Sáez Juan C, Burrell Justin C, Cahill Catherine M, Cullen D Kacy, Devi Lakshmi A, Gilbert Ryan J, Graham Zachary A, Gurvich Vadim J, Havton Leif A, Iyengar Ravi, Khanna Rajesh, Palermo Edmund F, Siddiq Mustafa, Toro Carlos A, Vasquez Walter, Zhao Wei, Cardozo Christopher P
Instituto de Neurociencias, Centro Interdisciplinario de Neurociencia, Universidad de Valparaíso, Valparaíso, Chile.
Center for Neurotrauma, Neurodegeneration and Restoration, CMC VA Medical Center, Philadelphia, PA, United States.
Front Pharmacol. 2024 Sep 13;15:1427147. doi: 10.3389/fphar.2024.1427147. eCollection 2024.
Over the past decade, boldine, a naturally occurring alkaloid found in several plant species including the Chilean Boldo tree, has garnered attention for its efficacy in rodent models of human disease. Some of the properties that have been attributed to boldine include antioxidant activities, neuroprotective and analgesic actions, hepatoprotective effects, anti-inflammatory actions, cardioprotective effects and anticancer potential. Compelling data now indicates that boldine blocks connexin (Cx) hemichannels (HCs) and that many if not all of its effects in rodent models of injury and disease are due to CxHC blockade. Here we provide an overview of boldine's pharmacological properties, including its efficacy in rodent models of common human injuries and diseases, and of its absorption, distribution, pharmacokinetics, and metabolism.
在过去十年中,波尔定碱,一种存在于包括智利波尔多树在内的多种植物中的天然生物碱,因其在人类疾病啮齿动物模型中的功效而受到关注。一些归因于波尔定碱的特性包括抗氧化活性、神经保护和镇痛作用、肝脏保护作用、抗炎作用、心脏保护作用和抗癌潜力。现在有令人信服的数据表明,波尔定碱可阻断连接蛋白(Cx)半通道(HCs),并且在损伤和疾病的啮齿动物模型中,其许多(如果不是全部)作用都归因于CxHC阻断。在此,我们概述了波尔定碱的药理特性,包括其在常见人类损伤和疾病啮齿动物模型中的功效,以及其吸收、分布、药代动力学和代谢情况。