Table 2.
Pharmacology of acetylshikonin.
| Pharmacological effect | Cell lines/model | Activity/Mechanism(s) of action | Application | Reference |
|---|---|---|---|---|
| Anticancer activity | HCT116 cells | Inhibition of EMT and autophagy; Upregulation of ROS; Induction of apoptosis and necrosis | In vitro | Xue & Li 2017; Vukic et al. 2017; Vukic et al. 2020 |
| HT29 cells | Suppression of invasion; Regulation of NF-κB and PI3K/Akt/mTOR pathway | In vitro | Zhu et al. 2018; Zhao and Yang 2019 | |
| SMMC-7721 cells | Induction of apoptosis; Cell cycle arrested at G2/M phase | In vitro | Wu et al. 2011 | |
| Hep3B cells | Upregulation and export of Nur77; Regulation of JNK pathway; Induction of ER stress | In vitro | Moon et al. 2014 | |
| HepG2 cells | Induction of apoptosis; Regulation of p53/PUMA/Bax pathway; Upregulation of ROS | In vitro | Park et al. 2017; Hong et al. 2019 | |
| LLC cells | Downregulation of VEGF and uPA; Induction of apoptosis | In vivo and in vitro | Lee et al. 2008; Xiong et al. 2009 | |
| NIH-H460 cells | Regulation of Nur77 pathway | In vitro | Liu et al. 2008 | |
| A549 cells | DNA fragmentation | In vitro | Eskandani and Nazemiyeh 2014 | |
| B16F10 cells | Regulation of p53 pathway | In vitro | Chen et al. 2016 | |
| A375 cells | Inhibition of EMT process; Regulation of PI3K/Akt/mTOR pathway | In vitro | Jiang et al. 2019 | |
| HL-60 cells | Inhibition of the extension of telomeres | In vitro | Lu et al. 2002 | |
| K562 cells | Induction of apoptosis; Upregulation of ROS and TNF-α; DAN damage; Regulation of NF-κB pathway | In vitro | Ahmed et al. 2016; Hao et al. 2020 | |
| OSCC cells | Regulation of JNK and p38 MAPK pathway | in vitro | Kim et al. 2016 | |
| YD10B cells | Downregulation of IL-8 and MMP | in vitro | Cho et al. 2018 | |
| KB-R5 cells | Regulation of m-TOR/PI3K/Akt pathway | In vitro | Wang et al. 2019 | |
| L-1 sarcoma cells | Inhibition of cutaneous angiogenesis | In vivo | Pietrosiuk et al. 2004a | |
| S180 sarcoma | Induction of necrosis | In vivo | Zeng et al. 2008 | |
| SGC-7901 cells | Induction of apoptosis | In vitro | Zeng et al. 2009 | |
| MDA-MB-231 cells | Cell cycle arrest at G0/G1; Inhibition of autophagy; Upregulation of ROS | In vitro | Vukic et al. 2020 | |
| PANC-1 cells | Regulation of NF-κB pathway | In vitro | Cho and Choi 2015 | |
| Siha cells | Activation of caspase-3 and caspase-8 | In vitro | Sun et al. 2014 | |
| SKOV3 cells | Induction of apoptosis | In vitro | He et al. 2019 | |
| EPG85.257RDB, MCF7MX, A2780RCIS cells | Reduction of BCRP, MDR1, and MRP2 pump activity | In vitro | Mirzaei et al. 2018 | |
| Anti-inflammatory activity | Leukocyte cells | Inhibition of leukotriene B4 | In vitro | Wang et al. 1994 |
| Carrageenan-induced paw edoema | Inhibition of TNF-α activation | In vivo | Kundakovic et al. 2006 | |
| RAW 264.7 cells | Downregulation of NF-κB activation; Inhibition of TNF-α, IL-1, and NO | In vitro | Cheng et al. 2008; Wei et al. 2011 | |
| Rat neutrophils | Suppression of phosphatidylinositol signalling; Inhibition of cyclooxygenase and 5-lipoxygenase activity | In vitro | Wang and Kuo 1997; Hsu et al. 2009 | |
| BV2 microglial cells | Regulation of NF-κB pathway; Upregulation of HO-1 | In vitro | Jayasooriya et al. 2015 | |
| Macrophages | Induction of apoptosis | In vitro | Koike et al. 2016 | |
| C57BL/6 mice | Suppression of IL-1β release and NLRP3 activation | In vitro | Zorman et al. 2016 | |
| Apolipoprotein E deficient mice | Regulation of NF-κB pathway | In vivo | Cui et al. 2018 | |
| MCD diet-induced mice | Regulation of AMPK/mTOR pathway | In vivo | Zeng et al. 2018 | |
| Smoke-induced mice | Downregulation of TNF-α, IL-6, IL-1β, and MCP-1; Upregulation of COX-2 and Nrf2 | In vivo | Zhang et al. 2019 | |
| TH2 cells | Downregulation of lgE, lgG1, IL-4, IL-5, and IL-13 | In vivo | Fan et al. 2019 | |
| Lipid-regulatory activity | AC-29 cells | Inhibition of ACAT-1 and ACAT-2 | In vitro | An et al. 2007 |
| 3T3-L1 cells | Inhibition of adipocyte differentiation and adipogenic transcription factor; Regulation of PKA signalling | In vitro | Gwon et al. 2012; Su et al. 2016a | |
| Spontaneous obese db/db mice | regulation of lipid metabolism | In vivo | Su et al. 2016b | |
| Antidiabetic activity | Diabetic mice | Regulation of TGF-β1/Smad pathway | In vivo | Li et al. 2018 |
| Alloxan-induced mice | Regulation of PLC-β3/PKCδ pathway | In vivo | Huang et al. 2019 | |
| CHO cells | Induction of DMR response | In vitro | Xu et al. 2019 | |
| Antioxidative activity | leukocytes | Reduction of NADPH oxidase | In vitro | Kawakami et al. 1996 |
| Neuroprotective effect | SH-SY5Y and PC12 cells | Suppression of loss of mitochondria membrane potential and the generation of ROS | In vitro | Wang et al. 2013 |
| d-galactose-induced mice | Regulation of SIRT1/p53/p21 pathway | In vivo | Li et al. 2018 |