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Table 2 TCM targeting ferroptosis against cancer

From: A review on the research progress of traditional Chinese medicine with anti-cancer effect targeting ferroptosis

Classification

Medicine

Mechanisms

Concentration in vivo or in vitro

Literature

TCM prescriptions

Shuganning injection

Increased HO-1, LIP, and ROS

MDA-MB-231 (10.47 μg/ml); Xenograft (112.5 mg/kg)

[75]

TCM prescriptions

Fuzhengkang'ai decoction

Inhibited GPX4, increased the level of Fe2+

H1299 (0.75 mg/ml); Xenograft (31 g/kg)

[11, 76]

TCM prescriptions

Yiqi Huayu decoction

Influenced ACSL4 and p53

AGS (11.20 mg/ml)

[77]

TCM

Scutellaria barbata

Inhibited GPX4 and SLC7A11

Up-regulated ACSL4

SMMC-7721, HepG2, Huh7 (44.26、42.19、52.01 μg/ml); Xenograft (140 g/10 g)

[78, 79]

TCM

ACP

Down-regulated GPX4 and SLC7A11

HGC-27; Xenograft in zebrafish embryos (90, 180 mg/ml)

[80, 81]

TCM extracted parts

The ethanol extract of CNC

Decreased GPX4、SLC7A11, FTH1

Increased P53、ACSL4

HCT116 (92.37 μg/ml); Xenograft (1.2, 2.4, or 4.8 g/kg/)

[83]

TCM extracted parts

LBP

Decreased SLC7A11, GPX4

MCF-7, MDA-MB-231(> 4.0 mg/ml)

[82]

TCM extracted parts

Huaier aqueous extract

Increased the level of ROS

NCI-H1299

[84]

Terpenes

Artemisinin

Promoted degrading ferritin in the lysosome, produced free iron;

Induced ROS

Hela (50 μM)

[87, 90]

Terpenes

Ursolic acid

Activated autophagic degradation of ferritin, induced ferrous ions overload

HOS, 143B (35 μM UA and 20 μM CIS)

[91]

Terpenes

Tagitinin C

Activated the PERK-Nrf2-HO-1 pathway to increase lipid peroxidation

HCT116

[92]

Terpenes

Triptolide

Inhibited Nrf2 and SLC7A11

HK1, FaDu

[93]

Terpenes

Cucurbitacin B

Decreased GPX4

CNE1 (0.016 μM); Xenograft (0.5,1 mg/kg)

[95]

Terpenes

Glycyrrhetinic acid

Activated NOX, inhibited SLC7A11, decrease GPX4

MDA-MB-231 (71.07 μM)

[94]

Terpenes

Ophiopogonin B

Inhibited GPX4 and SLC7A11

AGS, NCI-N87 (21.32 μM); Xenograft (50 mg/kg)

[96]

Terpenes

Curcumenol

By lncRNA H19 targeting miR-19b-3p to increase FTH1

H1299, H460; Xenograft (200 mg/kg)

[10]

Terpenes

Oleanolic acid

Induced ACSL4 and TFR1, inhibited FTH1 and GPX4

Hela; Xenograft (40,80 mg/kg)

[97]

Terpenes

β-Elemene

Induced the product of ROS, consumed GSH

HCT116 (125 μg/ml); Xenograft (50 mg/kg)

[98]

Flavonoids

Chrysin

Increased the level of ROS, degrading FTH1

PANC-1

[99]

Flavonoids

Baicalin

Decreased FTH1, increased ROS

5637; Xenograft (200 mg/kg)

[100]

Flavonoids

Nobiletin

Inhibited Keap/Nrf2/HO-1 pathway, down-regulated GPX4

SK-MEL-28 (53.63 μM)

[102]

Flavonoids

Ginkgetin

Increased transferrin, caused lipid peroxidation, and improved the level of LIP

A549

[101]

Flavonoids

Quercetin

Degrading ferritin

HepG2, Hep3B, HCT116 (25,50 μM)

[103, 104]

Flavonoids

Robustaflavone A

Decreased Nedd4, increased the expression of VDAC

MCF-7 (11.89 μM)

[105, 106]

Flavonoids

Auriculasin

Increased the level of ROS

HCT116, SW480 (5 μM)

[107]

Phenols

Curcumin

Decreased NCOA4, FTH1, and p53

A498, 786-O (sunitinib-resistant)

[108]

Phenols

6-Gingerol

Inhibited USP14, increased the level of ROS and Fe2+

A549; Xenograft (0.5 mg/kg)

[109]

Phenols

Gallic acid

Inhibited GPX4 and SCL7A11, increased TFR1

HCT-116, Caco-2

[110]

Quinones

Dihydroisotanshinone I

Inhibited GPX4

MCF-7 (5,10 μM), A549 (20 μM); Xenograft (30 mg/kg)

[111, 112]

Quinones

Tanshinone IIA

Up-regulated p53, decreased GSH and cysteine, increased ROS

BGC-823 (2.8 μM); Xenograft in NOD-SCID mice (50 mg/kg)

[113]

Quinones

Cryptotanshinone

Down-regulated GPX4 and FPN

A549 (20 μM)

[114, 115]

Polyprenylated xanthone

Gambogic acid

Regulated p53/SLC7A11/GPX4 pathway, disrupted redox homeostasis, increased ROS

A375, PCAP-1 (185 nM)

[116, 117]

Steroids

Bufotalin

Inhibited GPX4

A549 (4.21 μM); Xenograft (5,10 mg/kg)

[118]

Alkaloids

Matrine

Decreased GPX4, SLC7A1, increased TFR2 and the levels of ROS, Fe2+

HCT116 (6.1 mM); Xenograft (0.32 mmol/kg)

[119]

Steroids

Ruscogenin

Regulated TFR and FPN, caused the accumulation of iron

BxPC-3 (7.32 μM); Xenograft (5,10 mg/kg)

[120]

Dibenzyl compound

Erianin

Acting on calcium-regulatory protein calmodulin, up-regulated Fe2+

H460 (50 nM); Xenograft (100 mg/kg)

[121]

Polyacetylenes

Atractylodin

Inhibited GPX4, increased ACSL4 and TFR1

Huh7 (22.36 μM), Hccm (59.71 μM)

[122]

Alkaloids

Piperlongumine

Increased the levels of ROS

MIAPaCa-2, PANC-1 (14 μM)

[123]

Sesquiterpenes

Dihydroartemisinin

Decrased GCLC, GPX4 and HO-1

HepG2 (16.16 μM); Xenograft (40 mg/kg)

[124]

Sesquiterpenes

Artesunate

Induced the product of ROS, decreased GPX4, consumed GSH

KTCTL-26 (17.79 μM)

[125]

Terpenes

Compound a2

Decreased GPX4 protein and mRNA, induced the accumulation of Fe2+

MGC-803; Xenograft (5, 10, 20 mg/kg)

[126]