drug discovery and development. philippine pharmaseas drug discovery program marine drug discovery...
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Drug Discovery and Development
PHILIPPINE PHARMASEAS DRUG DISCOVERY PROGRAM
Marine Drug Discovery of
•Anti-Pain Agents from Turrid Snails
•Anti-Infective Agents from Sponge – Associated Microorganisms
Diverse drug lead compounds from bacterial symbionts in tropical marine mollusksA research collaboration between University of the Philippines Diliman, Oregon Health and Science University, University of Utah, Academy of Natural Sciences of Philadelphia and Ocean Genome Legacy Foundation, USA.
Philippine Mollusk Symbiont International Biodiversity Group (PMS-ICBG)
Drug Discovery Pipeline
Collection and isolation of microorganisms
High throughput bioactivity screening
Identification of isolates/Dereplication at producer level
Chemical extraction/Dereplication at compound level
Novel bioactive compounds
1 2
3 4 5
Isolation of Microorganisms
2,737
From database as of April 2012
Marine micoorganisms in collection
Isolation of morphologically distinct colony
Database and archiving of pure isolates
Field collection of marine sponges, gastropods
Antimicrobial Activity Pseudomonas aeruginosa (PA) Klebsiella pneumoniae (KP) Staphylococcus aureus (SA) Methicilin-resistant S. aureus (MRSA) Biofilm-forming S. epidermidisMammalian Cell CytotoxicityAntiviral ActivityAntifungal Activity Candida albicans (CA) Ampothericin-resistant C. albicans Neuroactivity Dorsal root ganglion assay DRG
Bioactivity Screening
169 78 11
Antimicrobial priority isolates
Cytotoxic priority isolates
Neuroactive priority isolates
4,872 Yields from assay events
HPLC Conditions:Shimadzu Prominence HPLC 1 Injected: 50 μLFlow rate: 3.0mL/min Solvent system:Binary gradient, Column: Phenomenex Luna C18 5-100 MeOH in 45 mins
250x10mm, 5μm (semi prep)
100% MeOH Diaion Fraction
1 2 3 4 56 7
8 9
Strategy for Finding High Value Compounds: Purifying compounds from Sponge MMO
Chemical DereplicationUV absorbance spectra
Hi-res mass spectra + fragmention data
NMR data (H-H COSY)
+ bioactivity andIsolate identity data
AntiMarin*Database
Compound matches
AntiMarin – is a combined database containing 55,000 reported terrestial and marine natural products
Recent tool
Materials Science
Magnetic Resonance Imaging
UP Diliman NMR FACILITY Service Form
USER INFORMATION
SAMPLE INFORMATION
EXPERIMENTAL INFORMATION
CONDITION/S OF USE
I understand and agree to the following: a. That I will be billed according to the half-hourly usage of the NMR plus consumables, if any, based on
current schedule of fees. b. Samples submitted will be disposed of after one (1) month of processing if not claimed. c. Data files of processed samples will be disposed of after one (1) month of processing. d. A minimum basic half-hour rate or 50% downpayment, whichever is higher, must be made upon
submission of sample. Additional 25% administrative charges will be applied to the total fees. Please pay at the UP Cashier.
e. The basic rate includes sample preparation. f. Processing includes e-mail of FID file. g. All experiments that will require more than 30-minute run time will be run during the night queue with a
50% discounted rate on a 2-hr block schedule. h. Day queue is from 8 AM to 5 PM and night queue is from 5 PM to 8 AM.
____________________________________________ Name and Signature of Project Leader/Researcher/Thesis Adviser
Half-hour rate UP certified UP System
PhP 400 PhP 550
Other academic institutions
PhP750
Government PhP 1,000 Industry/Private PhP 1,500 Consumables: Solvent NMR tubes
5 mm NMR tube (500 MHz, 7' long) = PhP 1,675/ NMR tube 3 mm NMR tube (500 MHz, 7' long) = PhP 1,584/NMR tube (for use in inverse detection probe) 5 mm NMR tube (400 MHz, 8' long) = PhP 1,488/tube CDCl3 = PhP 68.5/ml CD3OD = PhP 1,265/ ampoule D2O = PhP 1,886/ ampoule CD3CN = PhP 8,604/ ampoule DMSO-d6 = PhP 2,873/ ampoule Pyridine-d6 Acetone-d6
Processing
PhP 200 for e-mail and print-out of full and expanded spectrum with integration and chemical shifts of peaks indicated.
NMR User Fees
NMR Facility Core GroupAdministration: Dr. Armando Somintac (NIP) and Dr. Neil Andrew Bascos
(NIMBB)
Promotion and advertisements: Dr. Evangeline C. Amor (IC) and Dr. Christine C. Hernandez (IC)
Training and licensing: Dr. Florecita de Guzman (IC), Dr. Portia Mahal G. Sabido (IC), Dr. Aaron Villaraza (IC), Dr. Nemesio E. Montano (MSI)
Maintenance: Mr. Miguel Azcuna (MSI) and Ms. Arlene Bartolome (IC)
Housekeeping: Dr. Irene M. Villaseñor (IC)
Finance: Dr. Irene M. Villaseñor (IC)
Business: Dr. Gisela P. Concepcion (MSI)