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. 2022 Dec 31;24(1):728. doi: 10.3390/ijms24010728

Table 1.

Summary of studies (from 2017 to 2022) on sirtuin activators and inhibitors (1–7).

Sirtuin Organism Modulator Effect Reference
ACTIVATORS
Sirtuin 1 Human and Drosophila melanogaster ginsenosides (Panax ginseng Meyer extract)
  • -

    promoting mitochondrial biosynthesis;

  • -

    modification of the SIRT1 pathway, neuro- and cardioprotective effects;

 [156]
Mammalian cells (Mus musculus) resveratrol
  • -

    increased SIRT1 and AMPK activity, improved cardiac function in mice;

  • -

    reduced expression of parasitic cells;

 [157]
cucurbitacin E glucoside (CuE)
  • -

    inhibition of the NF-ĸB/NLRP3 signaling pathway;

  • -

    enhancing the SIRT1/Nrf2/HO-1 pathway, suppressing oxidative stress in liver cells in mice;

 [158]
quercetin
  • -

    SIRT1 increasing activity and PKM2 inhibition;

 [159]
Rattus norvegicus resveratrol
  • -

    reducing oxidative stress and reducing the level of cardiac biomarkers;

  • -

    activation of SIRT1 and protection of heart cells by reducing hyperlipidemia;

 [160]
Humans 1,4-dihydropyridine (DHP)
  • -

    activation of SIRT1 in the cells of the nucleus pulposus, protection in osteoarthritis of the spine;

 [161]
Sirtuin 2 Drosophila melanogaster food nitrites
  • -

    SIRT1 and 2 activators, regulation of metabolism;

 [162]
Human
(HepG2 cells)		 resveratrol
  • -

    SIRT2 activation through the Prx1 factor, antioxidant effect in the aging process;

 [163]
Sirtuin 3 Rattus rattus theacrine (1,3,7,9-tetramethyluric acid)
  • -

    non-toxic effect, reduction of liver fibrosis and fatty liver in rats by SIRT3 activating;

 [164]
Mus musculus dexmedetomidine
  • -

    upregulation of SIRT3, reduction of mitochondrial damage caused by ischemic kidney injury;

 [165]
Human oroxylin A
  • -

    cardioprotective effect by increasing the activity of SIRT3 in myocardial cells while preventing mitochondrial dysfunction in cardiac myocytes;

 [166]
Retama monosperma (L.) Boiss extract
  • -

    upregulation of SIRT3 in human HaCaT cells, treatment of skin scarring.

 [167]
Sirtuin 4 Mus musculus resveratrol
  • -

    upregulation of SIRT4 in cells (prolonged exposure), protective effect against excitotoxicity.

 [168]
Sirtuin 5 Mus musculus dioscin
  • -

    downregulation Of Mir-145-5p expression with upregulation of SIRT5 activity;

  • -

    reduction of oxidative stress;

 [169]
resveratrol
  • -

    recovery of cellular metabolism after subarachnoid hemorrhage.

 [170]
Sirtuin 6 Mus musculus glicyryzine
  • -

    anti-aging effect, upregulating SIRT6 in 24-month-old mice with cranial osteolysis;

 [171]
UBCS039
  • -

    SIRT6 overexpression, treatment of lung injury in mice by promoting M2 bone marrow-derived macrophage;

 [172]
Gami-Yukmijihwang-Tang extract
  • -

    regulation of SIRT6 pathways, prevention of histone H3 lysine 56 acetylations.

 [173]
Sirtuin 7 Bombyx mori resveratrol
  • -

    upregulation of SIRT7;

  • -

    activation of the SIRT7-FoxO-GST pathway;

 [174]
INHIBITORS
Sirtuin 1 Sprague Dawley rats EX-527
  • -

    EX-527 mediates in the p53-SIRT1 pathway, regulation of germ cell apoptosis Cr(VI)-induced;

 [43]
Rattus rattus
  • -

    decrease of sirt1 activity, memory impairment in rats, oxidative stress as the response to prior quercetin stimulation;

 [175]
  • -

    SIRT1 may be linked to morphine addiction in a rat model, and its inhibition could be a potential therapeutic strategy;

 [176]
Bone marrow cells-Mus musculus sirtinol
  • -

    inhibiting the activity of sirtuin 1 enhances the effects of astaxanthin, antioxidant and anti-inflammatory effects;

 [177]
Anser domesticus nicotinamide
  • -

    inhibition of SIRT1 activity, increased cell proliferation in primary hepatocytes, and involvement in the FoxO1 process.

 [178]
Sirtuin 1&2 hepatocellular carcinoma cells EX-527 & cambiol
  • -

    SIRT1 and 2 inhibitors increased the effectiveness of sorafenib treatment targeting HCC cells;

  • -

    reduction of MRP3 and BCRP expression;

 [179]
colorectal carcinoma HCT 116 (CCL-247) cell line BZD9L1
  • -

    SIRT1 nad SIRT2 inhibitor, anti-cancer activity through the p53 pathway;

 [180]
Sirtuin 1–3 murine Neuroblastoma cell line arekoline (Areca catechu extract)
  • -

    higher ability to inhibit the activity of sirtuins 1–3 than nicotinamide;

 [181]
Sirtuin 2 MCF-7 human breast cancer cell line thiadiazole derivatives
  • -

    new potential SIRT2 inhibitors marked as ST29 and ST30. ST29 showed antiproliferative activity, and ST30 was cytotoxic;

 [154]
Sirtuin 3 mass spectrometry of SIRT3 ampicillin trihydrate
  • -

    SIRT3 inhibitor, no additional information;

 [37]
Sirtuin 4 Human nicotinamide
  • -

    SIRT4 inhibition by homologous modeling and docking of NAD+;

 [182]
Sirtuin 5 fluorogenic peptide substrates and human sirtuins TW-37
  • -

    slight inhibition of SIRT5 activity;

 [183]
molecular docking 4-((4-(4-acetamidophenyl)thiazol-2-yl)amino)-2-hydroxybenzoic acid
  • -

    strong inhibition of SIRT5 activity, enhanced stability of inhibitors;

 [184]
Sirtuin 6 articular chondrocytes from human EX-527
  • -

    downregulation of SIRT6 with oxidative stress formation;

 [185]