Misoprostol is an orally active prostaglandin E1 (PGE1) analog used to prevent gastric ulcers, treat missed abortion, induce labor and induce miscarriage[1, 2]. Misoprostol is used to prevent gastric ulcers induced by nonsteroidal anti-inflammatory drugs. It can bind to prostaglandin receptors and directly act on parietal cells to inhibit gastric acid secretion[3].
In vitro, Misoprostol (10μM) pretreatment of human peripheral blood mononuclear cells (PBMC) and RAW264.7 cells for 90min significantly increased the phosphorylation of cAMP response element binding protein (CREB) in cells[4]. Misoprostol (10μM) treatment of HCT-116 cells for 2h significantly activated intracellular protein kinase A (PKA)[5]. Misoprostol (8ng/mL) treatment of 3D cultured annular cells significantly increased the epidermal growth factor (EGF) level of cells[6].
In vivo, oral administration of Misoprostol (0.2mg/kg/day) to rats with doxorubicin-induced cardiac injury for 6 days alleviated cardiac injury in rats, significantly reduced serum cardiac troponin-I (cTn-I) and brain natriuretic peptide (BNP) levels, and reduced lactate dehydrogenase (LDH), aspartate aminotransferase (AST), alanine aminotransferase (ALT), and creatine kinase isoenzyme-MB (CK-MB) activities[7].
References:
[1] Ahmed T A, Mohammed A H. Brief Overview About Prostaglandins & Misoprostol For Cervical Ripening[J]. Journal of Pharmaceutical Negative Results, 2023, 14(2).
[2] Chong Y S, Su L L, Arulkumaran S. Misoprostol: a quarter century of use, abuse, and creative misuse[J]. Obstetrical & gynecological survey, 2004, 59(2): 128-140.
[3] Sostres C, Lanas A. Prostaglandins and other mucosal protecting agents[J]. Pocket Guide to Gastrointestinal Drugs, 2014: 44-56.
[4] Gobejishvili L, Ghare S, Khan R, et al. Misoprostol modulates cytokine expression through a cAMP pathway: Potential therapeutic implication for liver disease[J]. Clinical Immunology, 2015, 161(2): 291-299.
[5] Field J T, Martens M D, Mughal W, et al. Misoprostol regulates Bnip3 repression and alternative splicing to control cellular calcium homeostasis during hypoxic stress[J]. Cell Death Discovery, 2018, 4(1): 98.
[6] Gruber H E, Hoelscher G, Loeffler B, et al. Prostaglandin E1 and misoprostol increase epidermal growth factor production in 3D-cultured human annulus cells[J]. The Spine Journal, 2009, 9(9): 760-766.
[7] Bilgic S, Ozgocmen M, Ozer M K, et al. Misoprostol ameliorates doxorubicin induced cardiac damage by decreasing oxidative stress and apoptosis in rats[J]. Biotechnic & Histochemistry, 2020, 95(7): 514-521.
Misoprostol是一种具口服活性的前列腺素E1（PGE1）类似物，用于预防胃溃疡、治疗过期流产、引产和诱导流产[1, 2]。Misoprostol用于预防非甾体抗炎药诱发的胃溃疡，能够与前列腺素受体结合直接作用于壁细胞来抑制胃酸分泌[3]。
在体外，Misoprostol（10μM）预处理人外周血单核细胞（PBMC）和RAW264.7细胞90min，显著增加了细胞中cAMP反应元件结合蛋白（CREB）的磷酸化[4]。Misoprostol（10μM）处理HCT-116细胞2h，显著激活了细胞内蛋白激酶A（PKA）[5]。Misoprostol（8ng/mL）处理3D培养的环状细胞，显著增加了细胞的表皮生长因子（EGF）水平[6]。
在体内，Misoprostol（0.2mg/kg/day）通过口服治疗阿霉素诱导的心脏损伤大鼠6天，减轻了大鼠的心脏损伤，显著降低了血清心肌肌钙蛋白-I（cTn-I）和脑钠肽（BNP）水平，降低了乳酸脱氢酶（LDH）、天冬氨酸转氨酶（AST）、丙氨酸转氨酶（ALT）和肌酸激酶同工酶-MB（CK-MB）活性[7]。