Esculetin modulates cytotoxicity induced by oxidants in NB4 human leukemia cells

Rubio, Virginia; García-Pérez, Ana Isabel; Herráez, Ángel; Tejedor, M. Cristina; Diez, José C.

doi:10.1016/j.etp.2017.08.001

Cited by 15 publications

(10 citation statements)

References 39 publications

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“…In combine application, administration of esculetin increased apoptotic effect caused by taxol in human hepatoma cells . In another study, it was shown that esculetin induces apoptosis and has protective effects on cell viability, late apoptosis and necrosis against oxidants in human leukaemia cells . In present study, we focused on apoptotic and necrotic cell deaths to study cell death in insulinoma INS‐1 cells.…”

Section: Discussionmentioning

confidence: 99%

“…[31] In another study, it was shown that esculetin induces apoptosis and has protective effects on cell viability, late apoptosis and necrosis against oxidants in human leukaemia cells. [32] In present study, we focused on apoptotic and necrotic cell deaths to study cell death in insulinoma INS-1 cells. As a result, it was determined that the major cell death mechanism was necrosis and this effect was dose-dependent.…”

Section: Discussionmentioning

confidence: 99%

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Investigation of cell death mechanism and activity of esculetin-loaded PLGA nanoparticles on insulinoma cellsin vitro

Kaçar

Bahadorı

Tekkeli

et al. 2020

Journal of Pharmacy and Pharmacology

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Aim The purpose of this study was to prepare targeted cancer therapy formulation against insulinoma INS‐1 cells and to study its effect on cell death with related mechanisms in vitro. Methods Polylactide‐co‐glycolide (PLGA) nano‐micelles were used for preparation of esculetin nano‐formulation (nano‐esculetin). The cells were treated with nano‐esculetin and free esculetin. Apoptotic and necrotic cell death percentages, cell proliferation, ATP and GTP reductions and insulin levels were investigated on insulinoma INS‐1 cells for both free and nano‐esculetin formulations. Results About 50 mg of PLGA was able to carry 20 mg esculetin in 20 ml of formulation. The obtained optimized formulation was 150 nm, with 92% encapsulation efficiency and a slow‐release behaviour was observed during release studies. Nano‐esculetin bearing 25, 50 and 100 μg esculetin and free esculetin in equivalent doses successfully decreased cell viability. The prevailing cell death mechanism was necrosis. Along with cell proliferation, intracellular insulin and the ratio of ATP and GTP were decreased even with 12.5, 25 and 50 μg esculetin bearing nano‐formulation and its equivalent free esculetin. Conclusions The results revealed that esculetin is able to show its anti‐tumor afficacy after loading to PLGA nano‐micelles and nano‐encapsulation intensifies its cytotoxic activity in vitro. Current study shows that esculetin and its nano formulations are promising agents in treatment of insulinoma.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Investigation of cell death mechanism and activity of esculetin-loaded PLGA nanoparticles on insulinoma cellsin vitro

Kaçar

Bahadorı

Tekkeli

et al. 2020

Journal of Pharmacy and Pharmacology

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“…There are promising fields for innovation and scientific research in the future about this taxon. The antiproliferative effects of aesculetin [ 21 , 22 ] open the way in the field of oncology; brunfelsamidine and cuscohygrine [ 19 , 23 ], in the fields of anesthesiology and reanimation; and most relevantly, furostan saponins for the treatment of leishmania and other intracellular parasites that produce malaria [ 32 ]. The small molecular size of the main components presented in Table 2 make them very good candidates to be tested in the future “in silico” discovery of new drugs.…”

Section: Discussionmentioning

confidence: 99%

Chiricaspi (Brunfelsia grandiflora, Solanaceae), a Pharmacologically Promising Plant

Luzuriaga-Quichimbo

Barco

Salas

et al. 2018

Plants

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This study’s objective was to evaluate the rescued traditional knowledge about the chiricaspi (Brunfelsia grandiflora s.l.), obtained in an isolated Canelo-Kichwa Amazonian community in the Pastaza province (Ecuador). This approach demonstrates well the value of biodiversity conservation in an endangered ecoregion. The authors describe the ancestral practices that remain in force today. They validated them through bibliographic revisions in data megabases, which presented activity and chemical components. The authors also propose possible routes for the development of new bioproducts based on the plant. In silico research about new drug design based on traditional knowledge about this species can produce significant progress in specific areas of childbirth, anesthesiology, and neurology.

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“…Esculetin was shown to induce many cellular processes in many cell types 2 . Esculetin evoked apoptotsis of hepatoma cells 3 , suppressed lung cancer 4 , and modulated viability in leukemia cells 5 .…”

Section: Introductionmentioning

confidence: 99%

Action of the natural compound esculetin on Ca2+ movement and survival in prostate cancer cells

Jan¹,

Kuo²,

Hao³

et al. 2021

Preprint

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Esculetin is derived from coumarin and is shown to be the main constituent of the Chinese herb Cortex Fraxini. The molecular paths underlying the action of esculetin are intensively studied. The outcome of esculetin on Ca2+ concentration ([Ca2+]i) in prostate cells is unexplored. Fura-2 was used to detect Ca2+ changes. Death was assessed by using WST-1. At doses of 25-100 mM, esculetin evoked [Ca2+]i raises. This signal was lessened by 15% by exclusion of Ca2+. Esculetin (100 μM) induced Mn2+ entry that implied Ca2+ influx. Esculetin-evoked Ca2+ influx was curbed by 50% by nifedipine (1 mM), econazole (0.5 mM) and SKF96365 (5 mM); phorbol 12-myristate 13 acetate (PMA; 1 nM; a protein kinase C [PKC] activator); and GF109203X (2 mM; a PKC inhibitor. In the absence of Ca2+, pretreatment with the endoplasmic reticulum (ER) Ca2+ pump inhibitor thapsigargin (1 mM) eradicated esculetin-induced [Ca2+]i raises. U73122, a phospholipase C (PLC) suppressor got rid of esculetin-caused [Ca2+]i rises. Esculetin (20-70 mM) evoked death which was not restrained by treatment with the Ca2+ binder BAPTA/AM. In summary, in PC3 cells, esculetin stimulated [Ca2+]i raises by Ca2+ influx through PKC-sensitive store-operated Ca2+ entry and PLC-associated ER Ca2+ discharging. Esculetin provoked Ca2+-independent cell death.

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Esculetin modulates cytotoxicity induced by oxidants in NB4 human leukemia cells

Cited by 15 publications

References 39 publications

Investigation of cell death mechanism and activity of esculetin-loaded PLGA nanoparticles on insulinoma cellsin vitro

Investigation of cell death mechanism and activity of esculetin-loaded PLGA nanoparticles on insulinoma cellsin vitro

Chiricaspi (Brunfelsia grandiflora, Solanaceae), a Pharmacologically Promising Plant

Action of the natural compound esculetin on Ca2+ movement and survival in prostate cancer cells

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