Synthetic antitumor lipids are metabolically stable lysophosphatidylcholine derivatives, encompassing a class of non-mutagenic drugs that selectively target cancerous cells. In this chapter we review the literature as relates to the clinical efficacy of these antitumor lipid drugs and how our understanding of their mode of action has evolved alongside key advances in our knowledge of membrane structure, organization, and function. First, the history of the development of this class of drugs is described, providing a summary of clinical outcomes of key members including edelfosine, miltefosine, perifosine, erufosine, and erucylphosphocholine. A detailed description of the biophysical properties of these drugs and specific drug-lipid interactions which may contribute to the selectivity of the antitumor lipids for cancer cells follows. An updated model on the mode of action of these lipid drugs as membrane disorganizing agents is presented. Membrane domain organization as opposed to targeting specific proteins on membranes is discussed. By altering membranes, these antitumor lipids inhibit many survival pathways while activating pro-apoptotic signals leading to cell demise.

01 Apr 2017·Journal of Ethnopharmacology

The protective effect of the active components of ERPC on diabetic peripheral neuropathy in rats

Article

Author: Wang, Hong-liang ; Guo, Shu-Zhen ; Liu, Yong-Gang ; Hao, Gai-mei ; Lv, Tian-tian ; Liu, Yong-gang ; Wang, Zheng-lin ; Shi, Tian-Jiao ; Guo, Shu-zhen ; Shi, Tian-jiao ; Wang, Wei ; Wang, Hong-Liang ; Han, Jing ; Wang, Yong ; Xing, Wei ; Li, Chun ; Wu, Yan ; Wang, Zheng-Lin ; Hao, Gai-Mei ; Lv, Tian-Tian

ETHNOPHARMACOLOGICAL RELEVANCEEuonymus alatus, Radix trichosanthis, Panax notoginseng and Coptis chinensis are popular plants used in traditional Chinese medicine to treat diabetes.AIM OF THE STUDYThe aim of the study is to investigate the therapeutic effect of the active components of Euonymus alatus, Radix trichosanthis, Panax notoginseng and Coptis chinensis (cERPC) on diabetic peripheral neuropathy in the rats and explore the underlying mechanism involved.METHODSAfter diabetes was induced in rats for 20 weeks, cERPC or water was administered for 12 weeks. After a hot plate test, motor nerve conduction velocity and sciatic nerve blood flow were determined; the sciatic nerves were isolated for toluidine blue staining; and the fibre area, fibre diameter, axon area, axon diameter and myelin thickness were evaluated. The levels of the myelin basic protein, myelin protein zero, Oct6 and Krox20 were measured by western blot or immunofluorescence.RESULTScERPC was efficient in reducing the response latency, increasing motor nerve conduction velocity, enhancing sciatic nerve blood flow and ameliorating the pathological changes in diabetic rats. cERPC also had a role in increasing the levels of myelin basic protein and myelin protein zero and improving the expression of Oct6 and Krox20 in sciatic nerves of diabetic rats.CONCLUSIONScERPC ameliorates diabetic peripheral neuropathy by attenuating electrophysiological, circulatory and morphological alterations, which is mediated by the Oct6-Krox20 pathway.

17 Nov 2015·Molecular Membrane BiologyQ4 · BIOLOGY

The influence of an antitumor lipid – erucylphosphocholine – on artificial lipid raft system modeled as Langmuir monolayer

Q4 · BIOLOGY

Article

Author: Zemla, Joanna ; Wnętrzak, Anita ; Łątka, Kazimierz ; Makyła-Juzak, Katarzyna ; Dynarowicz-Łątka, Patrycja

Outer layer of cellular membrane contains ordered domains enriched in cholesterol and sphingolipids, called 'lipid rafts', which play various biological roles, i.e., are involved in the induction of cell death by apoptosis. Recent studies have shown that these domains may constitute binding sites for selected drugs. For example alkylphosphocholines (APCs), which are new-generation antitumor agents characterized by high selectivity and broad spectrum of activity, are known to have their molecular targets located at cellular membrane and their selective accumulation in tumor cells has been hypothesized to be linked with the alternation of biophysical properties of lipid rafts. To get a deeper insight into this issue, interactions between representative APC: erucylphosphocholine, and artificial lipid raft system, modeled as Langmuir monolayer (composed of cholesterol and sphingomyelin mixed in 1:2 proportion) were investigated. The Langmuir monolayer experiments, based on recording surface pressure-area isotherms, were complemented with Brewster angle microscopy results, which enabled direct visualization of the monolayers structure. In addition, the investigated monolayers were transferred onto solid supports and studied with AFM. The interactions between model raft system and erucylphosphocholine were analyzed qualitatively (with mean molecular area values) as well as quantitatively (with ΔG(exc) function). The obtained results indicate that erucylphosphocholine introduced to raft-mimicking model membrane causes fluidizing effect and weakens the interactions between cholesterol and sphingomyelin, which results in phase separation at high surface pressures. This leads to the redistribution of cholesterol molecules in model raft, which confirms the results observed in biological studies.

100 Deals associated with Erucylphosphocholine

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Discovery	New Zealand	Keryx Biopharmaceuticals, Inc.	-
Neoplasms	Discovery	Israel	Keryx Biopharmaceuticals, Inc.	-
Neoplasms	Discovery	Canada	Æterna Zentaris, Inc.	-
Neoplasms	Discovery	Australia	Keryx Biopharmaceuticals, Inc.	-
Neoplasms	Discovery	Canada	Æterna Zentaris, Inc.	-
Neoplasms	Discovery	New Zealand	Keryx Biopharmaceuticals, Inc.	-
Neoplasms	Discovery	Israel	Keryx Biopharmaceuticals, Inc.	-
Neoplasms	Discovery	Australia	Keryx Biopharmaceuticals, Inc.	-
Neoplasms	Discovery	North America	Keryx Biopharmaceuticals, Inc.	-
Neoplasms	Discovery	North America	Keryx Biopharmaceuticals, Inc.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

Erucylphosphocholine

Overview

Basic Info

Structure/Sequence

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation