| Target | Macroautophagy/autophagy[1] |
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| In Vitro | CA-5f (0-40 μM, 6 hour) concentration- and time-dependently elevates the level of LC3B-II (a marker to monitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs[1]. CA-5f (20 μM, 6 hours) inhibits the degradation of autophagosomes when treated alone or in combination Bafilomycin A1 (100 nM) or Chloroquine (30 μM) in A549 cells and HUVECs[1]. CA-5f (20 μM) neither impairs the hydrolytic function nor the quantity of lysosomes[1]. CA-5f (20 μM, 96 hours) inhibits the growth of A549 cells, and less cytotoxic to normal HUVECs[1]. Cell Viability Assay[1] Cell Line: A549, HUVECs Concentration: 20 μM Incubation Time: 96 hours Result: Exhibited more cytotoxicity against A549 cells compared with normal HUVECs. Western Blot Analysis[1] Cell Line: A549 cells and HUVECs Concentration: 0-40 μM Incubation Time: 6 hours Result: Elevated LC3B-II (a marker to monitor autophagy) and SQSTM1 protein levels in a concentration- and time-dependent manner. |
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| In Vivo | CA-5f (40 mg/kg, i.p., every 2 days for up to 30 days) is well tolerated, and potently inhibits the growth of tumor in nude mice bearing A549 lung cancer cells[1]. CA-5f (40 mg/kg, i.p.) suppresses autophagic flux and induces apoptosis in nude mice bearing A549 lung cancer cells[1]. Animal Model: Nude mice bearing A549 lung cancer cells[1] Dosage: 40 mg/kg Administration: Injected via caudal vein, every 2 days for up to 30 days Result: Significantly suppressed tumor volume and weight in mice, increased the number of apoptotic cells in mice. |
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| References | Autophagy. 2019 Mar;15(3):391-406. |
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