TABLE 2.
Antitumor activity of TBMS-1.
| Tumor type | Cell lines/Model | Activity/mechanisms of action | Application | References |
|---|---|---|---|---|
| Lung cancer | NCI-H1299 cells | Overexpression of miR-126-5p inactivated the VEGF-A/VEGFR2/ERK signaling pathway to inhibit the activity of NCI-H1299 cells | In vitro | (Shi et al., 2018a; Shi et al., 2018b) |
| NCI-H1299 cells and NCI-H1975 cells | Disrupted the interaction between mitochondrial and lysosomal pathways leading to the killing of lung cancer cells | In vitro/in vivo | Wang et al. (2020a) | |
| A549 cells | Inhibited the proliferation and induced apoptosis of cells by increasing the Bax to Bcl-2 ratio, and decreasing COX-2 expression | In vitro | Zhang et al. (2011) | |
| A549 and PC9 cells | Decreased cell proliferation and expression of cell growth-associated proteins, such as p21, p15, and Cyc B1, upregulated expression of proapoptotic factors, Bax and cleavage of procaspase-3, downregulated expression of antiapoptotic factors, Mcl-1 and cIAP-1, and activated the MAPK-JNK signaling pathway | In vitro | Hao et al. (2015) | |
| NCL-H460 cells and NCL-H460 xenograft mice model | Stimulated the proteasomal degradation of VEGFR2 and Tie2, leading to inhibition of AKT/mTOR signaling | In vitro/in vivo | Gu et al. (2016) | |
| NCL-H460 cells | Exerted cytotoxicity in NCI-H460 lung cancer cells through nucleolar stress-induced p53/MDM2, mTOR, and NF-κB signaling pathways | In vitro | Lin et al. (2016) | |
| A549 cells | Increased the activity of Caspase-3, Caspase-9, and Parp to induce apoptosis | In vitro | Su et al. (2021) | |
| PGCL3 cells | Reduced the secretion and activity of MMP-2, and decreased the adhesion rate of laminin and fibronectin to influence the invasion and adhesion of PGCL3 cells | In vitro | Yu et al. (2008) | |
| Lewis lung cancer spontaneous metastasis mice model | Downregulated the expression of metastasis-promoting genes CD44v6 and ErBb-2, and upregulated the expression of metastasis-suppressing gene, nm23-H1 | In vivo | Wang et al. (2006a) | |
| A549/DDP cells | Upregulated the expression of p53 and Caspase-3, and reduced the ratio of Bcl-2/Bax to enhance the sensitivity of cancer cells to cisplatin | In vitro | Wang et al. (2020b) | |
| Nasopharyngeal cancer | CNE-2Z cells | Inactivated Bcl-2, activated Bax and MAPK to induce tumor cell apoptosis | In vitro | (Weng et al., 2003; Liu et al., 2007) |
| Oral cancer | SCC15 cells and CAL27 cells | Induced intrinsic apoptosis through the ERK1/2/Bcl-2/Caspase-9/Caspase-3/PARP pathway, and the extrinsic apoptotic by decreasing the expression of Caspase-3, Caspase-7, and Caspase-8, and inhibited metastasis by decreasing c-Myc and MMP-7 protein expression | In vitro | Wu et al. (2018) |
| Esophageal cancer | EC109 cells | Mitochondria-induced intrinsic apoptosis and p21/Cyc B1/cdc2 complex-related G2/M cell cycle arrest | In vitro | Xu et al. (2013) |
| Gastric cancer | BGC823 cells | Upregulated the expression of Bax and downregulated expression of Bcl-2 to increase the ratio of Bax to Bcl-2 | In vitro | Zhang et al. (2013) |
| Liver cancer | HepG2 cells | Promoted apoptosis signaling pathways and production of reactive oxygen species by regulating TNF-α, NF-κB, JNK, and p53 | In vitro | (Wang et al., 2011b; Yin et al., 2011) |
| HepG2 cells | Activated AMPK signaling pathway, increased the expression of Beclin 1, and LC3-Ⅱ/LC3-Ⅰ to induce autophagy | In vitro | Ruan et al. (2020) | |
| HepG2 cells | Reduced the expression and activity of MMP-2 and MMP-9 proteins in HepG2 cells to inhibit cell migration and invasion | In vitro | Zhong et al. (2016) | |
| Colorectal cancer | SW480 and HCT116 cells | Initiated autophagy by activating ROS/AMPK signaling and impaired autophagy flux by = inhibiting lysosomal proteolysis activity | In vitro | Yan et al. (2019) |
| SW480 and HCT-8 cells | Inhibited cell proliferation and invasion via suppressing the Wnt/β-catenin signaling pathway | In vitro | Bian et al. (2015) | |
| Glioblastoma | U87, LN229 cells and U87 xenograft mice model | Decreased the protein level of MET by increasing its ubiquitination degradation to inhibit proliferation, migration, and invasion of glioblastoma cells | In vitro/in vivo | Cao et al. (2019) |
| Glioma | U251 cells | Increased Bax/Bcl-2 and the concentration of ROS by promoting the release of cytochrome C and activation of Caspase-3 | In vitro | Jia et al. (2015) |
| U251 cells | Downregulated the expression of miR-21 and upregulated that of PDCD4 to induce cell apoptosis | In vitro | Jia et al. (2016) | |
| U251 cells | Upregulated the expression of FADD, Caspase-8, and Caspase-3 proteins to induce apoptosis | In vitro | Jia et al. (2014) | |
| U251 cells | Inhibited DNA synthesis and induced G2/M phase arrest by targeting the PI3K/Akt/p21 and the CDK1/Cyc B1 signaling cascades | In vitro | Cao et al. (2020) | |
| Cervical cancer | HeLa cells | Decreased mitochondrial membrane potential, increased Cytc and Bax/Bcl-2 | In vitro | (Ma et al., 2004; Wang et al., 2005; Wang et al., 2006b) |
| HeLa cells | Induced the depletion of mitochondrial transmembrane potential and activated the Caspase pathway to cause cell death. It activated the UPR signaling pathway to induce cytotoxic effects | In vitro | Xu et al. (2009) | |
| HeLa cells | Activated AMPK to initiate autophagy, blocked autophagic flux, and increased levels of damaged autophagy lysozyme to aggravate cytotoxic activity | In vitro | Feng et al. (2018) | |
| Ovarian cancer | A2780/DDP cells | Downregulated ERK1/2 and upregulated p38 signaling pathway to increase the inhibitory effect of cisplatin on A2780/DDP cells proliferation | In vitro | (Liu et al., 2011a; Liu et al., 2011b) |
| SKOV-3 cells | Increased Bax expression by inducing phosphorylation of p38 and MAPK and decreased Bcl-2 levels by reducing the phosphorylating of ERK1/2 to activate Caspase-3 | In vitro | Chen et al. (2012) | |
| Breast cancer | MDA-MB-231 cells and MDA-MB-231 xenograft mice model | Inhibited the binding ability of NF-κB to the promoter of CXCR4 to reduce the expression of CXCR4 and metastasis of breast cancer cells | In vitro/in vivo | Peng et al. (2016) |
| MDA-MB-231 cells | Induced autophagy through the PI3k-Akt-mTOR signal pathway | In vitro | (Jiang et al., 2019; Liu et al., 2019) | |
| Choriocarcinoma | JEG-3 cells | Induced mitochondrial dysfunction and regulated the p38/MAPK, ERK1/2 and PI3K/Akt signaling pathways | In vitro | Huang et al. (2011) |
| Prostate carcinoma | DU145 cells | Induced mitochondrial apoptosis by increasing ROS generation, mitochondrial dysfunction, endoplasmic reticulum stress, Bcl-2 family protein and cleaved caspase-3 expression, and activating ASK-1 and its downstream targets p38 and JNK. | In vitro | Yang et al. (2016) |
| Skin cancer | SCL-1 cells | Downregulated circ_0000376 to promote the expression of miR-203 to inhibit the proliferation, migration, and invasion of skin cancer cells, and accelerate cell apoptosis | In vitro | Wang et al. (2021a) |
| Leukemia | HL-60 cells | Decreased the expression of Cyc B1 and blocked the cell cycle | In vitro | Hu et al. (2003) |
| HL-60 cells | Induced the differentiation of HL-60 cells to more mature cells with the functional characteristics of granulocytes | In vitro | Yu et al. (1996) | |
| Melanoma | A375 cells | Blocked the cell cycle in G2/M phase and induced apoptosis of A375 cells by downregulating Bcl-2 and upregulating Bax | In vitro | Rasul et al. (2012) |
| MV3, A375 cells and MV3 xenograft mice model | Inhibited cell proliferation through rapid hyperactivation of MEK1/2-ERK1/2 cascade by promoting PTP1B | In vitro/in vivo | Du et al. (2020) | |
| A375 cells and B16 melanoma cells xenograft mice model | Bound to mTOR kinase to suppress activation of mTORC1 leading to disruption of PD-1/PD-L1 interaction and enhanced cytotoxic killing of cancer cells by T cells by decreasing the abundance of PD-L1 | In vitro/in vivo | Liu et al. (2021) |