Separation of leaves chloroform extract of Micromelum minutum (Rutaceae) yielded a new coumarin, 8-hydroxyisocapnolactone-2¢,3¢-diol. The structure of this compound was characterized by UV, IR, MS and NMR spectroscopic methods, including 1H, 13C, HSQC, COSY, HMBC dan NOESY experiments. This compound is significantly toksisk towards several cancer cell lines (CEM-SS, HL60, HeLa, HepG2, MCF7, T47D and NS1), active against chloroquin sensitive (D10) and resistance (FCR3) Plasmodium falciparum and showed strong antibacterial activity against Bacillus Subtilis mutan, Bacillus. Subtilis wild type, Pseudomonas Aeruginosa dan Staphylococcus aureus resisten meticilin). ABSTRAK Pemisahan ekstrak kloroform daun Micromelum minutum (Rutaceae) menghasilkan suatu kumarin baru, 8-hidroksiisokapnolakton-2΄,3΄-diol yang strukturnya diidentifikasi secara spektroskopi UV, IR, MS dan NMR termasuk 1H, 13C, HSQC, COSY, HMBC dan NOESY. Senyawa tersebut secara signifikan toksik terhadap beberapa sel kanker (CEM-SS, HL60, HeLa, HepG2, MCF7, T47D dan NS1), aktif terhadap Plasmodium falciparum yang sensitif (D10) maupun resisten (FCR3) kloroquin dan mempunyai aktivitas antibakteri yang kuat terhadap Bacillus Subtilis mutan, Bacillus. Subtilis wild type, Pseudomonas Aeruginosa dan Staphylococcus aureus resisten meticilin).