Developing new classes of anticancer molecules has always been a major scientific challenge owing to multidrug resistance of cancer cells to conventional chemotherapeutic agents. Microbial amphiphiles, particularly lipopeptides and glycolipids, have recently emerged as potential new-generation anticancer agents, owing to low toxicity, high efficacy and easy biodegradability. They exhibit anticancer activities by retarding cell cycle progression, inhibiting crucial signaling pathways such as Akt, extracellular signal-regulated kinase/c-Jun N-terminal kinase (ERK/JNK) and Janus kinase/signal transducer and activator of transcription (JAK/STAT), reducing angiogenesis, activating natural killer T (NKT) cells and inducing apoptosis through death...