作者机构:
[Liu, Zu Zhen] Hunan Society of Chinese Medicine;[Kim, Kwan-Woo; Kim, Youn-Chul] College of Pharmacy, Wonkwang University;[Yook, Chang Soo] School of Pharmacy, KyungHee University;[Li, Xiao Jun; Wang, Xiang; Li, Zhi; Liu, Xiang Qian] School of Pharmacy, Hunan University of Chinese Medicine
通讯机构:
School of Pharmacy, Hunan University of Chinese Medicine, Changsha, Hunan, China
摘要:
Multi-target drugs, such as the cocktail therapy used for treating AIDS, often show stronger efficacy than single target drugs in treating complicated diseases. This review will focus on clausenamide (clau), a small molecule compound originally isolated from the traditional Chinese herbal medicine, Clausenalansium. The finding of four chiral centers in clau molecules predicted the presence of 16 clau enantiomers, including (-)-dau and (+)-clau. All of the predicted enantiomers have been successfully synthesized via innovative chemical approaches, and pharmacological studies have demonstrated (-)-clau as a eutomer and (+)-clau as a distomer in improving cognitive function in both normal physiological and pathological conditions. Mechanistically, the nootropic effect of (-)-clau is mediated by its multi-target actions, which include mild elevation of intracellular Ca2+ concentrations, modulation of the cholinergic system, regulation of synaptic plasticity, and activation of cellular and molecular signaling pathways involved in learning and memory. Furthermore, (-)-clau suppresses the pathogenesis of Alzheimer's disease by inhibiting multiple etiological processes: (1) beta amyloid protein-induced intracellular Ca2+ overload and apoptosis and (2) tau hyperphosphorylation and neurodegeneration. In conclusion, the nature of the multi-target actions of (-)-clau substantiates it as a promising chiral drug candidate for enhancing human cognition in normal conditions and treating memory impairment in neurodegenerative diseases. (C) 2016 Elsevier Inc. All rights reserved.
作者机构:
School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China;Broad-Ocean Bio-Science and Technique Co., Ltd of Changsha, Changsha, Hunan 410205, China;Korea Research Institute of Bioscience and Biotechnology, Chungbuk, 363-883, South Korea
通讯机构:
School of Pharmacy, Hunan University of Chinese Medicine, Changsha, China
通讯机构:
[Liu, Shaojun] C;Cent S Univ, Xiang Ya Sch Med, Affiliated Hosp 3, Dept Digest Med, Changsha 410078, Hunan, Peoples R China.
关键词:
Folium Cordylines Fruticosae Anti-gastric Cancer MGC-803 cell
摘要:
The active components in Folium Cordylines Fruticosae were extracted by heat reflux method. The solvents used were distilled water and ethanol. The effects of two types of extracts on gastric cancer cells were compared; dry extract yields were calculated, as well as the inhibition rates of gastric cancer MGC-803 cell proliferation and the colony cell counts. The micro-Kjeldahl method was used to measure the cell protein contents and to make a comprehensive comparison. The results showed that the MGC-803 cell inhibition rates of three different concentrations (32.5, 75 and 150 mg/ml) of ethanol extracts increased with the increase of concentration, which was 48.9% at a concentration of 150 mg/ml; aqueous extract of Folium Cordylines Fruticosae had very low inhibitory activity at a low concentration (32.5 mg/ml), which was remained at about 20%. After being affected by two types of extracts, cells had uneven sizes, with very low brightness, while the normal cells presented a uniform full form, with high definition.