Table 1.
Antitumor activity of SIN when used alone.
| Activity | Cell Type or Model In Vitro (Effective Concentrations or IC50 Values) | Mechanism of Action | In Vivo | Year | Ref. | |
|---|---|---|---|---|---|---|
| Dose (mg/kg) | Therapeutic Effect | |||||
| Cytotoxicity | IL-1β-activated Hs701.T (IC50 = 0.125 mM) | ↓: JAK3, EDG4, IL-13, PCTAIRE-3, ERF-1, HHR6A, HSP27, Daxx, TNF-A, COL1A2, IL-6, SATB, IFITM1, TNFRII, JAG2, MMP-13, and PLG. | NR | 2006 | [19] | |
| Invasion and migration inhibition | THP-1 (effect was notable at 0.05 and 1mM concentrations) | ↓: CD147, MMP-2, and MMP-9. | NR | 2009 | [20] | |
| Cytotoxicity | NCI-H460 (inhibition rate was 85.89% at 607.2 μM) | ↑: Caspase-3/-9, depolarized cells, ΔΨm disruption, cytoplasm cytochrome c, and Bax/BcL-2 ratio. | NR | 2010 | [21] | |
| Cytotoxicity | PC-3 and DU-145 (IC50 was 121.4 μM for both cell lines) | ↓: PGE, COX-2, NF-κB, andp-NF-κB (p65). | NR | 2011 | [22] | |
| Cytotoxicity | NCI-H460 (607.1 μM) | ↓: AKT and ERK1/2. | NR | 2012 | [23] | |
| Cytotoxicity Invasion and migration inhibition |
MDA-MB-231 and 4T1 (SIN displayed cytotoxicity at 1 mM and showed invasion and migration inhibition at 0.25 and 0.5 mM) | ↑: CUEDC2. ↓: NF-κB binding to IκB, nuclear translocation of NF-κB, vimentin, tendine-C, CCK, MCP-1, IL-11, NF-κB activation, and p-IKK, IL-4/miR-324-5p. |
NR | 2015 | [24] | |
| Cytotoxicity | A549 (0.25 mM of SIN led to apoptosis) | ↑: E-cadherin. ↓: JAK2, STAT3, p-STAT3, Snail, N-cadherin, and vimentin. |
NR | 2016 | [25] | |
| Antitumor (invasion and metastasis inhibition) | HOS and U2OS cells (50–400 µM concentrations were selected for both cell lines) | ↑: TIMP-1 and TIMP-2 ↓: CXCR4, p-STAT3, VEGF, CD147, MMP-2, MMP-9, VEGF, RANKL, and p-NF-κB (p65) expression. |
150 mg/kg | ↓: RANKL-mediated osteolysis, cortical bone destruction, and number of osteoclasts. | 2016 | [26] |
| Antitumor | U87 and SF 767 (0.125–0.5 mM concentrations were selected for both cell lines) | ↓: Akt-mTOR. ↑: JNK, EB, and lysosome. |
75, 150 mg/kg | ↑: Cathepsin B/D. ↓: Tumor volume and weight, p62. |
2017 | [27] |
| Antitumor | B16-F10 (25–100 mM) | ↑: Beclin l, Bax, caspase-3, and LC3II/LC3I ratio. ↓: p-p62/SQSTML, PI3K/Akt/mTOR, and BcL-2. |
100 mg/kg | ↓: Tumor volume and weight, Ki67, and PCN. | 2018 | [28] |
| Antitumor | U87 and U251 (16 mM for both cell lines) | ↑: p53 expression. ↓: SIRT1 expression. |
100 mg/kg | ↓: U87 transplanted tumors growth. | 2018 | [29] |
| Antitumor | MDA-MB-231 (0.5 mM) | ↓: MMP-2, vimentin, IL-11, NF-κB, and it-mediated Shh pathways. | 15 mg/kg | ↑: Survival time of mice with lung metastatic breast cancer. ↓: Lung metastasis of breast cancer. |
2018 | [30] |
| Cytotoxicity | MDA-MB-231 and MCF-7 (1–16 μM concentrations for both cell lines) | ↑: p16, cleaved caspase-3/-9, PDCD-4, and miR-29. ↓: PCNA, Cyclin D1, CDK4, p-JNK, and p-MEK. |
NR | 2019 | [31] | |
| Cytotoxicity | MKN45 and SGC7901 (20 μM) | ↑: Bax, cleaved caspase-3, MMP-9, vimentin, AMPK, Wnt/β-catenin, and miR-204. ↓: Cyclin D1 and BcL-2. |
NR | 2019 | [32] | |
| Antitumor | NSCLC (25–100 μM concentrations were selected, but IC50 value was not reported) | ↓: p-Histone H3 (Ser10), Akt, and downstream kinase S6, HK. | 40 mg/kg | ↓: Tumor volume and weight. | 2020 | [33] |
| Cytotoxicity | Hep3B and HepG2 (2 and 4 mM for both cell lines) | ↓: p-AMPK, p-STAT3, and MARCH. | NR | 2021 | [34] | |
| Cytotoxicity | MDA-MB-231 SP (0.2–1 mM) | ↓: N-cadherin, vimentin, and MMP-2, MMP-9, p-PI3K, p-Akt, and p-mTOR. | NR | 2021 | [35] | |
| Cytotoxicity | HeyA8 (IC50 = 1.56 mM) | ↓: CDK1, p-CDK (Thr161), and p-Histone H3 (Ser10). | NR | 2021 | [36] | |
| Antitumor | SK-Hep1 (0.125–1 mM) | ↑: Cleaved caspase-9 and cleaved caspase-3. ↓: I3K/AKT1 pathway, PI3K, p85α, AKT1, BcL-2, pro-caspase-9, and pro-caspase-3. |
75, 150 mg/kg | ↓: Tumor volume and weight. | 2022 | [38] |
| Antitumor | HeLa (0.25–1 mM) | ↑: Caspase-3. ↓: Cells activity. |
70, 140 mg/kg | ↑: Tumor cell apoptosis. ↓: Tumor growth, activity of TrxR, and ROS. |
2022 | [39] |
| Cytotoxicity | Breast cancer SP cells (0.75 mM) | ↑: MiR-340-5P. ↓: SIAH2/HIF-1α pathway and epithelial interstitial transformation. |
NR | 2022 | [40] | |
| Antitumor | HT-29, HCT-116, and SW-480 (2.5 mM for these three cell lines) | ↓: IL-1β and TNF-α at mRNA and protein levels; ↑: CPT1A and LPCAT3. |
120 mg/kg | ↓: Rectal neoplasia production, length of colon, number and volume of tumors, colonic mucosal injury, necrosis, submucosal edema and inflammatory cell infiltration improvement, and colitis-related tumor. | 2022 | [41] |
NR: None reported. ↓: Decrease or inhibition. ↑: Increase or induction. If IC50 values were reported, we displayed them in the second column. If IC50 values were not reported, we only displayed effective concentrations in the second column.