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Minzhen Deng, Liping Huang, Baile Ning, Nanbu Wang, Qinxin Zhang, Caixia Zhu, Yongqi Fang
Alzheimer's disease (AD) is the most common neurodegenerative disorder in the elderly, and studies have suggested that β-asarone has pharmacological effects on beta-amyloid (Aβ) injected in the rat hippocampus. However, the effect of β-asarone on autophagy in the APP/PS1 transgenic mouse is unreported. APP/PS1 transgenic mice were randomly divided into six groups (n=10/group): an untreated group, an Aricept-treated group, a 3-MA-treated group, a rapamycin-treated group, an LY294002-treated group, a β-asarone-treated group...
October 10, 2016: Brain Research
Mercedes Unzeta, Gerard Esteban, Irene Bolea, Wieslawa A Fogel, Rona R Ramsay, Moussa B H Youdim, Keith F Tipton, José Marco-Contelles
HIGHLIGHTS ASS234 is a MTDL compound containing a moiety from Donepezil and the propargyl group from the PF 9601N, a potent and selective MAO B inhibitor. This compound is the most advanced anti-Alzheimer agent for preclinical studies identified in our laboratory.Derived from ASS234 both multipotent donepezil-indolyl (MTDL-1) and donepezil-pyridyl hybrids (MTDL-2) were designed and evaluated as inhibitors of AChE/BuChE and both MAO isoforms. MTDL-2 showed more high affinity toward the four enzymes than MTDL-1...
2016: Frontiers in Neuroscience
Yuji Mano, Koichiro Hotta, Kazutomi Kusano
A simple and selective assay for the determination of donepezil (Aricept(®)) and its three metabolites including 6-O-desmethyl (M1), 5-O-desmethyl (M2) and N-oxide (M6) metabolites in human plasma was developed and validated using liquid chromatography with tandem mass spectrometry. An analog of donepezil was used as an internal standard (IS) for all the analytes. The analytes and the IS were extracted from plasma by solid-phase extraction. The analytes were chromatographically separated on Cadenza CD-C18 column with gradient elution, then detected with electrospray positive ionization in multiple reaction monitoring mode...
September 2016: Journal of Chromatographic Science
Zhi-tao Hou, Zhong-ren Sun, Song-tao Liu, Sheng-biao Xiong, Yi-tian Liu, Xiao-xia Han, Hong-fang Sun, Yu-sheng Han, Hong-na Yin, Jin-qiao Xu, Dong-dong Li
OBJECTIVE: To observe the effect of electroacupuncture (EA) therapy on levels of oxygen free radicals (OFR) and hippocampal apoptosis-related protein expression in ischemic learning-memory disorder rats so as to investigate its mechanisms underlying improvement of ischemic learning-memory impairment. METHODS: A total of 60 SD rats were randomly divided into sham operation (sham), model, medication, and EA groups, with 15 rats in each group. The learning-memory disorder model was made by occlusion of bilateral carotid arteries...
December 2015: Zhen Ci Yan Jiu, Acupuncture Research
Min-zhen Deng, Li-ping Huang, Yong-qi Fang
OBJECTIVE: To observe the effects of the co-administration of total ginsenosides and volatile oil of Acorus tatarinowii on the ability of learning and memory and apoptosis in Alzheimer's disease (AD) mice model induced by D-galactose and aluminium chloride. METHODS: 50 Kunming (KM) mice were randomly divided into normal group, model group, Aricept group (1 mg/kg), Ding Zhi Wan group (10 g/kg) and co-administration of total ginsenosides and volatile oil of Acorus tatarinowii group (co-administered group, the doses of volatile oil of Acorus tatarinowii and total ginsenosides were 30 mg/kg and 150 mg/kg, respectively)...
May 2015: Zhong Yao Cai, Zhongyaocai, Journal of Chinese Medicinal Materials
Mikio Sakakibara, Mitsuhiko Kido, Jun Kuribayashi, Hiroshi Okada, Ataru Igarashi, Hiroyuki Kamei, Toshitaka Nabeshima
OBJECTIVE: The pharmacological effects of generic (GE) donepezil are the same as Aricept, its brand-name counterpart. However, little is known as to whether these two drugs provide the same quality of life (QOL). The study subjects were patients with Alzheimer's disease who were taking donepezil hydrochloride tablets, and were selected by visiting either the local pharmacies or the patients' homes. We chose the brand-name drug Aricept and its GE form donepezil to investigate, from a long-term caregiver's perspective, the influence of both drugs on the patients' QOL...
August 31, 2015: Clinical Psychopharmacology and Neuroscience: the Official Scientific Journal of the Korean College of Neuropsychopharmacology
Songlin Chen, Xiaoli Yao, Yinying Liang, Weiyi Mei, Xiaoyun Liu, Changran Zhang
OBJECTIVE: To study the efficacy and safety of combined Traditional Chinese Medicine (TCM) therapy based on nourishing marrow to improve intellect and reinforcing Qi to activate bloodon mild to moderate Alzheimer's disease (AD). METHODS: Sixty-six patients with AD, whose Mini-Mental State Examination (MMSE) score were from 10-24, were randomized equally into an intervention group and a control group. The control group was given Aricept (5 mg, once daily). The intervention group was further divided into Yang-Qi deficiency (n = 18) and of Yin-Qi deficiency (n = 15) subgroups...
June 2015: Journal of Traditional Chinese Medicine, Chung i Tsa Chih Ying Wen Pan
Hai-yan Hu, Zhi-yu Chen, Dong-mei Xu, Yi-hui Zhang, Yi-ru Wang, Wen-hua Wang, Xiao-yan Zhang
OBJECTIVE: To explore the mechanism of three kinds extracts (saponins, volatile components, polysaccharide components) of Qingxin Kaiqiao Recipe (QKR) in improving learning and memory capabilities of Alzheimer's disease (AD) rats. METHODS: A controlled comparison method was used. Totally 56 male SD rats were randomly divided into seven groups, i.e., the normal control group, the sham-operation group, the model group, the Aricept group, the saponin group, the benzene group, and the polysaccharide group, 8 in each group...
May 2015: Chinese Journal of Integrated Traditional and Western Medicine
Heii Arai, Kenta Sumitomo, Yukinori Sakata, Kasumi Daidoji, Takao Takase, Tetsumi Toyoda
BACKGROUND: There have been very few long-term studies involving a large study population; existing studies usually have no more than a few hundred patients with Alzheimer's disease. For these reasons, there are no detailed investigations regarding changes in activities of daily living evaluated by the Functional Assessment Staging Test (FAST). METHODS: A long-term, large-scale observational study of donepezil hydrochloride (Aricept(®); Eisai Co., Ltd, Tokyo, Japan) is currently in progress...
March 2016: Psychogeriatrics: the Official Journal of the Japanese Psychogeriatric Society
Wei Gu, Xiao-Xian Jin, Yan-Jun Zhang, Zhen-Jie Li, Yang Kong
OBJECTIVE: To compare the differences in the clinical efficacy on Alzheimer's disease between acupuncture and medicine. METHODS: One hundred and forty-one patients were randomized into an acupuncture group (72 cases) and a medicine group (69 cases). In the acupuncture group, the needling technique for benefiting qi, promoting blood circulation, regulating mind and improving intelligence was used at Shenting (GV 24), Baihui (GV 20), Fengchi (GB 20), Wangu (GB 12), Danzhong (CV 17), Zhangwan (CV 12), Qihai (CV 6), Xuehai (SP 10) and Zusanli (ST 36)...
December 2014: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
Ying Wang, Ying Wang, Yi Sui, Hongshuang Yu, Xiaoheng Shen, Shengdi Chen, Gang Pei, Jian Zhao, Jianqing Ding
Alzheimer's disease (AD) is a common neurodegenerative disease affecting cognitive function in the elderly, which is characterized by the presence of extracellular deposits of insoluble amyloid-β plaques and neuronal loss. Modern pharmacology and drug development usually follow a single-target principle, which might contribute to the failure of most compounds in clinical trials against AD. Considering AD is a multifactorial disease, a combination therapeutic strategy that applies drugs with different mechanisms would be an alternative way...
2015: Journal of Alzheimer's Disease: JAD
Jinhuan Liu, Jun Chen, Zihu Tan, Qiong Yang, Hanchao Lan, Yilin Zhao, Changsheng Liu, Li Qiu
OBJECTIVE: To explore the therapeutic effect evaluation of proton magnetic resonance spectroscopy ((1)H-MRS) in patients with vascular cognitive impairment no dementia (VCIND) with dioscorea modified pill. METHODS: A total of 100 patients with VCIND were randomly assigned into the dioscorea modified pill group (n = 50) and the aricept group (n = 50). And 50 healthy volunteers were recruited as normal group. Each patient was examined with (1)H-MRS and scored with mini-mental state examination (MMSE) and clinical dementia rating (CDR) scale pre- and post-treatment...
October 28, 2014: Zhonghua Yi Xue za Zhi [Chinese medical journal]
Joshua D Vardigan, Christopher E Cannon, Vanita Puri, Mandy Dancho, AmyJo Koser, Marion Wittmann, Scott D Kuduk, John J Renger, Jason M Uslaner
RATIONALE: The standards of care for Alzheimer's disease, acetylcholinesterase inhibitors such as donepezil (Aricept®), are dose-limited due to adverse side-effects. These adverse events lead to significant patient non-compliance, constraining the dose and magnitude of efficacy that can be achieved. Non-selective muscarinic receptor orthosteric agonists such as Xanomeline have been shown to be effective in treating symptoms as well, but were also poorly tolerated. Therefore, there is an unmet medical need for a symptomatic treatment that improves symptoms and is better tolerated...
June 2015: Psychopharmacology
Ananya Sadhu, Prabhat Upadhyay, Aruna Agrawal, Kaliappan Ilango, Dipankar Karmakar, Gur Prit Inder Singh, Govind Prasad Dubey
BACKGROUND AND OBJECTIVE: The enigmatic etiology of neurodegenerative diseases poses a challenge for the development of novel and efficient drugs. The objective of the present study was to evaluate the efficacy of a polyherbal (test) formulation on cognitive functions, inflammatory markers and oxidative stress in healthy elderly as well as senile dementia of Alzheimer's type (SDAT) patients. METHOD: A randomized double-blind placebo- and active-controlled clinical trial was performed in healthy elderly subjects and SDAT patients with an age range of 60-75 years...
December 2014: Clinical Drug Investigation
Dongmei Wang, Ling Liu, Xiaoying Zhu, Wenlan Wu, Yong Wang
The role of mitochondrial dysfunction and oxidative stress has been well-documented in Alzheimer's disease (AD). Bioflavonoids are being utilised as neuroprotectants in the treatment of various neurological disorders, including AD. Therefore, we conducted this current study in order to explore the effects of hesperidin (a flavanone glycoside) against amyloid-β (Aβ)-induced cognitive dysfunction, oxidative damage and mitochondrial dysfunction in mice. Three-month-old APPswe/PS1dE9 transgenic mice were randomly assigned to a vehicle group, two hesperidin (either 50 or 100 mg/kg per day) groups, or an Aricept (2...
November 2014: Cellular and Molecular Neurobiology
Patricia Spilman, Olivier Descamps, Olivia Gorostiza, Clare Peters-Libeu, Karen S Poksay, Alexander Matalis, Jesus Campagna, Alexander Patent, Rammohan Rao, Varghese John, Dale E Bredesen
Tropisetron was identified in a screen for candidates that increase the ratio of the trophic, neurite-extending peptide sAPPα to the anti-trophic, neurite-retractive peptide Aβ, thus reversing this imbalance in Alzheimer's disease (AD). We describe here a hierarchical screening approach to identify such drug candidates, moving from cell lines to primary mouse hippocampal neuronal cultures to in vivo studies. By screening a clinical compound library in the primary assay using CHO-7W cells stably transfected with human APPwt, we identified tropisetron as a candidate that consistently increased sAPPα...
March 10, 2014: Brain Research
Yin-Jie Zhang, Yuan Dai, Yong Hu, Yun-Tong Ma, Shi-Jun Xu, Yong-Yan Wang
OBJECTIVE: To study the effect of Tongluo Xingnao effervescent tablet on learning and memory of dementia rats induced by injection of Abeta25-35 in hippocampus and expression of insulin-degrading enzyme in hippocampus, in order to provide basis for preventing and treating senile dementia. METHOD: The dementia rat model was established by injecting Abeta25-35 in hippocampus. The rats were divided into the model control group, the Aricept (1.4 mg x kg(-1)) group, and Tongluo Xingnao effervescent tablet high dose (7...
September 2013: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Chaitanya Gadiko, Sudhakar Koundinya Tippabhotla, Satyanarayana Thota, Ramakrishna Battula, Sohel Md Khan, Venkateswarlu Vobalaboina
To assess the bioequivalence of two extended-release tablets of donepezil 23 mg, open label, randomized, single-dose, two-sequence, two-period crossover studies under fasting (n=74) and fed (n=94) conditions in healthy adult human volunteers were conducted. Subjects were randomized to either of the two treatment arms (test or reference) separated by a washout period of 28 days. Blood samples were collected up to 72 h post-dose and plasma samples were analyzed for donepezil using a validated LC-MS/MS method...
2013: Scientia Pharmaceutica
Shannon L Risacher, Yang Wang, Heather A Wishart, Laura A Rabin, Laura A Flashman, Brenna C McDonald, John D West, Robert B Santulli, Andrew J Saykin
OBJECTIVE: To determine the physiological impact of treatment with donepezil (Aricept) on neural circuitry supporting episodic memory encoding in patients with amnestic mild cognitive impairment (MCI) using functional magnetic resonance imaging (fMRI). METHODS: Eighteen patients with MCI and 20 age-matched healthy controls (HC) were scanned twice while performing an event-related verbal episodic encoding task. MCI participants were scanned before treatment and after approximately 3 months on donepezil; HC were untreated but rescanned at the same interval...
2013: Frontiers in Psychiatry
Kai Bin Liew, Kok Khiang Peh, Yvonne Tze Fung Tan
An easy, fast and validated RV-HPLC method was invented to quantify donepezil hydrochloride in drug solution and orally disintegrating tablet. The separation was carried out using reversed phase C-18 column (Agilent Eclipse Plus C-18) with UV detection at 268 nm. Method optimization was tested using various composition of organic solvent. The mobile phase comprised of phosphate buffer (0.01M), methanol and acetonitrile (50:30:20, v/v) adjusted to pH 2.7 with phosphoric acid (80%) was found as the optimum mobile phase...
September 2013: Pakistan Journal of Pharmaceutical Sciences
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