Research Cores Archive 9.4.2018

Samir Ross

Sourcing, Acquisition and Isolation Core (Core A)

Director: Dr. Samir Ross, Research Professor in the National Center for Natural Products Research

Core Description: Provides three services to CORE-NPN investigators: 
(1) provide CORE-NPN investigators rapid access to the material extracts that reside in the 
NCNPR repositories as well as access to collections that reside with collaborators; (2) provide for the bioassay directed isolation of active natural metabolites; and (3) scale-up the isolation of minor secondary metabolites that possess biological activity on cannabinoid and opioid receptor.

John Rimoldi 1

Chemistry and Drug Metabolism Pharmacokinetics (DMPK) Core

Director: Dr. John Rimoldi, Professor, Department of BioMolecular Sciences  
Co-Director: Dr. Chalet Tan, Associate Professor, Department of Pharmaceutics

Core Description:The Chemistry and DMPK Core provides lead optimization, analytical expertise, drug metabolism and pharmacokinetic data on natural products and related compounds that are determined by CORE-NPN investigators to have significant biological activity in the In Vitro (Core C) and In Vivo (Core D) Cores. In addition, the Chemistry and DMPK Core will make available the bulk-synthesis of compounds that have potential clinical usefulness. The Chemistry and DMPK Core will also have an advisory role for individual projects and other CORE-NPN investigators that require expertise in the area of exploration of structure-activity relationships, analytical method development and validation, chemical modifications to influence pharmacokinetic and metabolism properties, and pharmaceutical and chemical influences on solubility and formulation.

Babu Tekwani

In Vitro Pharmacology Core (Core C)

Director: Dr. Babu Tekwani – In Vitro Pharmacology Core

Core Description: Enables investigators to use in vitro assays to serve as a guide in the isolation and identification of biological-active natural products and to evaluate compounds predicted to have activities in these systems through rational drug design.  The In Vitro Pharmacology Core provides several functions related to understanding the mechanisms of actions of natural products on the endocannabinoid system that can lead to the development of new therapies. Core C also supports UM projects optimizing small molecule activity at the cannabinoid receptors (CB1 and CB2) and the opioid receptor subtypes (m,d, and k), which are currently available for use.  Specifically, Core C provides the ability to screen compounds in-house for biological activity and determine the site(s) as well as mechanism(s) of action. These core functions are dependent on the use of state-of-the-art technologies as well as time-tested laboratory methodologies. Using multi-label plate reader technologies and robotics, the core is able to rapidly assess compounds and extracts held in the Repository of the NCNPR at the University of Mississippi for specific receptor activities.  These receptors represent drug targets in areas as diverse as drug addiction, pain and obesity.

In Vivo Pharmacology Core (Core D)

Director: Dr. Nicole Ashpole, Assistant Professor, Department of BioMolecular Sciences

Core Description: Provides the resources associated with in vivo evaluations. This core provides assessments that include: conditioned place preference, locomotor activity, catalepsy and rotarod testing, core body temperature measurement, tail flick and hot plate assays, weight control, and forced swim.  The In Vivo Core focuses on screening natural products with overall effects on the endocannabinoid system and possible membership in four drug categories: opiate-like, stimulant-like, cannabinoid-like, and depressant-like compounds. While these categories have potential therapeutic uses, the categories are also associated with abuse potential and other negative side effects including, motor side effects, temperature dysregulation, changes in food intake, and cognitive impairments (memory and reaction time).

Michael Repka

Seongbong Jo

Biopharmaceutics-Clinical and Translational Core (Core E)

Director: Dr. Michael Repka, Chair and Professor of Pharmaceutics
Co-Director: Dr. Seongbong Jo,
Associate Professor of Pharmaceutics

Core Description: Provides two services to CORE-NPN investigators. The first mission of Core E is to provide the technical support and necessary expertise to perform preliminary translational studies such as preformulation studies, formulation developments studies, accelerated stability testing of the API and the dosage form, and preclinical studies and data interpretation. The second mission of Core E is to provide technical expertise and guide and facilitate preliminary clinical evaluation of agents that demonstrate potential usefulness in the preclinical studies. These clinical studies, however, will be performed and funded outside the auspices of Core E.  The Core E will develop and test the stability of the formulations and identify the most suitable formulation for clinical studies as well as assist the sourcing of clinical batches for testing/evaluation from approved cGMP compliant manufacturing sites. Core E also has in place a clinical team that will help undertake clinical trials when needed (funded by other mechanisms such as industry and other federal sources).