Icariin:
flavonoid mnoha tváří
Jiří
Patočka
Icariin je flavonoid, 8-prenylovaný derivát kaemferol-3,7-O-diglukosidu. Sloučenina byla izolována z několika druhů rostlin z rodu Epimedium (Liu et al., 2006) jejichž výtažky jsou pokládány za účinné afrodiziakální prostředky a používají se v tradiční čínské medicíně ke zvýšení erektilní funkce (Makarova et al., 2007). V poslední době je icariin předmětem zájmu západní medicíny, která předpokládá, že by mohl být využitelný k léčbě impotence, ale i v dalších indikacích (Pan et al., 2007b; Zheng et al., 2008; Xiao et al., 2016; Algandaby et al., 2017; Cao et al., 2017; Gu et al., 2017; Qiao et al., 2017).
Experimenty na zvířatech prokázaly jeho účinnost v mnoha indikacích a protože má několik mechanismů účinku a minimum nežádoucích účinků, jsou do něj vkládány velké naděje. Icariin je slabým inhibitorem cGMP-specifické fosfodiesterasy-5 (Jing et al., 2006; Ningh et al., 2006; Dell'Agli et al., 2008) a zvyšuje produkci oxidu dusnatého (Xu a Huang, 2007) a in vitro také napodobuje účinky testosteronu u potkanů (Zhang a Yang, 2006). Icariin je také slabým antioxidantem Xie et al., 2007; Zhao et al., 2007) a má u myší a potkanů antidepresivní (Pan et al., 2005, 2006, 2007a) a neuroprotektivní účinky (Pan et al., 2007b; Luo et al., 2007). Vykazuje rovněž protizánětlivé účinky (Hua et al., 2017). Opakovaně bylo v řadě testů prokázáno, že icariin je vhodným kandidátem pro léčbu erektilní dysfunkce (Liu et al., 2005, 2011; Zhang et al., 2013; Li et al., 2014; Wang et al., 2017; Xu et al., 2017).
Naprostá většina studií o biologických účincích icariinu byla získána v rámci preklinických testů a zkoušek, ale už se začínají objevovat i první pilotní a preklinické testy, které přináší nadějné výsledky (Indran et al., 2016; Xiao et al., 2016).
Literatura
Algandaby MM, Breikaa RM, Eid BG, Neamatallah TA, Abdel-Naim AB, Ashour OM. Icariin protects against thioacetamide-induced liver fibrosis in rats: Implication of anti-angiogenic and anti-autophagic properties. Pharmacol Rep. 2017; 69(4): 616-624.
Cao H, Zhang Y, Qian W, Guo XP, Sun C, Zhang L, Cheng XH. Effect of icariin on fracture healing in an ovariectomized rat model of osteoporosis. Exp Ther Med. 2017; 13(5): 2399-2404.
Dell'Agli M, Galli GV, Dal Cero E, et al. Potent inhibition of human phosphodiesterase-5 by icariin derivatives. J Nat Prod. 2008; 71(9): 1513–1517.
Gu ZF, Zhang ZT, Wang JY, Xu BB. Icariin exerts inhibitory effects on the growth and metastasis of KYSE70 human esophageal carcinoma cells via PI3K/AKT and STAT3 pathways. Environ Toxicol Pharmacol. 2017; 54: 7-13.
Hua WB, Zhang YK, Wu XH, Kang L, Tu J, Zhao KC, Li S, Wang K, Song Y, Luo RJ, Shao ZW, Yang C. Icariin Attenuates Interleukin-1β-Induced Inflammatory Response in Human Nucleus Pulposus Cells. Curr Pharm Des. 2017 Jun 15. doi: [Epub ahead of print]
Indran IR, Liang RL, Min TE, Yong EL. Preclinical studies and clinical evaluation of compounds from the genus Epimedium for osteoporosis and bone health. Pharmacol Ther. 2016; 162: 188-205.
Jiang Z, Hu B, Wang J, et al. Effect of icariin on cyclic GMP levels and on the mRNA expression of cGMP-binding cGMP-specific phosphodiesterase (PDE5) in penile cavernosum. J Huazhong Univ Sci Technol Med Sci. 2006; 26(4): 460–462.
Liu JJ, Li SP, Wang YT. Optimization for quantitative determination of four flavonoids in Epimedium by capillary zone electrophoresis coupled with diode array detection using central composite design. J Chromatogr A. 2006; 1103(2):344–349.
Liu T, Xin H, Li WR, Zhou F, Li GY, Gong YQ, Gao ZZ, Qin XC, Cui WS, Shindel AW, Xin ZC. Effects of icariin on improving erectile function in streptozotocin-induced diabetic rats. J Sex Med. 2011; 8(10): 2761-2772.
Liu WJ, Xin ZC, Xin H, Yuan YM, Tian L, Guo YL. Effects of icariin on erectilefunction and expression of nitric oxide synthase isoforms in castrated rats. Asian J Androl. 2005; 7(4): 381-388.
Li Y, Jiang J, He Y, Jiang R, Liu J, Fan Z, Cheng Y. Icariin combined with breviscapine improves the erectile function of spontaneously hypertensive rats. J Sex Med. 2014; 11(9): 2143-2152.
Luo Y, Nie J, Gong QH, Lu YF, Wu Q, Shi JS. Protective effects of icariin against learning and memory deficits induced by aluminium in rats. Clin Exp Pharmacol Physiol. 2007; 34(8): 792–795.
Makarova MN, Pozharitskaya ON, Shikov AN, Tesakova SV, Makarov VG, Tikhonov VP. Effect of lipid-based suspension of Epimedium koreanum Nakai extract on sexual behavior in rats. J Ethnopharmacol. 2007; 114(3): 412–416.
Ning H, Xin ZC, Lin G, Banie L, Lue TF, Lin CS (December 2006). Effects of icariin on phosphodiesterase-5 activity in vitro and cyclic guanosine monophosphate level in cavernous smooth muscle cells. Urology. 2006; 68(6): 1350–1354.
Pan Y, Kong LD, Xia X, Zhang W, Xia Z, Jiang F. Antidepressant-like effect of icariin and its possible mechanism in mice. Pharmacol Biochem Behav. 2005; 82(4): 686–694.
Pan Y, Kong LD, Li YC, Xia X, Kung HF, Jiang FX. Icariin from Epimedium brevicornum attenuates chronic mild stress-induced behavioral and neuroendocrinological alterations in male Wistar rats. Pharmacol Biochem Behav. 2007a; 87(1): 130–40.
Pan Y, Zhang WY, Xia X, Kong LD. Effects of icariin on hypothalamic-pituitary-adrenal axis action and cytokine levels in stressed Sprague-Dawley rats. Biol Pharm Bull.2006; 29(12): 2399–2403.
Qiao J, Sun S, Yuan L, Wang J. Effects of icariin on asthma mouse model are associated with regulation of prostaglandin D2 level. Allergol Immunopathol (Madr). 2017; pii: S0301-0546(17)30066-6
Wang X, Liu C, Xu Y, Chen P, Shen Y, Xu Y, Zhao Y, Chen W, Zhang X, Ouyang Y, Wang Y, Xie C, Zhou M, Liu C. Combination of mesenchymal stem cell injection with icariin for the treatment of diabetes-associated erectile dysfunction. PLoS One. 2017; 12(3): e0174145.
Xiao H, Wignall N, Brown ES. An open-label pilot study of icariin for co-morbid bipolar and alcohol use disorder. Am J Drug Alcohol Abuse. 2016; 42(2): 162-167.
Xie J, Sun W, Duan K, Zhang Y. Chemical constituents of roots of Epimedium wushanense and evaluation of their biological activities. Nat Prod Res. 2007; 21(7): 600–605.
Xu HB, Huang ZQ. Icariin enhances endothelial nitric-oxide synthase expression on human endothelial cells in vitro. Vascular Pharmacol, 2007; 47(1): 18–24.
Xu Y, Xin H, Wu Y, Guan R, Lei H, Fu X, Xin Z, Yang Y. Effect of icariin in combination with daily sildenafil on penile atrophy and erectile dysfunction in a rat model of bilateral cavernous nerves injury. Andrology. 2017; 5(3): 598-605.
Zhang J, Li AM, Liu BX, Han F, Liu F, Sun SP, Li X, Cui SJ, Xian SZ, Kong GQ, Xin ZC, Ji ZL. Effect of icarisid II on diabetic rats with erectile dysfunction and its potential mechanism via assessment of AGEs, autophagy, mTOR and the NO-cGMP pathway. Asian J Androl. 2013; 15(1): 143-148.
Zhang ZB, Yang QT. The testosterone mimetic properties of icariin. Asian J Androl. 2006; 8(5): 601–605.
Zhao F, Tang YZ, Liu ZQ (December 2007). Protective effect of icariin on DNA against radical-induced oxidative damage. J Pharm Pharmacol. 2007; 59(12): 1729–1732.
Zheng M, Qu L, Lou Y. Effects of icariin combined with Panax notoginseng saponins on ischemia reperfusion-induced cognitive impairments related with oxidative stress and CA1 of hippocampal neurons in rat. Phytother Res. 2008; 22(5): 597–604.
