Table 3.
Overview on the biological activities of chromanols linked to carcinogenesis.
| Apoptosis/Necrosis mediated | Proliferation | Viability | ||||||
|---|---|---|---|---|---|---|---|---|
| PARP-1 | Casp8 | Casp9 | Casp3 | Casp7 | ||||
| α-TOH | ||||||||
| PARP-1 CL MDA‐MB‐231 MCF-7 cells 23 µM no induction (Loganathan et al., 2013) |
Casp8 A MiaPaCa-2 50 µM no induction (Husain et al., 2011) |
Casp3 A MiaPaCa-2 50 µM no induction (Husain et al., 2011) |
Casp7 CL SW 480 cells HCT-116 100 µM no induction (Campbell et al., 2006) |
MDA-MB-435 > 2000 µM MCF-7 cells 290 µM no inhibiton (Guthrie et al., 1997) |
MDA-MB-435 230 µM no inhibition (Nesaretnam et al., 1995) |
h_cc cells 200 µM no reduction (Campbell et al., 2006) |
||
| PARP-1 CL SW 480 cells HCT-116 100 µM no induction (Campbell et al., 2006) |
Casp8 CL SW 480 cells HCT-116 100 µM no induction (Campbell et al., 2006) |
Casp3 CL SW 480 cells HCT-116 100 µM no induction (Campbell et al., 2006) |
m_NB2A cells inhibition h_ SaOs-2 cells no inhibition 50 µM (Azzi et al., 1993) |
Du-145 cells LNCaP cells CaCo-2 cells 25 µM inhibition SaOs-2 cells no inhibition (Gysin et al., 2002) |
MCF-7, MCF-7-C3 50 µM no reduction (Birringer et al., 2003) |
|||
| PC-3 HTB-82 50 µM inhibition (Galli et al., 2004) |
MCF-7 cells 23 µM no inhibition (Nesaretnam et al., 1998) |
|||||||
| MDA-MB-231 MCF-7 cells 46.5 µM no inhibition (Loganathan et al., 2013) |
HT-29 100 µM inhibition (Campbell et al., 2006) |
|||||||
| β-TOH | ||||||||
| Du-145 cells LNCaP cells SaOs-2 cells 25 µM inhibition (Gysin et al., 2002) |
m_NB2A cells h_ SaOs-2 cells 50 µM no inhibition (Azzi et al., 1993) |
MCF-7, MCF-7-C3 50 µM no reduction (Birringer et al., 2003) |
||||||
| γ-TOH | ||||||||
| PARP-1 CL SW 480 cells HCT-116 100 µM induction (Campbell et al., 2006) |
Casp8 CL SW 480 cells HCT-116 100 µM induction (Campbell et al., 2006) |
Casp3 CL SW 480 cells HCT-116 100 µM induction (Campbell et al., 2006) |
Casp7 CL SW 480 cells HCT-116 100 µM induction (Campbell et al., 2006) |
PC-3 cells HTB-82 cells 1 µM inhibition (Galli et al., 2004) |
h_cc cells 100 µM inhibition (Campbell et al., 2006) |
HCT-116, HT-29 50 µM no inhibition (Jang et al., 2016) |
h_cc cells 100 µM reduction (Campbell et al., 2006) |
|
| Du-145 cells LNCaP cells CaCo-2 cells SaOs-2 cells 25 µM inhibition (Gysin et al., 2002) |
tumor count m_BALB/c 0.1% diet reduction (Jiang et al., 2013) |
PC-3, LNCaP 50 µM inhibition (Jiang et al., 2012) |
MCF-7, MCF-7-C3 50 µM no reduction (Birringer et al., 2003) |
|||||
| δ-TOH | ||||||||
| MCF-7, MCF-7-C3 50 µM no reduction (Birringer et al., 2003) |
HCT-116 inhibition HT-29 no reduction 50 µM (Jang et al., 2016) |
|||||||
| α-T3 | ||||||||
| PARP-1 CL, MDA‐MB‐231, MCF-7 cells 23.5 µM induction (Loganathan et al., 2013) |
Casp8 A MiaPaCa-2 50 µM induction (Husain et al., 2011) |
Casp3 A MiaPaCa-2 50 µM induction (Husain et al., 2011) |
MDA-MB-435 211.9 µM MCF-7 cells 14.1 µM inhibition (Guthrie et al., 1997) |
m_B16(F10) 110 µM inhibition (He et al., 1997) |
SCID mice 200 mg/kg no reduction (Husain et al., 2011) |
MiaPaCa-2, 50 µM no reduction (Husain et al., 2011) |
||
| PARP-1 CL MiaPaCa-2 50 µM no induction (Husain et al., 2011) |
MDA-MB-231 22.5 µM MCF-7 cells 26.1 µM inhibition (Loganathan et al., 2013) |
MCF-7 23.5 µM no inhibition (Nesaretnam et al., 1998) |
MCF-7, MCF-7-C3 50 µM no reduction (Birringer et al., 2003) |
|||||
| β-T3 | ||||||||
| MiaPaCa-2, 50 µM reduction (Husain et al., 2011) |
||||||||
| γ-T3 | ||||||||
| PARP-1 CL, MDA‐MB‐231, MCF-7 cells 24.2 µM induction (Loganathan et al., 2013) |
Casp8 A MiaPaCa-2 50 µM induction (Husain et al., 2011) |
Casp9 CL PC-3, LNCaP 20 µM induction (Jiang et al., 2012) |
Casp3 A MCF-7, MCF-7-C3 50 µM induction (Birringer et al., 2003) |
Casp7 CL PC-3, LNCap 30/90 µM induction (Yap et al., 2008) |
SKBR3, BT474 5 µM inhibition (Alawin et al., 2016) |
rh_RLh-84 50 µM inhibition (Sakai et al., 2004) |
MiaPaCa-2, 50 µM reduction (Husain et al., 2011) |
PC-3, LNCaP 20 µM reduction (Jiang et al., 2012) |
| PARP-1 CL MiaPaCa-2 50 µM induction (Husain et al., 2011) |
Casp8 CL PC-3, LNCap 30/90 µM induction (Yap et al., 2008) |
Casp9 CL PC-3, LNCap 30/90 µM induction (Yap et al., 2008) |
Casp3 A MiaPaCa-2 50 µM induction (Husain et al., 2011) |
m_B16(F10) 20 µM inhibition (He et al., 1997) |
PC-3 32 µM inhibition (Yap et al., 2008) |
|||
| PARP-1 CL PC-3, LNCaP 20 µM induction (Jiang et al., 2012) |
Casp8 CL rh_RLh-84 25 µM induction (Sakai et al., 2004) |
Casp3 CL PC-3, LNCap 30/90 µM induction (Yap et al., 2008) |
MDA-MB-231 11.4 µM MCF-7 cells 15.4 µM inhibition (Loganathan et al., 2013) |
MCF-7 14.6 µM inhibition (Nesaretnam et al., 1998) |
||||
| PARP-1 CL PC-3, LNCap 30/90 µM induction (Yap et al., 2008) |
Casp3 CL rh_RLh-84 25 µM induction (Sakai et al., 2004) |
MDA-MB-435 73.2 µM MCF-7 cells 4.9 µM inhibition (Guthrie et al., 1997) |
||||||
| δ-T3 | ||||||||
| PARP-1 CL, MDA‐MB‐231, MCF-7 cells 25.2 µM induction (Loganathan et al., 2013) |
Casp8 A MiaPaCa-2 50 µM induction (Husain et al., 2011) |
Casp3 A MiaPaCa-2 50 µM induction (Husain et al., 2011) |
MDA-MB-435 226.8 µM MCF-7 cells 5 µM inhibition (Guthrie et al., 1997) |
PC-3 41 µM LNCap 75 µM inhibition (Yap et al., 2008) |
MiaPaCa-2, 50 µM reduction (Husain et al., 2011) |
|||
| PARP-1 CL MiaPaCa-2 50 µM induction (Husain et al., 2011) |
m_B16(F10) 10 µM inhibition (He et al., 1997) |
MCF-7 25.2 µM inhibition (Nesaretnam et al., 1998) |
||||||
| MDA-MB-231 MCF-7 cells 17 µM inhibition (Loganathan et al., 2013) |
||||||||
| α-T-13'-OH (tocopherol derived) | ||||||||
| PARP-1 CL HepG2 cells 20 µM no induction (Birringer et al., 2010) |
Casp9 CL HepG2 cells 20 µM no induction (Birringer et al., 2010) |
Casp3 CL HepG2 cells 20 µM no induction (Birringer et al., 2010) |
Casp7 CL HepG2 cells 20 µM no induction (Birringer et al., 2010) |
m_C6 cells 10 µM reduction (Mazzini et al., 2009) |
THP-1 ΜΦ 100 µM no reduction (Wallert et al., 2014a) |
|||
| α-T-13'-COOH (tocopherol derived) | ||||||||
| PARP-1 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
Casp9 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
Casp3 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
Casp7 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
THP-1 ΜΦ 7.4 µM reduction (Wallert et al., 2014a) |
HepG2 cells 13.5 µM reduction (Birringer et al., 2010) |
|||
| δ-T-13'-OH (tocopherol derived) | ||||||||
| PARP-1 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
Casp9 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
Casp3 CL HepG2 cells 20 µM no induction (Birringer et al., 2010) |
Casp7 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
THP-1 100 µM no reduction (Schmölz et al., 2017) |
HepG2 cells 50 µM no reduction (Birringer et al., 2010) |
|||
| δ-T-13'-COOH (tocopherol derived) | ||||||||
| PARP-1 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
Casp9 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
Casp3 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
Casp7 CL HepG2 cells 20 µM induction (Birringer et al., 2010) |
HCT-116 HT-29 8.9/8.6 µM reduction (Jang et al., 2016) |
HepG2 cells 6.5 µM reduction (Birringer et al., 2010) |
|||
| PARP-1 CL HCT-116 20 µM induction (Jang et al., 2016) |
Casp9 CL HCT-116 20 µM induction (Jang et al., 2016) |
m_C6 cells 10 µM reduction (Mazzini et al., 2009) |
HCT-116 HT-29 8.9/8.6 µM reduction (Jang et al., 2016) |
|||||
| THP-1 11.1 µM reduction (Schmölz et al., 2017) |
||||||||
| α-T-3'-COOH (tocopherol derived) | ||||||||
| PC-3 cells HTB-82 cells 1 µM inhibition (Galli et al., 2004) |
m_C6 cells 10 µM reduction (Mazzini et al., 2009) |
|||||||
| γ-T-3'-COOH (tocopherol derived) | ||||||||
| PC-3 cells HTB-82 cells 1 µM inhibition (Galli et al., 2004) |
m_C6 cells 10 µM reduction (Mazzini et al., 2009) |
|||||||
| δ-T3-13′-COOH | ||||||||
| PARP-1 CL HCT-116 20 µM induction (Jang et al., 2016) |
Casp9 CL HCT-116 20 µM induction (Jang et al., 2016) |
m_C6 cells 10 µM reduction (Mazzini et al., 2009) |
HCT-116 HT-29 16/17 µM reduction (Jang et al., 2016) |
|||||
| SCA E | ||||||||
| PARP-1 CL h_HL-60 25 µM induction (Heo et al., 2011) |
Casp9 CL h_HL-60 25 µM induction (Heo et al., 2011) |
Casp3 CL h_HL-60 25 µM induction (Heo et al., 2011) |
h_HL-60 50 µM inhibition (Heo et al., 2011) |
|||||
| α-AC | ||||||||
| HepaRG 10 µM no reduction (Richomme et al., 2017) |
||||||||
The effects of the respective compounds on carcinogenesis have been divided into apoptosis-mediated (PARP-1, caspases 3, 7, 8, and 9) activities as well as activities affecting proliferation and viability. The content of each cell of the table in the apoptosis section is constructed as follows (read from top to bottom): (i) investigated parameter; (ii) cell type model used for investigation; (iii) used concentration of the respective compound; (iv) observed effect on the studied parameter; (v) reference. The content of each table cell in the proliferation as well as viability section is constructed as follows (read from top to bottom): (i) cell type model used for investigation; (ii) used concentration of the respective compound; (iii) observed effect on the studied parameter; (iv) reference. The following abbreviations are used: A, activity; A549, adenocarcinomic human alveolar basal epithelial cells; BALB/c mice, albino laboratory-bred strain of the house mouse; LNCap, androgen-sensitive human prostate adenocarcinoma cells; Casp, caspase; MCF-7-C3, caspase 3 reconstituted MCF-7 cells; CL, cleavage; cc, colon cancer; MDA-MB-23, epithelial human breast cancer cell line; NB2A, fast-growing mouse neuroblastoma cell line; h, human; MCF-7, human breast cancer cell line established by Michigan Cancer Foundation-7; SKBR3, human breast cancer cell line isolated by the Memorial Sloan–Kettering Cancer Centere; BT-474, human breast carcinoma ductal cell line; SaOs-2, human cell line derived from primary osteosarcoma; SW-480, human cell line established from a lymph node metastasis; HCT-116, human colon cancer cell line; HT-29, human colorectal adenocarcinoma cell line; CaCo-2, human epithelial colorectal adenocarcinoma cells; THP-1, human immortalized monocyte-like cell line; HL-60, human leukemia cell line; HepG2, human liver cancer cell line; MiaPaCa-2, human pancreatic cancer cell line; Du-145, human prostate cancer cell line; PC-3, human prostate cancer cell line; B16(10), mouse skin melanoma cells; m, murine; m_C6, murine glial cancer cell line; PARP-1, poly (ADP-Ribose)-polymerase 1; HTB-82, rhabdomyosarcoma cell line; rh_RLh-84, rat hepatoma cell line; HepaRG, terminally differentiated hepatic cells derived from a human hepatic progenitor cell line.
All results obtained from in vivo studies are marked in gray.