Oxidative Medicine and Cellular Longevity / 2017 / Article / Tab 1

Review Article

Lysosomes as Oxidative Targets for Cancer Therapy

Table 1

The use of lysosomotropic agents as therapeutics in cancer.

Lysosomotropic AgentModelEffective dosesReference

SiramesineIn vitroBreast cancer lines: Mcf-7, Mcf-10A, and MDA-MB-4681–10 μM[18, 19, 30]
Cervix carcinoma cell lines: HeLa and ME-1801–10 μM
Colorectal cancer cell lines: Hkh2 and HCT1168 μM
Fibroblast cell line: NIH3&3-SrcY527F4–10 μM
Fibrosarcoma cell lines: WEHI-S and R45 μM
Mast cells (primary)2–20 μM
Osteosarcoma cell line: U2OS1–10 μM
Ovarian carcinoma cell line: SKOV38–10 μM
Prostate cancer cell lines: PC3 and Du145-P5–10 μM
In vivoWEHI-R4 in BALB-c mice25–100 mg/kg/d
Mcf-7 in SCID mice30–100 mg/kg/d
PC3-MDR in SCID mice30 mg/kg

DesipramineIn vitroBreast cancer lines: Mcf-7 and Mcf-10A25 μM[19]
Cervix carcinoma cell line: HeLa25–50 μM
Colorectal cancer cell lines: Hkh2 and HCT1168 μM
Fibroblast cell line: NIH3&3-SrcY527F8–25 μM
Osteosarcoma cell line: U2OS25–50 μM
Ovarian carcinoma cell line: SKOV375–100 μM
Prostate cancer cell lines: PC3 and Du145-P5–10 μM
In vivoMcf-7 in SCID mice30 mg/kg, 2×/wk

NortriptylineIn vitroBreast cancer line: Mcf-725–50 μM[19]
Cervix carcinoma cell line: HeLa25–50 μM
Colorectal cancer cell lines: Hkh2 and HCT1168 μM
Fibroblast cell line: NIH3&3-SrcY527F10–25 μM
Osteosarcoma cell line: U2OS25–50 μM
Ovarian carcinoma cell line: SKOV340–60 μM
Prostate cancer cell lines: PC3 and Du145-P40–80 μM

AmlodipineIn vitroBreast cancer line: Mcf-725–50 μM[19]
Fibroblast cell line: NIH3&3-SrcY527F10–30 μM
Ovarian carcinoma cell line: SKOV337.5–50 μM
Prostate cancer cell lines: PC3 and Du145-P40–50 μM

TerfenadineIn vitroBreast cancer line: Mcf-725–50 μM[19]
Colorectal cancer cell lines: Hkh2 and HCT1168 μM
Fibroblast cell line: NIH3&3-SrcY527F2.5–5 μM
Ovarian carcinoma cell line: SKOV36–8 μM
Prostate cancer cell lines: PC3 and Du145-P1–10 μM
In vivoMcf-7 in SCID mice10 mg/kg, 2×/wk

MefloquineIn vitroAML cells (primary)5–15 μM[14]
AML cell lines: HL60, KG1A OCI-AML2, and TEX1–10 μM
APL cell line: NB45–7 μM
CML cell line: K5626–10 μM
Dendritic cells (primary)25–50 μM
Erythroleukemic cell line: OCI-M27–9 μM
Gastric cancer cell lines: AGS, Hs746T, MKN45, MKN74,
NCI-N87, SNU1, SNU16, TCC1, YCC10, and YCC11
0.5–5 μM
Lymphosarcoma cell line: MDAY-D23–5 μM
Macrophage/monocyte cell lines: THP-1 and U9375–18 μM
Oral cancer cell line: KVP20C5 μM
Prostate cancer cell line: PC35–40 μM
In vivoK562, MDAY-D2, and OCI-AML2 in NOD-SCID mice50 mg/kg
Primary AML cells in NOD-SCID mice100 mg/kg/d
YCC or SNU1 in SCID miceUnknown
PC3 in C57B1/6J mice200 μg/25 mg

PrimaquineIn vitroBreast cancer cell line: Mcf-77 μM[58]
Colon cancer cell lines: Caco-2 and HT-2940–70 μM
Oral cancer cell line: KVB20C50–75 μM

AtovaquoneIn vitroOral cancer cell line: KVB20C2–12.5 μM[59]

CiprofloxacinIn vitroCervix carcinoma cell line: HeLa10 μg/ml[34]
Colorectal cancer cell line HCT1161–5 μM

PterostilbeneIn vitroAML cell lines: HL-60, MV4-11, and OCI-AML225–75 μM[58]
Macrophage cell lines: THP-1 and U93725–75 μM
Melanoma cell line: A37510–50 μM

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