Abstract The World Health Organization (WHO) redefined traditional medicine recently as comprising therapeutic practices that have been in existence, often for hundreds of years, before the development and spread of modern scientific medicine and are still in use today (WHO, 1991).[1] Traditional healers have used the drugs of herbal, herbomineral, and animal origin since the dawn of civilization to maintain health and treat disease. According to WHO, about 80% of the world's population use herbal drugs for their primary health care. These drugs are cheap with no or less side effects. The Annonaceous acetogenins are C-32 or C-34 long-chain fatty acids that have been combined with a 2-propanol unit at C-2 to form a terminal???-unsaturated?-lactone. They often cyclize to form one, two, or three tetrahydrofuran or tetrahydopyran rings near the middle of the alphabetic chain. To date, nearly 400 of these compounds have been isolated from several genera of the plant family, Annonaceae. The potential application of acetogenin molecules is linked to their marked properties: cytotoxic and antitumor (gigantecin, bullatacin, and rolliniastatin) and pesticidal (asimicine and annonin). Biochemically, acetogenins block mitochondrial respiration by inhibiting NADH-cytochrome-c oxidoreductase; this would explain their pesticidal activity among others.