TABLE 3.
The anti-cancer effects of jatrorrhizine and its complexes.
| Cancer type | Cells or tumor models | Application | Dosage | Suppressive effect | Mechanisms | References |
|---|---|---|---|---|---|---|
| Melanoma | C8161 human metastatic melanoma cell line | In vitro | 80, 160, 320 μmol/L, 48 h | Inhibition of cell proliferation and neovascularization | Cell cycle arrest, and upregulation of p21 and p27, p53 | Liu et al. (2013) |
| Matrigel plug assay in BALB/C nude mice | In vivo | 50 μg, 14 days | Reduced numbers of blood vessels | |||
| Colorectal cancer | SW480 human colon cancer cell line | In vitro | 25–200 μg/ml, 24 and 48 h | Inhibition of cell proliferation and cell viability | Singh et al. (2016) | |
| SW620 colorectal cancer cell line | In vitro | 100 μM | Inhibition of cell proliferation | Formation of complexes with oncogene KRAS promoter NHE G-quadruplex | Wen and Xie (2017) | |
| Human colorectal carcinoma cell lines HCT-116 and HT-29 | In vitro | IC50 of HCT-116: 6.99 ± 0.29 μM, 72 h | Suppression of cell growth and proliferation, inhibit migration and invasion | Promotion of apoptosis, induced nuclear morphological changes, block of cell cycle in S phase, repressed ∆Ψm, reduced β-catenin, F-actin and N-cadherin, and increased GSK-3β and E-cadherin | Wang et al. (2019a) | |
| IC50 of HT-29: 5.46 ± 0.13 μM, 72 h | ||||||
| 5, 10, 15 μM | ||||||
| 24, 48, and 72 h | ||||||
| HCT-116 nude mice xenograft model | In vivo | 5 mg/kg, 4 weeks | Inhibition of tumor growth and metastasis | Reduced tumor volume and weight, upregulation of GSK-3β and E-cadherin, and downregulation of β-catenin, F-actin and N-cadherin | ||
| Liver cancer | HepG2 and HCCLM3 liver cancer cells | In vitro | 0.5–16.0 µM, 48 h | Inhibition of cell viability, proliferation, invasion and migration | Promotion of apoptosis, downregulation of miR-221-3p and miR-15b-5p expression, and upregulation of Axin2 protein | Deng and Wan (2021) |
| Breast cancer | MDA-MB-231 triple-negative breast cancer cell line, MCF-7 estrogen receptor positive breast carcinoma cell line, and 4T1 mouse mammarycarcinoma cells | In vitro | 10, 20, 30 μM | Inhibition of cell proliferation | Repressed ∆Ψm, suppressed Wnt/β-catenin signaling and EMT expression via targeted TNIK, upregulation of GSK-3β and E-cadherin, and downregulation of β-catenin, F-actin and N-cadherin, up-regulate Bax, downregulation of Bcl-2, decreased Procaspase-3, Procaspase-8, Procaspase-9 and PARP | Sun et al. (2019) |
| 24 and 48 h | ||||||
| Orthotopic 4T1 tumour bearing mouse | In vivo | 2.5 mg/kg b.w | Inhibition of the growth and metastasis | Reduced tumor growth rate and improve survival rate, upregulation of GSK-3β and E-cadherin, downregulation of TNIK, p-TNIK, F-actin, β-catenin, and N-cadherin | ||
| 5 mg/kg b.w | ||||||
| 4 weeks | ||||||
| Thyroid cancer | SW1736, BHP7-13, and 8305C cell lines | In vitro | 1.5, 3, 6, 12, 24, 48 μM, 48 h | Inhibition of cell proliferation | Cell cycle arrest, increased accumulation of ROS, promoted the levels of cleaved caspase-3 and p-H2AX, suppressed pS6, p-ERK1/2, p-4E-BP1, p-AKT, KU70, ERCC1, RAD51 and KU80, downregulation of the PI3K/AKT/mTOR signaling pathway and promotion of DNA damage | Lu et al. (2020) |
| Female athymic nude mice | In vivo | 24.0 mg/kg, 14 days | Inhibition of tumor growth | Increased pH2AX and acetylated histone H3, histone H4 and cleaved caspase-3 | ||
| HeLa cancer | Human cervical (HeLa) cell line | In vitro | Pt1: IC50 = 15.01 ± 1.05 nM | Inhibition of cell proliferation | Targeting p53 and telomerase, repressed telomerase related-proteins (c-myc and hTERT), promoted DNA damage (activation of 53BP1, H2A.X, TRF1, and TRF2), decreased ∆Ψm, sub-G1 phase arrest and cell apoptosis | Qin et al. (2019b) |
| Pt2: 1.00 ± 0.17 nM | ||||||
| Human cervical (HeLa)-xenograft model | In vivo | Pt2: 2.0 mg/kg per 2 days, 21 days | Inhibition of tumor growth | |||
| Bladder cancer | Human bladder T-24 tumor cell | In vitro | Pt1:100.0 nM, 6 h | Inhibition of cell proliferation | Induced TRF1- and TRF2-telomeres damage, decreased hTERT and c-myc levels, increased ROS, cytochrome c, caspase-9, caspase-3, Apaf-1, inhibited Bcl-2, and cell cycle arrest (suppression of cyclin D1 and CDK2) | Qin et al. (2019a) |
| Pt2: 10.0 nM, 6 h | ||||||
| T-24 xenograft mouse models (nude mice) | In vivo | Pt1: 2.0 mg/kg per 2 days | Inhibition of tumor growth | |||
| Pt2: 2.0 mg/kg per 2 days |