Department of Pharmacology, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Erandwane, Pune, 411038, Maharashtra, India.
Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune, 411038, India.
Neurochem Res. 2023 Nov;48(11):3283-3295. doi: 10.1007/s11064-023-03992-y. Epub 2023 Jul 18.
Boldine is an alkaloid obtained from the medicinal herb Peumus boldus (Mol.) (Chilean boldo tree; boldo) and belongs to the family Monimiaceae. It exhibits a wide range of pharmacological effects such as antioxidant, anticancer, hepatoprotective, neuroprotective, and anti-diabetic properties. There is a dearth of information regarding its pharmacokinetics and toxicity in addition to its potential pharmacological activity. Boldine belongs to the aporphine alkaloid class and possesses lipophilic properties which enable its efficient absorption and distribution throughout the body, including the central nervous system. It exhibits potent free radical scavenging activity, thereby reducing oxidative stress and preventing neuronal damage. Through a variety of neuroprotective mechanisms, including suppression of AChE and BuChE activity, blocking of connexin-43 hemichannels, pannexin 1 channel, reduction of NF-κβ mediated interleukin release, and glutamate excitotoxicity which successfully reduces neuronal damage. These results point to its probable application in reducing neuroinflammation and oxidative stress in epilepsy, Alzheimer's disease (AD), and Parkinson's disease (PD). Moreover, its effects on serotonergic, dopaminergic, opioid, and cholinergic receptors were further investigated in order to determine its applicability for neurobehavioral dysfunctions. The article investigates the pharmacokinetics of boldine and reveals that it has a low oral bioavailability and a short half-life, requiring regular dosage to maintain therapeutic levels. The review studies boldine's potential therapeutic uses and mode of action while summarizing its neuroprotective benefits. Given the favorable results for boldine as a potential neurotherapeutic drug in laboratory animals, more research is required. However, in order to optimise its therapeutic potential, it must be more bioavailable with fewer detrimental side effects.
-boldine 是一种从药用植物 Peumus boldus（Mol.）（智利 Boldo 树；Boldo）中提取的生物碱，属于铁青树科。它具有广泛的药理作用，如抗氧化、抗癌、保肝、神经保护和抗糖尿病作用。除了潜在的药理活性外，关于其药代动力学和毒性的信息很少。Boldine 属于阿朴啡生物碱类，具有亲脂性，能够有效地吸收和分布到全身，包括中枢神经系统。它具有强大的自由基清除活性，从而减少氧化应激和防止神经元损伤。通过多种神经保护机制，包括抑制 AChE 和 BuChE 活性、阻断 connexin-43 半通道、pannexin 1 通道、减少 NF-κβ 介导的白细胞介素释放以及谷氨酸兴奋性毒性，成功减少神经元损伤。这些结果表明它可能在减少癫痫、阿尔茨海默病（AD）和帕金森病（PD）中的神经炎症和氧化应激方面具有应用潜力。此外，还进一步研究了其对 5-羟色胺能、多巴胺能、阿片能和胆碱能受体的影响，以确定其在神经行为功能障碍方面的适用性。本文研究了 boldine 的药代动力学，发现其口服生物利用度低，半衰期短，需要定期剂量维持治疗水平。综述研究了 boldine 的潜在治疗用途和作用模式，总结了其神经保护益处。鉴于 boldine 在实验室动物中作为一种有潜力的神经治疗药物的良好结果，需要进行更多的研究。然而，为了优化其治疗潜力，必须提高其生物利用度，减少有害的副作用。
