Table 2.
Selected pharmacological approaches aiming at white adipose tissue (WAT) browning and brown adipose tissue (BAT) activation.
| Intervention | Compound | Mechanism of Action | WAT | BAT | Experimental Model | Ref |
|---|---|---|---|---|---|---|
| ADRB3 stimulation | CL-316243 | ↑ PGC-1α | ↑ lipolysis | ↑ brown adipocytes ↑ activity |
C57BL/6 mice | [19] |
| isoprenaline | = | = | clinical study | [121] | ||
| mirabegron | = | ↑ activity | clinical study | [123] | ||
| PPARγ activation | rosiglitazone | ↑ PRDM16 | ↑ beige adipocytes | ↑ activity | C57BL/6 mice | [2] |
| ↑ beige adipocytes | C57BL/6 mice | [125] | ||||
| GQ-16 | ↑ beige adipocytes | ↑ brown adipocytes ↑ activity |
mice on high-fat diet | [126] | ||
| imatinib | ↑ beige adipocytes | C57BL/6 mice | [128] | |||
| pioglitazone | ↓ brown adipocytes ↓ activity |
clinical study | [130] | |||
| PPARα activation | fenofibrate | ↑ PRDM16 | ↑ beige adipocytes | mice with diet-induced obesity | [131] | |
| pemafibrate | ↑ beige adipocytes | ↑ activity | mice with diet-induced obesity | [132] | ||
| AMPK activation | A-769662 | ↑ PGC-1α | ↑ beige adipocytes | ↑ activity | obese ob/ob mice | [134] |
| ↑ beige adipocytes | ↑ activity | AMPK KO mice | [35] | |||
| AICAR | ? | ↑ energy dissipation | white rat adipocytes | [136] | ||
| cordycepin | ? | ↑ beige adipocytes | ↑ activity | mice on high-fat diet | [137] | |
| liraglutide | ↑ NO | ↑ beige adipocytes | ↑ activity | mice on high-fat diet | [139] | |
| SIRT1 activation | resveratrol | ↑ PPARγ | ↑ beige adipocytes | ↑ activity | mice on high-fat diet and 3T3-L1 adipocytes | [69] |
| ↑ AMPK | ↑ beige adipocytes | WAT-derived murine stromal vascular cells | [70] | |||
| SRT501, SRT1720 | ↑ PGC-1α | ↑ activity | mice on high-fat diet | [142] | ||
| SGLT2i | empagliflozin | ↑ M2 macrophages ↓ M2 macrophages |
↑ beige adipocytes | mice with diet-induced obesity | [143] | |
| MicroRNAs | miR-455 | ↑ HIF1an | ↑ beige adipocytes | ↑ brown adipocytes | human white adipocytes | [145] |
| miR-92a | ? | ↓ activity | clinical study | [146] |
↑ increase/enhancement; ↓ decrease/reduction; ? unknown mechanism; ADRB3—adrenergic receptor beta 3; AICAR—5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside; AMPK—AMP-activated protein kinase; HIF1an—hypoxia inducible factor 1 α subunit inhibitor; NO—nitric oxide; PPAR—proliferator-activated receptor; PGC-1α—PPARγ coactivator 1α; PRDM16—PR domain containing 16 transcription factor; SGLT2i—sodium-glucose cotransporter 2 inhibitors; SIRT1—sirtuin 1.