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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. Philippine Mollusk Symbiont International Biodiversity Group (PMS-ICBG).
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PHILIPPINE PHARMASEAS DRUG DISCOVERY PROGRAM Marine Drug Discovery of Anti-Pain Agents from Turrid Snails Anti-Infective Agents from Sponge – Associated Microorganisms
Philippine Mollusk Symbiont International Biodiversity Group (PMS-ICBG) Diverse drug lead compounds from bacterial symbionts in tropical marine mollusks A 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.
1 2 Drug Discovery Pipeline Collection and isolation of microorganisms High throughput bioactivity screening 5 3 Novel bioactive compounds 4 Chemical extraction/ Dereplication at compound level Identification of isolates/ Dereplication at producer level
2,737 Isolation of Microorganisms Marine micoorganisms in collection From database as of April 2012 Field collection of marine sponges, gastropods Isolation of morphologically distinct colony Database and archiving of pure isolates
169 Antimicrobial Activity Pseudomonas aeruginosa(PA) Klebsiellapneumoniae (KP) Staphylococcus aureus(SA) Methicilin-resistant S. aureus(MRSA) Biofilm-forming S. epidermidis Mammalian Cell Cytotoxicity Antiviral Activity Antifungal Activity Candida albicans (CA) Ampothericin-resistant C. albicans Neuroactivity Dorsal root ganglion assay DRG Antimicrobial priority isolates Bioactivity Screening 78 Cytotoxic priority isolates Neuroactive priority isolates 11 4,872 Yields from assay events
Strategy for Finding High Value Compounds: Purifying compounds from Sponge MMO HPLC Conditions: Shimadzu Prominence HPLC 1 Injected: 50 μL Flow 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 6 7 1 2 3 4 5 8 9
Chemical Dereplication UV absorbance spectra Compound matches Hi-res mass spectra + fragmention data AntiMarin* Database + bioactivity and Isolate identity data NMR data (H-H COSY) AntiMarin – is a combined database containing 55,000 reported terrestial and marine natural products Recent tool
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NMR Facility Core Group Administration: 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)