The Protective Effect of Icariin on Mitochondrial Transport and Distribution in Primary Hippocampal Neurons from 3× Tg-AD Mice

Icariin, a pharmacologically active component isolated from the Chinese herb Epimedium, has been shown to improve spatial learning and memory abilities in Alzheimer’s disease (AD) rats through inhibition of Aβ production and tau protein hyperphosphorylation. However, the potential mechanism of icariin-induced protective effects against mitochondrial dysfunctions in AD still remains unclear. In the present study, we investigated the effect of icariin on the modulation of mitochondrial transport and distribution in primary hippocampal cultures from triple-transgenic (3× Tg) AD mice. The results showed that icariin enhanced mitochondrial motility and increased mitochondrial index and mitochondrial length and size in the diseased neurons. Additionally, the expression of the key mitochondrial enzyme, pyruvate dehydrogenase-E1α (PDHE1α), and the post synaptic density protein 95 (PSD95), was preserved in AD neurons after icariin treatment, accompanied by a downregulation of Aβ and phosphorylated tau expression in the corresponding areas. Further study showed that icariin treatment resulted in a decrease in mitochondrial fission protein dynamin-related protein 1 (Drp1) and an increase in fusion protein Mitofusin 2 (Mfn2). These data indicate that icariin can promote mitochondrial transport, protect mitochondria against fragmentation and preserve the expression of mitochondrial and synaptic functional proteins in AD neurons. Thus, icariin may be a potential therapeutic complement for AD and other mitochondrial malfunction-related neuronal degenerative diseases.     

水解淫羊藿苷糖基的土壤细菌筛选

从20种土壤细菌中筛选出了对淫羊藿苷水解能力高的菌株Rhodanobncter sp．GS3054．该菌株30℃下发酵3～4d的发酵液提酶后对淫羊藿苷水解能力最佳；水解淫养藿苷成低糖基苷的最适反应条件为：50℃、pH6．0、底物20mg／mL，反应时间24h．     

古汉养生精中主要成分的HPLC法分析

采用高效液相色谱法测定古汉养生精中主要成分淫羊霍苷和黄芪甲苷。淫羊霍苷和黄芪甲苷的线性范围分别为0.094～0.470mg／mL和0.012～0．060mg／mL,回收率分别为98．69％和101．35％,相对标准偏差分别为0．48％和0．77％。     

Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review

In recent years, there has been considerable interest in icariin (ICA) and its derivates, icariside II (ICS) and icaritin (ICT), due to their wide range of potential applications in preventing cancer, cardiovascular disease, osteoporosis, delaying the effects of Alzheimer’s disease, treating erectile dysfunction, etc. However, their poor water solubility and membrane permeability, resulting in low bioavailability, dampens their potential beneficial effects. In this regard, several strategies have been developed, such as pharmaceutical technologies, structural transformations, and absorption enhancers. All these strategies manage to improve the bioavailability of the above-mentioned flavonoids, thus increasing their concentration in the desired places. This paper focuses on gathering the latest knowledge on strategies to improve bioavailability for enhancing the efficacy of icariin, icariside II, and icaritin. We conclude that there is an opportunity for many further improvements in this field. To the best of our knowledge, no such review articles scoping the bioavailability improvement of icariin and its derivates have been published to date. Therefore, this paper can be a good starting point for all those who want to deepen their understanding of the field.     

补肾健骨片水煎药材的提取、纯化及制剂工艺研究

研究了补肾健骨片水煎煮药材的提取、纯化及制剂工艺。采用正交设计法以淫羊藿苷含量、醇浸出物量为指标对提取工艺条件进行优化,采用离心法和醇沉法对除杂工艺进行比较,在制剂成型工艺中,对辅料进行筛选并确定用量。最佳提取工艺为药材加10倍量的水,浸泡1.0 h,回流提取2次,每次1.0 h,采用离心法除去杂质,每个处方的辅料用量为:1倍量的碳酸钙,质量分数为10%的糊精、0.5%的微晶纤维素和0.3%的硬脂酸镁。该工艺可以用于制备补肾健骨片。     

淫羊藿苷糖苷酶产生菌的筛选及其酶反应条件

从6株微生物菌株中筛选出了高产淫羊藿苷糖苷酶的菌株Absidasp.E9r,该菌所产淫羊藿苷糖苷酶能将多糖基的淫羊藿苷水解成低糖基的淫羊藿苷。通过实验确定了该淫羊藿苷糖苷酶的最适反应条件:pH值4.0,反应温度50℃,底物质量浓度20 mg/mL,反应时间20 h。     

碳酸钙复合胶囊的增强骨密度功能作用及安全性评价

该研究旨在评价一种碳酸钙复合胶囊（Calcium Carbonate Compound Capsule,Ca-CC）增强骨密度功能作用和安全性。经口给予60只雌性大鼠低（0.18 g/kg·bw）、中（0.35 g/kg·bw）、高（1.05 g/kg·bw）三个剂量的Ca-CC 90 d的干预。通过测定雌性大鼠生长发育指标、股骨骨密度、骨钙含量在评估增强骨密度功能作用。结果显示：高剂量组Ca-CC(1.05g/kg·bw)增强大鼠的股骨远心端、股骨中心骨密度分别为7.39%(P<0.05)、8.29%(P<0.01),增强骨钙含量为29.70%(P<0.01)。通过给予昆明种小鼠20.00 g/kg·bw剂量的Ca-CC进行安全性评价。在受试剂量范围内,Ca-CC无诱发菌株突变、精子畸变、解剖及组织学检查异常等现象。在30 d观察期,以0.88、1.75、3.50g/kg·bw为剂量的低、中、高三个剂量组中,Ca-CC对试验小鼠各项生理指标均无影响。以上结果表明,Ca-CC具有增强骨密度功能作用且安全性良好。     

高产淫羊藿苷酶菌种的筛选

从泡菜汁中分离出了高产淫羊藿苷酶的乳酸菌,提酶后检验了酶水解淫羊藿苷的能力,从中筛出能够高产淫羊藿苷酶的菌株,其特征与植物乳杆菌极为相似.该菌产酶对淫羊藿总苷中多糖基淫羊藿苷具有很好的水解作用,可以得到60%~70%的淫羊藿苷酶解产物,是一种安全高效的新菌.     

In Silico Insight into Potential Anti-Alzheimer’s Disease Mechanisms of Icariin

Herbal compounds that have notable therapeutic effect upon Alzheimer''s disease (AD) have frequently been found, despite the recent failure of late-stage clinical drugs. Icariin, which is isolated from Epimedium brevicornum, is widely reported to exhibit significant anti-AD effects in in vitro and in vivo studies. However, the molecular mechanism remains thus far unclear. In this work, the anti-AD mechanisms of icariin were investigated at a target network level assisted by an in silico target identification program (INVDOCK). The results suggested that the anti-AD effects of icariin may be contributed by: attenuation of hyperphosphorylation of tau protein, anti-inflammation and regulation of Ca²⁺ homeostasis. Our results may provide assistance in understanding the molecular mechanism and further developing icariin into promising anti-AD agents.