Celastrol-mediated autophagy regulation in cancer

Haroon, Muhammad; Kang, Sun Chul

doi:10.1186/s13765-020-00565-3

Applied Biological Chemistry

Table 1 Anticancer activities of celastrol in vivo

From: Celastrol-mediated autophagy regulation in cancer

Type of cancer	Cell lines & animal model	Dosage & administration	Mechanism	Results	Ref
Acute promyelocytic leukaemia	HL-60 cell implanted xenograft in nude mice	2 mg/kg/day (i.g.) for 21 days	DHODH-induced uridine metabolism disruption/p53/mitochondrial pathway of apoptosis	Apoptosis of APL cells	[97]
Breast cancer	Macrophages (RAW264.7), Female BALB/c mice	10 mg/kg, (i.p.) injection once a day for 14 days	Inhibited the expression of M2-like specific genes, such as MRC1, Arg1 and ameliorated STAT6 phosphorylation	Prevented cancer metastasis	[98]
Colon cancer	Azoxymethane (AOM) and DSS induced colon cancer in C57BL/6 J mice	2 mg/kg/day by gavage for 14 weeks	Downregulation of mutated p53 and p-p53 proteins, oncogenic proteins β-catenin, and PCNA and suppressed epithelial-mesenchymal transition (EMT)	Ameliorates ulcerative colitis-related colorectal cancer (UC-CRC)	[34]
Gastric cancer	AGS cell xenograft in mice	1–2 mg/kg/day (i.g.) for 12 days	Suppression of phosphorylation of AKT, mTOR and S6K	Induction of autophagy and apoptotic cell death	[52]
Glioma	ECV-304 cells, SHG-44 xenograft model	0.2 µg/ml, SC administration for 5 days a week for 4 weeks	Lowered the density of tumor microvessel (MVD) and decreased the level of VEGFR-1 and VEGFR-2 expression	Inhibited cell migration and angiogenesis	[99]
Hepatocellular carcinoma	DEN-induced HCC in rat	(10 mg/kg) for 6 days every week (i.g.) for 16 weeks	Suppressed the expression of the MDM2 protein and inhibited anti-apoptotic Bcl-xl and Bcl-2	Induction of apoptotic cell death	[100]
Hepatocellular carcinoma	Human HCC, HepG2 and Hepa3B cell lines in mice	2 mg/kg (i.p.) injection twice a week	CXCR4 expression was diminished	Induced cell apoptosis in vitro	[101]
Lung cancer	A549 or H1975 cell xenograft in Balb/c nude mice	1 or 3 mg/kg/days, or 5 mg/kg, twice/week (i.p.) for 3 weeks	Inhibit CIP2A-Akt pathway	Inhibited cell proliferation and induced apoptosis	[36]
Melanoma	B16 cell xenograft in C57BL/6 J mice	1–3 mg/kg (i.g.) once a day for 20 days	Inhibition of the PI3K/Akt/mTOR signaling pathway	Inhibits growth and induced apoptotic cell death	[27]
Osteosarcoma	HOS cell xenograft in nude mice	1–2 mg/kg/day (i.p.) for 7 days	Induction of JNK activation and ROS generation	Autophagic cell death	[28]
Pancreatic cancer	PANC-1 cell xenograft in nu/nu athymic female mice	3 mg/kg (i.p.) for 70 days	Disturbing the HSP90-CDC37 interaction	Antitumor activity	[102]

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