The Pharmacokinetic Property and Pharmacological Activity of Acteoside: A Review

Overview

Journal Biomed Pharmacother

Specialties Biology
General Medicine
Pharmacology

Date 2022 Jun 20

PMID 35724511

Authors

Yaosheng Xiao

Qun Ren

Longhuo Wu

Affiliations

Soon will be listed here.

Abstract

Acteoside (AC), a phenylpropanoid glycoside isolated from many dicotyledonous plants, has been demonstrated various pharmacological activities, including anti-oxidation, anti-inflammation, anti-cancer, neuroprotection, cardiovascular protection, anti-diabetes, bone and cartilage protection, hepatoprotection, and anti-microorganism. However, AC has a poor bioavailability, which can be potentially improved by different strategies. The health-promoting characteristics of AC can be attributed to its mediation in many signaling pathways, such as MAPK, NF-κB, PI3K/AKT, TGFβ/Smad, and AMPK/mTOR. Interestingly, docking simulation study indicates that AC can be an effective candidate to inhibit the activity of SARS-CoV2 main protease and protect against COVID-19. Many clinical trials for AC have been investigated, and it shows great potentials in drug development.

Citing Articles

Preconditioning with acteoside ameliorates myocardial ischemia‑reperfusion injury by targeting HSP90AA1 and the PI3K/Akt signaling pathway.

Li J, Guo Y, Yang Y, Xue Q, Cao H, Yang G Mol Med Rep. 2025; 31(3).

PMID: 39886969 PMC: 11795246. DOI: 10.3892/mmr.2025.13442.

Identification of Bioactive Compounds from the Roots of and Their In Silico and In Vitro AMPK Activation Potential.

Lee H, Youn I, Noh S, Kim H, Song E, Nam S Molecules. 2025; 29(24.

PMID: 39770103 PMC: 11679303. DOI: 10.3390/molecules29246009.

Protective Effect of Acteoside against Hydrogen Peroxide-Induced Oxidative Damage in Human Corneal Epithelial Cells.

Huang Y, Peng Q Bull Exp Biol Med. 2025; 178(2):213-217.

PMID: 39762699 DOI: 10.1007/s10517-025-06309-x.

Acteoside relieves diabetic retinopathy through the inhibition of Müller cell reactive hyperplasia by regulating TXNIP and mediating Kir4.1 channels in a PI3K/Akt-dependent manner.

Xi X, Liu X, Chen Q, Ma J, Wang X, Gui Y PLoS One. 2024; 19(12):e0312565.

PMID: 39689088 PMC: 11651567. DOI: 10.1371/journal.pone.0312565.

Research Progress of in the Treatment of Gastrointestinal Cancer.

Wang L, Ni B, Wang J, Zhou J, Wang J, Jiang J Integr Cancer Ther. 2024; 23:15347354241302049.

PMID: 39610320 PMC: 11605761. DOI: 10.1177/15347354241302049.

References

Funes L, Laporta O, Cerdan-Calero M, Micol V . Effects of verbascoside, a phenylpropanoid glycoside from lemon verbena, on phospholipid model membranes. Chem Phys Lipids. 2009; 163(2):190-9. DOI: 10.1016/j.chemphyslip.2009.11.004. View

Narayanankutty A . Inhibitory Potential of Dietary Nutraceuticals on Cellular PI3K/Akt Signaling: Implications in Cancer Prevention and Therapy. Curr Top Med Chem. 2021; 21(20):1816-1831. DOI: 10.2174/1568026621666210716152224. View

Wu W, Wu G, Cao D . Acteoside Presents Protective Effects on Cerebral Ischemia/reperfusion Injury Through Targeting CCL2, CXCL10, and ICAM1. Cell Biochem Biophys. 2021; 79(2):301-310. DOI: 10.1007/s12013-020-00965-8. View

Anter J, Tasset I, Demyda-Peyras S, Ranchal I, Moreno-Millan M, Romero-Jimenez M . Evaluation of potential antigenotoxic, cytotoxic and proapoptotic effects of the olive oil by-product "alperujo", hydroxytyrosol, tyrosol and verbascoside. Mutat Res Genet Toxicol Environ Mutagen. 2014; 772:25-33. DOI: 10.1016/j.mrgentox.2014.07.002. View

Su D, Li W, Xu Q, Liu Y, Song Y, Feng Y . New metabolites of acteoside identified by ultra-performance liquid chromatography/quadrupole-time-of-flight MS(E) in rat plasma, urine, and feces. Fitoterapia. 2016; 112:45-55. DOI: 10.1016/j.fitote.2016.05.004. View

Gao W, Zheng S, Hwang E, Yi T, Wang Y . Effects of phenylethanol glycosides from Orobanche cernua Loefling on UVB-Induced skin photodamage: a comparative study. Photochem Photobiol Sci. 2021; 20(5):599-614. DOI: 10.1007/s43630-021-00038-6. View

Nam S, Kim H, Jeong H . Attenuation of IL-32-induced caspase-1 and nuclear factor-κB activations by acteoside. Int Immunopharmacol. 2015; 29(2):574-582. DOI: 10.1016/j.intimp.2015.09.026. View

Ong P, Wang L, Dai X, Tseng S, Loo S, Sethi G . Judicious Toggling of mTOR Activity to Combat Insulin Resistance and Cancer: Current Evidence and Perspectives. Front Pharmacol. 2016; 7:395. PMC: 5079084. DOI: 10.3389/fphar.2016.00395. View

Lau C, Chen Z, Wong C, Yao X, He Z, Xu H . Attenuated endothelium-mediated relaxation by acteoside in rat aorta: Role of endothelial [Ca2+]i and nitric oxide/cyclic GMP pathway. Life Sci. 2004; 75(10):1149-57. DOI: 10.1016/j.lfs.2003.12.031. View

10.

Hayashi K, Nagamatsu T, Ito M, Hattori T, Suzuki Y . Acteoside, a component of Stachys sieboldii MIQ, may be a promising antinephritic agent (2): Effect of acteoside on leukocyte accumulation in the glomeruli of nephritic rats. Jpn J Pharmacol. 1994; 66(1):47-52. DOI: 10.1254/jjp.66.47. View

11.

Sun X, Qi H, Wu H, Qu Y, Wang K . Anti-pruritic and anti-inflammatory effects of natural verbascoside through selective inhibition of temperature-sensitive Ca-permeable TRPV3 channel. J Dermatol Sci. 2020; 97(3):229-231. DOI: 10.1016/j.jdermsci.2020.01.004. View

12.

Zhou F, Huang W, Li M, Zhong Y, Wang M, Lu B . Bioaccessibility and Absorption Mechanism of Phenylethanoid Glycosides Using Simulated Digestion/Caco-2 Intestinal Cell Models. J Agric Food Chem. 2018; 66(18):4630-4637. DOI: 10.1021/acs.jafc.8b01307. View

13.

Gao Y, Zong C, Liu F, Fang L, Cai R, Shi Y . Evaluation of the intestinal transport of a phenylethanoid glycoside-rich extract from Cistanche deserticola across the Caco-2 cell monolayer model. PLoS One. 2015; 10(2):e0116490. PMC: 4315399. DOI: 10.1371/journal.pone.0116490. View

14.

Khattab A, Teleb M, Kamel M . study of potential anti-SARS cell entry phytoligands from : a promising avenue for prophylaxis. Future Virol. 2021; 0(0). PMC: 8559586. DOI: 10.2217/fvl-2021-0031. View

15.

Cui Q, Pan Y, Xu X, Zhang W, Wu X, Qu S . The metabolic profile of acteoside produced by human or rat intestinal bacteria or intestinal enzyme in vitro employed UPLC-Q-TOF-MS. Fitoterapia. 2015; 109:67-74. DOI: 10.1016/j.fitote.2015.12.011. View

16.

Sheng G, Zhang J, Pu X, Ma J, Li C . Protective effect of verbascoside on 1-methyl-4-phenylpyridinium ion-induced neurotoxicity in PC12 cells. Eur J Pharmacol. 2002; 451(2):119-24. DOI: 10.1016/s0014-2999(02)02240-9. View

17.

Zhu M, Zhu H, Tan N, Wang H, Chu H, Zhang C . Central anti-fatigue activity of verbascoside. Neurosci Lett. 2016; 616:75-9. DOI: 10.1016/j.neulet.2016.01.042. View

18.

Kim K, Chun J, Lee K, Lee J, Park K, Han K . Effect of acteoside on the re-localization and abnormal morphology of mitochondria in porcine oocytes during in vitro maturation. J Assist Reprod Genet. 2016; 33(7):939-48. PMC: 4930786. DOI: 10.1007/s10815-016-0729-x. View

19.

Fan Y, Zhang K . Verbascoside inhibits the progression of atherosclerosis in high fat diet induced atherosclerosis rat model. J Physiol Pharmacol. 2021; 72(3). DOI: 10.26402/jpp.2021.3.03. View

20.

Kodani A, Kikuchi T, Tohda C . Acteoside Improves Muscle Atrophy and Motor Function by Inducing New Myokine Secretion in Chronic Spinal Cord Injury. J Neurotrauma. 2018; 36(12):1935-1948. PMC: 6599386. DOI: 10.1089/neu.2018.6000. View