Rubropunctatin,　a　metabolite　isolated　from　the　fungi　of　the　genus　Monascus,　is　a　natural　lead　compound　applied　for　the　suppression　of　tumors　with　good　anti-cancer　activity.　However,　its　poor　aqueous　solubility　has　limited　its　further　clinical　development　and　utilization.　Lecithin　and　chitosan　are　excellently　biocompatible　and　biode-gradable　natural　materials,　which　have　been　approved　by　the　FDA　as　drug　carrier.　Here,　we　report　for　the　first　time　the　construction　of　a　lecithin/chitosan　nanoparticle　drug　carrier　of　the　Monascus　pigment　rubropunctatin　by　electrostatic　self-assembly　between　lecithin　and　chitosan.　The　nanoparticles　are　near-spherical　with　a　size　110-120　nm.　They　are　soluble　in　water　and　possess　excellent　homogenization　capacity　and　dispersibility.　Our　in　vitro　drug　release　assay　showed　a　sustained　release　of　rubropunctatin.　CCK-8　assays　revealed　that　lecithin/chi-tosan　nanoparticles　loaded　with　rubropunctatin　(RCP-NPs)　had　significantly　enhanced　cytotoxicity　against　mouse　mammary　cancer　4T1　cells.　The　flow　cytometry　results　revealed　that　RCP-NPs　significantly　boosted　cellular　uptake　and　apoptosis.　The　tumor-bearing　mice　models　we　developed　indicated　that　RCP-NPs　effectively　inhibited　tumor　growth.　Our　present　findings　suggest　that　lecithin/chitosan　nanoparticle　drug　carriers　improve　the　anti-tumor　effect　of　the　Monascus　pigment　rubropunctatin.