Presentation is loading. Please wait.

Presentation is loading. Please wait.

Are plant N-alkylamide cosmenutriceuticals also active in the central nervous system? Lieselotte Veryser, Evelien Wynendaele, Lien Taevernier, Frederick.

Published byAnnabelle Thompson Modified over 6 years ago

Similar presentations

Presentation on theme: "Are plant N-alkylamide cosmenutriceuticals also active in the central nervous system? Lieselotte Veryser, Evelien Wynendaele, Lien Taevernier, Frederick."— Presentation transcript:

1 Are plant N-alkylamide cosmenutriceuticals also active in the central nervous system?
Lieselotte Veryser, Evelien Wynendaele, Lien Taevernier, Frederick Verbeke, Tanmayee Joshi, Pratima Tatke and Bart De Spiegeleer* DruQuaR laboratory, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium. 11 May 2014 O/Ref c

2 N-alkylamides E.g. analgesic, antimicrobial, insecticidal, sensory,
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS N-alkylamides Plant secundary metabolites Occurance > 25 plant families Wide structural diversity: central peptide bond Functionalities E.g. analgesic, antimicrobial, insecticidal, sensory, anti-inflammatory, immune-modulating … Traditional use Potential lead compounds for functional food, cosmetics and medicines

3 Alkamid®: online N-alkylamide database
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS Alkamid®: online N-alkylamide database Name Botanical occurance Chemistry Physico-chemical properties Functionality Traditional use

4 spilanthol pellitorine
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS Spilanthes Acmella Anacyclus Pyrethrum spilanthol deca-2E,6Z,8E-trienoic acid isobutylamide (a triene NAA) pellitorine deca-2E,4E-dienoic acid isobutylamide (a diene NAA)

5 INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS

6 Gut (Caco-2 cell monolayer) Blood-brain barrier (BBB)
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS To investigate the permeability of spilanthol and pellitorine through several biological barriers: Skin Oral mucosa Gut (Caco-2 cell monolayer) Blood-brain barrier (BBB) NAA NAA Gravensteen, Ghent, Belgium

7 In vitro skin permeability study: Franz Diffusion cell
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS In vitro skin permeability study: Franz Diffusion cell Dermatomed human skin (± 400 µm thick) (32°C) or pig oral mucosa Dose formulation containing pellitorine and spilanthol Sampling at regular time intervals Quantification using validated high-throughput HPLC-UV Ref figure:

8 In vitro gut permeation study in Caco-2 monolayers
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS In vitro gut permeation study in Caco-2 monolayers Caco-2 cell intestinal model Caco-2 cells grown to a monolayer on 0.4 µm polycarbonate membrane Transport: apical-to-basolateral + basolateral-to-apical Final sample volumes of 0.4 ml apically and 1.2 ml basolaterally for 12-mm filter supports Sampling at 15, 30, 60, 90 and 120 min from the acceptor solution Ref figure

9 MTR: INFLUX (blood to brain) EFFLUX (brain to blood)
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS INFLUX (blood to brain) MTR: IV injection isolation of serum and brain at specified time points EFFLUX (brain to blood) intraventricular injection isolation of serum and brain at specified time points Analytics by UPLC-MS In vivo blood-brain barrier (BBB) experiment

10 A. Vogel® Spilanthes acmella commercial extract
Skin permeability of spilanthol INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS Transmucosal data Formulation Receptor fluid Kp (x 10-3 cm/h) Indolphar® PBS + HPbCD 19.5 Buccaldol® 47.5 Ethanolic extract 5.27 10% PG 10.9 30% PG 11.7 Transdermal data Kp (x 10-4 cm/h) 65% EtOH PBS 4.38 EtOH/H2O 0.70 15.3 16.6 5.46 A. Vogel® Spilanthes acmella commercial extract 3.56 4.95 0.64 10% EtOH 37.9 30% EtOH 53.3 6.59 31.5 22.7 65% PG 2.94

11 Skin permeability PELLITORINE Transdermal effect of pellitorine (n=4)
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS Skin permeability PELLITORINE Transdermal effect of pellitorine (n=4)

12 Caco-2 cell monolayer permeability
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS Caco-2 cell monolayer permeability SPILANTHOL Apical-basolateral transport (n=2) Basolateral-apical transport (n=2)

13 Caco-2 cell monolayer permeability
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS Caco-2 cell monolayer permeability PELLITORINE Apical-basolateral transport (n=2) Basolateral-apical transport (n=2)

14 Blood-brain barrier transport of spilanthol
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS Blood-brain barrier transport of spilanthol MTR EFFLUX

15 → N-alkylamides: cosmenutriceuticals
INTRODUCTION OBJECTIVE METHODS RESULTS CONCLUSIONS Spilanthol/pellitorine passes skin oral mucosa gut (Caco-2 cell monolayer) blood-brain barrier → N-alkylamides: cosmenutriceuticals

16 C. U. Shah College of Pharmacy
DruQuaR laboratory Ghent University Ghent, Belgium Lieselotte Veryser Evelien Wynendaele Lien Taevernier Frederick Verbeke Prof. Bart De Spiegeleer C. U. Shah College of Pharmacy S.N.D.T. Women's University Santacruz Mumbai, India Tanmayee Joshi Prof. Pratima Tatke ACKNOWLEDGEMENT Financial support of this study: IWT and BOF Financial support of this symposium: FWO + FCWO The graslei, Ghent, Belgium

Download ppt "Are plant N-alkylamide cosmenutriceuticals also active in the central nervous system? Lieselotte Veryser, Evelien Wynendaele, Lien Taevernier, Frederick."

Similar presentations

Pharmacological P-gp identification Since P-gp mediated drug efflux is a major hurdle in CNS drug discovery, it is important to identify P-gp substrates.

Pharmacological P-gp identification Since P-gp mediated drug efflux is a major hurdle in CNS drug discovery, it is important to identify P-gp substrates.
IMPACT OF EXPERIMENTAL CONDITIONS ON IN VITRO PERMEABILITY: (1) CORRELATIONS IN INTER-LABORATORY Caco-2 Y.H. Lee 1, K.J. Lee 1, N. Johnson 1, J. Castelo.

IMPACT OF EXPERIMENTAL CONDITIONS ON IN VITRO PERMEABILITY: (1) CORRELATIONS IN INTER-LABORATORY Caco-2 Y.H. Lee 1, K.J. Lee 1, N. Johnson 1, J. Castelo.
Introduction: The objective of this study was to provide solubility, rabbit intestinal permeability, Caco-2 permeability, and hepatocyte metabolism.

Introduction: The objective of this study was to provide solubility, rabbit intestinal permeability, Caco-2 permeability, and hepatocyte metabolism.
Howard E. Gendelman, MD Larson Professor of Medicine and Infectious Diseases Chairman, Department of Pharmacology and Experimental Neuroscience Director,

Howard E. Gendelman, MD Larson Professor of Medicine and Infectious Diseases Chairman, Department of Pharmacology and Experimental Neuroscience Director,
Transport of PAMAM Dendrimers Across Biological Barriers Ghaith Al-Jayyoussi, Will Ford & Mark Gumbleton Welsh School of Pharmacy, Cardiff University,

Transport of PAMAM Dendrimers Across Biological Barriers Ghaith Al-Jayyoussi, Will Ford & Mark Gumbleton Welsh School of Pharmacy, Cardiff University,
Advanced Medicinal Chemistry

Advanced Medicinal Chemistry
Peripheral inflammatory pain (λ-carrageenan injection) promotes localized paw edema and hyperalgesia Peripheral inflammatory pain reduces morphine efficacy.

Peripheral inflammatory pain (λ-carrageenan injection) promotes localized paw edema and hyperalgesia Peripheral inflammatory pain reduces morphine efficacy.
LC-ESI-MS/MS analysis of nine basic pharmaceuticals in influent, effluent and surface water Jet C. Van De Steene and Willy E. Lambert Laboratory of Toxicology,

LC-ESI-MS/MS analysis of nine basic pharmaceuticals in influent, effluent and surface water Jet C. Van De Steene and Willy E. Lambert Laboratory of Toxicology,
In Vivo and In Vitro Bioavailability Assessment of Topical Corticosteroid: Applications in Pharma Industry Muhammad Qamar- uz- Zaman Assistant Professor,

In Vivo and In Vitro Bioavailability Assessment of Topical Corticosteroid: Applications in Pharma Industry Muhammad Qamar- uz- Zaman Assistant Professor,
INTRODUCTION Related impurities profile and in silico toxicity potential of the anti-malarial drug lumefantrine Sultan Suleman 1, Bram Baert 1, Elien Vangheluwe.

INTRODUCTION Related impurities profile and in silico toxicity potential of the anti-malarial drug lumefantrine Sultan Suleman 1, Bram Baert 1, Elien Vangheluwe.
OPTIMISING MEDICINES DEVELOPMENT

OPTIMISING MEDICINES DEVELOPMENT
Transdermal Drug Delivery – Assessment of in vitro skin permeation Shashank Jain.

Transdermal Drug Delivery – Assessment of in vitro skin permeation Shashank Jain.
Drug-Like Properties: Optimizing Pharmacokinetics and Safety During Drug Discovery Li Di and Edward H. Kerns ACS Short Course.

Drug-Like Properties: Optimizing Pharmacokinetics and Safety During Drug Discovery Li Di and Edward H. Kerns ACS Short Course.
Introduction Angiogenesis is the formation of new blood cells that sprout from pre-existing ones. Essential for a tumor to grow larger then 1-2 mm, which.

Introduction Angiogenesis is the formation of new blood cells that sprout from pre-existing ones. Essential for a tumor to grow larger then 1-2 mm, which.
Pharmacology Department

Pharmacology Department
MECHANISMS OF DRUG PERMEATION / TRANSPORT

MECHANISMS OF DRUG PERMEATION / TRANSPORT
INTRODUCTION Concentration-dependent peptide losses during the drying step in the sample preparation: influence of additives Adel Pezeshki 1,2, Valentijn.

INTRODUCTION Concentration-dependent peptide losses during the drying step in the sample preparation: influence of additives Adel Pezeshki 1,2, Valentijn.
Developing a Method for Measuring Amlodipine Levels in Cat Plasma By:Preston Bull Advisors: Mike Gallagher, Dr. Webster.

Developing a Method for Measuring Amlodipine Levels in Cat Plasma By:Preston Bull Advisors: Mike Gallagher, Dr. Webster.
Bioavailability Dr Mohammad Issa.

Bioavailability Dr Mohammad Issa.
Antibacterial Potential of Spilanthes Extract on Common Skin Bacteria Hayley Lonai, Department of Biology, York College Introduction The skin disease acne.

Antibacterial Potential of Spilanthes Extract on Common Skin Bacteria Hayley Lonai, Department of Biology, York College Introduction The skin disease acne.

Similar presentations

Ads by Google