EVALUATION OF THE CYTOTOXIC EFFECTS INDUCED BY 68Ga-NODAGA-c(RGDfK) AND 68Ga-DOTA-c(RGDfK) IN MURINE MALIGNANT MELANOMA

Panait, M.E.

doi:10.31925/farmacia.2021.5.8

Cited by 1 publication

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“…Current MM treatment strategies resort to surgery, chemotherapy, targeted therapy and immunotherapy. In recent years, there has been an improvement in the treatment of melanoma with the development of new therapeutic agents such as BRAF, CTLA4 and PD1 inhibitors [13,27]. Although major advances have been made in the treatment of melanoma, these types of new therapeutic approaches face many challenges.…”

Section: Introductionmentioning

confidence: 99%

In Vitro Insights Regarding the Role of Melanin in Melanoma Cells’ Response to Betulinic Acid Treatment

MELANIA¹

2022

FARMACIA

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Malignant melanoma (MM), the cancer arising from the normal-to-malignant switch of melanocytes, remains the most aggressive type of skin cancer with an annual increasing incidence worldwide. Based on the presence or absence of melanin, MM is divided in melanotic (pigmented) or amelanotic (non-pigmented) melanoma. Melanin is the natural pigment providing a protective role against harmful ultraviolet (UV) radiations and oxidative stress to epidermal melanocytes and surrounding keratinocytes. Recent studies reveal the ability of melanin to bind drugs via covalent and non-covalent bonds, leading to their accumulation within pigmented tissues which might influence the response of MM to chemotherapy. Betulinic acid (BA) is a pentacyclic triterpenoid possessing a multitude of therapeutic properties, including antimelanoma activity. The present study aimed to investigate the response of two MM cell lines to the antitumour effect of BA, considering their melanin content and to evaluate the cytotoxic potential of BA in healthy primary fibroblasts. The results reveal a dose-dependent decrease in the viability and confluence of all cell lines. However, SK-MEL-5 cells (IC50 =13.67 µM for 24 h, and 7.48 µM for 72 h) exerted a higher sensitivity to BA when compared to B16-F10 cells (IC50 = 52.12 µM for 24 h, and 25.54 for 72 h). BA induces a differential cytotoxicity in healthy, MM non-pigmented SK-MEL-5 and pigmented B16-F10 cells. Therefore, further studies are required to confirm the interaction between BA and melanin. RezumatMelanomul malign (MM), cancerul care rezultă din transformarea malignă a melanocitelor, rămâne cel mai agresiv tip de cancer cutanat, având o incidență anuală aflată în continuă creștere. În funcție de prezența sau absența melaninei, MM se clasifică în melanom melanotic (pigmentat) și amelanotic (nepigmentat). Melanina reprezintă pigmentul natural care oferă protecție melanocitelor și keratinocitelor epidermice împotriva radiațiilor ultraviolete (UV) și a stresului oxidativ. Studiile recente au evidențiat abilitatea melaninei de a lega medicamente prin legături covalente și non-covalente, rezultând acumularea lor la nivelul țesuturilor pigmentate, fenomen care poate influența răspunsul MM la chimioterapie. Acidul betulinic (BA) este un fitocompus din clasa triterpenelor pentaciclice care posedă o multitudine de proprietăți terapeutice, inclusiv activitate antimelanom. Acest studiu a urmărit investigarea răspunsului a două linii celulare de MM la efectul antitumoral al BA, având în vedere conținutul de melanină și evaluarea potențialului citotoxic al BA asupra unor celule sănătoase -fibroblaste primare. Rezultatele au arătat o scădere doză-dependentă în viabilitatea și confluența tuturor liniilor celulare. Totuși, linia celulară SK-MEL-5 (IC50 =13,67 µM pentru 24 h și 7,48 µM pentru 72 h) a manifestat o sensibilitate mai ridicată la acțiunea BA comparativ cu linia celulară B16-F10 (IC50 = 52,12 µM pentru 24 h și 25,54 pentru 72 h). BA induce o citotoxicitate dependentă de tipul de celule, celule sănătoas...

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Section: Introductionmentioning

confidence: 99%

In Vitro Insights Regarding the Role of Melanin in Melanoma Cells’ Response to Betulinic Acid Treatment

MELANIA¹

2022

FARMACIA

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show abstract

EVALUATION OF THE CYTOTOXIC EFFECTS INDUCED BY 68Ga-NODAGA-c(RGDfK) AND 68Ga-DOTA-c(RGDfK) IN MURINE MALIGNANT MELANOMA

Cited by 1 publication

References 14 publications

In Vitro Insights Regarding the Role of Melanin in Melanoma Cells’ Response to Betulinic Acid Treatment

In Vitro Insights Regarding the Role of Melanin in Melanoma Cells’ Response to Betulinic Acid Treatment

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