Englerin A, a selective inhibitor of renal cancer cell growth, from Phyllanthus engleri.
An extract from Phyllanthus engleri was identified in a bioinformatic analysis of NCI 60-cell natural product extract screening data that selectively inhibited the growth of renal cancer cell lines. Bioassay-guided fractionation yielded two new guaiane sesquiterpenes, englerins A (1) and B (2). Englerin A showed 1000-fold selectivity against six of eight renal cancer cell lines with GI(50) values ranging from 1-87 nM. The structures of 1 and 2 and their relative stereochemistry were established by spectroscopic methods.
Ratnayake
Ranjala
R
Molecular Targets Development Program, Center for Cancer Research, National Cancer Institute, NCIFrederick, Frederick, Maryland 21702, USA.
Covell
David
D
Ransom
Tanya T
TT
Gustafson
Kirk R
KR
Beutler
John A
JA
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001681:Biological Assay; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D007680:Kidney Neoplasms / Q000473:pathology*; D009682:Magnetic Resonance Spectroscopy / Q000592:standards; D008968:Molecular Conformation; D029803:Phyllanthus / Q000737:chemistry*; D024301:Plant Bark / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018547:Plant Stems / Q000737:chemistry; D012015:Reference Standards; D045789:Sesquiterpenes, Guaiane / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013237:Stereoisomerism
D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts; D045789:Sesquiterpenes, Guaiane; C534971:englerin A