Biological Activities of Emetine

Akinboye, Emmanuel S.; Bakare, Oladapo

doi:10.2174/1874848101104010008

Cited by 97 publications

(76 citation statements)

References 74 publications

(87 reference statements)

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“…In addition, any substituted group would result in conformational changes which appear to affect the space between the tricyclic and bicyclic ring system of emetine and consequently affect the bioactivity of the resulting analog including protein synthesis inhibitory and anticancer activities. 5,15,20 Hence, an appropriate substituent in this position would result in a clinically useful emetine prodrug, or an emetine derivative that does not have the same systemic toxicity as emetine. We are currently studying a diverse library of emetine analogs in this regard.…”

Section: Biologymentioning

confidence: 99%

“…5 well known anti-cancer alkaloid from Psychotria ipecacuanha. [6][7][8] Its anticancer activity was evaluated in several clinical studies up to Phase II for treating solid tumor, however narrow therapeutic index and dose dependent side effects stopped further studies.…”

Section: Introductionmentioning

confidence: 99%

“…81 (6H, br s),3.84 (3H, s),5.95 (1H, dd, J = 5.9, 12.8 Hz), 6.66 (1H, s), 6.69 (1H, s), 6.72 (1H,s), 7.20 (1H,s), 7.25 (1H, dd, J = 3.6, 11.8 Hz) 13. C NMR (100 MHz, CD 3 OD) d 216.5, 147.4, 147.3, 147.2, 147.1, 133.0, 131.1, 127.0, 126.5, 112.6, 112.0, 111.0, 110.3, 65.4, 63.3, 61.6, 58.0, 56.5, 56.2, 56.1, 56.0, 55.9, 52.5, 41.7, 41.3, 37.6, 29.4, 27.3, 23.7, 11.6.…”

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confidence: 99%

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Design, synthesis and cytotoxicity studies of dithiocarbamate ester derivatives of emetine in prostate cancer cell lines

Akinboye

Bamji

Kwabi-Addo

et al. 2015

Bioorganic & Medicinal Chemistry

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A small library of emetine dithiocarbamate ester derivatives were synthesized in 25-86% yield via derivatization of the N2'- position of emetine. Anticancer evaluation of these compounds in androgen receptor positive LNCaP and androgen receptor negative PC3 and DU145 prostate cancer cell lines revealed time dependent and dose-dependent cytotoxicity. With the exception of compound 4c, all the dithiocarbamate ester analogs in this study showed appreciable potency in all the prostate cancer cell lines (regardless of whether it is androgen receptor positive or negative) with a cytotoxicity IC50 value ranging from 1.312 ± 0.032 μM to 5.201 ± 0.125 μM by day 7 of treatment. Compared to the sodium dithiocarbamate salt 1, all the dithiocarbamate ester analogs (2 and 4a-4 g) displayed lower cytotoxicity than compound 1 (PC3, IC50 = 0.087 ± 0.005 μM; DU145, IC50 = 0.079 ± 0.003 μM and LNCaP, IC50 = 0.079 ± 0.003 μM) on day 7 of treatment. Consequently, it appears that S-alkylation of compound 1 leads to a more stable dithiocarbamate ester derivative that resulted in lower anticancer activity in the prostate cancer cell lines.

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Section: Biologymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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confidence: 99%

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Design, synthesis and cytotoxicity studies of dithiocarbamate ester derivatives of emetine in prostate cancer cell lines

Akinboye

Bamji

Kwabi-Addo

et al. 2015

Bioorganic & Medicinal Chemistry

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“…Emetine is an alkaloid that has been tested in Phase I and II clinical trials against solid tumors (45). Emetine has been used as an anti-protozoal drug and a cough suppressant, although its use is limited by cardiotoxicity (46,47).…”

Section: Emetine Binds Atgl With High Affinitymentioning

confidence: 99%

Emetine Di-HCl Attenuates Type 1 Diabetes Mellitus in Mice

Hudson

Dancho

et al. 2016

Mol Med

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Type 1 diabetes mellitus (T1D) is a chronic autoimmune disease characterized by β cell destruction, insulin deficiency and hyperglycemia. Activated macrophages and autoimmune T cells play a crucial role in the pathogenesis of hyperglycemia in NOD murine diabetes models, but the molecular mechanisms of macrophage activation are unknown. We recently identified pigment epithelium-derived factor (PEDF) as an adipocyte-derived factor that activates macrophages and mediates insulin resistance. Reasoning that PEDF might participate as a proinflammatory mediator in murine diabetes, we measured PEDF levels in NOD mice. PEDF levels are significantly elevated in pancreas, in parallel with pancreatic TNF levels in NOD mice. To identify experimental therapeutics, we screened 2,327 compounds in two chemical libraries (the NIH Clinical Collection and Pharmakon-1600) for leads that inhibit PEDF mediated TNF release in macrophage cultures. The lead molecule selected, "emetine" is a widely used emetic. It inhibited PEDF-mediated macrophage activation with an EC50 or 146 nmol/L. Administration of emetine to NOD mice and to C57Bl6 mice subjected to streptozotocin significantly attenuated hyperglycemia, reduced TNF levels in pancreas and attenuated insulitis. Together, these results suggest that targeting PEDF with emetine may attenuate TNF release and hyperglycemia in murine diabetes models. This suggests that further investigation of PEDF and emetine in the pathogenesis of human diabetes is warranted.

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“…This species is in critical danger of extinction according to the literature reports (Oliveira, Venturini, Rossi & Hastenreiter, 2010;Souza, Martins, Santana & Oliveira, 2008). Although it has not been categorized by the International Union for Conservation of Nature (IUCN), since the beginning of the 20th century, this plant has been overexploited for its potential in traditional medicine, since it was and still is used as emetic, expectorant, amebicide, diaphoretic, among other properties (Akinboye & Bakare, 2011;Ferreira, Cruz, Lima & Trindade, 2012;Botero, Urrea & Naranjo, 2015).…”

Section: Introductionmentioning

confidence: 99%

Ex situ potential conservation of ipecacuanha (Psychotria ipecacuanha (Brot.) Stokes.), a critically endangered medicinal plant species

2017

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Ex situ potential conservation of ipecacuanha (Psychotria ipecacuanha (Brot.) Stokes.), a critically endangered medicinal plant species Potencial de conservación ex situ de ipecacuana (Psychotria ipecacuanha (Brot.) Stokes.), una planta medicinal en peligro crítico de extinción Aura Inés Urrea Trujillo*, Catalina Botero Giraldo and Esther Julia Naranjo Gómez AbstractPsychotria ipecacuanha is a medicinal plant endangered in Colombia, due to the indiscriminate exploitation suffered several decades ago for its therapeutic importance. Its great medicinal value is due to emetine production and its derivatives, mainly in the roots. Given these concerns, the aim of this research was to evaluate different parameters for in vitro conservation of P. ipecacuanha by a limited plant growth, using as in vitro explants plant nodes. Plant growth response to 18, 23 and 25°C with and without addition to MS basal culture medium 15 and 30 gL-1 of mannitol osmotic regulator was evaluated. Registration of plant survival data (%), plant height (cm), plant development of axillary shoots, number of leaves, callus formation and vigour of developed buds and was initially performed at 3 months and then every two months until 12 months. The explants conserved for 9 months in culture medium without mannitol osmotic regulator and temperature of 18°C, showed response after transferring and reculturing in recovery culture medium for 6-8 weeks, this process had not achieved any effect on plant growth and vigour in the recovery phase. In addition, the critical parameters in the acclimatization process were determined.Keywords: in vitro conservation, plant limited growth, osmotic regulator, recovery phase, vigour. ResumenPsychotria ipecacuanha es una especie medicinal amenazada en Colombia, debido a la explotación indiscriminada que varias décadas atrás sufrió por su importancia terapéutica. Su gran valor medicinal se debe a la producción de emetina y sus derivados, principalmente en las raíces. Ante este panorama, el presente estudio tuvo como objetivo evaluar diferentes parámetros para la conservación in vitro de P. ipecacuanha por crecimiento limitado, usando como explantes nudos de plantas in vitro. Se evaluó la respuesta de crecimiento a 18, 23 y 25°C sin y con la adición al medio de cultivo basal MS del regulador osmótico manitol a 15 y 30 gL -1 . El registro de los datos de supervivencia (%), altura (cm), desarrollo de brotes axilares, número de hojas, formación de callo y vigor de los brotes desarrollados, se realizó inicialmente a los 3 meses y luego cada dos meses hasta completar 12 meses. Una temperatura de 18°C, sin la adición del regulador osmótico manitol al medio cultivo basal MS, permitió mantener vitroplantas de esta especie hasta por nueve meses, sin verse afectado el crecimiento y vigor en la etapa de recuperación. Además se logró determinar los parámetros críticos en el proceso de aclimatización.Palabras clave: Conservación in vitro, crecimiento limitado, etapa de recuperación, regulador osmótico, vigorosidad. 599 Introduction...

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Biological Activities of Emetine

Cited by 97 publications

References 74 publications

Design, synthesis and cytotoxicity studies of dithiocarbamate ester derivatives of emetine in prostate cancer cell lines

Design, synthesis and cytotoxicity studies of dithiocarbamate ester derivatives of emetine in prostate cancer cell lines

Emetine Di-HCl Attenuates Type 1 Diabetes Mellitus in Mice

Ex situ potential conservation of ipecacuanha (Psychotria ipecacuanha (Brot.) Stokes.), a critically endangered medicinal plant species

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