从中药益母草中提取的益母草碱对治疗脑中风具有明显疗效，能减少脑缺血造成的大脑皮质的梗死面积，改善神经功能缺损的症状。复旦大学药学院院长朱依谆教授率领其团队经五年多时间研究的这一成果，目前已作为国家一类新药候选药物在国家重大新药创制大平台孵育，并在最新一期（11月）国际脑中风疾病研究方面的最权威杂志《Stroke》上发表。
随着人口的老龄化，心脑血管疾病已成为我国第一死亡率的杀手, 脑中风导致的死亡则是威胁中国人健康的最重要因素之一。研究与开发治疗脑中风的特效药，日益受到医药科研工作者的广泛关注。
益母草具有改善血液循环、活血祛瘀的功效，是传统的妇科用药。由于提取益母草中的有效复合物成本高、工作量大，其单体有效成分的科学价值一直没有被系统完整地发掘出来。朱依谆教授从益母草具有改善血液循环这一独特功效得到启发，率领他的研究团队持续努力，探索出全新的合成路线和放大工艺，终于从益母草中成功提取到有效单体化合物――益母草碱，并已将其命名为“SCM-198”。
研究发现，在疾病状态下（如缺血、缺氧时），构成完整细胞基本元素之一的“线粒体”就会肿胀，造成细胞破裂，从而使脑组织坏死和心肌坏死，最后导致死亡。人体内的三磷酸腺苷是体内组织细胞活动所需能量的直接来源，细胞缺氧时，三磷酸腺苷的能量活性也会降低，导致细胞凋亡。而SCM-198的作用机制是通过降低脑细胞耗氧量，抑制线粒体氧化应激反应造成的细胞死亡，并激发三磷酸腺苷的活性，阻止细胞的进一步坏死、凋亡，以达到减少脑组织坏死的目的。在国家重大新药创制计划和国家杰出青年科学基金和上海市重点项目支持下，SCM-198的成药性研究即将完成。
《Stroke》杂志认为，“SCM-198”的成功研发，可能使益母草中的有效单体化合物成为未来临床上治疗脑中风的新型药物。
推荐原文出处：
Stroke. 41(11):2661-2668
Leonurine Protects Middle Cerebral Artery Occluded Rats Through Antioxidant Effect and Regulation of Mitochondrial Function.
Loh, Kok Poh PhD *; Qi, Jia MD *; Tan, Benny Kwong Huat MD, PhD; Liu, Xin Hua MD, PhD; Wei, Bang Guo PhD; Zhu, Yi Zhun MD, PhD
Abstract:
Background and Purpose-: Oxidative stress is known to be involved in ischemic stroke. Intense interest is drawn to the therapeutic potential of Chinese herbs on ischemic stroke because many of them contain antioxidant properties. Leonurine, 1 of the active compounds from purified Herba Leonuri, was studied to evaluate its possible therapeutic effects on ischemic stroke.
Method-: Middle cerebral artery occlusion was selected as our model of study. The animals were pretreated with Leonurine orally for 7 days and the surgery was done. One day after surgery, 2,3,5-triphenyltetrazolium chloride staining and neurological deficit score were carried out to evaluate the functional outcome of animals, whereas levels of superoxide dismutase, glutathione peroxidase, and malondialdehyde were analyzed for oxidative stress analysis. For mitochondrial studies, 3 hours after surgery, mitochondria were isolated for analysis of reactive oxygen species production, adenosine triphosphate biosynthesis, oxygen consumption, and respiratory control ratio value.
Result-: In in vivo experiments, Leonurine pretreatment reduced infarct volume, improved neurological deficit in stroke groups, increased activities of antioxidant enzymes superoxide dismutase and glutathione peroxidase, and decreased levels from the lipid peroxidation marker malondialdehyde. In terms of mitochondrial modulation, Leonurine inhibited mitochondrial reactive oxygen species production and adenosine triphosphate biosynthesis. Animal studies also demonstrated that the mitochondrial function and redox state were restored by Leonurine treatment.
Conclusions-: Leonurine has neuroprotective effects and carries a therapeutic potential of stroke prevention.
