Elsebai Mahmoud F, Mocan Andrei, Atanasov Atanas G
Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University Mansoura, Egypt.
Department of Pharmaceutical Botany, Iuliu Haţieganu University of Medicine and Pharmacy Cluj-Napoca, Romania.
Front Pharmacol. 2016 Dec 8;7:472. doi: 10.3389/fphar.2016.00472. eCollection 2016.
The different pharmacologic properties of plants-containing cynaropicrin, especially artichokes, have been known for many centuries. More recently, cynaropicrin exhibited a potential activity against all genotypes of hepatitis C virus (HCV). Cynaropicrin has also shown a wide range of other pharmacologic properties such as anti-hyperlipidemic, anti-trypanosomal, anti-malarial, antifeedant, antispasmodic, anti-photoaging, and anti-tumor action, as well as activation of bitter sensory receptors, and anti-inflammatory properties (e.g., associated with the suppression of the key pro-inflammatory NF-κB pathway). These pharmacological effects are very supportive factors to its outstanding activity against HCV. Structurally, cynaropicrin might be considered as a potential drug candidate, since it has no violations for the rule of five and its water-solubility could allow formulation as therapeutic injections. Moreover, cynaropicrin is a small molecule that can be easily synthesized and as the major constituent of the edible plant artichoke, which has a history of safe dietary use. In summary, cynaropicrin is a promising bioactive natural product that, with minor hit-to-lead optimization, might be developed as a drug for HCV.
含有洋蓟苦素的植物，尤其是洋蓟，其不同的药理特性已为人所知达数百年之久。最近，洋蓟苦素对所有丙型肝炎病毒（HCV）基因型均表现出潜在活性。洋蓟苦素还展现出广泛的其他药理特性，如抗高血脂、抗锥虫、抗疟疾、拒食、解痉、抗光老化和抗肿瘤作用，以及激活苦味感觉受体和抗炎特性（例如，与抑制关键的促炎NF-κB途径相关）。这些药理作用是其对HCV具有出色活性的非常有利的因素。从结构上看，洋蓟苦素可能被视为一种潜在的药物候选物，因为它没有违反五规则，并且其水溶性可以允许制成治疗性注射剂。此外，洋蓟苦素是一种小分子，易于合成，并且作为可食用植物洋蓟的主要成分，具有安全的饮食使用历史。总之，洋蓟苦素是一种有前景的生物活性天然产物，经过轻微的从苗头化合物到先导化合物的优化，可能被开发为一种治疗HCV的药物。
