after 72 h.

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Antitumor, Anti-Inflammatory and Analgesic Property of Embelin, a Plant Product

Cited by 164 publications

References 5 publications

Elevated cell proliferation and VEGF production by high-glucose conditions in Müller cells involve XIAP

Elevated cell proliferation and VEGF production by high-glucose conditions in Müller cells involve XIAP

Targeting XIAP for the treatment of malignancy

Dispersion and release of embelin from electrospun, biodegradable, polymeric membranes

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