Search

Alzheimer's disease (AD) is a progressive, neurodegenerative disorder that currently has reached epidemic proportions among elderly populations around the world. In China, available traditional Chinese medicines (TCMs) that organically combine functional foods with medicinal values are named "Medicine Food Homology (MFH)". In this review, we focused on MFH varieties for their traditional functional features, substance bases, clinical uses, and mechanisms of action (MOAs) for AD prevention and treatment. We consider the antiAD active constituents from MFH species, their effects on in vitro/in vivo AD models, and their drug targets and signal pathways by summing up the literature via a systematic electronic search (SciFinder, PubMed, and Web of Science). In this paper, several MFH plant sources are discussed in detail from in vitro/in vivo models and methods, to MOAs. We found that most of the MFH varieties exert neuroprotective effects and ameliorate cognitive impairments by inhibiting neuropathological signs (Aβ-induced toxicity, amyloid precursor protein, and phosphorylated Tau immunoreactivity), including anti-inflammation, antioxidative stress, antiautophagy, and antiapoptosis, etc. Indeed, some MFH substances and their related phytochemicals have a broad spectrum of activities, so they are superior to simple single-target drugs in treating chronic diseases. This review can provide significant guidance for people's healthy lifestyles and drug development for AD prevention and treatment.

Huang-Lian-Jie-Du Decoction (HLJDD), a well-known traditional Chinese formulation, has been proved to exert neuroprotective effects, however, the bioactive components in HLJDD still remain to be elucidated. In the present study, a rapid and effective method involving live cell biospecific extraction and HPLC-Q-Orbitrap HRMS/MS was utilized to rapidly screen and identify the neuroprotective compounds from the HLJDD crude extract directly. Firstly, sixteen principal components in HLJDD crude extract were identified by HPLC-Q-Orbitrap HRMS/MS analysis. After co-incubation with PC12 cells, which have been validated as the key target cells for neurodegenerative diseases, seven compounds of them were demonstrated to exhibit binding affinity to the target cells. Furthermore, three representative compounds named baicalin, wogonoside, and berberine were subsequently verified to exert cytoprotective effects on PC12 cells injured by hydrogen peroxide via inhibiting oxidative stress and cell apoptosis, indicating that these screened compounds may possess a potential for the treatment of neurodegenerative diseases and were responsible, in part at least, for the neuroprotective beneficial effects of HLJDD. Taken together, our study provides evidence that live cell biospecific extraction coupled with LC-HRMS/MS technique is an efficient method for rapid screening potential bioactive components in traditional Chinese medicines., (Copyright © 2021 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: Buyang Huanwu Decoction (BHD) is a multi-herbal composition commonly prescribed in the treatment of cerebrovascular diseases such as stroke. Although studies have been conducted at the cellular (in vitro), animal and human (in vivo) level, there was no detailed analysis on how the composition and proportion of BHD is modified according to target diseases., Aim of Study: The purpose of this study is to investigate the composition and proportion of each herb in BHD to summarize how the original BHD was modified according to the target disease., Materials and Methods: Electronic literature searches were performed in three databases, collecting sixty-eight studies for the final analysis. The studies were divided into three types: cell studies, animal experiments and clinical trial. In the analysis, the decoction formula including the composition and the weight proportion of the herbs in BHD used in the studies and the target diseases were examined., Results: The result showed that in cell studies, the targets were mostly cell differentiation, cell injury and immune activation. In animal studies, cerebrovascular diseases such as cerebral ischemia were the most identified target diseases followed by nervous system and cardiovascular diseases. While the proportions of the herbs in BHD used in these studies were in general similar to the original formula, some studies reduced the amount of Astragali Radix to half of the original amount. Modified BHDs were used in four studies for cerebrovascular and peripheral nerve diseases. However, no significant correlation has been observed between the target diseases and the change of the proportion of the herbs in BHD., Conclusions: The most commonly used formula was the original composition of BHD, and modified BHDs were reported to be used to treat cerebrovascular and nervous diseases. Further studies about the effects of BHD by composition and proportion of herbs are needed in the future., (Copyright © 2020 Elsevier B.V. All rights reserved.)

Bojungikgi-tang (BJIGT; Bu Zhong Yi Qi Tang in China, Hochuekkito in Japan) is a traditional Oriental herbal formula comprised of eight medicinal herbs that has long been used for the treatment of digestive disorders. A recent clinical study from South Korea reported that BJIGT-gamibang administration may be effective in treating dementia. We aimed to establish scientific evidence for the anti-dementia effects of BJIGT using in vitro and in vivo experimental models. We measured amyloid- β (Aβ) aggregation, β-secretase (BACE), and antioxidant activity in a cell free system. Neuroprotective effects were assessed using CCK-8. Imprinting control region (ICR) mice were divided into the following six groups: Normal control, Aβ-injected, Aβ-injection + oral BJIGT gavage (200, 400, or 800 mg/kg/day), and Aβ-injection + oral morin administration (10 mg/kg/day). Subsequently, behavioral evaluations were conducted and brain samples were collected from all the animals and assessed. BJIGT enhanced inhibition of Aβ aggregation and BACE activity in vivo, as well as antioxidant activity in in vitro, cell-free systems. BJIGT also exerted neuroprotective effects in a hydroperoxide (H₂O₂)-induced damaged HT22 hippocampal cell line model. In addition, BJIGT administration significantly ameliorated cognitive impairments in Aβ-injected mice, as assessed by the passive avoidance and Y-maze tests. Furthermore, BJIGT treatment suppressed Aβ aggregation and expression, as well as expression of Aβ, NeuN, and brain-derived neurotrophic factor (BDNF) in the hippocampi of Aβ-injected mice. Overall, our results demonstrate that, with further testing in clinical populations, BJIGT may have great utility for the treatment of dementia and especially Alzheimer's disease.

Oxidative stress, a predominant cause of apoptosis cascades triggered in neurodegenerative disorders, has been regarded as a critical inducement in the pathogenesis of Alzheimer's disease (AD). Gou Teng-San (GTS) is a traditional Chinese herbs preparation commonly utilized to alleviate cognitive dysfunction and psychological symptoms of patients with dementia. The present study aimed to investigate the protective effects of GTS40, an active fraction of GTS, on H 2 O 2 -induced oxidative damage and identify the potential active ingredients. Our results revealed that GTS40 exhibited radical scavenging activity, elevated cell viability, decreased the levels of intracellular reactive oxygen species (ROS), and stabilized mitochondrial transmembrane potential (MMP) in H 2 O 2 -treated PC12 cells. In addition, GTS40 blocked the apoptotic cascade by reversing the imbalance of Bcl-2/Bax and inhibiting the activity of caspase-3. Furthermore, an HPLC-QTOFMS method was developed to characterize major chemical constituents in GTS40. Our results revealed twenty-seven identified or tentatively characterized compounds through comparing their retention time (t R ) and MS spectra with reference standards. These results suggested that GTS40 was a promising active fraction that may be beneficial in the prevention and treatment of oxidative stress-mediated neurodegenerative disorders., (Copyright © 2017 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Yi-Gan San (YGS), a traditional Chinese medicine for dementia-related symptoms, was previously fractionated. One active fraction, YGS40 exhibited a neuroprotective effect against glutamate-induced cytotoxicity. In the present study, high-performance liquid chromatography, coupled with diode-array detection and quadrupole time-of-flight mass spectrometry, was applied for the identification of its chemical constituents and for quantification studies. The chemical profile of YGS40 consisted of sixty-four identified or tentatively characterized compounds. The levels of the major marker compounds increased significantly in the mixed decoction compared with those in the single plant decoction. The results suggest the high precision of the analyses of most of the constituents in YGS40 and establish the quantitative variations of the major marker compounds between the single and mixed decoction processes., (Copyright © 2014 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

This study developed a method for rapid screening neuroprotective compounds with FDA (fluorescein diacetate) labeled SH-SYSY cells, which was injuried by Glu (L-glutamic acid). The cell viability was determined by fluorescence automatic mi-croscopy screening system. Then, neuroprotective components from Gegen Qinlian decoction were screened by the proposed method. The results demonstrated that 4 chemical components, C15, D06, D07 and E05 from Gegen Qinlian decoction, showed significantly neuroprotective effects. Furthermore, 8 compounds (i. e. daidzin, 3'-methoxydaidzin, liquiritin apioside, 6-C-L-alpha-arabinopyranosyl-8-C-beta-D-glucopyranosyl chrysin, isoliquiritin apioside, baicalin, oroxylin-A-7-O-fP-D-glucuronide and wogonoside) were identified from these active components by LC-Q/TOF-MS technology (liquid chromatography quadrupole time of flight tandem mass spectrometry). These 8 compounds may be the potential neuroprotective substances in Gegen Qinlian decoction.

Objective: To analyse the muscone from serum and cerebrospinal fluid (CSF) of rabbits after intragastric administration of Tongqiao Huoxue granules (TQHXG) and provide the partial experimental reference on laying down quality standard of preparation of formula and offer new ideas on studying the relation between pharmacodynamics and its effective component of formula., Methods: Muscone from TQHXG was qualitative identified by the methods of thin-layer chromatography (TLC) and gas chromatography (GC). Muscone from blood and CSF of rabbits was examined by GC after intragastric administration of TQHXG. Compared with standard reference material of muscone, blank serum and blank CSF, the segmental component absorbed into CSF of rabbits was confirmed., Results: Spots of TQHXG on the chromatomap showed the same colour at the corresponding locality of the standard reference material. Detected by GC, chromatographic peaks appeared at the retention time of 4.8 minute in the chromatomaps of the serum with TQHXG, the CSF with TQHXG and standard reference material of muscone, while there were no chromatographic peaks in the chromatomaps of the blank serum, the blank CSF and methanol at the same time. The ingredient corresponding the chromatographic peaks at the retention time of 4.8 minute in the chromatomaps of the serum, CSF with TQHXG should be muscone., Conclusion: Muscone from TQHXG could penetrate blood brain barrier and could be one index of quality standard of preparation of TQHXG.

Ethnopharmacological Relevance: BAIMAI-SAN prescription is a famous Chinese minority complex prescription used for curing neuropathy., Materials and Methods: The Effective Compounds Groups of BAIMAI-SAN (ECGBM) is determined by high through-put screening, and it includes picroside II, verbascose, taurine and ellagic acid and borneol. To research the potential protective effect of ECGBM on the function of peripheral neuropathy, diabetic rats with peripheral neuropathy were induced by streptozotocin and treated with ECGBM (0.1, 0.3, 0.9 mg/kg/day i.g.) for 75 days. Primary cortical neuronal cultures were subjected to high d-glucitol, and treated with ECGBM prophylactically., Results: The administration resulted in reductions in speed of sciatic motor nerve conduction velocity (MNCV), sensory nerve conduction velocity (SNCV) and response speed to pain in the sciatic nerve fiber. Data from primary cortical neuronal cultures experiments indicated that neuronal survival rates were increased, and LDH release was decreased and the loss of neurite length was alleviated in ECGBM group., Conclusions: It is first report that ECGBM could protect the peripheral neuron in diabetic rat in vivo and in vitro. This activity may be associated with the neuron protective effect., (Crown Copyright © 2011. Published by Elsevier Ireland Ltd. All rights reserved.)

Paeoniflorin is one of the bioactive components of Paeonia lactiflora, a traditional Chinese herbal medicine. Some recent studies prove its distinguished neuroprotective effect. These neuroprotective mechanisms have become hot points and show closely correlated to activating adenosine A1 receptor, ameliorating the function of cholinergic nerve, regulating ion channel homeostasis, retarding oxidative stress and apoptosis of the neurocytes, promoting nerve growth, having an influence on astrocytes and being ableto penetrate though blood brain barrier. In this review, we present the neuroprotective mechanisms of paeoniflorin in the following eight aspects.

The lipid soluble fraction of curcuma longa, i.e. herbal medicament (HM) was isolated from rhizome of curcuma longa by solvent extraction method. The identification of chemical constituent present in HM was done with GC, GC-MS. The standardization of HM was done using HPLC method on the basis of three-marker compound isolated, i.e. ar-turmerone, turmerone and curlone. The effect of temperature, pH and light on stability of marker compounds of HM was studied. The composition of marker compound in HM was found to be 50-60%. The content of curcumnoids, another bioactive constituent present in HM was found to be 0.32-0.55%. The HM was found to be stable at different temperature and pH but light sensitive.

A rapid, simple and reliable high performance liquid chromatography (HPLC) method has been established for the analysis of the major alkaloids in Huperzia serrata, a traditional Chinese medicine (TCM) herb. After chromatographic separation on a reversed-phase C18 column with methanol-ammonium acetate (pH 6.0; 80 mM, 30/70, v/v) as the mobile phase, nine alkaloid compounds in the alkaloid extracts of H. serrata were identified by online diode array detection-MS and by comparing with data from literature and standard samples. One compound in the extract, huperzine A, is a drug for treating Alzheimer's disease. Its content was quantified by HPLC coupled with UV-vis. The method was the validated. The recovery rates were 96.8-97.7% with R.S.D <2.44%. The intra- and inter-day precisions, expressed as R.S.D., ranged from 0.53% to 1.51%. Good linear regression was observed in the concentration range of 5-100 microg/ml (r = 0.9997). The results demonstrate that this method is simple, selective, and suitable for the quality control of this TCM herb.