Chinese Herbs Interfering with Cancer Reprogramming Metabolism

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]