Author: Duan, Yanhong ; Ding, Kan ; Cao, Xiaohua ; Guo, Dean ; Lu, Jing ; Huang, Shichao ; Zhou, Xuan ; Yang, Yongfeng ; Zhou, Yue ; Zhou, Lishuang ; Pei, Gang ; Hu, Tingting

Alzheimer's disease (AD) is the most common degenerative disease of the central nervous system. It is associated with abnormal accumulation of amyloid-β (Aβ) plaques, impaired neurogenesis, and damaged cognitive functions. We have known for a long time that natural compounds and their derivatives have gained increasing attention in AD drug research due to their multiple effects and inherently enormous chemicals. In this study, we will demonstrate that polysaccharides from L. barbarum (LBP1), a traditional natural compound, can reduce Aβ level and improve the cognitive functions in APP/PS1 transgenic mouse. LBP1 can enhance neurogenesis as indicated by BrdU/NeuN double labeling. Furthermore, it can restore synaptic dysfunction at hippocampus CA3-CA1 pathway. Additionally, in vitro cell assay indicates that LBP1 may affect Aβ processing. In conclusion, our study indicates that LBP1 might be a potential therapeutic agent for the treatment of AD against multiple targets that include synaptic plasticity, Aβ pathology and neuropathology.

01 Feb 2014·Carbohydrate PolymersQ1 · CHEMISTRY

Antitumor and immunomodulatory effects of a water-soluble polysaccharide from Lilii Bulbus in mice

Q1 · CHEMISTRY

Article

Author: Gao, Rui-Lan ; Sun, Xin ; Xu, Min ; Huang, Qing-Cheng ; Xiong, Yao-Kang

Lilii Bulbus is a popular folk medicine in the worldwide and has attracted great attention due to its bioactivity against respiratory system diseases (include lung cancers). This study was the first report providing in vivo evidences of antitumor potential of the bioactive polysaccharide from Lilii Bulbus. One major fraction (LBP-1) was obtained by purifying the crude polysaccharides extracted from Lilii Bulbus. Chemical characterization analysis indicated that LBP-1 was only a glucan, whose average molecular weight was 30.5 kDa. Intraperitoneal administration of LBP-1 at the doses of 50-200mg/kg significantly inhibited the growth of Lewis lung carcinoma. Moreover, it could also obviously increase macrophage phagocytosis, splenocytes proliferation and cytokine (TNF-α, IL-2, IL-6 and IL-12) production to participate in the antitumor effects. LBP-1 could act as antitumor agent with immunomodulatory activity.

01 Apr 2012·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain

Q4 · MEDICINE

Article

Author: Fiona Jeremiah ; Jean E Cottney ; Jurgen Schulz ; Ruth Fields ; Kathryn Everett ; Robert A Campbell ; James Baker ; Angus J Morrison ; Takao Kiyoi ; Stuart Francis ; Susan Boyce ; John K Clark ; Maureen Deehan ; Iain Martin ; Maurice Maidment ; Alan Prosser ; Grant Wishart ; Paul D Ratcliffe ; Keneth Davies ; Julia M Adam

Novel, low brain penetrant, orally bioavailable CB1 receptor agonists were designed starting from a mature lead series of potent brain penetrant CB1 receptor agonists. Increasing the calculated polar surface area was found to be a good strategy for reducing brain penetration whilst retaining drug-like properties. This in silico approach led to the discovery of LBP1, an orally bioavailable, low brain penetrant CB1 receptor agonist with robust activity in rodent models of neuropathic pain and a good preclinical therapeutic profile, which was selected for clinical development.

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Preclinical	KR	LISCure Bioscience Co. Ltd.Startup	19 Jul 2021

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