Table 2.
Polyphenols and histone modifications
| Dietary Agent | Plant source | Molecular mechanism |
Histones and Gene targets |
In vitro model | In vivo model | Concentration | References |
|---|---|---|---|---|---|---|---|
| 3,3-diindolylmethane | Broccoli | ↓ HDAC expression |
COX-2 | Colon; Breast | Mouse: colon cancer | 10–60 µM | (196–198) |
|
6-methoxy-2E,9E- humuladien-8-one |
Ginger | HDAC inhibitor | Breast | 1.25 µM | (234) | ||
| Allicin | Garlic | Unknown | H4 acetylation | Erythroleukemia | 2–200 µM | (176) | |
| Allyl mercaptan | Garlic | HDAC inhibitor | H3/H4 acetylation p21WAF1 |
Erythroleukemia; Liver; Colon |
Rat: liver | 2–500 µM (100mg/kg) |
(173–175;177;178) |
| Anacardic acid | Cashew nuts | HAT inhibitor | H3K9 and H3K14 deacetylation NF-kB activation |
Leukemia; Plasmodium; Cervix; Embryonic kidney; Breast; Lymphoma; Prostate; Lung; Esophageal; Skin |
3–200 µM | (138;139;153–160) | |
| Biochanin A | Soy | HDAC inhibitor | RARβ | Esophageal; Prostate | 20–100 µM | (115) | |
| Butein | Varnish Tree | Induction of SIRT1 activity |
Cervix | Drosophila | 100 µM | (203;204) | |
| Caffeic acid | Coffea | HDAC inhibitor | Cervix; Colon | 1–2.54 mM | (152;235) | ||
| Catechin | Green tea | HAT inhibitor | Lymphocytes | 100 µM | (165) | ||
| Chlorogenic acid | Coffea | HDAC inhibitor | Cervix | 0.375 mM | (152) | ||
| Cinnamic acid | Cinnamon | HDAC inhibitor | Cervix; Colon | 1–2 mM | (152;235) | ||
|
Coumaric/ Hydroxycinnamic acid |
Cinnamon | HDAC inhibitor | Cervix; Colon | 1–2 mM | (235) | ||
| Curcumin | Turmeric | HAT and HDAC inhibitor |
H3/H4 deacetylation GATA4, EOMES, GZMB, PRF1 |
Cervix; HIV; Hepatoma; Leukemia; Prostate; Brain; Lymphoma; Lymphocytes; |
Plasmodium falciparum; Herpes virus Mouse: epilepsy Rat: diabetes, heart failure |
6.25–135 µM (0.3–75 mg/kg) |
(134–152) |
| Daidzein | Soy | HDAC inhibitor | Histones acetylation RARβ |
Esophageal; Prostate | 12.8–100 µM | (115;199) | |
| Diallyl disulfide | Garlic | HDAC inhibitor | H3/H4 acetylation p21WAF |
Erythroleukemia; Leukemia; Liver; Colon; Prostate; Fibroblasts |
Rat: colon cancer | 20–200 µM, (42–200 mg/kg) |
(173;175;177;179– 183;236) |
| Dihydrocoumarin | Yellow Sweet Clover | SIRT1 and SIRT2 inhibitor |
p53 acetylation | Lymphoblastoid cell line | 0.75–50 mM | (220) | |
| Epicatechin | Green tea | HAT inhibitor | Lymphocytes | 100 µM | (165) | ||
| Epicatechin gallate | Green tea | HAT inhibitor | Lymphocytes | 100 µM | (165) | ||
| Epigallocatechin | Green tea | HAT inhibitor | Lymphocytes; Colon | 100 µM | (165;166) | ||
|
Epigalocatechin-3- gallate |
Green tea | HAT inhibitor HMT inhibitor |
H3/H4 acetylation H3K27 tri-methylation NF-κB, IL-6, BMI-1, EZH2, SUZ12 |
Lymphocytes; Colon; Keratinocytes; Prostate |
5–100 µM | (105;165–167) | |
| Equol | Soy | HDAC inhibitor | H2A/H2B/H3/H4 acetylation | Drosophila | 12.8 µM | (199) | |
| Fisetin | Poison ivy | SIRT1 activator | Cervix; Drosophila | 100 µM | (203;204) | ||
| Flavone | Feijoa | HDAC inhibitor | Histones acetylation p16, p21, TRAIL |
Myeloid leukemia | 170–340 µM | (237) | |
| Garcinol | Garcinia | HAT inhibitor | Global gene expression down- regulation |
Leukemia; Cervix; Lymphocytes; HIV |
5–100 µM | (139;156;161– 164;238) |
|
| Genistein | Soy | HAT activator HDAC inhibitor |
H2A/H2B/H3/H4 acetylation p21, p16, PTEN, CCLD, p53, FOXA3, SIRT1, BTG3 hTERT, RARβ |
Esophageal; Prostate; Breast; Renal |
5–100 µM | (115;116;118;119;199–201) | |
| Isoliquiritigenin | Liquorice | SIRT1 activator | Cervix; Drosophila | 100 µM | (203;204) | ||
| Isothiocyanates | Broccoli, wasabi | HDAC inhibitor | H3/H4 acetylation, p21, GSTP1 |
Prostate; Erythroleukemia; Leukemia; Prostate |
20–100 µM | (128;174;193–195) | |
| Luteolin | Parsley, celery | SIRT1 activator | Cervix | 100 µM | (203) | ||
| Piceatannol | Grapes, blueberries | SIRT1 activator | Cervix; Drosophila | 100 µM | (203;204) | ||
| Polyphenon B | Black and green tea | ↑ HDAC1 expression |
Rat: liver cancer | 0.05 % | (168) | ||
| Quercetin | Citrus, apple, berries | SIRT1 activator HAT inhibitor |
IP-10, MIP-2 | Cervix; Drosophila; Small intestine; |
Mouse: bowel inflammation |
100 µM | (203;204;219) |
| Resveratrol* | Grapes, wine, eucalyptus |
SIRT1 activator | TNFα, IL-8, RBP | Cervix; Endothelial; Embryonic kidney; Macrophages; Lung; Liver; Cardiomyocytes; |
Yeast; Drosophila; Mouse: colon cancer; Rat: lung cancer |
10–200 µM | (203–212;239–242) |
| S-allylmercaptocysteine | Garlic | HDAC inhibitor | H3/H4 acetylation | Erythroleukemia; Colon | 20–250 µM | (176;178) | |
| Sanguinarine | Opium poppy | Histone methylation inhibitor HAT inhibitor |
H3K9/H3K4 demethylation H3/H4 deacetylation |
Liver; Cervix | 5–75 µM | (221) | |
| Silibinin | Milk thistle | ↑ histone acetylation |
H3/H4 acetylation p21, p27, CASP3, CASP9. |
Hepatoma | 120–240 µM | (243) | |
| Sulforaphane | Broccoli | HDAC inhibitor | H3/H4 acetylation RARβ, HBD-2, p21,BAX |
Esophageal; Prostate; Colon; Kidney; Breast |
Mouse: colon cancer; prostate cancer xenografts Human: blood |
15–25 µM (443 µg/kg, 68g) |
(115;166;185–191) |
| Theophylline | Black and green tea | HDAC activator | Alveolar macrophages; Epithelial cells; Blood monocytes |
10 µM | (169–172) | ||
| Ursolic Acid | Basil | HDAC inhibitor | Histone acetylation | Leukemia | 5–20 µg/ml | (244) |
*
This table only provides selected publications for resveratrol as a SIRT1 inhibitor.