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. 2021 Jun 9;476(10):3785–3814. doi: 10.1007/s11010-021-04201-6

Table 5.

In vitro studies on antidiabetic and cardioprotective effects of turmeric and turmeric-derived bioactive compounds

Disease/bioactivity Model Treatment Dose Main outcomes Reference
Diabetes
 High glucose-induced insulin resistance Rat insulinoma cell line INS-1 Curcumin 5–15 μM

⬆ Expression of:

insulin, GSIS, GCK, PDX-1, GLUT2;

⬆ Phosphorylation of:

IR, IRS1, PI3K, Akt

 [32]
 High glucose-induced oxidative stress and pancreatic β-cell apoptosis Min-6 mouse pancreatic β-cells Curcumin 1–10 μM

⬇ ROS, MDA, ⬆ SOD levels;

⬇ CHOP, ⬆ PGC-1α;

⬇ p-ERK1/2

 [30]
 Leptin-stimulated increase in intracellular glucose Rat hepatic stellar cells (HSCs) and immortalized human hepatocytes Curcumin 20 μM

⬇ Glucose level;

⬇ GLUT4 translocation to membrane;

⬇ Phosphorylation of:

IRS-1, PI3K, Akt;

⬆ Glucokinase activity;

⬆ G6P levels

 [94]
 Akt signaling pathway and glucose uptake 3T3-L1 adipocytes Curcumin

10–75 μM

(dose response);

50 μM

(time response)

[Dose-dependent]

⬇ Akt protein levels;

⬇ GLUT4 plasma membrane expression;

⬇ Glucose uptake;

⬆ LC3-II protein;

⬆ LC3-II/LC3-I ratio

 [95]
 Glucose uptake in GLUT1-expressing cells L929 mouse fibroblast cells, HK2 human kidney cells, immortalized human corneal-limbal epithelial (HCLE) cells Curcumin 25–200 μM

[Dose-dependent]

⬇ 2DG uptake (all three cell types);

⬇ Cytochalasin B binding (L929 cells)

 [96]
 Glucagon-like peptide-1 secretion GLUTag L cells Curcumin 25 μM

⬆ GLP-1 secretion

(the effect diminished by GW1100)

 [31]
 Human adipocyte differentiation and peroxisome proliferator-activated receptor gamma (PPAR-γ) ligand-binding activity Human preadipocytes

Turmeric extract (ethanol), curcumin, DMC, BDMC,

ar-turmerone

Turmeric extract:

2–20 μg mL−1

Others:

2–5 μg mL−1

[Dose-dependent]

⬆ adipocyte differentiation

(turmeric extract);

⬆ PPAR-γ ligand-binding activity

(all treatments)

 [101]
 Human adipocyte differentiation and PPAR-γ ligand-binding activity Human preadipocytes

Turmeric extracts (ethanol: E-ext; hexane: H-ext; ethanol extraction from hexane extraction residue: HE-ext), curcumin, DMC, BDMC,

ar-turmerone

[Adipocyte differentiation]

E-ext: 2–20 mg L−1

[GAL4-PPAR-γ chimera assay]

Turmeric ext:

5–10 mg L−1

Others:

2–5 mg L−1

[Dose-dependent]

⬆ adipocyte differentiation

(E-ext);

⬆ PPAR-γ ligand-binding activity

(all treatments)

 [102]
 Sterol regulatory element-binding protein (SREBP) pathway

Luciferase-expressing cancer cells Huh-7/SRE-Luc,

rat heptaocytes CRL-1601

 Curcumin

0.1–40 μM

(Huh-7/SRE-Luc)

10 μM

(CRL-1601)

[Dose-dependent]

⬇ Luciferase activity

(in Huh-7/SRE-Luc cells);

⬇ Intracellular cholesterol, TG;

⬇ Expression of mRNA:

SREBP-1, SREBP-2;

⬇ Expression of endogenous nuclear:

SREBP-1, SREBP-2;

(in CRL-1601 cells)

 [107]
 Inhibition of α-amylase and α-glucosidase

Chemical assays:

α-amylase inhibition,

α-glucosidase inhibition

Turmeric oil from fresh (FTO) and dried (DTO) rhizomes;

ar-tumerone

 0.1–100 μg mL−1

Inhibition of:

α-amylase,

α-glucosidase,

(ar-tumerone > DTO > FTO > acarbose)

 [99]
 In vitro antidiabetic potential

Chemical assays:

α-amylase inhibition,

α-glucosidase inhibition,

antiglycation activity

 Turmeric rhizome extracts using ethyl acetate (EtOAc Ex), methanol (MeOH Ex), and water (Water Ex) 0–600 μg mL−1

Inhibition of:

α-amylase

(EtOAc Ex > MeOH Ex > acarbose > Water Ex),

α-glucosidase

(EtOAc Ex > MeOH Ex > Water Ex > acarbose)

Antiglycation activity:

(EtOAc Ex > MeOH Ex > Water Ex)

 [97]
 Inactivation of human pancreatic α-amylase (HPA) Chemical assays (α-amylase inhibition, α-glucosidase inhibition) BDMC 2–15 μg mL−1 Inhibition of HPA (IC50 = 0.025 mM; Acarbose IC50 = 0.015 mM) [98]
CVD
 Monocyte adhesion to TNF-α-stimulated endothelial cells Primary human umbilical vein endothelial cells (HUVECs), human monocytic cell line U937 Curcumin 0.1–1 μM

[Dose-dependent]

⬇ Monocyte adhesion to HUVECs;

⬇ VCAM-1 gene expression

 [123]
 Cholesterol accumulation in foam cells Mouse macrophage cell line J774.A1 Curcumin 5–40 μM

[Dose-dependent]

⬇ oxLDL-induced intracellular cholesterol accumulation;

⬇ Dil-oxLDL binding;

⬇ SR-A expression;

⬆ SR-A turnover;

⬆ SR-A–ubiquitin–VCP complex formation;

⬆ ApoAI-mediated cholesterol efflux;

⬆ ABCA1 expression

(Curcumin’s effect on ABCA1 abolished by LXRα inhibition.)

 [28]
 Lipid accumulation in monocyte/macrophage Human acute monocytic leukemia THP-1 cells Curcumin 1–20 μM

[Dose-dependent]

In THP-1 and THP-1 differentiated macrophages:

⬆ Lipid accumulation;

⬆ CD36 and aP2 protein expression;

⬆ FOXO3a phosphorylation

 [125]
 TLR4 expression and NF-κB activation Mouse peritoneal macrophages (MPMs) Curcumin 10–25 μM

[Dose-dependent]

⬇ TLR4 mRNA level;

⬇ NF-κB activation

 [27]
 Hypoxia-induced cardiomyocyte apoptosis Mouse cardiac myocytes (MCMs) Curcumin 10 μM

⬆ miR-7a/b expression;

⬇ SP1 expression and cell apoptosis

(the effect diminished by miR-7a/b inhibitors)

 [129]
 TLR2 and MCP-1 expression Neonatal rat cardiomyocyte Curcumin 10 μM

⬇ TLR2 and MCP-1

(otherwise by TNF-α, PGN and H/R)

 [130]
 p300-HAT inhibitory activity In vitro HAT assay Curcumin, DMC, BDMC 20–60 μM

[Dose-dependent]

⬇ p300-induced acetylation of histone H3K9;

Inhibitory activity at 20 μM:

CUR > BDMC > DMC;

at 60 μM: CUR ≈ DMC ≈ BDMC

 [135]
 Cardiac fibrosis Cardiac fibroblasts (CFs) Curcumin 5–15 μM

[Dose-dependent]

⬇ Ang II-induced expression of:

collagen I, collagen III, and TGF-β1;

⬇ MMP-2 activity;

⬇ Ang II-induced CF cell proliferation and migration

(All above effects of curcumin diminished by SIRT1 siRNA.)

 [133]
 Phenylephrine-induced cardiomyocyte hypertrophy Primary neonatal rat cardiomyocytes Curcumin, DMC, BDMC 10 μM

⬇ Phenylephrine-induced:

acetylation of histone H3K9,

myocardial cell-surface area increase,

ANF and BNP expression

(CUR ≈ DMC ≈ BDMC)

None of the compounds changed morphology of cardiomyocytes

 [135]
 Noradrenaline‐induced cardiomyocyte hypertrophy Heart‐derived H9C2 cardiomyoblast cells, primary neonatal rat cardiomyocytes Curcumin 8 μM

⬇ Noradrenaline-stimulated increases in:

cell size,

protein concentration,

ANF expression,

nuclear localization of GATA4,

DNA-binding activity of GATA4

 [137]
 Phenylephrine-induced cardiomyocyte hypertrophy Primary neonatal rat cardiomyocytes Curcumin 5–10 μM

⬇ Phenylephrine (PE)- or p300-induced increases in:

cell surface area,

ANF and β-MHC promoter activities,

p300-GATA4 association,

GATA4 acetylation,

GATA4-DNA binding;

⬇ p300-induced increases in:

cell surface area,

ANF and β-MHC promoter activities

 [136]