<i>In vitro</i> anticancer activity and cytotoxicity of some papaver alkaloids on cancer and normal cell lines

Abstract

Background: The purpose of this study is to determine the effect of in vitro anticancer activity and cytotoxicity of 13 Papaver alkaloids (amurine, armepavine, berberine, isocorydine, isothebaine, macranthine, mecambrine, mecambridine, narkotine, orientalidine, oripavine, salutaridine and thebaine) against the human cervical cancer cell line (HeLa) compared to the normal African green monkey kidney epithelial cell line (Vero) using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Materials and Methods:The Vero and HeLa cell lines were treated with various concentrations (1-300 μg/mL) of alkaloids for 48 h. Values for cytotoxicity measured by MTT assay were expressed as the concentration that causes a 50% decrease in cell viability (IC 50 ) (μg/mL). Results: Berberine and macranthine were the most active alkaloids. Salutaridine exhibited no cytotoxic activity against two types of cell lines. Dose-dependent studies presented IC 50 of 12.08 μg/mL and IC 50 of 71.14 μg/mL for berberine and IC 50 of 24.16 μg/mL and IC 50 of >300 μg/mL for macranthine on the HeLa cells and the Vero cells respectively. Conclusion:The degree of selectivity of the compounds can be expressed by its Selectivity Index (SI) value. High SI value (>2) of a compound gives a selective toxicity towards cancer cells (SI = IC 50 for normal cells/IC 50 for cancer cells). Two alkaloids showed significant SI values, which are 12.42 for macranthine and 5.89 for berberine. Hence, macranthine and berberine display potential to be further exploited in the discovery and development of new anticancer agents.

Cytotoxic Effects of Plant Sap-Derived Extracellular Vesicles on Various Tumor Cell Types

“…A high SI suggests that malignant tumor cells are more affected than normal cells, and indicates a promising cytotoxic effect. Usually, drugs with an SI > 2 are considered selective [66][67][68][69]. The SI of DM-EVs for malignant breast tumor cells compared with normal cells was about 2 and that of PD-EVs for skin cancer cells was about 5, which is higher than that of cisplatin.…”

Antimutagenic, antigenotoxic and antiproliferative activities of Fraxinus angustifolia Vahl. leaves and stem bark extracts and their phytochemical composition

“…Thus, IC 50 values were calculated by non-linear concentration/response regression model. Furthermore, selectivity index (SI) was calculated [34] to compare the antiproliferative activity observed on cancer cells with that of the human normal-like fibroblast cell line (Tel-COFS02MA, ATCC1 CRL 4005™ purchased from American Type Culture Collection, Milan, Italy). A selective toxicity towards cancer cells occurs when SI value is greater than 2.…”

Sitotoksisitas dan Induksi Apoptosis Ekstrak Etanol Teripang holothuria atra Jaeger, 1833 pada beberapa Sel Kanker

“…Berdasarkan National Cancer Institute, ekstrak dinyatakan aktif memiliki aktivitas antikanker apabila memiliki nilai IC 50 < 30 g/ml, moderate aktif apabila memiliki nilai 30 < IC 50 <100 g/ml dan tidak aktif apabila nilai IC 50 > 100 g/ml (Putram, Setyaningsih, Tarm an, & Nursid, 2017 (Demirgan et al, 2016). Sel normal yang digunakan adalah sel Vero.…”

“…Nilai SI>2,0 berarti bahwa suatu senyawa dianggap memiliki selektivitas yang tinggi. Semakin tinggi indeks selektivitas suatu senyawa terhadap sel, maka senyawa tersebut semakin selektif dalam mematikan atau menghambat pertumbuhan suatu sel kanker dengan efek yang semakin kecil terhadap sel normal (Demirgan et al, 2016). Berdasarkan nilai IC 50 dan nilai SI, maka sel T47D digunakan dalam penelitian berikutnya untuk mengetahui efek ekstrak teripang dalam kemampuannya menginduksi apoptosis.…”