Lepidium meyenii Walp., known as maca, is a plant from family of Brassicaceae. Maca is an indigenous medicinal herb, which primarily cultivated at Highland Andes Plateau on the altitude of 4000 meter. The Peruvian used maca as important dietary supplement and food component, especially as fertility enhancer. In previous studies, maca exhibited aphrodisiac bioactivities on both male and female, including spermatogenesis enhancer, increase sperm quality parameters, enhance female fertility, and decrease menopausal symptoms. In this research, investigation on maca compounds were conducted, especially on new discovered compounds. The purpose of this research is to isolate secondary metabolites from maca, along with investigating their bioactivity properties. This research used dried tuberous roots or tubers part of maca as subject material. The 75% methanol aq. layer of methanol extract exhibited strong inhibition against inflammation in the model of human fLMF/CB-induced neutrophils on both superoxide anion generation assay (101.12% ± 0.26%; p < 0.001) and elastase release inhibition assay (110.88% ± 0.24%; p < 0.001) on initial anti-inflammatory activity assay. There were 11 alkaloids isolated during this study. Macapyrrolidinone A (1) was isolated first time in nature and became the first pyrrolidinone alkaloids found in maca, alongside new compound macapyrrolidinone B (2). Macapyrrolins D and E (3‒4) were isolated and determined as new pyrrole alkaloids. Two known pyrrole alkaloids, macapyrrolins A and C (5 and 6), a known pyridine alkaloid, macaridine (7), and 3-hydroxyphenylacetonitrile (8) were isolated, together with a mixture of three alkaloid amides or macamides, N-benzyloleamide (9), N-benzyllinoleamide (10), and N-benzyllinolenamide (11). Therefore, all the tests of various biological functions of maca and its compounds are still undergoing. The further discoveries on this study are expected to provide more understandings and new research perspectives about maca.