Table 6.
The active components from CHMs for cancer aerobic glycolysis inhibition and their mechanism.
| CHMs | Active components | Mechanism | Targets | Cancer model | Routes | References |
|---|---|---|---|---|---|---|
| Glycyrrhiza glabra (guang guo gan cao) | Glabridin | Inhibition of glucose transport and lactate formation | Downregulation of the GLUT-1 and LDH-A |
In vitro MDA-MB-231 cells |
\ | [354] |
| Pulsatilla chinensis (bai tou weng) | Quercetin | Inhibition of glucose transport and lactate formation | Downregulation of the GLUT-1, LDH-A and pyruvate kinase M2 (PKM2) |
In vivo Balb/c mice xenografted breast cancer (MCF-7 cells) In vitro MCF-7 and MDA-MB-231 cells |
Intraperitoneal injection | [355] |
| Oleanolic acid | Blockade of HIF-1α-mediated aerobic glycolysis | Reduction of the nuclear abundance of yes-associated protein |
In vitro MKN-45 and SGC-7901 cells |
\ | [356] | |
| Salvia miltiorrhiza (dan shen) | Rosmarinic acid | Suppression of glucose consumption and lactate generation | Inhibition of the expression of HIF-1α |
In vitro HCT-8, HCT-116, Ls174-T, and Lovo cells |
\ | [357] |
| Birch bark (hua shu pi) | Betulinic acid | Inhibition of lactate production, glucose uptake and extracellular acidification rate | Suppression cancer glycolysis via caveolin-1/NF-κB/c-Myc pathway and upregulation of glucose-regulated protein 78 |
In vivo Mammary-tumor-prone transgenic mice/ Balb/c mice lung colonization breast cancer (MDA-MB-231 cells) In vitro MDA-MB-231, BT-549 and MCF-7 cells |
Intraperitoneal injection | [349,358] |
| Cortex pseudolaricis (tu jing pi) | Pseudolaric acid B | Inhibition of glucose uptake, and ATP generation | p53 mutation or inactivation |
In vitro H1299 cells |
\ | [359] |
| Rabdosia rubescens (dong ling cao) | Oridonin | Inhibiting glucose uptake and reducing lactate export | Downregulation of the protein levels of GLUT1 and monocarboxylate transporter 1 (MCT1) |
In vivo Balb/c mice xenografted colorectal cancer (SW480 cells) In vitro p53-mutated colorectal cancer cells |
Intraperitoneal injection | [360] |
| Radix Dichroae (chang shan) | Halofuginone | Inhibition of glycolysis and lipid biosynthesis | Inhibition of protein kinase B/mammalian target of rapamycin complex 1 (Akt/mTORC1) pathway |
In vivo Balb/c nude mice xenografted colorectal cancer (HCT116 cells) In vitro SW480, HCT116, SW620, HT29 and DLD-1 cells |
Intraperitoneal injection | [361] |
| Radix liquiritiae (gan cao) | Licochalcone A | Inhibition of the glucose consumption and lactate production | Inhibition of HK2 expression and blockade of the Akt signaling pathway |
In vivo Balb/c nude mice xenografted gastric cancer (MKN45 cells) In vitro MKN45 and SGC7901 cells |
Intraperitoneal injection | [362] |
| Salvia miltiorrhiza (dan shen) | Tanshinone IIA | Dysregulation of gluconeogenesis | Suppression of the expression of lactate dehydrogenase B chains and malate dehydrogenase 1 |
In vitro CRL-1739 cells |
\ | [363] |
| Inhibition of glycolysis | Downregulation of glucose-6-phosphate isomerase (GPI) | |||||
| Cortex fraxini (qin pi) | Esculetin | Inhibition of the rates of glucose consumption and lactate production | Alteration of the conformation of glycolysis-related enzymes, phosphoglycerate kinase 2 (PGK2), glycerol-3-phosphate dehydrogenase (GPD2), and GPI |
In vivo Balb/c mice xenografted liver cancer (H22 cells) In vitro HepG2 cells |
Intraperitoneal injection | [364] |