Royal Botanic Gardens, Jodrell Laboratory, Kew, Richmond, Surrey, UK.
Drugs Aging. 2011 Jun 1;28(6):439-68. doi: 10.2165/11591310-000000000-00000.
Dementia pathologies such as Alzheimer's disease (AD) are reaching epidemic proportions, yet they are not successfully managed by effective symptomatic treatments. Only five drugs have been developed to alleviate cognitive symptoms, and more effective and safe treatments are needed for both the cognitive symptoms and behavioural and psychological symptoms of dementia (BPSD). As two of these licensed drugs (cholinesterase inhibitors [ChEIs]) are naturally derived (galantamine and rivastigmine), the potential for plants to yield new therapeutic agents has stimulated extensive research to discover new ChEIs together with plant extracts, phytochemicals and their derivatives with other mechanistic effects relevant to dementia treatment. This review presents the potential and actual therapeutic strategies for dementia in relation to the known mechanisms of dementia pathology. Phytochemicals that have shown mechanistic effects relevant to the pathological targets in dementia are discussed, with an emphasis on those showing positive clinical trial evidence. Those phytochemicals discussed include the alkaloid physostigmine, a ChEI from the calabar bean (Physostigma venenosum), which has been used as a template for the development of synthetic derivatives that inhibit acetylcholinesterase, including the drug rivastigmine. Also discussed are other ChEI alkaloids including huperzine A, from Huperzia serrata, and galantamine, originally from the snowdrop (Galanthus woronowii); both alkaloids improve cognitive functions in AD patients. Other phytochemicals discussed include cannabinoids (e.g. cannabidiol) from Cannabis sativa, which are emerging as potential therapeutic agents for BPSD, and resveratrol (occurs in various plants) and curcumin (from turmeric [Curcuma longa]), which have been investigated for their pharmacological activities relevant to dementia and their potential effects on delaying dementia progression. The review also discusses plant extracts, and their known constituents, that have shown relevant mechanistic effects for dementia and promising clinical data, but require more evidence for their clinical efficacy and safety. Such plants include Ginkgo biloba, which has been extensively studied in numerous clinical trials, with most outcomes showing positive effects on cognitive functions in dementia patients; however, more reliable and consistent clinical data are needed to confirm efficacy. Other plants and their extracts that have produced promising clinical data in dementia patients, with respect to cognition, include saffron (Crocus sativus), ginseng (Panax species), sage (Salvia species) and lemon balm (Melissa officinalis), although more extensive and reliable clinical data are required. Other plants that are used in traditional practices of medicine have been suggested to improve cognitive functions (e.g. Polygala tenuifolia) or have been associated with alleviation of BPSD (e.g. the traditional prescription yokukansan); such remedies are often prescribed as complex mixtures of different plants, which complicates interpretation of pharmacological and clinical data and introduces additional challenges for quality control. Evidence for the role of natural products in disease prevention, the primary but considerably challenging aim with respect to dementia, is limited, but the available epidemiological and clinical evidence is discussed, with most studies focused on ChEIs, nicotine (from Nicotiana species), curcumin, wine polyphenols such as resveratrol and G. biloba. Challenges for the development of phytochemicals as drugs and for quality control of standardized plant extracts are also considered.
痴呆症病理,如阿尔茨海默病(AD),正达到流行程度,但有效的对症治疗方法并不能成功地控制这些疾病。目前只有五种药物被开发出来用于缓解认知症状,对于痴呆症的认知症状以及行为和心理症状(BPSD),还需要更有效和安全的治疗方法。由于其中两种已获得许可的药物(胆碱酯酶抑制剂[ChEIs])是天然来源的(加兰他敏和利斯的明),植物产生新的治疗剂的潜力刺激了广泛的研究,以发现新的 ChEIs 以及具有其他与痴呆症治疗相关的机制作用的植物提取物、植物化学物质及其衍生物。本综述介绍了与痴呆症病理的已知机制相关的痴呆症的潜在和实际治疗策略。讨论了具有与痴呆症病理靶标相关的机制作用的植物化学物质,重点介绍了那些具有阳性临床试验证据的物质。所讨论的植物化学物质包括生物碱石杉碱甲,一种来自毒蕈碱(Physostigma venenosum)的 ChEI,它已被用作开发抑制乙酰胆碱酯酶的合成衍生物的模板,包括药物利斯的明。还讨论了其他 ChEI 生物碱,包括来自蛇足石杉(Huperzia serrata)的石杉碱甲和最初来自雪花莲(Galanthus woronowii)的加兰他敏;这两种生物碱都能改善 AD 患者的认知功能。所讨论的其他植物化学物质包括大麻(Cannabis sativa)中的大麻素(例如大麻二酚),它们作为 BPSD 的潜在治疗剂正在出现,以及白藜芦醇(存在于各种植物中)和姜黄素(来自姜黄[Curcuma longa]),它们的药理学活性与痴呆症有关,并且可能对延缓痴呆症的发展有潜在影响。该综述还讨论了植物提取物及其已知成分,它们对痴呆症具有相关的机制作用和有希望的临床数据,但需要更多的证据来证实其临床疗效和安全性。此类植物包括银杏,已在许多临床试验中进行了广泛研究,大多数结果表明对痴呆症患者的认知功能有积极影响;然而,需要更可靠和一致的临床数据来证实疗效。其他植物及其提取物在痴呆症患者的认知方面产生了有希望的临床数据,包括藏红花(Crocus sativus)、人参(Panax 属)、鼠尾草(Salvia 属)和柠檬香脂(Melissa officinalis),尽管需要更广泛和可靠的临床数据。其他用于传统医学实践的植物被认为可以改善认知功能(例如远志),或者与缓解 BPSD 有关(例如传统处方 Yokukansan);这些疗法通常作为不同植物的复杂混合物开处方,这使得对药理学和临床数据的解释变得复杂,并为质量控制带来了额外的挑战。关于天然产物在疾病预防中的作用的证据(痴呆症的主要但具有相当挑战性的目标)是有限的,但讨论了现有的流行病学和临床证据,大多数研究都集中在 ChEIs、尼古丁(来自 Nicotiana 属)、姜黄素、葡萄酒多酚(如白藜芦醇和银杏)上。还考虑了植物化学物质作为药物的开发和标准化植物提取物的质量控制的挑战。