Analgesic, anti-inflammatory and sedative/hypnotic effects of Icaritin, and its effect on chloride influx in mouse brain cortical cells

Fengyu Huang; Yaodong Zhang; Yinfeng Xu; Wei Xiang; Chaofan Xie

doi:10.14715/cmb/2019.65.7.17

Issue

Vol. 65 No. 7: Issue 7

Issue Published : October 14, 2019

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Analgesic, anti-inflammatory and sedative/hypnotic effects of Icaritin, and its effect on chloride influx in mouse brain cortical cells

https://doi.org/10.14715/cmb/2019.65.7.17

Fengyu Huang

Department of Anesthesiology, The First Affiliated Hospital of Sun Yat-sen University, China

Yaodong Zhang

Department of Anesthesiology, The First Affiliated Hospital of Sun Yat-sen University, China

Yinfeng Xu

Department of Orthopedics, The First Affiliated Hospital of Sun Yat-sen University, China

Wei Xiang

Department of Orthopedics, The Eight Affiliated Hospital of Sun Yat-sen University, China

Chaofan Xie

Department of Orthopedics, The First Affiliated Hospital of Sun Yat-sen University, China

Corresponding Author(s) : Chaofan Xie

eweth2@163.com

Cellular and Molecular Biology, Vol. 65 No. 7: Issue 7
Article Published : September 30, 2019

Abstract

Inflammation and insomnia are medical problems that may severely affect work and health, thereby necessitating strategies for their effective treatment. Icartin (ICT) is a major active monomeric component of icariin . Studies have revealed that ICT possesses several pharmacological properties such anti-inflammatory, anti-tumor, anti-fibrotic, anti-osteoporotic and neuroprotective effects. The present research was carried out to investigate the anti-inflammatory, analgesic and sedative/hypnotic effects of ICT. The results obtained revealed that ICT exerted a good anti-inflammatory effect related to the downregulations of inflammatory cytokines and the inhibition of COX-2 signaling pathway. Moreover, ICT enhanced Cl- influx in mouse cortical cells in a concentration-dependent manner. These data suggest that ICT exerts a hypnotic effect in mice through a mechanism associated with increased Cl- influx in cortical cells.

Keywords

Icaritin Analgesic Anti-Inflammatory Sedative-Hypnotic Cl- influx.

Huang, F., Zhang, Y., Xu, Y., Xiang, W., & Xie, C. (2019). Analgesic, anti-inflammatory and sedative/hypnotic effects of Icaritin, and its effect on chloride influx in mouse brain cortical cells. Cellular and Molecular Biology, 65(7), 99–104. https://doi.org/10.14715/cmb/2019.65.7.17

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References

Meek IL, Van DE Laar MA, E Vonkeman H. Non-steroidal anti-inflammatory drugs: an overview of cardiovascular risks. Pharmaceuticals (Basel) 2010; 3: 2146-2162.
Trelle S, Reichenbach S, Wandel S, Hildebrand P, Tschannen B, Villiger PM, et al. Cardiovascular safety of non - steroidal anti-inflammatory drugs: network meta-analysis. BMJ 2011; 342: 7086.
Kaufmann CN, Spira AP, Alexander GC, Rutkow L, Mojtabai R. Trends in prescribing of sedative - hypnotic medications in the USA: 1993-2010. Pharmacoepidemiol Drug Saf 2016; 25: 637-645.
Cock I, Van Vuuren SF. anti-proteus activity of some South African medicinal plants: their potential for the prevention of rheumatoid arthritis. Inflammopharmacology 2014; 22: 23-36.
Street R, Prinsloo G. Commercially important medicinal plants of South Africa: a review. J Chem 2013; 2013: 2.
Tong JS, Zhang QH, Huang X, Fu XQ, Qi ST, Wang YP, et al. Icaritin causes erk1/2 activation and induces apoptosis in human endometrial cancer cells. PLoS One 2011; 6: 16781.
Huang C, Chen X, Guo B, Huang W, Shen T, Sun X, et al. Induction of apoptosis by Icariside II through extrinsic and intrinsic pathways in human breast cancer MCF7 cells. Biosci Biotechnol Biochem 2012; 76: 1322-1328.
Zhang G, Qin L, Sheng H, Wang XL, Wang YX, Yeung DKW, et al. A novel semisynthesized small molecule icaritin reduces incidence of steroid associated osteonecrosis with inhibition of both thrombosis and lipid-deposition in A dose-dependent manner. Bone 2009; 44: 345-356.
Lai X, Ye Y, Sun C, Huang X, Tang X, Zeng, X, et al. Icaritin exhibits anti- inflammatory effects in the mouse peritoneal macrophages and peritonitis model. Int Immunopharmacol 2013; 16: 41-49.
Ye H, Lou YJ. Estrogenic effects of two derivatives of icariin on human breast cancer McF-7 cells. Phytomedicine 2005; 12: 735-741.
Ma HR, Wang J, Chen YF, Chen H, Wang WS, Aisa HA. Icariin and icaritin stimulate the proliferation of SKBr3 cells through the gper1-mediated modulation of the egfr-mapk signaling pathway. Int J Mol Med 2014; 33: 1627-1634.
Wu J, Du J, Xu C, Le J, Liu B, Xu Y, et al. In vivo and In vitro anti-inflammatory effects of will be a derivative of icariin. Immunopharmacol Immunotoxicol 2011; 33: 49-54.
Deng B, Jia L, Pan L, Song A, Wang Y, Tan H, et al. Wen- Luo Tong prevents glial activation and nociceptive sensitization in a rat model of oxaliplatin- induced neuropathic pain. Evid Based Complement Alternat Med 2016; 2016: 3629489.
Groesch S, Niederberger E, Geisslinger G. Investigational drugs targeting the prostaglandin E2 signaling pathway for the treatment of inflammatory pain. Expert Opin Investig Drugs 2017; 26: 51-61.
Cong XD, Wu Y, Dai DZ, Ding MJ, Zhang Y, Dai Y. The Activation of AQP4, p66Shc and endoplasmic reticulum stress is involved in inflammation by carrageenan and is suppressed by argirein, a derivative of rhein. J Pharm Pharmacol 2012; 64: 1138-1145.
Morris CJ. carrageenan-induced paw edema in the rat and mouse. Methods Mol Biol 2003; 225: 115-121.
Naito Y, Ji X, Tachibana S, Aoki S, Furuya M, Tazura Y, et al. The Effects of arachidonic acid intake on inflammatory reactions in dextran sodium sulphate - induced colitis in rats. Br J Nutr 2015; 114: 734-745.
Xie C, Li X, Wu J, Liang Z, Deng F, Xie W, et al. Anti- inflammatory activity of magnesium isoglycyrrhizinate through inhibition of phospholipase A2/arachidonic acid pathway. Inflammation 2015; 38: 1639-1648.
Ma H, Kim CS, Ma Y, Nam SY, Kim DS, Woo SS, et al. Magnolol enhances pentobarbital"induced sleeping behaviors: Possible involvement of GABAergic systems. Phytother Res 2009; 23: 1340-1344.
Han H, Ma Y, Eun JS, Li R, Hong JT, Lee MK, et al. Anxiolytic-like effects of sanjoinine A isolated from Zizyphi Spinosi Semen: Possible involvement of GABAergic transmission. Pharmacol Biochem Behav 2009; 92: 206-213.
Saper CB, Chou TC, Scammell TE. The sleep switch: hypothalamic control of sleep and wakefulness. Trends Neurosci 2001; 24: 726-731.

References

Meek IL, Van DE Laar MA, E Vonkeman H. Non-steroidal anti-inflammatory drugs: an overview of cardiovascular risks. Pharmaceuticals (Basel) 2010; 3: 2146-2162.

Trelle S, Reichenbach S, Wandel S, Hildebrand P, Tschannen B, Villiger PM, et al. Cardiovascular safety of non - steroidal anti-inflammatory drugs: network meta-analysis. BMJ 2011; 342: 7086.

Kaufmann CN, Spira AP, Alexander GC, Rutkow L, Mojtabai R. Trends in prescribing of sedative - hypnotic medications in the USA: 1993-2010. Pharmacoepidemiol Drug Saf 2016; 25: 637-645.

Cock I, Van Vuuren SF. anti-proteus activity of some South African medicinal plants: their potential for the prevention of rheumatoid arthritis. Inflammopharmacology 2014; 22: 23-36.

Street R, Prinsloo G. Commercially important medicinal plants of South Africa: a review. J Chem 2013; 2013: 2.

Tong JS, Zhang QH, Huang X, Fu XQ, Qi ST, Wang YP, et al. Icaritin causes erk1/2 activation and induces apoptosis in human endometrial cancer cells. PLoS One 2011; 6: 16781.

Huang C, Chen X, Guo B, Huang W, Shen T, Sun X, et al. Induction of apoptosis by Icariside II through extrinsic and intrinsic pathways in human breast cancer MCF7 cells. Biosci Biotechnol Biochem 2012; 76: 1322-1328.

Zhang G, Qin L, Sheng H, Wang XL, Wang YX, Yeung DKW, et al. A novel semisynthesized small molecule icaritin reduces incidence of steroid associated osteonecrosis with inhibition of both thrombosis and lipid-deposition in A dose-dependent manner. Bone 2009; 44: 345-356.

Lai X, Ye Y, Sun C, Huang X, Tang X, Zeng, X, et al. Icaritin exhibits anti- inflammatory effects in the mouse peritoneal macrophages and peritonitis model. Int Immunopharmacol 2013; 16: 41-49.

Ye H, Lou YJ. Estrogenic effects of two derivatives of icariin on human breast cancer McF-7 cells. Phytomedicine 2005; 12: 735-741.

Ma HR, Wang J, Chen YF, Chen H, Wang WS, Aisa HA. Icariin and icaritin stimulate the proliferation of SKBr3 cells through the gper1-mediated modulation of the egfr-mapk signaling pathway. Int J Mol Med 2014; 33: 1627-1634.

Wu J, Du J, Xu C, Le J, Liu B, Xu Y, et al. In vivo and In vitro anti-inflammatory effects of will be a derivative of icariin. Immunopharmacol Immunotoxicol 2011; 33: 49-54.

Deng B, Jia L, Pan L, Song A, Wang Y, Tan H, et al. Wen- Luo Tong prevents glial activation and nociceptive sensitization in a rat model of oxaliplatin- induced neuropathic pain. Evid Based Complement Alternat Med 2016; 2016: 3629489.

Groesch S, Niederberger E, Geisslinger G. Investigational drugs targeting the prostaglandin E2 signaling pathway for the treatment of inflammatory pain. Expert Opin Investig Drugs 2017; 26: 51-61.

Cong XD, Wu Y, Dai DZ, Ding MJ, Zhang Y, Dai Y. The Activation of AQP4, p66Shc and endoplasmic reticulum stress is involved in inflammation by carrageenan and is suppressed by argirein, a derivative of rhein. J Pharm Pharmacol 2012; 64: 1138-1145.

Morris CJ. carrageenan-induced paw edema in the rat and mouse. Methods Mol Biol 2003; 225: 115-121.

Naito Y, Ji X, Tachibana S, Aoki S, Furuya M, Tazura Y, et al. The Effects of arachidonic acid intake on inflammatory reactions in dextran sodium sulphate - induced colitis in rats. Br J Nutr 2015; 114: 734-745.

Xie C, Li X, Wu J, Liang Z, Deng F, Xie W, et al. Anti- inflammatory activity of magnesium isoglycyrrhizinate through inhibition of phospholipase A2/arachidonic acid pathway. Inflammation 2015; 38: 1639-1648.

Ma H, Kim CS, Ma Y, Nam SY, Kim DS, Woo SS, et al. Magnolol enhances pentobarbital"induced sleeping behaviors: Possible involvement of GABAergic systems. Phytother Res 2009; 23: 1340-1344.

Han H, Ma Y, Eun JS, Li R, Hong JT, Lee MK, et al. Anxiolytic-like effects of sanjoinine A isolated from Zizyphi Spinosi Semen: Possible involvement of GABAergic transmission. Pharmacol Biochem Behav 2009; 92: 206-213.

Saper CB, Chou TC, Scammell TE. The sleep switch: hypothalamic control of sleep and wakefulness. Trends Neurosci 2001; 24: 726-731.

Author biographies is not available.