Table 1.

Bioactive compounds isolated from Chinese herbs interfere with cancer metabolic reprogramming.

Bioactive compounds	Chinese herbs	Cancer model	Metabolic regulation	Potential mechanisms	References
Berberine	Coptis chinensis (Huang lian)	Breast cancer MCF-7 cells	Mitochondrial OXPHOS; glycolysis; fatty acid synthesis	Inhibits the phosphorylation of PKM2 and PFKP and regulates ACC and ACL pathways	[31]
Chrysophanol	Rheum palmatum (Da huang)	Human liver cancer Hep3B and J5 cells	Mitochondrial OXPHOS; ATP generation	Decreases levels of GST, SOD (Cu), SOD (Mn), and catalase and increases LDH activity	[32, 33]
Curcumin	Curcuma longa (Jiang huang)	ESCC EC109 cell; human colorectal cancer HCT116 and HT29 cells; human hepatoma HepG2 cells	Glycolysis; fatty acid synthesis	AMPK-dependent metabolic regulation; downregulates the activity of hexokinase II (HKII) and the expression of HKII and FAS	[34–36]
Ginsenoside 20(S)-Rg3	Panax ginseng (Ren shen)	Ovarian cancer cells	Glycolysis	Targets the STAT3/HK2 pathway	[37]
Neoalbaconol	Albatrellus confluens (Di hua jun)	Nasopharyngeal cancer C666-1 cells	Glucose consumption; ATP generation	Targets the PDK1-PI3K/Akt signaling pathway	[38]
Oleanolic acid	Ligustrum lucidum (Nv zhen); Olea europaea (Qi dun guo)	Human prostate carcinoma PC-3 cells; human breast cancer MCF-7 cells; human hepatoma HepG2 cells	Aerobic glycolysis; lipid metabolism; mitochondrial OXPHOS	Induces PKM2 to PKM1 switch, inhibits the phosphorylation of mTOR, and PPARγ, decreases expression of c-Myc-dependent hnRNPA1 and hnRNPA1, activates AMPK, and elevates COX-2 expression	[39–41]
Oridonin	Rabdosia rubescens (Dong ling cao)	Human colorectal cancer SW480 and SW620 cells; uveal melanoma OCM-1 and MUM2B cells	Fatty acid synthesis; cellular levels of palmitate and stearic acid	Inhibits FAS and SREBP1 mRNA and protein expression	[42, 43]
Osthole	Cnidium monnieri (She chuang zi)	Human ovarian cancer SKOV3 cells	Fatty acid synthesis	Inhibits the phosphorylation of Akt and mTOR and downregulates FASN expression	[44]
Prosapogenin A	Veratrum nigrum (Li lu)	Breast cancer MCF-7 cells	Glycolysis	Reduces the expression of STAT3, GLUT1, HK, and PFKL mRNA	[45]
Quercetin	Folium Mori (Sangye); Radix Bupleuri (Chai hu)	HepG2 cells; Dalton's lymphoma mice	Fatty acid synthesis; glycolysis	Decreases FASN expression, reduces NADPH levels, and downregulates PI3K-AKT-p53 pathway	[46, 47]
Shikonin	Lithospermum erythrorhizon (Zi cao)	Human macrophage U937 cells; human breast cancer SK-BR-3 cells; human promyeloblastic leukemia HL60 cells	Mitochondrial dysfunction; cellular lactate production; glucose consumption	Targets TrxR1 and inhibits PKM2 activity	[48–50]
Silibinin	Silybum marianum (Shui fei ji)	Transgenic adenocarcinoma of the mouse prostate; human colorectal carcinoma SW480 cells	Glucose content and uptake; lactate, citrate, phosphatidylcholine, and cholesterol levels; mitochondrial OXPHOS	Inhibits PIK3CA-AKT-MTOR and activates MAP2K1/2-MAPK1/3 pathways	[51, 52]
Tetrandrine	Stephania tetrandra (Fen fang ji)	Prostatic cancer PC-3 cells; renal carcinoma 786-O cells	Glucose uptake	Induces AMPK phosphorylation and OXPHOS impairment	[29]
Wogonin	Scutellaria baicalensis (Huang qin)	Resistant human colon cancer HCT116 cells	Glucose uptake; lactate generation	Decreases the expression of HKII, PDHK1, LDHA, and HIF-1α and inhibits PI3K/Akt signaling pathway	[53]
EGCG	Green tea (Lv cha)	Human pancreatic cancer MIA PaCa-2 cells; human tongue carcinoma cells; MCF-7 cells; MDA-MB-231 cells; HT-29 cells; A549 cells; LNCaP cells; lung cancer xenografts	Lactate production, anaerobic glycolysis; glucose consumption and uptake; fatty acid metabolism	Inhibits HK2 expression, LDHA activity, FAS activity, and FASN activity; mediates the insulin-response via GLUT1, GLUT4; and GLUT12, and activates AMPK pathway	[54–59]
Oroxylin A	Oroxylum indicum (Mu hu die)	HepG2 cells; MDA-MB-231 cells; MCF-7 cells; A549 cells; female athymic BALB/c nude mice	Glucose uptake; lactate generation; ROS accumulation; ATP generation; glycolysis	Suppresses mRNA levels of PDK1, LDHA, and HK II; inhibits HIF-1α expression and stability; promotes SOD2 gene expression and SIRT3 activation; inactivates the c-Src/AKT/HK II pathway	[60–63]