Markov A V, Sen'kova A V, Zenkova M A, Logashenko E B
Institute of Chemical Biology and Fundamental Medicine, Siberian Branch, Russian Academy of Sciences, Novosibirsk, 630090 Russia.
Mol Biol (Mosk). 2018 Mar-Apr;52(2):306-313. doi: 10.7868/S0026898418020143.
Due to wide spreading of inflammatory disease and imperfection of available anti-inflammatory drugs, mainly associated with their serious side effects, searching for new anti-inflammatory agents is a pressing problem. Natural triterpenoids and their synthetic analogs are a promising source of new drugs. In this study, we have investigated the anti-inflammatory and antitumor effects in vivo of the glycyrrhetinic acid derivative soloxolone methyl (SM), or methyl 2-cyano-3,12-dioxo-18βH-olean-9(ll),l(2)-dien-30-oate. SM was shown to efficiently suppress the development of edema in a mouse model of carrageenan- or histamine-induced acute inflammation. SM also inhibited the tumor growth and reduced the tumor cell count in the ascitic fluid in mice bearing Krebs-2 carcinoma, the development of which is accompanied by an inflammatory process in the surrounding tissues.
由于炎症性疾病的广泛传播以及现有抗炎药物的不完善,主要与其严重的副作用相关,寻找新的抗炎药物是一个紧迫的问题。天然三萜类化合物及其合成类似物是新药的一个有前景的来源。在本研究中,我们研究了甘草次酸衍生物索洛索隆甲酯(SM),即2-氰基-3,12-二氧代-18βH-齐墩果-9(11),1(2)-二烯-30-酸甲酯在体内的抗炎和抗肿瘤作用。在角叉菜胶或组胺诱导的急性炎症小鼠模型中,SM被证明能有效抑制水肿的发展。在携带克雷布斯-2癌的小鼠中,SM还抑制肿瘤生长并减少腹水液中的肿瘤细胞数量,该肿瘤的发展伴随着周围组织的炎症过程。