Pumpkin polysaccharides with various bioactivities are mainly taken orally, thus detailed knowledge of the intestinal transport of which are essential for understanding its bioactivities. The Caco-2 cells monolayer model (mimic intestinal epithelium) was successfully constructed and Cucurbia moschata polysaccharides (PPc-F) were successfully conjugated with fluorescein isothiocyanate (FITC) to evaluate the transcellular transport mechanism and subcellular localization of PPc. The transport process of PPc-F was energy-dependent, and a moderately-absorbed biological macromolecule according to the apparent permeability coefficients (P_app) value. The endocytosis process of PPc-F in Caco-2 cells included the clathrin- and caveolae (or lipid draft)-medicated routes. And the translocation process was related to endoplasmic reticulum (ER), golgi apparatus (GA), tubulin and the acidification of endosomes. As for the intracellular location of PPc-F, it was mainly accumulated in ER. The study provided an understanding of the transmembrane transport of PPc-F, and could help studying the mechanisms of its effects.

01 Dec 2016·Chemistry Central Journal

4-aroylpiperidines and 4-(α-hydroxyphenyl)piperidines as selective sigma-1 receptor ligands: synthesis, preliminary pharmacological evaluation and computational studies

Article

Author: Fidele Ntie-Kang ; Hermia N. Ikome ; Moses N. Ngemenya ; Zhude Tu ; Simon M. N. Efange ; Robert H. Mach

BACKGROUNDSigma (σ) receptors are membrane-bound proteins characterised by an unusual promiscuous ability to bind a wide variety of drugs and their high affinity for typical neuroleptic drugs, such as haloperidol, and their potential as alternative targets for antipsychotic agents. Sigma receptors display diverse biological activities and represent potential fruitful targets for therapeutic development in combating many human diseases. Therefore, they present an interesting avenue for further exploration. It was our goal to evaluate the potential of ring opened spipethiane (1) analogues as functional ligands (agonists) for σ receptors by chemical modification.RESULTSChemical modification of the core structure of the lead compound, (1), by replacement of the sulphur atom with a carbonyl group, hydroxyl group and 3-bromobenzylamine with the simultaneous presence of 4-fluorobenzoyl replacing the spirofusion afforded novel potent sigma-1 receptor ligands 7a-f, 8a-f and 9d-e. The sigma-1 receptor affinities of 7e, 8a and 8f were slightly lower than that of 1 and their selectivities for this receptor two to threefold greater than that of 1.CONCLUSIONSIt was found that these compounds have higher selectivities for sigma-1 receptors compared to 1. Quantitatitive structure-activity relationship studies revealed that sigma-1 binding is driven by hydrophobic interactions.Graphical abstractIdentified pharmacophore features for sigma binding.

01 Nov 2015·European Journal of Pharmaceutics and Biopharmaceutics

Simultaneous determination of active component and vehicle penetration from F-DPPC liposomes into porcine skin layers

Article

Author: Valenta, Claudia ; Reznicek, Gottfried ; Gehrig, Sebastian ; Geyer, Antonia ; Kieweler, Ruth ; Ogris, Manfred ; Mahrhauser, Denise-Silvia

Liposomes have been used as innovative delivery vehicles on skin for a number of years due to their positive influence on skin penetration. However, until now it is not entirely clear how and by which mechanism enhancement is achieved. In the present study, the skin permeation of a model substance incorporated into liposomes and a control formulation was compared to study the influence of the vehicle in Franz-type diffusion cell experiments. Furthermore, the penetration depths of both components were studied by simultaneous determination of the active substance and the vehicle component during tape stripping studies and horizontal sectioning. For these purposes we prepared liposomes with 1-palmitoyl-2-(16-fluoropalmitoyl)-sn-glycero-3-phosphocholine (F-DPPC), the monofluorinated analogue of dipalmitoylphosphaditylcholine (DPPC) loaded with sodium fluorescein (SoFl). A sodium-fluorescein solution was used as control formulation. While the semi-solid F-DPPC liposomes and the SoFl-solution performed equally well with similar permeation profiles during skin diffusion experiments, superior penetrated amounts of SoFl into the stratum corneum (SC) from F-DPPC liposomes compared to the SoFl-solution were observed possibly due to a "push" exerted by the vehicle F-DPPC. We also showed that SoFl penetrated through SC into the viable epidermis.

100 Deals associated with Emitefur

External Link

KEGG	Wiki	ATC	Drug Bank
D03987	-	-	-

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	NDA/BLA	Japan	Otsuka Pharmaceutical Co., Ltd.	-
Breast Cancer	NDA/BLA	-	Otsuka Holdings Co., Ltd.	-
Colorectal Cancer	NDA/BLA	-	Otsuka Holdings Co., Ltd.	-
Colorectal Cancer	NDA/BLA	Japan	Otsuka Pharmaceutical Co., Ltd.	-
Non-Small Cell Lung Cancer	NDA/BLA	-	Otsuka Holdings Co., Ltd.	-
Non-Small Cell Lung Cancer	NDA/BLA	Japan	Otsuka Pharmaceutical Co., Ltd.	-
Pancreatic Cancer	NDA/BLA	Japan	Otsuka Pharmaceutical Co., Ltd.	-
Stomach Cancer	NDA/BLA	-	Otsuka Holdings Co., Ltd.	-

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