The value of screening plant extracts to the U.S. pharmaceutical industry is the promise of finding patentable compounds to treat human diseases. Ethnobotanical rationale for selecting targeted plants allows a focused approach in finding compounds of pharmaceutical interest The Phytochemistry Section of """"""""Peruvian Medicinal Plants As Sources Of New Pharmaceuticals"""""""" provides the natural products chemistry support for isolating and identifying compounds with antiinfective and antiinflammation activity. These active compounds could provide a starting point for medicinal chemistry programs as well as validating the targets used for screening. Extraction procedures are described that reduce the hit rate resulting from non-specific interactions (e.g. tannins, polyphenolics etc.) so that the program can focus on finding new chemistry or new activities for known compounds. Isolation procedures include the use of scouting columns to determine optimal separation methodology, e.g., C18 HPLC or ion exchange chromatography. Bioassay- guided fractionation is then used to isolate the compound(s) responsible for the extracts activity. Dereplication techniques will play a major role in determining known active compounds. Databases such as """"""""Handbook of Antibiotic Compounds"""""""" (Berdy database) and CAS Online are used to dereplicate known compounds with minimal information. Structure determination on low microgram quantities of pure material can be completed using modem spectroscopic techniques including electrospray mass spectrometry and inverse-detected microprobe NMR.

National Institute of Health (NIH)
Fogarty International Center (FIC)
Research Project--Cooperative Agreements (U01)
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Aponte, Jose C; Jin, Zhuang; Vaisberg, Abraham J et al. (2011) Cytotoxic and anti-infective phenolic compounds isolated from Mikania decora and Cremastosperma microcarpum. Planta Med 77:1597-9
Aponte, Jose C; Yang, Han; Vaisberg, Abraham J et al. (2010) Cytotoxic and anti-infective sesquiterpenes present in Plagiochila disticha (Plagiochilaceae) and Ambrosia peruviana (Asteraceae). Planta Med 76:705-7
Aponte, José C; Vaisberg, Abraham J; Rojas, Rosario et al. (2009) A multipronged approach to the study of peruvian ethnomedicinal plants: a legacy of the ICBG-Peru Project. J Nat Prod 72:524-6
Aponte, Jose C; Vaisberg, Abraham J; Rojas, Rosario et al. (2008) Isolation of cytotoxic metabolites from targeted peruvian amazonian medicinal plants. J Nat Prod 71:102-5
Rojas, Rosario; Caviedes, Luz; Aponte, Jose C et al. (2006) Aegicerin, the first oleanane triterpene with wide-ranging antimycobacterial activity, isolated from Clavija procera. J Nat Prod 69:845-6
Milanowski, Dennis J; Winter, Rudolph E K; Elvin-Lewis, Memory P F et al. (2002) Geographic distribution of three alkaloid chemotypes of Croton lechleri. J Nat Prod 65:814-9
Okunade, A L; Lewis, W H; Elvin-Lewis, M P et al. (2001) Cinchonicine-derived alkaloids from the bark of the Peruvian Ladenbergia oblongifolia. Fitoterapia 72:717-9